876617-06-0Relevant articles and documents
2-ACYLAMINOTHIAZOLE DERIVATIVE OR SALT THEREOF
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Paragraph 0166, (2017/04/23)
To provide a compound useful as an active ingredient of a pharmacological composition for the treatment of urinary storage symptoms, dysuria, lower urinary tract diseases, and the like. [Solution] The inventors perfected the present invention after discov
2-ACYLAMINOTHIAZOLE DERIVATIVE AND SALT THEREOF
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, (2016/01/25)
[Problem] A compound which is useful as an active ingredient of a pharmaceutical composition for treating storage dysfunctions, voiding dysfunctions, and lower urinary tract diseases is provided. [Means for Solution] The present inventors have found that a thiazole derivative having pyrazine-2-carbonylamino substituted at the 2-position is an excellent muscarinic M3 receptor positive allosteric modulator, and is useful as an agent for preventing and/or treating bladder or urinary tract diseases, related to bladder contraction by a muscarinic M3 receptor, thereby completing the present invention. The 2-acylaminothiazole derivative or a salt thereof of the present invention can be used as an agent for preventing and/or treating bladder or urinary tract diseases, related to bladder contraction by a muscarinic M3 receptor, for example, voiding dysfunctions such as underactive bladder.
2-ACYLAMINOTHIAZOLE DERIVATIVE AND SALT THEREOF
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Paragraph 0412; 0413, (2016/10/07)
[Problem] A compound which is useful as an active ingredient of a pharmaceutical composition for treating storage dysfunctions, voiding dysfunctions, and lower urinary tract diseases is provided. [Means for Solution] The present inventors have found that a thiazole derivative having pyrazine-2-carbonylamino substituted at the 2-position is an excellent muscarinic M 3 receptor positive allosteric modulator, and is useful as an agent for preventing and/or treating bladder or urinary tract diseases, related to bladder contraction by a muscarinic M 3 receptor, thereby completing the present invention. The 2-acylaminothiazole derivative or a salt thereof of the present invention can be used as an agent for preventing and/or treating bladder or urinary tract diseases, related to bladder contraction by a muscarinic M 3 receptor, for example, voiding dysfunctions such as underactive bladder.
OXAZOLE DERIVATIVES AS HISTAMINE H3 RECEPTOR AGENTS, PREPARATION AND THERAPEUTIC USES
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Page/Page column 51-52, (2008/06/13)
The present invention discloses novel aryl oxazole compounds of Formula I (I), or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing and using such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using these compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases. Formula I (I) or a pharmaceutically acceptable salt thereof, wherein: m is independenlly at each occurrence 1, 2, or 3, Z independently represents carbon (substituted with hydrogen or the optional substituents indicated herein) or nitrogen, provided that when Z is nitrogen then R6 is not attached to Z; R1 and R2 are independently -(C1-C7) alkyl(optionally substituted with one to three halogens), or R1 and R2 and the nitrogen to which they are attached form an azetidinyl ring, a pyrrolidinyl ring, or a piperidinyl ring, wherein further the azetidinyl, pyrrolidinyl, or piperidinyl ring so formed may be optionally substituted one to three times with R5; R6 is independently at each occurrence -H, -halogen, or -CH3.
FUSED BENZENE DERIVATIVE AND USE
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Page/Page column 49, (2010/02/12)
The present invention provides a compound represented by the general formula: [wherein Ring A represents an optionally substituted 5- to 8-membered ring, Ring B represents a further optionally substituted 4- to 10-membered ring, Ring C represents a further optionally substituted benzene ring, X1 represents carbon atom, X2 represents a carbon atom, an oxygen atom, etc., W represents a nitrogen atom, etc., Y11 represents a group represented by the formula CR2R3' (wherein R2 represents a hydrogen atom, a cyano group, a nitro group, etc., and R3' represents a hydrogen atom, a cyano group, a nitro group, etc., respectively), Y21 represents a group represented by the formula CR4R5' (wherein R4 represents a hydrogen atom, a cyano group, a nitro group, etc., and R5' represents a hydrogen atom, a cyano group, a nitro group, etc., respectively), etc., and R1 represents an electron-withdrawing group, respectively. The formula represents a single bond or a double bond] or a salt thereof, which is useful as an androgen receptor modulator.
Direct Asymmetric Synthesis of Quaternary Carbon Centers via Addition-Elimination Process: Nitroolefination of α-Substituted δ-Lactones
Fuji, Kaoru,Node, Manabu,Nagasawa, Hideko,Naniwa, Yoshimitsu,Taga, Tooru,et al.
, p. 7921 - 7925 (2007/10/02)
The reactions of chiral nitro enamines 2a-c with zinc enolates 4-6 of α-substituted δ-lactones afforded α,α-disubstituted δ-lactones with a high ee through an addition-elimination process.The best results were obtained with the reaction of 2c with 5.Michael-type addition of the enolate onto the nitro enamine is kinetically controlled and decides the absolute stereochemistry of the product.A cyclic transition model is proposed to rationalize the S-selectivity.