AR056155A1 - Antagonistas del receptor 1 de la hormona de concentracion de melanina no basica - Google Patents
Antagonistas del receptor 1 de la hormona de concentracion de melanina no basicaInfo
- Publication number
- AR056155A1 AR056155A1 ARP060104665A ARP060104665A AR056155A1 AR 056155 A1 AR056155 A1 AR 056155A1 AR P060104665 A ARP060104665 A AR P060104665A AR P060104665 A ARP060104665 A AR P060104665A AR 056155 A1 AR056155 A1 AR 056155A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- hydrogen
- lower alkyl
- heterocycle
- cycloalkyl
- Prior art date
Links
- 239000005557 antagonist Substances 0.000 title 1
- 229940088597 hormone Drugs 0.000 title 1
- 239000005556 hormone Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 6
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 239000001257 hydrogen Substances 0.000 abstract 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 6
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 125000004429 atom Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical group 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- IQUPABOKLQSFBK-UHFFFAOYSA-N 2-nitrophenol Chemical compound OC1=CC=CC=C1[N+]([O-])=O IQUPABOKLQSFBK-UHFFFAOYSA-N 0.000 abstract 2
- 101100134925 Gallus gallus COR6 gene Proteins 0.000 abstract 2
- 101100477978 Hypocrea jecorina (strain QM6a) sor6 gene Proteins 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 208000019901 Anxiety disease Diseases 0.000 abstract 1
- 101150106280 Mchr1 gene Proteins 0.000 abstract 1
- 108700036626 Melanin-concentrating hormone receptor 1 Proteins 0.000 abstract 1
- 102100027375 Melanin-concentrating hormone receptor 1 Human genes 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 230000036506 anxiety Effects 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 229940124597 therapeutic agent Drugs 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
- A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
-
- 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
- A61P25/22—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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Pain & Pain Management (AREA)
- Emergency Medicine (AREA)
- Psychiatry (AREA)
- Child & Adolescent Psychology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Saccharide Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
Composiciones farmacéuticas que comprenden al menos un compuesto de acuerdo a la formula (1) y opcionalmente al menos un agente terapéutico adicional. Finalmente, métodos para el tratamiento de un paciente que sufre de una enfermedad o trastorno modulado por MCHR-1 tales como, por ejemplo, obesidad, diabetes, depresion o ansiedad, mediante administracion de una dosis terapéuticamente efectiva de un compuesto de acuerdo a la formula (1). Reivindicacion 1: Un compuesto o una sal farmacéuticamente aceptable o un estereoisomero o un profármaco o un solvato del mismo, caracterizado porque tiene la formula (1), en donde: R1 es independientemente seleccionado del grupo que consiste de hidrogeno, halogeno, alquilo inferior, cicloalquilo inferior, arilo, CF3, OR6 y SR6; R2 se selecciona del grupo que consiste de hidrogeno y alquilo inferior; R4 se selecciona del grupo que consiste de hidroxilo o G-D2-Zn, en donde R4 y R5 pueden ser tomados conjuntamente para formar un anillo de 4 a 7 átomos; R5 se selecciona del grupo que consiste de hidrogeno, hidroxilo, halogeno, alquilo inferior, cicloalquilo inferior, CF3, SR6, alcoxi inferior, cicloalcoxi inferior, CN, CONR7R7, SOR6, SO2R6, NR7COR7, NR7CO2R7, CO2R6, heteroarilo, NR7SO2R6 y COR6; m es un numero entero de 0 a 1; n es un numero entero de 1 a 3; G se selecciona del grupo que consiste de un enlace directo, O, S y CR7R7; D2 se selecciona del grupo que consiste de un enlace directo, alquilo inferior, cicloalquilo inferior y un heterociclo no básico de 4 a 6 miembros; Z se selecciona del grupo que consiste de hidrogeno, halogeno, hidroxilo, alcoxi inferior, cicloalquilo inferior, cicloalcoxi inferior, OCOR6, OC(O)C(O)R6, OCONR7R7, CN, CONR7R7, OR6, OSO2R6, SR6, SOR6, SO2R6, NR7COR7, NR7CONR7R7, NR7CO2R7, CO2R7, heterociclo, heteroarilo, OPO(OR6)2, NR6SO2R6 y COR6; R6 es independientemente seleccionado del grupo que consiste de hidrogeno, alquilo inferior, cicloalquilo inferior, heterociclo y heteroarilo; y R7 es independientemente seleccionado del grupo que consiste de hidrogeno, alquilo inferior, cicloalquilo inferior y heterociclo, en donde dos R7 y el átomo al cual se enlazan pueden formar un anillo de 4 a 7 átomos.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US73045305P | 2005-10-26 | 2005-10-26 | |
| US11/586,255 US8618115B2 (en) | 2005-10-26 | 2006-10-25 | Substituted thieno[3,2-d]pyrimidinones as MCHR1 antagonists and methods for using them |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR056155A1 true AR056155A1 (es) | 2007-09-19 |
Family
ID=37888159
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060104665A AR056155A1 (es) | 2005-10-26 | 2006-10-25 | Antagonistas del receptor 1 de la hormona de concentracion de melanina no basica |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US8618115B2 (es) |
| EP (2) | EP1948665B1 (es) |
| JP (1) | JP2009513658A (es) |
| KR (1) | KR20080067681A (es) |
| AR (1) | AR056155A1 (es) |
| AU (1) | AU2006306140A1 (es) |
| BR (1) | BRPI0617945A2 (es) |
| CA (1) | CA2627653A1 (es) |
| EA (1) | EA016126B1 (es) |
| GE (1) | GEP20115213B (es) |
| IL (1) | IL190898A0 (es) |
| NO (1) | NO20081772L (es) |
| NZ (1) | NZ567659A (es) |
| PE (1) | PE20070532A1 (es) |
| TW (1) | TW200728289A (es) |
| WO (1) | WO2007050726A2 (es) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7285557B2 (en) * | 2001-10-15 | 2007-10-23 | Smithkline Beecham P.L.C. | Pyrimidinones as melanin concentrating hormone receptor 1 |
| US7553836B2 (en) * | 2006-02-06 | 2009-06-30 | Bristol-Myers Squibb Company | Melanin concentrating hormone receptor-1 antagonists |
| AU2007283113A1 (en) | 2006-08-08 | 2008-02-14 | Sanofi-Aventis | Arylaminoaryl-alkyl-substituted imidazolidine-2,4-diones, processes for preparing them, medicaments comprising these compounds, and their use |
| WO2008061109A2 (en) * | 2006-11-15 | 2008-05-22 | Forest Laboratories Holdings Limited | Indazole derivatives useful as melanin concentrating receptor ligands |
| US7851622B2 (en) | 2007-04-25 | 2010-12-14 | Bristol-Myers Squibb Company | Non-basic melanin concentrating hormone receptor-1 antagonists |
| EP2242745A1 (de) * | 2008-02-07 | 2010-10-27 | Sanofi-Aventis | Neue phenyl-substituierte imidazolidine, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
| PE20091928A1 (es) * | 2008-05-29 | 2009-12-31 | Bristol Myers Squibb Co | Tienopirimidinas hidroxisustituidas como antagonistas de receptor-1 de hormona concentradora de melanina no basicos |
| EP2310372B1 (en) | 2008-07-09 | 2012-05-23 | Sanofi | Heterocyclic compounds, processes for their preparation, medicaments comprising these compounds, and the use thereof |
| US8415386B2 (en) * | 2008-10-08 | 2013-04-09 | Bristol-Myers Squibb Company | Azolopyrrolone melanin concentrating hormone receptor-1 antagonists |
| CN102245608A (zh) | 2008-10-08 | 2011-11-16 | 百时美施贵宝公司 | 吡咯并三嗪酮黑色素浓集激素受体-1拮抗剂 |
| WO2010068601A1 (en) | 2008-12-08 | 2010-06-17 | Sanofi-Aventis | A crystalline heteroaromatic fluoroglycoside hydrate, processes for making, methods of use and pharmaceutical compositions thereof |
| EP2405913A1 (en) | 2009-03-09 | 2012-01-18 | Bristol-Myers Squibb Company | Pyridone analogs useful as melanin concentrating hormone receptor-1 antagonists |
| EP2406233B1 (en) | 2009-03-09 | 2013-11-13 | Bristol-Myers Squibb Company | Aza pyridone analogs useful as melanin concentrating hormone receptor-1 antagonists |
| ES2443016T3 (es) | 2009-08-26 | 2014-02-17 | Sanofi | Nuevos hidratos cristalinos de fluoroglicósidos heteroaromáticos, productos farmacéuticos que comprenden estos compuestos, y su empleo |
| EP2766349B1 (de) | 2011-03-08 | 2016-06-01 | Sanofi | Mit carbozyklen oder heterozyklen substituierte oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
| EP2683699B1 (de) | 2011-03-08 | 2015-06-24 | Sanofi | Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| US8828995B2 (en) | 2011-03-08 | 2014-09-09 | Sanofi | Branched oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof |
| EP2683705B1 (de) | 2011-03-08 | 2015-04-22 | Sanofi | Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| EP2683700B1 (de) | 2011-03-08 | 2015-02-18 | Sanofi | Tetrasubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| HUP1100241A3 (en) | 2011-05-06 | 2013-12-30 | Richter Gedeon Nyrt | Oxetane substituted pyrimidones |
| CN103130819B (zh) * | 2011-12-01 | 2016-01-20 | 中国科学院上海药物研究所 | 噻吩[3,2-d]并嘧啶-4-酮类化合物、其制备方法、药物组合物及用途 |
| JP6440625B2 (ja) | 2012-11-14 | 2018-12-19 | ザ・ジョンズ・ホプキンス・ユニバーシティー | 精神分裂病を処置するための方法および組成物 |
| WO2015114663A1 (en) | 2014-01-30 | 2015-08-06 | Council Of Scientific & Industrial Research | Novel thieno [2,3-d]pyrimidin-4(3h)-one compounds with antimycobacterial properties |
| TWI698436B (zh) | 2014-12-30 | 2020-07-11 | 美商佛瑪治療公司 | 作為泛素特異性蛋白酶7抑制劑之吡咯并及吡唑并嘧啶 |
| MA41291A (fr) | 2014-12-30 | 2017-11-07 | Forma Therapeutics Inc | Dérivés de la pyrrolotriazinone et de l'imidazotriazinone en tant qu'inhibiteurs de la protéase spécifique de l'ubiquitine n° 7 (usp7) pour le traitement d'un cancer |
| JP2018504431A (ja) | 2015-02-05 | 2018-02-15 | フォーマ セラピューティクス,インコーポレイテッド | ユビキチン特異的プロテアーゼ7阻害物質としてのチエノピリミジノン |
| HK1248220A1 (zh) | 2015-02-05 | 2018-10-12 | Forma Therapeutics, Inc. | 喹唑啉酮和偶氮喹唑啉作为泛特丁胺蛋白酶7抑制剂 |
| HK1248221A1 (zh) | 2015-02-05 | 2018-10-12 | Forma Therapeutics, Inc. | 异噻唑啉酮类,吡唑并嘧啶酮类和吡咯并嘧啶酮作为泛蛋白特异性蛋白酶7抑制剂 |
| ES2950348T3 (es) | 2015-12-09 | 2023-10-09 | Novartis Ag | Moduladores de receptores NMDA de tienopirimidinona y usos de los mismos |
| PT3386591T (pt) | 2015-12-09 | 2020-10-01 | Cadent Therapeutics Inc | Moduladores de recetores nmda heteroaromáticos e suas utilizações |
| CN107216339B (zh) * | 2016-03-22 | 2021-05-04 | 中国科学院上海药物研究所 | 一种dppiv抑制剂马来酸盐的多晶型及其制备方法 |
| WO2018119374A1 (en) | 2016-12-22 | 2018-06-28 | Cadent Therapeutics | Nmda receptor modulators and uses thereof |
| IL280474B2 (en) | 2018-08-03 | 2023-09-01 | Cadent Therapeutics Inc | Heteroaromatic nmda receptor modulators and their uses |
| WO2021207550A1 (en) * | 2020-04-08 | 2021-10-14 | Remix Therapeutics Inc. | Compounds and methods for modulating splicing |
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-
2006
- 2006-10-25 AR ARP060104665A patent/AR056155A1/es not_active Application Discontinuation
- 2006-10-25 US US11/586,255 patent/US8618115B2/en active Active
- 2006-10-26 JP JP2008537932A patent/JP2009513658A/ja not_active Withdrawn
- 2006-10-26 BR BRPI0617945-2A patent/BRPI0617945A2/pt not_active IP Right Cessation
- 2006-10-26 KR KR1020087012373A patent/KR20080067681A/ko not_active Ceased
- 2006-10-26 WO PCT/US2006/041725 patent/WO2007050726A2/en not_active Ceased
- 2006-10-26 AU AU2006306140A patent/AU2006306140A1/en not_active Abandoned
- 2006-10-26 EA EA200801165A patent/EA016126B1/ru not_active IP Right Cessation
- 2006-10-26 NZ NZ567659A patent/NZ567659A/en not_active IP Right Cessation
- 2006-10-26 TW TW095139575A patent/TW200728289A/zh unknown
- 2006-10-26 PE PE2006001304A patent/PE20070532A1/es not_active Application Discontinuation
- 2006-10-26 EP EP06817387A patent/EP1948665B1/en active Active
- 2006-10-26 GE GEAP200610710A patent/GEP20115213B/en unknown
- 2006-10-26 CA CA002627653A patent/CA2627653A1/en not_active Abandoned
- 2006-10-26 EP EP10013754A patent/EP2298776A1/en not_active Withdrawn
-
2008
- 2008-04-11 NO NO20081772A patent/NO20081772L/no not_active Application Discontinuation
- 2008-04-15 IL IL190898A patent/IL190898A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2009513658A (ja) | 2009-04-02 |
| EP1948665A2 (en) | 2008-07-30 |
| AU2006306140A1 (en) | 2007-05-03 |
| WO2007050726A3 (en) | 2007-08-30 |
| PE20070532A1 (es) | 2007-06-14 |
| TW200728289A (en) | 2007-08-01 |
| EP1948665B1 (en) | 2013-02-27 |
| NZ567659A (en) | 2011-06-30 |
| EP2298776A1 (en) | 2011-03-23 |
| US8618115B2 (en) | 2013-12-31 |
| GEP20115213B (en) | 2011-05-10 |
| BRPI0617945A2 (pt) | 2011-08-09 |
| CA2627653A1 (en) | 2007-05-03 |
| NO20081772L (no) | 2008-05-19 |
| US20070093509A1 (en) | 2007-04-26 |
| EA016126B1 (ru) | 2012-02-28 |
| IL190898A0 (en) | 2008-11-03 |
| KR20080067681A (ko) | 2008-07-21 |
| WO2007050726A2 (en) | 2007-05-03 |
| EA200801165A1 (ru) | 2008-10-30 |
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