AR088208A1 - 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
- AR088208A1 AR088208A1 ARP120103650A ARP120103650A AR088208A1 AR 088208 A1 AR088208 A1 AR 088208A1 AR P120103650 A ARP120103650 A AR P120103650A AR P120103650 A ARP120103650 A AR P120103650A AR 088208 A1 AR088208 A1 AR 088208A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- pyridin
- substituents
- trifluoromethyl
- fluoro
- Prior art date
Links
- 208000030159 metabolic disease Diseases 0.000 title abstract 2
- 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 7
- 125000001424 substituent group Chemical group 0.000 abstract 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 3
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000001153 fluoro group Chemical group F* 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 3
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000002541 furyl group Chemical group 0.000 abstract 2
- 125000000842 isoxazolyl group Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 2
- 125000000168 pyrrolyl group Chemical group 0.000 abstract 2
- 125000000335 thiazolyl group Chemical group 0.000 abstract 2
- 125000001544 thienyl group Chemical group 0.000 abstract 2
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 abstract 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 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 Substances 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
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 239000000460 chlorine Substances 0.000 abstract 1
- 208000016097 disease of metabolism Diseases 0.000 abstract 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 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
- 125000001786 isothiazolyl group Chemical group 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 125000002971 oxazolyl group Chemical group 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
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000000437 thiazol-2-yl group Chemical group [H]C1=C([H])N=C(*)S1 0.000 abstract 1
- 125000001425 triazolyl group Chemical group 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Reproductive Health (AREA)
- Urology & Nephrology (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Child & Adolescent Psychology (AREA)
- Vascular Medicine (AREA)
- Pulmonology (AREA)
- Neurology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
Reivindicación 1: Un método para tratar, mejorar, o prevenir una enfermedad metabólica; que comprende administrar a un sujeto que lo necesita una cantidad terapéuticamente eficaz de un compuesto de la fórmula (1) o un enantiómero, diastereómero, o sal farmacéuticamente aceptable de este; en donde: Y es un heteroarilo seleccionado del grupo que consiste en tienilo, furanilo, tiazolilo, isotiazolilo, oxazolilo, pirrolilo, isoxazolilo, triazolilo, y [1,2,3]tiadiazolilo; en donde Y se sustituye, opcionalmente, con un sustituyente seleccionado 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, benzofuranilo, benzotienilo, 1H-pirrolo[3,2-b]piridin-5-ilo, 1H-tieno[2,3-c]pirazol-5-ilo, 1H-pirrolo[2,3-b]piridin-5-ilo, 1H-pirazolo[3,4-b]piridin-5-ilo, furo[2,3-b]piridin-2-ilo, quinazolinilo, y bencimidazolilo; en donde Z se sustituye, opcionalmente, independientemente, con uno a dos sustituyentes seleccionados del grupo que consiste en cloro, fluoro, alquilo C₁₋₄, alcoxi C₁₋₄, y trifluorometilo; y Z se sustituye con un sustituyente adicional que es (i) fenilo o (ii) un heteroarilo seleccionado del grupo que consiste en pirimidinilo, tienilo, quinolinilo, piridinilo, isoxazolilo, tiazolilo, bencimidazolilo, pirrolilo, furanilo, pirimidinilo, y pirazolilo; y en donde los sustituyentes fenilo y heteroarilo de Z se sustituyen, opcionalmente, independientemente, con uno a dos sustituyentes seleccionados del grupo que consiste en alquilo C₁₋₄; alcoxi C₁₋₄; uno a tres sustituyentes fluoro o cloro; trifluorometilo; trifluorometoxi; ciano; carboxi; aminocarbonilo; formilo; nitro; bromo; hidroxi; y alquilsulfonilo C₁₋₄; siempre y cuando un compuesto de la fórmula (1) es distinto de un compuesto en donde Y es tiazol-2-il y Z es 5-(2-fluoropiridin-3-il)-1H-benzimidazol-2-ilo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161541394P | 2011-09-30 | 2011-09-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR088208A1 true AR088208A1 (es) | 2014-05-14 |
Family
ID=47046854
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120103650A AR088208A1 (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) | US8987247B2 (es) |
| EP (1) | EP2760450A1 (es) |
| JP (1) | JP2014528428A (es) |
| KR (1) | KR20140068243A (es) |
| CN (1) | CN103957916A (es) |
| AR (1) | AR088208A1 (es) |
| CA (1) | CA2849782A1 (es) |
| MX (1) | MX2014003879A (es) |
| TW (1) | TW201313708A (es) |
| WO (1) | WO2013049289A1 (es) |
Families Citing this family (10)
| 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 |
| JP6653319B2 (ja) | 2015-03-30 | 2020-02-26 | 武田薬品工業株式会社 | 複素環化合物 |
| MY194647A (en) | 2016-03-31 | 2022-12-09 | Takeda Pharmaceuticals Co | Heterocyclic compound |
| EP3438109B1 (en) | 2016-03-31 | 2021-08-25 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| KR102011556B1 (ko) * | 2016-07-19 | 2019-08-16 | 연세대학교 산학협력단 | 2-모노아실글리세롤 절단 효소를 포함하는 간지방증 또는 비알코올성 지방간의 예방, 개선 또는 치료용 조성물 |
| WO2019065791A1 (ja) | 2017-09-29 | 2019-04-04 | 武田薬品工業株式会社 | 複素環化合物 |
| UY39066A (es) * | 2020-02-10 | 2021-08-31 | Janssen Pharmaceutica Nv | Moduladores de monoacilglicerol lipasa |
| EP4126825A1 (en) | 2020-03-26 | 2023-02-08 | Janssen Pharmaceutica NV | Aminocyclobutanes as monoacylglycerol lipase modulators |
| KR20220158008A (ko) | 2020-03-26 | 2022-11-29 | 얀센 파마슈티카 엔.브이. | 모노아실글리세롤 리파아제 조절제로서의 아자스피로사이클 |
| EP4126840A1 (en) | 2020-03-26 | 2023-02-08 | Janssen Pharmaceutica NV | Aryl piperidines as monoacylglycerol lipase modulators |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2915198B1 (fr) * | 2007-04-18 | 2009-12-18 | Sanofi Aventis | Derives de triazolopyridine-carboxamides et triazolopyridine -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 |
| BRPI1013545A2 (pt) * | 2009-04-22 | 2019-09-24 | Janssen Phamaceutica N V | azetidinil diamidas como inibidores de monoacilglicerol lipase |
| AU2010238746B2 (en) * | 2009-04-22 | 2015-02-19 | Janssen Pharmaceutica Nv | Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors |
-
2012
- 2012-09-27 KR KR1020147011424A patent/KR20140068243A/ko not_active Application Discontinuation
- 2012-09-27 MX MX2014003879A patent/MX2014003879A/es unknown
- 2012-09-27 CA CA2849782A patent/CA2849782A1/en not_active Abandoned
- 2012-09-27 WO PCT/US2012/057465 patent/WO2013049289A1/en active Application Filing
- 2012-09-27 JP JP2014533705A patent/JP2014528428A/ja not_active Withdrawn
- 2012-09-27 US US13/628,428 patent/US8987247B2/en active Active
- 2012-09-27 EP EP12775378.8A patent/EP2760450A1/en not_active Withdrawn
- 2012-09-27 CN CN201280059367.XA patent/CN103957916A/zh active Pending
- 2012-09-28 TW TW101135711A patent/TW201313708A/zh unknown
- 2012-10-01 AR ARP120103650A patent/AR088208A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| MX2014003879A (es) | 2014-09-01 |
| CN103957916A (zh) | 2014-07-30 |
| WO2013049289A1 (en) | 2013-04-04 |
| CA2849782A1 (en) | 2013-04-04 |
| US20130085129A1 (en) | 2013-04-04 |
| US8987247B2 (en) | 2015-03-24 |
| TW201313708A (zh) | 2013-04-01 |
| EP2760450A1 (en) | 2014-08-06 |
| JP2014528428A (ja) | 2014-10-27 |
| KR20140068243A (ko) | 2014-06-05 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |