113100-86-0Relevant articles and documents
Synthesis method of methyl 4-(3-bromopropyl)benzoate
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Paragraph 0028-0042, (2021/02/06)
The invention provides a synthetic method of methyl 4-(3-bromopropyl)benzoate, and relates to the field of medicinal chemistry. The invention provides a new scheme for synthesizing methyl 4-(3-bromopropyl)benzoate from 1-bromo-3-phenylpropane through a two-step one-pot method, and provides a new synthesis route for preparation and synthesis of methyl 4-(3-bromopropyl)benzoate. Moreover, accordingto the synthesis scheme, common raw materials are adopted as reactants, the reaction conditions are proper, the final product is synthesized with the cost remarkably reduced compared with the prior art, the preparation process is simple, the cost is low, large-scale production can be achieved, and a synthesis thought is provided for synthesis of the derivative of the compound.
Structure-Based Design of Dual-Acting Compounds Targeting Adenosine A2AReceptor and Histone Deacetylase as Novel Tumor Immunotherapeutic Agents
Yan, Wenzhong,Ling, Lijun,Wu, Yiran,Yang, Kexin,Liu, Ruiquan,Zhang, Jinfeng,Zhao, Simeng,Zhong, Guisheng,Zhao, Suwen,Jiang, Hualiang,Xie, Chengying,Cheng, Jianjun
, p. 16573 - 16597 (2021/12/02)
Adenosine is an immunosuppressive factor in the tumor microenvironment mainly through activation of the A2A adenosine receptor (A2AR), which is a mechanism hijacked by tumors to escape immune surveillance. Small-molecule A2AR antagonists are being evaluat
A nitric oxide donor nature of the benzofuran compounds (by machine translation)
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Paragraph 0067-0068, (2017/04/20)
The invention discloses a benzofuran compound with nitrous oxide donor property. The benzofuran compound is a compound shown by a general formula (I) or a pharmaceutically acceptable salt thereof, wherein in the formula, R1 or R2 represents independent hy
Discovery of highly selective EP4 receptor agonists that stimulate new bone formation and restore bone mass in ovariectomized rats
Cameron, Kimberly O.,Lefker, Bruce A.,Chu-Moyer, Margaret Y.,Crawford, David T.,Jardine, Paul DaSilva,DeNinno, Shari L.,Gilbert, Sandra,Grasser, William A.,Ke, HuaZhu,Lu, Bihong,Owen, Thomas A.,Paralkar, Vishwas M.,Qi, Hong,Scott, Dennis O.,Thompson, David D.,Tjoa, Christina M.,Zawistoski, Michael P.
, p. 1799 - 1802 (2007/10/03)
Heptanoic acid lactams, exemplified by 2, were identified as highly selective EP4 agonists via high throughput screening. Lead optimization led to the identification of lactams with a 30-fold increase in EP4 potency in vitro. Compounds demonstrated robust
EP4 receptor selective agonists in the treatment of osteoporosis
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, (2008/06/13)
This invention is directed to EP4 receptor selective prostaglandin agonists of the Formula I, wherein R2, X, Z and Q are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds. This invention is also directed to methods of treating conditions which present with low bone mass, particularly osteoporosis, frailty, an osteoporotic fracture, a bone defect, childhood idiopathic bone loss, alveolar bone loss, mandibular bone loss, bone fracture, osteotomy, bone loss associated with periodontitis, or prosthetic ingrowth in a mammal comprising administering those compounds.
Novel nonsteroidal selective estrogen receptor modulators. Carbon and heteroatom replacement of oxygen in the ethoxypiperidine region of raloxifene
Schmid, Christopher R.,Sluka, James P.,Duke, Kristen M.,Glasebrook, Andrew W.
, p. 523 - 528 (2007/10/03)
Compounds were synthesized where oxygen in the ethoxypiperidine region of raloxifene is replaced with carbon, sulfur, or nitrogen linkages. Thia- and aza-substituted compounds were prepared by novel methodology. The compounds were evaluated in vitro as se
Protein structure-based design, synthesis, and biological evaluation of 5-thia-2,6-diamino-4(3H)-oxopyrimidines: Potent inhibitors of glycinamide ribonucleotide transformylase with potent cell growth inhibition
Varney, Michael D.,Palmer, Cindy L.,Romines III, William H.,Boritzki, Theodore,Margosiak, Stephen A.,Almassy, Robert,Janson, Cheryl A.,Bartlett, Charlotte,Howland, Eleanor J.,Ferre, Rosanne
, p. 2502 - 2524 (2007/10/03)
The design, synthesis, biochemical, and biological evaluation of a novel series of 5-thia-2,6-diamino-4(3H)-oxopyrimidine inhibitors of glycinamide ribonucleotide transformylase (GART) are described. The compounds were designed using the X-ray crystal structure of human GART. The monocyclic 5- thiapyrimidinones were synthesized by coupling an alkyl thiol with 5-bromo- 2,6-diamino-4(3H)-pyrimidinone, 20. The bicyclic compounds were prepared in both racemic and diastereomerically pure forms using two distinct synthetic routes. The compounds were found to have human GART K(i)s ranging from 30 μM to 2 nM. The compounds inhibited the growth of both L1210 and CCRF-CEM cells in culture with potencies down to the low nanomolar range and were found to be selective for the de hove purine biosynthesis pathway. The most potent inhibitors had 2,5-disubstituted thiophene rings attached to the glutamate moiety. Placement of a methyl substituent at the 4-position of the thiophene ring to give compounds 10, 18, and 19 resulted in inhibitors with significantly decreased mFBP affinity.
Certain arylalkyl or pyridylalkyl hydroxamates useful for treating allergies and asthma
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, (2008/06/13)
Arylhydroxamates are provided having the structure STR1 wherein R1 is hydrogen, lower alkyl, aryl, lower alkenyl, cycloalkyl, or aralkyl; R2 is hydrogen, lower alkyl, aryl, cycloalkyl, alkanoyl or aroyl; m is 2 to 8; and STR2 wherein R3 is OH, COOH STR3 These compounds are useful as inhibitors of Δ5 -lipoxygenase and as such are useful as antiallergy agents.
