CY1117261T1 - [4-(5-αμινομεθυλο-2-φθορο-φαινυλο)-πιπεριδιν-1-υλο]-[7-φθορο-1-(2-μεθοξυ-αιθυλο)-4τριφθορο μεθοξυ-1η-ινδολ-3-υλο]-μεθανονη ως αναστολεας τρυπτασης maστοκυτταρων - Google Patents

[4-(5-αμινομεθυλο-2-φθορο-φαινυλο)-πιπεριδιν-1-υλο]-[7-φθορο-1-(2-μεθοξυ-αιθυλο)-4τριφθορο μεθοξυ-1η-ινδολ-3-υλο]-μεθανονη ως αναστολεας τρυπτασης maστοκυτταρων

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Publication number
CY1117261T1
CY1117261T1 CY20151101141T CY151101141T CY1117261T1 CY 1117261 T1 CY1117261 T1 CY 1117261T1 CY 20151101141 T CY20151101141 T CY 20151101141T CY 151101141 T CY151101141 T CY 151101141T CY 1117261 T1 CY1117261 T1 CY 1117261T1
Authority
CY
Cyprus
Prior art keywords
fluoro
methoxy
compound
piperidin
aminomethyl
Prior art date
Application number
CY20151101141T
Other languages
Greek (el)
English (en)
Inventor
Yong Mi Choi-Sledeski
Nakyen Choy
Gregory Bernard Poli
John J Shay Jr
Patrick Wai-Kwok Shum
Adam W Sledeski
Original Assignee
Sanofi
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 filed Critical Sanofi
Publication of CY1117261T1 publication Critical patent/CY1117261T1/el

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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
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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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    • A61P27/14—Decongestants or antiallergics
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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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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C07—ORGANIC CHEMISTRY
    • 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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    • C07D209/30—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
    • C07D213/36—Radicals substituted by singly-bound nitrogen 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
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40—Acylated substituent nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • 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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  • Orthopedic Medicine & Surgery (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
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  • Ophthalmology & Optometry (AREA)
  • Biomedical Technology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Virology (AREA)
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  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Cardiology (AREA)
  • Otolaryngology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyridine Compounds (AREA)
CY20151101141T 2008-08-22 2015-12-15 [4-(5-αμινομεθυλο-2-φθορο-φαινυλο)-πιπεριδιν-1-υλο]-[7-φθορο-1-(2-μεθοξυ-αιθυλο)-4τριφθορο μεθοξυ-1η-ινδολ-3-υλο]-μεθανονη ως αναστολεας τρυπτασης maστοκυτταρων CY1117261T1 (el)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US9101808P 2008-08-22 2008-08-22
US9101108P 2008-08-22 2008-08-22
EP09791693.6A EP2367812B1 (en) 2008-08-22 2009-08-20 [4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-[7-fluoro-1-(2-methoxy-ethyl)-4trifluoromethoxy-1h-indol-3-yl]methanone as an inhibitor of mast cell tryptase

Publications (1)

Publication Number Publication Date
CY1117261T1 true CY1117261T1 (el) 2017-04-26

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CY20151101141T CY1117261T1 (el) 2008-08-22 2015-12-15 [4-(5-αμινομεθυλο-2-φθορο-φαινυλο)-πιπεριδιν-1-υλο]-[7-φθορο-1-(2-μεθοξυ-αιθυλο)-4τριφθορο μεθοξυ-1η-ινδολ-3-υλο]-μεθανονη ως αναστολεας τρυπτασης maστοκυτταρων

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US (2) US8217178B2 (enExample)
EP (1) EP2367812B1 (enExample)
JP (1) JP5656834B2 (enExample)
KR (1) KR101630217B1 (enExample)
CN (2) CN103508936A (enExample)
AR (1) AR073117A1 (enExample)
AU (1) AU2009282884B8 (enExample)
BR (1) BRPI0916920A2 (enExample)
CA (1) CA2734877C (enExample)
CL (1) CL2009001759A1 (enExample)
CO (1) CO6341624A2 (enExample)
CR (1) CR20110093A (enExample)
CY (1) CY1117261T1 (enExample)
DK (1) DK2367812T3 (enExample)
DO (1) DOP2011000055A (enExample)
EC (1) ECSP11010841A (enExample)
ES (1) ES2556764T3 (enExample)
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MA (1) MA32639B1 (enExample)
MX (1) MX2011001135A (enExample)
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PT (1) PT2367812E (enExample)
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RU (1) RU2509766C2 (enExample)
SI (1) SI2367812T1 (enExample)
TW (1) TWI473613B (enExample)
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CN103508936A (zh) 2008-08-22 2014-01-15 赛诺菲-安万特 用于制备吲哚苄胺化合物的中间体
FR2955324A1 (fr) * 2010-01-15 2011-07-22 Sanofi Aventis [4-(5-aminomethyl-phenyl)-piperidin-1-yl]-1h-indol-3-yl]-methanones disubstituees
WO2011087652A1 (en) * 2009-12-23 2011-07-21 Sanofi Tropinone benzylamines as beta-tryptase inhibitors
AU2010333772B2 (en) * 2009-12-23 2016-07-14 Sanofi Prodrugs of [4[4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-(1H-pyrrolo-pyridin-yl)-methanones and synthesis thereof
WO2011079102A1 (en) * 2009-12-23 2011-06-30 Sanofi Indolyl-piperidinyl benzylamines as beta-tryptase inhibitors
JP2013515723A (ja) * 2009-12-23 2013-05-09 サノフイ 炎症性腸疾患の処置
JP2013520506A (ja) * 2010-02-24 2013-06-06 サノフイ 皮膚科学的なアレルギー状態の治療
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
US8648079B2 (en) 2011-10-07 2014-02-11 Takeda Pharmaceutical Company Limited Heterocyclic compounds
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US12102622B2 (en) 2021-02-10 2024-10-01 Iolyx Therapeutics, Inc. Methods for ophthalmic delivery of roflumilast
US12263160B2 (en) 2021-09-22 2025-04-01 Iolyx Therapeutics, Inc. Methods of treating ocular inflammatory diseases

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