- Pyrrolopyrazole derivative and preparation method and medical application thereof
-
The invention relates to a pyrrolopyrazole derivative and a preparation method and a medical application thereof. Specifically, the invention relates to a new pyrrolopyrazole derivative as shown in ageneral formula (I), a preparation method of the pyrrolopyrazole derivative and application of the pyrrolopyrazole derivative or a pharmaceutical composition containing the pyrrolopyrazole derivativeas a therapeutic agent, particularly as a gastric acid secretion inhibitor and potassium ion competitive acid blockers (P-CABs) in biological medicines, wherein substituents (R1, R2, R3 and R4) and groups (X) in the general formula (I) are the same as defined in the specification.
- -
-
Paragraph 0102; 0104
(2021/02/05)
-
- Identification and structure–activity relationship exploration of uracil-based benzoic acid and ester derivatives as novel dipeptidyl Peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus
-
Our previously reported carboxyl-containing DPP-4 inhibitors were highly potent but were poorly bioavailable. Esters of the carboxyl analogs exhibited a significant DPP-4 potency loss albeit with enhanced oral absorption. Herein, we described identificati
- Deng, Xiaoyan,Jiang, Neng,Jiang, Weizhe,Li, Qing,Meng, Liuwei,Xing, Junhao,Xu, Yanjun
-
-
- MODULATORS OF MAS-RELATED G-PROTEIN RECEPTOR X4 AND RELATED PRODUCTS AND METHODS
-
Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4 dependent condition more specifically, by contacting the MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having the structure of Formula (I): (I) or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein n, x, A, Q1, Q2, Z, R, R1, R2, R3, R4 and R5 are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.
- -
-
Page/Page column 110; 117
(2020/10/18)
-
- Quinazoline diketone salt compound containing piperazinone as well as preparation method, pharmaceutical composition and application thereof
-
The invention relates to a piperazinone-containing quinazoline-2,4-diketone salt compound serving as a PARP1/2 inhibitor, a preparation method thereof, a pharmaceutical composition containing the compound, and application of the compound serving as a drug, particularly serving as an antitumor drug or serving as a tumor drug sensitizer to be combined with the antitumor drug.
- -
-
Paragraph 0075-0078
(2020/07/02)
-
- WDR5-MLL1 INHIBITORS AND MODULATORS
-
Benzamides and picolinamides that are meta-substituted with imino-, guanidino-, or heterocycle-containing groups disrupt the WDR5-MLL1 protein-protein interaction, and have use in pharmaceutical compositions and in treating proliferative disorders and conditions in a subject, such as cancer.
- -
-
Paragraph 0998-0999
(2020/03/02)
-
- Optimization of the benzamide fragment targeting the S2′ site leads to potent dipeptidyl peptidase-IV inhibitors
-
Our recently successful identification of benzoic acid-based DPP-4 inhibitors spurs the further quest for in-depth structure-activity relationships (SAR) study in S2′ site DPP-4. Thus novel benzamide fragments were designed to target the S
- Deng, Xiaoyan,Wang, Na,Meng, Liuwei,Zhou, Siru,Huang, Junli,Xing, Junhao,He, Linhong,Jiang, Weizhe,Li, Qing
-
-
- QUINAZOLINE-2,4-DIONE DERIVATIVES AS PARP INHIBITORS
-
The present invention relates to compounds of formula (I) and compositions containing said compounds acting as PARP (Poly (ADP- ribose) polymerase) inhibitors. Moreover, the present invention provides processes for the preparation of the disclosed compounds, as well as methods of using them, for instance as a medicine, in particular for the treatment of cell proliferative disorders, such as cancer.
- -
-
Page/Page column 48-49
(2020/11/30)
-
- Discovery of quinazoline-2,4(1: H,3 H)-dione derivatives as novel PARP-1/2 inhibitors: Design, synthesis and their antitumor activity
-
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
- Zhou, Jie,Ji, Ming,Yao, Haiping,Cao, Ran,Zhao, Hailong,Wang, Xiaoyu,Chen, Xiaoguang,Xu, Bailing
-
supporting information
p. 3189 - 3202
(2018/05/15)
-
- 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
-
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.
- -
-
Paragraph 0245; 0247; 0248
(2018/11/22)
-
- Containing piperazinone quinazoline ketone PARP - 1/2 inhibitor and its preparation method, pharmaceutical composition and use thereof (by machine translation)
-
The invention discloses a new class of containing piperazinone quinazoline - 2, 4 (1 H, 3 H) - dione PARP - 1/2 inhibitor, and its preparation and pharmaceutical composition and use. Specifically, the invention relates to the general formula I shown containing of the piperazinone quinazoline - 2, 4 (1 H, 3 H) - dione derivatives and their pharmaceutically acceptable salt, and its preparation method, comprising one or more of the compounds of the composition, and the compounds in the preparation, the prevention and/or treatment with PARP - 1/2 of a disease associated with the use of the medicament. (by machine translation)
- -
-
Paragraph 0137; 0138
(2017/09/08)
-
- Quinazolinone PARP-1 inhibitors, medicinal composition containing inhibitors, and antitumor use of inhibitors
-
The invention discloses quinazolinyl-2,4(1H,3H)-dione PARP-1 inhibitors, and a preparation method, a medicinal composition and a use thereof. The invention concretely relates to quinazolinyl-2,4(1H,3H)-dione derivatives represented by general formula I, a medicinal salt and a preparation method thereof, a composition containing one or more of the compounds, and a use of the compounds in the preparation of tumor prevention and/or treatment medicines.
- -
-
Paragraph 0128; 0129; 0130
(2016/10/08)
-
- COMPOUNDS ACTIVE TOWARDS BROMODOMAINS
-
Disclosed are compounds towards bromodomains, pharmaceutical compositions containing the compounds and use of the compounds in therapy.
- -
-
-
- QUINAZOLINEDIONES AND THEIR USE
-
The present invention discloses compounds of formula (I), or pharmaceutically acceptable salts or prodrugs thereof, which inhibit the poly(ADP-ribose) polymerases (PARP) and therefore are useful for treating diseases, disorders, and conditions related to PARP. The present invention also discloses pharmaceutical compositions comprising a compound of formula (I), and methods of using such compounds to inhibit PARP enzymes, and to treat diseases, disorders, and conditions related to PARP.
- -
-
Page/Page column 35; 36
(2012/10/07)
-
- Design, synthesis and identification of novel colchicine-derived immunosuppressant
-
Synthesis and biological evaluation of various colchicine analogues through the mixed-lymphocyte reaction (MLR), lymphoproliferation, and inhibitory effects on the inflammatory genes are described. In addition, a new series of immunosuppressive agents developed on the structural basis of colchicine, as well as their structure-activity relationships is reported. The most potent analogue 20a exhibited an excellent immunosuppressive activity on in vivo skin-allograft model, which is comparable to that of cyclosporin A.
- Chang, Dong-Jo,Yoon, Eun-Young,Lee, Geon-Bong,Kim, Soon-Ok,Kim, Wan-Joo,Kim, Young-Myeong,Jung, Jong-Wha,An, Hongchan,Suh, Young-Ger
-
scheme or table
p. 4416 - 4420
(2010/04/05)
-
- ANTIVIRAL COMPOUNDS AND USE THEREOF
-
The invention relates to compounds, pharmaceutical compositions and methods useful for treating viral infection.
- -
-
Page/Page column 29
(2009/12/02)
-
- 8-OXOADENINE COMPOUND
-
An 8-oxoadenine compound useful as an immuno-modulator having specific activity against Th1/Th2, specifically a prophylactic and therapeutic agent for a topical application for allergic diseases, viral siseases and cancers, which is represented by the following formula (1): , wherein A is a group of a formula represented by the formula (2): , wherein R2 is a substituted or unsubstituted alkyl group and so on, R3 is hydrogen atom or an alkyl group, R is a halogen atom and so on, n is 0-2, X1 is oxygen atom, Z is straight or branched chain alkylene, and R1 is an alkyl group which is optionally substituted by hydroxy group, an alkoxy group, alkoxycarbonyl group and so on, or its pharmaceutically acceptable salt.
- -
-
Page/Page column 142
(2010/11/24)
-
- QUINAZOLINONE DERIVATIVES AND THEIR USE AS B-RAF INHIBITORS
-
The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.
- -
-
Page/Page column 81-82
(2008/06/13)
-
- NOVEL ADENINE COMPOUND AND USE THEREOF
-
A drug for topically administration which is effective as an antiallergic agent. The drug for topically administration contains as an active ingredient an adenine compound represented by the general formula (1): [wherein ring A represents a 6 to 10 membered, mono or bicyclic, aromatic hydrocarbon or a 5 to 10 membered, mono or bicyclic, aromatic heterocycle containing one to three heteroatoms selected among 0 to 2 nitrogen atoms, 0 or 1 oxygen atom, and 0 or 1 sulfur atom; n is an integer of 0 to 2; m is an integer of 0 to 2; R represents halogeno, (un)substituted alkyl, etc.; X1 represents oxygen, sulfur, NR1 (R1 represents hydrogen or alkyl), or a single bond; Y1 represents a single bond, alkylene; etc.; Y2 represents a single bond, alkylene, etc.; Z represents alkylene; and at least one of Q1 and Q2 represents -COOR10 (wherein R10 represents (un)substituted alkyl, etc.), etc.] or a pharmaceutically acceptable salt of the compound.
- -
-
Page/Page column 29
(2010/02/12)
-
- N-substituted peptidyl nitriles as cysteine cathepsin inhibitors
-
Compounds of the formula (I), wherein R1 is aryl or biaryl; R2 is aryl-lower alkyl, biaryl-lower alkyl, benzo-fused cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, aryloxy-lower alkyl, or aryl-C2-C7/sub
- -
-
-
- Superoxide dismutase mimetics: synthesis and structure-activity relationship study of MnTBAP analogues.
-
Carboxylic ester and amide-substituted analogues of [5,10,15,20-tetrakis(4-carboxyphenyl)-porphyrinato]manganese(III) chloride (MnTBAP) were synthesized and assayed as potential superoxide dismutase (SOD) mimetics. The tetraester analogues 4a and 4b were
- Gauuan, Polivina Jolicia F,Trova, Michael P,Gregor-Boros, Livia,Bocckino, Stephen B,Crapo, James D,Day, Brian J
-
p. 3013 - 3021
(2007/10/03)
-
- Unsymmetrical cyclic ureas as HIV-1 protease inhibitors: Novel biaryl indazoles as P2/P2' substituents
-
The preparation of unsymmetrical cyclic ureas bearing novel biaryl indazoles as P2/P2' substituents was undertaken, utilizing a Suzuki coupling reaction as the key step. Compound 6i was equipotent to the lead compound of the series SE063.
- Patel, Mona,Rodgers, James D.,McHugh Jr., Robert J.,Johnson, Barry L.,Cordova, Beverly C.,Klabe, Ronald M.,Bacheler, Lee T.,Erickson-Viitanen, Susan,Soo S, Ko
-
p. 3217 - 3220
(2007/10/03)
-
