ZA200309367B - Pyrrolidine derivatives as factor Xa inhibitors. - Google Patents
Pyrrolidine derivatives as factor Xa inhibitors. Download PDFInfo
- Publication number
- ZA200309367B ZA200309367B ZA200309367A ZA200309367A ZA200309367B ZA 200309367 B ZA200309367 B ZA 200309367B ZA 200309367 A ZA200309367 A ZA 200309367A ZA 200309367 A ZA200309367 A ZA 200309367A ZA 200309367 B ZA200309367 B ZA 200309367B
- Authority
- ZA
- South Africa
- Prior art keywords
- methyl
- oxopyrrolidin
- oxoethyl
- morpholin
- chloro
- Prior art date
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- 150000003235 pyrrolidines Chemical class 0.000 title 1
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- 239000001257 hydrogen Substances 0.000 claims description 40
- -1 substituent halogen Chemical class 0.000 claims description 35
- 125000001424 substituent group Chemical group 0.000 claims description 28
- 229910052757 nitrogen Inorganic materials 0.000 claims description 27
- 229940124530 sulfonamide Drugs 0.000 claims description 27
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- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 25
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 23
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 23
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- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims description 22
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Classifications
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- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A61P9/00—Drugs for disorders of the cardiovascular system
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- 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
- C07D207/04—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 no double bonds between ring members or between ring members and non-ring members
- C07D207/10—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 no 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
- C07D207/12—Oxygen or sulfur atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic 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
- C07D413/06—Heterocyclic 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
Landscapes
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- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pulmonology (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyrrole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
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| GBGB0114005.2A GB0114005D0 (en) | 2001-06-08 | 2001-06-08 | Chemical compounds |
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| US20050119266A1 (en) * | 2003-10-01 | 2005-06-02 | Yan Shi | Pyrrolidine and piperidine derivatives as factor Xa inhibitors |
| EP1637141B1 (en) | 2004-09-21 | 2011-11-16 | Trobio AB | Stabilized protease composition comprising a serine protease, morpholino derivatives and reversible inhibitors of said serine protease |
| CN101087609B (zh) * | 2004-10-26 | 2012-11-14 | 詹森药业有限公司 | 因子Xa化合物 |
| WO2006110726A2 (en) * | 2005-04-11 | 2006-10-19 | Glaxo Group Limited | Dosage formulations and methods of treatment and prevention |
| CN102380100A (zh) * | 2005-09-22 | 2012-03-21 | 特罗比奥股份公司 | 稳定的蛋白酶组合物 |
| JP5080476B2 (ja) * | 2005-09-22 | 2012-11-21 | トルービオ・アーベー | 安定化プロテアーゼ組成物 |
| DE102007028319A1 (de) | 2007-06-20 | 2008-12-24 | Bayer Healthcare Ag | Substituierte Oxazolidinone und ihre Verwendung |
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| DE102007028406A1 (de) | 2007-06-20 | 2008-12-24 | Bayer Healthcare Ag | Substituierte Oxazolidinone und ihre Verwendung |
| JP6393310B2 (ja) * | 2013-04-26 | 2018-09-19 | サノフイＳａｎｏｆｉ | ５−クロロ−チオフェン−２−カルボン酸［（ｓ）−２−［メチル−３−（２−オキソ−ピロリジン−１−イル）−ベンゼンスルホニルアミノ］−３−（４−メチル−ピペラジン−１−イル）−３−オキソ−プロプリル］アミドの酒石酸塩 |
| DE102014108210A1 (de) | 2014-06-11 | 2015-12-17 | Dietrich Gulba | Rodentizid |
| EP3078378B1 (en) | 2015-04-08 | 2020-06-24 | Vaiomer | Use of factor xa inhibitors for regulating glycemia |
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| DE4035961A1 (de) * | 1990-11-02 | 1992-05-07 | Thomae Gmbh Dr K | Cyclische iminoderivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung |
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| CA2268281A1 (en) | 1996-10-11 | 1998-04-23 | Cor Therapeutics, Inc. | Selective factor xa inhibitors |
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| AU4431400A (en) | 1999-05-12 | 2000-12-05 | Japan As Represented By President Of National Cancer Center | Anticancer agents containing ep1 antagonists as the active ingredient |
| AU773227B2 (en) | 1999-07-28 | 2004-05-20 | Aventis Pharmaceuticals Inc. | Substituted oxoazaheterocyclyl compounds |
| WO2002060894A2 (en) | 2001-01-30 | 2002-08-08 | Bristol-Myers Squibb Company | Sulfonamide lactam inhibitors of factor xa |
| GB0114005D0 (en) * | 2001-06-08 | 2001-08-01 | Glaxo Group Ltd | Chemical compounds |
| GB0114004D0 (en) * | 2001-06-08 | 2001-08-01 | Glaxo Group Ltd | Chemical compounds |
| GB0228552D0 (en) * | 2002-12-06 | 2003-01-15 | Glaxo Group Ltd | Chemical compounds |
| GB0228533D0 (en) * | 2002-12-06 | 2003-01-15 | Glaxo Group Ltd | Crystalline form |
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2001
- 2001-06-08 GB GBGB0114005.2A patent/GB0114005D0/en not_active Ceased
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2002
- 2002-06-06 WO PCT/GB2002/002721 patent/WO2002100830A1/en active IP Right Grant
- 2002-06-06 ES ES02738368T patent/ES2235050T3/es not_active Expired - Lifetime
- 2002-06-06 MX MXPA03011384A patent/MXPA03011384A/es active IP Right Grant
- 2002-06-06 DE DE60203006T patent/DE60203006T2/de not_active Expired - Lifetime
- 2002-06-06 PL PL02368082A patent/PL368082A1/xx unknown
- 2002-06-06 US US10/479,545 patent/US7186717B2/en not_active Expired - Fee Related
- 2002-06-06 HU HU0400156A patent/HUP0400156A3/hu unknown
- 2002-06-06 CA CA002449629A patent/CA2449629A1/en not_active Abandoned
- 2002-06-06 PT PT02738368T patent/PT1395553E/pt unknown
- 2002-06-06 DK DK02738368T patent/DK1395553T3/da active
- 2002-06-06 NZ NZ530004A patent/NZ530004A/en unknown
- 2002-06-06 KR KR1020037016070A patent/KR100877245B1/ko not_active IP Right Cessation
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- 2002-06-06 AR ARP020102128A patent/AR036086A1/es unknown
- 2002-06-06 BR BR0210207-2A patent/BR0210207A/pt not_active Application Discontinuation
- 2002-06-06 CZ CZ20033325A patent/CZ20033325A3/cs unknown
- 2002-06-06 SI SI200230101T patent/SI1395553T1/sl unknown
- 2002-06-06 AU AU2002311451A patent/AU2002311451B2/en not_active Ceased
- 2002-06-06 TW TW091112153A patent/TWI298719B/zh active
- 2002-06-06 JP JP2003503599A patent/JP4242274B2/ja not_active Expired - Fee Related
- 2002-06-06 AT AT02738368T patent/ATE289294T1/de not_active IP Right Cessation
- 2002-06-06 CN CNB028154002A patent/CN1256324C/zh not_active Expired - Fee Related
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- 2003-12-05 NO NO20035440A patent/NO326689B1/no not_active IP Right Cessation
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2004
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