摘要:
The present invention provides compounds having store overload-induced Ca2+ release (SOICR) inhibitory activity and methods for producing and using the same. In particular, compounds of the invention is of the formula: R1—X1-L-X2—R2, wherein R1, X1, L, X2, and R2 are those defined herein.
摘要:
Compounds of the formula (II): ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.1 is phenyl or naphthyl or substituted phenyl or naphthyl group; R.sub.2 is: ##STR2## wherein R.sub.5 is hydrogen or C.sub.1-6 alkyl, R.sub.6 is hydrogen or C.sub.1-6 alkyl, phenyl, tolyl or benzyl and R.sub.7 is hydrogen; R.sub.3 and R.sub.4 are each hydrogen atom or C.sub.1-4 alkyl, and X is CO, CHOH, CHCI or C.dbd.C R.sub.8 R.sub.9 wherein R.sub.8 and R.sub.9 are each hydrogen or C.sub.1-4 alkyl; or CR.sub.10 OH or CHR.sub.10, wherein R.sub.10 is C.sub.1-4 alkyl, have been found to be mood-modifying agents and anorexic agents.
摘要:
A process for making 5-(d-3-(tert-butylamino)-2-hydroxypropoxy)-1,2,3,4-tetrahydro-1-cis-2,3 naphthalenediol of the formula ##STR1## by reacting ##STR2## in an essentially water free environment with (a) M'IO.sub.3 wherein M' represents a suitable ion for forming the salt.(b) I.sub.2 (iodine)(c) CH.sub.3 COO.sup.- M".sup.+ wherein M" represents a suitable ion for forming the salt(d) glacial acetic acid and(e) ROH/M'"OH where R is alkyl and M'" is a suitable metal ion.
摘要:
The present invention relates to a compound of formula I, ##STR1## wherein A is straight chain alkylene of 2 to 4 carbon atoms, or straight chain alkenylene of 2 to 4 carbon atoms,n is 1, 2 or 3,R is hydrogen or halogen of atomic number from 9 to 35, andeither (i) R.sub.1 is a group of formula II, ##STR2## wherein R.sub.2 and R.sub.3, independently, are hydrogen or alkyl of 1 to 4 carbon atoms, andR.sub.4 is alkyl of 1 to 4 carbon atoms, alkoxyalkyl of 2 to 5 carbon atoms, alkylthioalkyl of 2 to 5 carbon atoms, phenylalkyl or phenoxyalkyl or phenylthioalkyl, wherein the alkyl moiety has from 1 to 3 carbon atoms, or phenyl, the phenyl ring of each of the last four radicals being unsubstituted or mono-substituted by, or disubstituted independently by, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, hydroxy or halogen of atomic number from 9 to 35, andR.sub.5 is hydrogen,or (ii) R.sub.1 and R.sub.5 together with the nitrogen atom to which they are bound are (a) 2,2,6,6-tetramethylpiperidinyl, (b) 2,2,5,5-tetramethylpyrrolidinyl,or (c) piperazinyl substituted in the 4 position by alkyl of 1 to 4 carbon atoms or phenyl which is unsubstituted, or mono-substituted by, or di-or tri-substituted independently by, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, or halogen of atomic number from 9 to 35,useful as anti-hypertensives.
摘要:
A PROCESS FOR THE RESOLUTION OF DL-5-(3-(TERT-BUTYLAMINO) - 2-HYDROXYPROPOXY)-3,4-DIHYDRO-1(2H)NAPHTHALEONONE INTO A (+) ISOMER AND A (-) ISOMER ACCORDING TO THE FOLLOWING SCHEMATIC DIAGRAM:
THE (-) ISOMER THUS OBTAINED IS ABOUT SIXTY TIMES MORE POTENT AS A B-ADRENERGIC BLOCKING AGENT THAT THE (+) ISOMER AND ABOUT TWICE THE POTENCY OF THE RACEMATE.
摘要:
Provided are polyglyceryl compositions comprising one or more polyglyceryl compounds having: (a) a node structure comprising at least three contiguous glyceryl remnant units; (b) one or more cationic groups each linked to the node structure by an independently selected linking group; and (c) one or more hydrophobic moieties each independently (i) linked to the node structure by a linking group, or (ii) constituting a portion of one of the one or more cationic groups, wherein the composition has an average degree of polymerization determined by hydroxyl value testing (DPOH) of from about 3 to about 20. Also provided are polyglyceryl compounds which may compose such compositions, and uses of the polyglyceryl compositions and compounds.
摘要:
5,6,7,8-Tetrahydro-1,6,7-naphthalenetriols having the formula ##STR1## wherein R.sup.8, R.sup.9 and R.sup.10 are the same or different and are hydrogen, lower alkyl, monocyclic aryl-lower alkyl, lower alkoxy, carboxy, or monocyclic cycloalkyl, are intermediates useful in the preparation of compounds used to treat coronary diseases.
摘要:
Compounds having the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are hydrogen or acyl, and R.sub.4 is lower alkyl having utility in the treatment of coronary diseases.
摘要:
The present invention features calcilytic compounds. "Calcilytic compounds" refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.
摘要:
This invention relates to new cyclic polymethylene phenoxyaminopropanols and related compounds of the formula AND TO SALTS OF SUCH COMPOUNDS, WHICH ARE USEFUL IN CORONARY DISEASES, LOWERING BLOOD PRESSURE, AS CENTRAL NERVOUS SYSTEM DEPRESSANTS, WATER SOFTENING AND CORROSION INHIBITION.