CA2560649A1 - [4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-(4-bromo-3-methyl-5-propoxy-thiophen-2-yl)-methanone hydrochloride as an inhibitor of mast cell tryptase - Google Patents

[4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-(4-bromo-3-methyl-5-propoxy-thiophen-2-yl)-methanone hydrochloride as an inhibitor of mast cell tryptase Download PDF

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Publication number
CA2560649A1
CA2560649A1 CA002560649A CA2560649A CA2560649A1 CA 2560649 A1 CA2560649 A1 CA 2560649A1 CA 002560649 A CA002560649 A CA 002560649A CA 2560649 A CA2560649 A CA 2560649A CA 2560649 A1 CA2560649 A1 CA 2560649A1
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CA
Canada
Prior art keywords
compound
pharmaceutical composition
inflammatory
pharmaceutically acceptable
present
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
CA002560649A
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English (en)
French (fr)
Inventor
Zhongli Gao
Larry Davis
Julian Levell
Mark Czekaj
Adam W. Sledeski
El-Bdaoui Haddad
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Aventis Pharmaceuticals Inc
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of CA2560649A1 publication Critical patent/CA2560649A1/en
Abandoned legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Biomedical Technology (AREA)
  • Vascular Medicine (AREA)
  • Oncology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Communicable Diseases (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Virology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CA002560649A 2004-03-26 2005-03-24 [4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-(4-bromo-3-methyl-5-propoxy-thiophen-2-yl)-methanone hydrochloride as an inhibitor of mast cell tryptase Abandoned CA2560649A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US55692704P 2004-03-26 2004-03-26
US60/556,927 2004-03-26
PCT/US2005/009899 WO2005097780A1 (en) 2004-03-26 2005-03-24 [4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-(4-bromo-3-methyl-5-propoxy-thiophen-2-yl)-methanone hydrochloride as an inhibitor of mast cell tryptase

Publications (1)

Publication Number Publication Date
CA2560649A1 true CA2560649A1 (en) 2005-10-20

Family

ID=34964263

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002560649A Abandoned CA2560649A1 (en) 2004-03-26 2005-03-24 [4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-(4-bromo-3-methyl-5-propoxy-thiophen-2-yl)-methanone hydrochloride as an inhibitor of mast cell tryptase

Country Status (25)

Country Link
US (1) US20070142435A1 (enExample)
EP (1) EP1737848A1 (enExample)
JP (1) JP2007530580A (enExample)
KR (1) KR20060130682A (enExample)
CN (1) CN1956978A (enExample)
AR (1) AR048336A1 (enExample)
AU (1) AU2005230934A1 (enExample)
BR (1) BRPI0509245A (enExample)
CA (1) CA2560649A1 (enExample)
CR (1) CR8603A (enExample)
DO (1) DOP2005000039A (enExample)
EC (1) ECSP066878A (enExample)
IL (1) IL178031A0 (enExample)
MA (1) MA28547B1 (enExample)
MX (1) MXPA06010610A (enExample)
NO (1) NO20064811L (enExample)
PA (1) PA8627601A1 (enExample)
PE (1) PE20060084A1 (enExample)
RU (1) RU2330034C1 (enExample)
TN (1) TNSN06278A1 (enExample)
TW (1) TW200602035A (enExample)
UA (1) UA83738C2 (enExample)
UY (1) UY28821A1 (enExample)
WO (1) WO2005097780A1 (enExample)
ZA (1) ZA200607752B (enExample)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20071148A1 (es) * 2006-03-29 2007-12-10 Sanofi Aventis Mejoras en la preparacion de intermedios que conducen a hidrocloruro de [4-(5-aminometil-2-fluoro-fenil)-piperidin-1-il]-(4-bromo-3-metil-5-propoxi-tiofen-2-il)-metanona
AR065616A1 (es) * 2007-03-07 2009-06-17 Sanofi Aventis Sintesis regioselectiva de ullmann de acido 4- bromo-3- metil-5- propoxi- tiofeno-2- carboxilico
WO2008115912A1 (en) * 2007-03-21 2008-09-25 Sanofi-Aventis Regio-specific synthesis of 4-bromo-3-methyl-5-propoxy-thiophene-2-carboxylic acid
AR065858A1 (es) * 2007-03-29 2009-07-08 Sanofi Aventis Metodo para preparar el inhibidor de triptasa [ 4-(5-aminoetil-2-fluoro-fenil)-piperidin-1-il]-(4-bromo-3-metil-5-propoxi-tiofen-2-il)-metanona.
WO2008121669A1 (en) * 2007-03-29 2008-10-09 Sanofi-Aventis 4-bromo-3-methyl-5-propoxythiophene-2-carboxylic acid 2,5-dioxo-pyrrolidin-1-yl ester, its regio-specific synthesis and intermediate thereto
ES2469824T3 (es) 2007-11-21 2014-06-20 Janssen Pharmaceutica N.V. Espiropiperidinas para su uso como inhibidores de la triptasa
WO2009094641A2 (en) * 2008-01-24 2009-07-30 Dor Biopharma, Inc. Topically active steroids for use in interstitial pulmonary fibrosis
WO2010022196A2 (en) * 2008-08-22 2010-02-25 Sanofi-Aventis [4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-[7-fluoro-1-(2-methoxy-ethyl)-4-trifluoromethoxy-1h-indol-3-yl]-methanone as an inhibitor of mast cell tryptase
TW201034675A (en) 2008-12-18 2010-10-01 Sanofi Aventis Method for treating macular degeneration
FR2955324A1 (fr) * 2010-01-15 2011-07-22 Sanofi Aventis [4-(5-aminomethyl-phenyl)-piperidin-1-yl]-1h-indol-3-yl]-methanones disubstituees
CN102574792B (zh) 2009-09-24 2014-07-09 赛诺菲-安万特美国有限责任公司 (4-氟-3-(哌啶-4-基)-苯甲基)-氨基甲酸叔丁酯的合成及其中间体
AU2010333779A1 (en) * 2009-12-23 2012-07-12 Sanofi Indolyl-piperidinyl benzylamines as beta-tryptase inhibitors
JP2013515724A (ja) * 2009-12-23 2013-05-09 サノフイ ベータ−トリプターゼ阻害剤としてのトロピノンベンジルアミン類
EP2515851A1 (en) * 2009-12-23 2012-10-31 Sanofi Treatment for inflammatory bowel disease
BR112012020965A2 (pt) * 2010-02-24 2016-05-03 Sanofi Sa tratamento de condições alérgicas dermatológicas
MX360706B (es) 2011-10-07 2018-11-14 Takeda Pharmaceuticals Co Compuestos de 1-arilcarbonil-4-oxi-piperidina utiles para el tratamiento de enfermedades neurodegenerativas.
UA126574C2 (uk) * 2017-02-10 2022-11-02 Дженентек, Інк. Антитіло проти триптази, його композиція та застосування

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0012362D0 (en) * 2000-05-22 2000-07-12 Aventis Pharma Ltd Chemical compounds
IL152830A0 (en) * 2000-05-22 2003-06-24 Aventis Pharma Inc Arylmethylamine derivatives for use as tryptase inhibitors

Also Published As

Publication number Publication date
AU2005230934A1 (en) 2005-10-20
CR8603A (es) 2007-06-08
TW200602035A (en) 2006-01-16
US20070142435A1 (en) 2007-06-21
RU2006137717A (ru) 2008-05-10
IL178031A0 (en) 2006-12-31
JP2007530580A (ja) 2007-11-01
ZA200607752B (en) 2008-05-28
RU2330034C1 (ru) 2008-07-27
UA83738C2 (en) 2008-08-11
CN1956978A (zh) 2007-05-02
KR20060130682A (ko) 2006-12-19
BRPI0509245A (pt) 2007-09-11
PE20060084A1 (es) 2006-03-09
UY28821A1 (es) 2005-10-31
TNSN06278A1 (en) 2007-12-03
NO20064811L (no) 2006-10-23
PA8627601A1 (es) 2006-01-23
WO2005097780A1 (en) 2005-10-20
MA28547B1 (fr) 2007-04-03
MXPA06010610A (es) 2006-12-15
DOP2005000039A (es) 2005-10-31
EP1737848A1 (en) 2007-01-03
ECSP066878A (es) 2006-11-24
AR048336A1 (es) 2006-04-19

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Legal Events

Date Code Title Description
EEER Examination request
FZDE Discontinued