JP2008528465A5 - - Google Patents
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- JP2008528465A5 JP2008528465A5 JP2007551739A JP2007551739A JP2008528465A5 JP 2008528465 A5 JP2008528465 A5 JP 2008528465A5 JP 2007551739 A JP2007551739 A JP 2007551739A JP 2007551739 A JP2007551739 A JP 2007551739A JP 2008528465 A5 JP2008528465 A5 JP 2008528465A5
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- JP
- Japan
- Prior art keywords
- group
- methyl
- hydrogen
- fluorine
- substituted
- 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.)
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- -1 2,6-dichlorophenyl Chemical group 0.000 claims 61
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 23
- 239000001257 hydrogen Substances 0.000 claims 22
- 229910052739 hydrogen Inorganic materials 0.000 claims 22
- 150000001875 compounds Chemical class 0.000 claims 19
- 150000002431 hydrogen Chemical class 0.000 claims 16
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 15
- 239000000460 chlorine Substances 0.000 claims 15
- 229910052801 chlorine Inorganic materials 0.000 claims 15
- 229910052731 fluorine Inorganic materials 0.000 claims 15
- 239000011737 fluorine Substances 0.000 claims 15
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 14
- 125000001424 substituent group Chemical group 0.000 claims 14
- 125000000623 heterocyclic group Chemical group 0.000 claims 13
- 125000002837 carbocyclic group Chemical group 0.000 claims 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims 8
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 8
- 229910052760 oxygen Inorganic materials 0.000 claims 8
- 201000010099 disease Diseases 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 229910052717 sulfur Inorganic materials 0.000 claims 7
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 6
- 125000005842 heteroatom Chemical group 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 125000004432 carbon atom Chemical group C* 0.000 claims 5
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 5
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 4
- 238000004519 manufacturing process Methods 0.000 claims 4
- 125000004486 1-methylpiperidin-3-yl group Chemical group CN1CC(CCC1)* 0.000 claims 3
- 125000001731 2-cyanoethyl group Chemical group [H]C([H])(*)C([H])([H])C#N 0.000 claims 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000004429 atom Chemical group 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 210000001685 thyroid gland Anatomy 0.000 claims 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 2
- FUFZNHHSSMCXCZ-UHFFFAOYSA-N 5-piperidin-4-yl-3-[3-(trifluoromethyl)phenyl]-1,2,4-oxadiazole Chemical class FC(F)(F)C1=CC=CC(C=2N=C(ON=2)C2CCNCC2)=C1 FUFZNHHSSMCXCZ-UHFFFAOYSA-N 0.000 claims 2
- 102000003903 Cyclin-dependent kinases Human genes 0.000 claims 2
- 108090000266 Cyclin-dependent kinases Proteins 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 2
- 150000001204 N-oxides Chemical class 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- SYRLJCGMLGNANZ-UHFFFAOYSA-N cyclohexanone;ethane-1,2-diol Chemical compound OCCO.O=C1CCCCC1 SYRLJCGMLGNANZ-UHFFFAOYSA-N 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 claims 2
- 208000019691 hematopoietic and lymphoid cell neoplasm Diseases 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- XMSZANIMCDLNKA-UHFFFAOYSA-N methyl hypofluorite Chemical group COF XMSZANIMCDLNKA-UHFFFAOYSA-N 0.000 claims 2
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims 2
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- OGYGFUAIIOPWQD-UHFFFAOYSA-N 1,3-thiazolidine Chemical compound C1CSCN1 OGYGFUAIIOPWQD-UHFFFAOYSA-N 0.000 claims 1
- PVOAHINGSUIXLS-UHFFFAOYSA-N 1-Methylpiperazine Chemical compound CN1CCNCC1 PVOAHINGSUIXLS-UHFFFAOYSA-N 0.000 claims 1
- OJWYYSVOSNWCCE-UHFFFAOYSA-N 2-methoxyethyl hypofluorite Chemical group COCCOF OJWYYSVOSNWCCE-UHFFFAOYSA-N 0.000 claims 1
- JPXYQOVMQWMUJG-UHFFFAOYSA-N 4-[(2,3-difluoro-6-methoxybenzoyl)amino]-n-(1-methylsulfonylpiperidin-4-yl)-1h-pyrazole-5-carboxamide Chemical compound COC1=CC=C(F)C(F)=C1C(=O)NC1=CNN=C1C(=O)NC1CCN(S(C)(=O)=O)CC1 JPXYQOVMQWMUJG-UHFFFAOYSA-N 0.000 claims 1
- LRUMTYRMHCAZLB-UHFFFAOYSA-N 4-[(2,6-dichlorobenzoyl)amino]-n-[4-(methoxymethoxy)cyclohexyl]-1h-pyrazole-5-carboxamide Chemical compound C1CC(OCOC)CCC1NC(=O)C1=NNC=C1NC(=O)C1=C(Cl)C=CC=C1Cl LRUMTYRMHCAZLB-UHFFFAOYSA-N 0.000 claims 1
- XHUWMMCNGHAEBI-UHFFFAOYSA-N 4-[(2-chloro-3,6-difluorobenzoyl)amino]-n-(1-methylsulfonylpiperidin-4-yl)-1h-pyrazole-5-carboxamide Chemical compound C1CN(S(=O)(=O)C)CCC1NC(=O)C1=NNC=C1NC(=O)C1=C(F)C=CC(F)=C1Cl XHUWMMCNGHAEBI-UHFFFAOYSA-N 0.000 claims 1
- TVQKRELLTXEYPC-UHFFFAOYSA-N 4-[(3-chloro-2,6-difluorobenzoyl)amino]-n-(1-methylsulfonylpiperidin-4-yl)-1h-pyrazole-5-carboxamide Chemical compound C1CN(S(=O)(=O)C)CCC1NC(=O)C1=NNC=C1NC(=O)C1=C(F)C=CC(Cl)=C1F TVQKRELLTXEYPC-UHFFFAOYSA-N 0.000 claims 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 1
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 1
- 108091007914 CDKs Proteins 0.000 claims 1
- 208000017897 Carcinoma of esophagus Diseases 0.000 claims 1
- 208000010667 Carcinoma of liver and intrahepatic biliary tract Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 102000002254 Glycogen Synthase Kinase 3 Human genes 0.000 claims 1
- 108010014905 Glycogen Synthase Kinase 3 Proteins 0.000 claims 1
- 206010073069 Hepatic cancer Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010061534 Oesophageal squamous cell carcinoma Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 201000010208 Seminoma Diseases 0.000 claims 1
- 208000036765 Squamous cell carcinoma of the esophagus Diseases 0.000 claims 1
- 206010042971 T-cell lymphoma Diseases 0.000 claims 1
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- YPWFISCTZQNZAU-UHFFFAOYSA-N Thiane Chemical compound C1CCSCC1 YPWFISCTZQNZAU-UHFFFAOYSA-N 0.000 claims 1
- 208000033781 Thyroid carcinoma Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000036142 Viral infection Diseases 0.000 claims 1
- 201000006083 Xeroderma Pigmentosum Diseases 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- 230000010261 cell growth Effects 0.000 claims 1
- 201000007455 central nervous system cancer Diseases 0.000 claims 1
- 208000025997 central nervous system neoplasm Diseases 0.000 claims 1
- 208000019065 cervical carcinoma Diseases 0.000 claims 1
- 210000003679 cervix uteri Anatomy 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 125000004188 dichlorophenyl group Chemical group 0.000 claims 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 1
- 125000006222 dimethylaminomethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])* 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 210000002615 epidermis Anatomy 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 208000007276 esophageal squamous cell carcinoma Diseases 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 208000021045 exocrine pancreatic carcinoma Diseases 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 210000000232 gallbladder Anatomy 0.000 claims 1
- 201000010175 gallbladder cancer Diseases 0.000 claims 1
- 201000007487 gallbladder carcinoma Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 208000010749 gastric carcinoma Diseases 0.000 claims 1
- 210000002768 hair cell Anatomy 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 201000002250 liver carcinoma Diseases 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 201000005296 lung carcinoma Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 201000008806 mesenchymal cell neoplasm Diseases 0.000 claims 1
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 201000005528 peripheral nervous system neoplasm Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 201000001514 prostate carcinoma Diseases 0.000 claims 1
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 1
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 1
- 201000006845 reticulosarcoma Diseases 0.000 claims 1
- 208000029922 reticulum cell sarcoma Diseases 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 201000008261 skin carcinoma Diseases 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 201000000498 stomach carcinoma Diseases 0.000 claims 1
- 208000001608 teratocarcinoma Diseases 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 208000013077 thyroid gland carcinoma Diseases 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
- 230000009385 viral infection Effects 0.000 claims 1
- 0 CC1CCN(*)CC1 Chemical compound CC1CCN(*)CC1 0.000 description 4
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US64621705P | 2005-01-21 | 2005-01-21 | |
| GB0501480A GB0501480D0 (en) | 2005-01-22 | 2005-01-22 | Pharmaceutical compounds |
| GB0501748A GB0501748D0 (en) | 2005-01-27 | 2005-01-27 | Pharmaceutical compounds |
| US65133905P | 2005-02-09 | 2005-02-09 | |
| PCT/GB2006/000191 WO2006077414A1 (en) | 2005-01-21 | 2006-01-20 | Pyrazole derivatives for the inhibition of cdk' s and gsk' s |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008528465A JP2008528465A (ja) | 2008-07-31 |
| JP2008528465A5 true JP2008528465A5 (https=) | 2009-03-12 |
Family
ID=35967182
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007551740A Withdrawn JP2008528466A (ja) | 2005-01-21 | 2006-01-20 | Cdkおよびgsk阻害ピラゾール誘導体 |
| JP2007551739A Pending JP2008528465A (ja) | 2005-01-21 | 2006-01-20 | Cdkおよびgskの阻害のためのピラゾール誘導体 |
| JP2007551742A Pending JP2008528467A (ja) | 2005-01-21 | 2006-01-20 | Cdkおよびgskの阻害のためのピラゾール誘導体 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007551740A Withdrawn JP2008528466A (ja) | 2005-01-21 | 2006-01-20 | Cdkおよびgsk阻害ピラゾール誘導体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007551742A Pending JP2008528467A (ja) | 2005-01-21 | 2006-01-20 | Cdkおよびgskの阻害のためのピラゾール誘導体 |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US20080306069A1 (https=) |
| EP (3) | EP1853600A1 (https=) |
| JP (3) | JP2008528466A (https=) |
| KR (3) | KR20070098927A (https=) |
| AR (3) | AR052559A1 (https=) |
| AU (3) | AU2006207311A1 (https=) |
| BR (2) | BRPI0606317A2 (https=) |
| CA (3) | CA2593468A1 (https=) |
| IL (3) | IL184499A0 (https=) |
| MA (3) | MA29255B1 (https=) |
| MX (3) | MX2007008784A (https=) |
| NO (3) | NO20073956L (https=) |
| PE (3) | PE20060876A1 (https=) |
| TN (3) | TNSN07278A1 (https=) |
| WO (3) | WO2006077419A1 (https=) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL2256106T3 (pl) | 2003-07-22 | 2015-08-31 | Astex Therapeutics Ltd | Związki 3,4-pochodne 1h-pirazolu i ich zastosowanie jako kinazy zależne od cyklin (cdk) i modulatory kinazy syntazy glikogenu-3 (gsk-3) |
| TW200533657A (en) | 2004-02-17 | 2005-10-16 | Esteve Labor Dr | Substituted pyrazoline compounds, their preparation and use as medicaments |
| JP5475234B2 (ja) * | 2005-01-21 | 2014-04-16 | アステックス・セラピューティクス・リミテッド | 医薬化合物 |
| US8404718B2 (en) | 2005-01-21 | 2013-03-26 | Astex Therapeutics Limited | Combinations of pyrazole kinase inhibitors |
| US20080139620A1 (en) * | 2005-01-21 | 2008-06-12 | Astex Therapeutics Limited | Pyrazole Derivatives For The Inhibition Of Cdk's And Gsk's |
| AR052559A1 (es) * | 2005-01-21 | 2007-03-21 | Astex Therapeutics Ltd | Derivados de pirazol para inhibir cdk's y gsk's |
| MX2007008781A (es) * | 2005-01-21 | 2007-09-11 | Astex Therapeutics Ltd | Compuestos farmaceuticos. |
| KR20070107707A (ko) * | 2005-01-21 | 2007-11-07 | 아스텍스 테라퓨틱스 리미티드 | 피라졸 키나제 억제제와 추가 항종양제의 조합물 |
| AR054425A1 (es) | 2005-01-21 | 2007-06-27 | Astex Therapeutics Ltd | Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico. |
| US20090036607A1 (en) * | 2005-03-03 | 2009-02-05 | Mitsubishi Rayon Co., Ltd. | Polymer particle, resin composition containing same, and molded body |
| EP1743890A1 (en) | 2005-07-15 | 2007-01-17 | Laboratorios Del Dr. Esteve, S.A. | 4,5-Dihydro-1H-pyrazole derivatives, their preparation and use as medicaments |
| EP1743892A1 (en) | 2005-07-15 | 2007-01-17 | Laboratorios del Dr. Esteve S.A. | Substituted pyrazoline compounds, their preparation and use as medicaments |
| US7897589B2 (en) | 2005-07-15 | 2011-03-01 | Laboratorios Del Dr. Esteve, S.A. | Substituted pyrazoline compounds, their preparation and use as medicaments |
| EP2027109A1 (en) * | 2006-05-05 | 2009-02-25 | Astex Therapeutics Limited | 4- (2, 6-dichloro-benzoylamino) -1h-pyrazole-s-carboxylic acid (1-methanesulph0nyl-piperidin-4-yl) -amide for the treatment of cancer |
| WO2007129062A1 (en) * | 2006-05-08 | 2007-11-15 | Astex Therapeutics Limited | Pharmaceutical combinations of diazole derivatives for cancer treatment |
| WO2008007122A2 (en) * | 2006-07-14 | 2008-01-17 | Astex Therapeutics Limited | Combinations of pyrazole derivatives for the inhibition of cdks and gsk's |
| EP2049516A2 (en) * | 2006-07-14 | 2009-04-22 | Astex Therapeutics Limited | Pharmaceutical compounds |
| WO2008009954A1 (en) * | 2006-07-21 | 2008-01-24 | Astex Therapeutics Limited | Medical use of cyclin dependent kinases inhibitors |
| US20110172230A1 (en) * | 2006-08-23 | 2011-07-14 | Takahiro Ishii | Urea compound or salt thereof |
| WO2008044041A1 (en) | 2006-10-12 | 2008-04-17 | Astex Therapeutics Limited | Pharmaceutical combinations |
| AU2007316558A1 (en) * | 2006-11-09 | 2008-05-15 | Abbott Gmbh & Co. Kg | Pharmaceutical dosage form for oral administration of tyrosine kinase inhibitor |
| FR2908409B1 (fr) * | 2006-11-10 | 2009-01-09 | Sanofi Aventis Sa | Pyrazoles substituees,compositions les contenant,procede de fabrication et utilisation |
| FR2913018A1 (fr) * | 2007-02-23 | 2008-08-29 | Sanofi Aventis Sa | Solution solide amorphe contenant un derive de pyrazole-3-carboxamide sous forme amorphe et des excipients stabilisateurs |
| EP2267459A1 (en) * | 2009-06-25 | 2010-12-29 | Universite Pierre Et Marie Curie - Paris VI | Method for determining the susceptibility of a cell strain to drugs |
| WO2012148994A1 (en) * | 2011-04-25 | 2012-11-01 | Usher Iii Initiative | Pyrazolopyridazines and methods for treating retinal-degenerative diseases and hearing loss associated with usher syndrome |
| DE102011106990B3 (de) * | 2011-07-08 | 2013-01-03 | Technische Universität Darmstadt | Verbindungen als Glykogen Synthase Kinase 3 (GSK-3) Inhibitoren für die Behandlung von GSK-3-vermittelten Erkrankungen |
| BRPI1107312B1 (pt) | 2011-11-25 | 2021-09-08 | Universidade Federal De Santa Catarina | Composto de acil-hidrazona |
| CA2860250C (en) * | 2012-02-21 | 2020-11-10 | Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.P.A. | 1h-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors |
| US20150099645A1 (en) * | 2012-03-14 | 2015-04-09 | Stephen Marx | Means and methods for diagnostics and therapeutics of diseases |
| US9227976B2 (en) | 2012-10-25 | 2016-01-05 | Usher Iii Initiative, Inc. | Pyrazolopyridazines and methods for treating retinal-degenerative diseases and hearing loss associated with usher syndrome |
| US8765762B2 (en) | 2012-10-25 | 2014-07-01 | Usher III, Initiative, Inc. | Pyrazolopyridazines and methods for treating retinal-degerative diseases and hearing loss associated with usher syndrome |
| WO2014066835A1 (en) * | 2012-10-25 | 2014-05-01 | Usher Iii Initiative, Inc. | Pyrazolopyridazines and methods for treating retinal-degenerative diseases and hearing loss associated with usher syndrome |
| US9409895B2 (en) | 2012-12-19 | 2016-08-09 | Novartis Ag | Autotaxin inhibitors |
| HK1212348A1 (en) | 2012-12-19 | 2016-06-10 | Novartis Ag | Autotaxin inhibitors |
| US9603804B2 (en) | 2013-04-25 | 2017-03-28 | Kyorin Pharmaceutical Co., Ltd. | Solid pharmaceutical composition |
| WO2014179144A1 (en) * | 2013-04-29 | 2014-11-06 | E. I. Du Pont De Nemours And Company | Fungicidal heterocyclic compounds |
| EP2980088A1 (en) | 2014-07-28 | 2016-02-03 | Bayer Pharma Aktiengesellschaft | Amino-substituted isothiazoles |
| WO2015113927A1 (en) * | 2014-01-29 | 2015-08-06 | Bayer Pharma Aktiengesellschaft | Amino-substituted isothiazoles |
| JP2017528460A (ja) * | 2014-09-10 | 2017-09-28 | エピザイム インコーポレイテッド | 不可逆的smyd阻害剤としてのイソオキサゾールカルボキサミド |
| AU2015371251B2 (en) | 2014-12-23 | 2020-06-11 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
| HK1246645A1 (zh) | 2015-03-27 | 2018-09-14 | 达纳-法伯癌症研究所股份有限公司 | 细胞周期蛋白依赖性激酶的抑制剂 |
| TWI730959B (zh) | 2015-05-19 | 2021-06-21 | 英商葛蘭素史克智慧財產發展有限公司 | 作為激酶抑制劑之雜環醯胺 |
| WO2019188200A1 (ja) | 2018-03-27 | 2019-10-03 | ダイキン工業株式会社 | スルファミン酸リチウムの製造方法及び新規スルファミン酸リチウム |
| JP7161122B2 (ja) | 2018-03-27 | 2022-10-26 | ダイキン工業株式会社 | 電解液、電気化学デバイス、リチウムイオン二次電池及びモジュール |
| PL3761435T3 (pl) | 2018-03-27 | 2023-02-06 | Daikin Industries, Ltd. | Roztwór elektrolitu, urządzenie elektrochemiczne, litowo-jonowa bateria akumulatorowa, moduł oraz związek |
| US12187701B2 (en) | 2018-06-25 | 2025-01-07 | Dana-Farber Cancer Institute, Inc. | Taire family kinase inhibitors and uses thereof |
| JP7660063B2 (ja) | 2018-12-28 | 2025-04-10 | ダナ-ファーバー キャンサー インスティテュート, インコーポレイテッド | サイクリン依存性キナーゼ7のインヒビターおよびそれらの使用 |
| CN111848579B (zh) * | 2019-04-26 | 2023-11-14 | 君实润佳(上海)医药科技有限公司 | 4-(2,6-二氯苯甲酰氨基)-n-(4-哌啶基)-1h-吡唑-3-甲酰胺的前药 |
| IL299695A (en) | 2020-07-09 | 2023-03-01 | Usher Iii Initiative Inc | Treatment of cancer, inflammatory diseases and autoimmune diseases |
| AU2022271290A1 (en) | 2021-05-07 | 2023-11-23 | Kymera Therapeutics, Inc. | Cdk2 degraders and uses thereof |
| TW202320750A (zh) * | 2021-10-25 | 2023-06-01 | 香港商優領醫藥科技(香港)有限公司 | 含四氫呋喃多環類衍生物、其藥學上可接受的鹽及其製備方法和應用 |
| TW202337434A (zh) * | 2022-02-11 | 2023-10-01 | 美商傳達治療有限公司 | Cdk抑制劑及其使用方法 |
| WO2026024674A1 (en) | 2024-07-22 | 2026-01-29 | Genesis Therapeutics, Inc. | Methods of treating skp2-associated cancers |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4282361A (en) * | 1978-03-16 | 1981-08-04 | Massachusetts Institute Of Technology | Synthesis for 7-alkylamino-3-methylpyrazolo [4,3-d]pyrimidines |
| US5502068A (en) * | 1995-01-31 | 1996-03-26 | Synphar Laboratories, Inc. | Cyclopropylpyrroloindole-oligopeptide anticancer agents |
| JP2000504014A (ja) * | 1996-01-30 | 2000-04-04 | メルク エンド カンパニー インコーポレーテッド | ファルネシル―タンパク質転移酵素の阻害剤 |
| US6020357A (en) * | 1996-12-23 | 2000-02-01 | Dupont Pharmaceuticals Company | Nitrogen containing heteroaromatics as factor Xa inhibitors |
| US6632815B2 (en) * | 1999-09-17 | 2003-10-14 | Millennium Pharmaceuticals, Inc. | Inhibitors of factor Xa |
| US20040087798A1 (en) * | 2000-03-14 | 2004-05-06 | Akira Yamada | Novel amide compounds |
| US6455559B1 (en) * | 2001-07-19 | 2002-09-24 | Pharmacia Italia S.P.A. | Phenylacetamido-pyrazole derivatives, process for their preparation and their use as antitumor agents |
| JPWO2002074298A1 (ja) * | 2001-03-21 | 2004-07-08 | 小野薬品工業株式会社 | Il−6産生阻害剤 |
| GB0218625D0 (en) * | 2002-08-10 | 2002-09-18 | Astex Technology Ltd | Pharmaceutical compounds |
| US7169797B2 (en) * | 2003-02-14 | 2007-01-30 | Abbott Laboratories | Protein-tyrosine phosphatase inhibitors and uses thereof |
| US7320989B2 (en) * | 2003-02-28 | 2008-01-22 | Encysive Pharmaceuticals, Inc. | Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-II receptor antagonists |
| TWI372050B (en) * | 2003-07-03 | 2012-09-11 | Astex Therapeutics Ltd | (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles |
| PL2256106T3 (pl) * | 2003-07-22 | 2015-08-31 | Astex Therapeutics Ltd | Związki 3,4-pochodne 1h-pirazolu i ich zastosowanie jako kinazy zależne od cyklin (cdk) i modulatory kinazy syntazy glikogenu-3 (gsk-3) |
| US20080139620A1 (en) * | 2005-01-21 | 2008-06-12 | Astex Therapeutics Limited | Pyrazole Derivatives For The Inhibition Of Cdk's And Gsk's |
| KR20070107707A (ko) * | 2005-01-21 | 2007-11-07 | 아스텍스 테라퓨틱스 리미티드 | 피라졸 키나제 억제제와 추가 항종양제의 조합물 |
| JP5475234B2 (ja) * | 2005-01-21 | 2014-04-16 | アステックス・セラピューティクス・リミテッド | 医薬化合物 |
| AR054425A1 (es) * | 2005-01-21 | 2007-06-27 | Astex Therapeutics Ltd | Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico. |
| MX2007008781A (es) * | 2005-01-21 | 2007-09-11 | Astex Therapeutics Ltd | Compuestos farmaceuticos. |
| AR052559A1 (es) * | 2005-01-21 | 2007-03-21 | Astex Therapeutics Ltd | Derivados de pirazol para inhibir cdk's y gsk's |
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- 2006-01-20 CA CA002593468A patent/CA2593468A1/en not_active Abandoned
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- 2006-01-20 AU AU2006207311A patent/AU2006207311A1/en not_active Abandoned
- 2006-01-20 JP JP2007551740A patent/JP2008528466A/ja not_active Withdrawn
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- 2006-01-20 BR BRPI0606317-9A patent/BRPI0606317A2/pt not_active IP Right Cessation
- 2006-01-20 WO PCT/GB2006/000196 patent/WO2006077419A1/en not_active Ceased
- 2006-01-20 JP JP2007551739A patent/JP2008528465A/ja active Pending
- 2006-01-20 US US11/814,443 patent/US20080306069A1/en not_active Abandoned
- 2006-01-20 CA CA002593465A patent/CA2593465A1/en not_active Abandoned
- 2006-01-20 WO PCT/GB2006/000193 patent/WO2006077416A1/en not_active Ceased
- 2006-01-20 PE PE2006000080A patent/PE20061073A1/es not_active Application Discontinuation
- 2006-01-20 KR KR1020077018917A patent/KR20070098928A/ko not_active Withdrawn
- 2006-01-20 WO PCT/GB2006/000191 patent/WO2006077414A1/en not_active Ceased
- 2006-01-20 BR BRPI0606107-9A patent/BRPI0606107A2/pt not_active IP Right Cessation
- 2006-01-20 KR KR1020077018915A patent/KR20070107049A/ko not_active Withdrawn
- 2006-01-20 US US11/814,446 patent/US20080194562A1/en not_active Abandoned
- 2006-01-20 AU AU2006207313A patent/AU2006207313A1/en not_active Abandoned
- 2006-01-20 JP JP2007551742A patent/JP2008528467A/ja active Pending
- 2006-01-20 EP EP06709562A patent/EP1846395A1/en not_active Withdrawn
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- 2006-01-20 CA CA002593656A patent/CA2593656A1/en not_active Abandoned
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2007
- 2007-07-09 IL IL184499A patent/IL184499A0/en unknown
- 2007-07-09 IL IL184502A patent/IL184502A0/en unknown
- 2007-07-09 IL IL184503A patent/IL184503A0/en unknown
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- 2007-07-20 TN TNP2007000279A patent/TNSN07279A1/en unknown
- 2007-07-27 NO NO20073956A patent/NO20073956L/no not_active Application Discontinuation
- 2007-07-27 NO NO20073960A patent/NO20073960L/no not_active Application Discontinuation
- 2007-07-27 NO NO20073955A patent/NO20073955L/no not_active Application Discontinuation
- 2007-08-16 MA MA30145A patent/MA29255B1/fr unknown
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- 2007-08-16 MA MA30144A patent/MA29254B1/fr unknown
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