- High Turnover Pd/C Catalyst for Nitro Group Reductions in Water. One-Pot Sequences and Syntheses of Pharmaceutical Intermediates
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Commercially available Pd/C can be used as a catalyst for nitro group reductions with only 0.4 mol % Pd loading. The reaction can be performed using either silane as a transfer hydrogenating agent or simply a hydrogen balloon (μ1 atm pressure). With this technology, a series of nitro compounds was reduced to the desired amines in high chemical yields. Both the catalyst and surfactant were recycled several times without loss of reactivity.
- Gallou, Fabrice,Li, Xiaohan,Lipshutz, Bruce H.,Takale, Balaram S.,Thakore, Ruchita R.
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supporting information
p. 8114 - 8118
(2021/10/25)
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- BENZYLAMINE DERIVATIVES AS DDRS INHIBITORS
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The present invention relates to a compounds of general formula (I) inhibiting DDR1 and DDR2, particularly the invention relates to compounds that are benzylamine derivatives, methods of preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. The compounds of the invention may be useful in the treatment of diseases or conditions associated with a dysregulation of DDRs, in particular fibrosis.
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Page/Page column 63-64
(2021/12/08)
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- KINASE INHIBITORS AND USES THEREOF
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This invention described herein relates to compounds of general formula (I) : (I), in which variable groups are as defined herein, and to their preparation and use. Uses for the compounds and for compositions containing them include treatment of cancer and other diseases mediated by protein kinases, such as Bcr-Abl kinase, and mutants thereof, such as the T315I mutant.
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Page/Page column 44; 45
(2020/10/21)
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- Tyrosine kinase inhibitor
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The invention discloses a tyrosine kinase inhibitor, i.e., a compound represented by a formula (I) shown in the description for treating or preventing protein kinase related diseases and pharmaceutical salts or configurational isomers thereof, wherein substituents R1, R2 and R3 are as defined in the description. The invention further discloses a preparation method for the compound represented by the formula (I), pharmaceutical compositions and use of the compounds in preparation of drugs for treating or preventing the protein kinase related diseases.
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- 1H-1,8- NAPHTHYRIDIN-2ONES AS ANTI PROLIFERATIVE COMPOUNDS
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The present invention relates to novel antiproliferative1H-1, 8-naphthyridin-2-ones of the general formula (I) or pharmaceutically acceptable salts thereof: In which the variable groups are as defined herein, and their preparation and use in therapeutic treatment of disorders related to inhibition of tyrosine kinases in warm blooded animals. The compounds can overcome imatinib induced drug resistance.
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Page/Page column 28; 29
(2015/12/30)
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- Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-AblT315I mutant
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abstract A series of pyrimidine alkynyl derivatives were designed and synthesized as new Bcr-Abl inhibitors by hybriding the structural moieties from GNF-7, ponatinib and nilotinib. One of the most potent compounds 4e strongly suppresses Bcr-AblWT and Bcr-AblT315I kinase with IC50 values of 5.0 and 9.0 nM, and inhibits the proliferation of K562 and murine Ba/F3 cells ectopically expressing Bcr-AblT315I cells with IC50 values of 2 and 50 nM, respectively. It also displays good pharmacokinetics properties with an oral bioavailability of 35.3% and T1/2 value of 48.7 h, and demonstrates significantly suppression on tumor growth in xenografted mice of K562 and Ba/F3 cells expressing Bcr-AblT315I. These inhibitors may serve as lead compounds for further developing new anticancer drugs overcoming the clinically acquired resistance against current Bcr-Abl inhibitors.
- Lu, Xiaoyun,Zhang, Zhang,Ren, Xiaomei,Pan, Xiaofeng,Wang, Deping,Zhuang, Xiaoxi,Luo, Jingfeng,Yu, Rongmin,Ding, Ke
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supporting information
p. 3458 - 3463
(2015/08/06)
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- Protein Kinase Inhibitors
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The present invention relates to compounds of Formula I: as well as pharmaceutically acceptable salts, hydrates, isomers, or solvates thereof, wherein the variables are described herein. The present invention further relates to pharmaceutical compositions which comprise the compounds of Formula I, and to methods for inhibiting protein kinase and methods of treating diseases, such as cancers, inflammation.
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- HETEROCYCLIC ALKYNYL BENZENE COMPOUNDS AND MEDICAL COMPOSITIONS AND USES THEREOF
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The heterocyclic alkynyl benzene compounds of formula (I), their pharmaceutically acceptable salts and stereoisomers thereof, as well as application in preparing drugs for preventing or treating tumors. The compounds can overcome the clinically induced resistance against Gleevec.
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Paragraph 0050; 0051
(2013/06/05)
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- HETEROCYCLIC ALKYNYL BENZENE COMPOUNDS AND MEDICAL COMPOSITIONS AND USES THEREOF
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The heterocyclic alkynyl benzene compounds of formula (I), their pharmaceutically acceptable salts and stereoisomers thereof, as well as application in preparing drugs for preventing or treating tumors. The compounds can overcome the clinically induced resistance against Gleevec.
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Paragraph 0125; 0129-0131
(2013/08/14)
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- METHODS AND COMPOSITIONS FOR RAF KINASE MEDIATED DISEASES
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The invention discloses methods and compositions for treating or preventing RAF kinase mediated diseases or conditions by administering a compound of Formula 1: or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the variables are defined as herein.
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- 9-(Arenethenyl)purines as dual Src/Abl kinase inhibitors targeting the inactive conformation: Design, synthesis, and biological evaluation
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A novel series of potent dual Src/Abl kinase inhibitors based on a 9-(arenethenyl)purine core has been identified. Unlike traditional dual Src/Abl inhibitors targeting the active enzyme conformation, these inhibitors bind to the inactive, DFG-out conformation of both kinases. Extensive SAR studies led to the discovery of potent and orally bioavailable inhibitors, some of which demonstrated in vivo efficacy. Once-daily oral administration of inhibitor 9i (AP24226) significantly prolonged the survival of mice injected intravenously with wild type Bcr-Abl expressing Ba/F3 cells at a dose of 10 mg/kg. In a separate model, oral administration of 9i to mice bearing subcutaneous xenografts of Src Y527F expressing NIH 3T3 cells elicited dose-dependent tumor shrinkage with complete tumor regression observed at the highest dose. Notably, several inhibitors (e.g., 14a, AP24163) exhibited modest cellular potency (IC50 = 300-400 nM) against the Bcr-Abl mutant T315I, a variant resistant to all currently marketed therapies for chronic myeloid leukemia. 2009 American Chemical Society.
- Huang, Wei-Sheng,Zhu, Xiaotian,Wang, Yihan,Azam, Mohammad,Wen, David,Sundaramoorthi, Raji,Thomas, R. Mathew,Liu, Shuangying,Banda, Geetha,Lentini, Scott P.,Das, Sasmita,Xu, Qihong,Keats, Jeff,Wang, Frank,Wardwell, Scott,Ning, Yaoyu,Snodgrass, Joseph T.,Broudy, Marc I.,Russian, Karin,Daley, George Q.,Iuliucci, John,Dalgarno, David C.,Clackson, Tim,Sawyer, Tomi K.,Shakespeare, William C.
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scheme or table
p. 4743 - 4756
(2010/03/03)
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- An efficient synthesis of nilotinib (AMN107)
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A concise synthesis of AMN107, a compound currently undergoing several phase II/III clinical trials for chronic myelogenous leukemia is described. The new procedure reduces the number of synthetic steps from eight to four, with an overall yield of 65%. Georg Thieme Verlag Stuttgart.
- Huang, Wei-Sheng,Shakespeare, William C.
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p. 2121 - 2124
(2008/03/28)
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- BICYCLIC HETEROARYL COMPOUNDS
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This invention relates to compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.
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Page/Page column 57
(2008/06/13)
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- UNSATURATED HETEROCYCLIC DERIVATIVES
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This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
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Page/Page column 38
(2008/06/13)
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