ES2561674T3 - Antagonistas de TRPV4 - Google Patents

Antagonistas de TRPV4 Download PDF

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Publication number
ES2561674T3
ES2561674T3 ES11760129.4T ES11760129T ES2561674T3 ES 2561674 T3 ES2561674 T3 ES 2561674T3 ES 11760129 T ES11760129 T ES 11760129T ES 2561674 T3 ES2561674 T3 ES 2561674T3
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Spain
Prior art keywords
4alkyl
independently
morpholinyl
piperidinyl
pyrrolidinyl
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Active
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ES11760129.4T
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English (en)
Inventor
Carl A. Brooks
Mui Cheung
Hilary S. Eidam
Ryan M. Fox
Mark A. Hilfiker
Eric S. Manas
Guosen Ye
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GlaxoSmithKline LLC
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GlaxoSmithKline LLC
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    • 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
    • C07D401/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • 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
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • 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
    • C07D401/14—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 three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Otolaryngology (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Un compuesto de Fórmula I:**Fórmula** en donde: R1 es independientemente H, CF3 o Me; R2 es independientemente OH, Oalquilo C1-4, alquilo C1-4, CH2OH, F, CH2Oalquilo C1-4, CF3 o CF2H; R3 es morfolinilo, piperidinilo, pirrolidinilo o hexahidroazepinilo; todos los cuales pueden estar sin sustituir o sustituidos con uno o dos R8; o R3 es N(alquilo C1-6 )2, en donde alquilo C1-6 puede estar sin sustituir o sustituido con OH o -OCH3; R4 es CF3, halo, OMe o alquilo; R5 es halo, ciano, CF3, alquilo C1-5, alquenilo C2-4, pirrolidinilo, morfolinilo, piperidinilo, fenilo, piridilo, pirazolilo, pirrolilo, piperazinilo, pirimidinilo, OH, O-alquil C1-4-OR6, OCF3, OCH2CF3, OCH2CN, OR6 o CH2R9; en donde el pirrolidinilo, morfolinilo, piperidinilo, fenilo, piridilo, pirazolilo, pirrolilo, piperazinilo o pirimidinilo puede estar sin sustituir o sustituido con uno o dos halo, OH, OR6 o R6; R6 es independientemente alquilo C1-4, cicloalquilo C3-6; R7 es independientemente halo, metilo o OMe; R8 es independientemente OH, Oalquilo C1-4, alquilo C1-4, CH2OH, F, CH2Oalquilo C1-4, CF3 o CF2H; R9 es independientemente pirrolidinilo, morfolinilo o piperidinilo; R10 es independientemente H, CF3 o Me; n es independientemente 0, 1 o 2; X es N o C; y es 1 o 2; o una de sus sales farmacéuticamente aceptables.
ES11760129.4T 2010-03-23 2011-03-23 Antagonistas de TRPV4 Active ES2561674T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US31643210P 2010-03-23 2010-03-23
US316432P 2010-03-23
PCT/US2011/029579 WO2011119701A1 (en) 2010-03-23 2011-03-23 Trpv4 antagonists

Publications (1)

Publication Number Publication Date
ES2561674T3 true ES2561674T3 (es) 2016-02-29

Family

ID=44673594

Family Applications (1)

Application Number Title Priority Date Filing Date
ES11760129.4T Active ES2561674T3 (es) 2010-03-23 2011-03-23 Antagonistas de TRPV4

Country Status (5)

Country Link
US (1) US8658636B2 (es)
EP (1) EP2549872B1 (es)
JP (1) JP5819397B2 (es)
ES (1) ES2561674T3 (es)
WO (1) WO2011119701A1 (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPWO2013146754A1 (ja) 2012-03-27 2015-12-14 塩野義製薬株式会社 Ｔｒｐｖ４阻害活性を有する芳香族複素５員環誘導体
US10335414B2 (en) 2012-12-03 2019-07-02 Indiana University Research And Technology Corporation Use of TRPV4 antagonists to ameliorate hydrocephalus and related materials and methods
WO2015046193A1 (ja) 2013-09-25 2015-04-02 塩野義製薬株式会社 Ｔｒｐｖ４阻害活性を有する芳香族複素環式アミン誘導体
WO2018156401A1 (en) 2017-02-24 2018-08-30 Indiana University Research And Technology Corporation Methods of inhibiting serum glucocorticoid induced kinase 1 (sgk1) as a treatment for salt and water balance diseases
BR112022019628A2 (pt) 2020-04-30 2022-11-16 Raqualia Pharma Inc Composto da fórmula (i), enantiômero único, composição farmacêutica, processo para a preparação desta, método para o tratamento de uma condição ou distúrbio mediado pela atividade antagonista do receptor de trpv4 em um animal incluindo um humano, uso de um composto e composto representado pela fórmula (i-d)
CA3189206A1 (en) 2020-07-16 2022-01-20 Raqualia Pharma Inc. Trpv4 inhibitor as therapeutic agent for ocular disease

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW531537B (en) 1995-12-27 2003-05-11 Janssen Pharmaceutica Nv 1-(1,2-disubstituted piperidinyl)-4-substituted piperidine derivatives
AR021354A1 (es) * 1998-11-20 2002-07-17 Smithkline Beecham Spa Procedimiento para la preparacion de un compuesto derivado de quinolina y un procedimiento para preparar una composicion farmaceutica
US6511649B1 (en) * 1998-12-18 2003-01-28 Thomas D. Harris Vitronectin receptor antagonist pharmaceuticals
SE0004054D0 (sv) * 2000-11-06 2000-11-06 Astrazeneca Ab N-type calcium channel antagonists for the treatment of pain
GB0028964D0 (en) * 2000-11-28 2001-01-10 Smithkline Beecham Spa Novel compounds
WO2007071055A1 (en) * 2005-12-21 2007-06-28 Painceptor Pharma Corporation Compositions and methods for modulating gated ion channels
EP2312947B1 (en) * 2008-07-25 2014-01-01 GlaxoSmithKline LLC Trpv4 antagonists
WO2011119693A1 (en) * 2010-03-23 2011-09-29 Glaxosmithkline Llc Trpv4 antagonists

Also Published As

Publication number Publication date
US20130012499A1 (en) 2013-01-10
US8658636B2 (en) 2014-02-25
WO2011119701A1 (en) 2011-09-29
EP2549872A4 (en) 2014-08-06
EP2549872B1 (en) 2015-11-25
JP2013522372A (ja) 2013-06-13
EP2549872A1 (en) 2013-01-30
JP5819397B2 (ja) 2015-11-24

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