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 |
|---|---|---|---|---|
| JP5487214B2 (ja) | 2008-12-19 | 2014-05-07 | ブリストル−マイヤーズ スクイブ カンパニー | キナーゼ阻害剤として有用なカルバゾールカルボキシアミド化合物 |
| JP5567137B2 (ja) | 2009-09-03 | 2014-08-06 | ブリストル−マイヤーズ スクイブ カンパニー | Ｊａｋ２阻害剤、ならびに骨髄増殖性疾患および癌の治療のためのそれらの使用 |
| CN105189488B (zh) * | 2013-02-27 | 2018-07-24 | 百时美施贵宝公司 | 用作溴区结构域抑制剂的咔唑化合物 |
| US9492460B2 (en) | 2013-02-27 | 2016-11-15 | Bristol-Myers Squibb Company | Carbazole compounds useful as bromodomain inhibitors |
| EP3016950B1 (en) * | 2013-07-02 | 2017-06-07 | Bristol-Myers Squibb Company | Tricyclic pyrido-carboxamide derivatives as rock inhibitors |
| US9914740B2 (en) * | 2013-07-02 | 2018-03-13 | Bristol-Myers Squibb Company | Tricyclic pyrido-carboxamide derivatives as rock inhibitors |
| GB201317363D0 (en) | 2013-10-01 | 2013-11-13 | Eisai Ltd | Novel compounds |
| ES2857848T3 (es) * | 2013-12-24 | 2021-09-29 | Bristol Myers Squibb Co | Compuestos tricíclicos como agentes antineoplásicos |
| US9458156B2 (en) | 2014-12-23 | 2016-10-04 | Bristol-Myers Squibb Company | Tricyclic compounds as anticancer agents |
| US20180022748A1 (en) * | 2015-02-02 | 2018-01-25 | Ucb Biopharma Sprl | 9h-pyrrolo-dipyridine derivatives |
| GB201512678D0 (en) * | 2015-07-20 | 2015-08-26 | Wista Lab Ltd | Methods of chemical synthesis |
| EP3365340B1 (en) | 2015-10-19 | 2022-08-10 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| US20170145025A1 (en) | 2015-11-19 | 2017-05-25 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| ES2916874T3 (es) | 2015-12-17 | 2022-07-06 | Incyte Corp | Derivados de N-fenil-piridina-2-carboxamida y su uso como moduladores de la interacción proteína/proteína PD-1/PD-L1 |
| AU2016379372A1 (en) | 2015-12-22 | 2018-08-02 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| ES2906460T3 (es) | 2016-05-06 | 2022-04-18 | Incyte Corp | Compuestos heterocíclicos como inmunomoduladores |
| ES2905980T3 (es) | 2016-05-26 | 2022-04-12 | Incyte Corp | Compuestos heterocíclicos como inmunomoduladores |
| BR112018076534A2 (pt) | 2016-06-20 | 2019-04-02 | Incyte Corporation | compostos heterocíclicos como imunomoduladores |
| KR102625861B1 (ko) * | 2016-06-28 | 2024-01-17 | 삼성디스플레이 주식회사 | 헤테로시클릭 화합물 및 이를 포함한 유기 발광 소자 |
| MA45669A (fr) | 2016-07-14 | 2019-05-22 | Incyte Corp | Composés hétérocycliques utilisés comme immunomodulateurs |
| ES2941716T3 (es) | 2016-08-29 | 2023-05-25 | Incyte Corp | Compuestos heterocíclicos como inmunomoduladores |
| ES2874756T3 (es) | 2016-12-22 | 2021-11-05 | Incyte Corp | Derivados de triazolo[1,5-A]piridina como inmunomoduladores |
| ES2899402T3 (es) | 2016-12-22 | 2022-03-11 | Incyte Corp | Derivados de piridina como inmunomoduladores |
| AU2017382870B2 (en) | 2016-12-22 | 2022-03-24 | Incyte Corporation | Benzooxazole derivatives as immunomodulators |
| WO2018119286A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Bicyclic heteroaromatic compounds as immunomodulators |
| CR20200520A (es) | 2018-03-30 | 2021-03-09 | Incyte Corp | Compuestos heterocíclicos como inmunomoduladores |
| WO2019217821A1 (en) | 2018-05-11 | 2019-11-14 | Incyte Corporation | Tetrahydro-imidazo[4,5-c]pyridine derivatives as pd-l1 immunomodulators |
| 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 |
| EP4010342A1 (en) | 2019-08-09 | 2022-06-15 | Incyte Corporation | Salts of a pd-1/pd-l1 inhibitor |
| CN114761013A (zh) | 2019-09-27 | 2022-07-15 | 迪斯克医药公司 | 治疗骨髓纤维化和相关病症的方法 |
| WO2021067217A1 (en) | 2019-09-30 | 2021-04-08 | Incyte Corporation | Pyrido[3,2-d]pyrimidine compounds as immunomodulators |
| 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 |
| BR112022009031A2 (pt) | 2019-11-11 | 2022-10-11 | Incyte Corp | Sais e formas cristalinas de um inibidor de pd-1/pd-l1 |
| US12129265B2 (en) | 2020-07-21 | 2024-10-29 | Ankh Life Sciences Limited | Therapeutic agents and uses thereof |
| US11780836B2 (en) | 2020-11-06 | 2023-10-10 | Incyte Corporation | Process of preparing a PD-1/PD-L1 inhibitor |
| US11866434B2 (en) | 2020-11-06 | 2024-01-09 | Incyte Corporation | Process for making a PD-1/PD-L1 inhibitor and salts and crystalline forms thereof |
| WO2022099075A1 (en) | 2020-11-06 | 2022-05-12 | Incyte Corporation | Crystalline form of a pd-1/pd-l1 inhibitor |
| 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 |
| EP4434968A4 (en) * | 2021-11-19 | 2025-10-22 | Nain Biotech Hangzhou Co Ltd | TETRAHYDROCARBAZOLE COMPOUND, PHARMACEUTICAL COMPOSITION AND USE THEREOF |
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 |
| WO2005067546A2 (en) * | 2004-01-13 | 2005-07-28 | Ambit Biosciences Corporation | Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases |
| TW200626142A (en) | 2004-09-21 | 2006-08-01 | Glaxo Group Ltd | Chemical compounds |
| NZ563687A (en) * | 2005-06-30 | 2011-07-29 | Smithkline Beecham Corp | 3-[1-(ethylsulfonyl)-4-piperidinyl]-5-[2-(1-methylethyl)-2,3-dihydro-1H-isoindol-5-yl]-1H-indole-7-carboxamide for inhibiting IKK2 (aka IKKbeta) |
| US8518964B2 (en) * | 2005-11-22 | 2013-08-27 | Merck Sharp & Dohme Corp. | Tricyclic compounds useful as inhibitors of kinases |
| US20080293802A1 (en) * | 2005-12-16 | 2008-11-27 | Smithline Beecham Corporation | Chemical Compounds |
-
2009
- 2009-12-17 US US13/140,184 patent/US8815840B2/en active Active
- 2009-12-17 JP JP2011542419A patent/JP5557849B2/ja not_active Expired - Fee Related
- 2009-12-17 CN CN200980157175.0A patent/CN102325752B/zh not_active Expired - Fee Related
- 2009-12-17 EP EP09793679.3A patent/EP2370407B1/en not_active Not-in-force
- 2009-12-17 ES ES09793679.3T patent/ES2490867T3/es active Active
- 2009-12-17 WO PCT/US2009/068394 patent/WO2010080474A1/en not_active Ceased
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