DE69404632T2 - Verfahren zur herstellung von trans-6-[2-(substituierte-pyrrol-1-yl)alkyl]pyran-2-one verwendbar als inhibitoren der cholesterol-synthese - Google Patents

Verfahren zur herstellung von trans-6-[2-(substituierte-pyrrol-1-yl)alkyl]pyran-2-one verwendbar als inhibitoren der cholesterol-synthese

Info

Publication number
DE69404632T2
DE69404632T2 DE69404632T DE69404632T DE69404632T2 DE 69404632 T2 DE69404632 T2 DE 69404632T2 DE 69404632 T DE69404632 T DE 69404632T DE 69404632 T DE69404632 T DE 69404632T DE 69404632 T2 DE69404632 T2 DE 69404632T2
Authority
DE
Germany
Prior art keywords
pyran
substituted
alkyl
pyrrol
inhibitors
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.)
Expired - Fee Related
Application number
DE69404632T
Other languages
English (en)
Other versions
DE69404632D1 (de
Inventor
Donald BUTLER
Tung Van Le
Thomas Nanninga
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.)
Warner Lambert Co LLC
Original Assignee
Warner Lambert Co LLC
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 Warner Lambert Co LLC filed Critical Warner Lambert Co LLC
Application granted granted Critical
Publication of DE69404632D1 publication Critical patent/DE69404632D1/de
Publication of DE69404632T2 publication Critical patent/DE69404632T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
DE69404632T 1993-03-03 1994-02-24 Verfahren zur herstellung von trans-6-[2-(substituierte-pyrrol-1-yl)alkyl]pyran-2-one verwendbar als inhibitoren der cholesterol-synthese Expired - Fee Related DE69404632T2 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US08/025,701 US5298627A (en) 1993-03-03 1993-03-03 Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis
PCT/US1994/002180 WO1994020492A1 (en) 1993-03-03 1994-02-24 Novel process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis

Publications (2)

Publication Number Publication Date
DE69404632D1 DE69404632D1 (de) 1997-09-04
DE69404632T2 true DE69404632T2 (de) 1998-01-29

Family

ID=21827596

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69404632T Expired - Fee Related DE69404632T2 (de) 1993-03-03 1994-02-24 Verfahren zur herstellung von trans-6-[2-(substituierte-pyrrol-1-yl)alkyl]pyran-2-one verwendbar als inhibitoren der cholesterol-synthese

Country Status (19)

Country Link
US (8) US5298627A (de)
EP (1) EP0687263B1 (de)
JP (1) JP3510253B2 (de)
KR (1) KR100302431B1 (de)
AT (1) ATE156127T1 (de)
AU (1) AU677047B2 (de)
CA (1) CA2155952C (de)
CZ (4) CZ284365B6 (de)
DE (1) DE69404632T2 (de)
DK (1) DK0687263T3 (de)
ES (1) ES2108435T3 (de)
FI (3) FI109999B (de)
GR (1) GR3024784T3 (de)
HU (1) HU222177B1 (de)
NO (3) NO308529B1 (de)
NZ (1) NZ262830A (de)
RU (1) RU2138497C1 (de)
SK (4) SK281110B6 (de)
WO (1) WO1994020492A1 (de)

Families Citing this family (151)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5298627A (en) * 1993-03-03 1994-03-29 Warner-Lambert Company Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis
DE4415331A1 (de) * 1994-05-02 1995-11-09 Sobrevin Fadenspeichervorrichtung mit einstellbarem Fadenabzugswiderstand
US5385929A (en) * 1994-05-04 1995-01-31 Warner-Lambert Company [(Hydroxyphenylamino) carbonyl] pyrroles
HRP960312B1 (en) 1995-07-17 2001-10-31 Warner Lambert Co NOVEL PROCESS FOR THE PRODUCTION OF AMORPHOUS /R-(R*, R*)/-2-(4-FLUOROPHENYL)-"beta", "delta"-DIHYDROXY-5-PHENYL-4-/(PHENYLAMINO)CARBONYL/-1H-PYRROLE -1-HEPTANOIC ACID CALCIUM SALT (2 : 1)
US6087511A (en) * 1996-07-16 2000-07-11 Warner-Lambert Company Process for the production of amorphous [R-(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl )-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid) calcium salt (2:1)
US20030105154A1 (en) * 2001-10-24 2003-06-05 Bisgaier Charles Larry Statin-carboxyalkylether combinations
AU755543B2 (en) * 1997-12-19 2002-12-12 Warner-Lambert Export Limited Process for the synthesis of 1,3-diols
SI20109A (sl) * 1998-12-16 2000-06-30 LEK, tovarna farmacevtskih in kemi�nih izdelkov, d.d. Stabilna farmacevtska formulacija
IN191236B (de) * 1999-05-25 2003-10-11 Ranbaxy Lab Ltd
US20040063969A1 (en) * 1999-10-18 2004-04-01 Egis Gyogyszergyar Rt. Process for the preparation of amorphous atorvastatin calcium
US7411075B1 (en) 2000-11-16 2008-08-12 Teva Pharmaceutical Industries Ltd. Polymorphic form of atorvastatin calcium
EP1237865B1 (de) 1999-12-17 2005-11-16 Pfizer Science and Technology Ireland Limited Herstellungsverfahren auf industrieller basis von atorvastatin trihydrat hemi-kalziumsalz in kristalliner form
CA2391357C (en) * 1999-12-17 2009-01-06 Warner Lambert Research And Development Ireland Limited A process for producing crystalline atorvastatin calcium
US7608445B1 (en) 1999-12-29 2009-10-27 Verenium Corporation Nitrilases, nucleic acids encoding them and methods for making and using them
US7300775B2 (en) 1999-12-29 2007-11-27 Verenium Corporation Methods for producing α-substituted carboxylic acids using nitrilases and strecker reagents
US20040014195A1 (en) * 1999-12-29 2004-01-22 Diversa Corporation Nitrilases, nucleic acids encoding them and methods for making and using them
US7521216B2 (en) 1999-12-29 2009-04-21 Verenium Corporation Nitrilases and methods for making and using them
US6777552B2 (en) * 2001-08-16 2004-08-17 Teva Pharmaceutical Industries, Ltd. Processes for preparing calcium salt forms of statins
IL155890A0 (en) * 2000-11-16 2003-12-23 Teva Pharma HYDROLYSIS OF [R(R*,R*)]-2-(4-FLUOROPHENYL)-beta,delta-DIHYDROXY-5-(1-METHYLETHYL)-3-PHENYL-4-[(PHENYLAMINO)CARBONYL]-1H-PYRROLE-1-HEPTANOIC ACID ESTERS WITH CALCIUM HYDROXIDE
IL156055A0 (en) * 2000-11-30 2003-12-23 Teva Pharma Novel crystal forms of atorvastatin hemi calcium and processes for their preparation as well as novel processes for preparing other forms
US7501450B2 (en) * 2000-11-30 2009-03-10 Teva Pharaceutical Industries Ltd. Crystal forms of atorvastatin hemi-calcium and processes for their preparation as well as novel processes for preparing other forms
WO2002051804A1 (en) * 2000-12-27 2002-07-04 Ciba Specialty Chemicals Holding Inc. Crystalline forms of atorvastatin
US6476235B2 (en) 2001-01-09 2002-11-05 Warner-Lambert Company Process for the synthesis of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide
EP1728785A1 (de) * 2001-01-09 2006-12-06 Warner-Lambert Company LLC 7-[(2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4-phenylcarbamoyl-pyrrol-1-yl]-heptanoic acid ester 3,5-dioxo-acetal
WO2002057229A1 (en) * 2001-01-19 2002-07-25 Biocon India Limited FORM V CRYSTALLINE [R-(R*,R*)]-2-(4-FLUOROPHENYL)-ß,$G(D)-DIHYDROXY-5-(1-METHYLETHYL)-3-PHENYL-4-[(PHENYLAMINO)CARBONYL]-1H-PYRROLE-1- HEPTANOIC ACID HEMI CALCIUM SALT. (ATORVASTATIN)
SI20814A (sl) 2001-01-23 2002-08-31 LEK, tovarna farmacevtskih in kemi�nih izdelkov, d.d. Priprava amorfnega atorvastatina
SI20848A (sl) 2001-03-14 2002-10-31 Lek, Tovarna Farmacevtskih In Kemijskih Izdelkov, D.D. Farmacevtska formulacija, ki vsebuje atorvastatin kalcij
CA2450111C (en) * 2001-06-29 2006-02-07 Warner-Lambert Company Llc Crystalline forms of [r-(r*,r*)]-2-(4-fluorophenyl)-beta, delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[phenylamino)carbonyl]-1h-pyrrole-1-heptanoic acid calcium salt(2:1)(atorvastatin)
WO2003004455A2 (de) * 2001-07-06 2003-01-16 Teva Pharmaceutical Industries Ltd. Synthesis and intermediates
CA2451159A1 (en) * 2001-07-06 2003-01-16 Teva Pharmaceutical Industries Ltd. Process for the preparation of 7-amino syn 3,5-dihydroxy heptanoic acid derivatives via 6-cyano syn 3,5-dihydroxy hexanoic acid derivatives
US7074818B2 (en) * 2001-07-30 2006-07-11 Dr. Reddy's Laboratories Limited Crystalline forms VI and VII of Atorvastatin calcium
EP1414796A1 (de) 2001-07-30 2004-05-06 Dr. Reddy's Laboratories Ltd. Kristalline formen vi und vii des kalzium atorvastatins
WO2003018547A2 (en) * 2001-08-31 2003-03-06 Morepen Laboratories Ltd. An improved process for the preparation of amorphous atorvastatin calcium salt (2:1)
CA2412012C (en) * 2001-11-20 2011-08-02 Ed. Geistlich Soehne Ag Fuer Chemische Industrie Resorbable extracellular matrix containing collagen i and collagen ii for reconstruction of cartilage
US20060020137A1 (en) * 2001-11-29 2006-01-26 Limor Tessler Novel crystal forms of atorvastatin hemi-calcium and processes for their preparation as well as novel processes for preparing other forms
UA77990C2 (en) * 2001-12-12 2007-02-15 Crystalline calcium salt of (2:1) [r-(r*,r*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1h-pyrroleheptanic acid
CZ296967B6 (cs) 2002-02-01 2006-08-16 Zentiva, A.S. Zpusob výroby amorfní formy hemivápenaté soli (3R,5R) 7-[3-fenyl-4-fenylkarbamoyl-2-(4-fluorfenyl)-5-isopropylpyrrol-1-yl]-3,5-dihydroxyheptanové kyseliny (atorvastatinu)
CN100379723C (zh) * 2002-02-19 2008-04-09 特瓦制药工业有限公司 阿托伐他汀半钙脱溶剂的方法和基本上不含有机溶剂的阿托伐他汀半钙
DE10212492B4 (de) * 2002-03-21 2012-02-02 Daimler Ag Kolbenpumpe
EP1496982A4 (de) * 2002-04-16 2006-07-19 Merck & Co Inc Feste formen von salzen mit tyrosinkinase-wirkung
AU2003251523A1 (en) 2002-06-13 2003-12-31 Diversa Corporation Processes for making (r)-ethyl 4-cyano-3-hydroxybutyric acid
US20060211761A1 (en) * 2002-07-08 2006-09-21 Yatendra Kumar Hmg-coa-reductase inhibitors
US7078430B2 (en) * 2002-07-08 2006-07-18 Ranbaxy Laboratories Limited HMG CoA-reductase inhibitors
RU2279430C2 (ru) * 2002-08-06 2006-07-10 Уорнер-Ламберт Компани Ллс Способ получения фениламида 5-(4-фторфенил)-1-[2-(2r,4r)-4-гидрокси-6-оксотетрагидропиран-2-ил)этил]-2-изопропил-4-фенил-1h-пиррол-3-карбоновой кислоты
WO2004022053A1 (en) * 2002-09-03 2004-03-18 Morepen Laboratories Limited Atorvastatin calcium form vi or hydrates thereof
SI21302A (sl) * 2002-10-11 2004-04-30 LEK farmacevtska dru�ba d.d. Stabiliziran farmacevtski izdelek z amorfno aktivno učinkovino
HRP20020885B1 (en) * 2002-11-11 2007-05-31 GlaxoSmithKline istra�iva�ki centar Zagreb d.o.o. SUBSTITUTED 9a-N-{N'-[4-(SULFONYL)PHENYLCARBAMOYL]}DERIVATIVES 9-DEOXO-9-DIHYDRO-9a-AZA-9a-HOMOERITHROMYCIN A AND 5-O-DESOZAMINYL-9-DEOXO-9-DIHYDRO-9a-AZA-9a-HOMOERITHRONOLIDE A
EP1424324A1 (de) * 2002-11-28 2004-06-02 Teva Pharmaceutical Industries Limited Kristalline Form F von Atorvastatin
US20040198800A1 (en) * 2002-12-19 2004-10-07 Geoffrey Allan Lipoxygenase inhibitors as hypolipidemic and anti-hypertensive agents
US20040132771A1 (en) * 2002-12-20 2004-07-08 Pfizer Inc Compositions of choleseteryl ester transfer protein inhibitors and HMG-CoA reductase inhibitors
AU2003283769A1 (en) 2002-12-20 2004-07-14 Pfizer Products Inc. Dosage forms comprising a cetp inhibitor and an hmg-coa reductase inhibitor
HU227041B1 (en) * 2003-03-24 2010-05-28 Richter Gedeon Nyrt Process for the synthesis of amorphous atorvastatin calcium
RS20050760A (sr) * 2003-04-14 2008-04-04 Warner-Lambert Company Llc., Postupak za izradu fenilamida 5-(4- fluorofenil)-1-(2-((2r, 4r)-4-hidroksi- 6-okso-tetrahidro-piran-2-il)etil)-2- izopropil-4-fenil-1h-pirol-3- karboksilne kiseline
US20050182125A1 (en) * 2003-05-16 2005-08-18 Ambit Biosciences Corporation Pyrrole compounds and uses thereof
US20040248972A1 (en) * 2003-05-16 2004-12-09 Ambit Biosciences Corporation Compounds and uses thereof
WO2004103960A2 (en) * 2003-05-16 2004-12-02 Ambit Biosciences Corporation Compounds and uses thereof
US7790197B2 (en) * 2003-06-09 2010-09-07 Warner-Lambert Company Llc Pharmaceutical compositions of atorvastatin
US7655692B2 (en) 2003-06-12 2010-02-02 Pfizer Inc. Process for forming amorphous atorvastatin
US20050271717A1 (en) * 2003-06-12 2005-12-08 Alfred Berchielli Pharmaceutical compositions of atorvastatin
US20040253305A1 (en) * 2003-06-12 2004-12-16 Luner Paul E. Pharmaceutical compositions of atorvastatin
BRPI0412786A (pt) * 2003-07-25 2006-09-26 Avecia Pharmaceuticals Ltd processo para a preparação de um composto, e, composto
CN1839114A (zh) 2003-08-21 2006-09-27 默克弗罗斯特加拿大有限公司 组织蛋白酶半胱氨酸蛋白酶抑制剂
CN101318923A (zh) * 2003-09-17 2008-12-10 沃尼尔·朗伯有限责任公司 [R－(R*,R*)]－2－(4－氟苯基)－β,δ－二羟基－5－(1－甲基乙基)－3－苯基－4－[(苯基氨基)羰基]－1H－吡咯－1－庚酸的结晶形式
US8227434B1 (en) 2003-11-04 2012-07-24 H. Lee Moffitt Cancer Center & Research Institute, Inc. Materials and methods for treating oncological disorders
CA2546601A1 (en) 2003-11-19 2005-06-09 Metabasis Therapeutics, Inc. Novel phosphorus-containing thyromimetics
BRPI0417138A (pt) * 2003-12-05 2007-02-21 Warner Lambert Co n-alquil-pirroles como inibidores de hmg-coa-redutase
US20050152323A1 (en) * 2004-01-12 2005-07-14 Vincent Bonnassieux Plug-in Wi-Fi access point device and system
CA2456430A1 (en) * 2004-01-28 2005-07-28 Brantford Chemicals Inc. Improved process for the preparation of amorphous atorvastatin calcium
PT1727795E (pt) 2004-03-17 2012-04-11 Ranbaxy Lab Ltd Processo para a produção de atorvastatina cálcica na forma amorfa
RU2330840C1 (ru) * 2004-04-16 2008-08-10 Пфайзер Продактс Инк. Способ получения аморфного кальций аторвастатина
ES2739493T3 (es) 2004-05-05 2020-01-31 Pfizer Prod Inc Formas de sal de de atorvastatina con benetamina
ES2586561T3 (es) * 2004-07-16 2016-10-17 Lek Pharmaceuticals D.D. Productos de degradación oxidativa de atorvastatina calcio
JP2008506764A (ja) 2004-07-20 2008-03-06 ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー ［Ｒ−（Ｒ＊，Ｒ＊）］−２−（４−フルオロフェニル）−β、δ−ジヒドロキシ−５−（１−メチルエチル）−３−フェニル−４−［（フェニルアミノ）カルボニル］−１Ｈ−ピロール−１−ヘプタン酸カルシウム塩（２：１）の新規形態
JP2008510798A (ja) * 2004-08-27 2008-04-10 バイオコン・リミテッド 非晶質アトルバスタチンカルシウムのための方法
AU2005298383A1 (en) 2004-10-28 2006-05-04 Warner-Lambert Company Llc Process for forming amorphous atorvastatin
US20090208539A1 (en) * 2004-11-22 2009-08-20 Adel Penhasi Stable atorvastatin formulations
JP2008521878A (ja) * 2004-12-02 2008-06-26 ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー 非晶質アトルバスタチンの医薬組成物及びその製造のための方法
KR20070085874A (ko) 2004-12-09 2007-08-27 머크 앤드 캄파니 인코포레이티드 에스트로겐 수용체 조절제
CA2498978A1 (en) 2005-02-28 2006-08-28 Apotex Pharmachem Inc. An improved process for the preparation of atorvastatin and intermediates
CA2499047A1 (en) * 2005-03-01 2006-09-01 Apotex Pharmachem Inc. Process for producing atorvastatin hemicalcium
DK1855674T3 (da) 2005-03-02 2014-10-20 Merck Sharp & Dohme Sammensætning til hæmning af cathepsin k
GB2424880A (en) * 2005-04-06 2006-10-11 Generics Crystalline forms of atorvastatin sodium, processes for their preparation and their use in inhibiting HMG-CoA reductase
EA014079B1 (ru) * 2005-04-08 2010-08-30 Эгиш Дьёдьсердьяр Ньильваношан Мюкёдё Ресвеньтаршашаг Новая полиморфная форма кристаллической гемикальциевой соли аторвастатина
ES2382814T3 (es) 2005-05-17 2012-06-13 Merck Sharp & Dohme Ltd. Ácido cis-4-[(4-clorofenil)sulfonil]-4-(2,5-difluorofenil)ciclohexanopropanoico para el tratamiento del cáncer
TW200804345A (en) * 2005-08-30 2008-01-16 Novartis Ag Substituted benzimidazoles and methods of preparation
EP1922315B1 (de) * 2005-09-09 2009-05-27 Pfizer Science and Technology Ireland Limited Herstellung eines atorvastatin-zwischenprodukts
CA2621507A1 (en) * 2005-09-09 2007-03-15 Pfizer Science And Technology Ireland Limited Preparation of an atorvastatin intermediate
US20090216029A1 (en) * 2005-09-16 2009-08-27 Yatendra Kumar Process for the production of atorvastatin calcium in amorphous form
CA2547216A1 (en) * 2005-09-21 2007-03-21 Renuka D. Reddy Process for annealing amorphous atorvastatin
US8084488B2 (en) * 2005-11-21 2011-12-27 Pfizer Inc. Forms of [R-(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid magnesium
TW200745026A (en) * 2005-12-13 2007-12-16 Teva Pharma Crystal form of atorvastatin hemi-calcium and processes for preparation thereof
EP1810667A1 (de) 2006-01-20 2007-07-25 KRKA, tovarna zdravil, d.d., Novo mesto Pharmazeutische Zusammensetzung enthaltend amorphes Atorvastatin
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
WO2007103223A1 (en) * 2006-03-01 2007-09-13 Teva Pharmaceutical Industries Ltd. Process for preparing a crystalline form of atorvastatin hemi-calcium
LT2010528T (lt) 2006-04-19 2017-12-27 Novartis Ag 6-o-pakeistieji benzoksazolo junginiai bei csf-1r signalo perdavimo slopinimo būdai
CA2664113C (en) 2006-09-22 2013-05-28 Merck & Co., Inc. Use of platencin and platensimycin as fatty acid synthesis inhibitors to treat obesity, diabetes and cancer
US20110218176A1 (en) 2006-11-01 2011-09-08 Barbara Brooke Jennings-Spring Compounds, methods, and treatments for abnormal signaling pathways for prenatal and postnatal development
WO2008053312A2 (en) * 2006-11-02 2008-05-08 Cadila Pharmaceuticals Limited Process for preparing amorphous atorvastatin hemi calcium salt and its intermediate
BRPI0806245B1 (pt) 2007-01-10 2022-01-25 Msd Italia S.R.L. Compostos de fórmula i e seus usos
US7834195B2 (en) * 2007-01-24 2010-11-16 Apotex Pharmachem Inc. Atorvastatin calcium propylene glycol solvates
WO2008106662A2 (en) 2007-03-01 2008-09-04 Verenium Corporation Nitrilases, nucleic acids encoding them and methods for making and using them
BRPI0808523A2 (pt) 2007-03-01 2014-08-19 Novartis Vaccines & Diagnostic Inibidores de pim cinase e métodos de seu uso
CA2685967A1 (en) 2007-05-21 2008-11-21 Novartis Ag Csf-1r inhibitors, compositions, and methods of use
EP2170076B1 (de) 2007-06-27 2016-05-18 Merck Sharp & Dohme Corp. 4-carboxybenzylamino-derivate als histondeacetylase-hemmer
US20110142883A1 (en) * 2007-07-20 2011-06-16 Actavis Group Ptc Ehf Amorphous Coprecipitates of Atorvastatin Pharmaceutically Acceptable Salts
WO2009082437A2 (en) 2007-12-21 2009-07-02 Ligand Pharmaceuticals Incorporated Selective androgen receptor modulators (sarms) and uses thereof
EP2075246A1 (de) 2007-12-27 2009-07-01 M. J. Institute of Research Verfahren zur Herstellung einer amorphen Form von Atorvastatin-Hemicalcium-Salz
CN101429195B (zh) * 2008-11-03 2010-12-15 华东师范大学 一种高纯度阿托伐他汀重要合成中间体的制备方法
EP2373609B1 (de) 2008-12-19 2013-10-16 KRKA, D.D., Novo Mesto Verwendung amphiphiler verbindungen zur kontrollierten kristallisation von statinen und statinzwischenprodukten
EP2327682A1 (de) 2009-10-29 2011-06-01 KRKA, D.D., Novo Mesto Verwendung von amphiphilen Verbindungen zur gesteuerten Kristallisation von Statinen und Statin Zwischenprodukte.
US8115015B2 (en) * 2009-01-26 2012-02-14 Cadila Healthcare Limited Process for the preparation of amorphous atorvastatin calcium
WO2010093601A1 (en) 2009-02-10 2010-08-19 Metabasis Therapeutics, Inc. Novel sulfonic acid-containing thyromimetics, and methods for their use
US8691825B2 (en) 2009-04-01 2014-04-08 Merck Sharp & Dohme Corp. Inhibitors of AKT activity
US8470805B2 (en) * 2009-04-30 2013-06-25 Kaohsiung Medical University Processes for preparing piperazinium salts of KMUP and use thereof
WO2011046771A1 (en) 2009-10-14 2011-04-21 Schering Corporation SUBSTITUTED PIPERIDINES THAT INCREASE p53 ACTIVITY AND THE USES THEREOF
WO2011163330A1 (en) 2010-06-24 2011-12-29 Merck Sharp & Dohme Corp. Novel heterocyclic compounds as erk inhibitors
KR20120011249A (ko) 2010-07-28 2012-02-07 주식회사 경보제약 아토바스타틴 헤미칼슘염의 신규한 결정형, 이의 수화물, 및 그의 제조방법
CA2805265A1 (en) 2010-08-02 2012-02-09 Merck Sharp & Dohme Corp. Rna interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (ctnnb1) gene expression using short interfering nucleic acid (sina)
WO2012024170A2 (en) 2010-08-17 2012-02-23 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF HEPATITIS B VIRUS (HBV) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
US8883801B2 (en) 2010-08-23 2014-11-11 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as mTOR inhibitors
US8946216B2 (en) 2010-09-01 2015-02-03 Merck Sharp & Dohme Corp. Indazole derivatives useful as ERK inhibitors
EP2615916B1 (de) 2010-09-16 2017-01-04 Merck Sharp & Dohme Corp. Kondensierte pyrazolderivate als neue erk-hemmer
WO2012058210A1 (en) 2010-10-29 2012-05-03 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACIDS (siNA)
TWI462739B (zh) 2010-11-02 2014-12-01 Univ Kaohsiung Medical Ｓｉｌｄｅｎａｆｉｌ－同族物四級銨哌嗪鹽類之製備及醫療用途
WO2012087772A1 (en) 2010-12-21 2012-06-28 Schering Corporation Indazole derivatives useful as erk inhibitors
US8791162B2 (en) 2011-02-14 2014-07-29 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
JP2014514321A (ja) 2011-04-21 2014-06-19 メルク・シャープ・アンド・ドーム・コーポレーション インスリン様増殖因子１受容体阻害剤
BRPI1101952B1 (pt) * 2011-04-25 2022-02-01 Universidade Estadual De Campinas - Unicamp Processo de obtenção de atorvastatina cálcica utilizando novos intermediários e atorvastatina assim obtida
EP2726456A1 (de) 2011-07-01 2014-05-07 DSM Sinochem Pharmaceuticals Netherlands B.V. Mikronisierte kristalle von atorvastatin-hemicalcium
US9023865B2 (en) 2011-10-27 2015-05-05 Merck Sharp & Dohme Corp. Compounds that are ERK inhibitors
DE102011119719A1 (de) 2011-11-30 2013-06-06 GEA CFS Bühl GmbH Verfahren zum Aufschneiden eines Lebensmittelriegels unter Verwendung eines Schwingungssensors
US20150299696A1 (en) 2012-05-02 2015-10-22 Sirna Therapeutics, Inc. SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS
WO2014052563A2 (en) 2012-09-28 2014-04-03 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
MX363243B (es) 2012-11-28 2019-03-14 Merck Sharp & Dohme Composiciones para tratar cáncer y usos de dichas composiciones.
RU2690663C2 (ru) 2012-12-20 2019-06-05 Мерк Шарп И Доум Корп. Замещенные имидазопиридины в качестве ингибиторов hdm2
US9540377B2 (en) 2013-01-30 2017-01-10 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as HDM2 inhibitors
US20160194368A1 (en) 2013-09-03 2016-07-07 Moderna Therapeutics, Inc. Circular polynucleotides
WO2015054089A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
WO2015051479A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
WO2015108988A2 (en) 2014-01-17 2015-07-23 Ligand Pharmaceuticals, Inc. Methods and compositions for modulating hormone levels
WO2015120580A1 (en) 2014-02-11 2015-08-20 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
JO3589B1 (ar) 2014-08-06 2020-07-05 Novartis Ag مثبطات كيناز البروتين c وطرق استخداماتها
CN105085497B (zh) * 2015-06-26 2017-12-26 上海应用技术学院 多取代吡咯类他汀含氟衍生物及其用途
CN108366957A (zh) 2015-11-06 2018-08-03 燿石治疗公司 用于治疗心血管疾病的吉卡宾组合
US10947234B2 (en) 2017-11-08 2021-03-16 Merck Sharp & Dohme Corp. PRMT5 inhibitors
CN108558726A (zh) * 2018-03-14 2018-09-21 湖北广济药业股份有限公司 一种高纯度阿托伐他汀钙的制备方法
WO2020033284A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
EP3833668A4 (de) 2018-08-07 2022-05-11 Merck Sharp & Dohme Corp. Prmt5-inhibitoren
AU2020408148A1 (en) 2019-12-17 2022-06-16 Merck Sharp & Dohme Llc PRMT5 inhibitors
CN111362856B (zh) * 2020-04-29 2023-08-18 福建海西新药创制股份有限公司 一种利用微反应装置生产阿托伐他汀钙的方法
CN116102482A (zh) * 2022-08-17 2023-05-12 重庆普佑生物医药有限公司 一种阿托伐他汀钙的制备方法

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4647576A (en) * 1984-09-24 1987-03-03 Warner-Lambert Company Trans-6-[2-(substitutedpyrrol-1-yl)alkyl]-pyran-2-one inhibitors of cholesterol synthesis
US4681893A (en) * 1986-05-30 1987-07-21 Warner-Lambert Company Trans-6-[2-(3- or 4-carboxamido-substituted pyrrol-1-yl)alkyl]-4-hydroxypyran-2-one inhibitors of cholesterol synthesis
DE3702283A1 (de) * 1987-01-27 1988-08-04 Bayer Ag Verfahren zur herstellung von 2-cyano-2-oximino-acetamid-derivaten
JPH0774194B2 (ja) * 1987-06-11 1995-08-09 財団法人微生物化学研究会 生理活性を有する新規なアクチノニン誘導体
US5149837A (en) * 1988-02-22 1992-09-22 Warner-Lambert Company Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis
US5003080A (en) * 1988-02-22 1991-03-26 Warner-Lambert Company Process for trans-6-(2-(substituted-pyrrol-1-yl)alkyl)pryan-2-one inhibitors of cholesterol synthesis
US5097045A (en) * 1989-02-01 1992-03-17 Warner-Lambert Company Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis
US5124482A (en) * 1988-02-22 1992-06-23 Warner-Lambert Company Process for trans-6-(2-substituted-pyrrol-1-yl)alkyl)pyran-2-one inhibitors of cholesterol synthesis
FI94339C (fi) * 1989-07-21 1995-08-25 Warner Lambert Co Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi
US5103024A (en) * 1990-10-17 1992-04-07 Warner-Lambert Company Process for the synthesis of (4r-cis)-1,1-dimethylethyl 6-cyanomethyl-2,2-dimethyl-1,3-dioxane-4-acetate
IE913866A1 (en) * 1990-11-28 1992-06-03 Ici Plc Aryl derivatives
US5155251A (en) * 1991-10-11 1992-10-13 Warner-Lambert Company Process for the synthesis of (5R)-1,1-dimethylethyl-6-cyano-5-hydroxy-3-oxo-hexanoate
US5298627A (en) * 1993-03-03 1994-03-29 Warner-Lambert Company Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis

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