JP6546596B2 - Nr2bの選択的オクタヒドロ−シクロペンタ[c]ピロール負調節因子 - Google Patents
Nr2bの選択的オクタヒドロ−シクロペンタ[c]ピロール負調節因子 Download PDFInfo
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- JP6546596B2 JP6546596B2 JP2016545243A JP2016545243A JP6546596B2 JP 6546596 B2 JP6546596 B2 JP 6546596B2 JP 2016545243 A JP2016545243 A JP 2016545243A JP 2016545243 A JP2016545243 A JP 2016545243A JP 6546596 B2 JP6546596 B2 JP 6546596B2
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- pyrrol
- octahydrocyclopenta
- hydroxy
- benzyl
- pyrrole
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- 0 **C(*)(CC1)CCN1I* Chemical compound **C(*)(CC1)CCN1I* 0.000 description 6
- MTOYTLBXGAYODC-UHFFFAOYSA-N C=CC/N=N\N[Br]=C Chemical compound C=CC/N=N\N[Br]=C MTOYTLBXGAYODC-UHFFFAOYSA-N 0.000 description 1
- LSQWMEZEZKNSLA-NOLUUDBRSA-N CC(C(CCO)c(cc1)ccc1O)N1C[C@H](C[C@](Cc2ccccc2)(C2)F)[C@H]2C1 Chemical compound CC(C(CCO)c(cc1)ccc1O)N1C[C@H](C[C@](Cc2ccccc2)(C2)F)[C@H]2C1 LSQWMEZEZKNSLA-NOLUUDBRSA-N 0.000 description 1
- MECAHFSQQZQZOI-UHFFFAOYSA-N CC(C)(C)OC(N(C1)CC1=C)=O Chemical compound CC(C)(C)OC(N(C1)CC1=C)=O MECAHFSQQZQZOI-UHFFFAOYSA-N 0.000 description 1
- QOFLPTJYZWTYNE-FVCICTRLSA-N CC(C)(C)c1ccc([C@@](C2)(C[C@@H](C3)[C@H]2CN3F)O)cc1 Chemical compound CC(C)(C)c1ccc([C@@](C2)(C[C@@H](C3)[C@H]2CN3F)O)cc1 QOFLPTJYZWTYNE-FVCICTRLSA-N 0.000 description 1
- MYTWNIBEFOQJBS-FVCICTRLSA-N CC(C)(C)c1ccc([C@@](C2)(C[C@@H]3[C@H]2CNC3)O)cc1 Chemical compound CC(C)(C)c1ccc([C@@](C2)(C[C@@H]3[C@H]2CNC3)O)cc1 MYTWNIBEFOQJBS-FVCICTRLSA-N 0.000 description 1
- QWVHZZVJXVHVHK-UHFFFAOYSA-N CC(C)(c(cc1)ccc1C(CBr)=O)O Chemical compound CC(C)(c(cc1)ccc1C(CBr)=O)O QWVHZZVJXVHVHK-UHFFFAOYSA-N 0.000 description 1
- XZIUKEJTWSKJBW-UHFFFAOYSA-N CC(c1ccc2[nH]nnc2c1)=O Chemical compound CC(c1ccc2[nH]nnc2c1)=O XZIUKEJTWSKJBW-UHFFFAOYSA-N 0.000 description 1
- PDEYDCVFGMWDBQ-UHFFFAOYSA-N CN(C(c(cc1)cc2c1[nH]nn2)=O)OC Chemical compound CN(C(c(cc1)cc2c1[nH]nn2)=O)OC PDEYDCVFGMWDBQ-UHFFFAOYSA-N 0.000 description 1
- SDZLYPFMASMVQF-UHFFFAOYSA-N FC(c1cc(C2OC2)ccc1)(F)F Chemical compound FC(c1cc(C2OC2)ccc1)(F)F SDZLYPFMASMVQF-UHFFFAOYSA-N 0.000 description 1
- WFLBQFSWPJODCW-IHRRRGAJSA-N N[C@]1(C[C@](Cc2ccccc2)(C2)O)[C@@H]2CNC1 Chemical compound N[C@]1(C[C@](Cc2ccccc2)(C2)O)[C@@H]2CNC1 WFLBQFSWPJODCW-IHRRRGAJSA-N 0.000 description 1
- GUOVBFFLXKJFEE-UHFFFAOYSA-N OC(c(cc1)cc2c1[nH]nn2)=O Chemical compound OC(c(cc1)cc2c1[nH]nn2)=O GUOVBFFLXKJFEE-UHFFFAOYSA-N 0.000 description 1
- XCEHEPNIWGDJSA-NGRWLJPCSA-N O[C@@](Cc1ccccc1)(C1)C[C@@H]2[C@H]1CN(CC(c(cc1)ccc1O)=O)C2 Chemical compound O[C@@](Cc1ccccc1)(C1)C[C@@H]2[C@H]1CN(CC(c(cc1)ccc1O)=O)C2 XCEHEPNIWGDJSA-NGRWLJPCSA-N 0.000 description 1
- NNIRHUJLEYJPPW-WDNDVIMCSA-N O[C@@](Cc1ccccc1)(C1)C[C@@H]2[C@H]1CNC2 Chemical compound O[C@@](Cc1ccccc1)(C1)C[C@@H]2[C@H]1CNC2 NNIRHUJLEYJPPW-WDNDVIMCSA-N 0.000 description 1
- XCEHEPNIWGDJSA-HATOLVCRSA-N O[C@](Cc1ccccc1)(C1)C[C@@H]2[C@H]1CN(CC(c(cc1)ccc1O)=O)C2 Chemical compound O[C@](Cc1ccccc1)(C1)C[C@@H]2[C@H]1CN(CC(c(cc1)ccc1O)=O)C2 XCEHEPNIWGDJSA-HATOLVCRSA-N 0.000 description 1
- HPFVHVCEUGWDMQ-UHFFFAOYSA-N Oc(c(F)cc(C(CBr)=O)c1)c1F Chemical compound Oc(c(F)cc(C(CBr)=O)c1)c1F HPFVHVCEUGWDMQ-UHFFFAOYSA-N 0.000 description 1
- LJYOFQHKEWTQRH-UHFFFAOYSA-N Oc(cc1)ccc1C(CBr)=O Chemical compound Oc(cc1)ccc1C(CBr)=O LJYOFQHKEWTQRH-UHFFFAOYSA-N 0.000 description 1
- SPBWTPSYDUTQIM-UHFFFAOYSA-N Oc1ccc(C(CBr)=O)nc1 Chemical compound Oc1ccc(C(CBr)=O)nc1 SPBWTPSYDUTQIM-UHFFFAOYSA-N 0.000 description 1
- YBMKFUSPXPIFMT-UHFFFAOYSA-N Oc1ncc(C(CBr)=O)nc1 Chemical compound Oc1ncc(C(CBr)=O)nc1 YBMKFUSPXPIFMT-UHFFFAOYSA-N 0.000 description 1
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- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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- C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
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- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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Applications Claiming Priority (3)
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| US201361883050P | 2013-09-26 | 2013-09-26 | |
| US61/883,050 | 2013-09-26 | ||
| PCT/US2014/057800 WO2015048507A1 (en) | 2013-09-26 | 2014-09-26 | Selective octahydro-cyclopenta[c] pyrrole negative modulators of nr2b |
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| JP2016536348A JP2016536348A (ja) | 2016-11-24 |
| JP2016536348A5 JP2016536348A5 (enExample) | 2017-11-24 |
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| TW (1) | TW201605791A (enExample) |
| UY (1) | UY35750A (enExample) |
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| AR097794A1 (es) | 2013-09-26 | 2016-04-13 | Mnemosyne Pharmaceuticals Inc | Moduladores octahidro-ciclopenta[c]pirrol negativos de nr2b |
| 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 |
| AU2016303558B2 (en) * | 2015-08-05 | 2020-08-06 | Indivior Uk Limited | Dopamine D3 receptor antagonists having a bicyclo moiety |
| WO2018232158A1 (en) * | 2017-06-15 | 2018-12-20 | Belite Bio, Inc. | Methods of treating metabolic diseases with fused bicyclic pyrroles |
| US11452881B2 (en) | 2019-01-03 | 2022-09-27 | Avive Solutions, Inc. | Defibrillator communications architecture |
| IL303357A (en) * | 2020-12-04 | 2023-08-01 | Novartis Ag | Dosage regimen for a nr2b-nmda receptor nam for the treatment of depression |
| WO2022204337A1 (en) * | 2021-03-26 | 2022-09-29 | Novartis Ag | Novel cyclopenta[c]pyrrol negative allosteric modulators of nr2b |
| IL305601A (en) * | 2021-03-26 | 2023-11-01 | Novartis Ag | Novel cyclopental[C]pyro-type negative allosteric modulators of NR2B |
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| US5532243A (en) | 1992-02-14 | 1996-07-02 | The Dupont Merck Pharmaceutical Company | Antipsychotic nitrogen-containing bicyclic compounds |
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| DE4341403A1 (de) | 1993-12-04 | 1995-06-08 | Basf Ag | N-substituierte 3-Azabicycloalkan-Derivate, ihre Herstellung und Verwendung |
| US5541217A (en) * | 1995-05-17 | 1996-07-30 | Ortho Pharmaceutical Corporation | 4-arylcyclopenta[c]pyrrole analgesics |
| US6369076B1 (en) * | 1999-10-29 | 2002-04-09 | Merck & Co. Inc. | 5-benzyl-octahydroindole and 6-benzyl-decahydroquinoline NMDA/NR2B antagonists |
| MXPA03008109A (es) * | 2001-03-07 | 2003-12-12 | Pfizer Prod Inc | Moduladores de la actividad de receptores de quimiocinas. |
| HUP0400467A3 (en) | 2001-04-19 | 2012-08-28 | Eisai R & D Man Co | 2-iminopyrrolidine derivatives, pharmaceutical compositions containing them and their use |
| 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 |
| ES2297727T3 (es) * | 2004-06-09 | 2008-05-01 | F. Hoffmann-La Roche Ag | Derivados de octahidropirrolo(3,4-c)pirrol y su empleo como agentes antiviricos. |
| 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 |
| JP2008536927A (ja) * | 2005-04-19 | 2008-09-11 | メルク エンド カムパニー インコーポレーテッド | N−アルキル−アザシクロアルキルnmda/nr2b拮抗物質 |
| US8299113B2 (en) | 2006-04-28 | 2012-10-30 | Laboratorios Del Dr. Esteve, S.A. | Bicyclic tetrahydropyrrole compounds |
| EP1849772A1 (en) | 2006-04-28 | 2007-10-31 | Laboratorios Del Dr. Esteve, S.A. | Bicyclic tetrahydropyrrole compounds |
| CN101230058A (zh) | 2007-01-23 | 2008-07-30 | 上海恒瑞医药有限公司 | 双环氮杂烷类衍生物、其制备方法及其在医药上的用途 |
| TW200845977A (en) | 2007-03-30 | 2008-12-01 | Targacept Inc | Sub-type selective azabicycloalkane derivatives |
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| CA2712352C (en) | 2008-01-23 | 2016-05-10 | Jiangsu Hansoh Pharmaceutical Co., Ltd. | Dicycloazaalkane derivates, preparation processes and medical uses thereof |
| US8211933B2 (en) | 2008-12-12 | 2012-07-03 | Vanderbilt University | 3.3.0 bicyclic GlyT1 inhibitors and methods of making and using same |
| FR2945534B1 (fr) | 2009-05-12 | 2012-11-16 | Sanofi Aventis | DERIVES DE CYCLOPENTAL[c]PYRROLE-2-CARBOXYLATES, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE |
| 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 |
| PL2521450T3 (pl) | 2010-01-07 | 2015-07-31 | Du Pont | Grzybobójcze związki heterocykliczne |
| US8796470B2 (en) | 2010-05-25 | 2014-08-05 | Abbvie Inc. | Substituted octahydrocyclopenta[c]pyrroles as calcium channel modulators |
| WO2011149995A1 (en) * | 2010-05-25 | 2011-12-01 | Abbott Laboratories | Novel substituted octahydrocyclopenta [c]pyrrol-4-amines as calcium channel blockers |
| US8501768B2 (en) | 2011-05-17 | 2013-08-06 | Hoffmann-La Roche Inc. | Hexahydrocyclopentapyrrolone, hexahydropyrrolopyrrolone, octahydropyrrolopyridinone and octahydropyridinone compounds |
| WO2012174199A1 (en) * | 2011-06-16 | 2012-12-20 | Merck Sharp & Dohme Corp. | Imidazopyridin-2-one derivatives |
| US9226923B2 (en) * | 2011-07-27 | 2016-01-05 | Nanjing Allgen Pharma Co. Ltd. | Spirocyclic molecules as protein kinase inhibitors |
| 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 |
| SMT201800497T1 (it) | 2011-12-21 | 2018-11-09 | Shanghai hengrui pharmaceutical co ltd | Derivato di pirrolo ad anello eteroarilico a sei elementi, relativo metodo di preparazione, e relativi usi medicinali |
| AU2013322838B2 (en) * | 2012-09-25 | 2018-02-01 | F. Hoffmann-La Roche Ag | New bicyclic derivatives |
| AR095079A1 (es) * | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| AR097794A1 (es) | 2013-09-26 | 2016-04-13 | Mnemosyne Pharmaceuticals Inc | Moduladores octahidro-ciclopenta[c]pirrol negativos de nr2b |
| AU2015238537B2 (en) * | 2014-03-26 | 2019-08-01 | F. Hoffmann-La Roche Ag | Bicyclic compounds as autotaxin (ATX) and lysophosphatidic acid (LPA) production inhibitors |
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| AR097794A1 (es) | 2016-04-13 |
| US20150225342A1 (en) | 2015-08-13 |
| EP3461827B1 (en) | 2022-02-23 |
| EP3461827A1 (en) | 2019-04-03 |
| TW201605791A (zh) | 2016-02-16 |
| US20230012073A1 (en) | 2023-01-12 |
| ES2910848T3 (es) | 2022-05-13 |
| WO2015048507A1 (en) | 2015-04-02 |
| CN105916843B (zh) | 2019-09-20 |
| US9540324B2 (en) | 2017-01-10 |
| JP2016536348A (ja) | 2016-11-24 |
| US20180325868A1 (en) | 2018-11-15 |
| US20170071906A1 (en) | 2017-03-16 |
| US11116749B2 (en) | 2021-09-14 |
| US12161624B2 (en) | 2024-12-10 |
| ES2707739T3 (es) | 2019-04-04 |
| EP3036221A4 (en) | 2017-01-25 |
| EP3036221A1 (en) | 2016-06-29 |
| CN105916843A (zh) | 2016-08-31 |
| US10052306B2 (en) | 2018-08-21 |
| EP3036221B1 (en) | 2018-11-07 |
| UY35750A (es) | 2015-04-30 |
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