HUP0303897A2 - Eljárások p38 kinázzal összafüggő esetek kezelésére, kináz inhibitorokként alkalmazható pirrolotriazin vegyületek és ezeket tartalmazó gyógyszerkészítmények - Google Patents
Eljárások p38 kinázzal összafüggő esetek kezelésére, kináz inhibitorokként alkalmazható pirrolotriazin vegyületek és ezeket tartalmazó gyógyszerkészítményekInfo
- Publication number
- HUP0303897A2 HUP0303897A2 HU0303897A HUP0303897A HUP0303897A2 HU P0303897 A2 HUP0303897 A2 HU P0303897A2 HU 0303897 A HU0303897 A HU 0303897A HU P0303897 A HUP0303897 A HU P0303897A HU P0303897 A2 HUP0303897 A2 HU P0303897A2
- Authority
- HU
- Hungary
- Prior art keywords
- group
- optionally substituted
- aryl
- atom
- hydrogen atom
- Prior art date
Links
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 102000002574 p38 Mitogen-Activated Protein Kinases Human genes 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 150000003921 pyrrolotriazines Chemical class 0.000 title 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 6
- 125000005843 halogen group Chemical group 0.000 abstract 5
- -1 methyl- Chemical group 0.000 abstract 5
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 3
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 3
- 125000003107 substituted aryl group Chemical group 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000002619 bicyclic group Chemical group 0.000 abstract 2
- 101001043818 Mus musculus Interleukin-31 receptor subunit alpha Proteins 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- MWPLVEDNUUSJAV-UHFFFAOYSA-N anthracene Chemical class C1=CC=CC2=CC3=CC=CC=C3C=C21 MWPLVEDNUUSJAV-UHFFFAOYSA-N 0.000 abstract 1
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
- A61P39/02—Antidotes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Abstract
A találmány tárgyát a p38 kroáz aktivitással összefüggő állapot(ok)kezelésére alkalmazható általános képletű vegyületek - ahol R3hidrogénatom, halogénatom, metil-, perfluor-metil-, metoxi-, ciano-vagy -NH2 csoport; X -O-, -OC(=O)-, -S-, -S(=O)-, -SO2-, -C(=O)-, -CO2-, -NR10-, -NR10C(=O)-, -NR10C(=O)NR11-, -NR10CO2, -NR10SO2, -NR10SO2NR11-, -SO2NR10, -C(=O)NR10 általános képletű csoport,halogénatom, nitro- vagy cianocsoport, vagy X hiányzik; Z -O-, -S-,=N- atom vagy =CR20- általános képletű csoport, ahol ha Z =CR20-, ez aszénatom az R4 és R5 csoporttal egy adott esetben szubsztituáltbiciklusos aril- vagy heteroarilcsoportot képezhet; R1 hidrogénatom, -CH3, -OH, -OCH3, -SH, -SCH3, és egyéb csoportok, valamint halogénatom,nitro- vagy cianocsoport; R2 a) hidrogénatom, azzal a feltétellel,hogy R2 hidrogénatomtól eltérő, ha X bizonyos általános képletűcsoportokat jelent; b) adott esetben szubsztituált alkil, alkenil,vagy alkinilcsoport; c) adott esetben szubsztituált aril- vagyheteroarilcsoport; és d) adott esetben szubsztituált heterociklusosvagy cikloalkilcsoport; vagy e) R2 hiányzik, ha X halogénatom, nitro-vagy cianocsoport; (i) R4 szubsztituált aril, heteroaril vagy adottesetben szubsztituált biciklusos 7-11 tagú telített vagy telítetlenkarbociklusos vagy heterociklusos gyűrű, és R5 hidrogénatom, alkilvagy szubsztituált alkilcsoport, azzal a feltétellel, hogy ha Zjelentése O vagy S, R5 hiányzik, vagy alternatív módon, (ii) R4 és R5a Z csoporttal együtt adott esetben szubsztituált biciklusos 7-11 tagúaril- vagy heteroarilcsoportot képez; R6 hidrogénatom, halogénatom,alkil, szubsztituált alkil, aril, szubsztituált aril, heterociklusos,szubsztituált heterociklusos vagy egyéb csoport - és a általánosképletű vegyületek, valamint gyógyászatilag alkalmazható sóik,prodrugjaik, szolvátjaik, továbbá alkalmazásaik képezik. A találmánykiterjed a vegyületeket tartalmazó gyógyszerkészítményekre is. Ó
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24987700P | 2000-11-17 | 2000-11-17 | |
| US31056101P | 2001-08-07 | 2001-08-07 | |
| PCT/US2001/049982 WO2002040486A2 (en) | 2000-11-17 | 2001-11-07 | METHODS OF TREATING p38 KINASE-ASSOCIATED CONDITIONS AND PYRROLOTRIAZINE COMPOUNDS USEFUL AS KINASE INHIBITORS |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HUP0303897A2 true HUP0303897A2 (hu) | 2004-03-01 |
Family
ID=26940426
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0303897A HUP0303897A2 (hu) | 2000-11-17 | 2001-11-07 | Eljárások p38 kinázzal összafüggő esetek kezelésére, kináz inhibitorokként alkalmazható pirrolotriazin vegyületek és ezeket tartalmazó gyógyszerkészítmények |
Country Status (32)
| Country | Link |
|---|---|
| EP (1) | EP1363910B1 (hu) |
| JP (1) | JP2004522713A (hu) |
| KR (1) | KR100847605B1 (hu) |
| CN (1) | CN1622946A (hu) |
| AR (1) | AR032637A1 (hu) |
| AT (1) | ATE318820T1 (hu) |
| AU (2) | AU2002232760B2 (hu) |
| BG (1) | BG107750A (hu) |
| BR (1) | BR0115446A (hu) |
| CA (1) | CA2429628A1 (hu) |
| CY (1) | CY1105250T1 (hu) |
| CZ (1) | CZ20031370A3 (hu) |
| DE (1) | DE60117607T2 (hu) |
| DK (1) | DK1363910T3 (hu) |
| EE (1) | EE200300227A (hu) |
| ES (1) | ES2259051T3 (hu) |
| GE (1) | GEP20063915B (hu) |
| HK (1) | HK1057555A1 (hu) |
| HR (1) | HRP20030485A2 (hu) |
| HU (1) | HUP0303897A2 (hu) |
| IL (1) | IL155570A0 (hu) |
| IS (1) | IS6816A (hu) |
| MX (1) | MXPA03004290A (hu) |
| MY (1) | MY127066A (hu) |
| NO (1) | NO20032229L (hu) |
| NZ (1) | NZ525334A (hu) |
| PE (1) | PE20020819A1 (hu) |
| PL (1) | PL366376A1 (hu) |
| PT (1) | PT1363910E (hu) |
| SK (1) | SK5402003A3 (hu) |
| WO (1) | WO2002040486A2 (hu) |
| YU (1) | YU37903A (hu) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6867300B2 (en) | 2000-11-17 | 2005-03-15 | Bristol-Myers Squibb Company | Methods for the preparation of pyrrolotriazine compounds useful as kinase inhibitors |
| US7700610B2 (en) | 2001-06-29 | 2010-04-20 | Ab Science | Use of tyrosine kinase inhibitors for treating allergic diseases |
| CA2452368A1 (en) | 2001-06-29 | 2003-01-09 | Ab Science | New potent, selective and non toxic c-kit inhibitors |
| ATE330608T1 (de) | 2001-06-29 | 2006-07-15 | Ab Science | Die verwendung von n-phenyl-2-pyrimidine-amine derivaten zur behandlung von entzündlichen erkrankungen |
| JP2004530722A (ja) * | 2001-06-29 | 2004-10-07 | アブ サイエンス | 骨喪失を治療するためのチロシンキナーゼ阻害剤の使用法 |
| WO2003004007A2 (en) | 2001-06-29 | 2003-01-16 | Ab Science | Use of tyrosine kinase inhibitors for treating inflammatory bowel diseases (ibd) |
| GB0124933D0 (en) | 2001-10-17 | 2001-12-05 | Glaxo Group Ltd | Chemical compounds |
| DE60316913T2 (de) | 2002-02-12 | 2008-11-20 | Smithkline Beecham Corp. | Nicotinamide und deren verwendung als p38 inhibitoren |
| RS52392B (en) | 2002-02-14 | 2013-02-28 | Pharmacia Corporation | SUBSTITUTED PYRIDINONES AS P38 MAP KINASE MODULATORS |
| US6900208B2 (en) | 2002-03-28 | 2005-05-31 | Bristol Myers Squibb Company | Pyrrolopyridazine compounds and methods of use thereof for the treatment of proliferative disorders |
| US7388009B2 (en) * | 2002-04-23 | 2008-06-17 | Bristol-Myers Squibb Company | Heteroaryl-substituted pyrrolo-triazine compounds useful as kinase inhibitors |
| RU2375363C2 (ru) | 2002-04-23 | 2009-12-10 | Бристол-Маерс Сквибб Компани | Пирролотриазиновые производные анилина, полезные в качестве ингибиторов киназы |
| EP1503996B1 (en) | 2002-04-23 | 2008-12-24 | Bristol-Myers Squibb Company | Aryl ketone pyrrolo-triazine compounds useful as kinase inhibitors |
| US6933386B2 (en) | 2002-07-19 | 2005-08-23 | Bristol Myers Squibb Company | Process for preparing certain pyrrolotriazine compounds |
| TWI329112B (en) | 2002-07-19 | 2010-08-21 | Bristol Myers Squibb Co | Novel inhibitors of kinases |
| AU2003265349A1 (en) | 2002-08-02 | 2004-02-23 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
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| WO2004063197A1 (en) * | 2003-01-09 | 2004-07-29 | Fujisawa Pharmaceutical Co., Ltd. | Pyrrolopyridazine derivatives |
| MXPA05008183A (es) * | 2003-02-05 | 2005-10-05 | Bristol Myers Squibb Co | Proceso para preparar pirrolotriazina como inhibidores de cinasa. |
| GB0308201D0 (en) | 2003-04-09 | 2003-05-14 | Smithkline Beecham Corp | Novel compounds |
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| GB0318814D0 (en) | 2003-08-11 | 2003-09-10 | Smithkline Beecham Corp | Novel compounds |
| US7419978B2 (en) * | 2003-10-22 | 2008-09-02 | Bristol-Myers Squibb Company | Phenyl-aniline substituted bicyclic compounds useful as kinase inhibitors |
| US7102001B2 (en) * | 2003-12-12 | 2006-09-05 | Bristol-Myers Squibb Company | Process for preparing pyrrolotriazine |
| CA2548326A1 (en) * | 2003-12-23 | 2005-07-14 | Novartis Ag | Bicyclic heterocyclic p-38 kinase inhibitors |
| US7064203B2 (en) | 2003-12-29 | 2006-06-20 | Bristol Myers Squibb Company | Di-substituted pyrrolotriazine compounds |
| MY145634A (en) | 2003-12-29 | 2012-03-15 | Bristol Myers Squibb Co | Pyrrolotriazine compounds as kinase inhibitors |
| US7459562B2 (en) | 2004-04-23 | 2008-12-02 | Bristol-Myers Squibb Company | Monocyclic heterocycles as kinase inhibitors |
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| US7439246B2 (en) | 2004-06-28 | 2008-10-21 | Bristol-Myers Squibb Company | Fused heterocyclic kinase inhibitors |
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| US20050288290A1 (en) * | 2004-06-28 | 2005-12-29 | Borzilleri Robert M | Fused heterocyclic kinase inhibitors |
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| US7504521B2 (en) | 2004-08-05 | 2009-03-17 | Bristol-Myers Squibb Co. | Methods for the preparation of pyrrolotriazine compounds |
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| WO2017151409A1 (en) | 2016-02-29 | 2017-09-08 | University Of Florida Research Foundation, Incorporated | Chemotherapeutic methods |
| US10342786B2 (en) | 2017-10-05 | 2019-07-09 | Fulcrum Therapeutics, Inc. | P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD |
| PL3691620T3 (pl) | 2017-10-05 | 2022-11-21 | Fulcrum Therapeutics, Inc. | Inhibitory kinazy p38 zmniejszają poziom ekspresji genu dux4 i dalszych genów do leczenia fshd |
| CN108516977A (zh) * | 2018-07-10 | 2018-09-11 | 刘凤娟 | 一种用于治疗恶性肿瘤的map激酶抑制剂的合成方法 |
| CN112028892B (zh) * | 2020-07-29 | 2022-12-16 | 天津全和诚科技有限责任公司 | 4-氨基-吡咯并三嗪衍生物在制备抗肺纤维化制剂中的应用 |
| CN112094219B (zh) * | 2020-09-10 | 2022-08-05 | 广东莱佛士制药技术有限公司 | 一种制备钾离子竞争性阻滞剂中间体的方法 |
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| CA2163399A1 (en) * | 1994-11-24 | 1996-05-25 | Katsuhiro Kawano | Triazine derivative, chymase activity inhibitor and nitric oxide production inhibitor |
| WO1999024033A1 (en) * | 1997-11-12 | 1999-05-20 | Shionogi & Co., Ltd. | Method for the treatment of disorders associated with apoptosis using n-heterocyclic glyoxylamide compounds |
| AU770377B2 (en) * | 1999-05-21 | 2004-02-19 | Bristol-Myers Squibb Company | Pyrrolotriazine inhibitors of kinases |
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