138091-52-8Relevant academic research and scientific papers
TRIAZA-SPIRODECANONES AS DDR1 INHIBITORS
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Page/Page column 78, (2017/01/26)
The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein L and R1 to R5 are as described herein, as well as processes for their manufacture, pharmaceutical compositions comprising them, and their use as medicaments.
D2 ANTAGONISTS, METHODS OF SYNTHESIS AND METHODS OF USE
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Page/Page column 23, (2012/01/06)
Provided are D2 or D3 antagonist compounds and pharmaceutical compositions of formula I and pharmaceutically acceptable salts thereof, or isomers thereof, wherein R1, R2 and R3 are as defined herein. The invention further comprises methods for making the compounds of the invention and methods for the treatment of conditions mediated by the dopamine D2 or D3 receptor from the compounds of the invention.
TRICYCLIC SPIROCYCLE DERIVATIVES AND METHODS OF USE
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Page/Page column 30, (2011/07/29)
The present invention relates to novel Tricyclic Spirocycle Derivatives, pharmaceutical compositions comprising the Tricyclic Spirocycle Derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or aired fasting glucose.
Spiroimidazolidinone NPC1L1 inhibitors. Part 2: Structure-activity studies and in vivo efficacy
Howell, Kobporn L.,Devita, Robert J.,Garcia-Calvo, Margarita,Meurer, Roger D.,Lisnock, Jeanmarie,Bull, Herbert G.,McMasters, Daniel R.,McCann, Margaret E.,Mills, Sander G.
scheme or table, p. 6929 - 6932 (2011/02/16)
Ezetimibe (Zetia), a cholesterol-absorption inhibitor (CAI) approved by the FDA for the treatment of hypercholesterolemia, is believed to target the intestine protein Niemann-Pick C1-Like 1 (NPC1L1) or its pathway. A spiroimidazolidinone NPC1L1 inhibitor identified by virtual screening showed moderate binding activity but was not efficacious in an in vivo rodent model of cholesterol absorption. Synthesis of analogs established the structure-activity relationships for binding activity, and resulted in compounds with in vivo efficacy, including 24, which inhibited plasma cholesterol absorption by 67% in the mouse, thereby providing proof-of-concept that non-β-lactams can be effective CAIs.
Synthesis and characterization of selective dopamine D2 receptor antagonists. 2. Azaindole, benzofuran, and benzothiophene analogs of L-741,626
Vangveravong, Suwanna,Taylor, Michelle,Xu, Jinbin,Cui, Jinquan,Calvin, Wesley,Babic, Sonja,Luedtke, Robert R.,MacH, Robert H.
experimental part, p. 5291 - 5300 (2010/09/09)
A series of indole, 7-azaindole, benzofuran, and benzothiophene compounds have been prepared and evaluated for affinity at D2-like dopamine receptors. These compounds share structural elements with the classical D 2-like dopamine rec
Practical synthesis of p-aminophenethylspiperone (NAPS), a high-affinity, selective D2-dopamine receptor antagonist
Jin, Chunyang,Mayer, Louise D.,Lewin, Anita H.,Rehder, Kenneth S.,Brine, George A.
, p. 816 - 823 (2008/09/16)
Because attempts to scale up the published synthetic preparation of p-aminophenethylspiperone (NAPS) by N-alkylation of spiperone with 4-nitrophenethyl bromide followed by reduction gave poor yields and difficulties during purification, an alternative synthetic approach has been developed. Use of 4-(N-tert-butyloxycarbonyl) aminophenethyl bromide to alkylate spiperone followed by the Boc group deprotection gave NAPS in 56% yield. This procedure provides an improved and efficient synthesis of the important high-affinity, selective D2-dopamine receptor antagonist NAPS. Copyright Taylor & Francis Group, LLC.
PYRAZOLONE COMPOUNDS AS METABOTROPIC GLUTAMATE RECEPTOR AGONISTS FOR THE TREATMENT OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS
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Page/Page column 238; 239, (2008/06/13)
Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, X, and n are as defined for Formula (I) in the description, processes for the preparation of the compounds and new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and the use of the compounds in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction.
SPIRO-SUBSTITUTED PYRROLOPYRIMIDINES
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Page 46; 47, (2008/06/13)
The invention provides compounds of formula (I) or a pharmaceutically acceptable salt or ester thereof formula (I) wherein the symbols have the meaning as defined in the description. Said compounds are inhibitors of cathepsin K and/or cathepsin S and are useful for the treatment of diseases and medical conditions in which cathepsin K and/or cathepsin S is implicated, e.g. various disorders including neuropathic pain, inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis, multiple sclerosis and tumours.
NOCICEPTIN ANALOGUES AND USES THEREOF
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Page 25, (2010/02/09)
The present invention relates to nociceptin analogues and uses thereof to modulate biological functions. In one aspect, the invention provides modified triazo-spiro compounds that include at least one specialized chemical group that is bound to the compou
2-CYANOPYRROLOPYRIMIDINES AND PHARMACEUTICAL USES THEREOF
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Page/Page column 39, (2010/02/08)
The invention relates to pyrrolo pyrimidines of formula (I), wherein Y represents -(CH2)t-O- or -(CH2)r-S-, p is 1 or 2, r is 1, 2 or 3, t is 1, 2 or 3, or Y is -(CH2)j- or -CH=CH-, j is 1 or 2; p is 1 or 2, or Y is -(CH2)f-, f is 1 or 2, p is 1, and the further radicals and symbols have the meaning as defined herein; their preparation, their use as pharmaceuticals, pharmaceutical compositions containing them, the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment of neuropathic pain and to a method for the treatment of such a disease in animals, especially in humans.
