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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    • 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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    • 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
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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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    • C07D209/30—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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    • C07D213/04—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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  • Neurosurgery (AREA)
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  • Otolaryngology (AREA)
  • Epidemiology (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyridine 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 (36)

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US (2) US8217178B2 (es)
EP (1) EP2367812B1 (es)
JP (1) JP5656834B2 (es)
KR (1) KR101630217B1 (es)
CN (2) CN103508936A (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)
ES (1) ES2556764T3 (es)
HR (1) HRP20151338T1 (es)
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MA (1) MA32639B1 (es)
MX (1) MX2011001135A (es)
MY (1) MY150599A (es)
NI (1) NI201100024A (es)
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)
ZA (1) ZA201100597B (es)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0916920A2 (pt) 2008-08-22 2015-11-24 Sanofi Aventis 4-(5-aminometil-2-fluoro-fenil)-piperidin-1-il]-[7-fluoro-1-(2-metóxi-etil)-4-trifluorometóxi-1h-indol-3-il]-metanona como inibidor de triptase de mastócito, seu uso e método de preparação, bem como forma cristalina
FR2955324A1 (fr) * 2010-01-15 2011-07-22 Sanofi Aventis [4-(5-aminomethyl-phenyl)-piperidin-1-yl]-1h-indol-3-yl]-methanones disubstituees
EP2516428A1 (en) * 2009-12-23 2012-10-31 Sanofi Tropinone benzylamines as beta-tryptase inhibitors
KR20120107999A (ko) * 2009-12-23 2012-10-04 사노피 염증성 장 질환의 치료
AU2010333779A1 (en) * 2009-12-23 2012-07-12 Sanofi Indolyl-piperidinyl benzylamines as beta-tryptase inhibitors
RU2012131146A (ru) 2009-12-23 2014-02-10 Санофи Пролекарства [4[4-(5-аминометил-2-фторфенил)пиперидин-1-ил]-(1н-пирролпиридинил)метанонов и их синтез
AR080255A1 (es) * 2010-02-24 2012-03-21 Sanofi Aventis Tratamiento de afecciones alergicas dermatologicas. composicion farmaceutica
EP2397074B1 (en) * 2010-06-19 2012-10-24 M Stenqvist AB A system and computer readable medium for determination of transpulmonary pressure in a patient connected to a breathing apparatus
CA2851087C (en) 2011-10-07 2019-09-24 Takeda Pharmaceutical Company Limited 1-arylcarbonyl-4-oxy-piperidine compounds useful for the treatment of neurodegenerative diseases
DE102020120900A1 (de) * 2020-08-07 2022-02-10 Drägerwerk AG & Co. KGaA Vorrichtung und Verfahren zur Messung der Lungen-Compliance
CA3206106A1 (en) 2021-02-10 2022-08-18 Bhaskar Chaudhuri Methods for ophthalmic delivery of roflumilast
US12263160B2 (en) 2021-09-22 2025-04-01 Iolyx Therapeutics, Inc. Methods of treating ocular inflammatory diseases

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5087240A (en) 1983-08-18 1992-02-11 Drug Delivery Systems Inc. Transdermal drug patch with conductive fibers
US4921475A (en) 1983-08-18 1990-05-01 Drug Delivery Systems Inc. Transdermal drug patch with microtubes
US4879119A (en) 1984-02-21 1989-11-07 Yamanouchi Pharmaceutical Co., Ltd. Patch
WO1988001213A1 (en) 1986-08-18 1988-02-25 Clinical Technologies Associates, Inc. Delivery systems for pharmacological agents
US5163899A (en) 1987-03-20 1992-11-17 Drug Delivery Systems Inc. Transdermal drug delivery system
US5312325A (en) 1987-05-28 1994-05-17 Drug Delivery Systems Inc Pulsating transdermal drug delivery system
GB8804164D0 (en) 1988-02-23 1988-03-23 Tucker J M Bandage for administering physiologically active compound
US5008110A (en) 1988-11-10 1991-04-16 The Procter & Gamble Company Storage-stable transdermal patch
US5088977A (en) 1988-12-21 1992-02-18 Drug Delivery Systems Inc. Electrical transdermal drug applicator with counteractor and method of drug delivery
US5013556A (en) 1989-10-20 1991-05-07 Liposome Technology, Inc. Liposomes with enhanced circulation time
ATE107176T1 (de) 1989-12-04 1994-07-15 Searle & Co System zur transdermalen albuterol applikation.
NZ241954A (en) 1991-03-15 1994-01-26 Amgen Inc Compositions of g-csf for pulmonary administration.
US5352456A (en) 1991-10-10 1994-10-04 Cygnus Therapeutic Systems Device for administering drug transdermally which provides an initial pulse of drug
CA2123809A1 (en) 1991-12-18 1993-06-24 Debra L. Wilfong Multilayered barrier structures
US5451569A (en) 1994-04-19 1995-09-19 Hong Kong University Of Science And Technology R & D Corporation Limited Pulmonary drug delivery system
RU2278115C2 (ru) * 1999-05-21 2006-06-20 Сайос Инк. ПРОИЗВОДНЫЕ ИНДОЛЬНОГО РЯДА В КАЧЕСТВЕ ИНГИБИТОРОВ p38 КИНАЗЫ
OA12274A (en) 2000-05-22 2006-05-09 Aventis Pharma Inc Arylmethylamine derivatives for use as tryptase inhibitors.
GB0012362D0 (en) * 2000-05-22 2000-07-12 Aventis Pharma Ltd Chemical compounds
EP1571150A1 (en) * 2004-03-02 2005-09-07 Aventis Pharma Deutschland GmbH Process for the preparation of tryptase inhibitors
DOP2005000039A (es) * 2004-03-26 2005-10-31 Aventis Pharma Inc Hidrocloruro de [4-(5-aminometil-2-fluoro-fenil)- piperidin-1-il]-(4-bomo-3-metil-5-propoxi-tiofen-2-il)-metanona como un inhibidor de la triptasa de mastocitos
AR065859A1 (es) * 2007-03-29 2009-07-08 Sanofi Aventis Ester de 2,5-dioxo-pirrolidin-1-ilo de acido 4-bromo-3-metil-5-propoxitiofen-2- carboxilico ,su sintesis regioespecifica y un intermedio del mismo
WO2008121666A1 (en) * 2007-03-29 2008-10-09 Sanofi-Aventis Use of 4-bromo-3-methyl-5-propoxythiophene-2-carboxylic acid 2,5-dioxo-pyrrolidin-1-yl ester for preparing the tryptase inhibitor [4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-(4-bromo-3-methyl-5-propoxy-thiophen-2-yl)-methanone
BRPI0916920A2 (pt) 2008-08-22 2015-11-24 Sanofi Aventis 4-(5-aminometil-2-fluoro-fenil)-piperidin-1-il]-[7-fluoro-1-(2-metóxi-etil)-4-trifluorometóxi-1h-indol-3-il]-metanona como inibidor de triptase de mastócito, seu uso e método de preparação, bem como forma cristalina

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