DE602004025569D1 - Makrozyklische motilin rezeptorantagonisten - Google Patents

Makrozyklische motilin rezeptorantagonisten

Info

Publication number
DE602004025569D1
DE602004025569D1 DE602004025569T DE602004025569T DE602004025569D1 DE 602004025569 D1 DE602004025569 D1 DE 602004025569D1 DE 602004025569 T DE602004025569 T DE 602004025569T DE 602004025569 T DE602004025569 T DE 602004025569T DE 602004025569 D1 DE602004025569 D1 DE 602004025569D1
Authority
DE
Germany
Prior art keywords
receptor antagonists
motilin receptor
group
macrocyclic
conformationally
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
DE602004025569T
Other languages
English (en)
Inventor
Graeme Fraser
Eric Marsault
Mark Peterson
Hamid Hoveyda
Sylvie Beaubien
Kamel Benakli
Robert Deziel
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Tranzyme Pharma Inc
Original Assignee
Tranzyme Pharma Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Tranzyme Pharma Inc filed Critical Tranzyme Pharma Inc
Publication of DE602004025569D1 publication Critical patent/DE602004025569D1/de
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C213/08Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22Hormones
    • A61K38/2214Motilins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12Antidiarrhoeals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C41/00Preparation of ethers; Preparation of compounds having groups, groups or groups
    • C07C41/01Preparation of ethers
    • C07C41/18Preparation of ethers by reactions not forming ether-oxygen bonds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C67/00Preparation of carboxylic acid esters
    • C07C67/30Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group
    • C07C67/333Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by isomerisation; by change of size of the carbon skeleton
    • C07C67/343Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D273/00Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0812Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0821Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0827Tripeptides containing heteroatoms different from O, S, or N
DE602004025569T 2003-06-18 2004-06-18 Makrozyklische motilin rezeptorantagonisten Active DE602004025569D1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US47922303P 2003-06-18 2003-06-18
PCT/CA2004/000913 WO2004111077A1 (en) 2003-06-18 2004-06-18 Macrocyclic antagonists of the motilin receptor

Publications (1)

Publication Number Publication Date
DE602004025569D1 true DE602004025569D1 (de) 2010-04-01

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
DE602004025569T Active DE602004025569D1 (de) 2003-06-18 2004-06-18 Makrozyklische motilin rezeptorantagonisten

Country Status (9)

Country Link
US (9) US7521420B2 (de)
EP (2) EP1633774B1 (de)
JP (1) JP4928261B2 (de)
AT (1) ATE457995T1 (de)
CA (1) CA2528375C (de)
DE (1) DE602004025569D1 (de)
DK (1) DK1633774T3 (de)
ES (1) ES2338789T3 (de)
WO (1) WO2004111077A1 (de)

Families Citing this family (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2284459C (en) * 1999-10-04 2012-12-11 Neokimia Inc. Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery
USRE42013E1 (en) 2003-06-18 2010-12-28 Tranzyme Pharma Inc. Macrocyclic modulators of the ghrelin receptor
US8921521B2 (en) 2003-06-18 2014-12-30 Ocera Therapeutics, Inc. Macrocyclic modulators of the Ghrelin receptor
US7476653B2 (en) * 2003-06-18 2009-01-13 Tranzyme Pharma, Inc. Macrocyclic modulators of the ghrelin receptor
USRE42624E1 (en) 2003-06-18 2011-08-16 Tranzyme Pharma Inc. Methods of using macrocyclic modulators of the ghrelin receptor
US7491695B2 (en) * 2003-06-18 2009-02-17 Tranzyme Pharma Inc. Methods of using macrocyclic modulators of the ghrelin receptor
US20090198050A1 (en) * 2003-06-18 2009-08-06 Tranzyme Pharma Inc. Macrocyclic Modulators of the Ghrelin Receptor
WO2004111077A1 (en) * 2003-06-18 2004-12-23 Tranzyme Pharma Inc. Macrocyclic antagonists of the motilin receptor
EP1648923B1 (de) * 2003-07-31 2008-12-31 Tranzyme Pharma Inc. Räumlich definierte makrocyclen, die peptidbindungssurrogate enthalten
EP2316846B1 (de) * 2003-07-31 2019-10-02 Ocera Therapeutics, Inc. Räumlich definierte makrozyklische Verbindungen zur Entdeckung von Arzneimitteln
JP5739766B2 (ja) * 2004-06-18 2015-06-24 オセラ セラピューティクス, インコーポレイテッド グレリン受容体の大環状モジュレーターの使用方法
WO2006046977A1 (en) * 2004-10-26 2006-05-04 Tranzyme Pharma, Inc. Macrocyclic ghrelin receptor antagonists and methods of using the same
US20090275648A1 (en) * 2005-06-13 2009-11-05 Fraser Graeme L Macrocyclic ghrelin receptor antagonists and inverse agonists and methods of using the same
CA2583345A1 (en) * 2005-06-13 2006-12-28 Tranzyme Pharma, Inc. Macrocyclic ghrelin receptor antagonists and inverse agonists and methods of using the same
US8088733B2 (en) 2006-07-06 2012-01-03 Tranzyme Pharma Inc. Methods of using macrocyclic agonists of the ghrelin receptor for treatment of gastrointestinal motility disorders
JP5684474B2 (ja) * 2006-09-11 2015-03-11 オセラ セラピューティクス, インコーポレイテッド 胃腸の運動障害疾患の治療のためのモチリン受容体の大環状アンタゴニスト
AU2008210434C8 (en) 2007-01-31 2014-03-27 Dana-Farber Cancer Institute, Inc. Stabilized p53 peptides and uses thereof
AU2015201862B2 (en) * 2007-02-09 2016-10-13 Tranzyme Pharma, Inc. Macrocyclic ghrelin receptor modulators and methods of using the same
EP2118080B1 (de) * 2007-02-09 2016-08-31 Ocera Therapeutics, Inc. Makrocyclische ghrelin-rezeptormodulatoren und verwendungsverfahren dafür
BRPI0809366B8 (pt) 2007-03-28 2021-05-25 Harvard College polipeptídeo substancialmente alfa-helicoidal, método para fabricação do mesmo, aminoácido e composição farmacêutica
US20080287371A1 (en) * 2007-05-17 2008-11-20 Tranzyme Pharma Inc. Macrocyclic antagonists of the motilin receptor for modulation of the migrating motor complex
US8338565B2 (en) * 2008-08-20 2012-12-25 Ensemble Therapeutics Corporation Macrocyclic compounds for inhibition of tumor necrosis factor alpha
SG177521A1 (en) * 2009-08-05 2012-02-28 Polyphor Ag Conformationally constrained, fully synthetic macrocyclic compounds
JP2013508410A (ja) * 2009-10-23 2013-03-07 トランザイム・ファーマ,インコーポレイテッド セリンプロテアーゼ酵素の大環状阻害剤を使用する方法
JP2013509434A (ja) 2009-10-30 2013-03-14 トランザイム・ファーマ,インコーポレイテッド 大環状グレリン受容体アンタゴニストおよびインバースアゴニストならびにその使用方法
US8859723B2 (en) 2010-08-13 2014-10-14 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
CN108929375A (zh) 2011-10-18 2018-12-04 爱勒让治疗公司 拟肽大环化合物
US8927500B2 (en) 2012-02-15 2015-01-06 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US8987414B2 (en) 2012-02-15 2015-03-24 Aileron Therapeutics, Inc. Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles
JP6526563B2 (ja) 2012-11-01 2019-06-05 エイルロン セラピューティクス,インコーポレイテッド 二置換アミノ酸ならびにその調製および使用の方法
US9119832B2 (en) 2014-02-05 2015-09-01 The Regents Of The University Of California Methods of treating mild brain injury
SG10201902594QA (en) 2014-09-24 2019-04-29 Aileron Therapeutics Inc Peptidomimetic macrocycles and uses thereof
MX2017011834A (es) 2015-03-20 2018-04-11 Aileron Therapeutics Inc Macrociclos peptidomimeticos y usos de los mismos.
MX2018005236A (es) * 2015-10-27 2018-08-15 Hoffmann La Roche Macrociclos peptidicos contra acinetobacter baumannii.
WO2017075535A1 (en) 2015-10-28 2017-05-04 Oxeia Biopharmaceuticals, Inc. Methods of treating neurodegenerative conditions
EP3388444A1 (de) * 2017-04-10 2018-10-17 F. Hoffmann-La Roche AG Antibakterielle peptidmakrozyklen und verwendung davon
US11505573B2 (en) 2018-03-28 2022-11-22 Hoffmann-La Roche Inc. Peptide macrocycles against Acinetobacter baumannii
US11819532B2 (en) 2018-04-23 2023-11-21 Hoffmann-La Roche Inc. Peptide macrocycles against Acinetobacter baumannii
CN108752214A (zh) * 2018-07-09 2018-11-06 上海华堇生物技术有限责任公司 一种2-羟基-β-硝基苯乙烯的新制备方法

Family Cites Families (152)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5175150A (en) 1985-08-31 1992-12-29 Kitasato, Kenkyusho Erythromycin derivative
US5008249A (en) 1985-08-31 1991-04-16 Kitasato Kenkyusho Therapeutic method of stimulating digestive tract contractile motion in mammals
US5695952A (en) 1986-09-12 1997-12-09 Kyowa Hakko Kogyo Co., Ltd. Method for producing Leu13 !motilin
GB8728820D0 (en) 1987-12-09 1988-01-27 Fisons Plc Compounds
US4920102A (en) 1988-04-18 1990-04-24 Eli Lilly And Company Method for treating gastrointestinal disorders
EP0358608A3 (de) * 1988-09-09 1990-10-31 Gesellschaft für Biotechnologische Forschung mbH (GBF) Mikrobizide makrozyklische Laktonderivate
US5459049A (en) * 1989-01-06 1995-10-17 Sanwa Kagaku Kenkyushko Co., Ltd. Motilin-like polypeptide and use thereof
EP0378078A1 (de) * 1989-01-06 1990-07-18 Sanwa Kagaku Kenkyusho Co., Ltd. Dem Motilin ähnliches Polypeptid und seine Verwendung
EP0413532A3 (en) * 1989-08-18 1991-05-15 Fisons Plc Macrocyclic compounds
US5143915A (en) * 1990-07-25 1992-09-01 E. R. Squibb & Sons, Inc. Dihydropyrimidine macrocyclic lactones useful as calcium antagonists and agonists
US5196452A (en) * 1991-01-29 1993-03-23 Genelabs Incorporated Macrocyclic anti-viral compound and method
US5554605A (en) 1991-04-09 1996-09-10 Abbott Laboratories Macrocyclic lactam prokinetic agents
WO1992018134A1 (en) * 1991-04-09 1992-10-29 Abbott Laboratories Macrocyclic lactam prokinetic agents
US5561137A (en) * 1991-09-05 1996-10-01 Abbott Laboratories Thio-heterocyclic macrolactam immunomodulators
US5604294A (en) * 1991-09-05 1997-02-18 Luly; Jay R. Macrocyclic immunomodulators
US5563172A (en) * 1991-09-05 1996-10-08 Abbott Laboratories Macrocyclic amide and urea immunomodulators
US5534632A (en) 1991-09-05 1996-07-09 Abbott Laboratories Macrocyclic carbamate immunomodulators
US5604234A (en) * 1991-09-05 1997-02-18 Abbott Laboratories Substituted thiol macrolactam immunomodulators
US5708002A (en) * 1991-09-05 1998-01-13 Abbott Laboratories Macrocyclic immunomodulators
EP0642516B1 (de) * 1991-09-05 2002-06-05 Abbott Laboratories Makrocyclische immunmodulatoren
US5457111A (en) * 1991-09-05 1995-10-10 Abbott Laboratories Macrocyclic immunomodulators
US5244889A (en) * 1991-11-26 1993-09-14 Ciba-Geigy Corporation Certain macrocyclic lactam derivatives
DE4200145A1 (de) 1992-01-07 1993-07-08 Kali Chemie Pharma Gmbh 7,10-epoxy-oxacyclododecan-derivate, verfahren und zwischenprodukte zu ihrer herstellung und diese verbindungen enthaltende arzneimittel
ATE138925T1 (de) 1992-03-19 1996-06-15 Takeda Chemical Industries Ltd Erythromycinderivate, herstellung und verwendung davon
MY113693A (en) * 1992-05-26 2002-05-31 Chugai Pharmaceutical Co Ltd Erythromycin derivatives having an enterokinesis stimulating action
US5328902A (en) * 1992-08-13 1994-07-12 American Cyanamid Co. 7-(substituted)-9-[(substituted glycyl)amido]-6-demethyl-6-deoxytetracyclines
US5292741A (en) * 1992-08-18 1994-03-08 Merck & Co., Inc. Macrocycles incorporating quinazolinones
US5252579A (en) * 1993-02-16 1993-10-12 American Home Products Corporation Macrocyclic immunomodulators
EP0690713A4 (de) * 1993-03-17 1996-04-03 Abbott Lab Substituiertes alicyclisches amin enthaltende makrocyclische immunomodulatoren
WO1994021634A1 (en) * 1993-03-17 1994-09-29 Abbott Laboratories Substituted alicyclic-aliphatic amine-containing macrocyclic immunomodulators
US5457194A (en) * 1993-03-17 1995-10-10 Abbott Laboratories Substituted aliphatic amine-containing macrocyclic immunomodulators
US5422341A (en) * 1993-08-06 1995-06-06 Ohmeda Pharmaceutical Products Division Inc. Motilin-like polypeptides with gastrointestinal motor stimulating activity
US5470830A (en) 1993-08-06 1995-11-28 Ohmeda Pharmaceutical Products Division Inc. Motilin-like polypeptides that inhibit gastrointestinal motor activity
US5612350A (en) * 1993-11-30 1997-03-18 Abbott Laboratories Macrocyclic immunomodulators with novel cyclohexyl ring replacements
BR9404831A (pt) 1993-12-07 1995-08-08 Lilly Co Eli Composto,formulação farmacêutica e processo de preparação de um composto
US5624949A (en) * 1993-12-07 1997-04-29 Eli Lilly And Company Protein kinase C inhibitors
ATE198602T1 (de) * 1994-02-04 2001-01-15 Merrell Pharma Inc Makrocyclische difluorostatonderivate als antivirale mittel
US6100377A (en) * 1994-06-10 2000-08-08 The Trustees Of The University Of Pennsylvania Constrained peptides
AUPM982594A0 (en) * 1994-12-02 1995-01-05 University Of Queensland, The HIV protease inhibitors
GB9511357D0 (en) * 1995-06-06 1995-08-02 Johnson Matthey Plc Improved antiviral compounds
US5811515A (en) 1995-06-12 1998-09-22 California Institute Of Technology Synthesis of conformationally restricted amino acids, peptides, and peptidomimetics by catalytic ring closing metathesis
US6124453A (en) * 1995-07-04 2000-09-26 Novartis Ag Macrolides
US6281352B1 (en) 1995-11-14 2001-08-28 Dupont Pharmaceuticals Company Macrocyclic compounds as metalloprotease inhibitors
KR100304210B1 (ko) * 1995-11-20 2001-11-05 피터 지. 스트링거 단백질키나아제c억제제
US5888971A (en) * 1996-02-20 1999-03-30 Ortho Pharmaceutical Corporation, Inc. Macrocyclic peptides useful in the treatment of thrombin related disorders
US5849691A (en) 1996-02-20 1998-12-15 The United States Of America As Represented By The Department Of Health And Human Services Peptidomimetic inhibitors of cathepsin D and plasmepsins I and II
IL117426A (en) * 1996-03-10 2005-09-25 Yissum Res Dev Co Synthetic pseudopeptides having osteogenic activity and pharmaceutical compositions containing the same
US5734012A (en) * 1996-05-16 1998-03-31 Ohmeda Pharmaceutical Products Division Inc. Cyclic motilin-like polypeptides with gastrointestinal motor stimulating activity
CA2207137A1 (en) * 1996-06-14 1997-12-14 James Erwin Fritz Scavenger assisted combinatorial process for preparing libraries of secondary amine compounds
US5712253A (en) * 1996-06-18 1998-01-27 Abbott Laboratories Macrocyclic 13-membered ring derivatives of erythromycins A and B
DE19644195A1 (de) * 1996-10-24 1998-04-30 Solvay Pharm Gmbh 10,13,15-Trioxatricyclo[9.2.1.1.·9·.·6·]-pentadecanon-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel
WO1998023629A1 (fr) * 1996-11-26 1998-06-04 Chugai Seiyaku Kabushiki Kaisha Composes de macrolides comportant une chaine a 13 elements, medicament les contenant et leur procede de preparation
US6867305B2 (en) * 1996-12-03 2005-03-15 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
MX9709494A (es) * 1996-12-04 1998-07-31 Pfizer Compuestos peptidicos ciclicos, procedimiento para su produccion, composiciones que los contienen y uso de los mismos.
US5952320A (en) * 1997-01-07 1999-09-14 Abbott Laboratories Macrocyclic inhibitors of matrix metalloproteinases and TNFα secretion
US6380158B1 (en) 1997-03-24 2002-04-30 Zymogenetics, Inc. Motilin homologs
US6291653B1 (en) 1997-03-24 2001-09-18 Zymogenetics, Inc. Antibodies to motilin homologs
WO1998042840A1 (en) 1997-03-24 1998-10-01 Zymogenetics, Inc. Motilin homologs
EP1015479A4 (de) 1997-04-11 2002-07-24 Lilly Co Eli Kombinatorische substanzbibliotheken von peptidomimetischen makrocyclen sowie die dazugehörigen verfahren
JP3583928B2 (ja) 1997-08-15 2004-11-04 中外製薬株式会社 フェネチルアミン誘導体
TW460478B (en) * 1997-08-15 2001-10-21 Chugai Pharmaceutical Co Ltd Phenethylamine derivatives
US5972939A (en) 1997-10-28 1999-10-26 Ortho-Mcneil Pharmaceutical, Inc. Cyclopentene derivatives useful as antagonists of the motilin receptor
JP4200393B2 (ja) 1997-11-25 2008-12-24 ソニー株式会社 情報処理装置および情報処理方法
US6080838A (en) * 1997-11-25 2000-06-27 University Of Virginia Patent Foundation Peptidomimetic of helix-turn-helix or gamma-turn
US6165985A (en) 1998-02-13 2000-12-26 Solvay Pharmaceuticals Gmbh 11-acetyl-12,13-dioxabicyclo[8.2.1]-tridecenone derivatives, processes for their preparation and pharmaceutical compositions comprising them
US6228986B1 (en) * 1998-04-13 2001-05-08 Ortho-Mcneil Pharmaceutical, Inc. Solid-phase synthesis of novel 14-membered macroycles for high throughput screening
EP1084113A1 (de) * 1998-06-11 2001-03-21 Du Pont Pharmaceuticals Company Verfahren zur herstellung von macrozyclischen metallproteaseinhibitoren
SE9802080D0 (sv) * 1998-06-11 1998-06-11 Hellstroem Pharmaceutical composition for the treatment of functional dyspepsia and/or irritable bowel syndrome and new use of substances therein
CA2330251A1 (en) 1998-06-12 1999-12-16 Merck & Co., Inc. Cloning and identification of the motilin receptor
EP1090012A4 (de) * 1998-07-02 2005-04-06 Merck & Co Inc Inhibitoren der prenyl-protein-transferase
EP1090011A4 (de) * 1998-07-02 2005-04-06 Merck & Co Inc Inhibitoren von prenyl-protein-transferase
WO2000001382A1 (en) * 1998-07-02 2000-01-13 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
TW509699B (en) * 1998-09-24 2002-11-11 Chugau Pharmaceutical Co Ltd Ethylamine derivatives
AUPP616498A0 (en) * 1998-09-25 1998-10-15 University Of Queensland, The Synthesis of cyclic peptides
AU1447700A (en) 1998-10-28 2000-05-15 Kosan Biosciences, Inc. Library of novel "unnatural" natural products
US6329376B1 (en) 1998-10-29 2001-12-11 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
CZ20012714A3 (cs) * 1999-01-28 2002-08-14 Chugai Seiyaku Kabushiki Kaisha Substituované deriváty fenetylaminu
US20020058286A1 (en) * 1999-02-24 2002-05-16 Danishefsky Samuel J. Synthesis of epothilones, intermediates thereto and analogues thereof
JP4269041B2 (ja) * 1999-03-02 2009-05-27 国立大学法人九州工業大学 新規な環状テトラペプチド誘導体とその医薬用途
US6121257A (en) * 1999-03-31 2000-09-19 Abbott Laboratories Sulfamate containing macrocyclic immunomodulators
US6608027B1 (en) * 1999-04-06 2003-08-19 Boehringer Ingelheim (Canada) Ltd Macrocyclic peptides active against the hepatitis C virus
CA2377721A1 (en) 1999-06-30 2001-01-04 Zymogenetics, Inc. Sgip peptides
US6420521B1 (en) 1999-06-30 2002-07-16 Zymogenetics, Inc. Short gastrointestinal peptides
DE19933701A1 (de) 1999-07-19 2001-01-25 Wilex Biotechnology Gmbh Zyklische peptidomimetische Urokinaserezeptorantagonisten
US6660832B1 (en) 1999-08-20 2003-12-09 Isis Pharmaceuticals, Inc. Macrocyclic compounds and preparation methods thereof
DE19942624A1 (de) 1999-08-28 2001-03-08 Chemotopix Gmbh Verfahren zur Herstellung von zyklischen Peptidomimetika
CA2384151A1 (en) * 1999-09-09 2001-03-15 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
CA2284459C (en) * 1999-10-04 2012-12-11 Neokimia Inc. Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery
GB9929318D0 (en) 1999-12-10 2000-02-02 Prometic Biosciences Limited Macrocyclic compounds and their use
US6566385B2 (en) * 2000-01-12 2003-05-20 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
AU2001230864A1 (en) * 2000-01-12 2001-07-24 Merck And Co., Inc. Inhibitors of prenyl-protein transferase
AU2001227757A1 (en) * 2000-01-12 2001-07-24 Merck And Co., Inc. Inhibitors of prenyl-protein transferase
AU2001227755A1 (en) * 2000-01-12 2001-07-24 Merck And Co., Inc. Inhibitors of prenyl-protein transferase
US6525074B2 (en) * 2000-01-12 2003-02-25 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
CA2397670C (en) 2000-01-18 2010-06-08 Mcgill University .beta.-turn peptidomimetic cyclic compounds
WO2001053331A2 (en) 2000-01-24 2001-07-26 Adherex Technologies, Inc. Peptidomimetic modulators of cell adhesion
WO2001068620A1 (en) 2000-03-13 2001-09-20 Ortho-Mcneil Pharmaceutical, Inc. Novel cyclopentene derivatives useful as antagonists of the motilin receptor
US6423714B2 (en) * 2000-03-13 2002-07-23 Ortho Mcneil-Pharmaceutical, Inc.. Cyclohexene derivatives useful as antagonists of the motilin receptor
WO2001068622A1 (en) 2000-03-13 2001-09-20 Ortho-Mcneil Pharmaceutical, Inc. Novel cyclobutene derivatives useful as antagonists of the motilin receptor
EP1268525B1 (de) 2000-04-05 2008-12-31 Schering Corporation Makrozyklische inhibitoren der ns3-serinprotease des hepatitis c-virus mit stickstoffhaltigen zyklischen p2-gruppen
AU2001251444A1 (en) * 2000-04-10 2001-10-23 Merck And Co., Inc. Inhibitors of prenyl-protein transferase
AU2001253246A1 (en) * 2000-04-10 2001-10-23 Merck And Co., Inc. Inhibitors of prenyl-protein transferase
US6610722B2 (en) * 2000-04-10 2003-08-26 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
AR030558A1 (es) * 2000-04-19 2003-08-27 Schering Corp COMPUESTOS MACROCICLICOS, QUE INCLUYEN ENANTIOMEROS, ESTEROISOMEROS, ROTAMEROS Y TAUTOMEROS, SALES Y SOLVATOS FARMACEUTICAMENTE ACEPTABLES, COMPOSICIoN FARMACEUTICA, UN METODO PARA SU PREPARACION Y EL USO DE DICHOS COMPUESTOS PARA LA ELABORACION DE UN MEDICAMENTO, INHIBIDORES DE LA SERINA PROTEASA,
US6511980B2 (en) * 2000-05-05 2003-01-28 Ortho Mcneil Pharmaceutical, Inc. Substituted diamine derivatives useful as motilin antagonists
ATE446758T1 (de) * 2000-05-31 2009-11-15 Pfizer Prod Inc Verwendung von wachstumshormonsekretagoga zur förderung der beweglichkeit des verdauungstrakts
US6721353B1 (en) 2000-06-21 2004-04-13 Cisco Technology, Inc. Network compatibility
US7018981B2 (en) 2000-08-24 2006-03-28 Chugai Seiyaku Kabushiki Kaisha Cyclic motilin receptor antagonists
US7115651B2 (en) * 2000-08-25 2006-10-03 Sloan-Kettering Institute For Cancer Research Macrocycles and uses thereof
US20050085426A1 (en) 2000-09-05 2005-04-21 Michel Bessodes Acid-sensitive compounds, preparation and use thereof
AU2001214172A1 (en) 2000-11-20 2002-05-27 Lead Chemical Co., Ltd. Macrocyclic compound
US7279304B2 (en) 2000-12-18 2007-10-09 President And Fellows Of Harvard College Methods for preparation of macrocyclic molecules and macrocyclic molecules prepared thereby
WO2002051413A2 (en) 2000-12-27 2002-07-04 Shire Biochem Inc. Macrocyclic anti-viral compounds
WO2002059141A1 (fr) 2001-01-25 2002-08-01 Chugai Seiyaku Kabushiki Kaisha Derives peptidiques
KR20020066476A (ko) 2001-02-12 2002-08-19 쥬가이 세이야쿠 가부시키가이샤 펩타이드 유도체의 제조방법
JP4310106B2 (ja) 2001-02-23 2009-08-05 ポリファー リミテッド 抗菌活性を有するテンプレート結合ペプチド擬似体
EP1392679B1 (de) 2001-05-10 2005-11-02 Solvay Pharmaceuticals GmbH Neue 1-amidomethylcarbonyl-piperidinderivate, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel
CA2450202A1 (en) 2001-06-12 2002-12-19 Elan Pharmaceuticals, Inc. Macrocycles useful in the treatment of alzheimer's disease
EP1395257A1 (de) 2001-06-12 2004-03-10 Elan Pharmaceuticals, Inc. Makrocyclische verbindungen zur behandlung der alzheimer-krankheit
DE10146104A1 (de) 2001-09-19 2003-04-03 Bayer Ag Antibakterielle Markrozyklen
AU2002363328A1 (en) * 2001-11-06 2003-05-19 President And Fellows Of Harvard College Methods for preparation of macrocyclic molecules macrocyclic molecules prepared thereby and substrates and solid supports for use therein
CN101157924A (zh) 2001-12-11 2008-04-09 人体基因组科学有限公司 嗜中性白细胞因子α
US6867185B2 (en) * 2001-12-20 2005-03-15 Bristol-Myers Squibb Company Inhibitors of hepatitis C virus
US7119072B2 (en) 2002-01-30 2006-10-10 Boehringer Ingelheim (Canada) Ltd. Macrocyclic peptides active against the hepatitis C virus
CA2369711A1 (en) 2002-01-30 2003-07-30 Boehringer Ingelheim (Canada) Ltd. Macrocyclic peptides active against the hepatitis c virus
US6972281B2 (en) * 2002-02-07 2005-12-06 University Of Ottawa Histogranin-like peptides and non-peptides, processes for their preparation and uses thereof
WO2003068168A2 (en) 2002-02-14 2003-08-21 The Brigham And Women's Hospital, Inc. Helical peptidomimetics and use b-amyloid-associated diseases
KR101210018B1 (ko) 2002-03-08 2012-12-07 에자이 알앤드디 매니지먼트 가부시키가이샤 약물로서 유용한 거대고리 화합물
US20030221432A1 (en) 2002-06-03 2003-12-04 Tucker Ronald M. Solid fuel combustion method and apparatus for the conversion of waste into useful energy
DE10226921A1 (de) 2002-06-17 2003-12-24 Bayer Ag Antibakterielle Amid-Makrozyklen
EP1515921B1 (de) 2002-06-24 2006-03-08 Rockwool International A/S Verfahren und vorrichtung zum regeln bei der herstellung von mineralwolle mittels eines kaskadenrotors
DE10232094A1 (de) 2002-07-15 2004-02-05 GESELLSCHAFT FüR BIOTECHNOLOGISCHE FORSCHUNG MBH (GBF) 5-Thiaepothilone und 15-disubstituierte Epothilone
DE10234422A1 (de) 2002-07-29 2004-02-12 Bayer Ag Antibakterielle Ester-Makrozyklen
EP1532164B1 (de) 2002-08-20 2012-09-26 Polyphor Ltd. Template-fixierte peptidmimetika mit antibakterieller wirkung
DE10239042A1 (de) 2002-08-21 2004-03-04 Schering Ag Makrozyclische Pyrimidine, deren Herstellung und Verwendung als Arzneimittel
US6747009B2 (en) * 2002-09-19 2004-06-08 Universiteit Leiden Peptidomimetic glutathione analogs
US6653334B1 (en) 2002-12-27 2003-11-25 Kowa Co., Ltd. Benzoxazole compound and pharmaceutical composition containing the same
WO2004111077A1 (en) 2003-06-18 2004-12-23 Tranzyme Pharma Inc. Macrocyclic antagonists of the motilin receptor
US7491695B2 (en) * 2003-06-18 2009-02-17 Tranzyme Pharma Inc. Methods of using macrocyclic modulators of the ghrelin receptor
US7476653B2 (en) * 2003-06-18 2009-01-13 Tranzyme Pharma, Inc. Macrocyclic modulators of the ghrelin receptor
US20090198050A1 (en) * 2003-06-18 2009-08-06 Tranzyme Pharma Inc. Macrocyclic Modulators of the Ghrelin Receptor
USRE42013E1 (en) 2003-06-18 2010-12-28 Tranzyme Pharma Inc. Macrocyclic modulators of the ghrelin receptor
EP1648923B1 (de) * 2003-07-31 2008-12-31 Tranzyme Pharma Inc. Räumlich definierte makrocyclen, die peptidbindungssurrogate enthalten
EP2316846B1 (de) 2003-07-31 2019-10-02 Ocera Therapeutics, Inc. Räumlich definierte makrozyklische Verbindungen zur Entdeckung von Arzneimitteln
MXPA06002435A (es) * 2003-09-03 2006-06-20 Kowa Co Compuesto activador del receptor activado por el proliferador de peroxisoma y composicion farmaceutica que lo contiene.
US20090275648A1 (en) * 2005-06-13 2009-11-05 Fraser Graeme L Macrocyclic ghrelin receptor antagonists and inverse agonists and methods of using the same
JP5684474B2 (ja) * 2006-09-11 2015-03-11 オセラ セラピューティクス, インコーポレイテッド 胃腸の運動障害疾患の治療のためのモチリン受容体の大環状アンタゴニスト
EP2118080B1 (de) * 2007-02-09 2016-08-31 Ocera Therapeutics, Inc. Makrocyclische ghrelin-rezeptormodulatoren und verwendungsverfahren dafür
US20080287371A1 (en) * 2007-05-17 2008-11-20 Tranzyme Pharma Inc. Macrocyclic antagonists of the motilin receptor for modulation of the migrating motor complex
US8018037B2 (en) 2009-04-16 2011-09-13 Mediatek Inc. Semiconductor chip package
MX2012003912A (es) 2009-09-30 2012-08-17 Tranzyme Pharma Inc Sales, solvatos y composiciones farmaceuticas de los agonistas macrociclicos del receptor de ghrelina y metodos para su uso.
JP2013509434A (ja) * 2009-10-30 2013-03-14 トランザイム・ファーマ,インコーポレイテッド 大環状グレリン受容体アンタゴニストおよびインバースアゴニストならびにその使用方法

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US20160221927A1 (en) 2016-08-04
US20120165566A1 (en) 2012-06-28
US20110245459A1 (en) 2011-10-06
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US8129561B2 (en) 2012-03-06
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