EA201171012A1 - Производные 5-фторбензотиазолов и 5-фторбензимидазолов, содержащие 6-замещенный триазолопиридазинсульфанил в положении 6: получение, применение в качестве лекарственных средств и применение в качестве ингибиторов met - Google Patents
Производные 5-фторбензотиазолов и 5-фторбензимидазолов, содержащие 6-замещенный триазолопиридазинсульфанил в положении 6: получение, применение в качестве лекарственных средств и применение в качестве ингибиторов metInfo
- Publication number
- EA201171012A1 EA201171012A1 EA201171012A EA201171012A EA201171012A1 EA 201171012 A1 EA201171012 A1 EA 201171012A1 EA 201171012 A EA201171012 A EA 201171012A EA 201171012 A EA201171012 A EA 201171012A EA 201171012 A1 EA201171012 A1 EA 201171012A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- cycloalkyl
- phenyl
- alkyl
- application
- substituted
- Prior art date
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
- C07D277/62—Benzothiazoles
- C07D277/68—Benzothiazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
- C07D277/82—Nitrogen atoms
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61P17/06—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
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
-
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
-
- 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
- A61P37/08—Antiallergic agents
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
-
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurology (AREA)
- Cardiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Obesity (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Emergency Medicine (AREA)
- Urology & Nephrology (AREA)
- Dermatology (AREA)
- Oncology (AREA)
- Vascular Medicine (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Ophthalmology & Optometry (AREA)
- Endocrinology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Thiazole And Isothizaole Compounds (AREA)
Abstract
Изобретение относится к новым соединениям формулы (I), в которой (II) представляет собой простую или двойную связь; F представляет собой атом фтора; Ra представляет собой Н, Hal, алкоксигруппу, O-циклоалкил, -O-гетероциклоалкил, -NH-циклоалкил, -NH-гетероциклоалкил, гетероарил, фенил, NHCO-алкил, NHCO-циклоалкил или NR1R2; Х представляет собой S, SO или SO; А представляет собой NH или S; W представляет собой Н, алкил или COR, где R представляет собой циклоалкил; алкил, имеющий при необходимости в качестве заместителя NR3R4, алкокси-, гидроксигруппу, фенил, гетероарил или гетероциклоалкил; алкоксигруппу, имеющую при необходимости в качестве заместителя NR3R4, точнее O-(CH)-NR3R4, O-фенил или O-(CH)-фенил, где фенил при необходимости является замещенным, а n=1-4; или NR1R2, где R1 представляет собой Н или алкил, a R2 представляет собой Н, циклоалкил или алкил; R3 и R4 представляют собой Н, алкил, циклоалкил, гетероарил или фенил; или R1, R2 и/или R3, R4 образуют с N цикл, содержащий при необходимости О, S, N и/или NH; причем любые гетероциклоалкилы, гетероарилы, фенилы и циклические радикалы при необходимости являются замещенными; причем эти данные соединения находятся в любых формах изомеров или солей, применимых в качестве лекарственных средств и предпочтительно в качестве ингибиторов MET.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR0900514A FR2941952B1 (fr) | 2009-02-06 | 2009-02-06 | Derives de 6-(6-substitue-triazolopyridazine-sulfanyl) 5-fluoro-benzothiazoles et 5-fluoro-benzimidazoles : preparation, application comme medicaments et utilisation comme inhibiteurs de met. |
| PCT/FR2010/050180 WO2010089509A1 (fr) | 2009-02-06 | 2010-02-04 | Derives de 6-(6-substitue-triazolopyridazine-sulfanyl) 5-fluoro-benzothiazoles et 5-fluoro-benzimidazoles : preparation, application comme medicaments et utilisation comme inhibiteurs de met |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| EA201171012A1 true EA201171012A1 (ru) | 2012-03-30 |
Family
ID=40886775
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201171012A EA201171012A1 (ru) | 2009-02-06 | 2010-02-04 | Производные 5-фторбензотиазолов и 5-фторбензимидазолов, содержащие 6-замещенный триазолопиридазинсульфанил в положении 6: получение, применение в качестве лекарственных средств и применение в качестве ингибиторов met |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US20120165326A1 (ru) |
| EP (1) | EP2393793A1 (ru) |
| JP (1) | JP2012517410A (ru) |
| KR (1) | KR20110126659A (ru) |
| CN (1) | CN102369191A (ru) |
| AR (1) | AR075251A1 (ru) |
| AU (1) | AU2010212234A1 (ru) |
| BR (1) | BRPI1008019A2 (ru) |
| CA (1) | CA2751474A1 (ru) |
| CO (1) | CO6420339A2 (ru) |
| EA (1) | EA201171012A1 (ru) |
| FR (1) | FR2941952B1 (ru) |
| IL (1) | IL214408A0 (ru) |
| MA (1) | MA33103B1 (ru) |
| MX (1) | MX2011008290A (ru) |
| SG (1) | SG173561A1 (ru) |
| TW (1) | TW201036977A (ru) |
| UY (1) | UY32422A (ru) |
| WO (1) | WO2010089509A1 (ru) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2966151B1 (fr) * | 2010-10-14 | 2012-11-09 | Sanofi Aventis | Derives de 6-(alkyl- ou cycloalkyl-triazolopyridazine-sulfanyl) benzothiazoles: preparation, application comme medicaments et utilisation comme inhibiteurs de met |
| MX339302B (es) | 2011-09-15 | 2016-05-19 | Novartis Ag | 3-(quinolin-6-il-tio)-[1,2,4]-triazolo-[4,3-a]-piridinas 6-sustituidas como cinasas de tirosina. |
| AU2018378935A1 (en) | 2017-12-07 | 2020-06-25 | The Regents Of The University Of Michigan | NSD family inhibitors and methods of treatment therewith |
| US20220143049A1 (en) | 2019-03-21 | 2022-05-12 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| JP2023500906A (ja) | 2019-11-08 | 2023-01-11 | インサーム（インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル） | キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1298125A1 (en) | 2001-09-26 | 2003-04-02 | Aventis Pharma S.A. | Substituted benzimidazole compounds and their use for the treatment of cancer |
| CA2630884A1 (en) * | 2005-11-30 | 2007-06-07 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-met and uses thereof |
| EA015754B1 (ru) * | 2005-12-21 | 2011-12-30 | Янссен Фармацевтика, Н.В. | Триазолопиридазины в качестве модуляторов тирозинкиназы |
| EP2032578A2 (en) * | 2006-05-30 | 2009-03-11 | Pfizer Products Incorporated | Triazolopyridazine derivatives |
| PE20080403A1 (es) * | 2006-07-14 | 2008-04-25 | Amgen Inc | Derivados heterociclicos fusionados y metodos de uso |
| PT2084162E (pt) * | 2006-10-23 | 2012-10-09 | Sgx Pharmaceuticals Inc | Triazoles bicíclicos como moduladores de proteína quinase |
| PA8792501A1 (es) * | 2007-08-09 | 2009-04-23 | Sanofi Aventis | Nuevos derivados de 6-triazolopiridacina-sulfanil benzotiazol y bencimidazol,su procedimiento de preparación,su aplicación como medicamentos,composiciones farmacéuticas y nueva utilización principalmente como inhibidores de met. |
-
2009
- 2009-02-06 FR FR0900514A patent/FR2941952B1/fr not_active Expired - Fee Related
-
2010
- 2010-02-04 MX MX2011008290A patent/MX2011008290A/es not_active Application Discontinuation
- 2010-02-04 EA EA201171012A patent/EA201171012A1/ru unknown
- 2010-02-04 CN CN2010800155638A patent/CN102369191A/zh active Pending
- 2010-02-04 MA MA34148A patent/MA33103B1/fr unknown
- 2010-02-04 SG SG2011056504A patent/SG173561A1/en unknown
- 2010-02-04 US US13/147,644 patent/US20120165326A1/en not_active Abandoned
- 2010-02-04 EP EP10708280A patent/EP2393793A1/fr not_active Withdrawn
- 2010-02-04 BR BRPI1008019A patent/BRPI1008019A2/pt not_active Application Discontinuation
- 2010-02-04 WO PCT/FR2010/050180 patent/WO2010089509A1/fr active Application Filing
- 2010-02-04 AU AU2010212234A patent/AU2010212234A1/en not_active Abandoned
- 2010-02-04 JP JP2011548753A patent/JP2012517410A/ja not_active Withdrawn
- 2010-02-04 CA CA2751474A patent/CA2751474A1/fr not_active Abandoned
- 2010-02-04 KR KR1020117020675A patent/KR20110126659A/ko not_active Application Discontinuation
- 2010-02-05 TW TW099103557A patent/TW201036977A/zh unknown
- 2010-02-05 UY UY0001032422A patent/UY32422A/es not_active Application Discontinuation
- 2010-02-05 AR ARP100100319A patent/AR075251A1/es unknown
-
2011
- 2011-08-02 IL IL214408A patent/IL214408A0/en unknown
- 2011-08-05 CO CO11099118A patent/CO6420339A2/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| TW201036977A (en) | 2010-10-16 |
| EP2393793A1 (fr) | 2011-12-14 |
| AR075251A1 (es) | 2011-03-16 |
| CA2751474A1 (fr) | 2010-08-12 |
| IL214408A0 (en) | 2011-09-27 |
| MX2011008290A (es) | 2011-11-04 |
| FR2941952A1 (fr) | 2010-08-13 |
| SG173561A1 (en) | 2011-09-29 |
| CO6420339A2 (es) | 2012-04-16 |
| MA33103B1 (fr) | 2012-03-01 |
| CN102369191A (zh) | 2012-03-07 |
| US20120165326A1 (en) | 2012-06-28 |
| WO2010089509A1 (fr) | 2010-08-12 |
| AU2010212234A1 (en) | 2011-08-25 |
| FR2941952B1 (fr) | 2011-04-01 |
| JP2012517410A (ja) | 2012-08-02 |
| BRPI1008019A2 (pt) | 2016-03-15 |
| KR20110126659A (ko) | 2011-11-23 |
| UY32422A (es) | 2010-09-30 |
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