160551-72-4Relevant academic research and scientific papers
TREATMENT OF CDK4/6 INHIBITOR RESISTANT NEOPLASTIC DISORDERS
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, (2020/10/19)
This invention is to methods for treating disorders involving abnormal cellular proliferation that have developed resistance to a selective CDK4/6 inhibitor.
HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF ABNORMAL CELLULAR PROLIFERATION
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Page/Page column 135, (2019/07/20)
This invention is in the area of heterocyclic-based compounds for the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers.
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
Iimuro, Atsuhiro,Higashida, Kosuke,Kita, Yusuke,Mashima, Kazushi
, p. 1929 - 1933 (2016/07/06)
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
Asymmetric Synthesis of CP-99,994 by Ring-expanding Amination of Monosubstituted Prolinols
Yamagiwa, Noriyuki,Watanuki, Sayaka,Nishina, Takahiro,Suto, Yutaka,Iwasaki, Genji
supporting information, p. 54 - 56 (2016/01/20)
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
Synthesis of versatile bifunctional derivatives of chiral diamines obtained through anchimerically assisted nucleophilic substitution reactions on diastereomeric phenylprolinols
Vargas-Caporali, Jorge,Cruz-Hernandez, Carlos,Juaristi, Eusebio
, p. 1275 - 1300 (2013/08/23)
Diastereomeric [(S)-1-benzylpyrrolidin-2-yl]-(R)-[(phenyl)- methanamine] and [(S)-1-benzylpyrrolidin-2-yl]-(S)-[(phenyl)methanamine], were synthesized by selective internal backside nucleophilic substitution of the corresponding activated phenylprolinols. X-Ray diffraction structures of crystalline acetamide derivatives confirmed the anticipated stereochemistry for a SNib reaction mechanism. In order to apply this reaction to the synthesis of bifunctional analogs, a series of fragments such as a thiourea moiety and sulfonamide functions were introduced for the functionalization of the primary amino group in the substrate, obtaining more stable and potentially useful derivatives.
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
Sultane, Prakash R.,Bhat, Ramakrishna G.
, p. 11349 - 11354 (2013/02/23)
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.
PHARMACEUTICAL COMPOSITIONS COMPRISING 2-METHOXY-5- (5-TRIFLUOROMETHYL-TETRAZOL-I-YL-BENZYL) - (2S-PHENYL-PIPERIDIN-3S-YL-)
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Page/Page column 18, (2008/12/07)
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.
A direct stereoselective approach to trans-2,3-disubstituted piperidines: Application in the synthesis of 2-Epi-CP-99,994 and (+)-epilupinine
Ahari, M'Hamed,Perez, Amandine,Menant, Christine,Vasse, Jean-Luc,Szymoniak, Jan
supporting information; experimental part, p. 2473 - 2476 (2009/05/27)
(Chemical Equation Presented) A simple synthesis of enantiomerically pure piperidine esters is described, offering a straightforward access to the trans-2,3-disubstituted piperidine skeleton which is present in a broad range of biologically active compounds.
The amino thiourea-catalyzed asymmetric nucleophilic reactions
Takemoto, Yoshiji,Miyabe, Hideto
, p. 269 - 275 (2008/02/06)
Bifunctional amino thiourea-catalyzed asymmetric additions of several nucleophiles into electron-deficient unsaturated compounds such as nitroolefins, α,β-unsaturated imides, imines, and azodicarboxylates are described. We discovered that bifunctional thi
Bifunctional-thiourea-catalyzed diastereo- And enantioselective Aza-Henry reaction
Xu, Xuenong,Furukawa, Tomihiro,Okino, Tomotaka,Miyabe, Hideto,Takemoto, Yoshiji
, p. 466 - 476 (2008/09/20)
Bifunctional thiourea 1a catalyzes aza-Henry reaction of nitroalkanes with N-Boc-imines to give syn-β-nitroamines with good to high diastereo- and enantioselectivity. Apart from the catalyst, the reaction requires no additional reagents such as a Lewis acid or a Lewis base. The N-protecting groups of the imines have a determining effect on the chirality of the prod ucts, that is, the reaction of N-Bocimines gives R adducts as major products, whereas the same reaction of N-phosphonoylimines furnishes the corresponding S adducts. Various types of nitroalkanes bearing aryl, alcohol, ether, and ester groups can be used as nucleophiles, providing access to a wide range of useful chiral building blocks in good yield and high enantiomeric excess. Synthetic versatility of the addition products is demonstrated by the transformation to chiral piperidine derivatives such as CP-99,994.
