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

    • 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
    • A61K9/2095Tabletting processes
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B29WORKING OF PLASTICS; WORKING OF SUBSTANCES IN A PLASTIC STATE IN GENERAL
    • B29BPREPARATION OR PRETREATMENT OF THE MATERIAL TO BE SHAPED; MAKING GRANULES OR PREFORMS; RECOVERY OF PLASTICS OR OTHER CONSTITUENTS OF WASTE MATERIAL CONTAINING PLASTICS
    • B29B9/00Making granules
    • B29B9/10Making granules by moulding the material, i.e. treating it in the molten state
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B29WORKING OF PLASTICS; WORKING OF SUBSTANCES IN A PLASTIC STATE IN GENERAL
    • B29CSHAPING OR JOINING OF PLASTICS; SHAPING OF MATERIAL IN A PLASTIC STATE, NOT OTHERWISE PROVIDED FOR; AFTER-TREATMENT OF THE SHAPED PRODUCTS, e.g. REPAIRING
    • B29C43/00Compression moulding, i.e. applying external pressure to flow the moulding material; Apparatus therefor
    • B29C43/003Compression moulding, i.e. applying external pressure to flow the moulding material; Apparatus therefor characterised by the choice of material
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B29WORKING OF PLASTICS; WORKING OF SUBSTANCES IN A PLASTIC STATE IN GENERAL
    • B29CSHAPING OR JOINING OF PLASTICS; SHAPING OF MATERIAL IN A PLASTIC STATE, NOT OTHERWISE PROVIDED FOR; AFTER-TREATMENT OF THE SHAPED PRODUCTS, e.g. REPAIRING
    • B29C43/00Compression moulding, i.e. applying external pressure to flow the moulding material; Apparatus therefor
    • B29C43/02Compression moulding, i.e. applying external pressure to flow the moulding material; Apparatus therefor of articles of definite length, i.e. discrete articles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63Esters of sulfonic acids
    • C07C309/64Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms
    • C07C309/65Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms of a saturated carbon skeleton
    • C07C309/66Methanesulfonates
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • 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
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2833Organic macromolecular compounds
    • A61K9/286Polysaccharides, e.g. gums; Cyclodextrin
    • A61K9/2866Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B29WORKING OF PLASTICS; WORKING OF SUBSTANCES IN A PLASTIC STATE IN GENERAL
    • B29KINDEXING 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
    • B29K2995/00Properties of moulding materials, reinforcements, fillers, preformed parts or moulds
    • B29K2995/0037Other properties
    • B29K2995/0056Biocompatible, e.g. biopolymers or bioelastomers

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (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)
  • Oil, Petroleum & Natural Gas (AREA)
  • Inorganic Chemistry (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Transplantation (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) US9918939B2 (ro)
EP (1) EP3027171B1 (ro)
JP (2) JP6153667B2 (ro)
KR (2) KR20170116203A (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
EA021293B1 (ru) 2008-12-08 2015-05-29 Джилид Коннектикут, Инк. ИМИДАЗОПИРАЗИНОВЫЕ ИНГИБИТОРЫ Syk, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ ИМИДАЗОПИРАЗИНОВЫЕ ИНГИБИТОРЫ Syk, И СПОСОБЫ ИХ ПРИМЕНЕНИЯ
PT2545052E (pt) 2010-03-11 2015-02-18 Gilead Connecticut Inc Inibidores da syk à base de imidazopiridinas
MD4684B1 (ro) 2013-07-30 2020-03-31 Gilead Connecticut INc. Formulări pe bază de imidazopirazine în calitate de inhibitori SYK
ES2822285T3 (es) * 2013-07-30 2021-04-30 Kronos Bio Inc Polimorfo de inhibidores de SYK
EP3076976B1 (en) 2013-12-04 2020-09-02 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
AU2015290000B2 (en) 2014-07-14 2018-05-17 Gilead Sciences, Inc. Combinations 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
HK1244453A1 (zh) 2015-04-21 2018-08-10 吉利德科学公司 使用syk抑制剂对慢性移植物抗宿主病的治疗
EP3881833B1 (en) 2015-06-30 2023-11-01 Genentech, Inc. Immediate-release tablets containing a drug and processes for forming the tablets
US10472369B2 (en) * 2016-02-26 2019-11-12 Crystal Pharmatech Co., Ltd. Crystalline forms of (6-(1H-indazol-6-yl)-N-[4-(4-(4-morpholinyl)phenyl]imidazo[1,2-A]pyrazin-8-amine) methanesulfonate
TW201822764A (zh) 2016-09-14 2018-07-01 美商基利科學股份有限公司 Syk抑制劑
CA3036384A1 (en) 2016-09-14 2018-03-22 Gilead Sciences, Inc. Syk inhibitors
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
US11384082B2 (en) 2017-08-25 2022-07-12 Kronos Bio, Inc. Hydrates of polymorphs of 6-(1H-indazol-6-YL)-N-(4-morpholinophenyl)-2,3-dihydroimidazo[1,2-A]pyrazin-8-amine bisemsylate as Syk inhibitors
US11040975B2 (en) 2017-12-08 2021-06-22 Merck Sharp & Dohme Corp. Carbocyclic nucleoside reverse transcriptase inhibitors
US11339168B2 (en) 2019-02-22 2022-05-24 Kronos Bio, Inc. Crystalline forms of 6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine 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
DE4337611A1 (de) 1993-11-04 1995-05-11 Boehringer Ingelheim Kg Neue Benzoylguanidine, ihre Herstellung und ihre Verwendung in Arzneimitteln
DE4337609A1 (de) 1993-11-04 1995-05-11 Boehringer Ingelheim Kg Neue Pyrazincarboxamidderivate, 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.
US6334997B1 (en) 1994-03-25 2002-01-01 Isotechnika, Inc. Method of using deuterated calcium channel blockers
ES2293638T3 (es) 1994-03-25 2008-03-16 Isotechnika, Inc. Mejora de la eficacia de farmacos por deuteracion.
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
JPH11505524A (ja) 1995-05-01 1999-05-21 藤沢薬品工業株式会社 イミダゾ1,2−aピリジンおよびイミダゾ1,2−aピリデジン誘導体、および骨吸収阻害剤としてのその用途
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
EP1175205B1 (en) * 1999-11-12 2006-06-14 Abbott Laboratories Solid dispersion comprising ritonavir, fenofibrate or griseofulvin
BR0016555A (pt) * 1999-12-23 2002-09-17 Pfizer Prod Inc Composições farmacêuticas que proporcionam concentrações acrescidas de droga
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
JP2004528295A (ja) 2001-01-30 2004-09-16 サイトピア ピーティワイ リミテッド キナーゼ阻害方法
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
WO2003070732A1 (en) 2002-02-19 2003-08-28 Pharmacia & Upjohn Company Fused bicyclic-n-bridged-heteroaromatic carboxamides for the treatment of disease
JP2005530739A (ja) 2002-04-19 2005-10-13 セルラー ジェノミクス,インコーポレーテッド イミダゾ[1,2−a]ピラジン−8−イルアミン、生成方法、および使用方法
JP4464814B2 (ja) 2002-05-14 2010-05-19 アバーント・ファーマシューティカルズ・(インディア)・リミテッド アントラニル酸誘導体の水和物の製造方法
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
ATE378336T1 (de) 2002-09-19 2007-11-15 Schering Corp Imidazopyridine als hemmstoffe cyclin abhängiger kinasen
KR20060010709A (ko) 2002-09-23 2006-02-02 쉐링 코포레이션 사이클린 의존성 키나제 억제제로서의 신규한 이미다조피라진
JP4799864B2 (ja) 2002-09-23 2011-10-26 シェーリング コーポレイション サイクリン依存性キナーゼインヒビターとしてのイミダゾピラジン
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
US7157460B2 (en) 2003-02-20 2007-01-02 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
US7186832B2 (en) 2003-02-20 2007-03-06 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
US7405295B2 (en) 2003-06-04 2008-07-29 Cgi Pharmaceuticals, Inc. Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds
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
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
WO2005019220A2 (en) 2003-08-11 2005-03-03 Cellular Genomics Inc. Substituted imidazo[1,2-a]pyrazines as modulators of kinase activity
US20050288295A1 (en) 2003-11-11 2005-12-29 Currie Kevin S Certain imidazo[1,2-a]pyrazin-8-ylamines, method of making, and method of use thereof
WO2005085252A1 (en) 2004-03-04 2005-09-15 Biofocus Discovery Limited Imidazo ‘1,2-a’ pyrazine compounds which interact with protein kinases
US8039009B2 (en) * 2004-06-17 2011-10-18 Forest Laboratories Holdings Limited Modified release formulations of memantine oral dosage forms
US7713973B2 (en) 2004-10-15 2010-05-11 Takeda Pharmaceutical Company Limited Kinase inhibitors
EP1812442A2 (en) 2004-11-10 2007-08-01 CGI Pharmaceuticals, Inc. Imidazo[1,2-a]pyrazin-8-ylamines useful as modulators of kinase activity
WO2007058942A2 (en) 2005-11-10 2007-05-24 Schering Corporation Imidazopyrazines as protein kinase inhibitors
SG174086A1 (en) 2006-08-30 2011-09-29 Cellzome Ltd Triazole derivatives as kinase inhibitors
AR063706A1 (es) 2006-09-11 2009-02-11 Cgi Pharmaceuticals Inc Determinadas amidas 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.
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
JP5643105B2 (ja) 2007-12-14 2014-12-17 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft 新規イミダゾ[1,2−a]ピリジン及びイミダゾ[1,2−b]ピリダジン誘導体
EP2252617A1 (en) 2008-02-13 2010-11-24 CGI Pharmaceuticals, Inc. 6-aryl-imidaz0[l, 2-a]pyrazine derivatives, method of making, and method of use thereof
BRPI0909818A2 (pt) 2008-03-07 2015-10-06 Pfizer métodos, formas de dosagem e conjunto para administrar ziprasidona sem alimentos
WO2009156284A1 (en) 2008-06-24 2009-12-30 F. Hoffmann-La Roche Ag Novel substituted pyridin-2-ones and pyridazin-3-ones
AU2009265813B2 (en) 2008-07-02 2014-04-10 F. Hoffmann-La Roche Ag Novel phenylpyrazinones as kinase inhibitors
EP2307413B1 (en) 2008-07-15 2015-09-09 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
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
SG171991A1 (en) * 2008-12-08 2011-07-28 Gilead Connecticut Inc Imidazopyrazine syk inhibitors
EA021293B1 (ru) * 2008-12-08 2015-05-29 Джилид Коннектикут, Инк. ИМИДАЗОПИРАЗИНОВЫЕ ИНГИБИТОРЫ Syk, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ ИМИДАЗОПИРАЗИНОВЫЕ ИНГИБИТОРЫ Syk, И СПОСОБЫ ИХ ПРИМЕНЕНИЯ
EP2512455B8 (en) 2009-12-18 2014-07-23 FrieslandCampina Nederland Holding B.V. Co-processed tablet excipient composition its preparation and use
PT2545052E (pt) 2010-03-11 2015-02-18 Gilead Connecticut Inc Inibidores da syk à base de imidazopiridinas
WO2013188856A1 (en) 2012-06-14 2013-12-19 Gilead Connecticut, Inc. Imidazopyrazine syk inhibitors
EP2884980A1 (en) * 2012-08-14 2015-06-24 Gilead Calistoga LLC Combination therapies for treating cancer
US20140148430A1 (en) 2012-11-26 2014-05-29 Gilead Connecticut, Inc. Imidazopyridines syk inhibitors
ES2822285T3 (es) * 2013-07-30 2021-04-30 Kronos Bio Inc Polimorfo de inhibidores de SYK
MD4684B1 (ro) * 2013-07-30 2020-03-31 Gilead Connecticut INc. Formulări pe bază de imidazopirazine în calitate de inhibitori SYK
EP3027601B1 (en) 2013-07-31 2017-10-25 Gilead Sciences, Inc. Syk inhibitors
EP3076976B1 (en) 2013-12-04 2020-09-02 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
TR201906413T4 (tr) * 2013-12-23 2019-05-21 Gilead Sciences Inc Bir makrosiklik hcv ns3 inhibe edici tripeptidin sentezi.

Also Published As

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

Similar Documents

Publication Publication Date Title
MD4684B1 (ro) Formulări pe bază de imidazopirazine în calitate de inhibitori SYK
CY1123059T1 (el) Αναστολη του διαυλου ιοντων παροδικου δυναμικου του υποδοχεα α1
PH12017502141A1 (en) Compounds and their methods of use
MX377916B (es) Compuestos 4-amino-imidazoquinolina.
PH12018500065A1 (en) Oxysterols and methods of use thereof
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
MX374513B (es) Compuestos de morfolinona de ácido heteroarilo como inhibidores mdm2 para el tratamiento de cáncer.
MX2016017147A (es) Compuestos de indazole substituidos como inhibidores de irak4.
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
JO3148B1 (ar) مركب مثبط لإشارات مسار notch
PH12016501462A1 (en) Neprilysin inhibitors
EA201790276A1 (ru) Новые имидазопиридазиновые соединения и их применение
EA201600434A1 (ru) Применение производных бензимидазолпролина
MX2016003522A (es) Derivados de quinazolinas y su uso como inhibidores de la adn metiltransferasa.
MX2015010619A (es) Cis-morfolinona y otros compuestos como inhibidores de mdm2 para el tratamiento del cancer.

Legal Events

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