[go: up one dir, main page]

PT1490062E - Miméticos de glucocorticóides, métodos para a sua preparação, composições farmacêuticas e suas utilizações - Google Patents

Miméticos de glucocorticóides, métodos para a sua preparação, composições farmacêuticas e suas utilizações Download PDF

Info

Publication number
PT1490062E
PT1490062E PT03714339T PT03714339T PT1490062E PT 1490062 E PT1490062 E PT 1490062E PT 03714339 T PT03714339 T PT 03714339T PT 03714339 T PT03714339 T PT 03714339T PT 1490062 E PT1490062 E PT 1490062E
Authority
PT
Portugal
Prior art keywords
making
methods
pharmaceutical compositions
glucocorticoid mimetics
glucocorticoid
Prior art date
Application number
PT03714339T
Other languages
English (en)
Inventor
Y Bekkali
R Betageri
Thomas A Gilmore
Mario G Cardozo
T M Kirrane
D Kuzmich
J Proudfoot
D Thomson
Ji Wang
R Zindell
C Harcken
D Riether
Hossein Razavi
H Takahashi
Original Assignee
Boehringer Ingelheim Pharma
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 Boehringer Ingelheim Pharma filed Critical Boehringer Ingelheim Pharma
Publication of PT1490062E publication Critical patent/PT1490062E/pt

Links

Classifications

    • 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
    • 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
    • A61P1/16—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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P27/16—Otologicals
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • 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
    • 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
    • A61P9/10—Drugs 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
    • 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
    • A61P9/12—Antihypertensives
    • 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
    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
    • C07D213/30—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D215/14—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/12—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
    • C07D217/14—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals
    • C07D217/16—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/12—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/08—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/26—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/12—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D261/18—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/56—Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/24—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/64—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/79—Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D307/80—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/14—Radicals substituted by singly bound hetero atoms other than halogen
    • C07D333/16—Radicals substituted by singly bound hetero atoms other than halogen by oxygen 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Transplantation (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Vascular Medicine (AREA)
PT03714339T 2002-03-26 2003-03-21 Miméticos de glucocorticóides, métodos para a sua preparação, composições farmacêuticas e suas utilizações PT1490062E (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US36775802P 2002-03-26 2002-03-26
US43181702P 2002-12-09 2002-12-09
US44240403P 2003-01-24 2003-01-24

Publications (1)

Publication Number Publication Date
PT1490062E true PT1490062E (pt) 2008-01-30

Family

ID=28678922

Family Applications (1)

Application Number Title Priority Date Filing Date
PT03714339T PT1490062E (pt) 2002-03-26 2003-03-21 Miméticos de glucocorticóides, métodos para a sua preparação, composições farmacêuticas e suas utilizações

Country Status (33)

Country Link
US (4) US6903215B2 (pt)
EP (1) EP1490062B1 (pt)
JP (1) JP4324480B2 (pt)
KR (1) KR101022977B1 (pt)
CN (1) CN1633296A (pt)
AR (1) AR039140A1 (pt)
AT (1) ATE381333T1 (pt)
AU (1) AU2003218342B8 (pt)
BR (1) BR0308784A (pt)
CA (1) CA2478156C (pt)
CL (1) CL2010000375A1 (pt)
CO (1) CO5611110A2 (pt)
CY (1) CY1107244T1 (pt)
DE (1) DE60318188T2 (pt)
DK (1) DK1490062T3 (pt)
EA (1) EA008830B1 (pt)
EC (1) ECSP045315A (pt)
ES (1) ES2298508T3 (pt)
HR (1) HRP20040887A2 (pt)
IL (1) IL163366A (pt)
MX (1) MXPA04009329A (pt)
NO (2) NO329386B1 (pt)
NZ (1) NZ535889A (pt)
PE (1) PE20040164A1 (pt)
PL (1) PL373043A1 (pt)
PT (1) PT1490062E (pt)
RS (1) RS51097B (pt)
SA (3) SA07280240B1 (pt)
TW (1) TWI326213B (pt)
UA (1) UA80120C2 (pt)
UY (1) UY27736A1 (pt)
WO (1) WO2003082280A1 (pt)
ZA (1) ZA200406225B (pt)

Families Citing this family (173)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005519897A (ja) * 2002-01-14 2005-07-07 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド グルココルチコイドミメチックス、その製造方法、それを含む医薬製剤及びその使用
KR101022977B1 (ko) * 2002-03-26 2011-03-18 베링거 인겔하임 파마슈티칼즈, 인코포레이티드 글루코코르티코이드 모사체, 이의 제조방법, 약제학적조성물 및 이의 용도
US7268152B2 (en) * 2002-03-26 2007-09-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
US7186864B2 (en) * 2002-05-29 2007-03-06 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
US7074806B2 (en) * 2002-06-06 2006-07-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
DE60322713D1 (de) 2002-08-21 2008-09-18 Boehringer Ingelheim Pharma Substituierte dihydrochinoline als glucocorticoid-mmimetika,verfahren zu deren herstellung, pharmazeutische zubereitungen und deren verwendung
DE60333371D1 (de) * 2002-08-29 2010-08-26 Boehringer Ingelheim Pharma 3-(sulfonamidoethyl)-indol-derivate zur verwendung als glucocorticoid-mimetika bei der behandlung von entzündlichen, allergischen und proliferativen erkrankungen
RU2005124558A (ru) * 2003-01-03 2006-04-10 Берингер Ингельхайм Фармасьютиклз, Инк. (Us) Производные 1-пропанола и 1-пропиламина и их применение в качестве глюкокортикоидных лигандов
AR044519A1 (es) 2003-05-02 2005-09-14 Novartis Ag Derivados de piridin-tiazol amina y de pirimidin-tiazol amina
GB0316290D0 (en) 2003-07-11 2003-08-13 Glaxo Group Ltd Novel compounds
UY28526A1 (es) 2003-09-24 2005-04-29 Boehringer Ingelheim Pharma Miméticos de glucocorticoides, métodos de preparación composiciones farmacéuticas y usos de los mismos
DE502004002403D1 (de) 2003-10-08 2007-02-01 Schering Ag Tetrahydronaphthalinderivate, verfahren zu ihrer herstellung und ihre verwendung als entzündungshemmer
US7638515B2 (en) 2003-10-08 2009-12-29 Bayer Schering Pharma Aktiengesellschaft Tetrahydronaphthalene derivatives, process for their production and their use as anti-inflammatory agents
US7662821B2 (en) 2003-10-08 2010-02-16 Bayer Schering Pharma Ag Tetrahydronaphthalene derivatives, process for their production and their use as anti-inflammatory agents
GB0401334D0 (en) 2004-01-21 2004-02-25 Novartis Ag Organic compounds
US7795272B2 (en) * 2004-03-13 2010-09-14 Boehringer Ingelheim Pharmaceutical, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof
US7179919B2 (en) * 2004-03-18 2007-02-20 Boehringer Ingelheim Pharmaceuticals, Inc. Stereoselective synthesis of certain trifluoromethyl-substituted alcohols
JP2007530541A (ja) * 2004-03-22 2007-11-01 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド グルココルチコイドミメチックスとしてのα−トリフルオロメチルアルコール又はアミン
CA2561164A1 (en) * 2004-04-01 2005-10-20 Elan Pharmaceuticals, Inc. Steroid sparing agents and their use
US20080153859A1 (en) 2004-04-05 2008-06-26 Hartmut Rehwinkel Multiply-substituted tetrahydronaphthalene derivatives, process for their production and their use as anti-inflammatory agents
CN102091068B (zh) * 2004-05-03 2012-09-19 詹森药业有限公司 作为选择性雄激素受体调节剂(sarms)的吲哚、苯并呋喃和苯并噻吩衍生物
GB0411056D0 (en) 2004-05-18 2004-06-23 Novartis Ag Organic compounds
DE102004025791A1 (de) * 2004-05-19 2005-12-15 Schering Ag Chromanol-Derivate, ein Verfahren zu ihrer Herstellung und ihre Verwendung als Entzündungshemmer
PE20060272A1 (es) 2004-05-24 2006-05-22 Glaxo Group Ltd (2r,3r,4s,5r,2'r,3'r,4's,5's)-2,2'-{trans-1,4-ciclohexanodiilbis-[imino(2-{[2-(1-metil-1h-imidazol-4-il)etil]amino}-9h-purin-6,9-diil)]}bis[5-(2-etil-2h-tetrazol-5-il)tetrahidro-3,4-furanodiol] como agonista a2a
TWI307630B (en) 2004-07-01 2009-03-21 Glaxo Group Ltd Immunoglobulins
KR101913531B1 (ko) 2004-07-28 2018-10-30 다케다 야쿠힌 고교 가부시키가이샤 피롤로〔2,3-ｃ〕피리딘 화합물, 그 제조 방법 및 용도
US20060030608A1 (en) * 2004-08-04 2006-02-09 Boehringer Ingelheim Pharmaceuticals, Inc. Anti aromatase compounds pharmaceutical compositions and uses thereof
GB0418045D0 (en) 2004-08-12 2004-09-15 Glaxo Group Ltd Compounds
DE102004044680B3 (de) * 2004-09-09 2006-06-08 Schering Ag Alkyliden-Tetrahydronaphthalinderivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Entzündungshemmer sowie diese enthaltende pharmazeutische Präparate
GT200500281A (es) 2004-10-22 2006-04-24 Novartis Ag Compuestos organicos.
GB0424284D0 (en) 2004-11-02 2004-12-01 Novartis Ag Organic compounds
DE102005020331A1 (de) * 2005-04-26 2006-11-02 Schering Ag 5-substituierte Chinolin- und Isochinolin-Derivate, ein Verfahren zu ihrer Herstellung und ihre Verwendung als Entzündungshemmer
GB0426164D0 (en) 2004-11-29 2004-12-29 Novartis Ag Organic compounds
DE102004063227A1 (de) * 2004-12-22 2006-07-06 Schering Ag Tricylische Aminoalkohole, Verfahren zu ihrer Herstellung und ihre Verwendung als Entzündungshemmer
US7741361B2 (en) 2004-12-27 2010-06-22 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
WO2006072599A2 (en) 2005-01-10 2006-07-13 Glaxo Group Limited Androstane 17-alpha carbonate derivatives for use in the treatment of allergic and inflammatory conditions
US20090176807A1 (en) * 2005-03-04 2009-07-09 John Robinson Regan Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
PE20061193A1 (es) 2005-03-25 2006-12-02 Glaxo Group Ltd DERIVADOS DE 3,4-DIHIDROPIRIMIDO[4,5-d]PIRIMIDIN-2-[1H]-0NA COMO INHIBIDORES DE QUINASA p38
UY29440A1 (es) 2005-03-25 2006-10-02 Glaxo Group Ltd Nuevos compuestos
EP1869003B1 (en) * 2005-04-14 2013-05-15 Glaxo Group Limited Indazoles as glucocorticoid receptor ligands
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
EP1893588A1 (en) * 2005-06-10 2008-03-05 Boehringer Ingelheim International GmbH Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
GB0514809D0 (en) 2005-07-19 2005-08-24 Glaxo Group Ltd Compounds
JPWO2007040166A1 (ja) * 2005-09-30 2009-04-16 大日本住友製薬株式会社 新規な縮合ピロール誘導体
ES2333820T3 (es) 2005-09-30 2010-03-01 Boehringer Ingelheim International Gmbh Sintesis estereoselectiva de determinados alcoholes trifluorometilo-sustituidos.
MY144906A (en) 2005-10-21 2011-11-30 Novartis Ag Human antibodies against il13 and therapeutic uses
BRPI0619518A2 (pt) * 2005-12-09 2011-10-11 Hoffmann La Roche moduladores do receptor de glicocorticoide, composição farmacêutica que os compreende e usos dos mesmos
AU2006324090B2 (en) * 2005-12-09 2012-05-31 F. Hoffmann-La Roche Ag Propionamide compounds as antiinflammatory agents
AR058109A1 (es) 2005-12-20 2008-01-23 Glaxo Group Ltd Acido 3 - (4 - {[4 -(4 -{[3 - (3, 3 - dimetil - 1 - piperidinil)propil]oxi}fenil) - 1 - piperidinil]carbonil} - 1 - naftalenil)propanoico como antagonistas de los receptotres de histamina h1/h3, composiciones farmaceuticas que los contienen y su uso en la preparacion de medicamentos para el tratamie
GB0526244D0 (en) 2005-12-22 2006-02-01 Novartis Ag Organic compounds
GB0601951D0 (en) 2006-01-31 2006-03-15 Novartis Ag Organic compounds
EP1834948A1 (de) 2006-03-15 2007-09-19 Bayer Schering Pharma Aktiengesellschaft Tetrahydronaphthalinderivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Entzündungshemmer
MX2008013411A (es) 2006-04-20 2008-11-04 Glaxo Group Ltd Nuevos compuestos.
RU2457209C2 (ru) 2006-04-21 2012-07-27 Новартис Аг Производные пурина, предназначенные для применения в качестве агонистов аденозинового рецептора а2а
GB0611587D0 (en) 2006-06-12 2006-07-19 Glaxo Group Ltd Novel compounds
CN101484187B (zh) * 2006-07-07 2012-12-26 博士伦公司 包含解离的糖皮质激素受体激动剂和免疫抑制剂的用于治疗干眼症的组合物
KR20090040369A (ko) * 2006-08-07 2009-04-23 보오슈 앤드 롬 인코포레이팃드 해리된 글루코코르티코이드 수용체 효능제와 항감염제의 조합을 이용한 감염증 및 그의 후유증의 치료
PT2056799E (pt) 2006-08-31 2013-11-06 Bausch & Lomb Composições e métodos para tratamento ou prevenção do glaucoma ou da sua progressão
US20110105559A1 (en) * 2006-09-11 2011-05-05 Rohrs Brian R Compositions and Methods for Treating, Controlling, Reducing, Ameliorating, or Preventing Allergy
US20110104159A1 (en) * 2006-09-11 2011-05-05 Rohrs Brian R Compositions and methods for treating, controlling, reducing, ameliorating, or preventing allergy
PL2061444T3 (pl) * 2006-09-11 2011-09-30 Bausch & Lomb Kompozycje i sposoby leczenia, traktowania, kontrolowania, redukowania, łagodzenia lub zapobiegania alergii
MX2009003185A (es) 2006-09-29 2009-04-03 Novartis Ag Pirazolopirimidinas como inhibidores de lipido cinasa pi3k.
WO2008055709A1 (en) * 2006-11-08 2008-05-15 Bayer Schering Pharma Aktiengesellschaft Indazole and indole derivatives as anti -inflammatory agents
EP1921067A1 (en) * 2006-11-08 2008-05-14 Bayer Schering Pharma Aktiengesellschaft Indole and indazole derivatives as anti-inflammatory agents
EP1921068A1 (en) * 2006-11-08 2008-05-14 Bayer Schering Pharma Aktiengesellschaft Indazole and indole derivatives as anti-inflammatory agents
JP2010512331A (ja) * 2006-12-06 2010-04-22 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング グルココルチコイド模倣薬、それらの製造方法、医薬組成物、及びこれらの使用
HRP20110201T1 (hr) 2007-01-10 2011-08-31 Irm Llc Spojevi i sastavi kao inhibitori proteaze kanalizirane aktivacije
PE20081889A1 (es) 2007-03-23 2009-03-05 Smithkline Beecham Corp Indol carboxamidas como inhibidores de ikk2
DE602008005140D1 (de) 2007-05-07 2011-04-07 Novartis Ag Organische verbindungen
US20090042936A1 (en) * 2007-08-10 2009-02-12 Ward Keith W Compositions and Methods for Treating or Controlling Anterior-Segment Inflammation
CN101801200B (zh) * 2007-09-17 2014-10-29 康奈尔大学 用于预防或治疗胃肠病症的支链脂肪酸
US20090087443A1 (en) 2007-09-27 2009-04-02 Bartels Stephen P Pharmacological Adjunctive Treatment Associated with Glaucoma Filtration Surgery
US8143280B2 (en) * 2007-09-27 2012-03-27 Hoffmann-La Roche Inc. Glucocorticoid receptor antagonists
AR069637A1 (es) 2007-12-10 2010-02-10 Novartis Ag Derivados de pirazinas
CN101910153B (zh) 2008-01-11 2014-01-22 诺华股份有限公司 作为激酶抑制剂的嘧啶类
US20090239836A1 (en) * 2008-03-24 2009-09-24 Mary Lee Ciolkowski Multifunctional Ophthalmic Compositions
US20090291073A1 (en) * 2008-05-20 2009-11-26 Ward Keith W Compositions Comprising PKC-theta and Methods for Treating or Controlling Ophthalmic Disorders Using Same
MX2010012814A (es) 2008-05-23 2010-12-20 Amira Pharmaceuticals Inc Inhibidor de proteina activadora de 5-lipoxigenasa.
WO2009147190A1 (en) 2008-06-05 2009-12-10 Glaxo Group Limited Novel compounds
WO2009147187A1 (en) 2008-06-05 2009-12-10 Glaxo Group Limited 4-carboxamide indazole derivatives useful as inhibitors of p13-kinases
ATE541846T1 (de) * 2008-06-06 2012-02-15 Boehringer Ingelheim Int Glucocorticoidmimetika, verfahren zu deren herstellung, pharmazeutische zusammensetzungen und anwendungen davon
WO2009150137A2 (en) 2008-06-10 2009-12-17 Novartis Ag Organic compounds
WO2010049073A1 (en) * 2008-10-30 2010-05-06 Bayer Schering Pharma Aktiengesellschaft 1,1,1-trifluoro-3-amino-3-heteroaryl-2-propanoles, a process for their production and their use as anti-inflammatory agents
PT2391366E (pt) 2009-01-29 2013-02-05 Novartis Ag Benzimidazoles substituídos para o tratamento de astrocitomas
WO2010094643A1 (en) 2009-02-17 2010-08-26 Glaxo Group Limited Quinoline derivatives and their uses for rhinitis and urticaria
WO2010102958A1 (en) 2009-03-09 2010-09-16 Glaxo Group Limited 4-oxadiazol-2 -yl- indazoles as inhibitors of p13 kinases
US8354539B2 (en) 2009-03-10 2013-01-15 Glaxo Group Limited Indole derivatives as IKK2 inhibitors
US20120058984A1 (en) 2009-03-17 2012-03-08 Catherine Mary Alder Pyrimidine derivatives used as itk inhibitors
WO2010107952A2 (en) 2009-03-19 2010-09-23 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF CONNECTIVE TISSUE GROWTH FACTOR (CTGF) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
US20120029054A1 (en) 2009-03-19 2012-02-02 Merck Sharp & Dohme Corp. RNA Interference Mediated Inhibition of GATA Binding Protein 3 (GATA3) Gene Expression Using Short Intefering Nucleic Acid (siNA)
US20120016010A1 (en) 2009-03-19 2012-01-19 Merck Sharp & Dohme Corp RNA Interference Mediated Inhibition of BTB and CNC Homology 1, Basic Leucine Zipper Transcription Factor 1 (BACH1) Gene Expression Using Short Interfering Nucleic Acid (siNA)
US20120035247A1 (en) 2009-03-19 2012-02-09 Merck Sharp & Dohme Corp. RNA Interference Mediated Inhibition of Signal Transducer and Activator of Transcription 6 (STAT6) Gene Expression Using Short Interfering Nucleic Acid (siNA)
EP2411019A2 (en) 2009-03-27 2012-02-01 Merck Sharp&Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF SIGNAL TRANSDUCER AND ACTIVATOR OF TRANSCRIPTION 1 (STAT1) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
WO2010111468A2 (en) 2009-03-27 2010-09-30 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF THE NERVE GROWTH FACTOR BETA CHAIN (NGFß) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (SINA)
US20120022143A1 (en) 2009-03-27 2012-01-26 Merck Sharp & Dohme Corp RNA Interference Mediated Inhibition of the Thymic Stromal Lymphopoietin (TSLP) Gene Expression Using Short Interfering Nucliec Acid (siNA)
KR20110138223A (ko) 2009-03-27 2011-12-26 머크 샤프 앤드 돔 코포레이션 짧은 간섭 핵산 (ｓｉＮＡ)을 사용한 세포간 부착 분자 1 (ＩＣＡＭ-1) 유전자 발현의 ＲＮＡ 간섭 매개 억제
WO2010111464A1 (en) 2009-03-27 2010-09-30 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF APOPTOSIS SIGNAL-REGULATING KINASE 1 (ASK1) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
US8456662B2 (en) * 2009-04-15 2013-06-04 Ricoh Company, Ltd. Control for display of multiple versions of a printable document for locked print
US20110077270A1 (en) * 2009-04-21 2011-03-31 Pfeffer Bruce A Compositions and Methods for Treating Ocular Inflammation with Lower Risk of Increased Intraocular Pressure
JP2012524754A (ja) 2009-04-24 2012-10-18 グラクソ グループ リミテッド Ｃｒａｃチャネル阻害剤としてのピラゾールおよびトリアゾ−ルカルボキサミド
AR076373A1 (es) 2009-04-24 2011-06-08 Glaxo Group Ltd N-pirazolil carboxamidas como inhibidores de canales de calcio
PL2899191T3 (pl) 2009-04-30 2018-01-31 Glaxo Group Ltd Indazole podstawione oksazolem jako inhibitory kinazy PI3
US20110130578A1 (en) 2009-06-03 2011-06-02 Boehringer Ingelheim International Gmbh Stereoselective synthesis of certain trifluoromethyl-substituted alcohols
US20100312013A1 (en) 2009-06-03 2010-12-09 Boehringer Ingelheim International Gmbh Steroselective synthesis of certain trifluoromethyl-substituted alcohols
US8420819B2 (en) * 2009-06-03 2013-04-16 Boehringer Ingelheim International Gmbh Process for optimizing the particle size of an active pharmaceutical ingredient by crystallization
US20110130567A1 (en) 2009-06-03 2011-06-02 Boehringer Ingelheim International Gmbh Steroselective synthesis of certain trifluoromethyl-substituted alcohols
US20110130591A1 (en) * 2009-06-03 2011-06-02 Boehringer Ingelheim International Gmbh Steroselective synthesis of certain trifluoromethyl-substituted alcohols
JP2013500962A (ja) 2009-07-31 2013-01-10 カディラ ヘルスケア リミティド グルココルチコイド受容体のモジュレーターとしての新規化合物
US8389526B2 (en) 2009-08-07 2013-03-05 Novartis Ag 3-heteroarylmethyl-imidazo[1,2-b]pyridazin-6-yl derivatives
BR112012003262A8 (pt) 2009-08-12 2016-05-17 Novartis Ag compostos de hidrazona heterocíclica e seus usos para tratar câncer e inflamação
PE20121148A1 (es) 2009-08-17 2012-09-07 Intellikine Llc Compuestos heterociclicos y usos de los mismos
BR112012008061A2 (pt) 2009-08-20 2016-03-01 Novartis Ag compostos de oxima heterocíclica
JP2013508414A (ja) 2009-10-22 2013-03-07 バーテックス ファーマシューティカルズ インコーポレイテッド 嚢胞性線維症および他の慢性疾患の治療のための組成物
EP2507231A1 (en) 2009-12-03 2012-10-10 Glaxo Group Limited Indazole derivatives as pi 3 - kinase inhibitors
US20120238559A1 (en) 2009-12-03 2012-09-20 Glaxo Group Limited Novel compounds
WO2011067365A1 (en) 2009-12-03 2011-06-09 Glaxo Group Limited Benzpyrazole derivatives as inhibitors of p13 kinases
EP2512438B1 (en) 2009-12-16 2017-01-25 3M Innovative Properties Company Formulations and methods for controlling mdi particle size delivery
WO2011110575A1 (en) 2010-03-11 2011-09-15 Glaxo Group Limited Derivatives of 2-[2-(benzo- or pyrido-) thiazolylamino]-6-aminopyridine, useful in the treatment of respiratoric, allergic or inflammatory diseases
US8247436B2 (en) 2010-03-19 2012-08-21 Novartis Ag Pyridine and pyrazine derivative for the treatment of CF
GB201007203D0 (en) 2010-04-29 2010-06-16 Glaxo Group Ltd Novel compounds
US9326987B2 (en) 2010-09-08 2016-05-03 Glaxo Group Limited Indazole derivatives for use in the treatment of influenza virus infection
HUE026059T2 (en) 2010-09-08 2016-05-30 Glaxosmithkline Ip Dev Ltd N- [5- [4- (5 - {[(2R, 6S) -2,6-dimethyl-4-morpholinyl] methyl} -1,3-oxazol-2-yl) -1H-indazol-6-yl ] Polymorphs and salts of 2 - (methyloxy) -3-pyridinyl] methanesulfonamide
WO2012034095A1 (en) 2010-09-09 2012-03-15 Irm Llc Compounds and compositions as trk inhibitors
UY33597A (es) 2010-09-09 2012-04-30 Irm Llc Compuestos y composiciones como inhibidores de la trk
WO2012035055A1 (en) 2010-09-17 2012-03-22 Glaxo Group Limited Novel compounds
US8372845B2 (en) 2010-09-17 2013-02-12 Novartis Ag Pyrazine derivatives as enac blockers
WO2012052458A1 (en) 2010-10-21 2012-04-26 Glaxo Group Limited Pyrazole compounds acting against allergic, immune and inflammatory conditions
US9149462B2 (en) 2010-10-21 2015-10-06 Glaxo Group Limited Pyrazole compounds acting against allergic, inflammatory and immune disorders
GB201018124D0 (en) 2010-10-27 2010-12-08 Glaxo Group Ltd Polymorphs and salts
EP2673277A1 (en) 2011-02-10 2013-12-18 Novartis AG [1, 2, 4]triazolo [4, 3 -b]pyridazine compounds as inhibitors of the c-met tyrosine kinase
JP5808826B2 (ja) 2011-02-23 2015-11-10 インテリカイン， エルエルシー 複素環化合物およびその使用
BR112013021638A2 (pt) 2011-02-25 2016-08-02 Irm Llc "compostos inibidores de trk, seu uso e composições que os compreendem"
GB201104153D0 (en) 2011-03-11 2011-04-27 Glaxo Group Ltd Novel compounds
EP2683716A1 (en) 2011-03-11 2014-01-15 Glaxo Group Limited Pyrido[3,4-b]pyrazine derivatives as syk inhibitors
US20120316199A1 (en) 2011-06-07 2012-12-13 Ward Keith W Compositions and methods for treating, controlling, reducing, or ameliorating inflammatory pain
UY34305A (es) 2011-09-01 2013-04-30 Novartis Ag Derivados de heterociclos bicíclicos para el tratamiento de la hipertensión arterial pulmonar
EP2755976B1 (en) 2011-09-15 2018-07-18 Novartis AG 6-substituted 3-(quinolin-6-ylthio)-[1,2,4]triazolo[4,3-a]pyridines as c-met tyrosine kinase inhibitors
WO2013038381A1 (en) 2011-09-16 2013-03-21 Novartis Ag Pyridine/pyrazine amide derivatives
WO2013038373A1 (en) 2011-09-16 2013-03-21 Novartis Ag Pyridine amide derivatives
ES2882807T3 (es) 2011-09-16 2021-12-02 Novartis Ag Heterociclil carboxamidas N-sustituidas
CN103946221B (zh) 2011-09-16 2016-08-03 诺华股份有限公司 用于治疗囊性纤维化的杂环化合物
WO2013038378A1 (en) 2011-09-16 2013-03-21 Novartis Ag Pyridine amide derivatives
US20130209543A1 (en) 2011-11-23 2013-08-15 Intellikine Llc Enhanced treatment regimens using mtor inhibitors
US8809340B2 (en) 2012-03-19 2014-08-19 Novartis Ag Crystalline form
JP2015512425A (ja) 2012-04-03 2015-04-27 ノバルティス アーゲー チロシンキナーゼ阻害剤との組合せ製品及びそれらの使用
US9073921B2 (en) 2013-03-01 2015-07-07 Novartis Ag Salt forms of bicyclic heterocyclic derivatives
WO2014151147A1 (en) 2013-03-15 2014-09-25 Intellikine, Llc Combination of kinase inhibitors and uses thereof
US10155001B2 (en) 2013-06-14 2018-12-18 Inserm (Institut National De La Sante Et De La Recherche Medicale) RAC1 inhibitors for inducing bronchodilation
JP6494634B2 (ja) 2013-09-22 2019-04-03 キャリター・サイエンシーズ・リミテッド・ライアビリティ・カンパニーＣａｌｉｔｏｒ Ｓｃｉｅｎｃｅｓ， Ｌｌｃ 置換されているアミノピリミジン化合物および使用方法
CA2923995A1 (en) 2013-10-17 2015-04-23 Glaxosmithkline Intellectual Property Development Limited Pi3k inhibitor for treatment of respiratory disease
WO2015055691A1 (en) 2013-10-17 2015-04-23 Glaxosmithkline Intellectual Property Development Limited Pi3k inhibitor for treatment of respiratory disease
WO2015084804A1 (en) 2013-12-03 2015-06-11 Novartis Ag Combination of mdm2 inhibitor and braf inhibitor and their use
EP3312164B1 (en) 2014-03-28 2020-12-09 Calitor Sciences, LLC Substituted heteroaryl compounds and methods of use
CN106458979B (zh) 2014-04-24 2020-03-27 诺华股份有限公司 作为磷脂酰肌醇3-激酶抑制剂的氨基吡嗪衍生物
EP3134396B1 (en) 2014-04-24 2019-09-18 Novartis AG Amino pyridine derivatives as phosphatidylinositol 3-kinase inhibitors
BR112016023967A2 (pt) 2014-04-24 2017-08-15 Novartis Ag derivados de pirazina como inibidores de fosfatidilinositol 3-cinase
TW201625247A (zh) 2014-05-12 2016-07-16 葛蘭素史密斯克藍智慧財產權有限公司 用於治療傳染性疾病之醫藥組合物
WO2016011658A1 (en) 2014-07-25 2016-01-28 Novartis Ag Combination therapy
AU2015294889B2 (en) 2014-07-31 2018-03-15 Novartis Ag Combination therapy
JP2018527362A (ja) 2015-09-11 2018-09-20 サンシャイン・レイク・ファーマ・カンパニー・リミテッドＳｕｎｓｈｉｎｅ Ｌａｋｅ Ｐｈａｒｍａ Ｃｏ．，Ｌｔｄ． 置換されたヘテロアリール化合物および使用方法
CN105418529B (zh) * 2015-12-30 2017-07-18 商丘师范学院 一种含4‑硝基异噁唑基三氟甲基叔醇化合物及其制备方法
CN105622536B (zh) * 2015-12-30 2018-06-29 商丘师范学院 一种三氟甲基化烯基异噁唑化合物及其制备方法和应用
GB201602527D0 (en) 2016-02-12 2016-03-30 Glaxosmithkline Ip Dev Ltd Chemical compounds
EP3497100A1 (en) 2016-08-08 2019-06-19 GlaxoSmithKline Intellectual Property Development Limited Chemical compounds
GB201706102D0 (en) 2017-04-18 2017-05-31 Glaxosmithkline Ip Dev Ltd Chemical compounds
GB201712081D0 (en) 2017-07-27 2017-09-13 Glaxosmithkline Ip Dev Ltd Chemical compounds
US10683297B2 (en) 2017-11-19 2020-06-16 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
US10751339B2 (en) 2018-01-20 2020-08-25 Sunshine Lake Pharma Co., Ltd. Substituted aminopyrimidine compounds and methods of use
AU2020290094B2 (en) 2019-06-10 2024-01-18 Novartis Ag Pyridine and pyrazine derivative for the treatment of CF, COPD, and bronchiectasis
PE20220346A1 (es) 2019-08-28 2022-03-14 Novartis Ag Derivados de 1,3-fenil heteroarilo sustituidos y su uso en el tratamiento de enfermedades
TW202140550A (zh) 2020-01-29 2021-11-01 瑞士商諾華公司 使用抗ｔｓｌｐ抗體治療炎性或阻塞性氣道疾病之方法
WO2021191875A1 (en) 2020-03-26 2021-09-30 Glaxosmithkline Intellectual Property Development Limited Cathepsin inhibitors for preventing or treating viral infections

Family Cites Families (80)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1017612B (de) 1954-02-05 1957-10-17 Thomae Gmbh Dr K Verfahren zur Herstellung von tertiaeren Aminen, ihren Saeureadditionssalzen und quaternaeren Ammoniumverbindungen
US3772273A (en) * 1969-01-17 1973-11-13 Allied Chem Derivatives of quinoxaline
NL8402755A (nl) 1983-09-22 1985-04-16 Sandoz Ag Azool-derivaten, werkwijze voor het bereiden daarvan, preparaten die ze bevatten, en toepassing daarvan.
JPS60163814A (ja) 1984-02-06 1985-08-26 Wataru Mori グルココルチコイド拮抗剤
GB8406000D0 (en) 1984-03-07 1984-04-11 Ici Plc Olefine derivatives
US4551534A (en) * 1984-03-30 1985-11-05 American Home Products Corporation Aralkyl or aryloxyalkyl 1,7-naphthyridine-3-carboxylic acid esters
DE3514696A1 (de) * 1985-04-24 1986-11-06 Bayer Ag, 5090 Leverkusen N-indolylethyl-sulfonsaeureamide, verfahren zu ihrer herstellung und ihre verwendung
GB8617652D0 (en) 1986-07-18 1986-08-28 Ici Plc Acylanilide derivatives
GB8617653D0 (en) 1986-07-18 1986-08-28 Ici Plc Amide derivatives
GB2210875B (en) 1987-10-09 1991-05-29 Farmos Oy Aromatase inhibiting 4(5)-imidazoles
US5039691A (en) 1989-06-08 1991-08-13 Marion Merrell Dow Inc. 5-(1-(imidazol)methyl)-3,3-disubstituted-2(3H)furanone derivatives
US5206377A (en) * 1991-12-05 1993-04-27 Whitby Research, Inc. Compounds useful as antiproliferative agents
JPH05194404A (ja) 1992-01-22 1993-08-03 Zeria Pharmaceut Co Ltd カルボスチリル誘導体
GB9201755D0 (en) 1992-01-28 1992-03-11 British Bio Technology Compounds
US5948820A (en) * 1994-08-22 1999-09-07 Yoshitomi Pharmaceutical Industries, Ltd. Benzene compound and pharmaceutical use thereof
NZ300739A (en) 1994-12-22 2000-05-26 Ligand Pharm Inc Steroid receptor modulator compounds
US5688808A (en) * 1994-12-22 1997-11-18 Ligand Pharmaceuticals Incorporated Steroid receptor modulator compounds and methods
AU703203B2 (en) 1996-01-30 1999-03-18 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
DE19723722A1 (de) 1997-05-30 1998-12-10 Schering Ag Nichtsteroidale Gestagene
JPH1180131A (ja) 1997-09-01 1999-03-26 Mitsubishi Chem Corp エチニルピリミジン誘導体
ZA9811898B (en) 1997-12-29 2000-06-28 Ortho Mcneil Pharm Inc Anti-Inflammatory Compounds.
AU766441B2 (en) 1998-02-13 2003-10-16 Abbott Laboratories Glucocorticoid-selective anti-inflammatory agents
US6506766B1 (en) 1998-02-13 2003-01-14 Abbott Laboratories Glucocortiocoid-selective antinflammatory agents
ES2196721T3 (es) * 1998-02-16 2003-12-16 Ajinomoto Kk Metodo para producir un derivado de acido fenilpropionico opticamente activo.
US6169106B1 (en) * 1998-04-15 2001-01-02 Boehringer Ingelheim Pharma Kg Indolinones having kinase inhibitory activity
DE19816624A1 (de) 1998-04-15 1999-10-21 Boehringer Ingelheim Pharma Neue substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel
AU751569B2 (en) 1998-06-08 2002-08-22 Karo Bio Ab Treatment of diabetes
US6187918B1 (en) * 1999-03-15 2001-02-13 Dupont Pharmaceuticals Company Catalysts for asymmetric addition of organozinc reagents to aldehydes and method for preparation
NZ510845A (en) * 1998-09-25 2003-10-31 Boehringer Ingelheim Pharma Novel substituted indolinones with an inhibitory effect on various kinases and cyclin/CDK complexes
DE19856475A1 (de) 1998-11-27 2000-05-31 Schering Ag Nichtsteroidale Entzündungshemmer
EP1175383B1 (en) 1999-04-30 2018-03-14 Pfizer Products Inc. Glucocorticoid receptor modulators
CN1454211A (zh) 1999-07-16 2003-11-05 布里斯托尔-迈尔斯斯奎布药品公司 作为Xa因子抑制剂的含氮杂双环化合物
US6436986B1 (en) 1999-09-01 2002-08-20 Abbott Laboratories Glucocorticoid receptor antagonists for treatment of diabetes
US6329534B1 (en) 1999-09-01 2001-12-11 Abbott Laboratories Glucocorticoid receptor antagonists for treatment of diabetes
IL139197A0 (en) 1999-10-29 2001-11-25 Pfizer Prod Inc Use of corticotropin releasing factor antagonists and related compositions
US7713989B2 (en) 2000-04-27 2010-05-11 Dow Robert L Glucocorticoid receptor modulators
US6852734B2 (en) 2000-05-02 2005-02-08 Meiji Seika Kaisha, Ltd. Indole derivatives exhibiting chymase-inhibitory activities and process for preparation thereof
EP1157682A1 (en) 2000-05-25 2001-11-28 Cilag AG Blister package for topiramate tablets
DE10038639A1 (de) 2000-07-28 2002-02-21 Schering Ag Nichtsteroidale Entzündungshemmer
AU2001280984A1 (en) 2000-07-28 2002-02-13 Inspire Pharmaceuticals, Inc. Use of indole derivatives for the manufacture of a medicament for reducing intracular pressure
US7030116B2 (en) * 2000-12-22 2006-04-18 Aventis Pharmaceuticals Inc. Compounds and compositions as cathepsin inhibitors
MXPA03005601A (es) 2000-12-22 2004-12-02 Axys Pharm Inc Nuevos compuestos y composiciones como inhibidores de catepsina.
US6583180B2 (en) 2001-02-14 2003-06-24 Abbott Laboratories Glucocorticoid receptor modulators
MXPA03007261A (es) 2001-02-14 2006-03-09 Abbott Lab Moduladores del receptor de glucocorticoides.
WO2003012046A2 (en) * 2001-07-27 2003-02-13 The Regents Of The University Of California Stk15 (stk6) gene polymorphism and methods of determining cancer risk
GB0124299D0 (en) 2001-10-10 2001-11-28 Astrazeneca Ab Crystal structure of enzyme and uses thereof
WO2003032997A1 (de) 2001-10-17 2003-04-24 Boehringer Ingelheim Pharma Gmbh & Co. Kg Pyrimidinderivate, arzneimittel enthaltend diese verbindungen, deren verwendung und verfahren zu ihrer herstellung
JP2005519897A (ja) 2002-01-14 2005-07-07 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド グルココルチコイドミメチックス、その製造方法、それを含む医薬製剤及びその使用
KR101022977B1 (ko) * 2002-03-26 2011-03-18 베링거 인겔하임 파마슈티칼즈, 인코포레이티드 글루코코르티코이드 모사체, 이의 제조방법, 약제학적조성물 및 이의 용도
US7268152B2 (en) 2002-03-26 2007-09-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
DE10215316C1 (de) 2002-04-02 2003-12-18 Schering Ag Chinolin- und Isochinolin-Derivate, ein pharmazeutisches Mittel und ihre Verwendung als Entzündungshemmer
US6897224B2 (en) * 2002-04-02 2005-05-24 Schering Ag Quinoline and isoquinoline derivatives, a process for their production and their use as inflammation inhibitors
US7186864B2 (en) 2002-05-29 2007-03-06 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
US7074806B2 (en) 2002-06-06 2006-07-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
ITMI20021247A1 (it) * 2002-06-07 2003-12-09 Menarini Ricerche Spa Antagonisti basici non peptidici della bradichinina e loro impiego informulazioni farmaceutiche
GB0215650D0 (en) 2002-07-05 2002-08-14 Cyclacel Ltd Bisarylsufonamide compounds
DE60322713D1 (de) 2002-08-21 2008-09-18 Boehringer Ingelheim Pharma Substituierte dihydrochinoline als glucocorticoid-mmimetika,verfahren zu deren herstellung, pharmazeutische zubereitungen und deren verwendung
DE60333371D1 (de) 2002-08-29 2010-08-26 Boehringer Ingelheim Pharma 3-(sulfonamidoethyl)-indol-derivate zur verwendung als glucocorticoid-mimetika bei der behandlung von entzündlichen, allergischen und proliferativen erkrankungen
US7112584B2 (en) * 2002-12-20 2006-09-26 Schering Ag Nonsteroidal antiinflammatory agents
RU2005124558A (ru) 2003-01-03 2006-04-10 Берингер Ингельхайм Фармасьютиклз, Инк. (Us) Производные 1-пропанола и 1-пропиламина и их применение в качестве глюкокортикоидных лигандов
JP2006515014A (ja) * 2003-01-30 2006-05-18 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド ＰＫＣ−θのインヒビターとして有用な２，４−ジアミノピリミジン誘導体
WO2004071389A2 (en) 2003-02-15 2004-08-26 Glaxo Group Limited Non-steroidal infalmmation inhibitors
US20040224992A1 (en) * 2003-02-27 2004-11-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
WO2004089415A2 (en) 2003-04-11 2004-10-21 Novo Nordisk A/S COMBINATIONS OF AN 11β-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITOR AND A GLUCOCORTICOID RECEPTOR AGONIST
WO2005019202A1 (en) 2003-08-20 2005-03-03 Amgen Inc. Substituted pyrimdinone derivatives and methods of use
UY28526A1 (es) 2003-09-24 2005-04-29 Boehringer Ingelheim Pharma Miméticos de glucocorticoides, métodos de preparación composiciones farmacéuticas y usos de los mismos
JP4949845B2 (ja) * 2003-10-03 2012-06-13 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド タンパク質キナーゼインヒビター結合アッセイにおける使用のための蛍光プローブ
CA2542741A1 (en) * 2003-10-16 2005-05-06 Boehringer Ingelheim Pharmaceuticals, Inc. Stereoselective synthesis of certain trifluoromethyl-substituted alcohols
US7795272B2 (en) * 2004-03-13 2010-09-14 Boehringer Ingelheim Pharmaceutical, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof
US7179919B2 (en) 2004-03-18 2007-02-20 Boehringer Ingelheim Pharmaceuticals, Inc. Stereoselective synthesis of certain trifluoromethyl-substituted alcohols
JP2007530541A (ja) * 2004-03-22 2007-11-01 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド グルココルチコイドミメチックスとしてのα−トリフルオロメチルアルコール又はアミン
US7256300B2 (en) * 2004-03-30 2007-08-14 Boehringer Ingelheim Pharmaceuticals, Inc. Stereoselective synthesis of certain trifluoromethyl-substituted alcohols
US20060030608A1 (en) * 2004-08-04 2006-02-09 Boehringer Ingelheim Pharmaceuticals, Inc. Anti aromatase compounds pharmaceutical compositions and uses thereof
KR20070068432A (ko) 2004-10-29 2007-06-29 아스트라제네카 아베 염증 질환의 치료를 위한 글루코코르티코이드 수용체조절제로서의 신규 술폰아미드 유도체
US8101619B2 (en) * 2004-12-08 2012-01-24 Solvay Pharmaceuticals B.V. Phenylpiperazine derivatives with a combination of partial dopamine-D2 receptor agonism and serotonin reuptake inhibition
US7741361B2 (en) 2004-12-27 2010-06-22 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
US20090176807A1 (en) * 2005-03-04 2009-07-09 John Robinson Regan Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
EP1893588A1 (en) * 2005-06-10 2008-03-05 Boehringer Ingelheim International GmbH Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
ES2333820T3 (es) * 2005-09-30 2010-03-01 Boehringer Ingelheim International Gmbh Sintesis estereoselectiva de determinados alcoholes trifluorometilo-sustituidos.
ATE541846T1 (de) * 2008-06-06 2012-02-15 Boehringer Ingelheim Int Glucocorticoidmimetika, verfahren zu deren herstellung, pharmazeutische zusammensetzungen und anwendungen davon

Also Published As

Publication number Publication date
AU2003218342B2 (en) 2008-07-10
EA008830B1 (ru) 2007-08-31
DE60318188T2 (de) 2008-12-11
BR0308784A (pt) 2005-01-11
MXPA04009329A (es) 2005-01-25
JP4324480B2 (ja) 2009-09-02
HRP20040887A2 (en) 2005-04-30
KR20040095343A (ko) 2004-11-12
TWI326213B (en) 2010-06-21
KR101022977B1 (ko) 2011-03-18
RS51097B (sr) 2010-10-31
US7932392B2 (en) 2011-04-26
CY1107244T1 (el) 2012-11-21
JP2005527555A (ja) 2005-09-15
AU2003218342A1 (en) 2003-10-13
PL373043A1 (en) 2005-08-08
SA03240209B1 (ar) 2008-01-30
ZA200406225B (en) 2006-05-31
AR039140A1 (es) 2005-02-09
PE20040164A1 (es) 2004-05-21
EP1490062B1 (en) 2007-12-19
DK1490062T3 (da) 2008-04-28
CA2478156C (en) 2011-02-15
US20050282881A1 (en) 2005-12-22
SA07280239B1 (ar) 2009-12-15
SA07280240B1 (ar) 2009-11-15
ES2298508T3 (es) 2008-05-16
NZ535889A (en) 2006-03-31
DE60318188D1 (de) 2008-01-31
EA200401194A1 (ru) 2005-04-28
CA2478156A1 (en) 2003-10-09
NO329386B1 (no) 2010-10-11
UA80120C2 (en) 2007-08-27
US6903215B2 (en) 2005-06-07
US20040023999A1 (en) 2004-02-05
ATE381333T1 (de) 2008-01-15
US7553966B2 (en) 2009-06-30
WO2003082280A1 (en) 2003-10-09
CO5611110A2 (es) 2006-02-28
RS82804A (sr) 2007-02-05
US8212040B2 (en) 2012-07-03
ECSP045315A (es) 2004-10-26
EP1490062A1 (en) 2004-12-29
US20050059714A1 (en) 2005-03-17
AU2003218342B8 (en) 2008-07-31
TW200306829A (en) 2003-12-01
UY27736A1 (es) 2003-10-31
NO20044031L (no) 2004-10-19
CL2010000375A1 (es) 2010-08-20
CN1633296A (zh) 2005-06-29
US20060189647A1 (en) 2006-08-24
IL163366A (en) 2010-11-30
NO20100827L (no) 2004-10-19

Similar Documents

Publication Publication Date Title
AU2003240947A8 (en) Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
PT1490062E (pt) Miméticos de glucocorticóides, métodos para a sua preparação, composições farmacêuticas e suas utilizações
TWI340138B (en) Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
AU2003230700A1 (en) Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
ZA200709430B (en) Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
EP1551376A4 (en) IMMUNOMODULATORY COMPOSITIONS, THEIR METHODS OF PREPARATION AND USE
IL164925A (en) Pharmaceuticals and kits containing combinations of valsartan, amlodipine and hydrochloride azide
HUP0500610A3 (en) Indazoles, benzothiazoles, and benzoisothiazoles, pharmaceutical compositions comprises thereof and their uses
AU2002363236A1 (en) Compounds, pharmaceutical compositions and methods of use therefor
HUP0401935A3 (en) Pharmaceutical composition based on micronized progesterone, preparation method and uses thereof
IL166621A0 (en) Polymorph of n-methyl-n-(3-ä-3-Ä2-thienylcarbonylÜ-pyrazol-Ä1,5-alphaÜpyrimidin-7-ylüacetamide and pharmaceutical compositions containing the same
AU2003239614A8 (en) Cardiolipin compositions, methods of preparation and use
IL209789A0 (en) Metabolites of 3-(2-dimethylaminomethyl-cyclohexyl)- phenol, pharmaceutical compositions comprising the same and uses thereof
AU2003291828A1 (en) Microspheres and related processes and pharmaceutical compositions
AU2003275268A8 (en) Hemostatic compositions and methods
GB0108470D0 (en) Pharmaceutical compositions and their use
AU2003297079A8 (en) Anti-filming materials, compositions and methods
AU2003297840A8 (en) Chemopreventive and therapeutic aspects of polyphenolic compositions and assays
PL374761A1 (en) N-benzodioxolyl, n-benzodioxanyl and n-benzodioxepinyl arylcarbonxamide derivatives, and pharmaceutical compositions comprising them
EP1556056A4 (en) X-Nitro Compounds, Pharmaceutical Compositions And Their Uses
HUP0401644A3 (en) Aminobenzoephenones, pharmaceutical compositions containing them and use thereof
HUP0303469A3 (en) Phtalazinon-derivatives, their use and pharmaceutical compositions containing them
AU2003295713A8 (en) Methods of providing controlled-release pharmaceutical compositions and controlled-release pharmaceutical compositions
IL153176A (en) Phenylpiperazines and pharmaceutical compositions comprising them
AU2003258772A8 (en) Novel neutracetical and pharmaceutical compositions and their uses