CN105492444B - 作为rock抑制剂的三环吡啶-甲酰胺衍生物 - Google Patents
作为rock抑制剂的三环吡啶-甲酰胺衍生物 Download PDFInfo
- Publication number
- CN105492444B CN105492444B CN201480047827.6A CN201480047827A CN105492444B CN 105492444 B CN105492444 B CN 105492444B CN 201480047827 A CN201480047827 A CN 201480047827A CN 105492444 B CN105492444 B CN 105492444B
- Authority
- CN
- China
- Prior art keywords
- formamides
- pyridine
- independently selected
- methyl
- chromenes
- 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
- 0 *C1(*)Oc2cnccc2-c(cc2)c1cc2C(N(*)I*)=O Chemical compound *C1(*)Oc2cnccc2-c(cc2)c1cc2C(N(*)I*)=O 0.000 description 12
- ADSHFRMFRSOQMK-UHFFFAOYSA-N CC(C)(C)OC(c1cc(C(OC)=O)ccc1-c(ccnc1)c1F)O Chemical compound CC(C)(C)OC(c1cc(C(OC)=O)ccc1-c(ccnc1)c1F)O ADSHFRMFRSOQMK-UHFFFAOYSA-N 0.000 description 1
- CEXVLVNZCGTQOG-UHFFFAOYSA-N CC(Nc1ncc(C=O)c(-c(c(F)c2)ccc2C(OC)=O)c1)=O Chemical compound CC(Nc1ncc(C=O)c(-c(c(F)c2)ccc2C(OC)=O)c1)=O CEXVLVNZCGTQOG-UHFFFAOYSA-N 0.000 description 1
- PBSHTJLLXCGDDK-ZBSUFXJCSA-N CC1c(ccc(C(NCc2ccccc2)=O)c2)c2N(CC#N)/C1=C/N=C\C Chemical compound CC1c(ccc(C(NCc2ccccc2)=O)c2)c2N(CC#N)/C1=C/N=C\C PBSHTJLLXCGDDK-ZBSUFXJCSA-N 0.000 description 1
- RDFUKHLDQFKKKA-UHFFFAOYSA-N CCC(C)(C)OB(B1OC(C)(C)C(C)(C)O1)OCC Chemical compound CCC(C)(C)OB(B1OC(C)(C)C(C)(C)O1)OCC RDFUKHLDQFKKKA-UHFFFAOYSA-N 0.000 description 1
- YMVGYYSDIIIVKV-UHFFFAOYSA-N CCc1cccc(C(OC)=O)c1 Chemical compound CCc1cccc(C(OC)=O)c1 YMVGYYSDIIIVKV-UHFFFAOYSA-N 0.000 description 1
- AOWDHLHIYRJMLH-GATIEOLUSA-N COC(Nc1ncc2OCC3=CC(C(/N=C\CCC4=CC=CCC4)=O)=CCC3c2c1)=O Chemical compound COC(Nc1ncc2OCC3=CC(C(/N=C\CCC4=CC=CCC4)=O)=CCC3c2c1)=O AOWDHLHIYRJMLH-GATIEOLUSA-N 0.000 description 1
- ZXGBVIJNXQHZNP-UHFFFAOYSA-N COC(c(cc1)cc(C=O)c1Br)=O Chemical compound COC(c(cc1)cc(C=O)c1Br)=O ZXGBVIJNXQHZNP-UHFFFAOYSA-N 0.000 description 1
- NRKXGUOPJRNYJP-UHFFFAOYSA-N COC(c1cc(C=O)c(B(O)O)cc1)=O Chemical compound COC(c1cc(C=O)c(B(O)O)cc1)=O NRKXGUOPJRNYJP-UHFFFAOYSA-N 0.000 description 1
- MPOVZJDNPONVJX-UHFFFAOYSA-N COC(c1cc(Cl)ccc1-c(ccnc1)c1F)=O Chemical compound COC(c1cc(Cl)ccc1-c(ccnc1)c1F)=O MPOVZJDNPONVJX-UHFFFAOYSA-N 0.000 description 1
- HXZJFTIDZBKGFX-UHFFFAOYSA-N COC(c1ccc(c2ccncc2[o]2)c2c1)=O Chemical compound COC(c1ccc(c2ccncc2[o]2)c2c1)=O HXZJFTIDZBKGFX-UHFFFAOYSA-N 0.000 description 1
- NMIXNZZPNYZUJH-UHFFFAOYSA-N COC(c1ccc2-c(ncnc3)c3OCc2c1)=O Chemical compound COC(c1ccc2-c(ncnc3)c3OCc2c1)=O NMIXNZZPNYZUJH-UHFFFAOYSA-N 0.000 description 1
- FHAGKUVBNFJZIN-FQEVSTJZSA-N C[C@@H](CNC(c1ccc(-c2ccncc2C(N2CCCN3CCCC3)=O)c2c1)=O)c(cc1)ccc1F Chemical compound C[C@@H](CNC(c1ccc(-c2ccncc2C(N2CCCN3CCCC3)=O)c2c1)=O)c(cc1)ccc1F FHAGKUVBNFJZIN-FQEVSTJZSA-N 0.000 description 1
- YKROEWGQMKPWRE-CQSZACIVSA-N C[C@H](c(cc1)ccc1F)NC(c1ccc(-c2ccncc2C(N2CC=O)=O)c2c1)=O Chemical compound C[C@H](c(cc1)ccc1F)NC(c1ccc(-c2ccncc2C(N2CC=O)=O)c2c1)=O YKROEWGQMKPWRE-CQSZACIVSA-N 0.000 description 1
- BMEMOHHPYXVQJC-CQSZACIVSA-N C[C@H](c(cc1)ccc1F)NC(c1ccc(-c2ccncc2C(N2CCO)=O)c2c1)=O Chemical compound C[C@H](c(cc1)ccc1F)NC(c1ccc(-c2ccncc2C(N2CCO)=O)c2c1)=O BMEMOHHPYXVQJC-CQSZACIVSA-N 0.000 description 1
- OPVSJIZFISHPHE-OAHLLOKOSA-N C[C@H](c1ccccc1)NC(c1ccc(c(ccnc2)c2[n]2CC#N)c2c1)=O Chemical compound C[C@H](c1ccccc1)NC(c1ccc(c(ccnc2)c2[n]2CC#N)c2c1)=O OPVSJIZFISHPHE-OAHLLOKOSA-N 0.000 description 1
- JFBMFWHEXBLFCR-UHFFFAOYSA-N Cc1nccc(Br)c1 Chemical compound Cc1nccc(Br)c1 JFBMFWHEXBLFCR-UHFFFAOYSA-N 0.000 description 1
- NAJUGSPESYHSNO-UHFFFAOYSA-N N#Cc1ccc(-c2ccncc2C(O2)=O)c2c1 Chemical compound N#Cc1ccc(-c2ccncc2C(O2)=O)c2c1 NAJUGSPESYHSNO-UHFFFAOYSA-N 0.000 description 1
- SVAJSAMDBJJLHR-LJQANCHMSA-N N=C[C@H](c1ccccc1)NC(c1ccc2-c3ccncc3OCc2c1)=O Chemical compound N=C[C@H](c1ccccc1)NC(c1ccc2-c3ccncc3OCc2c1)=O SVAJSAMDBJJLHR-LJQANCHMSA-N 0.000 description 1
- SMLOVOGAGJNHIL-UHFFFAOYSA-N NC(c(cc1)cc2c1-c1ccncc1OC2)=O Chemical compound NC(c(cc1)cc2c1-c1ccncc1OC2)=O SMLOVOGAGJNHIL-UHFFFAOYSA-N 0.000 description 1
- AWGKNSICQDCNTN-UHFFFAOYSA-N OC(c1ccc(-c2ccncc2C(O2)=O)c2c1)=O Chemical compound OC(c1ccc(-c2ccncc2C(O2)=O)c2c1)=O AWGKNSICQDCNTN-UHFFFAOYSA-N 0.000 description 1
- SXZJUBJSRPSDLE-UHFFFAOYSA-N OC(c1ccc(c2ccncc2[o]2)c2c1)=O Chemical compound OC(c1ccc(c2ccncc2[o]2)c2c1)=O SXZJUBJSRPSDLE-UHFFFAOYSA-N 0.000 description 1
- VAEFYSIKWBIUHC-UHFFFAOYSA-N OC(c1cccc(CNC(c(cc2)cc3c2-c2ccncc2OC3)=O)c1)=O Chemical compound OC(c1cccc(CNC(c(cc2)cc3c2-c2ccncc2OC3)=O)c1)=O VAEFYSIKWBIUHC-UHFFFAOYSA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
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- A61P11/06—Antiasthmatics
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- 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
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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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Biomedical Technology (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Virology (AREA)
- Hospice & Palliative Care (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Ophthalmology & Optometry (AREA)
- Molecular Biology (AREA)
- Diabetes (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Vascular Medicine (AREA)
- Hematology (AREA)
- Gynecology & Obstetrics (AREA)
- Endocrinology (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361842098P | 2013-07-02 | 2013-07-02 | |
| US61/842,098 | 2013-07-02 | ||
| PCT/US2014/044988 WO2015002915A1 (en) | 2013-07-02 | 2014-07-01 | Tricyclic pyri do-carboxam i d e derivatives as rock inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN105492444A CN105492444A (zh) | 2016-04-13 |
| CN105492444B true CN105492444B (zh) | 2018-09-07 |
Family
ID=51211901
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201480047827.6A Expired - Fee Related CN105492444B (zh) | 2013-07-02 | 2014-07-01 | 作为rock抑制剂的三环吡啶-甲酰胺衍生物 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US9914740B2 (https=) |
| EP (1) | EP3016951B1 (https=) |
| JP (1) | JP6434968B2 (https=) |
| CN (1) | CN105492444B (https=) |
| AR (1) | AR096788A1 (https=) |
| ES (1) | ES2633987T3 (https=) |
| TW (1) | TW201506024A (https=) |
| WO (1) | WO2015002915A1 (https=) |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9708337B2 (en) | 2013-02-22 | 2017-07-18 | Bristol-Myers Squibb Company | Aryl amide-based kinase inhibitors |
| WO2014134391A1 (en) | 2013-02-28 | 2014-09-04 | Bristol-Myers Squibb Company | Phenylpyrazole derivatives as potent rock1 and rock2 inhibitors |
| AR094929A1 (es) | 2013-02-28 | 2015-09-09 | Bristol Myers Squibb Co | Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2 |
| US9914740B2 (en) | 2013-07-02 | 2018-03-13 | Bristol-Myers Squibb Company | Tricyclic pyrido-carboxamide derivatives as rock inhibitors |
| EP3016950B1 (en) | 2013-07-02 | 2017-06-07 | Bristol-Myers Squibb Company | Tricyclic pyrido-carboxamide derivatives as rock inhibitors |
| WO2015054358A1 (en) | 2013-10-11 | 2015-04-16 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| US9902702B2 (en) | 2014-07-15 | 2018-02-27 | Bristol-Myers Squibb Company | Spirocycloheptanes as inhibitors of rock |
| US10123993B2 (en) | 2015-01-09 | 2018-11-13 | Bristol-Myers Squibb Company | Cyclic ureas as inhibitors of rock |
| ES2730112T3 (es) | 2015-03-09 | 2019-11-08 | Bristol Myers Squibb Co | Lactamas como inhibidores de ROCK |
| ES2740224T3 (es) | 2015-04-10 | 2020-02-05 | Bristol Myers Squibb Co | 6H-isocromeno[3,4-c]piridinas y benzo[c][1,7]naftiridin-6-(5H)-onas como inhibidores de la cinasa asociada a adaptador 1 (AAK1) |
| KR20180011843A (ko) | 2015-06-11 | 2018-02-02 | 바실리어 파마슈티카 인터내셔널 리미티드 | 유출-펌프 억제제 및 이의 치료적 용도 |
| DK3341376T3 (da) * | 2015-08-26 | 2021-03-29 | Fundacion Del Sector Publico Estatal Centro Nac De Investigaciones Oncologicas Carlos Iii F S P Cnio | Kondenserede tricykliske forbindelser som proteinkinase-inhibitorer |
| TWI730032B (zh) | 2016-01-13 | 2021-06-11 | 美商必治妥美雅史谷比公司 | 作為rock抑制劑之螺庚烷水楊酸醯胺及相關化合物 |
| WO2017156071A1 (en) | 2016-03-09 | 2017-09-14 | Blade Therapeutics, Inc. | Cyclic keto-amide compounds as calpain modulators and methods of production and use thereof |
| WO2017205709A1 (en) | 2016-05-27 | 2017-11-30 | Bristol-Myers Squibb Company | Triazolones and tetrazolones as inhibitors of rock |
| EP3481835A4 (en) | 2016-07-05 | 2020-02-26 | Blade Therapeutics, Inc. | CALPAIN MODULATORS AND THERAPEUTIC USE THEREOF |
| JP6903731B2 (ja) | 2016-07-07 | 2021-07-14 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | 強力で選択的なrock阻害剤としてのラクタム、環状尿素、およびカルバメート、およびトリアゾロン誘導体 |
| JP7113810B2 (ja) | 2016-07-07 | 2022-08-05 | ブリストル-マイヤーズ スクイブ カンパニー | Rock阻害剤としてのスピロラクタム |
| ES2829550T3 (es) | 2016-07-07 | 2021-06-01 | Bristol Myers Squibb Co | Ureas cíclicas espiro-condensadas como inhibidores de ROCK |
| BR112019006110A2 (pt) | 2016-09-28 | 2019-09-10 | Blade Therapeutics Inc | moduladores de calpaína e usos terapêuticos dos mesmos |
| KR102511441B1 (ko) * | 2016-11-30 | 2023-03-16 | 브리스톨-마이어스 스큅 컴퍼니 | 트리시클릭 Rho 키나제 억제제 |
| JP6906105B2 (ja) * | 2017-06-16 | 2021-07-21 | 成都先導薬物開発股▲ふん▼有限公司Hitgen Ltd. | Rockを阻害する化合物及びその使用 |
| US11306081B2 (en) | 2017-07-12 | 2022-04-19 | Bristol-Myers Squibb Company | Phenylacetamides as inhibitors of rock |
| TW201908293A (zh) | 2017-07-12 | 2019-03-01 | 美商必治妥美雅史谷比公司 | 作為rock抑制劑之5員及雙環雜環醯胺 |
| US11447487B2 (en) | 2017-07-12 | 2022-09-20 | Bristol-Myers Squibb Company | Spiroheptanyl hydantoins as rock inhibitors |
| US12060341B2 (en) | 2017-07-12 | 2024-08-13 | Bristol-Myers Squibb Company | Spiroheptanyl hydantoins as ROCK inhibitors |
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| US9914740B2 (en) | 2018-03-13 |
| EP3016951B1 (en) | 2017-05-31 |
| JP2016523922A (ja) | 2016-08-12 |
| AR096788A1 (es) | 2016-02-03 |
| EP3016951A1 (en) | 2016-05-11 |
| WO2015002915A1 (en) | 2015-01-08 |
| ES2633987T3 (es) | 2017-09-26 |
| TW201506024A (zh) | 2015-02-16 |
| CN105492444A (zh) | 2016-04-13 |
| US20160152628A1 (en) | 2016-06-02 |
| JP6434968B2 (ja) | 2018-12-05 |
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