247569-07-9Relevant academic research and scientific papers
Pyrrolidine integrin regulator and application thereof
-
Paragraph 0254-0258, (2021/09/08)
Disclosed are a compound as represented by formula I, and a racemate, a stereoisomer, a tautomer, an isotopic marker, a nitrogen oxide, a solvate, a polymorph, a metabolite, an ester, and a prodrug thereof or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising same, a preparation method therefor, and the medical use thereof. The structure of formula I is as follows:
Economical synthesis of tert-butyl (S)-3-aminopyrrolidine-1-carboxylate from L-aspartic acid
Han, Zhi-Jian,Li, Yang-Bing,Gu, Bao-Hong,Li, Yu-Min,Chen, Hao
, p. 2452 - 2456 (2018/10/20)
3-Aminopyrrolidine building block was used as the intermediate for many pharmaceutically active substances. Starting from L-aspartic acid, optically active (S)-tert-butyl-3-aminopyrrolidine-1-carboxylate was synthesized, and the reaction conditions were optimized in each step. The procedure of each step was discussed in detail and could be useful for the industrial preparation. This process was featured by readily available starting material, mild reaction conditions, easy work-up, and economy.
Discovery of quinazoline-2,4(1: H,3 H)-dione derivatives as novel PARP-1/2 inhibitors: Design, synthesis and their antitumor activity
Zhou, Jie,Ji, Ming,Yao, Haiping,Cao, Ran,Zhao, Hailong,Wang, Xiaoyu,Chen, Xiaoguang,Xu, Bailing
supporting information, p. 3189 - 3202 (2018/05/15)
Novel quinazoline-2,4(1H,3H)-dione derivatives bearing a 3-amino pyrrolidine moiety were designed and synthesized as PARP-1/2 inhibitors. Structure-activity relationships were examined which revealed a number of potent PARP-1/2 inhibitors with moderate se
3-amino nafoxidine-containing quinazoline ketone PARP (Poly Adenosine Diphosphate Ribose Polymerase)-1/2 inhibitor as well as preparation method, medicinal composition and application thereof
-
Paragraph 0516; 0519; 0520; 0549; 0552; 0553, (2018/11/22)
The invention discloses a novel 3-amino nafoxidine-containing quinazoline-2,4(1H, 3H)-diketone PARP-1/2 (Poly Adenosine Diphosphate Ribose Polymerase) inhibitor as well as a preparation method, a medicinal composition and application thereof. Specifically, the invention relates to a 3-amino nafoxidine-containing quinazoline-2,4(1H, 3H)-diketone derivative and a medicinal salt thereof of formula (I) as shown in the specification, a preparation method thereof, a composition with one or more such compounds, preparation of the compounds, and application thereof in preparing medicines for preventing and/or treating PARP-1/2 related diseases.
Discovery of 2-substituted 1H-benzo[d]immidazole-4-carboxamide derivatives as novel poly(ADP-ribose)polymerase-1 inhibitors with in?vivo anti-tumor activity
Zhou, Jie,Ji, Ming,Zhu, Zhixiang,Cao, Ran,Chen, Xiaoguang,Xu, Bailing
supporting information, p. 26 - 41 (2017/03/23)
Novel 1H-benzo[d]immidazole-4-carboxamide derivatives bearing five-membered or six-membered N-heterocyclic moieties at the 2-position were designed and synthesized as PARP-1 inhibitors. Structure-activity relationships were conducted and led to a number of potent PARP-1 inhibitors having IC50 values in the single or double digit nanomolar level. Some potent PARP-1 inhibitors also had similar inhibitory activities against PARP-2. Among all the synthesized compounds, compound 10a and 11e displayed strong potentiation effects on temozolomide (TMZ) in MX-1?cells (PF50?=?7.10, PF50?=?4.17). In?vivo tumor growth inhibition was investigated using compound 10a in combination with TMZ, and it was demonstrated that compound 10a could strongly potentiate the cytotoxicity of TMZ in MX-1 xenograft tumor model. Two co-crystal structures of compounds 11b and 15e complexed with PARP-1 were achieved and demonstrated a unique binding mode of these benzo-imidazole derivatives.
HETEROCYCLIC PYRAZOLE-CARBOXAMIDES AS P2Y12 ANTAGONISTS
-
Page/Page column 125, (2009/07/25)
The present invention relates to compounds of the formula I, wherein R1; R2; Z; A; B; D; Q; J; V; G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
AZACYCLYLBENZAMIDE DERIVATIVES AS HISTAMINE-3 ANTAGONISTS
-
Page/Page column 42, (2009/01/20)
The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor
MUSCARINIC RECEPTOR AGONISTS THAT ARE EFFECTIVE IN THE TREATMENT OF PAIN, ALZHEIMER'S DISEASE AND SCHIZOPHRENIA
-
Page/Page column 75-76, (2008/06/13)
Compounds of Formula IA, or pharmaceutically acceptable salts thereof: IA wherein G1, G2, G3, G4, R1, R2, X, Y, Z and n are as defined in the specification as well as salts and pharmaceutic
A flexible carbanionic approach to protected trans-(2R,3S)-2-substituted 3-aminopyrrolidines: Application to the asymmetric synthesis of (+)-absouline
Tang, Tian,Ruan, Yuan-Ping,Ye, Jian-Liang,Huang, Pei-Qiang
, p. 231 - 234 (2007/10/03)
Based on the use of phenyl thioether (3S)-7 as a synthetic equivalent to the N- and α-dianions (3S)-2a, a new carbanionic approach to trans-(2R,3S)-2-substituted 3-aminopyrrolidines (10) is described. Application of the method to the asymmetric synthesis
Process for the manufacture of 3-amino-pyrrolidine derivatives
-
Page 5, (2008/06/13)
The invention is concerned with a process for the manufacture of 3-amino-pyrrolidine derivatives of the formula wherein R1 signifies hydrogen or an amino protecting group; Z signifies hydrogen or an amino protecting group; and * represents a center of chirality. 3-Amino-pyrrolidine derivatives, especially optically active 3-amino-pyrrolidine derivatives, are intermediates for the production of agrochemicals and of pharmaceutically active substances such as, for example, of vinylpyrrolidinone-cephalosporin derivatives.
