85070-58-2Relevant academic research and scientific papers
NOVEL IMIDAZOLE COMPOUND AND USE THEREOF AS MELANOCORTIN RECEPTOR AGONIST
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, (2018/10/04)
The present invention relates to a novel imidazole compound or a pharmaceutically acceptable salt thereof having a melanocortin receptor agonistic activity, and medical use thereof. The present invention relates to an imidazole compound represented by general formula [I] [wherein: Ring A represents an optionally substituted aryl group or the like; R1 represents a hydrogen atom, an optionally substituted alkyl group, or the like; R2 represents a hydrogen atom, a halogen atom, or the like; and R3 represents an optionally substituted alkyl group] or a pharmaceutically acceptable salt thereof.
Pharmaceutical compositions (by machine translation)
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, (2019/01/31)
[Problem] imidazole compound or its pharmacologically acceptable salt in the melanocortin receptor activity that operates as an active ingredient of a pharmaceutical composition comprising. "I" general formula [a]" Formula, the aryl group may be substituted A ring represents a; R1 Represents a hydrogen atom, or an alkyl group which may be substituted represented; R2 Represents a hydrogen atom, a halogen atom or represents a; R3 The alkyl group may be substituted " represented by the imidazole compound, its pharmacologically acceptable salt as an active ingredient in a pharmaceutical composition. [Drawing] no (by machine translation)
Synthesis of a new fluorine-18-labeled bexarotene analogue for PET imaging of retinoid X receptor
Wang, Min,Davis, Toni,Gao, Mingzhang,Zheng, Qi-Huang
, p. 1742 - 1747 (2015/03/14)
The reference standard 2-fluoro-4-(1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)vinyl)ben-zoic acid was synthesized from 2,5-dimethyl-2,5-hexanediol and 2-fluoro-4-methylbenzoic acid in 10 steps with 3% overall chemical yield. The precursor 2-nitro-4-(1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetra-hydronaphthalen-2-yl)vinyl)benzoic acid was synthesized from 2,5-dimethyl-2,5-hexanediol and dimethyl-2-nitroterephthalate in seven steps with 2% overall chemical yield. The target tracer 2-[18F]flu-oro-4-(1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)vinyl)benzoic acid was synthesized from its nitro-precursor by the nucleophilic substitution with K[18F]F/Kryptofix 2.2.2 and isolated by HPLC combined with solid-phase extraction (SPE) purification in 20-30% radiochemical yield with 37-370 GBq/μmol specific activity at end of bombardment (EOB).
AMIDE DERIVATIVES AS LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS
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, (2015/03/13)
The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, formula (I) wherein R1. X, m. R2, Y, R3, Z, n, R4. A and B are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
NOVEL COMPOUNDS
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, (2015/03/04)
The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, X, m, R2, Y, R3, Z, n, R4, A and B are as defined in the specification, processes for their prep
Synthesis of a new fluorine-18-labeled bexarotene analogue for PET imaging of retinoid X receptor
Wang, Min,Davis, Toni,Gao, Mingzhang,Zheng, Qi-Huang
, p. 1742 - 1747 (2014/04/17)
The reference standard 2-fluoro-4-(1-(3,5,5,8,8-pentamethyl-5,6,7,8- tetrahydronaphthalen-2-yl)vinyl)benzoic acid was synthesized from 2,5-dimethyl-2,5-hexanediol and 2-fluoro-4-methylbenzoic acid in 10 steps with 3% overall chemical yield. The precursor 2-nitro-4-(1-(3,5,5,8,8-pentamethyl-5, 6,7,8-tetrahydronaphthalen-2-yl)vinyl)benzoic acid was synthesized from 2,5-dimethyl-2,5-hexanediol and dimethyl-2-nitroterephthalate in seven steps with 2% overall chemical yield. The target tracer 2-[18F]fluoro-4-(1- (3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)vinyl)benzoic acid was synthesized from its nitro-precursor by the nucleophilic substitution with K[18F]F/Kryptofix 2.2.2 and isolated by HPLC combined with solid-phase extraction (SPE) purification in 20-30% radiochemical yield with 37-370 GBq/μmol specific activity at end of bombardment (EOB).
Design, synthesis, and structure-activity relationship of a novel series of GluN2C-selective potentiators
Zimmerman, Sommer S.,Khatri, Alpa,Garnier-Amblard, Ethel C.,Mullasseril, Praseeda,Kurtkaya, Natalie L.,Gyoneva, Stefka,Hansen, Kasper B.,Traynelis, Stephen F.,Liotta, Dennis C.
, p. 2334 - 2356 (2014/04/17)
NMDA receptors are tetrameric complexes composed of GluN1 and GluN2A-D subunits that mediate a slow Ca2+-permeable component of excitatory synaptic transmission. NMDA receptors have been implicated in a wide range of neurological diseases and thus represent an important therapeutic target. We herein describe a novel series of pyrrolidinones that selectively potentiate only NMDA receptors that contain the GluN2C subunit. The most active analogues tested were over 100-fold selective for recombinant GluN2C-containing receptors over GluN2A/B/D-containing NMDA receptors as well as AMPA and kainate receptors. This series represents the first class of allosteric potentiators that are selective for diheteromeric GluN2C-containing NMDA receptors.
PIPERIDINE DERIVATIVES USEFUL AS GPR119 AGONISTS
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, (2013/05/21)
Substituted piperidine compounds and pharmaceutically acceptable salts thereof are disclosed. Pharmaceutical compositions and methods of treatment are also included. The present invention relates to G-protein coupled receptor agonists. In particular, the present invention is directed to agonists of GPR 119 that are useful for the treatment of diabetes, especially type 2 diabetes, obesity, the metabolic syndrome and related diseases and conditions.
HETEROCYCLIC DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-D]PYRIMIDINES AS JANUS KINASE INHIBITORS
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, (2011/04/14)
The present invention provides heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3 djpyrimidines of Formula Ia or a pharmaceutically acceptable salt thereof; wherein: A is H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-I4 cycloalkyl, C2-13 heterocycloalkyl, C6-14 aryl, C1-14 heteroaryl, C3-14 cycloalkyl-C1-4 alkyl, C2-13 heterocycloalkyl-C1-4 alkyl, C6-14 aryl-C1-4 alkyl, or C14 heteroaryl-C14 alkyl, wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-14 cycloalkyl, C2-13 heterocycloalkyl, C6-14 aryl, C1-14 heteroaryl, C3-14 cycloalkyl-C1-4 alkyl, C2-13 heterocycloalkyl-C1-4 alkyl, C6-14 aryl-C1-4 alkyl, and C1-14 heteroaryl-C1-4 alkyl are each optionally substituted with I, 2, 3, 4, 5, or 6 independently selected R8 substituents; L is absent, C(=O), C(=O)NH, S(=O), or S(O)2; X is CH or N; Y is H, cyano, halo, C1-4 alkyl, or C1-4 haloalkyl; Z is CR7 or N; R1, R2, and R3 are each independently H, hydroxyl, halo, C1-3 alkyl, or C1-3 haloalkyl; R4 and R5 are each independently H, C1-3 alkyl, or C1-3 haloalkyl; or R4 and R5 together with the carbon atom to which they are attached can form a 3-, 4-, 5-, 6- υr 7-membered cycloalkyl ring; as well as their compositions and methods of use, that modulate the activity of Janus kinases (JAKs) and are useful in the treatment of diseases related to the activity of JAKs including, for example inflammatory disorders, autoimmune disorders, cancer, and other diseases.
Synthesis and structure-activity relationship of novel RXR antagonists: Orally active anti-diabetic and anti-obesity agents
Sakaki, Junichi,Kishida, Masashi,Konishi, Kazuhide,Gunji, Hiroki,Toyao, Atsushi,Matsumoto, Yuki,Kanazawa, Takanori,Uchiyama, Hidefumi,Fukaya, Hiroaki,Mitani, Hironobu,Arai, Yoshie,Kimura, Masaaki
, p. 4804 - 4807 (2008/09/19)
A series of diazepinylbenzoic acid derivatives were synthesized and tested in the inhibition assay of the transactivation of RXR. Oral treatment of cyano derivatives (16f) was found to show anti-diabetic and anti-obesity effects in KK-Ay mice.
