TW201204735A - Inhibitors of protein tyrosine kinase activity - Google Patents
Inhibitors of protein tyrosine kinase activity Download PDFInfo
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- TW201204735A TW201204735A TW100112308A TW100112308A TW201204735A TW 201204735 A TW201204735 A TW 201204735A TW 100112308 A TW100112308 A TW 100112308A TW 100112308 A TW100112308 A TW 100112308A TW 201204735 A TW201204735 A TW 201204735A
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- Prior art keywords
- alkyl
- heterocyclyl
- group
- compound
- cvc6
- Prior art date
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- 230000000694 effects Effects 0.000 title claims abstract description 53
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 title abstract description 26
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 title abstract description 26
- 239000003112 inhibitor Substances 0.000 title description 12
- 150000001875 compounds Chemical class 0.000 claims abstract description 704
- 239000000203 mixture Substances 0.000 claims abstract description 118
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 109
- 201000010099 disease Diseases 0.000 claims abstract description 84
- 238000000034 method Methods 0.000 claims abstract description 66
- 230000005764 inhibitory process Effects 0.000 claims abstract description 31
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- 125000000217 alkyl group Chemical group 0.000 claims description 525
- 125000000623 heterocyclic group Chemical group 0.000 claims description 375
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- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims description 144
- 125000003118 aryl group Chemical group 0.000 claims description 134
- -1 _〇H Inorganic materials 0.000 claims description 133
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 131
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 claims description 118
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims description 101
- 125000001072 heteroaryl group Chemical group 0.000 claims description 99
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 91
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 75
- 150000003839 salts Chemical class 0.000 claims description 71
- 125000001424 substituent group Chemical group 0.000 claims description 63
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 62
- 125000001820 oxy group Chemical group [*:1]O[*:2] 0.000 claims description 53
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- 150000004677 hydrates Chemical class 0.000 claims description 36
- 230000002401 inhibitory effect Effects 0.000 claims description 36
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims description 35
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- 206010036790 Productive cough Diseases 0.000 claims description 7
- KJTLSVCANCCWHF-UHFFFAOYSA-N Ruthenium Chemical compound [Ru] KJTLSVCANCCWHF-UHFFFAOYSA-N 0.000 claims description 7
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Classifications
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/005—Enzyme inhibitors
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
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- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US32480310P | 2010-04-16 | 2010-04-16 |
Publications (1)
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| TW201204735A true TW201204735A (en) | 2012-02-01 |
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| TW100112307A TW201204734A (en) | 2010-04-16 | 2011-04-08 | Selected inhibitors of protein tyrosine kinase activity |
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Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105777776B (zh) * | 2007-08-29 | 2021-06-08 | 梅特希尔基因公司 | 蛋白酪氨酸激酶活性的抑制剂 |
| UA100262C2 (uk) * | 2008-03-05 | 2012-12-10 | Метилген Інк. | Інгібітори активності протеїнтирозинкінази |
| EP2563794A4 (en) * | 2010-04-16 | 2013-12-04 | Methylgene Inc | INHIBITORS OF PROTEIN TYROSINE KINASE ACTIVITY AND ITS USE FOR THE TREATMENT OF EYE DISEASES |
| US20130090327A1 (en) * | 2011-09-30 | 2013-04-11 | Methylgene Inc. | Inhibitors of Protein Tyrosine Kinase Activity |
| WO2013044361A1 (en) * | 2011-09-30 | 2013-04-04 | Methylgene Inc. | Inhibitors of protein tyrosine kinase activity |
| WO2013044362A1 (en) * | 2011-09-30 | 2013-04-04 | Methylgene Inc. | Selected inhibitors of protein tyrosine kinase activity |
| US9085517B2 (en) | 2011-12-15 | 2015-07-21 | Pfizer Limited | Sulfonamide derivatives |
| US10544117B2 (en) | 2014-09-10 | 2020-01-28 | Temple University—Of the Commonwealth System of Higher Education | 5-hydroxytryptamine receptor 7 activity modulators and their method of use |
| WO2016183150A1 (en) * | 2015-05-12 | 2016-11-17 | Temple University-Of The Commonwealth System Of Higher Education | Novel sigma-2 receptor binders and their method of use |
| JP6664170B2 (ja) * | 2015-08-31 | 2020-03-13 | 広栄化学工業株式会社 | アミノヒドロキシピリジン化合物の製造方法 |
| CN108530464B (zh) * | 2017-03-02 | 2020-10-27 | 深圳海王医药科技研究院有限公司 | 一种多靶点激酶抑制剂 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050020619A1 (en) * | 2003-07-24 | 2005-01-27 | Patrick Betschmann | Thienopyridine kinase inhibitors |
| CN101031570B (zh) * | 2004-07-30 | 2012-09-05 | 梅特希尔基因公司 | Vegf受体和hgf受体信号的抑制剂 |
| AU2006229343A1 (en) * | 2005-03-28 | 2006-10-05 | Kirin Pharma Kabushiki Kaisha | Thienopyridine derivative, or quinoline derivative, or quinazoline derivative, having c-Met autophosphorylation inhibiting potency |
| JO2787B1 (en) * | 2005-04-27 | 2014-03-15 | امجين إنك, | Alternative amide derivatives and methods of use |
| NZ563774A (en) * | 2005-05-20 | 2010-04-30 | Methylgene Inc | Inhibitors of VEGF receptor and HGF receptor signaling |
| KR101378716B1 (ko) * | 2005-05-20 | 2014-04-10 | 메틸진 인코포레이티드 | Ｖｅｇｆ 수용체 및 ｈｇｆ 수용체 신호전달의 억제제 |
| CN105777776B (zh) * | 2007-08-29 | 2021-06-08 | 梅特希尔基因公司 | 蛋白酪氨酸激酶活性的抑制剂 |
| ES2593279T3 (es) * | 2007-08-29 | 2016-12-07 | Methylgene Inc. | Procesos e intermedios para preparar inhibidores de cinasa heterocíclicos condensados |
| UA100262C2 (uk) * | 2008-03-05 | 2012-12-10 | Метилген Інк. | Інгібітори активності протеїнтирозинкінази |
| EP2563794A4 (en) * | 2010-04-16 | 2013-12-04 | Methylgene Inc | INHIBITORS OF PROTEIN TYROSINE KINASE ACTIVITY AND ITS USE FOR THE TREATMENT OF EYE DISEASES |
| WO2013044361A1 (en) * | 2011-09-30 | 2013-04-04 | Methylgene Inc. | Inhibitors of protein tyrosine kinase activity |
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2011
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- 2011-04-08 EP EP11768307.8A patent/EP2563795A4/en not_active Withdrawn
- 2011-04-08 AR ARP110101191A patent/AR080871A1/es unknown
- 2011-04-08 WO PCT/CA2011/000390 patent/WO2011127565A1/en not_active Ceased
- 2011-04-08 CA CA2796008A patent/CA2796008A1/en not_active Abandoned
- 2011-04-08 CN CN2011800297313A patent/CN102947315A/zh active Pending
- 2011-04-08 KR KR1020127030161A patent/KR20130058006A/ko not_active Withdrawn
- 2011-04-08 AU AU2011241422A patent/AU2011241422B2/en not_active Ceased
- 2011-04-08 CN CN201180029735.1A patent/CN103025740B/zh not_active Expired - Fee Related
- 2011-04-08 UA UAA201211687A patent/UA108878C2/ru unknown
- 2011-04-08 US US13/082,944 patent/US8455484B2/en not_active Expired - Fee Related
- 2011-04-08 JP JP2013504076A patent/JP2013525286A/ja not_active Ceased
- 2011-04-08 PH PH1/2012/502070A patent/PH12012502070A1/en unknown
- 2011-04-08 TW TW100112307A patent/TW201204734A/zh unknown
- 2011-04-08 EA EA201291055A patent/EA201291055A1/ru unknown
- 2011-04-08 TW TW100112308A patent/TW201204735A/zh unknown
- 2011-04-08 SG SG2012076733A patent/SG184883A1/en unknown
- 2011-04-08 AU AU2011241420A patent/AU2011241420B2/en not_active Ceased
- 2011-04-08 EA EA201291052A patent/EA201291052A1/ru unknown
- 2011-04-08 MX MX2012012032A patent/MX2012012032A/es not_active Application Discontinuation
- 2011-04-08 KR KR1020127029841A patent/KR20130100234A/ko not_active Withdrawn
- 2011-04-08 NZ NZ602954A patent/NZ602954A/en not_active IP Right Cessation
- 2011-04-08 PH PH1/2012/502073A patent/PH12012502073A1/en unknown
- 2011-04-08 WO PCT/CA2011/000394 patent/WO2011127567A1/en not_active Ceased
- 2011-04-08 NZ NZ602948A patent/NZ602948A/en not_active IP Right Cessation
- 2011-04-08 CA CA2796054A patent/CA2796054A1/en not_active Abandoned
- 2011-04-08 JP JP2013504075A patent/JP2013523846A/ja not_active Ceased
- 2011-04-08 US US13/082,923 patent/US8906852B2/en not_active Expired - Fee Related
- 2011-04-08 SG SG2012076725A patent/SG184882A1/en unknown
- 2011-04-08 AR ARP110101195A patent/AR080875A1/es unknown
- 2011-04-08 MX MX2012012031A patent/MX2012012031A/es active IP Right Grant
- 2011-04-08 MY MYPI2012004621A patent/MY157319A/en unknown
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2012
- 2012-10-05 ZA ZA2012/07482A patent/ZA201207482B/en unknown
- 2012-10-09 ZA ZA2012/07557A patent/ZA201207557B/en unknown
- 2012-11-15 CO CO12207310A patent/CO6630193A2/es active IP Right Grant
- 2012-11-15 CO CO12207317A patent/CO6640224A2/es active IP Right Grant
-
2014
- 2014-06-18 US US14/308,408 patent/US20140315801A1/en not_active Abandoned
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