RU2009113615A - Ингибитор киназы - Google Patents
Ингибитор киназы Download PDFInfo
- Publication number
- RU2009113615A RU2009113615A RU2009113615/04A RU2009113615A RU2009113615A RU 2009113615 A RU2009113615 A RU 2009113615A RU 2009113615/04 A RU2009113615/04 A RU 2009113615/04A RU 2009113615 A RU2009113615 A RU 2009113615A RU 2009113615 A RU2009113615 A RU 2009113615A
- Authority
- RU
- Russia
- Prior art keywords
- patient
- compound according
- administering
- effective amount
- need
- Prior art date
Links
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 25
- 150000003839 salts Chemical class 0.000 claims abstract 9
- FBOZXECLQNJBKD-ZDUSSCGKSA-N L-methotrexate Chemical compound C=1N=C2N=C(N)N=C(N)C2=NC=1CN(C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 FBOZXECLQNJBKD-ZDUSSCGKSA-N 0.000 claims abstract 4
- 150000001204 N-oxides Chemical class 0.000 claims abstract 4
- 206010003246 arthritis Diseases 0.000 claims abstract 4
- 208000018937 joint inflammation Diseases 0.000 claims abstract 4
- 229960000485 methotrexate Drugs 0.000 claims abstract 4
- 239000000651 prodrug Substances 0.000 claims abstract 4
- 229940002612 prodrug Drugs 0.000 claims abstract 4
- 206010039073 rheumatoid arthritis Diseases 0.000 claims abstract 4
- 239000012453 solvate Substances 0.000 claims abstract 4
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims abstract 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims abstract 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims abstract 3
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims abstract 2
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims abstract 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical group Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims abstract 2
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 claims abstract 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 claims abstract 2
- 206010025323 Lymphomas Diseases 0.000 claims abstract 2
- OFOBLEOULBTSOW-UHFFFAOYSA-L Malonate Chemical compound [O-]C(=O)CC([O-])=O OFOBLEOULBTSOW-UHFFFAOYSA-L 0.000 claims abstract 2
- 229910002651 NO3 Inorganic materials 0.000 claims abstract 2
- 206010028980 Neoplasm Diseases 0.000 claims abstract 2
- NHNBFGGVMKEFGY-UHFFFAOYSA-N Nitrate Chemical compound [O-][N+]([O-])=O NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 claims abstract 2
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 claims abstract 2
- 229910019142 PO4 Inorganic materials 0.000 claims abstract 2
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 claims abstract 2
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims abstract 2
- 230000033115 angiogenesis Effects 0.000 claims abstract 2
- 239000003937 drug carrier Substances 0.000 claims abstract 2
- 230000002401 inhibitory effect Effects 0.000 claims abstract 2
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims abstract 2
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims abstract 2
- 239000010452 phosphate Substances 0.000 claims abstract 2
- YGSDEFSMJLZEOE-UHFFFAOYSA-M salicylate Chemical compound OC1=CC=CC=C1C([O-])=O YGSDEFSMJLZEOE-UHFFFAOYSA-M 0.000 claims abstract 2
- 229960001860 salicylate Drugs 0.000 claims abstract 2
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims abstract 2
- IIACRCGMVDHOTQ-UHFFFAOYSA-M sulfamate Chemical compound NS([O-])(=O)=O IIACRCGMVDHOTQ-UHFFFAOYSA-M 0.000 claims abstract 2
- 229940095064 tartrate Drugs 0.000 claims abstract 2
- WXTMDXOMEHJXQO-UHFFFAOYSA-N 2,5-dihydroxybenzoic acid Chemical compound OC(=O)C1=CC(O)=CC=C1O WXTMDXOMEHJXQO-UHFFFAOYSA-N 0.000 claims 2
- -1 di-n-toluotartrate Chemical compound 0.000 claims 2
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical group N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 1
- SRSXLGNVWSONIS-UHFFFAOYSA-M benzenesulfonate Chemical compound [O-]S(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-M 0.000 claims 1
- 229940077388 benzenesulfonate Drugs 0.000 claims 1
- HCAJEUSONLESMK-UHFFFAOYSA-N cyclohexylsulfamic acid Chemical compound OS(=O)(=O)NC1CCCCC1 HCAJEUSONLESMK-UHFFFAOYSA-N 0.000 claims 1
- CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical compound CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 claims 1
- 229940114119 gentisate Drugs 0.000 claims 1
- SUMDYPCJJOFFON-UHFFFAOYSA-N isethionic acid Chemical compound OCCS(O)(=O)=O SUMDYPCJJOFFON-UHFFFAOYSA-N 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Otolaryngology (AREA)
- Transplantation (AREA)
- Endocrinology (AREA)
- Oncology (AREA)
- Ophthalmology & Optometry (AREA)
- Emergency Medicine (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Abstract
1. Соединение формулы (I): ! ! или соответствующий N-оксид, или пролекарство, или фармацевтически приемлемая соль, или сольват такого соединения и N-оксид и пролекарство соли и сольвата. ! 2. Фармацевтическая композиция, содержащая соединение по п.1, вместе с по крайней мере одним фармацевтически приемлемым носителем или наполнителем. ! 3. Способ лечения воспаления суставов у пациента, включающий введение нуждающемуся в этом пациенту эффективного количества соединения по п.1. ! 4. Способ лечения ревматоидного артрита у пациента, включающий введение нуждающемуся в этом пациенту эффективного количества соединения по п.1. ! 5. Способ лечения воспаления суставов у пациента, включающий введение нуждающемуся в этом пациенту эффективного количества соединения по п.1, в сочетании с метотрексатом. ! 6. Способ лечения ревматоидного артрита у пациента, включающий введение нуждающемуся в этом пациенту эффективного количества соединения по п.1, в сочетании с метотрексатом. ! 7. Способ лечения опухоли у пациента, включающий введение нуждающемуся в этом пациенту эффективного количества соединения по п.1. ! 8. Способ лечения лимфомы из клеток мантийной зоны у пациента, включающий введение нуждающемуся в этом пациенту эффективного количества соединения по п.1. ! 9. Способ ингибирования ангиогенеза у пациента, включающий введение нуждающемуся в этом пациенту эффективного количества соединения по п.1. ! 10. Соединение по п.1, где соль выбирают из гидрохлорида, гидробромида, сульфата, фосфата, нитрата, сульфамата, ацетата, цитрата, лактата, тартрата, малоната, оксалата, салицилата, пропионата, сукцината, фумарата, малеата, метилен-бис-b-гидрокс�
Claims (13)
2. Фармацевтическая композиция, содержащая соединение по п.1, вместе с по крайней мере одним фармацевтически приемлемым носителем или наполнителем.
3. Способ лечения воспаления суставов у пациента, включающий введение нуждающемуся в этом пациенту эффективного количества соединения по п.1.
4. Способ лечения ревматоидного артрита у пациента, включающий введение нуждающемуся в этом пациенту эффективного количества соединения по п.1.
5. Способ лечения воспаления суставов у пациента, включающий введение нуждающемуся в этом пациенту эффективного количества соединения по п.1, в сочетании с метотрексатом.
6. Способ лечения ревматоидного артрита у пациента, включающий введение нуждающемуся в этом пациенту эффективного количества соединения по п.1, в сочетании с метотрексатом.
7. Способ лечения опухоли у пациента, включающий введение нуждающемуся в этом пациенту эффективного количества соединения по п.1.
8. Способ лечения лимфомы из клеток мантийной зоны у пациента, включающий введение нуждающемуся в этом пациенту эффективного количества соединения по п.1.
9. Способ ингибирования ангиогенеза у пациента, включающий введение нуждающемуся в этом пациенту эффективного количества соединения по п.1.
10. Соединение по п.1, где соль выбирают из гидрохлорида, гидробромида, сульфата, фосфата, нитрата, сульфамата, ацетата, цитрата, лактата, тартрата, малоната, оксалата, салицилата, пропионата, сукцината, фумарата, малеата, метилен-бис-b-гидроксинафтоата, гентизата, изетионата, ди-n-толуотартрата, метансульфоната, этансульфоната, бензолсульфоната, n-толуолсульфоната, циклогексилсульфамата и хинната.
11. Соединение по п.1, где соль представляет собой гидрохлорид.
12. Соединение по п.1, где соль представляет собой ацетат.
13. Соединение по п.1, где соль представляет собой цитрат.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US82516806P | 2006-09-11 | 2006-09-11 | |
| US60/825,168 | 2006-09-11 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2009113615A true RU2009113615A (ru) | 2010-10-20 |
| RU2440352C2 RU2440352C2 (ru) | 2012-01-20 |
Family
ID=39032357
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2009113615/04A RU2440352C2 (ru) | 2006-09-11 | 2007-09-11 | Ингибитор киназы |
Country Status (32)
| Country | Link |
|---|---|
| US (2) | US8658649B2 (ru) |
| EP (1) | EP2094708B1 (ru) |
| JP (1) | JP5161237B2 (ru) |
| KR (1) | KR101443056B1 (ru) |
| CN (2) | CN103804383A (ru) |
| AR (1) | AR062745A1 (ru) |
| AU (1) | AU2007296592B8 (ru) |
| BR (1) | BRPI0716781A2 (ru) |
| CA (1) | CA2663175C (ru) |
| CL (1) | CL2007002617A1 (ru) |
| CO (1) | CO6160236A2 (ru) |
| CR (1) | CR10636A (ru) |
| DK (1) | DK2094708T3 (ru) |
| ES (1) | ES2437318T3 (ru) |
| GT (1) | GT200900055A (ru) |
| HN (1) | HN2009000455A (ru) |
| IL (1) | IL197381A (ru) |
| MA (1) | MA30781B1 (ru) |
| MX (1) | MX2009002616A (ru) |
| MY (1) | MY148107A (ru) |
| NI (1) | NI200900021A (ru) |
| NO (1) | NO20091265L (ru) |
| NZ (1) | NZ575496A (ru) |
| PE (1) | PE20081372A1 (ru) |
| PT (1) | PT2094708E (ru) |
| RU (1) | RU2440352C2 (ru) |
| TN (2) | TN2009000049A1 (ru) |
| TW (1) | TWI399379B (ru) |
| UA (1) | UA94622C2 (ru) |
| UY (1) | UY30584A1 (ru) |
| WO (1) | WO2008033798A2 (ru) |
| ZA (1) | ZA200901073B (ru) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK2250172T3 (da) | 2008-02-25 | 2012-01-16 | Hoffmann La Roche | Pyrrolopyrazinkinaseinhibitorer |
| CN101952295B (zh) | 2008-02-25 | 2013-11-20 | 霍夫曼-拉罗奇有限公司 | 吡咯并吡嗪激酶抑制剂 |
| CA2716223A1 (en) | 2008-02-25 | 2009-09-03 | F. Hoffmann-La Roche Ag | Pyrrolopyrazine kinase inhibitors |
| PL2247592T3 (pl) | 2008-02-25 | 2012-01-31 | Hoffmann La Roche | Pirolopirazynowe inhibitory kinazy |
| ATE519763T1 (de) | 2008-02-25 | 2011-08-15 | Hoffmann La Roche | Pyrrolopyrazin-kinasehemmer |
| MX2010008308A (es) * | 2008-03-10 | 2010-08-11 | Sanofi Aventis | Tratamiento para trastornos relacionados con los ojos. |
| FR2929851B1 (fr) * | 2008-04-09 | 2012-11-30 | Centre Nat Rech Scient | Molecules inhibant une voie metabolique impliquant la proteine tyrosine kinase syk et procede d'identification de ces molecules |
| PA8851701A1 (es) | 2008-12-03 | 2010-07-27 | Sanofi Aventis | Tratamiento para la glomerulonefritis |
| EP2373655A1 (en) | 2008-12-04 | 2011-10-12 | Sanofi | Crystalline forms |
| TW201034675A (en) * | 2008-12-18 | 2010-10-01 | Sanofi Aventis | Method for treating macular degeneration |
| US20110112101A1 (en) * | 2009-03-05 | 2011-05-12 | Sanofi-Aventis | Treatment for ocular-related disorders |
| AR075869A1 (es) * | 2009-03-19 | 2011-05-04 | Sanofi Aventis | Sintesis de azaindoles |
| US8440689B2 (en) | 2009-12-23 | 2013-05-14 | Takeda Pharmaceutical Company Limited | Fused heteroaromatic pyrrolidinones |
| US8481541B2 (en) * | 2010-03-22 | 2013-07-09 | Hoffmann-La Roche Inc. | Pyrrolopyrazine kinase inhibitors |
| US8518945B2 (en) | 2010-03-22 | 2013-08-27 | Hoffmann-La Roche Inc. | Pyrrolopyrazine kinase inhibitors |
| TWI496785B (zh) | 2010-05-20 | 2015-08-21 | Hoffmann La Roche | 吡咯并吡激酶抑制劑 |
| RU2012152352A (ru) * | 2010-05-20 | 2014-06-27 | Ф. Хоффманн-Ля Рош Аг | ПРОИЗВОДНЫЕ ПИРРОЛО[2,3-b]ПИРАЗИН-7-КАРБОКСАМИДА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ JAK И SYK |
| EP2441755A1 (en) | 2010-09-30 | 2012-04-18 | Almirall, S.A. | Pyridine- and isoquinoline-derivatives as Syk and JAK kinase inhibitors |
| EP2489663A1 (en) | 2011-02-16 | 2012-08-22 | Almirall, S.A. | Compounds as syk kinase inhibitors |
| EP2723739B1 (en) | 2011-06-22 | 2016-08-24 | Takeda Pharmaceutical Company Limited | Substituted 6-aza-isoindolin-1-one derivatives |
| WO2014029732A1 (en) * | 2012-08-21 | 2014-02-27 | F. Hoffmann-La Roche Ag | Pyrrolo[2,3-b]pyrazines as syk inhibitors |
| SG11201600373YA (en) * | 2013-07-31 | 2016-02-26 | Gilead Sciences Inc | Syk inhibitors |
| JP2022526713A (ja) | 2019-03-21 | 2022-05-26 | オンクセオ | がんの処置のための、キナーゼ阻害剤と組み合わせたDbait分子 |
| JP2023500906A (ja) | 2019-11-08 | 2023-01-11 | インサーム(インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル) | キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| CN116969927B (zh) * | 2023-06-07 | 2024-03-19 | 中南民族大学 | 一种从荜茇中提取分离的化合物及该化合物在制备抗炎药物中的应用 |
Family Cites Families (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1141949A (en) | 1966-02-23 | 1969-02-05 | Sterling Drug Inc | 7-azaindole derivatives |
| US3992392A (en) | 1973-04-27 | 1976-11-16 | The Ohio State University Research Foundation | Synthesis of indoles from anilines and intermediates therein |
| SE9100920D0 (sv) | 1991-03-27 | 1991-03-27 | Astra Ab | New active compounds |
| GB9226855D0 (en) * | 1992-12-23 | 1993-02-17 | Erba Carlo Spa | Vinylene-azaindole derivatives and process for their preparation |
| US6075037A (en) | 1994-06-09 | 2000-06-13 | Smithkline Beecham Corporation | Endothelin receptor antagonists |
| FR2732969B1 (fr) | 1995-04-14 | 1997-05-16 | Adir | Nouveaux composes pyridiniques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| KR20000057137A (ko) | 1996-11-19 | 2000-09-15 | 스티븐 엠. 오드레 | 아릴 및 헤테로아릴로 치환된 융합 피롤 항염증제 |
| US6312835B1 (en) | 1997-02-13 | 2001-11-06 | Queen's University At Kingston | Luminescent compounds and methods of making and using same |
| CA2283961A1 (en) | 1997-03-19 | 1998-09-24 | Basf Aktiengesellschaft | Pyrrolo[2,3d]pyrimidines and their use as tyrosine kinase inhibitors |
| AU7132998A (en) | 1997-04-24 | 1998-11-13 | Ortho-Mcneil Corporation, Inc. | Substituted pyrrolopyridines useful in the treatment of inflammatory diseases |
| ID24300A (id) | 1997-08-05 | 2000-07-13 | Pfizer Prod Inc | 4-AMINOPIROL(3,2-d)PIRIMIDIN SEBAGAI ANTAGONIS-ANTAGONIS RESEPTOR NEUROPEPTIDA Y |
| TR200001079T2 (tr) | 1997-10-20 | 2000-07-21 | F.Hoffmann-La Roche Ag | Bisiklik kinaz inhibitörleri. |
| WO1999045016A2 (en) | 1998-03-06 | 1999-09-10 | Metabasis Therapeutics, Inc. | Novel prodrugs for phosphorus-containing compounds |
| JP2002510685A (ja) | 1998-04-02 | 2002-04-09 | メルク エンド カムパニー インコーポレーテッド | 性腺刺激ホルモン放出ホルモン拮抗薬 |
| AU3210799A (en) | 1998-04-02 | 1999-10-25 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| DE69942801D1 (de) | 1998-05-26 | 2010-11-11 | Chugai Pharmaceutical Co Ltd | Heterozyklische indolderivate und mono- oder diazaindol-derivate |
| CZ2001959A3 (cs) | 1998-09-18 | 2001-12-12 | Basf Aktiengesellschaft | 4-Aminopyrrolopyrimidiny jako inhibitory kinasy |
| PE20010306A1 (es) | 1999-07-02 | 2001-03-29 | Agouron Pharma | Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa |
| GB9930698D0 (en) * | 1999-12-24 | 2000-02-16 | Rhone Poulenc Rorer Ltd | Chemical compounds |
| CN1615873A (zh) * | 1999-12-24 | 2005-05-18 | 阿文蒂斯药物有限公司 | 氮杂吲哚类化合物 |
| US6770666B2 (en) | 1999-12-27 | 2004-08-03 | Japan Tobacco Inc. | Fused-ring compounds and use thereof as drugs |
| YU54202A (sh) | 2000-01-18 | 2006-01-16 | Agouron Pharmaceuticals Inc. | Jedinjenja indazola, farmaceutske smeše i postupci za stimulisanje i inhibiranje ćelijske proliferacije |
| DE10009000A1 (de) | 2000-02-25 | 2001-08-30 | Basf Ag | Verfahren zur Herstellung substituierter Indole |
| EP1265897A1 (en) | 2000-03-20 | 2002-12-18 | Axys Pharmaceuticals, Inc. | Non-amidine containing protease inhibitors |
| 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 |
| US6673923B2 (en) | 2000-05-03 | 2004-01-06 | Tularik Inc. | Pyrazole antimicrobial agents |
| MXPA02010763A (es) | 2000-06-14 | 2003-03-10 | Warner Lambert Co | Heterociclicos biciclos-6,5 fusionados. |
| AU2002211828A1 (en) | 2000-10-02 | 2002-04-15 | Merck & Co., Inc. | Inhibitors of prenyl-protein transferase |
| GB0115109D0 (en) * | 2001-06-21 | 2001-08-15 | Aventis Pharma Ltd | Chemical compounds |
| WO2003000690A1 (en) | 2001-06-25 | 2003-01-03 | Aventis Pharmaceuticals Inc. | Synthesis of heterocyclic compounds employing microwave technology |
| AR035543A1 (es) | 2001-06-26 | 2004-06-16 | Japan Tobacco Inc | Agente terapeutico para la hepatitis c que comprende un compuesto de anillo condensado, compuesto de anillo condensado, composicion farmaceutica que lo comprende, compuestos de benzimidazol, tiazol y bifenilo utiles como intermediarios para producir dichos compuestos, uso del compuesto de anillo con |
| IL161576A0 (en) | 2001-10-26 | 2004-09-27 | Aventis Pharma Inc | Benzimidazoles and analogues and their use as protein kinases inhibitors |
| US20040082365A1 (en) * | 2002-07-18 | 2004-04-29 | Celerica Ltd | Digitization and transmitting cellular RF signals by several light wavelengths |
| EP1388541A1 (en) | 2002-08-09 | 2004-02-11 | Centre National De La Recherche Scientifique (Cnrs) | Pyrrolopyrazines as kinase inhibitors |
| WO2005014543A1 (ja) | 2003-08-06 | 2005-02-17 | Japan Tobacco Inc. | 縮合環化合物及びそのhcvポリメラーゼ阻害剤としての利用 |
| EP1778687A2 (en) * | 2004-07-27 | 2007-05-02 | SGX Pharmaceuticals, Inc. | Fused ring heterocycle kinase modulators |
| GB0420719D0 (en) | 2004-09-17 | 2004-10-20 | Addex Pharmaceuticals Sa | Novel allosteric modulators |
| FR2876582B1 (fr) | 2004-10-15 | 2007-01-05 | Centre Nat Rech Scient Cnrse | Utilisation de derives de pyrrolo-pyrazines pour la fabrication de medicaments pour le traitement de la mucoviscidose et de maladies liees a un defaut d'adressage des proteines dans les cellules |
| ES2424255T3 (es) | 2004-11-08 | 2013-09-30 | Baxter International Inc. | Composiciones particuladas de inhibidores de tubulina |
| EP1814883A1 (en) * | 2004-11-22 | 2007-08-08 | Vertex Pharmaceuticals Incorporated | Bicyclic inhibitors or rho kinase |
| US20110112101A1 (en) | 2009-03-05 | 2011-05-12 | Sanofi-Aventis | Treatment for ocular-related disorders |
-
2007
- 2007-09-10 CL CL200702617A patent/CL2007002617A1/es unknown
- 2007-09-11 PT PT78422078T patent/PT2094708E/pt unknown
- 2007-09-11 CA CA2663175A patent/CA2663175C/en not_active Expired - Fee Related
- 2007-09-11 AU AU2007296592A patent/AU2007296592B8/en not_active Ceased
- 2007-09-11 JP JP2009538434A patent/JP5161237B2/ja not_active Expired - Fee Related
- 2007-09-11 DK DK07842207.8T patent/DK2094708T3/da active
- 2007-09-11 TW TW096133786A patent/TWI399379B/zh not_active IP Right Cessation
- 2007-09-11 BR BRPI0716781-4A2A patent/BRPI0716781A2/pt not_active IP Right Cessation
- 2007-09-11 PE PE2007001220A patent/PE20081372A1/es not_active Application Discontinuation
- 2007-09-11 CN CN201310652393.XA patent/CN103804383A/zh active Pending
- 2007-09-11 MY MYPI20090720A patent/MY148107A/en unknown
- 2007-09-11 CN CNA2007800336608A patent/CN101511838A/zh active Pending
- 2007-09-11 EP EP07842207.8A patent/EP2094708B1/en active Active
- 2007-09-11 WO PCT/US2007/078103 patent/WO2008033798A2/en not_active Ceased
- 2007-09-11 RU RU2009113615/04A patent/RU2440352C2/ru not_active IP Right Cessation
- 2007-09-11 MX MX2009002616A patent/MX2009002616A/es active IP Right Grant
- 2007-09-11 KR KR1020097005040A patent/KR101443056B1/ko not_active Expired - Fee Related
- 2007-09-11 NZ NZ575496A patent/NZ575496A/en not_active IP Right Cessation
- 2007-09-11 ES ES07842207.8T patent/ES2437318T3/es active Active
- 2007-09-11 UY UY30584A patent/UY30584A1/es not_active Application Discontinuation
- 2007-09-11 AR ARP070104013A patent/AR062745A1/es not_active Application Discontinuation
- 2007-11-09 UA UAA200903417A patent/UA94622C2/ru unknown
-
2009
- 2009-02-16 ZA ZA2009/01073A patent/ZA200901073B/en unknown
- 2009-02-17 TN TN2009000049A patent/TN2009000049A1/fr unknown
- 2009-02-17 TN TN2009000050A patent/TN2009000050A1/fr unknown
- 2009-02-17 NI NI200900021A patent/NI200900021A/es unknown
- 2009-02-25 CR CR10636A patent/CR10636A/es not_active Application Discontinuation
- 2009-03-03 IL IL197381A patent/IL197381A/en not_active IP Right Cessation
- 2009-03-10 US US12/401,254 patent/US8658649B2/en not_active Expired - Fee Related
- 2009-03-10 GT GT200900055A patent/GT200900055A/es unknown
- 2009-03-10 HN HN2009000455A patent/HN2009000455A/es unknown
- 2009-03-11 CO CO09025278A patent/CO6160236A2/es unknown
- 2009-03-26 NO NO20091265A patent/NO20091265L/no not_active Application Discontinuation
- 2009-04-06 MA MA31765A patent/MA30781B1/fr unknown
-
2014
- 2014-01-28 US US14/166,396 patent/US20140142110A1/en not_active Abandoned
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| RU2009113615A (ru) | Ингибитор киназы | |
| US20210292289A1 (en) | Heterocyclic glutaminase inhibitors | |
| US10047078B2 (en) | Aminothiazole compounds | |
| TW200607807A (en) | Macrocyclic beta-secretase inhibitors | |
| JP2017517548A (ja) | グルタミナーゼ阻害剤との併用療法 | |
| ES2672468T3 (es) | Momelotinib deuterado | |
| JP2010502767A5 (ru) | ||
| EA201070167A1 (ru) | Замещенные производные индазола, активные как ингибиторы киназы | |
| WO2008005956A3 (en) | Pyrrolotriazine kinase inhibitors | |
| TW200621249A (en) | Substituted amide beta secretase inhibitors | |
| MY143466A (en) | Inhibitors of tyrosine kinases | |
| EP3116872A1 (en) | Combination therapy with glutaminase inhibitors | |
| AR056786A1 (es) | Compuesto de 1h- imidazo ( 4,5-c) piridin-2-ilo, composicion farmaceutica que lo comprende, procedimiento para preparar dicha composicion, su uso para preparar unmedicamento, uso de una combinacion que omprende al compuesto y al menos un agente antineoplasico para preparar un medicamento y dicha com | |
| TW200738729A (en) | Heterocycles as nicotinic acid receptor agonists for the treatment of dyslipidemia | |
| TWI750539B (zh) | 新穎藥物組成物及其用途 | |
| MXPA04002338A (es) | Derivados de carbazol y su uso como antagonistas receptores del npy5. | |
| WO2008079873A3 (en) | Thiazolyl compounds useful as kinase inhibitors | |
| JP6730194B2 (ja) | アンドロゲン合成モジュレーター | |
| JP6434410B2 (ja) | アンドロゲン合成モジュレーター | |
| US20250235426A1 (en) | Pharmaceutical Combination and Use Thereof | |
| WO2022165185A1 (en) | Cancer-selective target degradation by targeting group caged protacs | |
| CA2526989A1 (en) | Hydroxyamidine and hydroxyguanidine compounds as urokinase inhibitors | |
| JP2017514816A5 (ru) | ||
| EP1868435A2 (en) | Combinations, methods and compositions for treating cancer | |
| TNSN06278A1 (en) | [4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-(4-bromo-3-methyl-5-propoxy-thiophen-2-yl)-methanone hydrochloride as an inhibitor of mast cell tryptase |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | The patent is invalid due to non-payment of fees |
Effective date: 20160912 |