[go: up one dir, main page]

MX2013012983A - Composiciones y metodos para la produccion de compuestos de pirimidina con actividad inhibidora de tirosina cinasa de bruton. - Google Patents

Composiciones y metodos para la produccion de compuestos de pirimidina con actividad inhibidora de tirosina cinasa de bruton.

Info

Publication number
MX2013012983A
MX2013012983A MX2013012983A MX2013012983A MX2013012983A MX 2013012983 A MX2013012983 A MX 2013012983A MX 2013012983 A MX2013012983 A MX 2013012983A MX 2013012983 A MX2013012983 A MX 2013012983A MX 2013012983 A MX2013012983 A MX 2013012983A
Authority
MX
Mexico
Prior art keywords
formula
pyrimidine
pyridine compounds
compositions
production
Prior art date
Application number
MX2013012983A
Other languages
English (en)
Other versions
MX354412B (es
Inventor
Brian L Hodous
Lesley Liu-Bujalski
Reinaldo Jones
Donald Bankston
Theresa L Johnson
Igor Mochalkin
Ngan Nguyen
Hui Qiu
Andreas Goutopoulos
Nadia Brugger
Original Assignee
Merck Patent Gmbh
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 Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of MX2013012983A publication Critical patent/MX2013012983A/es
Publication of MX354412B publication Critical patent/MX354412B/es

Links

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
    • A61K31/69—Boron compounds
    • 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
    • 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
    • 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
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61P11/04—Drugs for disorders of the respiratory system for throat disorders
    • 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
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • 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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/02—Local antiseptics
    • 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
    • A61P37/02—Immunomodulators
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/68—One oxygen atom attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with 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
    • C07D213/72—Nitrogen atoms
    • C07D213/73—Unsubstituted amino or imino radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with 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
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • 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
    • 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
    • C07D239/49—Two nitrogen atoms with an aralkyl radical, or substituted aralkyl radical, attached in position 5, e.g. trimethoprim
    • 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
    • C07D403/04—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
    • C07D403/14—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 three or more hetero rings
    • 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
    • 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
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • 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
    • C07D471/08—Bridged 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
    • C07D471/10—Spiro-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
    • C07D487/10—Spiro-condensed 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/022—Boron compounds without C-boron linkages

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Reproductive Health (AREA)
  • Pain & Pain Management (AREA)
  • Otolaryngology (AREA)
  • Communicable Diseases (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)

Abstract

La presente invención proporciona nuevos compuestos de pirimidina y piridina de acuerdo con la Fórmula (I), Fórmula (II), Fórmula (III), Fórmula (IV) y Fórmula (V), su manufactura y uso para el tratamiento de enfermedades hiperproliferativas, incluyendo, pero no se limitan a, cáncer, lupus, enfermedades alérgicas, enfermedad de Sjogren y artritis reumatoide. En las modalidades preferidas, la presente invención describe inhibidores de cinasa irreversibles, que incluyen, pero no se limitan a, inhibidores de tirosina cinasa de Bruton.
MX2013012983A 2011-06-10 2012-06-10 Composiciones y metodos para la produccion de compuestos de pirimidina con actividad inhibidora de tirosina cinasa de bruton. MX354412B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161495773P 2011-06-10 2011-06-10
PCT/US2012/041803 WO2012170976A2 (en) 2011-06-10 2012-06-10 Compositions and methods for the production of pyrimidine and pyridine compounds with btk inhibitory activity

Publications (2)

Publication Number Publication Date
MX2013012983A true MX2013012983A (es) 2013-12-06
MX354412B MX354412B (es) 2018-03-05

Family

ID=46317541

Family Applications (2)

Application Number Title Priority Date Filing Date
MX2013012983A MX354412B (es) 2011-06-10 2012-06-10 Composiciones y metodos para la produccion de compuestos de pirimidina con actividad inhibidora de tirosina cinasa de bruton.
MX2018002621A MX373151B (es) 2011-06-10 2012-06-10 Composiciones y métodos para la producción de compuestos de pirimidina y piridina con actividad inhibidora de tirosina cinasa de bruton (btk).

Family Applications After (1)

Application Number Title Priority Date Filing Date
MX2018002621A MX373151B (es) 2011-06-10 2012-06-10 Composiciones y métodos para la producción de compuestos de pirimidina y piridina con actividad inhibidora de tirosina cinasa de bruton (btk).

Country Status (24)

Country Link
US (4) US9073947B2 (es)
EP (2) EP2718270B1 (es)
JP (4) JP2014517016A (es)
KR (5) KR20140007954A (es)
CN (2) CN103814016B (es)
AU (2) AU2012267491B2 (es)
BR (1) BR112013030442B1 (es)
CA (1) CA2833771C (es)
CY (1) CY1125494T1 (es)
DK (1) DK2718270T3 (es)
EA (2) EA027584B1 (es)
ES (1) ES2923760T3 (es)
HR (1) HRP20220886T1 (es)
HU (1) HUE059230T2 (es)
IL (1) IL229863A (es)
LT (1) LT2718270T (es)
MX (2) MX354412B (es)
PL (1) PL2718270T3 (es)
PT (1) PT2718270T (es)
RS (1) RS63418B1 (es)
SG (3) SG10201604682VA (es)
SI (1) SI2718270T1 (es)
WO (1) WO2012170976A2 (es)
ZA (1) ZA201307632B (es)

Families Citing this family (82)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20140007954A (ko) * 2011-06-10 2014-01-20 메르크 파텐트 게엠베하 Btk 억제 활성을 갖는 피리미딘 및 피리딘 화합물의 조성물 및 제조방법
WO2014055934A2 (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
WO2014093230A2 (en) * 2012-12-10 2014-06-19 Merck Patent Gmbh Compositions and methods for the production of pyrimidine and pyridine compounds with btk inhibitory activity
RU2015137298A (ru) * 2013-03-05 2017-04-10 Ф. Хоффманн-Ля Рош Аг Ингибиторы тирозинкиназы брутона
HK1218756A1 (zh) * 2013-03-11 2017-03-10 默克专利有限公司 用作激酶活性调节剂的6-[4-(1h-咪唑-2-基)哌啶-1-基]嘧啶-4-胺衍生物
ES2619125T3 (es) 2013-04-25 2017-06-23 Beigene, Ltd. Compuestos heterocíclicos fusionados como inhibidores de proteína cinasa
CN104140395B (zh) * 2013-05-08 2018-07-24 中国医学科学院药物研究所 丁炔酰胺衍生物及其制法和药物组合物与用途
CN104447727B (zh) * 2013-09-02 2018-04-27 广东东阳光药业有限公司 取代的氨基嘧啶类化合物及其使用方法和用途
IL296026B2 (en) 2013-09-13 2024-10-01 Beigene Switzerland Gmbh Anti-pd1 antibodies and their use as therapeutics and diagnostics
AU2014321420B2 (en) * 2013-09-22 2017-06-15 Sunshine Lake Pharma Co., Ltd. Substituted aminopyrimidine compounds and methods of use
SI3052476T1 (sl) * 2013-09-30 2020-12-31 Guangzhou Innocare Pharma Tech Co., Ltd. Substituirani nikotinimidni inhibitorji BTK in njihova priprava in uporaba pri zdravljenju raka, vnetja in avtoimunske bolezni
PT3060550T (pt) * 2013-10-21 2019-08-27 Merck Patent Gmbh Compostos de heteroarilo como inibidores de btk e utilizações dos mesmos
US9512084B2 (en) 2013-11-29 2016-12-06 Novartis Ag Amino pyrimidine derivatives
EP3079682A4 (en) * 2013-12-13 2017-08-30 Dana-Farber Cancer Institute, Inc. Methods to treat lymphoplasmacytic lymphoma
JP6879740B2 (ja) * 2013-12-13 2021-06-02 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 リンパ形質細胞性リンパ腫を処置する方法
RU2016139697A (ru) 2014-03-12 2018-04-12 Новартис Аг Комбинация, содержащая ингибитор btk и ингибитор akt
WO2015164294A1 (en) * 2014-04-22 2015-10-29 The Feinstein Institute For Medical Research Treatment of solid tumors by inhibiting mrk/zak
JP6526189B2 (ja) 2014-07-03 2019-06-05 ベイジーン リミテッド 抗ｐｄ−ｌ１抗体並びにその治療及び診断のための使用
WO2016025621A1 (en) * 2014-08-13 2016-02-18 Celgene Avilomics Research, Inc. Methods of treatment using an erk inhibitor
WO2016025651A1 (en) * 2014-08-13 2016-02-18 Celgene Avilomics Research, Inc. Combinations of an erk inhibitor and a tor inhibitor and related methods
WO2016025650A1 (en) * 2014-08-13 2016-02-18 Celgene Avilomics Research, Inc. Combinations of an erk inhibitor and a cdk4/6 inhibitor and related methods
WO2016025567A1 (en) * 2014-08-13 2016-02-18 Celgene Avilomics Research, Inc. Oral formulations and uses thereof
DK3179858T3 (da) 2014-08-13 2019-07-22 Celgene Car Llc Forme og sammensætninger af en ERK-inhibitor
CA2965178C (en) 2014-10-22 2023-09-26 Dana-Farber Cancer Institute, Inc. Thiazolyl-containing compounds for treating proliferative diseases
CN107209186A (zh) * 2014-12-11 2017-09-26 默克专利有限公司 Btk抑制剂的测定
CN105837576B (zh) * 2015-01-14 2019-03-26 湖北生物医药产业技术研究院有限公司 Btk抑制剂
WO2016134668A1 (en) * 2015-02-28 2016-09-01 Sunshine Lake Pharma Co., Ltd. Substituted aminopyrimidine compounds and methods of use
CN104844573A (zh) * 2015-04-17 2015-08-19 中国药科大学 嘧啶类btk抑制剂、其制备方法及医药用途
EP3302550B1 (en) 2015-05-26 2019-08-28 MorphoSys AG Combination of an anti-cd19 antibody and a bruton's tyrosine kinase inhibitor and uses thereof
JP6469238B2 (ja) 2015-09-18 2019-02-13 科研製薬株式会社 ビアリール誘導体及びそれを含有する医薬
RU2022100782A (ru) * 2015-11-04 2022-02-03 Мерк Патент Гмбх Способы лечения злокачественной опухоли с использованием соединений пиримидина и пиридина с btk ингибирующей активностью
ES2964946T3 (es) * 2015-11-17 2024-04-10 Merck Patent Gmbh Métodos para tratar esclerosis múltiple usando compuestos de pirimidina con actividad inhibidora de tirosina cinasa de bruton
WO2017111076A1 (ja) * 2015-12-24 2017-06-29 協和発酵キリン株式会社 α、β不飽和アミド化合物
CN105732638B (zh) * 2016-01-22 2018-01-30 成都倍特药业有限公司 一种具有螺环或桥环结构的布鲁顿酪氨酸激酶抑制剂及其制备方法
KR20250079083A (ko) * 2016-06-10 2025-06-04 비타이 파마슈티컬즈, 엘엘씨 메닌-mll 상호 작용의 억제제
WO2018007885A1 (en) 2016-07-05 2018-01-11 Beigene, Ltd. COMBINATION OF A PD-l ANTAGONIST AND A RAF INHIBITOR FOR TREATING CANCER
SG11201901141WA (en) 2016-08-16 2019-03-28 Beigene Ltd Crystalline form of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof
PT3500299T (pt) 2016-08-19 2024-02-21 Beigene Switzerland Gmbh Combinação de zanubrutinib com um anticorpo anti-cd20 ou anti-pd-1 para utilização no tratamento do cancro
EP3515414B1 (en) 2016-09-19 2022-11-30 MEI Pharma, Inc. Combination therapy
CN110461847B (zh) 2017-01-25 2022-06-07 百济神州有限公司 (S)-7-(1-(丁-2-炔酰基)哌啶-4-基)-2-(4-苯氧基苯基)-4,5,6,7-四氢吡唑并[1,5-a]嘧啶-3-甲酰胺的结晶形式、其制备及用途
US10464923B2 (en) 2017-02-27 2019-11-05 Merck Patent Gmbh Crystalline forms of 1-(4-{[6-amino-5-(4-phenoxy-phenyl)-pyrimidin-4-ylamino]-methyl}-piperidin-1-yl)-propenone
EP3618818A4 (en) * 2017-05-03 2020-12-09 Vivace Therapeutics, Inc. NON-CONDENSED TRICYCLIC COMPOUNDS
KR20200019979A (ko) * 2017-06-23 2020-02-25 쿄와 기린 가부시키가이샤 α, β 불포화 아미드 화합물
TWI877099B (zh) 2017-06-26 2025-03-21 英屬開曼群島商百濟神州有限公司 抗ｐｄ－１抗體或其抗原結合片段在製備治療用於患有肝細胞癌（ｈｃｃ）之藥物的用途
WO2019034009A1 (en) 2017-08-12 2019-02-21 Beigene, Ltd. BTK INHIBITOR WITH ENHANCED DOUBLE SELECTIVITY
TWI694995B (zh) * 2017-11-06 2020-06-01 美商美國禮來大藥廠 Btk抑制劑化合物
CN109824603B (zh) * 2017-11-23 2021-03-12 浙江省化工研究院有限公司 一种嘧啶胺类化合物、其制备方法及应用
WO2019108795A1 (en) 2017-11-29 2019-06-06 Beigene Switzerland Gmbh Treatment of indolent or aggressive b-cell lymphomas using a combination comprising btk inhibitors
US11325896B2 (en) 2017-12-20 2022-05-10 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor M4
US20210113568A1 (en) 2018-04-27 2021-04-22 Ono Pharmaceutical Co., Ltd. PREVENTIVE AND/OR THERAPEUTIC AGENT FOR AUTOIMMUNE DISEASE COMPRISING COMPOUND HAVING Btk INHIBITORY ACTIVITY AS ACTIVE INGREDIENT
MY206797A (en) * 2018-06-19 2025-01-08 Merck Patent Gmbh Novel crystalline forms of 1-(4-{[6-amino-5-(4-phenoxy-phenyl)-pyrimidin-4-ylamino]-methyl}-4-fluoro-piperidin-1-yl)-propenone, salt forms thereof, and processes to obtain
CA3106772A1 (en) * 2018-07-20 2020-01-23 Merck Patent Gmbh A substituted amino-pyrimidine compound for use in a method for treatment and prevention of multiple sclerosis
CA3103943A1 (en) 2018-07-25 2020-01-30 Novartis Ag Nlrp3 inflammasome inhibitors
CA3111126A1 (en) 2018-08-31 2020-03-05 Stichting Katholieke Universiteit Synergistic combinations of amino acid depletion agent sensitizers (aadas) and amino acid depletion agents (aada), and therapeutic methods of use thereof
KR102190019B1 (ko) 2018-10-23 2020-12-15 삼진제약주식회사 쇼그렌 증후군 예방 또는 치료용 조성물
CN111499613B (zh) * 2019-01-31 2023-05-12 浙江海正药业股份有限公司 N-甲酰胺衍生物、其制备方法及其在医药上的用途
CN114364798A (zh) 2019-03-21 2022-04-15 欧恩科斯欧公司 用于治疗癌症的Dbait分子与激酶抑制剂的组合
AR119731A1 (es) 2019-05-17 2022-01-05 Novartis Ag Inhibidores del inflamasoma nlrp3
TWI856111B (zh) 2019-06-10 2024-09-21 瑞士商百濟神州瑞士有限責任公司 一種含有布魯頓氏酪胺酸激酶抑制劑的口服固體錠劑及其製備方法
JP2023500906A (ja) 2019-11-08 2023-01-11 インサーム（インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル） キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
WO2021211782A1 (en) * 2020-04-15 2021-10-21 Telios Pharma, Inc. Methods of treating acute lung injury and acute respiratory distress syndrome
AU2021325431B2 (en) 2020-08-14 2024-01-18 Novartis Ag Heteroaryl substituted spiropiperidinyl derivatives and pharmaceutical uses thereof
CN112250666B (zh) * 2020-10-09 2022-01-14 广东东阳光药业有限公司 取代的嘧啶类化合物及其用途
EP4255569A4 (en) * 2020-12-02 2024-10-23 Telios Pharma, Inc. METHODS AND COMPOSITIONS FOR THE TREATMENT OF AN OPHTHALMIC CONDITION
CN118434732A (zh) 2020-12-10 2024-08-02 建新公司 Tolebrutinib的晶型及其制备方法和用途
WO2022140246A1 (en) 2020-12-21 2022-06-30 Hangzhou Jijing Pharmaceutical Technology Limited Methods and compounds for targeted autophagy
WO2022212893A1 (en) 2021-04-02 2022-10-06 Biogen Ma Inc. Combination treatment methods of multiple sclerosis
JP2024517183A (ja) * 2021-04-27 2024-04-19 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド 転写増強アソシエートドメイン（ｔｅａｄ）転写因子阻害剤及びその使用
TW202311262A (zh) 2021-05-14 2023-03-16 美商錫達斯醫藥股份有限公司 Menin-mll交互作用之抑制劑
CN117561248A (zh) * 2021-07-07 2024-02-13 杭州领业医药科技有限公司 伊沃替尼和其盐的晶型及其制备方法和用途
WO2023285696A1 (en) 2021-07-15 2023-01-19 Sandoz Ag Mandelate form of 1-(4-(((6-amino-5-(4-phenoxyphenyl)pyrimidin-4-yl)amino)methyl)piperidin-1-yl)prop-2-en-1-one
CN115703770B (zh) * 2021-08-10 2025-07-18 深圳范恩柯尔精准医疗有限公司 嘧啶胺类化合物及其组合物和用途
CN116199668B (zh) * 2021-09-13 2025-06-13 都创(上海)医药开发有限公司 Evobrutinib化合物盐型及其制备方法
TWI878871B (zh) * 2022-05-09 2025-04-01 大陸商浙江同源康醫藥股份有限公司 多環類化合物及其用途
US11786531B1 (en) 2022-06-08 2023-10-17 Beigene Switzerland Gmbh Methods of treating B-cell proliferative disorder
CN119343340A (zh) * 2022-06-22 2025-01-21 普林斯匹亚生物制药公司 制备修饰的btk抑制剂的方法
US20260000669A1 (en) 2022-06-24 2026-01-01 Merck Patent Gmbh Treatment regimen for autoimmune diseases and inflammatory diseases
UY40374A (es) 2022-08-03 2024-02-15 Novartis Ag Inhibidores de inflamasoma nlrp3
WO2024091511A1 (en) * 2022-10-25 2024-05-02 Light Horse Therapeutics, Inc. Heterocyclic tead inhibitors
CN117986236B (zh) * 2022-11-07 2024-12-31 天津征程医药科技有限公司 氘代的嘧啶衍生物以及包含该化合物的药物组合物
US12414950B1 (en) 2024-05-21 2025-09-16 Telios Pharma Inc. Methods of treating indolent systemic mastocytosis

Family Cites Families (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB712595A (en) * 1952-01-30 1954-07-28 Rhone Poulenc Sa New pyrimidines and processes for their production
US5002949A (en) * 1990-05-01 1991-03-26 American Home Products Corporation 5-substituted-6-aminopyrimidine derivatives
GB9012316D0 (en) * 1990-06-01 1990-07-18 Wellcome Found Pharmacologically active cns compounds
US5055476A (en) * 1990-08-13 1991-10-08 Hoechst-Roussel Pharmaceuticals Incorporated 3-(1,2-benzisoxazol-3-yl)-4-pyridinamines and derivatives
JPH0583246A (ja) * 1991-07-29 1993-04-02 Fujitsu Ltd 網状回線の通信方式
JPH08283246A (ja) 1994-06-01 1996-10-29 Nippon Soda Co Ltd ピリミジン誘導体、その製造方法及び有害生物防除剤
ES2079323B1 (es) * 1994-06-21 1996-10-16 Vita Invest Sa Derivados de indol utiles para el tratamiento de la migraña, composicion y uso correspondientes.
US5525606A (en) * 1994-08-01 1996-06-11 The United States Of America As Represented By The Department Of Health And Human Services Substituted 06-benzylguanines and 6(4)-benzyloxypyrimidines
DE19604190A1 (de) * 1996-02-06 1997-08-07 Hoechst Ag Nagelwachstumsfördernde Zubereitungen
US6440965B1 (en) * 1997-10-15 2002-08-27 Krenitsky Pharmaceuticals, Inc. Substituted pyrimidine derivatives, their preparation and their use in the treatment of neurodegenerative or neurological disorders of the central nervous system
US6887870B1 (en) * 1999-10-12 2005-05-03 Bristol-Myers Squibb Company Heterocyclic sodium/proton exchange inhibitors and method
ATE419239T1 (de) 2000-10-20 2009-01-15 Eisai R&D Man Co Ltd Verfahren zur herstellung von 4-phenoxy chinolin derivaten
EP1348706B1 (en) * 2000-12-08 2009-08-19 Takeda Pharmaceutical Company Limited Substituted thiazole derivatives bearing 3-pyridyl groups, process for preparing the same and use thereof
GB0115602D0 (en) * 2001-06-26 2001-08-15 Syngenta Participations Ag Organic compounds
US20050171131A1 (en) * 2003-09-26 2005-08-04 Christi Kosogof Diaminopyrimidine derivatives as growth hormone secrectgogue receptor (GHS-R) antagonists
WO2005073224A2 (en) 2004-01-23 2005-08-11 Amgen Inc Quinoline quinazoline pyridine and pyrimidine counds and their use in the treatment of inflammation angiogenesis and cancer
US7528138B2 (en) * 2004-11-04 2009-05-05 Vertex Pharmaceuticals Incorporated Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases
CN101184493A (zh) * 2005-03-04 2008-05-21 阿尔斯根公司 用乙胺嘧啶及类似物治疗肌萎缩性侧索硬化
GB0512844D0 (en) * 2005-06-23 2005-08-03 Novartis Ag Organic compounds
RU2008121974A (ru) 2005-11-03 2009-12-10 Айрм Ллк (Bm) Соединения и композиции в качестве ингибиторов протеинкиназ
DE102005060449A1 (de) * 2005-12-17 2007-06-21 Bayer Cropscience Ag Carboxamide
CN101437512A (zh) * 2006-01-27 2009-05-20 阿雷生物药品公司 葡萄糖激酶活化剂
WO2007092531A2 (en) 2006-02-06 2007-08-16 Irm Llc Compounds and compositions as protein kinase inhibitors
US8063225B2 (en) * 2006-08-14 2011-11-22 Chembridge Corporation Tricyclic compound derivatives useful in the treatment of neoplastic diseases, inflammatory disorders and immunomodulatory disorders
AR063946A1 (es) * 2006-09-11 2009-03-04 Cgi Pharmaceuticals Inc Determinadas pirimidinas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden.
US20110294842A9 (en) * 2006-10-12 2011-12-01 Xenon Pharmaceuticals Inc. Spiro (furo [3, 2-c] pyridine-3-3' -indol) -2' (1'h)-one derivatives and related compounds for the treatment of sodium-channel mediated diseases, such as pain
WO2008046216A1 (en) * 2006-10-18 2008-04-24 Methylgene, Inc. Kinase inhibitors and uses thereof
TWI409259B (zh) * 2006-11-08 2013-09-21 必治妥美雅史谷比公司 吡啶酮化合物
SG10201508035TA (en) * 2007-03-28 2015-10-29 Pharmacyclics Inc Inhibitors of bruton's tyrosine kinase
EP2170887A2 (en) * 2007-06-07 2010-04-07 Amgen Inc. Heterocyclic compounds as raf kinase modulators
GB0719644D0 (en) * 2007-10-05 2007-11-14 Cancer Rec Tech Ltd Therapeutic compounds and their use
TWI475996B (zh) * 2007-10-19 2015-03-11 Celgene Avilomics Res Inc 雜芳基化合物及其用途
WO2009122180A1 (en) * 2008-04-02 2009-10-08 Medical Research Council Pyrimidine derivatives capable of inhibiting one or more kinases
BRPI0914682B8 (pt) * 2008-06-27 2021-05-25 Avila Therapeutics Inc compostos de heteroarila e composições compreendendo os referidos compostos
TW201030001A (en) * 2008-11-14 2010-08-16 Amgen Inc Pyridine and pyrimidine derivatives as phosphodiesterase 10 inhibitors
UY32582A (es) * 2009-04-28 2010-11-30 Amgen Inc Inhibidores de fosfoinositida 3 cinasa y/u objetivo mamífero
WO2010144647A1 (en) 2009-06-12 2010-12-16 Bristol-Myers Squibb Company Nicotinamide compounds useful as kinase modulators
US9029359B2 (en) * 2009-09-04 2015-05-12 Biogen Idec Ma, Inc. Heteroaryl Btk inhibitors
PL2473049T3 (pl) * 2009-09-04 2019-07-31 Biogen Ma Inc. Inhibitory kinazy tyrozynowej brutona
MX2012002641A (es) * 2009-09-10 2012-03-14 Hoffmann La Roche Inhibidores de cinasa janus (jak).
KR101301533B1 (ko) * 2010-02-09 2013-09-04 한미사이언스 주식회사 암세포 성장 억제 효과를 갖는 신규 피리미딘 유도체
UY33304A (es) * 2010-04-02 2011-10-31 Amgen Inc Compuestos heterocíclicos y sus usos
EP2563773A1 (en) * 2010-04-29 2013-03-06 Deciphera Pharmaceuticals, LLC Pyridone amides and analogs exhibiting anti-cancer and anti-proliferative activites
WO2011143495A1 (en) * 2010-05-13 2011-11-17 Amgen Inc. Heteroaryloxyheterocyclyl compounds as pde10 inhibitors
MA34300B1 (fr) * 2010-05-13 2013-06-01 Amgen Inc Composés azotés hétérocycliques convenant comme inhibiteurs de la pde10
EP2593453B1 (en) * 2010-07-15 2014-09-17 Bristol-Myers Squibb Company Azaindazole compounds
KR20140007954A (ko) * 2011-06-10 2014-01-20 메르크 파텐트 게엠베하 Btk 억제 활성을 갖는 피리미딘 및 피리딘 화합물의 조성물 및 제조방법
CN103930407B (zh) * 2011-09-12 2019-02-26 默克专利有限公司 用作激酶活性调节剂的氨基嘧啶衍生物
TWI566701B (zh) 2012-02-01 2017-01-21 日本農藥股份有限公司 芳烷氧基嘧啶衍生物及包含該衍生物作為有效成分的農園藝用殺蟲劑及其使用方法
TW201414734A (zh) * 2012-07-10 2014-04-16 Takeda Pharmaceutical 氮雜吲哚衍生物

Also Published As

Publication number Publication date
BR112013030442A2 (pt) 2016-09-27
SG194219A1 (en) 2013-11-29
US20140162983A1 (en) 2014-06-12
CY1125494T1 (el) 2025-05-09
LT2718270T (lt) 2022-08-10
CA2833771C (en) 2021-08-03
IL229863A (en) 2017-06-29
EP4056562A1 (en) 2022-09-14
ZA201307632B (en) 2017-06-28
JP2016185953A (ja) 2016-10-27
CN103814016B (zh) 2017-03-08
SG10201604682VA (en) 2016-07-28
CN106831732B (zh) 2019-12-24
KR20150144817A (ko) 2015-12-28
SG10201801668WA (en) 2018-03-28
SI2718270T1 (sl) 2022-11-30
WO2012170976A2 (en) 2012-12-13
KR20140007954A (ko) 2014-01-20
MX354412B (es) 2018-03-05
RS63418B1 (sr) 2022-08-31
CN106831732A (zh) 2017-06-13
US20150259363A1 (en) 2015-09-17
EA201790228A1 (ru) 2017-08-31
EA027584B1 (ru) 2017-08-31
JP6298096B2 (ja) 2018-03-20
PL2718270T3 (pl) 2022-08-08
US10016448B2 (en) 2018-07-10
US9580449B2 (en) 2017-02-28
KR20180084153A (ko) 2018-07-24
BR112013030442B1 (pt) 2021-11-09
JP2018115165A (ja) 2018-07-26
DK2718270T3 (da) 2022-08-01
IL229863A0 (en) 2014-03-06
US20180243324A1 (en) 2018-08-30
KR20170021367A (ko) 2017-02-27
HK1197234A1 (en) 2015-01-09
HRP20220886T1 (hr) 2022-10-28
CN103814016A (zh) 2014-05-21
JP6849834B2 (ja) 2021-03-31
EA031153B1 (ru) 2018-11-30
MX373151B (es) 2020-04-21
ES2923760T3 (es) 2022-09-30
EP2718270B1 (en) 2022-04-27
KR101880966B1 (ko) 2018-07-23
JP6853204B2 (ja) 2021-03-31
WO2012170976A3 (en) 2013-04-11
HUE059230T2 (hu) 2022-10-28
PT2718270T (pt) 2022-07-29
US20170136048A1 (en) 2017-05-18
EP2718270A2 (en) 2014-04-16
CA2833771A1 (en) 2012-12-13
AU2017235978A1 (en) 2017-10-19
US10413562B2 (en) 2019-09-17
US9073947B2 (en) 2015-07-07
EA201301353A1 (ru) 2014-05-30
JP2014517016A (ja) 2014-07-17
AU2017235978B2 (en) 2019-04-04
KR20190011343A (ko) 2019-02-01
AU2012267491B2 (en) 2017-07-06
AU2012267491A1 (en) 2013-10-31
JP2020073593A (ja) 2020-05-14

Similar Documents

Publication Publication Date Title
MX2013012983A (es) Composiciones y metodos para la produccion de compuestos de pirimidina con actividad inhibidora de tirosina cinasa de bruton.
WO2014093230A3 (en) Compositions and methods for the production of pyrimidine and pyridine compounds with btk inhibitory activity
PH12018502125A1 (en) Bipyrazole derivatives as jak inhibitors
PH12016500531A1 (en) Compound inhibiting activities of btk and/or jak3 kinases
TN2015000368A1 (en) Quinazoline inhibitors of activating mutant forms of epidermal growth factor receptor
WO2014145028A3 (en) N-acyl-n&#39;-(pyridin-2-yl) ureas and analogs exhibiting anti-cancer and anti-proliferative activities
WO2014145029A3 (en) N-acyl-n&#39;-(pyridin-2-yl) ureas and analogs exhibiting anti-cancer and anti-proliferative activities
SA515360007B1 (ar) مركبات عطرية غير متجانسة كمثبطات بروتونز تيروسين كيناز ( btk)
BR112015000399A2 (pt) derivados de pirazolil pirimidina
BR112013032720A2 (pt) &#34;derivados de azetidinil fenil, piridil ou pirazinil carboxamida como inibidores de jak, composição e uso dos referidos derivados&#34;
MY171831A (en) Novel fused pyrimidine compound or salt thereof
NZ702571A (en) 4-(substituted-amino)-7h-pyrrolo[2,3-d]pyrimidines as lrrk2 inhibitors
AU2012258977A8 (en) Inhibitors of LRRK2 kinase activity
IN2014KN02410A (es)
BR112015009942A2 (pt) derivados de tiofeno fundidos tricíclicos como inibidores de jak
PH12014502496B1 (en) Bicyclically substituted uracils and the use thereof
MX2014002836A (es) Derivados de aminopirimidina para usarse como moduladores de la actividad de cinasa.
PH12015501586A1 (en) 2,3-dihydroimidazol[1,2-c]pyrimidin-5(1h)-one based lipoprotein-associated phospholipase a2 (lp-pla2) inhibitors
TN2015000120A1 (en) Oxazolidin-2-one-pyrimidine derivatives
MX341577B (es) Derivados biciclicos de pirimidin-urea o carbamato sustituidos con morfolino como inhibidores del blanco de rapamicina de mamifero.
UA110978C2 (uk) Азетидинілфенілові, піридилові або піразинілкарбоксамідні похідні як інгібітори jak
UA106617C2 (uk) N-(ГЕТЕРО)АРИЛПІРОЛІДИНОВІ ПОХІДНІ ПІРАЗОЛ-4-ІЛПІРОЛО[2,3-d]ПІРИМІДИНІВ І ПІРОЛ-3-ІЛПІРОЛО[2,3-d]ПІРИМІДИНІВ ЯК ІНГІБІТОРИ ЯНУС-КІНАЗИ

Legal Events

Date Code Title Description
FG Grant or registration