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PE20120775A1 - Derivados de tienopirimidindiona como moduladores de trpa1 - Google Patents

Derivados de tienopirimidindiona como moduladores de trpa1

Info

Publication number
PE20120775A1
PE20120775A1 PE2011001705A PE2011001705A PE20120775A1 PE 20120775 A1 PE20120775 A1 PE 20120775A1 PE 2011001705 A PE2011001705 A PE 2011001705A PE 2011001705 A PE2011001705 A PE 2011001705A PE 20120775 A1 PE20120775 A1 PE 20120775A1
Authority
PE
Peru
Prior art keywords
thiazol
optionally substituted
cyane
subfamily
cycloalkylalkyl
Prior art date
Application number
PE2011001705A
Other languages
English (en)
Inventor
Sukeerthi Kumar
Abraham Thomas
Sanjay Margal
Neelima Khairatkar-Joshi
Indranil Mukhopadhyay
Nayan Taterao Waghmare
Original Assignee
Glenmark Pharmaceuticals Sa
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42780205&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20120775(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Glenmark Pharmaceuticals Sa filed Critical Glenmark Pharmaceuticals Sa
Publication of PE20120775A1 publication Critical patent/PE20120775A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • A61P11/14—Antitussive agents
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    • 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
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
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    • A—HUMAN NECESSITIES
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    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
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    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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    • A—HUMAN NECESSITIES
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    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Otolaryngology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA (I) DONDE: R1 Y R2 SON CADA UNO H, ALQUILO C1-C4, HALOALQUILO, ALQUENILO, CICLOALQUILO, ENTRE OTROS; R3 ES H, CICLOALQUILALQUILO, CICLOALQUENILO OPCIONALMENTE SUSTITUIDO, ALQUINILO, ENTRE OTROS; L ES UN LIGADOR DE PREFERENCIA -CH2-, -C(O)-; Z1 Y Z2 SON CADA UNO S, CRa; V ES H, ARILO OPCIONALMENTE SUSTITUIDO, CIANO, NITRO, ENTRE OTROS; U ES ARILO OPCIONALMENTE SUSTITUIDO, TIAZOL, ISOXAZOL, IMIDAZOL, PIRAZOL, TIADIAZOL, PIRIMIDINA, ENTRE OTROS; Ra ES H, CIANO, HALOGENO, ALQUILO, HALOALQUILO, CICLOALQUILALQUILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 2-(1,3-DIMETIL-2,4-DIOXO-1,2,3,4-TETRAHIDROTIENO[2,3-d]PIRIMIDIN-5-IL)-N-[4-(TRIFLUOROMETIL)-1,3-TIAZOL-2-IL]ACETAMIDA; N-[4-(3,4-DICLOROFENIL)-1,3-TIAZOL-2-IL]-2-(1,3-DIMETIL-2,4-DIOXO-1,2,3,4-TETRAHIDROTIENO[2,3-d]PIRIMIDIN-5-IL)ACETAMIDA. REFERIDA ADEMAS A UNA COMPOSICION FARMACEUTICA. DICHO COMPUESTO ES UN DERIVADO DE TIENOPIRIMIDINDIONA MODULADOR DEL RECEPTOR POTENCIAL TRANSITORIO DE LA SUBFAMILIA A (TRPA) UTIL PARA TRATAR O PREVENIR ENFERMEDADES RELACIONADAS CON RECEPTOR POTENCIAL TRANSITORIO DE LA SUBFAMILIA A, MIEMBRO 1(TRPA1)
PE2011001705A 2009-03-23 2010-03-23 Derivados de tienopirimidindiona como moduladores de trpa1 PE20120775A1 (es)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
IN665MU2009 2009-03-23
US17135509P 2009-04-21 2009-04-21
IN2213MU2009 2009-09-23
US25199409P 2009-10-15 2009-10-15
IN2906MU2009 2009-12-16
US29447010P 2010-01-12 2010-01-12

Publications (1)

Publication Number Publication Date
PE20120775A1 true PE20120775A1 (es) 2012-06-27

Family

ID=42780205

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2011001704A PE20120834A1 (es) 2009-03-23 2010-03-22 Derivados de furopirimidindiona como moduladores de trpa1
PE2011001705A PE20120775A1 (es) 2009-03-23 2010-03-23 Derivados de tienopirimidindiona como moduladores de trpa1

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PE2011001704A PE20120834A1 (es) 2009-03-23 2010-03-22 Derivados de furopirimidindiona como moduladores de trpa1

Country Status (22)

Country Link
US (4) US20120178766A1 (es)
EP (3) EP2411395B1 (es)
JP (2) JP2012521406A (es)
KR (2) KR20110128898A (es)
CN (3) CN102361874A (es)
AP (1) AP2948A (es)
AU (2) AU2010227225A1 (es)
BR (2) BRPI1013705A2 (es)
CA (2) CA2756535A1 (es)
DK (3) DK2411395T3 (es)
EA (2) EA201190138A1 (es)
ES (3) ES2424341T3 (es)
HU (1) HUE024538T2 (es)
IL (2) IL215177A (es)
MX (1) MX2011009822A (es)
PE (2) PE20120834A1 (es)
PL (3) PL2411395T3 (es)
PT (3) PT2411395E (es)
SG (4) SG184767A1 (es)
SI (3) SI2411395T1 (es)
WO (2) WO2010109329A1 (es)
ZA (2) ZA201107649B (es)

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EA023857B1 (ru) 2009-03-23 2016-07-29 Гленмарк Фармасеутикалс С.А. Сочлененные производные пиримидиндионов в качестве модуляторов trpa1
JP5694560B2 (ja) 2010-12-20 2015-04-01 グレンマーク ファーマシューティカルズ， エセ．アー． Ｔｒｐａ１アンタゴニストとしての２−アミノ−４−アリールチアゾール化合物
EP2520566A1 (en) 2011-05-06 2012-11-07 Orion Corporation New Pharmaceutical Compounds
CN103826637A (zh) * 2011-06-13 2014-05-28 格兰马克药品股份有限公司 使用trpa1拮抗剂治疗呼吸疾患
WO2012176105A1 (en) 2011-06-22 2012-12-27 Glenmark Pharmaceuticals Sa Pharmaceutical composition comprising a trpa1 antagonist and a leukotriene receptor antagonist
US20140107113A1 (en) * 2011-06-22 2014-04-17 Glenmark Pharmaceuticals S.A. Pharmaceutical composition comprising a trpa1 antagonist and a beta-2 agonist
WO2013014597A1 (en) 2011-07-25 2013-01-31 Glenmark Pharmaceuticals Sa Pharmaceutical composition comprising a trpa1 antagonist and a steroid
EP2787991A1 (en) 2011-12-05 2014-10-15 Glenmark Pharmaceuticals S.A. Pharmaceutical composition comprising a trpa1 antagonist and an anticholinergic agent
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NZ706989A (en) 2012-10-01 2018-07-27 Orion Corp N-prop-2-ynyl carboxamide derivatives and their use as trpa1 antagonists
JP2016522251A (ja) * 2013-06-20 2016-07-28 グレンマーク ファーマシューティカルズ， エセ．アー． Ｔｒｐａ１アンタゴニストを含むナノ粒子製剤
US9532988B2 (en) 2013-10-15 2017-01-03 Glenmark Pharmaceuticals S.A. Pharmaceutical composition comprising a TRPA1 antagonist and an analgesic agent
WO2016023830A1 (en) * 2014-08-11 2016-02-18 Hydra Biosciences, Inc. Pyrido[2,3-d]pyrimidine-2,4(1h,3h)-dione derivatives
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US10329265B2 (en) 2014-08-22 2019-06-25 Duke University TRPA1 and TRPV4 inhibitors and methods of using the same for organ-specific inflammation and itch
WO2016042501A1 (en) * 2014-09-16 2016-03-24 Glenmark Pharmaceuticals S.A. Trpa1 antagonist for the treatment of pain associated to diabetic neuropathic pain
US11229628B2 (en) 2015-01-09 2022-01-25 Duke University TRPA1 and TRPV4 inhibitors and methods of using the same for organ-specific inflammation and itch
WO2017060488A1 (en) 2015-10-09 2017-04-13 Almirall, S.A. New trpa1 antagonists
WO2017064068A1 (en) 2015-10-14 2017-04-20 Almirall, S.A. New trpa1 antagonists
US11564911B2 (en) 2016-04-07 2023-01-31 Duke University Small molecule dual-inhibitors of TRPV4 and TRPA1 for sanitizing and anesthetizing
CN114874209B (zh) * 2017-03-07 2024-08-06 豪夫迈·罗氏有限公司 噁二唑瞬时受体电位通道抑制剂
CN109422749B (zh) * 2017-08-21 2023-01-24 重庆医药工业研究院有限责任公司 一种抑制单羧酸转运蛋白的嘧啶二酮衍生物
TW202229292A (zh) * 2020-10-14 2022-08-01 德商百靈佳殷格翰國際股份有限公司 作為trpa1抑制劑之四唑衍生物
TW202229293A (zh) * 2020-10-14 2022-08-01 德商百靈佳殷格翰國際股份有限公司 作為trpa1抑制劑之四唑衍生物
CN116940575A (zh) * 2021-02-23 2023-10-24 深圳市康哲药业有限公司 噻吩并嘧啶二酮类化合物及其应用
EP4323367A1 (en) 2021-04-14 2024-02-21 Boehringer Ingelheim International GmbH 3h,4h-thieno[2,3-d]pyrimidin-4-one derivatives as trpa1 inhibitors
CN114656480B (zh) * 2022-04-27 2024-01-26 成都施贝康生物医药科技有限公司 噻吩并嘧啶类化合物、异构体或盐及其制备方法和用途
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