- Substituted aza indole compounds and salts thereof, composition and use thereof
-
The invention provides a substituted azaindole compound having a structure as represented by a formula (I) and a pharmaceutically acceptable salt and a medicinal preparation thereof. The compound is used for adjusting activity of protein kinase and adjusting intercellular or intracellular signal response. The invention further relates to a pharmaceutical composition including the compound and a method of applying the pharmaceutical composition to treatment of highly proliferative diseases of mammals, especially of mankind.
- -
-
Paragraph 0402; 0404; 0405
(2018/11/03)
-
- SUBSTITUTED AZAINDOLE COMPOUNDS, SALTS, PHARMACEUTICAL COMPOSITIONS THEREOF AND METHODS OF USE
-
The present invention provides substituted azaindole prodrugs, methods of making said prodrugs, pharmaceutical compositions of said prodrugs and methods of using said prodrugs and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as cancer.
- -
-
Paragraph 0306-0308
(2014/03/24)
-
- PRODRUGS OF FUSED HETEROCYCLIC INHIBITORS OF D-AMINO ACID OXIDASE
-
The invention relates to prodrugs of fused heterocyclic inhibitors of D-amino oxidase (DAAO) and methods of treating diseases and conditions, wherein modulation of D-amino acid oxidase activity, D-serine levels, D-serine oxidative products and NMDA receptor activity in the nervous system of a mammalian subject is effective.
- -
-
Page/Page column 98
(2011/02/26)
-
- GABA ANALOGS, COMPOSITIONS, AND METHODS FOR MANUFACTURING THEREOF
-
The invention provides novel compounds of Formula (I), pharmaceutical compositions and methods of synthesis thereof.
- -
-
Page/Page column 23-24
(2009/10/22)
-
- GABA ANALOGS, COMPOSITIONS AND METHODS FOR MANUFACTURING THEREOF
-
The invention provides novel compounds of Formula (I), pharmaceutical compositions and methods of synthesis thereof.
- -
-
Page/Page column 9
(2008/12/05)
-
- Phosphonic acid derivatives as inhibitors of protein tyrosine phosphatase 1B (PTP-1B)
-
The invention encompasses the novel class of compounds represented by formula I, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and conditions related to diabetes.
- -
-
-
- Biphenyl-substituted quinoline derivatives
-
Compounds of the formula wherein X, R1, R2, R3, R4, R5, R6, A, B, D and E are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.
- -
-
-
- Quinoxaline biphenyl angiotensin II inhibitors
-
Angiotensin II inhibition is exhibited by STR1 wherein: X is --CH2 -- or O; R is hydrogen, alkyl, aryl, cycloalkyl, aralkyl, or cycloalkylalkyl; R1 and R2 are each independently O or absent; R3 is hydrogen, alkyl, alkenyl, alkoxy, cycloalkyl, aryl, aralkyl, cycloalkylalkyl, halo, haloalkyl, or haloalkoxy; R4 is hydrogen, alkyl, alkenyl, alkoxy, aryl, cycloalkyl, aralkyl, cycloalkylalkyl, --R8 --OH, or --R8 CO2 R9 ; and the remaining symbols are as defined in the specification.
- -
-
-
- Indole- and benzimidazole-substituted imidazole and benzimidazole derivatives
-
Novel compounds are disclosed having the formula STR1 wherein X, R1, R2, R3, R4, and R5 are substituents. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.
- -
-
-
- Method for preparing phosphinic acids used in preparing ace inhibitors and intermediates produced thereby
-
A method is provided for preparing phosphinic acid compounds, which are useful in preparing certain angiotensin converting enzyme inhibitors, which have the formula STR1 wherein R 1 is lower alkyl, aryl, arylalkyl, cycloalkyl or cycloalkylalkyl;R 2 is hydrogen, lower alkyl or arylalkyl;X is hydrogen, lower alkyl or phenyl;Y is hydrogen, lower alkyl, phenyl or alkoxy, or together X and Y are --(CH 2) 2 --, --(CH 2) 3 --, --CH CH--, or STR2 and n is 0 or 1including salts thereof and stereoisomers thereof, which method includes the steps of reacting a phosphinic acid ester of the structure STR3 wherein R 3 is a group removable by hydrogenolysis such as benzyl or substituted benzyl, with a halo ester of the structure STR4 in the presence of an organic base to form a phosphinic acid ester of the structure STR5 hydrogenating the above ester to form a diastereomic mixture of a phosphinic acid of the structure STR6 recrystallizing to recover the preferred racemic mixture and resolving same employing a resolving agent, preferably L-cinchonidine, to form the corresponding resolved salt which may be acidified to the corresponding acid. In addition, novel intermediates which are acids and salts as described above are also provided.
- -
-
-
- RETROPINACOLIN REARRANGEMENT OF ACYLOXYCARBOCATIONS FROM α-BRANCHED ALDEHYDES
-
α-Chloroalkyl esters, formed by the addition of acyl chlorides to α-branched aldehydes, undergo quantitative rearrangement under the influence of antimony pentachloride, giving stable 1,3-dioxolanium salts.
- Luk'yanov, S. M.,Borodaev, S. V.,Borodaeva, S. V.
-
p. 1872 - 1875
(2007/10/02)
-