IL173271A - Affected derivatives of h1-pyrazole-3-carboxylic acid conserved in position 4, a process for preparing and using them to produce the drug - Google Patents

Affected derivatives of h1-pyrazole-3-carboxylic acid conserved in position 4, a process for preparing and using them to produce the drug

Info

Publication number
IL173271A
IL173271A IL173271A IL17327106A IL173271A IL 173271 A IL173271 A IL 173271A IL 173271 A IL173271 A IL 173271A IL 17327106 A IL17327106 A IL 17327106A IL 173271 A IL173271 A IL 173271A
Authority
IL
Israel
Prior art keywords
pyrazole
medicaments
substituted
manufacture
preparation
Prior art date
Application number
IL173271A
Other languages
English (en)
Hebrew (he)
Other versions
IL173271A0 (en
Original Assignee
Astex Therapeutics Ltd
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
Priority claimed from GBGB0317127.9A external-priority patent/GB0317127D0/en
Application filed by Astex Therapeutics Ltd filed Critical Astex Therapeutics Ltd
Publication of IL173271A0 publication Critical patent/IL173271A0/en
Publication of IL173271A publication Critical patent/IL173271A/en

Links

Classifications

    • 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
    • C07D231/14—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 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
    • C07D231/38—Nitrogen 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4152—1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • 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
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P31/20—Antivirals for DNA viruses
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C04—CEMENTS; CONCRETE; ARTIFICIAL STONE; CERAMICS; REFRACTORIES
    • C04B—LIME, MAGNESIA; SLAG; CEMENTS; COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDING MATERIALS; ARTIFICIAL STONE; CERAMICS; REFRACTORIES; TREATMENT OF NATURAL STONE
    • C04B35/00—Shaped ceramic products characterised by their composition; Ceramics compositions; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/622—Forming processes; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/626—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B
    • C04B35/63—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B using additives specially adapted for forming the products, e.g.. binder binders
    • C04B35/632—Organic additives
    • 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
    • C07D231/14—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 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
    • 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
    • C07D231/14—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 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
    • C07D231/38—Nitrogen atoms
    • C07D231/40—Acylated on said nitrogen atom
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D405/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • 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

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Ceramic Engineering (AREA)
  • Manufacturing & Machinery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Molecular Biology (AREA)
  • Diabetes (AREA)
  • Inorganic Chemistry (AREA)
  • Materials Engineering (AREA)
  • Structural Engineering (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Rheumatology (AREA)
IL173271A 2003-07-22 2006-01-19 Affected derivatives of h1-pyrazole-3-carboxylic acid conserved in position 4, a process for preparing and using them to produce the drug IL173271A (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US48904603P 2003-07-22 2003-07-22
GBGB0317127.9A GB0317127D0 (en) 2003-07-22 2003-07-22 Pharmaceutical compounds
US56976304P 2004-05-10 2004-05-10
PCT/GB2004/003179 WO2005012256A1 (en) 2003-07-22 2004-07-22 3, 4-disubstituted 1h-pyrazole compounds and their use as cyclin dependent kinases (cdk) and glycogen synthase kinase-3 (gsk-3) modulators

Publications (2)

Publication Number Publication Date
IL173271A0 IL173271A0 (en) 2006-06-11
IL173271A true IL173271A (en) 2016-03-31

Family

ID=34119458

Family Applications (1)

Application Number Title Priority Date Filing Date
IL173271A IL173271A (en) 2003-07-22 2006-01-19 Affected derivatives of h1-pyrazole-3-carboxylic acid conserved in position 4, a process for preparing and using them to produce the drug

Country Status (19)

Country Link
US (6) US7385059B2 (https=)
EP (2) EP2256106B1 (https=)
JP (1) JP4681548B2 (https=)
KR (1) KR101204247B1 (https=)
AU (1) AU2004261459B2 (https=)
BR (1) BRPI0412259B1 (https=)
CA (1) CA2532965C (https=)
CY (2) CY1112903T1 (https=)
EC (1) ECSP066298A (https=)
EG (1) EG27104A (https=)
IL (1) IL173271A (https=)
IS (1) IS2898B (https=)
MA (1) MA27936A1 (https=)
MX (1) MXPA06000794A (https=)
NO (1) NO335069B1 (https=)
NZ (1) NZ544756A (https=)
PL (2) PL1651612T3 (https=)
TN (1) TNSN06019A1 (https=)
WO (1) WO2005012256A1 (https=)

Families Citing this family (99)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2532965C (en) * 2003-07-22 2013-05-14 Astex Therapeutics Limited 3, 4-disubstituted 1h-pyrazole compounds and their use as cyclin dependent kinases (cdk) and glycogen synthase kinase-3 (gsk-3) modulators
MXPA06007326A (es) 2003-12-23 2007-01-26 Astex Therapeutics Ltd Derivados de pirazol como moduladores de proteina cinasa.
TW200533657A (en) * 2004-02-17 2005-10-16 Esteve Labor Dr Substituted pyrazoline compounds, their preparation and use as medicaments
WO2006070202A1 (en) * 2004-12-30 2006-07-06 Astex Therapeutics Limited Pyrazole derivatives having kinase modulating activity
EP1845975A1 (en) * 2005-01-21 2007-10-24 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors and further antitumor agents
US20080139620A1 (en) * 2005-01-21 2008-06-12 Astex Therapeutics Limited Pyrazole Derivatives For The Inhibition Of Cdk's And Gsk's
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
CN101146791B (zh) * 2005-01-21 2013-01-09 阿斯泰克斯治疗有限公司 作为激酶抑制剂的4-(2，6-二氯-苯甲酰基氨基)-1h-吡唑-3-甲酸哌啶-4-基酰胺的酸加成盐
CN101146532B (zh) 2005-01-21 2012-05-09 阿斯泰克斯治疗有限公司 药物化合物
AR053662A1 (es) * 2005-01-21 2007-05-16 Astex Therapeutics Ltd Compuestos de pirazol inhibidores de la actividad quinasa cdk y gsk
AR054425A1 (es) * 2005-01-21 2007-06-27 Astex Therapeutics Ltd Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico.
WO2008007113A2 (en) * 2006-07-14 2008-01-17 Astex Therapeutics Limited Pharmaceutical combinations
MX2007008781A (es) 2005-01-21 2007-09-11 Astex Therapeutics Ltd Compuestos farmaceuticos.
EP1847531A4 (en) * 2005-02-09 2009-04-22 Takeda Pharmaceutical PYRAZOLE DERIVATIVE
US20090036607A1 (en) * 2005-03-03 2009-02-05 Mitsubishi Rayon Co., Ltd. Polymer particle, resin composition containing same, and molded body
JP5154406B2 (ja) 2005-04-13 2013-02-27 アステックス、セラピューティックス、リミテッド 医薬化合物
JP2008543919A (ja) * 2005-06-21 2008-12-04 アステックス・セラピューティクス・リミテッド 医薬化合物
US8343953B2 (en) 2005-06-22 2013-01-01 Astex Therapeutics Limited Pharmaceutical compounds
WO2006136837A2 (en) 2005-06-23 2006-12-28 Astex Therapeutics Limited Pharmaceutical combinations comprising pyrazole derivatives as protein kinase modulators
EP1757587A1 (en) * 2005-07-15 2007-02-28 Laboratorios Del Dr. Esteve, S.A. Substituted pyrazoline compounds, their preparation and use as medicaments
US7897589B2 (en) * 2005-07-15 2011-03-01 Laboratorios Del Dr. Esteve, S.A. Substituted pyrazoline compounds, their preparation and use as medicaments
EP1743892A1 (en) 2005-07-15 2007-01-17 Laboratorios del Dr. Esteve S.A. Substituted pyrazoline compounds, their preparation and use as medicaments
EP1743890A1 (en) * 2005-07-15 2007-01-17 Laboratorios Del Dr. Esteve, S.A. 4,5-Dihydro-1H-pyrazole derivatives, their preparation and use as medicaments
EP2258358A3 (en) 2005-08-26 2011-09-07 Braincells, Inc. Neurogenesis with acetylcholinesterase inhibitor
EP2275095A3 (en) 2005-08-26 2011-08-17 Braincells, Inc. Neurogenesis by muscarinic receptor modulation
EP1940389A2 (en) 2005-10-21 2008-07-09 Braincells, Inc. Modulation of neurogenesis by pde inhibition
AU2006308889A1 (en) 2005-10-31 2007-05-10 Braincells, Inc. GABA receptor mediated modulation of neurogenesis
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
CA2648923A1 (en) 2006-04-11 2007-10-18 Vertex Pharmaceuticals Incorporated Thiazoles, imidazoles, and pyrazoles useful as inhibitors of protein kinases
US20090318500A1 (en) * 2006-05-05 2009-12-24 Astex Therapeutics Limited 4-(2, 6-Dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid (1-methanesulphonyl-piperidin-4-yl)-amide for the Treatment of Cancer
US20090142337A1 (en) * 2006-05-08 2009-06-04 Astex Therapeutics Limited Pharmaceutical Combinations of Diazole Derivatives for Cancer Treatment
EP2382975A3 (en) 2006-05-09 2012-02-29 Braincells, Inc. Neurogenesis by modulating angiotensin
JP4884072B2 (ja) * 2006-05-12 2012-02-22 三井化学アグロ株式会社 複素環誘導体ならびにその殺虫剤としての使用方法
EP2043635A2 (en) * 2006-06-29 2009-04-08 Astex Therapeutics Limited Pharmaceutical combinations
EP2046330A2 (en) * 2006-07-14 2009-04-15 Astex Therapeutics Limited Pharmaceutical combinations
JP2009543771A (ja) * 2006-07-14 2009-12-10 アステックス・セラピューティクス・リミテッド 医薬化合物
WO2008009954A1 (en) * 2006-07-21 2008-01-24 Astex Therapeutics Limited Medical use of cyclin dependent kinases inhibitors
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
AR063028A1 (es) 2006-10-06 2008-12-23 Banyu Pharma Co Ltd Derivados heterociclicos de piridin-2-carboxamida activadores de glucoquinasas, utiles para el tratamiento de diabetes y obesidad y composiciones farmaceuticas que los contienen.
JP5410285B2 (ja) * 2006-10-12 2014-02-05 アステックス、セラピューティックス、リミテッド 医薬化合物
WO2008044041A1 (en) 2006-10-12 2008-04-17 Astex Therapeutics Limited Pharmaceutical combinations
EP2073807A1 (en) 2006-10-12 2009-07-01 Astex Therapeutics Limited Pharmaceutical combinations
JP5518478B2 (ja) 2006-10-12 2014-06-11 アステックス、セラピューティックス、リミテッド 医薬化合物
GB0620259D0 (en) 2006-10-12 2006-11-22 Astex Therapeutics Ltd Pharmaceutical compounds
CN101573352A (zh) 2006-10-21 2009-11-04 艾博特股份有限两合公司 杂环化合物和其作为糖原合酶激酶3抑制剂的用途
KR100832747B1 (ko) * 2006-10-27 2008-05-27 한국화학연구원 아미노피라졸 유도체, 이의 제조 방법 및 이를 함유하는허혈성 질환의 예방 또는 치료용 조성물
FR2908409B1 (fr) 2006-11-10 2009-01-09 Sanofi Aventis Sa Pyrazoles substituees,compositions les contenant,procede de fabrication et utilisation
GB0704932D0 (en) 2007-03-14 2007-04-25 Astex Therapeutics Ltd Pharmaceutical compounds
WO2009036022A1 (en) * 2007-09-10 2009-03-19 Board Of Regents, The University Of Texas System Enhancement of polysaccharide-mediated nucleic acid delivery
EP2070916A1 (de) 2007-12-10 2009-06-17 Bayer Schering Pharma Aktiengesellschaft 2-Aryl-thiazol-4-carbonsäureamid-Derivate, deren Herstellung und Verwendung als Arzneimittel
EP2070925A1 (de) 2007-12-10 2009-06-17 Bayer Schering Pharma Aktiengesellschaft Neue 2-substituierte Tiazol-4-carbonsäureamid-Derivative deren Herstellung und Verwendung als Arzneimittel
EP2070924A1 (de) 2007-12-10 2009-06-17 Bayer Schering Pharma Aktiengesellschaft Neue 2-Hetarylthiazol-4-carbonsäureamid-Derivative, deren Herstellung und Verwendung als Arzneimittel
EP2085397A1 (en) * 2008-01-21 2009-08-05 Esteve Quimica, S.A. Crystalline form of abacavir
GB0806527D0 (en) 2008-04-11 2008-05-14 Astex Therapeutics Ltd Pharmaceutical compounds
EP2151234A1 (en) * 2008-07-28 2010-02-10 Laboratorios Del. Dr. Esteve, S.A. Pharmaceutical formulation comprising a CB1-receptor compound in a solid solution and/or solid dispersion
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
WO2011090738A2 (en) 2009-12-29 2011-07-28 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
WO2012002527A1 (ja) * 2010-07-02 2012-01-05 あすか製薬株式会社 複素環化合物及びｐ２７Ｋｉｐ１分解阻害剤
MX336726B (es) 2010-09-27 2016-01-27 Abbott Gmbh & Co Kg Compuestos heterociclicos y su uso como inhibidores de la glucogeno sintasa quinasa-3.
US9090592B2 (en) 2010-12-30 2015-07-28 AbbVie Deutschland GmbH & Co. KG Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors
US9382239B2 (en) 2011-11-17 2016-07-05 Dana-Farber Cancer Institute, Inc. Inhibitors of c-Jun-N-terminal kinase (JNK)
WO2013106432A1 (en) * 2012-01-09 2013-07-18 X-Rx, Inc. Benzhydrol-pyrazole derivatives having kinase inhibitory activity and uses thereof
WO2013126283A1 (en) 2012-02-20 2013-08-29 E. I. Du Pont De Nemours And Company Fungicidal pyrazoles
PH12017500997A1 (en) 2012-04-04 2018-02-19 Samumed Llc Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof
CN103012428A (zh) * 2013-01-08 2013-04-03 中国药科大学 4-(五元杂环并嘧啶/吡啶取代)氨基-1H-3-吡唑甲酰胺类CDK/Aurora双重抑制剂及其用途
US9572815B2 (en) 2013-03-15 2017-02-21 St. Jude Children's Research Hospital Methods and compositions of p27KIP1 transcriptional modulators
WO2014165851A1 (en) 2013-04-05 2014-10-09 The Children's Hospital Of Philadelphia Transient up-regulation of myc in b-cell lymphomas
GB201313664D0 (en) * 2013-07-31 2013-09-11 Univ Cardiff Bcl-3 inhibitors
FR3011239A1 (fr) * 2013-10-01 2015-04-03 Univ Claude Bernard Lyon Nouveaux derives comprenant un groupe pyrazole et un groupe indole, utiles en tant qu'inhibiteurs de la kinase gsk3
EP3057956B1 (en) 2013-10-18 2021-05-05 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2015058126A1 (en) 2013-10-18 2015-04-23 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
US9830586B2 (en) * 2014-03-31 2017-11-28 Ncr Corporation Electronic payments
JP6854762B2 (ja) 2014-12-23 2021-04-07 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド サイクリン依存性キナーゼ７（ｃｄｋ７）の阻害剤
WO2016140501A1 (en) * 2015-03-04 2016-09-09 Kainos Medicine, Inc. Pyridine n-oxide for enhancer of zeste homolog 2 inhibitors
US10155765B2 (en) 2015-03-12 2018-12-18 Merck Sharp & Dohme Corp. Carboxamide inhibitors of IRAK4 activity
USRE50776E1 (en) 2015-03-27 2026-02-03 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
US20180161340A1 (en) 2015-06-18 2018-06-14 St. Jude Children's Research Hospital Methods and compositions for the prevention and treatment of hearing loss
AU2016319125B2 (en) 2015-09-09 2021-04-08 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
ES2969565T3 (es) 2015-09-30 2024-12-13 Max Planck Ges Zur Foerderung Derwissenschaften E V Derivados heteroarílicos como inhibidores de la sepiapterina reductasa
MX380092B (es) 2015-11-06 2025-03-11 Samumed Llc Tratamiento de la osteoartritis.
AR108325A1 (es) 2016-04-27 2018-08-08 Samumed Llc Isoquinolin-3-il carboxamidas y preparación y uso de las mismas
MX390577B (es) 2016-06-01 2025-03-20 Samumed Llc Proceso de preparación de n-(5-(3-(7-(3-fluorofenil)-3h-imidazo[4,5-c]piridin-2-il)-1h-indazol-5-il)piridin-3-il)-3-metilbutanamida.
BR112019003722A2 (pt) 2016-08-23 2019-05-28 Eisai R&D Man Co Ltd terapias de combinação para o tratamento de carcinoma hepatocelular
MX2019010981A (es) 2017-03-16 2020-09-07 Eisai R&D Man Co Ltd Terapias de combinacion para el tratamiento de cancer de mama.
CN109705090B (zh) * 2017-10-25 2023-06-20 上海君实生物医药科技股份有限公司 3,4-二取代的1h-吡唑化合物的酒石酸加成盐及其晶型
GEP20227433B (en) 2018-04-26 2022-10-25 Pfizer 2-amino-pyridine or 2-amino-pyrimidine derivatives as cyclin dependent kinase inhibitors
EP3810132A4 (en) * 2018-06-25 2022-06-22 Dana-Farber Cancer Institute, Inc. TAIRE FAMILY KINASE INHIBITORS AND RELATED USES
EP3813826A4 (en) * 2018-06-26 2022-07-06 BioSplice Therapeutics, Inc. METHOD OF TREATMENT OF CANCER USING A CLK INHIBITOR
US11945803B2 (en) 2018-08-07 2024-04-02 Tosk, Inc. Modulators of RAS GTPase
US12281126B2 (en) 2018-12-28 2025-04-22 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
WO2020146779A1 (en) * 2019-01-11 2020-07-16 The Regents Of The University Of California mTORC1 INHIBITORS FOR ACTIVATING AUTOPHAGY
US20230000842A1 (en) * 2019-01-17 2023-01-05 Samumed, Llc Methods of treating cartilage disorders through inhibition of clk and dyrk
WO2020150545A1 (en) * 2019-01-17 2020-07-23 Samumed, Llc Pyrazole derivatives as modulators of the wnt/b-catenin signaling pathway
WO2020159942A1 (en) 2019-01-29 2020-08-06 Tosk, Inc. Pyrazolopyrimidine modulators of ras gtpase
WO2020214537A1 (en) 2019-04-15 2020-10-22 Tosk, Inc. Modulators of ras gtpase
US11857551B1 (en) 2020-07-10 2024-01-02 Ting Therapeutics Llc Methods for the prevention and treatment of hearing loss
US12180220B2 (en) 2020-10-14 2024-12-31 Tosk, Inc. Heteroaryl modulators of RAS GTPase
CN115124527B (zh) * 2022-05-31 2024-03-12 武汉智汇农耀科技有限公司 一种杂环酰胺-氮杂吲哚类化合物及其制备方法和应用、一种除草剂
WO2026024674A1 (en) 2024-07-22 2026-01-29 Genesis Therapeutics, Inc. Methods of treating skp2-associated cancers

Family Cites Families (164)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2917432A (en) 1954-10-05 1959-12-15 Burroughs Wellcome Co Leukemia treatment
US3046301A (en) 1959-10-29 1962-07-24 Burroughs Wellcome Co Method of making chlorambucil
GB1354939A (en) 1971-10-28 1974-06-05 Ici Ltd Process for the manufacture of 1,1,2-triphenylalk-1-enes
US4005063A (en) 1973-10-11 1977-01-25 Abbott Laboratories [Des-gly]10 -GnRH nonapeptide anide analogs in position 6 having ovulation-inducing activity
GB1524747A (en) 1976-05-11 1978-09-13 Ici Ltd Polypeptide
US4282361A (en) * 1978-03-16 1981-08-04 Massachusetts Institute Of Technology Synthesis for 7-alkylamino-3-methylpyrazolo [4,3-d]pyrimidines
DE2845574A1 (de) 1978-10-19 1980-04-24 Deutsches Krebsforsch Durch heterocyclische ringe oder alkylreste substituierte analoga von ccnu und verfahren zu deren herstellung
ATE28864T1 (de) 1982-07-23 1987-08-15 Ici Plc Amide-derivate.
US4666828A (en) 1984-08-15 1987-05-19 The General Hospital Corporation Test for Huntington's disease
US4683202A (en) 1985-03-28 1987-07-28 Cetus Corporation Process for amplifying nucleic acid sequences
US4801531A (en) 1985-04-17 1989-01-31 Biotechnology Research Partners, Ltd. Apo AI/CIII genomic polymorphisms predictive of atherosclerosis
US4978672A (en) 1986-03-07 1990-12-18 Ciba-Geigy Corporation Alpha-heterocyclc substituted tolunitriles
JPS6425763A (en) 1987-04-24 1989-01-27 Mitsubishi Chem Ind Pyrazoles and insecticide and acaricide containing said pyrazoles as active ingredient
US5164196A (en) 1987-05-19 1992-11-17 Ventech Research, Inc. Crotoxin complex as cytotoxic agent
EP0308020A3 (en) 1987-09-18 1990-12-05 Merck & Co. Inc. 5-(aryl and heteroaryl)-6-(aryl and heteroaryl)-1,2-dihydro-2-oxo 3-pyridinecarboxylic acids and derivatives thereof
US5002755A (en) 1988-02-18 1991-03-26 Vanderbilt University Method of controlling nephrotoxicity of anti-tumor plaintum compounds
US5272057A (en) 1988-10-14 1993-12-21 Georgetown University Method of detecting a predisposition to cancer by the use of restriction fragment length polymorphism of the gene for human poly (ADP-ribose) polymerase
US5192659A (en) 1989-08-25 1993-03-09 Genetype Ag Intron sequence analysis method for detection of adjacent and remote locus alleles as haplotypes
WO1991018599A2 (de) 1990-05-26 1991-12-12 Byk Gulden Lomberg Chemische Fabrik Gmbh 1,4-dihydropyridine zur anwendung bei der überwindung von arzneimittelresistenzen
FR2665898B1 (fr) 1990-08-20 1994-03-11 Sanofi Derives d'amido-3 pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant.
IL100110A0 (en) 1990-12-26 1992-08-18 American Cyanamid Co Insecticidal and synergistic miticidal compositions
PL170837B1 (pl) 1991-10-18 1997-01-31 Monsanto Co S rod ek g r zybobó j c zy PL PL PL PL PL PL
DK0752248T3 (da) 1992-11-13 2000-11-13 Idec Pharma Corp Terapeutisk anvendelse af kimæriske og radioaktivt mærkede antistoffer mod humant B-lymfocytbegrænset differentieringsantig
CZ284157B6 (cs) 1992-12-17 1998-08-12 Pfizer Inc. Pyrazolové a pyrazolopyrimidinové sloučeniny jako takové a pro léčbu chorob a farmaceutické prostředky na jejich bázi
JP3156026B2 (ja) 1993-12-27 2001-04-16 株式会社大塚製薬工場 ホスホン酸ジエステル誘導体
US5773001A (en) 1994-06-03 1998-06-30 American Cyanamid Company Conjugates of methyltrithio antitumor agents and intermediates for their synthesis
WO1996014843A2 (en) 1994-11-10 1996-05-23 Cor Therapeutics, Inc. Pharmaceutical pyrazole compositions useful as inhibitors of protein kinases
US5502068A (en) 1995-01-31 1996-03-26 Synphar Laboratories, Inc. Cyclopropylpyrroloindole-oligopeptide anticancer agents
GB9514380D0 (en) 1995-07-13 1995-09-13 Knoll Ag Therapeutic agents
EP0951541B1 (en) 1995-07-31 2005-11-30 Urocor, Inc. Biomarkers and targets for diagnosis, prognosis and management of prostate disease
US6218529B1 (en) 1995-07-31 2001-04-17 Urocor, Inc. Biomarkers and targets for diagnosis, prognosis and management of prostate, breast and bladder cancer
US5675024A (en) 1995-11-22 1997-10-07 Allergan Aryl or heteroaryl amides of tetrahydronaphthalene, chroman, thiochroman and 1,2,3,4,-tetrahydroquinoline carboxylic acids, having an electron withdrawing substituent in the aromatic or heteroaromatic moiety, having retinoid-like biological activity
US5663357A (en) 1995-11-22 1997-09-02 Allergan Substituted heteroarylamides having retinoid-like biological activity
AU703203B2 (en) 1996-01-30 1999-03-18 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
CA2249665A1 (en) 1996-04-03 1997-10-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
WO1997036585A1 (en) 1996-04-03 1997-10-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AU716381B2 (en) 1996-04-03 2000-02-24 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AU2381397A (en) 1996-04-19 1997-11-12 Novo Nordisk A/S Modulators of molecules with phosphotyrosine recognition units
US6057122A (en) 1996-05-03 2000-05-02 Abbott Laboratories Antiangiogenic peptides polynucleotides encoding same and methods for inhibiting angiogenesis
JP2000511558A (ja) 1996-06-21 2000-09-05 アラーガン・セイルズ・インコーポレイテッド レチノイドおよび／またはレチノイド拮抗剤様生物学的活性を有する置換テトラヒドロナフタレンおよびジヒドロナフタレン誘導体
US6268308B1 (en) 1996-08-27 2001-07-31 Syngenta Crop Protection, Inc. Herbicidal S-substituted 1,2,4,6-thiatriazines
TW523506B (en) 1996-12-18 2003-03-11 Ono Pharmaceutical Co Sulfonamide or carbamide derivatives and drugs containing the same as active ingredients
AU730224B2 (en) 1996-12-23 2001-03-01 Du Pont Pharmaceuticals Company Nitrogen containing heteroaromatics as factor Xa inhibitors
US6020357A (en) 1996-12-23 2000-02-01 Dupont Pharmaceuticals Company Nitrogen containing heteroaromatics as factor Xa inhibitors
US6306393B1 (en) 1997-03-24 2001-10-23 Immunomedics, Inc. Immunotherapy of B-cell malignancies using anti-CD22 antibodies
US6723719B1 (en) * 1997-04-25 2004-04-20 Pfizer Inc Pyrazolopyrimidinones which inhibit type 5 cyclic guanosine 3′,5′—monophosphate phosphodiesterase (cGMP PDE5) for the treatment of sexual dysfunction
EP1019394A1 (en) * 1997-05-22 2000-07-19 G.D. Searle & Co. PYRAZOLE DERIVATIVES AS p38 KINASE INHIBITORS
SK174699A3 (en) 1997-06-19 2000-08-14 Du Pont Pharm Co Inhibitors of factor xa with a neutral p1 specificity group
PL342447A1 (en) 1997-10-27 2001-06-04 Agouron Pharma Substituted 4-amino thiazol-2-yl compounds as inhibitors of cyclin-dependent kinases
ATE260103T1 (de) 1997-12-19 2004-03-15 Schering Ag Ortho-anthranilamide derivate als antikoagulantien
EP1042299A1 (en) 1997-12-22 2000-10-11 Du Pont Pharmaceuticals Company Nitrogen containing heteroaromatics with ortho-substituted p1's as factor xa inhibitors
WO1999067235A1 (en) 1998-06-25 1999-12-29 Sumitomo Pharmaceuticals Co., Ltd. Five-membered ring compounds
WO2000006169A1 (en) 1998-07-29 2000-02-10 Merck & Co., Inc. Integrin receptor antagonists
JP2000186092A (ja) 1998-12-22 2000-07-04 Kyowa Hakko Kogyo Co Ltd Ｕｃｎ−０１の製造法
CA2348740A1 (en) 1998-12-23 2000-07-06 Ruth R. Wexler Thrombin or factor xa inhibitors
EP1175419B1 (en) 1999-04-02 2003-05-28 Bristol-Myers Squibb Pharma Company Aryl sulfonyls as factor xa inhibitors
EP1169038B9 (en) 1999-04-15 2013-07-10 Bristol-Myers Squibb Company Cyclic protein tyrosine kinase inhibitors
US6166244A (en) 1999-05-07 2000-12-26 Allergan Sales, Inc. Oxygen, sulfur and nitrogen substituted cyclohexene and cyclohexane derivatives having retinoid-like biological activity
AU5284000A (en) 1999-05-24 2000-12-12 Cor Therapeutics, Inc. Inhibitors of factor xa
FR2795726A1 (fr) 1999-06-30 2001-01-05 Aventis Cropscience Sa Nouveaux pyrazoles fongicides
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
US6127382A (en) 1999-08-16 2000-10-03 Allergan Sales, Inc. Amines substituted with a tetrahydroquinolinyl group an aryl or heteroaryl group and an alkyl group, having retinoid-like biological activity
US6093838A (en) 1999-08-16 2000-07-25 Allergan Sales, Inc. Amines substituted with a dihydro-benzofuranyl or with a dihydro-isobenzofuranyl group, an aryl or heteroaryl group and an alkyl group, having retinoid-like biological activity
AU6936500A (en) 1999-08-24 2001-03-19 Regents Of The University Of California, The Non-quinoline inhibitors of malaria parasites
CZ2002959A3 (cs) 1999-09-17 2002-07-17 Millennium Pharmaceuticals, Inc. Inhibitory faktoru Xa
ES2316383T3 (es) 1999-09-17 2009-04-16 Millennium Pharmaceuticals, Inc. Benzamidas e inhibidores relacionados del factor xa.
US6632815B2 (en) 1999-09-17 2003-10-14 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
JP2003513075A (ja) 1999-11-05 2003-04-08 スミスクライン ビーチャム パブリック リミテッド カンパニー 複合５ｈｔ１ａ、５ｈｔ１ｂおよび５ｈｔ１ｄ受容体活性を有するイソキノリンおよびキナゾリン誘導体
YU54202A (sh) 2000-01-18 2006-01-16 Agouron Pharmaceuticals Inc. Jedinjenja indazola, farmaceutske smeše i postupci za stimulisanje i inhibiranje ćelijske proliferacije
HN2001000008A (es) 2000-01-21 2003-12-11 Inc Agouron Pharmaceuticals Compuesto de amida y composiciones farmaceuticas para inhibir proteinquinasas, y su modo de empleo
EP1259887A4 (en) 2000-01-25 2003-08-13 Vistaprint Usa Inc Managing print jobs
KR20010111298A (ko) 2000-02-05 2001-12-17 버텍스 파마슈티칼스 인코포레이티드 Ｅｒｋ의 억제제로서 유용한 피라졸 조성물
WO2001058869A2 (en) 2000-02-11 2001-08-16 Bristol-Myers Squibb Company Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators in treating respiratory and non-respiratory diseases
WO2001064642A2 (en) 2000-02-29 2001-09-07 Cor Therapeutics, Inc. Benzamides and related inhibitors of factor xa
AU2001241128A1 (en) 2000-03-14 2001-09-24 Fujisawa Pharmaceutical Co. Ltd. Novel amide compounds
MY138097A (en) 2000-03-22 2009-04-30 Du Pont Insecticidal anthranilamides
US6613917B1 (en) 2000-03-23 2003-09-02 Allergan, Inc. Amines substituted with a dihydronaphthalenyl, chromenyl, or thiochromenyl group, an aryl or heteroaryl group and an alkyl group, having retinoid-like biological activity
CN100355751C (zh) 2000-03-29 2007-12-19 西克拉塞尔有限公司 2－取代的4－杂芳基－嘧啶、其组合物及其用途
MXPA02010222A (es) * 2000-04-18 2003-05-23 Agouron Pharma Pirazoles para inhibir proteina cinasa.
WO2001081345A1 (en) 2000-04-20 2001-11-01 Mitsubishi Pharma Corporation Aromatic amide compounds
JP2004507455A (ja) 2000-04-25 2004-03-11 ブリストル−マイヤーズ　スクイブ　カンパニー サイクリン依存性キナーゼ阻害剤としての、５−チオ−、スルフィニル−およびスルホニルピラゾロ［３，４−ｂ］−ピリジンの用途
WO2001081316A2 (en) 2000-04-27 2001-11-01 Abbott Laboratories Substituted phenyl farnesyltransferase inhibitors
US6414013B1 (en) 2000-06-19 2002-07-02 Pharmacia & Upjohn S.P.A. Thiophene compounds, process for preparing the same, and pharmaceutical compositions containing the same background of the invention
AU2001273040A1 (en) 2000-06-27 2002-01-08 Du Pont Pharmaceuticals Company Factor xa inhibitors
BR0112856A (pt) 2000-07-31 2003-07-01 Smithkline Beecham Plc Método para o tratamento dos distúrbios, composto ou um sal ou solvato deste, processo para a preparação dos mesmos, composição farmacêutico, método de tratamento e/ou profilaxia de um ou mais dos distúrbios, uso de um composto, e, método para o tratamento de diabetes, grande depressão, depressão manìaca, ansiedade, esquizofrenia e distúrbios do sono, em mamìferos humanos e não humanos
NZ523656A (en) * 2000-08-31 2004-11-26 Pfizer Prod Inc Pyrazole derivatives and their use as protein kinase inhibitors
WO2002022605A1 (en) 2000-09-15 2002-03-21 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
AU2001212168A1 (en) 2000-10-20 2002-05-06 Bristol-Myers Squibb Pharma Company Acylsemicarbazides and their use as cyclin dependent kinase (CDK) inhibitors
US6455559B1 (en) * 2001-07-19 2002-09-24 Pharmacia Italia S.P.A. Phenylacetamido-pyrazole derivatives, process for their preparation and their use as antitumor agents
US6989385B2 (en) 2000-12-21 2006-01-24 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
DE10064823A1 (de) 2000-12-22 2002-06-27 Knoll Ag Integrinrezeptorliganden
US7105682B2 (en) * 2001-01-12 2006-09-12 Amgen Inc. Substituted amine derivatives and methods of use
US6878714B2 (en) 2001-01-12 2005-04-12 Amgen Inc. Substituted alkylamine derivatives and methods of use
US6995162B2 (en) * 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
GB0102687D0 (en) 2001-02-02 2001-03-21 Pharmacia & Upjohn Spa Oxazolyl-pyrazole derivatives active as kinase inhibitors,process for their preparation and pharmaceutical compositions comprising them
MY130778A (en) 2001-02-09 2007-07-31 Vertex Pharma Heterocyclic inhibitiors of erk2 and uses thereof
CN1492758A (zh) 2001-02-28 2004-04-28 C���ֶ� 抗肿瘤和抗转移作用的方法和制剂
ES2364550T3 (es) 2001-03-05 2011-09-06 E. I. Du Pont De Nemours And Company Agentes de control de plagas de invertebrados de diamidas heterocíclicas.
DE10110750A1 (de) 2001-03-07 2002-09-12 Bayer Ag Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften
GB0106661D0 (en) * 2001-03-16 2001-05-09 Pfizer Ltd Pharmaceutically active compounds
WO2002074312A1 (en) * 2001-03-16 2002-09-26 Pfizer Limited Pyrazolo`4,3-d.pyrimidinone compounds as cgmp pde inhibitors
JPWO2002074298A1 (ja) 2001-03-21 2004-07-08 小野薬品工業株式会社 Ｉｌ−６産生阻害剤
CN1289471C (zh) 2001-04-16 2006-12-13 先灵公司 作为cxc－趋化因子受体配体的3,4－二取代的环丁烯－1,2－二酮
US6905669B2 (en) 2001-04-24 2005-06-14 Supergen, Inc. Compositions and methods for reestablishing gene transcription through inhibition of DNA methylation and histone deacetylase
US6989245B2 (en) 2001-05-11 2006-01-24 The Burnham Institute Screening, diagnostic and therapeutic methods relating to RIZ
WO2002094183A2 (en) 2001-05-18 2002-11-28 Tap Pharmaceutical Products Inc. A method for tumor treatment with fumagillol derivatives
RU2299198C2 (ru) 2001-05-21 2007-05-20 Е.И.Дюпон Де Немур Энд Компани Диамиды антраниловой кислоты, способ борьбы с насекомыми, композиция для борьбы с насекомыми
US20030236198A1 (en) 2001-06-13 2003-12-25 Genesoft, Inc. Antipathogenic benzamide compounds
EP1423380B1 (en) 2001-08-03 2010-12-15 Vertex Pharmaceuticals Incorporated Pyrazole-derived kinase inhibitors and uses thereof
WO2003011287A1 (en) 2001-08-03 2003-02-13 Vertex Pharmaceuticals Incorporated Pyrazolon derivatives as inhibitors of gsk-3
US20030078232A1 (en) 2001-08-08 2003-04-24 Elfatih Elzein Adenosine receptor A3 agonists
AUPR738301A0 (en) 2001-08-30 2001-09-20 Starpharma Limited Chemotherapeutic agents
CA2457922A1 (en) 2001-08-31 2003-03-13 University Of Connecticut Novel pyrazole analogs acting on cannabinoid receptors
CN101851173A (zh) 2001-09-14 2010-10-06 梅特希尔基因公司 组蛋白脱乙酰化酶抑制剂
JP2005505595A (ja) 2001-10-12 2005-02-24 シェーリング　コーポレイション Ｃｘｃ−ケモカインレセプターアンタゴニストとしての３，４−二置換マレイミド化合物
HN2002000317A (es) * 2001-11-02 2003-05-21 Pfizer Inhibidores de pde9 para tratamiento de trastornos cardiovasculares
CA2466375A1 (en) 2001-11-08 2003-05-15 Pharmacia & Upjohn Company Azabicyclic-substituted-heteroaryl compounds for the treatment of disease
WO2003048081A2 (en) 2001-12-04 2003-06-12 Bristol-Myers Squibb Company Glycinamides as factor xa inhibitors
US20030166932A1 (en) 2002-01-04 2003-09-04 Beard Richard L. Amines substituted with a dihydronaphthalenyl, chromenyl, or thiochromenyl group, an aryl or heteroaryl group and an alkyl group, having retinoid-like biological activity
MXPA04005939A (es) 2002-01-22 2005-01-25 Warner Lambert Co 2-(piridin-2-ilamino)-pirido[2,3-d]pirimidin-7-onas.
US7205307B2 (en) 2002-02-14 2007-04-17 Icagen, Inc. Pyrimidines as novel openers of potassium ion channels
CN101259120B (zh) 2002-03-04 2012-07-04 Hdac默克研究有限责任公司 辛二酰苯胺异羟肟酸或其可药用盐在制备诱导末期分化的药物的用途
EP1485093B1 (en) 2002-03-12 2010-11-03 Merck Sharp & Dohme Corp. Di-aryl substituted tetrazole modulators of metabotropic glutamate receptor-5
ATE478872T1 (de) * 2002-03-28 2010-09-15 Ustav Ex Botan Av Cr V V I I O Pyrazoloä4,3-düpyrimidine, verfahren zu ihrer herstellung und therapeutische anwendung
US6995168B2 (en) 2002-05-31 2006-02-07 Euro-Celtique S.A. Triazaspiro compounds useful for treating or preventing pain
AU2003249369A1 (en) 2002-06-21 2004-01-06 Cellular Genomics, Inc. Certain amino-substituted monocycles as kinase modulators
ATE425753T1 (de) 2002-08-02 2009-04-15 Genesoft Pharmaceuticals Inc Biaryl-verbindungen mit antiinfektiver wirkung
GB0218625D0 (en) 2002-08-10 2002-09-18 Astex Technology Ltd Pharmaceutical compounds
MY133311A (en) 2002-09-19 2007-11-30 Schering Corp Novel imidazopyridines as cyclin dependent kinase inhibitors
US6737382B1 (en) 2002-10-23 2004-05-18 Nippon Soda Co. Ltd. Insecticidal aminothiazole derivatives
WO2004039795A2 (en) 2002-10-29 2004-05-13 Fujisawa Pharmaceutical Co., Ltd. Amide compounds for the treatment of hyperlipidemia
US20050026877A1 (en) 2002-12-03 2005-02-03 Novacea, Inc. Pharmaceutical compositions comprising active vitamin D compounds
US7202257B2 (en) 2003-12-24 2007-04-10 Deciphera Pharmaceuticals, Llc Anti-inflammatory medicaments
US7144911B2 (en) 2002-12-31 2006-12-05 Deciphera Pharmaceuticals Llc Anti-inflammatory medicaments
KR101076018B1 (ko) 2003-01-08 2011-10-21 유니버시티 오브 워싱톤 항균제
US7169797B2 (en) 2003-02-14 2007-01-30 Abbott Laboratories Protein-tyrosine phosphatase inhibitors and uses thereof
US7320989B2 (en) * 2003-02-28 2008-01-22 Encysive Pharmaceuticals, Inc. Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-II receptor antagonists
TW200505902A (en) 2003-03-20 2005-02-16 Schering Corp Cannabinoid receptor ligands
EP2385041B1 (en) 2003-05-01 2013-09-18 Bristol-Myers Squibb Company Pyrazole-amine compounds useful as kinase inhibitors
WO2004099127A1 (en) 2003-05-07 2004-11-18 Novo Nordisk A/S Novel compounds as kinase inhibitors
MXPA05012081A (es) 2003-05-09 2006-02-22 Pharmacia & Upjohn Co Llc Derivados de pirimidina sustituidos.
WO2005000309A2 (en) 2003-06-27 2005-01-06 Ionix Pharmaceuticals Limited Chemical compounds
WO2005000356A1 (ja) 2003-06-27 2005-01-06 Ono Pharmaceutical Co., Ltd. 尿路疾患治療剤
TWI372050B (en) * 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
CA2532965C (en) * 2003-07-22 2013-05-14 Astex Therapeutics Limited 3, 4-disubstituted 1h-pyrazole compounds and their use as cyclin dependent kinases (cdk) and glycogen synthase kinase-3 (gsk-3) modulators
SE0303396D0 (sv) 2003-12-16 2003-12-16 Astrazeneca Ab Chemical compounds
EP1718306A2 (en) 2004-02-20 2006-11-08 Chiron Corporation Modulation of inflammatory and metastatic processes
EA012451B1 (ru) 2004-03-11 2009-10-30 4Сц Аг Новые амидозамещённые гидрокси-6-фенилфенантридины
US20060084691A1 (en) 2004-10-18 2006-04-20 Bilal Piperdi Combined treatment with bortezomib and an epidermal growth factor receptor kinase inhibitor
MX2007008781A (es) * 2005-01-21 2007-09-11 Astex Therapeutics Ltd Compuestos farmaceuticos.
US20080139620A1 (en) * 2005-01-21 2008-06-12 Astex Therapeutics Limited Pyrazole Derivatives For The Inhibition Of Cdk's And Gsk's
EP1845975A1 (en) * 2005-01-21 2007-10-24 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors and further antitumor agents
AR054425A1 (es) 2005-01-21 2007-06-27 Astex Therapeutics Ltd Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico.
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
AR053662A1 (es) * 2005-01-21 2007-05-16 Astex Therapeutics Ltd Compuestos de pirazol inhibidores de la actividad quinasa cdk y gsk
CN101146532B (zh) * 2005-01-21 2012-05-09 阿斯泰克斯治疗有限公司 药物化合物
WO2008007113A2 (en) 2006-07-14 2008-01-17 Astex Therapeutics Limited Pharmaceutical combinations
US20090318500A1 (en) 2006-05-05 2009-12-24 Astex Therapeutics Limited 4-(2, 6-Dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid (1-methanesulphonyl-piperidin-4-yl)-amide for the Treatment of Cancer
US20090142337A1 (en) * 2006-05-08 2009-06-04 Astex Therapeutics Limited Pharmaceutical Combinations of Diazole Derivatives for Cancer Treatment
EP2043635A2 (en) 2006-06-29 2009-04-08 Astex Therapeutics Limited Pharmaceutical combinations
EP2046330A2 (en) 2006-07-14 2009-04-15 Astex Therapeutics Limited Pharmaceutical combinations
JP2009543771A (ja) 2006-07-14 2009-12-10 アステックス・セラピューティクス・リミテッド 医薬化合物
WO2008009954A1 (en) 2006-07-21 2008-01-24 Astex Therapeutics Limited Medical use of cyclin dependent kinases inhibitors
WO2008044041A1 (en) 2006-10-12 2008-04-17 Astex Therapeutics Limited Pharmaceutical combinations

Also Published As

Publication number Publication date
MA27936A1 (fr) 2006-06-01
AU2004261459A1 (en) 2005-02-10
IS8310A (is) 2006-02-17
JP2006528163A (ja) 2006-12-14
US7825140B2 (en) 2010-11-02
EG27104A (en) 2015-06-09
CA2532965A1 (en) 2005-02-10
EP1651612B9 (en) 2012-09-05
NO335069B1 (no) 2014-09-01
EP1651612B1 (en) 2012-04-11
KR101204247B1 (ko) 2012-11-22
US7385059B2 (en) 2008-06-10
US20140371213A1 (en) 2014-12-18
WO2005012256A1 (en) 2005-02-10
NO20060855L (no) 2006-04-21
US7745638B2 (en) 2010-06-29
EP2256106B1 (en) 2015-05-06
WO2005012256A8 (en) 2005-04-07
US20110003799A1 (en) 2011-01-06
PL2256106T3 (pl) 2015-08-31
US20120213791A1 (en) 2012-08-23
BRPI0412259A (pt) 2006-08-22
NZ544756A (en) 2009-09-25
US9051278B2 (en) 2015-06-09
CY1112903T1 (el) 2016-04-13
CY1116298T1 (el) 2017-02-08
AU2004261459B2 (en) 2008-06-26
TNSN06019A1 (en) 2007-10-03
BRPI0412259B1 (pt) 2019-08-20
US20060194843A1 (en) 2006-08-31
US20080269207A1 (en) 2008-10-30
IL173271A0 (en) 2006-06-11
IS2898B (is) 2014-09-15
US8080666B2 (en) 2011-12-20
ECSP066298A (es) 2006-07-28
EP2256106A1 (en) 2010-12-01
KR20060113637A (ko) 2006-11-02
JP4681548B2 (ja) 2011-05-11
EP1651612A1 (en) 2006-05-03
US8779147B2 (en) 2014-07-15
US20080200509A1 (en) 2008-08-21
HK1090041A1 (en) 2006-12-15
PL1651612T3 (pl) 2012-09-28
CA2532965C (en) 2013-05-14
MXPA06000794A (es) 2006-08-23

Similar Documents

Publication Publication Date Title
IL173271A (en) Affected derivatives of h1-pyrazole-3-carboxylic acid conserved in position 4, a process for preparing and using them to produce the drug
IL166058A0 (en) Novel thiophenylglycoside derivatives methods for production thereof medicaments comprising said compounds and use thereof
IL167038A (en) Pyrazole derivatives, pharmaceutical compositions containing the same, use thereof in the manufacture of medicaments and intermediate for production thereof
PL378168A1 (pl) Dihydropterydynony, sposoby ich wytwarzania i ich zastosowanie w postaci leków
AU2003289872A8 (en) Novel xanthin derivatives, production and use thereof as medicaments
IL164292A (en) Quinoline and isoquinoline derivatives, method for the production thereof and use thereof in the manufacture of medicaments
IL173204A0 (en) Novel cyanopyrrolidides, methods for the production thereof, and use of the same as medicaments
IL175487A (en) Pyrazole derivatives, a process for their preparation and use in the manufacture of drugs and drugs for inhibiting trk activity
IL213597A0 (en) Compounds, pharmaceutical compositions comprising them and their use in the manufacture of medicaments
IL191790B (en) The history of xanthine, their production and their use as medicines
IL231576A (en) Derivatives of adamantyl-acetamide, the pharmaceutical compositions containing them and their use in the preparation of medicines
IL176913A0 (en) 7-phenylamino-4-quinolone-3-carboxylic acid derivatives, methods for production and use thereof as medicaments
IL212477A0 (en) Biaryl heterocyclic compounds, methods of making the same, pharmaceutical compositions comprising them and their use in the preparation of medicaments
PL378065A1 (pl) Podstawione związki N-aryloheterocykliczne, sposób ich wytwarzania oraz ich zastosowanie jako środków leczniczych
IL174647A (en) Pyrazolopyridines and analogs thereof, pharmaceutical compositions comprising them and their use in the manufacture of medicaments
IL163102A (en) Dihydrobenzodiazepin-2-one derivatives, process for their preparation and use thereof in the preparation of medicaments for the treatment of neurological disorders
IL204947A0 (en) Phenylacetamido-thiazole derivatives, process for their preparation and their use in the manufacture of medicaments, pharmaceutical compositions and kits comprising them
TWI345975B (en) Crystalline micronisate, process for the manufacture thereof and use thereof for the preparation of a medicament
AU2003292239A8 (en) Novel carboxamides, the production and use thereof as medicaments
IL216516A0 (en) Nitrooxy derivatives of glucocorticoids, process for their preparation and use thereof in the manufacture of medicaments
IL166039A0 (en) New effector conjugates process for their production and their pharmaceutical use
IL179758A0 (en) Substituted tetrahydro - 2h - isoquinolin - 1 - one derivatives, method for the production thereof, and use of the same as medicaments
PL377741A1 (pl) Pochodne diarylocykloalkilowe, sposób ich wytwarzania i ich zastosowanie jako środka leczniczego
ZA200604432B (en) Thiozolidinones production and use thereof as medicaments
PT1638943E (pt) Novos derivados de imidazoles, sua preparação e sua utilização como medicamento

Legal Events

Date Code Title Description
FF Patent granted
KB Patent renewed
KB Patent renewed