- 1,5,7-TRISUBSTITUTED ISOQUINOLINE DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF IN MEDICINES
-
The present disclosure relates to 1,5,7-trisubstituted isoquinoline derivatives, their preparation and pharmaceutical use. In particular, the present disclosure discloses a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, and a preparation method and use thereof. The definitions of the groups in the formula can be found in the specification and claims.
- -
-
Paragraph 0150; 0181-0182; 0203; 0205
(2020/08/30)
-
- Synthetic method of 4-(n-azetidin -2-3-)-1- one-methyl piperazinedione dihydrochloride (by machine translation)
-
The synthesis method provided by the invention, comprises 3 - the following steps: 4 - (of: reacting ;4) sodium hydride) - 1 - with tert-butyl carboxylate and methyl iodomethane, 3 - and. the. method disclosed by the invention, can be used for the reactio
- -
-
Paragraph 0032; 0035-0036; 0042; 0045-0046; 0051; 0054-0055
(2019/12/29)
-
- 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 0165; 0166
(2017/09/08)
-
- Discovery of DA-1229: A potent, long acting dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes
-
A series of β-amino amide containing substituted piperazine-2-one derivatives was synthesized and evaluated as inhibitors of dipeptidyl pepdidase-4 (DPP-4) for the treatment of type 2 diabetes. As results of intensive SAR study of the series, (R)-4-[(R)-3-amino-4-(2,4,5-trifluorophenyl)- butanoyl]-3-(t-butoxymethyl)-piperazin-2-one (DA-1229) displayed potent DPP-4 inhibition pattern in several animal models, was selected for clinical development.
- Kim, Heung Jae,Kwak, Woo Young,Min, Jong Pil,Lee, Jae Young,Yoon, Tae Hyun,Kim, Ha Dong,Shin, Chang Yell,Kim, Mi Kyung,Choi, Song Hyen,Kim, Hae Sun,Yang, Eun Kyoung,Cheong, Ye Hwang,Chae, Yu Na,Park, Kyung Jin,Jang, Ji Myun,Choi, Soo Jung,Son, Moon Ho,Kim, Soon Hoe,Yoo, Moohi,Lee, Bong Jin
-
scheme or table
p. 3809 - 3812
(2011/07/31)
-
- PYRAZOLE DERIVATIVE
-
A compound represented by Formula (I): wherein Ar1 represents Formula (II): Ar2 represents a 5- or 6-membered aromatic heterocyclic group which may be substituted; and X represents Formula (III): a salt thereof, or a solvate of the compound or the salt. A potent platelet aggregation suppressant which does not inhibit COX-1 and COX-2 is provided.
- -
-
Page/Page column 63
(2010/11/27)
-
- HIV INTEGRASE INHIBITORS
-
Substituted hydroxytetrahydropyrrolopyrazinone and substituted hydroxytetrahydro-pyrazolopyrazinone compounds of Formula (I) are inhibitors of HIV integrase and inhibitors of HIV replication: (I) wherein R1, R2, R3, R
- -
-
Page/Page column 30
(2008/06/13)
-
- HIV INTEGRASE INHIBITORS
-
Hydroxy-substituted pyrazinopyrrolopyridazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I) wherein R1, R2, R3, R4, R5, R6 and R7 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
- -
-
-
- HYDROXY PYRIDOPYRROLOPYRAZINE DIONE COMPOUNDS USEFUL AS HIV INTEGRASE INHIBITORS
-
Hydroxy-substituted pyridopyrrolopyrazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I): (I) wherein a, b, A, B, R1, R2, R3, R4, R5, R6, R7 and R8 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
- -
-
Page/Page column 95
(2010/02/11)
-
- Piperazinonephenyloxazolidinone derivatives and their use as antibacterial agents
-
PCT No. PCT/GB97/00169 Sec. 371 Date Jul. 27, 1998 Sec. 102(e) Date Jul. 27, 1998 PCT Filed Jan. 21, 1997 PCT Pub. No. WO97/27188 PCT Pub. Date Jul. 31, 1997The invention concerns a compound of formula (I) wherein: R1 is of the formula -NHC(=O)(1-4C)alkyl, -NHS(O)n(1-4C)alkyl wherein n is 0, 1 or 2 or R1 is hydroxy; R2 and R3 are independently hydrogen or fluoro; R4 is hydrogen, methyl, ethyl or oxo; R5 is hydrogen, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl or of the formula R6(CH2)m- wherein either m is 1-4 and R6 is, for example, trifluoromethyl, difluoromethyl, fluoromethyl, (1-4C)alkoxy, (1-4C)alkyl S(O)p- wherein p is 0, 1 or 2, (1-6C)alkanoyloxy, di-(+E,uns N+EE -(1-4C)alkyl)amino, +E,uns N+EE -((1-4C)alkyl)(1-4C)alkanoylamino, cyano, carboxy, (1-4C)alkoxycarbonyl, carbamoyl, di-(+E,uns N+EE -(1-4C)alkyl)carbamoyl, +E,uns N+EE -((1-4C)alkyl)(1-4C)alkanesulphonamido, +E,uns N+EE 1-((1-4C)alkyl)-di-(+E,uns N+EE 3-(1-4C)alkyl)ureido, or of the formula -OC(=O)NR7(R8) or -N(R9)SO2NR7(R8) wherein R7 and R8 are independently hydrogen or (1-4C)alkyl and R9 is (1-4C)alkyl; or m is 2-4 and R6 is, for example, hydroxy, (1-4C)alkanoylamino, amino, (1-4C)alkylamino, (1-4C)alkanesulphonamido, ureido, di-(+E,uns N+EE 3-(1-4C)alkyl)ureido or of the formula -NHSO2NR7(R8); and pharmaceutically-acceptable salts thereof; processes for their preparation; pharmaceutical compositions containing them and their use as antibacterial agents.
- -
-
-
- New Histidyl amino acid derivatives, and pharmaceutical composition comprising the same
-
A compound of the formula: STR1 wherein R1 is lower alkyl optionally substituted with a substituent selected from the group consisting of acyl, hydroxy, lower alkoxy, aryl, lower alkylthio and a group of the formula: STR2 in which R5 is hydrogen or acyl and R6 is hydrogen or lower alkyl; aryl; or amino optionally substituted with substituent(s) selected from the group consisting of lower alkyl and acyl; and R2 is hydrogen or lower alkyl; or R1 and R2 are taken together with the attached nitrogen atom to form a heterocyclic group optionally substituted with substituent(s) selected from the group consisting of lower alkyl, hydroxy(lower )alkyl, lower alkoxy(lower)alkyl, acyl(lower)alkyl, oxo and acyl; R3 is hydrogen or lower alkyl; and R4 is lower alkyl; and its pharmaceutically acceptable salt, processes for the preparation thereof and pharmaceutical composition comprising the same.
- -
-
-
- Novel penicillins and cephalosporins and process for producing the same
-
Novel penicillins and cephalosporins and non-toxic salts thereof, which contain a mono- or di-oxo- or thioxo-piperazino(thio)carbonylamino group in molecule. These compounds are valuable antibacterial compounds for use in mammals including man. This disclosure relates to such compounds and a process for the preparation thereof.
- -
-
-
- Novel penicillins and cephalosporins and process for producing the same
-
Novel penicillins and cephalosporins and non-toxic salts thereof, which contain a mono- or di-oxo- or thioxo-piperazino(thio)carbonylamino group have been prepared. These compounds are valuable antibacterial compounds for use in mammals including man. A process for the preparation of the compounds has also been discovered.
- -
-
-
- Dibenzo-epines: Effect of the basic side-chain on neuroleptic activity
-
Structure-activity relationships in a series of dibenzo[b,f][1,4]thiazepines and -oxazepines and dibenzo[b,e][1,4]diazepines having different basic substituents in the 11-position were studied with reference to their neuroleptic activity. A high degree of structure-specificity was found for the piperazinyl moiety as well as for the distances between the distal nitrogen atom of this group and the tricyclic ring system, which distances are probably of importance for receptor binding. It was shown that the N-oxides of the neuroleptic agents clotiapine, loxapine and clozapine were inactive in in vitro binding tests involving central dopaminergic receptors, and it is very likely therefore that the in vivo activity of these N-oxides in the rat is due to their enzymatic reduction to the active parent compounds. All derivatives having a basic side-chain other than N-alkylpiperazinyl were inactive neuroleptically, with the exception of the N-methyl-4-piperidyl derivative which showed relatively weak effects.
- Burki,Fischer,Hunziker,et al.
-
p. 479 - 485
(2007/10/05)
-