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

Info

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
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

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • 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
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • A61P11/08—Bronchodilators
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/14—Decongestants or antiallergics
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero 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
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12—Radicals substituted by oxygen atoms
    • 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
    • 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
    • C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—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
    • 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
    • C07D213/38—Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—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
    • 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
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Communicable Diseases (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Otolaryngology (AREA)
  • Virology (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Indole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Η παρούσα εφεύρεση εστιάζεται σε ένωση τύπου ινδολο βενζυλαμίνης χρήσιμη ως αναστολέας ενζύμου τρυπτάσης. Επιπλέον, η παρούσα εφεύρεση εστιάζεται στη χρήση της ένωσης για τη θεραπεία ασθενούς πάσχοντος από, ή υποκείμενου σε, φυσιολογική κατάσταση που έχει ανάγκη βελτίωσης μέσω αναστολής ενζύμου τρυπτάσης, που περιλαμβάνει χορήγηση στον ασθενή θεραπευτικώς αποτελεσματικής ποσότητας της ένωσης. Περαιτέρω, η παρούσα εφεύρεση εστιάζεται σε φαρμακευτική σύνθεση που περιλαμβάνει φαρμακευτικώς αποτελεσματική ποσότητα της ένωσης του τύπου I, και φαρμακευτικά αποδεκτό φορέα.
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

Family

ID=41198646

Family Applications (1)

Application Number Title Priority Date Filing Date
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

Country Status (37)

Country Link
US (2) US8217178B2 (el)
EP (1) EP2367812B1 (el)
JP (1) JP5656834B2 (el)
KR (1) KR101630217B1 (el)
CN (2) CN103508936A (el)
AR (1) AR073117A1 (el)
AU (1) AU2009282884B8 (el)
BR (1) BRPI0916920A2 (el)
CA (1) CA2734877C (el)
CL (1) CL2009001759A1 (el)
CO (1) CO6341624A2 (el)
CR (1) CR20110093A (el)
CY (1) CY1117261T1 (el)
DK (1) DK2367812T3 (el)
DO (1) DOP2011000055A (el)
EC (1) ECSP11010841A (el)
ES (1) ES2556764T3 (el)
HK (1) HK1156598A1 (el)
HR (1) HRP20151338T1 (el)
HU (1) HUE026331T2 (el)
IL (2) IL211265A (el)
MA (1) MA32639B1 (el)
MX (1) MX2011001135A (el)
MY (1) MY150599A (el)
NI (1) NI201100024A (el)
NZ (1) NZ591234A (el)
PE (1) PE20100235A1 (el)
PL (1) PL2367812T3 (el)
PT (1) PT2367812E (el)
RS (1) RS54413B1 (el)
RU (1) RU2509766C2 (el)
SI (1) SI2367812T1 (el)
TW (1) TWI473613B (el)
UA (1) UA104148C2 (el)
UY (1) UY32069A (el)
WO (1) WO2010022196A2 (el)
ZA (1) ZA201100597B (el)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY150599A (en) 2008-08-22 2014-01-30 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
FR2955324A1 (fr) * 2010-01-15 2011-07-22 Sanofi Aventis [4-(5-aminomethyl-phenyl)-piperidin-1-yl]-1h-indol-3-yl]-methanones disubstituees
MX2012006805A (es) * 2009-12-23 2012-07-10 Sanofi Sa Indolil-piperidinil bencilaminas como inhibidores de beta-triptasa.
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
ES2481790T3 (es) * 2009-12-23 2014-07-31 Sanofi Profármacos de [4[4-(5-aminometil-2-fluoro-fenil)-piperidin-1-il]-(1H-pirrolo-piridin-il)-metanonas y síntesis de los mismos
JP2013515723A (ja) * 2009-12-23 2013-05-09 サノフイ 炎症性腸疾患の処置
KR20130009769A (ko) * 2010-02-24 2013-01-23 사노피 피부과 알레르기성 병태의 치료
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
US9193709B2 (en) 2011-10-07 2015-11-24 Takeda Pharmaceutical Company Limited 1-arylcarbonyl-4-oxy-piperidine compounds useful for the treatment of neurodegenerative diseases

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4921475A (en) * 1983-08-18 1990-05-01 Drug Delivery Systems Inc. Transdermal drug patch with microtubes
US5087240A (en) * 1983-08-18 1992-02-11 Drug Delivery Systems Inc. Transdermal drug patch with conductive fibers
US4879119A (en) * 1984-02-21 1989-11-07 Yamanouchi Pharmaceutical Co., Ltd. Patch
EP0318512B1 (en) * 1986-08-18 1998-06-17 Emisphere Technologies, 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
PT96059B (pt) * 1989-12-04 1998-07-31 Searle & Co Sistema de camada unica para a administracao de um medicamento por via transdermica
AU643141B2 (en) * 1991-03-15 1993-11-04 Amgen, Inc. Pulmonary administration of granulocyte colony stimulating factor
US5352456A (en) * 1991-10-10 1994-10-04 Cygnus Therapeutic Systems Device for administering drug transdermally which provides an initial pulse of drug
JPH07502219A (ja) * 1991-12-18 1995-03-09 ミネソタ　マイニング　アンド　マニュファクチャリング　カンパニー 多重層型バリアー構造体
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
CA2409827C (en) * 2000-05-22 2010-06-01 Aventis Pharmaceuticals Products 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
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.
MY150599A (en) 2008-08-22 2014-01-30 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

Also Published As

Publication number Publication date
US8497379B2 (en) 2013-07-30
HK1156598A1 (en) 2012-06-15
RU2509766C2 (ru) 2014-03-20
ZA201100597B (en) 2011-09-28
EP2367812A2 (en) 2011-09-28
AU2009282884A1 (en) 2010-02-25
CA2734877A1 (en) 2010-02-25
IL211265A (en) 2014-09-30
JP2012500794A (ja) 2012-01-12
CN102149705A (zh) 2011-08-10
MX2011001135A (es) 2011-03-21
PE20100235A1 (es) 2010-03-29
DK2367812T3 (en) 2015-12-21
TWI473613B (zh) 2015-02-21
TW201021794A (en) 2010-06-16
UA104148C2 (ru) 2014-01-10
ES2556764T3 (es) 2016-01-20
EP2367812B1 (en) 2015-09-16
NI201100024A (es) 2011-08-08
AR073117A1 (es) 2010-10-13
JP5656834B2 (ja) 2015-01-21
IL211265A0 (en) 2011-04-28
PL2367812T3 (pl) 2016-03-31
WO2010022196A3 (en) 2010-07-22
CL2009001759A1 (es) 2010-07-23
CR20110093A (es) 2011-05-27
KR20110057157A (ko) 2011-05-31
UY32069A (es) 2010-03-26
PT2367812E (pt) 2016-01-20
US20110201647A1 (en) 2011-08-18
US8217178B2 (en) 2012-07-10
HUE026331T2 (en) 2016-06-28
DOP2011000055A (es) 2011-04-30
KR101630217B1 (ko) 2016-06-14
IL221434A (en) 2014-07-31
CA2734877C (en) 2014-04-29
CO6341624A2 (es) 2011-11-21
SI2367812T1 (sl) 2016-01-29
CN102149705B (zh) 2013-08-07
RS54413B1 (en) 2016-04-28
RU2011110745A (ru) 2012-09-27
US20120283445A1 (en) 2012-11-08
MY150599A (en) 2014-01-30
HRP20151338T1 (hr) 2016-01-15
AU2009282884B8 (en) 2014-07-03
ECSP11010841A (es) 2011-03-31
NZ591234A (en) 2012-03-30
BRPI0916920A2 (pt) 2015-11-24
MA32639B1 (fr) 2011-09-01
AU2009282884B2 (en) 2014-01-23
WO2010022196A2 (en) 2010-02-25
CN103508936A (zh) 2014-01-15

Similar Documents

Publication Publication Date Title
CY1117261T1 (el) [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
BR112012017123A2 (pt) composto de n-(1h-indazol-4-il)imidazo [1,2-a]piridina-3-carboxamida como inibidores de cfms
ATE517882T1 (de) Chinolinderivate
EA201100971A1 (ru) Производные пиримидининдола для лечения злокачественного новообразования
EA201071038A1 (ru) Производные 1-бензил-3-гидроксиметилиндазола и их применение для лечения заболеваний, основанных на экспрессии mcp-1, cx3cr1 и p40
DOP2005000039A (es) 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
EA200800147A1 (ru) Способ получения олмесартан медоксомила
EA201391720A1 (ru) Замещенные диоксопиперидинилфталимидные производные
MX2010007714A (es) Piridinas fusionadas activas como inhibidores de c-met.
EA201270144A1 (ru) Комбинированная терапия при лечении диабета
EA201290517A1 (ru) Гетероароматические арилтриазольные производные в качестве ингибиторов фермента pde10a
EA201290516A1 (ru) Гетероароматические производные соединения фенилимидазола в качестве ингибиторов фермента pde10a
EA201071039A1 (ru) Новые производные 1-бензил-3-гидроксиметилиндазола и их применение для лечения заболеваний, основанных на экспрессии mcp-1, cx3cr1 и p40
EA201170722A1 (ru) Лактамы в качестве ингибиторов бета-секретазы
SE0401342D0 (sv) Therapeutic compounds
EA201001196A1 (ru) Соединения 4-пиридинона и их применение для лечения рака
ATE485037T1 (de) Krebsbehandlung mittels fts und 2-deoxyglucose
EA201071043A1 (ru) Новые производные 1-бензил-3-гидроксиметилиндазола и их применение при лечении заболеваний, обусловленных экспрессией mcp-1 и cx3cr1
TW200637817A (en) 5-aminoindole derivatives
DE602005010744D1 (de) Piperazinylpyridinderivate als mittel gegen adipositas
NZ592927A (en) PHOSPHODIESTERASE TYPE III (PDE III) INHIBITORS OR CA2+-SENSITIZING AGENTS such as pimobendan FOR THE TREATMENT OF HYPERTROPHIC CARDIOMYOPATHY
ATE492534T1 (de) 1h-indol-5-ylpiperazin-1-ylmethanonderivate
EA200901474A1 (ru) Соли [4-(6-фтор-7-метиламино-2,4-диоксо-1,4-дигидро-2н-хиназолин-3-ил)фенил]-5-хлортиофен-2-илсульфонилмочевины в различных кристаллических формах и фармацевтические композиции на их основе
EA201071352A1 (ru) Трициклические азотсодержащие соединения и их применение в качестве бактерицидных средств
EA201270747A1 (ru) Композиции и способы для профилактики и лечения ран