CN103079563B - 作为食欲素受体拮抗剂的脯氨酸磺酰胺衍生物 - Google Patents
作为食欲素受体拮抗剂的脯氨酸磺酰胺衍生物 Download PDFInfo
- Publication number
- CN103079563B CN103079563B CN201180040497.4A CN201180040497A CN103079563B CN 103079563 B CN103079563 B CN 103079563B CN 201180040497 A CN201180040497 A CN 201180040497A CN 103079563 B CN103079563 B CN 103079563B
- Authority
- CN
- China
- Prior art keywords
- phenyl
- pyrrolidine
- methoxy
- amide
- disorders
- 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
Links
- WYUIWKFIFOJVKW-UHFFFAOYSA-N Cc(cc1)cc(Cl)c1Cl Chemical compound Cc(cc1)cc(Cl)c1Cl WYUIWKFIFOJVKW-UHFFFAOYSA-N 0.000 description 1
- GYPMBQZAVBFUIZ-UHFFFAOYSA-N Cc(cc1)cc(OC)c1OC Chemical compound Cc(cc1)cc(OC)c1OC GYPMBQZAVBFUIZ-UHFFFAOYSA-N 0.000 description 1
- LRLRAYMYEXQKID-UHFFFAOYSA-N Cc1ccc(C(F)(F)F)cc1 Chemical compound Cc1ccc(C(F)(F)F)cc1 LRLRAYMYEXQKID-UHFFFAOYSA-N 0.000 description 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/401—Proline; Derivatives thereof, e.g. captopril
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
-
- 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
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
-
- 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
- C07D207/46—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
- C07D207/48—Sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Toxicology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| WOPCT/IB2010/053799 | 2010-08-24 | ||
| IB2010053799 | 2010-08-24 | ||
| IBPCT/IB2010/053799 | 2010-08-24 | ||
| PCT/IB2011/053693 WO2012025877A1 (en) | 2010-08-24 | 2011-08-23 | Proline sulfonamide derivatives as orexin receptor antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103079563A CN103079563A (zh) | 2013-05-01 |
| CN103079563B true CN103079563B (zh) | 2015-07-08 |
Family
ID=44658790
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201180040497.4A Expired - Fee Related CN103079563B (zh) | 2010-08-24 | 2011-08-23 | 作为食欲素受体拮抗剂的脯氨酸磺酰胺衍生物 |
Country Status (9)
| Country | Link |
|---|---|
| US (3) | US8895606B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2608787B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP5744203B2 (cg-RX-API-DMAC7.html) |
| KR (1) | KR101802726B1 (cg-RX-API-DMAC7.html) |
| CN (1) | CN103079563B (cg-RX-API-DMAC7.html) |
| CA (1) | CA2807000C (cg-RX-API-DMAC7.html) |
| ES (1) | ES2769607T3 (cg-RX-API-DMAC7.html) |
| TW (1) | TW201209037A (cg-RX-API-DMAC7.html) |
| WO (1) | WO2012025877A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5744203B2 (ja) | 2010-08-24 | 2015-07-08 | アクテリオン ファーマシューティカルズ リミテッドActelion Pharmaceuticals Ltd | オレキシン受容体拮抗薬としてのプロリンスルフォンアミド誘導体 |
| CN104334544B (zh) | 2012-06-04 | 2016-10-19 | 埃科特莱茵药品有限公司 | 苯并咪唑脯氨酸衍生物 |
| SI3077389T1 (en) | 2013-12-03 | 2018-01-31 | Idorsia Pharmaceuticals Ltd | (S) - (2- (6-CHLORO-7-METHYL-1 H-BENZO (D) IMIDAZOL-2-YL) -2-METHYLPYROLIDIN-1-YL (5-METHOXY-2- (2H- , 2,3-TRIAZOL-2-IL) PHENYL) METHANONE AND ITS USE AS ANTAGONISTS OF OREXIN RECEPTOR |
| UA119151C2 (uk) | 2013-12-03 | 2019-05-10 | Ідорсія Фармасьютікалз Лтд | КРИСТАЛІЧНА СОЛЬОВА ФОРМА (S)-(2-(6-ХЛОР-7-МЕТИЛ-1H-БЕНЗО[d]ІМІДАЗОЛ-2-ІЛ)-2-МЕТИЛПІРОЛІДИН-1-ІЛ)(5-МЕТОКСИ-2-(2H-1,2,3-ТРИАЗОЛ-2-ІЛ)ФЕНІЛ)МЕТАНОНУ ЯК АНТАГОНІСТ ОРЕКСИНОВОГО РЕЦЕПТОРА |
| CA2930053A1 (en) | 2013-12-04 | 2015-06-11 | Actelion Pharmaceuticals Ltd | Use of benzimidazole-proline derivatives |
| WO2021207678A1 (en) * | 2020-04-09 | 2021-10-14 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Kappa opioid receptor antagonists for treating pain-related sleep disorders |
| EP4356909A1 (en) * | 2022-10-17 | 2024-04-24 | Selabtec Sciences, SLU | 1-(sulfonyl)-n-phenylpyrrolidine-2-carboxamides derivatives and use thereof |
| WO2025224168A1 (en) | 2024-04-24 | 2025-10-30 | Idorsia Pharmaceuticals Ltd | Aryl sulfone and sulfanone derivatives as orexin receptor modulators |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5822111B2 (ja) | 1977-10-29 | 1983-05-06 | 協和醗酵工業株式会社 | 柑橘類果実の改質剤 |
| JPS5581857A (en) | 1978-12-15 | 1980-06-20 | Kyowa Hakko Kogyo Co Ltd | Modifier of citrus fruit |
| US6291453B1 (en) * | 1997-07-31 | 2001-09-18 | Athena Neurosciences, Inc. | 4-amino-phenylalanine type compounds which inhibit leukocyte adhesion mediated by VLA-4 |
| HUP0101275A3 (en) | 1998-03-26 | 2002-12-28 | Japan Tobacco Inc | Amide derivatives and pharmaceutical compositions containing them as nociceptin antagonists |
| DE10035144A1 (de) | 2000-07-19 | 2002-01-31 | Merck Patent Gmbh | Cyclische Aminosäurederivate |
| GB0225938D0 (en) | 2002-11-06 | 2002-12-11 | Glaxo Group Ltd | Novel compounds |
| US7288538B2 (en) | 2003-02-20 | 2007-10-30 | Encysive Pharmaceuticals, Inc. | Phenylenediamine urotensin-II receptor antagonists and CCR-9 antagonists |
| EP2415760A3 (en) | 2003-02-20 | 2012-02-22 | Encysive Pharmaceuticals, Inc. | CCR-9 antagonists |
| CN1898227A (zh) | 2003-12-22 | 2007-01-17 | 安斯泰来制药有限公司 | 作为前列腺素e2激动剂或拮抗剂的鸟氨酸衍生物 |
| CN1926109B (zh) | 2004-03-01 | 2011-04-13 | 埃科特莱茵药品有限公司 | 经取代的1,2,3,4-四氢异喹啉衍生物 |
| WO2006022442A1 (ja) | 2004-08-24 | 2006-03-02 | Santen Pharmaceutical Co., Ltd. | ジヒドロオロテートデヒドロゲナーゼ阻害活性を有する新規複素環アミド誘導体 |
| US8143288B2 (en) | 2005-06-06 | 2012-03-27 | Bristol-Myers Squibb Company | Inhibitors of HCV replication |
| US7998959B2 (en) | 2006-01-12 | 2011-08-16 | Incyte Corporation | Modulators of 11-β hydroxyl steroid dehydrogenase type 1, pharmaceutical compositions thereof, and methods of using the same |
| AU2007226203A1 (en) | 2006-03-15 | 2007-09-20 | Actelion Pharmaceuticals Ltd | Tetrahydroisoquinoline derivatives to enhance memory function |
| JP2009543790A (ja) | 2006-07-14 | 2009-12-10 | メルク エンド カムパニー インコーポレーテッド | 2−置換プロリンビス−アミドオレキシン受容体アンタゴニスト |
| PE20091010A1 (es) | 2007-10-10 | 2009-08-08 | Actelion Pharmaceuticals Ltd | Derivados de tetrahidroquinolina |
| CA2709784A1 (en) | 2007-12-21 | 2009-07-09 | University Of Rochester | Method for altering the lifespan of eukaryotic organisms |
| US8084612B2 (en) * | 2008-01-08 | 2011-12-27 | Purdue Pharma L.P. | Proline analogs as ligands for cannabinoid receptors |
| JP5346043B2 (ja) * | 2008-02-12 | 2013-11-20 | エフ.ホフマン−ラ ロシュ アーゲー | ピペリジンスルホンアミド誘導体 |
| US8629157B2 (en) | 2009-01-05 | 2014-01-14 | Boehringer Ingelheim International Gmbh | Pyrrolidine compounds which modulate the CB2 receptor |
| ES2350548B1 (es) | 2009-06-25 | 2011-09-29 | Institut Univ. De Ciència I Tecnologia, S.A. | N-fenil-1-sulfonil-2-pirrolidinacarboxamidas para la identificacion de actividad biologica y farmacologica. |
| ES2351323B1 (es) | 2009-06-26 | 2011-10-05 | Institut Univ. De Ciència I Tecnologia, S.A. | Bibliotecas de n-fenil-1-sulfonil-2-pirrolidinacarboxamidas para el descubrimiento de farmacos. |
| ES2351452B1 (es) | 2009-07-01 | 2011-10-05 | Institut Univ. De Ciència I Tecnologia, S.A. | Bibliotecas de n-fenil-1-sulfonil-2-pirrolidinacarboxamidas para la identificacion de actividad biologica y farmacologica. |
| JP5744203B2 (ja) | 2010-08-24 | 2015-07-08 | アクテリオン ファーマシューティカルズ リミテッドActelion Pharmaceuticals Ltd | オレキシン受容体拮抗薬としてのプロリンスルフォンアミド誘導体 |
| CN104334544B (zh) | 2012-06-04 | 2016-10-19 | 埃科特莱茵药品有限公司 | 苯并咪唑脯氨酸衍生物 |
-
2011
- 2011-08-23 JP JP2013525400A patent/JP5744203B2/ja not_active Expired - Fee Related
- 2011-08-23 CN CN201180040497.4A patent/CN103079563B/zh not_active Expired - Fee Related
- 2011-08-23 CA CA2807000A patent/CA2807000C/en active Active
- 2011-08-23 EP EP11758563.8A patent/EP2608787B1/en active Active
- 2011-08-23 US US13/818,647 patent/US8895606B2/en active Active
- 2011-08-23 WO PCT/IB2011/053693 patent/WO2012025877A1/en not_active Ceased
- 2011-08-23 ES ES11758563T patent/ES2769607T3/es active Active
- 2011-08-23 KR KR1020137007125A patent/KR101802726B1/ko not_active Expired - Fee Related
- 2011-08-23 TW TW100130171A patent/TW201209037A/zh unknown
-
2014
- 2014-10-31 US US14/530,532 patent/US9000029B2/en active Active
-
2015
- 2015-03-05 US US14/639,934 patent/US9211279B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| TW201209037A (en) | 2012-03-01 |
| CN103079563A (zh) | 2013-05-01 |
| EP2608787B1 (en) | 2019-11-20 |
| US9211279B2 (en) | 2015-12-15 |
| CA2807000C (en) | 2018-12-04 |
| JP2013538206A (ja) | 2013-10-10 |
| US9000029B2 (en) | 2015-04-07 |
| US20150246021A1 (en) | 2015-09-03 |
| US8895606B2 (en) | 2014-11-25 |
| KR20130110160A (ko) | 2013-10-08 |
| KR101802726B1 (ko) | 2017-11-29 |
| EP2608787A1 (en) | 2013-07-03 |
| JP5744203B2 (ja) | 2015-07-08 |
| ES2769607T3 (es) | 2020-06-26 |
| WO2012025877A1 (en) | 2012-03-01 |
| CA2807000A1 (en) | 2012-03-01 |
| US20130150424A1 (en) | 2013-06-13 |
| US20150057328A1 (en) | 2015-02-26 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| TR01 | Transfer of patent right | ||
| TR01 | Transfer of patent right |
Effective date of registration: 20171108 Address after: Swiss A Skei Weil Patentee after: ACTELION PHARMACEUTICALS LTD. Address before: Swiss A Skei Weil Patentee before: Actelion Pharmaceuticals Ltd. |
|
| CF01 | Termination of patent right due to non-payment of annual fee | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20150708 |