EA200201026A1 - Фармацевтически активные производные пирролидина - Google Patents
Фармацевтически активные производные пирролидинаInfo
- Publication number
- EA200201026A1 EA200201026A1 EA200201026A EA200201026A EA200201026A1 EA 200201026 A1 EA200201026 A1 EA 200201026A1 EA 200201026 A EA200201026 A EA 200201026A EA 200201026 A EA200201026 A EA 200201026A EA 200201026 A1 EA200201026 A1 EA 200201026A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- pyrrolidine derivatives
- formula
- present
- group
- pyrrolidine
- Prior art date
Links
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical class C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 title 1
- 150000003235 pyrrolidines Chemical class 0.000 abstract 4
- 208000005107 Premature Birth Diseases 0.000 abstract 3
- 208000005171 Dysmenorrhea Diseases 0.000 abstract 2
- 206010013935 Dysmenorrhoea Diseases 0.000 abstract 2
- 206010036590 Premature baby Diseases 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 230000002265 prevention Effects 0.000 abstract 2
- 239000000126 substance Substances 0.000 abstract 2
- XNOPRXBHLZRZKH-UHFFFAOYSA-N Oxytocin Natural products N1C(=O)C(N)CSSCC(C(=O)N2C(CCC2)C(=O)NC(CC(C)C)C(=O)NCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(CCC(N)=O)NC(=O)C(C(C)CC)NC(=O)C1CC1=CC=C(O)C=C1 XNOPRXBHLZRZKH-UHFFFAOYSA-N 0.000 abstract 1
- 101800000989 Oxytocin Proteins 0.000 abstract 1
- 102000004279 Oxytocin receptors Human genes 0.000 abstract 1
- 108090000876 Oxytocin receptors Proteins 0.000 abstract 1
- 102100031951 Oxytocin-neurophysin 1 Human genes 0.000 abstract 1
- 208000006399 Premature Obstetric Labor Diseases 0.000 abstract 1
- 230000003042 antagnostic effect Effects 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- XNOPRXBHLZRZKH-DSZYJQQASA-N oxytocin Chemical compound C([C@H]1C(=O)N[C@H](C(N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CSSC[C@H](N)C(=O)N1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)=O)[C@@H](C)CC)C1=CC=C(O)C=C1 XNOPRXBHLZRZKH-DSZYJQQASA-N 0.000 abstract 1
- 229960001723 oxytocin Drugs 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P25/08—Antiepileptics; Anticonvulsants
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- 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
- C07D207/18—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 one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—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 one double bond between ring members or between a ring member and a non-ring member 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
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- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- 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
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- C07—ORGANIC CHEMISTRY
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- 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
- C07D405/12—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 chain containing hetero atoms as chain links
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- Organic Chemistry (AREA)
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- Neurology (AREA)
- Biomedical Technology (AREA)
- Gynecology & Obstetrics (AREA)
- Immunology (AREA)
- Pregnancy & Childbirth (AREA)
- Virology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Vascular Medicine (AREA)
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- Molecular Biology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Tropical Medicine & Parasitology (AREA)
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Abstract
Настоящее изобретение относится к производным пирролидина формулы (I)Указанные вещества предназначены для применения в качестве фармацевтически активных соединений. Производные пирролидина формулы (I) можно особенно эффективно использовать для лечения и/или профилактики преждевременных родов, рождения недоношенного ребенка и дисменореи. В частности, настоящее изобретение относится к производным пирролидина, обладающим модуляторной, а именно антагонистической активностью в отношении рецептора окситоцина. Более предпочтительно указанные соединения предназначены для лечения и/или профилактики заболеваний, опосредованных окситоцином, включая преждевременные роды, рождение недоношенного ребенка и дисменорею. Настоящее изобретение далее относится к новым производным пирролидина, а также к способам получения указанных веществ, в которых Х выбирают из группы, включающей CRR, NOR, NNRR; А выбирают из группы, включающей -(С=O)-, -(С=O)=O-, -C(=NH), -(C=O)-NH-, -(C=S)-NH, -SO-, -SONH-, CH-; В означает группу -(C=O)-NRRили представляет гетероциклический остаток формулы (а)где Q означает NR, О или S; n означает целое число, выбираемое из 0, 1 или 2; Y, Z и Е вместе с 2 атомами углерода, к которым они присоединены, образуют 5-6-членное арильное или гетероарильное кольцо.Международная заявка была опубликована вместе с отчетом о международном поиске.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP00106034 | 2000-03-27 | ||
| PCT/EP2001/003171 WO2001072705A1 (en) | 2000-03-27 | 2001-03-20 | Pharmaceutically active pyrrolidine derivatives as bax inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA200201026A1 true EA200201026A1 (ru) | 2003-02-27 |
| EA006424B1 EA006424B1 (ru) | 2005-12-29 |
Family
ID=8168169
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200201026A EA006424B1 (ru) | 2000-03-27 | 2001-03-20 | Фармацевтически активные производные пирролидина |
Country Status (33)
| Country | Link |
|---|---|
| US (2) | US7211601B2 (ru) |
| EP (1) | EP1268419B1 (ru) |
| JP (2) | JP2003528854A (ru) |
| KR (1) | KR100714585B1 (ru) |
| CN (1) | CN1296354C (ru) |
| AR (1) | AR029499A1 (ru) |
| AT (1) | ATE330940T1 (ru) |
| AU (2) | AU2001256209B2 (ru) |
| BG (1) | BG107132A (ru) |
| BR (1) | BR0109900A (ru) |
| CA (1) | CA2401242A1 (ru) |
| CY (1) | CY1105519T1 (ru) |
| CZ (1) | CZ20023243A3 (ru) |
| DE (1) | DE60120940T2 (ru) |
| DK (1) | DK1268419T3 (ru) |
| EA (1) | EA006424B1 (ru) |
| EE (1) | EE200200555A (ru) |
| ES (1) | ES2261404T3 (ru) |
| HK (1) | HK1054031B (ru) |
| HR (1) | HRP20020705A2 (ru) |
| HU (1) | HUP0300994A2 (ru) |
| IL (1) | IL151912A0 (ru) |
| MX (1) | MXPA02009382A (ru) |
| NO (1) | NO323969B1 (ru) |
| NZ (1) | NZ521060A (ru) |
| PL (1) | PL358001A1 (ru) |
| PT (1) | PT1268419E (ru) |
| SI (1) | SI1268419T1 (ru) |
| SK (1) | SK13832002A3 (ru) |
| UA (1) | UA74362C2 (ru) |
| WO (1) | WO2001072705A1 (ru) |
| YU (1) | YU73502A (ru) |
| ZA (1) | ZA200206799B (ru) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU5222201A (en) * | 2000-03-27 | 2001-10-15 | Applied Research Systems | Pharmaceutically active pyrrolidine derivatives as bax inhibitors |
| ES2397305T3 (es) * | 2001-06-18 | 2013-03-06 | Merck Serono Sa | Derivados de oxadiazol y tiadiazol-oxima de pirrolidina que son antagonistas del receptor oxitocina |
| AR034897A1 (es) * | 2001-08-07 | 2004-03-24 | Hoffmann La Roche | Derivados n-monoacilados de o-fenilendiaminas, sus analogos heterociclicos de seis miembros y su uso como agentes farmaceuticos |
| US7030141B2 (en) * | 2001-11-29 | 2006-04-18 | Christopher Franklin Bigge | Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade |
| US7405234B2 (en) | 2002-05-17 | 2008-07-29 | Bristol-Myers Squibb Company | Bicyclic modulators of androgen receptor function |
| UA78058C2 (en) | 2002-07-05 | 2007-02-15 | Applied Research Systems | Pyrrolidine derivative as oxitocin antagonists |
| EP1567487A4 (en) * | 2002-11-15 | 2005-11-16 | Bristol Myers Squibb Co | OPEN-CHAINED, PROLYL-FROSTED MODULATORS OF ANDROGEN RECEPTOR FUNCTION |
| DE602004024170D1 (de) * | 2003-02-27 | 2009-12-31 | Merck Serono Sa Coinsins | Pyrrolidin-derivate als oxytocin antagonisten |
| US7820702B2 (en) | 2004-02-04 | 2010-10-26 | Bristol-Myers Squibb Company | Sulfonylpyrrolidine modulators of androgen receptor function and method |
| ES2296137T3 (es) * | 2004-02-26 | 2008-04-16 | Laboratoires Serono Sa | Metodo para preparar pirrolidin-oximas. |
| US7625923B2 (en) | 2004-03-04 | 2009-12-01 | Bristol-Myers Squibb Company | Bicyclic modulators of androgen receptor function |
| US7696241B2 (en) | 2004-03-04 | 2010-04-13 | Bristol-Myers Squibb Company | Bicyclic compounds as modulators of androgen receptor function and method |
| WO2010080357A1 (en) * | 2008-12-18 | 2010-07-15 | Boehringer Ingelheim International Gmbh | Serotonin 5-ht2b receptor inhibitors |
| WO2013042782A1 (ja) | 2011-09-22 | 2013-03-28 | 武田薬品工業株式会社 | 縮合複素環化合物 |
| EP2845850A1 (en) | 2013-09-10 | 2015-03-11 | ObsEva S.A. | Pyrrolidine derivatives as oxytocin/vasopressin V1a receptors antagonists |
| EP2886107A1 (en) * | 2013-12-17 | 2015-06-24 | ObsEva S.A. | Oral formulations of pyrrolydine derivatives |
| EA201891873A1 (ru) | 2014-07-02 | 2019-04-30 | Обсева Са | Кристаллический о-метилоксим (3z,5s)-5-(гидроксиметил)-1-[(2'-метил-1,1'-бифенил-4-ил)карбонил]пирролидин-3-он, полезный в способах лечения состояний, связанных с активностью ot-r |
| CN114621962B (zh) * | 2022-03-21 | 2024-05-14 | 广西大学 | 花生AhBI-1基因VIGS沉默体系 |
| TW202435864A (zh) | 2023-02-09 | 2024-09-16 | 大陸商上海葆正醫藥科技有限公司 | 亞胺化合物及其製備方法和應用 |
| CN117044622A (zh) * | 2023-09-22 | 2023-11-14 | 贵州师范大学 | 一种无花瓣芥菜型油菜的选育方式 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL23907A (en) | 1964-08-05 | 1971-05-26 | Upjohn Co | Lincomycin analogues and a process for their production |
| US3555007A (en) | 1968-07-22 | 1971-01-12 | Upjohn Co | 7-deoxy-7-halo lincomycin d derivatives |
| US3674647A (en) | 1970-10-07 | 1972-07-04 | Upjohn Co | Preparation of lincomycin analogues |
| ZA801424B (en) * | 1979-03-12 | 1981-03-25 | Warner Lambert Co | Novel antibactrial amide compounds and process means for producing the same |
| US4596819A (en) * | 1984-01-23 | 1986-06-24 | Warner-Lambert Company | Modified tripeptides |
| GB9316162D0 (en) | 1993-08-04 | 1993-09-22 | Zeneca Ltd | Fungicides |
| CA2210138A1 (en) | 1995-01-24 | 1996-08-01 | Peter D. Williams | Tocolytic oxytocin receptor antagonists |
| US5756497A (en) | 1996-03-01 | 1998-05-26 | Merck & Co., Inc. | Tocolytic oxytocin receptor antagonists |
| AR016133A1 (es) * | 1997-07-31 | 2001-06-20 | Wyeth Corp | Compuesto de carbamiloxi que inhiben la adhesion de leucocitos mediada por vla-4, compuestos que son prodrogas de dichos compuestos, composicionfarmaceutica, metodo para fijar vla-4 a una muestra biologica, metodo para el tratamiento de una condicion inflamatoria |
| US6329418B1 (en) * | 1998-04-14 | 2001-12-11 | The Procter & Gamble Company | Substituted pyrrolidine hydroxamate metalloprotease inhibitors |
| WO2000004005A1 (en) * | 1998-07-14 | 2000-01-27 | Ono Pharmaceutical Co., Ltd. | Amino acid derivatives and drugs containing the same as the active ingredient |
| DE69931975T2 (de) * | 1998-08-07 | 2006-10-05 | Applied Research Systems Ars Holding N.V. | FSH Mimetika zur Behandlung von Infertilität |
| EA200100815A1 (ru) * | 1999-01-27 | 2002-08-29 | Орто-Макнейл Фармасьютикал, Инк. | Пептидильные гетероциклические кетоны, применимые в качестве ингибиторов триптазы |
| AU759022B2 (en) * | 1999-02-18 | 2003-04-03 | Kaken Pharmaceutical Co., Ltd. | Novel amide derivatives as growth hormone secretagogues |
| JP2002539191A (ja) * | 1999-03-15 | 2002-11-19 | アクシス・ファーマシューティカルズ・インコーポレイテッド | プロテアーゼ阻害剤としての新規化合物及び組成物 |
| CA2372176A1 (en) * | 1999-05-05 | 2000-11-09 | Merck & Co., Inc. | Novel prolines as antimicrobial agents |
| GB0000079D0 (en) * | 2000-01-05 | 2000-02-23 | Ferring Bv | Novel antidiuretic agents |
| AU5222201A (en) * | 2000-03-27 | 2001-10-15 | Applied Research Systems | Pharmaceutically active pyrrolidine derivatives as bax inhibitors |
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