JP2013526609A5 - - Google Patents
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- JP2013526609A5 JP2013526609A5 JP2013512166A JP2013512166A JP2013526609A5 JP 2013526609 A5 JP2013526609 A5 JP 2013526609A5 JP 2013512166 A JP2013512166 A JP 2013512166A JP 2013512166 A JP2013512166 A JP 2013512166A JP 2013526609 A5 JP2013526609 A5 JP 2013526609A5
- Authority
- JP
- Japan
- Prior art keywords
- compound according
- alkyl
- optionally substituted
- halogen
- hydroxy
- 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.)
- Granted
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- 150000001875 compounds Chemical class 0.000 claims description 65
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 42
- 125000001424 substituent group Chemical group 0.000 claims description 27
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 24
- 229910052736 halogen Inorganic materials 0.000 claims description 23
- 150000002367 halogens Chemical class 0.000 claims description 23
- 125000000217 alkyl group Chemical group 0.000 claims description 22
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 22
- 201000010099 disease Diseases 0.000 claims description 20
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 19
- 208000035475 disorder Diseases 0.000 claims description 18
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 16
- 125000003545 alkoxy group Chemical group 0.000 claims description 15
- 125000001188 haloalkyl group Chemical group 0.000 claims description 15
- 150000001408 amides Chemical class 0.000 claims description 14
- -1 pyrrolopyridinyl Chemical group 0.000 claims description 14
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 13
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 12
- 229910052805 deuterium Inorganic materials 0.000 claims description 12
- 239000003814 drug Substances 0.000 claims description 10
- 125000001072 heteroaryl group Chemical group 0.000 claims description 9
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims description 8
- 230000001404 mediated effect Effects 0.000 claims description 8
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 7
- 229910052799 carbon Inorganic materials 0.000 claims description 7
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 7
- 229910052731 fluorine Inorganic materials 0.000 claims description 7
- 239000011737 fluorine Substances 0.000 claims description 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 7
- 206010061218 Inflammation Diseases 0.000 claims description 6
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 6
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 6
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 6
- 230000004054 inflammatory process Effects 0.000 claims description 6
- 230000002093 peripheral effect Effects 0.000 claims description 6
- 229940124597 therapeutic agent Drugs 0.000 claims description 6
- 206010020772 Hypertension Diseases 0.000 claims description 5
- 230000006378 damage Effects 0.000 claims description 5
- 125000001041 indolyl group Chemical group 0.000 claims description 5
- 201000001119 neuropathy Diseases 0.000 claims description 5
- 230000007823 neuropathy Effects 0.000 claims description 5
- 208000033808 peripheral neuropathy Diseases 0.000 claims description 5
- 150000003839 salts Chemical class 0.000 claims description 5
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims description 4
- 208000024827 Alzheimer disease Diseases 0.000 claims description 4
- 201000001320 Atherosclerosis Diseases 0.000 claims description 4
- 206010007558 Cardiac failure chronic Diseases 0.000 claims description 4
- 206010011878 Deafness Diseases 0.000 claims description 4
- 208000008960 Diabetic foot Diseases 0.000 claims description 4
- 208000032928 Dyslipidaemia Diseases 0.000 claims description 4
- 201000005569 Gout Diseases 0.000 claims description 4
- 206010060378 Hyperinsulinaemia Diseases 0.000 claims description 4
- 201000001431 Hyperuricemia Diseases 0.000 claims description 4
- 206010022489 Insulin Resistance Diseases 0.000 claims description 4
- 208000017170 Lipid metabolism disease Diseases 0.000 claims description 4
- 208000001145 Metabolic Syndrome Diseases 0.000 claims description 4
- 206010028980 Neoplasm Diseases 0.000 claims description 4
- 208000008589 Obesity Diseases 0.000 claims description 4
- 206010030113 Oedema Diseases 0.000 claims description 4
- 208000017442 Retinal disease Diseases 0.000 claims description 4
- 206010038923 Retinopathy Diseases 0.000 claims description 4
- 208000025865 Ulcer Diseases 0.000 claims description 4
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 4
- 206010012601 diabetes mellitus Diseases 0.000 claims description 4
- 230000010370 hearing loss Effects 0.000 claims description 4
- 231100000888 hearing loss Toxicity 0.000 claims description 4
- 208000016354 hearing loss disease Diseases 0.000 claims description 4
- 208000006454 hepatitis Diseases 0.000 claims description 4
- 231100000283 hepatitis Toxicity 0.000 claims description 4
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 4
- 201000001421 hyperglycemia Diseases 0.000 claims description 4
- 230000003451 hyperinsulinaemic effect Effects 0.000 claims description 4
- 201000008980 hyperinsulinism Diseases 0.000 claims description 4
- 208000017169 kidney disease Diseases 0.000 claims description 4
- 238000004519 manufacturing process Methods 0.000 claims description 4
- 235000020824 obesity Nutrition 0.000 claims description 4
- 229910052760 oxygen Inorganic materials 0.000 claims description 4
- 208000028173 post-traumatic stress disease Diseases 0.000 claims description 4
- 229910052717 sulfur Inorganic materials 0.000 claims description 4
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 4
- 231100000397 ulcer Toxicity 0.000 claims description 4
- 208000018737 Parkinson disease Diseases 0.000 claims description 3
- 208000030886 Traumatic Brain injury Diseases 0.000 claims description 3
- 125000003118 aryl group Chemical group 0.000 claims description 3
- 125000004432 carbon atom Chemical group C* 0.000 claims description 3
- 230000003291 dopaminomimetic effect Effects 0.000 claims description 3
- 230000004770 neurodegeneration Effects 0.000 claims description 3
- 230000037361 pathway Effects 0.000 claims description 3
- 230000009529 traumatic brain injury Effects 0.000 claims description 3
- 208000023275 Autoimmune disease Diseases 0.000 claims description 2
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims description 2
- 208000020925 Bipolar disease Diseases 0.000 claims description 2
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims description 2
- 206010011903 Deafness traumatic Diseases 0.000 claims description 2
- OHLUUHNLEMFGTQ-UHFFFAOYSA-N N-methylacetamide Chemical compound CNC(C)=O OHLUUHNLEMFGTQ-UHFFFAOYSA-N 0.000 claims description 2
- 208000002946 Noise-Induced Hearing Loss Diseases 0.000 claims description 2
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims description 2
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims description 2
- 229910052801 chlorine Inorganic materials 0.000 claims description 2
- 239000000460 chlorine Substances 0.000 claims description 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 2
- 208000016097 disease of metabolism Diseases 0.000 claims description 2
- 210000003027 ear inner Anatomy 0.000 claims description 2
- SCMLRESZJCKCTC-KMYQRJGFSA-N gtpl8173 Chemical group C12=CC=C(CSCC)C=C2C2=C(CNC3=O)C3=C3C4=CC(CSCC)=CC=C4N4C3=C2N1[C@]1(C)[C@@](O)(C(=O)OC)C[C@H]4O1 SCMLRESZJCKCTC-KMYQRJGFSA-N 0.000 claims description 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims description 2
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims description 2
- 208000027866 inflammatory disease Diseases 0.000 claims description 2
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims description 2
- 208000030159 metabolic disease Diseases 0.000 claims description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 2
- 229910052757 nitrogen Inorganic materials 0.000 claims description 2
- 125000004193 piperazinyl group Chemical group 0.000 claims description 2
- 208000020016 psychiatric disease Diseases 0.000 claims description 2
- 125000004076 pyridyl group Chemical group 0.000 claims description 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims description 2
- 231100000331 toxic Toxicity 0.000 claims description 2
- 230000002588 toxic effect Effects 0.000 claims description 2
- 125000004103 aminoalkyl group Chemical group 0.000 claims 2
- 208000006011 Stroke Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 125000003368 amide group Chemical group 0.000 claims 1
- 230000006735 deficit Effects 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- QJQAMHYHNCADNR-UHFFFAOYSA-N n-methylpropanamide Chemical compound CCC(=O)NC QJQAMHYHNCADNR-UHFFFAOYSA-N 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 238000000034 method Methods 0.000 description 34
- 102100025184 Mitogen-activated protein kinase kinase kinase 13 Human genes 0.000 description 10
- 210000004027 cell Anatomy 0.000 description 10
- 230000000694 effects Effects 0.000 description 6
- 230000001629 suppression Effects 0.000 description 6
- 101001005602 Homo sapiens Mitogen-activated protein kinase kinase kinase 11 Proteins 0.000 description 4
- 102100025207 Mitogen-activated protein kinase kinase kinase 11 Human genes 0.000 description 4
- 230000004083 survival effect Effects 0.000 description 4
- 230000005764 inhibitory process Effects 0.000 description 3
- 208000028389 Nerve injury Diseases 0.000 description 2
- 208000036110 Neuroinflammatory disease Diseases 0.000 description 2
- 208000027418 Wounds and injury Diseases 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- 230000005907 cancer growth Effects 0.000 description 2
- 230000006870 function Effects 0.000 description 2
- 210000002064 heart cell Anatomy 0.000 description 2
- 210000003494 hepatocyte Anatomy 0.000 description 2
- 210000002865 immune cell Anatomy 0.000 description 2
- 230000005931 immune cell recruitment Effects 0.000 description 2
- 230000006872 improvement Effects 0.000 description 2
- 208000014674 injury Diseases 0.000 description 2
- 210000002540 macrophage Anatomy 0.000 description 2
- 210000000274 microglia Anatomy 0.000 description 2
- 210000001616 monocyte Anatomy 0.000 description 2
- 230000008764 nerve damage Effects 0.000 description 2
- 210000000653 nervous system Anatomy 0.000 description 2
- 230000004766 neurogenesis Effects 0.000 description 2
- 230000003959 neuroinflammation Effects 0.000 description 2
- 230000002265 prevention Effects 0.000 description 2
- 230000035755 proliferation Effects 0.000 description 2
- 230000001737 promoting effect Effects 0.000 description 2
- 230000009467 reduction Effects 0.000 description 2
- 230000002207 retinal effect Effects 0.000 description 2
- 229940124834 selective serotonin reuptake inhibitor Drugs 0.000 description 2
- 239000012896 selective serotonin reuptake inhibitor Substances 0.000 description 2
- 210000000225 synapse Anatomy 0.000 description 2
- 230000001720 vestibular Effects 0.000 description 2
- 0 *c(c1c2)c[n]c1ncc2-c1ccc(CN(CC2)CC*2[Rh])cc1 Chemical compound *c(c1c2)c[n]c1ncc2-c1ccc(CN(CC2)CC*2[Rh])cc1 0.000 description 1
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 description 1
- 208000027626 Neurocognitive disease Diseases 0.000 description 1
- 108091000080 Phosphotransferase Proteins 0.000 description 1
- 230000009692 acute damage Effects 0.000 description 1
- 125000003710 aryl alkyl group Chemical group 0.000 description 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 description 1
- 229910052739 hydrogen Inorganic materials 0.000 description 1
- 150000002431 hydrogen Chemical class 0.000 description 1
- 239000001257 hydrogen Substances 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- WFKAJVHLWXSISD-UHFFFAOYSA-N isobutyramide Chemical compound CC(C)C(N)=O WFKAJVHLWXSISD-UHFFFAOYSA-N 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 125000006578 monocyclic heterocycloalkyl group Chemical group 0.000 description 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 description 1
- 210000005036 nerve Anatomy 0.000 description 1
- 230000001537 neural effect Effects 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 102000020233 phosphotransferase Human genes 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 230000003977 synaptic function Effects 0.000 description 1
- 230000000007 visual effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US34769410P | 2010-05-24 | 2010-05-24 | |
| US61/347,694 | 2010-05-24 | ||
| PCT/US2011/037758 WO2011149950A2 (en) | 2010-05-24 | 2011-05-24 | Bicyclic heteroaryl kinase inhibitors and methods of use |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013526609A JP2013526609A (ja) | 2013-06-24 |
| JP2013526609A5 true JP2013526609A5 (OSRAM) | 2014-07-10 |
| JP6086326B2 JP6086326B2 (ja) | 2017-03-01 |
Family
ID=45004716
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013512166A Active JP6086326B2 (ja) | 2010-05-24 | 2011-05-24 | 二環式ヘテロアリールキナーゼ阻害剤および使用方法 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US8846909B2 (OSRAM) |
| EP (1) | EP2576549A4 (OSRAM) |
| JP (1) | JP6086326B2 (OSRAM) |
| CN (1) | CN103153994B (OSRAM) |
| AU (1) | AU2011258465B2 (OSRAM) |
| CA (1) | CA2800176C (OSRAM) |
| NZ (1) | NZ603644A (OSRAM) |
| WO (1) | WO2011149950A2 (OSRAM) |
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| JP5930278B2 (ja) | 2008-11-25 | 2016-06-08 | ユニバーシティー オブ ロチェスター | Ｍｌｋ阻害剤および使用方法 |
| CA2800176C (en) | 2010-05-24 | 2018-08-28 | University Of Rochester | Bicyclic heteroaryl kinase inhibitors and methods of use |
| SG186820A1 (en) | 2010-07-02 | 2013-02-28 | Gilead Sciences Inc | Napht- 2 -ylacetic acid derivatives to treat aids |
| BR112012033689A2 (pt) | 2010-07-02 | 2019-09-24 | Gilead Sciences Inc | derivados de ácido 2-quinolinil-acético como compostos de hiv antivirais |
| DE102011009961A1 (de) * | 2011-02-01 | 2012-08-02 | Merck Patent Gmbh | 7-Azaindolderivate |
| ES2615734T3 (es) | 2011-04-21 | 2017-06-08 | Gilead Sciences, Inc. | Compuestos de benzotiazol y su uso farmacéutico |
| WO2013042139A1 (en) | 2011-09-23 | 2013-03-28 | Advinus Therapeutics Limited | Amide compounds, compositions and applications thereof |
| US9376392B2 (en) | 2012-01-04 | 2016-06-28 | Gilead Sciences, Inc. | 2-(tert-butoxy)-2-(7-methylquinolin-6-yl) acetic acid derivatives for treating AIDS |
| US9284323B2 (en) | 2012-01-04 | 2016-03-15 | Gilead Sciences, Inc. | Naphthalene acetic acid derivatives against HIV infection |
| CN102627646A (zh) * | 2012-03-19 | 2012-08-08 | 苏州四同医药科技有限公司 | 一种3-碘-5-溴-4,7-二氮杂吲哚的制备方法 |
| MX2014005002A (es) | 2012-04-20 | 2014-07-09 | Gilead Sciences Inc | Derivados de acido benzotiazol-6-il acetico y su uso para tratar una infeccion por vih. |
| EP2844658B1 (en) * | 2012-05-03 | 2019-03-20 | Genentech, Inc. | Pyrazole aminopyrimidine derivatives as lrrk2 modulators for use in the treatment of parkinson's disease |
| MX2015004615A (es) * | 2012-10-16 | 2015-07-17 | Hoffmann La Roche | Inhibidores de serina/treonina cinasa. |
| US10485800B2 (en) | 2012-11-30 | 2019-11-26 | The University Of Rochester | Mixed lineage kinase inhibitors for HIV/AIDS therapies |
| FR2999575A1 (fr) * | 2012-12-18 | 2014-06-20 | Centre Nat Rech Scient | 3,5-diaryl-azaindoles comme inhibiteurs de la proteine dyrk1a pour le traitement des deficiences cognitives liees au syndrome de down et a la maladie d'alzheimer |
| TWI498325B (zh) * | 2013-01-18 | 2015-09-01 | Hoffmann La Roche | ３－取代吡唑及其用途 |
| MA42164B1 (fr) | 2013-05-01 | 2019-12-31 | Hoffmann La Roche | Composes biheteroaryle et leurs utilisations |
| MX2016008110A (es) | 2013-12-20 | 2016-08-19 | Hoffmann La Roche | Derivados de pirazol como inhibidores de la cinasa de cremallera de leucina dual (dlk) y usos de los mismos. |
| CN104478909B (zh) * | 2014-11-19 | 2017-01-04 | 上海泰坦科技股份有限公司 | 杂环硼酸类化合物的合成工艺 |
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| CN105859761B (zh) * | 2016-04-26 | 2018-06-26 | 丽水学院 | 一种芳香硼酸酯化合物合成方法 |
| US10577365B2 (en) * | 2016-12-23 | 2020-03-03 | Felicitex Therapeutics, Inc. | Derivatives of quinoline as inhibitors of DYRK1A and/or DYRK1B kinases |
| EP3759072A4 (en) | 2018-03-01 | 2021-11-03 | The Trustees of Columbia University in the City of New York | COMPOUNDS, COMPOSITIONS AND METHODS FOR RELATING TOXIC STRESS FROM ENDOPLASMIC RETICULUM |
| CN113015526A (zh) | 2018-09-19 | 2021-06-22 | 豪夫迈·罗氏有限公司 | 螺环2,3-二氢-7-氮杂吲哚化合物及其用途 |
| WO2020103896A1 (en) * | 2018-11-22 | 2020-05-28 | Beigene, Ltd. | Pyrrolo[2,3-b]pyridines as hpk1 inhibitor and uses thereof |
| TWI848141B (zh) | 2019-07-04 | 2024-07-11 | 英屬開曼群島商百濟神州有限公司 | 及其用途 |
| TW202116771A (zh) | 2019-07-17 | 2021-05-01 | 英屬開曼群島商百濟神州有限公司 | 作為ｈｐｋ１抑制劑之三環化合物及其用途 |
| US11560366B2 (en) * | 2019-10-21 | 2023-01-24 | Board Of Regents, The University Of Texas System | Bicyclo[1.1.1]pentane inhibitors of dual leucine zipper (DLK) kinase for the treatment of disease |
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| WO2022228365A1 (zh) * | 2021-04-27 | 2022-11-03 | 南京明德新药研发有限公司 | 六元杂芳并脲环的衍生物及其应用 |
| WO2022243649A1 (fr) * | 2021-05-21 | 2022-11-24 | Centre National De La Recherche Scientifique (Cnrs) | Nouveaux derives azaindole en tant qu'agents anticancereux |
| WO2023064218A1 (en) * | 2021-10-11 | 2023-04-20 | Halia Therapeutics, Inc. | Tyro3 inhibitors |
| US11661409B1 (en) | 2022-01-31 | 2023-05-30 | Pioneura Corporation | Acid addition salts, compositions, and methods of treating |
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| CN118126036A (zh) * | 2022-12-01 | 2024-06-04 | 复旦大学 | 7-氮杂吲哚类化合物及其制备方法和应用 |
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-
2011
- 2011-05-24 CA CA2800176A patent/CA2800176C/en active Active
- 2011-05-24 JP JP2013512166A patent/JP6086326B2/ja active Active
- 2011-05-24 EP EP11787254.9A patent/EP2576549A4/en not_active Withdrawn
- 2011-05-24 US US13/698,829 patent/US8846909B2/en active Active
- 2011-05-24 CN CN201180036376.2A patent/CN103153994B/zh active Active
- 2011-05-24 AU AU2011258465A patent/AU2011258465B2/en active Active
- 2011-05-24 WO PCT/US2011/037758 patent/WO2011149950A2/en not_active Ceased
- 2011-05-24 NZ NZ603644A patent/NZ603644A/en unknown
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