57469-91-7Relevant academic research and scientific papers
SUBSTITUTED AMINO TRIAZOLOPYRIMIDINE AND AMINO TRIAZOLOPYRAZINE ADENOSINE RECEPTOR ANTAGONISTS, PHARMACEUTICAL COMPOSITIONS AND THEIR USE
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Page/Page column 58; 96-97, (2020/06/10)
In its many embodiments, the present invention provides certain substituted amino triazolopyrimidine and amino triazolopyrazine compounds of Formula (IA) and Formula (IB): and, and pharmaceutically acceptable salts thereof, wherein, R1, n, R2, and R3 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and their use in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.
COMPOSITION HAVING A MUGUET ODOR
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Page/Page column 23, (2018/08/12)
The present invention relates to a composition of matter comprising a) at least one compound of formula (I) in the form of any one of its isomers or a mixture thereof; wherein R1 represents a hydrogen atom or a C1-2 alkyl group; R2 represents a hydrogen atom or a methyl group; and R represents a group of formula –[CH2]nC(Me)2OH, wherein n is 1 or 2; said R being, relative to position 1, an ortho, meta or para substituent of the aromatic ring; and b) at least one compound of formula (II) in the form of any one of its isomers or a mixture thereof; wherein R1, R2 and R have the same meaning as defined in formula (I); said R being, relative to position 1, an ortho, meta or para substituent of the aromatic ring; their uses as perfuming ingredients as well as the composition and consumer product including such a composition of matter and the process to prepare it.
HETEROCYCLIC COMPOUND
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Paragraph 0564; 0965; 0966, (2017/04/11)
The present invention provides a heterocyclic compound having a CDK8 and/or CDK19 inhibitory effect. The present invention provides a compound represented by formula (I) (in the formula, the symbols are as defined in the description) or a salt thereof.
Pd(II)-catalyzed hydroxyl-directed C-H olefination enabled by monoprotected amino acid ligands
Lu, Yi,Wang, Dong-Hui,Engle, Keary M.,Yu, Jin-Quan
supporting information; experimental part, p. 5916 - 5921 (2010/07/05)
A novel Pd(II)-catalyzed ortho-C-H olefination protocol has been developed using spatially remote, unprotected tertiary, secondary, and primary alcohols as the directing groups. Mono-N-protected amino acid ligands were found to promote the reaction, and an array of olefin coupling partners could be used. When electron-deficient alkenes were used, the resulting olefinated intermediates underwent subsequent Pd(II)-catalyzed oxidative intramolecular cyclization to give the corresponding pyran products, which could be converted into ortho-alkylated alcohols under hydrogenolysis conditions. The mechanistic details of the oxidative cyclization step are discussed and situated in the context of the overall catalytic cycle.
4-AMINO-5-OXO-7, 8-DIHYDROPYRIMIDO [5,4-F] [1,4] OXAZEPIN-6 (5H) -YL) PHENYL DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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Page/Page column 53-54, (2010/08/09)
The invention provides compounds of Formula (I), wherein R1, R2a, R2b, R3, m and A are as defined herein, as well as compositions thereof and methods for treating a disease, condition or disorder that is modulated by the inhibition of the diacylglycerol O-acyltransferase 1 (DGAT-1) enzyme by administering the compounds of the present invention and/or compositions thereof.
1-SUBSTITUTED-3- BETA-D-GLUCOPYRANOSYLATED NITROGENOUS HETERO- CYCLIC COMPOUNDS AND MEDICINES CONTAINING THE SAME
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Page/Page column 26, (2008/06/13)
A compound having an SGLT1 and/or SGLT2 inhibitory activity which is usable as an agent for the prevention or treatment of diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, obesity, etc. It is a 1-substituted-3-(β-D
PIPERAZINYLPHENALKYL LACTAM/AMINE LIGANDS FOR THE 5HT1B RECEPTOR
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Page/Page column 82, (2010/11/30)
The present invention relates to novel derivatives, that are compounds of Formula (I), wherein R1, R2, R3, R14, X, Y, n and m are defined herein, their pharmaceutically acceptable salts, pharmaceutical compositions and methods using said compounds in treating or preventing depression, anxiety, obsessive compulsive disorder (OCD) and other disorders for which selective antagonists, inverse agonists and partial agonists of serotonin 1 (5-HT1) receptors, specifically, antagonists of 5-HT1B are useful.
NOVEL BENZYL(IDENE)-LACTAM DERIVATIVES
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Page/Page column 36, (2008/06/13)
The present invention relates to novel benzyl(idene)-lactam derivatives, compounds of the formula (I) wherein R1 is a group of the formula G1 or G2 depicted below, wherein R1, R3, R6, R13, X, a, n and m are as defined herein, their pharmaceutically acceptable salts, and pharmaceutical compositions which include selective antagonists, inverse agonists and partial agonists of serotonin 1 (5-HT1) receptors, specifically, of one or both of the 5-HT1A and 5-HT1B receptors. The compounds of the invention are useful in treating or preventing depression, anxiety, obsessive compulsive disorder (OCD) and other disorders for which a 5-HT1 agonist or antagonist is indicated and have reduced potential for cardiac side effects, in particular QTc prolongation.
Bicyclic nitrogen heterocycles
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, (2008/06/13)
Amino-substituted dihydropyrimido[4,5-d]pyrimidinones of the formula in which R1 represents hydrogen, lower alkyl, aryl, aryl-lower alkyl, heteroaryl, heteroaryl-lower alkyl, lower cycloalkyl or lower cycloalkyl-lower alkyl, R2 represents lower alkyl, aryl, aryl-lower alkyl, heteroaryl, heteroaryl-lower alkyl, lower cycloalkyl or lower cycloalkyl-lower alkyl, and R3 represents hydrogen, lower alkyl, aryl, aryl-lower alkyl, heteroaryl, heteroaryl-lower alkyl, lower cycloalkyl, lower cycloalkenyl or lower cycloalkyl-lower alkyl, and pharmaceutically acceptable salts thereof are protein kinase inhibitors. They can be used in the treatment or prophylaxis of inflammatory, immunological, oncological, bronchopulmonary, dermatological and cardiovascular disorders, in the treatment of asthma, central nervous system disorders or diabetic complications or for the prevention of graft rejection following transplant surgery.
Substituted biphenylsulfonamide endothelin antagonists
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, (2008/06/13)
Compounds of the formula inhibit the activity of endothelin. The symbols are defined as follows: R2 and R3 are each independently (a) hydrogen; (b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, aryloxy, aralkyl or aralkoxy, any of which may be substituted with Z1, Z2 and Z3; (c) halo; (d) hydroxyl; (e) cyano; (f) nitro; (g) -C(O)H or -C(O)R6; (h) -CO2H or -CO2R6; (i) -SH, -S(O)nR6, -S(O)m-OH, -S(O)m-OR6, -O-S(O)m-R6, -O-S(O)mOH or -O-S(O)m-OR6; (j) -Z4-NR7R8; or (k) -Z4-N(R11)-Z5-NR9R10; and the remaining symbols are as defined in the specification.
