- Synthesis and structure-activity relationships of CP-122,721, a second-generation NK-1 receptor antagonist
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The synthesis and SAR of benzylamine side chain analogs of the NK-1 receptor antagonist CP-99,994 are described. The 5-trifluoromethoxy analog, CP-122,721, shows superior in vivo blockade of NK-1 receptor mediated responses.
- Rosen, Terry J.,Coffman, Karen J.,McLean, Stafford,Crawford, Rosemary T.,Bryce, Dianne K.,Gohda, Yoshiko,Tsuchiya, Megumi,Nagahisa, Atsushi,Nakane, Masami,Lowe III, John A.
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- Asymmetric Synthesis of CP-99,994 by Ring-expanding Amination of Monosubstituted Prolinols
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A stereospecific synthesis of the biologically active compound (+)-CP-99,994 was achieved. The key step in this process was a ring-expansion rearrangement, in which threo-fused monosubstituted prolinol was effectively transformed to 2,3- disubstituted pip
- Yamagiwa, Noriyuki,Watanuki, Sayaka,Nishina, Takahiro,Suto, Yutaka,Iwasaki, Genji
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- Asymmetric Hydrogenation of 3-Amido-2-arylpyridinium Salts by Triply Chloride-Bridged Dinuclear Iridium Complexes Bearing Enantiopure Diphosphine Ligands: Synthesis of Neurokinin-1 Receptor Antagonist Derivatives
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We describe a most straightforward synthetic method for preparing neurokinin-1 (NK1) receptor antagonist derivatives by asymmetric hydrogenation of 3-amido-2-arylpyridinium salts using dinuclear iridium complexes with enantiopure diphosphine ligands, affo
- Iimuro, Atsuhiro,Higashida, Kosuke,Kita, Yusuke,Mashima, Kazushi
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p. 1929 - 1933
(2016/07/06)
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- Stereoselective approach to cis -2,3-disubstituted piperidines via reduction of N -acyliminium ion intermediate: Enantioselective synthesis of (+)-(2 S,3 S)-CP-99,994
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A very simple and efficient stereoselective approach to cis-2,3-disubstituted piperidines via the reduction of N-acyliminium ion intermediates is described. Application of this methodology is exemplified by the enantioselective total synthesis of (+)-(2S,3S)-CP-99,994.
- Sultane, Prakash R.,Bhat, Ramakrishna G.
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p. 11349 - 11354
(2013/02/23)
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- PHARMACEUTICAL COMPOSITIONS COMPRISING 2-METHOXY-5- (5-TRIFLUOROMETHYL-TETRAZOL-I-YL-BENZYL) - (2S-PHENYL-PIPERIDIN-3S-YL-)
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The present invention relates to pharmaceutical compositions comprising the NK1 receptor antagonist [2-Methoxy-5-(5-trifuoromethyl-tetrazol-1-yl)-benzyl]-(2S-phenyl- piperidin-3S-yl)-amine, or a pharmaceutically acceptable salt or solvate thereof, and a sodium channel blocker, as a combined preparation for simultaneous or sequential administration and to the use of such compositions in the treatment of certain disorders, including epilepsy, mood disorders and pain.
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Page/Page column 18
(2008/12/07)
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- Method for producing optical-active cis-piperidine derivatives
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An optical-active cis-piperidine derivative of high chemical purity and high optical purity is efficiently produced through optical resolution of a cis-piperidine derivative mixture, racemic cis-piperidine derivative with an optical-active tartaric acid d
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- RADIOLABELED NEUROKININ-1 RECEPTOR ANTAGONISTS
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The present invention is directed to radiolabeled neurokinin-1 receptor antagonists which are useful for the labeling and diagnostic imaging of neurokinin-1 receptors in mammals.
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- Pharmaceutical agents for the treatment of emesis
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The present invention relates to a novel process for preparing and resolving 3-amino-2-phenylpiperidine and for synthesizing from the enantiomers of such compound certain pharmaceutically active substituted 2-phenyl-3-benzylaminopiperidines. The substitut
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- F-18 radiolabeled neurokinin-1 receptor antagonists
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The present invention is directed to radiolabeled neurokinin-1 receptor antagonists which are useful for the labeling and diagnostic imaging of neurokinin-1 receptors in mammals.
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- Substituted benzylamino nitrogen containing non-aromatic heterocycles
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The present invention relates to novel substituted benzylamino nitrogen containing non-aromatic heterocycles and, specifically, to compounds of the formula STR1 wherein W, R1, R2, R3 and A are as defined in the specification, and to intermediates used in the synthesis of such compounds. The novel compounds of formula I are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.
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- STEREOSELECTIVE PREPARATION OF SUBSTITUTED PIPERIDINES
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Novel processes are disclosed for the stereoselective preparation of substituted piperidine derivatives of the formulae STR1 wherein R 1 and R 2 are defined as below, useful as substance P receptor antagonists and in treating diseases mediated by an exces
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- Tetrazole NK1 receptor antagonists: The identification of an exceptionally potent orally active antiemetic compound
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The medicinal chemistry strategy which led to the identification of GR205171, an orally active non-peptide neurokinin-1 receptor antagonist that is the most potent broad-spectrum antiemetic agent reported to date.
- Armour,Chung,Congreve,Evans,Guntrip,Hubbard,Kay,Middlemiss,Mordaunt,Pegg,Vinader,Ward,Watson
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p. 1015 - 1020
(2007/10/03)
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- 3-aminopiperidine derivatives and related nitrogen containing heterocycles and pharmaceutical compositions and use
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The present invention relates to novel 3-aminopiperidine derivatives and related nitrogen containing heterocyclic compounds, and specifically, to compounds of the formula STR1 wherein R1, R2, R3, R4, R5/su
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- 3-Aminopiperidine derivatives and related nitrogen containing heterocycles
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The present invention relates to novel 3-aminopiperidine derivatives and related nitrogen containing heterocyclic compounds, and specifically, to compounds of the formula wherein R1, R2, R3, R4, R5, R6, R7, Rsu
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