CN102666550B - 作为orl-1受体拮抗剂的螺环哌啶化合物 - Google Patents
作为orl-1受体拮抗剂的螺环哌啶化合物 Download PDFInfo
- Publication number
- CN102666550B CN102666550B CN201080051845.3A CN201080051845A CN102666550B CN 102666550 B CN102666550 B CN 102666550B CN 201080051845 A CN201080051845 A CN 201080051845A CN 102666550 B CN102666550 B CN 102666550B
- Authority
- CN
- China
- Prior art keywords
- methyl
- pyran
- mmol
- fluoro
- compound
- 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
- ALDFBAMFJCZMRT-UHFFFAOYSA-N CC(c1cccc(F)c1-[n]1nc(C)c(CN(CC2)CCC2(c([s]2)c3cc2Cl)OCC3(F)F)c1)=O Chemical compound CC(c1cccc(F)c1-[n]1nc(C)c(CN(CC2)CCC2(c([s]2)c3cc2Cl)OCC3(F)F)c1)=O ALDFBAMFJCZMRT-UHFFFAOYSA-N 0.000 description 1
- HVIAOFIEKAUDPM-QGZVFWFLSA-N CCC[C@]1(CCNC(OC(C)(C)C)=O)OCCc2c1[s]cc2 Chemical compound CCC[C@]1(CCNC(OC(C)(C)C)=O)OCCc2c1[s]cc2 HVIAOFIEKAUDPM-QGZVFWFLSA-N 0.000 description 1
- KGFCOCLGHPXYIN-UHFFFAOYSA-N Cc(c(C=O)c1)n[n]1-c1c(COC(NC)=O)cccc1F Chemical compound Cc(c(C=O)c1)n[n]1-c1c(COC(NC)=O)cccc1F KGFCOCLGHPXYIN-UHFFFAOYSA-N 0.000 description 1
- QNJASCCBDIAEPG-UHFFFAOYSA-N Cc(c(C=O)c1)n[n]1-c1c(COC)cccc1F Chemical compound Cc(c(C=O)c1)n[n]1-c1c(COC)cccc1F QNJASCCBDIAEPG-UHFFFAOYSA-N 0.000 description 1
- QTOTZWFQCWGMHS-UHFFFAOYSA-N Cc(c(CN(CC1)CCC1(c([s]1)c2cc1Cl)OCC2(F)F)c1)n[n]1-c(c(F)ccc1)c1F Chemical compound Cc(c(CN(CC1)CCC1(c([s]1)c2cc1Cl)OCC2(F)F)c1)n[n]1-c(c(F)ccc1)c1F QTOTZWFQCWGMHS-UHFFFAOYSA-N 0.000 description 1
- 0 OCc(c(C*(CC1)CCC1(c([s]1)c2cc1Cl)OCC2(F)F)c1)n[n]1-c(c(F)ccc1)c1F Chemical compound OCc(c(C*(CC1)CCC1(c([s]1)c2cc1Cl)OCC2(F)F)c1)n[n]1-c(c(F)ccc1)c1F 0.000 description 1
Classifications
-
- 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
- C07D495/12—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 three hetero rings
- C07D495/20—Spiro-condensed systems
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
-
- 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
- A61P25/06—Antimigraine agents
-
- 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
- A61P25/24—Antidepressants
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Child & Adolescent Psychology (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09382245 | 2009-11-16 | ||
| EP09382245.0 | 2009-11-16 | ||
| US29862810P | 2010-01-27 | 2010-01-27 | |
| US61/298,628 | 2010-01-27 | ||
| PCT/US2010/056449 WO2011060217A1 (en) | 2009-11-16 | 2010-11-12 | Spiropiperidine compounds as orl-1 receptor antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102666550A CN102666550A (zh) | 2012-09-12 |
| CN102666550B true CN102666550B (zh) | 2015-07-15 |
Family
ID=41800752
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201080051845.3A Expired - Fee Related CN102666550B (zh) | 2009-11-16 | 2010-11-12 | 作为orl-1受体拮抗剂的螺环哌啶化合物 |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US20120214784A1 (https=) |
| EP (1) | EP2501704B1 (https=) |
| JP (1) | JP5723381B2 (https=) |
| KR (1) | KR101368130B1 (https=) |
| CN (1) | CN102666550B (https=) |
| AU (1) | AU2010319400B2 (https=) |
| BR (1) | BR112012011710A2 (https=) |
| CA (1) | CA2781041C (https=) |
| DK (1) | DK2501704T3 (https=) |
| EA (1) | EA020391B1 (https=) |
| ES (1) | ES2436241T3 (https=) |
| HR (1) | HRP20130969T1 (https=) |
| MX (1) | MX2012005690A (https=) |
| PL (1) | PL2501704T3 (https=) |
| PT (1) | PT2501704E (https=) |
| RS (1) | RS53017B (https=) |
| SI (1) | SI2501704T1 (https=) |
| WO (1) | WO2011060217A1 (https=) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106883246B (zh) * | 2009-12-04 | 2020-05-29 | 桑诺维恩药品公司 | 多环化合物及其使用方法 |
| TWI582096B (zh) * | 2011-12-06 | 2017-05-11 | 美國禮來大藥廠 | 用於酒精依賴及濫用處理之４',５'－二氫螺［哌啶－４,７'－噻吩并[２，３－c]哌喃］化合物 |
| TW201416370A (zh) | 2012-07-31 | 2014-05-01 | Lilly Co Eli | 用於治療焦慮之ｏｒｌ－１受體拮抗劑 |
| US20140206667A1 (en) | 2012-11-14 | 2014-07-24 | Michela Gallagher | Methods and compositions for treating schizophrenia |
| JO3638B1 (ar) * | 2015-09-09 | 2020-08-27 | Lilly Co Eli | مركبات مفيدة في تثبيط ror - جاما- t |
| CA3032141A1 (en) | 2016-07-29 | 2018-02-01 | Vadim ALEXANDROV | Compounds and compositions and uses thereof |
| UA125519C2 (uk) | 2016-07-29 | 2022-04-13 | Суновіон Фармасьютікалз Інк. | Сполуки і композиції і їх застосування |
| KR20190037305A (ko) | 2016-08-10 | 2019-04-05 | 바이엘 크롭사이언스 악티엔게젤샤프트 | 해충 방제제로서의 치환된 2-헤테로시클릴 이미다졸릴-카르복스아미드 |
| IL268694B2 (en) | 2017-02-16 | 2023-10-01 | Sunovion Pharmaceuticals Inc | Treatment of schizophrenia |
| DK3589637T3 (da) * | 2017-03-02 | 2021-06-14 | Lilly Co Eli | Forbindelser, der er anvendelige til inhibering af ROR-GAMMA-T |
| PL3589638T3 (pl) | 2017-03-02 | 2021-09-27 | Eli Lilly And Company | Związki użyteczne do hamowania ror-gamma-t |
| BR112020001433A2 (pt) | 2017-08-02 | 2020-07-28 | Sunovion Pharmaceuticals Inc. | compostos de isocromano e usos dos mesmos |
| EA202091945A1 (ru) | 2018-02-16 | 2021-01-18 | Суновион Фармасьютикалз Инк. | Соли, кристаллические формы и способы их получения |
| TWI848031B (zh) | 2018-12-17 | 2024-07-11 | 美商維泰克斯製藥公司 | Apol1抑制劑及其使用方法 |
| MX2021010880A (es) | 2019-03-14 | 2022-01-18 | Sunovion Pharmaceuticals Inc | Sales de un compuesto de isocromanilo y formas cristalinas, procesos de preparacion, usos terapeuticos y composiciones farmaceuticas de las mismas. |
| EP3766879A1 (en) | 2019-07-19 | 2021-01-20 | Basf Se | Pesticidal pyrazole derivatives |
| CN115734785A (zh) | 2020-04-14 | 2023-03-03 | 桑诺维恩药品公司 | (S)-(4,5-二氢-7H-噻吩并[2,3-c]吡喃-7-基)-N-甲基甲胺用于治疗神经和精神方面的病症 |
| WO2021252863A1 (en) | 2020-06-12 | 2021-12-16 | Vertex Pharmaceuticals Incorporated | Solid forms of apol1 inhibitor and using the same |
| IL300298B2 (en) | 2020-08-26 | 2025-06-01 | Vertex Pharma | Inhibitors of apol1 and methods of using same |
| CN119343353A (zh) * | 2022-02-08 | 2025-01-21 | 弗特克斯药品有限公司 | 作为APOL1抑制剂的2-甲基-4',5'-二氢螺[哌啶-4,7'-噻吩并[2,3-c]吡喃]衍生物和其使用方法 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005016913A1 (en) * | 2003-08-19 | 2005-02-24 | Pfizer Japan, Inc. | Tetrahydroisoquinoline or isochroman compounds as orl-1 receptor ligands for the treatment of pain and cns disorders |
| WO2005066183A1 (de) * | 2003-12-23 | 2005-07-21 | Grünenthal GmbH | Spirocyclische cyclohexan-derivate mit affinität zum orl1-rezeptor |
| CN101227903A (zh) * | 2005-06-02 | 2008-07-23 | 詹森药业有限公司 | 用作orl-1受体调节剂的新型3-螺环吲哚基衍生物 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2003235912A1 (en) | 2002-05-10 | 2003-11-11 | Taisho Pharmaceutical Co., Ltd. | Spiro-ring compound |
| CA2563164A1 (en) * | 2004-03-29 | 2005-10-06 | Pfizer Inc. | Alpha aryl or heteroaryl methyl beta piperidino propanoic acid compounds as orl1-receptor antagonists |
| DE102004039382A1 (de) * | 2004-08-13 | 2006-02-23 | Grünenthal GmbH | Spirocyclische Cyclohexan-Derivate |
-
2010
- 2010-11-12 ES ES10782486T patent/ES2436241T3/es active Active
- 2010-11-12 EP EP10782486.4A patent/EP2501704B1/en active Active
- 2010-11-12 PT PT107824864T patent/PT2501704E/pt unknown
- 2010-11-12 SI SI201030389T patent/SI2501704T1/sl unknown
- 2010-11-12 RS RS20130484A patent/RS53017B/sr unknown
- 2010-11-12 AU AU2010319400A patent/AU2010319400B2/en not_active Ceased
- 2010-11-12 DK DK10782486.4T patent/DK2501704T3/da active
- 2010-11-12 KR KR1020127012503A patent/KR101368130B1/ko not_active Expired - Fee Related
- 2010-11-12 WO PCT/US2010/056449 patent/WO2011060217A1/en not_active Ceased
- 2010-11-12 US US13/504,176 patent/US20120214784A1/en not_active Abandoned
- 2010-11-12 BR BR112012011710A patent/BR112012011710A2/pt active Search and Examination
- 2010-11-12 CN CN201080051845.3A patent/CN102666550B/zh not_active Expired - Fee Related
- 2010-11-12 PL PL10782486T patent/PL2501704T3/pl unknown
- 2010-11-12 EA EA201290355A patent/EA020391B1/ru not_active IP Right Cessation
- 2010-11-12 MX MX2012005690A patent/MX2012005690A/es active IP Right Grant
- 2010-11-12 CA CA2781041A patent/CA2781041C/en not_active Expired - Fee Related
- 2010-11-12 HR HRP20130969AT patent/HRP20130969T1/hr unknown
- 2010-11-12 JP JP2012538997A patent/JP5723381B2/ja active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005016913A1 (en) * | 2003-08-19 | 2005-02-24 | Pfizer Japan, Inc. | Tetrahydroisoquinoline or isochroman compounds as orl-1 receptor ligands for the treatment of pain and cns disorders |
| WO2005066183A1 (de) * | 2003-12-23 | 2005-07-21 | Grünenthal GmbH | Spirocyclische cyclohexan-derivate mit affinität zum orl1-rezeptor |
| CN1922189A (zh) * | 2003-12-23 | 2007-02-28 | 格吕伦塔尔有限公司 | 对orl1受体具有亲合力的螺环环己烷衍生物 |
| CN101227903A (zh) * | 2005-06-02 | 2008-07-23 | 詹森药业有限公司 | 用作orl-1受体调节剂的新型3-螺环吲哚基衍生物 |
Non-Patent Citations (1)
| Title |
|---|
| Design, synthesis, and structure–activity relationship study of a novel class of ORL1 receptor antagonists based on N-biarylmethyl spiropiperidine;Takashi Yoshizumi，等;《Bioorganic & Medicinal Chemistry Letters》;20080516;第18卷(第13期);第3778-3782页，参见全文 * |
Also Published As
| Publication number | Publication date |
|---|---|
| EA020391B1 (ru) | 2014-10-30 |
| DK2501704T3 (da) | 2013-10-14 |
| EA201290355A1 (ru) | 2012-10-30 |
| AU2010319400A1 (en) | 2012-06-07 |
| CA2781041C (en) | 2015-01-06 |
| KR101368130B1 (ko) | 2014-02-27 |
| CA2781041A1 (en) | 2011-05-19 |
| CN102666550A (zh) | 2012-09-12 |
| PL2501704T3 (pl) | 2014-02-28 |
| ES2436241T3 (es) | 2013-12-27 |
| MX2012005690A (es) | 2012-06-13 |
| PT2501704E (pt) | 2013-12-05 |
| WO2011060217A1 (en) | 2011-05-19 |
| EP2501704A1 (en) | 2012-09-26 |
| US20120214784A1 (en) | 2012-08-23 |
| SI2501704T1 (sl) | 2013-11-29 |
| RS53017B (sr) | 2014-04-30 |
| AU2010319400B2 (en) | 2013-12-19 |
| JP5723381B2 (ja) | 2015-05-27 |
| HRP20130969T1 (hr) | 2013-11-22 |
| EP2501704B1 (en) | 2013-09-18 |
| KR20120082927A (ko) | 2012-07-24 |
| JP2013510870A (ja) | 2013-03-28 |
| BR112012011710A2 (pt) | 2016-03-01 |
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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 | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20150715 Termination date: 20201112 |
|
| CF01 | Termination of patent right due to non-payment of annual fee |