AR072899A1 - Derivados de terpiridina-carboxamida antagonistas de receptores de orexina, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del insomnio y la obesidad. - Google Patents
Derivados de terpiridina-carboxamida antagonistas de receptores de orexina, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del insomnio y la obesidad.Info
- Publication number
- AR072899A1 AR072899A1 ARP090102972A ARP090102972A AR072899A1 AR 072899 A1 AR072899 A1 AR 072899A1 AR P090102972 A ARP090102972 A AR P090102972A AR P090102972 A ARP090102972 A AR P090102972A AR 072899 A1 AR072899 A1 AR 072899A1
- Authority
- AR
- Argentina
- Prior art keywords
- unsubstituted
- substituted
- substituents selected
- alkyl
- cycloalkyl
- Prior art date
Links
- 208000008589 Obesity Diseases 0.000 title 1
- 108050000742 Orexin Receptor Proteins 0.000 title 1
- 102000008834 Orexin receptor Human genes 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 235000020824 obesity Nutrition 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000001424 substituent group Chemical group 0.000 abstract 26
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 8
- 125000000217 alkyl group Chemical group 0.000 abstract 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 7
- 125000000623 heterocyclic group Chemical group 0.000 abstract 6
- 125000003342 alkenyl group Chemical group 0.000 abstract 5
- 125000000304 alkynyl group Chemical group 0.000 abstract 5
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 5
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 5
- 229910052736 halogen Inorganic materials 0.000 abstract 5
- 150000002367 halogens Chemical class 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 5
- 125000001624 naphthyl group Chemical group 0.000 abstract 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 3
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 150000002431 hydrogen Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 238000006467 substitution reaction Methods 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/06—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom containing only hydrogen and carbon atoms in addition to the ring nitrogen atom
- C07D213/22—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom containing only hydrogen and carbon atoms in addition to the ring nitrogen atom containing two or more pyridine rings directly linked together, e.g. bipyridyl
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
- C07D213/82—Amides; Imides in position 3
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychology (AREA)
- Anesthesiology (AREA)
- Child & Adolescent Psychology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
Abstract
Reivindicacion 1: Un compuesto de la formula (1) en la que A se selecciona entre el grupo que consiste en fenilo, naftilo y heteroarilo; R1a, R1b y R1c se seleccionan independientemente entre el grupo que consiste en: (1) hidrogeno, (2) halogeno, (3) hidroxilo, (4) -(C=O)m-On-alquilo C1-6, donde m es 0 o 1, n es 0 o 1 (donde si m es 0 o n es 0, está presente un enlace) y donde el alquilo está sin sustituir o sustituido por uno o más sustituyentes seleccionados entre R13, (5) - (C=O)m-On-cicloalquilo C3-6, donde el cicloalquilo está sin sustituir o sustituido por uno o más sustituyentes seleccionados entre R13, (6) -(C=O)m-alquenilo C2-4, donde el alquenilo está sin sustituir o sustituido por uno o más sustituyentes seleccionados entre R13, (7) -(C=O)m-alquinilo C2-4, donde el alquinilo esta sin sustituir o sustituido por uno o más sustituyentes seleccionados entre R13, (8) -(C=O)m-On-fenilo o -(C=O)m-On-naftilo, donde el fenilo o el naftilo está sin sustituir o sustituido por uno o más sustituyentes seleccionados entre R13, (9) -(C=O)m-On-heterociclo, donde el heterociclo está sin sustituir o sustituido por uno o más sustituyentes seleccionados entre R13, (10) -(C=O)m-NR10R11, donde R10 y R11 se seleccionan independientemente entre el grupo que consiste en: (a) hidrogeno, (b) alquilo C1-6, que está sin sustituir o sustituido por R13, (c) alquenilo C3-6, que esta sin sustituir o sustituido por R13, (d) alquinilo C3-6, que está sin sustituir o sustituido por R13, (e) cicloalquilo C3-6 que está sin sustituir o sustituido por R13, (f) fenilo, que está sin sustituir o sustituido por R13, y (g) heterociclo, que está sin sustituir o sustituido por R13, (11) -S(O)2-NR10R11, (12) -S(O)q-R12, donde q es 0, 1 o 2 y donde R12 se selecciona entre las definiciones de R10 y R11, (13) -CO2H, (14) -CN, y (15) -NO2; R2a, R2b y R2c pueden estar ausentes si la valencia de A no permite tal sustitucion y se seleccionan independientemente entre el grupo que consiste en: (1) hidrogeno, (2) halogeno, (3) hidroxilo, (4) -(C=O)m-On-alquilo C1-6, donde el alquilo está sin sustituir o sustituido por uno o más sustituyentes seleccionados entre R13, (5) -(C=O)m-On-cicloalquilo C3-6, donde el cicloalquilo está sin sustituir o sustituido por uno o más sustituyentes seleccionados entre R13, (6) -(C=O)m-alquenilo C2-4, donde el alquenilo está sin sustituir o sustituido por uno o más sustituyentes seleccionados entre R13, (7) -(C=O)m-alquinilo C2-4, donde el alquinilo esta sin sustituir o sustituido por uno o más sustituyentes seleccionados entre R13, (8) -(C=O)m-On-fenilo o -(C=O)m-On-naftilo, donde el fenilo o el naftilo está sin sustituir o sustituido por uno o más sustituyentes seleccionados entre R13, (9) -(C=O)m-On-heterociclo, donde el heterociclo está sin sustituir o sustituido por uno o más sustituyentes seleccionados entre R13, (10) -(C=O)m-NR10R11, (11) -S(O)2-NR10R11, (12) -S(O)q-R12, (13) -CO2H, (14) -CN, y (15) -NO2; R3a, R3b y R3c se seleccionan independientemente entre el grupo que consiste en: (1) hidrogeno, (2) halogeno, (3) hidroxilo, (4) -(C=O)m-On-alquilo C1-6, donde el alquilo está sin sustituir o sustituido por uno o más sustituyentes seleccionados entre R13, (5) -(C=O)m-On-cicloalquilo C3-6, donde el cicloalquilo está sin sustituir o sustituido por uno o más sustituyentes seleccionados entre R13, (6) -(C=O)m-alquenilo C2-4, donde el alquenilo está sin sustituir o sustituido por uno o más sustituyentes seleccionados entre R13, (7) -(C=O)m-alquinilo C2-4, donde el alquinilo esta sin sustituir o sustituido por uno o más sustituyentes seleccionados entre R13, (8) -(C=O)m-On-fenilo o -(C=O)m-On-naftilo, donde el fenilo o el naftilo está sin sustituir o sustituido por uno o más sustituyentes seleccionados entre R13, (9) -(C=O)m-On-heterociclo, donde el heterociclo está sin sustituir o sustituido por uno o más sustituyentes seleccionados entre R13, (10) -(C=O)m-NR10R11, (11) -S(O)2-NR10R11, (12) -S(O)q-R12, (13) -CO2H, (14) -CN, y (15) -NO2; R4 y R5 se seleccionan independientemente entre H y alquilo C1-6, que está sin sustituir o sustituido por uno o más sustituyentes seleccionados entre R13, o R4 y R5 pueden estar unidos juntos para formar un cicloalquilo C3-6 con el átomo de C al que están unidos, donde el cicloalquilo está sin sustituir o sustituido por uno o más sustituyentes seleccionados entre R13; R6 es hidrogeno, alquilo C1-6, o cicloalquilo C3-6, que está sin sustituir o sustituido por uno o más sustituyentes seleccionados de R13; R13 se selecciona entre el grupo que consiste en: (1) halogeno, (2) hidroxilo, (3) -(C=O)m-On-alquilo C1-6, donde el alquilo está sin sustituir o sustituido por uno o más sustituyentes seleccionados entre R14, (4) -On-perfluoroalquilo C1-3, (5) -(C=O)m-On-cicloalquilo C3-6, donde el cicloalquilo está sin sustituir o sustituido por uno o más sustituyentes seleccionados entre R14, (6) -(C=O)m-alquenilo C2-4, donde el alquenilo está sin sustituir o sustituido por uno o más sustituyentes seleccionados entre R14, (7) -(C=O)m-alquinilo C2-4, donde el alquinilo está sin sustituir o sustituido por uno o más sustituyentes seleccionados entre R14, (8) -(C=O)m-On-fenilo o -(C=O)m-On-naftilo, donde el fenilo o el naftilo está sin sustituir o sustituido por uno o más sustituyentes seleccionados entre R14, (9) -(C=O)m-On-heterociclo, donde el heterociclo está sin sustituir o sustituido por uno o más sustituyentes seleccionados entre R14, (10) -(C=O)m-NR10R11, (11) -S(O)2-NR10R11, (12) -S(O)q-R12, (13) -CO2H, (14) -CN, y (15) -NO2; R14 se selecciona entre el grupo que consiste en: (1) hidroxilo, (2) halogeno, (3) alquilo C1-6, (4) -cicloalquilo C3-6, (5) -O-alquilo C1-6, (6) -O(C=O)-alquilo C1-6, (7) -NH-alquilo C1-6 (8) fenilo, (9) heterociclo, (10) -CO2H, y (11) -CN; o una sal farmacéuticamente aceptable de los mismos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US18820308P | 2008-08-07 | 2008-08-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR072899A1 true AR072899A1 (es) | 2010-09-29 |
Family
ID=41162729
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090102972A AR072899A1 (es) | 2008-08-07 | 2009-08-03 | Derivados de terpiridina-carboxamida antagonistas de receptores de orexina, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del insomnio y la obesidad. |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US8349872B2 (es) |
| EP (1) | EP2323985B1 (es) |
| JP (1) | JP2011530522A (es) |
| KR (1) | KR20110041553A (es) |
| CN (1) | CN102171188A (es) |
| AR (1) | AR072899A1 (es) |
| AU (1) | AU2009279694A1 (es) |
| BR (1) | BRPI0917004A2 (es) |
| CA (1) | CA2732682A1 (es) |
| CO (1) | CO6351717A2 (es) |
| IL (1) | IL210962A0 (es) |
| MX (1) | MX2011001412A (es) |
| RU (1) | RU2011108281A (es) |
| TW (1) | TW201008927A (es) |
| WO (1) | WO2010017260A1 (es) |
| ZA (1) | ZA201100866B (es) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2695621A1 (en) * | 2007-08-09 | 2009-02-12 | Merck Sharp & Dohme Corp. | Pyridine carboxamide orexin receptor antagonists |
| US7691878B2 (en) * | 2007-08-27 | 2010-04-06 | Theravance, Inc. | Heteroarylalkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists |
| AR072899A1 (es) | 2008-08-07 | 2010-09-29 | Merck Sharp & Dohme | Derivados de terpiridina-carboxamida antagonistas de receptores de orexina, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del insomnio y la obesidad. |
| AU2009308982A1 (en) | 2008-10-30 | 2010-05-06 | Merck Sharp & Dohme Corp. | Pyridazine carboxamide orexin receptor antagonists |
| JP2012507539A (ja) * | 2008-10-30 | 2012-03-29 | メルク・シャープ・エンド・ドーム・コーポレイション | ２，５−二置換フェニルカルボキサミド・オレキシン受容体アンタゴニスト |
| PE20110852A1 (es) * | 2008-10-30 | 2011-11-25 | Merck Sharp & Dohme | Antagonistas del receptor de orexina de isonicotinamida |
| WO2011050200A1 (en) | 2009-10-23 | 2011-04-28 | Janssen Pharmaceutica Nv | Fused heterocyclic compounds as orexin receptor modulators |
| PT2491038T (pt) | 2009-10-23 | 2016-07-14 | Janssen Pharmaceutica Nv | Octahidropirrolo[3,4-c]pirrolos disubstituídos como modeladores de recetores de orexina |
| WO2011050202A1 (en) | 2009-10-23 | 2011-04-28 | Janssen Pharmaceutica Nv | Fused heterocyclic compounds as orexin receptor modulators |
| WO2012145581A1 (en) | 2011-04-20 | 2012-10-26 | Janssen Pharmaceutica Nv | Disubstituted octahy-dropyrrolo [3,4-c] pyrroles as orexin receptor modulators |
| CN102329264B (zh) * | 2011-06-28 | 2015-03-04 | 中国科学院福建物质结构研究所 | 一种有机白光发射材料L-Cl的制备和用途 |
| IN2014CN00827A (es) * | 2011-08-16 | 2015-04-03 | Merck Sharp & Dohme | |
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| US9440982B2 (en) | 2012-02-07 | 2016-09-13 | Eolas Therapeutics, Inc. | Substituted prolines/piperidines as orexin receptor antagonists |
| US8883857B2 (en) | 2012-12-07 | 2014-11-11 | Baylor College Of Medicine | Small molecule xanthine oxidase inhibitors and methods of use |
| WO2016025669A1 (en) | 2014-08-13 | 2016-02-18 | Eolas Therapeutics, Inc. | Difluoropyrrolidines as orexin receptor modulators |
| WO2016065586A1 (en) | 2014-10-30 | 2016-05-06 | Merck Sharp & Dohme Corp. | Pyrazole, triazole and tetrazole orexin receptor antagonists |
| WO2016065584A1 (en) | 2014-10-30 | 2016-05-06 | Merck Sharp & Dohme Corp. | Piperidine oxadiazole and thiadiazole orexin receptor antagonists |
| WO2016065587A1 (en) | 2014-10-30 | 2016-05-06 | Merck Sharp & Dohme Corp. | Pyrazole orexin receptor antagonists |
| WO2016065585A1 (en) | 2014-10-30 | 2016-05-06 | Merck Sharp & Dohme Corp. | Piperidine isoxazole and isothiazole orexin receptor antagonists |
| WO2016065583A1 (en) | 2014-10-30 | 2016-05-06 | Merck Sharp & Dohme Corp. | Oxazole orexin receptor antagonists |
| US10000499B2 (en) | 2014-11-26 | 2018-06-19 | Merck Sharp & Dohme Corp. | Methyl diazepane orexin receptor antagonists |
| WO2016085783A1 (en) | 2014-11-26 | 2016-06-02 | Merck Sharp & Dohme Corp. | Bridged diazepane orexin receptor antagonists |
| WO2016086358A1 (en) | 2014-12-02 | 2016-06-09 | Merck Sharp & Dohme Corp. | Hydroxymethyl piperidine orexin receptor antagonists |
| WO2016086357A1 (en) | 2014-12-02 | 2016-06-09 | Merck Sharp & Dohme Corp. | Methyl oxazole orexin receptor antagonists |
| US10011595B2 (en) | 2014-12-19 | 2018-07-03 | Merck Sharp & Dohme Corp. | Ethyldiamine orexin receptor antagonists |
| WO2016095204A1 (en) | 2014-12-19 | 2016-06-23 | Merck Sharp & Dohme Corp. | Pyrrolidine orexin receptor antagonists |
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| KR102559922B1 (ko) | 2016-03-10 | 2023-07-25 | 얀센 파마슈티카 엔.브이. | 오렉신-2 수용체 길항제를 사용한 우울증의 치료 방법 |
| GB201702174D0 (en) | 2017-02-09 | 2017-03-29 | Benevolentai Bio Ltd | Orexin receptor antagonists |
| GB201707499D0 (en) | 2017-05-10 | 2017-06-21 | Benevolentai Bio Ltd | Orexin receptor antagonists |
| GB201707504D0 (en) | 2017-05-10 | 2017-06-21 | Benevolentai Bio Ltd | Orexin receptor antagonists |
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| US5585388A (en) | 1995-04-07 | 1996-12-17 | Sibia Neurosciences, Inc. | Substituted pyridines useful as modulators of acetylcholine receptors |
| US6194581B1 (en) | 1995-04-07 | 2001-02-27 | Merck & Co., Inc. | Substituted pyridines useful as modulators of acetylcholine receptors |
| WO2008109437A2 (en) | 2007-03-02 | 2008-09-12 | Northwestern University | Compositions and treatments for seizure-related disorders |
| US6362009B1 (en) | 1997-11-21 | 2002-03-26 | Merck & Co., Inc. | Solid phase synthesis of heterocycles |
| US6174901B1 (en) | 1998-12-18 | 2001-01-16 | Amgen Inc. | Substituted pyridine and pyridazine compounds and methods of use |
| GB0126292D0 (en) * | 2001-11-01 | 2002-01-02 | Smithkline Beecham Plc | Compounds |
| GB0130341D0 (en) | 2001-12-19 | 2002-02-06 | Smithkline Beecham Plc | Compounds |
| US20040116479A1 (en) | 2002-10-04 | 2004-06-17 | Fortuna Haviv | Method of inhibiting angiogenesis |
| EP1669348A4 (en) | 2003-09-30 | 2009-03-11 | Eisai R&D Man Co Ltd | NEW ANTIPILIC AGENT CONTAINING A HETEROCYCLIC COMPOUND |
| HUP0400405A3 (en) | 2004-02-10 | 2009-03-30 | Sanofi Synthelabo | Pyrimidine derivatives, process for producing them, their use, pharmaceutical compositions containing them and their intermediates |
| US20070149547A1 (en) | 2004-02-12 | 2007-06-28 | Celine Bonnefous | Bipyridyl amides as modulators of metabotropic glutamate receptor-5 |
| CA2603345C (en) | 2005-04-01 | 2017-05-02 | Insa Rouen | New heterocyclic compounds, their preparation and their use as medicaments, in particular as anti-alzheimer agents |
| WO2006110626A1 (en) | 2005-04-12 | 2006-10-19 | Merck & Co., Inc. | Amidopropoxyphenyl orexin receptor antagonists |
| WO2007061763A2 (en) | 2005-11-22 | 2007-05-31 | Merck & Co., Inc. | Indole orexin receptor antagonists |
| WO2008108991A1 (en) | 2007-03-02 | 2008-09-12 | Merck & Co., Inc. | Bipyridine carboxamide orexin receptor antagonists |
| CA2695621A1 (en) | 2007-08-09 | 2009-02-12 | Merck Sharp & Dohme Corp. | Pyridine carboxamide orexin receptor antagonists |
| AR072899A1 (es) | 2008-08-07 | 2010-09-29 | Merck Sharp & Dohme | Derivados de terpiridina-carboxamida antagonistas de receptores de orexina, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del insomnio y la obesidad. |
| JP2012507539A (ja) | 2008-10-30 | 2012-03-29 | メルク・シャープ・エンド・ドーム・コーポレイション | ２，５−二置換フェニルカルボキサミド・オレキシン受容体アンタゴニスト |
| PE20110852A1 (es) | 2008-10-30 | 2011-11-25 | Merck Sharp & Dohme | Antagonistas del receptor de orexina de isonicotinamida |
| AU2009308982A1 (en) | 2008-10-30 | 2010-05-06 | Merck Sharp & Dohme Corp. | Pyridazine carboxamide orexin receptor antagonists |
| US20120065205A1 (en) | 2009-06-01 | 2012-03-15 | Mercer Swati P | Pyrazine carboxamide orexin receptor antagonists |
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2009
- 2009-08-03 AR ARP090102972A patent/AR072899A1/es unknown
- 2009-08-04 TW TW098126245A patent/TW201008927A/zh unknown
- 2009-08-05 US US12/536,079 patent/US8349872B2/en active Active
- 2009-08-05 RU RU2011108281/04A patent/RU2011108281A/ru not_active Application Discontinuation
- 2009-08-05 AU AU2009279694A patent/AU2009279694A1/en not_active Abandoned
- 2009-08-05 CN CN2009801395000A patent/CN102171188A/zh active Pending
- 2009-08-05 WO PCT/US2009/052786 patent/WO2010017260A1/en not_active Ceased
- 2009-08-05 MX MX2011001412A patent/MX2011001412A/es not_active Application Discontinuation
- 2009-08-05 CA CA2732682A patent/CA2732682A1/en not_active Abandoned
- 2009-08-05 KR KR1020117004956A patent/KR20110041553A/ko not_active Withdrawn
- 2009-08-05 EP EP09791168.9A patent/EP2323985B1/en active Active
- 2009-08-05 BR BRPI0917004A patent/BRPI0917004A2/pt not_active Application Discontinuation
- 2009-08-05 JP JP2011522202A patent/JP2011530522A/ja not_active Withdrawn
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2011
- 2011-01-30 IL IL210962A patent/IL210962A0/en unknown
- 2011-02-02 ZA ZA2011/00866A patent/ZA201100866B/en unknown
- 2011-02-23 CO CO11022223A patent/CO6351717A2/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| JP2011530522A (ja) | 2011-12-22 |
| CA2732682A1 (en) | 2010-02-11 |
| AU2009279694A1 (en) | 2010-02-11 |
| KR20110041553A (ko) | 2011-04-21 |
| US8349872B2 (en) | 2013-01-08 |
| CN102171188A (zh) | 2011-08-31 |
| US20100035931A1 (en) | 2010-02-11 |
| WO2010017260A1 (en) | 2010-02-11 |
| EP2323985A1 (en) | 2011-05-25 |
| CO6351717A2 (es) | 2011-12-20 |
| TW201008927A (en) | 2010-03-01 |
| ZA201100866B (en) | 2011-10-26 |
| EP2323985B1 (en) | 2017-01-11 |
| BRPI0917004A2 (pt) | 2016-02-16 |
| RU2011108281A (ru) | 2012-09-20 |
| MX2011001412A (es) | 2011-04-04 |
| IL210962A0 (en) | 2011-04-28 |
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