JP2014507414A - 代謝疾患及び炎症疾患の治療に有用なアゼチジン誘導体 - Google Patents
代謝疾患及び炎症疾患の治療に有用なアゼチジン誘導体 Download PDFInfo
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- JP2014507414A JP2014507414A JP2013549769A JP2013549769A JP2014507414A JP 2014507414 A JP2014507414 A JP 2014507414A JP 2013549769 A JP2013549769 A JP 2013549769A JP 2013549769 A JP2013549769 A JP 2013549769A JP 2014507414 A JP2014507414 A JP 2014507414A
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- Prior art keywords
- methyl
- azetidine
- chloro
- alkyl
- compound
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- 0 C*(C)C(CC1)(*1C(CCN)=O)C(*(C)*)=O Chemical compound C*(C)C(CC1)(*1C(CCN)=O)C(*(C)*)=O 0.000 description 3
- HDCSJRCBTWALPL-UHFFFAOYSA-N CC(CC1)(C(N(CC(NC)=O)Cc(cc2)ccc2Cl)=O)N1C(Cc1cc(C)cc(C)c1)=O Chemical compound CC(CC1)(C(N(CC(NC)=O)Cc(cc2)ccc2Cl)=O)N1C(Cc1cc(C)cc(C)c1)=O HDCSJRCBTWALPL-UHFFFAOYSA-N 0.000 description 1
- JRLPEMVDPFPYPJ-UHFFFAOYSA-N CCc1ccc(C)cc1 Chemical compound CCc1ccc(C)cc1 JRLPEMVDPFPYPJ-UHFFFAOYSA-N 0.000 description 1
- XPZIFETWEXBNGS-XVNBXDOJSA-N COc1cc(OC)c(CNS(/C=C/CCl)(=O)=O)cc1 Chemical compound COc1cc(OC)c(CNS(/C=C/CCl)(=O)=O)cc1 XPZIFETWEXBNGS-XVNBXDOJSA-N 0.000 description 1
- XRYJXFNGPZNSFR-UHFFFAOYSA-N COc1cc(OC)c(CNS(CCCNCc(cc2)ccc2Cl)(=O)=O)cc1 Chemical compound COc1cc(OC)c(CNS(CCCNCc(cc2)ccc2Cl)(=O)=O)cc1 XRYJXFNGPZNSFR-UHFFFAOYSA-N 0.000 description 1
- FQSLJQDOLLSARN-GFCCVEGCSA-N C[C@@](CC1)(C(O)=O)N1C(c(cc1)ccc1Br)=O Chemical compound C[C@@](CC1)(C(O)=O)N1C(c(cc1)ccc1Br)=O FQSLJQDOLLSARN-GFCCVEGCSA-N 0.000 description 1
- MKIOLLPNPWBWBG-RXMQYKEDSA-N C[C@@]1(C=O)NCC1 Chemical compound C[C@@]1(C=O)NCC1 MKIOLLPNPWBWBG-RXMQYKEDSA-N 0.000 description 1
- YMVFJGSXZNNUDW-UHFFFAOYSA-N NCc(cc1)ccc1Cl Chemical compound NCc(cc1)ccc1Cl YMVFJGSXZNNUDW-UHFFFAOYSA-N 0.000 description 1
- PENYBFRQSLVMLW-UHFFFAOYSA-N O=C(Oc(cccc1)c1Cl)Cl Chemical compound O=C(Oc(cccc1)c1Cl)Cl PENYBFRQSLVMLW-UHFFFAOYSA-N 0.000 description 1
- GPKDGVXBXQTHRY-UHFFFAOYSA-N O=S(CCCCl)(Cl)=O Chemical compound O=S(CCCCl)(Cl)=O GPKDGVXBXQTHRY-UHFFFAOYSA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
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- 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
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- A61K31/403—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 condensed with carbocyclic rings, e.g. carbazole
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- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—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
- 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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- C—CHEMISTRY; METALLURGY
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- C—CHEMISTRY; METALLURGY
- 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
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- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
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- C07D—HETEROCYCLIC COMPOUNDS
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- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
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- C07D—HETEROCYCLIC COMPOUNDS
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- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161434077P | 2011-01-19 | 2011-01-19 | |
| US61/434,077 | 2011-01-19 | ||
| PCT/EP2012/050297 WO2012098033A1 (en) | 2011-01-19 | 2012-01-10 | Azetidine derivatives useful for the treatment of metabolic and inflammatory diseases |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014507414A true JP2014507414A (ja) | 2014-03-27 |
| JP2014507414A5 JP2014507414A5 (enExample) | 2015-03-12 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013549769A Pending JP2014507414A (ja) | 2011-01-19 | 2012-01-10 | 代謝疾患及び炎症疾患の治療に有用なアゼチジン誘導体 |
Country Status (18)
| Country | Link |
|---|---|
| US (2) | US8759334B2 (enExample) |
| EP (1) | EP2665704A1 (enExample) |
| JP (1) | JP2014507414A (enExample) |
| KR (1) | KR20140040104A (enExample) |
| CN (1) | CN103328442A (enExample) |
| AR (1) | AR084857A1 (enExample) |
| AU (1) | AU2012208693B2 (enExample) |
| BR (1) | BR112013018286A2 (enExample) |
| CA (1) | CA2824460A1 (enExample) |
| CO (1) | CO6741223A2 (enExample) |
| GB (1) | GB2489382A (enExample) |
| MX (1) | MX2013008257A (enExample) |
| PH (1) | PH12013501437A1 (enExample) |
| RU (1) | RU2013138372A (enExample) |
| SG (1) | SG191291A1 (enExample) |
| TW (1) | TW201245144A (enExample) |
| WO (1) | WO2012098033A1 (enExample) |
| ZA (1) | ZA201304822B (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPWO2017006968A1 (ja) * | 2015-07-07 | 2018-04-19 | 日本たばこ産業株式会社 | 7H−ピロロ[2,3−d]ピリミジン誘導体の製造方法及びその中間体 |
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| SG191291A1 (en) * | 2011-01-19 | 2013-07-31 | Galapagos Nv | Azetidine derivatives useful for the treatment of metabolic and inflammatory diseases |
| CN105916500A (zh) | 2013-11-27 | 2016-08-31 | 欧洲筛选有限公司 | 用于治疗炎性疾病的化合物、药物组合物和方法 |
| US9839644B2 (en) | 2014-09-09 | 2017-12-12 | ARKAY Therapeutics, LLC | Formulations and methods for treatment of metabolic syndrome |
| KR101656662B1 (ko) * | 2014-11-18 | 2016-09-12 | 한국생명공학연구원 | 2-옥소-1,2,3,4-테트라하이드로피리미딘-5-카르복사미드 유도체를 유효성분으로 함유하는 대사성 질환 예방 또는 치료용 약학적 조성물 |
| PL3560932T3 (pl) | 2016-12-21 | 2026-06-29 | Japan Tobacco Inc. | Sposób wytwarzania pochodnych 7H‑pirolo[2,3‑d]pirymidyny i ich syntetycznych produktów pośrednich |
| BR102018007822A2 (pt) | 2017-04-20 | 2018-11-06 | Gilead Sciences, Inc. | composto, métodos para inibir pd-1, pd-l1 e/ou interação de pd-1/pd-l1 e para tratamento de câncer, composição farmacêutica, e, kit para tratamento de ou prevenção de câncer ou uma doença ou condição |
| WO2019160882A1 (en) | 2018-02-13 | 2019-08-22 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| KR102591947B1 (ko) | 2018-04-19 | 2023-10-25 | 길리애드 사이언시즈, 인코포레이티드 | Pd-1/pd-l1 억제제 |
| CN108863980A (zh) * | 2018-07-05 | 2018-11-23 | 浙江工业大学 | 一种合成1-(5-苯并噻唑基)乙酮的方法 |
| PE20210642A1 (es) | 2018-07-13 | 2021-03-23 | Gilead Sciences Inc | Inhibidores de pd-1/pd-l1 |
| US11236085B2 (en) | 2018-10-24 | 2022-02-01 | Gilead Sciences, Inc. | PD-1/PD-L1 inhibitors |
| CN110684000B (zh) * | 2019-10-18 | 2021-08-31 | 上海皓元医药股份有限公司 | 苯并呋喃衍生物的制备方法 |
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| SG191291A1 (en) * | 2011-01-19 | 2013-07-31 | Galapagos Nv | Azetidine derivatives useful for the treatment of metabolic and inflammatory diseases |
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- 2012-01-10 EP EP12700552.8A patent/EP2665704A1/en not_active Withdrawn
- 2012-01-10 KR KR1020137020884A patent/KR20140040104A/ko not_active Withdrawn
- 2012-01-10 WO PCT/EP2012/050297 patent/WO2012098033A1/en not_active Ceased
- 2012-01-10 CA CA2824460A patent/CA2824460A1/en not_active Abandoned
- 2012-01-10 MX MX2013008257A patent/MX2013008257A/es not_active Application Discontinuation
- 2012-01-10 RU RU2013138372/04A patent/RU2013138372A/ru not_active Application Discontinuation
- 2012-01-10 GB GB1213267.6A patent/GB2489382A/en not_active Withdrawn
- 2012-01-10 US US13/980,798 patent/US8759334B2/en not_active Expired - Fee Related
- 2012-01-10 JP JP2013549769A patent/JP2014507414A/ja active Pending
- 2012-01-10 CN CN2012800059625A patent/CN103328442A/zh active Pending
- 2012-01-10 PH PH1/2013/501437A patent/PH12013501437A1/en unknown
- 2012-01-10 BR BR112013018286A patent/BR112013018286A2/pt not_active IP Right Cessation
- 2012-01-10 AU AU2012208693A patent/AU2012208693B2/en not_active Expired - Fee Related
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- 2013-08-15 CO CO13194671A patent/CO6741223A2/es unknown
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2014
- 2014-06-23 US US14/311,574 patent/US20140371198A1/en not_active Abandoned
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|---|---|---|---|---|
| JPWO2017006968A1 (ja) * | 2015-07-07 | 2018-04-19 | 日本たばこ産業株式会社 | 7H−ピロロ[2,3−d]ピリミジン誘導体の製造方法及びその中間体 |
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|---|---|
| GB201213267D0 (en) | 2012-09-05 |
| AU2012208693A1 (en) | 2013-03-21 |
| TW201245144A (en) | 2012-11-16 |
| CN103328442A (zh) | 2013-09-25 |
| CO6741223A2 (es) | 2013-08-30 |
| BR112013018286A2 (pt) | 2016-11-16 |
| AU2012208693B2 (en) | 2015-02-26 |
| CA2824460A1 (en) | 2012-07-26 |
| AR084857A1 (es) | 2013-06-26 |
| PH12013501437A1 (en) | 2013-09-16 |
| US20140371198A1 (en) | 2014-12-18 |
| RU2013138372A (ru) | 2015-02-27 |
| US20130303515A1 (en) | 2013-11-14 |
| GB2489382A (en) | 2012-09-26 |
| MX2013008257A (es) | 2013-08-12 |
| SG191291A1 (en) | 2013-07-31 |
| US8759334B2 (en) | 2014-06-24 |
| ZA201304822B (en) | 2014-03-26 |
| WO2012098033A1 (en) | 2012-07-26 |
| KR20140040104A (ko) | 2014-04-02 |
| EP2665704A1 (en) | 2013-11-27 |
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