CN102395592A - 作为trpa1调节剂的异噻唑并嘧啶二酮衍生物 - Google Patents

作为trpa1调节剂的异噻唑并嘧啶二酮衍生物 Download PDF

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Publication number
CN102395592A
CN102395592A CN2010800168801A CN201080016880A CN102395592A CN 102395592 A CN102395592 A CN 102395592A CN 2010800168801 A CN2010800168801 A CN 2010800168801A CN 201080016880 A CN201080016880 A CN 201080016880A CN 102395592 A CN102395592 A CN 102395592A
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CN
China
Prior art keywords
dimethyl
pyrimidin
acetamide
thiazolo
dioxo
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Pending
Application number
CN2010800168801A
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English (en)
Chinese (zh)
Inventor
苏克尔斯·库马尔
亚伯拉罕·托马斯
桑杰·玛格尔
尼利马·坎拉特卡-乔希
因德拉尼尔·穆霍帕拉艾
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Ichnos Sciences SA
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Glenmark Pharmaceuticals SA
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Application filed by Glenmark Pharmaceuticals SA filed Critical Glenmark Pharmaceuticals SA
Publication of CN102395592A publication Critical patent/CN102395592A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—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
    • 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
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P17/04—Antipruritics
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Otolaryngology (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
CN2010800168801A 2009-03-23 2010-03-22 作为trpa1调节剂的异噻唑并嘧啶二酮衍生物 Pending CN102395592A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
IN665/MUM/2009 2009-03-23
IN665MU2009 2009-03-23
US17135509P 2009-04-21 2009-04-21
US61/171,355 2009-04-21
PCT/IB2010/000834 WO2010109328A1 (en) 2009-03-23 2010-03-22 Isothiazolo-pyrimidinedione derivatives as trpa1 modulators

Publications (1)

Publication Number Publication Date
CN102395592A true CN102395592A (zh) 2012-03-28

Family

ID=42236291

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2010800168801A Pending CN102395592A (zh) 2009-03-23 2010-03-22 作为trpa1调节剂的异噻唑并嘧啶二酮衍生物

Country Status (22)

Country Link
US (1) US8575178B2 (https=)
EP (1) EP2411397B1 (https=)
JP (1) JP2012521405A (https=)
KR (1) KR20120001746A (https=)
CN (1) CN102395592A (https=)
AP (1) AP2011005888A0 (https=)
AU (1) AU2010227224A1 (https=)
BR (1) BRPI1009372A2 (https=)
CA (1) CA2756534A1 (https=)
DK (1) DK2411397T3 (https=)
EA (1) EA201190191A1 (https=)
ES (1) ES2424340T3 (https=)
IL (1) IL215179A0 (https=)
MX (1) MX2011009821A (https=)
PE (1) PE20120764A1 (https=)
PL (1) PL2411397T3 (https=)
PT (1) PT2411397E (https=)
SG (2) SG174403A1 (https=)
SI (1) SI2411397T1 (https=)
UA (1) UA107342C2 (https=)
WO (1) WO2010109328A1 (https=)
ZA (1) ZA201107646B (https=)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018233648A1 (zh) * 2017-06-21 2018-12-27 南京明德新药研发股份有限公司 作为TLR8激动剂的异噻唑并[4,3-d]嘧啶-5,7-二胺衍生物
CN112794860A (zh) * 2021-03-24 2021-05-14 上海肇钰医药科技有限公司 噁唑嘧啶酮酰胺类化合物或其可药用盐，制备方法及用途
CN114656480A (zh) * 2022-04-27 2022-06-24 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

Families Citing this family (20)

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AP3280A (en) 2009-03-23 2015-05-31 Glenmark Pharmaceuticals Sa Fused pyrimidine-dione derivatives as TRPA1 modulators
PT2411395E (pt) 2009-03-23 2013-06-06 Glenmark Pharmaceuticals Sa Derivados de furopirimidinadiona como moduladores de 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
JP2014517031A (ja) 2011-06-13 2014-07-17 グレンマーク ファーマシューティカルズ， エセ．アー． Ｔｒｐａ１アンタゴニストを使用した呼吸器疾患の治療
JP2014517062A (ja) 2011-06-22 2014-07-17 グレンマーク ファーマシューティカルズ， エセ．アー． ＴＲＰＡ１アンタゴニスト及びβ２アゴニストを含む医薬組成物
WO2012176105A1 (en) 2011-06-22 2012-12-27 Glenmark Pharmaceuticals Sa Pharmaceutical composition comprising a trpa1 antagonist and a leukotriene receptor antagonist
US20140148423A1 (en) 2011-07-25 2014-05-29 Glenmark Pharmaceuticals S.A. Pharmaceutical composition comprising a trpa1 antagonist and a steroid
TWI640519B (zh) * 2011-11-29 2018-11-11 泰緯生命科技股份有限公司 Ｈｅｃ１活性調控因子及其調節方法
EP2787991A1 (en) 2011-12-05 2014-10-15 Glenmark Pharmaceuticals S.A. Pharmaceutical composition comprising a trpa1 antagonist and an anticholinergic agent
MY165622A (en) 2012-06-08 2018-04-18 Glenmark Pharmaceuticals Sa Amides of 2-amino-4aryl thiazole compounds and their salts
PL2903965T3 (pl) 2012-10-01 2017-08-31 Orion Corporation Pochodne n-prop-2-ynylokarboksamidu i ich zastosowanie jako antagonistów trpa1
WO2014076021A1 (en) 2012-11-14 2014-05-22 F. Hoffmann-La Roche Ag Imidazopyridine derivatives
EP3010489A1 (en) 2013-06-20 2016-04-27 Glenmark Pharmaceuticals S.A. Nanoparticulate formulation comprising a trpa1 antagonist
AU2014335868A1 (en) 2013-10-15 2016-05-05 Glenmark Pharmaceuticals S.A. Pharmaceutical composition comprising a trpa1 antagonist and an analgesic agent
WO2015155306A1 (en) * 2014-04-11 2015-10-15 Almirall, S.A. New trpa1 antagonists
WO2016042501A1 (en) 2014-09-16 2016-03-24 Glenmark Pharmaceuticals S.A. Trpa1 antagonist for the treatment of pain associated to diabetic neuropathic pain
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
WO2025264860A2 (en) 2024-06-18 2025-12-26 Yale University Methods of treating post-covid airway disease

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MICHAEL BANDELL，等: "Noxious Cold Ion Channel TRPA1 Is Activated by Pungent Compounds and Bradykinin", 《NEURON》, vol. 41, no. 6, 25 March 2004 (2004-03-25), pages 849 - 857, XP002518916, DOI: doi:10.1016/S0896-6273(04)00150-3 *

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018233648A1 (zh) * 2017-06-21 2018-12-27 南京明德新药研发股份有限公司 作为TLR8激动剂的异噻唑并[4,3-d]嘧啶-5,7-二胺衍生物
CN112794860A (zh) * 2021-03-24 2021-05-14 上海肇钰医药科技有限公司 噁唑嘧啶酮酰胺类化合物或其可药用盐，制备方法及用途
CN112794860B (zh) * 2021-03-24 2021-06-29 上海肇钰医药科技有限公司 噁唑嘧啶酮酰胺类化合物或其可药用盐，制备方法及用途
CN114656480A (zh) * 2022-04-27 2022-06-24 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
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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KR20120001746A (ko) 2012-01-04
SG174403A1 (en) 2011-10-28
AU2010227224A2 (en) 2011-10-27
UA107342C2 (en) 2014-12-25
WO2010109328A1 (en) 2010-09-30
CA2756534A1 (en) 2010-09-30
ZA201107646B (en) 2012-06-25
JP2012521405A (ja) 2012-09-13
PE20120764A1 (es) 2012-06-27
EP2411397B1 (en) 2013-05-29
SG184766A1 (en) 2012-10-30
US20120010223A1 (en) 2012-01-12
BRPI1009372A2 (pt) 2016-05-31
EA201190191A1 (ru) 2012-11-30
EP2411397A1 (en) 2012-02-01
PT2411397E (pt) 2013-06-06
US8575178B2 (en) 2013-11-05
MX2011009821A (es) 2012-01-25
SI2411397T1 (sl) 2013-07-31
IL215179A0 (en) 2011-12-29
DK2411397T3 (da) 2013-08-05
ES2424340T3 (es) 2013-10-01
AP2011005888A0 (en) 2011-10-31
AU2010227224A1 (en) 2011-09-29
PL2411397T3 (pl) 2013-10-31
HK1166081A1 (en) 2012-10-19

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Application publication date: 20120328