ES2560095T3 - Amidas bicíclicas para mejorar las respuestas sinápticas glutamatérgicas - Google Patents
Amidas bicíclicas para mejorar las respuestas sinápticas glutamatérgicas Download PDFInfo
- Publication number
- ES2560095T3 ES2560095T3 ES08795126.5T ES08795126T ES2560095T3 ES 2560095 T3 ES2560095 T3 ES 2560095T3 ES 08795126 T ES08795126 T ES 08795126T ES 2560095 T3 ES2560095 T3 ES 2560095T3
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- unsubstituted
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- unbranched
- alkyl
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- -1 Bicyclic amides Chemical class 0.000 title description 5
- 230000000848 glutamatergic effect Effects 0.000 title description 2
- 230000009782 synaptic response Effects 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 abstract description 20
- 102000003678 AMPA Receptors Human genes 0.000 abstract description 6
- 108090000078 AMPA Receptors Proteins 0.000 abstract description 6
- 125000000217 alkyl group Chemical group 0.000 abstract description 4
- 229910052760 oxygen Inorganic materials 0.000 abstract description 4
- 150000003839 salts Chemical class 0.000 abstract description 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract description 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract description 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract description 2
- 125000003118 aryl group Chemical group 0.000 abstract description 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract description 2
- 125000004181 carboxyalkyl group Chemical group 0.000 abstract description 2
- 125000005026 carboxyaryl group Chemical group 0.000 abstract description 2
- 229910052736 halogen Inorganic materials 0.000 abstract description 2
- 150000002367 halogens Chemical class 0.000 abstract description 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract description 2
- 239000001301 oxygen Substances 0.000 abstract description 2
- 239000012453 solvate Substances 0.000 abstract description 2
- 125000004963 sulfonylalkyl group Chemical group 0.000 abstract description 2
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- UUDAMDVQRQNNHZ-UHFFFAOYSA-N (S)-AMPA Chemical compound CC=1ONC(=O)C=1CC(N)C(O)=O UUDAMDVQRQNNHZ-UHFFFAOYSA-N 0.000 description 1
- HEMGYNNCNNODNX-UHFFFAOYSA-N 3,4-diaminobenzoic acid Chemical compound NC1=CC=C(C(O)=O)C=C1N HEMGYNNCNNODNX-UHFFFAOYSA-N 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
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- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 1
- 206010012289 Dementia Diseases 0.000 description 1
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 1
- 208000020358 Learning disease Diseases 0.000 description 1
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- IDBPHNDTYPBSNI-UHFFFAOYSA-N N-(1-(2-(4-Ethyl-5-oxo-2-tetrazolin-1-yl)ethyl)-4-(methoxymethyl)-4-piperidyl)propionanilide Chemical compound C1CN(CCN2C(N(CC)N=N2)=O)CCC1(COC)N(C(=O)CC)C1=CC=CC=C1 IDBPHNDTYPBSNI-UHFFFAOYSA-N 0.000 description 1
- HOKKHZGPKSLGJE-GSVOUGTGSA-N N-Methyl-D-aspartic acid Chemical compound CN[C@@H](C(O)=O)CC(O)=O HOKKHZGPKSLGJE-GSVOUGTGSA-N 0.000 description 1
- 229910002651 NO3 Inorganic materials 0.000 description 1
- NHNBFGGVMKEFGY-UHFFFAOYSA-N Nitrate Chemical compound [O-][N+]([O-])=O NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 description 1
- IOVCWXUNBOPUCH-UHFFFAOYSA-M Nitrite anion Chemical compound [O-]N=O IOVCWXUNBOPUCH-UHFFFAOYSA-M 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 description 1
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- IVLVTNPOHDFFCJ-UHFFFAOYSA-N fentanyl citrate Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O.C=1C=CC=CC=1N(C(=O)CC)C(CC1)CCN1CCC1=CC=CC=C1 IVLVTNPOHDFFCJ-UHFFFAOYSA-N 0.000 description 1
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- VZCYOOQTPOCHFL-OWOJBTEDSA-L fumarate(2-) Chemical compound [O-]C(=O)\C=C\C([O-])=O VZCYOOQTPOCHFL-OWOJBTEDSA-L 0.000 description 1
- 229930195712 glutamate Natural products 0.000 description 1
- 229940015043 glyoxal Drugs 0.000 description 1
- XMBWDFGMSWQBCA-UHFFFAOYSA-N hydrogen iodide Chemical compound I XMBWDFGMSWQBCA-UHFFFAOYSA-N 0.000 description 1
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- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- YSVQLWJDHYBITL-UHFFFAOYSA-N ppse Chemical compound C[Si](C)(C)OP(=O)=O YSVQLWJDHYBITL-UHFFFAOYSA-N 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- UTEQROVYZDJSOO-UHFFFAOYSA-N quinoxaline-6-carbonyl chloride Chemical compound N1=CC=NC2=CC(C(=O)Cl)=CC=C21 UTEQROVYZDJSOO-UHFFFAOYSA-N 0.000 description 1
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- LSNNMFCWUKXFEE-UHFFFAOYSA-L sulfite Chemical compound [O-]S([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-L 0.000 description 1
- 230000000946 synaptic effect Effects 0.000 description 1
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- 230000002123 temporal effect Effects 0.000 description 1
- 210000003478 temporal lobe Anatomy 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-M toluene-4-sulfonate Chemical compound CC1=CC=C(S([O-])(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-M 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
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- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- WBYWAXJHAXSJNI-VOTSOKGWSA-M trans-cinnamate Chemical compound [O-]C(=O)\C=C\C1=CC=CC=C1 WBYWAXJHAXSJNI-VOTSOKGWSA-M 0.000 description 1
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Classifications
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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- A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D487/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/08—Bridged systems
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- General Chemical & Material Sciences (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Emergency Medicine (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Hydrogenated Pyridines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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| US964362P | 2007-08-10 | ||
| PCT/US2008/009508 WO2009023126A2 (en) | 2007-08-10 | 2008-08-08 | Bicyclic amides for enhancing glutamatergic synaptic responses |
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| ES2560095T3 true ES2560095T3 (es) | 2016-02-17 |
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| AU2007342365B2 (en) | 2007-01-03 | 2012-11-15 | Les Laboratoires Servier | 3-substituted-[1,2,3]-benzotriazinone compound for enhancing glutamatergic synaptic responses |
| US8013003B2 (en) | 2007-05-17 | 2011-09-06 | Cortex Pharmaceuticals, Inc. | Di-substituted amides for enhancing glutamatergic synaptic responses |
| KR20100045507A (ko) | 2007-08-10 | 2010-05-03 | 코텍스 파마슈티칼스, 인크. | 글루타메이트성 시냅스 반응을 향상시키기 위한 비시클릭 아미드 |
| US8168632B2 (en) | 2007-08-10 | 2012-05-01 | Cortex Pharmaceuticals, Inc. | Bicyclic amide derivatives for the treatment of respiratory disorders |
| SG173168A1 (en) * | 2009-02-02 | 2011-08-29 | Cortex Pharma Inc | Bicyclic amide derivatives for enhancing glutamatergic synaptic responses |
| US9440982B2 (en) | 2012-02-07 | 2016-09-13 | Eolas Therapeutics, Inc. | Substituted prolines/piperidines as orexin receptor antagonists |
| CN104220065A (zh) | 2012-02-07 | 2014-12-17 | Eolas治疗公司 | 取代的脯氨酸/哌啶用作食欲素受体拮抗剂 |
| US10221170B2 (en) | 2014-08-13 | 2019-03-05 | Eolas Therapeutics, Inc. | Difluoropyrrolidines as orexin receptor modulators |
| US9739787B2 (en) | 2015-09-01 | 2017-08-22 | Abdulmohsen Ebrahim Alterki | Method for diagnosing sleep apnea by measuring adipsin and betatrophin levels |
| SMT202200323T1 (it) | 2016-02-12 | 2022-09-14 | Astrazeneca Ab | Piperidine alo-sostituite come modulatori del recettore di oressina |
| US20190112300A1 (en) * | 2016-03-29 | 2019-04-18 | Arnold Stan Lippa | Compositions And Methods For Treating Attention Deficit Disorders |
| CA3140170A1 (en) | 2019-06-04 | 2020-12-10 | Belew Mekonnen | Imidazolo derivatives, compositions and methods as orexin antagonists |
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| US3723436A (en) | 1971-02-25 | 1973-03-27 | Sun Oil Co | Process for aromatic lactams |
| FR2597103B1 (fr) | 1986-04-15 | 1988-12-16 | Provesan Sa | Procede de preparation de derives d'oxazinobenzothiazine 6,6-dioxyde |
| PT1156043E (pt) | 1992-07-24 | 2004-03-31 | Univ California | Drogas que aumentam as respostas sinapticas mediadas por receptores de ampa |
| US20020099050A1 (en) | 1993-07-23 | 2002-07-25 | Lynch Gary S. | Drugs that enhance synaptic responses mediated by AMPA receptors |
| US5650409A (en) | 1995-06-02 | 1997-07-22 | Cortex Pharmaceuticals, Inc. | Benzoyl piperidines/pyrrolidines for enhancing synaptic response |
| US5736543A (en) | 1996-04-03 | 1998-04-07 | The Regents Of The University Of California | Benzoxazines for enhancing synaptic response |
| AU4416197A (en) | 1996-09-17 | 1998-04-14 | Regents Of The University Of California, The | Positive ampa receptor modulation to enhance brain neurotrophic factor expression |
| US6110935A (en) | 1997-02-13 | 2000-08-29 | The Regents Of The University Of California | Benzofurazan compounds for enhancing glutamatergic synaptic responses |
| JP2001520978A (ja) | 1997-10-27 | 2001-11-06 | コーテックス ファーマシューティカルズ， インコーポレイテッド | アンパカインおよび神経遮断薬を用いる精神分裂病の処置 |
| US5985871A (en) | 1997-12-24 | 1999-11-16 | Cortex Pharmaceuticals, Inc. | Benzoxazine compounds for enhancing synaptic response |
| JP2002504481A (ja) | 1998-02-18 | 2002-02-12 | ニューロサーチ、アクティーゼルスカブ | 新規化合物及び陽性ａｍｐａレセプターモジュレーターとしてこれを使用する方法 |
| US6713474B2 (en) | 1998-09-18 | 2004-03-30 | Abbott Gmbh & Co. Kg | Pyrrolopyrimidines as therapeutic agents |
| US6303542B1 (en) | 2000-08-18 | 2001-10-16 | Rohm And Haas Company | Herbicidal 3-substituted-phenyl-1,2,3-benzotriazin-4-ones |
| PA8535601A1 (es) * | 2000-12-21 | 2002-11-28 | Pfizer | Derivados benzimidazol y piridilimidazol como ligandos para gabaa |
| AUPS255202A0 (en) | 2002-05-27 | 2002-06-13 | Monash University | Agents and methods for the treatment of disorders associated with motor neuron degeneration |
| WO2004089416A2 (en) * | 2003-04-11 | 2004-10-21 | Novo Nordisk A/S | Combination of an 11beta-hydroxysteroid dehydrogenase type 1 inhibitor and an antihypertensive agent |
| US20050085446A1 (en) | 2003-04-14 | 2005-04-21 | Babu M.K. M. | Fluoroquinolone formulations and methods of making and using the same |
| GB0317482D0 (en) | 2003-07-25 | 2003-08-27 | Pfizer Ltd | Nicotinamide derivatives useful as pde4 inhibitors |
| CN1897950A (zh) | 2003-10-14 | 2007-01-17 | 惠氏公司 | 稠合芳基和杂芳基衍生物及其使用方法 |
| KR20090047534A (ko) | 2006-08-31 | 2009-05-12 | 더 거버너스 오브 더 유니버시티 오브 앨버타 | 양성 알로스테릭 ａｍｐａ 수용체 조절인자를 사용하여 호흡 저하를 억제하는 방법 |
| AU2007342365B2 (en) | 2007-01-03 | 2012-11-15 | Les Laboratoires Servier | 3-substituted-[1,2,3]-benzotriazinone compound for enhancing glutamatergic synaptic responses |
| KR20090098999A (ko) | 2007-01-03 | 2009-09-18 | 코텍스 파마슈티칼스, 인크. | 글루타메이트에 의한 시냅스 반응을 향상시키기 위한 3-치환된-[1,2,3]벤조트리아지논 화합물 |
| US8013003B2 (en) | 2007-05-17 | 2011-09-06 | Cortex Pharmaceuticals, Inc. | Di-substituted amides for enhancing glutamatergic synaptic responses |
| KR20100045507A (ko) | 2007-08-10 | 2010-05-03 | 코텍스 파마슈티칼스, 인크. | 글루타메이트성 시냅스 반응을 향상시키기 위한 비시클릭 아미드 |
| CN101801939A (zh) | 2007-09-20 | 2010-08-11 | 科泰克斯药品公司 | 用于增强谷氨酸能突触反应的3-取代1,2,3-三嗪-4-酮类和3-取代1,3-嘧啶酮类 |
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2008
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- 2008-08-08 MX MX2010001630A patent/MX2010001630A/es unknown
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- 2008-08-08 CA CA2702292A patent/CA2702292A1/en not_active Abandoned
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- 2008-08-08 AU AU2008287445A patent/AU2008287445A1/en not_active Abandoned
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2010
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2012
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