AR073282A1 - Compuestos de imidazolidina como moduladores del receptor de androgenos - Google Patents
Compuestos de imidazolidina como moduladores del receptor de androgenosInfo
- Publication number
- AR073282A1 AR073282A1 ARP090103461A ARP090103461A AR073282A1 AR 073282 A1 AR073282 A1 AR 073282A1 AR P090103461 A ARP090103461 A AR P090103461A AR P090103461 A ARP090103461 A AR P090103461A AR 073282 A1 AR073282 A1 AR 073282A1
- Authority
- AR
- Argentina
- Prior art keywords
- halo
- cyano
- optionally substituted
- alkyl
- nitro
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
- C07D233/60—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- 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
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- 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
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- 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
- A61P35/00—Antineoplastic agents
-
- 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
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
-
- 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
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/26—Androgens
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
- C07D233/72—Two oxygen atoms, e.g. hydantoin
- C07D233/74—Two oxygen atoms, e.g. hydantoin with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to other ring members
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
- C07D233/72—Two oxygen atoms, e.g. hydantoin
- C07D233/76—Two oxygen atoms, e.g. hydantoin with substituted hydrocarbon radicals attached to the third ring carbon atom
- C07D233/78—Radicals substituted by oxygen atoms
Abstract
Composiciones farmacéuticas, para la prevencion y el tratamiento de una variedad de afecciones en mamíferos, incluido el ser humano, que incluyen, a modo de ejemplos no Iimitativos, caquexia, osteoporosis, sarcopenia, disminucion de la líbido y/o disfuncion sexual. Reivindicacion 1: Un compuesto de acuerdo con la formula (1) en donde X es O o s; R1 es H; o R1 se selecciona de alquilo C1-6, cicloalquilo C3-7, alquenilo C3-6, alquinilo C3-6 y acilo C1-6, cada uno de los cuales puede estar opcionalmente sustituido con ciano, uno o varios halo, hidroxilo o aIcoxi C1-6; R2a se selecciona de H, P(O)(OH)2 y C(O)(CH2)n1C(O)OH; o R2a se selecciona de acilo C1-6 y alqueniIo C3-6; cada uno de los cuales puede estar opcionalmente sustituido con arilo, amino o carboxi; n1 es 0, 1, 2, 3 o 4; cada R2b y R2c se selecciona independientemente de H y aIquilo C1-6, o R2b y R2c se pueden unir para formar un cicloalquilo C3-7; R3a es H, halo, ciano o nitro; o R3a es alquilo C1-6 opciorialmente sustituido con halo, ciano, nitro, hidroxilo o alcoxi C1-4; o R3a es amido opcionalmente sustituido con alquino C1-6; cada R3b es independientemente halo, ciano o nitro; o cada R3b es independientemente alquilo C1-6 opcionalmerte sustituido con ciano o halo; o cada R3b es amido opcionalmente sustituido con alquilo C1-6; cada R4a y R4b es independientemente H, halo. ciano, carboxi o nitro; a cada R4a y R4b se selecciona de alquilo C1-6 y alcoxi C1-6; cada uno de los cuales puede estar opcionalmente sustituido por uno o varios halo o alcoxi C1-6; o R4a y R4b se unen para formar un cicloalquilo de 5 o 6 miembros, heterocicloalquilo de 5 o 6 miembros, arilo de 5 o 6 miembros, o heteroarilo de 5 o 6 miembros; R4c es halo, ciano o nitro; y m1 es 0, 1 o 2; o sales farmacéuticamente aceptables, y los solvatos de los compuestos o los solvatos de sus sales farmacéuticamente aceptables; o sus estereoisomeros.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US19191808P | 2008-09-11 | 2008-09-11 | |
GB0900333.6A GB2463514C (en) | 2008-09-11 | 2009-01-09 | Imidazolidine compounds and uses therefor |
Publications (1)
Publication Number | Publication Date |
---|---|
AR073282A1 true AR073282A1 (es) | 2010-10-28 |
Family
ID=40379370
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP090103461A AR073282A1 (es) | 2008-09-11 | 2009-09-09 | Compuestos de imidazolidina como moduladores del receptor de androgenos |
Country Status (20)
Country | Link |
---|---|
US (2) | US7968581B2 (es) |
EP (1) | EP2344460B1 (es) |
JP (1) | JP5595402B2 (es) |
KR (1) | KR101705157B1 (es) |
CN (1) | CN102149687B (es) |
AR (1) | AR073282A1 (es) |
AU (1) | AU2009290849B2 (es) |
BR (1) | BRPI0919290A2 (es) |
CA (1) | CA2736364C (es) |
CO (1) | CO6382130A2 (es) |
ES (1) | ES2552684T3 (es) |
GB (1) | GB2463514C (es) |
HK (1) | HK1141015A1 (es) |
IL (1) | IL211277A (es) |
MX (1) | MX2011002374A (es) |
NZ (1) | NZ591374A (es) |
RU (1) | RU2488584C2 (es) |
TW (1) | TWI449698B (es) |
WO (1) | WO2010029119A1 (es) |
ZA (1) | ZA201101707B (es) |
Families Citing this family (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8168667B2 (en) * | 2006-05-31 | 2012-05-01 | Galapagos Nv | Imidazolidine derivatives, uses therefor, preparation thereof and compositions comprising such |
CN103608333B (zh) | 2011-03-10 | 2016-01-06 | 苏州开拓药业有限公司 | 雄激素受体拮抗剂及其用途 |
GB201311107D0 (en) * | 2013-06-21 | 2013-08-07 | Univ Edinburgh | Bioorthogonal methods and compounds |
ES2934319T3 (es) * | 2013-07-18 | 2023-02-21 | Baylor College Medicine | Métodos y composiciones para el tratamiento de la atrofia muscular, la debilidad muscular y/o la caquexia |
CN105979943A (zh) * | 2013-10-25 | 2016-09-28 | 厄恩斯特.D.布什 | 肌营养不良的治疗方法 |
EP3089975B1 (en) * | 2013-12-31 | 2018-06-06 | Ipsen Pharma S.A.S. | Novel imidazolidine-2, 4-dione derivatives |
JP7028987B2 (ja) * | 2017-12-06 | 2022-03-02 | アイブライト メディカル テクノロジー (ペキン) カンパニー リミテッド | オルソケラトロジーレンズおよびその製造方法 |
HUE059318T2 (hu) | 2018-04-19 | 2022-11-28 | Tvardi Therapeutics Inc | STAT3 inhibitorok |
US11026905B2 (en) | 2018-04-19 | 2021-06-08 | Tvardi Therapeutics, Inc. | STAT3 inhibitors |
CN115052584A (zh) | 2020-01-24 | 2022-09-13 | 特维迪疗法公司 | 治疗性化合物及其制剂和用途 |
CN113024513A (zh) * | 2021-03-22 | 2021-06-25 | 中国药科大学 | 新型雄激素受体降解剂、制备方法和医药用途 |
CN113801064A (zh) * | 2021-09-26 | 2021-12-17 | 甘肃省化工研究院有限责任公司 | 一种[3+2]环加成反应构建苯基乙内酰脲的方法 |
Family Cites Families (27)
Publication number | Priority date | Publication date | Assignee | Title |
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JPS5136332B1 (es) * | 1970-12-09 | 1976-10-07 | ||
GB1601310A (en) * | 1978-05-23 | 1981-10-28 | Lilly Industries Ltd | Aryl hydantoins |
DE2855770A1 (de) | 1978-12-22 | 1980-07-10 | Bayer Ag | Hydantoine |
US4753957A (en) | 1981-09-28 | 1988-06-28 | Rohm And Haas Company | Substituted 2,4-imidazolidinediones and fungicidal compositions |
EP0091596B1 (de) | 1982-04-08 | 1991-09-11 | Shell Internationale Researchmaatschappij B.V. | Neue Hydantoine, ihre Herstellung und Verwendung |
FR2619381B1 (fr) * | 1987-08-13 | 1989-12-08 | Roussel Uclaf | Nouvelles imidazolidines substituees par un radical hydroxymethyle et un radical phenyl substitue, leur procede de preparation, leur application comme medicaments, les compositions pharmaceutiques les renfermant et un intermediaire pour leur preparation |
JP2566792B2 (ja) | 1987-09-30 | 1996-12-25 | 株式会社資生堂 | 発毛、養毛促進剤 |
JPH0219363A (ja) | 1988-07-06 | 1990-01-23 | Fujisawa Pharmaceut Co Ltd | イミダゾリジン誘導体 |
US4992443A (en) | 1990-03-12 | 1991-02-12 | William Chelen | Method of treating motion sickness |
US5346913A (en) | 1992-05-26 | 1994-09-13 | Rohm And Haas Company | N-iodopropargyl hydantoin compounds, compositions, preparation, and use as antimicrobial agents |
JP3137430B2 (ja) | 1992-06-10 | 2001-02-19 | 鐘淵化学工業株式会社 | 5,5−二置換ヒダントインの製造法 |
US6846525B2 (en) | 1993-03-19 | 2005-01-25 | Xerox Corporation | Recording sheets containing purine, pyrimidine, benzimidazole, imidazolidine, urazole, pyrazole, triazole, benzotriazole, tetrazole, and pyrazine compounds |
TW521073B (en) * | 1994-01-05 | 2003-02-21 | Hoechst Marion Roussel Inc | New optionally substituted phenylimidazolidines, their preparation process, their use as anti-androgenic agent and the pharmaceutical compositions containing them |
FR2715402B1 (fr) * | 1994-01-05 | 1996-10-04 | Roussel Uclaf | Nouvelles phénylimidazolines éventuellement substituées, leur procédé et des intermédiaires de préparation, leur application comme médicaments et les compositions pharmaceutiques les renfermant. |
AU1884595A (en) | 1994-04-29 | 1995-11-29 | Pfizer Inc. | Novel acyclic and cyclic amides as neurotransmitter release enhancers |
EP0760239A3 (en) | 1995-09-01 | 1999-04-14 | Pfizer Inc. | Therapeutic agents for use in cancer therapy |
FR2741342B1 (fr) * | 1995-11-22 | 1998-02-06 | Roussel Uclaf | Nouvelles phenylimidazolidines fluorees ou hydroxylees, procede, intermediaires de preparation, application comme medicaments, nouvelle utilisation et compositions pharmaceutiques |
DE69811867T2 (de) | 1997-03-03 | 2003-11-20 | Boehringer Ingelheim Pharma | Kleine moleküle anwendbar in der behandlung von entzündgskrankheiten |
US6355664B1 (en) | 1997-03-03 | 2002-03-12 | Boehringer Ingelheim Pharmaceuticals, Inc. | Phenylpyrrolidines, phenylimidazolidines, 3-phenyl-1,3-oxizolidines and 3-phenyl-1,3-thiazolidines and their use in the treatment of inflammatory disease |
UA57081C2 (uk) | 1997-06-16 | 2003-06-16 | Пфайзер Продактс Інк. | Фармацевтична композиція для лікування раку або доброякісних проліферативних хвороб у ссавців, спосіб лікування, фармацевтична композиція для інгібування ненормального росту клітин у ссавців та спосіб інгібування |
US6492553B1 (en) | 1998-01-29 | 2002-12-10 | Aventis Pharamaceuticals Inc. | Methods for preparing N-[(aliphatic or aromatic)carbonyl)]-2-aminoaetamide compounds and for cyclizing such compounds |
DE19912383A1 (de) | 1998-03-27 | 1999-09-30 | Degussa | Verfahren zur Herstellung von cyclischen 4-Oxoamidinen |
DE60129222T2 (de) | 2000-05-11 | 2008-03-06 | Consejo Superior de Investigaciónes Científicas | Heterocyclischen inhibitoren von glycogen synthase kinase gsk-3 |
US6846643B2 (en) | 2000-08-14 | 2005-01-25 | Boehringer Ingelheim Pharmaceuticals, Inc. | Methods and molecules useful for identifying molecules that bind LFA-1 and for determining receptor occupancy |
CN101056862B (zh) * | 2004-09-10 | 2013-03-13 | 詹森药业有限公司 | 作为选择性雄激素受体调节剂(sarms)的咪唑烷-2-酮衍生物 |
WO2007047146A2 (en) | 2005-10-11 | 2007-04-26 | Intermune, Inc. | Inhibitors of viral replication |
GB0610765D0 (en) * | 2006-05-31 | 2006-07-12 | Proskelia Sas | Imidazolidine derivatives, uses therefor, preparation thereof and compositions comprising such |
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2009
- 2009-01-09 GB GB0900333.6A patent/GB2463514C/en not_active Expired - Fee Related
- 2009-09-09 AR ARP090103461A patent/AR073282A1/es unknown
- 2009-09-10 BR BRPI0919290-5A patent/BRPI0919290A2/pt not_active Application Discontinuation
- 2009-09-10 ES ES09782854.5T patent/ES2552684T3/es active Active
- 2009-09-10 RU RU2011113749/04A patent/RU2488584C2/ru not_active IP Right Cessation
- 2009-09-10 JP JP2011526487A patent/JP5595402B2/ja not_active Expired - Fee Related
- 2009-09-10 MX MX2011002374A patent/MX2011002374A/es active IP Right Grant
- 2009-09-10 US US12/557,368 patent/US7968581B2/en active Active
- 2009-09-10 CA CA2736364A patent/CA2736364C/en not_active Expired - Fee Related
- 2009-09-10 CN CN200980135475.9A patent/CN102149687B/zh not_active Expired - Fee Related
- 2009-09-10 EP EP09782854.5A patent/EP2344460B1/en active Active
- 2009-09-10 AU AU2009290849A patent/AU2009290849B2/en not_active Ceased
- 2009-09-10 KR KR1020117007686A patent/KR101705157B1/ko active IP Right Grant
- 2009-09-10 NZ NZ591374A patent/NZ591374A/en not_active IP Right Cessation
- 2009-09-10 WO PCT/EP2009/061733 patent/WO2010029119A1/en active Application Filing
- 2009-09-11 TW TW098130825A patent/TWI449698B/zh not_active IP Right Cessation
-
2010
- 2010-08-02 HK HK10107354.3A patent/HK1141015A1/xx not_active IP Right Cessation
-
2011
- 2011-02-17 IL IL211277A patent/IL211277A/en not_active IP Right Cessation
- 2011-03-04 ZA ZA2011/01707A patent/ZA201101707B/en unknown
- 2011-04-08 CO CO11043783A patent/CO6382130A2/es not_active Application Discontinuation
- 2011-06-23 US US13/167,682 patent/US8383608B2/en active Active
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