CL2009001759A1 - Compuesto (4-(5-aminometil-2-fluorofenil)piperidin-1-il)(7-fluoro-1(2-metoxietil)-4-trifluorometoxi-1h-indol-3-il)metanona; forma cristalina a de la sal benzoato; compuestos intermediarios; composicion farmaceutica; y uso en el tratamiento de enfermedades inflamatorias, tales como epoc, alergia,dermatitis atopica, entre otras. - Google Patents

Compuesto (4-(5-aminometil-2-fluorofenil)piperidin-1-il)(7-fluoro-1(2-metoxietil)-4-trifluorometoxi-1h-indol-3-il)metanona; forma cristalina a de la sal benzoato; compuestos intermediarios; composicion farmaceutica; y uso en el tratamiento de enfermedades inflamatorias, tales como epoc, alergia,dermatitis atopica, entre otras.

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Publication number
CL2009001759A1
CL2009001759A1 CL2009001759A CL2009001759A CL2009001759A1 CL 2009001759 A1 CL2009001759 A1 CL 2009001759A1 CL 2009001759 A CL2009001759 A CL 2009001759A CL 2009001759 A CL2009001759 A CL 2009001759A CL 2009001759 A1 CL2009001759 A1 CL 2009001759A1
Authority
CL
Chile
Prior art keywords
compound
fluoro
pharmaceutical composition
indol
aminomethyl
Prior art date
Application number
CL2009001759A
Other languages
English (en)
Inventor
Yong-Mi Choi-Sledeski
Choy Nakyen
Gregory Bernard Poli
Jr John J Shay
Patrick Wai-Kwok Shum
Adam W Sledeski
Original Assignee
Sanofi Aventis
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 Sanofi Aventis filed Critical Sanofi Aventis
Publication of CL2009001759A1 publication Critical patent/CL2009001759A1/es

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
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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
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    • 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
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A—HUMAN NECESSITIES
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    • 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]
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/26—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring
    • C07C271/28—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring to a carbon atom of a non-condensed six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
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    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
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    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
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    • C07F7/10—Compounds having one or more C—Si linkages containing nitrogen having a Si-N linkage

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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Physical Education & Sports Medicine (AREA)
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  • Dermatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
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  • Virology (AREA)
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  • Gastroenterology & Hepatology (AREA)
  • Otolaryngology (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Indole Compounds (AREA)

Abstract

LA PRESENTE INVENCIÓN SE REFIERE AL COMPUESTO (4-(S-AMINOMETIL-2-FLUOROFENILLPIPERIDIN-1-I1L(7-FLUORO-1( 2-METOXIETIL -4-(TRIFLUOROMETOXI)-1 H-INDOL-3-I1LMETANONA ÚTIL COMO UN INHIBIDOR DE TRIPTASA. ADEMÁS, LA PRESENTE INVENCIÓN SE REFIERE AL USO DEL COMPUESTO PARA TRATAR A UN PACIENTE QUE PADECE, O ES PROPENSO A<br /> PADECER, UNA AFECCIÓN FISIOLÓGICA QUE NECESITA MEJORARSE POR LA INHIBICIÓN DE TRIPTASA, QUE COMPRENDE ADMINISTRAR AL PACIENTE UNA CANTIDAD TERAPÉUTICAMENTE EFICAZ DEL COMPUESTO. ADEMÁS, LA PRESENTE INVENCIÓN SE REFIERE A UNA COMPOSICIÓN FARMACÉUTICA QUE COMPRENDE UNA CANTIDAD FARMACÉUTICAMENTE EFICAZ DEL COMPUESTO DE FÓRMULA 1, Y UN VEHICULO FARMACÉUTICAMENTE ACEPTABLE, A LOS COMPUESTOS INTERMEDIARIOS, Y A LA PREPARACIÓN DEL COMPUESTO INTERMEDIARIO HIDROCLORURO DE 2,2,2TRIFLUORO- N-(FL UORO-3-PIRIDIN-4-IL-BENCII)-ACETAMIDA.
CL2009001759A 2008-08-22 2009-08-21 Compuesto (4-(5-aminometil-2-fluorofenil)piperidin-1-il)(7-fluoro-1(2-metoxietil)-4-trifluorometoxi-1h-indol-3-il)metanona; forma cristalina a de la sal benzoato; compuestos intermediarios; composicion farmaceutica; y uso en el tratamiento de enfermedades inflamatorias, tales como epoc, alergia,dermatitis atopica, entre otras. CL2009001759A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US9101108P 2008-08-22 2008-08-22
US9101808P 2008-08-22 2008-08-22

Publications (1)

Publication Number Publication Date
CL2009001759A1 true CL2009001759A1 (es) 2010-07-23

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CL2009001759A CL2009001759A1 (es) 2008-08-22 2009-08-21 Compuesto (4-(5-aminometil-2-fluorofenil)piperidin-1-il)(7-fluoro-1(2-metoxietil)-4-trifluorometoxi-1h-indol-3-il)metanona; forma cristalina a de la sal benzoato; compuestos intermediarios; composicion farmaceutica; y uso en el tratamiento de enfermedades inflamatorias, tales como epoc, alergia,dermatitis atopica, entre otras.

Country Status (37)

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US (2) US8217178B2 (es)
EP (1) EP2367812B1 (es)
JP (1) JP5656834B2 (es)
KR (1) KR101630217B1 (es)
CN (2) CN102149705B (es)
AR (1) AR073117A1 (es)
AU (1) AU2009282884B8 (es)
BR (1) BRPI0916920A2 (es)
CA (1) CA2734877C (es)
CL (1) CL2009001759A1 (es)
CO (1) CO6341624A2 (es)
CR (1) CR20110093A (es)
CY (1) CY1117261T1 (es)
DK (1) DK2367812T3 (es)
DO (1) DOP2011000055A (es)
EC (1) ECSP11010841A (es)
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MX (1) MX2011001135A (es)
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NZ (1) NZ591234A (es)
PE (1) PE20100235A1 (es)
PL (1) PL2367812T3 (es)
PT (1) PT2367812E (es)
RS (1) RS54413B1 (es)
RU (1) RU2509766C2 (es)
SI (1) SI2367812T1 (es)
TW (1) TWI473613B (es)
UA (1) UA104148C2 (es)
UY (1) UY32069A (es)
WO (1) WO2010022196A2 (es)
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Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS54413B1 (en) 2008-08-22 2016-04-28 Sanofi [4- (5-AMINOMETHYL-2-FLUORO-PHENYL) -PIPERIDIN-1-IL] - [7-FLUORO-1- (2-METHOXY-ETHYL) -4TRIFLUOROMETOXY-1H-INDOL-3-IL] METHANONE AS INHIBITOR MASTOCYT TRIPTASES
FR2955324A1 (fr) * 2010-01-15 2011-07-22 Sanofi Aventis [4-(5-aminomethyl-phenyl)-piperidin-1-yl]-1h-indol-3-yl]-methanones disubstituees
SG181592A1 (en) * 2009-12-23 2012-07-30 Sanofi Sa Treatment for inflammatory bowel disease
AR079662A1 (es) * 2009-12-23 2012-02-08 Sanofi Aventis Indolil-piperidinil bencilaminas como inhibidores de beta-triptasa
WO2011087652A1 (en) * 2009-12-23 2011-07-21 Sanofi Tropinone benzylamines as beta-tryptase inhibitors
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