855481-84-4Relevant articles and documents
Pyrazole and quinolinone derivatives, their preparation and their use in therapy
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Paragraph 0933; 0934; 0935; 0936, (2017/09/09)
The invention relates to a compound corresponding to a formula (I). In the formula (I), R1, R2 and R2 are defined in the claim 1. The invention also relates to a preparation method and a therapeutic application of the compound.
[...] derivatives, their preparation and for therapeutic use
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Paragraph 0101-0102, (2020/10/03)
PROBLEM TO BE SOLVED: To provide a new compound which is a reversible and selective inhibitor of type 2 methionine aminopeptidase and is effective for lung and liver fibrosis, and diseases, in which reactivation of angiogenesis is involved, such as diabetic retinopathy, age-related macular degeneration, psoriasis, cancer, and the like, and to provide a pharmaceutical composition containing the compound.SOLUTION: There are provided the compound represented by formula (I) and the pharmaceutical composition containing the compound. In the formula (I), R1 is a 1-4C alkyl group or the like, R2 is a pyridyloxy group, a pyridylamino group, or the like, and R3 is hydrogen, a halogen, a 1-6C alkyl group, a carboxyl group, or the like.
PYRAZOLOQUINOLINONE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
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Paragraph 0849-0850, (2014/09/03)
The invention relates to compounds corresponding to formula (I), in which R1, R2 and R3 are as defined in Claim 1, and also to the process for preparing them and to their therapeutic use.
PYRAZOLOQUINOLINONE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
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Paragraph 0841; 0842, (2013/04/10)
The invention relates to compounds corresponding to formula (I) in which R1, R2 and R3 are as defined in Claim 1, and also to the process for preparing them and to their therapeutic use.
PYRAZOLOQUINOLINONE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
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Page/Page column 58, (2013/04/13)
The invention relates to compounds corresponding to formula (I), in which R1, R2 and R3 are as defined in Claim 1, and also to the process for preparing them and to their therapeutic use.
Pyrazoloquinolinone derivatives, preparation thereof and therapeutic use thereof
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Paragraph 0086, (2013/04/10)
The invention relates to compounds corresponding to formula (I) in which R1, R2 and R3 are as defined in Claim 1, and also to the process for preparing them and to their therapeutic use.
Discovery of a novel series of biphenyl benzoic acid derivatives as potent and selective human β3-adrenergic receptor agonists with good oral bioavailability. Part I
Imanishi, Masashi,Tomishima, Yasuyo,Itou, Shinji,Hamashima, Hitoshi,Nakajima, Yutaka,Washizuka, Kenichi,Sakurai, Minoru,Matsui, Shigeo,Imamura, Emiko,Ueshima, Koji,Yamamoto, Takao,Yamamoto, Nobuhiro,Ishikawa, Hirofumi,Nakano, Keiko,Unami, Naoko,Hamada, Kaori,Matsumura, Yasuhiro,Takamura, Fujiko,Hattori, Kouji
, p. 1925 - 1944 (2008/12/20)
A novel class of biphenyl analogues containing a benzoic acid moiety based on lead compound 8i have been identified as potent and selective human β3 adrenergic receptor (β3-AR) agonists with good oral bioavailability and long plasma half-life. After further substituent effects were investigated at the terminal phenyl ring of lead compound 8i, we have discovered that more lipophilic substitution at the R position improved potency and selectivity. As a result of these studies, 10a and 10e were identified as the leading candidates with the best balance of potency, selectivity, and pharmacokinetic profiles. In addition, compounds 10a and 10e were evaluated to be efficacious for a carbachol-induced increase of intravesical pressure, such as an overactive bladder model in anesthetized dogs. This represents the first demonstrated result dealing with β3- AR agonists.
Aminoalcohol derivatives
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Page/Page column 7, (2010/02/12)
The present invention relates to a compound formula[I]: wherein X is bond, —CH2—, —O— or —NH—, R1 and R12 are each independently hydrogen, halogen, lower alkyl, etc., R2 is hydrogen or optionally substituted lower alkyl, R3 is hydrogen or an amino protective group, R4, R5 and R6 are each independently hydrogen or optionally substituted lower alkyl, R7 is -Z-R13, in which Z is bond, etc., and R13 is carboxy, lower alkoxycarbonyl, (lower alkylsulfonyl)carbamoyl or lower alkanoylsulfamoyl, R8 is —Y—R9, in which Y is bond, —CH2—, —O—, —S—, etc., and R9 is hydrogen, lower alkyl, cyclo(lower)alkyl, etc., and R11 is hydrogen, lower alkyl, lower alkoxy, etc., or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.
