JP2006512400A5 - - Google Patents
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- JP2006512400A5 JP2006512400A5 JP2004570761A JP2004570761A JP2006512400A5 JP 2006512400 A5 JP2006512400 A5 JP 2006512400A5 JP 2004570761 A JP2004570761 A JP 2004570761A JP 2004570761 A JP2004570761 A JP 2004570761A JP 2006512400 A5 JP2006512400 A5 JP 2006512400A5
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- JP
- Japan
- Prior art keywords
- group
- substituted
- alkyl
- halogen
- compound according
- 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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- -1 3-fluoropyrrolidinyl Chemical group 0.000 claims 27
- 150000001875 compounds Chemical class 0.000 claims 23
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 18
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 16
- 229910052736 halogen Inorganic materials 0.000 claims 15
- 150000002367 halogens Chemical class 0.000 claims 15
- 125000000217 alkyl group Chemical group 0.000 claims 14
- 229910052757 nitrogen Inorganic materials 0.000 claims 14
- 229910052760 oxygen Inorganic materials 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 11
- 125000005842 heteroatom Chemical group 0.000 claims 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
- 229910052717 sulfur Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 9
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical group [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 claims 8
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 8
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 8
- 239000001301 oxygen Chemical group 0.000 claims 8
- 229910052698 phosphorus Inorganic materials 0.000 claims 8
- 239000011574 phosphorus Chemical group 0.000 claims 8
- 239000011593 sulfur Chemical group 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 7
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 208000035475 disorder Diseases 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- 125000002757 morpholinyl group Chemical group 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 125000003107 substituted aryl group Chemical group 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical class [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000003282 alkyl amino group Chemical group 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000003386 piperidinyl group Chemical group 0.000 claims 3
- 230000002062 proliferating effect Effects 0.000 claims 3
- HZAXFHJVJLSVMW-UHFFFAOYSA-N 2-Aminoethan-1-ol Chemical compound NCCO HZAXFHJVJLSVMW-UHFFFAOYSA-N 0.000 claims 2
- 206010016654 Fibrosis Diseases 0.000 claims 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000016097 disease of metabolism Diseases 0.000 claims 2
- 210000003584 mesangial cell Anatomy 0.000 claims 2
- 208000030159 metabolic disease Diseases 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims 2
- JWZZKOKVBUJMES-UHFFFAOYSA-N (+-)-Isoprenaline Chemical compound CC(C)NCC(O)C1=CC=C(O)C(O)=C1 JWZZKOKVBUJMES-UHFFFAOYSA-N 0.000 claims 1
- ZCCPVTVGEQLONB-UHFFFAOYSA-N 1-(1,3-dioxolan-2-yl)-n-methylmethanamine Chemical compound CNCC1OCCO1 ZCCPVTVGEQLONB-UHFFFAOYSA-N 0.000 claims 1
- QAFODUGVXFNLBE-UHFFFAOYSA-N 1-methoxybutan-2-amine Chemical compound CCC(N)COC QAFODUGVXFNLBE-UHFFFAOYSA-N 0.000 claims 1
- ZUUQKDDUUOFCNP-UHFFFAOYSA-N 2-(1,3-dioxolan-2-yl)-n-methylethanamine Chemical compound CNCCC1OCCO1 ZUUQKDDUUOFCNP-UHFFFAOYSA-N 0.000 claims 1
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims 1
- YMWIVSQHIYQMIX-UHFFFAOYSA-N 3-(3h-2-benzofuran-1-ylidene)-1-(piperidin-1-ylmethyl)indol-2-one Chemical compound C12=CC=CC=C2C(=C2C3=CC=CC=C3CO2)C(=O)N1CN1CCCCC1 YMWIVSQHIYQMIX-UHFFFAOYSA-N 0.000 claims 1
- AQWAKTUEFVVFOU-UHFFFAOYSA-N 3-[(4-morpholin-4-ylanilino)methylidene]-1-(piperidin-1-ylmethyl)indol-2-one Chemical compound C12=CC=CC=C2C(=CNC=2C=CC(=CC=2)N2CCOCC2)C(=O)N1CN1CCCCC1 AQWAKTUEFVVFOU-UHFFFAOYSA-N 0.000 claims 1
- JUXBOSKOSVRRMW-UHFFFAOYSA-N 3-[5-(dimethylamino)-3h-2-benzofuran-1-ylidene]-1-(piperidin-1-ylmethyl)indol-2-one Chemical compound O1CC2=CC(N(C)C)=CC=C2C1=C(C1=CC=CC=C11)C(=O)N1CN1CCCCC1 JUXBOSKOSVRRMW-UHFFFAOYSA-N 0.000 claims 1
- KDHWOCLBMVSZPG-UHFFFAOYSA-N 3-imidazol-1-ylpropan-1-amine Chemical compound NCCCN1C=CN=C1 KDHWOCLBMVSZPG-UHFFFAOYSA-N 0.000 claims 1
- 125000004364 3-pyrrolinyl group Chemical group [H]C1=C([H])C([H])([H])N(*)C1([H])[H] 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 206010063209 Chronic allograft nephropathy Diseases 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims 1
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010038933 Retinopathy of prematurity Diseases 0.000 claims 1
- 208000034841 Thrombotic Microangiopathies Diseases 0.000 claims 1
- 208000031737 Tissue Adhesions Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- KPCZJLGGXRGYIE-UHFFFAOYSA-N [C]1=CC=CN=C1 Chemical group [C]1=CC=CN=C1 KPCZJLGGXRGYIE-UHFFFAOYSA-N 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 206010064930 age-related macular degeneration Diseases 0.000 claims 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 230000007882 cirrhosis Effects 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 230000003176 fibrotic effect Effects 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 125000004594 isoindolinyl group Chemical group C1(NCC2=CC=CC=C12)* 0.000 claims 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 1
- 208000002780 macular degeneration Diseases 0.000 claims 1
- 230000003211 malignant effect Effects 0.000 claims 1
- BCDBHIAXYFPJCT-UHFFFAOYSA-N methyl piperidine-3-carboxylate Chemical compound COC(=O)C1CCCNC1 BCDBHIAXYFPJCT-UHFFFAOYSA-N 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 201000009925 nephrosclerosis Diseases 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- IPBPLHNLRKRLPJ-UHFFFAOYSA-N oxan-4-ylmethanamine Chemical compound NCC1CCOCC1 IPBPLHNLRKRLPJ-UHFFFAOYSA-N 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 230000011664 signaling Effects 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
- 230000029663 wound healing Effects 0.000 claims 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30697502A | 2002-11-27 | 2002-11-27 | |
| US10/307,097 | 2002-11-27 | ||
| US10/306,975 | 2002-11-27 | ||
| US10/307,097 US6699863B1 (en) | 2002-11-27 | 2002-11-27 | Kinase inhibitors for the treatment of disease |
| US10/389,416 | 2003-03-13 | ||
| US10/389,416 US6747025B1 (en) | 2002-11-27 | 2003-03-13 | Kinase inhibitors for the treatment of disease |
| PCT/US2003/036988 WO2004050621A2 (en) | 2002-11-27 | 2003-11-19 | Indol derivatives and their use as kinase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011123575A Division JP2011225582A (ja) | 2002-11-27 | 2011-06-01 | 疾患の治療のためのキナーゼ阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2006512400A JP2006512400A (ja) | 2006-04-13 |
| JP2006512400A5 true JP2006512400A5 (enExample) | 2006-11-02 |
| JP4879492B2 JP4879492B2 (ja) | 2012-02-22 |
Family
ID=45041406
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004570761A Expired - Fee Related JP4879492B2 (ja) | 2002-11-27 | 2003-11-19 | 疾患の治療のためのキナーゼ阻害剤 |
| JP2011123575A Pending JP2011225582A (ja) | 2002-11-27 | 2011-06-01 | 疾患の治療のためのキナーゼ阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011123575A Pending JP2011225582A (ja) | 2002-11-27 | 2011-06-01 | 疾患の治療のためのキナーゼ阻害剤 |
Country Status (1)
| Country | Link |
|---|---|
| JP (2) | JP4879492B2 (enExample) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4879492B2 (ja) * | 2002-11-27 | 2012-02-22 | アラーガン、インコーポレイテッド | 疾患の治療のためのキナーゼ阻害剤 |
| JP2010502741A (ja) * | 2006-09-11 | 2010-01-28 | キュリス，インコーポレイテッド | Ｐｔｋインヒビターとしての亜鉛結合部分を含む置換２−インドリノン |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19816624A1 (de) * | 1998-04-15 | 1999-10-21 | Boehringer Ingelheim Pharma | Neue substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel |
| IL139934A (en) * | 1998-05-29 | 2007-10-31 | Sugen Inc | History 2 - Indulinone converted to pyrrole and pharmaceutical preparations containing them |
| DE19824922A1 (de) * | 1998-06-04 | 1999-12-09 | Boehringer Ingelheim Pharma | Neue substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel |
| JP2002522452A (ja) * | 1998-08-04 | 2002-07-23 | スージェン・インコーポレーテッド | 蛋白質キナーゼの調節剤３−メチリデニル−２−インドリノン |
| EP1117397A1 (en) * | 1998-08-31 | 2001-07-25 | Sugen, Inc. | Geometrically restricted 2-indolinone derivatives as modulators of protein kinase activity |
| PL346898A1 (en) * | 1998-09-25 | 2002-03-11 | Boehringer Ingelheim Pharma | Novel substituted indolinones with an inhibitory effect on various kinases and cyclin/cdk complexes |
| GB9904933D0 (en) * | 1999-03-04 | 1999-04-28 | Glaxo Group Ltd | Compounds |
| ES2257313T3 (es) * | 1999-08-27 | 2006-08-01 | BOEHRINGER INGELHEIM PHARMA GMBH & CO.KG | Indolinonas sustituidas en calidad de inhibidores de tirosina quinasa. |
| UA75054C2 (uk) * | 1999-10-13 | 2006-03-15 | Бьорінгер Інгельхайм Фарма Гмбх & Ко. Кг | Заміщені в положенні 6 індолінони, їх одержання та їх застосування як лікарського засобу |
| MY128449A (en) * | 2000-05-24 | 2007-02-28 | Sugen Inc | Prodrugs of 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives |
| DE10054019A1 (de) * | 2000-11-01 | 2002-05-23 | Boehringer Ingelheim Pharma | Neue substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel |
| CN1155572C (zh) * | 2001-01-19 | 2004-06-30 | 中国人民解放军军事医学科学院毒物药物研究所 | 吲哚类衍生物及其抗肿瘤用途 |
| DE10117204A1 (de) * | 2001-04-06 | 2002-10-10 | Boehringer Ingelheim Pharma | In 6-Stellung substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel |
| DE10233366A1 (de) * | 2002-07-23 | 2004-02-12 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | In 6-Stellung substituierte Indolinonderivate, ihre Herstellung und ihre Verwendung als Arzneimittel |
| JP4879492B2 (ja) * | 2002-11-27 | 2012-02-22 | アラーガン、インコーポレイテッド | 疾患の治療のためのキナーゼ阻害剤 |
-
2003
- 2003-11-19 JP JP2004570761A patent/JP4879492B2/ja not_active Expired - Fee Related
-
2011
- 2011-06-01 JP JP2011123575A patent/JP2011225582A/ja active Pending
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