AR036108A1 - Derivados de oxadiazol, respectivamente de tiadiazol-pirrolidina, uso de dichos derivados en la preparacion de composiciones para modular, bloquear o antagonizar la actividad de oxitocina con sus receptores y/o el tratamiento y/o prevencion de enfermedades mediadas por la oxitocina , inclusive en la - Google Patents
Derivados de oxadiazol, respectivamente de tiadiazol-pirrolidina, uso de dichos derivados en la preparacion de composiciones para modular, bloquear o antagonizar la actividad de oxitocina con sus receptores y/o el tratamiento y/o prevencion de enfermedades mediadas por la oxitocina , inclusive en laInfo
- Publication number
- AR036108A1 AR036108A1 ARP020102353A ARP020102353A AR036108A1 AR 036108 A1 AR036108 A1 AR 036108A1 AR P020102353 A ARP020102353 A AR P020102353A AR P020102353 A ARP020102353 A AR P020102353A AR 036108 A1 AR036108 A1 AR 036108A1
- Authority
- AR
- Argentina
- Prior art keywords
- aryl
- alkyl
- heteroaryl
- group
- derivatives
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 2
- WCPAKWJPBJAGKN-UHFFFAOYSA-N oxadiazole Chemical class C1=CON=N1 WCPAKWJPBJAGKN-UHFFFAOYSA-N 0.000 title abstract 2
- 201000010099 disease Diseases 0.000 title 1
- 230000006806 disease prevention Effects 0.000 title 1
- 125000003118 aryl group Chemical group 0.000 abstract 5
- 125000001072 heteroaryl group Chemical group 0.000 abstract 5
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- 229920006395 saturated elastomer Polymers 0.000 abstract 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- UGUHFDPGDQDVGX-UHFFFAOYSA-N 1,2,3-thiadiazole Chemical group C1=CSN=N1 UGUHFDPGDQDVGX-UHFFFAOYSA-N 0.000 abstract 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- 208000005171 Dysmenorrhea Diseases 0.000 abstract 1
- 206010013935 Dysmenorrhoea Diseases 0.000 abstract 1
- 102000004279 Oxytocin receptors Human genes 0.000 abstract 1
- 108090000876 Oxytocin receptors Proteins 0.000 abstract 1
- 206010036595 Premature delivery Diseases 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000002877 alkyl aryl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000005213 alkyl heteroaryl group Chemical group 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 238000009472 formulation Methods 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 150000004866 oxadiazoles Chemical class 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- UXUYQXXOPCMNLU-UHFFFAOYSA-N pyrrolidine;thiadiazole Chemical compound C1CCNC1.C1=CSN=N1 UXUYQXXOPCMNLU-UHFFFAOYSA-N 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 238000012384 transportation and delivery Methods 0.000 abstract 1
Classifications
-
- 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/06—Antiabortive agents; Labour repressants
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
-
- 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
- C07D413/14—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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Diabetes (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Se describen y reivindican derivados de oxadiazol, respectivamente, de tiadiazol-pirrolidina, de fórmula (1), así como también sus isómeros geométricos, sus formas ópticamente activas como enantiómeros, diastereómeros y sus formas racémicas, así como las sales farmacéuticamente aceptables de los mismos, donde: A es seleccionado entre el grupo formado por -(C=O)-, -(C=O)-O-, -SO2-, -SO2NH-, -C(=NH)-, -(C=O)-NH-, -(C=S)-NH, -CH2-. B es un anillo oxadiazol o tiadiazol. R1 es seleccionado entre el grupo que comprende alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, heteroarilo, alquilo C1-6 arilo, alquilo C1-6 heteroarilo; R1 puede formar con el átomo O al cual se encuentra fijado un anillo heterocíclico de 3-8 miembros, saturado o insaturado, que puede contener 1-2 heteroátomos seleccionados entre N, S y O y que es opcionalmente fusionado con arilo, heteroarilo o un anillo cicloalquilo saturado o insaturado de 3-8 miembros; R2 es seleccionado entre el grupo que comprende alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, heteroarilo, cicloalquilo de 3-8 miembros saturado o insaturado y, acilo, alquilo C1-6 arilo, alquilo C1-6 heteroarilo, donde dichos grupos cicloalquilo o arilo o heteroarilo pueden fusionarse con otros 1-2 grupos cicloalquilo o arilo o heteroarilo. R3, R4, R5 y R6 son independientemente seleccionados entre sí a partir del grupo formado por H o un grupo formado por hidrógeno, halógeno, alquilo C1-6, alcoxi C1-6. Dichos compuestos son antagonistas de los receptores de las oxitocinas; dichos compuestos han demostrado ser aplicables en la formulación de composiciones para el tratamiento y, respectivamente, prevención de trastornos que ocurren en las tareas previas a los partos, inclusive cuando se trata de partos prematuros, y de dismenorrea. Se describen y reivindican además los objetos restantes mencionados en el título.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01113632 | 2001-06-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR036108A1 true AR036108A1 (es) | 2004-08-11 |
Family
ID=8177641
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020102353A AR036108A1 (es) | 2001-06-18 | 2002-06-21 | Derivados de oxadiazol, respectivamente de tiadiazol-pirrolidina, uso de dichos derivados en la preparacion de composiciones para modular, bloquear o antagonizar la actividad de oxitocina con sus receptores y/o el tratamiento y/o prevencion de enfermedades mediadas por la oxitocina , inclusive en la |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US7115639B2 (es) |
| EP (1) | EP1444225B1 (es) |
| JP (1) | JP4426284B2 (es) |
| KR (1) | KR20040030678A (es) |
| CN (1) | CN100564378C (es) |
| AR (1) | AR036108A1 (es) |
| AU (1) | AU2002319237B2 (es) |
| BG (1) | BG108424A (es) |
| BR (1) | BR0211030A (es) |
| CA (1) | CA2449578C (es) |
| CZ (1) | CZ20033475A3 (es) |
| EA (1) | EA006212B1 (es) |
| EE (1) | EE200400022A (es) |
| ES (1) | ES2397305T3 (es) |
| HR (1) | HRP20031017A2 (es) |
| HU (1) | HUP0400238A2 (es) |
| IL (1) | IL159219A0 (es) |
| MX (1) | MXPA03011441A (es) |
| MY (1) | MY128890A (es) |
| NO (1) | NO20035399L (es) |
| PL (1) | PL367275A1 (es) |
| RS (1) | RS99503A (es) |
| SK (1) | SK15552003A3 (es) |
| UA (1) | UA75145C2 (es) |
| WO (1) | WO2002102799A2 (es) |
| ZA (1) | ZA200309402B (es) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1444225B1 (en) | 2001-06-18 | 2012-10-10 | Merck Serono SA | Pyrrolidine oxadiazole- and thiadiazole oxime derivatives being oxytocin receptor antagonists. |
| ES2333719T3 (es) | 2003-02-27 | 2010-02-26 | Merck Serono Sa | Derivados de pirrolidina en calidad de antagonistas de oxitocina. |
| EA011026B1 (ru) * | 2004-02-26 | 2008-12-30 | Лаборатуар Сероно Са | Способ получения пирролидиноксимов |
| PL2559690T3 (pl) | 2005-05-10 | 2016-09-30 | Modulatory 2,3-dioksygenazy indoloaminy i sposoby ich zastosowania | |
| TWI382974B (zh) | 2005-12-20 | 2013-01-21 | 英塞特公司 | 作為吲哚胺２，３-二氧化酶調節劑之ｎ-羥基甲脒基雜環化物 |
| JP5319532B2 (ja) * | 2006-09-19 | 2013-10-16 | インサイト・コーポレイション | インドールアミン２，３−ジオキシゲナーゼのモジュレーターとしてのｎ−ヒドロキシアミジノヘテロサイクル |
| CL2007002650A1 (es) | 2006-09-19 | 2008-02-08 | Incyte Corp | Compuestos derivados de heterociclo n-hidroxiamino; composicion farmaceutica, util para tratar cancer, infecciones virales y desordenes neurodegenerativos entre otras. |
| ES2524266T3 (es) | 2008-07-08 | 2014-12-04 | Incyte Corporation | 1,2,5-Oxadiazoles como inhibidores de la indoleamina 2,3-dioxigenasa |
| EP2845850A1 (en) | 2013-09-10 | 2015-03-11 | ObsEva S.A. | Pyrrolidine derivatives as oxytocin/vasopressin V1a receptors antagonists |
| EA201991770A1 (ru) | 2013-11-08 | 2019-12-30 | Инсайт Холдингс Корпорейшн | Способ синтеза ингибитора индоламин-2,3-диоксигеназы |
| EP2886107A1 (en) | 2013-12-17 | 2015-06-24 | ObsEva S.A. | Oral formulations of pyrrolydine derivatives |
| EP3753921A1 (en) | 2014-07-02 | 2020-12-23 | ObsEva S.A. | Crystalline (3z,5s)-5-(hydroxymethyl)-1-[(2'-methyl-1,1'-biphenyl-4-yl)carbonyl]pyrrolidin-3-one o-methyloxime useful in methods of treating conditions related to the ot-r activity |
| 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 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2722190B1 (fr) * | 1994-07-05 | 1996-10-04 | Sanofi Sa | Derives de 1-benzyl-1,3-dihydro-2h-benzimidazol-2-one, leur preparation, les compositions pharmaceutique en contenant |
| EP0805681A4 (en) | 1995-01-24 | 1998-05-06 | Merck & Co Inc | TOCOLYTIC OXYTOCIN RECEPTOR ANTAGONISTS |
| US5756497A (en) | 1996-03-01 | 1998-05-26 | Merck & Co., Inc. | Tocolytic oxytocin receptor antagonists |
| FR2757157B1 (fr) * | 1996-12-13 | 1999-12-31 | Sanofi Sa | Derives d'indolin-2-one, procede pour leur preparation et compositions pharmaceutiques les contenant |
| EP1176959B1 (en) | 1999-05-05 | 2006-03-08 | Merck & Co., Inc. | Novel prolines as antimicrobial agents |
| ES2261404T3 (es) * | 2000-03-27 | 2006-11-16 | Applied Research Systems Ars Holding N.V. | Derivados de pirrolidina utiles como inhibidores de bax. |
| DK1268418T3 (da) | 2000-03-27 | 2006-09-25 | Applied Research Systems | Farmaceutisk aktive pyrrolidinderivater som Bax-inhibitorer |
| US7312358B2 (en) * | 2000-10-17 | 2007-12-25 | Laboratoires Serono Sa | Pharmaceutically active sulfanilide derivatives |
| IL157995A0 (en) * | 2001-03-20 | 2004-03-28 | Applied Research Systems | The use of pyrrolidine ester derivatives in modulation of oxytoxin activity, some new such derivatives, their preparation and pharmaceutical compositions containing them |
| EP1444225B1 (en) | 2001-06-18 | 2012-10-10 | Merck Serono SA | Pyrrolidine oxadiazole- and thiadiazole oxime derivatives being oxytocin receptor antagonists. |
| WO2003053437A1 (en) * | 2001-12-20 | 2003-07-03 | Applied Research Systems Ars Holding N.V. | Triazoles as oxytocin antagonists |
| UA78058C2 (en) * | 2002-07-05 | 2007-02-15 | Applied Research Systems | Pyrrolidine derivative as oxitocin antagonists |
-
2002
- 2002-06-14 EP EP02748785A patent/EP1444225B1/en not_active Expired - Lifetime
- 2002-06-14 PL PL02367275A patent/PL367275A1/xx not_active Application Discontinuation
- 2002-06-14 CN CNB028159446A patent/CN100564378C/zh not_active Expired - Fee Related
- 2002-06-14 CZ CZ20033475A patent/CZ20033475A3/cs unknown
- 2002-06-14 UA UA20031211897A patent/UA75145C2/uk unknown
- 2002-06-14 KR KR10-2003-7016485A patent/KR20040030678A/ko not_active Ceased
- 2002-06-14 JP JP2003506272A patent/JP4426284B2/ja not_active Expired - Fee Related
- 2002-06-14 MX MXPA03011441A patent/MXPA03011441A/es active IP Right Grant
- 2002-06-14 EA EA200400049A patent/EA006212B1/ru not_active IP Right Cessation
- 2002-06-14 AU AU2002319237A patent/AU2002319237B2/en not_active Ceased
- 2002-06-14 IL IL15921902A patent/IL159219A0/xx unknown
- 2002-06-14 ES ES02748785T patent/ES2397305T3/es not_active Expired - Lifetime
- 2002-06-14 HU HU0400238A patent/HUP0400238A2/hu unknown
- 2002-06-14 RS YU99503A patent/RS99503A/sr unknown
- 2002-06-14 HR HR20031017A patent/HRP20031017A2/xx not_active Application Discontinuation
- 2002-06-14 SK SK1555-2003A patent/SK15552003A3/sk not_active Application Discontinuation
- 2002-06-14 BR BR0211030-0A patent/BR0211030A/pt not_active IP Right Cessation
- 2002-06-14 WO PCT/EP2002/006629 patent/WO2002102799A2/en not_active Ceased
- 2002-06-14 EE EEP200400022A patent/EE200400022A/xx unknown
- 2002-06-14 CA CA2449578A patent/CA2449578C/en not_active Expired - Fee Related
- 2002-06-14 US US10/480,992 patent/US7115639B2/en not_active Expired - Fee Related
- 2002-06-18 MY MYPI20022260A patent/MY128890A/en unknown
- 2002-06-21 AR ARP020102353A patent/AR036108A1/es unknown
-
2003
- 2003-12-03 ZA ZA200309402A patent/ZA200309402B/en unknown
- 2003-12-04 NO NO20035399A patent/NO20035399L/no unknown
- 2003-12-08 BG BG108424A patent/BG108424A/xx unknown
-
2006
- 2006-06-09 US US11/449,802 patent/US20060229343A1/en not_active Abandoned
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