JP5584215B2 - ヘテロ環ｐｉｍキナーゼ阻害剤 - Google Patents
ヘテロ環ｐｉｍキナーゼ阻害剤 Download PDFInfo
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- JP5584215B2 JP5584215B2 JP2011524404A JP2011524404A JP5584215B2 JP 5584215 B2 JP5584215 B2 JP 5584215B2 JP 2011524404 A JP2011524404 A JP 2011524404A JP 2011524404 A JP2011524404 A JP 2011524404A JP 5584215 B2 JP5584215 B2 JP 5584215B2
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- amino
- cycloalkyl
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- alkyl
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- 125000000623 heterocyclic group Chemical group 0.000 title description 12
- 229940122016 Pim kinase inhibitor Drugs 0.000 title 1
- -1 hydroxy, nitro, amino, imino Chemical group 0.000 claims description 186
- 150000001875 compounds Chemical class 0.000 claims description 116
- 125000000217 alkyl group Chemical group 0.000 claims description 110
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 89
- 238000000034 method Methods 0.000 claims description 69
- 125000003545 alkoxy group Chemical group 0.000 claims description 55
- 229910052739 hydrogen Inorganic materials 0.000 claims description 51
- 239000001257 hydrogen Substances 0.000 claims description 51
- 125000003118 aryl group Chemical group 0.000 claims description 47
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 46
- OKKJLVBELUTLKV-UHFFFAOYSA-N methanol Natural products OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 41
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 41
- 125000001424 substituent group Chemical group 0.000 claims description 41
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 39
- 206010028980 Neoplasm Diseases 0.000 claims description 31
- 150000003839 salts Chemical class 0.000 claims description 31
- 125000001072 heteroaryl group Chemical group 0.000 claims description 30
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 28
- 125000003342 alkenyl group Chemical group 0.000 claims description 25
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims description 24
- 125000000304 alkynyl group Chemical group 0.000 claims description 22
- 201000011510 cancer Diseases 0.000 claims description 22
- 238000011282 treatment Methods 0.000 claims description 21
- 125000002252 acyl group Chemical group 0.000 claims description 20
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 19
- 230000000694 effects Effects 0.000 claims description 19
- 101000595531 Homo sapiens Serine/threonine-protein kinase pim-1 Proteins 0.000 claims description 18
- 102100036077 Serine/threonine-protein kinase pim-1 Human genes 0.000 claims description 18
- 125000004414 alkyl thio group Chemical group 0.000 claims description 18
- 239000003814 drug Substances 0.000 claims description 18
- 229920006395 saturated elastomer Polymers 0.000 claims description 18
- 125000003282 alkyl amino group Chemical group 0.000 claims description 16
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 16
- 125000004104 aryloxy group Chemical group 0.000 claims description 16
- 125000004432 carbon atom Chemical group C* 0.000 claims description 16
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 15
- 125000000000 cycloalkoxy group Chemical group 0.000 claims description 15
- 125000005844 heterocyclyloxy group Chemical group 0.000 claims description 15
- 125000004423 acyloxy group Chemical group 0.000 claims description 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 14
- 125000005553 heteroaryloxy group Chemical group 0.000 claims description 14
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 14
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 14
- 239000003795 chemical substances by application Substances 0.000 claims description 12
- 125000003441 thioacyl group Chemical group 0.000 claims description 12
- 150000003573 thiols Chemical class 0.000 claims description 12
- 108091000080 Phosphotransferase Proteins 0.000 claims description 11
- 229910052736 halogen Inorganic materials 0.000 claims description 11
- 150000002367 halogens Chemical class 0.000 claims description 11
- 102000020233 phosphotransferase Human genes 0.000 claims description 11
- 125000004442 acylamino group Chemical group 0.000 claims description 10
- AEOCXXJPGCBFJA-UHFFFAOYSA-N ethionamide Chemical compound CCC1=CC(C(N)=S)=CC=N1 AEOCXXJPGCBFJA-UHFFFAOYSA-N 0.000 claims description 10
- 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 description 9
- 125000003386 piperidinyl group Chemical group 0.000 claims description 9
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims description 8
- 125000001188 haloalkyl group Chemical group 0.000 claims description 8
- 230000010354 integration Effects 0.000 claims description 8
- YELDUWMYYRJMJD-UHFFFAOYSA-N 2-sulfamoylguanidine Chemical compound NC(N)=NS(N)(=O)=O YELDUWMYYRJMJD-UHFFFAOYSA-N 0.000 claims description 7
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims description 7
- 125000004103 aminoalkyl group Chemical group 0.000 claims description 7
- 125000005129 aryl carbonyl group Chemical group 0.000 claims description 7
- ZSIQJIWKELUFRJ-UHFFFAOYSA-N azepane Chemical compound C1CCCNCC1 ZSIQJIWKELUFRJ-UHFFFAOYSA-N 0.000 claims description 7
- 125000003739 carbamimidoyl group Chemical group C(N)(=N)* 0.000 claims description 7
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims description 7
- 125000005223 heteroarylcarbonyl group Chemical group 0.000 claims description 7
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 7
- 125000004193 piperazinyl group Chemical group 0.000 claims description 7
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims description 7
- 125000006448 cycloalkyl cycloalkyl group Chemical group 0.000 claims description 6
- ODHWZXUUXOFUQZ-WBVHZDCISA-N n-[4-[(3s,5r)-3-amino-5-methylpiperidin-1-yl]pyridin-3-yl]-2-(2,6-difluorophenyl)quinazolin-8-amine Chemical compound C1[C@H](C)C[C@H](N)CN1C1=CC=NC=C1NC1=CC=CC2=CN=C(C=3C(=CC=CC=3F)F)N=C12 ODHWZXUUXOFUQZ-WBVHZDCISA-N 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 6
- 125000005099 aryl alkyl carbonyl group Chemical group 0.000 claims description 5
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 5
- 239000003112 inhibitor Substances 0.000 claims description 5
- 230000001566 pro-viral effect Effects 0.000 claims description 5
- 229940124597 therapeutic agent Drugs 0.000 claims description 5
- WAISNUDWNYJNMT-DYESRHJHSA-N (3r,4r)-3-amino-1-[3-[[2-(2,6-difluorophenyl)quinazolin-8-yl]amino]pyridin-4-yl]piperidin-4-ol Chemical compound C1C[C@@H](O)[C@H](N)CN1C1=CC=NC=C1NC1=CC=CC2=CN=C(C=3C(=CC=CC=3F)F)N=C12 WAISNUDWNYJNMT-DYESRHJHSA-N 0.000 claims description 4
- WAISNUDWNYJNMT-UTKZUKDTSA-N (3r,4s)-3-amino-1-[3-[[2-(2,6-difluorophenyl)quinazolin-8-yl]amino]pyridin-4-yl]piperidin-4-ol Chemical compound C1C[C@H](O)[C@H](N)CN1C1=CC=NC=C1NC1=CC=CC2=CN=C(C=3C(=CC=CC=3F)F)N=C12 WAISNUDWNYJNMT-UTKZUKDTSA-N 0.000 claims description 4
- HXHFVYQPJRIKLE-DLBZAZTESA-N (3r,5s)-5-amino-1-[3-[[2-(2,6-difluorophenyl)quinolin-8-yl]amino]pyridin-4-yl]piperidin-3-ol Chemical compound C1[C@@H](N)C[C@@H](O)CN1C1=CC=NC=C1NC1=CC=CC2=CC=C(C=3C(=CC=CC=3F)F)N=C12 HXHFVYQPJRIKLE-DLBZAZTESA-N 0.000 claims description 4
- 239000004480 active ingredient Substances 0.000 claims description 4
- CJCNVDWBDYXQMZ-CRAIPNDOSA-N n-[4-[(3r,4r)-3-amino-4-fluoropiperidin-1-yl]pyridin-3-yl]-2-(2,6-difluorophenyl)quinazolin-8-amine Chemical compound C1C[C@@H](F)[C@H](N)CN1C1=CC=NC=C1NC1=CC=CC2=CN=C(C=3C(=CC=CC=3F)F)N=C12 CJCNVDWBDYXQMZ-CRAIPNDOSA-N 0.000 claims description 4
- ODHWZXUUXOFUQZ-DOTOQJQBSA-N n-[4-[(3r,5s)-3-amino-5-methylpiperidin-1-yl]pyridin-3-yl]-2-(2,6-difluorophenyl)quinazolin-8-amine Chemical compound C1[C@@H](C)C[C@@H](N)CN1C1=CC=NC=C1NC1=CC=CC2=CN=C(C=3C(=CC=CC=3F)F)N=C12 ODHWZXUUXOFUQZ-DOTOQJQBSA-N 0.000 claims description 4
- OAYLGJMFKMEJKI-HNNXBMFYSA-N n-[4-[(3s)-3-aminopiperidin-1-yl]pyridin-3-yl]-2-(1,3-thiazol-2-yl)quinazolin-8-amine Chemical compound C1[C@@H](N)CCCN1C1=CC=NC=C1NC1=CC=CC2=CN=C(C=3SC=CN=3)N=C12 OAYLGJMFKMEJKI-HNNXBMFYSA-N 0.000 claims description 4
- BMYXNSDMYMRNAW-INIZCTEOSA-N n-[4-[(3s)-3-aminopiperidin-1-yl]pyridin-3-yl]-2-(2,6-difluorophenyl)quinazolin-8-amine Chemical compound C1[C@@H](N)CCCN1C1=CC=NC=C1NC1=CC=CC2=CN=C(C=3C(=CC=CC=3F)F)N=C12 BMYXNSDMYMRNAW-INIZCTEOSA-N 0.000 claims description 4
- AJEKKBSRNRYYET-KRWDZBQOSA-N n-[4-[(3s)-3-aminopiperidin-1-yl]pyridin-3-yl]-2-(2-fluorophenyl)quinazolin-8-amine Chemical compound C1[C@@H](N)CCCN1C1=CC=NC=C1NC1=CC=CC2=CN=C(C=3C(=CC=CC=3)F)N=C12 AJEKKBSRNRYYET-KRWDZBQOSA-N 0.000 claims description 4
- JLQSMFNIARXKCU-RDJZCZTQSA-N n-[4-[(3s,5r)-3-amino-5-(fluoromethyl)piperidin-1-yl]pyridin-3-yl]-2-(2,6-difluorophenyl)quinazolin-8-amine Chemical compound C1[C@@H](N)C[C@@H](CF)CN1C1=CC=NC=C1NC1=CC=CC2=CN=C(C=3C(=CC=CC=3F)F)N=C12 JLQSMFNIARXKCU-RDJZCZTQSA-N 0.000 claims description 4
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 claims description 3
- 201000010099 disease Diseases 0.000 claims description 3
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims description 3
- 238000000338 in vitro Methods 0.000 claims description 3
- 230000002401 inhibitory effect Effects 0.000 claims description 3
- JZBBTWBWAAABLO-NRFANRHFSA-N n-[4-[(3s)-3-aminopiperidin-1-yl]pyridin-3-yl]-2-[3-(1,3-thiazol-2-yl)phenyl]quinazolin-8-amine Chemical compound C1[C@@H](N)CCCN1C1=CC=NC=C1NC1=CC=CC2=CN=C(C=3C=C(C=CC=3)C=3SC=CN=3)N=C12 JZBBTWBWAAABLO-NRFANRHFSA-N 0.000 claims description 3
- 230000036961 partial effect Effects 0.000 claims description 3
- HQICZWRMSXLUFU-UHFFFAOYSA-N 1-[3-[[2-(2,6-difluorophenyl)quinazolin-8-yl]amino]pyridin-4-yl]piperidine-3,5-diamine Chemical compound C1C(N)CC(N)CN1C1=CC=NC=C1NC1=CC=CC2=CN=C(C=3C(=CC=CC=3F)F)N=C12 HQICZWRMSXLUFU-UHFFFAOYSA-N 0.000 claims description 2
- WNRDIKVAZGENRX-UHFFFAOYSA-N n-[4-(3-aminoazepan-1-yl)pyridin-3-yl]-2-(2,6-difluorophenyl)quinazolin-8-amine Chemical compound C1C(N)CCCCN1C1=CC=NC=C1NC1=CC=CC2=CN=C(C=3C(=CC=CC=3F)F)N=C12 WNRDIKVAZGENRX-UHFFFAOYSA-N 0.000 claims description 2
- VWDOGNVHWKGFOS-UHFFFAOYSA-N n-[4-(3-aminocyclohexen-1-yl)pyridin-3-yl]-2-(2,6-difluorophenyl)quinazolin-8-amine Chemical compound NC1CCCC(C=2C(=CN=CC=2)NC=2C3=NC(=NC=C3C=CC=2)C=2C(=CC=CC=2F)F)=C1 VWDOGNVHWKGFOS-UHFFFAOYSA-N 0.000 claims description 2
- BMYXNSDMYMRNAW-MRXNPFEDSA-N n-[4-[(3r)-3-aminopiperidin-1-yl]pyridin-3-yl]-2-(2,6-difluorophenyl)quinazolin-8-amine Chemical compound C1[C@H](N)CCCN1C1=CC=NC=C1NC1=CC=CC2=CN=C(C=3C(=CC=CC=3F)F)N=C12 BMYXNSDMYMRNAW-MRXNPFEDSA-N 0.000 claims description 2
- XPBFQTIASOFUJQ-HNNXBMFYSA-N n-[4-[(3s)-3-aminopiperidin-1-yl]pyrimidin-5-yl]-2-(2,6-difluorophenyl)quinazolin-8-amine Chemical compound C1[C@@H](N)CCCN1C1=NC=NC=C1NC1=CC=CC2=CN=C(C=3C(=CC=CC=3F)F)N=C12 XPBFQTIASOFUJQ-HNNXBMFYSA-N 0.000 claims description 2
- CJCNVDWBDYXQMZ-YJBOKZPZSA-N n-[4-[(3s,4s)-3-amino-4-fluoropiperidin-1-yl]pyridin-3-yl]-2-(2,6-difluorophenyl)quinazolin-8-amine Chemical compound C1C[C@H](F)[C@@H](N)CN1C1=CC=NC=C1NC1=CC=CC2=CN=C(C=3C(=CC=CC=3F)F)N=C12 CJCNVDWBDYXQMZ-YJBOKZPZSA-N 0.000 claims description 2
- QEPUHWQDZRVJLO-ZWKOTPCHSA-N n-[4-[(3s,5r)-3-amino-5-ethoxypiperidin-1-yl]pyridin-3-yl]-2-(2,6-difluorophenyl)quinazolin-8-amine Chemical compound C1[C@H](OCC)C[C@H](N)CN1C1=CC=NC=C1NC1=CC=CC2=CN=C(C=3C(=CC=CC=3F)F)N=C12 QEPUHWQDZRVJLO-ZWKOTPCHSA-N 0.000 claims description 2
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Immunology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Transplantation (AREA)
- Pulmonology (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
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| HUE029236T2 (en) | 2007-06-13 | 2017-02-28 | Incyte Holdings Corp | (R) -3- (4- (7H-Pyrrolo [2,3-d] pyrimidin-4-yl) -1H-pyrazol-1-yl) -3-cyclopentylpropanenitrile Crystalline salts of Janus kinase inhibitor |
| MY156727A (en) | 2009-05-22 | 2016-03-15 | Incyte Corp | N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| EP2432472B1 (en) | 2009-05-22 | 2019-10-02 | Incyte Holdings Corporation | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors |
| TW201113285A (en) | 2009-09-01 | 2011-04-16 | Incyte Corp | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| EP3354652B1 (en) | 2010-03-10 | 2020-05-06 | Incyte Holdings Corporation | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| AR084691A1 (es) | 2010-05-21 | 2013-06-05 | Incyte Corp | Formulacion de uso topico para un inhibidor de jak y metodo para tratar trastorno de la piel |
| CA2818542A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| WO2012068440A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors |
| MY165963A (en) | 2011-06-20 | 2018-05-18 | Incyte Holdings Corp | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
| EP2734205B1 (en) | 2011-07-21 | 2018-03-21 | Tolero Pharmaceuticals, Inc. | Heterocyclic protein kinase inhibitors |
| TW201313721A (zh) | 2011-08-18 | 2013-04-01 | Incyte Corp | 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物 |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
| TW201406761A (zh) | 2012-05-18 | 2014-02-16 | Incyte Corp | 做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物 |
| TWI761825B (zh) | 2012-11-15 | 2022-04-21 | 美商英塞特控股公司 | 盧梭利替尼之緩釋性劑型 |
| EP2943485B1 (en) | 2013-01-14 | 2017-09-20 | Incyte Holdings Corporation | Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors |
| ME03780B (me) | 2013-01-15 | 2021-04-20 | Incyte Holdings Corp | Jedinjenja tiazolkarboksamida i piridinkarboksamida korisna kao inhibitori pim kinaze |
| MX384910B (es) | 2013-03-06 | 2025-03-14 | Incyte Holdings Corp | Procesos e intermedios para hacer un inhibidor de jak. |
| SG11201600815WA (en) | 2013-08-07 | 2016-03-30 | Incyte Corp | Sustained release dosage forms for a jak1 inhibitor |
| TW201605866A (zh) | 2013-08-23 | 2016-02-16 | 英塞特公司 | 可用作ｐｉｍ激酶抑制劑之呋喃并－及噻吩并－吡啶甲醯胺化合物 |
| WO2015184305A1 (en) | 2014-05-30 | 2015-12-03 | Incyte Corporation | TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1 |
| WO2016010897A1 (en) | 2014-07-14 | 2016-01-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors |
| US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| WO2016196244A1 (en) | 2015-05-29 | 2016-12-08 | Incyte Corporation | Pyridineamine compounds useful as pim kinase inhibitors |
| AR105967A1 (es) | 2015-09-09 | 2017-11-29 | Incyte Corp | Sales de un inhibidor de pim quinasa |
| WO2017059251A1 (en) | 2015-10-02 | 2017-04-06 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
| CN108373476B (zh) * | 2017-01-13 | 2021-06-01 | 成都地奥制药集团有限公司 | 一种激酶抑制剂及其制备和应用 |
| US10596161B2 (en) | 2017-12-08 | 2020-03-24 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| JP7393348B2 (ja) | 2018-01-30 | 2023-12-06 | インサイト・コーポレイション | （１－（３－フルオロ－２（トリフルオロメチル）イソニコチニル）ピぺリジン―４－オン）を作製するためのプロセス及び中間体 |
| CN113768934A (zh) | 2018-03-30 | 2021-12-10 | 因赛特公司 | 使用jak抑制剂治疗化脓性汗腺炎 |
| CA3095580A1 (en) | 2018-04-13 | 2019-10-17 | Sumitomo Dainippon Pharma Oncology, Inc. | Pim kinase inhibitors for treatment of myeloproliferative neoplasms and fibrosis associated with cancer |
| CN109369513B (zh) * | 2018-11-20 | 2020-08-25 | 都创(上海)医药科技有限公司 | 一种fbdd常用分子片段的制备方法 |
| CN111362922A (zh) * | 2018-12-26 | 2020-07-03 | 上海喆邺生物科技有限公司 | 2,4-二氨基嘧啶衍生物及其用途 |
| AU2020221247B2 (en) | 2019-02-12 | 2024-12-12 | Sumitomo Pharma America, Inc. | Formulations comprising heterocyclic protein kinase inhibitors |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| TW202237119A (zh) | 2020-12-10 | 2022-10-01 | 美商住友製藥腫瘤公司 | Ａｌｋ﹘５抑制劑和彼之用途 |
| JP2026509318A (ja) | 2022-10-31 | 2026-03-18 | スミトモ・ファーマ・アメリカ・インコーポレイテッド | 骨髄増殖性新生物を治療するためのｐｉｍ１阻害剤 |
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| ATE528302T1 (de) * | 2005-08-29 | 2011-10-15 | Vertex Pharma | 3,5-disubstituierte pyrid-2-one, die als hemmer der tec-familie von nicht-rezeptor tyrosin- kinasen nützlich sind |
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| WO2008153947A2 (en) * | 2007-06-07 | 2008-12-18 | Amgen Inc. | Heterocyclic compounds as raf kinase modulators |
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2009
- 2009-08-31 WO PCT/EP2009/061188 patent/WO2010026122A1/en not_active Ceased
- 2009-08-31 AU AU2009289317A patent/AU2009289317A1/en not_active Abandoned
- 2009-08-31 KR KR1020117007561A patent/KR20110056399A/ko not_active Withdrawn
- 2009-08-31 US US13/061,009 patent/US8759338B2/en not_active Expired - Fee Related
- 2009-08-31 MX MX2011002362A patent/MX2011002362A/es not_active Application Discontinuation
- 2009-08-31 JP JP2011524404A patent/JP5584215B2/ja not_active Expired - Fee Related
- 2009-08-31 EP EP09782379.3A patent/EP2344473B1/en not_active Not-in-force
- 2009-08-31 EA EA201100427A patent/EA201100427A1/ru unknown
- 2009-08-31 CA CA2735782A patent/CA2735782A1/en not_active Abandoned
- 2009-08-31 BR BRPI0918846A patent/BRPI0918846A2/pt not_active IP Right Cessation
- 2009-08-31 CN CN200980142961.3A patent/CN102197032B/zh not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| WO2010026122A1 (en) | 2010-03-11 |
| KR20110056399A (ko) | 2011-05-27 |
| AU2009289317A1 (en) | 2010-03-11 |
| CN102197032A (zh) | 2011-09-21 |
| EP2344473B1 (en) | 2014-04-16 |
| CA2735782A1 (en) | 2010-03-11 |
| US20110195956A1 (en) | 2011-08-11 |
| EA201100427A1 (ru) | 2011-10-31 |
| US8759338B2 (en) | 2014-06-24 |
| EP2344473A1 (en) | 2011-07-20 |
| JP2012501313A (ja) | 2012-01-19 |
| BRPI0918846A2 (pt) | 2019-09-24 |
| CN102197032B (zh) | 2014-07-23 |
| MX2011002362A (es) | 2011-04-04 |
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