JP2010522210A5 - - Google Patents
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- Publication number
- JP2010522210A5 JP2010522210A5 JP2009554762A JP2009554762A JP2010522210A5 JP 2010522210 A5 JP2010522210 A5 JP 2010522210A5 JP 2009554762 A JP2009554762 A JP 2009554762A JP 2009554762 A JP2009554762 A JP 2009554762A JP 2010522210 A5 JP2010522210 A5 JP 2010522210A5
- Authority
- JP
- Japan
- Prior art keywords
- aliphatic
- optionally substituted
- compound according
- ring
- compound
- 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
- 150000001875 compounds Chemical class 0.000 claims description 146
- 125000001931 aliphatic group Chemical group 0.000 claims description 113
- 229910052736 halogen Inorganic materials 0.000 claims description 58
- 150000002367 halogens Chemical class 0.000 claims description 54
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 48
- 125000000623 heterocyclic group Chemical group 0.000 claims description 44
- 229920006395 saturated elastomer Polymers 0.000 claims description 44
- 229910052799 carbon Inorganic materials 0.000 claims description 35
- 229910052757 nitrogen Inorganic materials 0.000 claims description 31
- -1 COOR ′ Chemical group 0.000 claims description 30
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 30
- 125000001424 substituent group Chemical group 0.000 claims description 29
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 27
- 125000003118 aryl group Chemical group 0.000 claims description 26
- 125000005843 halogen group Chemical group 0.000 claims description 26
- 229910052739 hydrogen Inorganic materials 0.000 claims description 26
- 125000001072 heteroaryl group Chemical group 0.000 claims description 25
- 125000004429 atom Chemical group 0.000 claims description 22
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 22
- 229910052717 sulfur Chemical group 0.000 claims description 21
- 125000005842 heteroatom Chemical group 0.000 claims description 19
- 239000003814 drug Substances 0.000 claims description 18
- 239000000203 mixture Substances 0.000 claims description 18
- 125000002723 alicyclic group Chemical group 0.000 claims description 16
- 201000010099 disease Diseases 0.000 claims description 16
- 229910052760 oxygen Inorganic materials 0.000 claims description 16
- 208000035475 disorder Diseases 0.000 claims description 14
- 125000000217 alkyl group Chemical group 0.000 claims description 12
- 239000003795 chemical substances by application Substances 0.000 claims description 12
- 229940079593 drug Drugs 0.000 claims description 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 12
- 238000000034 method Methods 0.000 claims description 10
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 9
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 9
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 9
- 239000001301 oxygen Chemical group 0.000 claims description 9
- 239000011593 sulfur Chemical group 0.000 claims description 9
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 7
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims description 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 6
- 206010012601 diabetes mellitus Diseases 0.000 claims description 6
- 239000001257 hydrogen Substances 0.000 claims description 6
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims description 6
- 229940124597 therapeutic agent Drugs 0.000 claims description 6
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 4
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 4
- 108010025020 Nerve Growth Factor Proteins 0.000 claims description 4
- 102000007072 Nerve Growth Factors Human genes 0.000 claims description 4
- 201000004681 Psoriasis Diseases 0.000 claims description 4
- 206010052779 Transplant rejections Diseases 0.000 claims description 4
- 229940124599 anti-inflammatory drug Drugs 0.000 claims description 4
- 230000001028 anti-proliverative effect Effects 0.000 claims description 4
- 208000006673 asthma Diseases 0.000 claims description 4
- 239000012472 biological sample Substances 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 4
- 230000000694 effects Effects 0.000 claims description 4
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 4
- 125000001188 haloalkyl group Chemical group 0.000 claims description 4
- 239000002955 immunomodulating agent Substances 0.000 claims description 4
- 229940121354 immunomodulator Drugs 0.000 claims description 4
- 229960003444 immunosuppressant agent Drugs 0.000 claims description 4
- 239000003018 immunosuppressive agent Substances 0.000 claims description 4
- 208000033065 inborn errors of immunity Diseases 0.000 claims description 4
- 230000002401 inhibitory effect Effects 0.000 claims description 4
- 201000006417 multiple sclerosis Diseases 0.000 claims description 4
- 239000003900 neurotrophic factor Substances 0.000 claims description 4
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 4
- 208000028529 primary immunodeficiency disease Diseases 0.000 claims description 4
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 4
- 230000001404 mediated effect Effects 0.000 claims description 3
- 206010065040 AIDS dementia complex Diseases 0.000 claims description 2
- 201000004384 Alopecia Diseases 0.000 claims description 2
- 208000024827 Alzheimer disease Diseases 0.000 claims description 2
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims description 2
- 208000023275 Autoimmune disease Diseases 0.000 claims description 2
- 208000019838 Blood disease Diseases 0.000 claims description 2
- 208000020084 Bone disease Diseases 0.000 claims description 2
- 208000020446 Cardiac disease Diseases 0.000 claims description 2
- 208000009329 Graft vs Host Disease Diseases 0.000 claims description 2
- 208000023105 Huntington disease Diseases 0.000 claims description 2
- 206010020751 Hypersensitivity Diseases 0.000 claims description 2
- 206010020880 Hypertrophy Diseases 0.000 claims description 2
- 206010025323 Lymphomas Diseases 0.000 claims description 2
- 208000014767 Myeloproliferative disease Diseases 0.000 claims description 2
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims description 2
- 208000018737 Parkinson disease Diseases 0.000 claims description 2
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims description 2
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims description 2
- 208000006011 Stroke Diseases 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 230000000172 allergic effect Effects 0.000 claims description 2
- 208000030961 allergic reaction Diseases 0.000 claims description 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 2
- 239000003443 antiviral agent Substances 0.000 claims description 2
- 208000010216 atopic IgE responsiveness Diseases 0.000 claims description 2
- 239000008280 blood Substances 0.000 claims description 2
- 210000004369 blood Anatomy 0.000 claims description 2
- 125000002837 carbocyclic group Chemical group 0.000 claims description 2
- 125000004432 carbon atom Chemical group C* 0.000 claims description 2
- 210000004413 cardiac myocyte Anatomy 0.000 claims description 2
- 230000000973 chemotherapeutic effect Effects 0.000 claims description 2
- 238000002512 chemotherapy Methods 0.000 claims description 2
- 230000001066 destructive effect Effects 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 208000024908 graft versus host disease Diseases 0.000 claims description 2
- 208000024963 hair loss Diseases 0.000 claims description 2
- 230000003676 hair loss Effects 0.000 claims description 2
- 208000019622 heart disease Diseases 0.000 claims description 2
- 208000014951 hematologic disease Diseases 0.000 claims description 2
- 208000018706 hematopoietic system disease Diseases 0.000 claims description 2
- 208000027866 inflammatory disease Diseases 0.000 claims description 2
- 208000028867 ischemia Diseases 0.000 claims description 2
- 208000032839 leukemia Diseases 0.000 claims description 2
- 208000019423 liver disease Diseases 0.000 claims description 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 2
- 210000000056 organ Anatomy 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 230000002062 proliferating effect Effects 0.000 claims description 2
- 230000010410 reperfusion Effects 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- 201000000980 schizophrenia Diseases 0.000 claims description 2
- 239000007787 solid Substances 0.000 claims description 2
- 238000002054 transplantation Methods 0.000 claims description 2
- 239000003981 vehicle Substances 0.000 claims description 2
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 5
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 4
- 125000006592 (C2-C3) alkenyl group Chemical group 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 10
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 10
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 8
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 description 4
- 125000004043 oxo group Chemical group O=* 0.000 description 4
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 description 2
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 description 2
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 description 2
- 125000004122 cyclic group Chemical group 0.000 description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 2
- XSXHWVKGUXMUQE-UHFFFAOYSA-N osmium dioxide Inorganic materials O=[Os]=O XSXHWVKGUXMUQE-UHFFFAOYSA-N 0.000 description 2
- 102000015617 Janus Kinases Human genes 0.000 description 1
- 108010024121 Janus Kinases Proteins 0.000 description 1
- 108091000080 Phosphotransferase Proteins 0.000 description 1
- 125000003342 alkenyl group Chemical group 0.000 description 1
- 238000010835 comparative analysis Methods 0.000 description 1
- UHCBBWUQDAVSMS-UHFFFAOYSA-N fluoroethane Chemical compound CCF UHCBBWUQDAVSMS-UHFFFAOYSA-N 0.000 description 1
- 230000031146 intracellular signal transduction Effects 0.000 description 1
- 229940043355 kinase inhibitor Drugs 0.000 description 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 102000020233 phosphotransferase Human genes 0.000 description 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 description 1
- 125000003107 substituted aryl group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91946907P | 2007-03-22 | 2007-03-22 | |
| US60/919,469 | 2007-03-22 | ||
| PCT/US2008/057797 WO2008116139A2 (en) | 2007-03-22 | 2008-03-21 | N-heterocyclic compounds useful as inhibitors of janus kinases |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013228193A Division JP2014024867A (ja) | 2007-03-22 | 2013-11-01 | Ｊａｋ阻害薬として有用なｎ−複素環式化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010522210A JP2010522210A (ja) | 2010-07-01 |
| JP2010522210A5 true JP2010522210A5 (https=) | 2013-12-19 |
| JP5642973B2 JP5642973B2 (ja) | 2014-12-17 |
Family
ID=39730636
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009554762A Expired - Fee Related JP5642973B2 (ja) | 2007-03-22 | 2008-03-21 | Ｊａｋ阻害薬として有用なｎ−複素環式化合物 |
| JP2013228193A Withdrawn JP2014024867A (ja) | 2007-03-22 | 2013-11-01 | Ｊａｋ阻害薬として有用なｎ−複素環式化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013228193A Withdrawn JP2014024867A (ja) | 2007-03-22 | 2013-11-01 | Ｊａｋ阻害薬として有用なｎ−複素環式化合物 |
Country Status (10)
| Country | Link |
|---|---|
| US (3) | US20100160287A1 (https=) |
| EP (1) | EP2144878A2 (https=) |
| JP (2) | JP5642973B2 (https=) |
| KR (1) | KR20090129488A (https=) |
| CN (1) | CN101778825A (https=) |
| AU (1) | AU2008228768A1 (https=) |
| CA (1) | CA2681516A1 (https=) |
| IL (1) | IL201064A0 (https=) |
| MX (1) | MX2009010127A (https=) |
| WO (1) | WO2008116139A2 (https=) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2672172T3 (es) * | 2006-12-29 | 2018-06-12 | Rigel Pharmaceuticals, Inc. | Triazoles N3-heteroarilsustituidos y triazoles N5-heteroarilsustituidos útiles como inhibidores de Axl |
| TW201100441A (en) | 2009-06-01 | 2011-01-01 | Osi Pharm Inc | Amino pyrimidine anticancer compounds |
| CA2767091A1 (en) * | 2009-07-15 | 2011-01-20 | Abbott Laboratories | Pyrrolopyrazine inhibitors of kinases |
| AU2010339531A1 (en) | 2009-12-30 | 2012-08-23 | Arqule, Inc. | Substituted naphthalenyl-pyrimidine compounds |
| JP2013147428A (ja) * | 2010-04-27 | 2013-08-01 | Dainippon Sumitomo Pharma Co Ltd | 新規２−ヘテロアリール単環ピリミジン誘導体 |
| WO2012030948A1 (en) | 2010-09-01 | 2012-03-08 | Ambit Biosciences Corporation | Quinazoline compounds and methods of use thereof |
| US9133224B2 (en) | 2010-11-29 | 2015-09-15 | OSI Pharmaceuticals, LLC | Macrocyclic kinase inhibitors |
| CA2819373A1 (en) * | 2010-12-09 | 2012-06-14 | Amgen Inc. | Bicyclic compounds as pim inhibitors |
| EP2688886A1 (en) | 2011-03-22 | 2014-01-29 | Amgen Inc. | Azole compounds as pim inhibitors |
| JP6116554B2 (ja) | 2011-07-07 | 2017-04-19 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ | がんの処置のための置換されたアザ複素環 |
| EP4556010A3 (en) | 2011-11-30 | 2025-07-23 | Emory University | Jak inhibitors for use in the prevention or treatment of a viral disease caused by a coronaviridae |
| WO2014126954A1 (en) * | 2013-02-13 | 2014-08-21 | OSI Pharmaceuticals, LLC | Regioselective synthesis of substituted pyrimidines |
| US20220143049A1 (en) | 2019-03-21 | 2022-05-12 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| 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 |
| EP4054579A1 (en) | 2019-11-08 | 2022-09-14 | Institut National de la Santé et de la Recherche Médicale (INSERM) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| WO2021231798A1 (en) | 2020-05-13 | 2021-11-18 | Disc Medicine, Inc. | Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3867386A (en) * | 1969-11-04 | 1975-02-18 | American Home Prod | 5-amino-2,6-substituted-7h-pyrrolo(2,3-d)pyrimidines and related compounds |
| US3631036A (en) * | 1969-11-04 | 1971-12-28 | American Home Prod | 5-amino-2 6-substituted-7h-pyrrolo(2 3-d) pyrimidines and related compounds |
| IL117659A (en) * | 1995-04-13 | 2000-12-06 | Dainippon Pharmaceutical Co | Substituted 2-phenyl pyrimidino amino acetamide derivative process for preparing the same and a pharmaceutical composition containing same |
| ZA977427B (en) * | 1996-09-04 | 1998-03-02 | Dainippon Pharmaceutical Co | 2,4-disubstituted pyrimidine derivative, process for preparing the same, and a pharmaceutical composition containing the same. |
| JP2003146987A (ja) * | 1999-05-31 | 2003-05-21 | Dainippon Pharmaceut Co Ltd | ２−アリールプリン−９−アセトアミド誘導体 |
| US7037916B2 (en) * | 1999-07-15 | 2006-05-02 | Pharmacopeia Drug Discovery, Inc. | Pyrimidine derivatives as IL-8 receptor antagonists |
| ATE250053T1 (de) * | 1999-07-15 | 2003-10-15 | Pharmacopeia Inc | Bradikinin b1 rezeptor antagonisten |
| AU2003237121A1 (en) * | 2002-04-26 | 2003-11-10 | Vertex Pharmaceuticals Incorporated | Pyrrole derivatives as inhibitors of erk2 and uses thereof |
| CL2003002353A1 (es) * | 2002-11-15 | 2005-02-04 | Vertex Pharma | Compuestos derivados de diaminotriazoles, inhibidores d ela proteina quinasa; composicion farmaceutica; procedimiento de preparacion; y su uso del compuesto en el tratamiento de enfermedades de desordenes alergicos, proliferacion, autoinmunes, condic |
| WO2004069829A1 (en) * | 2003-01-10 | 2004-08-19 | Pharmacopeia Drug Discovery, Inc. | (2s)-2-((pyrimidin-4-yl)amino)-4-methylpentanoic acid aminoethylamid derivatives as il-8 receptor modulators for the treatment of atherosclerosis and rheumatoid arthritis |
| CL2004000409A1 (es) * | 2003-03-03 | 2005-01-07 | Vertex Pharma | Compuestos derivados de 2-(cilo sustituido)-1-(amino u oxi sustituido)-quinazolina, inhibidores de canales ionicos de sodio y calcio dependientes de voltaje; composicion farmaceutica; y uso del compuesto en el tratamiento de dolor agudo, cronico, neu |
| TWI372624B (en) * | 2004-03-30 | 2012-09-21 | Vertex Pharma | Azaindoles useful as inhibitors of jak and other protein kinases |
| ATE482213T1 (de) * | 2004-11-04 | 2010-10-15 | Vertex Pharma | Als inhibitoren von proteinkinasen geeignete pyrazoloä1,5-aüpyrimidine |
| EP1814883A1 (en) * | 2004-11-22 | 2007-08-08 | Vertex Pharmaceuticals Incorporated | Bicyclic inhibitors or rho kinase |
| CA2591413A1 (en) * | 2004-12-16 | 2006-06-22 | Vertex Pharmaceuticals Incorporated | Pyrid-2-ones useful as inhibitors of tec family protein kinases for the treatment of inflammatory, proliferative and immunologically-mediated diseases |
| WO2006127587A1 (en) * | 2005-05-20 | 2006-11-30 | Vertex Pharmaceuticals Incorporated | Pyrrolopyridines useful as inhibitors of protein kinase |
| ZA200802685B (en) * | 2005-09-30 | 2009-10-28 | Vertex Pharma | Deazapurines useful as inhibitors of janus kinases |
| CN102532133A (zh) * | 2006-01-17 | 2012-07-04 | 沃泰克斯药物股份有限公司 | 适用作詹纳斯激酶抑制剂的吖吲哚类 |
| WO2007125331A2 (en) | 2006-04-26 | 2007-11-08 | Cancer Research Technology Limited | Amino-ethyl-amino-aryl (aeaa) compounds and their use |
| AU2007338754A1 (en) * | 2006-12-21 | 2008-07-03 | Vertex Pharmaceuticals Incorporated | 5-cyan0-4- (pyrrolo [2, 3B] pyridine-3-yl) -pyrimidine derivatives useful as protein kinase inhibitors |
-
2008
- 2008-03-21 CN CN200880014699A patent/CN101778825A/zh active Pending
- 2008-03-21 JP JP2009554762A patent/JP5642973B2/ja not_active Expired - Fee Related
- 2008-03-21 KR KR1020097022156A patent/KR20090129488A/ko not_active Withdrawn
- 2008-03-21 EP EP08744172A patent/EP2144878A2/en not_active Withdrawn
- 2008-03-21 AU AU2008228768A patent/AU2008228768A1/en not_active Abandoned
- 2008-03-21 CA CA002681516A patent/CA2681516A1/en not_active Abandoned
- 2008-03-21 WO PCT/US2008/057797 patent/WO2008116139A2/en not_active Ceased
- 2008-03-21 MX MX2009010127A patent/MX2009010127A/es not_active Application Discontinuation
-
2009
- 2009-09-21 IL IL201064A patent/IL201064A0/en unknown
- 2009-09-22 US US12/564,156 patent/US20100160287A1/en not_active Abandoned
-
2011
- 2011-10-25 US US13/280,670 patent/US8686143B2/en not_active Expired - Fee Related
-
2013
- 2013-11-01 JP JP2013228193A patent/JP2014024867A/ja not_active Withdrawn
-
2014
- 2014-02-05 US US14/172,963 patent/US20140221336A1/en not_active Abandoned
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