JP2009523822A5 - - Google Patents
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- Publication number
- JP2009523822A5 JP2009523822A5 JP2008551474A JP2008551474A JP2009523822A5 JP 2009523822 A5 JP2009523822 A5 JP 2009523822A5 JP 2008551474 A JP2008551474 A JP 2008551474A JP 2008551474 A JP2008551474 A JP 2008551474A JP 2009523822 A5 JP2009523822 A5 JP 2009523822A5
- Authority
- JP
- Japan
- Prior art keywords
- ring
- compound
- formula
- aliphatic
- halo
- 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 63
- 125000001931 aliphatic group Chemical group 0.000 claims 29
- 239000000203 mixture Substances 0.000 claims 26
- 125000005843 halogen group Chemical group 0.000 claims 24
- 125000005842 heteroatom Chemical group 0.000 claims 15
- 229910052757 nitrogen Inorganic materials 0.000 claims 14
- 238000000034 method Methods 0.000 claims 13
- 229910052760 oxygen Inorganic materials 0.000 claims 13
- 229910052717 sulfur Inorganic materials 0.000 claims 13
- 239000003795 chemical substances by application Substances 0.000 claims 12
- 230000008878 coupling Effects 0.000 claims 9
- 238000010168 coupling process Methods 0.000 claims 9
- 238000005859 coupling reaction Methods 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 8
- 150000001334 alicyclic compounds Chemical class 0.000 claims 7
- 239000003814 drug Substances 0.000 claims 7
- 102000001253 Protein Kinase Human genes 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 238000006880 cross-coupling reaction Methods 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 108060006633 protein kinase Proteins 0.000 claims 6
- 229940124597 therapeutic agent Drugs 0.000 claims 6
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 239000013256 coordination polymer Substances 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 125000004429 atom Chemical group 0.000 claims 3
- 239000012472 biological sample Substances 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 3
- 230000002401 inhibitory effect Effects 0.000 claims 3
- 208000019838 Blood disease Diseases 0.000 claims 2
- 208000020084 Bone disease Diseases 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 108010025020 Nerve Growth Factor Proteins 0.000 claims 2
- 102000007072 Nerve Growth Factors Human genes 0.000 claims 2
- 102100031463 Serine/threonine-protein kinase PLK1 Human genes 0.000 claims 2
- 239000002260 anti-inflammatory agent Substances 0.000 claims 2
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 2
- 230000001028 anti-proliverative effect Effects 0.000 claims 2
- 239000003443 antiviral agent Substances 0.000 claims 2
- 230000015572 biosynthetic process Effects 0.000 claims 2
- 210000003169 central nervous system Anatomy 0.000 claims 2
- 238000010511 deprotection reaction Methods 0.000 claims 2
- 230000001066 destructive effect Effects 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 239000002552 dosage form Substances 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 208000014951 hematologic disease Diseases 0.000 claims 2
- 208000018706 hematopoietic system disease Diseases 0.000 claims 2
- 239000002955 immunomodulating agent Substances 0.000 claims 2
- 229940121354 immunomodulator Drugs 0.000 claims 2
- 230000002584 immunomodulator Effects 0.000 claims 2
- 229960003444 immunosuppressant agent Drugs 0.000 claims 2
- 239000003018 immunosuppressive agent Substances 0.000 claims 2
- 208000033065 inborn errors of immunity Diseases 0.000 claims 2
- 208000019423 liver disease Diseases 0.000 claims 2
- 239000003900 neurotrophic factor Substances 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 108010056274 polo-like kinase 1 Proteins 0.000 claims 2
- 239000002243 precursor Substances 0.000 claims 2
- 208000028529 primary immunodeficiency disease Diseases 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 208000037979 autoimmune inflammatory disease Diseases 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 210000003679 cervix uteri Anatomy 0.000 claims 1
- 230000000973 chemotherapeutic effect Effects 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 229940127089 cytotoxic agent Drugs 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 230000001861 immunosuppressant effect Effects 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 210000002429 large intestine Anatomy 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000011278 mitosis Effects 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 201000000050 myeloid neoplasm Diseases 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 230000000269 nucleophilic effect Effects 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
- 0 C*/C1=C\C=C\C(\CIOc2c(C(OC)=O)[s]c(*)c2)=C\C=C1 Chemical compound C*/C1=C\C=C\C(\CIOc2c(C(OC)=O)[s]c(*)c2)=C\C=C1 0.000 description 2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US76109706P | 2006-01-23 | 2006-01-23 | |
| US60/761,097 | 2006-01-23 | ||
| PCT/US2007/001726 WO2007087283A2 (en) | 2006-01-23 | 2007-01-23 | Thiophene-carboxamides useful as inhibitors of protein kinases |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012281195A Division JP2013056942A (ja) | 2006-01-23 | 2012-12-25 | プロテインキナーゼのインヒビターとして有用なチオフェン−カルボキサミド |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009523822A JP2009523822A (ja) | 2009-06-25 |
| JP2009523822A5 true JP2009523822A5 (enExample) | 2011-03-10 |
| JP5498703B2 JP5498703B2 (ja) | 2014-05-21 |
Family
ID=38179584
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008551474A Expired - Fee Related JP5498703B2 (ja) | 2006-01-23 | 2007-01-23 | プロテインキナーゼのインヒビターとして有用なチオフェン−カルボキサミド |
| JP2012281195A Pending JP2013056942A (ja) | 2006-01-23 | 2012-12-25 | プロテインキナーゼのインヒビターとして有用なチオフェン−カルボキサミド |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012281195A Pending JP2013056942A (ja) | 2006-01-23 | 2012-12-25 | プロテインキナーゼのインヒビターとして有用なチオフェン−カルボキサミド |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US7915305B2 (enExample) |
| EP (2) | EP2474546A1 (enExample) |
| JP (2) | JP5498703B2 (enExample) |
| CN (1) | CN101400678A (enExample) |
| AU (1) | AU2007208358A1 (enExample) |
| CA (1) | CA2637335A1 (enExample) |
| WO (1) | WO2007087283A2 (enExample) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR055616A1 (es) | 2005-09-06 | 2007-08-29 | Smithkline Beecham Corp | Compuestos de tiofeno bencimidazol |
| JP5498703B2 (ja) | 2006-01-23 | 2014-05-21 | バーテックス ファーマシューティカルズ インコーポレイテッド | プロテインキナーゼのインヒビターとして有用なチオフェン−カルボキサミド |
| EP2418210A1 (en) | 2006-04-13 | 2012-02-15 | Vertex Pharmceuticals Incorporated | Thiophene-carboxamides useful as inhibitors of protein kinases |
| WO2007139795A1 (en) | 2006-05-23 | 2007-12-06 | Vertex Pharmaceuticals Incorporated | Thiophene-carboxamides useful as inhibitors of protein kinases |
| JP2009538309A (ja) * | 2006-05-23 | 2009-11-05 | バーテックス ファーマシューティカルズ インコーポレイテッド | プロテインキナーゼのインヒビターとして有用なチオフェンカルボキサミド |
| JP2009539770A (ja) * | 2006-06-02 | 2009-11-19 | スミスクライン ビーチャム コーポレーション | Ｐｌｋに対する活性を有するベンゾイミダゾール置換チオフェン誘導体 |
| US7615643B2 (en) | 2006-06-02 | 2009-11-10 | Smithkline Beecham Corporation | Benzimidazole thiophene compounds |
| SG187396A1 (en) | 2007-07-19 | 2013-02-28 | Lundbeck & Co As H | 5-membered heterocyclic amides and related compounds |
| EP2320737B1 (en) * | 2008-08-05 | 2013-07-17 | Merck Sharp & Dohme Corp. | Pyrazolo-[1,5-a]-pyridines as mark inhibitors |
| JP5641664B2 (ja) | 2009-10-30 | 2014-12-17 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプＪａｎｓｓｅｎ Ｐｈａｒｍａｃｅｕｔｉｃａ Ｎａａｍｌｏｚｅ Ｖｅｎｎｏｏｔｓｃｈａｐ | イミダゾ［１，２−ｂ］ピリダジン誘導体およびＰＤＥ１０阻害剤としてのそれらの使用 |
| AR080754A1 (es) | 2010-03-09 | 2012-05-09 | Janssen Pharmaceutica Nv | Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10 |
| US8933070B2 (en) | 2010-07-02 | 2015-01-13 | University Health Network | Methods of targeting PTEN mutant diseases and compositions therefor |
| BR112013033375B1 (pt) | 2011-06-27 | 2022-05-10 | Janssen Pharmaceutica N.V | Derivados de 1-aril-4-metil-[1,2,4]triazolo[4,3-a]quinoxa-lina, seu uso, composição farmacêutica que os compreende, processo de preparação dos mesmos, solução estéril e composto intermediário |
| JO3407B1 (ar) | 2012-05-31 | 2019-10-20 | Eisai R&D Man Co Ltd | مركبات رباعي هيدرو بيرازولو بيريميدين |
| AU2013283426B2 (en) | 2012-06-26 | 2018-02-22 | Janssen Pharmaceutica Nv | Combinations comprising PDE 2 inhibitors such as 1-aryl-4-methyl- [1,2,4] triazolo [4,3-a] quinoxaline compounds and PDE 10 inhibitors for use in the treatment of neurological or metabolic disorders |
| WO2014009305A1 (en) | 2012-07-09 | 2014-01-16 | Janssen Pharmaceutica Nv | Inhibitors of phosphodiesterase 10 enzyme |
| CN108135916B (zh) * | 2015-06-19 | 2022-01-28 | 北京科辉智药生物科技有限责任公司 | 手性特异性含硼化合物及其在治疗癌症或淀粉样变性中的应用 |
| WO2018081719A1 (en) * | 2016-10-31 | 2018-05-03 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Small molecule inhibitors of nek2 and uses thereof |
| BR112022024729A2 (pt) | 2020-06-05 | 2023-02-28 | Kinnate Biopharma Inc | Inibidores de quinases do receptor do fator de crescimento de fibroblastos |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1255802B (it) | 1992-08-07 | 1995-11-16 | Luso Farmaco Inst | Derivati imidazolici ad attivita' a ii antagonista |
| CA2230896A1 (en) | 1995-09-01 | 1997-03-13 | Signal Pharmaceuticals, Inc. | Pyrimidine carboxylates and related compounds and methods for treating inflammatory conditions |
| BR9804865B1 (pt) | 1997-04-24 | 2011-08-23 | pesticida 3-(fenil substituìdo)-5-(tienil ou furil)-1,2,4-triazóis, composição para controlar insetos ou ácaros, bem como processo para controlar insetos, ácaros, moscas brancas e afìdios, para proteger plantas de afìdios, ácaros ou insetos. | |
| DE19744026A1 (de) | 1997-10-06 | 1999-04-08 | Hoechst Marion Roussel De Gmbh | Pyrazol-Derivate, ihre Herstellung und ihre Verwendung in Arzneimitteln |
| PT957099E (pt) | 1998-04-15 | 2003-02-28 | Pfizer Prod Inc | Carboxamidas heterociclicas |
| JP4610740B2 (ja) | 1998-10-23 | 2011-01-12 | ダウ・アグロサイエンス・エル・エル・シー | ３−（置換フェニル）−５−チエニル又はフリル）−１，２，４−トリアゾールの製造法及びそこで用いられる新規な中間体 |
| WO2001064646A2 (en) | 2000-03-01 | 2001-09-07 | Tularik Inc. | Hydrazones and analogs as cholesterol lowering agents |
| US7273868B2 (en) | 2000-04-28 | 2007-09-25 | Tanabe Seiyaku Co., Ltd. | Pyrazine derivatives |
| KR20040004705A (ko) | 2001-06-08 | 2004-01-13 | 시토비아 인크. | 카스파제의 활성제 및 아폽토시스의 유도제로서의 치환된3-아릴-5-아릴-[1,2,4]-옥사디아졸과 유사체 및 이의 용도 |
| WO2003037886A2 (en) | 2001-10-30 | 2003-05-08 | Pharmacia Corporation | Heteroaromatic carboxamide derivatives for the treatment of inflammation |
| US7064204B2 (en) | 2002-05-30 | 2006-06-20 | King Pharmacueticals Reserch And Development, Inc. | Pharmaceutically active compounds having a tricyclic pyrazolotriazolopyrimidine ring structure and methods of use |
| BR0313160A (pt) * | 2002-08-08 | 2005-07-12 | Smithkline Beecham Corp | Composto, composição farmacêutica, métodos para tratar uma condição e um neoplasmo suscetìvel em um animal em um animal, processo para preparar um composto e uso de um composto |
| US7144876B2 (en) | 2002-12-18 | 2006-12-05 | Cytovia, Inc. | 3,5-Disubstituted-[1,2,4]-oxadiazoles and analogs as activators of caspases and inducers of apoptosis and the use thereof |
| ES2326808T3 (es) * | 2003-04-01 | 2009-10-20 | Smithkline Beecham Corporation | Compuestos de imidazotriazina para el tratamiento de enfermedades cancerosas. |
| US20050090529A1 (en) | 2003-07-31 | 2005-04-28 | Pfizer Inc | 3,5 Disubstituted indazole compounds with nitrogen-bearing 5-membered heterocycles, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation |
| WO2005037827A1 (en) | 2003-10-16 | 2005-04-28 | Smithkline Beecham Corporation | Process for preparing benzimidazole thiophenes |
| EP1708697A4 (en) | 2004-01-30 | 2007-11-28 | Smithkline Beecham Corp | CHEMICAL COMPOUNDS |
| GB0402809D0 (en) | 2004-02-09 | 2004-03-10 | Glaxo Group Ltd | Chemical compounds |
| RU2006138036A (ru) | 2004-03-30 | 2008-05-10 | Чирон Корпорейшн (Us) | Производные замещенного тиофена в качестве противораковых средств |
| TW200604168A (en) | 2004-04-02 | 2006-02-01 | Vertex Pharma | Azaindoles useful as inhibitors of rock and other protein kinases |
| JP4935357B2 (ja) | 2004-11-08 | 2012-05-23 | Ｍｓｄ株式会社 | 新規縮環イミダゾール誘導体 |
| WO2006066172A1 (en) | 2004-12-17 | 2006-06-22 | Amgen, Inc. | Aminopyrimidine compounds and methods of use |
| EP1924572B1 (en) * | 2005-09-06 | 2009-12-30 | SmithKline Beecham Corporation | Regioselective process for preparing benzimidazole thiophenes |
| JP5498703B2 (ja) | 2006-01-23 | 2014-05-21 | バーテックス ファーマシューティカルズ インコーポレイテッド | プロテインキナーゼのインヒビターとして有用なチオフェン−カルボキサミド |
| EP2418210A1 (en) | 2006-04-13 | 2012-02-15 | Vertex Pharmceuticals Incorporated | Thiophene-carboxamides useful as inhibitors of protein kinases |
| JP2009538309A (ja) | 2006-05-23 | 2009-11-05 | バーテックス ファーマシューティカルズ インコーポレイテッド | プロテインキナーゼのインヒビターとして有用なチオフェンカルボキサミド |
| WO2007139795A1 (en) | 2006-05-23 | 2007-12-06 | Vertex Pharmaceuticals Incorporated | Thiophene-carboxamides useful as inhibitors of protein kinases |
-
2007
- 2007-01-23 JP JP2008551474A patent/JP5498703B2/ja not_active Expired - Fee Related
- 2007-01-23 EP EP11181807A patent/EP2474546A1/en not_active Withdrawn
- 2007-01-23 CA CA002637335A patent/CA2637335A1/en not_active Abandoned
- 2007-01-23 AU AU2007208358A patent/AU2007208358A1/en not_active Abandoned
- 2007-01-23 CN CNA2007800088133A patent/CN101400678A/zh active Pending
- 2007-01-23 EP EP07762463A patent/EP1989205B1/en not_active Not-in-force
- 2007-01-23 US US11/656,876 patent/US7915305B2/en not_active Expired - Fee Related
- 2007-01-23 WO PCT/US2007/001726 patent/WO2007087283A2/en not_active Ceased
-
2011
- 2011-02-24 US US13/033,872 patent/US8399478B2/en not_active Expired - Fee Related
-
2012
- 2012-12-25 JP JP2012281195A patent/JP2013056942A/ja active Pending
-
2013
- 2013-02-15 US US13/768,119 patent/US8759389B1/en not_active Expired - Fee Related
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