RU2636584C2 - Гетероарильные соединения и их применение - Google Patents

Гетероарильные соединения и их применение Download PDF

Info

Publication number
RU2636584C2
RU2636584C2 RU2012123546A RU2012123546A RU2636584C2 RU 2636584 C2 RU2636584 C2 RU 2636584C2 RU 2012123546 A RU2012123546 A RU 2012123546A RU 2012123546 A RU2012123546 A RU 2012123546A RU 2636584 C2 RU2636584 C2 RU 2636584C2
Authority
RU
Russia
Prior art keywords
group
compound
cancer
kinase
ring
Prior art date
Application number
RU2012123546A
Other languages
English (en)
Russian (ru)
Other versions
RU2012123546A (ru
Inventor
Джасвиндер СИНГХ
Рассел ПЕТТЕР
Ричланд Вэйн ТЕСТЕР
Артур Ф. КЛЮГ
Хормоз Маздиясни
III Вильям Фредерик ВЕСТЛИН
Децян НЮ
Лисинь ЦЯО
Original Assignee
Селджен Авиломикс Рисерч,Инк.
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 Селджен Авиломикс Рисерч,Инк. filed Critical Селджен Авиломикс Рисерч,Инк.
Publication of RU2012123546A publication Critical patent/RU2012123546A/ru
Application granted granted Critical
Publication of RU2636584C2 publication Critical patent/RU2636584C2/ru

Links

Images

Classifications

    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not 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
    • A61K31/495—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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/535—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
    • A61K31/535—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
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P25/28—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
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • 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
    • 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
    • C07D239/28—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • 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
    • C07D239/28—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/12—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
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 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
    • C07D413/02—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychiatry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Otolaryngology (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Reproductive Health (AREA)
RU2012123546A 2009-12-29 2010-12-29 Гетероарильные соединения и их применение RU2636584C2 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US12/648,693 US8338439B2 (en) 2008-06-27 2009-12-29 2,4-disubstituted pyrimidines useful as kinase inhibitors
US12/648,693 2009-12-29
PCT/US2010/062432 WO2011090760A1 (en) 2009-12-29 2010-12-29 Heteroaryl compounds and uses thereof

Publications (2)

Publication Number Publication Date
RU2012123546A RU2012123546A (ru) 2014-02-10
RU2636584C2 true RU2636584C2 (ru) 2017-11-24

Family

ID=44307129

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2012123546A RU2636584C2 (ru) 2009-12-29 2010-12-29 Гетероарильные соединения и их применение

Country Status (16)

Country Link
US (5) US8338439B2 (enExample)
EP (1) EP2519235B1 (enExample)
JP (2) JP5879270B2 (enExample)
KR (2) KR20170086547A (enExample)
CN (2) CN106146407A (enExample)
AU (2) AU2010343055B2 (enExample)
BR (1) BR112012018345B1 (enExample)
CA (1) CA2783624C (enExample)
IL (2) IL220155B (enExample)
MX (2) MX2012007507A (enExample)
NZ (2) NZ700236A (enExample)
PH (1) PH12012501346A1 (enExample)
RU (1) RU2636584C2 (enExample)
SG (1) SG181962A1 (enExample)
TW (1) TWI592405B (enExample)
WO (1) WO2011090760A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2702631C2 (ru) * 2014-10-11 2019-10-09 Шанхай Хэнсох Биомедикал Ко., Лтд. Ингибитор egfr и его получение и применение

Families Citing this family (319)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7989465B2 (en) * 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
AU2008314632B2 (en) 2007-10-19 2015-05-28 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
KR101860057B1 (ko) 2008-05-21 2018-05-21 어리어드 파마슈티칼스, 인코포레이티드 키나아제 억제제로서 포스포러스 유도체
US11351168B1 (en) 2008-06-27 2022-06-07 Celgene Car Llc 2,4-disubstituted pyrimidines useful as kinase inhibitors
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
EP2361248B1 (en) 2008-06-27 2018-09-19 Celgene CAR LLC Heteroaryl compounds and uses thereof
KR101705158B1 (ko) 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Ｅｇｆｒ 억제제 및 질환 치료방법
AR076550A1 (es) * 2009-05-06 2011-06-22 Portola Pharm Inc Inhibidores de la janus tirosina kinasa (jak)
JP2012529535A (ja) 2009-06-12 2012-11-22 ブリストル−マイヤーズ スクイブ カンパニー キナーゼモジュレーターとして有用なニコチンアミド化合物
CN102713618B (zh) 2009-09-16 2015-07-15 新基阿维罗米克斯研究公司 蛋白激酶复合物和抑制剂
US8466155B2 (en) * 2009-10-02 2013-06-18 Boehringer Ingelheim International Gmbh Pyrimidines
CN102812167A (zh) 2009-12-30 2012-12-05 阿维拉制药公司 蛋白的配体-介导的共价修饰
WO2011146313A1 (en) 2010-05-19 2011-11-24 The University Of North Carolina At Chapel Hill Pyrazolopyrimidine compounds for the treatment of cancer
MX2012013274A (es) 2010-05-21 2013-05-28 Chemilia Ab Novedosos derivados de la pirimidina.
PT2576541T (pt) 2010-06-04 2016-07-08 Hoffmann La Roche Derivados de aminopirimidina como moduladores de lrrk2
EP2603081B1 (en) 2010-08-10 2016-10-05 Celgene Avilomics Research, Inc. Besylate salt of a btk inhibitor
TWI545115B (zh) 2010-11-01 2016-08-11 阿維拉製藥公司 雜環化合物及其用途
US9238629B2 (en) 2010-11-01 2016-01-19 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
WO2012064706A1 (en) * 2010-11-10 2012-05-18 Avila Therapeutics, Inc. Mutant-selective egfr inhibitors and uses thereof
CA2812669C (en) 2010-11-10 2018-11-06 F. Hoffmann-La Roche Ag Pyrazole aminopyrimidine derivatives as lrrk2 modulators
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
RU2013147417A (ru) 2011-03-24 2015-04-27 Кемилиа Аб Новые производные пиримидина
ES2759615T3 (es) 2011-04-01 2020-05-11 Univ Utah Res Found Análogos de N-fenilpirimidina-2-amina sustituidos como inhibidores de la quinasa AXL
JP6147727B2 (ja) 2011-04-01 2017-06-14 ユニヴァーシティー オブ ユタ リサーチ ファウンデーション チロシン受容体キナーゼｂｔｋ阻害剤としての置換ｎ−（３−（ピリミジン−４−イル）フェニル）アクリルアミド類似体
KR101962488B1 (ko) 2011-04-22 2019-03-26 시그날 파마소티칼 엘엘씨 치환된 디아미노카르복스아미드 및 디아미노카르보니트릴 피리미딘, 그의 조성물, 및 그를 사용하는 치료 방법
PL2701510T3 (pl) 2011-04-25 2017-07-31 Usher Iii Initiative Inc Pirazolopirydazyny oraz sposoby leczenia zwyrodnieniowych chorób siatkówki i utraty słuchu związanych z zespołem ushera
EP2704572B1 (en) 2011-05-04 2015-12-30 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
ES2791308T3 (es) 2011-07-27 2020-11-03 Astrazeneca Ab Derivados de 2-(2,4,5-anilino sustituido)pirimidina como moduladores de EGFR útiles para tratar el cáncer
JP2014532060A (ja) 2011-10-03 2014-12-04 ザ・ユニヴァーシティ・オヴ・ノース・キャロライナ・アト・チャペル・ヒル 癌を治療するためのピロロピリミジン化合物
AR088570A1 (es) 2011-10-28 2014-06-18 Celgene Avilomics Res Inc Metodos para tratar una enfermedad o trastorno relacionado con la tirosina quinasa de bruton
US9586965B2 (en) 2012-01-13 2017-03-07 Acea Biosciences Inc. Pyrrolo[2,3-d]pyrimidine compounds as inhibitors of protein kinases
US10799504B2 (en) 2012-01-13 2020-10-13 ACEA Therapeutics, Inc. Heterocyclic compounds and uses as anticancer agents
US9464089B2 (en) 2012-01-13 2016-10-11 Acea Biosciences Inc. Heterocyclic compounds and uses thereof
US9034885B2 (en) 2012-01-13 2015-05-19 Acea Biosciences Inc. EGFR modulators and uses thereof
EP2805940B1 (en) 2012-01-17 2016-11-23 Astellas Pharma Inc. Pyrazine carboxamide compound
CN104302178B (zh) 2012-03-15 2018-07-13 西建卡尔有限责任公司 表皮生长因子受体激酶抑制剂的固体形式
PT2825042T (pt) 2012-03-15 2018-11-16 Celgene Car Llc Sais de um inibidor de cinases do recetor do fator de crescimento epidérmico
US20150166591A1 (en) * 2012-05-05 2015-06-18 Ariad Pharmaceuticals, Inc. Methods and compositions for raf kinase mediated diseases
US9133134B2 (en) 2012-05-16 2015-09-15 Pharmacyclics Llc Inhibitors of bruton's tyrosine kinase
KR20150018789A (ko) 2012-05-22 2015-02-24 더 유니버시티 오브 노쓰 캐롤라이나 엣 채플 힐 암의 치료를 위한 피리미딘 화합물
HUE042374T2 (hu) 2012-06-13 2019-06-28 Incyte Holdings Corp Szubsztituált triciklusos vegyületek mint FGFR inhibitorok
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
US20150216865A1 (en) * 2012-09-04 2015-08-06 Celgene Avilomics Research, Inc. Methods of treating a bruton's tyrosine kinase disease or disorder
EP3680238A1 (en) * 2012-10-04 2020-07-15 University of Utah Research Foundation Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors
CA2887465A1 (en) 2012-10-04 2014-04-10 University Of Utah Research Foundation Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors
US9562047B2 (en) 2012-10-17 2017-02-07 The University Of North Carolina At Chapel Hill Pyrazolopyrimidine compounds for the treatment of cancer
US9227976B2 (en) 2012-10-25 2016-01-05 Usher Iii Initiative, Inc. Pyrazolopyridazines and methods for treating retinal-degenerative diseases and hearing loss associated with usher syndrome
US8765762B2 (en) 2012-10-25 2014-07-01 Usher III, Initiative, Inc. Pyrazolopyridazines and methods for treating retinal-degerative diseases and hearing loss associated with usher syndrome
EP2922827A4 (en) * 2012-11-20 2016-06-08 Celgene Avilomics Res Inc METHOD FOR THE TREATMENT OF A DISEASE OR DISEASE RELATED TO BRUTON TYROSINE KINASE
US20140142128A1 (en) * 2012-11-20 2014-05-22 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with bruton's tyrosine kinase
EP2922546A4 (en) * 2012-11-20 2016-06-08 Celgene Avilomics Res Inc METHOD FOR THE TREATMENT OF A DISEASE OR DISEASE RELATED TO BRUTON TYROSINE KINASE
WO2014081709A2 (en) * 2012-11-20 2014-05-30 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with bruton's tyrosine kinase
US9771330B2 (en) 2012-11-27 2017-09-26 The University Of North Carolina At Chapel Hill Pyrimidine compounds for the treatment of cancer
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
WO2014100748A1 (en) * 2012-12-21 2014-06-26 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
US20140213555A1 (en) * 2013-01-25 2014-07-31 Rigel Pharmaceuticals, Inc. Compounds and method for treating autoimmune diseases
KR20150119012A (ko) * 2013-02-08 2015-10-23 셀진 아빌로믹스 리서치, 인코포레이티드 Erk 억제제 및 이의 용도
WO2014130856A2 (en) * 2013-02-21 2014-08-28 Wayne Rothbaum Treatment of skeletal-related disorders
WO2014134391A1 (en) 2013-02-28 2014-09-04 Bristol-Myers Squibb Company Phenylpyrazole derivatives as potent rock1 and rock2 inhibitors
TW201444798A (zh) 2013-02-28 2014-12-01 必治妥美雅史谷比公司 作爲強效ｒｏｃｋ１及ｒｏｃｋ２抑制劑之苯基吡唑衍生物
BR112015022993B1 (pt) 2013-03-14 2021-12-14 Sumitomo Dainippon Pharma Oncology, Inc. Inibidores de jak2 e alk2, composição farmacêutica compreendendo os referidos inibidores e uso destes
EP2970190A1 (en) 2013-03-14 2016-01-20 Respivert Limited Kinase inhibitors
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
HUE036571T2 (hu) 2013-04-19 2018-07-30 Incyte Holdings Corp Biciklusos heterociklusok mint FGFR inhibitorok
LT2989106T (lt) 2013-04-25 2017-04-10 Beigene, Ltd. Kondensuoti heterocikliniai junginiai kaip baltymų kinazės inhibitoriai
HK1222644A1 (zh) * 2013-05-06 2017-07-07 Clovis Oncology, Inc. 一种可作为表皮生长因子受体激酶抑制剂的盐式
GB201309085D0 (en) 2013-05-20 2013-07-03 Redx Pharma Ltd Compounds
RS58273B1 (sr) 2013-06-26 2019-03-29 Abbvie Inc Primarni karboksamidi kao btk inhibitori
CN105377835B (zh) * 2013-07-11 2018-08-17 贝达药业股份有限公司 酪氨酸蛋白激酶调节剂及其应用方法
ES2761572T3 (es) * 2013-07-11 2020-05-20 Acea Therapeutics Inc Derivados de pirimidina como inhibidores de quinasa
KR101828187B1 (ko) 2013-08-12 2018-02-09 다이호야쿠힌고교 가부시키가이샤 신규 축합 피리미딘 화합물 또는 그 염
US9492471B2 (en) 2013-08-27 2016-11-15 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase
EA034666B1 (ru) 2013-09-13 2020-03-04 Бейджин Свитзерланд Гмбх Антитело против pd-1 и его применение для лечения рака или вирусной инфекции и фрагмент антитела
CN104262328B (zh) * 2013-09-18 2016-09-07 北京韩美药品有限公司 抑制btk和/或jak3激酶活性的化合物
HRP20191430T1 (hr) 2013-10-21 2019-11-01 Merck Patent Gmbh Spojevi heteroarila kao inhibitori btk i njihove uporabe
KR102671643B1 (ko) 2013-10-25 2024-05-31 파마싸이클릭스 엘엘씨 이식편 대 숙주 질환의 치료 및 예방 방법
US9415049B2 (en) 2013-12-20 2016-08-16 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
NZ715903A (en) 2014-01-30 2017-06-30 Signal Pharm Llc Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use
US11039620B2 (en) 2014-02-19 2021-06-22 Corning Incorporated Antimicrobial glass compositions, glasses and polymeric articles incorporating the same
US11039621B2 (en) 2014-02-19 2021-06-22 Corning Incorporated Antimicrobial glass compositions, glasses and polymeric articles incorporating the same
US9622483B2 (en) 2014-02-19 2017-04-18 Corning Incorporated Antimicrobial glass compositions, glasses and polymeric articles incorporating the same
CN104860941B (zh) 2014-02-25 2017-03-22 上海海雁医药科技有限公司 2,4‑二取代苯‑1,5‑二胺衍生物及其应用以及由其制备的药物组合物和药用组合物
WO2015131080A1 (en) 2014-02-28 2015-09-03 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
WO2015134805A1 (en) * 2014-03-07 2015-09-11 Celgene Avilomics Research, Inc. Methods of treating a bruton's tyrosine kinase disease or disorder
US9603850B2 (en) 2014-04-11 2017-03-28 The University Of North Carolina At Chapel Hill MerTK-specific pyrazolopyrimidine compounds
JP6321821B2 (ja) 2014-04-14 2018-05-09 シャンハイ ハイヤン ファーマシューティカル テクノロジー カンパニー リミテッドＳｈａｎｇｈａｉ Ｈａｉｙａｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌ Ｔｅｃｈｎｏｌｏｇｙ Ｃｏ．， Ｌｔｄ． ２，３，４，６−４置換ベンゼン−１，５−ジアミン誘導体、その製造方法および医薬品における使用
US20150297605A1 (en) * 2014-04-16 2015-10-22 Signal Pharmaceuticals, Llc Methods for treating cancer using tor kinase inhibitor combination therapy
WO2015158310A1 (zh) * 2014-04-18 2015-10-22 山东轩竹医药科技有限公司 一种酪氨酸激酶抑制剂及其用途
CN104130265B (zh) * 2014-04-29 2017-01-25 苏州景泓生物技术有限公司 一种含有螺环或桥环的嘧啶类化合物
GB201410430D0 (en) 2014-06-11 2014-07-23 Redx Pharma Ltd Compounds
KR102130600B1 (ko) 2014-07-03 2020-07-08 베이진 엘티디 Pd-l1 항체와 이를 이용한 치료 및 진단
CN105315285B (zh) * 2014-07-25 2017-12-08 上海海雁医药科技有限公司 2,4‑二取代7H‑吡咯并[2,3‑d]嘧啶衍生物、其制法与医药上的用途
MY195016A (en) 2014-08-04 2023-01-03 Nuevolution As Optionally Fused Heterocyclyl-Substituted Derivatives of Pyrimidine Useful for The Treatment of Inflammatory, Metabolic, Oncologic and Autoimmune Diseases
EP4578865A3 (en) 2014-08-12 2025-07-30 Monash University Lymph directing prodrugs
TW201613892A (en) 2014-08-13 2016-04-16 Celgene Avilomics Res Inc Forms and compositions of an ERK inhibitor
EP4070795A1 (en) * 2014-08-25 2022-10-12 Salk Institute for Biological Studies Novel ulk1 inhibitors and methods using same
CN105399686B (zh) * 2014-09-16 2018-05-22 深圳微芯生物科技有限责任公司 嘧啶衍生物、其制备方法及其应用
CN105399685B (zh) * 2014-09-16 2018-05-22 深圳微芯生物科技有限责任公司 作为选择性jak3和/或jak1激酶抑制剂的芳杂环化合物的制备方法及其应用
CN105481778B (zh) * 2014-09-16 2019-06-04 深圳微芯生物科技股份有限公司 嘧啶衍生物、其制备方法及其应用
SMT202100311T1 (it) 2014-09-17 2021-07-12 Celgene Car Llc Inibitori di mk2 e loro usi
WO2016060963A1 (en) 2014-10-14 2016-04-21 Sunshine Lake Pharma Co., Ltd. Substituted heteroaryl compounds and methods of use
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
DK3215518T3 (da) 2014-10-29 2021-05-25 Bicyclerd Ltd Bicykliske peptidligander, der er specifikke for mt1-mmp
CN105601573B (zh) * 2014-11-24 2021-07-02 中国科学院上海药物研究所 2-氨基嘧啶类化合物及其药物组合物和应用
CN107209186A (zh) 2014-12-11 2017-09-26 默克专利有限公司 Btk抑制剂的测定
ES2877642T3 (es) 2014-12-16 2021-11-17 Signal Pharm Llc Formulaciones de 2-(terc-butilamino)-4-((1R,3R,4R)-3-hidroxi-4-metilciclohexilamino)-pirimidin-5-carboxamida
ES2882954T3 (es) 2014-12-16 2021-12-03 Signal Pharm Llc Usos médicos que comprenden métodos para la medición de la inhibición de la quinasa c-Jun N-terminal en la piel
US20180022710A1 (en) 2015-01-29 2018-01-25 Signal Pharmaceuticals, Llc Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide
JP6093486B2 (ja) 2015-01-30 2017-03-08 大鵬薬品工業株式会社 縮合ピリミジン化合物の新規な塩及びその結晶
KR101858421B1 (ko) * 2015-01-30 2018-05-15 다이호야쿠힌고교 가부시키가이샤 면역 질환의 예방 및/또는 치료제
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
MX388991B (es) 2015-02-20 2025-03-20 Incyte Corp Heterociclos biciclicos como inhibidores de receptores del factor de crecimiento fibroblastico (fgfr)
WO2016138352A1 (en) 2015-02-27 2016-09-01 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
WO2017004134A1 (en) 2015-06-29 2017-01-05 Nimbus Iris, Inc. Irak inhibitors and uses thereof
CN108137559B (zh) * 2015-07-09 2021-11-02 默克专利有限公司 用作btk抑制剂的嘧啶衍生物及其用途
WO2017019487A1 (en) 2015-07-24 2017-02-02 Celgene Corporation Methods of synthesis of (1r,2r,5r)-5-amino-2-methylcyclohexanol hydrochloride and intermediates useful therein
US20170209462A1 (en) 2015-08-31 2017-07-27 Pharmacyclics Llc Btk inhibitor combinations for treating multiple myeloma
TWI707852B (zh) 2015-09-02 2020-10-21 美商林伯士拉克許米公司 Tyk2 抑制劑及其用途
WO2017041139A1 (en) 2015-09-08 2017-03-16 Monash University Lymph directing prodrugs
WO2017044720A1 (en) 2015-09-11 2017-03-16 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
WO2017046604A1 (en) 2015-09-16 2017-03-23 Redx Pharma Plc Pyrazolopyrimidine derivatives as btk inhibitors for the treatment of cancer
CN106554347B (zh) * 2015-09-25 2020-10-30 浙江博生医药有限公司 Egfr激酶抑制剂及其制备方法和应用
KR20180067584A (ko) 2015-10-09 2018-06-20 아세아 테라퓨틱스 인코포레이티드 피롤로피리미딘 키나아제 억제제의 약학적 염, 물리적 형태 및 조성물, 및 이들의 제조 방법
LT3365334T (lt) * 2015-10-21 2024-09-10 Otsuka Pharmaceutical Co., Ltd. Benzolaktamo junginiai kaip baltymų kinazės inhibitoriai
MX389001B (es) 2015-10-23 2025-03-20 Navitor Pharm Inc Moduladores de interacción de sestrina-gator2 y sus usos.
WO2017106352A1 (en) 2015-12-14 2017-06-22 Raze Therapeutics, Inc. Caffeine inhibitors of mthfd2 and uses thereof
MA55064A (fr) 2015-12-16 2021-09-29 Loxo Oncology Inc Composés utilisés comme inhibiteurs de kinase
CN107021963A (zh) 2016-01-29 2017-08-08 北京诺诚健华医药科技有限公司 吡唑稠环类衍生物、其制备方法及其在治疗癌症、炎症和免疫性疾病上的应用
HRP20211220T1 (hr) 2016-03-09 2021-10-29 Raze Therapeutics Inc. Inhibitori 3-fosfoglicerat dehidrogenaze i njihova upotreba
WO2017156179A1 (en) 2016-03-09 2017-09-14 Raze Therapeutics, Inc. 3-phosphoglycerate dehydrogenase inhibitors and uses thereof
US10709708B2 (en) 2016-03-17 2020-07-14 The University Of North Carolina At Chapel Hill Method of treating cancer with a combination of MER tyrosine kinase inhibitor and an epidermal growth factor receptor (EGFR) inhibitor
CN109153722A (zh) 2016-04-08 2019-01-04 X4 制药有限公司 用于治疗癌症的方法
CN105968056A (zh) * 2016-05-28 2016-09-28 大连医科大学 二芳基嘧啶类化合物，组合物及用途
EP3471726A4 (en) 2016-06-21 2019-10-09 X4 Pharmaceuticals, Inc. CXCR4 INHIBITORS AND USES THEREOF
WO2017223243A1 (en) 2016-06-21 2017-12-28 X4 Pharmaceuticals, Inc. Cxcr4 inhibitors and uses thereof
JP7054529B2 (ja) 2016-06-21 2022-04-14 エックス４ ファーマシューティカルズ， インコーポレイテッド Ｃｘｃｒ４阻害剤およびその使用
CN109475536B (zh) 2016-07-05 2022-05-27 百济神州有限公司 用于治疗癌症的PD-l拮抗剂和RAF抑制剂的组合
TWI865873B (zh) 2016-08-16 2024-12-11 瑞士商百濟神州瑞士有限責任公司 (s)-7-(1-丙烯醯基六氫吡啶-4-基)-2-(4-苯氧基苯基)-4,5,6,7-四氫吡唑並[1,5-a]嘧啶-3-甲醯胺的晶型、其製備和用途
FI3500299T3 (fi) 2016-08-19 2024-02-14 Beigene Switzerland Gmbh Tsanubrutinibin yhdistelmä cd20-tai pd-1-vasta-aineen kanssa käytettäväksi syövän hoidossa
CN106316886A (zh) * 2016-08-24 2017-01-11 泰州精英化成医药科技有限公司 顺式‑3‑（叔丁氧羰基氨基）环己烷甲酸的制备方法
EP3515414B1 (en) 2016-09-19 2022-11-30 MEI Pharma, Inc. Combination therapy
WO2018071794A1 (en) 2016-10-14 2018-04-19 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
EP3528816A4 (en) 2016-10-21 2020-04-08 Nimbus Lakshmi, Inc. TYK2 INHIBITORS AND USES THEREOF
CN107973754B (zh) * 2016-10-25 2020-04-14 清华大学 一种小分子抑制剂及其制备方法与其在多发性骨髓瘤治疗中的应用
JP2020023441A (ja) * 2016-11-02 2020-02-13 国立大学法人九州大学 Ｅｇｆｒ阻害及び腫瘍治療に有用な新規化合物
CN110139669A (zh) 2016-11-03 2019-08-16 朱诺治疗学股份有限公司 T细胞疗法和btk抑制剂的组合疗法
EP3538091A4 (en) 2016-11-08 2020-06-10 Navitor Pharmaceuticals, Inc. PHENYL AMINO PIPERIDINE MTORC INHIBITORS AND USES THEREOF
CN110177544A (zh) 2016-11-29 2019-08-27 普尔泰克健康有限公司 用于递送治疗剂的外泌体
US11091451B2 (en) 2016-12-05 2021-08-17 Raze Therapeutics, Inc. SHMT inhibitors and uses thereof
EP3559018A1 (en) 2016-12-23 2019-10-30 Bicyclerd Limited Peptide derivatives having novel linkage structures
CN106632273A (zh) * 2016-12-29 2017-05-10 大连医科大学 含唑杂环的嘧啶类化合物，组合物及其用途
EP3565638B8 (en) 2017-01-06 2024-04-10 BicycleRD Limited Bicycle conjugate for treating cancer
CN108329274B (zh) * 2017-01-13 2021-09-03 正大天晴药业集团股份有限公司 布鲁顿酪氨酸激酶抑制剂
EP3573989A4 (en) 2017-01-25 2020-11-18 Beigene, Ltd. CRYSTALLINE FORMS OF (S) -7- (1- (BUT-2-YNOYL) PIPERIDIN-4-YL) -2- (4-PHENOXYPHENYL) -4, 5, 6, 7-TETRAHY DROPYRAZOLO [1, 5-A ] PYRIMIDINE-3-CARBOXAMIDE, PREPARATION AND ASSOCIATED USES
CN108498477A (zh) * 2017-02-27 2018-09-07 江苏奥赛康药业股份有限公司 一种2-氨基嘧啶类化合物的药用组合物及其制备方法
EP4338802A3 (en) 2017-03-08 2024-09-04 Takeda Pharmaceutical Company Limited Tyk2 inhibitors, uses, and methods for production thereof
EP3375784A1 (en) 2017-03-14 2018-09-19 Artax Biopharma Inc. Aza-dihydro-acridone derivatives
EP3375778A1 (en) 2017-03-14 2018-09-19 Artax Biopharma Inc. Aryl-piperidine derivatives
JP2020516682A (ja) 2017-04-07 2020-06-11 エイシア セラピューティクス， インコーポレイテッド ピロロピリミジンキナーゼの薬学的な塩、物理的形態および組成物、ならびにその作製方法
JOP20190233A1 (ar) 2017-04-14 2019-10-02 Biogen Ma Inc نظائر بنزوازيبين بوصفها عوامل مثبطة لتيروزين كيناز بروتون
GB201706327D0 (en) 2017-04-20 2017-06-07 Otsuka Pharma Co Ltd A pharmaceutical compound
EP3615550A1 (en) 2017-04-27 2020-03-04 BicycleTx Limited Bicyclic peptide ligands and uses thereof
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
BR112019027402A2 (pt) 2017-06-22 2020-07-07 Celgene Corporation tratamento de carcinoma hepatocelular caracterizado por infecção pelo vírus da hepatite b
EP3645549A1 (en) 2017-06-26 2020-05-06 BicycleRD Limited Bicyclic peptide ligands with detectable moieties and uses thereof
US11597768B2 (en) 2017-06-26 2023-03-07 Beigene, Ltd. Immunotherapy for hepatocellular carcinoma
ES2994013T3 (en) 2017-07-28 2025-01-15 Takeda Pharmaceuticals Co Tyk2 inhibitors and uses thereof
JP7670481B2 (ja) 2017-08-04 2025-04-30 バイスクルテクス・リミテッド Ｃｄ１３７に対して特異的な二環式ペプチドリガンド
CN110997677A (zh) 2017-08-12 2020-04-10 百济神州有限公司 具有改进的双重选择性的Btk抑制剂
US20200291096A1 (en) 2017-08-14 2020-09-17 Bicyclerd Limited Bicyclic peptide ligand sting conjugates and uses thereof
US20200283482A1 (en) 2017-08-14 2020-09-10 Bicyclerd Limited Bicyclic peptide ligand prr-a conjugates and uses thereof
KR20200041954A (ko) * 2017-08-18 2020-04-22 북경한미약품 유한공사 화합물, 이의 약제학적 조성물, 및 이의 용도 및 응용
EP3675838A4 (en) 2017-08-29 2021-04-21 PureTech LYT, Inc. LIPID PRODRUGS DIRECTED TO THE LYMPHATIC SYSTEM
US11883497B2 (en) 2017-08-29 2024-01-30 Puretech Lyt, Inc. Lymphatic system-directing lipid prodrugs
KR102383561B1 (ko) * 2017-09-07 2022-04-06 한국화학연구원 테트라히드로이소퀴놀린기로 치환된 피리미딘 유도체 화합물, 이의 광학이성질체, 또는 이의 약학적으로 허용 가능한 염, 및 이를 유효성분으로 포함하는 암 예방 또는 치료용 조성물
WO2019060693A1 (en) 2017-09-22 2019-03-28 Kymera Therapeutics, Inc. CRBN LIGANDS AND USES THEREOF
AU2018338314B2 (en) 2017-09-22 2024-12-12 Kymera Therapeutics, Inc Protein degraders and uses thereof
EP3707138B1 (en) 2017-11-06 2022-07-13 Bristol-Myers Squibb Company Isofuranone compounds useful as hpk1 inhibitors
WO2019099311A1 (en) 2017-11-19 2019-05-23 Sunshine Lake Pharma Co., Ltd. Substituted heteroaryl compounds and methods of use
US11786529B2 (en) 2017-11-29 2023-10-17 Beigene Switzerland Gmbh Treatment of indolent or aggressive B-cell lymphomas using a combination comprising BTK inhibitors
US11304954B2 (en) 2017-12-19 2022-04-19 Puretech Lyt, Inc. Lipid prodrugs of mycophenolic acid and uses thereof
TWI825046B (zh) 2017-12-19 2023-12-11 英商拜西可泰克斯有限公司 Epha2特用之雙環胜肽配位基
EP3727362A4 (en) 2017-12-19 2021-10-06 PureTech LYT, Inc. MYCOPHENOLIC ACID LIPID PRODRUGS AND THEIR USES
GB201721265D0 (en) 2017-12-19 2018-01-31 Bicyclerd Ltd Bicyclic peptide ligands specific for EphA2
US11608345B1 (en) 2017-12-19 2023-03-21 Puretech Lyt, Inc. Lipid prodrugs of rapamycin and its analogs and uses thereof
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc Irak degraders and uses thereof
EP3737675A4 (en) 2018-01-12 2022-01-05 Kymera Therapeutics, Inc. Crbn ligands and uses thereof
EP3737666A4 (en) 2018-01-12 2022-01-05 Kymera Therapeutics, Inc. PROTEIN DEGRADATION AGENTS AND ASSOCIATED USES
CN111867581B (zh) 2018-01-29 2023-12-26 默克专利股份有限公司 Gcn2抑制剂及其用途
EP4616913A3 (en) 2018-01-29 2025-12-10 Merck Patent GmbH Gcn2 inhibitors and uses thereof
TWI798334B (zh) 2018-01-31 2023-04-11 大陸商迪哲（江蘇）醫藥股份有限公司 Ｅｒｂｂ／ｂｔｋ抑制劑
CA3091775A1 (en) 2018-02-23 2019-08-29 Bicycletx Limited Multimeric bicyclic peptide ligands
JP7317032B2 (ja) 2018-02-27 2023-07-28 アルタックス バイオファーマ インコーポレイテッド Ｔｃｒ－ｎｃｋ相互作用の阻害剤としてのクロメン誘導体
EP3773591A4 (en) 2018-04-05 2021-12-22 Sumitomo Dainippon Pharma Oncology, Inc. AXL KINASE INHIBITORS AND THEIR USE
AU2019257651B2 (en) 2018-04-24 2023-05-25 Vertex Pharmaceuticals Incorporated Pteridinone compounds and uses thereof
AU2019261308B2 (en) 2018-04-24 2022-09-08 Merck Patent Gmbh Antiproliferation compounds and uses thereof
EP3784664B1 (en) 2018-04-26 2025-02-19 Pfizer Inc. 2-amino-pyridine or 2-amino-pyrimidine derivatives as cyclin dependent kinase inhibitors
CN112584902A (zh) 2018-05-03 2021-03-30 朱诺治疗学股份有限公司 嵌合抗原受体（car）t细胞疗法和激酶抑制剂的组合疗法
EP3788047B1 (en) 2018-05-04 2024-09-04 Incyte Corporation Solid forms of an fgfr inhibitor and processes for preparing the same
BR112020022373A2 (pt) 2018-05-04 2021-02-02 Incyte Corporation sais de um inibidor de fgfr
PL3813946T3 (pl) 2018-06-15 2024-09-02 Janssen Pharmaceutica Nv Analogi rapamycyny i ich zastosowania
US11180531B2 (en) 2018-06-22 2021-11-23 Bicycletx Limited Bicyclic peptide ligands specific for Nectin-4
GB201810316D0 (en) 2018-06-22 2018-08-08 Bicyclerd Ltd Peptide ligands for binding to EphA2
EP3817748A4 (en) 2018-07-06 2022-08-24 Kymera Therapeutics, Inc. TRICYCLIC CRBN LIGANDS AND USES THEREOF
WO2020010227A1 (en) 2018-07-06 2020-01-09 Kymera Therapeutics, Inc. Protein degraders and uses thereof
US11040038B2 (en) 2018-07-26 2021-06-22 Sumitomo Dainippon Pharma Oncology, Inc. Methods for treating diseases associated with abnormal ACVR1 expression and ACVR1 inhibitors for use in the same
US10548889B1 (en) 2018-08-31 2020-02-04 X4 Pharmaceuticals, Inc. Compositions of CXCR4 inhibitors and methods of preparation and use
WO2020051424A1 (en) 2018-09-07 2020-03-12 Pic Therapeutics Eif4e inhibitors and uses thereof
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
US11414431B2 (en) 2018-10-15 2022-08-16 Nimbus Lakshmi, Inc. Substituted pyrazolo[1,5-a]pyrimidines as TYK2 inhibitors
EP3870597A1 (en) 2018-10-23 2021-09-01 BicycleTx Limited Bicyclic peptide ligands and uses thereof
CN109608444B (zh) * 2018-11-27 2022-02-11 中国药科大学 含异吲哚啉酮的erk抑制剂及其制备方法与用途
SG11202105424PA (en) 2018-11-30 2021-06-29 Kymera Therapeutics Inc Irak degraders and uses thereof
CN113271938A (zh) 2018-11-30 2021-08-17 林伯士拉克许米公司 Tyk2抑制剂和其用途
GB201820288D0 (en) 2018-12-13 2019-01-30 Bicycle Tx Ltd Bicycle peptide ligaands specific for MT1-MMP
GB201820295D0 (en) 2018-12-13 2019-01-30 Bicyclerd Ltd Bicyclic peptide ligands specific for MT1-MMP
GB201820325D0 (en) 2018-12-13 2019-01-30 Bicyclerd Ltd Bicyclic peptide ligands specific for psma
EP3670659A1 (en) 2018-12-20 2020-06-24 Abivax Biomarkers, and uses in treatment of viral infections, inflammations, or cancer
WO2020128526A1 (en) 2018-12-21 2020-06-25 Bicycletx Limited Bicyclic peptide ligands specific for pd-l1
US11174264B2 (en) 2019-01-23 2021-11-16 Nimbus Lakshmi, Inc. TYK2 inhibitors and uses thereof
CN109776495A (zh) * 2019-01-31 2019-05-21 李佳睿 抗肿瘤化合物及其制备方法与用途
WO2020165600A1 (en) 2019-02-14 2020-08-20 Bicycletx Limited Bicyclic peptide ligand sting conjugates and uses thereof
WO2020168197A1 (en) 2019-02-15 2020-08-20 Incyte Corporation Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors
WO2020180959A1 (en) 2019-03-05 2020-09-10 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as cdk2 inhibitors
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
KR20210144844A (ko) 2019-03-29 2021-11-30 아스트라제네카 아베 비-소세포 폐암의 치료에 사용하기 위한 오시머티닙
JP2022528887A (ja) 2019-04-02 2022-06-16 バイスクルテクス・リミテッド バイシクルトキシンコンジュゲートおよびその使用
KR20220006139A (ko) 2019-04-05 2022-01-14 카이메라 쎄라퓨틱스 인코포레이티드 Stat 분해제 및 이의 용도
WO2020223558A1 (en) 2019-05-01 2020-11-05 Incyte Corporation Tricyclic amine compounds as cdk2 inhibitors
WO2020223469A1 (en) 2019-05-01 2020-11-05 Incyte Corporation N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer
SI3966206T1 (sl) 2019-05-10 2023-12-29 Deciphera Pharmaceuticals, Llc Heteroarilaminopirimidinski amidni zaviralci avtofagije in načini njihove uporabe
HRP20231730T1 (hr) 2019-05-10 2024-05-10 Deciphera Pharmaceuticals, Llc Fenilaminopirimidin amidni inhibitori autofagije i postupci njihove primjene
CN114502540A (zh) 2019-05-31 2022-05-13 医肯纳肿瘤学公司 Tead抑制剂和其用途
WO2020249001A1 (zh) 2019-06-10 2020-12-17 百济神州瑞士有限责任公司 一种含有布鲁顿氏酪氨酸激酶抑制剂的口服固体片剂及其制备方法
US12521438B2 (en) 2019-06-10 2026-01-13 Kymera Therapeutics, Inc. SMARCA degraders and uses thereof
CA3143489A1 (en) 2019-06-17 2020-12-24 Deciphera Pharmaceuticals, Llc Aminopyrimidine amide autophagy inhibitors and methods of use thereof
WO2020257495A1 (en) * 2019-06-18 2020-12-24 Purdue Research Foundation Inhibitors of erythrocyte band 3 tyrosine phosphorylation and uses thereof
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
TWI862640B (zh) 2019-07-30 2024-11-21 英商拜西可泰克斯有限公司 異質雙環肽複合物
CN110305140B (zh) * 2019-07-30 2020-08-04 上海勋和医药科技有限公司 二氢吡咯并嘧啶类选择性jak2抑制剂
TW202115024A (zh) 2019-08-14 2021-04-16 美商英塞特公司 作為cdk2 抑制劑之咪唑基嘧啶基胺化合物
JP2022548594A (ja) 2019-09-11 2022-11-21 ビンシア・バイオサイエンシーズ・インコーポレイテッド Ｕｓｐ３０阻害剤及びその使用
CA3150108A1 (en) 2019-09-13 2021-03-18 Neelu Kaila Hpk1 antagonists and uses thereof
CN112574207B (zh) * 2019-09-30 2023-04-11 南京药石科技股份有限公司 Erk1/2蛋白激酶抑制剂及其用途
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
PE20221905A1 (es) 2019-10-11 2022-12-23 Incyte Corp Aminas biciclicas como inhibidoras de la cdk2
KR20220100879A (ko) 2019-10-14 2022-07-18 인사이트 코포레이션 Fgfr 저해제로서의 이환식 헤테로사이클
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
TW202120092A (zh) * 2019-11-08 2021-06-01 大陸商深圳微芯生物科技股份有限公司 化合物用於預防或治療移植物抗宿主病的用途
JP2023503385A (ja) * 2019-11-26 2023-01-27 シェンチェン チップスクリーン バイオサイエンシズ カンパニー、リミテッド 非晶質形態の芳香族複素環式化合物を含む組成物、並びにその調製方法及びその使用
WO2021113479A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
KR20220131900A (ko) 2019-12-04 2022-09-29 인사이트 코포레이션 Fgfr 억제제의 유도체
KR20220128345A (ko) 2019-12-05 2022-09-20 아나쿠리아 테라퓨틱스, 인코포레이티드 라파마이신 유사체 및 이의 용도
JP2023509366A (ja) 2019-12-17 2023-03-08 カイメラ セラピューティクス， インコーポレイテッド Ｉｒａｋ分解剤およびそれらの使用
WO2021127283A2 (en) 2019-12-17 2021-06-24 Kymera Therapeutics, Inc. Irak degraders and uses thereof
TWI872177B (zh) 2019-12-20 2025-02-11 丹麥商紐韋盧森公司 對核受體具有活性之化合物
US11447479B2 (en) 2019-12-20 2022-09-20 Nuevolution A/S Compounds active towards nuclear receptors
PH12022551522A1 (en) 2019-12-23 2024-01-29 Kymera Therapeutics Inc Smarca degraders and uses thereof
WO2021138391A1 (en) 2019-12-30 2021-07-08 Tyra Biosciences, Inc. Indazole compounds
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CN111620852B (zh) * 2020-01-19 2023-05-09 镇江植生源农业科技有限公司 一种5-氯-嘧啶-2,4-二胺类化合物及其制备方法和应用
IL295362A (en) 2020-02-05 2022-10-01 Puretech Lyt Inc Lipid prodrugs of neurosteroids
EP4114529A1 (en) 2020-03-03 2023-01-11 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
PH12022552458A1 (en) 2020-03-19 2024-01-22 Kymera Therapeutics Inc Mdm2 degraders and uses thereof
US11613532B2 (en) 2020-03-31 2023-03-28 Nuevolution A/S Compounds active towards nuclear receptors
MX2022012260A (es) 2020-03-31 2022-11-30 Nuevolution As Compuestos activos frente a receptores nucleares.
TW202204331A (zh) 2020-04-07 2022-02-01 美商米突倍基公司 Cd38抑制劑
TW202210483A (zh) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Irak降解劑之結晶型
US20230250110A1 (en) 2020-06-03 2023-08-10 Kymera Therapeutics, Inc. Deuterated irak degraders and uses thereof
CN111646978B (zh) * 2020-06-11 2021-12-21 浙江大学 N2-取代烷氧芳环-2-氨基嘧啶类衍生物及应用
US20230257350A1 (en) * 2020-07-02 2023-08-17 The Cleveland Clinic Foundation Compounds and methods of promoting oligodendrocyte precursor differentiation
KR20230074721A (ko) 2020-08-17 2023-05-31 바이사이클티엑스 리미티드 Nectin-4에 특이적인 이환 콘쥬게이트 및 이의 용도
WO2022063106A1 (en) * 2020-09-22 2022-03-31 Beigene, Ltd. Indoline compounds and derivatives as egfr inhibitors
WO2022072632A1 (en) * 2020-09-30 2022-04-07 Scorpion Therapeutics, Inc. Bicyclic compounds for use in the treatment cancer
US12331046B2 (en) 2020-10-23 2025-06-17 Nimbus Clotho, Inc. CTPS1 inhibitors and uses thereof
WO2022120353A1 (en) 2020-12-02 2022-06-09 Ikena Oncology, Inc. Tead inhibitors and uses thereof
KR20230131189A (ko) 2020-12-02 2023-09-12 이케나 온콜로지, 인코포레이티드 Tead 억제제 및 이의 용도
MX2023007852A (es) 2020-12-30 2023-07-07 Kymera Therapeutics Inc Degradadores de cinasas asociadas al receptor de interleucina-1 (irak) y usos de los mismos.
MX2023009059A (es) 2021-02-02 2023-09-15 Liminal Biosciences Ltd Antagonistas de gpr84 y usos de estos.
KR20230153387A (ko) 2021-02-02 2023-11-06 리미널 바이오사이언시스 리미티드 Gpr84 길항제 및 이의 용도
CN117120090A (zh) 2021-02-12 2023-11-24 林伯士萨顿公司 Hpk1拮抗剂和其用途
IL304905A (en) 2021-02-15 2023-10-01 Kymera Therapeutics Inc IRAK4 joints and their uses
WO2022174268A1 (en) 2021-02-15 2022-08-18 Kymera Therapeutics, Inc. Irak4 degraders and uses thereof
CN117295737A (zh) 2021-03-05 2023-12-26 林伯士萨顿公司 Hpk1拮抗剂和其用途
WO2022213062A1 (en) 2021-03-29 2022-10-06 Nimbus Saturn, Inc. Hpk1 antagonists and uses thereof
CN115160319B (zh) * 2021-04-01 2023-12-26 西安新通药物研究股份有限公司 含1,3-苯并二氧戊环结构的化合物及其制备方法与用途
US20240216330A1 (en) 2021-04-02 2024-07-04 Biogen Ma Inc. Combination treatment methods of multiple sclerosis
KR20240007155A (ko) 2021-04-09 2024-01-16 님버스 클리오, 인코포레이티드 Cbl-b 조절제 및 이의 용도
WO2022221170A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
JP2024514879A (ja) 2021-04-16 2024-04-03 イケナ オンコロジー， インコーポレイテッド Ｍｅｋ阻害剤及びその使用
AU2022271290A1 (en) 2021-05-07 2023-11-23 Kymera Therapeutics, Inc. Cdk2 degraders and uses thereof
EP4352060A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
TW202313611A (zh) 2021-06-09 2023-04-01 美商英塞特公司 作為ｆｇｆｒ抑制劑之三環雜環
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
EP4392421A1 (en) 2021-08-25 2024-07-03 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
JP2024534127A (ja) 2021-08-25 2024-09-18 ピク セラピューティクス， インコーポレイテッド ｅＩＦ４Ｅ阻害剤及びその使用
WO2023076556A1 (en) 2021-10-29 2023-05-04 Kymera Therapeutics, Inc. Irak4 degraders and synthesis thereof
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
WO2023114984A1 (en) 2021-12-17 2023-06-22 Ikena Oncology, Inc. Tead inhibitors and uses thereof
IL314437A (en) 2022-01-31 2024-09-01 Kymera Therapeutics Inc IRAK joints and their uses
WO2023173053A1 (en) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2023173057A1 (en) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Mek inhibitors and uses thereof
US12233056B2 (en) 2022-04-06 2025-02-25 Syntara Limited Lysyl oxidase inhibitors for treating myeloid malignancies
WO2023211889A1 (en) 2022-04-25 2023-11-02 Ikena Oncology, Inc. Polymorphic compounds and uses thereof
WO2023220655A1 (en) 2022-05-11 2023-11-16 Celgene Corporation Methods to overcome drug resistance by re-sensitizing cancer cells to treatment with a prior therapy via treatment with a t cell therapy
WO2023230205A1 (en) 2022-05-25 2023-11-30 Ikena Oncology, Inc. Mek inhibitors and uses thereof
US11786531B1 (en) 2022-06-08 2023-10-17 Beigene Switzerland Gmbh Methods of treating B-cell proliferative disorder
IL318577A (en) 2022-08-02 2025-03-01 Liminal Biosciences Ltd ARYL-TRIAZOLYL AND RELATED GPR84 ANTAGONISTS AND THEIR USES
JP2025527248A (ja) 2022-08-02 2025-08-20 リミナル・バイオサイエンシーズ・リミテッド 置換ピリドンｇｐｒ８４アンタゴニスト及びその使用
TW202416950A (zh) 2022-08-02 2024-05-01 英商利米那生物科技有限公司 雜芳基甲醯胺及相關gpr84拮抗劑及其用途
CN115448906B (zh) * 2022-09-26 2024-04-02 深圳大学 一种2-苯胺基嘧啶类衍生物及其制备方法与应用
WO2024112894A1 (en) 2022-11-22 2024-05-30 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
WO2024264017A2 (en) 2023-06-23 2024-12-26 Kymera Therapeutics, Inc. Irak degraders and uses thereof
WO2025062372A1 (en) 2023-09-21 2025-03-27 Takeda Pharmaceutical Company Limited Tyk2 inhibitors for use in the treatment of inflammatory bowel disease
TW202515850A (zh) * 2023-09-22 2025-04-16 大陸商江蘇恆瑞醫藥股份有限公司 雜芳基類化合物、其製備方法及其在醫藥上的應用
CN119707835A (zh) * 2024-11-25 2025-03-28 沈阳药科大学 2-氨基嘧啶-5-甲酰胺类化合物及用于制备治疗和/或预防癌症药物中的用途

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2299201C2 (ru) * 2000-07-11 2007-05-20 Астразенека Аб Производные пиримидина, способ их получения (варианты), фармацевтические композиции (варианты) и способ ингибирования
US20080194603A1 (en) * 2006-10-19 2008-08-14 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US20080300268A1 (en) * 2007-06-04 2008-12-04 Avila Therapeutics, Inc. Heterocyclic compounds and uses thereof
WO2009017838A2 (en) * 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
US20090137588A1 (en) * 2007-10-19 2009-05-28 Avila Therapeutics, Inc. Heteroaryl compounds and uses thereof

Family Cites Families (169)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4032637A (en) 1972-09-26 1977-06-28 Sandoz Ltd. Method of promoting sleep
US4709016A (en) 1982-02-01 1987-11-24 Northeastern University Molecular analytical release tags and their use in chemical analysis
US5650270A (en) 1982-02-01 1997-07-22 Northeastern University Molecular analytical release tags and their use in chemical analysis
US4650750A (en) 1982-02-01 1987-03-17 Giese Roger W Method of chemical analysis employing molecular release tag compounds
US5516931A (en) 1982-02-01 1996-05-14 Northeastern University Release tag compounds producing ketone signal groups
GB8608335D0 (en) 1986-04-04 1986-05-08 Pfizer Ltd Pharmaceutically acceptable salts
US5453510A (en) 1990-07-13 1995-09-26 Burroughs Wellcome Co. Neuromuscular blocking agents
JPH0741461A (ja) 1993-05-27 1995-02-10 Eisai Co Ltd スルホン酸エステル誘導体
EP0813525B9 (en) 1995-03-10 2004-02-04 Berlex Laboratories, Inc. Benzamidine derivatives their preparation and their use as anti-coagulants
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
GB9619284D0 (en) 1996-09-16 1996-10-30 Celltech Therapeutics Ltd Chemical compounds
GB9622363D0 (en) 1996-10-28 1997-01-08 Celltech Therapeutics Ltd Chemical compounds
ATE401312T1 (de) 1997-12-15 2008-08-15 Astellas Pharma Inc Pyrimidin-5-carboxamid-derivate
US6303652B1 (en) 1998-08-21 2001-10-16 Hughes Institute BTK inhibitors and methods for their identification and use
ATE342892T1 (de) 1998-08-29 2006-11-15 Astrazeneca Ab Pyrimidine verbindungen
PL204427B1 (pl) 1998-11-10 2010-01-29 Janssen Pharmaceutica Nv Hamująca replikację wirusa HIV pochodna pirymidyny, sposób jej wytwarzania i zastosowanie oraz kompozycja farmaceutyczna
US6262088B1 (en) 1998-11-19 2001-07-17 Berlex Laboratories, Inc. Polyhydroxylated monocyclic N-heterocyclic derivatives as anti-coagulants
US6127376A (en) 1998-12-04 2000-10-03 Berlex Laboratories, Inc. Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants
GB9828511D0 (en) 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
US6495558B1 (en) 1999-01-22 2002-12-17 Amgen Inc. Kinase inhibitors
EP1150955A2 (en) 1999-02-04 2001-11-07 Millennium Pharmaceuticals, Inc. G-protein coupled heptahelical receptor binding compounds and methods of use thereof
GB9914258D0 (en) 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
HRP20010969B1 (en) 1999-06-29 2005-04-30 Egis Gy�Gyszergy�R Rt. Novel piperazinylalkylthiopyrimidine derivatives,
EP1246823A1 (en) 1999-12-28 2002-10-09 Pharmacopeia, Inc. Pyrimidine and triazine kinase inhibitors
WO2001060816A1 (en) 2000-02-17 2001-08-23 Amgen Inc. Kinase inhibitors
GB0004887D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004888D0 (en) * 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
US7034019B2 (en) 2000-05-08 2006-04-25 Janssen Pharmaceutica N.V. Prodrugs of HIV replication inhibiting pyrimidines
US7427689B2 (en) 2000-07-28 2008-09-23 Georgetown University ErbB-2 selective small molecule kinase inhibitors
US6881737B2 (en) 2001-04-11 2005-04-19 Amgen Inc. Substituted triazinyl acrylamide derivatives and methods of use
JO3429B1 (ar) 2001-08-13 2019-10-20 Janssen Pharmaceutica Nv مشتقات برميدينات مثبطة فيروس الايدز
US6939874B2 (en) 2001-08-22 2005-09-06 Amgen Inc. Substituted pyrimidinyl derivatives and methods of use
WO2003030909A1 (en) 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer
JP2005507423A (ja) 2001-11-01 2005-03-17 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ グリコーゲン合成酵素キナーゼ３ベータ阻害剤（ｇｓｋ３阻害剤）としてのヘテロアリールアミン
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
JP2005522438A (ja) 2002-02-08 2005-07-28 スミスクライン ビーチャム コーポレーション ピリミジン化合物
GB0206215D0 (en) 2002-03-15 2002-05-01 Novartis Ag Organic compounds
JP2005534286A (ja) 2002-03-21 2005-11-17 サネシス ファーマシューティカルズ， インコーポレイテッド キナーゼインヒビターの同定
US20040002395A1 (en) * 2002-06-27 2004-01-01 Poynor Raymond L. Bridge weight for metal wood golf club
JP2006514989A (ja) 2002-07-29 2006-05-18 ライジェル ファーマシューティカルズ ２，４−ピリミジンジアミン化合物による自己免疫疾患の治療および予防方法
CA2439440A1 (en) 2002-09-05 2004-03-05 Emory University Treatment of tuberous sclerosis associated neoplasms
AU2002951853A0 (en) 2002-10-04 2002-10-24 Commonwealth Scientific And Industrial Research Organisation Crystal structure of erbb2 and uses thereof
WO2004050068A1 (en) 2002-11-29 2004-06-17 Janssen Pharmaceutica N.V. Pharmaceutical compositions comprising a basic respectively acidic drug compound, a surfactant and a physiologically tolerable water-soluble acid respectively base
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
JP5602333B2 (ja) 2003-02-07 2014-10-08 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Ｈｉｖ感染の予防のためのピリミジン誘導体
EP1597251B1 (en) 2003-02-20 2009-06-10 SmithKline Beecham Corporation Pyrimidine compounds
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
US20050014753A1 (en) 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors
US20050043233A1 (en) 2003-04-29 2005-02-24 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation, migration or apoptosis of myeloma cells or angiogenesis
US7504396B2 (en) 2003-06-24 2009-03-17 Amgen Inc. Substituted heterocyclic compounds and methods of use
KR20120062863A (ko) 2003-07-30 2012-06-14 리겔 파마슈티칼스, 인크. 자가면역 질환의 치료 또는 예방에 사용하기 위한 2,4-피리미딘디아민 화합물
SI1663242T1 (sl) 2003-08-07 2011-09-30 Rigel Pharmaceuticals Inc 2,4-pirimidindiaminske spojine in uporabe kot antiproliferativna sredstva
PL2287156T3 (pl) * 2003-08-15 2013-11-29 Novartis Ag 2,4-Di(fenyloamino)-pirymidyny stosowane w leczeniu chorób nowotworowych, chorób zapalnych i zaburzeń układu immunologicznego
GB0321710D0 (en) * 2003-09-16 2003-10-15 Novartis Ag Organic compounds
EP1663992A1 (en) 2003-09-18 2006-06-07 Novartis AG 2,4-di (phenylamino) pyrimidines useful in the treatment of proliferative disorders
US7511137B2 (en) 2003-12-19 2009-03-31 Rigel Pharmaceuticals, Inc. Stereoisomers and stereoisomeric mixtures of 1-(2,4-pyrimidinediamino)-2-cyclopentanecarboxamide synthetic intermediates
ES2389203T3 (es) 2004-01-12 2012-10-24 Ym Biosciences Australia Pty Ltd Inhibidores de quinasa selectivos
WO2005070890A2 (en) 2004-01-16 2005-08-04 Wyeth Quinoline intermediates of receptor tyrosine kinase inhibitors and the synthesis thereof
CA2557794A1 (en) 2004-03-15 2005-10-06 Eli Lilly And Company Opioid receptor antagonists
US7558717B2 (en) 2004-04-28 2009-07-07 Vertex Pharmaceuticals Incorporated Crystal structure of human JAK3 kinase domain complex and binding pockets thereof
CA2566531A1 (en) 2004-05-18 2005-12-15 Rigel Pharmaceuticals, Inc. Cycloalkyl substituted pyrimidinediamine compounds and their uses
EP1598343A1 (de) 2004-05-19 2005-11-23 Boehringer Ingelheim International GmbH 2-Arylaminopyrimidine als PLK Inhibitoren
ES2564127T5 (es) 2004-06-04 2020-03-26 Genentech Inc Mutaciones en EGFR
US7521457B2 (en) 2004-08-20 2009-04-21 Boehringer Ingelheim International Gmbh Pyrimidines as PLK inhibitors
GB0419161D0 (en) 2004-08-27 2004-09-29 Novartis Ag Organic compounds
US7622486B2 (en) 2004-09-23 2009-11-24 Reddy Us Therapeutics, Inc. Pyridine compounds, process for their preparation and compositions containing them
EP1797048B1 (en) 2004-09-30 2011-08-17 Tibotec Pharmaceuticals Hiv inhibiting 5-carbo- or heterocyclic substituted pyrimidines
WO2006044457A1 (en) 2004-10-13 2006-04-27 Wyeth N-benzenesulfonyl substituted anilino-pyrimidine analogs
EP2100899A3 (en) 2004-10-20 2009-09-30 Proteolix, Inc. Compounds for proteasome enzyme inhibition
WO2006053109A1 (en) 2004-11-10 2006-05-18 Synta Pharmaceuticals Corp. Heteroaryl compounds
GB2420559B (en) 2004-11-15 2008-08-06 Rigel Pharmaceuticals Inc Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses
WO2006068770A1 (en) 2004-11-24 2006-06-29 Rigel Pharmaceuticals, Inc. Spiro-2, 4-pyrimidinediamine compounds and their uses
MY169441A (en) 2004-12-08 2019-04-11 Janssen Pharmaceutica Nv 2,4, (4,6) pyrimidine derivatives
JP5208516B2 (ja) * 2004-12-30 2013-06-12 エグゼリクシス， インコーポレイテッド キナーゼモジュレーターとしてのピリミジン誘導体および使用方法
AU2006204724A1 (en) 2005-01-14 2006-07-20 Millennium Pharmaceuticals, Inc. Cinnamide and hydrocinnamide derivatives with raf-kinase inhibitory activity
DK1856135T3 (da) 2005-01-19 2010-04-12 Rigel Pharmaceuticals Inc Prodrugs af 2,4-pyrimidindiamin-forbindelser og deres anvendelser
EP2505591A1 (en) 2005-02-11 2012-10-03 Memorial Sloan-Kettering Cancer Center Methods and compositions for detecting a drug resistant EGFR mutant
US20060247250A1 (en) * 2005-03-16 2006-11-02 Targegen, Inc. Pyrimidine inhibitors of kinases
DE102005016634A1 (de) * 2005-04-12 2006-10-19 Merck Patent Gmbh Neuartige Aza-Hetercyclen als Kinase-Inhibitoren
WO2007027238A2 (en) 2005-05-03 2007-03-08 Rigel Pharmaceuticals, Inc. Jak kinase inhibitors and their uses
WO2006124874A2 (en) 2005-05-12 2006-11-23 Kalypsys, Inc. Inhibitors of b-raf kinase
WO2006128172A2 (en) 2005-05-26 2006-11-30 Synta Pharmaceuticals Corp. Method for treating b cell regulated autoimmune disorders
WO2006128129A2 (en) 2005-05-26 2006-11-30 Synta Pharmaceuticals Corp. Method for treating cancer
WO2006129100A1 (en) 2005-06-03 2006-12-07 Glaxo Group Limited Novel compounds
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
CN101282945A (zh) * 2005-06-08 2008-10-08 里格尔药品股份有限公司 抑制jak途径的组合物和方法
ES2651349T3 (es) * 2005-06-08 2018-01-25 Rigel Pharmaceuticals, Inc. Composiciones y métodos para la inhibición de la ruta JAK
AU2006283592A1 (en) 2005-08-22 2007-03-01 Amgen Inc. Pyrazolopyridine and pyrazolopyrimidine compounds useful as kinase enzymes modulators
US8101625B2 (en) 2005-10-21 2012-01-24 Exelixis, Inc. Pyrimidinones as Casein Kinase II (CK2) modulators
MX391408B (es) 2005-11-01 2025-03-21 Impact Biomedicines Inc Inhibidores de biaril meta-pirimidina de cinasas.
CA2626479A1 (en) * 2005-11-03 2007-05-18 Irm Llc Protein kinase inhibitors
US7713987B2 (en) 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
EP1968950A4 (en) * 2005-12-19 2010-04-28 Genentech Inc PYRIMIDINKINASEINHIBITOREN
TW200736232A (en) * 2006-01-26 2007-10-01 Astrazeneca Ab Pyrimidine derivatives
JP2009525337A (ja) 2006-01-30 2009-07-09 エクセリクシス， インク． Ｊａｋ−２調節因子としての４−アリール−２−アミノ−ピリミジン類又は４−アリール−２−アミノアルキル−ピリミジン類と使用方法
PT1984357E (pt) 2006-02-17 2013-12-23 Rigel Pharmaceuticals Inc Compostos de 2,4-pirimidinadiamina para tratamento ou prevenção de doenças autoimunes
ES2622493T3 (es) 2006-02-24 2017-07-06 Rigel Pharmaceuticals, Inc. Composiciones y métodos para la inhibición de la ruta de JAK
RU2452737C2 (ru) 2006-03-30 2012-06-10 Тиботек Фармасьютикалз Лтд. 5-(гидроксиметилен- и аминометилен)замещенные пиримидины, ингибирующие вич
AU2007233737B2 (en) 2006-03-30 2012-11-29 Janssen Sciences Ireland Uc HIV inhibiting 5-amido substituted pyrimidines
GB0608386D0 (en) 2006-04-27 2006-06-07 Senexis Ltd Compounds
JP5682051B2 (ja) 2006-05-18 2015-03-11 ファーマサイクリックス，インク． 細胞内キナーゼ阻害剤
DE102006027156A1 (de) 2006-06-08 2007-12-13 Bayer Schering Pharma Ag Sulfimide als Proteinkinaseinhibitoren
CA2656290A1 (en) 2006-07-05 2008-01-10 Exelixis, Inc. Methods of using igf1r and abl kinase modulators
RU2009105826A (ru) 2006-07-21 2010-08-27 Новартис АГ (CH) 2,4-ди(ариламино)питимидин-5-карбоксамидные соединения в качестве ингибиторов jak-киназ
DE102006041382A1 (de) 2006-08-29 2008-03-20 Bayer Schering Pharma Ag Carbamoyl-Sulfoximide als Proteinkinaseinhibitoren
HUE028086T2 (en) 2006-09-22 2016-11-28 Pharmacyclics Llc Inhibitors of bruton's tyrosine kinase
ES2403546T3 (es) 2006-11-03 2013-05-20 Pharmacyclics, Inc. Sonda de actividad de la tirosina-cinasa de Bruton y procedimiento de utilización
JP5264759B2 (ja) 2006-11-21 2013-08-14 ライジェル ファーマシューティカルズ， インコーポレイテッド ２，４−ピリミジンジアミン化合物のプロドラッグ塩およびそれらの使用
EA017405B9 (ru) * 2006-12-08 2014-05-30 АйАрЭм ЭлЭлСи Соединения и композиции в качестве ингибиторов протеинкиназы
CA2670645A1 (en) * 2006-12-19 2008-07-03 Genentech, Inc. Pyrimidine kinase inhibitors
EP1939185A1 (de) 2006-12-20 2008-07-02 Bayer Schering Pharma Aktiengesellschaft Neuartige Hetaryl-Phenylendiamin-Pyrimidine als Proteinkinaseinhibitoren zur Behandlung von Krebs
US9006243B2 (en) 2006-12-29 2015-04-14 Janssen R&D Ireland HIV inhibiting 6-substituted pyrimidines
CN106045965A (zh) 2006-12-29 2016-10-26 爱尔兰詹森科学公司 抑制hiv的5,6‑取代的嘧啶类化合物
PE20081636A1 (es) 2007-01-26 2009-01-10 Smithkline Beecham Corp Inhibidores de antranilamida para aurora quinasa
WO2008092199A1 (en) 2007-01-31 2008-08-07 Cytopia Research Pty Ltd Thiopyrimidine-based compounds and uses thereof
DE102007010801A1 (de) 2007-03-02 2008-09-04 Bayer Cropscience Ag Diaminopyrimidine als Fungizide
BRPI0809189A2 (pt) 2007-03-20 2014-09-09 Smithkline Beecham Corp Composto ou um sal do mesmo, composição farmacêutica, métodos para tratar um distúrbio em um mamífero e para tratar câncer em um mamífero, e, uso de um composto
EA200901138A1 (ru) 2007-03-20 2010-04-30 Смитклайн Бичем Корпорейшн Производные дианилинопиримидина как ингибиторы киназы wee1, фармацевтическая композиция и применение
WO2008118822A1 (en) 2007-03-23 2008-10-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US7834024B2 (en) 2007-03-26 2010-11-16 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
US8809273B2 (en) 2007-03-28 2014-08-19 Pharmacyclics, Inc. Inhibitors of Bruton's tyrosine kinase
US20120065201A1 (en) 2007-03-28 2012-03-15 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
NZ582485A (en) * 2007-07-17 2012-05-25 Rigel Pharmaceuticals Inc Cyclic amine substituted pyrimidinediamines as pkc inhibitors
US20090088371A1 (en) 2007-08-28 2009-04-02 Rigel Pharmaceuticals, Inc. Combination therapy with syk kinase inhibitor
EP2190826A2 (en) 2007-08-28 2010-06-02 Irm Llc 2-biphenylamino-4-aminopyrimidine derivatives as kinase inhibitors
WO2009032703A1 (en) 2007-08-28 2009-03-12 Irm Llc 2- (het) arylamino-6-aminopyridine derivatives and fused forms thereof as anaplastic lymphoma kinase inhibitors
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
CA2710118A1 (en) 2007-12-20 2009-07-02 Cellzome Limited Sulfamides as zap-70 inhibitors
CA2715962C (en) 2008-02-22 2017-03-07 Rigel Pharmaceuticals, Inc. Use of 2,4-pyrimidinediamines for the treatment of atherosclerosis
EP2276747A1 (en) 2008-03-11 2011-01-26 Cellzome Limited Sulfonamides as zap-70 inhibitors
US8205348B2 (en) 2008-03-19 2012-06-26 Zashiki-Warashi Manufacturing Inc. Tile spacer and holder therefor
CL2009000600A1 (es) 2008-03-20 2010-05-07 Bayer Cropscience Ag Uso de compuestos de diaminopirimidina como agentes fitosanitarios; compuestos de diaminopirimidina; su procedimiento de preparacion; agente que los contiene; procedimiento para la preparacion de dicho agente; y procedimiento para combatir plagas de animales y/u hongos dañinos patogenos de plantas.
DE102008018910A1 (de) * 2008-04-14 2009-12-31 Basf Coatings Ag Verfahren zur Herstellung effektpigmenthaltiger Farbrezepturen
WO2009127642A2 (en) 2008-04-15 2009-10-22 Cellzome Limited Use of lrrk2 inhibitors for neurodegenerative diseases
DK2321283T3 (en) 2008-04-16 2016-10-31 Portola Pharm Inc 2,6-diamino-pyrimidine-5-ylcarboxamides as inhibitors of Syk OR JAK Kinases
US8138339B2 (en) * 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
EP2323993B1 (en) * 2008-04-16 2015-06-03 Portola Pharmaceuticals, Inc. 2,6-diamino- pyrimidin- 5-yl-carboxamides as syk or jak kinases inhibitors
JP2011518836A (ja) 2008-04-24 2011-06-30 インサイト・コーポレイション 大環状化合物およびそれらのキナーゼ阻害剤としての使用
KR101860057B1 (ko) 2008-05-21 2018-05-21 어리어드 파마슈티칼스, 인코포레이티드 키나아제 억제제로서 포스포러스 유도체
EP2361248B1 (en) 2008-06-27 2018-09-19 Celgene CAR LLC Heteroaryl compounds and uses thereof
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
AU2009270856B2 (en) 2008-07-16 2013-07-25 Pharmacyclics Llc Inhibitors of Bruton's tyrosine kinase for the treatment of solid tumors
WO2010025833A1 (de) 2008-09-03 2010-03-11 Bayer Cropscience Ag Alkoxy- und alkylthio-substituierte anilinopyrimidine
US20110245156A1 (en) 2008-12-09 2011-10-06 Cytokine Pharmasciences, Inc. Novel antiviral compounds, compositions, and methods of use
CA2748758C (en) 2009-01-15 2017-06-13 F. Hoffmann-La Roche Ag Antibodies against phosphorylated tyrosines on erythropoietin receptor (epor)
EP2414337B1 (en) 2009-04-03 2013-05-01 Cellzome GmbH Methods for the identification of kinase interacting molecules and for the purification of kinase proteins
KR101705158B1 (ko) * 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Ｅｇｆｒ 억제제 및 질환 치료방법
HUE026647T2 (en) 2009-05-08 2016-07-28 Astellas Pharma Inc Diamino heterocyclic carboxamide compound
WO2010146132A1 (en) 2009-06-18 2010-12-23 Cellzome Limited Sulfonamides and sulfamides as zap-70 inhibitors
US7718662B1 (en) 2009-10-12 2010-05-18 Pharmacyclics, Inc. Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase
US20110207736A1 (en) 2009-12-23 2011-08-25 Gatekeeper Pharmaceuticals, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
US20130137709A1 (en) 2010-05-05 2013-05-30 Nathanael S. Gray Compounds that modulate EGFR activity and methods for treating or preventing conditions therewith
CA3113343C (en) 2010-06-03 2024-10-08 Pharmacyclics Llc USE OF BRUTON'S TYROSINE KINASE INHIBITORS IN THE TREATMENT OF FOLLICULAR LYMPHOMA
US20120071497A1 (en) 2010-06-03 2012-03-22 Pharmacyclics, Inc. Methods of treating abc-dlbcl using inhibitors of bruton's tyrosine kinase
WO2011153553A2 (en) 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition
EP2603081B1 (en) 2010-08-10 2016-10-05 Celgene Avilomics Research, Inc. Besylate salt of a btk inhibitor
TWI545115B (zh) 2010-11-01 2016-08-11 阿維拉製藥公司 雜環化合物及其用途
US9238629B2 (en) 2010-11-01 2016-01-19 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
WO2012061415A1 (en) 2010-11-01 2012-05-10 Portola Pharmaceuticals, Inc. Oxypyrimidines as syk modulators
WO2012064706A1 (en) 2010-11-10 2012-05-18 Avila Therapeutics, Inc. Mutant-selective egfr inhibitors and uses thereof
CN102558149A (zh) 2010-12-29 2012-07-11 中国医学科学院药物研究所 嘧啶衍生物、及其制法和药物组合物与用途
EP2704572B1 (en) 2011-05-04 2015-12-30 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
JP6068451B2 (ja) 2011-05-17 2017-01-25 ザ・リージエンツ・オブ・ザ・ユニバーシテイ・オブ・カリフオルニア キナーゼ阻害剤
BR112014009276A8 (pt) 2011-10-19 2017-06-20 Pharmacyclics Inc uso de inibidores de tirosina quinase de bruton (btk)
CN103159742B (zh) 2011-12-16 2015-08-12 北京韩美药品有限公司 5-氯嘧啶类化合物及其作为egfr酪氨酸激酶抑制剂的应用
CN104302178B (zh) 2012-03-15 2018-07-13 西建卡尔有限责任公司 表皮生长因子受体激酶抑制剂的固体形式
CN111329989A (zh) 2012-11-02 2020-06-26 药品循环有限责任公司 Tec家族激酶抑制剂辅助疗法
JP6800750B2 (ja) 2013-08-02 2020-12-16 ファーマサイクリックス エルエルシー 固形腫瘍の処置方法

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2299201C2 (ru) * 2000-07-11 2007-05-20 Астразенека Аб Производные пиримидина, способ их получения (варианты), фармацевтические композиции (варианты) и способ ингибирования
US20080194603A1 (en) * 2006-10-19 2008-08-14 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US20080300268A1 (en) * 2007-06-04 2008-12-04 Avila Therapeutics, Inc. Heterocyclic compounds and uses thereof
WO2009017838A2 (en) * 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
US20090137588A1 (en) * 2007-10-19 2009-05-28 Avila Therapeutics, Inc. Heteroaryl compounds and uses thereof

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
Pubchem, 20100201 CID 44594695. *
US 2005085637 A1, 21/04/2005. US 2006270694 A1, 30/11. 2006. *
Wenjun Zhou et al., Novel mutant-selective EGFR kinase inhibitors against EGFR T790M Nature, 20091224 not Macmillan Journals Ltd., etc. Vol:462, Nr:7276, Page(s):1070 - 1074. *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2702631C2 (ru) * 2014-10-11 2019-10-09 Шанхай Хэнсох Биомедикал Ко., Лтд. Ингибитор egfr и его получение и применение

Also Published As

Publication number Publication date
IL235621A0 (en) 2014-12-31
JP5879270B2 (ja) 2016-03-08
US20140213574A1 (en) 2014-07-31
US10010548B2 (en) 2018-07-03
MX2012007507A (es) 2012-08-01
CN106146407A (zh) 2016-11-23
BR112012018345B1 (pt) 2021-10-19
US20190192512A1 (en) 2019-06-27
CN102740847B (zh) 2016-06-29
EP2519235A4 (en) 2013-07-31
EP2519235A1 (en) 2012-11-07
US8710222B2 (en) 2014-04-29
NZ600631A (en) 2014-10-31
RU2012123546A (ru) 2014-02-10
KR101747159B1 (ko) 2017-06-15
CA2783624C (en) 2019-08-20
PH12012501346A1 (en) 2012-12-17
WO2011090760A4 (en) 2011-09-29
US8338439B2 (en) 2012-12-25
US9409921B2 (en) 2016-08-09
NZ700236A (en) 2016-06-24
AU2010343055A1 (en) 2012-06-21
EP2519235B1 (en) 2018-11-21
KR20170086547A (ko) 2017-07-26
TWI592405B (zh) 2017-07-21
AU2010343055B2 (en) 2016-11-10
JP2016117749A (ja) 2016-06-30
CA2783624A1 (en) 2011-07-28
TW201124399A (en) 2011-07-16
BR112012018345A2 (pt) 2018-07-10
US20130065899A1 (en) 2013-03-14
JP2013515786A (ja) 2013-05-09
US20100249092A1 (en) 2010-09-30
IL220155B (en) 2019-05-30
US20170100397A1 (en) 2017-04-13
SG181962A1 (en) 2012-08-30
KR20120118020A (ko) 2012-10-25
IL220155A0 (en) 2012-07-31
AU2017200697A1 (en) 2017-02-23
US10596172B2 (en) 2020-03-24
WO2011090760A1 (en) 2011-07-28
MX341825B (es) 2016-09-05
CN102740847A (zh) 2012-10-17

Similar Documents

Publication Publication Date Title
RU2636584C2 (ru) Гетероарильные соединения и их применение
JP6853307B2 (ja) ヘテロアリール化合物およびそれらの使用
US11351168B1 (en) 2,4-disubstituted pyrimidines useful as kinase inhibitors

Legal Events

Date Code Title Description
HZ9A Changing address for correspondence with an applicant
PC43 Official registration of the transfer of the exclusive right without contract for inventions

Effective date: 20190902