cas 51285-13-3, N'-Hydroxycyclopropanecarboximidamide

Articles about 51285-13-3Total 25 be found

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BAX INHIBITORS AND USES THEREOF
A compound having formula (I) or (II) for use inhibiting Bax mediated cell death and/or apoptosis.
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Paragraph 00225; 00226

(2021/01/23)

2-(1,2,4-Oxadiazol-5-yl)anilines Based on Amidoximes and Isatoic Anhydrides: Synthesis and Structure Features
Abstract: An efficient one-pot method was developed for the synthesis of 2-(1,2,4-oxadiazol-5-yl)anilines via the reaction of amidoximes with isatoic anhydrides in a NaOH–DMSO medium at ambient temperature. The method allows to obtain structurally diverse
Baykov, S. V.,Kotlyarova, V. D.,Shetnev, A. A.,Tarasenko, M. V.
p. 768 - 778
(2021/06/26)

SSAO INHIBITOR
The present invention provides an SSAO inhibitor and an application thereof in preparing a drug for treating a disease related to SSAO. In particular, the present invention provides a compound shown in formula (IV) and a pharmaceutically acceptable salt thereof.
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Paragraph 0183-0185

(2020/04/02)

Design, synthesis and biological activities of piperidine-spirooxadiazole derivatives as α7 nicotinic receptor antagonists
α: 7 nicotinic acetylcholine receptors (nAChRs) expressed in the nervous and immune systems have been suggested to play important roles in the control of inflammation. However, the lack of antagonist tools specifically inhibiting α7 nAChR impedes the validation of the channel as therapeutic target. To discover a selective α7 antagonist, we started a pharmacophore-based virtual screening and identified a piperidine-spirooxadiazole derivative T761–0184 that acts as a α7 antagonist. A series of novel piperidine-spirooxadiazole derivatives were subsequently synthesized and evaluated using two-electrode voltage clamp (TEVC) assay in Xenopus oocytes. Lead compounds from two series inhibited α7 with their IC50 values ranging from 3.3 μM to 13.7 μM. Compound B10 exhibited α7 selectivity over other α4β2 and α3β4 nAChR subtypes. The analysis of structure-activity relationship (SAR) provides valuable insights for further development of selective α7 nAChR antagonists.
Zhang, Han,He, Xiaomeng,Wang, Xintong,Yu, Bo,Zhao, Siqi,Jiao, Peili,Jin, Hongwei,Liu, Zhenming,Wang, KeWei,Zhang, Liangren,Zhang, Lihe
(2020/09/03)

Continued exploration of 1,2,4-oxadiazole periphery for carbonic anhydrase-targeting primary arene sulfonamides: Discovery of subnanomolar inhibitors of membrane-bound hCA IX isoform that selectively kill cancer cells in hypoxic environment
An expanded set of diversely substituted 1,2,4-oxadiazole-containing primary aromatic sulfonamides was synthesized and tested for inhibition of human carbonic anhydrase I, II, IX and XII isoforms. The initial biochemical profiling revealed a significantly
Krasavin, Mikhail,Shetnev, Anton,Sharonova, Tatyana,Baykov, Sergey,Kalinin, Stanislav,Nocentini, Alessio,Sharoyko, Vladimir,Poli, Giulio,Tuccinardi, Tiziano,Presnukhina, Sofia,Tennikova, Tatiana B.,Supuran, Claudiu T.
p. 92 - 105
(2019/01/04)

Discovery of BR102375, a new class of non-TZD PPARγ full agonist for the treatment of type 2 diabetes
As a potential treatment of type 2 diabetes, a novel PPARγ non-TZD full agonist, compound 18 (BR102375) was identified from the original lead BR101549 by the SAR efforts of the labile metabolite control through bioisosteres approach. In vitro assessments
Choung, Wonken,Yang, Deokmo,Kim,Choi, Hyukjoon,Lee, Bo Ram,Park, Min,Jang, Su Min,Lim, Jae Soo,Kim, Woo Sik,Kim, Kyung-Hee,Chin, Jungwook,Jung, Kyungjin,Lee, Geumwoo,Hong,Jang, Tae-ho,Joo, Jeongmin,Hwang, Hayoung,Myung, Jayhyuk,Kim, Seong Heon
p. 2275 - 2282
(2019/06/27)

Reactions of pentafluoropyridine with amidoximes
Abstract: In this paper, site reactivity of amidoximes with pentafluoropyridine under basic conditions in dry CH3CN was investigated. The aromatic nucleophilic substitution of pentafluoropyridine with amidoximes occurs in the 4-position of the
Ranjbar-Karimi, Reza,Karbakhsh-Ravari, Asma,Poorfreidoni, Alireza
p. 2397 - 2405
(2017/10/30)

Copper-catalyzed one-pot synthesis of 1,2,4-triazoles from nitriles and hydroxylamine
A simple and efficient copper-catalyzed one-pot synthesis of substituted 1,2,4-triazoles through reactions of two nitriles with hydroxylamine has been developed. The protocol uses simple and readily available nitriles and hydroxylamine hydrochloride as th
Xu, Hao,Ma, Shuang,Xu, Yuanqing,Bian, Longxiang,Ding, Tao,Fang, Xiaomin,Zhang, Wenkai,Ren, Yanrong
supporting information
p. 1789 - 1794
(2015/02/19)

NEW BICYCLIC COMPOUND FOR MODULATING G PROTEIN-COUPLED RECEPTORS
The present invention relates to a bicyclic compound for modulating G protein-coupled receptors. The inventive compound provides preventing or treating a disease associated with the modulation of G protein-coupled receptors, particularly GPR119 G protein-coupled receptors.
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Paragraph 0216-0218

(2013/10/22)

NEW BICYCLIC COMPOUND FOR MODULATING G PROTEIN-COUPLED RECEPTORS
The present invention relates to a bicyclic compound for modulating G protein-coupled receptors. The inventive compound provides preventing or treating a disease associated with the modulation of G protein-coupled receptors, particularly GPR119 G protein-coupled receptors.
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Page/Page column 31

(2012/07/27)

MODULATORS OF THE GPR119 RECEPTOR AND THE TREATMENT OF DISORDERS RELATED THERETO
The present invention relates to compounds of Formula I and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as single pharmaceutical agents or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.
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Page/Page column 167; 168

(2012/11/07)

Substituted 3-(1,2,4-Oxadiazol-5-yl)-5-Phenylpiperidines
The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases
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Page/Page column 20

(2012/06/01)

TRICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS
The present invention relates to tricyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthama, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases. (I)
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Page/Page column 82

(2012/09/10)

FUSED HETEROCYCLIC RING COMPOUND
A compound represented by the following formula or a salt thereof, which has an GPR119 agonist action, is useful for the prophylaxis or treatment of diabetes, obesity and the like, and shows superior efficacy: wherein P: substituted 6-membered aromatic ring, Q: (substituted) 6-membered aromatic ring, A1: CR4aR4b, NR4c, O, S, SO or SO2 {R4a-4c: H etc.}, L1: (substituted) C1-5 alkylene, L2: a bond or (substituted) C1-3 alkylene, L3-4: (substituted) C1-3 alkylene, R1: H, X, CN, (substituted) hydrocarbon, (substituted) heterocycle or (substituted) OH, or (substituted) 4- to 8-membered (heterocyclic) ring together with A1, R2: H, CN, (substituted) hydrocarbon, and R3a: -COSRA1, (substituted) 5- or 6-membered aromatic ring {RA1: (substituted) hydrocarbon or (substituted) heterocycle}.
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Page/Page column 95

(2012/01/11)

OXADIAZOLE COMPOUNDS, THEIR PREPARATION AND USE
The present invention relates to oxadiazole compounds in all their stereoisomeric and tautomeric forms and mixtures thereof in all ratios; and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable prodrugs and pharmaceutically acceptable polymorphs. The invention also relates to processes for the manufacture of the oxadiazole compounds and to pharmaceutical compositions containing them. The said compounds and their pharmaceutical compositions are useful in the treatment of cancer, particularly chronic myeloid leukemia (CML). The present invention further provides a method of treatment of cancer by administering a therapeutically effective amount of said compounds or their pharmaceutical compositions, to a mammal in need thereof.
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Page/Page column 82

(2011/09/30)

SUBSTITUTED PIPERIDINES
The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular diseases and tumour diseases.
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Page/Page column 14

(2010/12/29)

PTSA-ZnCl2: An efficient catalyst for the synthesis of 1,2,4-oxadiazoles from amidoximes and organic nitriles
(Chemical Equation Presented) PTSA-ZnCl2 has been proved to be an efficient and mild catalyst for the synthesis of 3,5-disubstituted-1,2,4- oxadiazoles from amidoximes and organic nitriles.
Augustine, John Kallikat,Akabote, Vani,Hegde, Shrivatsa Ganapati,Alagarsamy, Padma
supporting information; experimental part
p. 5640 - 5643
(2009/12/08)

Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119
GPR119 is a rhodopsin-like GPCR expressed in pancreatic β-cells and incretin releasing cells in the GI tract. As with incretins, GPR119 increases cAMP levels in these cell types, thus making it a highly attractive potential target for the treatment of dia
Semple, Graeme,Fioravanti, Beatriz,Pereira, Guillherme,Calderon, Imelda,Uy, Jane,Choi, Karoline,Xiong, Yifeng,Ren, Albert,Morgan, Michael,Dave, Vibha,Thomsen, William,Unett, David J.,Xing, Charles,Bossie, Stuart,Carroll, Chris,Chu, Zhi-Liang,Grottick, Andrew J.,Hauser, Erin K.,Leonard, James,Jones, Robert M.
scheme or table
p. 5172 - 5175
(2009/07/01)

THIAZOLYL-DIHYDRO-CYCLOPENTAPYRAZOLE
Disclosed are compounds of general formula (I), wherein the groups R1, R2, Ra and Rb have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers and the mixtures
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Page/Page column 24

(2008/06/13)

THIAZOLYL-DIHYDRO-CHINAZOLINE
Disclosed are compounds of general formula (I), wherein the groups A, R1, R2, Ra and Rb have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers and the mixtures thereof, and optionally the pharmacologically acceptable acid addition salts, solvates and hydrates thereof, and processes for preparing these thiazolyl-dihydro-quinazolines and the use thereof as pharmaceutical compositions.
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Page/Page column 26

(2008/06/13)

THIAZOLYL-DIHYDRO-INDAZOLE
Disclosed are compounds of general formula (I), wherein the groups R1, R2, Ra and Rb have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers and the mixtures thereof, and optionally the pharmacologically acceptable acid addition salts, solvates and hydrates thereof, and processes for preparing these thiazolyl-dihydro-indazoles and the use thereof as pharmaceutical compositions.
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Page/Page column 25

(2008/06/13)

DPP-IV INHIBITORS
The invention relates to compounds of formula (I), Z-C(R1R 2)-C(R3NH2)-C(R4R5)-X-N(R 6R7), wherein Z, R1-7 and X have the meaning as cited in the description and the claims. Said compounds are useful as DPP-lV inhibitors. The invention also relates to the
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Page/Page column 56

(2010/02/14)

1,2,4-OXADIAZOLYL-PHENOXYALKYLISOXAZOLES AND THEIR USE AS ANTIVIRAL AGENTS
Compounds of the formula wherein: R1 is alkyl, alkoxy, hydroxy, cycloalkyl, hydroxyalkyl, alkoxyalkyl, hydroxyalkoxy, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxycarbonyl, carboxy, or cyanomethyl; Y is alkylene of 3 to 9 carbon atoms, R2 and R3 independently are hydrogen, alkyl, alkoxy, halo, cyano, trifluoromethyl and nitro; R4 is alkoxy, hydroxy, halomethyl, dihalomethyl, trihalomethyl, dihaloethyl, cycloalkyl, heterocyclyl, alkoxycarbonyl, hydroxyalkyl, alkoxyalkyl, alkanecarbonyloxyalkyl, cyano, halo, thioalkyl, alkylthioalkyl, alkylthio, thio, 2,2,2-trifluoro-ethyl, (4-methylphenyl)sulfonyloxymethyl, N=Q or CON=Q, where N=Q is amino, alkylamino or dialkylamino; R5 is hydrogen or halo or alkyl
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(2008/06/13)

Oxadiazole and its salts, their use in treating dementia
The compound (3R, 4R)-3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-1-azabicyclo[2.2.1]heptane and its salts behave as a functionally selective muscarinic agonist and are useful in the treatment of neurological and mental disorders, preferably in a pharmaceutical formulation comprising the active compound in association with a pharmaceutically acceptable carrier. The compound can be prepared by methods analogous to those known in the art via suitable chiral intermediates and cyclopropyl carboxamide oxime.
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(2008/06/13)

ENANTIOSELECTIVE SYNTHESIS OF 3-SUBSTITUTED 1-AZABICYCLO(2.2.1)HEPTANES
A process for preparing a substantially pure enantiomer of a compound formula (I) STR1 wherein X is O or S; andR. sup.2 represents hydrogen,--CF 3,--OR 7,--SR 7,--NR 7 R 8,--CN,--COOR 7,--CONR 7 R 8, or a saturated or unsaturated, substituted or unsubstituted hydrocarbon group, wherein R. sup.7 and R. sup.8 are independently selected from hydrogen and C 1-2 alkyl provided that--NR 7 R 8 is other than NH 2 ; which process comprises cyclization of a compound of formula (10) or salt thereof: STR2 wherein X and R 2 are as defined in formula (I); and R 4 is a labile leaving group and optionally epimerizing the endo-diastereomer so prepared to produce the corresponding exo-diastereomer.
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(2008/06/13)