BR112016006151A2 - imidazopiridazinas úteis como inibidores da via de sinalização do par-2 - Google Patents

imidazopiridazinas úteis como inibidores da via de sinalização do par-2

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Publication number
BR112016006151A2
BR112016006151A2 BR112016006151A BR112016006151A BR112016006151A2 BR 112016006151 A2 BR112016006151 A2 BR 112016006151A2 BR 112016006151 A BR112016006151 A BR 112016006151A BR 112016006151 A BR112016006151 A BR 112016006151A BR 112016006151 A2 BR112016006151 A2 BR 112016006151A2
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BR
Brazil
Prior art keywords
compounds
par
inhibitors
signaling pathway
useful
Prior art date
Application number
BR112016006151A
Other languages
English (en)
Inventor
Liu Bingcan
Elie SAYEGH Camil
Sturino Claudio
Yannopoulos Constantin
Vallee Frederic
Szychowski Janek
Lacoste Jean-Eric
Martel Julien
J Farmer Luc
St-Onge Miguel
Bubenik Monica
Fournier Pierre-Andre
Lessard Stephanie
K Ramtohul Yeeman
Original Assignee
Vertex Pharma
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 Vertex Pharma filed Critical Vertex Pharma
Publication of BR112016006151A2 publication Critical patent/BR112016006151A2/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring 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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

a invenção refere-se a compostos úteis como inibidores da via de sinalização do par-2. a invenção também se refere a composições farmaceuticamente aceitáveis compreendendo os compostos desta invenção; métodos de tratamento de várias doenças, distúrbios e condições usando os compostos desta invenção; processos para preparar os compostos desta invenção; intermediários para a preparação dos compostos desta invenção; e métodos de uso dos compostos em aplicações in vitro, tal como o estudo de gpcrs em fenômenos biológicos e patológicos; o estudo de vias de transdução de sinal intracelular mediados por tais gpcrs; e a avaliação comparativa dos novos inibidores da via de sinalização do par-2. os compostos desta invenção têm a fórmula i: i em que as variáveis são como definidas no presente docu-mento.
BR112016006151A 2013-09-25 2014-09-25 imidazopiridazinas úteis como inibidores da via de sinalização do par-2 BR112016006151A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361882173P 2013-09-25 2013-09-25
US201361901617P 2013-11-08 2013-11-08
PCT/US2014/057390 WO2015048245A1 (en) 2013-09-25 2014-09-25 Imidazopyridazines useful as inhibitors of the par-2 signaling pathway

Publications (1)

Publication Number Publication Date
BR112016006151A2 true BR112016006151A2 (pt) 2017-08-01

Family

ID=52293160

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112016006151A BR112016006151A2 (pt) 2013-09-25 2014-09-25 imidazopiridazinas úteis como inibidores da via de sinalização do par-2

Country Status (12)

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US (2) US10030024B2 (pt)
EP (1) EP3049418A1 (pt)
JP (1) JP2016531864A (pt)
KR (1) KR20160060120A (pt)
CN (1) CN105683192A (pt)
AU (2) AU2014326596B2 (pt)
BR (1) BR112016006151A2 (pt)
CA (1) CA2924690A1 (pt)
HK (2) HK1223096A1 (pt)
IL (1) IL244739A0 (pt)
TW (1) TW201602109A (pt)
WO (1) WO2015048245A1 (pt)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201602109A (zh) 2013-09-25 2016-01-16 維泰克斯製藥公司 作為ｐａｒ－２訊息傳遞路徑之抑制劑之咪唑并嗒
WO2017093180A1 (de) 2015-12-01 2017-06-08 Bayer Cropscience Aktiengesellschaft Kondensierte bicyclische heterocyclen-derivate als schädlingsbekämpfungsmittel
US10550089B2 (en) * 2016-05-12 2020-02-04 Heptares Therapeutics Limited Inhibitors of protease-activated receptor-2
AU2017268039A1 (en) * 2016-05-20 2018-12-06 Takeda Pharmaceutical Company Limited Treatment of pain
RU2019107162A (ru) 2016-08-15 2020-09-15 Байер Кропсайенс Акциенгезельшафт Конденсированные бициклические гетероциклические производные в качестве средств для борьбы с вредителями
US10227349B2 (en) * 2016-08-31 2019-03-12 Eisai R&D Management Co., Ltd. Pyrazolo[1,5-a]pyrimidine compound
WO2018057588A1 (en) * 2016-09-21 2018-03-29 Vertex Pharmaceuticals Incorporated Furo[3,2-b]pyridine compounds useful as inhibitors of the par-2 signaling pathway
US11690847B2 (en) 2016-11-30 2023-07-04 Case Western Reserve University Combinations of 15-PGDH inhibitors with corticosteroids and/or TNF inhibitors and uses thereof
WO2018145080A1 (en) 2017-02-06 2018-08-09 Case Western Reserve University Compositions and methods of modulating short-chain dehydrogenase activity
EP3692045A1 (de) 2017-10-04 2020-08-12 Bayer Aktiengesellschaft Heterocyclen-derivate als schädlingsbekämpfungsmittel
WO2019124567A1 (en) * 2017-12-20 2019-06-27 Takeda Pharmaceutical Company Limited Inhibitors of protease activated receptor-2
MX2020008110A (es) * 2018-02-26 2020-11-06 Eisai R&D Man Co Ltd Sal de compuesto de pirazolo[1,5-a]pirimidina y cristales de la misma.
BR112020017624A2 (pt) 2018-03-12 2020-12-22 Bayer Aktiengesellschaft Derivados heterocíclicos bicíclicos condensados como agentes de controle de pragas
WO2019201921A1 (de) 2018-04-20 2019-10-24 Bayer Aktiengesellschaft Heterocyclen-derivate als schädlingsbekämpfungsmittel
US20220193048A1 (en) 2019-04-05 2022-06-23 Universite De Bretagne Occidentale Protease-activated receptor-2 inhibitors for the treatment of sensory neuropathy induced by a marine neurotoxic poisoning
EP4255904A2 (en) 2020-12-03 2023-10-11 Domain Therapeutics Novel par-2 inhibitors
CN116981673A (zh) 2021-03-17 2023-10-31 豪夫迈·罗氏有限公司 新颖噻二唑并嘧啶酮衍生物
WO2023233033A1 (en) 2022-06-03 2023-12-07 Domain Therapeutics Novel par-2 inhibitors

Family Cites Families (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ514144A (en) * 1999-04-01 2001-09-28 Pfizer Prod Inc Aminopyrimidines as sorbitol dehydrogenase inhibitors
US7696168B2 (en) 2000-04-21 2010-04-13 Tufts Medical Center, Inc. G protein coupled receptor agonists and antagonists and methods of activating and inhibiting G protein coupled receptors using the same
EP2348047A1 (en) 2000-04-21 2011-07-27 New England Medical Center G protein coupled receptor (GPCR) agonists and antagonists and methods of activating and inhibiting GPCR using the same
CA2465326C (en) * 2001-11-01 2011-03-29 Icagen, Inc. Pyrazolopyrimidines for decreasing ion flow through a voltage-dependent sodium channel
JP2003286171A (ja) * 2002-03-28 2003-10-07 Sumitomo Pharmaceut Co Ltd Ｐａｒ阻害剤
GB0213286D0 (en) 2002-06-10 2002-07-24 Univ Edinburgh Par-2-Activating peptide derivative and pharmaceutical composition using the same
JP2004170323A (ja) * 2002-11-22 2004-06-17 Sumitomo Pharmaceut Co Ltd 皮膚疾患治療剤のスクリーニング方法
JPWO2005030773A1 (ja) * 2003-09-26 2006-12-07 大日本住友製薬株式会社 新規ピラゾロピリミジン誘導体
US8268789B2 (en) 2004-09-30 2012-09-18 Kowa Company, Ltd. PAR-2 antagonists
JP4927566B2 (ja) 2004-12-28 2012-05-09 興和株式会社 Ｐａｒ−２アゴニスト
US8133864B2 (en) 2005-03-29 2012-03-13 Kowa Company, Ltd. PAR-2 agonist
US20080318960A1 (en) 2005-05-26 2008-12-25 Ethan Burstein PAR2-modulating compounds and their use
US20070123508A1 (en) 2005-05-27 2007-05-31 Roger Olsson PAR2-modulating compounds and their use
WO2007076055A2 (en) 2005-12-22 2007-07-05 Entremed, Inc. Compositions and methods comprising proteinase activated receptor antagonists
US7888482B2 (en) 2006-02-10 2011-02-15 Amgen Inc. Antibodies that bind PAR-2
CL2008001887A1 (es) 2007-06-29 2008-10-03 Amgen Inc Proteinas de union a antigeno que se unen al receptor activado por proteasas 2 (par-2); acido nucleico que las codifica; vector y celula huesped; metodo de produccion; y composicion que las comprende.
WO2009059307A1 (en) 2007-11-01 2009-05-07 Washington University In St. Louis Compositions and methods for treating pruritus
AR070911A1 (es) 2008-03-19 2010-05-12 Regeneron Pharma Uso de antagonistas del receptor par2 activado con proteasa
US20100119506A1 (en) 2008-08-05 2010-05-13 Boehringer Ingelheim International Gmbh Effectors of PAR-2 Activation and Their Use in the Modulation of Inflammation
US8852569B2 (en) 2008-08-28 2014-10-07 The General Hospital Corporation Prevention and treatment of itch with cysteine protease inhibition
CA2758322C (en) 2009-04-10 2019-04-02 Tufts Medical Center, Inc. Par-1 activation by metalloproteinase-1 (mmp-1)
EP2427205A2 (en) 2009-05-04 2012-03-14 INSERM - Institut National de la Santé et de la Recherche Médicale Par2 agonists for use in the treatment or prevention of influenza virus type a infections
US20120107329A1 (en) 2009-06-10 2012-05-03 University Of Maryland, Baltimore EGFR and PAR2 Regulation of Intestinal Permeability
JO3246B1 (ar) 2009-09-09 2018-03-08 Regeneron Pharma اجسام مضادة بشرية ذات ألفة تفاعل عالية مع مستقبل 2 المفعل بالبروتين البشري
EP2335717A1 (en) 2009-11-16 2011-06-22 Institut National De La Recherche Agronomique PAR-1 antagonists for use in the treatment or prevention of influenza virus type a infections
JP5883863B2 (ja) 2010-07-28 2016-03-15 ザ ユニバーシティ オブ クィーンズランド プロテアーゼ活性化受容体の調節剤
JP5894161B2 (ja) 2010-08-25 2016-03-23 ネオファーム カンパニー， リミテッド 新規の複素環化合物及びこれを用いた炎症性疾患治療用組成物
FR2969657B1 (fr) 2010-12-22 2014-02-07 Fabre Pierre Dermo Cosmetique Nouvelle bacterie et extraits de ladite bacterie et leur utilisation en dermatologie
WO2012090207A2 (en) 2010-12-30 2012-07-05 Hadasit Medical Research Services & Development Limited Par1 and par2 c-tail peptides and peptide mimetics
GB201101517D0 (en) 2011-01-28 2011-03-16 Proximagen Ltd Receptor antagonists
WO2012139137A2 (en) 2011-04-08 2012-10-11 Tufts Medical Center, Inc. Pepducin design and use
EP2736523A4 (en) 2011-07-28 2015-10-28 Univ Queensland PROTEASE ACTIVATED RECEPTOR MODULATORS
KR101412119B1 (ko) 2011-09-29 2014-06-27 주식회사 펩트론 생리적 안정성을 증가시킨 ｐａｒ―2 활성화 펩타이드 및 이를 함유하는 약제학적 조성물
JP6148676B2 (ja) 2011-11-04 2017-06-14 リポテック， エセ．ア． 活性化受容体を阻害するペプチド、および化粧品組成物または薬学的組成物におけるそれらの使用
WO2013173676A1 (en) 2012-05-18 2013-11-21 Tufts Medical Center, Inc Polypeptide and lipophilic moiety conjugate compositions, formulations, and uses related thereto
GB201213700D0 (en) 2012-08-01 2012-09-12 Proximagen Ltd Receptor antagnists II
WO2014138727A1 (en) 2013-03-08 2014-09-12 Board Of Regents, The University Of Texas System Suppression of malignant mesothelioma by overexpression or stimulation of endothelial protein c receptors (epcr)
US20160095897A1 (en) 2013-04-22 2016-04-07 Institut National De La Recherche Agronomique Par-4 antagonists for use in the treatment or prevention of influenza virus type a infections
TW201602109A (zh) 2013-09-25 2016-01-16 維泰克斯製藥公司 作為ｐａｒ－２訊息傳遞路徑之抑制劑之咪唑并嗒
US9790506B2 (en) 2013-10-02 2017-10-17 The Regents Of The University Of California Diagnostic and screening methods for atopic dermatitis
EP3102947B1 (en) 2014-02-04 2018-11-14 CellTrend GmbH Diagnosis of cancer by detecting auto-antibodies against par1
JP5719050B2 (ja) 2014-02-28 2015-05-13 ザ プロクター アンド ギャンブルカンパニー 角化細胞のｐａｒ２活性化を阻害するための組成物及び方法
US20160000791A1 (en) 2014-07-07 2016-01-07 Mayo Foundation For Medical Education And Research Par1 modulation to alter myelination
WO2016005369A1 (en) 2014-07-08 2016-01-14 Celltrend Gmbh Par2 antibodies for diagnosis of graft intolerance of a liver transplant
WO2016138132A1 (en) 2015-02-25 2016-09-01 The Trustees Of Columbia University In The City Of New York Dipeptidyl peptidase-iv(dpp4) inhibitors, methods and compositions for suppressing adipose tissue inflammation

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AU2014326596A1 (en) 2016-04-07
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CA2924690A1 (en) 2015-04-02
US20160311825A1 (en) 2016-10-27
US10030024B2 (en) 2018-07-24
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HK1225386A1 (zh) 2017-09-08
AU2019201532A1 (en) 2019-03-28
US20190119282A1 (en) 2019-04-25
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WO2015048245A1 (en) 2015-04-02

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