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
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- 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 (cg-RX-API-DMAC7.html) | 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 |
| CA3079617A1 (en) | 2017-10-20 | 2019-04-25 | Vanderbilt University | Antagonists of the muscarinic acetylcholine receptor m4 |
| WO2019089676A1 (en) | 2017-10-31 | 2019-05-09 | Vanderbilt University | Antagonists of the muscarinic acetylcholine receptor m4 |
| CA3090130A1 (en) | 2018-02-02 | 2019-08-08 | Vanderbilt University | Antagonists of the muscarinic acetylcholine receptor m4 |
| SG11202008113RA (en) | 2018-03-05 | 2020-09-29 | Arcus Biosciences Inc | Arginase inhibitors |
| EP3980420B1 (en) | 2019-06-04 | 2023-04-19 | Boehringer Ingelheim International GmbH | Imidazopyrazine derivatives and the use thereof as medicament |
| EP3980401A1 (en) * | 2019-06-04 | 2022-04-13 | 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 |
| IL303357A (en) * | 2020-12-04 | 2023-08-01 | Novartis Ag | Dosage regimen for a nr2b-nmda receptor nam for the treatment of depression |
| JP2021058765A (ja) * | 2021-01-19 | 2021-04-15 | 株式会社藤商事 | 遊技機 |
| EP4313042A4 (en) * | 2021-03-26 | 2025-01-15 | Novartis AG | NEW CYCLOPENTA[C PYRROL NEGATIVE ALLOSTERIC MODULATORS OF NR2B |
| CA3212203A1 (en) * | 2021-03-26 | 2022-09-29 | Novartis Ag | Novel cyclopenta[c]pyrrol negative allosteric modulators of nr2b |
| JP2025518778A (ja) | 2022-06-02 | 2025-06-19 | ノバルティス アーゲー | 鬱病性障害の治療に使用するためのオンファスプロジルの皮下投与及び投与方法 |
| EP4649143A1 (en) | 2023-01-12 | 2025-11-19 | Novartis AG | Engineered ketoreductase polypeptides |
| 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 |
| WO2005121145A2 (en) | 2004-06-09 | 2005-12-22 | F. Hoffmann-La Roche Ag | Octahydro-pyrrolo[3,4-c] derivatives and their use as antiviral compounds |
| JP2008507543A (ja) | 2004-07-22 | 2008-03-13 | グラクソ グループ リミテッド | 抗細菌剤 |
| HUP0401523A3 (en) | 2004-07-29 | 2007-05-02 | Richter Gedeon Vegyeszet | Indole-2-carboxamide derivatives, pharmaceutical compositions containing them and process for producing them |
| AU2006236625A1 (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 |
| WO2007128458A1 (en) | 2006-04-28 | 2007-11-15 | Laboratorios Del Dr. Esteve, S.A. | Bicyclic tetrahydropyrrole compounds |
| TW200845977A (en) | 2007-03-30 | 2008-12-01 | Targacept Inc | Sub-type selective azabicycloalkane derivatives |
| EP2217596B8 (en) | 2007-10-22 | 2013-11-20 | Merck Sharp & Dohme Corp. | Bicyclic heterocycle derivatives and their use as modulators of the activity of gpr119 |
| WO2009094866A1 (en) | 2008-01-23 | 2009-08-06 | Shanghai Hengrui Pharmaceutical Co., Ltd. | Dicycloazaalkane derivates, preparation processes and medical uses thereof |
| EP2378885A4 (en) | 2008-12-12 | 2013-01-02 | Univ Vanderbilt | 3.3.0 BICYCLIC GLYT1 INHIBITORS AND METHOD FOR THE PRODUCTION AND USE THEREOF |
| 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 |
| WO2011085170A1 (en) | 2010-01-07 | 2011-07-14 | E. I. Du Pont De Nemours And Company | Fungicidal heterocyclic compounds |
| US8796470B2 (en) | 2010-05-25 | 2014-08-05 | Abbvie Inc. | 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 |
| SI2796460T1 (sl) | 2011-12-21 | 2018-10-30 | Jiangsu Hengrui Medicine Co. Ltd | Pirolni šestčlenski derivat heteroarilnega obroča, postopek priprave zanj in medicinske uporabe le-tega |
| ES2753163T3 (es) * | 2012-09-25 | 2020-04-07 | Hoffmann La Roche | Derivados de hexahidropirrolo[3,4-c]pirrol y compuestos relacionados como inhibidores de la autotaxina (ATX) y como inhibidores de la producción de ácido lisofosfatídico (LPA) para tratar, por ejemplo, enfermedades renales |
| 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 |
| EP3461827B1 (en) * | 2013-09-26 | 2022-02-23 | Cadent Therapeutics, Inc. | Selective octahydro-cyclopenta[c]pyrrole negative modulators of nr2b |
| SG11201607839UA (en) | 2014-03-26 | 2016-10-28 | Hoffmann La Roche | Bicyclic compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors |
| 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 EP EP21202255.2A patent/EP3974420B1/en active Active
- 2015-09-23 ES ES20159713T patent/ES2911004T3/es active Active
- 2015-09-23 CN CN201580051671.3A patent/CN106795111B/zh active Active
- 2015-09-23 LT LTEP15844057.8T patent/LT3197868T/lt unknown
- 2015-09-23 JP JP2017516358A patent/JP6473227B2/ja active Active
- 2015-09-23 PT PT158440578T patent/PT3197868T/pt unknown
- 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 EA EA201790713A patent/EA034937B1/ru not_active IP Right Cessation
- 2015-09-23 PL PL15844057T patent/PL3197868T3/pl unknown
- 2015-09-23 SI SI201531255T patent/SI3197868T1/sl unknown
- 2015-09-23 ES ES15844057T patent/ES2791327T3/es active Active
- 2015-09-23 MX MX2017003940A patent/MX374657B/es active IP Right Grant
- 2015-09-23 CA CA2962569A patent/CA2962569C/en active Active
- 2015-09-23 EP EP15844057.8A patent/EP3197868B1/en active Active
- 2015-09-23 TN TN2017000076A patent/TN2017000076A1/en unknown
- 2015-09-23 AP AP2017009832A patent/AP2017009832A0/en unknown
- 2015-09-23 SG SG11201702023QA patent/SG11201702023QA/en unknown
- 2015-09-23 RS RS20200721A patent/RS60497B1/sr unknown
- 2015-09-23 MY MYPI2017700652A patent/MY182342A/en unknown
- 2015-09-23 ES ES21202255T patent/ES2956546T3/es active Active
- 2015-09-23 HR HRP20200959TT patent/HRP20200959T1/hr unknown
- 2015-09-23 KR KR1020177007813A patent/KR102479356B1/ko active Active
- 2015-09-23 WO PCT/US2015/051694 patent/WO2016049165A1/en not_active Ceased
- 2015-09-23 NZ NZ729569A patent/NZ729569A/en not_active IP Right Cessation
- 2015-09-23 EP EP23185898.6A patent/EP4282412A3/en active Pending
- 2015-09-23 AU AU2015320721A patent/AU2015320721B2/en active Active
- 2015-09-23 BR BR112017006093-0A patent/BR112017006093B1/pt active IP Right Grant
- 2015-09-23 CU CU2017000037A patent/CU24482B1/es unknown
- 2015-09-23 EP EP20159713.5A patent/EP3683207B1/en active Active
- 2015-09-23 HU HUE15844057A patent/HUE049698T2/hu unknown
- 2015-09-23 CR CR20170114A patent/CR20170114A/es unknown
- 2015-09-23 PE PE2017000506A patent/PE20170893A1/es unknown
- 2015-09-25 UY UY0001036326A patent/UY36326A/es active IP Right Grant
- 2015-09-25 AR ARP150103084A patent/AR103199A1/es active IP Right Grant
- 2015-09-25 TW TW104131936A patent/TWI687407B/zh active
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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 JP JP2019008873A patent/JP6772307B2/ja active Active
- 2019-01-23 US US16/255,500 patent/US10781174B2/en 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