BR9810340A - Sìntese e uso de compostos retinóides com atividades de hormÈnio negativo e/ou antagonistas - Google Patents

Sìntese e uso de compostos retinóides com atividades de hormÈnio negativo e/ou antagonistas

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Publication number
BR9810340A
BR9810340A BR9810340-7A BR9810340A BR9810340A BR 9810340 A BR9810340 A BR 9810340A BR 9810340 A BR9810340 A BR 9810340A BR 9810340 A BR9810340 A BR 9810340A
Authority
BR
Brazil
Prior art keywords
retinoid
negative
hormone
retinoids
administered
Prior art date
Application number
BR9810340-7A
Other languages
English (en)
Inventor
Elliott S Klein
Alan T Johnson
Andrew M Standeven
Richard L Beard
Samuel J Gillett
Tien T Duong
Sunil Nagpal
Vidyasagar Vuligonda
Min Teng
Roshantha A Chandraratna
Original Assignee
Allergan Sales 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 Allergan Sales Inc filed Critical Allergan Sales Inc
Publication of BR9810340A publication Critical patent/BR9810340A/pt

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    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/46—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms containing six-membered aromatic rings and other rings, e.g. cyclohexylphenylacetic acid
    • C07C57/50—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms containing six-membered aromatic rings and other rings, e.g. cyclohexylphenylacetic acid containing condensed ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/16—Emollients or protectives, e.g. against radiation
    • 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
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
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    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • C07C233/87—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
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    • C07C69/76—Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring
    • C07C69/84—Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring
    • C07C69/90—Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring with esterified hydroxyl and carboxyl groups
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Abstract

Patente de Invenção: <B>"SìNTESE E USO DE COMPOSTOS RETINóIDES COM ATIVIDADES DE HORMÈNIO NEGATIVO E/OU ANTAGONISTAS"<D>. Derivados do tipo benzopirano, benzotiopirano, 1,2-dihidroquinolina e 5,6-dihidronaftaleno substituídos com arila e com arila e (3-oxo-1-propenila) possuem atividades biológicas do tipo hormónio negativo e/ou antagonista de retinóides. Os antagonistas de RAR inventados podem ser administrados a mamíferos, inclusive humanos, com a finalidade de prevenir ou diminuir a ação de agonistas de RAR nos sítios receptores ligados. Especificamente, os agonistas de RAR são administrados ou co-administrados com drogas retinóides para prevenir ou melhorar toxidez ou efeitos secundários causados por retinóides ou vitamina A ou precursores de vitamina A. os hormónios negativos de retinóides podem ser usados para potencializar as atividades de outros retinóides e agonistas de receptores nucleares. Por exemplo, o hormónio negativo de retinóide chamado AGN 193109 aumentou eficazmente a eficácia de outros retinóides e hormónios esteróides em ensaios de transativação in vitro. Adicionalmente, ensaios de transativação podem ser usados para identificar compostos tendo atividade de hormónio negativo. Estes ensaios baseiam-se na capacidade dos hormónios negativos para sub-regular a atividade de receptores de retinóides quiméricos construídos para possuir um domínio ativador de transcrição constitutiva.
BR9810340-7A 1997-06-24 1998-06-24 Sìntese e uso de compostos retinóides com atividades de hormÈnio negativo e/ou antagonistas BR9810340A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US08/880,823 US5877207A (en) 1996-03-11 1997-06-24 Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities
PCT/US1998/013065 WO1998058922A1 (en) 1997-06-24 1998-06-24 Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities

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BR9810340A true BR9810340A (pt) 2000-09-19

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BR9810340-7A BR9810340A (pt) 1997-06-24 1998-06-24 Sìntese e uso de compostos retinóides com atividades de hormÈnio negativo e/ou antagonistas

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Country Link
US (1) US5877207A (pt)
EP (2) EP0991636B1 (pt)
JP (1) JP4295361B2 (pt)
KR (1) KR100512058B1 (pt)
CN (1) CN1142928C (pt)
AT (1) ATE289998T1 (pt)
AU (1) AU729140B2 (pt)
BR (1) BR9810340A (pt)
CA (1) CA2294601A1 (pt)
DE (1) DE69829183T2 (pt)
WO (1) WO1998058922A1 (pt)

Families Citing this family (92)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5952345A (en) 1995-09-01 1999-09-14 Allergan Sales, Inc. Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities
US6008204A (en) 1995-09-01 1999-12-28 Allergan Sales, Inc. Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities
CA2344653A1 (en) * 1998-09-29 2000-04-06 Gamida Cell Ltd. Methods of controlling proliferation and differentiation of stem and progenitor cells
DE69923854T2 (de) * 1998-10-08 2006-01-12 Allergan, Inc., Irvine Rar-antagonisten zur verhütung für männer
US6521641B1 (en) * 1998-10-08 2003-02-18 Allergan, Inc. Male anti-fertility agents
CA2254429A1 (en) * 1998-11-19 2000-05-19 Tully Michael Underhill Compositions for promoting chondrogenesis
WO2000034435A2 (en) * 1998-12-08 2000-06-15 Clontech Laboratories, Inc. Cis-element reporter constructs and uses thereof
WO2000061233A2 (en) 1999-04-14 2000-10-19 Allergan Sales, Inc. Methods and compositions for the treatment and prevention of lung disease involving a specific rar-gamma agonist
WO2000061232A2 (en) 1999-04-14 2000-10-19 Allergan Sales, Inc. Methods and compositions for the treatment and prevention of lung disease involving a specific rar-beta antagonist
US6043381A (en) * 1999-05-07 2000-03-28 Allergan Sales, Inc. Process for preparing substituted benzo[1,2-g]-chrom-3-ene, benzo[1,2-g]-thiochrom-3-ene and benzo[1,2-g]-1,2-dihydroquinoline derivatives
US6166244A (en) * 1999-05-07 2000-12-26 Allergan Sales, Inc. Oxygen, sulfur and nitrogen substituted cyclohexene and cyclohexane derivatives having retinoid-like biological activity
US6177588B1 (en) 1999-05-07 2001-01-23 Allergan Sales, Inc. 1-alkoxy and 1-acyloxy substituted cyclohex-1-ene compounds and sulfur and 1-alkoxycarbonyl analogs having retinoid-like biological activity
US6906057B1 (en) 1999-06-11 2005-06-14 Allergan, Inc. Methods for modulating FXR receptor activity
JP2003502337A (ja) 1999-06-11 2003-01-21 アラーガン・セイルズ・インコーポレイテッド 核ホルモン受容体調節活性を有するオルガノシリル化合物
US6093838A (en) * 1999-08-16 2000-07-25 Allergan Sales, Inc. Amines substituted with a dihydro-benzofuranyl or with a dihydro-isobenzofuranyl group, an aryl or heteroaryl group and an alkyl group, having retinoid-like biological activity
US6127382A (en) * 1999-08-16 2000-10-03 Allergan Sales, Inc. Amines substituted with a tetrahydroquinolinyl group an aryl or heteroaryl group and an alkyl group, having retinoid-like biological activity
US6313168B1 (en) * 1999-12-15 2001-11-06 Allergan Sales, Inc. Use of retinoid receptor antagonists in the treatment of cartilage and bone pathologies
US20030114482A1 (en) * 1999-12-15 2003-06-19 Maurizio Pacifici Use of retinoid receptor antagonists or agonists in the treatment of cartilage and bone pathologies
AU2291001A (en) 1999-12-23 2001-07-03 Emory University Chalcone and its analogs as agents for the inhibition of angiogenesis and related disease states
US20030125252A1 (en) * 2000-03-14 2003-07-03 Underhill T. Michael Compositions and methods for affecting osteogenesis
US6613917B1 (en) * 2000-03-23 2003-09-02 Allergan, Inc. Amines substituted with a dihydronaphthalenyl, chromenyl, or thiochromenyl group, an aryl or heteroaryl group and an alkyl group, having retinoid-like biological activity
WO2002022113A2 (en) 2000-09-13 2002-03-21 Bristol-Myers Squibb Company Retinoic acid receptor antagonists as promoters of angiogenesis
US20020193403A1 (en) * 2001-05-03 2002-12-19 Allergan Sales, Inc. Methods of treating hyperlipidemia
US7482366B2 (en) 2001-12-21 2009-01-27 X-Ceptor Therapeutics, Inc. Modulators of LXR
AU2002351412B2 (en) * 2001-12-21 2010-05-20 Exelixis Patent Company Llc Modulators of LXR
IL152904A0 (en) * 2002-01-24 2003-06-24 Gamida Cell Ltd Utilization of retinoid and vitamin d receptor antagonists for expansion of renewable stem cell populations
WO2003062404A1 (en) * 2002-01-25 2003-07-31 Gamida-Cell Ltd. Methods of expanding stem and progenitor cells and expanded cell populations obtained thereby
US6720423B2 (en) 2002-04-30 2004-04-13 Allergan, Inc. Dihydrobenzofuran and dihydrobenzothiophene 2,4-pentadienoic acid derivatives having selective activity for retinoid X (RXR) receptors
US6620963B1 (en) 2002-09-19 2003-09-16 Allergan, Inc. TRICYCLO[6.2.202,7]DODECA-2(7),3,5-TRIEN-4-CARBONYLAMINO-PHENYL AND TRICYCLO[6.2.202,7]DODECA-2(7),3,5-TRIEN-4-CARBONYLAMINO-HETEROARYL AND RELATED COMPOUNDS HAVING RARα RECEPTOR SELECTIVE BIOLOGICAL ACTIVITY
US7105566B2 (en) * 2002-10-22 2006-09-12 Allergan, Inc. Methods of treatment during vascular procedures
US20050027003A1 (en) * 2003-07-30 2005-02-03 Allergan, Inc. Methods of therapeutic treatment using retinoids with reduced side effects
US20050026958A1 (en) * 2003-07-30 2005-02-03 Allergan, Inc. Methods of therapeutic treatment using amounts of retinoid components
US20050026950A1 (en) * 2003-07-30 2005-02-03 Allergan, Inc. Methods of therapeutic treatment using retinoids to achieve consistent bioavailability
US20050026949A1 (en) * 2003-07-30 2005-02-03 Allergan, Inc. Methods of therapeutic treatment using amounts of retinoids without regard to body weight
US20050101582A1 (en) 2003-11-12 2005-05-12 Allergan, Inc. Compositions and methods for treating a posterior segment of an eye
US20060141049A1 (en) * 2003-11-12 2006-06-29 Allergan, Inc. Triamcinolone compositions for intravitreal administration to treat ocular conditions
US20070224278A1 (en) * 2003-11-12 2007-09-27 Lyons Robert T Low immunogenicity corticosteroid compositions
MXPA06007255A (es) * 2003-12-26 2006-08-18 Allergan Inc Oximas de chalcona disubstituidas que tienen actividad antagonista de los receptores retinoides rar?.
EP1706095B1 (en) 2004-01-20 2008-12-24 Allergan, Inc. Compositions for localized therapy of the eye, comprising preferably triamcinolone acetonide and hyaluronic acid
US8722097B2 (en) 2004-04-30 2014-05-13 Allergan, Inc. Oil-in-water method for making polymeric implants containing a hypotensive lipid
US8591885B2 (en) 2004-04-30 2013-11-26 Allergan, Inc. Carbonic anhydrase inhibitor sustained release intraocular drug delivery systems
US20050244461A1 (en) * 2004-04-30 2005-11-03 Allergan, Inc. Controlled release drug delivery systems and methods for treatment of an eye
US20050244466A1 (en) * 2004-04-30 2005-11-03 Allergan, Inc. Photodynamic therapy in conjunction with intraocular implants
US8119154B2 (en) * 2004-04-30 2012-02-21 Allergan, Inc. Sustained release intraocular implants and related methods
US20050244463A1 (en) * 2004-04-30 2005-11-03 Allergan, Inc. Sustained release intraocular implants and methods for treating ocular vasculopathies
US9498457B2 (en) 2004-04-30 2016-11-22 Allergan, Inc. Hypotensive prostamide-containing biodegradable intraocular implants and related implants
US20050244465A1 (en) * 2004-04-30 2005-11-03 Allergan, Inc. Drug delivery systems and methods for treatment of an eye
WO2005110374A1 (en) * 2004-04-30 2005-11-24 Allergan, Inc. Intraocular drug delivery systems containing a therapeutic component, a cyclodextrin, and a polymeric component
US20050244471A1 (en) * 2004-04-30 2005-11-03 Allergan, Inc. Estradiol derivative and estratopone containing sustained release intraocular implants and related methods
US7799336B2 (en) 2004-04-30 2010-09-21 Allergan, Inc. Hypotensive lipid-containing biodegradable intraocular implants and related methods
US20050244462A1 (en) * 2004-04-30 2005-11-03 Allergan, Inc. Devices and methods for treating a mammalian eye
BRPI0510485A (pt) 2004-04-30 2007-11-13 Allergan Inc implantes inibidores de tirosina cinase intravìtreos biodegradáveis
US20050244478A1 (en) * 2004-04-30 2005-11-03 Allergan, Inc. Anti-excititoxic sustained release intraocular implants and related methods
US8455656B2 (en) 2004-04-30 2013-06-04 Allergan, Inc. Kinase inhibitors
US8673341B2 (en) * 2004-04-30 2014-03-18 Allergan, Inc. Intraocular pressure reduction with intracameral bimatoprost implants
US7993634B2 (en) 2004-04-30 2011-08-09 Allergan, Inc. Oil-in-oil emulsified polymeric implants containing a hypotensive lipid and related methods
US8147865B2 (en) 2004-04-30 2012-04-03 Allergan, Inc. Steroid-containing sustained release intraocular implants and related methods
US20070059336A1 (en) * 2004-04-30 2007-03-15 Allergan, Inc. Anti-angiogenic sustained release intraocular implants and related methods
US20050244458A1 (en) * 2004-04-30 2005-11-03 Allergan, Inc. Sustained release intraocular implants and methods for treating ocular neuropathies
US8425929B2 (en) * 2004-04-30 2013-04-23 Allergan, Inc. Sustained release intraocular implants and methods for preventing retinal dysfunction
US7771742B2 (en) * 2004-04-30 2010-08-10 Allergan, Inc. Sustained release intraocular implants containing tyrosine kinase inhibitors and related methods
AU2005271700B2 (en) * 2004-07-12 2010-11-11 Allergan, Inc. Opthalmic compositions and methods for treating ophthalmic conditions
EP1799812A4 (en) 2004-09-16 2009-09-09 Gamida Cell Ltd EX VIVO CULTIVATION METHODS OF STEM CELLS AND PRECURSOR BY CO-CULTURE WITH MESENCHYMAL CELLS
WO2006043965A1 (en) * 2004-10-14 2006-04-27 Allergan, Inc. Therapeutic ophthalmic compositions containing retinal friendly excipients and related methods
PT1937244T (pt) 2005-09-30 2018-11-07 Io Therapeutics Llc Tratamento do cancro com agonistas específicos de rxr
PL1957636T3 (pl) * 2005-10-27 2018-12-31 Viacyte, Inc. Grzbietowa i brzuszna endoderma jelita przedniego wykazująca ekspresję pdx1
US8846393B2 (en) 2005-11-29 2014-09-30 Gamida-Cell Ltd. Methods of improving stem cell homing and engraftment
CA2651487A1 (en) * 2006-05-16 2007-11-29 Vitae Pharmaceuticals, Inc. Methods for treating chemotherapy and radiation therapy side effects
US8969415B2 (en) 2006-12-01 2015-03-03 Allergan, Inc. Intraocular drug delivery systems
US7911053B2 (en) * 2007-04-19 2011-03-22 Marvell World Trade Ltd. Semiconductor packaging with internal wiring bus
US8082730B2 (en) * 2008-05-20 2011-12-27 Caterpillar Inc. Engine system having particulate reduction device and method
RU2567792C2 (ru) 2009-11-09 2015-11-10 Аллерган, Инк. Композиции и способы стимулирования роста волос
AU2012352149B2 (en) 2011-12-13 2017-06-01 Io Therapeutics, Inc. Autoimmune disorder treatment using RXR agonists
BR112014020119A2 (pt) 2012-02-13 2020-10-27 Gamida-Cell Ltd cultura de células-tronco mesenquimais
US9175266B2 (en) 2012-07-23 2015-11-03 Gamida Cell Ltd. Enhancement of natural killer (NK) cell proliferation and activity
US9567569B2 (en) 2012-07-23 2017-02-14 Gamida Cell Ltd. Methods of culturing and expanding mesenchymal stem cells
CN103044477B (zh) * 2012-12-07 2015-08-05 中国科学院广州生物医药与健康研究院 三甲基硅取代苯并吡喃类化合物及其应用
RU2641021C2 (ru) 2013-02-15 2018-01-17 Аллерган, Инк. Имплантат для пролонгированной доставки лекарственного средства
EP3368080B8 (en) 2015-10-31 2023-04-26 IO Therapeutics, Inc. Treatment of nervous system disorders using combinations of rxr agonists and thyroid hormones
EP4098257A1 (en) 2015-11-25 2022-12-07 IO Therapeutics, Inc. Use of cyp26-resistant rar alpha selective agonists in the treatment of cancer
MX2018010863A (es) 2016-03-10 2019-01-10 Io Therapeutics Inc Tratamiento contra trastornos musculares con combinaciones de agonistas rxr y hormonas tiroideas.
CN114470218A (zh) 2016-03-10 2022-05-13 Io治疗公司 用rxr激动剂与甲状腺激素的组合的自身免疫疾病的治疗
CN107176945B (zh) * 2016-03-11 2021-06-08 中国科学院上海有机化学研究所 一种视黄酸类化合物、其制备方法、中间体及应用
KR102277395B1 (ko) * 2016-06-02 2021-07-15 호유 가부시키가이샤 알 알레르기의 항원
EP3468600A4 (en) 2016-06-10 2019-11-13 IO Therapeutics, Inc. RETINOID COMPOUNDS AND RELECTIVE REXINOIDS OF THE RECEPTOR AND IMMUNE MODULATORS FOR IMMUNOTHERAPY OF CANCER
US10213401B2 (en) 2017-07-13 2019-02-26 Io Therapeutics, Inc. Immunomodulatory and differentiating function selective retinoid and rexinoid compounds in combination with immune modulators for cancer immunotherapy
CA3073953A1 (en) 2017-08-31 2019-03-07 Io Therapeutics, Inc. Rar selective agonists in combination with immune modulators for cancer immunotherapy
EP3684348A4 (en) 2017-09-20 2021-08-18 IO Therapeutics, Inc. TREATMENT OF DISEASE WITH SELECTIVE RXR AGONIST ESTERS
CN110090237B (zh) * 2019-05-30 2021-05-28 四川农业大学 一种用于治疗维生素a中毒所致肝损伤和骨损伤的药物及用途
US10966950B2 (en) 2019-06-11 2021-04-06 Io Therapeutics, Inc. Use of an RXR agonist in treating HER2+ cancers
AU2020408043A1 (en) * 2019-12-19 2022-07-28 Orphagen Pharmaceuticals, Inc. RAR-alpha compounds for inflammatory disease and male contraception
WO2023108012A1 (en) 2021-12-07 2023-06-15 Io Therapeutics, Inc. Use of an rxr agonist and taxanes in treating her2+ cancers

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2138000A1 (en) * 1994-01-03 1995-07-04 John E. Starrett, Jr. Retinoid-like compounds
US5776699A (en) * 1995-09-01 1998-07-07 Allergan, Inc. Method of identifying negative hormone and/or antagonist activities
US5675024A (en) * 1995-11-22 1997-10-07 Allergan Aryl or heteroaryl amides of tetrahydronaphthalene, chroman, thiochroman and 1,2,3,4,-tetrahydroquinoline carboxylic acids, having an electron withdrawing substituent in the aromatic or heteroaromatic moiety, having retinoid-like biological activity

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