JP2013544277A5 - - Google Patents
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- Publication number
- JP2013544277A5 JP2013544277A5 JP2013541446A JP2013541446A JP2013544277A5 JP 2013544277 A5 JP2013544277 A5 JP 2013544277A5 JP 2013541446 A JP2013541446 A JP 2013541446A JP 2013541446 A JP2013541446 A JP 2013541446A JP 2013544277 A5 JP2013544277 A5 JP 2013544277A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- aryl
- cycloalkyl
- pharmaceutically acceptable
- heteroaryl
- 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.)
- Ceased
Links
- 125000003118 aryl group Chemical group 0.000 claims 26
- 125000000217 alkyl group Chemical group 0.000 claims 23
- 125000003710 aryl alkyl group Chemical group 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 15
- 125000001072 heteroaryl group Chemical group 0.000 claims 14
- 150000003839 salts Chemical class 0.000 claims 14
- 125000000753 cycloalkyl group Chemical group 0.000 claims 13
- 125000003545 alkoxy group Chemical group 0.000 claims 12
- 125000005843 halogen group Chemical group 0.000 claims 11
- -1 hydroxy, amino Chemical group 0.000 claims 8
- 125000001424 substituent group Chemical group 0.000 claims 8
- 206010012289 Dementia Diseases 0.000 claims 7
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 7
- 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
- 125000001188 haloalkyl group Chemical group 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 125000004103 aminoalkyl group Chemical group 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 208000024891 symptom Diseases 0.000 claims 4
- 125000001622 2-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C(*)C([H])=C([H])C2=C1[H] 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 3
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims 3
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims 3
- 230000007278 cognition impairment Effects 0.000 claims 3
- 208000010877 cognitive disease Diseases 0.000 claims 3
- 125000004438 haloalkoxy group Chemical group 0.000 claims 3
- 201000000980 schizophrenia Diseases 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 208000028698 Cognitive impairment Diseases 0.000 claims 2
- 208000023105 Huntington disease Diseases 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- 208000028017 Psychotic disease Diseases 0.000 claims 2
- 125000003282 alkyl amino group Chemical group 0.000 claims 2
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims 2
- 125000004104 aryloxy group Chemical group 0.000 claims 2
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 2
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- YEHNWRNMGIYLAL-NSHDSACASA-N (5s)-5-amino-2-benzyl-7-hydroxy-4,5-dihydropyrazolo[3,4-b]pyridin-6-one Chemical compound C([C@@H](C(N(O)C1=N2)=O)N)C1=CN2CC1=CC=CC=C1 YEHNWRNMGIYLAL-NSHDSACASA-N 0.000 claims 1
- ABBLRYAESUTTSD-NSHDSACASA-N (5s)-5-amino-3-benzyl-7-hydroxy-1-methyl-4,5-dihydropyrazolo[3,4-b]pyridin-6-one Chemical compound O=C([C@@H](N)CC=12)N(O)C=1N(C)N=C2CC1=CC=CC=C1 ABBLRYAESUTTSD-NSHDSACASA-N 0.000 claims 1
- AUAOKUNOKVGYJP-JTQLQIEISA-N (5s)-5-amino-7-hydroxy-2-phenyl-4,5-dihydropyrazolo[3,4-b]pyridin-6-one Chemical compound C([C@@H](C(N(O)C1=N2)=O)N)C1=CN2C1=CC=CC=C1 AUAOKUNOKVGYJP-JTQLQIEISA-N 0.000 claims 1
- 206010065040 AIDS dementia complex Diseases 0.000 claims 1
- 208000031091 Amnestic disease Diseases 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 1
- 206010003805 Autism Diseases 0.000 claims 1
- 208000020706 Autistic disease Diseases 0.000 claims 1
- 208000020925 Bipolar disease Diseases 0.000 claims 1
- 201000006474 Brain Ischemia Diseases 0.000 claims 1
- 206010048962 Brain oedema Diseases 0.000 claims 1
- 206010008120 Cerebral ischaemia Diseases 0.000 claims 1
- 208000027691 Conduct disease Diseases 0.000 claims 1
- 206010010904 Convulsion Diseases 0.000 claims 1
- 206010011878 Deafness Diseases 0.000 claims 1
- 206010012218 Delirium Diseases 0.000 claims 1
- 208000012661 Dyskinesia Diseases 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 206010019196 Head injury Diseases 0.000 claims 1
- 208000010496 Heart Arrest Diseases 0.000 claims 1
- 206010061216 Infarction Diseases 0.000 claims 1
- 208000020358 Learning disease Diseases 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 208000036626 Mental retardation Diseases 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 208000019022 Mood disease Diseases 0.000 claims 1
- 208000007101 Muscle Cramp Diseases 0.000 claims 1
- 208000008238 Muscle Spasticity Diseases 0.000 claims 1
- 208000029578 Muscle disease Diseases 0.000 claims 1
- 208000021642 Muscular disease Diseases 0.000 claims 1
- 208000037212 Neonatal hypoxic and ischemic brain injury Diseases 0.000 claims 1
- 208000028389 Nerve injury Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 208000017442 Retinal disease Diseases 0.000 claims 1
- 206010038923 Retinopathy Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 208000005392 Spasm Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 208000007271 Substance Withdrawal Syndrome Diseases 0.000 claims 1
- 208000009205 Tinnitus Diseases 0.000 claims 1
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 1
- 206010046543 Urinary incontinence Diseases 0.000 claims 1
- 206010047700 Vomiting Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 230000007000 age related cognitive decline Effects 0.000 claims 1
- 230000001476 alcoholic effect Effects 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 208000006752 brain edema Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 206010008118 cerebral infarction Diseases 0.000 claims 1
- 230000007882 cirrhosis Effects 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 230000019771 cognition Effects 0.000 claims 1
- 230000003920 cognitive function Effects 0.000 claims 1
- 231100000895 deafness Toxicity 0.000 claims 1
- 230000007812 deficiency Effects 0.000 claims 1
- 230000006735 deficit Effects 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 231100000040 eye damage Toxicity 0.000 claims 1
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 claims 1
- 208000016354 hearing loss disease Diseases 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 230000002218 hypoglycaemic effect Effects 0.000 claims 1
- 230000028993 immune response Effects 0.000 claims 1
- 208000035231 inattentive type attention deficit hyperactivity disease Diseases 0.000 claims 1
- 230000007574 infarction Effects 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 208000014674 injury Diseases 0.000 claims 1
- 238000007917 intracranial administration Methods 0.000 claims 1
- 201000003723 learning disability Diseases 0.000 claims 1
- 208000002780 macular degeneration Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 230000008764 nerve damage Effects 0.000 claims 1
- 230000000926 neurological effect Effects 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 208000033300 perinatal asphyxia Diseases 0.000 claims 1
- 208000028173 post-traumatic stress disease Diseases 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 208000020016 psychiatric disease Diseases 0.000 claims 1
- 208000019116 sleep disease Diseases 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 210000000278 spinal cord Anatomy 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 231100000886 tinnitus Toxicity 0.000 claims 1
- 230000008733 trauma Effects 0.000 claims 1
- 206010044652 trigeminal neuralgia Diseases 0.000 claims 1
- 230000008673 vomiting Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41880210P | 2010-12-01 | 2010-12-01 | |
| US61/418,802 | 2010-12-01 | ||
| PCT/IB2011/055158 WO2012073143A1 (en) | 2010-12-01 | 2011-11-17 | Kat ii inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013544277A JP2013544277A (ja) | 2013-12-12 |
| JP2013544277A5 true JP2013544277A5 (https=) | 2014-09-25 |
Family
ID=45444662
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013541446A Ceased JP2013544277A (ja) | 2010-12-01 | 2011-11-17 | Ｋａｔｉｉ阻害剤 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US8598200B2 (https=) |
| EP (1) | EP2646443B1 (https=) |
| JP (1) | JP2013544277A (https=) |
| KR (1) | KR101544290B1 (https=) |
| CN (1) | CN103228660A (https=) |
| AU (1) | AU2011336214B2 (https=) |
| CA (1) | CA2819102A1 (https=) |
| DK (1) | DK2646443T3 (https=) |
| ES (1) | ES2524423T3 (https=) |
| MX (1) | MX2013005773A (https=) |
| SG (1) | SG190207A1 (https=) |
| WO (1) | WO2012073143A1 (https=) |
| ZA (1) | ZA201303360B (https=) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2646417A1 (en) | 2010-12-01 | 2013-10-09 | Pfizer Inc | Kat ii inhibitors |
| US20140206667A1 (en) | 2012-11-14 | 2014-07-24 | Michela Gallagher | Methods and compositions for treating schizophrenia |
| BR112016024455B1 (pt) | 2014-04-23 | 2023-02-07 | Mitsubishi Tanabe Pharma Corporation | Composto heterocíclico bicíclico ou tricíclico |
| WO2016164754A1 (en) | 2015-04-09 | 2016-10-13 | Eisai R&D Management Co., Ltd. | Fgfr4 inhibitors |
| WO2016164703A1 (en) | 2015-04-09 | 2016-10-13 | Eisai R & D Management Co., Ltd. | Fgfr4 inhibitors |
| CA2998753A1 (en) | 2015-09-18 | 2017-03-23 | St. Jude Children's Research Hospital | Methods and compositions of inhibiting dcn1-ubc12 interaction |
| US10793582B2 (en) | 2015-10-22 | 2020-10-06 | Mitsubishi Tanabe Pharma Corporation | Bicyclic heterocyclic compound |
| WO2020257790A1 (en) * | 2019-06-20 | 2020-12-24 | University Of Kentucky Research Foundation | Pharmaceutically active pyrazolo-pyridone modulators of dcn1/2-mediated cullin neddylation |
| CN115038443A (zh) | 2019-11-22 | 2022-09-09 | 因西特公司 | 包含alk2抑制剂和jak2抑制剂的组合疗法 |
| KR102698413B1 (ko) | 2020-05-05 | 2024-08-26 | 뉴베일런트, 아이엔씨. | 헤테로방향족 거대환식 에터 화학치료제 |
| IL297832A (en) | 2020-05-05 | 2023-01-01 | Nuvalent Inc | Macrocyclic heteroaromatic chemotherapeutic agents |
| WO2022165382A1 (en) * | 2021-01-29 | 2022-08-04 | Neurawell Therapeutics | Phenylethylidenehydrazine combination therapies |
| IL311444A (en) | 2021-10-01 | 2024-05-01 | Nuvalent Inc | Solid forms, pharmaceutical compositions and preparation of heteroaromatic macrocyclic ether compounds |
| WO2025096981A1 (en) * | 2023-11-03 | 2025-05-08 | Cellarity, Inc. | Modulators of dcn-1 and methods of use thereof |
| US12473285B2 (en) | 2023-11-03 | 2025-11-18 | Cellarity, Inc. | DCN-1 modulating compounds and methods of use thereof |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4282361A (en) | 1978-03-16 | 1981-08-04 | Massachusetts Institute Of Technology | Synthesis for 7-alkylamino-3-methylpyrazolo [4,3-d]pyrimidines |
| US5519055A (en) * | 1993-08-06 | 1996-05-21 | University Of Maryland At Baltimore | Substituted kynurenines and process for their preparation |
| US7276608B2 (en) * | 2003-07-11 | 2007-10-02 | Bristol-Myers Squibb Company | Tetrahydroquinoline derivatives as cannabinoid receptor modulators |
| GT200500186A (es) | 2004-07-07 | 2006-03-02 | Regimenes anticonceptivos con antagonistas del receptor de progesterona y kits | |
| JP2008517994A (ja) | 2004-10-28 | 2008-05-29 | ファルマシア・アンド・アップジョン・カンパニー・エルエルシー | 新規医薬品 |
| CA2626897A1 (en) | 2005-11-03 | 2007-05-18 | Joshua Close | Histone deacetylase inhibitors with aryl-pyrazolyl motifs |
| CA2635209A1 (en) | 2006-01-12 | 2007-08-02 | Merck & Co., Inc. | Fluorinated arylamide derivatives |
| EP2049548A1 (en) | 2006-07-27 | 2009-04-22 | UCB Pharma, S.A. | Fused oxazoles & thiazoles as histamine h3- receptor ligands |
| WO2009064836A2 (en) * | 2007-11-15 | 2009-05-22 | University Of Maryland, Baltimore | Kynurenine-aminotransferase inhibitors |
| WO2009095752A1 (en) * | 2008-01-29 | 2009-08-06 | Glenmark Pharmaceuticals, S.A. | Fused pyrazole derivatives as cannabinoid receptor modulators |
| US9293849B2 (en) | 2008-07-30 | 2016-03-22 | Bal Seal Engineering, Inc. | Electrical connector using a canted coil multi-metallic wire |
| WO2010146488A1 (en) * | 2009-06-18 | 2010-12-23 | Pfizer Inc. | Bicyclic and tricyclic compounds as kat ii inhibitors |
-
2011
- 2011-11-17 DK DK11804801.6T patent/DK2646443T3/en active
- 2011-11-17 CN CN2011800578092A patent/CN103228660A/zh active Pending
- 2011-11-17 CA CA2819102A patent/CA2819102A1/en not_active Abandoned
- 2011-11-17 EP EP11804801.6A patent/EP2646443B1/en not_active Not-in-force
- 2011-11-17 WO PCT/IB2011/055158 patent/WO2012073143A1/en not_active Ceased
- 2011-11-17 MX MX2013005773A patent/MX2013005773A/es active IP Right Grant
- 2011-11-17 SG SG2013035399A patent/SG190207A1/en unknown
- 2011-11-17 ES ES11804801.6T patent/ES2524423T3/es active Active
- 2011-11-17 AU AU2011336214A patent/AU2011336214B2/en not_active Expired - Fee Related
- 2011-11-17 JP JP2013541446A patent/JP2013544277A/ja not_active Ceased
- 2011-11-17 KR KR1020137014065A patent/KR101544290B1/ko not_active Expired - Fee Related
- 2011-11-30 US US13/307,636 patent/US8598200B2/en not_active Expired - Fee Related
-
2013
- 2013-05-09 ZA ZA2013/03360A patent/ZA201303360B/en unknown
- 2013-10-31 US US14/068,707 patent/US8933095B2/en not_active Expired - Fee Related
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