AR088087A1 - Inhibidores de la monoacilglicerol lipasa para el tratamiento de enfermedades metabolicas y trastornos relacionados - Google Patents
Inhibidores de la monoacilglicerol lipasa para el tratamiento de enfermedades metabolicas y trastornos relacionadosInfo
- Publication number
- AR088087A1 AR088087A1 ARP120103651A ARP120103651A AR088087A1 AR 088087 A1 AR088087 A1 AR 088087A1 AR P120103651 A ARP120103651 A AR P120103651A AR P120103651 A ARP120103651 A AR P120103651A AR 088087 A1 AR088087 A1 AR 088087A1
- Authority
- AR
- Argentina
- Prior art keywords
- compound
- thiazol
- trifluoromethyl
- pyridinyl
- pyridin
- Prior art date
Links
- 208000030159 metabolic disease Diseases 0.000 title abstract 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- -1 [1,2,3] thiadiazolyl Chemical group 0.000 abstract 13
- 150000001875 compounds Chemical class 0.000 abstract 10
- 238000000034 method Methods 0.000 abstract 4
- 208000016097 disease of metabolism Diseases 0.000 abstract 3
- 125000000437 thiazol-2-yl group Chemical group [H]C1=C([H])N=C(*)S1 0.000 abstract 3
- 125000004495 thiazol-4-yl group Chemical group S1C=NC(=C1)* 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000001153 fluoro group Chemical group F* 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000012453 solvate Substances 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 125000006345 2,2,2-trifluoroethoxymethyl group Chemical group [H]C([H])(*)OC([H])([H])C(F)(F)F 0.000 abstract 1
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical group [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 abstract 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical group [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- HKKPDZNDQBHUOD-UHFFFAOYSA-N [4-[1-[3-chloro-6-(trifluoromethyl)-1-benzothiophene-2-carbonyl]azetidin-3-yl]piperazin-1-yl]-(1,3-thiazol-4-yl)methanone Chemical compound S1C2=CC(C(F)(F)F)=CC=C2C(Cl)=C1C(=O)N(C1)CC1N(CC1)CCN1C(=O)C1=CSC=N1 HKKPDZNDQBHUOD-UHFFFAOYSA-N 0.000 abstract 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 abstract 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 abstract 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 abstract 1
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 abstract 1
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 abstract 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Chemical group BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 abstract 1
- 229910052794 bromium Inorganic materials 0.000 abstract 1
- 125000001246 bromo group Chemical group Br* 0.000 abstract 1
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000004281 furazan-3-yl group Chemical group [H]C1=NON=C1* 0.000 abstract 1
- 125000002541 furyl group Chemical group 0.000 abstract 1
- 125000002883 imidazolyl group Chemical group 0.000 abstract 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 abstract 1
- 125000001041 indolyl group Chemical group 0.000 abstract 1
- 229910052740 iodine Chemical group 0.000 abstract 1
- 239000011630 iodine Chemical group 0.000 abstract 1
- 125000004501 isothiazol-5-yl group Chemical group S1N=CC=C1* 0.000 abstract 1
- 125000001786 isothiazolyl group Chemical group 0.000 abstract 1
- 125000000842 isoxazolyl group Chemical group 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 125000002971 oxazolyl group Chemical group 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 abstract 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 abstract 1
- 125000003831 tetrazolyl group Chemical group 0.000 abstract 1
- 125000000335 thiazolyl group Chemical group 0.000 abstract 1
- 125000001544 thienyl group Chemical group 0.000 abstract 1
- 125000001425 triazolyl group Chemical group 0.000 abstract 1
Classifications
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- 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
-
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Reproductive Health (AREA)
- Urology & Nephrology (AREA)
- Neurology (AREA)
- Child & Adolescent Psychology (AREA)
- Vascular Medicine (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Reivindicación 1: Un método para tratar, mejorar, o prevenir una enfermedad metabólica; el método comprende administrar a un sujeto que lo necesita, una cantidad terapéuticamente eficaz de un compuesto de la fórmula (1) o un enantiómero, diastereómero, solvato, o sal farmacéuticamente aceptable de este; en donde: Y es un heteroarilo seleccionado del grupo que consiste en tienilo, furanilo, tiazolilo, isotiazolilo, oxazolilo, piridinilo, isoxazolilo, imidazolilo, furazan-3-il, pirazolilo, triazolilo, tetrazolilo, y [1,2,3]tiadiazolilo; en donde Y se sustituye, opcionalmente, independientemente, con uno a dos sustituyentes seleccionados del grupo que consiste en fluoro, cloro, bromo, alquilo C₁₋₄, ciano, y trifluorometilo; Z es un heteroarilo seleccionado del grupo que consiste en indolilo, indazolilo, benzoxazolilo, benzotiazolilo, benzotienilo, benzofuranilo, imidazo[1,2-a]piridin-2-il, pirrolo[2,3-b]piridinilo, pirrolo[3,2-b]piridinilo, tieno[2,3-b]piridinilo, quinolinilo, quinazolinilo, y bencimidazolilo; en donde dicho Z se sustituye, opcionalmente, independientemente, con uno a dos sustituyentes seleccionados del grupo que consiste en alquilo C₁₋₄, trifluorometilo, 2,2,2-trifluoroetoxi-metilo, 2,2,2-trifluoroetoxi, trifluorometiltio, cloro, fluoro, bromo, y yodo; siempre y cuando un compuesto de la fórmula (1) sea distinto de un compuesto en donde Y es tiazol-4-ilo y Z es 5-fluoro-3H-bencimidazol-2-ilo; un compuesto en donde Y es tiazol-2-ilo y Z es 5-fluoro-1H-bencimidazol-2-ilo; un compuesto en donde Y es tiazol-4-ilo y Z es 5-cloro-benzofuran-2-ilo; un compuesto en donde Y es isotiazol-5-ilo y Z es 6-trifluorometil-1H-indol-2-ilo; un compuesto en donde Y es tiazol-4-ilo y Z es 5-trifluorometil-1H-pirrolo[3,2-b]piridin-2-ilo; un compuesto en donde Y es tiazol-2-ilo y Z es 8-bromo-6-cloro-imidazo[1,2-a]piridin-2-ilo; o un compuesto en donde Y es tiazol-2-ilo y Z es 6-trifluorometil-imidazo[1,2-a]piridin-2-ilo. Reivindicación 9: Un método para tratar, mejorar, o prevenir una enfermedad metabólica; el método comprende administrar a un sujeto que lo necesita una cantidad terapéuticamente eficaz de 1-(1-{[3-cloro-6-(trifluorometil)-1-benzotiofen-2-il]carbonilo}azetidin-3-il)-4-(1,3-tiazol-4-ilcarbonil)piperazina de fórmula (2), o un solvato o sal farmacéuticamente aceptable de este. Reivindicación 12: El uso del compuesto de fórmula (2) como en la reivindicación 9 para la preparación de un medicamento o composición farmacéutica para el tratamiento de una enfermedad metabólica que es obesidad o diabetes, en un sujeto que lo necesita.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161541403P | 2011-09-30 | 2011-09-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR088087A1 true AR088087A1 (es) | 2014-05-07 |
Family
ID=47116336
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120103651A AR088087A1 (es) | 2011-09-30 | 2012-10-01 | Inhibidores de la monoacilglicerol lipasa para el tratamiento de enfermedades metabolicas y trastornos relacionados |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US9375430B2 (es) |
| EP (1) | EP2760451A1 (es) |
| JP (1) | JP2014528429A (es) |
| KR (1) | KR20140068241A (es) |
| CN (1) | CN103841973A (es) |
| AR (1) | AR088087A1 (es) |
| CA (1) | CA2850100A1 (es) |
| MX (1) | MX2014003883A (es) |
| TW (1) | TW201328695A (es) |
| WO (1) | WO2013049293A1 (es) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3087067B1 (en) | 2013-12-26 | 2018-10-24 | Takeda Pharmaceutical Company Limited | 4-(piperrazin-1-yl)-pyrrolidin-2-one compounds as monoacylglycerol lipase (magl) inhibitors |
| WO2016158956A1 (ja) | 2015-03-30 | 2016-10-06 | 武田薬品工業株式会社 | 複素環化合物 |
| US10610520B2 (en) | 2016-03-31 | 2020-04-07 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| EP3436444B1 (en) | 2016-03-31 | 2020-05-13 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| EP3689879B1 (en) | 2017-09-29 | 2025-02-12 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| WO2023130023A1 (en) | 2021-12-29 | 2023-07-06 | Psy Therapeutics, Inc. | Inhibiting monoacylglycerol lipase (magl) |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20090082435A1 (en) * | 2005-04-28 | 2009-03-26 | The Regents Of The University Of California | Methods, Compositions, And Compounds For Modulation Of Monoacylglycerol Lipase, Pain, And Stress-Related Disorders |
| WO2008019357A2 (en) * | 2006-08-07 | 2008-02-14 | Ironwood Pharmaceuticals, Inc. | Indole compounds |
| FR2915198B1 (fr) * | 2007-04-18 | 2009-12-18 | Sanofi Aventis | Derives de triazolopyridine-carboxamides et triazolopyridine -carboxamides, leur preparation et leur application en therapeutique. |
| FR2915199B1 (fr) * | 2007-04-18 | 2010-01-22 | Sanofi Aventis | Derives de triazolopyridine-carboxamides et triazolopyrimidine-carboxamides, leur preparation et leur application en therapeutique. |
| WO2009117444A1 (en) * | 2008-03-17 | 2009-09-24 | Northeastern University | Inhibitors of fatty acid amide hydrolase and monoacylglycerol lipase for modulation of cannabinoid receptors |
| AR076381A1 (es) * | 2009-04-22 | 2011-06-08 | Janssen Pharmaceutica Nv | Azetidinil diamidas como inhibidores de monoacilglicerol lipasa |
-
2012
- 2012-09-27 MX MX2014003883A patent/MX2014003883A/es unknown
- 2012-09-27 EP EP12780572.9A patent/EP2760451A1/en not_active Withdrawn
- 2012-09-27 CN CN201280048300.6A patent/CN103841973A/zh active Pending
- 2012-09-27 US US13/628,452 patent/US9375430B2/en active Active
- 2012-09-27 JP JP2014533708A patent/JP2014528429A/ja not_active Withdrawn
- 2012-09-27 CA CA2850100A patent/CA2850100A1/en not_active Abandoned
- 2012-09-27 KR KR1020147011417A patent/KR20140068241A/ko not_active Withdrawn
- 2012-09-27 WO PCT/US2012/057470 patent/WO2013049293A1/en not_active Ceased
- 2012-09-28 TW TW101135732A patent/TW201328695A/zh unknown
- 2012-10-01 AR ARP120103651A patent/AR088087A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| US20130085130A1 (en) | 2013-04-04 |
| JP2014528429A (ja) | 2014-10-27 |
| WO2013049293A1 (en) | 2013-04-04 |
| KR20140068241A (ko) | 2014-06-05 |
| TW201328695A (zh) | 2013-07-16 |
| EP2760451A1 (en) | 2014-08-06 |
| MX2014003883A (es) | 2014-08-27 |
| US9375430B2 (en) | 2016-06-28 |
| CA2850100A1 (en) | 2013-04-04 |
| CN103841973A (zh) | 2014-06-04 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |