JP2006511583A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2006511583A5 JP2006511583A5 JP2004563946A JP2004563946A JP2006511583A5 JP 2006511583 A5 JP2006511583 A5 JP 2006511583A5 JP 2004563946 A JP2004563946 A JP 2004563946A JP 2004563946 A JP2004563946 A JP 2004563946A JP 2006511583 A5 JP2006511583 A5 JP 2006511583A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- aryl
- heterocyclyl
- heteroaryl
- carbon
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
- 229910052799 carbon Inorganic materials 0.000 claims 99
- 125000003118 aryl group Chemical group 0.000 claims 88
- 125000000623 heterocyclic group Chemical group 0.000 claims 67
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 64
- -1 M 2 Chemical group 0.000 claims 64
- 125000001072 heteroaryl group Chemical group 0.000 claims 64
- 125000003710 aryl alkyl group Chemical group 0.000 claims 61
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 58
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 51
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 51
- 125000002950 monocyclic group Chemical group 0.000 claims 48
- 125000002877 alkyl aryl group Chemical group 0.000 claims 45
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims 41
- 229910052757 nitrogen Inorganic materials 0.000 claims 31
- 125000001475 halogen functional group Chemical group 0.000 claims 30
- 229910052739 hydrogen Inorganic materials 0.000 claims 30
- 150000001875 compounds Chemical class 0.000 claims 29
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 20
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 20
- 125000000217 alkyl group Chemical group 0.000 claims 17
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 16
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 15
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 15
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 15
- 208000035475 disorder Diseases 0.000 claims 14
- 229910052760 oxygen Inorganic materials 0.000 claims 11
- 102100034069 MAP kinase-activated protein kinase 2 Human genes 0.000 claims 10
- 101710141394 MAP kinase-activated protein kinase 2 Proteins 0.000 claims 10
- 125000004093 cyano group Chemical group *C#N 0.000 claims 10
- 125000000449 nitro group Chemical class [O-][N+](*)=O 0.000 claims 10
- 229910052717 sulfur Inorganic materials 0.000 claims 10
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 8
- 230000002401 inhibitory effect Effects 0.000 claims 7
- 108060008682 Tumor Necrosis Factor Proteins 0.000 claims 6
- 102000000852 Tumor Necrosis Factor-alpha Human genes 0.000 claims 6
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 230000001404 mediated effect Effects 0.000 claims 6
- 239000001301 oxygen Substances 0.000 claims 6
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 5
- 125000004429 atom Chemical group 0.000 claims 5
- 239000011593 sulfur Substances 0.000 claims 5
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 claims 4
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 4
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 4
- 125000005865 C2-C10alkynyl group Chemical group 0.000 claims 4
- 101100516568 Caenorhabditis elegans nhr-7 gene Proteins 0.000 claims 4
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 4
- 208000027418 Wounds and injury Diseases 0.000 claims 4
- 208000014674 injury Diseases 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 4
- 229940124789 MK2 inhibitor Drugs 0.000 claims 3
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 3
- 125000000278 alkyl amino alkyl group Chemical group 0.000 claims 3
- 125000000304 alkynyl group Chemical group 0.000 claims 3
- 125000004103 aminoalkyl group Chemical group 0.000 claims 3
- 230000006378 damage Effects 0.000 claims 3
- 125000004985 dialkyl amino alkyl group Chemical group 0.000 claims 3
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 3
- 125000006413 ring segment Chemical group 0.000 claims 3
- 201000005671 spondyloarthropathy Diseases 0.000 claims 3
- 201000004624 Dermatitis Diseases 0.000 claims 2
- LELOWRISYMNNSU-UHFFFAOYSA-N Hydrocyanic acid Natural products N#C LELOWRISYMNNSU-UHFFFAOYSA-N 0.000 claims 2
- 208000012902 Nervous system disease Diseases 0.000 claims 2
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims 2
- 208000006045 Spondylarthropathies Diseases 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000003282 alkyl amino group Chemical group 0.000 claims 2
- 208000010668 atopic eczema Diseases 0.000 claims 2
- 210000002808 connective tissue Anatomy 0.000 claims 2
- 125000004663 dialkyl amino group Chemical group 0.000 claims 2
- 208000030533 eye disease Diseases 0.000 claims 2
- 208000015181 infectious disease Diseases 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 230000001225 therapeutic effect Effects 0.000 claims 2
- 210000001519 tissue Anatomy 0.000 claims 2
- SQQWBSBBCSFQGC-JLHYYAGUSA-N ubiquinone-2 Chemical compound COC1=C(OC)C(=O)C(C\C=C(/C)CCC=C(C)C)=C(C)C1=O SQQWBSBBCSFQGC-JLHYYAGUSA-N 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- DMTVLHOJTLJUHG-UHFFFAOYSA-N 2-(2-aminoethyl)-5-(2-quinolin-3-ylpyridin-4-yl)pyrazole-3-carboxylic acid;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.C1=C(C(O)=O)N(CCN)N=C1C1=CC=NC(C=2C=C3C=CC=CC3=NC=2)=C1 DMTVLHOJTLJUHG-UHFFFAOYSA-N 0.000 claims 1
- FBUFDEIWIUCPAH-UHDJGPCESA-N 2-(2-aminoethyl)-5-[2-[(e)-2-phenylethenyl]pyridin-4-yl]pyrazole-3-carboxylic acid;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.C1=C(C(O)=O)N(CCN)N=C1C1=CC=NC(\C=C\C=2C=CC=CC=2)=C1 FBUFDEIWIUCPAH-UHDJGPCESA-N 0.000 claims 1
- GUXZPWFWFJSWPE-UHFFFAOYSA-N 2-(2-aminoethyl)-5-[2-[4-(hydroxymethyl)phenyl]pyridin-4-yl]pyrazole-3-carboxylic acid;dihydrochloride Chemical compound Cl.Cl.C1=C(C(O)=O)N(CCN)N=C1C1=CC=NC(C=2C=CC(CO)=CC=2)=C1 GUXZPWFWFJSWPE-UHFFFAOYSA-N 0.000 claims 1
- YMUBHZPDPYZUOR-UHFFFAOYSA-N 2-(3-aminopropyl)-5-[2-(3-nitrophenyl)pyridin-4-yl]pyrazole-3-carboxylic acid;dihydrochloride Chemical compound Cl.Cl.C1=C(C(O)=O)N(CCCN)N=C1C1=CC=NC(C=2C=C(C=CC=2)[N+]([O-])=O)=C1 YMUBHZPDPYZUOR-UHFFFAOYSA-N 0.000 claims 1
- INZWSXZYNJIFSJ-UHFFFAOYSA-N 6-(aminomethyl)-2-(2-quinolin-3-ylpyridin-4-yl)-6,7-dihydro-5h-pyrazolo[1,5-a]pyrazin-4-one Chemical compound C1=CC=CC2=CC(C=3N=CC=C(C=3)C3=NN4CC(NC(=O)C4=C3)CN)=CN=C21 INZWSXZYNJIFSJ-UHFFFAOYSA-N 0.000 claims 1
- GGRWZJIJWLJCQA-UHFFFAOYSA-N 6-(hydroxymethyl)-2-(2-quinolin-3-ylpyridin-4-yl)-6,7-dihydro-5h-pyrazolo[1,5-a]pyrazin-4-one Chemical compound C1=CC=CC2=CC(C=3N=CC=C(C=3)C3=NN4CC(NC(=O)C4=C3)CO)=CN=C21 GGRWZJIJWLJCQA-UHFFFAOYSA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000032467 Aplastic anaemia Diseases 0.000 claims 1
- 208000027496 Behcet disease Diseases 0.000 claims 1
- 208000009137 Behcet syndrome Diseases 0.000 claims 1
- 208000017283 Bile Duct disease Diseases 0.000 claims 1
- 206010006811 Bursitis Diseases 0.000 claims 1
- 241000222122 Candida albicans Species 0.000 claims 1
- 206010007134 Candida infections Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000035473 Communicable disease Diseases 0.000 claims 1
- 206010010741 Conjunctivitis Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 201000003883 Cystic fibrosis Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 208000018035 Dental disease Diseases 0.000 claims 1
- 206010012335 Dependence Diseases 0.000 claims 1
- 208000005171 Dysmenorrhea Diseases 0.000 claims 1
- 208000017701 Endocrine disease Diseases 0.000 claims 1
- 208000000624 Esophageal and Gastric Varices Diseases 0.000 claims 1
- 206010051012 Gastric varices Diseases 0.000 claims 1
- 208000007882 Gastritis Diseases 0.000 claims 1
- 206010017943 Gastrointestinal conditions Diseases 0.000 claims 1
- 208000018522 Gastrointestinal disease Diseases 0.000 claims 1
- 201000005569 Gout Diseases 0.000 claims 1
- 206010018634 Gouty Arthritis Diseases 0.000 claims 1
- 208000009889 Herpes Simplex Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000012659 Joint disease Diseases 0.000 claims 1
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 1
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 1
- 208000000913 Kidney Calculi Diseases 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 208000023178 Musculoskeletal disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010029148 Nephrolithiasis Diseases 0.000 claims 1
- 206010029164 Nephrotic syndrome Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000025157 Oral disease Diseases 0.000 claims 1
- 206010034912 Phobia Diseases 0.000 claims 1
- 206010035664 Pneumonia Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010037423 Pulmonary oedema Diseases 0.000 claims 1
- 208000017442 Retinal disease Diseases 0.000 claims 1
- 206010038910 Retinitis Diseases 0.000 claims 1
- 206010038923 Retinopathy Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 201000001880 Sexual dysfunction Diseases 0.000 claims 1
- 206010040744 Sinus headache Diseases 0.000 claims 1
- 208000007107 Stomach Ulcer Diseases 0.000 claims 1
- 206010042674 Swelling Diseases 0.000 claims 1
- 208000000491 Tendinopathy Diseases 0.000 claims 1
- 206010043255 Tendonitis Diseases 0.000 claims 1
- 206010043269 Tension headache Diseases 0.000 claims 1
- 208000008548 Tension-Type Headache Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 206010046851 Uveitis Diseases 0.000 claims 1
- 206010046914 Vaginal infection Diseases 0.000 claims 1
- 201000008100 Vaginitis Diseases 0.000 claims 1
- 208000036142 Viral infection Diseases 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 230000009692 acute damage Effects 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 230000000172 allergic effect Effects 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 206010006451 bronchitis Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 201000003984 candidiasis Diseases 0.000 claims 1
- 208000015114 central nervous system disease Diseases 0.000 claims 1
- 208000018631 connective tissue disease Diseases 0.000 claims 1
- 238000010276 construction Methods 0.000 claims 1
- 230000001054 cortical effect Effects 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 208000010643 digestive system disease Diseases 0.000 claims 1
- 208000032625 disorder of ear Diseases 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000005917 gastric ulcer Diseases 0.000 claims 1
- 208000018685 gastrointestinal system disease Diseases 0.000 claims 1
- 208000007565 gingivitis Diseases 0.000 claims 1
- 208000014951 hematologic disease Diseases 0.000 claims 1
- 230000009610 hypersensitivity Effects 0.000 claims 1
- 208000013643 idiopathic inflammatory myopathy Diseases 0.000 claims 1
- 208000026278 immune system disease Diseases 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 208000019423 liver disease Diseases 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 208000030194 mouth disease Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 208000031225 myocardial ischemia Diseases 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 230000000926 neurological effect Effects 0.000 claims 1
- 150000002829 nitrogen Chemical group 0.000 claims 1
- 208000030212 nutrition disease Diseases 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 208000019899 phobic disease Diseases 0.000 claims 1
- 201000006292 polyarteritis nodosa Diseases 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 230000035755 proliferation Effects 0.000 claims 1
- WGYKZJWCGVVSQN-UHFFFAOYSA-N propylamine Chemical group CCCN WGYKZJWCGVVSQN-UHFFFAOYSA-N 0.000 claims 1
- 208000020016 psychiatric disease Diseases 0.000 claims 1
- 208000005333 pulmonary edema Diseases 0.000 claims 1
- 208000023504 respiratory system disease Diseases 0.000 claims 1
- 201000003068 rheumatic fever Diseases 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 201000000306 sarcoidosis Diseases 0.000 claims 1
- 231100000872 sexual dysfunction Toxicity 0.000 claims 1
- 208000017520 skin disease Diseases 0.000 claims 1
- 230000008961 swelling Effects 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
- 201000004415 tendinitis Diseases 0.000 claims 1
- 206010043778 thyroiditis Diseases 0.000 claims 1
- 230000000451 tissue damage Effects 0.000 claims 1
- 231100000827 tissue damage Toxicity 0.000 claims 1
- 208000004371 toothache Diseases 0.000 claims 1
- 230000000472 traumatic effect Effects 0.000 claims 1
- 208000019553 vascular disease Diseases 0.000 claims 1
- 230000009385 viral infection Effects 0.000 claims 1
- 230000029663 wound healing Effects 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US43496202P | 2002-12-20 | 2002-12-20 | |
| PCT/US2003/040932 WO2004058176A2 (en) | 2002-12-20 | 2003-12-19 | Acyclic pyrazole compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2006511583A JP2006511583A (ja) | 2006-04-06 |
| JP2006511583A5 true JP2006511583A5 (https=) | 2007-02-01 |
Family
ID=32682131
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004563888A Withdrawn JP2006514043A (ja) | 2002-12-20 | 2003-12-19 | マイトジェン活性化タンパク質キナーゼ−活性化タンパク質キナーゼ−2を阻害する化合物 |
| JP2004563946A Withdrawn JP2006511583A (ja) | 2002-12-20 | 2003-12-19 | マイトジェン活性化プロテインキナーゼ−活性化プロテインキナーゼ−2を阻害するための非環式ピラゾール化合物 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004563888A Withdrawn JP2006514043A (ja) | 2002-12-20 | 2003-12-19 | マイトジェン活性化タンパク質キナーゼ−活性化タンパク質キナーゼ−2を阻害する化合物 |
Country Status (15)
| Country | Link |
|---|---|
| US (3) | US20040152739A1 (https=) |
| EP (2) | EP1572682A4 (https=) |
| JP (2) | JP2006514043A (https=) |
| KR (1) | KR20050104339A (https=) |
| CN (1) | CN1747949A (https=) |
| AU (2) | AU2003301226A1 (https=) |
| BR (2) | BR0317430A (https=) |
| CA (2) | CA2509565A1 (https=) |
| IL (1) | IL169177A0 (https=) |
| MX (2) | MXPA05006568A (https=) |
| NO (1) | NO20053396L (https=) |
| PL (1) | PL377461A1 (https=) |
| RU (1) | RU2005119173A (https=) |
| WO (2) | WO2004058762A1 (https=) |
| ZA (1) | ZA200504898B (https=) |
Families Citing this family (156)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050043346A1 (en) * | 2003-08-08 | 2005-02-24 | Pharmacia Italia S.P.A. | Pyridylpyrrole derivatives active as kinase inhibitors |
| JP2007501827A (ja) * | 2003-08-08 | 2007-02-01 | ファルマシア・イタリア・エス・ピー・エー | キナーゼ阻害剤として活性なピリミジルピロール誘導体 |
| EP1663204B1 (en) * | 2003-08-29 | 2014-05-07 | Exelixis, Inc. | C-kit modulators and methods of use |
| PL1664041T3 (pl) | 2003-09-22 | 2008-12-31 | Euro Celtique Sa | Przydatne do leczenia bólu związki fenylowo-karboksyamidowe |
| SI1664016T1 (sl) | 2003-09-22 | 2009-04-30 | Euro Celtique Sa | Terapevtska sredstva, uporabna za zdravljenje bolečine |
| US7462612B2 (en) | 2004-03-26 | 2008-12-09 | Vertex Pharmaceuticals Incorporated | Pyridine inhibitors of ERK2 and uses thereof |
| ES2377430T3 (es) * | 2004-09-02 | 2012-03-27 | Genentech, Inc. | Inhibidores piridílicos de la señalización de hedgehog |
| US20090018145A1 (en) | 2004-10-19 | 2009-01-15 | Compass Pharmaceuticals Llc | Compositions and their use as anti-tumor agents |
| DE102004054665A1 (de) * | 2004-11-12 | 2006-05-18 | Bayer Cropscience Gmbh | Substituierte bi- und tricyclische Pyrazol-Derivate Verfahren zur Herstellung und Verwendung als Herbizide und Pflanzenwachstumsregulatoren |
| US20060115453A1 (en) * | 2004-11-12 | 2006-06-01 | Yaffe Michael B | Methods and compositions for treating cellular proliferative diseases |
| CN101103018A (zh) * | 2004-11-16 | 2008-01-09 | 神经化学(国际)有限公司 | 治疗cns和淀粉样蛋白-相关疾病的化合物 |
| US7473694B2 (en) | 2005-03-17 | 2009-01-06 | Teijin Pharma Limited | Pyrazolopyrimidine derivatives or pharmaceutically acceptable salts thereof |
| CN101142219A (zh) * | 2005-03-17 | 2008-03-12 | 帝人制药株式会社 | 吡唑并嘧啶衍生物或其医学上容许的盐 |
| US7417053B2 (en) | 2005-04-07 | 2008-08-26 | Teijin Pharma Limited | Pyrazolo[1,5-a]pyridine derivatives or pharmaceutically acceptable salts thereof |
| FR2885904B1 (fr) * | 2005-05-19 | 2007-07-06 | Aventis Pharma Sa | Nouveaux derives du fluorene, compositions les contenant et utilisation |
| BRPI0612287A8 (pt) * | 2005-06-27 | 2019-01-22 | Exelixis Inc | composição para uso farmacêutico no tratamento de doenças através da medicina nuclear e métodos de uso e para modulação de atividade de receptor nuclear |
| GB0520958D0 (en) * | 2005-10-14 | 2005-11-23 | Cyclacel Ltd | Compound |
| AR056155A1 (es) | 2005-10-26 | 2007-09-19 | Bristol Myers Squibb Co | Antagonistas del receptor 1 de la hormona de concentracion de melanina no basica |
| WO2007063946A1 (ja) * | 2005-11-30 | 2007-06-07 | Fujifilm Ri Pharma Co., Ltd. | アミロイドの凝集及び/又は沈着に起因する疾患の診断薬及び治療薬 |
| US20070142414A1 (en) * | 2005-12-16 | 2007-06-21 | Pharmacia Italia S.P.A. | N-substituted pyrrolopyridinones active as kinase inhibitors |
| US7618982B2 (en) * | 2005-12-19 | 2009-11-17 | Nerviano Medical Sciences S.R.L. | Heteroarylpyrrolopyridinones active as kinase inhibitors |
| CA2635531C (en) * | 2005-12-29 | 2014-06-17 | Lexicon Pharmaceutical Inc. | Multicyclic amino acid derivatives and methods of their use |
| US7553836B2 (en) | 2006-02-06 | 2009-06-30 | Bristol-Myers Squibb Company | Melanin concentrating hormone receptor-1 antagonists |
| US7951824B2 (en) * | 2006-02-17 | 2011-05-31 | Hoffman-La Roche Inc. | 4-aryl-pyridine-2-carboxyamide derivatives |
| WO2007096334A1 (en) * | 2006-02-24 | 2007-08-30 | Pfizer Italia Srl | Pyrrolopyrrolones active as kinase inhibitors |
| BRPI0709680B8 (pt) | 2006-03-27 | 2021-05-25 | Nerviano Medical Sciences Srl | derivados de pirrol, tiofeno e furano substituídos por piridil e piridimil como inibidores de quinase |
| WO2007135398A1 (en) * | 2006-05-22 | 2007-11-29 | Astrazeneca Ab | Indole derivatives |
| PE20080668A1 (es) * | 2006-08-30 | 2008-07-17 | Novartis Ag | Compuestos heterociclicos como inhibidores de la cinasa-2 de proteina activada por cinasa de proteina activada por mitogeno |
| CA2662359A1 (en) | 2006-09-21 | 2008-03-27 | Novartis Ag | Pyrrole derivatives useful for the treatment of cytokine-mediated diseases |
| CA2667003A1 (en) | 2006-10-20 | 2008-05-02 | Merck & Co., Inc. | Substituted imidazoles as bombesin receptor subtype-3 modulators |
| CA2666310C (en) | 2006-10-20 | 2012-07-31 | Merck & Co., Inc. | Substituted imidazoles as bombesin receptor subtype-3 modulators |
| US8106070B2 (en) | 2006-10-20 | 2012-01-31 | Merck Sharp & Dohme Corp. | Substituted imidazoles as bombesin receptor subtype-3 modulators |
| AU2007319786A1 (en) * | 2006-11-15 | 2008-05-22 | Vertex Pharmaceuticals Incorporated | Compounds useful as protein kinase inhibitors |
| WO2008059370A2 (en) | 2006-11-17 | 2008-05-22 | Pfizer Japan Inc. | Substituted bicyclocarboxyamide compounds |
| KR20090094125A (ko) | 2006-12-08 | 2009-09-03 | 엑셀리시스, 인코포레이티드 | Lxr 및 fxr 조절자 |
| CN101605788A (zh) | 2006-12-11 | 2009-12-16 | 默克公司 | 用作铃蟾肽受体亚型-3调节剂的取代的二氮杂磺酰胺类化合物 |
| WO2008133669A2 (en) | 2006-12-14 | 2008-11-06 | Gilead Sciences, Inc. | Viral inhibitors |
| AU2007342674B2 (en) * | 2007-01-10 | 2013-09-19 | Purdue Research Foundation | Polypeptide inhibitors of HSP27 kinase and uses therefor |
| UY30892A1 (es) | 2007-02-07 | 2008-09-02 | Smithkline Beckman Corp | Inhibidores de la actividad akt |
| ES2546816T3 (es) * | 2007-02-27 | 2015-09-28 | Nerviano Medical Sciences S.R.L. | Isoquinolinpirrolopiridinonas activas como inhibidores de cinasa |
| EP2143714B1 (en) | 2007-04-04 | 2013-06-05 | Kowa Company, Ltd. | Tetrahydroisoquinoline compound |
| CA2685962A1 (en) * | 2007-05-08 | 2009-02-05 | Burnham Institute For Medical Research | Tissue non-specific alkaline phosphatase inhibitors and uses thereof for treating vascular calcification |
| CA2687306A1 (en) | 2007-05-18 | 2008-11-27 | Bayer Schering Pharma Aktiengesellschaft | Heteroaryl substituted pyrazole derivatives useful for treating hyper-proliferative disorders and diseases associated with angiogenesis |
| DE102007026341A1 (de) * | 2007-06-06 | 2008-12-11 | Merck Patent Gmbh | Benzoxazolonderivate |
| EP2003129B1 (en) | 2007-06-11 | 2017-08-09 | Nerviano Medical Sciences S.r.l. | 1H-Pyrido[3,4-B]indol-1-one and 2,3,4,9-Tetrahydro-1H-Beta-Carbolin-1-one Derivatives |
| EP2170306A1 (en) * | 2007-06-26 | 2010-04-07 | Lexicon Pharmaceuticals, Inc. | Methods of treating serotonin-mediated diseases and disorders |
| US7875622B2 (en) | 2007-07-11 | 2011-01-25 | Lexicon Pharmaceuticals, Inc. | Methods and compositions for treating pulmonary hypertension and related diseases and disorders |
| DE102007032507A1 (de) | 2007-07-12 | 2009-04-02 | Merck Patent Gmbh | Pyridazinonderivate |
| MX2009014247A (es) | 2007-07-16 | 2010-01-28 | Novartis Ag | Compuestos heterociclicos utiles como inhibidores de mk2. |
| JP5703466B2 (ja) * | 2007-08-07 | 2015-04-22 | パーデュー・リサーチ・ファウンデーションPurdue Research Foundation | キナーゼ阻害薬およびその使用 |
| DE102007038957A1 (de) * | 2007-08-17 | 2009-02-19 | Merck Patent Gmbh | 6-Thioxo-pyridazinderivate |
| DE102007061963A1 (de) * | 2007-12-21 | 2009-06-25 | Merck Patent Gmbh | Pyridazinonderivate |
| US8343966B2 (en) * | 2008-01-11 | 2013-01-01 | Novartis Ag | Organic compounds |
| CA2714181C (en) * | 2008-02-04 | 2013-12-24 | Mercury Therapeutics, Inc. | Ampk modulators |
| US20090281089A1 (en) * | 2008-04-11 | 2009-11-12 | Genentech, Inc. | Pyridyl inhibitors of hedgehog signalling |
| DE102008019907A1 (de) | 2008-04-21 | 2009-10-22 | Merck Patent Gmbh | Pyridazinonderivate |
| PE20091928A1 (es) | 2008-05-29 | 2009-12-31 | Bristol Myers Squibb Co | Tienopirimidinas hidroxisustituidas como antagonistas de receptor-1 de hormona concentradora de melanina no basicos |
| DE102008028905A1 (de) | 2008-06-18 | 2009-12-24 | Merck Patent Gmbh | 3-(3-Pyrimidin-2-yl-benzyl)-[1,2,4]triazolo[4,3-b]pyridazinderivate |
| US20110098221A1 (en) * | 2008-06-26 | 2011-04-28 | Hong Lin | INHIBITORS OF Akt ACTIVITY |
| GB0812969D0 (en) | 2008-07-15 | 2008-08-20 | Sentinel Oncology Ltd | Pharmaceutical compounds |
| JP5693452B2 (ja) * | 2008-08-04 | 2015-04-01 | シーエイチディーアイ ファウンデーション,インコーポレーテッド | 特定のキヌレニン−3−モノオキシゲナーゼインヒビター、医薬組成物およびそれらの使用方法 |
| DE102008037790A1 (de) * | 2008-08-14 | 2010-02-18 | Merck Patent Gmbh | Bicyclische Triazolderivate |
| AU2009304596A1 (en) | 2008-10-17 | 2010-04-22 | Akaal Pharma Pty Ltd | S1P receptors modulators |
| WO2010043000A1 (en) * | 2008-10-17 | 2010-04-22 | Akaal Pharma Pty Ltd | S1p receptors modulators and their use thereof |
| DE102009041242A1 (de) | 2009-09-11 | 2011-12-15 | Bayer Schering Pharma Aktiengesellschaft | Heterocyclisch substituierte Aryl-Verbindungen und ihre Verwendung |
| DE102009041241A1 (de) | 2009-09-11 | 2011-08-04 | Bayer Schering Pharma Aktiengesellschaft, 13353 | Substituierte Aryl-Verbindungen und ihre Verwendung |
| DE102008057344A1 (de) | 2008-11-14 | 2010-05-20 | Bayer Schering Pharma Aktiengesellschaft | Aminoalkyl-substituierte Aryl-Verbindungen und ihre Verwendung |
| DE102008057364A1 (de) | 2008-11-14 | 2010-05-20 | Bayer Schering Pharma Aktiengesellschaft | Substituierte Aryl-Verbindungen und ihre Verwendung |
| DE102008057343A1 (de) | 2008-11-14 | 2010-05-20 | Bayer Schering Pharma Aktiengesellschaft | Heterocyclisch substituierte Aryl-Verbindungen und ihre Verwendung |
| WO2010061903A1 (ja) * | 2008-11-27 | 2010-06-03 | 塩野義製薬株式会社 | Pi3k阻害活性を有するピリミジン誘導体およびピリジン誘導体 |
| CA2744104C (en) | 2008-12-10 | 2017-07-18 | Purdue Research Foundation | Cell-permeant peptide-based inhibitor of kinases |
| SI2361250T1 (sl) | 2008-12-22 | 2013-12-31 | Merck Patent Gmbh | Nove polimorfne oblike 6-(1-metil-1h-pirazol-4-il)-2-(3-(5-(2-morfolin-4-il-etoksi)-pirimidin- 2-il)-benzil)-2h-piridazin-3-on dihidrogenfosfata in postopki za proizvodnjo le-tega |
| WO2010107768A1 (en) | 2009-03-18 | 2010-09-23 | Schering Corporation | Bicyclic compounds as inhibitors of diacylglycerol acyltransferase |
| AR077463A1 (es) | 2009-07-09 | 2011-08-31 | Irm Llc | Derivados de imidazo[1, 2 - a]pirazina y su uso en medicamentos para el tratamiento de enfermedades parasitarias |
| US9890195B2 (en) | 2009-07-27 | 2018-02-13 | Purdue Research Foundation | MK2 inhibitor compositions and methods to enhance neurite outgrowth, neuroprotection, and nerve regeneration |
| AU2014277711B2 (en) * | 2009-12-14 | 2016-10-27 | Merck Sharp & Dohme B.V. | MK2 inhibitors |
| RU2012129887A (ru) * | 2009-12-14 | 2014-01-27 | Мсд Осс Б.В. | Ингибиторы мк2 |
| CA2787365A1 (en) * | 2010-01-25 | 2011-07-28 | Chdi Foundation, Inc. | Certain kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof |
| CN102753168A (zh) * | 2010-02-10 | 2012-10-24 | 莱西肯医药有限公司 | 用于治疗转移性骨病的色氨酸羟化酶抑制剂 |
| US8686048B2 (en) * | 2010-05-06 | 2014-04-01 | Rhizen Pharmaceuticals Sa | Immunomodulator and anti-inflammatory compounds |
| MX339640B (es) | 2010-06-09 | 2016-06-01 | Janssen Pharmaceutica Nv * | Derivados de 5, 6-dihidro-2h-[1, 4] oxazin-3-il-amina utiles como inhibidores de la beta-secretasa (bace). |
| BR112013006353A2 (pt) * | 2010-09-22 | 2024-01-16 | Janssen Pharmaceutica Nv | Derivados de 4,7-di-hifro-pirazolo[1,5-a]pirazin-6-ilamina úteis como inibidores de beta-secretase (bace) |
| EP2655376B1 (en) | 2010-12-22 | 2017-08-23 | Janssen Pharmaceutica NV | 5,6-DIHYDRO-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) |
| CN103415519B (zh) | 2011-03-01 | 2016-03-02 | 詹森药业有限公司 | 作为β-分泌酶(BACE)抑制剂有用的6,7-二氢-吡唑[1,5-a]吡嗪-4-基胺衍生物 |
| AU2012224632B2 (en) | 2011-03-09 | 2016-06-16 | Janssen Pharmaceutica Nv | 3,4-dihydro-pyrrolo[1,2-a]pyrazin-1-ylamine derivatives useful as inhibitors of beta-secretase (BACE) |
| HUE044867T2 (hu) * | 2011-05-12 | 2019-11-28 | Proteostasis Therapeutics Inc | Proteosztázis szabályzók |
| SI2750677T1 (sl) | 2011-08-30 | 2017-10-30 | Chdi Foundation, Inc. | Inhibitorji kinurenin-3-monooksigenaze, farmacevtski sestavki in postopki njihove uporabe |
| CA2848540A1 (en) | 2011-09-15 | 2013-03-21 | Arizona Board Of Regents, A Body Corporate Of The State Of Arizona Acting For And On Behalf Of Arizona State University | Therapeutic compounds |
| WO2013134636A1 (en) | 2012-03-09 | 2013-09-12 | Purdue Research Foundation | Compositions and methods for delivery of kinase inhibiting peptides |
| HRP20191755T1 (hr) | 2012-09-07 | 2019-12-27 | Boehringer Ingelheim International Gmbh | Alkoksipirazoli kao aktivatori topljive gvanilat ciklaze |
| ES2755772T3 (es) | 2012-11-07 | 2020-04-23 | Nerviano Medical Sciences Srl | Pirimidinil y piridinilpirrolopiridinonas sustituidas, proceso para su preparación y su uso como inhibidores de cinasas |
| EP2746260A1 (en) | 2012-12-21 | 2014-06-25 | Basf Se | Substituted [1,2,4]triazole and imidazole compounds |
| EP2746259A1 (en) | 2012-12-21 | 2014-06-25 | Basf Se | Substituted [1,2,4]triazole and imidazole compounds |
| EP2951157A1 (en) * | 2013-02-04 | 2015-12-09 | Merck Patent GmbH | Positive allosteric modulators of mglur3 |
| EP3943087A1 (en) | 2013-03-15 | 2022-01-26 | Celgene CAR LLC | Heteroaryl compounds and uses thereof |
| US9321786B2 (en) | 2013-03-15 | 2016-04-26 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| CA2908098A1 (en) | 2013-03-15 | 2014-09-25 | Celgene Avilomics Research, Inc. | Mk2 inhibitors and uses thereof |
| CA2903813C (en) * | 2013-03-15 | 2023-08-29 | Epizyme, Inc. | Carm1 inhibitors and uses thereof |
| CN105307657B (zh) | 2013-03-15 | 2020-07-10 | 西建卡尔有限责任公司 | 杂芳基化合物和其用途 |
| BR112015030597A2 (pt) | 2013-06-12 | 2017-07-25 | Janssen Pharmaceutica Nv | derivados 4-amino-6-fenil-6,7-di-hidro[1,2,3]triazolo[1,5-a]pirazina como inibidores de beta-secretase (bace) |
| MX368326B (es) | 2013-06-12 | 2019-09-27 | Janssen Pharmaceutica Nv | Derivados de 4-amino-6-fenil-5,6-dihidroimidazo[1,5-a]pirazin-3(2h )-ona como inhibidores de beta-secretasa (bace). |
| KR102243134B1 (ko) | 2013-06-12 | 2021-04-22 | 얀센 파마슈티카 엔.브이. | 베타-세크레타제(bace) 저해제로서의 4-아미노-6-페닐-5,6-디하이드로이미다조[1,5-a]피라진 유도체 |
| WO2015109318A2 (en) | 2014-01-17 | 2015-07-23 | Arizona Board Of Regents, A Body Corporate Of The State Of Arizona, Acting For And On Behalf Of Arizona State University | Therapeutic methods |
| EP3105218B1 (en) | 2014-02-13 | 2019-09-25 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| EP3105219B9 (en) | 2014-02-13 | 2018-10-03 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| US9527835B2 (en) | 2014-02-13 | 2016-12-27 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| JP6602779B2 (ja) | 2014-02-13 | 2019-11-06 | インサイト・コーポレイション | Lsd1阻害剤としてのシクロプロピルアミン類 |
| US10342795B2 (en) * | 2014-03-27 | 2019-07-09 | Janssen Pharmaceutica Nv | Substituted 4,5,6,7-tetrahydro-pyrazolo[1,5-a]pyrimidine derivatives and 2,3-dihydro-1H-imidazo[1,2-b]pyrazole derivatives as ROS1 inhibitors |
| ES2715676T3 (es) * | 2014-03-27 | 2019-06-05 | Janssen Pharmaceutica Nv | Derivados de 4,5,6,7-tetrahidro-pirazolo[1,5-a]pirazina sustituidos y derivados de 5,6,7,8-tetrahidro-4h-pirazolo[1,5-a][1,4]diazepina como inhibidores de ros1 |
| WO2015172196A1 (en) * | 2014-05-13 | 2015-11-19 | Monash University | Heterocyclic compounds and use of same |
| WO2015191630A1 (en) * | 2014-06-10 | 2015-12-17 | Sanford-Burnham Medical Research Institute | Metabotropic glutamate receptor negative allosteric modulators (nams) and uses thereof |
| WO2016007731A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyridines and imidazopyrazines as lsd1 inhibitors |
| US9695180B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors |
| US9695167B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors |
| US9758523B2 (en) | 2014-07-10 | 2017-09-12 | Incyte Corporation | Triazolopyridines and triazolopyrazines as LSD1 inhibitors |
| AU2015289492B2 (en) | 2014-07-17 | 2020-02-20 | Chdi Foundation, Inc. | Methods and compositions for treating HIV-related disorders |
| WO2016032882A1 (en) * | 2014-08-25 | 2016-03-03 | Stc.Unm | Inhibition of mk2 in the treatment of cancer |
| RS62017B1 (sr) | 2014-09-17 | 2021-07-30 | Celgene Car Llc | Mk2 inhibitori i njihova upotreba |
| US10301306B2 (en) | 2014-12-15 | 2019-05-28 | Bristol-Myers Squibb Company | Substituted dihydro-1H-pyrrolo[3,2-c]pyridin-4(5H)-ones as RIPK3 inhibitors |
| ES2768823T3 (es) | 2014-12-18 | 2020-06-23 | Janssen Pharmaceutica Nv | Derivados de 2,3,4,5-tetrahidropiridin-6-amina y 3,4-dihidro-2H-pirrol-5-amina útiles como inhibidores de beta-secretasa |
| JP6654477B2 (ja) * | 2015-03-17 | 2020-02-26 | 株式会社日本触媒 | ホウ素含有化合物 |
| EP3277689B1 (en) | 2015-04-03 | 2019-09-04 | Incyte Corporation | Heterocyclic compounds as lsd1 inhibitors |
| JP6549735B2 (ja) | 2015-06-09 | 2019-07-24 | アッヴィ・インコーポレイテッド | 核内受容体調節剤 |
| WO2016198908A1 (en) | 2015-06-09 | 2016-12-15 | Abbvie Inc. | Ror nuclear receptor modulators |
| MY189367A (en) | 2015-08-12 | 2022-02-08 | Incyte Corp | Salts of an lsd1 inhibitor |
| EP3390387B1 (en) | 2015-12-18 | 2021-11-17 | Bayer Pharma Aktiengesellschaft | Heteroarylbenzimidazole compounds |
| US10059718B2 (en) | 2016-01-04 | 2018-08-28 | Tabomedex Biosciences, LLC | Fused quadracyclic compounds, compositions and uses thereof |
| TWI833686B (zh) | 2016-04-22 | 2024-03-01 | 美商英塞特公司 | Lsd1 抑制劑之調配物 |
| WO2017207534A1 (en) | 2016-06-03 | 2017-12-07 | Bayer Pharma Aktiengesellschaft | Substituted heteroarylbenzimidazole compounds |
| US10231947B2 (en) | 2017-01-23 | 2019-03-19 | Arizona Board Of Regents On Behalf Of Arizona State University | Isochroman compounds and methods of use thereof |
| US10238655B2 (en) | 2017-01-23 | 2019-03-26 | Arizona Board Of Regents On Behalf Of Arizona State University | Dihydroindene and tetrahydronaphthalene compounds |
| US10238626B2 (en) | 2017-01-23 | 2019-03-26 | Arizona Board Of Regents On Behalf Of Arizona State University | Therapeutic compounds |
| WO2018170203A1 (en) | 2017-03-16 | 2018-09-20 | Celgene Car Llc | Mk2 inhibitors, synthesis thereof, and intermediates thereto |
| EP3596085A4 (en) | 2017-03-16 | 2020-11-25 | Celgene CAR LLC | DEUTERATED ANALOGUES OF MK2 INHIBITORS AND THEIR USES |
| WO2018170200A1 (en) | 2017-03-16 | 2018-09-20 | Celgene Car Llc | Heteroaryl compounds useful as mk2 inhibitors |
| US10882867B2 (en) | 2017-03-16 | 2021-01-05 | Celgene Car Llc | Forms and compositions of a MK2 inhibitor |
| US11098057B2 (en) | 2017-03-16 | 2021-08-24 | Celgene Car Llc | 9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-F]quinolin-8-one compounds and uses thereof |
| CN110691597A (zh) | 2017-04-24 | 2020-01-14 | 诺华股份有限公司 | 2-氨基-1-(2-(4-氟苯基)-3-(4-氟苯基氨基)-8,8-二甲基-5,6-二氢咪唑并[1,2-a]吡嗪-7(8H)-基)乙酮及其组合的治疗方案 |
| TWI782056B (zh) | 2017-07-14 | 2022-11-01 | 日商鹽野義製藥股份有限公司 | 具有mgat2抑制活性的縮合環衍生物 |
| WO2019172830A1 (en) * | 2018-03-07 | 2019-09-12 | Andren Per | Pyridinium, quinolinium, acridinium, pyrylium, chromenylium or xanthylizum reactive desorption and/or laser ablation ionization matrices and use thereof |
| US10968200B2 (en) | 2018-08-31 | 2021-04-06 | Incyte Corporation | Salts of an LSD1 inhibitor and processes for preparing the same |
| KR102128509B1 (ko) * | 2018-12-19 | 2020-07-01 | 한국과학기술연구원 | 말단 아민기에 아릴 또는 헤테로아릴기가 치환된 신규한 히드라존 유도체 및 이의 용도 |
| MX2021008050A (es) | 2019-01-11 | 2021-08-05 | Shionogi & Co | Derivado de dihidropirazolopirazinona que tiene actividad inhibidora de monoacilglicerol aciltransferasa 2 (mgat2). |
| CN113661164B (zh) * | 2019-04-08 | 2025-03-04 | 珠海宇繁生物科技有限责任公司 | 一种cdk激酶抑制剂及其应用 |
| US12570612B2 (en) | 2019-10-11 | 2026-03-10 | Chengdu Mfs Pharma. Co., Ltd. | Substituted nitrogen heterocyclic compound and anesthetic effect thereof |
| CN110724106B (zh) * | 2019-10-11 | 2023-05-05 | 成都麻沸散医药科技有限公司 | 取代吡唑甲酸酯类衍生物及其用途 |
| EP4188928B1 (en) | 2020-07-29 | 2024-07-24 | Bayer Aktiengesellschaft | Substituted 1 h-pyrrolo[3,2-b]pyridin compounds and methods of use thereof |
| TW202229282A (zh) * | 2020-09-30 | 2022-08-01 | 美商史考皮恩治療有限公司 | 治療癌症之方法 |
| US20240067657A1 (en) * | 2020-12-29 | 2024-02-29 | Merck Sharp & Dohme Llc | Amido-substituted pyridyl compounds and methods of use thereof for the treatment of herpesviruses |
| CN116670142A (zh) | 2021-02-01 | 2023-08-29 | 细胞基因公司 | Mk2抑制剂、其合成和其中间体 |
| CN114605267B (zh) * | 2022-03-18 | 2024-02-23 | 北京格林凯默科技有限公司 | 2-溴-n,n-二甲基苯胺的制备方法 |
| TW202400582A (zh) * | 2022-05-13 | 2024-01-01 | 大陸商上海湃隆生物科技有限公司 | 驅動蛋白kif18a抑制劑及其應用 |
| CN120225203A (zh) | 2022-11-04 | 2025-06-27 | 勃林格殷格翰国际有限公司 | 用于治疗系统性硬化症的可溶性鸟苷酸环化酶活化剂 |
| CN120344531A (zh) * | 2022-12-11 | 2025-07-18 | 江苏豪森药业集团有限公司 | 哌啶酮衍生物、其制备方法及其医药用途 |
| CN116496151B (zh) * | 2023-04-26 | 2024-08-23 | 长沙医学院 | 一种利用Catellani策略制备芴酮衍生物的方法 |
| WO2025245367A1 (en) * | 2024-05-22 | 2025-11-27 | Psy Therapeutics, Inc. | Inhibiting catechol-o-methyltransferase (comt) |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3169966A (en) * | 1961-01-24 | 1965-02-16 | Ciba Geigy Corp | Aminopyrazoles |
| DE69323185T2 (de) * | 1992-02-24 | 1999-07-08 | Smithkline Beecham Corp., Philadelphia, Pa. 19101 | Proteinkinase c-inhibitor |
| PL310386A1 (en) * | 1993-02-22 | 1995-12-11 | Merck & Co Inc | Antagonists of factor i receptors |
| JP3714685B2 (ja) * | 1994-05-18 | 2005-11-09 | 第一サントリーファーマ株式会社 | ハイメニアルディシン及びその誘導体並びにそれらの合成中間体の製造法並びにその合成中間体 |
| US5616577A (en) * | 1994-08-25 | 1997-04-01 | Smithkline Beecham Corporation | Protein Kinase C inhibitor |
| US5591740A (en) * | 1995-06-07 | 1997-01-07 | Osteoarthritis Sciences, Incorporated | Use of debromohymenialdisine for treating osteoarthritis |
| US6008204A (en) * | 1995-09-01 | 1999-12-28 | Allergan Sales, Inc. | Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities |
| US6046208A (en) * | 1996-01-11 | 2000-04-04 | Smithkline Beecham Corporation | Substituted imidazole compounds |
| US6218136B1 (en) * | 1996-03-12 | 2001-04-17 | Smithkline Beecham Corporation | Methods of the identification of pharmaceutically active compounds |
| EP0912548A1 (en) * | 1996-07-11 | 1999-05-06 | Pfizer Inc. | Pyridylpyrrole compounds useful as interleukin- and tnf antagonists |
| US6096753A (en) * | 1996-12-05 | 2000-08-01 | Amgen Inc. | Substituted pyrimidinone and pyridone compounds and methods of use |
| US6514977B1 (en) * | 1997-05-22 | 2003-02-04 | G.D. Searle & Company | Substituted pyrazoles as p38 kinase inhibitors |
| US6489325B1 (en) * | 1998-07-01 | 2002-12-03 | Smithkline Beecham Corporation | Substituted imidazole compounds |
| US6251914B1 (en) * | 1997-07-02 | 2001-06-26 | Smithkline Beecham Corporation | Cycloalkyl substituted imidazoles |
| ES2339196T3 (es) * | 1997-07-18 | 2010-05-17 | Novo Nordisk Health Care Ag | Uso de fviia o fviiai para el tratamiento de disfuncion endotelial y para la inhibicion de angiogenesis, respectivamente. |
| US6022884A (en) * | 1997-11-07 | 2000-02-08 | Amgen Inc. | Substituted pyridine compounds and methods of use |
| AU1924699A (en) * | 1997-12-19 | 1999-07-12 | Smithkline Beecham Corporation | Compounds of heteroaryl substituted imidazole, their pharmaceutical compositionsand uses |
| US6197954B1 (en) * | 1998-01-30 | 2001-03-06 | The Trustees Of Columbia University In The City Of New York | Intermediates for the synthesis of debromohymenialdisine and processes thereof |
| MXPA01002173A (es) * | 1998-08-28 | 2003-07-14 | Scios Inc | Inhibidores de p38-alfa cinasa. |
| US6143892A (en) * | 1998-11-20 | 2000-11-07 | G. D. Searle & Co. | Process for making 5-substituted pyrazoles |
| CN1136217C (zh) * | 1998-12-17 | 2004-01-28 | 霍夫曼-拉罗奇有限公司 | 作为jnk蛋白质激酶抑制剂的4-芳基羟吲哚 |
| WO2000040243A1 (en) * | 1999-01-08 | 2000-07-13 | Smithkline Beecham Corporation | Novel compounds |
| US6211361B1 (en) * | 1999-07-20 | 2001-04-03 | State Of Oregon Acting By And Through The Oregon State Board Of Higher Education On Behalf Of Oregon, State Univeristy | Method for making debromohymenialdisine and analogs thereof |
| KR20010111298A (ko) * | 2000-02-05 | 2001-12-17 | 버텍스 파마슈티칼스 인코포레이티드 | Erk의 억제제로서 유용한 피라졸 조성물 |
| HUP0301932A3 (en) * | 2000-05-22 | 2007-09-28 | Leo Pharma As | Benzophenones as inhibitors of il-1 beta and tnf-alpha, pharmaceutical compositions containing them and use of them for producing pharmaceutical compositions |
-
2003
- 2003-12-19 ZA ZA200504898A patent/ZA200504898B/en unknown
- 2003-12-19 AU AU2003301226A patent/AU2003301226A1/en not_active Withdrawn
- 2003-12-19 BR BR0317430-1A patent/BR0317430A/pt not_active Application Discontinuation
- 2003-12-19 JP JP2004563888A patent/JP2006514043A/ja not_active Withdrawn
- 2003-12-19 KR KR1020057011474A patent/KR20050104339A/ko not_active Withdrawn
- 2003-12-19 WO PCT/US2003/040811 patent/WO2004058762A1/en not_active Ceased
- 2003-12-19 US US10/742,494 patent/US20040152739A1/en not_active Abandoned
- 2003-12-19 MX MXPA05006568A patent/MXPA05006568A/es not_active Application Discontinuation
- 2003-12-19 WO PCT/US2003/040932 patent/WO2004058176A2/en not_active Ceased
- 2003-12-19 BR BR0317525-1A patent/BR0317525A/pt not_active IP Right Cessation
- 2003-12-19 US US10/742,072 patent/US20040209897A1/en not_active Abandoned
- 2003-12-19 CN CNA2003801096266A patent/CN1747949A/zh active Pending
- 2003-12-19 RU RU2005119173/04A patent/RU2005119173A/ru not_active Application Discontinuation
- 2003-12-19 JP JP2004563946A patent/JP2006511583A/ja not_active Withdrawn
- 2003-12-19 AU AU2003297431A patent/AU2003297431A1/en not_active Abandoned
- 2003-12-19 PL PL377461A patent/PL377461A1/pl unknown
- 2003-12-19 EP EP03814309A patent/EP1572682A4/en not_active Withdrawn
- 2003-12-19 CA CA002509565A patent/CA2509565A1/en not_active Abandoned
- 2003-12-19 CA CA002510298A patent/CA2510298A1/en not_active Abandoned
- 2003-12-19 MX MXPA05006569A patent/MXPA05006569A/es unknown
- 2003-12-19 EP EP03814268A patent/EP1572693A1/en not_active Withdrawn
-
2005
- 2005-06-15 IL IL169177A patent/IL169177A0/en unknown
- 2005-07-13 NO NO20053396A patent/NO20053396L/no not_active Application Discontinuation
-
2007
- 2007-12-17 US US11/958,229 patent/US20080113971A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2006511583A5 (https=) | ||
| RU2005119173A (ru) | Ациклические пиразольные соединения | |
| AU2022202403B2 (en) | Aryl, heteroaryl, and heterocyclic pharmaceutical compounds for treatment of medical disorders | |
| JP7216682B2 (ja) | Usp30阻害剤としての1-シアノ-ピロリジン化合物 | |
| JP7600123B2 (ja) | ユビキチンプロテオソーム経路を介してbtkを分解するための二官能性化合物 | |
| JP6517928B2 (ja) | キナーゼ阻害剤として有用なインドールカルボキシアミド | |
| CN109790168B (zh) | 取代的吡咯嗪化合物及其用途 | |
| JP5925394B2 (ja) | 抗レトロウイルス剤としての(ヘテロ)アリールアセトアミド誘導体 | |
| JP7010935B2 (ja) | Usp30の阻害剤としての活性を有するシアノ置換ヘテロ環 | |
| CN114072393B (zh) | 作为mrgx2抑制剂的3-氨基-4h-苯并[e][1,2,4]噻二嗪1,1-二氧化物衍生物 | |
| CN115298184B (zh) | 杂环rip1抑制化合物 | |
| KR102821964B1 (ko) | 치환된 피롤로피리미딘 jak 억제제 및 이의 제조 및 사용 방법 | |
| US20240294505A1 (en) | 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamides for the treatment of cancer | |
| CN112384510A (zh) | Rip1抑制性化合物以及制备和使用其的方法 | |
| KR20090106604A (ko) | 축합 피리딘 화합물 | |
| WO2002015662A3 (en) | Quinuclidine-substituted heteroaryl moieties for treatment of disease (nicotinic acetylcholine receptor antagonists | |
| TW201639827A (zh) | TGF-β抑制劑 | |
| PT1689751E (pt) | Novas 5,7-diaminopirazolo[4,3-d]pirimidinas com actividade inibidora de pde-5 | |
| JP2022548602A (ja) | アゾール縮合ピリダジン-3(2h)-オン誘導体 | |
| TW200418861A (en) | Pyrrolopyridazine derivatives | |
| JP2013533868A (ja) | タンパク質チロシンキナーゼ阻害剤としての新規ホモピペラジン誘導体およびそれらの医薬使用 | |
| US9193724B2 (en) | Triazolopyridyl compounds as aldosterone synthase inhibitors | |
| CN113332292A (zh) | 6,7-二氢-5H-吡唑并[5,1-b][1,3]噁嗪-2-甲酰胺化合物 | |
| CN118510775A (zh) | 作为ripk1抑制剂的异噁唑烷及其用途 | |
| JP6605121B2 (ja) | ヤヌスキナーゼ1選択的阻害剤及びその医薬用途 |