BRPI0411729A - dicetopiperazinas substituìdas e seu uso como antagonistas da oxitocina - Google Patents
dicetopiperazinas substituìdas e seu uso como antagonistas da oxitocinaInfo
- Publication number
- BRPI0411729A BRPI0411729A BRPI0411729A BRPI0411729A BR PI0411729 A BRPI0411729 A BR PI0411729A BR PI0411729 A BRPI0411729 A BR PI0411729A BR PI0411729 A BRPI0411729 A BR PI0411729A
- Authority
- BR
- Brazil
- Prior art keywords
- oxytocin antagonists
- substituted
- substituted diketopiperazines
- antagonists
- diketopiperazines
- Prior art date
Links
- 239000003336 oxytocin antagonist Substances 0.000 title 1
- 229940121361 oxytocin antagonists Drugs 0.000 title 1
- -1 2-indanyl Chemical group 0.000 abstract 2
- 239000005557 antagonist Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 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
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
- 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
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P5/10—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
-
- 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
- A61P5/10—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
- A61P5/12—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH for decreasing, blocking or antagonising the activity of the posterior pituitary hormones
-
- 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
- A61P5/36—Antigestagens
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/06—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members
- C07D241/08—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
-
- 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
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Reproductive Health (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Child & Adolescent Psychology (AREA)
- Hematology (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Obesity (AREA)
- Gastroenterology & Hepatology (AREA)
- Psychiatry (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)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
"DICETOPIPERAZINAS SUBSTITUìDAS E SEU USO COMO ANTAGONISTAS DA OXITOCINA". Compostos de fórmula (I), em que R~ 1~, é 2-indanil, R~ 2~ é 1-metilpropila, R~ 3~ é 2-metil-1,3-oxazol-4-ila, e R~ 4~ e R~ 5~, juntamente com o átomo de nitrogênio ao qual estão ligados, representam morfolino, processo para sua preparação, composições farmacêuticas que os contenham e seu uso em medicina.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0314738A GB0314738D0 (en) | 2003-06-24 | 2003-06-24 | Novel compounds |
| PCT/EP2004/006814 WO2005000840A1 (en) | 2003-06-24 | 2004-06-22 | Substituted diketopiperazines and their use as oxytocin antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0411729A true BRPI0411729A (pt) | 2006-08-08 |
Family
ID=27637257
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0411729 BRPI0411729A (pt) | 2003-06-24 | 2004-06-22 | dicetopiperazinas substituìdas e seu uso como antagonistas da oxitocina |
Country Status (30)
| Country | Link |
|---|---|
| US (6) | US8071594B2 (pt) |
| EP (1) | EP1641787B1 (pt) |
| JP (1) | JP5128126B2 (pt) |
| KR (1) | KR101131378B1 (pt) |
| CN (2) | CN101597282A (pt) |
| AR (1) | AR044869A1 (pt) |
| AT (1) | ATE361295T1 (pt) |
| AU (1) | AU2004251868B2 (pt) |
| BR (1) | BRPI0411729A (pt) |
| CA (1) | CA2530310C (pt) |
| CY (1) | CY1107703T1 (pt) |
| DE (1) | DE602004006268T2 (pt) |
| DK (1) | DK1641787T3 (pt) |
| EG (1) | EG24929A (pt) |
| ES (1) | ES2285474T3 (pt) |
| GB (1) | GB0314738D0 (pt) |
| HR (1) | HRP20070286T3 (pt) |
| IL (1) | IL172529A (pt) |
| IS (1) | IS2463B (pt) |
| MA (1) | MA27887A1 (pt) |
| MX (1) | MXPA05014068A (pt) |
| MY (1) | MY140653A (pt) |
| NO (1) | NO332677B1 (pt) |
| NZ (1) | NZ544006A (pt) |
| PL (1) | PL1641787T3 (pt) |
| PT (1) | PT1641787E (pt) |
| RU (1) | RU2343152C2 (pt) |
| TW (1) | TWI340745B (pt) |
| WO (1) | WO2005000840A1 (pt) |
| ZA (1) | ZA200509890B (pt) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0130677D0 (en) * | 2001-12-21 | 2002-02-06 | Glaxo Group Ltd | Medicaments and novel compounds |
| GB0314738D0 (en) | 2003-06-24 | 2003-07-30 | Glaxo Group Ltd | Novel compounds |
| GB0414093D0 (en) | 2004-06-23 | 2004-07-28 | Glaxo Group Ltd | Novel compounds |
| GB0414100D0 (en) * | 2004-06-23 | 2004-07-28 | Glaxo Group Ltd | Novel compounds |
| GB0428235D0 (en) * | 2004-12-23 | 2005-01-26 | Glaxo Group Ltd | Novel compounds |
| JP2013509391A (ja) | 2009-10-30 | 2013-03-14 | グラクソ グループ リミテッド | （３ｒ，６ｒ）−３−（２，３−ジヒドロ−１ｈ−インデン−２−イル）−１−［（１ｒ）−１−（２，６−ジメチル−３−ピリジニル）−２−（４−モルホリニル）−２−オキソエチル］−６−［（１ｓ）−１−メチルプロピル］−２，５−ピペラジンジオンの新規結晶性形態 |
| RU2017100906A (ru) | 2014-06-16 | 2018-07-16 | Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед | Ретосибан для лечения преждевременных родов |
| SG10202009723PA (en) | 2016-01-04 | 2020-11-27 | ObsEva SA | Alpha-amino esters of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal polymorph thereof |
| WO2018015497A2 (en) | 2016-07-21 | 2018-01-25 | ObsEva S.A. | Oxytocin antagonist dosing regimens for promoting embryo implantation and preventing miscarriage |
| CN106674031A (zh) * | 2016-11-18 | 2017-05-17 | 浙江工业大学 | R‑2‑二氢茚氨酸的制备方法 |
| US20220323410A1 (en) | 2019-09-03 | 2022-10-13 | ObsEva S.A. | Oxytocin antagonist dosing regimens for promoting embryo implantation and preventing miscarriage |
| CN115380122A (zh) | 2020-02-10 | 2022-11-22 | 奥布赛瓦股份公司 | 用于催产素受体拮抗剂疗法的生物标志物 |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4596819A (en) * | 1984-01-23 | 1986-06-24 | Warner-Lambert Company | Modified tripeptides |
| US5091387A (en) * | 1990-03-02 | 1992-02-25 | Merck & Co., Inc. | Spirocyclic oxytocin antagonists |
| GB9217331D0 (en) | 1992-08-14 | 1992-09-30 | Xenova Ltd | Pharmaceutical compounds |
| US5464788A (en) * | 1994-03-24 | 1995-11-07 | Merck & Co., Inc. | Tocolytic oxytocin receptor antagonists |
| US5817751A (en) * | 1994-06-23 | 1998-10-06 | Affymax Technologies N.V. | Method for synthesis of diketopiperazine and diketomorpholine derivatives |
| US5968938A (en) * | 1997-06-18 | 1999-10-19 | Merck & Co., Inc. | Piperazine oxytocin receptor antagonists |
| GB2326639A (en) | 1997-06-18 | 1998-12-30 | Merck & Co Inc | Piperazine Oxytocin Receptor Antagonists |
| YU47600A (sh) | 1998-01-27 | 2002-09-19 | Aventis Pharmaceuticals Products Inc. | SUPSTITUISANI OKSOAZAHETEROCIKLIL INHIBITORI FAKTORA Xa |
| EP1051397B1 (en) | 1998-01-29 | 2008-12-31 | Aventis Pharmaceuticals Inc. | Method for preparing an n- (aliphatic or aromatic)carbonyl -2-aminoacetamide compound and a cyclyzed compound |
| EP1070084A4 (en) * | 1998-03-16 | 2001-09-12 | Ontogen Corp | PIPERAZINE AS INHIBITORS OF FRUKTOSE-1,6-BISPHOSPHATASE (FBPASE) |
| GB2372740A (en) | 2001-01-17 | 2002-09-04 | Xenova Ltd | Diketopiperazines |
| GB0130677D0 (en) * | 2001-12-21 | 2002-02-06 | Glaxo Group Ltd | Medicaments and novel compounds |
| US20030229001A1 (en) | 2002-01-31 | 2003-12-11 | Pfizer Inc. | Treatment of male sexual dysfunction |
| GB0314738D0 (en) * | 2003-06-24 | 2003-07-30 | Glaxo Group Ltd | Novel compounds |
| GB0314733D0 (en) | 2003-06-24 | 2003-07-30 | Glaxo Group Ltd | Medicaments |
| GB0414100D0 (en) * | 2004-06-23 | 2004-07-28 | Glaxo Group Ltd | Novel compounds |
| GB0414093D0 (en) * | 2004-06-23 | 2004-07-28 | Glaxo Group Ltd | Novel compounds |
| GB0414092D0 (en) * | 2004-06-23 | 2004-07-28 | Glaxo Group Ltd | Novel compounds |
| GB0428235D0 (en) | 2004-12-23 | 2005-01-26 | Glaxo Group Ltd | Novel compounds |
| JP6224597B2 (ja) | 2011-09-27 | 2017-11-01 | バイオメッド バレー ディスカバリーズ，インコーポレイティド | グリオーマを処置するための組成物及び方法 |
-
2003
- 2003-06-24 GB GB0314738A patent/GB0314738D0/en not_active Ceased
-
2004
- 2004-06-22 DE DE200460006268 patent/DE602004006268T2/de not_active Expired - Lifetime
- 2004-06-22 AT AT04740230T patent/ATE361295T1/de active
- 2004-06-22 DK DK04740230T patent/DK1641787T3/da active
- 2004-06-22 BR BRPI0411729 patent/BRPI0411729A/pt not_active Application Discontinuation
- 2004-06-22 PL PL04740230T patent/PL1641787T3/pl unknown
- 2004-06-22 KR KR1020057024715A patent/KR101131378B1/ko not_active Expired - Fee Related
- 2004-06-22 EP EP04740230A patent/EP1641787B1/en not_active Expired - Lifetime
- 2004-06-22 MX MXPA05014068A patent/MXPA05014068A/es active IP Right Grant
- 2004-06-22 NZ NZ544006A patent/NZ544006A/en not_active IP Right Cessation
- 2004-06-22 WO PCT/EP2004/006814 patent/WO2005000840A1/en not_active Ceased
- 2004-06-22 CN CNA2008101088194A patent/CN101597282A/zh active Pending
- 2004-06-22 HR HR20070286T patent/HRP20070286T3/xx unknown
- 2004-06-22 RU RU2006101859A patent/RU2343152C2/ru not_active IP Right Cessation
- 2004-06-22 US US10/561,498 patent/US8071594B2/en not_active Expired - Fee Related
- 2004-06-22 PT PT04740230T patent/PT1641787E/pt unknown
- 2004-06-22 AU AU2004251868A patent/AU2004251868B2/en not_active Ceased
- 2004-06-22 ES ES04740230T patent/ES2285474T3/es not_active Expired - Lifetime
- 2004-06-22 MY MYPI20042430 patent/MY140653A/en unknown
- 2004-06-22 JP JP2006516041A patent/JP5128126B2/ja not_active Expired - Fee Related
- 2004-06-22 CN CNB2004800178348A patent/CN100404532C/zh not_active Expired - Fee Related
- 2004-06-22 CA CA 2530310 patent/CA2530310C/en not_active Expired - Fee Related
- 2004-06-22 AR ARP040102182 patent/AR044869A1/es not_active Application Discontinuation
- 2004-06-23 TW TW093118010A patent/TWI340745B/zh not_active IP Right Cessation
-
2005
- 2005-12-06 ZA ZA200509890A patent/ZA200509890B/en unknown
- 2005-12-12 IL IL172529A patent/IL172529A/en active IP Right Grant
- 2005-12-21 MA MA28677A patent/MA27887A1/fr unknown
- 2005-12-21 EG EGNA2005000854 patent/EG24929A/xx active
-
2006
- 2006-01-20 IS IS8248A patent/IS2463B/is unknown
- 2006-01-24 NO NO20060383A patent/NO332677B1/no not_active IP Right Cessation
-
2007
- 2007-07-24 CY CY071100990T patent/CY1107703T1/el unknown
-
2011
- 2011-09-13 US US13/231,211 patent/US8357685B2/en not_active Expired - Fee Related
-
2012
- 2012-12-14 US US13/715,433 patent/US20130102783A1/en not_active Abandoned
-
2013
- 2013-11-05 US US14/072,376 patent/US8937179B2/en not_active Expired - Fee Related
-
2014
- 2014-12-15 US US14/570,812 patent/US20150105387A1/en not_active Abandoned
-
2015
- 2015-11-20 US US14/946,920 patent/US9452169B2/en not_active Expired - Fee Related
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| BR9702074A (pt) | Compostos biaril heterocíclicos composições farmacêuticas e cosméticas que os contêm e suas utilizações | |
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