- TRPML MODULATORS
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The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
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Paragraph 0297-299
(2021/06/26)
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- PHARMACEUTICAL CONSISTING OF CYCLIC AMINOMETHYL PYRIMIDINE DERIVATIVE
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PROBLEM TO BE SOLVED: To provide a cyclic aminomethyl pyrimidine derivative and a pharmaceutically acceptable salt thereof exhibiting effects on dopamine D4 receptor with high selectivity and useful as a treatment agent of central nervous system diseases such as attention deficit hyperkinesis disorder. SOLUTION: There is provide a compound represented by the formula (1) and a pharmaceutically acceptable salt thereof. (1), where n and m are each independently 1 or 2, Ra is a C1-6 alkyl group, a C3-6 cycloalkyl group or an amino group, Rb is H, a C1-6 alkyl group or an alkyl group-substituted/unsubstituted amino group, Rb is H when Ra is the amino group, Rc1 and Rc2 are each independently H or a C1-6 alkyl group, Rd1 and Rd2 are each independently H, F or a C1-6 alkyl group, a ring Q is substituted/unsubstituted 5- to 10-membered nitrogen-containing heteroaryl group and bond containing break lines is a single bond or a double bond. SELECTED DRAWING: None COPYRIGHT: (C)2016,JPOandINPIT
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Paragraph 0256
(2016/10/10)
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- TRIAZOLOBENZODIAZEPINES AND THEIR USE AS VASOPRESSIN ANTAGONISTS
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Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein R represents H, C1-6 alkyl, SO2R1, SO2NR1R2, or COR1; R1 and R2 independently represent C1-6alkyl; and Ring A represents a phenyl ring or a pyridinyl ring; may be useful in the treatment of anxiety, cardiovascular disease (including angina, atherosclerosis, hypertension, heart failure, edema, hypernatremia), dysmenorrhoea (primary and secondary), endometriosis, emesis (including motion sickness), intrauterine growth retardation, inflammation (including rheumatoid arthritis), mittlesmerchz, preclampsia, premature ejaculation, premature (preterm) labor and Raynaud's disease.
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Page/Page column 29
(2010/10/20)
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- Synthesis, SAR studies, and evaluation of 1,4-benzoxazepine derivatives as selective 5-HT1A receptor agonists with neuroprotective effect: Discovery of Piclozotan
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A new series of 1,4-benzoxazepine derivatives was designed, synthesized, and evaluated for binding to 5-HT1A receptor and cerebral anti-ischemic effect. A lot of compounds exhibited nanomolar affinity for 5-HT1A receptor with good selectivity over both dopamine D 2 and α1-adrenergic receptors. Among these compounds, 3-chloro-4-[4-[4-(2-pyridinyl)-1,2,3,6-tetrahydropyridin-1-yl]butyl]- 1, 4-benzoxazepin-5(4H)-one (50: SUN N4057 (Piclozotan) as 2HCl salt) showed remarkable neuroprotective activity in a transient middle cerebral artery occlusion (t-MCAO) model.
- Kamei, Katsuhide,Maeda, Noriko,Nomura, Kayoko,Shibata, Makoto,Katsuragi-Ogino, Ryoko,Koyama, Makoto,Nakajima, Mika,Inoue, Teruyoshi,Ohno, Tomochika,Tatsuoka, Toshio
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p. 1978 - 1992
(2007/10/03)
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- Benzimidazoles that are useful in treating sexual dysfunction
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The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction, wherein L is C1-4 alkyl;RA, RB, RC, RD, and RE, are as described in the specification;Z is selected from the group consisting of N, C and CH; andA is aryl and heteroaryl as described in the specification.
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- Oximes and hydrazones that are useful in treating sexual dysfunction
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The present invention relates to oximes and hydrazones of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.
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Page/Page column 47
(2010/02/13)
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- Acetamides and benzamides that are useful in treating sexual dysfunction
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The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.
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- Benzimidazoles that are useful in treating sexual dysfunction
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The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.
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- Discovery of 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a dopaminergic agent with a novel mode of action for the potential treatment of erectile dysfunction
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A new class of agents with potential utility for the treatment of erectile dysfunction has been discovered, guided by the hypothesis that selective D 4 agonists are erectogenic but devoid of the side effects typically associated with dopaminergic agents. The lead agent 2-(4-pyridin-2-ylpiperazin- 1-ylmethyl)-1H-benzimidazole (1, ABT-724) was discovered by optimization of a series of benzimidazole arylpiperazines. This highly selective D4 agonist was found to be very potent and efficacious in vivo, eliciting penile erections in rats at a dose of 0.03 μmol/kg, with a positive response rate of 77% erectile incidence. Even at high doses, it was devoid of side effects in animal models of central nervous system behaviors, emesis, or nausea. The structure-activity relationship of the parent benzimidazole series leading to 1 is described, with the detailed in vitro and in vivo profiles described. Distinctive structural features were discovered that are associated with D 4 selective agonism in this series of analogues.
- Cowart, Marlon,Latshaw, Steven P.,Bhatia, Pramila,Daanen, Jerome F.,Rohde, Jeffrey,Nelson, Sherry L.,Patel, Meena,Kolasa, Teodozyi,Nakane, Masaki,Uchic, Marie E.,Miller, Loan N.,Terranova, Marc A.,Chang, Renjie,Donnelly-Roberts, Diana L.,Namovic, Marian T.,Hollingsworth, Peter R.,Martino, Brenda R.,Lynch III, James J.,Sullivan, James P.,Hsieh, Gin C.,Moreland, Robert B.,Brioni, Jorge D.,Stewart, Andrew O.
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p. 3853 - 3864
(2007/10/03)
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- BENZIMIDAZOLES THAT ARE USEFUL IN TREATING SEXUAL DYSFUNCTION
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The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.
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- Benzimidazoles that are useful in treating sexual dysfunction
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The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.
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- Acetamides and benzamides that are useful in treating sexual dysfunction
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The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.
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- Acetamides and benzamides that are useful in treating sexual dysfunction
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The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.
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- Benzimidazoles that are useful in treating sexual dysfunction
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The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.
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- Benzimidazoles that are useful in treating sexual dysfunction
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The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.
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- 3-thienyl and 3-furanyl pyrrolidine modulators of chemokine receptor activity
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The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4fare defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.
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- Spirohydantoin compounds and uses thereof
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Spirohydantoin compounds and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of ben
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- MORPHOLINONE AND MORPHOLINE DERIVATIVES AND USES THEREOF
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This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human α 1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the α 1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
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- Oxazolidinones as alpha 1A receptor antagonists
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This invention is directed to oxazolidinone compounds which are selective antagonists for human alpha 1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where the antagonism of the alpha 1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
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- Quinazoline-4-amino-2-(piperidine-1-yl-4-substituted) derivatives having antihypertensive activity, a method for their preparation and their pharmaceutical use
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New quinazolines are described of general formula (I), in which Ar is an unsubstituted phenyl group or a phenyl group mono-substituted with a methoxy, ethoxy or methyl group; an unsubstituted pyridyl group (2-, 3- or 4-yl) or a pyridyl group mono-substituted with a methoxy or methyl group; an unsubstituted furyl group (2- or 3-yl) or a furyl group substituted with a methoxy or methyl group; a benzofuryl group (2- or 3-yl); an indolyl group (2- or 3-yl); a thiophenyl group (2- or 3-yl); a naphthyl group (1- or 2-yl) and their salts obtained from pharmaceutically acceptable inorganic or organic acids. These new quinazolines are useful in the treatment of hypertension, congestive heart failure, prostate hypertrophy, various urinary tract disorders and pathological symptoms caused by hyperactivity or disfunctioning of the noradrenergic neural system. STR1
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- Aryl substituted heterocycles
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The present invention concerns the novel use of aryl substituted heterocycles of formula I, set out below, which antagonize the pharmacological actions of one of ent endogenous neuropeptide tachykinins an the neurokinin 2 (NK2) receptor making them useful whenever such antagonism is desired, such as in the treatment of asthma and related conditions. The invention also provides pharmaceutical compositions containing the aryl substituted heterocycles for use in such treatment. Certain novel aryl substituted heterocycles of formula I and novel intermediates for their manufacture are also provided. STR1
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- From bipyridines to tobacco alkaloids and related compounds
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Starting from structural considerations which led to the hypothesis that a chemical relationship could exist between two families of natural compounds (mainly pyridinic and pyrrolidinic alkaloids), experiments were carried out in order to establish a correlation route between the two studied classes. Of special interest was the central position of nicotine in these studies, and the main part of this work was devoted to the synthesis of nicotine starting from bipyridines. It was thus necessary to determine the conditions for selective reactions on one aromatic ring of bipyridines (N-methylation, N-oxidation and reduction of the heterocycle). Ring contraction procedure allowed us to obtain nicotine from the parent compound (3,3′-bipyridine). Complementary studies yielded various isomers of piperidinylpyridines (hexahydro derivatives of bipyridines) in a regiochemically controlled manner by means of original methods. Elsevier,.
- Plaquevent, Jean-Christophe,Chichaoui, Ilhame
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p. 369 - 379
(2007/10/03)
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- Reduction Regiospecifique des Bipyridines
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A method for the specific reduction of bipyridines through the use of the N-oxo derivatives is described.
- Plaquevent, Jean-Christophe,Chichaoui, Ilhame
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p. 5287 - 5288
(2007/10/02)
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