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
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- 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 (enExample) | 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 (enExample) |
| EP (1) | EP2576549A4 (enExample) |
| JP (1) | JP6086326B2 (enExample) |
| CN (1) | CN103153994B (enExample) |
| AU (1) | AU2011258465B2 (enExample) |
| CA (1) | CA2800176C (enExample) |
| NZ (1) | NZ603644A (enExample) |
| WO (1) | WO2011149950A2 (enExample) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8877772B2 (en) | 2008-11-25 | 2014-11-04 | University Of Rochester | Substituted pyrrolo[2,3-B]pyridines as MLK inhibitors |
| WO2011149950A2 (en) | 2010-05-24 | 2011-12-01 | University Of Rochester | Bicyclic heteroaryl kinase inhibitors and methods of use |
| US9102614B2 (en) | 2010-07-02 | 2015-08-11 | Gilead Sciences, Inc. | Naphth-2-ylacetic acid derivatives to treat AIDS |
| WO2012003498A1 (en) | 2010-07-02 | 2012-01-05 | Gilead Sciences, Inc. | 2 -quinolinyl- acetic acid derivatives as hiv antiviral compounds |
| DE102011009961A1 (de) * | 2011-02-01 | 2012-08-02 | Merck Patent Gmbh | 7-Azaindolderivate |
| PE20141066A1 (es) | 2011-04-21 | 2014-09-05 | Gilead Sciences Inc | Compuestos de benzotiazol |
| JP2014527981A (ja) | 2011-09-23 | 2014-10-23 | アドヴィナス・セラピューティックス・リミテッド | アミド化合物、組成物およびその用途 |
| 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 |
| WO2013103738A1 (en) | 2012-01-04 | 2013-07-11 | Gilead Sciences, Inc. | Napthalene 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 |
| PH12014500842A1 (en) | 2012-04-20 | 2014-06-09 | Gilead Sciences Inc | Benzothiazol-6-yl acetic acid derivatives and their use for treating an hiv infection |
| KR102091895B1 (ko) * | 2012-05-03 | 2020-04-14 | 제넨테크, 인크. | 파킨슨병의 치료에 사용하기 위한 lrrk2 조절제로서의 피라졸 아미노피리미딘 유도체 |
| JP2015533151A (ja) * | 2012-10-16 | 2015-11-19 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | セリン／スレオニンキナーゼ阻害剤 |
| WO2014085795A1 (en) | 2012-11-30 | 2014-06-05 | 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 |
| SG10201707002VA (en) | 2013-05-01 | 2017-10-30 | Hoffmann La Roche | Biheteroaryl compounds and uses thereof |
| 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 |
| GB201509893D0 (en) * | 2015-06-08 | 2015-07-22 | Ucb Biopharma Sprl | Therapeutic agents |
| EP3383875B1 (en) * | 2015-11-30 | 2022-02-09 | Council Of Scientific & Industrial Research | 3-pyrimidinyl pyrrolo [2,3-b] pyridine as anticancer agents and the process for the preparation thereof |
| 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 |
| EP4183786A1 (en) * | 2016-12-23 | 2023-05-24 | Felicitex Therapeutics, Inc. | Derivatives of quinolines 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 |
| CN113166139A (zh) * | 2018-11-22 | 2021-07-23 | 百济神州有限公司 | 作为HPK1抑制剂的吡咯并[2,3-b]吡啶及其用途 |
| 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 |
| WO2021013083A1 (en) | 2019-07-17 | 2021-01-28 | Beigene, Ltd. | Tricyclic compounds as hpk1 inhibitor and the use thereof |
| 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 |
| US20250041451A1 (en) * | 2021-04-06 | 2025-02-06 | Perceive Biotherapeutics, Inc. | Gene therapy for hearing loss |
| 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 |
| US11479541B1 (en) | 2022-01-31 | 2022-10-25 | Pioneura Corporation | Acid addition salts, compositions, and methods of treating thereof |
| 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 |
| WO2025229111A1 (en) | 2024-05-01 | 2025-11-06 | Basf Se | Pyrimidinone derivatives as pesticidal compounds |
Family Cites Families (68)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4933438A (en) | 1984-02-29 | 1990-06-12 | University Of Florida | Brain-specific analogues of centrally acting amines |
| US6150354A (en) | 1987-01-15 | 2000-11-21 | Bonnie Davis | Compounds for the treatment of Alzheimer's disease |
| US5133974A (en) | 1989-05-05 | 1992-07-28 | Kv Pharmaceutical Company | Extended release pharmaceutical formulations |
| EP0584185B1 (en) | 1991-05-14 | 1999-08-11 | Ernir Snorrason | Treatment of fatigue syndrome with cholinesterase inhibitors |
| IT1250421B (it) | 1991-05-30 | 1995-04-07 | Recordati Chem Pharm | Composizione farmaceutica a rilascio controllato con proprieta' bio-adesive. |
| US6537579B1 (en) | 1993-02-22 | 2003-03-25 | American Bioscience, Inc. | Compositions and methods for administration of pharmacologically active compounds |
| FR2710265B1 (fr) | 1993-09-22 | 1995-10-20 | Adir | Composition pharmaceutique bioadhésive pour la libération contrôlée de principes actifs. |
| US5618819A (en) | 1994-07-07 | 1997-04-08 | Adir Et Compagnie | 1,3-dihydro-2H-pyrrolo[2,3-b]pyridin-2-one and oxazolo[4,5-b]pyridin-2-(3H)-one compounds |
| US6548084B2 (en) | 1995-07-20 | 2003-04-15 | Smithkline Beecham Plc | Controlled release compositions |
| US6245347B1 (en) | 1995-07-28 | 2001-06-12 | Zars, Inc. | Methods and apparatus for improved administration of pharmaceutically active compounds |
| DE19541260A1 (de) | 1995-11-06 | 1997-05-07 | Lohmann Therapie Syst Lts | Therapeutische Zubereitung zur transdermalen Applikation von Wirkstoffen durch die Haut |
| US6512010B1 (en) | 1996-07-15 | 2003-01-28 | Alza Corporation | Formulations for the administration of fluoxetine |
| CN1277550A (zh) | 1997-09-11 | 2000-12-20 | 尼科梅德丹麦有限公司 | 非甾体抗炎药物(NSAIDs)的改进释放的复合型组合物 |
| US6624200B2 (en) | 1998-08-25 | 2003-09-23 | Columbia Laboratories, Inc. | Bioadhesive progressive hydration tablets |
| GB9721437D0 (en) | 1997-10-10 | 1997-12-10 | Glaxo Group Ltd | Heteroaromatic compounds and their use in medicine |
| US6607751B1 (en) | 1997-10-10 | 2003-08-19 | Intellipharamaceutics Corp. | Controlled release delivery device for pharmaceutical agents incorporating microbial polysaccharide gum |
| US6403597B1 (en) | 1997-10-28 | 2002-06-11 | Vivus, Inc. | Administration of phosphodiesterase inhibitors for the treatment of premature ejaculation |
| US6248864B1 (en) | 1997-12-31 | 2001-06-19 | Adherex Technologies, Inc. | Compounds and methods and modulating tissue permeability |
| US6613358B2 (en) | 1998-03-18 | 2003-09-02 | Theodore W. Randolph | Sustained-release composition including amorphous polymer |
| US6312717B1 (en) | 1998-07-07 | 2001-11-06 | Bristol-Myers Squibb Company | Method for treatment of anxiety and depression |
| US20020009478A1 (en) | 1998-08-24 | 2002-01-24 | Douglas Joseph Dobrozsi | Oral liquid mucoadhesive compositions |
| SE9802864D0 (sv) | 1998-08-27 | 1998-08-27 | Pharmacia & Upjohn Ab | Transdermally administered tolterodine as antimuscarinic agent for the treatment of overactive bladder |
| PL196945B1 (pl) | 1998-10-01 | 2008-02-29 | Novartis Ag | Doustna kompozycja farmaceutyczna o kontrolowanym uwalnianiu zawierająca rywastygminę oraz jej zastosowanie |
| US6248363B1 (en) | 1999-11-23 | 2001-06-19 | Lipocine, Inc. | Solid carriers for improved delivery of active ingredients in pharmaceutical compositions |
| GB9904995D0 (en) | 1999-03-04 | 1999-04-28 | Glaxo Group Ltd | Substituted aza-oxindole derivatives |
| GB9904933D0 (en) | 1999-03-04 | 1999-04-28 | Glaxo Group Ltd | Compounds |
| US6498176B1 (en) | 1999-03-04 | 2002-12-24 | Smithklinebeecham Corporation | 3-(anilinomethylene) oxindoles as protein tyrosine kinase and protein serine/threonine kinase inhibitors |
| US6624171B1 (en) | 1999-03-04 | 2003-09-23 | Smithkline Beecham Corporation | Substituted aza-oxindole derivatives |
| FR2792527B1 (fr) | 1999-04-22 | 2004-08-13 | Ethypharm Lab Prod Ethiques | Microgranules de ketoprofene, procede de preparation et compositions pharmaceutiques |
| US6541020B1 (en) | 1999-07-09 | 2003-04-01 | Trimeris, Inc. | Methods and compositions for administration of therapeutic reagents |
| MXPA02000670A (es) | 1999-07-21 | 2002-07-02 | Astrazeneca Ab | Nuevos compuestos. |
| US6562375B1 (en) | 1999-08-04 | 2003-05-13 | Yamanouchi Pharmaceuticals, Co., Ltd. | Stable pharmaceutical composition for oral use |
| JP2003508422A (ja) | 1999-09-02 | 2003-03-04 | ノストラム・ファーマスーティカルズ・インコーポレイテッド | 放出制御ペレット製剤 |
| US6544548B1 (en) | 1999-09-13 | 2003-04-08 | Keraplast Technologies, Ltd. | Keratin-based powders and hydrogel for pharmaceutical applications |
| US6080736A (en) | 1999-10-27 | 2000-06-27 | Janus Pharmaceuticals, Inc. | Methods and compositions for treating and preventing anxiety and anxiety disorders using optically pure (R) tofisopam |
| US6461631B1 (en) | 1999-11-16 | 2002-10-08 | Atrix Laboratories, Inc. | Biodegradable polymer composition |
| US6482439B2 (en) | 1999-12-29 | 2002-11-19 | Nanodelivery, Inc. | Drug delivery system exhibiting permeability control |
| US6589549B2 (en) | 2000-04-27 | 2003-07-08 | Macromed, Incorporated | Bioactive agent delivering system comprised of microparticles within a biodegradable to improve release profiles |
| US6524621B2 (en) | 2000-05-01 | 2003-02-25 | Aeropharm Technology Inc. | Core formulation |
| US6482440B2 (en) | 2000-09-21 | 2002-11-19 | Phase 2 Discovery, Inc. | Long acting antidepressant microparticles |
| US6524615B2 (en) | 2001-02-21 | 2003-02-25 | Kos Pharmaceuticals, Incorporated | Controlled release pharmaceutical composition |
| JP4343534B2 (ja) | 2001-03-02 | 2009-10-14 | ゲーペーツェー バイオテック アクチェンゲゼルシャフト | ３ハイブリッド・アッセイ・システム |
| GB0115109D0 (en) * | 2001-06-21 | 2001-08-15 | Aventis Pharma Ltd | Chemical compounds |
| US20030187026A1 (en) | 2001-12-13 | 2003-10-02 | Qun Li | Kinase inhibitors |
| JP4787150B2 (ja) | 2003-03-06 | 2011-10-05 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | Ｊｎｋ阻害剤 |
| GB2400101A (en) | 2003-03-28 | 2004-10-06 | Biofocus Discovery Ltd | Compounds capable of binding to the active site of protein kinases |
| AR045595A1 (es) | 2003-09-04 | 2005-11-02 | Vertex Pharma | Composiciones utiles como inhibidores de proteinas quinasas |
| US20060011139A1 (en) | 2004-07-16 | 2006-01-19 | Applied Materials, Inc. | Heated substrate support for chemical vapor deposition |
| WO2006015123A1 (en) | 2004-07-27 | 2006-02-09 | Sgx Pharmaceuticals, Inc. | Pyrrolo-pyridine kinase modulators |
| US7361764B2 (en) | 2004-07-27 | 2008-04-22 | Sgx Pharmaceuticals, Inc. | Pyrrolo-pyridine kinase modulators |
| US7709645B2 (en) | 2004-07-27 | 2010-05-04 | Sgx Pharmaceuticals, Inc. | Pyrrolo-pyridine kinase modulators |
| US7626021B2 (en) * | 2004-07-27 | 2009-12-01 | Sgx Pharmaceuticals, Inc. | Fused ring heterocycle kinase modulators |
| CN101065016A (zh) | 2004-09-24 | 2007-10-31 | 詹森药业有限公司 | 蛋白激酶的抑制剂咪唑并[4,5－b]吡嗪酮 |
| CA2585544A1 (en) | 2004-10-27 | 2006-05-11 | Janssen Pharmaceutica N.V. | Pyridine imidazoles and aza-indoles as progesterone receptor modulators |
| EP1828180A4 (en) | 2004-12-08 | 2010-09-15 | Glaxosmithkline Llc | 1H-pyrrolo [2,3-BETA] PYRIDINE |
| JP2008530212A (ja) | 2005-02-16 | 2008-08-07 | シェーリング コーポレイション | Ｃｘｃｒ３アンタゴニスト活性を有するピペラジン−ピペリジン |
| JP2007108926A (ja) | 2005-10-12 | 2007-04-26 | Denso Corp | 運転支援装置及びプログラム |
| US7732447B2 (en) | 2006-06-22 | 2010-06-08 | Cephalon, Inc. | Fused [d]pyridazin-7-ones |
| KR101410453B1 (ko) | 2006-08-02 | 2014-06-27 | 싸이토키네틱스, 인코포레이티드 | 소정의 화학 물질, 조성물 및 방법 |
| MX2009004077A (es) * | 2006-10-19 | 2009-05-05 | Signal Pharm Llc | Compuestos de heteroarilo, composiciones de los mismos, y su uso como inhibidores de proteina cinasas. |
| GB0706168D0 (en) | 2007-03-29 | 2007-05-09 | Glaxo Group Ltd | Compounds |
| EP2078020A4 (en) | 2007-04-10 | 2011-10-19 | Sgx Pharmaceuticals Inc | HETEROCYCLIC MODULATORS WITH FUSED CYCLES FOR KINASES |
| KR101524817B1 (ko) | 2007-04-18 | 2015-06-01 | 깃세이 야쿠힌 고교 가부시키가이샤 | 질소 함유 축합환 유도체, 그것을 함유하는 의약 조성물 및 그 의약 용도 |
| WO2009054941A1 (en) | 2007-10-25 | 2009-04-30 | Merck & Co., Inc. | Therapeutic compounds |
| RU2503676C2 (ru) * | 2008-02-25 | 2014-01-10 | Ф.Хоффманн-Ля Рош Аг | Пирролопиразиновые ингибиторы киназы |
| RU2478636C2 (ru) | 2008-08-05 | 2013-04-10 | Дайити Санкио Компани, Лимитед | ПРОИЗВОДНЫЕ ИМИДАЗОПИРИДИН-2-ОНА, ОБЛАДАЮЩИЕ mTOR ИНГИБИРУЮЩЕЙ АКТИВНОСТЬЮ |
| US8877772B2 (en) | 2008-11-25 | 2014-11-04 | University Of Rochester | Substituted pyrrolo[2,3-B]pyridines as MLK inhibitors |
| WO2011149950A2 (en) | 2010-05-24 | 2011-12-01 | University Of Rochester | Bicyclic heteroaryl kinase inhibitors and methods of use |
-
2011
- 2011-05-24 WO PCT/US2011/037758 patent/WO2011149950A2/en not_active Ceased
- 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 EP EP11787254.9A patent/EP2576549A4/en not_active Withdrawn
- 2011-05-24 AU AU2011258465A patent/AU2011258465B2/en active Active
- 2011-05-24 CA CA2800176A patent/CA2800176C/en active Active
- 2011-05-24 JP JP2013512166A patent/JP6086326B2/ja active Active
- 2011-05-24 NZ NZ603644A patent/NZ603644A/en unknown
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