AR057656A1 - Compuestos moduladores de receptores de androgeno y metodods relacionados - Google Patents

Compuestos moduladores de receptores de androgeno y metodods relacionados

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Publication number
AR057656A1
AR057656A1 ARP060102851A ARP060102851A AR057656A1 AR 057656 A1 AR057656 A1 AR 057656A1 AR P060102851 A ARP060102851 A AR P060102851A AR P060102851 A ARP060102851 A AR P060102851A AR 057656 A1 AR057656 A1 AR 057656A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
heteroalkyl
haloalkyl
heterohaloalkyl
hydrogen
Prior art date
Application number
ARP060102851A
Other languages
English (en)
Inventor
Lin Zhi
Oeveren Cornelis A Van
Bijan Pedram
Todd Miller
Original Assignee
Ligand Pharm Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ligand Pharm Inc filed Critical Ligand Pharm Inc
Publication of AR057656A1 publication Critical patent/AR057656A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/06—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton
    • C07C229/18—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to carbon atoms of six-membered aromatic rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C237/06—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C275/42—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/26—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C317/32—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C07D209/16—Tryptamines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/38—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/22—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with hetero atoms directly attached to ring nitrogen atoms
    • C07D295/26—Sulfur atoms
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Compuestos que se unen a los receptores de androgenos y modulan la actividad y/o cantidad de los mismos y métodos para su elaboracion y uso. También se proveen composiciones que incluyen tales compuestos y métodos para prepararlas. Reivindicacion 1: Un compuesto con una estructura seleccionada entre formulas (1) y la formula (Ia) caracterizado porque: R1 R2 y R3 se seleccionan en forma independiente entre hidrogeno, halogeno, ORA, SRA, NRARB, C1-C4 alquilo opcionalmente sustituido, C1-C4 haloalquilo opcionalmente sustituido, C1-C4 heteroalquilo opcionalmente sustituido, C1-C4 heterohaloalquilo opcionalmente sustituido y QT; R4,F5, R6, R7 R8 y R9 se seleccionan en forma independiente entre hidrogeno, C1,C6 heteroalquilo opcionalmente sustituido, C1-C6 haloalquilo opcionalmente sustituido, C1-C6 heteroalquilo opcionalmente sustituido, C1-C6 heterohaloalquilo opcionalmente sustituido y QT; RA y RB se seleccionan en forma independiente entre hidrogeno, C1-C6 haloalquilo, C1- C6heteroalquilo, C1-C6 heterohaloalquilo y QT; o RA y RB se unen para formar un anillo no aromático; RC y RD se seleccionan en forma independiente entre hidrogeno C1-C6alquilo, C1-C6 haloalquilo, C1-C6 heteroalquilo y C1-C6 heterohaloalquilo; o RC y RD se unen para formar un anillo no aromático; RE se selecciona entre hidrogeno, ORA, NRA, CORA, C1-C6 alquilo C1-C haloalquilo C1-C6 heterohaloalquilo; m se selecciona entre 0, 1 y 2; G se selecciona entre -CO-, -CS-, -SO2-y un enlace; V se selecciona entre O, S y NRE; X se selecciona entre O; S y NRA; con la salvedad de que al menos uno de RA, R1, R2, R3, R4, R5, R6, R7, R8 y R9 es QT, Q se selecciona entre C2-C12 alquilo opcionalmente sustituido, C2-C12 haloalquilo opcionalmente sustituido, C2-C12 heteroalquilo opcionalmente sustituido, C2-C12 arilalquilo opcionalmente sustituido, C2-C12 arilhaloalquilo opcionalmente sustituido y C2-C12 heteroarilheteroalquilo opcionalmente sustituido; y T se selecciona entre NO2, OH, CN, CO2R1, JRA (O)RCRD, RCS(O)2NRCRD, C(V)RC, C(V)ORC, OC(V)RC, C(V)NRCRD, OC(V)NRCRD, NRAC(V)RC, NRCC(V)NRCRD, NRCCO2RC; S(O)mRC, NRCSO2RD; SO2RD, SO2NRC, SO2NRCRD, C7-C10 haloalquilo opcionalmente sustituido y C7-C10 heteroalquilo opcionalmente sustituido, con la salvedad de que si R4, R5, R6, R7, R8, o R9 es QT, entonces T no es S(O)mRC; y sales aceptables para uso farmacéutico y prodrogas de los mismos.
ARP060102851A 2005-07-01 2006-06-30 Compuestos moduladores de receptores de androgeno y metodods relacionados AR057656A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US69594905P 2005-07-01 2005-07-01

Publications (1)

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AR057656A1 true AR057656A1 (es) 2007-12-12

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US (1) US20090227571A1 (es)
AR (1) AR057656A1 (es)
WO (1) WO2007005887A2 (es)

Families Citing this family (39)

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US7026484B2 (en) * 2001-02-23 2006-04-11 Ligand Pharmaceuticals Incorporated Tricyclic androgen receptor modulator compounds and methods
WO2005090282A1 (en) * 2004-03-12 2005-09-29 Ligand Pharmaceuticals Incorporated Androgen receptor modulator compounds and methods
CN101137655A (zh) 2005-06-17 2008-03-05 配体药物公司 雄激素受体调节剂化合物和方法
EP1957059A1 (en) * 2005-11-21 2008-08-20 Hadasit Medical Research Services And Development Ltd. Androgen-receptor (ar) ligands for use in the treatment and diagnosis of ar-related pathologies
WO2008012845A1 (en) * 2006-07-26 2008-01-31 Stmicroelectronics S.R.L. Use of nitroaniline derivatives for the production of nitric oxide
WO2009082437A2 (en) 2007-12-21 2009-07-02 Ligand Pharmaceuticals Incorporated Selective androgen receptor modulators (sarms) and uses thereof
WO2009089277A2 (en) 2008-01-08 2009-07-16 The Trustees Of The University Of Pennsylvania Rel inhibitors and methods of use thereof
US8268872B2 (en) 2008-02-22 2012-09-18 Radius Health, Inc. Selective androgen receptor modulators
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US9969751B2 (en) * 2009-06-10 2018-05-15 Techfields Pharma Co., Ltd. High penetration prodrug compositions of antimicrobials and antimicrobial-related compounds
AR078793A1 (es) 2009-10-27 2011-12-07 Orion Corp Derivados de carboxamidas no esteroidales y acil hidrazona moduladores de receptores androgenicos de tejido selectivo (sarm), composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del cancer de prostata entre otros
CA2788907A1 (en) 2010-02-04 2011-08-11 Radius Health, Inc. Selective androgen receptor modulators
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RU2460544C2 (ru) * 2010-11-19 2012-09-10 Федеральное государственное бюджетное учреждение "Ростовский научно-исследовательский онкологический институт" Министерства здравоохранения и социального развития Российской Федерации (ФГБУ РНИОН Минздравсоцразвития России) Способ определения эффективности лечения рака предстательной железы
US9682960B2 (en) 2013-12-19 2017-06-20 Endorecherche, Inc. Non-steroidal antiandrogens and selective androgen receptor modulators with a pyridyl moiety
CA2943611A1 (en) 2014-03-28 2015-10-01 Duke University Method of treating cancer using selective estrogen receptor modulators
US9421264B2 (en) 2014-03-28 2016-08-23 Duke University Method of treating cancer using selective estrogen receptor modulators
US20170273922A1 (en) * 2014-10-03 2017-09-28 The Royal Institution For The Advacement Of Learning/Mcgill University Urea and bis-urea based compounds and analogues thereof useful in the treatment of androgen receptor mediated diseases or disorders
US10806720B2 (en) 2015-04-21 2020-10-20 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US10035763B2 (en) 2015-04-21 2018-07-31 Gtx, Inc. Selective androgen receptor degrader (SARD) ligands and methods of use thereof
KR20170138536A (ko) 2015-04-21 2017-12-15 지티엑스, 인코포레이티드 선택적 안드로겐 수용체 분해제(sard) 리간드 및 이의 사용 방법
US10093613B2 (en) 2015-04-21 2018-10-09 Gtx, Inc. Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US10865184B2 (en) 2015-04-21 2020-12-15 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US10017471B2 (en) 2015-04-21 2018-07-10 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US10441570B2 (en) 2015-04-21 2019-10-15 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) Ligands and methods of use thereof
US9834507B2 (en) 2015-04-21 2017-12-05 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US10654809B2 (en) 2016-06-10 2020-05-19 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
CN107709290B (zh) 2015-04-21 2023-02-28 Gtx公司 选择性雄激素受体降解剂(sard)配体和其使用方法
IL255148B2 (en) 2015-04-29 2023-04-01 Radius Pharmaceuticals Inc 1901 rad for use in a method to inhibit a cancerous growth or induce tumor regression in a patient who is resistant to the drug and/or has cancer positive for an estrogen receptor alpha mutation
US11230523B2 (en) 2016-06-10 2022-01-25 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
KR102397890B1 (ko) 2016-06-22 2022-05-12 일립시스 파마 리미티드 Ar+ 유방암 치료 방법
KR102322802B1 (ko) 2017-01-05 2021-11-04 래디어스 파마슈티컬스, 인코포레이티드 Rad1901-2hcl의 다형 형태
CN110662536B (zh) 2017-03-29 2023-06-23 普渡研究基金会 激酶网络抑制剂及其用途
IL279853B1 (en) 2018-07-04 2024-09-01 Radius Pharmaceuticals Inc Polymorphic forms of RAD 1901-2HCL
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CN111116451A (zh) * 2020-01-16 2020-05-08 宁波大学 一种多取代色胺基苯甲酰胺类化合物及其制备方法和用途

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WO2007005887A2 (en) 2007-01-11
WO2007005887A3 (en) 2007-04-19

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