MD4684B1 - Formulări pe bază de imidazopirazine în calitate de inhibitori SYK - Google Patents
Formulări pe bază de imidazopirazine în calitate de inhibitori SYK Download PDFInfo
- 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
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)
- 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.
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)
| 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)
| 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. |
-
2014
- 2014-07-29 MD MDA20160012A patent/MD4684B1/ro not_active IP Right Cessation
- 2014-07-29 HK HK16110531.7A patent/HK1222329A1/zh unknown
- 2014-07-29 AP AP2016009007A patent/AP2016009007A0/xx unknown
- 2014-07-29 CA CA2919522A patent/CA2919522C/en not_active Expired - Fee Related
- 2014-07-29 PL PL14752967T patent/PL3027171T3/pl unknown
- 2014-07-29 KR KR1020177027419A patent/KR20170116203A/ko not_active Withdrawn
- 2014-07-29 TW TW103125871A patent/TW201601728A/zh unknown
- 2014-07-29 NZ NZ715745A patent/NZ715745A/en not_active IP Right Cessation
- 2014-07-29 JP JP2016531839A patent/JP6153667B2/ja not_active Expired - Fee Related
- 2014-07-29 PT PT147529671T patent/PT3027171T/pt unknown
- 2014-07-29 BR BR112016001678A patent/BR112016001678A2/pt not_active IP Right Cessation
- 2014-07-29 SI SI201431583T patent/SI3027171T1/sl unknown
- 2014-07-29 SG SG11201600378SA patent/SG11201600378SA/en unknown
- 2014-07-29 ES ES14752967T patent/ES2795973T3/es active Active
- 2014-07-29 AU AU2014296314A patent/AU2014296314B2/en not_active Ceased
- 2014-07-29 CN CN201480043494.XA patent/CN105431137A/zh active Pending
- 2014-07-29 UA UAA201600654A patent/UA115815C2/uk unknown
- 2014-07-29 PE PE2016000198A patent/PE20160605A1/es unknown
- 2014-07-29 EP EP14752967.1A patent/EP3027171B1/en active Active
- 2014-07-29 MX MX2016001480A patent/MX2016001480A/es unknown
- 2014-07-29 WO PCT/US2014/048741 patent/WO2015017466A1/en not_active Ceased
- 2014-07-29 EA EA201690127A patent/EA201690127A1/ru unknown
- 2014-07-29 US US14/906,248 patent/US9918939B2/en active Active
- 2014-07-29 KR KR1020167004789A patent/KR20160036590A/ko not_active Abandoned
- 2014-07-29 US US14/445,970 patent/US9382256B2/en active Active
- 2014-07-30 AR ARP140102858A patent/AR097159A1/es unknown
- 2014-07-30 PY PY201401432623A patent/PY1432623A/es unknown
- 2014-07-30 UY UY35684A patent/UY35684A/es not_active Application Discontinuation
-
2016
- 2016-01-12 IL IL243577A patent/IL243577A0/en unknown
- 2016-01-25 PH PH12016500170A patent/PH12016500170A1/en unknown
- 2016-01-29 CL CL2016000241A patent/CL2016000241A1/es unknown
- 2016-02-29 CR CR20160099A patent/CR20160099A/es unknown
- 2016-06-09 US US15/178,164 patent/US9949932B2/en active Active
-
2017
- 2017-05-30 JP JP2017106578A patent/JP6530444B2/ja active Active
Also Published As
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) |