JP2012512886A5 - - Google Patents
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- Publication number
- JP2012512886A5 JP2012512886A5 JP2011542419A JP2011542419A JP2012512886A5 JP 2012512886 A5 JP2012512886 A5 JP 2012512886A5 JP 2011542419 A JP2011542419 A JP 2011542419A JP 2011542419 A JP2011542419 A JP 2011542419A JP 2012512886 A5 JP2012512886 A5 JP 2012512886A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- hydrogen
- membered
- cycloalkyl
- 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.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims 51
- 125000005842 heteroatom Chemical group 0.000 claims 39
- 229910052739 hydrogen Inorganic materials 0.000 claims 39
- 229910052760 oxygen Inorganic materials 0.000 claims 38
- 125000000623 heterocyclic group Chemical group 0.000 claims 37
- 239000001257 hydrogen Substances 0.000 claims 36
- 229910052717 sulfur Inorganic materials 0.000 claims 32
- 150000002431 hydrogen Chemical class 0.000 claims 29
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 20
- 229910052799 carbon Inorganic materials 0.000 claims 18
- 125000003386 piperidinyl group Chemical group 0.000 claims 18
- 150000001875 compounds Chemical class 0.000 claims 17
- -1 (+) -O Chemical class 0.000 claims 15
- 229910052757 nitrogen Inorganic materials 0.000 claims 15
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 15
- 150000001721 carbon Chemical group 0.000 claims 13
- 125000002757 morpholinyl group Chemical group 0.000 claims 13
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 11
- 125000004193 piperazinyl group Chemical group 0.000 claims 11
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 9
- DHKHKXVYLBGOIT-UHFFFAOYSA-N acetaldehyde Diethyl Acetal Natural products CCOC(C)OCC DHKHKXVYLBGOIT-UHFFFAOYSA-N 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- 125000004076 pyridyl group Chemical group 0.000 claims 6
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 5
- 125000002393 azetidinyl group Chemical group 0.000 claims 5
- 125000002883 imidazolyl group Chemical group 0.000 claims 5
- 125000002837 carbocyclic group Chemical group 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- 125000003725 azepanyl group Chemical group 0.000 claims 3
- 125000002576 diazepinyl group Chemical group N1N=C(C=CC=C1)* 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 3
- 125000003226 pyrazolyl group Chemical group 0.000 claims 3
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 3
- 125000005988 1,1-dioxo-thiomorpholinyl group Chemical group 0.000 claims 2
- 125000005960 1,4-diazepanyl group Chemical group 0.000 claims 2
- 125000005962 1,4-oxazepanyl group Chemical group 0.000 claims 2
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000005961 oxazepanyl group Chemical group 0.000 claims 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- 241000907681 Morpho Species 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000017733 acquired polycythemia vera Diseases 0.000 claims 1
- 125000002047 benzodioxolyl group Chemical group O1OC(C2=C1C=CC=C2)* 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 239000001307 helium Substances 0.000 claims 1
- 229910052734 helium Inorganic materials 0.000 claims 1
- SWQJXJOGLNCZEY-UHFFFAOYSA-N helium atom Chemical compound [He] SWQJXJOGLNCZEY-UHFFFAOYSA-N 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- BQJCRHHNABKAKU-KBQPJGBKSA-N morphine Chemical group O([C@H]1[C@H](C=C[C@H]23)O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O BQJCRHHNABKAKU-KBQPJGBKSA-N 0.000 claims 1
- 206010028537 myelofibrosis Diseases 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 208000037244 polycythemia vera Diseases 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 206010043554 thrombocytopenia Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US13904208P | 2008-12-19 | 2008-12-19 | |
| US61/139,042 | 2008-12-19 | ||
| PCT/US2009/068394 WO2010080474A1 (en) | 2008-12-19 | 2009-12-17 | Carbazole and carboline kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012512886A JP2012512886A (ja) | 2012-06-07 |
| JP2012512886A5 true JP2012512886A5 (https=) | 2013-01-24 |
| JP5557849B2 JP5557849B2 (ja) | 2014-07-23 |
Family
ID=41625988
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011542419A Expired - Fee Related JP5557849B2 (ja) | 2008-12-19 | 2009-12-17 | カルバゾールおよびカルボリンキナーゼ阻害剤 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US8815840B2 (https=) |
| EP (1) | EP2370407B1 (https=) |
| JP (1) | JP5557849B2 (https=) |
| CN (1) | CN102325752B (https=) |
| ES (1) | ES2490867T3 (https=) |
| WO (1) | WO2010080474A1 (https=) |
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8084620B2 (en) | 2008-12-19 | 2011-12-27 | Bristol-Myers Squibb Company | Carbazole carboxamide compounds useful as kinase inhibitors |
| MX2012002480A (es) | 2009-09-03 | 2012-03-26 | Bristol Myers Squibb Co | Inhibidores de jak2 y su uso en el tratamiento de enfermedades mieloproliferativas y cancer. |
| US9492460B2 (en) * | 2013-02-27 | 2016-11-15 | Bristol-Myers Squibb Company | Carbazole compounds useful as bromodomain inhibitors |
| EP2961747B1 (en) | 2013-02-27 | 2017-11-15 | Bristol-Myers Squibb Company | Carbazole compounds useful as bromodomain inhibitors |
| AR096788A1 (es) * | 2013-07-02 | 2016-02-03 | Bristol Myers Squibb Co | Compuestos tricíclicos de carboxamida como inhibidores potentes de rock |
| WO2015002926A1 (en) * | 2013-07-02 | 2015-01-08 | Bristol-Myers Squibb Company | Tricyclic pyrido-carboxamide derivatives as rock inhibitors |
| GB201317363D0 (en) | 2013-10-01 | 2013-11-13 | Eisai Ltd | Novel compounds |
| US9458156B2 (en) | 2014-12-23 | 2016-10-04 | Bristol-Myers Squibb Company | Tricyclic compounds as anticancer agents |
| KR102457145B1 (ko) * | 2013-12-24 | 2022-10-19 | 브리스톨-마이어스 스큅 컴퍼니 | 항암제로서의 트리시클릭 화합물 |
| EA036518B1 (ru) * | 2015-02-02 | 2020-11-18 | Юсб Байофарма Спрл | Производные 9h-пирролодипиридина |
| GB201512678D0 (en) * | 2015-07-20 | 2015-08-26 | Wista Lab Ltd | Methods of chemical synthesis |
| WO2017070089A1 (en) | 2015-10-19 | 2017-04-27 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| SG10202004618TA (en) | 2015-11-19 | 2020-06-29 | Incyte Corp | Heterocyclic compounds as immunomodulators |
| MA44075A (fr) | 2015-12-17 | 2021-05-19 | Incyte Corp | Dérivés de n-phényl-pyridine-2-carboxamide et leur utilisation en tant que modulateurs des interactions protéine/protéine pd-1/pd-l1 |
| AU2016379372A1 (en) | 2015-12-22 | 2018-08-02 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| AR108396A1 (es) | 2016-05-06 | 2018-08-15 | Incyte Corp | Compuestos heterocíclicos como inmunomoduladores |
| WO2017205464A1 (en) | 2016-05-26 | 2017-11-30 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| HUE060256T2 (hu) | 2016-06-20 | 2023-02-28 | Incyte Corp | Heterociklusos vegyületek mint immunmodulátorok |
| KR102625861B1 (ko) * | 2016-06-28 | 2024-01-17 | 삼성디스플레이 주식회사 | 헤테로시클릭 화합물 및 이를 포함한 유기 발광 소자 |
| EP3484866B1 (en) | 2016-07-14 | 2022-09-07 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| WO2018044783A1 (en) | 2016-08-29 | 2018-03-08 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| JP7101678B2 (ja) | 2016-12-22 | 2022-07-15 | インサイト・コーポレイション | 免疫調節剤としての複素環式化合物 |
| ES2874756T3 (es) | 2016-12-22 | 2021-11-05 | Incyte Corp | Derivados de triazolo[1,5-A]piridina como inmunomoduladores |
| US20180179202A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| WO2018119221A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Pyridine derivatives as immunomodulators |
| SMT202500157T1 (it) | 2018-03-30 | 2025-05-12 | Incyte Corp | Composti eterociclici come immunomodulatori |
| HUE061503T2 (hu) | 2018-05-11 | 2023-07-28 | Incyte Corp | Tetrahidro-imidazo[4,5-C]piridin-származékok mint PD-L1 immunmodulátorok |
| GB201809102D0 (en) * | 2018-06-04 | 2018-07-18 | Univ Oxford Innovation Ltd | Compounds |
| US10947253B2 (en) | 2019-08-05 | 2021-03-16 | Ankh Life Sciences Limited | Fused polycyclic dimers |
| JP7665593B2 (ja) | 2019-08-09 | 2025-04-21 | インサイト・コーポレイション | Ｐｄ－１／ｐｄ－ｌ１阻害剤の塩 |
| US20220372135A1 (en) | 2019-09-27 | 2022-11-24 | Disc Medicine, Inc. | Methods for treating myelofibrosis and related conditions |
| PE20221038A1 (es) | 2019-09-30 | 2022-06-17 | Incyte Corp | Compuestos de pirido[3,2-d] pirimidina como inmunomoduladores |
| CN114829350B (zh) * | 2019-10-04 | 2024-05-28 | 百时美施贵宝公司 | 经取代的咔唑化合物 |
| CA3160131A1 (en) | 2019-11-11 | 2021-05-20 | Incyte Corporation | Salts and crystalline forms of a pd-1/pd-l1 inhibitor |
| US12129265B2 (en) | 2020-07-21 | 2024-10-29 | Ankh Life Sciences Limited | Therapeutic agents and uses thereof |
| TW202233615A (zh) | 2020-11-06 | 2022-09-01 | 美商英塞特公司 | Ｐｄ—１／ｐｄ—ｌ１抑制劑之結晶形式 |
| WO2022099018A1 (en) | 2020-11-06 | 2022-05-12 | Incyte Corporation | Process of preparing a pd-1/pd-l1 inhibitor |
| CR20230230A (es) | 2020-11-06 | 2023-07-27 | Incyte Corp | Proceso para hacer un inhibidor de pd-1/pdl1 y sales y formas cristalinas del mismo |
| CN113880836B (zh) * | 2021-10-18 | 2023-03-14 | 浙江中医药大学 | 1,5,8-三取代γ-咔啉类衍生物及其制备方法和应用 |
| CN118284598B (zh) * | 2021-11-19 | 2025-06-24 | 杭州拿因生物科技有限责任公司 | 四氢咔唑类化合物、其药物组合物及用途 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5532261A (en) * | 1994-12-12 | 1996-07-02 | Merck & Co., Inc. | Carbapenem antibiotics, compositions containing such compounds and methods of use |
| US20050239806A1 (en) * | 2004-01-13 | 2005-10-27 | Ambit Biosciences Corporation | Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases |
| PE20060748A1 (es) * | 2004-09-21 | 2006-10-01 | Smithkline Beecham Corp | Derivados de indolcarboxamida como inhibidores de quinasa ikk2 |
| AR055343A1 (es) * | 2005-06-30 | 2007-08-22 | Smithkline Beecham Corp | Derivados de indolcarboxamida inhibidores de quinasas ikk2 |
| JP5249772B2 (ja) * | 2005-11-22 | 2013-07-31 | メルク・シャープ・アンド・ドーム・コーポレーション | キナーゼの阻害剤として有用な三環式化合物 |
| EP1959737A4 (en) * | 2005-12-16 | 2010-12-08 | Glaxosmithkline Llc | CHEMICAL COMPOUNDS |
-
2009
- 2009-12-17 EP EP09793679.3A patent/EP2370407B1/en not_active Not-in-force
- 2009-12-17 JP JP2011542419A patent/JP5557849B2/ja not_active Expired - Fee Related
- 2009-12-17 US US13/140,184 patent/US8815840B2/en active Active
- 2009-12-17 CN CN200980157175.0A patent/CN102325752B/zh not_active Expired - Fee Related
- 2009-12-17 WO PCT/US2009/068394 patent/WO2010080474A1/en not_active Ceased
- 2009-12-17 ES ES09793679.3T patent/ES2490867T3/es active Active