103500-23-8Relevant articles and documents
INHIBITORS OF APOL1 AND METHODS OF USING SAME
-
Paragraph 00334, (2020/07/14)
The disclosure provides at least one entity chosen from compounds of formula (I), solid state forms of the same, compositions comprising the same, and methods of using the same, including use in treating focal segmental glomerulosclerosis (FSGS) and/or non-diabetic kidney disease (NDKD).
CHEMICAL COMPOUNDS
-
Page/Page column 86, (2020/06/01)
A compound of formula (I), wherein Ar1, R21, R23, R24, R25, R26, R27, A, X, Y and W are as defined herein. The compounds of the present invention are inhibitors of hematopoietic prostaglandin D synthase (H-PGDS) and can be useful in the treatment of Duchenne muscular dystrophy. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting H-PGDS activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
PEPTIDOMIMETIC COMPOUNDS AND ANTIBODY-DRUG CONJUGATES THEREOF
-
, (2015/07/07)
This invention relates to peptidomimetic linkers and anti-body drug conjugates thereof, to pharmaceutical compositions containing them, and to their use in therapy for the prevention or treatment of cancer.
4-PYRIDINONETRIAZINE DERIVATIVES AS HIV INTEGRASE INHIBITORS
-
Page/Page column 61, (2014/07/08)
The present invention relates to 4-Pyridinonetriazine Derivatives of Formula (I); and pharmaceutically acceptable salts thereof, wherein A, X, Y, R1, R2, R3 and R5 are as defined herein. The present invention also relates to compositions comprising at least one 4-Pyridinonetriazine Derivative, and methods of using the 4-Pyridinonetriazine Derivatives for treating or preventing HIV infection in a subject.
SELECTIVE KINASE INHIBITORS
-
, (2013/06/06)
Provided are pyrimidine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
IMIDAZOTHIAZOLE DERIVATIVE HAVING 4,7-DIAZASPIROY2.5¨OCTANE RING STRUCTURE
-
Page/Page column 93, (2011/04/18)
There is provided a novel compound that inhibits the interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity. The present invention provides an imidazothiazole derivative represented by the following formula (1) having various substituents that inhibits the interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity: wherein R1 R2, R3, R4, R5, Ar1, and Ar2 in formula (1) each have the same meanings as defined in the specification.
HYDROXY PYRIDOPYRROLOPYRAZINE DIONE COMPOUNDS USEFUL AS HIV INTEGRASE INHIBITORS
-
Page/Page column 115, (2010/02/11)
Hydroxy-substituted pyridopyrrolopyrazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I): (I) wherein a, b, A, B, R1, R2, R3, R4, R5, R6, R7 and R8 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
Inactivation of γ-Aminobutyric Acid Aminotransferase by (S,E)-4-Amino-5-fluoropent-2-enoic Acid and Effect on the Enzyme of (E)-3-(1-Aminocyclopropyl)-2-propenoic Acid
Silverman, Richard B.,Invergo, Benedict J.,Mathew, Jacob
, p. 1840 - 1846 (2007/10/02)
(S,E)-4-Amino-5-fluoropent-2-enoic acid (6) is synthesized in six steps starting from the known γ-aminobutyric acid aminotransferase (γ-Abu-T) inactivator, (S)-4-amino-5-fluoropentanoic acid (1).Compound 6 is a mechanism-based inactivator of γ-Abu-T: time-dependent inactivation is saturable and protected by substrate; thiols do not protect the enzyme from inactivation; no enzyme activity returns upon dialysis.This compound (6) binds 50 times more tightly to γ-Abu-T than does the saturated analogue (1).No transamination of 6 occurs prior to inactivation.However, five molecules of 6 are required to inactivate the enzyme with concomitant release of five fluoride ions.Therefore, four molecules are being converted to product for each inactivation event. (E)-3-(1-Aminocyclopropyl)-2-propenoic acid is synthesized in seven steps from 1-aminocyclopropanecarboxylic acid.It is prepared as a cyclopropyl derivative of the proposed intermediate in the inactivation of γ-Abu-T by 6.The cyclopropyl derivative, however, is a noncompetitive inhibitor and does not inactivate the enzyme.This study shows the usefulness and hazards of incorporation of a trans double bond into potential γ-Abu-T inactivators.
