- Compound with dopamine D3 receptor adjusting activity, and applications thereof
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The invention relates to a compound with dopamine D3 receptor adjusting activity, and applications thereof, and more specifically discloses dopamine receptor D3R as a novel target of post-traumatic stress disorder (PTSD) in prevention, treatment/or auxiliary treatment of PTSD, and screening of anti-PTSD medicines, and relates to applications of a compound with dopamine receptor D3R adjusting activity in preparation of medicines used for preventing, treatment and/or auxiliary treatment of PTSD.
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- ANTI-INFECTIVE HETEROCYCLIC COMPOUNDS AND USES THEREOF
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The present invention relates to heterocyclic compounds of Formula I useful as anti-infective agents. The present invention further relates to a method of treating an infection by administering such compounds, and to pharmaceutical compositions comprising such compounds.
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Page/Page column 8; 9; 76; 77
(2018/04/11)
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- NOVEL 2-AMINO-PYRIDINE AND 2-AMINO-PYRIMIDINE DERIVATIVES AND MEDICINAL USE THEREOF
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Provided is a compound superior in an autotaxin inhibitory action and the like, effective as a prophylactic or therapeutic drug for diseases involving ATX. The present invention relates to a compound represented by the following formula (I): [wherein each symbol is as described in the DESCRIPTION], which has a superior autotaxin inhibitory action and is useful as a prophylactic or therapeutic drug for diseases involving ATX.
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Paragraph 0243-0244
(2017/03/14)
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- NOVEL DOPAMINE D3 RECEPTOR LIGANDS AND PREPARATION AND MEDICAL USES OF THE SAME
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The present invention relates to a novel piperazine derivative represented by Formula I having an activity for regulating dopamine D3 receptor, stereoisomers thereof, pharmaceutically acceptable salts or solvates, and a pharmaceutical composition comprising the compound, a process for preparing the same, and use thereof in the prevention or treatment of a disease associated with central nervous system dysfunction, such as Parkinson''s disease, schizophrenia, drug addiction and relapse, as well as kidney protection and immunoregulation, or as a tool for researching D3R function or diseases associated with D3R dysfunction.
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- NOVEL DOPAMINE D3 RECEPTOR LIGANDS, THE PREPARATION AND USE THEREOF
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The invention discloses novel piperazine derivatives represented by formula I having activity for modulating dopamine D3 receptor, their stereoisomers, pharmaceutical salts, solvates, and the pharmaceutical compositions containing such compounds, their preparation and the use of such compounds for preventing or treating the diseases correlated with central nervous system disorder, such as Parkinson's disease, schizophrenia, drug addiction and relapse and the like, as well as the use of such compounds for kidney protection and immune modulation, or as implemental medicine for researching the function of D3R and the diseases correlated with disorder of D3R function.
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- A convenient route to 2-substituted benzothiazole-6-carboxylic acids using nitrobenzene as oxidant
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Various substituted benzothiazole-6-carboxylic acids (4a-i) have been prepared by the condensation of 4-amino-3-mercaptobenzoic acid and aldehydes in nitrobenzene as oxidant. Compound 4i was found to be a good candidate as an inhibitor of ss-hematin formation in vitro.
- Charris, Jaime,Camacho, Jose,Ferrer, Rosa,Lobo, Gricela,Barazarte, Arthur,Gamboa, Neira,Rodrigues, Juan,Lopez, Simon
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p. 769 - 770
(2007/10/03)
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- COMPOUND INHIBITING DIPEPTIDYL PEPTIDASE IV
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The invention aims to provide a dipeptidyl peptidase IV inhibitor which is satisfactory in respect of activity, stability and safety and has an excellent action as a pharmaceutical agent. The invention is directed to a compound represented by the following general formula or a pharmaceutically acceptable salt thereof: wherein R1 and R2 each represents hydrogen, an optionally substituted C1-6 alkyl group, or -COOR5 whereupon R5 represents hydrogen or an optionally substituted C1-6 alkyl group, or R1 and R2, together with a carbon atom to which they are bound, represent a 3- to 6-membered cycloalkyl group, R3 represents hydrogen or an optionally substituted C6-10 aryl group, R4 represents a hydrogen or a cyano group, D represents -CONR6-, -CO- or -NR6CO-, R6 represents hydrogen or an optionally substituted C1-6 alkyl group, E represents -(CH2)m- whereupon m is an integer of 1 to 3, -CH2OCH2-, or -SCH2-, n is an integer of 0 to 3, and A represents an optionally substituted bicyclic heterocyclic group or bicyclic hydrocarbon group.
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Page/Page column 25
(2010/02/14)
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- Antirheumatic agents: Novel methotrexate derivatives bearing a benzoxazine or benzothiazine moiety
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Novel methotrexate (MTX) derivatives bearing dihydro-2H-1,4- benzothiazine or dihydro-2H-1,4-benzoxazine were synthesized and tested for in vitro antiproliferative activities against human synovial cells (hSC) and human peripheral blood mononuclear cells (hPBMC) obtained from patients with rheumatoid arthritis and healthy volunteers, respectively. In vivo antiarthritic activities of these derivatives were also evaluated in a rat adjuvant arthritis model. N-[[4-[(2,4-Diaminopteridin-6-yl)methyl]-3,4- dihydro-2H-1,4-benzothiazin-7-yl]carbonyl]-L-glutamic acid (3c) exhibited more potent antiproliferative activities in hSC and hPBMC than MTX in vitro. Antiproliferative activities of N-[[4-[(2,4-diaminopteridin-6-yl)methyl]- 3,4-dihydro-2H-1,4-benzoxazin-7-yl]carbonyl]-L-homoglutamic acid (3b) and N- [[4-[(2,4-diaminopteridin-6-yl)methyl]-3,4-dihydro-2H-1,4-benzothiazin-7- yl]carbonyl]-L-homoglutamic acid (3d) (MX-68) were comparable to that of MTX in these in vitro assays. Compounds 3b,d (MX-68) significantly suppressed progression of the adjuvant arthritis in a dose-dependent manner ranging from 0.5 to 2.5 mg/kg (po). In addition, 3d (MX-68) completely suppressed this progression at the dose of 2.5 mg/kg (po). Importantly, 3d (MX-68) having benzothiazine and homoglutamate, as expected, did not undergo polyglutamation, a process which may be responsible for the associated side effects of MTX. These results suggest that 3d (MX-68) is a potent and safe candidate antirheumatic agent, absent of the side effects of MTX.
- Matsuoka, Hiroharu,Ohi, Nobuhiro,Mihara, Masahiko,Suzuki, Hiroshi,Miyamoto, Katsuhito,Maruyama, Noriaki,Tsuji, Keiichiro,Kato, Nobuaki,Akimoto, Toshio,Takeda, Yasuhisa,Yano, Keiichi,Kuroki, Toshio
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p. 105 - 111
(2007/10/03)
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- 10,11-Dihydrodibenzo[b,f][1,4]thiazepine carboxylic acids esters and amides thereof
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Novel dibenzo[b,f][1,4]thiazepine derivatives are employed in the treatment and control of allergic conditions such as allergic asthma.
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