- Regioselective titanium tetrachloride mediated five membered hetero-cyclisations
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Highly regioselective titanium IV mediated, Dieckmann type cyclisation in the synthesis of 5-membered nitrogen and sulfur heterocycles is described.
- Deshmukh,Gangakhedkar,Sampath Kumar
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- An aza-nucleoside, fragment-like inhibitor of the DNA repair enzyme alkyladenine glycosylase (AAG)
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The DNA repair enzyme AAG has been shown in mice to promote tissue necrosis in response to ischaemic reperfusion or treatment with alkylating agents. A chemical probe inhibitor is required for investigations of the biological mechanism causing this phenomenon and as a lead for drugs that are potentially protective against tissue damage from organ failure and transplantation, and alkylative chemotherapy. Herein, we describe the rationale behind the choice of arylmethylpyrrolidines as appropriate aza-nucleoside mimics for an inhibitor followed by their synthesis and the first use of a microplate-based assay for quantification of their inhibition of AAG. We finally report the discovery of an imidazol-4-ylmethylpyrrolidine as a fragment-sized, weak inhibitor of AAG.
- Al Yahyaei, Balqees,Chu, Shuyu,Elliott, Ruan M.,Howlin, Brendan J.,Imperato, Manuel,Lopez, Arnaud,Mas Claret, Eduard,Meira, Lisiane B.,Whelligan, Daniel K.
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- Pyrrolidine [3,4-d] pyrimidine derivatives, preparation method and its application
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The invention discloses a pyrrolidine[3,4-d]pyrimidine derivative and a preparation method and an application thereof. The pyrrolidine[3,4-d]pyrimidine derivative is an inhibitor of a type I insulin-like growth factor receptor (IGF-1R), and has a good IGF-1R inhibiting function and a good cancer cell proliferation inhibiting function, so that the pyrrolidine[3,4-d]pyrimidine derivative can be taken as a therapeutic agent for treating tumors and relevant diseases.
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Paragraph 0102-0104
(2016/12/01)
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- BICYCLIC PYRIMIDINE DERIVATIVES
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[wherein m and n may be the same or different and each represents an integer of 1 to 3 wherein m + n is 4 or less; R1 represents NR4R5 (wherein R4 and R5 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl or the like); R2 represents the above Formula (II), Formula (IV) or the like; A represents a single bond, -C(=O)-, -SO2-, -OC(=O)- or the like; and R3 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aralkyl or the like]ψBicyclic pyrimidine derivatives represented by the above Formula (I), or quaternary ammonium salts thereof, or pharmaceutically acceptable salts thereof, or the like, are provided. These have anti-inflammatory activities or modulation activities on the functions of TARC and/or MDC and are useful for treating and/or preventing a disease which is related to T cells, such as an allergic disease, an autoimmune disease or transplant rejection.
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Page/Page column 302
(2008/06/13)
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- 6,7-dihydropyrrol[3,4-c]pyrido[2,3-d]pyrimidine derivatives
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The present invention concerns compounds of the formula: STR1 wherein R is a lower alkyl group, an aryl group or an alkylaryl group and X and Y are the same or different, and each is OH, NH2, or SH. The aryl group or the aryl moiety of the alkylaryl group may be unsubstituted, monosubstituted, disubstituted or trisubstituted. If substituted, each substituent may independently be an alkyl group, an alkyloxy group or a halogen. The present invention also provides methods for synthesizing the compounds described above.
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- Benzopyrans and intermediates for the preparation of pyrrolo benzopyrans
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Novel 7-alkyl-(and 7-cycloalkyl-loweralkyl)9-hydroxy-4,4-di-lower-alkyl-1,2,3,4-tetrahydro-[1]benzopyrano[3,4-c]pyrroles; 7-alkyl-(and 7-cycloalkyl-lower-alkyl)9-hydroxy-4,4-di-lower alkyl-1,2,3,4,3a,9b-hexahydro[1]benzopyrano[3,4-c]pyrroles, and certain ester and ether derivatives thereof. These compounds exhibit CNS activity, and are useful as sedatives or tranquilizers.
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