JP2017528502A5 - - Google Patents
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- JP2017528502A5 JP2017528502A5 JP2017516358A JP2017516358A JP2017528502A5 JP 2017528502 A5 JP2017528502 A5 JP 2017528502A5 JP 2017516358 A JP2017516358 A JP 2017516358A JP 2017516358 A JP2017516358 A JP 2017516358A JP 2017528502 A5 JP2017528502 A5 JP 2017528502A5
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- JP
- Japan
- Prior art keywords
- alkyl
- compound
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- pharmaceutical composition
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims 13
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 6
- 208000027534 Emotional disease Diseases 0.000 claims 4
- 102000007399 Nuclear hormone receptor Human genes 0.000 claims 4
- 108020005497 Nuclear hormone receptor Proteins 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 208000020925 Bipolar disease Diseases 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 150000001768 cations Chemical class 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 239000002184 metal Substances 0.000 claims 3
- 229910052751 metal Inorganic materials 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 208000028552 Treatment-Resistant Depressive disease Diseases 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 208000024714 major depressive disease Diseases 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 125000006413 ring segment Chemical group 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 102000034527 Retinoid X Receptors Human genes 0.000 claims 1
- 108010038912 Retinoid X Receptors Proteins 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 125000002029 aromatic hydrocarbon group Chemical group 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 208000028683 bipolar I disease Diseases 0.000 claims 1
- 208000025307 bipolar depression Diseases 0.000 claims 1
- 230000005978 brain dysfunction Effects 0.000 claims 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 210000005036 nerve Anatomy 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462056284P | 2014-09-26 | 2014-09-26 | |
| US62/056,284 | 2014-09-26 | ||
| PCT/US2015/051694 WO2016049165A1 (en) | 2014-09-26 | 2015-09-23 | N-alkylaryl-5-oxyaryl-octahydro-cyclopenta[c]pyrrole negative allosteric modulators of nr2b |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019008873A Division JP6772307B2 (ja) | 2014-09-26 | 2019-01-23 | ＮＲ２ＢのＮ−アルキルアリール−５−オキシアリール−オクタヒドロ−シクロペンタ［ｃ］ピロールネガティブアロステリックモジュレーター |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017528502A JP2017528502A (ja) | 2017-09-28 |
| JP2017528502A5 true JP2017528502A5 (enExample) | 2018-11-08 |
| JP6473227B2 JP6473227B2 (ja) | 2019-02-20 |
Family
ID=55581945
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017516358A Active JP6473227B2 (ja) | 2014-09-26 | 2015-09-23 | ＮＲ２ＢのＮ−アルキルアリール−５−オキシアリール−オクタヒドロ−シクロペンタ［ｃ］ピロールネガティブアロステリックモジュレーター |
| JP2019008873A Active JP6772307B2 (ja) | 2014-09-26 | 2019-01-23 | ＮＲ２ＢのＮ−アルキルアリール−５−オキシアリール−オクタヒドロ−シクロペンタ［ｃ］ピロールネガティブアロステリックモジュレーター |
| JP2020166129A Active JP7216060B2 (ja) | 2014-09-26 | 2020-09-30 | ＮＲ２ＢのＮ－アルキルアリール－５－オキシアリール－オクタヒドロ－シクロペンタ［ｃ］ピロールネガティブアロステリックモジュレーター |
| JP2023006525A Active JP7612722B2 (ja) | 2014-09-26 | 2023-01-19 | ＮＲ２ＢのＮ－アルキルアリール－５－オキシアリール－オクタヒドロ－シクロペンタ［ｃ］ピロールネガティブアロステリックモジュレーター |
| JP2024228390A Pending JP2025060835A (ja) | 2014-09-26 | 2024-12-25 | ＮＲ２ＢのＮ－アルキルアリール－５－オキシアリール－オクタヒドロ－シクロペンタ［ｃ］ピロールネガティブアロステリックモジュレーター |
Family Applications After (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019008873A Active JP6772307B2 (ja) | 2014-09-26 | 2019-01-23 | ＮＲ２ＢのＮ−アルキルアリール−５−オキシアリール−オクタヒドロ−シクロペンタ［ｃ］ピロールネガティブアロステリックモジュレーター |
| JP2020166129A Active JP7216060B2 (ja) | 2014-09-26 | 2020-09-30 | ＮＲ２ＢのＮ－アルキルアリール－５－オキシアリール－オクタヒドロ－シクロペンタ［ｃ］ピロールネガティブアロステリックモジュレーター |
| JP2023006525A Active JP7612722B2 (ja) | 2014-09-26 | 2023-01-19 | ＮＲ２ＢのＮ－アルキルアリール－５－オキシアリール－オクタヒドロ－シクロペンタ［ｃ］ピロールネガティブアロステリックモジュレーター |
| JP2024228390A Pending JP2025060835A (ja) | 2014-09-26 | 2024-12-25 | ＮＲ２ＢのＮ－アルキルアリール－５－オキシアリール－オクタヒドロ－シクロペンタ［ｃ］ピロールネガティブアロステリックモジュレーター |
Country Status (40)
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO3579B1 (ar) * | 2014-09-26 | 2020-07-05 | Luc Therapeutics Inc | مُعدِلات تفاغرية سالبة لمستقبل nr2b من المركب n-ألكيل أريل-5-أوكسي أريل-ثامن هيدرو-خماسي الحلقة [c] بيرول |
| US11299481B2 (en) | 2017-10-20 | 2022-04-12 | Vanderbilt University | Antagonists of the muscarinic acetylcholine receptor M4 |
| EP3703680B1 (en) | 2017-10-31 | 2024-05-15 | Vanderbilt University | Antagonists of the muscarinic acetylcholine receptor m4 |
| JP7352294B2 (ja) | 2018-02-02 | 2023-09-28 | ヴァンダービルト ユニバーシティー | ムスカリン性アセチルコリン受容体ｍ４のアンタゴニスト |
| KR102656571B1 (ko) | 2018-03-05 | 2024-04-11 | 아르커스 바이오사이언시즈 인코포레이티드 | 아르기나아제 억제제 |
| US12398143B2 (en) | 2019-06-04 | 2025-08-26 | Boehringer Ingelheim International Gmbh | Imidazopyrazine derivatives and the use thereof as medicament |
| WO2020245136A1 (en) * | 2019-06-04 | 2020-12-10 | Boehringer Ingelheim International Gmbh | Purine derivatives, as nr2b negative modulators and the use thereof as medicament, in particular for treating depressive disorders |
| CN111481543A (zh) * | 2020-05-21 | 2020-08-04 | 苏州健雄职业技术学院 | Nr2b负变构调节剂联合gaba受体调节剂在制备治疗阿尔兹海默症的药物中的用途 |
| CN116744922A (zh) * | 2020-12-04 | 2023-09-12 | 诺华股份有限公司 | Nr2b-nmda受体nam在治疗抑郁症中的剂量方案 |
| MX2023006567A (es) * | 2020-12-04 | 2023-06-16 | Novartis Ag | Regimen de dosificacion para un nam del receptor nr2b-nmda para el tratamiento de la depresion. |
| JP2021058765A (ja) * | 2021-01-19 | 2021-04-15 | 株式会社藤商事 | 遊技機 |
| CA3212203A1 (en) * | 2021-03-26 | 2022-09-29 | Novartis Ag | Novel cyclopenta[c]pyrrol negative allosteric modulators of nr2b |
| JP2024512066A (ja) * | 2021-03-26 | 2024-03-18 | ノバルティス アーゲー | ＮＲ２Ｂの負のアロステリックモジュレーターである新規なシクロペンタ［ｃ］ピロール |
| KR20250019704A (ko) | 2022-06-02 | 2025-02-10 | 노파르티스 아게 | 우울증 장애의 치료에 사용하기 위한 온파스프로딜의 피하 투여 및 투약 방법 |
| CN120981566A (zh) | 2023-01-12 | 2025-11-18 | 诺华股份有限公司 | 工程化酮还原酶多肽 |
| WO2025120013A1 (en) | 2023-12-06 | 2025-06-12 | Novartis Ag | Compositions and methods for treating depression disorders |
Family Cites Families (32)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US5532243A (en) | 1992-02-14 | 1996-07-02 | The Dupont Merck Pharmaceutical Company | Antipsychotic nitrogen-containing bicyclic compounds |
| US5262564A (en) | 1992-10-30 | 1993-11-16 | Octamer, Inc. | Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents |
| DE4341403A1 (de) | 1993-12-04 | 1995-06-08 | Basf Ag | N-substituierte 3-Azabicycloalkan-Derivate, ihre Herstellung und Verwendung |
| US5726172A (en) * | 1996-01-16 | 1998-03-10 | Merck & Co., Inc. | Tocolytic oxytocin receptor antagonists |
| US6369076B1 (en) * | 1999-10-29 | 2002-04-09 | Merck & Co. Inc. | 5-benzyl-octahydroindole and 6-benzyl-decahydroquinoline NMDA/NR2B antagonists |
| JP4845873B2 (ja) | 2004-03-03 | 2011-12-28 | ケモセントリックス インコーポレーティッド | 二環式および架橋した窒素複素環 |
| US7696241B2 (en) | 2004-03-04 | 2010-04-13 | Bristol-Myers Squibb Company | Bicyclic compounds as modulators of androgen receptor function and method |
| PT1761542E (pt) * | 2004-06-09 | 2008-03-26 | Hoffmann La Roche | Derivados de octa-hidro-pirrolo[3,4-c) pirrole e o seu uso com agentes antivirais |
| US20070270417A1 (en) | 2004-07-22 | 2007-11-22 | Glaxo Group Limited | Antibacterial Agents |
| HUP0401523A3 (en) | 2004-07-29 | 2007-05-02 | Richter Gedeon Vegyeszet | Indole-2-carboxamide derivatives, pharmaceutical compositions containing them and process for producing them |
| WO2006113471A2 (en) | 2005-04-19 | 2006-10-26 | Merck & Co., Inc. | N-alkyl-azacycloalkyl nmda/nr2b antagonists |
| EP1849772A1 (en) | 2006-04-28 | 2007-10-31 | Laboratorios Del Dr. Esteve, S.A. | Bicyclic tetrahydropyrrole compounds |
| US8299113B2 (en) | 2006-04-28 | 2012-10-30 | Laboratorios Del Dr. Esteve, S.A. | Bicyclic tetrahydropyrrole compounds |
| TW200845977A (en) | 2007-03-30 | 2008-12-01 | Targacept Inc | Sub-type selective azabicycloalkane derivatives |
| KR20100075643A (ko) | 2007-10-22 | 2010-07-02 | 쉐링 코포레이션 | 비사이클릭 헤테로사이클 유도체 및 ｇｐｒ119의 활성의 조절인자로서의 이의 용도 |
| MX2010008049A (es) | 2008-01-23 | 2010-11-12 | Jiangsu Hansoh Pharmaceutical Co Ltd | Derivados de dicicloazaalcano, sus procesos de preparacion y usos medicos. |
| US8211933B2 (en) | 2008-12-12 | 2012-07-03 | Vanderbilt University | 3.3.0 bicyclic GlyT1 inhibitors and methods of making and using same |
| FR2945533B1 (fr) | 2009-05-12 | 2011-05-27 | Sanofi Aventis | Derives de cyclopenta°c!pyrrolyl-alkylcarbamates d'heterocycles a 5 chainons, leur preparation et leur application en therapeutique |
| FR2945534B1 (fr) * | 2009-05-12 | 2012-11-16 | Sanofi Aventis | DERIVES DE CYCLOPENTAL[c]PYRROLE-2-CARBOXYLATES, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE |
| KR20120112755A (ko) | 2010-01-07 | 2012-10-11 | 이 아이 듀폰 디 네모아 앤드 캄파니 | 살진균제 복소환 화합물 |
| WO2011149993A2 (en) | 2010-05-25 | 2011-12-01 | Abbott Laboratories | SUBSTITUTED OCTAHYDROCYCLOPENTA[c]PYRROLES AS CALCIUM CHANNEL MODULATORS |
| CN102432598A (zh) * | 2010-09-29 | 2012-05-02 | 江苏恒瑞医药股份有限公司 | 三环化合物、其制备方法及其在医药上的应用 |
| FR2974729B1 (fr) | 2011-05-02 | 2013-04-19 | Servier Lab | Nouvelle association entre le 4-{3-[cis-hexahydrocyclopenta[c]pyrrol-2(1h)-yl]propoxy}benzamide et un inhibiteur de l'acetylcholinesterase et les compositions pharmaceutiques qui la contiennent |
| US8501768B2 (en) | 2011-05-17 | 2013-08-06 | Hoffmann-La Roche Inc. | Hexahydrocyclopentapyrrolone, hexahydropyrrolopyrrolone, octahydropyrrolopyridinone and octahydropyridinone compounds |
| JO3611B1 (ar) | 2011-08-10 | 2020-08-27 | Janssen Sciences Ireland Uc | سايكلو بنتا (سي (بيرول 4,3 ثاني هيدرو 1 hمستبدله [8,1] نافثيريدينونات مضادة للجراثيم |
| DK2796460T3 (en) | 2011-12-21 | 2018-08-27 | Jiangsu Hengrui Medicine Co | SEXUAL PYRROL HETEROARYL RING DERIVATIVES, METHOD OF PREPARATION AND MEDICAL APPLICATIONS THEREOF |
| BR112015004111A2 (pt) * | 2012-09-25 | 2017-07-04 | Hoffmann La Roche | novos derivados bicíclicos |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| US9418332B2 (en) | 2013-08-16 | 2016-08-16 | Qualcomm Incorporated | Post ghost plasticity |
| UY35750A (es) * | 2013-09-26 | 2015-04-30 | Mnemosyne Pharmaceuticals Inc | Moduladores octahidro-ciclopenta[c] pirrol negativos de nr2b |
| SI3122750T1 (sl) | 2014-03-26 | 2019-12-31 | F. Hoffmann-La Roche Ag | Biciklične spojine kot zaviralci proizvodnje avtotaksina (ATX) in lizofosfatidne kisline (LPA) |
| JO3579B1 (ar) | 2014-09-26 | 2020-07-05 | Luc Therapeutics Inc | مُعدِلات تفاغرية سالبة لمستقبل nr2b من المركب n-ألكيل أريل-5-أوكسي أريل-ثامن هيدرو-خماسي الحلقة [c] بيرول |
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2015
- 2015-09-22 JO JOP/2015/0237A patent/JO3579B1/ar active
- 2015-09-23 RS RS20200721A patent/RS60497B1/sr unknown
- 2015-09-23 JP JP2017516358A patent/JP6473227B2/ja active Active
- 2015-09-23 EP EP23185898.6A patent/EP4282412A3/en active Pending
- 2015-09-23 PE PE2017000506A patent/PE20170893A1/es unknown
- 2015-09-23 CU CU2017000037A patent/CU24482B1/es unknown
- 2015-09-23 MX MX2017003940A patent/MX374657B/es active IP Right Grant
- 2015-09-23 BR BR112017006093-0A patent/BR112017006093B1/pt active IP Right Grant
- 2015-09-23 NZ NZ729569A patent/NZ729569A/en not_active IP Right Cessation
- 2015-09-23 US US15/506,592 patent/US10239835B2/en active Active
- 2015-09-23 DK DK15844057.8T patent/DK3197868T3/da active
- 2015-09-23 WO PCT/US2015/051694 patent/WO2016049165A1/en not_active Ceased
- 2015-09-23 AU AU2015320721A patent/AU2015320721B2/en active Active
- 2015-09-23 PT PT158440578T patent/PT3197868T/pt unknown
- 2015-09-23 EP EP21202255.2A patent/EP3974420B1/en active Active
- 2015-09-23 SI SI201531255T patent/SI3197868T1/sl unknown
- 2015-09-23 HR HRP20200959TT patent/HRP20200959T1/hr unknown
- 2015-09-23 TN TN2017000076A patent/TN2017000076A1/en unknown
- 2015-09-23 CR CR20170114A patent/CR20170114A/es unknown
- 2015-09-23 EA EA201790713A patent/EA034937B1/ru not_active IP Right Cessation
- 2015-09-23 ES ES15844057T patent/ES2791327T3/es active Active
- 2015-09-23 KR KR1020177007813A patent/KR102479356B1/ko active Active
- 2015-09-23 PL PL15844057T patent/PL3197868T3/pl unknown
- 2015-09-23 ES ES20159713T patent/ES2911004T3/es active Active
- 2015-09-23 MY MYPI2017700652A patent/MY182342A/en unknown
- 2015-09-23 ES ES21202255T patent/ES2956546T3/es active Active
- 2015-09-23 LT LTEP15844057.8T patent/LT3197868T/lt unknown
- 2015-09-23 HU HUE15844057A patent/HUE049698T2/hu unknown
- 2015-09-23 EP EP15844057.8A patent/EP3197868B1/en active Active
- 2015-09-23 SG SG11201702023QA patent/SG11201702023QA/en unknown
- 2015-09-23 EP EP20159713.5A patent/EP3683207B1/en active Active
- 2015-09-23 CA CA2962569A patent/CA2962569C/en active Active
- 2015-09-23 AP AP2017009832A patent/AP2017009832A0/en unknown
- 2015-09-23 CN CN201580051671.3A patent/CN106795111B/zh active Active
- 2015-09-25 TW TW104131936A patent/TWI687407B/zh active
- 2015-09-25 AR ARP150103084A patent/AR103199A1/es active IP Right Grant
- 2015-09-25 UY UY0001036326A patent/UY36326A/es active IP Right Grant
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2017
- 2017-02-13 ZA ZA2017/01061A patent/ZA201701061B/en unknown
- 2017-02-28 CL CL2017000474A patent/CL2017000474A1/es unknown
- 2017-03-02 IL IL250909A patent/IL250909B/en active IP Right Grant
- 2017-03-15 CO CONC2017/0002494A patent/CO2017002494A2/es unknown
- 2017-03-17 PH PH12017500513A patent/PH12017500513A1/en unknown
- 2017-03-24 GT GT201700062A patent/GT201700062A/es unknown
- 2017-04-24 EC ECIEPI201725302A patent/ECSP17025302A/es unknown
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2019
- 2019-01-23 US US16/255,500 patent/US10781174B2/en active Active
- 2019-01-23 JP JP2019008873A patent/JP6772307B2/ja active Active
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2020
- 2020-06-15 CY CY20201100542T patent/CY1123533T1/el unknown
- 2020-08-12 US US16/991,684 patent/US20200369610A1/en not_active Abandoned
- 2020-09-30 JP JP2020166129A patent/JP7216060B2/ja active Active
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2022
- 2022-05-03 US US17/735,386 patent/US12145909B2/en active Active
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2023
- 2023-01-19 JP JP2023006525A patent/JP7612722B2/ja active Active
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2024
- 2024-12-25 JP JP2024228390A patent/JP2025060835A/ja active Pending