199105-03-8Relevant articles and documents
N-(PHENYL)-2-(PHENYL)PYRIMIDINE-4-CARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS AS HPK1 INHIBITORS FOR TREATING CANCER
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Page/Page column 175, (2019/09/12)
The present invention relates to N-(phenyl)-2-(phenyl)pyrimidine-4- carboxamide derivatives and related compounds of formula I as HPK1 (Hematopoietic progenitor kinase 1) inhibitors for treating cancer, such as e.g. breast cancer, colorectal cancer, lung cancer, ovarian cancer, and pancreatic cancer. Preferred compounds are e.g. N-(5-Fluoro-2-(2-(pyridin-2-yl)pyrrolidin-l-yl)phenyl)-2-(2- fluoro-6-methoxyphenyl)pyrimidine-4-carboxamide and N-(5-Fluoro-2- (hexahydropyrrolo[3,4-b]pyrrol-l(2H)-yl)phenyl)-2-(2-fluoro-6- methoxyphenyl)pyrimidine-4-carboxamide.
Practical synthesis of pharmaceutically relevant molecules enriched in sp3 character
Campbell, Peter S.,Jamieson, Craig,Simpson, Iain,Watson, Allan J. B.
, p. 46 - 49 (2017/12/27)
The expedient synthesis of compounds enriched in sp3 character is key goal in modern drug discovery. Herein, we report how a single pot Suzuki-Miyaura-hydrogenation can be used to furnish lead and fragment-like products in good to excellent yields. The approach has been successfully applied in formats amenable to parallel synthesis, in an asymmetric sense, and in the preparation of molecules with annotated biological activity.
SMALL MOLECULE AGONISTS OF NEUROTENSIN RECEPTOR 1
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, (2016/04/26)
Provided herein are small molecule neurotensin receptor agonists, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.
ANILINOPIPERAZINE DERIVATIVES AND METHODS OF USE THEREOF
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Page/Page column 119, (2008/12/05)
The present invention relates to novel Anilinopiperazine Derivatives of Formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, cancer, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.
Substituted piperidines and methods of use
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Page 34, (2010/02/05)
Selected substituted piperidine compounds are effective for prophylaxis and treatment of diseases, such as obesity and the like. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving activation of the melanocortin receptor. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
N-SUBSTITUTED NAPHTHALENE CARBOXAMIDES AS NEUROKININ-RECEPTOR ANTAGONISTS
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, (2008/06/13)
A compound of formula I wherein: R is alkyl; R1 is optionally substituted phenyl 2-oxo-tetrahydro-1(2H)-pyrimidinyl, or 2-oxo-1-piperidinyl; R2 is hydrogen, alkoxy, alkanoyloxy, alkoxycarbonyl, alkanoylamino, acyl, alkyl, carbamoyl, N-alkylcarbamoyl, N,N-dialkylcarbamoyl where the alkyl groups are the same or different, hydroxy, thioacyl, thiocarbamoyl, N-alkylthiocarbamoyl, or N,N-dialkylthiocarbamoyl where the alkyl groups are the same or different. X1 and X2 are independently hydrogen or halo, provided that at least one of X1 or X2 is halo; and R3, R4, R5 and R6 are independently hydrogen, cyano, nitro, trifluoromethoxy, trifluoromethyl, or alkylsulfonyl are antagonists of at least one tachykinin receptor and are useful in the treatment of depression, anxiety, asthma, pain, inflammation, urinary incontinence and other disease conditions. Process for their preparation are described, as are compositions containing them and their use.
Serine derived NK1 antagonists 2: A pharmacophore model for arylsulfonamide binding
Elliott,Broughton,Cascieri,Chicchi,Huscroft,Kurtz,MacLeod,Sadowski,Stevenson
, p. 1851 - 1856 (2007/10/03)
Modifications to the spirocyclic aryl sulfonamide portion of serine derived NK1 antagonists allow a partial pharmacophore model to be developed.