摘要:
A chromogenic compound of normally colorless form is disclosed having the following structural formula: ##STR1## wherein A and B can be ##STR2## X and Y can be aryl and heterocyclic, each substituted Z is hydrogen and E can be tetrachloro-and tetrabromo-substituted ##STR3## STRUCTURES. The compound is eligible for use in pressure-sensitive record materials and manifold marking systems. Because of light absorption characteristics, selected compounds of this invention are especially useful where machine readability and machine copiability are important.
摘要:
THE COMPOUNDS ARE OF THE CLASS OF INDOLE DERIVATIVES, MORE PARTICULARLY INDOLE DERIVATIVES SUBSTITUTED IN 2- AND 3-POSITIONS AND ACID ADDITION SALTS THEREOF. THE COMPOUNDS ARE USEFUL AS ANALGESIC, ANTI-INFLAMMATORY, ANTITUSSIVE, TRANQUILIZING, ANTI-ALLERGIC AND ANAESTHESIA-POTENTIATING AGENTS. AN ILLUSTRATIVE EMBODIMENT IS 2-BENZOYL-3(2-PYRROLIDINOETHOXY)INDOLE.
WHEREIN X IS HYDROGEN, LOWER-ALKYL, HALOGEN OR -CF3; WHEREIN R1 AND R2 ARE LOWER-ALKYL OR -C6H4X'' IN WHICH X'' IS HYDROGEN, LOWER-ALKYL, HALOGEN, LOWER-ALKOXY OR -CF3; WHEREIN R3 IS LOWER-ALKYL OR TOGETHER -N(R3)2 IS 1-PYRROLIDINYL, 1-PIPERIDINYL OR 4-MORPHOLINYL; AND WHEREIN N IS AN INTEGER FROM 2 TO 4, INCLUSIVE, ARE MADE FROM 3H-INDOL-3-OLS. THE PRODUCTS AS WELL AS THEIR PHARMACOLGICALLY ACCEPTABLE ACID ADDITION SALTS HAVE SEDATIVE ACTIVITY AND CAN BE ADMINISTERED TO TRANQUILIZE MAMMALS.
摘要:
NEW 3-SUBSTITUTED-1 - INDOLE- AND 4,5,6,7 - TETRAHYDROINDOLE-LOWER-ALKANOIC ACIDS AND ESTERS HAVING USEFUL ANTIINFLAMMATORY ACTIVITY AND PREPARED BY ALKYLATION OF A 3 - SUBSTITUTED - INDOLE WITH AN APPROPRIATE HALO-LOWER-ALKANOIC ACID OR ESTER OR BY CYCLIZATION OF A 2-(2-R2-2-OXOETHYL) CYCLOHEXANONE OR 2-(1 -PHENYL-2-OXO-LOWER-ALKYL) CYCLOHEXANONE WITH AN AMINO ACID OR ESTER.
摘要:
A compound having one of the following structures of Formula (IV) or (V):
or a stereoisomer, salt, or tautomer thereof, wherein R1, R2, R3, R4, R5 R6, R7, R8, R10, R11a R11b, R12a R12b, X, Y, and Z are as defined herein. Pharmaceutical composition comprising the compounds, and their use in methods of treating diseases are also described.
摘要:
The disclosure relates to novel compounds and methods of use of the compounds to maintain the Gαi2 protein in its inactive GDP-bound state. The disclosure describes the knockdown or inhibition of Gαi2 negatively regulated migration of breast and ovarian cancer cell lines. The novel compounds inhibit the migratory behavior of PC3, DU145 and E006AA prostate cancer cell lines. Specifically, the novel compounds block the activation of Gαi2 in oxytocin-stimulated prostate cancer PC3 cells and inhibits the migratory capability of DU145 cells overexpressing constitutively active form of Gαi2, under basal and EGF-stimulated conditions.
摘要:
The present invention relates to novel compounds which are capable of inhibiting certain amine oxidase enzymes. These compounds are useful for treatment of a variety of indications, e.g., fibrosis, cancer and/or angiogenesis in human subjects as well as in pets and livestock. In addition, the present invention relates to pharmaceutical compositions containing these compounds, as well as various uses thereof.