MX2022008103A - Formulaciones de inhibidores de la cinasa amorfa y metodos de estas. - Google Patents

Formulaciones de inhibidores de la cinasa amorfa y metodos de estas.

Info

Publication number
MX2022008103A
MX2022008103A MX2022008103A MX2022008103A MX2022008103A MX 2022008103 A MX2022008103 A MX 2022008103A MX 2022008103 A MX2022008103 A MX 2022008103A MX 2022008103 A MX2022008103 A MX 2022008103A MX 2022008103 A MX2022008103 A MX 2022008103A
Authority
MX
Mexico
Prior art keywords
amorphous
methods
kinase inhibitor
inhibitor formulations
formulations
Prior art date
Application number
MX2022008103A
Other languages
English (en)
Inventor
Michael D Kaufman
Corey Bloom
Scott Bone
Fred Jordan
Original Assignee
Deciphera Pharmaceuticals Llc
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 Deciphera Pharmaceuticals Llc filed Critical Deciphera Pharmaceuticals Llc
Priority claimed from PCT/US2020/067557 external-priority patent/WO2021138483A1/en
Publication of MX2022008103A publication Critical patent/MX2022008103A/es

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1652Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1617Organic compounds, e.g. phospholipids, fats
    • A61K9/1623Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1635Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682Processes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2009Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2027Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2072Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Abstract

En el presente documento se proporciona un compuesto amorfo representado por la Fórmula (I): (ver Fórmula) Fórmula (I) que es útil en el tratamiento de los trastornos relacionados con la actividad de las cinasas c-KIT y PDGFRa y las formas oncogénicas de estas.
MX2022008103A 2019-12-30 2020-12-30 Formulaciones de inhibidores de la cinasa amorfa y metodos de estas. MX2022008103A (es)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201962955073P 2019-12-30 2019-12-30
US201962955062P 2019-12-30 2019-12-30
US202062968724P 2020-01-31 2020-01-31
US202062968695P 2020-01-31 2020-01-31
PCT/US2020/067557 WO2021138483A1 (en) 2019-12-30 2020-12-30 Amorphous kinase inhibitor formulations and methods of use thereof

Publications (1)

Publication Number Publication Date
MX2022008103A true MX2022008103A (es) 2022-09-19

Family

ID=76547083

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2022008103A MX2022008103A (es) 2019-12-30 2020-12-30 Formulaciones de inhibidores de la cinasa amorfa y metodos de estas.

Country Status (16)

Country Link
US (5) US11185535B2 (es)
EP (2) EP4084778B1 (es)
JP (1) JP2023509629A (es)
KR (1) KR20220123057A (es)
CN (1) CN115135308A (es)
AU (2) AU2020419197B2 (es)
BR (1) BR112022013109A2 (es)
CA (1) CA3163053A1 (es)
DK (1) DK4084778T3 (es)
FI (1) FI4084778T3 (es)
IL (1) IL293866A (es)
LT (1) LT4084778T (es)
MX (1) MX2022008103A (es)
PL (1) PL4084778T3 (es)
RS (1) RS65058B1 (es)
SI (1) SI4084778T1 (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20220045189A (ko) 2019-08-12 2022-04-12 데시페라 파마슈티칼스, 엘엘씨. 위장관 기질 종양을 치료하는 방법
WO2021030405A1 (en) 2019-08-12 2021-02-18 Deciphera Pharmaceuticals, Llc Ripretinib for treating gastrointestinal stromal tumors
KR20220123057A (ko) 2019-12-30 2022-09-05 데시페라 파마슈티칼스, 엘엘씨. 비정질 키나아제 억제제 제형 및 이의 사용 방법
CA3163051A1 (en) 2019-12-30 2021-07-08 Michael D. Kaufman Compositions of 1-(4-bromo-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl)-3-phenylurea
EP4247795A1 (en) 2020-11-18 2023-09-27 Deciphera Pharmaceuticals, LLC Gcn2 and perk kinase inhibitors and methods of use thereof
US11779572B1 (en) 2022-09-02 2023-10-10 Deciphera Pharmaceuticals, Llc Methods of treating gastrointestinal stromal tumors

Family Cites Families (295)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1115350B (de) 1959-04-17 1961-10-19 Siemens Ag Selbstschalter, insbesondere Leitungsschutz-schalter, mit einem aus einem Kniegelenk bestehenden Antriebsmechanismus fuer das Schaltorgan
GB971307A (en) 1961-03-02 1964-09-30 Wellcome Found 5-anilinopyrimidines
GB1127875A (en) 1967-03-23 1968-09-18 Parke Davis & Co 4-(5-nitro-2-furyl) thiazolyl hydantoins and hydrouracils
US3949002A (en) 1970-11-13 1976-04-06 Imperial Chemical Industries Limited Process for producing sulfone containing thiophenols
US3818024A (en) 1972-02-16 1974-06-18 Velsicol Chemical Corp Benzothiazol substituted thiadiazolidines
CH565887A5 (es) 1972-08-22 1975-08-29 Ciba Geigy Ag
US3939122A (en) 1973-04-11 1976-02-17 Bayer Aktiengesellschaft Process for the preparation of compounds which contain hydantoin rings
FR2337554A1 (fr) 1976-01-08 1977-08-05 Buzas Andre Nouveaux derives de la pyrazolidinedione
JPS5915247B2 (ja) 1976-09-14 1984-04-09 古河電気工業株式会社 電力制御による走行体の定位置停止方式
US4093624A (en) 1977-01-31 1978-06-06 Icn Pharmaceuticals, Inc. 1,2,4-Thiadiazolidine-3,5-dione
FR2396549A2 (fr) 1977-07-06 1979-02-02 Buzas Andre Nouveaux derives de la pyrazolidinedione
US4256758A (en) 1979-06-11 1981-03-17 Merck & Co., Inc. 4-Substituted-3-hydroxy-3-pyrroline-2,5-dione inhibitors of glycolic acid oxidase
US4296237A (en) 1979-09-11 1981-10-20 Merck & Co., Inc. 4-(Pyridyl, piperazinyl and thiazolyl substituted thiazolyl)-3-hydroxy-3-pyrroline-2,5-diones
US4298743A (en) 1979-09-11 1981-11-03 Merck & Co., Inc. 4-(Substituted phenyl thiazolyl)-3-hydroxy-3-pyrroline-2,5-diones
US4432992A (en) 1979-11-05 1984-02-21 Merck & Co., Inc. 4-[5(and 4)-Substituted-2-thienyl]-3-hydroxy-3-pyrroline-2,5-dione inhibitors of glycolic acid oxidase
US4366189A (en) 1979-12-21 1982-12-28 Ciba-Geigy Corporation 4-Heterocyclyl-4'-vinylstilbenes
JPS59177557A (ja) 1983-03-28 1984-10-08 Fuji Photo Film Co Ltd ハロゲン化銀カラ−写真感光材料
DE3406329A1 (de) 1984-02-22 1985-08-22 Merck Patent Gmbh, 6100 Darmstadt Pyridone
US4816454A (en) 1984-09-21 1989-03-28 Cassella Aktiengesellschaft 4,5-dihydro-3(2H)-pyridazinones and their pharmacological use
US5514691A (en) 1993-05-20 1996-05-07 Immunopharmaceutics, Inc. N-(4-halo-isoxazolyl)-sulfonamides and derivatives thereof that modulate the activity of endothelin
US5103014A (en) 1987-09-30 1992-04-07 American Home Products Corporation Certain 3,3'-[[[(2-phenyl-4-thiazolyl)methoxy]phenyl]methylene]dithiobis-propanoic acid derivatives
AU606808B2 (en) 1988-06-29 1991-02-14 Otsuka Pharmaceutical Factory, Inc. Arylcarboxamide substituted by alkylphosphonates, process for preparing the same and a pharmaceutical composition containing the same
FR2662162B1 (fr) 1990-05-18 1995-01-20 Adir Nouveaux derives de l'amino piperidine, de l'amino pyrrolidine et de l'amino perhydroazepine, leurs procedes de preparation et les compositions pharmaceutiques qui les contiennent.
GB9012936D0 (en) 1990-06-11 1990-08-01 Fujisawa Pharmaceutical Co Thiophene derivatives,processes for preparation thereof and pharmaceutical composition comprising the same
US5254715A (en) 1990-11-07 1993-10-19 Warner-Lambert Company Aminosulfonyl carbamates
CA2078790C (en) 1991-01-21 1998-10-06 Susumu Kamata 3-benzylidene-1-carbamoyl-2-pyrrolidone analogues
US5162360A (en) 1991-06-24 1992-11-10 Warner-Lambert Company 2-heteroatom containing urea and thiourea ACAT inhibitors
GB9816837D0 (en) 1998-08-04 1998-09-30 Zeneca Ltd Amide derivatives
GB9125515D0 (en) 1991-11-29 1992-01-29 Merck Sharp & Dohme Therapeutic agents
US5658924A (en) 1992-12-01 1997-08-19 The Green Cross Corporation 1,8-naphthyridin-2-one derivative and use thereof
DE4302702A1 (de) 1993-02-01 1994-08-04 Bayer Ag Arylaminosulfonylharnstoffe
WO1994021617A1 (en) 1993-03-19 1994-09-29 Dowelanco A process for preparing halogenated isothiazoles
WO1994022872A1 (en) 1993-03-30 1994-10-13 Yoshitomi Pharmaceutical Industries, Ltd. Cell adhesion inhibitor and thienotriazolodiazepine compound
WO1994024095A1 (en) 1993-04-16 1994-10-27 Abbott Laboratories Immunosuppressive agents
CA2123728A1 (en) 1993-05-21 1994-11-22 Noriyoshi Sueda Urea derivatives and their use as acat inhibitors
WO1995006044A1 (en) 1993-08-20 1995-03-02 Smithkline Beecham Plc Amide and urea derivatives as 5ht1d receptor antagonists
DE4337847A1 (de) 1993-11-05 1995-05-11 Bayer Ag Substituierte Phenylaminosulfonylharnstoffe
WO1995015954A1 (en) 1993-12-07 1995-06-15 Smithkline Beecham Plc Heterocyclic biphenylylamides useful as 5ht1d antagonists
DE4343831A1 (de) 1993-12-22 1995-06-29 Magyar Tudomanyos Akademia Substituierte Sulfonylharnstoffe
FR2715155B1 (fr) 1994-01-19 1996-07-26 Mayoly Spindler Inhibiteurs de la monoamine oxydase B et leurs procédés de préparation.
DE4414840A1 (de) 1994-04-28 1995-11-02 Bayer Ag Substituierte Phenylaminosulfonylharnstoffe
ATE360617T1 (de) 1994-06-15 2007-05-15 Otsuka Pharma Co Ltd Benzoheterocyclische verbindungen verwendbar als vasopressin- oder oxytocin-modulatoren
ATE235471T1 (de) 1994-11-24 2003-04-15 Basilea Pharmaceutica Ag Neue benzylpyrimidine
US5494925A (en) 1994-12-02 1996-02-27 Sterling Winthrop Inc. 2-heterocyclyloxymethyl and 2-heterocyclylthiomethyl-1,2,5-thiadiazolidin-3-one 1,1-dioxides and compositions and method of use thereof
ES2153907T3 (es) 1994-12-22 2001-03-16 Smithkline Beecham Plc Compuestos espiro tetraciclicos, procedimiento para su preparacion y su uso como antagonistas del receptor 5ht1d.
CN1151147C (zh) 1995-02-02 2004-05-26 史密丝克莱恩比彻姆有限公司 作为5-ht受体拮抗剂的吲哚衍生物
KR100423818B1 (ko) 1995-04-24 2004-07-05 가부시키가이샤 한도오따이 에네루기 켄큐쇼 액정화합물및이를함유하는액정조성물
US6123964A (en) * 1995-10-27 2000-09-26 Merck & Co., Inc. Wet granulation formulation of a growth hormone secretagogue
JPH09221476A (ja) 1995-12-15 1997-08-26 Otsuka Pharmaceut Co Ltd 医薬組成物
GB9605945D0 (en) 1996-03-21 1996-05-22 Smithkline Beecham Plc Novel compounds
GB9607219D0 (en) 1996-04-04 1996-06-12 Smithkline Beecham Plc Novel compounds
CN1515248A (zh) 1996-04-23 2004-07-28 ��̩��˹ҩ��ɷ����޹�˾ 用作肌苷-5'-一磷酸脱氢酶抑制剂的脲衍生物
US6147088A (en) 1996-05-20 2000-11-14 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
WO1997045400A1 (en) 1996-05-24 1997-12-04 Neurosearch A/S Phenyl derivatives containing an acidic group, their preparation and their use as chloride channel blockers
GB9623833D0 (en) 1996-11-16 1997-01-08 Zeneca Ltd Chemical compound
US6020357A (en) 1996-12-23 2000-02-01 Dupont Pharmaceuticals Company Nitrogen containing heteroaromatics as factor Xa inhibitors
ATE230742T1 (de) 1997-03-27 2003-01-15 Great Lakes Chemical Europ 2-(2'-hydroxphenyl)-benzotriazole und ihre verwendung als lichtschutzmittel für organische polymere
US6187799B1 (en) 1997-05-23 2001-02-13 Onyx Pharmaceuticals Inhibition of raf kinase activity using aryl ureas
PT1019040E (pt) 1997-05-23 2005-01-31 Bayer Pharmaceuticals Corp Inibicao da actividade de p38-quinase por meio de arilureias
US6235786B1 (en) 1997-08-06 2001-05-22 Abbott Laboratories Reverse hydroxamate inhibitors of matrix metalloproteinases
US6294573B1 (en) 1997-08-06 2001-09-25 Abbott Laboratories Reverse hydroxamate inhibitors of matrix metalloproteinases
NZ502702A (en) 1997-09-23 2002-10-25 Astrazeneca Ab Amide derivatives for the treatment of diseases mediated by TNF, IL-1, IL-6 or IL-8
IT1295933B1 (it) 1997-10-30 1999-05-28 Great Lakes Chemical Italia 2-(2'-idrossifenil)benzotriazoli e procedimento per la loro preparazione
EP1028953A1 (en) 1997-11-03 2000-08-23 Boehringer Ingelheim Pharmaceuticals Inc. Aromatic heterocyclic compounds as anti-inflammatory agents
IL136738A0 (en) 1997-12-22 2001-06-14 Bayer Ag Inhibition of p38 kinase activity using substituted heterocyclic ureas
DE69836563T2 (de) 1997-12-22 2007-05-16 Bayer Pharmaceuticals Corp., West Haven INHIBIERUNG DER p38 KINASE-AKTIVITÄT DURCH DIE VERWENDUNG VON ARYL- UND HETEROARYL-SUBSTITUIERTEN HARNSTOFFEN
US20070244120A1 (en) 2000-08-18 2007-10-18 Jacques Dumas Inhibition of raf kinase using substituted heterocyclic ureas
US7329670B1 (en) 1997-12-22 2008-02-12 Bayer Pharmaceuticals Corporation Inhibition of RAF kinase using aryl and heteroaryl substituted heterocyclic ureas
US7517880B2 (en) 1997-12-22 2009-04-14 Bayer Pharmaceuticals Corporation Inhibition of p38 kinase using symmetrical and unsymmetrical diphenyl ureas
TR200002617T2 (tr) 1997-12-22 2000-11-21 Bayer Corporation Aril ve heteroaril sübstitüentli heterosiklik üreler kullanılarak RAF kinazın inhibe edilmesi
US20080300281A1 (en) 1997-12-22 2008-12-04 Jacques Dumas Inhibition of p38 Kinase Activity Using Aryl and Heteroaryl Substituted Heterocyclic Ureas
BR9814374B1 (pt) 1997-12-22 2013-09-17 "urÉias heterocÍclicas substituÍdas e composiÇÕes compreendendo as mesmas"
NZ333399A (en) 1997-12-24 2000-05-26 Sankyo Co Cyclooxygenase-2 inhibitors (COX-2) for the prevention and treatment of tumors, cachexia and tumor-metastasis
SI0928790T1 (en) 1998-01-02 2003-06-30 F. Hoffmann-La Roche Ag Thiazole derivatives
JPH11209350A (ja) 1998-01-26 1999-08-03 Eisai Co Ltd 含窒素複素環誘導体およびその医薬
EP0956855B1 (en) 1998-04-24 2003-03-12 K.U. Leuven Research & Development Immunosuppressive effects of 8 substituted xanthine derivatives
PT1077931E (pt) 1998-05-15 2005-03-31 Astrazeneca Ab Derivados de bezamida para o tratamento de doencas mediadas por citocinas
US6197599B1 (en) 1998-07-30 2001-03-06 Guorong Chin Method to detect proteins
AU753360B2 (en) 1998-07-31 2002-10-17 Nippon Soda Co., Ltd. Phenylazole compounds, process for producing the same and drugs for hyperlipemia
US6455520B1 (en) 1998-09-25 2002-09-24 Astra Zeneca Ab Benzamide derivatives and their use as cytokine inhibitors
DE69922526T2 (de) 1998-10-08 2005-06-02 Smithkline Beecham Plc, Brentford 3-(3-chloro-4-hydroxyphenylamino)-4-(2-nitrophenyl)-1h-pyrrol-2,5-dion als glykogen synthase kinase-3 inhibitor (gsk-3)
GB9823873D0 (en) 1998-10-30 1998-12-30 Pharmacia & Upjohn Spa 2-ureido-thiazole derivatives,process for their preparation,and their use as antitumour agents
WO2000042012A1 (en) 1999-01-13 2000-07-20 Bayer Corporation φ-CARBOXYARYL SUBSTITUTED DIPHENYL UREAS AS RAF KINASE INHIBITORS
CA2359244C (en) 1999-01-13 2013-10-08 Bayer Corporation .omega.-carboxy aryl substituted diphenyl ureas as p38 kinase inhibitors
US7928239B2 (en) 1999-01-13 2011-04-19 Bayer Healthcare Llc Inhibition of RAF kinase using quinolyl, isoquinolyl or pyridyl ureas
US8124630B2 (en) 1999-01-13 2012-02-28 Bayer Healthcare Llc ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
UA73492C2 (en) 1999-01-19 2005-08-15 Aromatic heterocyclic compounds as antiinflammatory agents
HUP0202248A3 (en) 1999-03-12 2006-06-28 Boehringer Ingelheim Pharma Compounds useful as anti-inflammatory agents
JP2000275886A (ja) 1999-03-23 2000-10-06 Konica Corp 電子写真感光体、それを用いたプロセスカートリッジ及び画像形成装置
US6548529B1 (en) 1999-04-05 2003-04-15 Bristol-Myers Squibb Company Heterocyclic containing biphenyl aP2 inhibitors and method
US6410254B1 (en) 1999-05-18 2002-06-25 Cytokinetics Compositions and assays utilizing ADP or phosphate for detecting protein modulators
AU5283600A (en) 1999-05-24 2000-12-12 Cor Therapeutics, Inc. Inhibitors of factor xa
JP3972163B2 (ja) 1999-06-18 2007-09-05 株式会社大塚製薬工場 ホスホン酸ジエステル誘導体
NZ517694A (en) 1999-08-13 2005-03-24 Vertex Pharma Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
AR035016A1 (es) 1999-08-25 2004-04-14 Takeda Chemical Industries Ltd Composicion de azol promotor de produccion/secrecion de neurotrofina, compuesto prodroga del mismo, composicion farmaceutica que lo comprende y uso del mismo para preparar esta ultima.
US7071199B1 (en) 1999-09-17 2006-07-04 Abbott Gmbh & Cco. Kg Kinase inhibitors as therapeutic agents
US6525046B1 (en) 2000-01-18 2003-02-25 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatic heterocyclic compounds as antiinflammatory agents
US6906063B2 (en) 2000-02-04 2005-06-14 Portola Pharmaceuticals, Inc. Platelet ADP receptor inhibitors
GB0008264D0 (en) 2000-04-04 2000-05-24 Smithkline Beecham Plc Novel method and compounds
US6500628B1 (en) 2000-05-25 2002-12-31 Millennium Pharmaceuticals, Inc. Nucleic acid molecules encoding human kinase and phosphatase homologues and uses therefor
WO2001096298A2 (en) 2000-06-14 2001-12-20 Warner-Lambert Company 1,2,4-trisubstituted benzenes as inhibitors of 15-lipoxygenase
EP1296977A1 (en) 2000-06-23 2003-04-02 Bristol-Myers Squibb Pharma Company Heteroaryl-phenyl substituted factor xa inhibitors
AU2001277723A1 (en) 2000-08-11 2002-02-25 Nippon Chemiphar Co., Ltd. Ppardelta activators
US6645990B2 (en) 2000-08-15 2003-11-11 Amgen Inc. Thiazolyl urea compounds and methods of uses
US20020173507A1 (en) 2000-08-15 2002-11-21 Vincent Santora Urea compounds and methods of uses
WO2002026712A2 (en) 2000-09-29 2002-04-04 Millennium Pharmaceuticals, Inc. Quaternary amines and related inhibitors of factor xa
IL155196A0 (en) 2000-10-05 2003-11-23 Fujisawa Pharmaceutical Co Benzamide derivatives and pharmaceutical compositions containing the same
WO2002060869A2 (en) 2000-10-19 2002-08-08 Smithkline Beecham Corporation Use of p38 inhibitors for the treatment of inflammation-enhanced cough
RU2301066C2 (ru) 2000-10-27 2007-06-20 Новартис Аг Лечение желудочно-кишечных стромальных опухолей
US7235576B1 (en) 2001-01-12 2007-06-26 Bayer Pharmaceuticals Corporation Omega-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
JP2002226464A (ja) 2001-01-30 2002-08-14 Sumitomo Pharmaceut Co Ltd トリアリール類縁体およびその利用
JP2004518739A (ja) 2001-02-15 2004-06-24 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド 抗炎症剤として有用なヘテロアリール置換尿素化合物の合成方法
US20030165873A1 (en) 2001-03-02 2003-09-04 Come Jon H. Three hybrid assay system
DE60219793T2 (de) 2001-07-11 2008-01-24 Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield Verfahren zur Behandlung von Cytokin-Vermittelten Erkrankungen
EP1281399A3 (en) 2001-08-01 2004-02-11 Warner-Lambert Company Dual inhibitors of wax ester and cholesteryl ester synthesis for inhibiting sebum production
EP1427412A1 (en) 2001-09-13 2004-06-16 Boehringer Ingelheim Pharmaceuticals Inc. Methods of treating cytokine mediated diseases
MXPA04005137A (es) 2001-12-03 2005-06-03 Bayer Pharmaceuticals Corp Compuestos de aril urea en combinacion con otros agentes citostaticos para el tratamiento de canceres humanos.
AU2002360763A1 (en) 2001-12-19 2003-07-09 Atherogenics, Inc. Chalcone derivatives and their use to treat diseases
US20050090474A1 (en) 2002-01-16 2005-04-28 Zvi Naor Methods and compositions for enhancing and inhibiting fertilization
WO2003063822A2 (en) 2002-02-01 2003-08-07 Pfizer Products Inc. Method for making homogeneous spray-dried solid amorphous drug dispersions utilizing modified spray-drying apparatus
MXPA04007435A (es) 2002-02-01 2004-10-11 Pfizer Prod Inc Metodo para preparar dispersiones solidas amorfas de farmacos secadas por pulverizacion utilizando inyectores a presion.
AU2003209119A1 (en) 2002-02-11 2003-09-04 Bayer Pharmaceuticals Corporation Pyridine, quinoline, and isoquinoline n-oxides as kinase inhibitors
WO2003068223A1 (en) 2002-02-11 2003-08-21 Bayer Corporation Aryl ureas with raf kinase and angiogenesis inhibiting activity
MXPA04007832A (es) 2002-02-11 2005-09-08 Bayer Pharmaceuticals Corp Aril-ureas con actividad inhibitoria de angiogenesis.
CA2473634C (en) 2002-02-25 2011-11-29 Boehringer Ingelheim Pharmaceuticals, Inc. 1,4-disubstituted benzofused cycloalkyl urea compounds useful in treating cytokine mediated diseases
AU2003210305B2 (en) 2002-02-28 2006-07-06 F. Hoffmann-La Roche Ag Thiazole derivatives as NPY receptor antagonists
US6995144B2 (en) 2002-03-14 2006-02-07 Eisai Co., Ltd. Nitrogen containing heterocyclic compounds and medicines containing the same
US20030225089A1 (en) 2002-04-10 2003-12-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Pharmaceutical compositions based on anticholinergics and p38 kinase inhibitors
JP2005538975A (ja) 2002-07-03 2005-12-22 アステックス テクノロジー リミテッド p38MAPキナーゼ阻害薬としての3−(ヘテロ)アリールメトキシピリジン類およびそれらの類縁体
US20040138216A1 (en) 2002-12-23 2004-07-15 Boehringer Ingelheim Pharma Gmbh & Co. Kg Process for the preparation of an essentially pure polymorph of an n-pyrazolyl-n'-naphthyl-urea
US7279576B2 (en) 2002-12-31 2007-10-09 Deciphera Pharmaceuticals, Llc Anti-cancer medicaments
US20040171075A1 (en) 2002-12-31 2004-09-02 Flynn Daniel L Modulation of protein functionalities
US7202257B2 (en) 2003-12-24 2007-04-10 Deciphera Pharmaceuticals, Llc Anti-inflammatory medicaments
US20080045706A1 (en) 2002-12-31 2008-02-21 Flynn Daniel L Anti-inflammatory medicaments
WO2005024755A2 (en) 2002-12-31 2005-03-17 Deciphera Pharmaceuticals, Llc. Medicaments for the treatment of neurodegenerative disorders or diabetes
US7144911B2 (en) 2002-12-31 2006-12-05 Deciphera Pharmaceuticals Llc Anti-inflammatory medicaments
JP4927533B2 (ja) 2003-02-28 2012-05-09 ニッポネックス インコーポレイテッド 癌その他の疾患の治療に有用な置換ピリジン誘導体
UY28213A1 (es) 2003-02-28 2004-09-30 Bayer Pharmaceuticals Corp Nuevos derivados de cianopiridina útiles en el tratamiento de cáncer y otros trastornos.
MXPA05009103A (es) 2003-02-28 2006-04-18 Bayer Pharmaceuticals Corp Derivados de 2-oxo-1,3,5-perhidrotriazapina utiles en el tratamiento de trastornos hiper-proliferativos, por angiogenesis, e inflamatorios.
US20050014753A1 (en) 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors
WO2004113352A1 (en) 2003-06-19 2004-12-29 Amedis Pharmaceuticals Ltd. Silylated heterocyclylurea derivatives as cytokine-inhibitors
WO2005002673A1 (en) 2003-07-03 2005-01-13 Astex Therapeutics Limited Raf kinase inhibitors
US8754238B2 (en) 2003-07-22 2014-06-17 Arena Pharmaceuticals, Inc. Diaryl and arylheteroaryl urea derivatives as modulators of the 5-HT2A serotonin receptor useful for the prophylaxis and treatment of disorders related thereto
CL2004001884A1 (es) 2003-08-04 2005-06-03 Pfizer Prod Inc Procedimiento de secado por pulverizacion para la formacion de dispersiones solidas amorfas de un farmaco y polimeros.
EP1673343A4 (en) 2003-10-08 2008-09-10 Irm Llc COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
US20050197371A1 (en) 2003-11-13 2005-09-08 Ambit Biosciences Corporation Urea derivatives as PDGFR modulators
US20070191336A1 (en) 2003-12-24 2007-08-16 Flynn Daniel L Anti-inflammatory medicaments
US20080220497A1 (en) 2003-12-24 2008-09-11 Flynn Daniel L Modulation of protein functionalities
ATE548353T1 (de) 2004-03-23 2012-03-15 Arena Pharm Inc Verfahren zur herstellung von substituierte n- aryl-n'-ä3-(1h-pyrazol-5-yl)phenylü-harnstoffe and intermediate davon.
MXPA06012394A (es) 2004-04-30 2007-01-31 Bayer Pharmaceuticals Corp Derivados de pirazolilurea sustituidos utiles en el tratamiento de cancer.
EP1773826A4 (en) 2004-07-02 2009-06-03 Exelixis Inc MODULATORS OF C-MET AND THEIR METHOD OF USE
EP1786422A2 (en) 2004-08-16 2007-05-23 Prosidion Limited Aryl urea derivatives for treating obesity
US7888364B2 (en) 2004-09-02 2011-02-15 Curis, Inc. Pyridyl inhibitors of hedgehog signalling
US20070054916A1 (en) 2004-10-01 2007-03-08 Amgen Inc. Aryl nitrogen-containing bicyclic compounds and methods of use
US8003657B2 (en) 2004-10-13 2011-08-23 Merck Patent Gmbh Heterocyclic substituted bisarylurea derivatives
WO2006046552A1 (ja) 2004-10-27 2006-05-04 Toyama Chemical Co., Ltd. 新規な含窒素複素環化合物およびその塩
GT200500321A (es) 2004-11-09 2006-09-04 Compuestos y composiciones como inhibidores de proteina kinase.
JP2008523072A (ja) 2004-12-07 2008-07-03 ルーカス ファーマシューティカルズ, インコーポレイテッド タンパク質キナーゼの阻害剤
WO2006081034A2 (en) 2004-12-23 2006-08-03 Deciphera Pharmaceuticals, Llc Anti-inflammatory medicaments
EP1835934A4 (en) 2004-12-23 2010-07-28 Deciphera Pharmaceuticals Llc ENZYME MODULATORS AND TREATMENTS
GB0500435D0 (en) 2005-01-10 2005-02-16 Novartis Ag Organic compounds
US7622583B2 (en) 2005-01-14 2009-11-24 Chemocentryx, Inc. Heteroaryl sulfonamides and CCR2
AU2006206687A1 (en) 2005-01-19 2006-07-27 Arena Pharmaceuticals, Inc. Diaryl and arylheteroaryl urea derivatives as modulators of the 5-HT2A serotonin receptor useful for the prophylaxis or treatment of progressive multifocal leukoencephalopathy
AR052886A1 (es) 2005-01-26 2007-04-11 Arena Pharm Inc Procedimientos para preparar fenilpirazol ureas sustituidas y para la obtencion de sus intermediarios de sintesis
US9265731B2 (en) 2005-01-28 2016-02-23 Bend Research, Inc. Drying of drug-containing particles
BRPI0608252A2 (pt) 2005-03-10 2010-04-06 Cgi Pharmaceuticals Inc entidades quìmicas, composições farmacêuticas compreendendo as mesmas, métodos utilizando as referidas entidades quìmicas e uso das referidas entidades quìmicas
DE102005015253A1 (de) 2005-04-04 2006-10-05 Merck Patent Gmbh Pyrazolderivate
AU2006301458A1 (en) 2005-10-13 2007-04-19 Devgen N.V. Kinase inhibitors
CA2631746A1 (en) 2005-12-01 2007-06-07 Bayer Healthcare Llc Urea compounds useful in the treatment of cancer
TW200804349A (en) 2005-12-23 2008-01-16 Kalypsys Inc Novel substituted pyrimidinyloxy ureas as inhibitors of protein kinases
JP2009522363A (ja) 2006-01-04 2009-06-11 ローカス ファーマシューティカルズ、インク. プロテインキナーゼの阻害剤
US20090124633A1 (en) 2006-04-12 2009-05-14 Alfred Jonczyk N-oxides of heterocyclic substituted bisarylureas for treating kinase-mediated diseases
CA2649994A1 (en) 2006-04-26 2007-11-08 Cancer Research Technology Limited Imidazo[4,5-b]pyridin-2-one and oxazolo[4,5-b]pyridin-2-one compounds and analogs thereof as cancer therapeutic compounds
US20090312321A1 (en) 2006-05-15 2009-12-17 Irm Llc Compositions and methods for fgf receptor kinases inhibitors
WO2007137107A2 (en) 2006-05-19 2007-11-29 Abbott Laboratories Inhibitors of diacylglycerol o-acyltransferase type 1 enzyme
WO2008033858A2 (en) 2006-09-11 2008-03-20 Cgi Pharmaceuticals, Inc. Kinase inhibitors, and methods of using and identifying kinase inhibitors
US8188113B2 (en) 2006-09-14 2012-05-29 Deciphera Pharmaceuticals, Inc. Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
CN101553232A (zh) 2006-09-14 2009-10-07 迪赛孚尔制药有限公司 用于治疗增殖性疾病的激酶抑制剂
US7897762B2 (en) 2006-09-14 2011-03-01 Deciphera Pharmaceuticals, Llc Kinase inhibitors useful for the treatment of proliferative diseases
US7790756B2 (en) 2006-10-11 2010-09-07 Deciphera Pharmaceuticals, Llc Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases
US20120225057A1 (en) 2006-10-11 2012-09-06 Deciphera Pharmaceuticals, Llc Methods and compositions for the treatment of myeloproliferative diseases and other proliferative diseases
AU2007309279B2 (en) 2006-10-20 2011-03-24 Irm Llc Compositions and methods for modulating c-kit and PDGFR receptors
US20080248487A1 (en) 2007-04-09 2008-10-09 Flynn Daniel L Modulation of protein functionalities
US20080248548A1 (en) 2007-04-09 2008-10-09 Flynn Daniel L Modulation of protein functionalities
PL2139484T3 (pl) 2007-04-10 2013-12-31 Exelixis Inc Sposoby leczenia raka z zastosowaniem pirydopirymidynonów jako inhibitorów PI3K alfa
US20110189167A1 (en) 2007-04-20 2011-08-04 Flynn Daniel L Methods and Compositions for the Treatment of Myeloproliferative Diseases and other Proliferative Diseases
CA2678639A1 (en) 2007-04-20 2008-10-30 Deciphera Pharmaceuticals, Llc Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases
BRPI0816320A2 (pt) 2007-09-04 2015-03-24 Biolipox Ab Composto, formulação farmacêutica, uso de um composto, método de tratamento de uma doença, produto de combinação, e, processos para a preparação deu um composto, de uma formulação farmacêutica, e de um produto de combinação
US8389567B2 (en) 2007-12-12 2013-03-05 Calcimedica, Inc. Compounds that modulate intracellular calcium
CN102083828B (zh) 2008-02-22 2013-11-13 Irm责任有限公司 作为c-kit和pdgfr激酶抑制剂的杂环化合物和组合物
JP2011513339A (ja) 2008-03-05 2011-04-28 9222−9129 ケベック インコーポレイテッド タンパク質チロシンキナーゼ活性の阻害剤
US20090281089A1 (en) 2008-04-11 2009-11-12 Genentech, Inc. Pyridyl inhibitors of hedgehog signalling
EP2274280A2 (en) 2008-04-16 2011-01-19 Biolipox AB Bis-aryl compounds for use as medicaments
US20110112193A1 (en) 2008-05-14 2011-05-12 Peter Nilsson Bis-aryl compounds for use as medicaments
WO2010011837A1 (en) 2008-07-24 2010-01-28 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as kinase modulators
EA201170627A1 (ru) 2008-10-29 2011-10-31 ДЕСИФЕРА ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Циклопропанамиды и аналоги, проявляющие противораковые и антипролиферативные активности
US9724664B2 (en) 2009-03-27 2017-08-08 Bend Research, Inc. Spray-drying process
US8669289B2 (en) 2009-04-24 2014-03-11 The Jackson Laboratory Methods and compositions relating to hematologic malignancies
AU2010249790A1 (en) 2009-05-22 2011-12-08 Exelixis, Inc. Benzoxazepines based P13K/mT0R inhibitors against proliferative diseases
US8394858B2 (en) 2009-12-03 2013-03-12 Novartis Ag Cyclohexane derivatives and uses thereof
US20110237563A1 (en) 2010-03-23 2011-09-29 Dominique Costantini Fast dissolving drug delivery systems
WO2011123788A1 (en) 2010-04-01 2011-10-06 Duke University Compositions and methods for the treatment of cancer
US8569319B2 (en) 2010-04-29 2013-10-29 Deciphera Pharmaceuticals, LLS Pyridone amides and analogs exhibiting anti-cancer and anti-proliferative activities
RU2012151012A (ru) 2010-04-29 2014-06-10 ДЕСИФЕРА ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Циклопропиловые дикарбоксамиды и аналоги, обладающие противораковым и антипролиферативным действием
US9296722B2 (en) 2010-05-27 2016-03-29 Ambit Biosciences Corporation Azolyl urea compounds and methods of use thereof
JP5789259B2 (ja) 2010-07-16 2015-10-07 協和発酵キリン株式会社 含窒素芳香族複素環誘導体
WO2012035131A1 (en) 2010-09-16 2012-03-22 University Of Zurich Treatment of abl overexpressing b-cell lymphoma
WO2012040502A1 (en) 2010-09-24 2012-03-29 Bend Research, Inc. High-temperature spray drying process and apparatus
US20140147415A1 (en) 2010-11-05 2014-05-29 Ab Science Treatment of mastocytosis with masitinib
EA201390766A1 (ru) 2010-11-24 2013-11-29 Экселиксис, Инк. БЕНЗОКСАЗЕПИНЫ КАК ИНГИБИТОРЫ PI3K/mTOR И СПОСОБЫ ИХ ИСПОЛЬЗОВАНИЯ И ПОЛУЧЕНИЯ
US20130288984A1 (en) 2011-01-11 2013-10-31 Glaxosmithkline Llc Combination
AU2012240240A1 (en) 2011-04-04 2013-05-09 Netherlands Cancer Institute Methods and compositions for predicting resistance to anticancer treatment with protein kinase inhibitors
CN102731385A (zh) 2011-04-08 2012-10-17 湖南有色凯铂生物药业有限公司 3-氯-及3-甲氧基-n-甲基-2-吡啶酰胺化合物及其作为抗癌药物的应用
CA2843417C (en) 2011-07-29 2018-08-21 Medivation Prostate Therapeutics, Inc. Treatment of breast cancer
WO2013036232A2 (en) 2011-09-08 2013-03-14 Deciphera Pharmaceuticals, Llc Methods and compositions for the treatment of myeloproliferative diseases and other proliferative diseases
US20130071403A1 (en) 2011-09-20 2013-03-21 Vical Incorporated Synergistic anti-tumor efficacy using alloantigen combination immunotherapy
ES2650608T3 (es) * 2011-10-14 2018-01-19 Array Biopharma, Inc. Dispersión sólida
WO2013078295A2 (en) 2011-11-22 2013-05-30 Deciphera Pharmaceuticals, Llc Pyridone amides and analogs exhibiting anti-cancer and anti-proliferative activities
KR101338510B1 (ko) 2011-12-09 2013-12-11 포항공과대학교 산학협력단 아미노퀴놀론 화합물을 포함하는 간염, 간경변, 또는 간암의 예방 또는 치료용 의약 조성물
AR090151A1 (es) 2012-03-07 2014-10-22 Lilly Co Eli Compuestos inhibidores de raf
US9187474B2 (en) 2012-03-07 2015-11-17 Deciphera Pharmaceuticals, Llc Raf inhibitor compounds
UA122044C2 (uk) * 2012-03-23 2020-09-10 Еррей Біофарма Інк. Лікування раку головного мозку
US9254288B2 (en) 2012-05-07 2016-02-09 The Translational Genomics Research Institute Susceptibility of tumors to tyrosine kinase inhibitors and treatment thereof
WO2013177420A2 (en) 2012-05-23 2013-11-28 St. Jude Children's Research Hospital Methods and compositions for the treatment of bcr-abl positive lymphoblastic leukemias
US8461179B1 (en) 2012-06-07 2013-06-11 Deciphera Pharmaceuticals, Llc Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
CA2875970C (en) 2012-06-07 2017-07-04 Deciphera Pharmaceuticals, Llc Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
WO2014015056A2 (en) 2012-07-17 2014-01-23 Washington University Anti-mucus drugs and uses therefor
JP2015530378A (ja) 2012-08-29 2015-10-15 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung 変形性関節症の処置のためのddr2インヒビター
EP2890815B1 (en) 2012-08-31 2019-03-20 The Regents of the University of Colorado Methods for diagnosis and treatment of cancer
AU2013311705A1 (en) 2012-09-10 2015-02-05 F. Hoffmann-La Roche Ag 6-amino acid heteroaryldihydropyrimidines for the treatment and prophylaxis of Hepatitis B virus infection
WO2014040242A1 (zh) 2012-09-12 2014-03-20 湖南有色凯铂生物药业有限公司 3-氯-及3-甲氧基-n-甲基-2-吡啶酰胺化合物及其作为抗癌药物的应用
CN103664787B (zh) 2012-09-17 2015-09-09 南京圣和药业股份有限公司 炔杂芳环化合物及其应用
US20150275306A1 (en) 2012-10-10 2015-10-01 Stichting Het Nederlands Kanker Instituut Antoni van Leeuwenhoek Ziekenhuis Methods and means for predicting resistance to anti-cancer treatment
FR3000493A1 (fr) 2012-12-28 2014-07-04 Oribase Pharma Nouveaux inhibiteurs de proteines kinases
FR3000492B1 (fr) 2012-12-28 2015-09-11 Oribase Pharma Nouveaux derives azaindole en tant qu'inhibiteurs multikinases
EP2968536B1 (en) 2013-03-13 2023-06-28 The United States of America, as represented by The Secretary, Department of Health and Human Services Methods for modulating chemotherapeutic cytotoxicity
CN104045642B (zh) 2013-03-14 2016-08-24 上海医药工业研究院 含嘧啶或吡啶的稠环化合物及其作为抗肿瘤药物的应用
US9012635B2 (en) 2013-03-15 2015-04-21 Deciphera Pharmaceuticals, Llc Pyridone amides and analogs exhibiting anti-cancer and anti-proliferative activities
WO2014145015A2 (en) 2013-03-15 2014-09-18 Deciphera Pharmaceuticals, Llc Imidazolidinones and analogs exhibiting anti-cancer and anti-proliferative activities
WO2014145029A2 (en) 2013-03-15 2014-09-18 Deciphera Pharmaceuticals, Llc N-acyl-n'-(pyridin-2-yl) ureas and analogs exhibiting anti-cancer and anti-proliferative activities
AU2014233414B2 (en) 2013-03-15 2018-07-12 Deciphera Pharmaceuticals, Llc. N-acyl-N'-(pyridin-2-yl) ureas and analogs exhibiting anti-cancer and anti-proliferative activities
US9193719B2 (en) 2013-03-15 2015-11-24 Deciphera Pharmaceuticals, Llc 1,2,4-triazol-5-ones and analogs exhibiting anti-cancer and anti-proliferative activities
MX365574B (es) 2013-03-15 2019-06-06 Deciphera Pharmaceuticals Llc 2-aminopirimidin-6-onas y analogos que exhiben actividades anticancerosas y antiproliferativas.
US20160101106A1 (en) 2013-05-07 2016-04-14 Inhibikase Therapeutics, Inc. Methods for treating hcv infection
FR3008979B1 (fr) 2013-07-23 2015-07-24 Servier Lab Nouveaux derives phosphates, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US10111897B2 (en) 2013-10-03 2018-10-30 Duke University Compositions and methods for treating cancer with JAK2 activity
WO2015069217A1 (en) 2013-11-05 2015-05-14 Baylor College Of Medicine Src kinase inhibition as treatment for lympangioleiomyomatosis and tuberous sclerosis
US9457019B2 (en) 2013-11-07 2016-10-04 Deciphera Pharmaceuticals, Llc Methods for inhibiting tie-2 kinase useful in the treatment of cancer
KR20160070188A (ko) 2013-11-07 2016-06-17 데시페라 파마슈티칼스, 엘엘씨. 암치료에 유용한 tie2 키나아제의 억제 방법
WO2015076213A1 (ja) 2013-11-22 2015-05-28 独立行政法人国立成育医療研究センター 急性リンパ芽球性白血病の新規キメラ遺伝子atf7ip-pdgfrb
WO2015092423A1 (en) 2013-12-20 2015-06-25 Respivert Limited Urea derivatives useful as kinase inhibitors
WO2015106292A1 (en) 2014-01-13 2015-07-16 Coferon, Inc. Bcr-abl tyrosine-kinase ligands capable of dimerizing in an aqueous solution, and methods of using same
WO2015106294A1 (en) 2014-01-13 2015-07-16 Coferon,Inc. Bivalent bcr-abl tyrosine kinase ligands, and methods of using same
CA2944043A1 (en) 2014-03-25 2015-10-01 University Of Utah Research Foundation Peptide inhibitors of bcr-abl oligomerization
WO2015184443A1 (en) 2014-05-30 2015-12-03 The Regents Of The University Of Colorado Activating ntrk1 gene fusions predictive of kinase inhibitor therapy
BR112017002231A2 (pt) 2014-08-07 2018-07-17 Pharmacyclics Llc novas formulações de um inibidor de tirosina cinase de bruton
CN105461699B (zh) 2014-09-25 2019-07-09 广东东阳光药业有限公司 取代的杂环化合物及其使用方法和用途
WO2016061231A1 (en) 2014-10-14 2016-04-21 Deciphera Pharmaceuticals, Llc Inhibition of tumor cell interactions with the microenvironment resulting in a reduction in tumor growth and disease progression
EP3206752A1 (en) 2014-10-14 2017-08-23 Deciphera Pharmaceuticals, LLC Inhibition of trk kinase mediated tumor growth and disease progression
US20170360791A1 (en) 2014-12-04 2017-12-21 Astex Pharmaceuticals, Inc. Pharmaceutical compositions for increasing the bioavailability of poorly soluble drugs
US20160166679A1 (en) 2014-12-12 2016-06-16 Purdue Research Foundation Method of treatment using folate conjugates and tyrosine kinase inhibitors
EP3034092A1 (en) 2014-12-17 2016-06-22 Université de Lausanne Adoptive immunotherapy for treating cancer
WO2016103223A1 (en) 2014-12-23 2016-06-30 Fratagene Therapeutics Ltd. Methods of treating friedreich's ataxia using src inhibitors
WO2016114322A1 (ja) 2015-01-13 2016-07-21 国立大学法人京都大学 筋萎縮性側索硬化症の予防及び/又は治療剤
US9637488B2 (en) 2015-01-29 2017-05-02 Fuqiang Ruan Heterocyclic compounds as inhibitors of class I PI3KS
WO2016135046A1 (en) 2015-02-24 2016-09-01 Academisch Medisch Centrum Inhibitors of raf1, mst1, and pkl1 for use in the treatment of a retrovirus
WO2016154524A1 (en) 2015-03-26 2016-09-29 Emory University Carbonic anhydrase inhibitors and uses related thereto
CA2987281A1 (en) 2015-05-29 2016-12-08 Ignyta, Inc. Compositions and methods for treating patients with rtk mutant cells
EP3120851A1 (en) 2015-07-21 2017-01-25 Pangaea Biotech S.L. 4-amino-6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)-pyrido[2,3-d]pyrimidin-7(8h)-one for treatment of solid cancers
WO2017042944A1 (ja) 2015-09-10 2017-03-16 国立大学法人山梨大学 フィラデルフィア染色体陽性(Ph+)急性リンパ性白血病(ALL)の治療薬又は治療方法
KR20180097530A (ko) 2015-11-02 2018-08-31 예일 유니버시티 단백질분해 표적화 키메라 화합물(Proteolysis Targeting Chimera compound) 및 그의 제조 및 사용 방법
CA3010101A1 (en) 2015-12-29 2017-07-06 Board Of Regents, The University Of Texas System Inhibition of p38 mapk for the treatment of cancer
CA3015753A1 (en) 2016-02-26 2017-08-31 Celgene Corporation Idh2 inhibitors for the treatment of haematological maligancies and solid tumours
WO2017214514A1 (en) 2016-06-09 2017-12-14 Bioxcel Corporation Use of src family kinase inhibitor in ribosomal disorder
WO2018005737A1 (en) 2016-06-29 2018-01-04 The General Hospital Corporation Renal clearable organic nanocarriers
SI3513809T1 (sl) 2016-09-13 2022-07-29 Kyowa Kirin Co.,Ltd. Medicinski sestavek, ki vsebuje tivozanib
AU2017325844A1 (en) 2016-09-14 2019-03-07 Gilead Sciences, Inc. SYK inhibitors
TW201822764A (zh) 2016-09-14 2018-07-01 美商基利科學股份有限公司 Syk抑制劑
US11932870B2 (en) 2016-12-05 2024-03-19 Fate Therapeutics, Inc. Compositions and methods for immune cell modulation in adoptive immunotherapies
CN106822128A (zh) 2017-02-24 2017-06-13 南华大学附属第医院 酪氨酸激酶抑制剂dcc‑2036的新应用
CA3060416A1 (en) 2017-04-21 2018-10-25 Epizyme, Inc. Combination therapies with ehmt2 inhibitors
US11802875B2 (en) 2017-05-30 2023-10-31 Albert Einstein College Of Medicine Method for treating neoadjuvant chemotherapy-induced metastasis
EP3630110A1 (en) 2017-05-30 2020-04-08 Deciphera Pharmaceuticals, Inc. Use of 1-[4-bromo-5-[1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl]-2-fluorophenyl]-3-phenylurea and analogs for the treatment of cancers associated with genetic abnormalities in platelet derived growth factor receptoralpha
BR112020007972A2 (pt) * 2017-10-27 2020-10-20 Plexxikon, Inc. formulações de composto que modula quinases
CA3089630A1 (en) 2018-01-31 2019-08-08 Deciphera Pharmaceuticals, Llc Combination therapy for the treatment of mastocytosis
CN115192726A (zh) 2018-04-03 2022-10-18 深圳大学 免疫激动剂靶向化合物的合成及其应用
FI3902547T3 (fi) 2018-12-28 2023-12-05 Deciphera Pharmaceuticals Llc Csf1r-inhibiittoreita käytettäväksi syövän hoitamisessa
EP3938363A1 (en) * 2019-03-11 2022-01-19 Teva Pharmaceuticals International GmbH Solid state forms of ripretinib
AU2020274011B2 (en) 2019-05-10 2024-02-15 Deciphera Pharmaceuticals, Llc Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof
TW202108573A (zh) 2019-05-10 2021-03-01 美商迪賽孚爾製藥有限公司 苯基胺基嘧啶醯胺自噬抑制劑及其使用方法
KR20220045189A (ko) 2019-08-12 2022-04-12 데시페라 파마슈티칼스, 엘엘씨. 위장관 기질 종양을 치료하는 방법
WO2021030405A1 (en) 2019-08-12 2021-02-18 Deciphera Pharmaceuticals, Llc Ripretinib for treating gastrointestinal stromal tumors
CA3163051A1 (en) 2019-12-30 2021-07-08 Michael D. Kaufman Compositions of 1-(4-bromo-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl)-3-phenylurea
KR20220123057A (ko) 2019-12-30 2022-09-05 데시페라 파마슈티칼스, 엘엘씨. 비정질 키나아제 억제제 제형 및 이의 사용 방법
CN114902895B (zh) 2022-04-06 2023-12-12 安徽科技学院 一种基于蔬菜种植的能源回收式大棚

Also Published As

Publication number Publication date
US20230270728A1 (en) 2023-08-31
US20220265622A1 (en) 2022-08-25
CA3163053A1 (en) 2021-07-08
SI4084778T1 (sl) 2024-01-31
EP4084778B1 (en) 2023-11-01
RS65058B1 (sr) 2024-02-29
US11576903B2 (en) 2023-02-14
IL293866A (en) 2022-08-01
US20220031677A1 (en) 2022-02-03
CN115135308A (zh) 2022-09-30
US11185535B2 (en) 2021-11-30
DK4084778T3 (da) 2023-12-11
LT4084778T (lt) 2024-01-25
FI4084778T3 (fi) 2023-12-18
EP4327827A2 (en) 2024-02-28
KR20220123057A (ko) 2022-09-05
PL4084778T3 (pl) 2024-03-04
BR112022013109A2 (pt) 2022-09-06
US11801237B2 (en) 2023-10-31
EP4084778A1 (en) 2022-11-09
AU2020419197B2 (en) 2023-08-31
AU2020419197A1 (en) 2022-06-30
JP2023509629A (ja) 2023-03-09
US20220265623A1 (en) 2022-08-25
AU2023248048A1 (en) 2023-10-26
US20210196692A1 (en) 2021-07-01

Similar Documents

Publication Publication Date Title
MX2022008103A (es) Formulaciones de inhibidores de la cinasa amorfa y metodos de estas.
PH12018502125A1 (en) Bipyrazole derivatives as jak inhibitors
MX2021013110A (es) Compuestos heterociclicos como inhibidores de la cinasa ret.
GEP20207105B (en) 1,1,1-trifluoro-3-hydroxypropan-2-yl carbamate derivatives and 1,1,1-trifluoro-4-hydroxybutan-2yl carbamate derivatives as magl inhibitors
EP4104837A3 (en) Heterocyclic compounds as ret kinase inhibitors
UA113156C2 (xx) Циклобутилзаміщені похідні піролопіридину й піролопіримідину як інгібітори jak
NZ708864A (en) Substituted pyrimidine aminoalkyl-quinazolones as phosphatidylinositol 3-kinase inhibitors
NZ630719A (en) Imidazo [1, 2 - b] pyridazine - based compounds, compositions comprising them, and uses thereof
MX336051B (es) Diarilacetileno hidracido que contiene inhibidores de tirosina quinasa.
PH12015501755A1 (en) Azabenzimidazole compounds as inhibitors of pde4 isozymes for the treatment of cns and other disorders
MD20160132A2 (ro) Săruri de adiţie ale (S)-2-(1-(6-amino-5-cianopirimidin-4-ilamino)etil)-4-oxo-3-fenil-3,4-dihidropirolo[1,2-f][1,2,4]triazin-5-carbonitrilului
PH12020500528A1 (en) Pyrimidine compound as jak kinase inhibitor
MX2016016530A (es) Inhibidores de fosfatidilinositol 3-quinasa.
JO3794B1 (ar) المركبات متعددة الحلقات كمثبطات لتيروزين كيناز بروتون
MX2023005636A (es) Inhibidores de bcl6 derivados de bencimidazolona.
MX2019013561A (es) Compuestos de pirrolopiridina-anilina para el tratamiento de trastornos dermicos.
MX2013013557A (es) Derivados de alcoholes 1-fenil-2-piridinil alquilicos como inhibidores de fosfodiesterasa.
MX2018007084A (es) Inhibidores de la tirosina quinasa de bruton y metodos de su uso.
PH12021550857A1 (en) Compounds, compositions, and methods for modulating cdk9 activity
MX2022013941A (es) Inhibidores de imino sulfanona de enpp1.
ZA202201364B (en) Deuterated compounds for use in the treatment of cancer
TN2017000485A1 (en) Tricyclic compounds and their use as phosphodiesterase inhibitors
MY195576A (en) Novel Amino-Imidazopyridine Derivatives as Janus Kinase Inhibitors and Pharmaceutical use Thereof
MX2018010177A (es) Compuestos de 6,7-dihidro-5h-pirazolo[5,1-b][1,3]oxazina-2-carboxa mida.
MX2011012522A (es) Inhibidores de pirazol sustituido de proteina cinasa c-met.