ECSP099065A - Derivados de cinamoil-piperazina y su utilización como antagonistas de par-1 - Google Patents

Derivados de cinamoil-piperazina y su utilización como antagonistas de par-1

Info

Publication number
ECSP099065A
ECSP099065A EC2009009065A ECSP099065A ECSP099065A EC SP099065 A ECSP099065 A EC SP099065A EC 2009009065 A EC2009009065 A EC 2009009065A EC SP099065 A ECSP099065 A EC SP099065A EC SP099065 A ECSP099065 A EC SP099065A
Authority
EC
Ecuador
Prior art keywords
par
cinamoil
piperazina
antagonist
derivatives
Prior art date
Application number
EC2009009065A
Other languages
English (en)
Inventor
Michel Perez
Marie Lamothe
Grand Bruno Le
Robert Letienne
Original Assignee
Pf Medicament
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 Pf Medicament filed Critical Pf Medicament
Publication of ECSP099065A publication Critical patent/ECSP099065A/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • 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
    • 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
    • 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
    • A61P35/00—Antineoplastic 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
    • 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
    • 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
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61P9/06—Antiarrhythmics
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

La presente invención se refiere a compuestos que responden a la fórmula general (I): en la que:R1 representa halógeno, CN, NO2; R2 representa hidrógeno, halógeno; n representa 1 ó 2; R3 representa fenilo sustituido con uno o varios halógenos o alquilos C1-C6; o un ciclohexilo; así como a sus sales y solvatos terapéuticamente aceptables. Estos compuestos son útiles como antagonistas del receptor-1 activado por proteasa (PAR-1), particularmente en el tratamiento de trombosis
EC2009009065A 2006-06-19 2009-01-13 Derivados de cinamoil-piperazina y su utilización como antagonistas de par-1 ECSP099065A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
FR0605419A FR2902426B1 (fr) 2006-06-19 2006-06-19 Derives de cinnamoyl-piperazine

Publications (1)

Publication Number Publication Date
ECSP099065A true ECSP099065A (es) 2009-02-27

Family

ID=37846050

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2009009065A ECSP099065A (es) 2006-06-19 2009-01-13 Derivados de cinamoil-piperazina y su utilización como antagonistas de par-1

Country Status (31)

Country Link
US (2) US8217046B2 (es)
EP (1) EP2041104B1 (es)
JP (1) JP5356222B2 (es)
KR (1) KR101468752B1 (es)
CN (1) CN101472907B (es)
AR (1) AR061520A1 (es)
AT (1) ATE478059T1 (es)
AU (1) AU2007263051B2 (es)
BR (1) BRPI0713132B8 (es)
CA (1) CA2655527C (es)
CR (1) CR10509A (es)
DE (1) DE602007008572D1 (es)
EC (1) ECSP099065A (es)
ES (1) ES2349324T3 (es)
FR (1) FR2902426B1 (es)
GE (1) GEP20115201B (es)
IL (1) IL195972A (es)
MA (1) MA30756B1 (es)
MX (1) MX2008016447A (es)
MY (1) MY144461A (es)
NO (1) NO341389B1 (es)
NZ (1) NZ573764A (es)
PL (1) PL2041104T3 (es)
PT (1) PT2041104E (es)
RU (1) RU2440997C2 (es)
SA (1) SA07280330B1 (es)
TN (1) TNSN08522A1 (es)
TW (1) TWI404710B (es)
UA (1) UA96947C2 (es)
WO (1) WO2007147824A1 (es)
ZA (1) ZA200900303B (es)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR3014693B1 (fr) 2013-12-16 2016-01-08 Pf Medicament Utilisation de la 3-(2-chloro-phenyl)-1-[4-(4-fluoro-benzyl)-piperazin-1-yl]-propenone pour la prevention et/ou le traitement des pathologies fonctionnelles pelvi-perineales
EP3143036B1 (en) 2014-05-11 2023-08-02 Tel Hashomer Medical Research Infrastructure and Services Ltd. Par-1 based therapeutic conjugates and uses thereof
WO2016066789A1 (fr) * 2014-10-31 2016-05-06 Pierre Fabre Medicament Utilisation d'antagonistes par-1 pour la prevention et/ou le traitement des pathologies fonctionnelles pelvi-perineales
CN104529860B (zh) * 2015-01-13 2016-06-01 佛山市赛维斯医药科技有限公司 一种含硝基苯和二烯氟代金刚烷结构的化合物及制备方法
CN104496924B (zh) * 2015-01-13 2016-04-13 佛山市赛维斯医药科技有限公司 卤苯二烯四氮唑类化合物、其制备方法和用途
CN104496879A (zh) * 2015-01-13 2015-04-08 佛山市赛维斯医药科技有限公司 一种含腈基苯和二烯氟代金刚烷结构的化合物和用途
CN104496922B (zh) * 2015-01-13 2016-04-06 佛山市赛维斯医药科技有限公司 腈基苯二烯四氮唑类化合物、其制备方法和用途
CN105949116A (zh) * 2016-06-08 2016-09-21 青岛理工大学 酰基哌嗪类化合物及其制备方法和用途
EP3278802A1 (en) 2016-08-04 2018-02-07 Metabolys New treatment for the non alcoholic steatohepatitis and fibrosis
RU2662308C1 (ru) * 2017-12-25 2018-07-25 Феркат Адельзянович Халиуллин Средство для лечения и профилактики тромбоза
IL278311B2 (en) 2018-05-02 2024-02-01 Tel Hashomer Medical Res Infrastructure & Services Ltd Preparations and methods for the treatment of glioblastoma
FR3090317B1 (fr) * 2018-12-19 2021-05-07 Cvasthera Utilisation d’un antagoniste de par-1 pour le traitement d’une maladie inflammatoire chronique intestinale
KR102791326B1 (ko) * 2021-09-29 2025-04-04 주성수 피페론구민계 화합물을 유효성분으로 포함하는 혈관질환 예방 또는 치료용 약학적 조성물

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS61106564A (ja) * 1984-10-30 1986-05-24 Terumo Corp 不飽和脂肪酸アミド誘導体およびこれを含有する血小板凝集抑制剤
JPS6219577A (ja) * 1985-07-16 1987-01-28 Kanebo Ltd 新規なベンジルピペラジン誘導体および該化合物を有効成分とする医薬組成物
SE9201956D0 (sv) * 1992-06-25 1992-06-25 Kabi Pharmacia Ab Novel nicotinicacid esters
US6207665B1 (en) * 1997-06-12 2001-03-27 Schering Aktiengesellschaft Piperazine derivatives and their use as anti-inflammatory agents
WO2002076965A1 (en) * 2001-03-23 2002-10-03 John Matsoukas Non peptide mimetics based on the active sequence s42fllr46 of the thrombin receptor for the treatment of thrombosis and cancer
GB0224917D0 (en) * 2002-10-25 2002-12-04 Novartis Ag Organic compounds
EP1562925B1 (en) * 2002-11-07 2007-01-03 Merck & Co., Inc. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
CN1775762A (zh) * 2005-12-06 2006-05-24 山东大学 川芎嗪酰基哌嗪衍生物、制备方法和药物组合物与应用
FR2917622B1 (fr) * 2007-06-19 2009-10-23 Pierre Fabre Medicament Sa Utilisation d'un antagoniste par1 dans le traitement de la fibrillation atriale.

Also Published As

Publication number Publication date
RU2440997C2 (ru) 2012-01-27
US20090176803A1 (en) 2009-07-09
TWI404710B (zh) 2013-08-11
PL2041104T3 (pl) 2011-01-31
KR101468752B1 (ko) 2014-12-03
ES2349324T3 (es) 2010-12-30
ATE478059T1 (de) 2010-09-15
JP2009541260A (ja) 2009-11-26
IL195972A0 (en) 2009-09-01
EP2041104A1 (en) 2009-04-01
NO341389B1 (no) 2017-10-30
CA2655527C (en) 2014-12-23
US20120232097A1 (en) 2012-09-13
AU2007263051A1 (en) 2007-12-27
CR10509A (es) 2009-02-05
NO20090270L (no) 2009-03-03
PT2041104E (pt) 2010-11-08
TW200808742A (en) 2008-02-16
BRPI0713132A2 (pt) 2012-04-17
BRPI0713132B1 (pt) 2020-10-20
BRPI0713132B8 (pt) 2021-05-25
CN101472907B (zh) 2012-08-29
JP5356222B2 (ja) 2013-12-04
DE602007008572D1 (de) 2010-09-30
TNSN08522A1 (en) 2010-04-14
MY144461A (en) 2011-09-30
NZ573764A (en) 2011-01-28
EP2041104B1 (en) 2010-08-18
IL195972A (en) 2014-05-28
FR2902426A1 (fr) 2007-12-21
ZA200900303B (en) 2009-12-30
MA30756B1 (fr) 2009-10-01
US8513258B2 (en) 2013-08-20
HK1127353A1 (en) 2009-09-25
CN101472907A (zh) 2009-07-01
US8217046B2 (en) 2012-07-10
GEP20115201B (en) 2011-04-11
MX2008016447A (es) 2009-01-22
WO2007147824A1 (en) 2007-12-27
SA07280330B1 (ar) 2010-10-23
AR061520A1 (es) 2008-09-03
KR20090031572A (ko) 2009-03-26
UA96947C2 (ru) 2011-12-26
FR2902426B1 (fr) 2008-09-05
AU2007263051B2 (en) 2011-10-20
CA2655527A1 (en) 2007-12-27
RU2008152247A (ru) 2010-07-27

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