- TREATMENT OF CDK4/6 INHIBITOR RESISTANT NEOPLASTIC DISORDERS
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This invention is to methods for treating disorders involving abnormal cellular proliferation that have developed resistance to a selective CDK4/6 inhibitor.
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- HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF ABNORMAL CELLULAR PROLIFERATION
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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.
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Page/Page column 135
(2019/07/20)
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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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supporting information
p. 54 - 56
(2016/01/20)
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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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- Synthesis of versatile bifunctional derivatives of chiral diamines obtained through anchimerically assisted nucleophilic substitution reactions on diastereomeric phenylprolinols
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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.
- Vargas-Caporali, Jorge,Cruz-Hernandez, Carlos,Juaristi, Eusebio
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p. 1275 - 1300
(2013/08/23)
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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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- A direct stereoselective approach to trans-2,3-disubstituted piperidines: Application in the synthesis of 2-Epi-CP-99,994 and (+)-epilupinine
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(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.
- Ahari, M'Hamed,Perez, Amandine,Menant, Christine,Vasse, Jean-Luc,Szymoniak, Jan
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supporting information; experimental part
p. 2473 - 2476
(2009/05/27)
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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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- The amino thiourea-catalyzed asymmetric nucleophilic reactions
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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
- Takemoto, Yoshiji,Miyabe, Hideto
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p. 269 - 275
(2008/02/06)
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- Hemiaminals as substrates for sulfur ylides: Direct asymmetric syntheses of functionalised pyrrolidines and piperidines
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Phenyl stabilised chiral sulfur ylides react with five-membered-ring hemiaminals to give functionalised pyrrolidines directly with high enantioselectivity. The reaction can be diverted to give piperidines instead by isolation of the intermediate epoxide and treatment with TMSOTf. The Royal Society of Chemistry 2006.
- Kokotos, Christoforos G.,Aggarwal, Varinder K.
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p. 2156 - 2158
(2008/03/14)
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- Bifunctional-thiourea-catalyzed diastereo- And enantioselective Aza-Henry reaction
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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.
- Xu, Xuenong,Furukawa, Tomihiro,Okino, Tomotaka,Miyabe, Hideto,Takemoto, Yoshiji
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p. 466 - 476
(2008/09/20)
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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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- SYNTHESIS OF ARYL-SUBSTITUTED PIPERIDINES BY HYDROGENATION OF ARYL-SUBSTITUTED PYRIDINES
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The invention is a process to hydrogenate an aryl-substituted pyridine, such as 2-phenyl-3-aminopyridine, without over-reducing the aryl ring using a specific Pt/C catalyst.
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- 5-PHENYLBENZYLAMINE COMPOUNDS, PROCESS FOR THEIR PRODUCTION AND INTERMEDIATES FOR THEIR SYNTHESIS
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The present invention relates to a 5-phenylbenzylamine compound represented by the formula [1]: wherein Ring A represents a phenyl group having a substituent(s), ???Ra, Rb1 and Rb2 each represent hydrogen atom, a halogen a
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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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- 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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p. 281 - 284
(2007/10/03)
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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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