PE20231384A1 - Agonistas de bicicloheptano pirrolidina de los receptores de orexina - Google Patents
Agonistas de bicicloheptano pirrolidina de los receptores de orexinaInfo
- Publication number
- PE20231384A1 PE20231384A1 PE2023000316A PE2023000316A PE20231384A1 PE 20231384 A1 PE20231384 A1 PE 20231384A1 PE 2023000316 A PE2023000316 A PE 2023000316A PE 2023000316 A PE2023000316 A PE 2023000316A PE 20231384 A1 PE20231384 A1 PE 20231384A1
- Authority
- PE
- Peru
- Prior art keywords
- methyl
- alkyl
- pyrrolidine
- cycloalkyl
- orexin receptors
- Prior art date
Links
- 108050000742 Orexin Receptor Proteins 0.000 title abstract 3
- 102000008834 Orexin receptor Human genes 0.000 title abstract 3
- 239000000556 agonist Substances 0.000 title abstract 2
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 title 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 3
- -1 bicyclo[4.1.0]heptane pyrrolidine Chemical compound 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 208000019888 Circadian rhythm sleep disease Diseases 0.000 abstract 1
- 208000028698 Cognitive impairment Diseases 0.000 abstract 1
- 208000007590 Disorders of Excessive Somnolence Diseases 0.000 abstract 1
- 208000035895 Guillain-Barré syndrome Diseases 0.000 abstract 1
- 206010053712 Hypersomnia-bulimia syndrome Diseases 0.000 abstract 1
- 208000001456 Jet Lag Syndrome Diseases 0.000 abstract 1
- 201000008178 Kleine-Levin syndrome Diseases 0.000 abstract 1
- 206010049567 Miller Fisher syndrome Diseases 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 206010041349 Somnolence Diseases 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 208000033915 jet lag type circadian rhythm sleep disease Diseases 0.000 abstract 1
- 230000000926 neurological effect Effects 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 208000020016 psychiatric disease Diseases 0.000 abstract 1
- 230000036385 rapid eye movement (rem) sleep Effects 0.000 abstract 1
- 201000002859 sleep apnea Diseases 0.000 abstract 1
Classifications
-
- 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
-
- 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
- C07D403/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/14—Nitrogen atoms not forming part of a nitro radical
-
- 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
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D491/04—Ortho-condensed 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
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
Abstract
Esta referidos a compuestos derivados de biciclo[4.1.0]heptano pirrolidina De Formula I, en donde: Anillo A es como se indica a continuacion; X es O, NH-; R1 es alquilo C1-6, cicloalquilo C3-6 o heterociclilo; R2a y R2b son H, alquilo C1-6, entre otros; R2c y R2d son H o F; R3 es alquilo C1-6, cicloalquilo C3-6, entre otras opciones; R5 y R6 son H, alquilo C1-6 o cicloalquilo C3-6. Entre los compuestos preferidos tenemos los siguientes: (2R,3S,5R)-5-Metil-3-(metilsulfonamido)-2-(((6-fenilbiciclo[4.1.0]heptan-3- il)oxi)metil)pirrolidin-1-carboxilato de metilo; (2R,3S,5R)-2-(((6-(3,5-difluorofenil)biciclo[4.1.0]heptan-3-il)oxi)metil)-3-((N,Ndimetilsulfamoil)amino)-5-metilpirrolidin-1-carboxilato de metilo; entre otros. Estos compuestos son agonistas de los receptores de orexina y se emplean en el tratamiento o prevencion de trastornos y enfermedades neurologicas y psiquiatricas en las que estan involucrados los receptores de orexina como apnea del sueno, interrupciones del sueno REM, descompensacion horaria, somnolencia diurna excesiva, enfermedad de Alzheimer o deterioro cognitivo, enfermedad de Parkinson, sindrome de Guillain-Barre, sindrome de Kleine Levin, entre otros
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US202063066908P | 2020-08-18 | 2020-08-18 | |
US202163226798P | 2021-07-29 | 2021-07-29 | |
PCT/US2021/046098 WO2022040070A1 (en) | 2020-08-18 | 2021-08-16 | Bicycloheptane pyrrolidine orexin receptor agonists |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20231384A1 true PE20231384A1 (es) | 2023-09-12 |
Family
ID=77655694
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2023000316A PE20231384A1 (es) | 2020-08-18 | 2021-08-16 | Agonistas de bicicloheptano pirrolidina de los receptores de orexina |
Country Status (18)
Country | Link |
---|---|
US (2) | US20230365533A1 (es) |
EP (1) | EP4200295A1 (es) |
JP (1) | JP7443625B2 (es) |
KR (1) | KR20230053639A (es) |
CN (1) | CN116249697A (es) |
AU (1) | AU2021329805B2 (es) |
BR (1) | BR112023002957A2 (es) |
CA (1) | CA3189908A1 (es) |
CL (1) | CL2023000468A1 (es) |
CO (1) | CO2023001795A2 (es) |
CR (1) | CR20230089A (es) |
DO (1) | DOP2023000036A (es) |
EC (1) | ECSP23012026A (es) |
IL (1) | IL300610A (es) |
MX (1) | MX2023001840A (es) |
PE (1) | PE20231384A1 (es) |
TW (1) | TW202227417A (es) |
WO (1) | WO2022040070A1 (es) |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US11542276B2 (en) | 2019-11-25 | 2023-01-03 | Alkermes, Inc. | Substituted macrocyclic compounds and related methods of treatment |
US11760747B2 (en) | 2020-12-21 | 2023-09-19 | Alkermes, Inc. | Substituted piperidino compounds and related methods of treatment |
Family Cites Families (147)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US2263702A (en) | 1939-01-18 | 1941-11-25 | Konstruktion Und Verwertung Au | Centrifugal clutch construction |
US3914250A (en) | 1974-08-01 | 1975-10-21 | American Home Prod | 1,4-Diazepino{8 6,5,4-jk{9 carbazoles |
US4919602A (en) | 1987-12-21 | 1990-04-24 | Janszen Arthur W | Apparatus for repairing windshields |
WO1990005525A1 (en) | 1988-11-23 | 1990-05-31 | Pfizer Inc. | Quinuclidine derivatives as substance p antagonists |
US5232929A (en) | 1990-11-28 | 1993-08-03 | Pfizer Inc. | 3-aminopiperidine derivatives and related nitrogen containing heterocycles and pharmaceutical compositions and use |
US5112820A (en) | 1990-03-05 | 1992-05-12 | Sterling Drug Inc. | Anti-glaucoma compositions containing 2- and 3-aminomethyl-6-arylcarbonyl- or 6-phenylthio-2,3-dihydropyrrolo-(1,2,3-de)-1,4-benzoxazines and method of use thereof |
US5081122A (en) | 1990-03-05 | 1992-01-14 | Sterling Drug Inc. | Antiglaucoma compositions containing 4-arylcarbonyl-1-(4-morpholinyl)-lower-alkyl)-1H-indoles and method of use thereof |
US4973587A (en) | 1990-03-08 | 1990-11-27 | Sterling Drug Inc. | 3-arylcarbonyl-1-aminoalkyl-1H-indole-containing antiglaucoma method |
US5013837A (en) | 1990-03-08 | 1991-05-07 | Sterling Drug Inc. | 3-Arylcarbonyl-1H-indole-containing compounds |
DE69220258T2 (de) | 1991-02-11 | 1997-12-18 | Merck Sharp & Dohme | Azabicyclische Verbindungen, diese enthaltende pharmazeutische Zubereitungen und ihre therapeutische Verwendung |
DK0573522T3 (da) | 1991-03-01 | 1995-03-06 | Pfizer | 1-Azabicyclo(3,2,2)nonan-3-aminderivater |
ATE136885T1 (de) | 1991-08-20 | 1996-05-15 | Merck Sharp & Dohme | Azacyclische verbindungen, verfahren zu ihrer herstellung und diese enthaltende pharmazeutische zubereitungen |
GB9211193D0 (en) | 1992-05-27 | 1992-07-08 | Merck Sharp & Dohme | Therapeutic agents |
FR2692575B1 (fr) | 1992-06-23 | 1995-06-30 | Sanofi Elf | Nouveaux derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant. |
US5637699A (en) | 1992-06-29 | 1997-06-10 | Merck & Co., Inc. | Process for preparing morpholine tachykinin receptor antagonists |
US5387595A (en) | 1992-08-26 | 1995-02-07 | Merck & Co., Inc. | Alicyclic compounds as tachykinin receptor antagonists |
US5536716A (en) | 1992-12-11 | 1996-07-16 | Merck & Co., Inc. | Spiro piperidines and homologs which promote release of growth hormone |
US5292736A (en) | 1993-02-26 | 1994-03-08 | Sterling Winthrop Inc. | Morpholinoalkylindenes as antiglaucoma agents |
US5496833A (en) | 1993-04-13 | 1996-03-05 | Merck Sharp & Dohme Limited | Piperidine tachykinin receptor antagonists |
KR970707101A (ko) | 1994-11-07 | 1997-12-01 | 스피겔 알렌 제이 | 치환된 벤질아민 유도체; 신규한 부류의 신경펩타이드 y1 특이적 리간드(certain substituted benzylamine derivatives; a new class of neuropeptide y1 specific ligands) |
US5532237A (en) | 1995-02-15 | 1996-07-02 | Merck Frosst Canada, Inc. | Indole derivatives with affinity for the cannabinoid receptor |
US5831115A (en) | 1995-04-21 | 1998-11-03 | Abbott Laboratories | Inhibitors of squalene synthase and protein farnesyltransferase |
US5739106A (en) | 1995-06-07 | 1998-04-14 | Rink; Timothy J. | Appetite regulating compositions |
FR2741621B1 (fr) | 1995-11-23 | 1998-02-13 | Sanofi Sa | Nouveaux derives de pyrazole, procede pour leur preparation et compositions pharmaceutiques en contenant |
AU7626496A (en) | 1995-12-01 | 1997-06-27 | Ciba-Geigy Ag | Heteroaryl compounds |
WO1997019682A1 (en) | 1995-12-01 | 1997-06-05 | Synaptic Pharmaceutical Corporation | Aryl sulfonamide and sulfamide derivatives and uses thereof |
AU7692996A (en) | 1995-12-01 | 1997-06-27 | Ciba-Geigy Ag | Receptor antagonists |
AU7692896A (en) | 1995-12-01 | 1997-06-27 | Novartis Ag | Quinazolin-2,4-diazirines as NPY receptor antagonist |
AU7692696A (en) | 1995-12-01 | 1997-06-27 | Novartis Ag | Heteroaryl derivatives |
AU1856997A (en) | 1996-02-02 | 1997-08-22 | Merck & Co., Inc. | Method for raising hdl cholesterol levels |
US6017919A (en) | 1996-02-06 | 2000-01-25 | Japan Tobacco Inc. | Compounds and pharmaceutical use thereof |
GB9606805D0 (en) | 1996-03-30 | 1996-06-05 | Glaxo Wellcome Inc | Medicaments |
CA2273102A1 (en) | 1996-12-03 | 1998-06-11 | Banyu Pharmaceutical Co., Ltd. | Urea derivatives |
WO1998025907A1 (fr) | 1996-12-12 | 1998-06-18 | Banyu Pharmaceutical Co., Ltd. | Derives de pyrazole |
AU5410598A (en) | 1996-12-13 | 1998-07-03 | Banyu Pharmaceutical Co., Ltd. | Novel aminopyrazole derivatives |
EP0945440B1 (en) | 1996-12-16 | 2004-05-26 | Banyu Pharmaceutical Co., Ltd. | Aminopyrazole derivatives |
JP2001508799A (ja) | 1997-01-21 | 2001-07-03 | スミスクライン・ビーチャム・コーポレイション | 新規カンナビノイド受容体モジュレータ |
CN1246845A (zh) | 1997-02-04 | 2000-03-08 | 纳幕尔杜邦公司 | 杀菌的羧酰胺 |
WO1998037061A1 (de) | 1997-02-21 | 1998-08-27 | Bayer Aktiengesellschaft | Arylsulfonamide und analoga und ihre verwendung zur behandlung von neurodegenerativen erkrankungen |
WO1998040356A1 (fr) | 1997-03-12 | 1998-09-17 | Banyu Pharmaceutical Co., Ltd. | Medicaments contenant des derives d'aminopyridine comme ingredient actif |
EP0979228A4 (en) | 1997-03-18 | 2000-05-03 | Smithkline Beecham Corp | CANNABINOID RECEPTOR AGONISTS |
FR2761266B1 (fr) | 1997-03-28 | 1999-07-02 | Sanofi Sa | Composition pharmaceutique formee par granulation humide pour l'administration orale d'un derive du n-piperidino-3- pyrazolecarboxamide, de ses sels et de leurs solvates |
FR2761265B1 (fr) | 1997-03-28 | 1999-07-02 | Sanofi Sa | Composition pharmaceutique pour l'administration orale d'un derive du n-piperidino-3-pyrazolecarboxamide, de ses sels et de leurs solvates |
US6258837B1 (en) | 1997-04-23 | 2001-07-10 | Banyu Pharmaceutical Co., Ltd. | Neuropeptide Y receptor antagonist |
US6001836A (en) | 1997-05-28 | 1999-12-14 | Bristol-Myers Squibb Company | Dihydropyridine NPY antagonists: cyanoguanidine derivatives |
KR20010021696A (ko) | 1997-07-11 | 2001-03-15 | 미즈노 마사루 | 퀴놀린 화합물 및 그의 의약용도 |
AU9185598A (en) | 1997-09-25 | 1999-04-12 | Banyu Pharmaceutical Co., Ltd. | Novel neuropeptide y receptor antagonists |
WO1999027965A1 (fr) | 1997-11-28 | 1999-06-10 | Banyu Pharmaceutical Co., Ltd. | Agents anti-hyperlipemiques |
AU3464599A (en) | 1998-04-02 | 1999-10-25 | Neurogen Corporation | Aminoalkyl substituted 9h-pyridino(2,3-b)indole and 9h-pyrimidino(4,5-b)indole derivatives |
US6140354A (en) | 1998-04-29 | 2000-10-31 | Ortho-Mcneil Pharmaceutical, Inc. | N-substituted aminotetralins as ligands for the neuropeptide Y Y5 receptor useful in the treatment of obesity and other disorders |
US6329395B1 (en) | 1998-06-08 | 2001-12-11 | Schering Corporation | Neuropeptide Y5 receptor antagonists |
HN1998000027A (es) | 1998-08-19 | 1999-06-02 | Bayer Ip Gmbh | Arilsulfonamidas y analagos |
DE19837627A1 (de) | 1998-08-19 | 2000-02-24 | Bayer Ag | Neue Aminosäureester von Arylsulfonamiden und Analoga |
US6358951B1 (en) | 1998-08-21 | 2002-03-19 | Pfizer Inc. | Growth hormone secretagogues |
US6337332B1 (en) | 1998-09-17 | 2002-01-08 | Pfizer Inc. | Neuropeptide Y receptor antagonists |
CA2350714A1 (en) | 1998-11-10 | 2000-05-18 | Merck & Co., Inc. | Spiro-indolines as y5 receptor antagonists |
DK1183245T3 (da) | 1999-04-22 | 2007-09-24 | Lundbeck & Co As H | Selektive NPY(Y5)-antagonister |
US6340683B1 (en) | 1999-04-22 | 2002-01-22 | Synaptic Pharmaceutical Corporation | Selective NPY (Y5) antagonists (triazines) |
CA2373035A1 (en) | 1999-05-05 | 2000-11-16 | Scott Dax | 3a,4,5,9b-tetrahydro-1h-benz[e]indol-2-yl amine-derived neuropeptide y receptors ligands useful in the treatment of obesity and other disorders |
US6291476B1 (en) | 1999-05-12 | 2001-09-18 | Ortho-Mcneil Pharmaceutical, Inc. | Pyrazole carboxamides useful for the treatment of obesity and other disorders |
ES2250126T3 (es) | 1999-06-30 | 2006-04-16 | H. Lundbeck A/S | Antagonistas selectivos del npy(y5). |
WO2001007409A1 (en) | 1999-07-23 | 2001-02-01 | Astrazeneca Uk Limited | Carbazole derivatives and their use as neuropeptide y5 receptor ligands |
HUP0202143A3 (en) | 1999-07-28 | 2003-12-29 | Ortho Mcneil Pharm Inc | Amine and amide derivatives as ligands for the neuropeptide y y5 receptor pharmaceutical compositions containing them and their use |
US6462053B1 (en) | 1999-08-20 | 2002-10-08 | Banyu Pharmaceutical Co., Ltd. | Spiro compounds |
TWI279402B (en) | 1999-08-20 | 2007-04-21 | Banyu Pharma Co Ltd | Spiro compounds having NPY antagonistic activities and agents containing the same |
WO2001021169A1 (fr) | 1999-09-20 | 2001-03-29 | Takeda Chemical Industries, Ltd. | Antagonistes de l'hormone de concentration de la melanine |
AU7315700A (en) | 1999-09-20 | 2001-04-24 | Takeda Chemical Industries Ltd. | Melanin concentrating hormone antagonist |
US6414002B1 (en) | 1999-09-22 | 2002-07-02 | Bristol-Myers Squibb Company | Substituted acid derivatives useful as antidiabetic and antiobesity agents and method |
CA2379585C (en) | 1999-09-30 | 2006-06-20 | James W. Darrow | Certain alkylene diamine-substituted pyrazolo[1,5,-a]-1,5-pyrimidines and pyrazolo[1,5-a]-1,3,5-triazines |
CZ20021086A3 (cs) | 1999-09-30 | 2002-10-16 | Neurogen Corporation | Alkylendiaminem substituované heterocykly |
PL354982A1 (en) | 1999-09-30 | 2004-03-22 | Neurogen Corporation | Amino substituted pyrazolo[1,5,-a]-1,5-pyrimidines and pyrazolo[1,5-a]-1,3,5-triazines |
CZ20022100A3 (cs) | 1999-12-16 | 2002-09-11 | Schering Corporation | Substituované imidazolové deriváty a farmaceutický prostředek |
WO2001056592A1 (en) | 2000-02-01 | 2001-08-09 | Novo Nordisk A/S | Use of compounds for the regulation of food intake |
CA2399791A1 (en) | 2000-02-11 | 2001-08-16 | Bristol-Myers Squibb Company | Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators in treating respiratory and non-respiratory diseases |
WO2001062738A1 (fr) | 2000-02-22 | 2001-08-30 | Banyu Pharmaceutical Co., Ltd. | Composes a base d'imidazoline |
US6531478B2 (en) | 2000-02-24 | 2003-03-11 | Cheryl P. Kordik | Amino pyrazole derivatives useful for the treatment of obesity and other disorders |
FR2805818B1 (fr) | 2000-03-03 | 2002-04-26 | Aventis Pharma Sa | Derives d'azetidine, leur preparation et les compositions pharmaceutiques les contenant |
FR2805817B1 (fr) | 2000-03-03 | 2002-04-26 | Aventis Pharma Sa | Compositions pharmaceutiques contenant des derives d'azetidine, les nouveaux derives d'azetidine et leur preparation |
FR2805810B1 (fr) | 2000-03-03 | 2002-04-26 | Aventis Pharma Sa | Compositions pharmaceutiques contenant des derives de 3- amino-azetidine, les nouveaux derives et leur preparation |
EP1132389A1 (en) | 2000-03-06 | 2001-09-12 | Vernalis Research Limited | New aza-indolyl derivatives for the treatment of obesity |
EP1142886A1 (en) | 2000-04-07 | 2001-10-10 | Aventis Pharma Deutschland GmbH | Percyquinnin, a process for its production and its use as a pharmaceutical |
PT1285651E (pt) | 2000-04-28 | 2010-10-21 | Takeda Pharmaceutical | Antagonistas da hormona concentradora da melanina |
GB0010757D0 (en) | 2000-05-05 | 2000-06-28 | Astrazeneca Ab | Chemical compounds |
GB0011013D0 (en) | 2000-05-09 | 2000-06-28 | Astrazeneca Ab | Chemical compounds |
US6432960B2 (en) | 2000-05-10 | 2002-08-13 | Bristol-Myers Squibb Company | Squarate derivatives of dihydropyridine NPY antagonists |
WO2001085173A1 (en) | 2000-05-10 | 2001-11-15 | Bristol-Myers Squibb Company | Alkylamine derivatives of dihydropyridine npy antagonists |
US6444675B2 (en) | 2000-05-10 | 2002-09-03 | Bristol-Myers Squibb Company | 4-alkyl and 4-cycloalkyl derivatives of dihydropyridine NPY antagonists |
US7229986B2 (en) | 2000-05-16 | 2007-06-12 | Takeda Pharmaceutical Company Ltd. | Melanin-concentrating hormone antagonist |
WO2001087335A2 (en) | 2000-05-17 | 2001-11-22 | Eli Lilly And Company | Method for selectively inhibiting ghrelin action |
US6391881B2 (en) | 2000-05-19 | 2002-05-21 | Bristol-Myers Squibb Company | Thiourea derivatives of dihydropyridine NPY antagonists |
SE0001899D0 (sv) | 2000-05-22 | 2000-05-22 | Pharmacia & Upjohn Ab | New compounds |
EP1299362A4 (en) | 2000-07-05 | 2004-11-03 | Synaptic Pharma Corp | SELECTIVE RECEPTOR ANTAGONISTS OF MELANINE CONCENTRATING HORMON-1 (MCH1) AND THEIR USE |
CA2414198A1 (en) | 2000-07-06 | 2002-01-17 | Neurogen Corporation | Melanin concentrating hormone receptor ligands |
MXPA03000738A (es) | 2000-07-24 | 2003-06-04 | Ardana Bioscience Ltd | Antagonistas de grelina. |
ATE305933T1 (de) | 2000-07-31 | 2005-10-15 | Hoffmann La Roche | Piperazin derivate |
CN1474810A (zh) | 2000-09-14 | 2004-02-11 | ���鹫˾ | 取代脲,神经肽yy5受体拮抗剂 |
EA006102B1 (ru) | 2000-10-13 | 2005-08-25 | Эли Лилли Энд Компани | Замещенные дипептиды в качестве средств, усиливающих секрецию гормона роста |
AU2167002A (en) | 2000-10-16 | 2002-06-11 | Hoffmann La Roche | Indoline derivatives and their use as 5-ht2 receptor ligands |
WO2002036596A2 (en) | 2000-11-03 | 2002-05-10 | Wyeth | CYCLOALKYL[b][1,4]DIAZEPINO[6,7,1-hi]INDOLES AND DERIVATIVES |
DK1337518T3 (da) | 2000-11-20 | 2009-10-19 | Biovitrum Ab Publ | Piperazinylpyrazinforbindelser som antagonister for serotonin-5-HT2-receptoren |
IL155702A0 (en) | 2000-11-20 | 2003-11-23 | Biovitrum Ab | Piperazinylpyrazine compounds as agonist or antagonist of serotonin 5-ht2 receptor |
ES2249384T3 (es) | 2000-12-12 | 2006-04-01 | Neurogen Corporation | Espiro(isobenzofuran-1,4'-piperadin)-3-onas y 3h-espirobenzofuran-1,4-piperidinas. |
GB0030710D0 (en) | 2000-12-15 | 2001-01-31 | Hoffmann La Roche | Piperazine derivatives |
AU2002234056B2 (en) | 2000-12-21 | 2005-04-07 | Schering Corporation | Heteroaryl urea neuropeptide Y Y5 receptor antagonists |
KR20040011447A (ko) | 2000-12-22 | 2004-02-05 | 쉐링 코포레이션 | 피페리딘 mch 길항제 및 비만 치료에 있어서의 이의 용도 |
US6610685B2 (en) | 2000-12-27 | 2003-08-26 | Hoffmann-La Roche Inc. | Fused indole derivatives |
HUP0400058A2 (hu) | 2001-02-02 | 2004-04-28 | Takeda Chemical Industries, Ltd. | Kondenzált heterogyűrűs vegyületek, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk |
US6900329B2 (en) | 2001-03-21 | 2005-05-31 | Schering Corporation | MCH antagonists and their use in the treatment of obesity |
CA2441235C (en) | 2001-03-21 | 2011-05-24 | Pharmacopeia, Inc. | Aryl and biaryl compounds having mch modulatory activity |
EP1373216B1 (en) | 2001-03-22 | 2004-12-15 | Solvay Pharmaceuticals B.V. | 4,5-dihydro-1h-pyrazole derivatives having cb1-antagonistic activity |
US6573287B2 (en) | 2001-04-12 | 2003-06-03 | Bristo-Myers Squibb Company | 2,1-oxazoline and 1,2-pyrazoline-based inhibitors of dipeptidyl peptidase IV and method |
DE60235617D1 (de) | 2001-04-12 | 2010-04-22 | Pharmacopeia Llc | Arly und diaryl piperidinderivate verwendbar als mch-hemmer |
FR2824825B1 (fr) | 2001-05-15 | 2005-05-06 | Servier Lab | Nouveaux derives d'alpha-amino-acides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
BR0209932A (pt) | 2001-05-22 | 2004-10-13 | Neurogen Corp | Composto ou sal farmaceuticamente aceitável do mesmo, composição farmacêutica, preparação farmacêutica embalada, métodos para modular ligação de mch a um receptor de mch e de mvc, para alterar a atividade de transdução de sinal de um receptor de mch em uma célula, para tratar uma doença ou distúrbio associado com a ativação de receptor de mch patogênico obesidade e para determinar a presença ou ausência de receptor de mch em uma amostra, e, uso de um composto |
WO2002094825A1 (fr) | 2001-05-22 | 2002-11-28 | Banyu Pharmaceutical Co., Ltd. | Nouveau derive de spiropiperidine |
US7098239B2 (en) | 2001-06-20 | 2006-08-29 | Merck & Co., Inc | Dipeptidyl peptidase inhibitors for the treatment of diabetes |
JP2005500308A (ja) | 2001-06-20 | 2005-01-06 | メルク エンド カムパニー インコーポレーテッド | 糖尿病を治療するためのジペプチジルペプチダーゼ阻害剤 |
GB0115517D0 (en) | 2001-06-25 | 2001-08-15 | Ferring Bv | Novel antidiabetic agents |
ZA200300833B (en) | 2001-06-27 | 2004-02-10 | Probiodrug Ag | Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents. |
DE60221983T2 (de) | 2001-06-27 | 2008-05-15 | Smithkline Beecham Corp. | Fluorpyrrolidine als dipeptidyl-peptidase inhibitoren |
DE60223920T2 (de) | 2001-06-27 | 2008-11-13 | Smithkline Beecham Corp. | Pyrrolidine als dipeptidyl-peptidase-inhibitoren |
DE60235212D1 (de) | 2001-06-27 | 2010-03-11 | Smithkline Beecham Corp | Fluoropyrrolidine als Dipeptidylpeptidasehemmer |
EP1404675B1 (en) | 2001-07-03 | 2008-03-12 | Novo Nordisk A/S | Dpp-iv-inhibiting purine derivatives for the treatment of diabetes |
CN1671386A (zh) | 2001-07-05 | 2005-09-21 | H·隆德贝克有限公司 | 作为mch选择性拮抗剂的取代苯胺基哌啶 |
UA74912C2 (en) | 2001-07-06 | 2006-02-15 | Merck & Co Inc | Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes |
AU2002319627A1 (en) | 2001-07-20 | 2003-03-03 | Merck And Co., Inc. | Substituted imidazoles as cannabinoid receptor modulators |
BRPI0104510B8 (pt) | 2001-07-27 | 2021-05-25 | Embrapa Pesquisa Agropecuaria | peptídeos antibióticos da família das phylloseptinas isolados da secreção da pele de phylloseptina hypocondrialis e composição antimicrobiana relacionada |
DE60231880D1 (de) | 2001-08-07 | 2009-05-20 | Banyu Pharma Co Ltd | Spiro isobenzofurane als neuropeptid y rezeptor antagonisten |
JP2005320249A (ja) | 2002-05-01 | 2005-11-17 | Banyu Pharmaceut Co Ltd | 2−アミノピラジン誘導体の製造方法 |
AR040241A1 (es) | 2002-06-10 | 2005-03-23 | Merck & Co Inc | Inhibidores de la 11-beta-hidroxiesteroide deshidrogrenasa 1 para el tratamiento de la diabetes obesidad y dislipidemia |
US7105526B2 (en) | 2002-06-28 | 2006-09-12 | Banyu Pharmaceuticals Co., Ltd. | Benzimidazole derivatives |
US6869966B2 (en) | 2002-09-30 | 2005-03-22 | Banyu Pharmaceutical Co., Ltd. | N-substituted-2-oxodihydropyridine derivatives |
MY134457A (en) | 2002-11-22 | 2007-12-31 | Merck & Co Inc | Substituted amides |
JO2397B1 (en) | 2002-12-20 | 2007-06-17 | ميرك شارب اند دوم كوربوريشن | Terazol derivatives as beta-hydroxy steroid dihydrogenase-1 inhibitors |
EP1636181A1 (en) | 2003-06-11 | 2006-03-22 | Merck & Co., Inc. | Substituted 3-alkyl and 3-alkenyl azetidine derivatives |
JP5976011B2 (ja) | 2011-04-05 | 2016-08-23 | 武田薬品工業株式会社 | スルホンアミド誘導体およびその用途 |
PL3411358T3 (pl) | 2016-02-04 | 2022-02-28 | Takeda Pharmaceutical Company Limited | Podstawiony związek piperydynowy i jego zastosowanie |
EP3594203B1 (en) | 2017-03-08 | 2021-08-04 | Takeda Pharmaceutical Company Limited | Substituted pyrrolidine compound and use thereof |
US11034700B2 (en) | 2017-03-08 | 2021-06-15 | Takeda Pharmaceutical Company Limited | Substituted pyrrolidine compound and use thereof |
BR112020000823A2 (pt) | 2017-08-03 | 2020-07-21 | Takeda Pharmaceutical Company Limited | composto, medicamento, métodos para ativar um receptor de orexina tipo 2 e para profilaxia ou tratamento de narcolepsia, e, uso de um composto ou sal. |
US11319286B2 (en) * | 2017-08-03 | 2022-05-03 | Takeda Pharmaceutical Company Limited | Heterocyclic compound and application thereof |
EP3816153B1 (en) | 2018-06-29 | 2023-10-18 | Takeda Pharmaceutical Company Limited | Heterocyclic compound and use thereof |
US20210269420A1 (en) | 2018-06-29 | 2021-09-02 | Takeda Pharmaceutical Company Limited | Heterocyclic compound and application thereof |
US20230042358A1 (en) | 2018-12-12 | 2023-02-09 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
EP3896060B1 (en) | 2018-12-12 | 2023-08-16 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
US20230040770A1 (en) | 2019-01-31 | 2023-02-09 | Takeda Pharmaceutical Company Limited | Heterocyclic compound and use thereof |
EP3924058A1 (en) * | 2019-02-13 | 2021-12-22 | Merck Sharp & Dohme Corp. | 5-alkyl pyrrolidine orexin receptor agonists |
-
2021
- 2021-08-16 TW TW110130112A patent/TW202227417A/zh unknown
- 2021-08-16 EP EP21766336.8A patent/EP4200295A1/en active Pending
- 2021-08-16 BR BR112023002957A patent/BR112023002957A2/pt unknown
- 2021-08-16 US US18/040,896 patent/US20230365533A1/en active Pending
- 2021-08-16 KR KR1020237008981A patent/KR20230053639A/ko unknown
- 2021-08-16 CA CA3189908A patent/CA3189908A1/en active Pending
- 2021-08-16 MX MX2023001840A patent/MX2023001840A/es unknown
- 2021-08-16 WO PCT/US2021/046098 patent/WO2022040070A1/en active Application Filing
- 2021-08-16 CN CN202180067840.8A patent/CN116249697A/zh active Pending
- 2021-08-16 US US17/402,932 patent/US11680060B2/en active Active
- 2021-08-16 PE PE2023000316A patent/PE20231384A1/es unknown
- 2021-08-16 CR CR20230089A patent/CR20230089A/es unknown
- 2021-08-16 IL IL300610A patent/IL300610A/en unknown
- 2021-08-16 JP JP2023511949A patent/JP7443625B2/ja active Active
- 2021-08-16 AU AU2021329805A patent/AU2021329805B2/en active Active
-
2023
- 2023-02-15 CL CL2023000468A patent/CL2023000468A1/es unknown
- 2023-02-16 EC ECSENADI202312026A patent/ECSP23012026A/es unknown
- 2023-02-17 CO CONC2023/0001795A patent/CO2023001795A2/es unknown
- 2023-02-17 DO DO2023000036A patent/DOP2023000036A/es unknown
Also Published As
Publication number | Publication date |
---|---|
CN116249697A (zh) | 2023-06-09 |
JP7443625B2 (ja) | 2024-03-05 |
US11680060B2 (en) | 2023-06-20 |
TW202227417A (zh) | 2022-07-16 |
KR20230053639A (ko) | 2023-04-21 |
EP4200295A1 (en) | 2023-06-28 |
CO2023001795A2 (es) | 2023-03-17 |
AU2021329805A1 (en) | 2023-03-09 |
CR20230089A (es) | 2023-04-11 |
ECSP23012026A (es) | 2023-03-31 |
WO2022040070A1 (en) | 2022-02-24 |
IL300610A (en) | 2023-04-01 |
US20230365533A1 (en) | 2023-11-16 |
US20220056017A1 (en) | 2022-02-24 |
CA3189908A1 (en) | 2022-02-24 |
JP2023533604A (ja) | 2023-08-03 |
BR112023002957A2 (pt) | 2023-04-04 |
CL2023000468A1 (es) | 2023-08-04 |
MX2023001840A (es) | 2023-03-13 |
DOP2023000036A (es) | 2023-04-16 |
AU2021329805B2 (en) | 2024-02-29 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
PE20231384A1 (es) | Agonistas de bicicloheptano pirrolidina de los receptores de orexina | |
MX344308B (es) | Derivados de quinolina carboxamida y quinolina carbonitrilo como moduladores alostericos negativos de mglur2, composiciones y su uso. | |
PE20211380A1 (es) | Nuevos compuestos heterociclicos como inhibidores de monoacilglicerol lipasa | |
EA202090987A8 (ru) | Новые пролекарства на основе катехоламина для применения в лечении болезни паркинсона | |
RU2008100019A (ru) | Способ лечения чрезмерной дневной сонливости (варианты) | |
CO6551729A2 (es) | Moduladores alostericos positivos de receptores de m1 de quinolina amida | |
RU2009136592A (ru) | Терапевтические агенты | |
DOP2011000135A (es) | Moduladores de aril metil benzoquinazolinona alostericos positivos del receptor m1 | |
TN2020000161A1 (en) | CHROMANE, ISOCHROMANE AND DIHYDROISOBENZOFURAN DERIVATIVES AS mGIuR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE | |
PE20061295A1 (es) | Derivados de acetileno | |
RU2009103307A (ru) | ПРОИЗВОДНЫЕ ИМИДАЗО[1, 2-a]ПИРИДИН-2-КАРБОКСАМИДОВ, ИХ ПОЛУЧЕНИЕ И ПРИМЕНЕНИЕ В ТЕРАПИИ | |
PH12021550659A1 (en) | Monoacylglycerol lipase modulators | |
PE20110833A1 (es) | Nuevas octahidrociclopenta[c]pirrol-4-aminas sustituidas como bloqueantes de los canales de calcio | |
PE20220710A1 (es) | Nuevos inhibidores heterociclicos de monoacilglicerol lipasa (magl) | |
JOP20220180A1 (ar) | مُعدلات ليباز أُحادِيُّ الجلِيسِريد | |
PE20220514A1 (es) | Inhibidores de monoacilglicerol lipasa (magl) heterociclicos | |
NZ630281A (en) | Acylaminocycloalkyl compounds suitable for treating disorders that respond to modulation of dopamine d3 receptor | |
PE20230846A1 (es) | Compuestos heterociclicos como agonistas del receptor de activacion expresado en las celulas mieloides 2 | |
MX2019007100A (es) | Derivados de tiazina y oxazina biciclicos como inhibidores de beta-secretasa y metodos de uso. | |
DE602004005502D1 (de) | Comt-inhibitoren | |
DE60307106D1 (de) | 9,11-cycloendoperoxyd prodrugs von prostaglandinanalogen für die behandlung von okularer hypertension und glaukoma | |
BR0309778A (pt) | Compostos 3,4-di-hidroquinolin-2(1h)-ona como antagonistas do receptor nr2b | |
AR050919A1 (es) | Amidas del acido 5 y 6-aminoalquil indol-2-carboxilico 3-sustituidas y analogos relacionados como inhibidores de la caseina cinasa ie | |
NZ714111A (en) | Alpha-substituted glycinamide derivative | |
PE20080190A1 (es) | Derivados de cromano y cromeno y sus usos |