512822-50-3Relevant articles and documents
SUBSTITUTED 4-PIPERIDINYL-QUINAZOLINES, 4-PIPERIDINYL-PYRIMIDINE-2-AMINES, AND RELATED COMPOUNDS AND THEIR USE IN TREATING MEDICAL CONDITIONS
-
, (2022/03/22)
The invention provides substituted 4-piperidinyl-quinazolines, 4-piperidinyl-pyrimidine-2-amines, and related compounds, pharmaceutical compositions, their use for inhibiting ERK5 activity, and their use in the treatment of medical disorders, such as cancer.
ARYLMETHYLENE HETEROCYCLIC COMPOUNDS AS KV1.3 POTASSIUM SHAKER CHANNEL BLOCKERS
-
, (2021/04/17)
A compound of Formula (I) or a pharmaceutically acceptable salt thereof is described, wherein the substituents are as defined herein. Pharmaceutical compositions comprising the same and method of using the same are also described.
THERAPEUTIC METHODS AND COMPOUNDS
-
Page/Page column 65-66, (2020/11/03)
The invention provides a compound of formula I: (I) or a pharmaceutically acceptable salt thereof, wherein R1-R5 Y have any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful to treat malaria.
COMPOUNDS USEFUL FOR ALTERING THE LEVELS OF BILE ACIDS FOR THE TREATMENT OF DIABETES AND CARDIOMETABOLIC DISEASE
-
, (2018/03/09)
Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as Cyp8b1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for diabetes and cardiovascular disease.
COMPOUNDS USEFUL FOR ALTERING THE LEVELS OF BILE ACIDS FOR THE TREATMENT OF DIABETES AND CARDIOMETABOLIC DISEASE
-
Page/Page column 79, (2018/03/09)
Described herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as Cyp8b1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for diabetes and cardiovascular disease.
2′ Biaryl amides as novel and subtype selective M1 agonists. Part I: Identification, synthesis, and initial SAR
Budzik, Brian,Garzya, Vincenzo,Shi, Dongchuan,Foley, James J.,Rivero, Ralph A.,Langmead, Christopher J.,Watson, Jeannette,Wu, Zining,Forbes, Ian T.,Jin, Jian
scheme or table, p. 3540 - 3544 (2010/08/22)
Biaryl amides were discovered as novel and subtype selective M1 muscarinic acetylcholine receptor agonists. The identification, synthesis, and initial structure-activity relationships that led to compounds 3j and 4c, possessing good M1 agonist potency and intrinsic activity, and subtype selectivity for M1 over M2-5, are described.
2′ Biaryl amides as novel and subtype selective M1 agonists. Part II: Further optimization and profiling
Budzik, Brian,Garzya, Vincenzo,Shi, Dongchuan,Walker, Graham,Lauchart, Yann,Lucas, Adam J.,Rivero, Ralph A.,Langmead, Christopher J.,Watson, Jeannette,Wu, Zining,Forbes, Ian T.,Jin, Jian
experimental part, p. 3545 - 3549 (2010/08/22)
Further optimization of the biaryl amide series via extensively exploring structure-activity relationships resulted in potent and subtype selective M 1 agonists exemplified by compounds 9a and 9j with good rat PK properties including CNS penetration. Synthesis, structure-activity relationships, subtype selectivity for M1 over M2-5, and DMPK properties of these novel compounds are described.
1,2,4-OXADIAZOLE SUBSTITUTED PIPERIDINE AND PIPERAZINE DERIVATIVES AS SMO ANTAGONISTS
-
Page/Page column 49, (2010/04/03)
The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts, stereoisomers or tautomers thereof which are inhibitors of the Sonic Hedgehog pathway, in particular Smo antagonists. Thus the compounds of this invention are useful for the treatment of diseases associated with abnormal hedgehog pathway activation, including cancer, for example basal cell carcinoma, medulloblastoma, prostate, pancreatic, breast, colon, bone and small cell lung cancers, and cancers of the upper GI tract.
ANTI-INFLAMMATORY COMPOUNDS
-
Page/Page column 31-32, (2008/06/13)
The use of a steroid sulfatase inhibitor in the preparation of a medicament for the treatment of inflammatory diseases.
COMBINATION OF A STEROID SULFATASE INHIBITOR AND AN ASCOMYCIN
-
Page/Page column 33-34, (2010/11/23)
A combination of a steroid sulfatase inhibitor and an ascomycin, which combination is useful as a pharmaceutical.