JP2016509583A5 - - Google Patents
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- Publication number
- JP2016509583A5 JP2016509583A5 JP2015549787A JP2015549787A JP2016509583A5 JP 2016509583 A5 JP2016509583 A5 JP 2016509583A5 JP 2015549787 A JP2015549787 A JP 2015549787A JP 2015549787 A JP2015549787 A JP 2015549787A JP 2016509583 A5 JP2016509583 A5 JP 2016509583A5
- Authority
- JP
- Japan
- Prior art keywords
- nhr
- alkyl
- nhc
- tautomer
- solvate
- 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
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- 125000000217 alkyl group Chemical group 0.000 claims 78
- -1 2-cyclopropylethynyl Chemical group 0.000 claims 50
- 239000012453 solvate Substances 0.000 claims 30
- 150000003839 salts Chemical class 0.000 claims 29
- 150000001875 compounds Chemical class 0.000 claims 26
- 229910052757 nitrogen Inorganic materials 0.000 claims 22
- 229910052736 halogen Inorganic materials 0.000 claims 17
- 150000002367 halogens Chemical class 0.000 claims 17
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 16
- 125000003545 alkoxy group Chemical group 0.000 claims 16
- 125000001072 heteroaryl group Chemical group 0.000 claims 15
- 125000003118 aryl group Chemical group 0.000 claims 11
- 229910052799 carbon Inorganic materials 0.000 claims 10
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 9
- 125000005842 heteroatom Chemical group 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 8
- 125000004429 atom Chemical group 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 7
- 125000001424 substituent group Chemical group 0.000 claims 7
- 125000000623 heterocyclic group Chemical group 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 239000000470 constituent Substances 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims 4
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 4
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 4
- 102000001253 Protein Kinase Human genes 0.000 claims 4
- 102000016971 Proto-Oncogene Proteins c-kit Human genes 0.000 claims 4
- 108010014608 Proto-Oncogene Proteins c-kit Proteins 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 108060006633 protein kinase Proteins 0.000 claims 4
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 3
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 claims 3
- RGSFGYAAUTVSQA-UHFFFAOYSA-N Cyclopentane Chemical compound C1CCCC1 RGSFGYAAUTVSQA-UHFFFAOYSA-N 0.000 claims 3
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 3
- DMEGYFMYUHOHGS-UHFFFAOYSA-N heptamethylene Natural products C1CCCCCC1 DMEGYFMYUHOHGS-UHFFFAOYSA-N 0.000 claims 3
- 125000006239 protecting group Chemical group 0.000 claims 3
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 2
- ZOXJGFHDIHLPTG-UHFFFAOYSA-N Boron Chemical group [B] ZOXJGFHDIHLPTG-UHFFFAOYSA-N 0.000 claims 2
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 claims 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 229910052796 boron Inorganic materials 0.000 claims 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- HGCIXCUEYOPUTN-UHFFFAOYSA-N cyclohexene Chemical compound C1CCC=CC1 HGCIXCUEYOPUTN-UHFFFAOYSA-N 0.000 claims 2
- LPIQUOYDBNQMRZ-UHFFFAOYSA-N cyclopentene Chemical compound C1CC=CC1 LPIQUOYDBNQMRZ-UHFFFAOYSA-N 0.000 claims 2
- 125000006255 cyclopropyl carbonyl group Chemical group [H]C1([H])C([H])([H])C1([H])C(*)=O 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([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
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 2
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 125000000355 1,3-benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000000586 2-(4-morpholinyl)ethoxy group Chemical group [H]C([H])(O*)C([H])([H])N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H] 0.000 claims 1
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims 1
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 1
- 125000001845 4 membered carbocyclic group Chemical group 0.000 claims 1
- WNWVKZTYMQWFHE-UHFFFAOYSA-N 4-ethylmorpholine Chemical group [CH2]CN1CCOCC1 WNWVKZTYMQWFHE-UHFFFAOYSA-N 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- 125000001054 5 membered carbocyclic group Chemical group 0.000 claims 1
- CWDWFSXUQODZGW-UHFFFAOYSA-N 5-thiazolyl Chemical group [C]1=CN=CS1 CWDWFSXUQODZGW-UHFFFAOYSA-N 0.000 claims 1
- 125000004008 6 membered carbocyclic group Chemical group 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 101100240519 Caenorhabditis elegans nhr-13 gene Proteins 0.000 claims 1
- PMPVIKIVABFJJI-UHFFFAOYSA-N Cyclobutane Chemical compound C1CCC1 PMPVIKIVABFJJI-UHFFFAOYSA-N 0.000 claims 1
- XDTMQSROBMDMFD-UHFFFAOYSA-N Cyclohexane Chemical compound C1CCCCC1 XDTMQSROBMDMFD-UHFFFAOYSA-N 0.000 claims 1
- 206010051066 Gastrointestinal stromal tumour Diseases 0.000 claims 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Natural products C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 claims 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims 1
- 230000001548 androgenic effect Effects 0.000 claims 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000006637 cyclobutyl carbonyl group Chemical group 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000004850 cyclobutylmethyl group Chemical group C1(CCC1)C* 0.000 claims 1
- 125000006639 cyclohexyl carbonyl group Chemical group 0.000 claims 1
- 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 1
- 125000004210 cyclohexylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- ICPMUWPXCAVOOQ-UHFFFAOYSA-N cycloocta-1,3,5-triene Chemical compound C1CC=CC=CC=C1 ICPMUWPXCAVOOQ-UHFFFAOYSA-N 0.000 claims 1
- WJTCGQSWYFHTAC-UHFFFAOYSA-N cyclooctane Chemical compound C1CCCCCCC1 WJTCGQSWYFHTAC-UHFFFAOYSA-N 0.000 claims 1
- 239000004914 cyclooctane Substances 0.000 claims 1
- 125000006638 cyclopentyl carbonyl group Chemical group 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000004851 cyclopentylmethyl group Chemical group C1(CCCC1)C* 0.000 claims 1
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims 1
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 125000004130 indan-2-yl group Chemical group [H]C1=C([H])C([H])=C2C(=C1[H])C([H])([H])C([H])(*)C2([H])[H] 0.000 claims 1
- 125000004498 isoxazol-4-yl group Chemical group O1N=CC(=C1)* 0.000 claims 1
- 208000008585 mastocytosis Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 1
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000004483 piperidin-3-yl group Chemical group N1CC(CCC1)* 0.000 claims 1
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 1
- 125000002206 pyridazin-3-yl group Chemical group [H]C1=C([H])C([H])=C(*)N=N1 0.000 claims 1
- 125000004940 pyridazin-4-yl group Chemical group N1=NC=C(C=C1)* 0.000 claims 1
- PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical compound C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 claims 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 1
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 1
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims 1
- 150000003254 radicals Chemical class 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 claims 1
- ITMCEJHCFYSIIV-UHFFFAOYSA-M triflate Chemical compound [O-]S(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-M 0.000 claims 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 1
- 229920002554 vinyl polymer Polymers 0.000 claims 1
- 0 *c1ccccc1 Chemical compound *c1ccccc1 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261745409P | 2012-12-21 | 2012-12-21 | |
| US61/745,409 | 2012-12-21 | ||
| US201361784928P | 2013-03-14 | 2013-03-14 | |
| US61/784,928 | 2013-03-14 | ||
| PCT/US2013/076995 WO2014100620A2 (en) | 2012-12-21 | 2013-12-20 | Compounds and methods for kinase modulation, and indications therefor |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018019358A Division JP2018109013A (ja) | 2012-12-21 | 2018-02-06 | キナーゼ調節のための化合物および方法、ならびにその適応 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016509583A JP2016509583A (ja) | 2016-03-31 |
| JP2016509583A5 true JP2016509583A5 (OSRAM) | 2017-02-09 |
| JP6385954B2 JP6385954B2 (ja) | 2018-09-05 |
Family
ID=50001255
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015549787A Active JP6385954B2 (ja) | 2012-12-21 | 2013-12-20 | キナーゼ調節のための化合物および方法、ならびにその適応 |
| JP2018019358A Withdrawn JP2018109013A (ja) | 2012-12-21 | 2018-02-06 | キナーゼ調節のための化合物および方法、ならびにその適応 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018019358A Withdrawn JP2018109013A (ja) | 2012-12-21 | 2018-02-06 | キナーゼ調節のための化合物および方法、ならびにその適応 |
Country Status (33)
| Country | Link |
|---|---|
| US (2) | US9676748B2 (OSRAM) |
| EP (1) | EP2935248B1 (OSRAM) |
| JP (2) | JP6385954B2 (OSRAM) |
| KR (1) | KR102212923B1 (OSRAM) |
| CN (1) | CN105308036B (OSRAM) |
| AR (1) | AR094263A1 (OSRAM) |
| AU (1) | AU2013361127B2 (OSRAM) |
| BR (1) | BR112015014752B1 (OSRAM) |
| CA (1) | CA2895239C (OSRAM) |
| CL (1) | CL2015001785A1 (OSRAM) |
| CY (1) | CY1120421T1 (OSRAM) |
| DK (1) | DK2935248T3 (OSRAM) |
| ES (1) | ES2664985T3 (OSRAM) |
| HR (1) | HRP20180499T1 (OSRAM) |
| HU (1) | HUE036739T2 (OSRAM) |
| IL (1) | IL239458B (OSRAM) |
| LT (1) | LT2935248T (OSRAM) |
| ME (1) | ME03000B (OSRAM) |
| MX (1) | MX365640B (OSRAM) |
| NZ (1) | NZ711896A (OSRAM) |
| PE (1) | PE20151280A1 (OSRAM) |
| PH (1) | PH12015501370A1 (OSRAM) |
| PL (1) | PL2935248T3 (OSRAM) |
| PT (1) | PT2935248T (OSRAM) |
| RS (1) | RS57117B1 (OSRAM) |
| RU (1) | RU2666146C2 (OSRAM) |
| SG (2) | SG11201504754QA (OSRAM) |
| SI (1) | SI2935248T1 (OSRAM) |
| SM (1) | SMT201800230T1 (OSRAM) |
| TW (1) | TWI617552B (OSRAM) |
| UY (1) | UY35240A (OSRAM) |
| WO (1) | WO2014100620A2 (OSRAM) |
| ZA (1) | ZA201504872B (OSRAM) |
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| PT1993360T (pt) | 2005-12-28 | 2017-05-25 | Vertex Pharma | Formas sólidas de n-[2,4-bis(1,1-dimetiletil)-5-hidroxifenil]-1,4-di-hidro-4-oxoquinolina-3-carboxamida |
| WO2008063888A2 (en) | 2006-11-22 | 2008-05-29 | Plexxikon, Inc. | Compounds modulating c-fms and/or c-kit activity and uses therefor |
| BRPI0814423B1 (pt) | 2007-07-17 | 2022-04-19 | Plexxikon, Inc | Compostos que modulam quinase e composição farmacêutica compreendendo os mesmos |
| WO2009143018A2 (en) | 2008-05-19 | 2009-11-26 | Plexxikon, Inc. | Compounds and methods for kinase modulation, and indications therefor |
| EP2501236B1 (en) | 2009-11-18 | 2017-03-29 | Plexxikon Inc. | N-[2-fluoro-3-(4-amino-7H-pyrrolo[2,3-d]pyrimidine-5-carbonyl)-phenyl]-4-benzenesulfonamide derivatives as Raf protein kinase modulators for the treatment of cancer |
| MX2012007429A (es) | 2009-12-23 | 2012-07-23 | Plexxikon Inc | Compuestos y metodos para la modulacion de quinasa e indicaciones de la misma. |
| TWI619713B (zh) | 2010-04-21 | 2018-04-01 | 普雷辛肯公司 | 用於激酶調節的化合物和方法及其適應症 |
| AU2012214762B2 (en) | 2011-02-07 | 2015-08-13 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| CA2836474A1 (en) | 2011-05-17 | 2012-11-22 | Plexxikon Inc. | Kinase modulation and indications therefor |
| US9358235B2 (en) | 2012-03-19 | 2016-06-07 | Plexxikon Inc. | Kinase modulation, and indications therefor |
| WO2014039714A2 (en) | 2012-09-06 | 2014-03-13 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| JP6284547B2 (ja) | 2012-12-21 | 2018-02-28 | アリオス バイオファーマ インク． | 置換ヌクレオシド、置換ヌクレオチドおよびそれらの類似体 |
| UA111305C2 (uk) | 2012-12-21 | 2016-04-11 | Пфайзер Інк. | Конденсовані лактами арилу та гетероарилу |
| BR112015014752B1 (pt) | 2012-12-21 | 2022-07-05 | Plexxikon, Inc | Compostos e seus uso para modulação de cinase |
| JP6294953B2 (ja) | 2013-03-14 | 2018-03-14 | ヤンセン ファーマシューティカ エヌ．ベー． | Ｐ２ｘ７調節物質 |
| ES2689526T3 (es) | 2013-03-14 | 2018-11-14 | Janssen Pharmaceutica Nv | Moduladores de P2X7 |
| TWI627174B (zh) | 2013-03-14 | 2018-06-21 | 比利時商健生藥品公司 | Ｐ２ｘ７調控劑 |
| DK2970283T3 (da) | 2013-03-14 | 2021-01-25 | Boehringer Ingelheim Int | Substituerede 2-aza-bicyclo[2.2.1]heptan-3-carboxylsyre-(benzyl-cyano-methyl)-amider som inhibitorer af cathepsin-c |
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| WO2014160521A1 (en) | 2013-03-15 | 2014-10-02 | Blueprint Medicines Corporation | Piperazine derivatives and their use as kit modulators |
| RU2680100C9 (ru) | 2013-03-15 | 2019-04-18 | Плексксикон Инк. | Гетероциклические соединения и их применения |
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| WO2015058129A1 (en) | 2013-10-17 | 2015-04-23 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
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