84773-28-4Relevant academic research and scientific papers
FUSED MORPHOLINOPYRIMIDINES AND METHODS OF USE THEREOF
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Paragraph 0386-0387, (2017/05/14)
The present disclosure relates to Fused Morpholinopyrimidines, pharmaceutical compositions comprising an effective amount of a Fused Morpholinopyrimidine and methods for using a Fused Morpholinopyrimidine in the treatment of a neurodegenerative disease, comprising administering to a subject in need thereof an effective amount of a Fused Morpholinopyrimidine.
FUSED MORPHOLINOPYRIMIDINES AND METHODS OF USE THEREOF
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Paragraph 0350, (2015/08/03)
The present disclosure relates to Fused Morpholinopyrimidines, pharmaceutical compositions comprising an effective amount of a Fused Morpholinopyrimidine and methods for using a Fused Morpholinopyrimidine in the treatment of a neurodegenerative disease, comprising administering to a subject in need thereof an effective amount of a Fused Morpholinopyrimidine.
FUSED MORPHOLINOPYRIMIDINES AND METHODS OF USE THEREOF
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Paragraph 0231, (2015/10/05)
The present disclosure relates to Fused Morpholinopyrimidines, pharmaceutical compositions comprising an effective amount of a Fused Morpholinopyrimidine and methods for using a Fused Morpholinopyrimidine in the treatment of a neurodegenerative disease, comprising administering to a subject in need thereof an effective amount of a Fused Morpholinopyrimidine.
MODULATORS FOR AMYLOID BETA
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Page/Page column 32, (2010/04/28)
The invention relates to compounds of formula (I) wherein R1 is hydrogen, lower alkyl or is lower alkyl substituted by hydroxy; R2 is hydrogen, lower alkoxy or lower alkyl; R3 /R4 are independently from each other hydrogen, halogen, lower alkyl, C(O)O-low
ARYL-PHENYL-SULFONAMIDE-PHENYLENE COMPOUNDS AND THEIR USE
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Page/Page column 92, (2010/04/25)
The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-phenylene compounds of the following formula (I) (collectively referred to herein as "APSAP compounds"). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in treatment, for example, of inflammation and/or joint destruction and/or bone loss; of disorders mediated by excessive and/or inappropriate and/or prolonged activation of the immune system; of inflammatory and autoimmune disorders, for example, rheumatoid arthritis, psoriasis, psoriatic arthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, inflammatory bowel disease, ankylosing spondylitis, and the like; of disorders associated with bone loss, such as bone loss associated with excessive osteoclast activity in rheumatoid arthritis, osteoporosis, cancer-associated bone disease, Paget's disease and the like, etc.; and of cancer, such as a haematological malignancy, a solid tumour, etc.
PYRIMIDINE-2,4-DIONE DERIVATIVES AS GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS
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Page 43-44, (2008/06/13)
GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure formula (I) wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6, R7 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
Synthesis of single-enantiomer 6-hydroxy-7-phenyl-1,4-oxazepan-5-ones
Becker, Christopher W.,Dembofsky, Bruce T.,Hall, James E.,Jacobs, Robert T.,Pivonka, Don E.,Ohnmacht, Cyrus J.
, p. 2549 - 2561 (2007/10/03)
An efficient two-step preparation of (6R,7R)-6-hydroxy-7-phenyl-1,4- oxazepan-5-ones (1) starting from aminoethanols and (2R,3S)-3-phenyloxirane-2- carboxylic ethyl ester or potassium salt has been described. The most efficient catalyst identified for the
Synthesis of (5R)-4-methyl-5-phenyl-1,3,4-oxadiazinan-2-one and some N-acyl derivatives from (R)-phenylglycine
Rodrigues, Alessandro,Olivato, Paulo Roberto,Rittner, Roberto
, p. 2578 - 2582 (2007/10/03)
(5R)-4-Methyl-5-phenyl-1,3,4-oxadiazinan-2-one was synthesized from (R)-phenylglycine in five steps and in 65% overall yield. In addition, a convenient and practical method for N-acylation of 1,3,4-oxadiazinan-2-one directly with acids in the presence of
Highly potent inhibitors of TNF-α production. Part II: Metabolic stabilization of a newly found chemical lead and conformational analysis of an active diastereoisomer
Matsui, Toshiaki,Kondo, Takashi,Nishita, Yoshitaka,Itadani, Satoshi,Tsuruta, Hiroshi,Fujita, Setsuko,Omawari, Nagashige,Sakai, Masaru,Nakazawa, Shuichi,Ogata, Akihito,Mori, Hideaki,Kamoshima, Wataru,Terai, Kouichiro,Ohno, Hiroyuki,Obata, Takaaki,Nakai, Hisao,Toda, Masaaki
, p. 3787 - 3805 (2007/10/03)
Design and synthesis of metabolically stabilized inhibitors of TNF-α production, which could be new drug candidates, are reported. Conformational analysis of an active diastereoisomer was performed based on biological evaluations of the conformationally f
SYNTHESE D'AMINOPHOSPHINEPHOSPHINITES CHIRAUX. UTILISATION EN REDUCTION ASYMETRIQUE CATALYTIQUE
Karim, A.,Mortreux, A.,Petit, F.,Buono, G.,Pfeiffer, G.,Siv, C.
, p. 93 - 104 (2007/10/02)
The chiral aminophosphinephosphinites ligands (AMPP) are directly synthesized from natural amino alcohols or by reduction of formyl esters of α-amino acids and PPh2Cl. Their cationic rhodium complexes have been found to be excellent catalysts for enantioselective hydrogenation of dehydroamino acids (ee ca. 86percent, yield ca. 100percent) for example.Asymmetric reduction of ketones can also be performed with the new alkyl AMPP* modified rhodium catalyst (ee 50percent).
