JP2009532375A5 - - Google Patents
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- Publication number
- JP2009532375A5 JP2009532375A5 JP2009503222A JP2009503222A JP2009532375A5 JP 2009532375 A5 JP2009532375 A5 JP 2009532375A5 JP 2009503222 A JP2009503222 A JP 2009503222A JP 2009503222 A JP2009503222 A JP 2009503222A JP 2009532375 A5 JP2009532375 A5 JP 2009532375A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- substituted
- hetero
- heteroaryl
- 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.)
- Withdrawn
Links
- 125000000217 alkyl group Chemical group 0.000 claims 32
- -1 Cyano, thio, hydroxy Chemical group 0.000 claims 21
- 150000001875 compounds Chemical class 0.000 claims 20
- 125000005842 heteroatom Chemical group 0.000 claims 19
- 125000000753 cycloalkyl group Chemical group 0.000 claims 14
- 125000001072 heteroaryl group Chemical group 0.000 claims 12
- 150000001602 bicycloalkyls Chemical group 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 9
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 9
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims 8
- 125000003545 alkoxy group 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
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 6
- 125000004104 aryloxy group Chemical group 0.000 claims 5
- 125000001424 substituent group Chemical group 0.000 claims 5
- 108091000080 Phosphotransferase Proteins 0.000 claims 4
- 125000003282 alkyl amino group Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 4
- 102000020233 phosphotransferase Human genes 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 4
- 125000002813 thiocarbonyl group Chemical group *C(*)=S 0.000 claims 4
- 125000001841 imino group Chemical group [H]N=* 0.000 claims 3
- 229940124530 sulfonamide Drugs 0.000 claims 3
- 150000003456 sulfonamides Chemical class 0.000 claims 3
- KLCZBRKMUCNDCV-UHFFFAOYSA-N 2-(3-ethylsulfonylphenyl)-6-methyl-n-(5-methyl-1h-pyrazol-3-yl)thieno[2,3-d]pyrimidin-4-amine Chemical compound CCS(=O)(=O)C1=CC=CC(C=2N=C3SC(C)=CC3=C(NC3=NNC(C)=C3)N=2)=C1 KLCZBRKMUCNDCV-UHFFFAOYSA-N 0.000 claims 2
- 102000003989 Aurora kinases Human genes 0.000 claims 2
- 108090000433 Aurora kinases Proteins 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 125000004103 aminoalkyl group Chemical group 0.000 claims 2
- 230000003796 beauty Effects 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 230000007170 pathology Effects 0.000 claims 2
- 238000002560 therapeutic procedure Methods 0.000 claims 2
- WTFDKXPWENAHLZ-UHFFFAOYSA-N 2-(1-ethylsulfonylindol-6-yl)-6-methyl-n-(5-methyl-1h-pyrazol-3-yl)thieno[2,3-d]pyrimidin-4-amine Chemical class C1=C2N(S(=O)(=O)CC)C=CC2=CC=C1C(N=C1SC(C)=CC1=1)=NC=1NC=1C=C(C)NN=1 WTFDKXPWENAHLZ-UHFFFAOYSA-N 0.000 claims 1
- YZNUVPBHHKMLGU-UHFFFAOYSA-N 2-(1-ethylsulfonylindol-6-yl)-n-(5-methyl-1h-pyrazol-3-yl)thieno[3,4-d]pyrimidin-4-amine Chemical compound C1=C2N(S(=O)(=O)CC)C=CC2=CC=C1C(=NC1=CSC=C11)N=C1NC=1C=C(C)NN=1 YZNUVPBHHKMLGU-UHFFFAOYSA-N 0.000 claims 1
- PZAUICCHVNZUHL-UHFFFAOYSA-N 2-(3-ethylsulfonylphenyl)-n-(5-methyl-1h-pyrazol-3-yl)thieno[3,4-d]pyrimidin-4-amine Chemical compound CCS(=O)(=O)C1=CC=CC(C2=NC3=CSC=C3C(NC3=NNC(C)=C3)=N2)=C1 PZAUICCHVNZUHL-UHFFFAOYSA-N 0.000 claims 1
- GEIWCEXZZYXLCD-UHFFFAOYSA-N 2-[3-[(dimethylamino)methyl]-1-ethylsulfonylindol-6-yl]-6-methyl-n-(5-methyl-1h-pyrazol-3-yl)thieno[2,3-d]pyrimidin-4-amine Chemical compound C1=C2N(S(=O)(=O)CC)C=C(CN(C)C)C2=CC=C1C(N=C1SC(C)=CC1=1)=NC=1NC=1C=C(C)NN=1 GEIWCEXZZYXLCD-UHFFFAOYSA-N 0.000 claims 1
- 206010003571 Astrocytoma Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 102000001253 Protein Kinase Human genes 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000008385 Urogenital Neoplasms Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000005157 alkyl carboxy group Chemical group 0.000 claims 1
- 125000005277 alkyl imino group Chemical group 0.000 claims 1
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 1
- AIMMVWOEOZMVMS-UHFFFAOYSA-N cyclopropanecarboxamide Chemical compound NC(=O)C1CC1 AIMMVWOEOZMVMS-UHFFFAOYSA-N 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 238000001361 intraarterial administration Methods 0.000 claims 1
- 238000007918 intramuscular administration Methods 0.000 claims 1
- 238000007912 intraperitoneal administration Methods 0.000 claims 1
- 238000007913 intrathecal administration Methods 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 239000002502 liposome Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- XAFOLUXJAZUULV-UHFFFAOYSA-N n-[4-[6-methyl-4-[(5-methyl-1h-pyrazol-3-yl)amino]thieno[2,3-d]pyrimidin-2-yl]sulfanylphenyl]cyclopropanecarboxamide Chemical compound N1C(C)=CC(NC=2C=3C=C(C)SC=3N=C(SC=3C=CC(NC(=O)C4CC4)=CC=3)N=2)=N1 XAFOLUXJAZUULV-UHFFFAOYSA-N 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 108060006633 protein kinase Proteins 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 1
- 238000007920 subcutaneous administration Methods 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 230000000699 topical effect Effects 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US78851506P | 2006-03-30 | 2006-03-30 | |
| PCT/US2007/065272 WO2007117995A2 (en) | 2006-03-30 | 2007-03-27 | Kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2009532375A JP2009532375A (ja) | 2009-09-10 |
| JP2009532375A5 true JP2009532375A5 (https=) | 2010-05-06 |
Family
ID=38312442
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009503222A Withdrawn JP2009532375A (ja) | 2006-03-30 | 2007-03-27 | キナーゼ阻害剤 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US20090247554A1 (https=) |
| EP (1) | EP1999135A2 (https=) |
| JP (1) | JP2009532375A (https=) |
| WO (1) | WO2007117995A2 (https=) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2009290474A1 (en) | 2008-09-11 | 2010-03-18 | Pfizer Inc. | Heteroaryls amide derivatives and their use as glucokinase activators |
| EP2389374A1 (en) | 2009-01-20 | 2011-11-30 | Pfizer Inc. | Substituted pyrazinone amides |
| EP2604604A1 (en) | 2009-03-11 | 2013-06-19 | Pfizer Inc | Benzofuranyl derivatives used as glucokinase inhibitors |
| CA2754685A1 (en) | 2009-03-11 | 2010-09-16 | Pfizer Inc. | Substituted indazole amides |
| WO2011049625A1 (en) | 2009-10-20 | 2011-04-28 | Mansour Samadpour | Method for aflatoxin screening of products |
| NZ599830A (en) | 2009-11-05 | 2014-08-29 | Rhizen Pharmaceuticals Sa | Novel kinase modulators |
| KR101483215B1 (ko) * | 2010-01-29 | 2015-01-16 | 한미약품 주식회사 | 단백질 키나아제 저해활성을 갖는 비시클릭 헤테로아릴 유도체 |
| MX2012013197A (es) | 2010-05-12 | 2013-04-03 | Abbvie Inc | Inhibidores de indazol de cinasa. |
| WO2011158149A1 (en) | 2010-06-18 | 2011-12-22 | Pfizer Inc. | 2-(3,5-disubstitutedphenyl)pyrimidin-4(3h)-one derivatives |
| EP2611812A1 (en) * | 2010-09-01 | 2013-07-10 | Ambit Biosciences Corporation | Thienopyridine and thienopyrimidine compounds and methods of use thereof |
| PH12013502240B1 (en) | 2011-05-04 | 2018-06-27 | Rhizen Pharmaceuticals Sa | Novel compounds as modulators of protein kinase |
| RS56494B1 (sr) | 2012-07-04 | 2018-01-31 | Rhizen Pharmaceuticals S A | Selektivni inhibitori pi3k delta |
| EP2769723A1 (en) * | 2013-02-22 | 2014-08-27 | Ruprecht-Karls-Universität Heidelberg | Compounds for use in inhibiting HIV capsid assembly |
| CN106232122A (zh) | 2013-09-27 | 2016-12-14 | 林伯士艾瑞斯公司 | Irak抑制剂和其用途 |
| US11214565B2 (en) | 2015-11-20 | 2022-01-04 | Denali Therapeutics Inc. | Compound, compositions, and methods |
| US11028080B2 (en) | 2016-03-11 | 2021-06-08 | Denali Therapeutics Inc. | Substituted pyrimidines as LRKK2 inhibitors |
| SMT202100699T1 (it) | 2016-06-16 | 2022-01-10 | Denali Therapeutics Inc | Pirimidin-2-ilammino-1h-pirazoli come inibitori di lrrk2 per l'uso nel trattamento di disturbi neurodegenerativi |
| JP7311228B2 (ja) * | 2017-06-30 | 2023-07-19 | ベイジン タイド ファーマシューティカル カンパニー リミテッド | Ｒｈｏ－関連プロテインキナーゼ阻害剤、それを含む医薬組成物並びにその調製方法及び使用 |
| AU2018312349A1 (en) | 2017-08-01 | 2020-02-06 | Theravance Biopharma R&D Ip, Llc | Pyrazolo and triazolo bicyclic compounds as JAK kinase inhibitors |
| CN113498352A (zh) | 2019-01-23 | 2021-10-12 | 施万生物制药研发Ip有限责任公司 | 作为jak抑制剂的咪唑并[1,5-a]吡啶、1,2,4-三唑并[4,3-a]吡啶和咪唑并[1,5-a]吡嗪 |
| US11697648B2 (en) | 2019-11-26 | 2023-07-11 | Theravance Biopharma R&D Ip, Llc | Fused pyrimidine pyridinone compounds as JAK inhibitors |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4505228B2 (ja) * | 2002-01-10 | 2010-07-21 | バイエル・シェーリング・ファルマ・アクチェンゲゼルシャフト | Ｒｈｏ−キナーゼ阻害剤 |
| ES2217956B1 (es) * | 2003-01-23 | 2006-04-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de 4-aminotieno(2,3-d)pirimidin-6-carbonitrilo. |
-
2007
- 2007-03-27 JP JP2009503222A patent/JP2009532375A/ja not_active Withdrawn
- 2007-03-27 EP EP07759499A patent/EP1999135A2/en not_active Withdrawn
- 2007-03-27 US US12/295,124 patent/US20090247554A1/en not_active Abandoned
- 2007-03-27 WO PCT/US2007/065272 patent/WO2007117995A2/en not_active Ceased
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