JP2010519204A5 - - Google Patents
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- JP2010519204A5 JP2010519204A5 JP2009549625A JP2009549625A JP2010519204A5 JP 2010519204 A5 JP2010519204 A5 JP 2010519204A5 JP 2009549625 A JP2009549625 A JP 2009549625A JP 2009549625 A JP2009549625 A JP 2009549625A JP 2010519204 A5 JP2010519204 A5 JP 2010519204A5
- Authority
- JP
- Japan
- Prior art keywords
- independently
- compound
- aryl
- heteroaryl
- heterocycle
- 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.)
- Pending
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- 150000001875 compounds Chemical class 0.000 claims 59
- 125000003118 aryl group Chemical group 0.000 claims 26
- 125000001072 heteroaryl group Chemical group 0.000 claims 26
- 125000000623 heterocyclic group Chemical group 0.000 claims 23
- 125000000753 cycloalkyl group Chemical group 0.000 claims 15
- -1 heterocyclealkyl Chemical group 0.000 claims 15
- 239000008194 pharmaceutical composition Substances 0.000 claims 14
- 150000003839 salts Chemical class 0.000 claims 13
- 125000003710 aryl alkyl group Chemical group 0.000 claims 12
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 12
- 125000000217 alkyl group Chemical group 0.000 claims 10
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 10
- 125000004093 cyano group Chemical group *C#N 0.000 claims 9
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 9
- 241000124008 Mammalia Species 0.000 claims 8
- 125000005843 halogen group Chemical group 0.000 claims 8
- 125000001424 substituent group Chemical group 0.000 claims 8
- 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 7
- 125000003342 alkenyl group Chemical group 0.000 claims 7
- 125000000304 alkynyl group Chemical group 0.000 claims 7
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 6
- IOJUPLGTWVMSFF-UHFFFAOYSA-N benzothiazole Chemical compound C1=CC=C2SC=NC2=C1 IOJUPLGTWVMSFF-UHFFFAOYSA-N 0.000 claims 6
- 125000000259 cinnolinyl group Chemical group N1=NC(=CC2=CC=CC=C12)* 0.000 claims 6
- 125000004404 heteroalkyl group Chemical group 0.000 claims 6
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 6
- 125000001624 naphthyl group Chemical group 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 125000004193 piperazinyl group Chemical group 0.000 claims 6
- 125000004076 pyridyl group Chemical group 0.000 claims 6
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 229940079593 drug Drugs 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- KTZQTRPPVKQPFO-UHFFFAOYSA-N 1,2-benzoxazole Chemical compound C1=CC=C2C=NOC2=C1 KTZQTRPPVKQPFO-UHFFFAOYSA-N 0.000 claims 3
- BCMCBBGGLRIHSE-UHFFFAOYSA-N 1,3-benzoxazole Chemical compound C1=CC=C2OC=NC2=C1 BCMCBBGGLRIHSE-UHFFFAOYSA-N 0.000 claims 3
- QUKPALAWEPMWOS-UHFFFAOYSA-N 1h-pyrazolo[3,4-d]pyrimidine Chemical compound C1=NC=C2C=NNC2=N1 QUKPALAWEPMWOS-UHFFFAOYSA-N 0.000 claims 3
- JJTNLWSCFYERCK-UHFFFAOYSA-N 7h-pyrrolo[2,3-d]pyrimidine Chemical compound N1=CN=C2NC=CC2=C1 JJTNLWSCFYERCK-UHFFFAOYSA-N 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 230000001363 autoimmune Effects 0.000 claims 3
- 125000005334 azaindolyl group Chemical group N1N=C(C2=CC=CC=C12)* 0.000 claims 3
- 125000002393 azetidinyl group Chemical group 0.000 claims 3
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 3
- 125000000928 benzodioxinyl group Chemical group O1C(=COC2=C1C=CC=C2)* 0.000 claims 3
- 125000002047 benzodioxolyl group Chemical group O1OC(C2=C1C=CC=C2)* 0.000 claims 3
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 3
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 3
- 125000005433 dihydrobenzodioxinyl group Chemical group O1C(COC2=C1C=CC=C2)* 0.000 claims 3
- 125000005043 dihydropyranyl group Chemical group O1C(CCC=C1)* 0.000 claims 3
- 125000005044 dihydroquinolinyl group Chemical group N1(CC=CC2=CC=CC=C12)* 0.000 claims 3
- 125000002883 imidazolyl group Chemical group 0.000 claims 3
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 3
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims 3
- 125000001041 indolyl group Chemical group 0.000 claims 3
- 125000001786 isothiazolyl group Chemical group 0.000 claims 3
- 125000000842 isoxazolyl group Chemical group 0.000 claims 3
- 125000002757 morpholinyl group Chemical group 0.000 claims 3
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 claims 3
- 125000002971 oxazolyl group Chemical group 0.000 claims 3
- 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 claims 3
- 125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 claims 3
- 125000003373 pyrazinyl group Chemical group 0.000 claims 3
- 125000003226 pyrazolyl group Chemical group 0.000 claims 3
- 125000002098 pyridazinyl group Chemical group 0.000 claims 3
- 125000005494 pyridonyl group Chemical group 0.000 claims 3
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 3
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims 3
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims 3
- 125000000335 thiazolyl group Chemical group 0.000 claims 3
- 125000001544 thienyl group Chemical group 0.000 claims 3
- 125000001425 triazolyl group Chemical group 0.000 claims 3
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 2
- 125000006586 (C3-C10) cycloalkylene group Chemical group 0.000 claims 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- 206010012438 Dermatitis atopic Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 125000004450 alkenylene group Chemical group 0.000 claims 2
- 125000004419 alkynylene group Chemical group 0.000 claims 2
- 201000008937 atopic dermatitis Diseases 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 208000010247 contact dermatitis Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 201000005962 mycosis fungoides Diseases 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 2
- 125000000547 substituted alkyl group Chemical group 0.000 claims 2
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 2
- 208000026872 Addison Disease Diseases 0.000 claims 1
- 208000035285 Allergic Seasonal Rhinitis Diseases 0.000 claims 1
- 201000004384 Alopecia Diseases 0.000 claims 1
- 208000023328 Basedow disease Diseases 0.000 claims 1
- 208000009137 Behcet syndrome Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 201000004624 Dermatitis Diseases 0.000 claims 1
- 206010012442 Dermatitis contact Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 108010068370 Glutens Proteins 0.000 claims 1
- 208000003807 Graves Disease Diseases 0.000 claims 1
- 208000035895 Guillain-Barré syndrome Diseases 0.000 claims 1
- 206010021067 Hypopituitarism Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 102000014150 Interferons Human genes 0.000 claims 1
- 108010050904 Interferons Proteins 0.000 claims 1
- 208000000185 Localized scleroderma Diseases 0.000 claims 1
- 206010049567 Miller Fisher syndrome Diseases 0.000 claims 1
- 208000031845 Pernicious anaemia Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 1
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 1
- 206010037575 Pustular psoriasis Diseases 0.000 claims 1
- 206010063837 Reperfusion injury Diseases 0.000 claims 1
- 206010039085 Rhinitis allergic Diseases 0.000 claims 1
- 208000009359 Sezary Syndrome Diseases 0.000 claims 1
- 208000021388 Sezary disease Diseases 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 201000009594 Systemic Scleroderma Diseases 0.000 claims 1
- 206010042953 Systemic sclerosis Diseases 0.000 claims 1
- 230000006044 T cell activation Effects 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 208000024780 Urticaria Diseases 0.000 claims 1
- 206010047642 Vitiligo Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 229940100198 alkylating agent Drugs 0.000 claims 1
- 239000002168 alkylating agent Substances 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 201000010105 allergic rhinitis Diseases 0.000 claims 1
- 231100000360 alopecia Toxicity 0.000 claims 1
- 208000004631 alopecia areata Diseases 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 230000000340 anti-metabolite Effects 0.000 claims 1
- 229940100197 antimetabolite Drugs 0.000 claims 1
- 239000002256 antimetabolite Substances 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 230000003115 biocidal effect Effects 0.000 claims 1
- 230000017531 blood circulation Effects 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 208000025302 chronic primary adrenal insufficiency Diseases 0.000 claims 1
- 230000003111 delayed effect Effects 0.000 claims 1
- 201000001981 dermatomyositis Diseases 0.000 claims 1
- 238000002059 diagnostic imaging Methods 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 235000021312 gluten Nutrition 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 229940088597 hormone Drugs 0.000 claims 1
- 239000005556 hormone Substances 0.000 claims 1
- 229940124452 immunizing agent Drugs 0.000 claims 1
- 230000006698 induction Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 229940079322 interferon Drugs 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 208000037906 ischaemic injury Diseases 0.000 claims 1
- 230000000302 ischemic effect Effects 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 201000008383 nephritis Diseases 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 208000017983 photosensitivity disease Diseases 0.000 claims 1
- 201000010914 pustulosis of palm and sole Diseases 0.000 claims 1
- 208000011797 pustulosis palmaris et plantaris Diseases 0.000 claims 1
- 208000009954 pyoderma gangrenosum Diseases 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 210000002966 serum Anatomy 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 208000005057 thyrotoxicosis Diseases 0.000 claims 1
- 238000002054 transplantation Methods 0.000 claims 1
- AEWDLXUAHPHIPM-UHFFFAOYSA-N COc1cc2nccc(OCCN(C(C=C3)=O)N=C3c(cc3)ccc3F)c2cc1 Chemical compound COc1cc2nccc(OCCN(C(C=C3)=O)N=C3c(cc3)ccc3F)c2cc1 AEWDLXUAHPHIPM-UHFFFAOYSA-N 0.000 description 1
- WVXAYXKCTSNEDD-UHFFFAOYSA-N COc1cc2nccc(OCCN(C(C=C3)=O)N=C3c(cc3F)cc(F)c3F)c2cc1 Chemical compound COc1cc2nccc(OCCN(C(C=C3)=O)N=C3c(cc3F)cc(F)c3F)c2cc1 WVXAYXKCTSNEDD-UHFFFAOYSA-N 0.000 description 1
- JPNCSUACTCRKEU-UHFFFAOYSA-N COc1cc2nccc(OCCN(C(C=C3)=O)N=C3c3cc4ccccc4[s]3)c2cc1 Chemical compound COc1cc2nccc(OCCN(C(C=C3)=O)N=C3c3cc4ccccc4[s]3)c2cc1 JPNCSUACTCRKEU-UHFFFAOYSA-N 0.000 description 1
- POWQKVGHPULXHD-UHFFFAOYSA-N C[n]1ncc(C(C=C2)=NN(CCOc3c(ccc(OC)c4)c4ncc3)C2=O)c1 Chemical compound C[n]1ncc(C(C=C2)=NN(CCOc3c(ccc(OC)c4)c4ncc3)C2=O)c1 POWQKVGHPULXHD-UHFFFAOYSA-N 0.000 description 1
- LVPPGKJARBYRFE-UHFFFAOYSA-N Cc1cc(C(C=C2)=NN(CCOc3c(ccc(OC)c4)c4ncc3)C2=O)ncc1 Chemical compound Cc1cc(C(C=C2)=NN(CCOc3c(ccc(OC)c4)c4ncc3)C2=O)ncc1 LVPPGKJARBYRFE-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US90203007P | 2007-02-16 | 2007-02-16 | |
| PCT/US2008/002007 WO2008103277A2 (en) | 2007-02-16 | 2008-02-15 | Nitrogen-containing heterocyclyl ketones and their use as c-met inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010519204A JP2010519204A (ja) | 2010-06-03 |
| JP2010519204A5 true JP2010519204A5 (enExample) | 2012-04-05 |
Family
ID=39563458
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009549625A Pending JP2010519204A (ja) | 2007-02-16 | 2008-02-15 | 窒素含有複素環ケトン類およびそれらのc−Met阻害薬としての使用 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US8314087B2 (enExample) |
| EP (1) | EP2114898A2 (enExample) |
| JP (1) | JP2010519204A (enExample) |
| AU (1) | AU2008219166B2 (enExample) |
| CA (1) | CA2676173A1 (enExample) |
| MX (1) | MX2009008531A (enExample) |
| WO (1) | WO2008103277A2 (enExample) |
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| DE102008019907A1 (de) * | 2008-04-21 | 2009-10-22 | Merck Patent Gmbh | Pyridazinonderivate |
| EP2296653B1 (en) | 2008-06-03 | 2016-01-27 | Intermune, Inc. | Compounds and methods for treating inflammatory and fibrotic disorders |
| EP2660239B1 (en) | 2008-07-25 | 2016-11-23 | VIIV Healthcare Company | Chemical compounds as synthetic intermediates |
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| JP5836367B2 (ja) | 2010-05-12 | 2015-12-24 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | Atrキナーゼ阻害剤として有用な化合物 |
| CA2841142C (en) | 2010-06-23 | 2020-12-15 | Ryan D. Morin | Biomarkers for non-hodgkin lymphomas and uses thereof |
| JP2013529643A (ja) | 2010-06-23 | 2013-07-22 | バーテックス ファーマシューティカルズ インコーポレイテッド | Atrキナーゼ阻害剤として有用なピロロピラジン誘導体 |
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| EP2776429A1 (en) | 2011-11-09 | 2014-09-17 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
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| UA112897C2 (uk) | 2012-05-09 | 2016-11-10 | Байєр Фарма Акцієнгезелльшафт | Біциклічно заміщені урацили та їх застосування для лікування і/або профілактики захворювань |
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