MD4684B1 - Formulări pe bază de imidazopirazine în calitate de inhibitori SYK - Google Patents

Formulări pe bază de imidazopirazine în calitate de inhibitori SYK Download PDF

Info

Publication number
MD4684B1
MD4684B1 MDA20160012A MD20160012A MD4684B1 MD 4684 B1 MD4684 B1 MD 4684B1 MD A20160012 A MDA20160012 A MD A20160012A MD 20160012 A MD20160012 A MD 20160012A MD 4684 B1 MD4684 B1 MD 4684B1
Authority
MD
Moldova
Prior art keywords
imidazopyrazine
based formulations
syk inhibitors
pharmaceutical compositions
relates
Prior art date
Application number
MDA20160012A
Other languages
English (en)
Russian (ru)
Other versions
MD20160012A2 (ro
Inventor
Б Ли
Диана СПЕРГЕР
Димитриос СТЕФАНИДИС
Мелисса Джин КАСТИЛ
Роучанак Пакдаман
Original Assignee
Gilead Connecticut INc.
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=51359427&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=MD4684(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Gilead Connecticut INc. filed Critical Gilead Connecticut INc.
Publication of MD20160012A2 publication Critical patent/MD20160012A2/ro
Publication of MD4684B1 publication Critical patent/MD4684B1/ro

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2095—Tabletting processes
    • 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
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B29—WORKING OF PLASTICS; WORKING OF SUBSTANCES IN A PLASTIC STATE IN GENERAL
    • B29B—PREPARATION OR PRETREATMENT OF THE MATERIAL TO BE SHAPED; MAKING GRANULES OR PREFORMS; RECOVERY OF PLASTICS OR OTHER CONSTITUENTS OF WASTE MATERIAL CONTAINING PLASTICS
    • B29B9/00—Making granules
    • B29B9/10—Making granules by moulding the material, i.e. treating it in the molten state
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B29—WORKING OF PLASTICS; WORKING OF SUBSTANCES IN A PLASTIC STATE IN GENERAL
    • B29C—SHAPING OR JOINING OF PLASTICS; SHAPING OF MATERIAL IN A PLASTIC STATE, NOT OTHERWISE PROVIDED FOR; AFTER-TREATMENT OF THE SHAPED PRODUCTS, e.g. REPAIRING
    • B29C43/00—Compression moulding, i.e. applying external pressure to flow the moulding material; Apparatus therefor
    • B29C43/003—Compression moulding, i.e. applying external pressure to flow the moulding material; Apparatus therefor characterised by the choice of material
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B29—WORKING OF PLASTICS; WORKING OF SUBSTANCES IN A PLASTIC STATE IN GENERAL
    • B29C—SHAPING OR JOINING OF PLASTICS; SHAPING OF MATERIAL IN A PLASTIC STATE, NOT OTHERWISE PROVIDED FOR; AFTER-TREATMENT OF THE SHAPED PRODUCTS, e.g. REPAIRING
    • B29C43/00—Compression moulding, i.e. applying external pressure to flow the moulding material; Apparatus therefor
    • B29C43/02—Compression moulding, i.e. applying external pressure to flow the moulding material; Apparatus therefor of articles of definite length, i.e. discrete articles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63—Esters of sulfonic acids
    • C07C309/64—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms
    • C07C309/65—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms of a saturated carbon skeleton
    • C07C309/66—Methanesulfonates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
    • A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B29—WORKING OF PLASTICS; WORKING OF SUBSTANCES IN A PLASTIC STATE IN GENERAL
    • B29K—INDEXING SCHEME ASSOCIATED WITH SUBCLASSES B29B, B29C OR B29D, RELATING TO MOULDING MATERIALS OR TO MATERIALS FOR MOULDS, REINFORCEMENTS, FILLERS OR PREFORMED PARTS, e.g. INSERTS
    • B29K2995/00—Properties of moulding materials, reinforcements, fillers, preformed parts or moulds
    • B29K2995/0037—Other properties
    • B29K2995/0056—Biocompatible, e.g. biopolymers or bioelastomers

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Mechanical Engineering (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Inorganic Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Transplantation (AREA)
  • Neurology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Invenţia se referă la compoziţii farmaceutice, care conţin o sare de bis-mesilat a compusului cu formula (I):(I),sau un hidrat al acesteia şi cel puţin un polimer acceptabil farmaceutic. Invenţia de asemenea, se referă la utilizarea compoziţiilor farmaceutice în tratamentul cancerului şi bolilor autoimune.
MDA20160012A 2013-07-30 2014-07-29 Formulări pe bază de imidazopirazine în calitate de inhibitori SYK MD4684B1 (ro)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361860198P 2013-07-30 2013-07-30
PCT/US2014/048741 WO2015017466A1 (en) 2013-07-30 2014-07-29 Formulation of syk inhibitors

Publications (2)

Publication Number Publication Date
MD20160012A2 MD20160012A2 (ro) 2016-07-31
MD4684B1 true MD4684B1 (ro) 2020-03-31

Family

ID=51359427

Family Applications (1)

Application Number Title Priority Date Filing Date
MDA20160012A MD4684B1 (ro) 2013-07-30 2014-07-29 Formulări pe bază de imidazopirazine în calitate de inhibitori SYK

Country Status (30)

Country Link
US (3) US9382256B2 (ro)
EP (1) EP3027171B1 (ro)
JP (2) JP6153667B2 (ro)
KR (2) KR20160036590A (ro)
CN (1) CN105431137A (ro)
AP (1) AP2016009007A0 (ro)
AR (1) AR097159A1 (ro)
AU (1) AU2014296314B2 (ro)
BR (1) BR112016001678A2 (ro)
CA (1) CA2919522C (ro)
CL (1) CL2016000241A1 (ro)
CR (1) CR20160099A (ro)
EA (1) EA201690127A1 (ro)
ES (1) ES2795973T3 (ro)
HK (1) HK1222329A1 (ro)
IL (1) IL243577A0 (ro)
MD (1) MD4684B1 (ro)
MX (1) MX2016001480A (ro)
NZ (1) NZ715745A (ro)
PE (1) PE20160605A1 (ro)
PH (1) PH12016500170A1 (ro)
PL (1) PL3027171T3 (ro)
PT (1) PT3027171T (ro)
PY (1) PY1432623A (ro)
SG (1) SG11201600378SA (ro)
SI (1) SI3027171T1 (ro)
TW (1) TW201601728A (ro)
UA (1) UA115815C2 (ro)
UY (1) UY35684A (ro)
WO (1) WO2015017466A1 (ro)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101743784B1 (ko) 2008-12-08 2017-06-05 질레드 코네티컷 인코포레이티드 이미다조피라진 ｓｙｋ 억제제
ES2530449T3 (es) 2010-03-11 2015-03-02 Gilead Connecticut Inc Inhibidores de Syk de imidazopiridinas
EA029281B1 (ru) * 2013-07-30 2018-03-30 Джилид Коннектикут, Инк. Полиморф ингибиторов syk
SG11201600378SA (en) 2013-07-30 2016-02-26 Gilead Connecticut Inc Formulation of syk inhibitors
US9687492B2 (en) * 2013-12-04 2017-06-27 Gilead Sciences, Inc. Methods for treating cancers
US9290505B2 (en) 2013-12-23 2016-03-22 Gilead Sciences, Inc. Substituted imidazo[1,2-a]pyrazines as Syk inhibitors
TWI735853B (zh) 2013-12-23 2021-08-11 美商克洛諾斯生技有限公司 脾酪胺酸激酶抑制劑
CA2955180A1 (en) 2014-07-14 2016-01-21 Gilead Sciences, Inc. Combinations comprising entospletinib and a vinca-alkaloid for treating cancers
TW201639573A (zh) * 2015-02-03 2016-11-16 吉李德科學股份有限公司 有關治療癌症之合併治療
CA2983611A1 (en) 2015-04-21 2016-10-27 Gilead Sciences, Inc. Treatment of chronic graft versus host disease with syk inhibitors
IL256299B2 (en) * 2015-06-30 2023-11-01 Genentech Inc Immediate-release tablets containing a drug and processes for creating the tablets
CN109071547A (zh) * 2016-02-26 2018-12-21 苏州晶云药物科技股份有限公司 (6-(1H-吲唑-6-基)-N-[4-(4-吗啉基)苯基]咪唑并[1,2-a]吡嗪-8-胺)甲磺酸盐的新晶型
WO2018053190A1 (en) * 2016-09-14 2018-03-22 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
WO2018195471A1 (en) 2017-04-21 2018-10-25 Gilead Sciences, Inc. Syk inhibitors in combination with hypomethylating agents
AU2018257901A1 (en) * 2017-04-24 2019-11-14 Samus Therapeutics, Inc. Hsp90 inhibitor oral formulations and related methods
CN115028640A (zh) * 2017-08-25 2022-09-09 吉利德科学公司 Syk抑制剂的多晶型物
US11040975B2 (en) 2017-12-08 2021-06-22 Merck Sharp & Dohme Corp. Carbocyclic nucleoside reverse transcriptase inhibitors
WO2020172431A1 (en) 2019-02-22 2020-08-27 Gilead Sciences, Inc. Solid forms of condensed pyrazines as syk inhibitors
CN113402506B (zh) * 2021-06-17 2023-06-16 四川大学 中间体和制备方法及其在合成长春布宁上的应用
WO2024037910A1 (en) * 2022-08-17 2024-02-22 Institut National de la Santé et de la Recherche Médicale Syk inhibitors for use in the treatment of cancer

Family Cites Families (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2607813B1 (fr) 1986-12-05 1989-03-31 Montpellier I Universite Alkylamino-8 imidazo (1,2-a) pyrazines et derives, leur preparation et leur application en therapeutique
US5137876A (en) 1990-10-12 1992-08-11 Merck & Co., Inc. Nucleoside antiviral and anti-inflammatory compounds and compositions and methods for using same
DE4327027A1 (de) 1993-02-15 1994-08-18 Bayer Ag Imidazoazine
DE4337609A1 (de) 1993-11-04 1995-05-11 Boehringer Ingelheim Kg Neue Pyrazincarboxamidderivate, ihre Herstellung und ihre Verwendung in Arzneimitteln
DE4337611A1 (de) 1993-11-04 1995-05-11 Boehringer Ingelheim Kg Neue Benzoylguanidine, ihre Herstellung und ihre Verwendung in Arzneimitteln
FR2711993B1 (fr) 1993-11-05 1995-12-01 Rhone Poulenc Rorer Sa Médicaments contenant des dérivés de 7H-imidazol[1,2-a]pyrazine-8-one, les nouveaux composés et leur préparation.
CN1087725C (zh) 1994-03-25 2002-07-17 同位素技术有限公司 用氘代方法增强药物效果
US6334997B1 (en) 1994-03-25 2002-01-01 Isotechnika, Inc. Method of using deuterated calcium channel blockers
FR2723373B1 (fr) 1994-08-02 1996-09-13 Rhone Poulenc Rorer Sa Forme purifiee de streptogramines, sa preparation et les compositions pharmaceutiques qui la contiennent
AU5348396A (en) 1995-05-01 1996-11-21 Fujisawa Pharmaceutical Co., Ltd. Imidazo 1,2-a pyridine and imidazo 1,2-a pyridezine derivati ves and their use as bone resorption inhibitors
US5593997A (en) 1995-05-23 1997-01-14 Pfizer Inc. 4-aminopyrazolo(3-,4-D)pyrimidine and 4-aminopyrazolo-(3,4-D)pyridine tyrosine kinase inhibitors
SE9704404D0 (sv) 1997-11-28 1997-11-28 Astra Ab New compounds
DE19948434A1 (de) 1999-10-08 2001-06-07 Gruenenthal Gmbh Substanzbibliothek enthaltend bicyclische Imidazo-5-amine und/oder bicyclische Imidazo-3-amine
WO2001034119A2 (en) * 1999-11-12 2001-05-17 Abbott Laboratories Inhibitors of crystallization in a solid dispersion
DZ3227A1 (fr) * 1999-12-23 2001-07-05 Pfizer Prod Inc Compositions pharmaceutiques fournissant des concentrations de medicaments ameliorees
JP2001302667A (ja) 2000-04-28 2001-10-31 Bayer Ag イミダゾピリミジン誘導体およびトリアゾロピリミジン誘導体
GB0018473D0 (en) 2000-07-27 2000-09-13 Merck Sharp & Dohme Therapeutic agents
DE10050663A1 (de) 2000-10-13 2002-04-18 Gruenenthal Gmbh Verwendung von substituierten Imidazo[1,2-a]pyridin-, -pyrimidin- und pyrazin-3-yl-amin-Derivaten zur Herstellung von Medikamenten zur NOS-Inhibierung
EP1363702A4 (en) 2001-01-30 2007-08-22 Cytopia Pty Ltd PROCESS FOR INHIBITING KINASES
GB0103926D0 (en) 2001-02-17 2001-04-04 Astrazeneca Ab Chemical compounds
WO2002076985A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
US6858613B2 (en) 2002-02-19 2005-02-22 Pfizer Inc. Fused bicyclic-N-bridged-heteroaromatic carboxamides for the treatment of disease
CA2482991A1 (en) 2002-04-19 2003-10-30 Cellular Genomics, Inc. Imidazo[1,2-a]pyrazin-8-ylamines method of making and method of use thereof
CA2485430C (en) 2002-05-14 2011-12-06 Xenova Limited Process for the preparation of a hydrate of an anthranilic acid derivative
WO2004022562A1 (en) 2002-09-09 2004-03-18 Cellular Genomics, Inc. 6-ARYL-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINES, METHOD OF MAKING, AND METHOD OF USE THEREOF
DE60317529T2 (de) 2002-09-19 2008-09-25 Schering Corp. Imidazopyridine als hemmstoffe cyclin abhängiger kinasen
DE60317353T2 (de) 2002-09-23 2008-08-28 Schering Corp. Imidazopyrazine als cdk-inhibitoren
AU2003275031B2 (en) 2002-09-23 2006-08-17 Schering Corporation Novel imidazopyrazines as cyclin dependent kinase inhibitors
US7160885B2 (en) 2003-02-10 2007-01-09 Cgi Pharmaceuticals, Inc. Certain 6, 8-(heteroaryl or aryl) disubstituted imidazo[1,2-a]pyrazines as modulators of Hsp90 complex activity
US7186832B2 (en) 2003-02-20 2007-03-06 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
US7157460B2 (en) 2003-02-20 2007-01-02 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
US20060183746A1 (en) 2003-06-04 2006-08-17 Currie Kevin S Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds
WO2005014599A1 (en) 2003-06-04 2005-02-17 Cellular Genomics, Inc. Imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of bruton’s tyrosine kinase by such compounds
WO2005005429A1 (en) 2003-06-30 2005-01-20 Cellular Genomics, Inc. Certain heterocyclic substituted imidazo[1,2-a]pyrazin-8-ylamines and methods of inhibition of bruton’s tyrosine kinase by such compounds
US7259164B2 (en) 2003-08-11 2007-08-21 Cgi Pharmaceuticals, Inc. Certain substituted imidazo[1,2-a]pyrazines, as modulators of kinase activity
WO2005047290A2 (en) 2003-11-11 2005-05-26 Cellular Genomics Inc. Imidazo[1,2-a] pyrazin-8-ylamines as kinase inhibitors
WO2005085252A1 (en) 2004-03-04 2005-09-15 Biofocus Discovery Limited Imidazo ‘1,2-a’ pyrazine compounds which interact with protein kinases
JP2008503475A (ja) * 2004-06-17 2008-02-07 フォーレスト ラボラトリーズ， インコーポレイテッド メマンチンの放出が改変された製剤
DE602005023333D1 (de) 2004-10-15 2010-10-14 Takeda Pharmaceutical Kinaseinhibitoren
EP1812442A2 (en) 2004-11-10 2007-08-01 CGI Pharmaceuticals, Inc. Imidazo[1,2-a]pyrazin-8-ylamines useful as modulators of kinase activity
CA2628455A1 (en) 2005-11-10 2007-05-24 Merck Sharp & Dohme Corp. Imidazopyrazines as protein kinase inhibitors
ES2549862T3 (es) 2006-08-30 2015-11-02 Cellzome Limited Derivados de triazol como inhibidores de quinasa
PE20080839A1 (es) 2006-09-11 2008-08-23 Cgi Pharmaceuticals Inc Determinadas amidas sustituidas, metodo de elaboracion y metodo de uso de las mismas
CL2008002793A1 (es) 2007-09-20 2009-09-04 Cgi Pharmaceuticals Inc Compuestos derivados de amidas sustituidas, inhibidores de la actividad de btk; composicion farmaceutica que los comprende; utiles en el tratamiento del cancer, trastornos oseos, enfermedades autoinmunes, entre otras
CN101952283B (zh) 2007-12-14 2013-04-17 霍夫曼-拉罗奇有限公司 咪唑并[1，2-a]吡啶和咪唑并[1，2-b]哒嗪衍生物
NZ587039A (en) 2008-02-13 2013-01-25 Gilead Connecticut Inc 6-aryl-imidazo[1, 2-a]pyrazine derivatives, method of making, and method of use thereof
CA2719115A1 (en) 2008-03-07 2009-09-11 Pfizer Inc. Methods, dosage forms, and kits for administering ziprasidone without food
EP2297142B1 (en) 2008-06-24 2015-10-14 F. Hoffmann-La Roche AG Novel substituted pyridin-2-ones and pyridazin-3-ones
CA2728683C (en) 2008-07-02 2017-05-02 F.Hoffmann-La Roche Ag Novel phenylpyrazinones as kinase inhibitors
CA2726460C (en) 2008-07-15 2017-02-21 F. Hoffmann-La Roche Ag Novel phenyl-imidazopyridines and pyridazines
TWI453207B (zh) 2008-09-08 2014-09-21 Signal Pharm Llc 胺基三唑并吡啶，其組合物及使用其之治療方法
KR101745732B1 (ko) 2008-12-08 2017-06-12 질레드 코네티컷 인코포레이티드 이미다조피라진 ｓｙｋ 억제제
KR101743784B1 (ko) 2008-12-08 2017-06-05 질레드 코네티컷 인코포레이티드 이미다조피라진 ｓｙｋ 억제제
US8450321B2 (en) 2008-12-08 2013-05-28 Gilead Connecticut, Inc. 6-(1H-indazol-6-yl)-N-[4-(morpholin-4-yl)phenyl]imidazo-[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a SYK inhibitor
US10071059B2 (en) 2009-12-18 2018-09-11 Frieslandcampina Nederland Holding B.V. Co-processed tablet excipient composition its preparation and use
ES2530449T3 (es) 2010-03-11 2015-03-02 Gilead Connecticut Inc Inhibidores de Syk de imidazopiridinas
WO2013188856A1 (en) 2012-06-14 2013-12-19 Gilead Connecticut, Inc. Imidazopyrazine syk inhibitors
US20140051696A1 (en) * 2012-08-14 2014-02-20 Gilead Calistoga Llc Therapies for treating cancer
US20140148430A1 (en) 2012-11-26 2014-05-29 Gilead Connecticut, Inc. Imidazopyridines syk inhibitors
SG11201600378SA (en) * 2013-07-30 2016-02-26 Gilead Connecticut Inc Formulation of syk inhibitors
EA029281B1 (ru) * 2013-07-30 2018-03-30 Джилид Коннектикут, Инк. Полиморф ингибиторов syk
JP6159028B2 (ja) 2013-07-31 2017-07-05 ギリアード サイエンシーズ， インコーポレイテッド Ｓｙｋ阻害剤
US9687492B2 (en) 2013-12-04 2017-06-27 Gilead Sciences, Inc. Methods for treating cancers
US9290505B2 (en) 2013-12-23 2016-03-22 Gilead Sciences, Inc. Substituted imidazo[1,2-a]pyrazines as Syk inhibitors
PL3087085T3 (pl) * 2013-12-23 2019-07-31 Gilead Sciences, Inc. Synteza makrocyklicznego tripeptydu hamującego NS3 HCV

Also Published As

Publication number Publication date
CL2016000241A1 (es) 2016-06-17
US20150038504A1 (en) 2015-02-05
HK1222329A1 (zh) 2017-06-30
WO2015017466A1 (en) 2015-02-05
KR20170116203A (ko) 2017-10-18
US9949932B2 (en) 2018-04-24
US9918939B2 (en) 2018-03-20
CA2919522A1 (en) 2015-02-05
MX2016001480A (es) 2017-01-05
UA115815C2 (uk) 2017-12-26
CA2919522C (en) 2019-02-26
SI3027171T1 (sl) 2020-08-31
US20160166580A1 (en) 2016-06-16
CR20160099A (es) 2016-07-11
AR097159A1 (es) 2016-02-24
PT3027171T (pt) 2020-06-18
TW201601728A (zh) 2016-01-16
PL3027171T3 (pl) 2020-08-24
PH12016500170A1 (en) 2016-04-25
NZ715745A (en) 2017-06-30
CN105431137A (zh) 2016-03-23
EP3027171B1 (en) 2020-03-25
JP6153667B2 (ja) 2017-06-28
MD20160012A2 (ro) 2016-07-31
EA201690127A1 (ru) 2016-07-29
KR20160036590A (ko) 2016-04-04
AU2014296314B2 (en) 2017-07-27
SG11201600378SA (en) 2016-02-26
PY1432623A (es) 2017-09-01
AU2014296314A1 (en) 2016-01-28
EP3027171A1 (en) 2016-06-08
JP2017178963A (ja) 2017-10-05
UY35684A (es) 2015-02-27
JP6530444B2 (ja) 2019-06-12
AP2016009007A0 (en) 2016-01-31
ES2795973T3 (es) 2020-11-25
BR112016001678A2 (pt) 2017-09-19
US9382256B2 (en) 2016-07-05
IL243577A0 (en) 2016-02-29
JP2016525579A (ja) 2016-08-25
PE20160605A1 (es) 2016-07-20
US20170020821A1 (en) 2017-01-26

Similar Documents

Publication Publication Date Title
MD20160012A2 (ro) Formulare de inhibitori SYK
PH12017502141A1 (en) Compounds and their methods of use
MX377916B (es) Compuestos 4-amino-imidazoquinolina.
PH12018500065A1 (en) Oxysterols and methods of use thereof
PH12016502382A1 (en) Substituted indazole compounds as irak4 inhibitors
MD20160106A2 (ro) Compuşi aril sau heteroaril biciclici condensaţi şi utilizarea acestora ca inhibitori IRAK4
MX377845B (es) Inhibidores de calicreína plasmática humana.
MX368703B (es) Un inhibidor de mdm2 derivado de acido benzoico para el tratamiento del cancer.
MX2015012850A (es) Inhibidores de la arginina metiltransferasa y usos de los mismos.
MD4666B1 (ro) Inhibitori ai Syk
MD20160017A2 (ro) Polimorf al inhibitorilor SYK
EA201650031A1 (ru) Производные пирролидин-2,5-диона, фармацевтические композиции и способы применения в качестве ингибиторов ido1
UA117830C2 (uk) Похідні біпіразолу як інгібітори jak
PH12018500061A1 (en) Oxysterols and methods of use thereof
EA201492287A1 (ru) Дейтерированные производные руксолитиниба
MD20150043A2 (ro) Inhibitori ai histon-demetilazelor
EA201891063A1 (ru) Производные дигидроимидазопиразинона, применимые в лечении рака
MX2016002544A (es) Compuestos utiles como inmunomoduladores.
JO3148B1 (ar) مركب مثبط لإشارات مسار notch
PH12016501462A1 (en) Neprilysin inhibitors
EA201600434A1 (ru) Применение производных бензимидазолпролина
EA201790276A1 (ru) Новые имидазопиридазиновые соединения и их применение
MX2016003522A (es) Derivados de quinazolinas y su uso como inhibidores de la adn metiltransferasa.
MX362896B (es) Cis-morfolinona y otros compuestos como inhibidores de mdm2 para el tratamiento del cáncer.
MX390051B (es) Antagonistas de ep4.

Legal Events

Date Code Title Description
KA4A Patent for invention lapsed due to non-payment of fees (with right of restoration)