HUP0102210A2 - Substituted indolinones, the production thereof and their use for producing medicaments and medicaments containing same - Google Patents
Substituted indolinones, the production thereof and their use for producing medicaments and medicaments containing sameInfo
- Publication number
- HUP0102210A2 HUP0102210A2 HU0102210A HUP0102210A HUP0102210A2 HU P0102210 A2 HUP0102210 A2 HU P0102210A2 HU 0102210 A HU0102210 A HU 0102210A HU P0102210 A HUP0102210 A HU P0102210A HU P0102210 A2 HUP0102210 A2 HU P0102210A2
- Authority
- HU
- Hungary
- Prior art keywords
- alkyl
- medicaments
- optionally substituted
- production
- group
- Prior art date
Links
- JYGFTBXVXVMTGB-UHFFFAOYSA-N indolin-2-one Chemical class C1=CC=C2NC(=O)CC2=C1 JYGFTBXVXVMTGB-UHFFFAOYSA-N 0.000 title abstract 2
- 239000003814 drug Substances 0.000 title 2
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 102000016736 Cyclin Human genes 0.000 abstract 1
- 108050006400 Cyclin Proteins 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- 230000002159 abnormal effect Effects 0.000 abstract 1
- 239000008186 active pharmaceutical agent Substances 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 125000001589 carboacyl group Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 230000004663 cell proliferation Effects 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 1
- 230000003612 virological effect Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/32—Oxygen atoms
- C07D209/34—Oxygen atoms in position 2
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
A találmány tárgyát az általános képletű szubsztituált indolinonok -ahol X O vagy S; R1 H, alkoxi-karbonil- vagy alkanoilcsoport; R2karboxi-, alkoxi-karbonil- vagy adott esetben egy vagy kétalkilcsoporttal szubsztituált karbamoilcsoport; R3 H vagy adottesetben szubsztituált alkilcsoport; R4 H, alkil- vagy adott esetbenszubsztituált cikloalkil-, fenil- vagy naftilcsoport, olyan 5 vagy 6tagú heteroaromás csoport, amelyek két szomszédos szénatomjára egyfenilgyűrű kondenzálódhat; és R5 H vagy alkilcsoport -izomerjeik éssóik, előállításuk és gyógyszerhatóanyagként való alkalmazásuk képezi.A fenti vegyületek a különböző kinázokra, valamint a vírusosciklinekre gátló hatásúak, így pl. A rendellenes sejtburjánzáskezelésére alkalmasak. ÓThe subject of the invention is the substituted indolinones of the general formula -where X is O or S; R 1 H, alkoxycarbonyl or alkanoyl; R 2 is a carboxy, alkoxycarbonyl, or optionally substituted carbamoyl group with one or two alkyl groups; R3 is H or optionally substituted alkyl; R4 H, an alkyl or optionally substituted cycloalkyl, phenyl or naphthyl group, a 5- or 6-membered heteroaromatic group whose two adjacent carbon atoms can be condensed with a single phenyl ring; and R5 H or alkyl group isomers and their salts, their production and use as active pharmaceutical ingredients. The above compounds have inhibitory effects on various kinases and viral cyclins, such as They are suitable for the treatment of abnormal cell proliferation. HE
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19824922A DE19824922A1 (en) | 1998-06-04 | 1998-06-04 | Novel substituted indolinones, their preparation and their use as pharmaceuticals |
| PCT/EP1999/003692 WO1999062882A1 (en) | 1998-06-04 | 1999-05-28 | Substituted indolinones, the production thereof and their use as medicaments |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0102210A2 true HUP0102210A2 (en) | 2001-11-28 |
| HUP0102210A3 HUP0102210A3 (en) | 2002-12-28 |
Family
ID=7869856
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0102210A HUP0102210A3 (en) | 1998-06-04 | 1999-05-28 | Substituted indolinones, the production thereof and their use for producing medicaments and medicaments containing same |
Country Status (23)
| Country | Link |
|---|---|
| EP (1) | EP1100779A1 (en) |
| JP (1) | JP2002516906A (en) |
| KR (1) | KR20010043973A (en) |
| CN (1) | CN1303374A (en) |
| AU (1) | AU764782B2 (en) |
| BG (1) | BG104938A (en) |
| BR (1) | BR9910898A (en) |
| CA (1) | CA2328291A1 (en) |
| CO (1) | CO5050294A1 (en) |
| DE (1) | DE19824922A1 (en) |
| EA (1) | EA003514B1 (en) |
| EE (1) | EE200000723A (en) |
| HR (1) | HRP20000831A2 (en) |
| HU (1) | HUP0102210A3 (en) |
| ID (1) | ID27035A (en) |
| IL (1) | IL138702A0 (en) |
| NO (1) | NO20006138L (en) |
| PL (1) | PL344467A1 (en) |
| SK (1) | SK18222000A3 (en) |
| TR (1) | TR200003515T2 (en) |
| WO (1) | WO1999062882A1 (en) |
| YU (1) | YU73900A (en) |
| ZA (1) | ZA200005435B (en) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19816624A1 (en) * | 1998-04-15 | 1999-10-21 | Boehringer Ingelheim Pharma | Novel substituted indolinones, their preparation and their use as pharmaceuticals |
| US6624171B1 (en) | 1999-03-04 | 2003-09-23 | Smithkline Beecham Corporation | Substituted aza-oxindole derivatives |
| GB9904933D0 (en) * | 1999-03-04 | 1999-04-28 | Glaxo Group Ltd | Compounds |
| US6762180B1 (en) | 1999-10-13 | 2004-07-13 | Boehringer Ingelheim Pharma Kg | Substituted indolines which inhibit receptor tyrosine kinases |
| UA75054C2 (en) * | 1999-10-13 | 2006-03-15 | Бьорінгер Інгельхайм Фарма Гмбх & Ко. Кг | Substituted in position 6 indolinones, producing and use thereof as medicament |
| JP2004517049A (en) | 2000-09-01 | 2004-06-10 | グラクソ グループ リミテッド | Substituted oxindole derivatives as tyrosine kinase inhibitors |
| JP2004508366A (en) * | 2000-09-01 | 2004-03-18 | グラクソ グループ リミテッド | Oxindole derivatives |
| DE10117204A1 (en) * | 2001-04-06 | 2002-10-10 | Boehringer Ingelheim Pharma | Indolinones substituted in the 6-position, their preparation and their use as medicaments |
| CA2452392A1 (en) | 2001-06-29 | 2003-01-16 | Ab Science | Use of tyrosine kinase inhibitors for treating inflammatory bowel diseases (ibd) |
| JP2005500041A (en) | 2001-06-29 | 2005-01-06 | アブ サイエンス | Potent, selective and non-toxic C-KIT inhibitor |
| ATE345839T1 (en) | 2001-06-29 | 2006-12-15 | Ab Science | THE USE OF TYROSINE KINASE INHIBITORS FOR THE TREATMENT OF ALLERGY DISEASES |
| WO2003002109A2 (en) * | 2001-06-29 | 2003-01-09 | Ab Science | Use of tyrosine kinase inhibitors for treating autoimmune diseases |
| JP2004537537A (en) * | 2001-06-29 | 2004-12-16 | アブ サイエンス | Uses of tyrosine kinase inhibitors to treat inflammatory diseases |
| US6765012B2 (en) | 2001-09-27 | 2004-07-20 | Allergan, Inc. | 3-(Arylamino)methylene-1,3-dihydro-2H-indol-2-ones as kinase inhibitors |
| US7169936B2 (en) | 2002-07-23 | 2007-01-30 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Indolinone derivatives substituted in the 6-position, their preparation and their use as medicaments |
| JP4879492B2 (en) * | 2002-11-27 | 2012-02-22 | アラーガン、インコーポレイテッド | Kinase inhibitors for the treatment of diseases |
| DE102004012070A1 (en) * | 2004-03-12 | 2005-09-29 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | New cycloalkyl-containing 5-acylindolinones, their preparation and their use as medicaments |
| PE20060777A1 (en) * | 2004-12-24 | 2006-10-06 | Boehringer Ingelheim Int | INDOLINONE DERIVATIVES FOR THE TREATMENT OR PREVENTION OF FIBROTIC DISEASES |
| SG177128A1 (en) * | 2006-12-05 | 2012-01-30 | Arena Pharm Inc | Processes for preparing (r)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1h-3-benzazepine and intermediates thereof |
| GB0706072D0 (en) * | 2007-03-28 | 2007-05-09 | Sterix Ltd | Compound |
| US20170065529A1 (en) | 2015-09-09 | 2017-03-09 | Boehringer Ingelheim International Gmbh | Pharmaceutical dosage form for immediate release of an indolinone derivative |
| CN101735071A (en) * | 2009-12-04 | 2010-06-16 | 大连凯飞精细化工有限公司 | Method for producing 4-N,N-dimethylamino methylaniline |
| CN103102352B (en) * | 2011-11-15 | 2015-08-12 | 山东亨利医药科技有限责任公司 | Tyrosine kinase inhibitor indolinone derivative |
| CN103130775B (en) * | 2011-11-22 | 2015-09-30 | 山东亨利医药科技有限责任公司 | As the dihydroindole ketone derivate of tyrosine kinase inhibitor |
| GB201208775D0 (en) | 2012-05-18 | 2012-07-04 | Uni I Oslo | Chemical compounds |
| CN103848814B (en) * | 2012-12-06 | 2016-08-17 | 山东亨利医药科技有限责任公司 | The full ketone derivatives of substituted indole as tyrosine kinase inhibitor |
| US11530206B2 (en) | 2019-05-10 | 2022-12-20 | Deciphera Pharmaceuticals, Llc | Phenylaminopyrimidine amide autophagy inhibitors and methods of use thereof |
| WO2024050297A1 (en) * | 2022-09-02 | 2024-03-07 | Deciphera Pharmaceuticals, Llc | Ulk inhibitors and methods of use thereof |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE838623A (en) * | 1976-02-16 | 1976-06-16 | 3-HYDROXYMETHYLENE-2-INDOLINONE DERIVATIVES AND PROCESS FOR THEIR PRODUCTION | |
| US4145422A (en) * | 1977-09-06 | 1979-03-20 | Abbott Laboratories | Aminomethylene oxindoles |
| US5880141A (en) * | 1995-06-07 | 1999-03-09 | Sugen, Inc. | Benzylidene-Z-indoline compounds for the treatment of disease |
| ES2251741T3 (en) * | 1996-08-23 | 2006-05-01 | Sugen, Inc. | INDOLINONA COMBINATORY LIBRARIES AND RELATED PRODUCTS AND METHODS FOR THE TREATMENT OF DISEASES. |
| GB9718913D0 (en) * | 1997-09-05 | 1997-11-12 | Glaxo Group Ltd | Substituted oxindole derivatives |
-
1998
- 1998-06-04 DE DE19824922A patent/DE19824922A1/en not_active Withdrawn
-
1999
- 1999-05-28 JP JP2000552094A patent/JP2002516906A/en active Pending
- 1999-05-28 TR TR2000/03515T patent/TR200003515T2/en unknown
- 1999-05-28 ID IDW20002523A patent/ID27035A/en unknown
- 1999-05-28 SK SK1822-2000A patent/SK18222000A3/en unknown
- 1999-05-28 EP EP99926454A patent/EP1100779A1/en not_active Withdrawn
- 1999-05-28 EE EEP200000723A patent/EE200000723A/en unknown
- 1999-05-28 YU YU73900A patent/YU73900A/en unknown
- 1999-05-28 AU AU43707/99A patent/AU764782B2/en not_active Ceased
- 1999-05-28 HU HU0102210A patent/HUP0102210A3/en unknown
- 1999-05-28 WO PCT/EP1999/003692 patent/WO1999062882A1/en not_active Application Discontinuation
- 1999-05-28 CA CA002328291A patent/CA2328291A1/en not_active Abandoned
- 1999-05-28 CN CN99806884A patent/CN1303374A/en active Pending
- 1999-05-28 IL IL13870299A patent/IL138702A0/en unknown
- 1999-05-28 EA EA200100001A patent/EA003514B1/en not_active IP Right Cessation
- 1999-05-28 PL PL99344467A patent/PL344467A1/en unknown
- 1999-05-28 KR KR1020007013597A patent/KR20010043973A/en not_active Application Discontinuation
- 1999-05-28 BR BR9910898-4A patent/BR9910898A/en not_active IP Right Cessation
- 1999-06-04 CO CO99035396A patent/CO5050294A1/en unknown
-
2000
- 2000-10-05 ZA ZA200005435A patent/ZA200005435B/en unknown
- 2000-11-13 BG BG104938A patent/BG104938A/en active Pending
- 2000-12-01 HR HR20000831A patent/HRP20000831A2/en not_active Application Discontinuation
- 2000-12-01 NO NO20006138A patent/NO20006138L/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| BG104938A (en) | 2001-06-29 |
| YU73900A (en) | 2003-04-30 |
| HUP0102210A3 (en) | 2002-12-28 |
| NO20006138L (en) | 2001-02-01 |
| IL138702A0 (en) | 2001-10-31 |
| ZA200005435B (en) | 2002-01-07 |
| CA2328291A1 (en) | 1999-12-09 |
| EA200100001A1 (en) | 2001-08-27 |
| HRP20000831A2 (en) | 2001-12-31 |
| EP1100779A1 (en) | 2001-05-23 |
| CN1303374A (en) | 2001-07-11 |
| KR20010043973A (en) | 2001-05-25 |
| SK18222000A3 (en) | 2001-08-06 |
| ID27035A (en) | 2001-02-22 |
| DE19824922A1 (en) | 1999-12-09 |
| CO5050294A1 (en) | 2001-06-27 |
| NO20006138D0 (en) | 2000-12-01 |
| BR9910898A (en) | 2001-02-13 |
| AU764782B2 (en) | 2003-08-28 |
| EA003514B1 (en) | 2003-06-26 |
| TR200003515T2 (en) | 2001-06-21 |
| EE200000723A (en) | 2002-04-15 |
| JP2002516906A (en) | 2002-06-11 |
| PL344467A1 (en) | 2001-11-05 |
| WO1999062882A1 (en) | 1999-12-09 |
| AU4370799A (en) | 1999-12-20 |
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