JP2012522793A5 - - Google Patents
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- Publication number
- JP2012522793A5 JP2012522793A5 JP2012503692A JP2012503692A JP2012522793A5 JP 2012522793 A5 JP2012522793 A5 JP 2012522793A5 JP 2012503692 A JP2012503692 A JP 2012503692A JP 2012503692 A JP2012503692 A JP 2012503692A JP 2012522793 A5 JP2012522793 A5 JP 2012522793A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- heteroaryl
- optionally substituted
- aryl
- cycloalkyl
- 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
Links
- 125000000217 alkyl group Chemical group 0.000 claims 18
- 150000001875 compounds Chemical class 0.000 claims 12
- 125000001072 heteroaryl group Chemical group 0.000 claims 11
- 125000003118 aryl group Chemical group 0.000 claims 10
- 125000000623 heterocyclic group Chemical group 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 7
- 150000002431 hydrogen Chemical class 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 6
- 239000012453 solvate Substances 0.000 claims 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 4
- 125000003710 aryl alkyl group Chemical group 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 2
- 208000007848 Alcoholism Diseases 0.000 claims 2
- 208000004454 Hyperalgesia Diseases 0.000 claims 2
- 208000002193 Pain Diseases 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- ZPUCINDJVBIVPJ-LJISPDSOSA-N cocaine Chemical compound O([C@H]1C[C@@H]2CC[C@@H](N2C)[C@H]1C(=O)OC)C(=O)C1=CC=CC=C1 ZPUCINDJVBIVPJ-LJISPDSOSA-N 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 206010015037 epilepsy Diseases 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- BQJCRHHNABKAKU-KBQPJGBKSA-N morphine Chemical compound O([C@H]1[C@H](C=C[C@H]23)O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O BQJCRHHNABKAKU-KBQPJGBKSA-N 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 208000011117 substance-related disease Diseases 0.000 claims 2
- SNICXCGAKADSCV-JTQLQIEISA-N (-)-Nicotine Chemical compound CN1CCC[C@H]1C1=CC=CN=C1 SNICXCGAKADSCV-JTQLQIEISA-N 0.000 claims 1
- 206010001497 Agitation Diseases 0.000 claims 1
- 208000024827 Alzheimer 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
- 208000036864 Attention deficit/hyperactivity disease 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
- 208000032841 Bulimia Diseases 0.000 claims 1
- 206010006550 Bulimia nervosa Diseases 0.000 claims 1
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 206010010904 Convulsion Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 201000010374 Down Syndrome Diseases 0.000 claims 1
- 206010013654 Drug abuse Diseases 0.000 claims 1
- 208000012661 Dyskinesia Diseases 0.000 claims 1
- 208000001914 Fragile X syndrome Diseases 0.000 claims 1
- 206010019196 Head injury Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 206010020853 Hypertonic bladder Diseases 0.000 claims 1
- 206010065390 Inflammatory pain Diseases 0.000 claims 1
- 201000006347 Intellectual Disability Diseases 0.000 claims 1
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 claims 1
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 claims 1
- 208000019693 Lung disease Diseases 0.000 claims 1
- 208000026139 Memory disease Diseases 0.000 claims 1
- 102000012777 Metabotropic Glutamate 5 Receptor Human genes 0.000 claims 1
- 108010065028 Metabotropic Glutamate 5 Receptor Proteins 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 208000019022 Mood disease Diseases 0.000 claims 1
- 208000003445 Mouth Neoplasms Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 claims 1
- 208000009722 Overactive Urinary Bladder Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 201000007100 Pharyngitis Diseases 0.000 claims 1
- 206010034912 Phobia Diseases 0.000 claims 1
- 208000004550 Postoperative Pain Diseases 0.000 claims 1
- 208000028017 Psychotic disease Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 206010046543 Urinary incontinence Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 230000016571 aggressive behavior Effects 0.000 claims 1
- 206010001584 alcohol abuse Diseases 0.000 claims 1
- 208000025746 alcohol use disease Diseases 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 208000022531 anorexia Diseases 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229960003920 cocaine Drugs 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 206010061428 decreased appetite Diseases 0.000 claims 1
- 206010013663 drug dependence Diseases 0.000 claims 1
- 201000006549 dyspepsia Diseases 0.000 claims 1
- 208000028329 epileptic seizure Diseases 0.000 claims 1
- 208000021302 gastroesophageal reflux disease Diseases 0.000 claims 1
- 230000009610 hypersensitivity Effects 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 208000037906 ischaemic injury Diseases 0.000 claims 1
- 229960004502 levodopa Drugs 0.000 claims 1
- 208000012987 lip and oral cavity carcinoma Diseases 0.000 claims 1
- 206010027175 memory impairment 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
- 229960005181 morphine Drugs 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 210000004498 neuroglial cell Anatomy 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 229960002715 nicotine Drugs 0.000 claims 1
- SNICXCGAKADSCV-UHFFFAOYSA-N nicotine Natural products CN1CCCC1C1=CC=CN=C1 SNICXCGAKADSCV-UHFFFAOYSA-N 0.000 claims 1
- 229940005483 opioid analgesics Drugs 0.000 claims 1
- 208000020629 overactive bladder Diseases 0.000 claims 1
- 235000006408 oxalic acid Nutrition 0.000 claims 1
- 208000019899 phobic disease Diseases 0.000 claims 1
- 208000028173 post-traumatic stress disease Diseases 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 230000001953 sensory effect Effects 0.000 claims 1
- 230000000391 smoking effect Effects 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
- 208000019206 urinary tract infection Diseases 0.000 claims 1
- 208000009935 visceral pain Diseases 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US16666109P | 2009-04-03 | 2009-04-03 | |
| US61/166,661 | 2009-04-03 | ||
| US25579009P | 2009-10-28 | 2009-10-28 | |
| US61/255,790 | 2009-10-28 | ||
| PCT/US2010/029575 WO2010114971A1 (en) | 2009-04-03 | 2010-04-01 | Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012522793A JP2012522793A (ja) | 2012-09-27 |
| JP2012522793A5 true JP2012522793A5 (https=) | 2013-05-16 |
| JP5651681B2 JP5651681B2 (ja) | 2015-01-14 |
Family
ID=42244504
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012503692A Expired - Fee Related JP5651681B2 (ja) | 2009-04-03 | 2010-04-01 | 代謝型グルタミン酸受容体５介在障害の治療のための化合物、およびその使用方法 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20120029190A1 (https=) |
| EP (1) | EP2414340A1 (https=) |
| JP (1) | JP5651681B2 (https=) |
| CA (1) | CA2756989A1 (https=) |
| WO (1) | WO2010114971A1 (https=) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011073339A1 (en) | 2009-12-18 | 2011-06-23 | Janssen Pharmaceutica Nv | Bicyclic thiazoles as allosteric modulators of mglur5 receptors |
| CN102666551B (zh) | 2009-12-18 | 2014-12-10 | 詹森药业有限公司 | 作为mglur5受体的变构调节剂的双环噻唑 |
| USRE48301E1 (en) | 2010-07-09 | 2020-11-10 | Abbvie B.V. | Fused heterocyclic derivatives as S1P modulators |
| CA2806103A1 (en) | 2010-08-31 | 2012-03-08 | Vanderbilt University | Bicyclic oxazole and thiazole compounds and their use as allosteric modulators of mglur5 receptors |
| WO2012078817A1 (en) | 2010-12-08 | 2012-06-14 | Vanderbilt University | Bicyclic pyrazole compounds as allosteric modulators of mglur5 receptors |
| JP2013545822A (ja) * | 2010-12-17 | 2013-12-26 | ヴァンダービルト ユニバーシティー | ｍＧｌｕＲ５受容体のアロステリック調節剤としての、二環式トリアゾールラクタムおよびピラゾールラクタム |
| US8975276B2 (en) | 2011-06-29 | 2015-03-10 | Bristol-Myers Squibb Company | Inhibitors of PDE10 |
| TWI567079B (zh) * | 2011-07-15 | 2017-01-21 | 健生醫藥公司 | 作為伽瑪分泌酶調節劑之新穎的經取代的吲哚衍生物 |
| EP2799431B1 (en) | 2011-12-28 | 2018-01-24 | FUJIFILM Corporation | Novel nicotinamide derivative or salt thereof |
| WO2013192343A1 (en) * | 2012-06-20 | 2013-12-27 | Vanderbilt University | Substituted bicyclic alkoxy pyrazole analogs as allosteric modulators of mglur5 receptors |
| US20150336985A1 (en) | 2012-06-22 | 2015-11-26 | E. I. Du Pont De Nemours And Company | Fungicidal heterocyclic compounds |
| JP2016011257A (ja) * | 2012-10-23 | 2016-01-21 | 大日本住友製薬株式会社 | テトラヒドロオキサゾロピリジン誘導体 |
| AU2013366668B2 (en) | 2012-12-20 | 2017-07-20 | Janssen Pharmaceutica Nv | Novel tricyclic 3,4-dihydro-2H-pyrido[1,2-alpha]pyrazine -1,6-dione derivatives as gamma secretase modulators |
| ES2612215T3 (es) | 2013-01-17 | 2017-05-12 | Janssen Pharmaceutica, N.V. | Novedosos derivados de pirido-piperazinona sustituidos como moduladores de gamma secretasa |
| GB201321749D0 (en) * | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| US10562897B2 (en) | 2014-01-16 | 2020-02-18 | Janssen Pharmaceutica Nv | Substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-diones as gamma secretase modulators |
| JP6691127B2 (ja) * | 2014-12-29 | 2020-04-28 | レコルダーティ アイルランド リミテッドＲｅｃｏｒｄａｔｉ Ｉｒｅｌａｎｄ Ｌｉｍｉｔｅｄ | ヘテロシクリルアルキン誘導体およびそれらのｍＧｌｕＲ５受容体のモジュレーターとしての使用 |
| WO2016171181A1 (ja) * | 2015-04-21 | 2016-10-27 | 大日本住友製薬株式会社 | ２位置換縮合ピラゾール誘導体 |
| UA123633C2 (uk) | 2015-11-03 | 2021-05-05 | Тереванс Байофарма Ар Енд Ді Айпі, Елелсі | Сполуки інгібітору jak-кінази для лікування респіраторного захворювання |
| US10040804B2 (en) | 2016-12-21 | 2018-08-07 | Biotheryx, Inc. | Compounds targeting proteins, compositions, methods, and uses thereof |
| WO2018165392A1 (en) | 2017-03-09 | 2018-09-13 | Theravance Biopharma R&D Ip, Llc | Jak inhibitors containing a 4-membered heterocyclic amide |
| AR111495A1 (es) | 2017-05-01 | 2019-07-17 | Theravance Biopharma R&D Ip Llc | Compuestos de imidazo-piperidina fusionada como inhibidores de jak |
| KR20200003121A (ko) | 2017-05-01 | 2020-01-08 | 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 | Jak 저해제 화합물의 결정형 |
| WO2018204233A1 (en) | 2017-05-01 | 2018-11-08 | Theravance Biopharma R&D Ip, Llc | Methods of treatment using a jak inhibitor compound |
| EA202091113A1 (ru) | 2017-11-02 | 2020-08-28 | Айкурис Гмбх Унд Ко. Кг | Новые высокоактивные аминотиазолзамещенные индол-2-карбоксамиды, активные в отношении вируса гепатита b (hbv) |
| FI3837258T3 (fi) | 2018-09-04 | 2024-05-27 | Theravance Biopharma R&D Ip Llc | Dimetyyliaminoatsetidiiniamideja jak-estäjinä |
| UA127328C2 (uk) | 2018-09-04 | 2023-07-19 | Тереванс Байофарма Ар Енд Ді Айпі, Елелсі | 5-7-членні гетероциклічні аміди як інгібітори jak |
| JP2021535176A (ja) | 2018-09-04 | 2021-12-16 | セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー | Ｊａｋ阻害剤およびその中間体を調製するためのプロセス |
| KR20210084512A (ko) | 2018-10-29 | 2021-07-07 | 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 | Jak 억제제로서 2-아자비시클로 헥산 화합물 |
| TW202144343A (zh) | 2020-03-02 | 2021-12-01 | 美商施萬生物製藥研發 Ip有限責任公司 | Jak抑制劑化合物之結晶水合物 |
| JP7539545B2 (ja) * | 2020-07-03 | 2024-08-23 | 武漢朗来科技発展有限公司 | 複素環化合物及びその使用 |
| EP4359402B1 (en) | 2021-06-25 | 2026-03-11 | Theravance Biopharma R&D IP, LLC | Imidazolo indazole compounds as jak inhibitors |
| WO2023107722A1 (en) * | 2021-12-10 | 2023-06-15 | Prothena Biosciences Limited | Compounds for use in treating neurological disorders |
| WO2024067660A1 (zh) * | 2022-09-29 | 2024-04-04 | 苏州爱科百发生物医药技术有限公司 | 氮杂稠环类化合物、其制备方法及其在医药上的应用 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE1620508A1 (de) * | 1965-07-23 | 1969-09-18 | Thomae Gmbh Dr K | Verfahren zur Herstellung neuer 4,5,6,7-Tetrahydrothiazolo-[5,4-c]-pyridine |
| US3503990A (en) * | 1967-01-31 | 1970-03-31 | Endo Lab | 6-aryl-4,5,6,7-tetrahydro-4-oxoindole derivatives |
| US3621027A (en) * | 1968-03-18 | 1971-11-16 | Endo Lab | 1-aminoalkyl-2,6-diaryl 4,5,6,7 tetrahydro-4-oxindales |
| KR100710453B1 (ko) * | 2003-05-13 | 2007-04-24 | 에프. 호프만-라 로슈 아게 | 아데노신 수용체 리간드로서의 2-이미다조-벤조싸이아졸 |
| US20070185100A1 (en) * | 2004-02-18 | 2007-08-09 | Astrazeneca Ab | Poly-heterocyclic compounds and their use as metabotropic glutamate receptor antagonists |
| US7585881B2 (en) * | 2004-02-18 | 2009-09-08 | Astrazeneca Ab | Additional heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists |
| TW200800204A (en) * | 2005-08-15 | 2008-01-01 | Astrazeneca Ab | Bicyclic piperazines as metabotropic glutatmate receptor antagonists |
| GB0622202D0 (en) * | 2006-11-07 | 2006-12-20 | Addex Pharmaceuticals Sa | Novel compounds |
| WO2009092764A1 (en) * | 2008-01-24 | 2009-07-30 | Ucb Pharma, S.A. | Compounds comprising a cyclobutoxy group |
-
2010
- 2010-04-01 WO PCT/US2010/029575 patent/WO2010114971A1/en not_active Ceased
- 2010-04-01 JP JP2012503692A patent/JP5651681B2/ja not_active Expired - Fee Related
- 2010-04-01 US US13/262,608 patent/US20120029190A1/en not_active Abandoned
- 2010-04-01 EP EP10712266A patent/EP2414340A1/en not_active Withdrawn
- 2010-04-01 CA CA2756989A patent/CA2756989A1/en not_active Abandoned
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