BR112017006093A2 - moduladores alostéricos negativos de n-alquilaril-5-oxiaril-octa-hidro-ciclopenta[c] pirrol de nr2b - Google Patents
moduladores alostéricos negativos de n-alquilaril-5-oxiaril-octa-hidro-ciclopenta[c] pirrol de nr2bInfo
- Publication number
- BR112017006093A2 BR112017006093A2 BR112017006093A BR112017006093A BR112017006093A2 BR 112017006093 A2 BR112017006093 A2 BR 112017006093A2 BR 112017006093 A BR112017006093 A BR 112017006093A BR 112017006093 A BR112017006093 A BR 112017006093A BR 112017006093 A2 BR112017006093 A2 BR 112017006093A2
- Authority
- BR
- Brazil
- Prior art keywords
- oxyaryl
- alkylaryl
- nr2b
- allosteric modulators
- negative allosteric
- Prior art date
Links
- 229940126662 negative allosteric modulator Drugs 0.000 title abstract 2
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 abstract 2
- 101100240516 Caenorhabditis elegans nhr-10 gene Proteins 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 229910052757 nitrogen Chemical group 0.000 abstract 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/52—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Abstract
a presente invenção refere-se a moduladores alostéricos negativos de n-alquilaril-5-oxiaril-octadi-hidrociclopent[c]pirrol de receptores de nr2b úteis no tratamento de doenças neurológicas tendo a fórmula i onde r1, r2, l1, l2, x, y, e y? são descritos aqui. em um aspecto, compostos da fórmula i são descritos e sais farmaceuticamente aceitáveis, profármacos, solvatos, hidratos, tautômeros ou este-reoisômeros dos mesmos, em que: l1 é c1-c5 alquila linear ou ramifi-cada substituída com um ou mais substituintes selecionados a partir do grupo consistindo em oh, or10, nh2, nhr10 e n(r10)(r10?) contanto que não mais do que um oxigênio ou nitrogênio seja ligado a qualquer carbo-no.
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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| BR112017006093A2 true BR112017006093A2 (pt) | 2017-12-19 |
| BR112017006093B1 BR112017006093B1 (pt) | 2023-03-21 |
Family
ID=55581945
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112017006093-0A BR112017006093B1 (pt) | 2014-09-26 | 2015-09-23 | Moduladores alostéricos negativos de n-alquilaril-5-oxiaril-octa- hidro-ciclopenta[c]pirrol de nr2b |
Country Status (40)
| Country | Link |
|---|---|
| US (4) | US10239835B2 (pt) |
| EP (4) | EP3974420B1 (pt) |
| JP (4) | JP6473227B2 (pt) |
| KR (1) | KR102479356B1 (pt) |
| CN (1) | CN106795111B (pt) |
| AP (1) | AP2017009832A0 (pt) |
| AR (1) | AR103199A1 (pt) |
| AU (1) | AU2015320721B2 (pt) |
| BR (1) | BR112017006093B1 (pt) |
| CA (1) | CA2962569C (pt) |
| CL (1) | CL2017000474A1 (pt) |
| CO (1) | CO2017002494A2 (pt) |
| CR (1) | CR20170114A (pt) |
| CU (1) | CU24482B1 (pt) |
| CY (1) | CY1123533T1 (pt) |
| DK (1) | DK3197868T3 (pt) |
| EA (1) | EA034937B1 (pt) |
| EC (1) | ECSP17025302A (pt) |
| ES (3) | ES2791327T3 (pt) |
| GT (1) | GT201700062A (pt) |
| HR (1) | HRP20200959T1 (pt) |
| HU (1) | HUE049698T2 (pt) |
| IL (1) | IL250909B (pt) |
| JO (1) | JO3579B1 (pt) |
| LT (1) | LT3197868T (pt) |
| MX (1) | MX2017003940A (pt) |
| MY (1) | MY182342A (pt) |
| NZ (1) | NZ729569A (pt) |
| PE (1) | PE20170893A1 (pt) |
| PH (1) | PH12017500513A1 (pt) |
| PL (1) | PL3197868T3 (pt) |
| PT (1) | PT3197868T (pt) |
| RS (1) | RS60497B1 (pt) |
| SG (1) | SG11201702023QA (pt) |
| SI (1) | SI3197868T1 (pt) |
| TN (1) | TN2017000076A1 (pt) |
| TW (1) | TWI687407B (pt) |
| UY (1) | UY36326A (pt) |
| WO (1) | WO2016049165A1 (pt) |
| ZA (1) | ZA201701061B (pt) |
Families Citing this family (11)
| 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 |
| EP3697759A4 (en) | 2017-10-20 | 2021-05-12 | Vanderbilt University | MUSCARINIAN ACETYLCHOLINE RECEPTOR ANTAGONISTS M4 |
| US11352344B2 (en) | 2017-10-31 | 2022-06-07 | Vanderbilt University | Antagonists of the muscarinic acetylcholine receptor M4 |
| WO2019152809A1 (en) | 2018-02-02 | 2019-08-08 | Vanderbilt University | Antagonists of the muscarinic acetylcholine receptor m4 |
| 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 |
| JP2023551943A (ja) | 2020-12-04 | 2023-12-13 | ノバルティス アーゲー | うつ病の処置のためのｎｒ２ｂ－ｎｍｄａ受容体ｎａｍについての投薬レジメン |
| JP2021058765A (ja) * | 2021-01-19 | 2021-04-15 | 株式会社藤商事 | 遊技機 |
| IL305601A (en) * | 2021-03-26 | 2023-11-01 | Novartis Ag | Novel cyclopental[C]pyro-type 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 |
| TW202402271A (zh) | 2022-06-02 | 2024-01-16 | 瑞士商諾華公司 | Ｎｒ２ｂ—ｎｍｄａ受體ｎａｍ用於憂鬱障礙的劑量 |
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| 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 |
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| MX2011006169A (es) | 2008-12-12 | 2011-06-27 | Univ Vanderbilt | Inhibidores 3.3.0-biciclicos de giyt1 y metodos para hacer y utilizar los mismos. |
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| FR2945534B1 (fr) | 2009-05-12 | 2012-11-16 | Sanofi Aventis | DERIVES DE CYCLOPENTAL[c]PYRROLE-2-CARBOXYLATES, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE |
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| 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 LT LTEP15844057.8T patent/LT3197868T/lt unknown
- 2015-09-23 JP JP2017516358A patent/JP6473227B2/ja active Active
- 2015-09-23 EP EP21202255.2A patent/EP3974420B1/en active Active
- 2015-09-23 PE PE2017000506A patent/PE20170893A1/es unknown
- 2015-09-23 AP AP2017009832A patent/AP2017009832A0/en unknown
- 2015-09-23 ES ES15844057T patent/ES2791327T3/es active Active
- 2015-09-23 CU CU2017000037A patent/CU24482B1/es unknown
- 2015-09-23 ES ES21202255T patent/ES2956546T3/es active Active
- 2015-09-23 DK DK15844057.8T patent/DK3197868T3/da active
- 2015-09-23 SG SG11201702023QA patent/SG11201702023QA/en unknown
- 2015-09-23 HU HUE15844057A patent/HUE049698T2/hu unknown
- 2015-09-23 NZ NZ729569A patent/NZ729569A/en unknown
- 2015-09-23 EP EP20159713.5A patent/EP3683207B1/en active Active
- 2015-09-23 SI SI201531255T patent/SI3197868T1/sl unknown
- 2015-09-23 CA CA2962569A patent/CA2962569C/en active Active
- 2015-09-23 BR BR112017006093-0A patent/BR112017006093B1/pt active IP Right Grant
- 2015-09-23 TN TN2017000076A patent/TN2017000076A1/en unknown
- 2015-09-23 WO PCT/US2015/051694 patent/WO2016049165A1/en active Application Filing
- 2015-09-23 CR CR20170114A patent/CR20170114A/es unknown
- 2015-09-23 PT PT158440578T patent/PT3197868T/pt unknown
- 2015-09-23 US US15/506,592 patent/US10239835B2/en active Active
- 2015-09-23 AU AU2015320721A patent/AU2015320721B2/en active Active
- 2015-09-23 KR KR1020177007813A patent/KR102479356B1/ko active IP Right Grant
- 2015-09-23 MY MYPI2017700652A patent/MY182342A/en unknown
- 2015-09-23 CN CN201580051671.3A patent/CN106795111B/zh active Active
- 2015-09-23 PL PL15844057T patent/PL3197868T3/pl unknown
- 2015-09-23 EP EP15844057.8A patent/EP3197868B1/en active Active
- 2015-09-23 EP EP23185898.6A patent/EP4282412A3/en active Pending
- 2015-09-23 EA EA201790713A patent/EA034937B1/ru not_active IP Right Cessation
- 2015-09-23 MX MX2017003940A patent/MX2017003940A/es active IP Right Grant
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- 2015-09-25 UY UY0001036326A patent/UY36326A/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
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2019
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2020
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2022
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