HRP20161036T1 - IMIDAZOPIRAZIN Syk INHIBITORI - Google Patents
IMIDAZOPIRAZIN Syk INHIBITORI Download PDFInfo
- Publication number
- HRP20161036T1 HRP20161036T1 HRP20161036TT HRP20161036T HRP20161036T1 HR P20161036 T1 HRP20161036 T1 HR P20161036T1 HR P20161036T T HRP20161036T T HR P20161036TT HR P20161036 T HRP20161036 T HR P20161036T HR P20161036 T1 HRP20161036 T1 HR P20161036T1
- Authority
- HR
- Croatia
- Prior art keywords
- pharmaceutically acceptable
- compound
- acceptable salt
- leukemia
- lymphoma
- Prior art date
Links
- ZKAMEFMDQNTDFK-UHFFFAOYSA-N 1h-imidazo[4,5-b]pyrazine Chemical compound C1=CN=C2NC=NC2=N1 ZKAMEFMDQNTDFK-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 19
- 150000003839 salts Chemical class 0.000 claims 19
- 206010028980 Neoplasm Diseases 0.000 claims 7
- 201000011510 cancer Diseases 0.000 claims 7
- 238000000034 method Methods 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 230000000694 effects Effects 0.000 claims 5
- 210000004027 cell Anatomy 0.000 claims 4
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 4
- 238000000338 in vitro Methods 0.000 claims 4
- 208000032839 leukemia Diseases 0.000 claims 4
- 208000003950 B-cell lymphoma Diseases 0.000 claims 3
- 206010025323 Lymphomas Diseases 0.000 claims 3
- 239000013543 active substance Substances 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 2
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- 208000017604 Hodgkin disease Diseases 0.000 claims 2
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 2
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 2
- 206010021245 Idiopathic thrombocytopenic purpura Diseases 0.000 claims 2
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 2
- 208000034578 Multiple myelomas Diseases 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 2
- 208000031981 Thrombocytopenic Idiopathic Purpura Diseases 0.000 claims 2
- 230000000172 allergic effect Effects 0.000 claims 2
- 208000010668 atopic eczema Diseases 0.000 claims 2
- 208000037979 autoimmune inflammatory disease Diseases 0.000 claims 2
- 201000003710 autoimmune thrombocytopenic purpura Diseases 0.000 claims 2
- 210000003719 b-lymphocyte Anatomy 0.000 claims 2
- 238000002512 chemotherapy Methods 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 230000007062 hydrolysis Effects 0.000 claims 2
- 238000006460 hydrolysis reaction Methods 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 101710181757 1,2-dihydroxy-3-keto-5-methylthiopentene dioxygenase Proteins 0.000 claims 1
- 101710094863 Acireductone dioxygenase Proteins 0.000 claims 1
- 208000004736 B-Cell Leukemia Diseases 0.000 claims 1
- 206010039085 Rhinitis allergic Diseases 0.000 claims 1
- 206010047112 Vasculitides Diseases 0.000 claims 1
- 206010047115 Vasculitis Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 claims 1
- 201000010105 allergic rhinitis Diseases 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 229940127089 cytotoxic agent Drugs 0.000 claims 1
- 238000001514 detection method Methods 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000009277 hairy cell leukemia Diseases 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 201000003068 rheumatic fever Diseases 0.000 claims 1
- 230000035945 sensitivity Effects 0.000 claims 1
Classifications
-
- 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
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- 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
- A61P11/16—Central respiratory analeptics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
- C12Q1/02—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving viable microorganisms
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
- C12Q1/48—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase
- C12Q1/485—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase involving kinase
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
- G01N33/573—Immunoassay; Biospecific binding assay; Materials therefor for enzymes or isoenzymes
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
- G01N2333/90—Enzymes; Proenzymes
- G01N2333/91—Transferases (2.)
- G01N2333/912—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
- G01N2333/91205—Phosphotransferases in general
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Molecular Biology (AREA)
- Zoology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Wood Science & Technology (AREA)
- Pulmonology (AREA)
- Biochemistry (AREA)
- Microbiology (AREA)
- Biotechnology (AREA)
- Physics & Mathematics (AREA)
- Analytical Chemistry (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- General Engineering & Computer Science (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Epidemiology (AREA)
- Cell Biology (AREA)
- Pathology (AREA)
- General Physics & Mathematics (AREA)
- Food Science & Technology (AREA)
- Rheumatology (AREA)
- Neurology (AREA)
- Physical Education & Sports Medicine (AREA)
Claims (17)
1. Spoj koji ima strukturu:
[image]
ili njegova farmaceutski prihvatljiva sol.
2. Farmaceutski pripravak naznačen time da sadrži:
spoj iz patentnog zahtjeva 1, ili njegovu farmaceutski prihvatljivu sol; i najmanje jedan farmaceutski prihvatljiv nosač, odabrano iz skupine koja se sastoji od nosača, adjuvanata, i ekscipijenata.
3. Spoj iz patentnog zahtjeva 1, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku liječenja osobe kojoj je to potrebno.
4. Spoj iz patentnog zahtjeva 1, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku liječenja osobe koja ima bolest koja reagira na inhibiciju Syk aktivnosti odabrano iz, liječenja karcinoma, uključujući B-stanični limfom i leukemiju, alergijske poremećaje, autoimune bolesti i inflamatorne bolesti kao što su: SLE, reumatični artritis, multiple vaskulitidi, idiopatska trombocitopenijska purpura (ITP), mijastenija gravis, alergijski rinitis, kronična opstruktivna bolest pluća ("COPD"), sindrom akutnog respiratornog poremećaja odraslih ("ARDs") i astma.
5. Spoj iz patentnog zahtjeva 1, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku liječenja osobe koja ima bolest izabranu iz grupe koja se sastoji od karcinoma, autoimune bolesti, inflamatorne bolesti, i alergijskog poremećaja.
6. Spoj iz patentnog zahtjeva 1, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku liječenja osobe koja ima karcinom.
7. Spoj iz patentnog zahtjeva 1, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku liječenja osobe koja ima limfom ili leukemiju.
8. Spoj iz patentnog zahtjeva 1, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku liječenja osobe koja ima bolest izabranu iz grupe koja se sastoji od B-ćelijskog limfoma, Hodgkin’sovog limfoma, ne-Hodgkin’sovog limfoma, leukemija "hairy" stanica (kronična limfoidna leukemija), multipli mijeloma, kronične mijeloidne leukemije, akutne mijeloidne leukemije, kronične limfocitne leukemije, i akutne limfocitne leukemije.
9. Spoj za upotrebu prema bilo kojem od patentnih zahtjeva od 3 do 8, ili njegova farmaceutski prihvatljiva sol, naznačen time da je dan osobi, u kombinaciji sa jednim ili više dodatnih aktivnih agenasa.
10. Spoj iz patentnog zahtjeva 1, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku liječenja karcinoma kod osobe kojoj je to potrebno, obuhvaća primjenu na ljude terapeutski efikasne količine spoja ili farmaceutski prihvatljive soli zajedno sa drugim aktivnim agensom korisnim u liječenju karcinoma.
11. Spoj za upotrebu prema patentnom zahtjevu 10, ili njegova farmaceutski prihvatljiva sol, naznačen time da se drugi aktivni agens primjenjuje prije, istovremeno, ili nakon tretmana sa spojem ili farmaceutski prihvatljivom soli.
12. Spoj za upotrebu prema patentnom zahtjevu 10 ili 11, ili njegova farmaceutski prihvatljiva sol, naznačen time da je karcinom limfom ili leukemija.
13. Spoj za upotrebu prema patentnom zahtjevu 12, ili njegova farmaceutski prihvatljiva sol, naznačen time da su limfom ili leukemija odabrani iz grupe koja se sastoji od B-ćelijskog limfoma, Hodgkin’sovog limfoma, ne-Hodgkin’sovog limfoma, leukemije "hairy" stanica (kronična limfoidna leukemija), multiple mijeloma, kronične mijeloidne leukemije, akutne mijeloidne leukemije, kronične limfocitne leukemije, i akutne limfocitne leukemije.
14. Spoj iz patentnog zahtjeva 1, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku povećanja osjetljivosti stanica karcinoma na kemoterapiju kod osobe koja je podvrgnuta kemoterapiji sa hemoterapeutskim agensom.
15. Postupak za utvrđivanje prisustva Syk-a u uzorku, naznačen time da sadrži kontakt uzorka sa spojem iz patentnog zahtjeva 1, ili njegovom farmaceutski prihvatljivom soli, pod uvjetima koji dozvoljavaju detekciju Syk aktivnosti, detektiranje nivoa Syk aktivnosti u uzorku, i iz toga utvrđivanje prisustva ili odsustva Syk-a u uzorku.
16. In vitro postupak za inhibiciju B-stanične aktivnosti naznačen time da obuhvaća kontakt stanica sa ekspresijom Syk sa Spojm iz patentnog zahtjeva 1, ili njegovim farmaceutski prihvatljivim solima, u količini dovoljnoj da detektirano umanji razinu B-stanične aktivnosti in vitro.
17. In vitro postupak za inhibiranje ATP hidrolize, naznačen time da postupak obuhvaća kontaktiranje stanica koje eksprimiraju Syk sa spojem iz patentnog zahtjeva 1, ili njegovim farmaceutski prihvatljivim solima, u količini dovoljnoj da detektirano umanji nivo ATP hidrolize in vitro.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US12058708P | 2008-12-08 | 2008-12-08 | |
| US14051408P | 2008-12-23 | 2008-12-23 | |
| US24097909P | 2009-09-09 | 2009-09-09 | |
| EP13005979.3A EP2716157B1 (en) | 2008-12-08 | 2009-12-07 | Imidazopyrazine Syk inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20161036T1 true HRP20161036T1 (hr) | 2017-06-16 |
Family
ID=42242994
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20161036TT HRP20161036T1 (hr) | 2008-12-08 | 2016-08-17 | IMIDAZOPIRAZIN Syk INHIBITORI |
Country Status (30)
| Country | Link |
|---|---|
| US (7) | US8455493B2 (hr) |
| EP (3) | EP2373169B1 (hr) |
| JP (4) | JP5567587B2 (hr) |
| KR (4) | KR101745732B1 (hr) |
| CN (2) | CN104744476B (hr) |
| AU (1) | AU2009325132B2 (hr) |
| BR (1) | BRPI0922225B1 (hr) |
| CA (1) | CA2746023C (hr) |
| CL (1) | CL2011001360A1 (hr) |
| CO (1) | CO6390078A2 (hr) |
| CY (1) | CY1118377T1 (hr) |
| DK (1) | DK2716157T3 (hr) |
| EA (3) | EA024140B1 (hr) |
| ES (2) | ES2590804T3 (hr) |
| HR (1) | HRP20161036T1 (hr) |
| HU (1) | HUE030427T2 (hr) |
| IL (3) | IL213365A (hr) |
| LT (1) | LT2716157T (hr) |
| MX (1) | MX2011006091A (hr) |
| NZ (1) | NZ593459A (hr) |
| PE (2) | PE20140975A1 (hr) |
| PL (2) | PL2373169T3 (hr) |
| PT (2) | PT2716157T (hr) |
| RS (1) | RS55055B1 (hr) |
| SG (1) | SG171991A1 (hr) |
| SI (2) | SI2373169T1 (hr) |
| SM (1) | SMT201600267B (hr) |
| TW (2) | TWI529172B (hr) |
| VN (1) | VN28228A1 (hr) |
| WO (1) | WO2010068257A1 (hr) |
Families Citing this family (66)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| KR101745732B1 (ko) | 2008-12-08 | 2017-06-12 | 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 |
| BRPI0922226A2 (pt) | 2008-12-08 | 2015-12-29 | Gilead Connecticut Inc | inibidores de syk imidazopirazina. |
| IN2012DN01961A (hr) * | 2009-08-17 | 2015-08-21 | Intellikine Llc | |
| AU2011226689B2 (en) * | 2010-03-11 | 2016-09-01 | Kronos Bio, Inc. | Imidazopyridines Syk inhibitors |
| US9127000B2 (en) | 2011-02-23 | 2015-09-08 | Intellikine, LLC. | Heterocyclic compounds and uses thereof |
| EP2706852B1 (en) | 2011-05-10 | 2018-08-22 | Merck Sharp & Dohme Corp. | Bipyridylaminopyridines as syk inhibitors |
| JP2014513687A (ja) | 2011-05-10 | 2014-06-05 | メルク・シャープ・アンド・ドーム・コーポレーション | Ｓｙｋ阻害薬としてのピリジルアミノピリジン |
| JP2014513686A (ja) | 2011-05-10 | 2014-06-05 | メルク・シャープ・アンド・ドーム・コーポレーション | Ｓｙｋ阻害薬としてのアミノピリミジン |
| WO2013052394A1 (en) | 2011-10-05 | 2013-04-11 | Merck Sharp & Dohme Corp. | 2-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors |
| WO2013052393A1 (en) | 2011-10-05 | 2013-04-11 | Merck Sharp & Dohme Corp. | 3-PYRIDYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS |
| WO2013052391A1 (en) | 2011-10-05 | 2013-04-11 | Merck Sharp & Dohme Corp. | PHENYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS |
| AR090650A1 (es) | 2012-04-12 | 2014-11-26 | Alcon Res Ltd | Tratamiento para respuestas inflamatorias inducidas por microbios en el ojo |
| US20130338142A1 (en) * | 2012-06-14 | 2013-12-19 | Gilead Connecticut, Inc. | Imidazopyrazine syk inhibitors |
| US9242984B2 (en) | 2012-06-20 | 2016-01-26 | Merck Sharp & Dohme Corp. | Pyrazolyl derivatives as Syk inhibitors |
| WO2013192128A1 (en) | 2012-06-20 | 2013-12-27 | Merck Sharp & Dohme Corp. | Imidazolyl analogs as syk inhibitors |
| EP2863915B1 (en) | 2012-06-22 | 2017-12-06 | Merck Sharp & Dohme Corp. | SUBSTITUTED DIAZINE AND TRIAZINE SPLEEN TYROSINE KINASE (Syk) INHIBITORS |
| EP2863916B1 (en) | 2012-06-22 | 2018-07-18 | Merck Sharp & Dohme Corp. | Substituted pyridine spleen tyrosine kinase (syk) inhibitors |
| AU2013302617A1 (en) * | 2012-08-14 | 2015-02-05 | Gilead Calistoga Llc | Combination therapies for treating cancer |
| WO2014031438A2 (en) | 2012-08-20 | 2014-02-27 | Merck Sharp & Dohme Corp. | SUBSTITUTED PHENYL SPLEEN TYROSINE KINASE (Syk) INHIBITORS |
| WO2014048065A1 (en) | 2012-09-28 | 2014-04-03 | Merck Sharp & Dohme Corp. | Triazolyl derivatives as syk inhibitors |
| EP2931281B1 (en) | 2012-12-12 | 2018-01-17 | Merck Sharp & Dohme Corp. | Amino-pyrimidine-containing spleen tyrosine kinase inhibitors |
| EP2934525B1 (en) | 2012-12-21 | 2019-05-08 | Merck Sharp & Dohme Corp. | Thiazole-substituted aminopyridines as spleen tyrosine kinase inhibitors |
| EP2988744A4 (en) | 2013-04-26 | 2016-11-02 | Merck Sharp & Dohme | THIAZOLSUBSTITUTED AMINOHETEROARYLE AS MILZTYROSINKINASE INHIBITOR |
| WO2014176216A1 (en) | 2013-04-26 | 2014-10-30 | Merck Sharp & Dohme Corp. | Thiazole-substituted aminopyrimidines as spleen tyrosine kinase inhibitors |
| WO2015017460A1 (en) | 2013-07-30 | 2015-02-05 | Gilead Connecticut, Inc. | Polymorph of syk inhibitors |
| EP3027171B1 (en) * | 2013-07-30 | 2020-03-25 | Gilead Connecticut, Inc. | Formulation of syk inhibitors |
| ES2656192T3 (es) | 2013-07-31 | 2018-02-26 | Gilead Sciences, Inc. | Inhibidores de SKY |
| MX2016007311A (es) | 2013-12-04 | 2016-09-07 | Gilead Sciences Inc | Metodos para tratar canceres. |
| US9670196B2 (en) | 2013-12-20 | 2017-06-06 | Merck Sharp & Dohme Corp. | Thiazole-substituted aminoheteroaryls as Spleen Tyrosine Kinase inhibitors |
| WO2015094997A1 (en) | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors |
| EP3083559B1 (en) | 2013-12-20 | 2021-03-10 | Merck Sharp & Dohme Corp. | Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors |
| US9290505B2 (en) | 2013-12-23 | 2016-03-22 | Gilead Sciences, Inc. | Substituted imidazo[1,2-a]pyrazines as Syk inhibitors |
| UY35898A (es) * | 2013-12-23 | 2015-07-31 | Gilead Sciences Inc | ?compuestos inhibidores de syk y composiciones que los comprenden?. |
| WO2015138273A1 (en) | 2014-03-13 | 2015-09-17 | Merck Sharp & Dohme Corp. | 2-pyrazine carboxamides as spleen tyrosine kinase inhibitors |
| EP3152214B1 (en) | 2014-06-04 | 2020-01-29 | Merck Sharp & Dohme Corp. | Imidazo-pyrazine derivatives useful as soluble guanylate cyclase activators |
| TW201617074A (zh) | 2014-07-14 | 2016-05-16 | 吉李德科學股份有限公司 | Ｓｙｋ（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 |
| MX2017013496A (es) * | 2015-04-21 | 2018-02-09 | Gilead Sciences Inc | Tratamiento de enfermedad cronica de injerto contra hospedero con inhibidores de tirosina cinasa de bazo (syk). |
| RU2017139771A (ru) * | 2015-05-12 | 2019-06-13 | Зено Роялтис Энд Майлстоунс, Ллс | Бициклические соединения |
| WO2016197987A1 (zh) * | 2015-06-12 | 2016-12-15 | 杭州英创医药科技有限公司 | 作为Syk抑制剂和/或Syk-HDAC双重抑制剂的杂环化合物 |
| WO2017106564A1 (en) | 2015-12-17 | 2017-06-22 | Gilead Sciences, Inc. | Combination of a jak inhibitor and a syk inhibitor for treating cancers and inflammatory disorders |
| US20190160035A1 (en) * | 2016-07-28 | 2019-05-30 | Qbiotics Limited | Method of treatment |
| CA3036384A1 (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 |
| WO2018108083A1 (zh) * | 2016-12-12 | 2018-06-21 | 杭州英创医药科技有限公司 | 作为Syk抑制剂和/或Syk-HDAC双重抑制剂的杂环化合物 |
| WO2018195471A1 (en) | 2017-04-21 | 2018-10-25 | Gilead Sciences, Inc. | Syk inhibitors in combination with hypomethylating agents |
| US20200172529A1 (en) * | 2017-08-18 | 2020-06-04 | Beijing Hanmi Pharm. Co., Ltd. | Chemical Compound, Pharmaceutical Composition Thereof, and Use and Application Thereof |
| 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 |
| CA3079292A1 (en) | 2017-10-19 | 2019-04-25 | Bayer Animal Health Gmbh | Use of fused heteroaromatic pyrrolidones for treatment and prevention of diseases in animals |
| CN109879878A (zh) * | 2017-12-06 | 2019-06-14 | 朱允涛 | 一种氘代的咪唑并吡嗪类脾酪氨酸激酶（Syk）抑制剂 |
| US12012394B2 (en) | 2018-02-19 | 2024-06-18 | Washington University | Alpha-synuclein ligands |
| CA3102279A1 (en) | 2018-06-01 | 2019-12-05 | Cornell University | Combination therapy for pi3k-associated disease or disorder |
| CN113950479A (zh) | 2019-02-22 | 2022-01-18 | 克洛诺斯生物股份有限公司 | 作为syk抑制剂的缩合吡嗪的固体形式 |
| AU2020242287A1 (en) | 2019-03-21 | 2021-09-02 | INSERM (Institut National de la Santé et de la Recherche Médicale) | A Dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| EP4157848A4 (en) * | 2020-06-01 | 2024-07-17 | Nanjing Ruijie Pharma Co., Ltd. | COMPOUNDS AND THEIR USES AS SPLEEN TYROSINE KINASE INHIBITORS |
| WO2022064459A1 (en) | 2020-09-28 | 2022-03-31 | 1ST Biotherapeutics, Inc. | Indazoles as hematopoietic progenitor kinase 1 (hpk1) inhibitors and methods of using same |
| KR102560178B1 (ko) * | 2021-02-10 | 2023-07-27 | 재단법인 대구경북첨단의료산업진흥재단 | 이미다조[1,5-a]피라진 유도체 화합물 및 이를 유효성분으로 함유하는 암 또는 자가면역질환의 예방 또는 치료용 약학적 조성물 |
| CN113480543B (zh) * | 2021-07-07 | 2022-05-17 | 无锡市第二人民医院 | 2,6,8-多取代咪唑并[1,2-a]吡嗪及其合成方法和应用 |
| IL315365A (en) * | 2022-03-14 | 2024-11-01 | Purdue Research Foundation | Spleen tyrosine kinase inhibitor, composition and methods of use |
| KR20250037566A (ko) * | 2022-07-25 | 2025-03-17 | 셀진 코포레이션 | Irak3 결합제로서의 치환된 이미다조피라진 화합물 |
| WO2024102970A1 (en) * | 2022-11-11 | 2024-05-16 | Kronos Bio, Inc. | Compounds for modulating syk activity and e3 ubiquitin ligase activity |
Family Cites Families (76)
| 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. |
| US6334997B1 (en) * | 1994-03-25 | 2002-01-01 | Isotechnika, Inc. | Method of using deuterated calcium channel blockers |
| KR100477070B1 (ko) * | 1994-03-25 | 2006-04-21 | 이소테크니카 인코포레이티드 | 중수소화작용에의한의약품의효능강화법 |
| 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 |
| US6249495B1 (en) | 1997-02-27 | 2001-06-19 | Matsushita Electric Industrial Co., Ltd. | Stepping motor control method and disk drive apparatus |
| 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 |
| 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 |
| WO2001098685A1 (en) | 2000-06-19 | 2001-12-27 | Tay Armin S | Axial position changing transmission mechanism |
| 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 |
| WO2002101221A2 (en) | 2000-11-20 | 2002-12-19 | Cryoco, Inc. | A method and apparatus for the preparation and usage of a cryogenic propellant or explosive system |
| DK174233B1 (da) | 2000-12-27 | 2002-10-07 | Dss Danish Separation Systems | Sanitært spiralfilteranlæg |
| 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 |
| US7003125B2 (en) | 2001-09-12 | 2006-02-21 | Seung-Hwan Yi | Micromachined piezoelectric microspeaker and fabricating method thereof |
| CA2476681A1 (en) | 2002-02-19 | 2003-08-28 | Bruce N. Rogers | Fused bicyclic-n-bridged-heteroaromatic carboxamides for the treatment of disease |
| KR20050008691A (ko) * | 2002-04-19 | 2005-01-21 | 셀룰러 지노믹스 아이엔씨 | 이미다조[1,2-ａ]피라진-8-일 아민, 그의 제조방법 및사용방법 |
| US20040072081A1 (en) | 2002-05-14 | 2004-04-15 | Coleman Thomas P. | Methods for etching photolithographic reticles |
| US7288075B2 (en) | 2002-06-27 | 2007-10-30 | Ethicon, Inc. | Methods and devices utilizing rheological materials |
| JP2004053714A (ja) | 2002-07-17 | 2004-02-19 | Fuji Xerox Co Ltd | 画像定着装置及び画像定着方法 |
| US6761361B2 (en) | 2002-08-09 | 2004-07-13 | Credo Technology Corporation | Drill and drive apparatus with improved tool holder |
| US20040026867A1 (en) | 2002-08-09 | 2004-02-12 | Adams David J. | Bearing seal |
| US7312341B2 (en) * | 2002-09-09 | 2007-12-25 | Cgi Pharmaceuticals, Inc. | 6-aryl-imidazo[1,2-a] pyrazin-8-ylamines, method of making, and method of use thereof |
| AR041291A1 (es) | 2002-09-19 | 2005-05-11 | Schering Corp | Imidazopiridinas como inhibidores de quinasa dependientes de ciclina |
| CN1694886A (zh) | 2002-09-23 | 2005-11-09 | 先灵公司 | 作为周期素依赖性激酶抑制剂的咪唑并吡嗪 |
| AU2003275031B2 (en) * | 2002-09-23 | 2006-08-17 | Schering Corporation | Novel imidazopyrazines as cyclin dependent kinase inhibitors |
| JP4056346B2 (ja) | 2002-09-30 | 2008-03-05 | 三洋電機株式会社 | 非水電解質二次電池 |
| MXPA05004580A (es) | 2002-10-29 | 2005-07-26 | Transave Inc | Liberacion sostenida de anti - infecciosos. |
| WO2004072081A1 (en) | 2003-02-10 | 2004-08-26 | Cellular Genomics, Inc. | Certain 8-heteroaryl-6-phenyl-imidazo[1,2-a]pyrazines as modulators of kinase activity |
| AR043002A1 (es) * | 2003-02-18 | 2005-07-13 | Altana Pharma Ag | Imidazopirazinas 6-substituidos |
| 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 |
| US7456393B2 (en) | 2003-04-10 | 2008-11-25 | Ge Homeland Protection, Inc. | Device for testing surfaces of articles for traces of explosives and/or drugs |
| 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 |
| WO2005019220A2 (en) | 2003-08-11 | 2005-03-03 | Cellular Genomics Inc. | Substituted imidazo[1,2-a]pyrazines as modulators of kinase activity |
| US7236749B2 (en) | 2003-10-15 | 2007-06-26 | Honeywell International Inc. | Stuck microphone deselection system and method |
| 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 |
| JP2006099930A (ja) | 2004-09-01 | 2006-04-13 | Tdk Corp | 情報記録媒体、記録再生装置およびスタンパー |
| US8145601B2 (en) | 2004-09-09 | 2012-03-27 | Microsoft Corporation | Method, system, and apparatus for providing resilient data transfer in a data protection system |
| EP1812439B2 (en) * | 2004-10-15 | 2017-12-06 | 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 |
| CN101124227A (zh) * | 2004-11-10 | 2008-02-13 | Cgi制药有限公司 | 可用作激酶活性调节剂的咪唑并[1,2-a]吡嗪-8-基胺 |
| JP4883959B2 (ja) | 2005-08-17 | 2012-02-22 | Ｎｔｎ株式会社 | 回転検出装置および回転検出装置付き軸受 |
| GB0520838D0 (en) * | 2005-10-13 | 2005-11-23 | Glaxo Group Ltd | Novel compounds |
| AR056785A1 (es) * | 2005-11-10 | 2007-10-24 | Schering Corp | COMPUESTOS DE IMIDAZO[1,2-A]PIRAZINAS, uTILES COMO INHIBIDORES, REGULADORES O MODULADORES DE PROTEINQUINASAS |
| JP4837378B2 (ja) | 2006-01-04 | 2011-12-14 | 株式会社日立製作所 | データの改竄を防止する記憶装置 |
| US7446352B2 (en) | 2006-03-09 | 2008-11-04 | Tela Innovations, Inc. | Dynamic array architecture |
| DE102006032495A1 (de) | 2006-07-13 | 2008-02-07 | Nokia Siemens Networks Gmbh & Co.Kg | Verfahren und Vorrichtung zur Vermeidung von Interferenzen in einem zellulären Funkkommunikationssystem |
| US20080025821A1 (en) | 2006-07-25 | 2008-01-31 | Applied Materials, Inc. | Octagon transfer chamber |
| SG174086A1 (en) | 2006-08-30 | 2011-09-29 | Cellzome Ltd | Triazole derivatives as kinase inhibitors |
| ES2307402B1 (es) | 2006-10-30 | 2009-09-30 | Archivel Farma, S.L. | Vacuna profilactica contra la tuberculosis. |
| WO2008138843A1 (en) * | 2007-05-10 | 2008-11-20 | Galapagos N.V. | Imidazopyridines and triazolopyrimidines useful for the treatment of joint degenerative & inflammatory diseases |
| CA2708361C (en) | 2007-12-14 | 2016-06-07 | F. Hoffmann-La Roche Ag | Novel imidazo[1,2-a]pyridine and imidazo[1,2-b]pyridazine derivatives |
| 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 |
| US8426424B2 (en) * | 2008-05-06 | 2013-04-23 | Cgi Pharmaceuticals, Inc. | Certain substituted amides, method of making, and method of use thereof |
| CN102066370B (zh) | 2008-07-15 | 2014-05-14 | 霍夫曼-拉罗奇有限公司 | 苯基-咪唑并吡啶类和哒嗪类 |
| 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 |
| KR101745732B1 (ko) | 2008-12-08 | 2017-06-12 | 질레드 코네티컷 인코포레이티드 | 이미다조피라진 ｓｙｋ 억제제 |
| BRPI0922226A2 (pt) | 2008-12-08 | 2015-12-29 | Gilead Connecticut Inc | inibidores de syk imidazopirazina. |
| US20110112995A1 (en) | 2009-10-28 | 2011-05-12 | Industrial Technology Research Institute | Systems and methods for organizing collective social intelligence information using an organic object data model |
| AU2011226689B2 (en) | 2010-03-11 | 2016-09-01 | Kronos Bio, Inc. | Imidazopyridines Syk inhibitors |
| JP5554746B2 (ja) | 2011-05-06 | 2014-07-23 | 株式会社日立製作所 | ガス絶縁母線及びガス絶縁母線の異物除去方法 |
| US20140148430A1 (en) | 2012-11-26 | 2014-05-29 | Gilead Connecticut, Inc. | Imidazopyridines syk inhibitors |
-
2009
- 2009-12-07 KR KR1020117015724A patent/KR101745732B1/ko active Active
- 2009-12-07 BR BRPI0922225-1A patent/BRPI0922225B1/pt not_active IP Right Cessation
- 2009-12-07 HU HUE13005979A patent/HUE030427T2/en unknown
- 2009-12-07 MX MX2011006091A patent/MX2011006091A/es active IP Right Grant
- 2009-12-07 AU AU2009325132A patent/AU2009325132B2/en active Active
- 2009-12-07 KR KR1020177002329A patent/KR20170013414A/ko not_active Ceased
- 2009-12-07 TW TW103135973A patent/TWI529172B/zh active
- 2009-12-07 EA EA201400197A patent/EA024140B1/ru active IP Right Revival
- 2009-12-07 NZ NZ593459A patent/NZ593459A/xx not_active IP Right Cessation
- 2009-12-07 CN CN201510093652.9A patent/CN104744476B/zh active Active
- 2009-12-07 EP EP20090832228 patent/EP2373169B1/en active Active
- 2009-12-07 EP EP13005979.3A patent/EP2716157B1/en active Active
- 2009-12-07 WO PCT/US2009/006445 patent/WO2010068257A1/en active Application Filing
- 2009-12-07 SI SI200931249T patent/SI2373169T1/sl unknown
- 2009-12-07 TW TW098141713A patent/TWI478922B/zh active
- 2009-12-07 JP JP2011539524A patent/JP5567587B2/ja active Active
- 2009-12-07 PL PL09832228T patent/PL2373169T3/pl unknown
- 2009-12-07 LT LTEP13005979.3T patent/LT2716157T/lt unknown
- 2009-12-07 SG SG2011041241A patent/SG171991A1/en unknown
- 2009-12-07 EA EA201690111A patent/EA201690111A1/ru unknown
- 2009-12-07 DK DK13005979.3T patent/DK2716157T3/en active
- 2009-12-07 VN VN201101623A patent/VN28228A1/vi unknown
- 2009-12-07 PL PL13005979T patent/PL2716157T3/pl unknown
- 2009-12-07 RS RS20160667A patent/RS55055B1/sr unknown
- 2009-12-07 ES ES13005979.3T patent/ES2590804T3/es active Active
- 2009-12-07 CA CA2746023A patent/CA2746023C/en not_active Expired - Fee Related
- 2009-12-07 PT PT130059793T patent/PT2716157T/pt unknown
- 2009-12-07 PT PT98322282T patent/PT2373169E/pt unknown
- 2009-12-07 EP EP16164453.9A patent/EP3123864A1/en not_active Withdrawn
- 2009-12-07 SI SI200931503A patent/SI2716157T1/sl unknown
- 2009-12-07 KR KR1020177014984A patent/KR20170066685A/ko not_active Ceased
- 2009-12-07 US US12/632,140 patent/US8455493B2/en active Active
- 2009-12-07 ES ES09832228.2T patent/ES2545610T3/es active Active
- 2009-12-07 PE PE2014000121A patent/PE20140975A1/es active IP Right Grant
- 2009-12-07 CN CN200980156331.1A patent/CN102307474B/zh active Active
- 2009-12-07 KR KR1020147035525A patent/KR101748925B1/ko active Active
- 2009-12-07 EA EA201190042A patent/EA020461B1/ru active IP Right Revival
- 2009-12-07 PE PE2011001178A patent/PE20120058A1/es active IP Right Grant
-
2011
- 2011-06-05 IL IL213365A patent/IL213365A/en not_active IP Right Cessation
- 2011-06-07 CL CL2011001360A patent/CL2011001360A1/es unknown
- 2011-06-21 CO CO11077863A patent/CO6390078A2/es active IP Right Grant
-
2013
- 2013-04-23 US US13/868,967 patent/US8765761B2/en active Active
- 2013-04-23 US US13/868,971 patent/US8748607B2/en active Active
-
2014
- 2014-05-07 JP JP2014095907A patent/JP5832586B2/ja active Active
- 2014-05-09 US US14/274,618 patent/US9120811B2/en active Active
- 2014-06-09 US US14/300,189 patent/US9212191B2/en active Active
- 2014-08-27 IL IL234326A patent/IL234326A/en not_active IP Right Cessation
- 2014-11-23 IL IL235837A patent/IL235837A0/en unknown
-
2015
- 2015-08-12 JP JP2015159313A patent/JP6132445B2/ja active Active
- 2015-10-13 US US14/882,278 patent/US9796718B2/en active Active
-
2016
- 2016-08-05 SM SM201600267T patent/SMT201600267B/it unknown
- 2016-08-17 HR HRP20161036TT patent/HRP20161036T1/hr unknown
- 2016-08-18 CY CY20161100814T patent/CY1118377T1/el unknown
-
2017
- 2017-03-13 JP JP2017047354A patent/JP2017101090A/ja not_active Withdrawn
- 2017-09-28 US US15/719,399 patent/US20180086769A1/en not_active Abandoned
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| HRP20161036T1 (hr) | IMIDAZOPIRAZIN Syk INHIBITORI | |
| Kyriakopoulos et al. | Identification and treatment of T2-low asthma in the era of biologics | |
| KR102568333B1 (ko) | Jak 저해제 화합물을 사용하는 치료 방법 | |
| Zhang et al. | NHBA isolated from Gastrodia elata exerts sedative and hypnotic effects in sodium pentobarbital-treated mice | |
| JP2013533310A5 (hr) | ||
| Qi et al. | Fasudil, an inhibitor of Rho-associated coiled-coil kinase, attenuates hyperoxia-induced pulmonary fibrosis in neonatal rats | |
| JP2015505303A5 (hr) | ||
| Meade et al. | Why do asthmatic subjects respond so strongly to inhaled adenosine? | |
| Polosa et al. | Adenosine receptors as promising therapeutic targets for drug development in chronic airway inflammation | |
| Turner et al. | Effects of nebulised magnesium sulphate on inflammation and function of the guinea-pig airway | |
| Shook et al. | Recent advances in developing antiviral therapies for respiratory syncytial virus | |
| Knabe et al. | CCSP counterbalances airway epithelial-driven neutrophilic chemotaxis | |
| EP4126002A1 (en) | Methods of treating pulmonary injury with cgrp inhibitors | |
| US20240252493A1 (en) | Apelin Receptor Modulators for Treating Age-Related Muscle Conditions | |
| Kong et al. | Efficacy and safety of chimeric antigen receptor T cell therapy in relapsed/refractory diffuse large B-cell lymphoma with different HBV status: a retrospective study from a single center | |
| Ponnoth et al. | Adenosine receptors and vascular inflammation | |
| Shindo et al. | Priming effect of platelet activating factor on leukotriene C4 from stimulated eosinophils of asthmatic patients. | |
| Smith et al. | Adenosine receptor subtypes in the airways responses to 5′‐adenosine monophosphate inhalation of sensitized guinea‐pigs | |
| Poynter | Do insights from mice imply that combined Th2 and Th17 therapies would benefit select severe asthma patients? | |
| Hsiao et al. | Combination Of Theophylline With Long-Acting Beta-2 Adrenergic Receptor Agonist Inhibits Cigarette Smoke Induced Airway Inflammation | |
| Danese et al. | Editorial (Thematic Issue: New Mechanisms and Targets for IBD Therapy: Translational Gastroenterology Comes of Age) | |
| Obiefuna et al. | A novel A1 adenosine receptor antagonist (L-97-1) reduces allergic responses to house dust mite in an allergic rabbit model of asthma | |
| Dong et al. | The role of ICOSL in children with neutrophilic asthma | |
| Caramori et al. | Drugs for the Treatment of Airway Disease | |
| Nakaji et al. | Effect Of Repeated Cough Induced By Citric Acid Exposures On Cough Sensitivity And Airway Pathology In Guinea Pigs |