Abstract: A compound with alpha 1-blocking activity having the formula: ##STR1## wherein R.sub.1 is --H, --CH.sub.3 or --COCH.sub.3 ; R.sub.2 is --H or CH.sub.3 ; and R.sub.3 is ##STR2## wherein .SIGMA. is --H or one or more substituents selected from the group consisting of halogen, --OH and --OCH.sub.3 ; or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
April 9, 1982
Date of Patent:
April 4, 1989
Assignee:
Societe Cortial S.A.
Inventors:
Henri Pontagnier, Christian Courtiol, Marie-Helene Creuzet, Claude Feniou, Gisele Prat
Abstract: Novel mercapto-acylamino acids useful in the treatment of hypertension and combinations of mercapto-acylamino acids and atrial natriuretic peptides useful for treating hypertension are disclosed.
Type:
Grant
Filed:
March 27, 1987
Date of Patent:
January 31, 1989
Assignee:
Schering Corporation
Inventors:
Martin F. Haslanger, Bernard R. Neustadt, Elizabeth M. Smith
Abstract: Administering divided dose of oral Clonidine potentiated by an intramuscular tricyclic antidepressant alleviates the abstinence syndrome resulting from withdrawal of nicotine by smoking cessation. Patient response to the Clonidine/tricyclic serves as the basis for titrating the dosages of transdermal Clonidine and oral buspar administered daily for two weeks following the office visit. Behavioral counseling, supported by written and audio materials on diet, nutrition, exercise, stress management, and habit control, are provided to the patient. Following up support groups are also made available.
Abstract: A compound of the formula: ##STR1## wherein R.sub.1 is hydrogen, alkyl or acyl, R.sub.2 is hydroxy, alkoxy or amino, is useful as an antidiabetic agent.
Abstract: This invention relates to amino acid, dipeptide and tripeptide derivatives of 2,6-diamino-3-haloheptanedioic acids, processes for preparing the same, and their use as antibacterial agents.
Type:
Grant
Filed:
January 27, 1986
Date of Patent:
March 8, 1988
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Ekkehard H. Bohme, Fritz Gerhart, William Higgins
Abstract: New 3-[N-(mercaptoacyl)]amino-4-arylbutanoic acid derivatives are now provided, which exhibit analgesic activity and are effective to enhance the analgesia induced by a known analgesic compound, ]D-ala.sup.2,met.sup.5 ]-enkephalin (DAME).
Type:
Grant
Filed:
May 20, 1985
Date of Patent:
January 12, 1988
Assignee:
Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
Abstract: This invention relates to pharmaceutical compositions containing a class of 5-phenyl-1,3-dioxoalkenyl compounds useful as inhibitors of leukotriene biosynthesis and thus useful in the treatment of conditions associated with leukotrienes. This invention also relates to the use of the 5-phenyl-1,3-dioxoalkenyl compounds in the inhibition of leukotriene biosynthesis and thus in the treatment of conditions associated with leukotrienes. This invention further relates to a novel process for the preparation of the 5-phenyl-1,3-dioxoalkenyl compounds.
Abstract: Polyene compounds represented by the general formula ##STR1## where R.dbd.H or lower alkyl group of from 1 to 5 carbon atoms ##STR2## n is 0-1 x is O or S; andR.sub.1 =an alkyl group of from 1 to 5 carbon atoms; and the pharmaceutically acceptable salts thereof.and the pharmaceutically acceptable salts thereof.The foregoing compounds have been found to be effective in regulating the formation of lipoxygenese and as such possess therapeutic value in the treatment of inflammatory conditions and allergic responses.
Abstract: Novel compounds of the general formula ##STR1## wherein Ar represents a substituted or unsubstituted aromatic or heterocyclic group; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NR.sub.2 COR.sub.1, --NR.sub.2 CONR.sub.1 R.sub.3, --NR.sub.2 SO.sub.2 R.sub.1, --NR.sub.2 SO.sub.2 NR.sub.1 R.sub.3, or --NR.sub.2 COOR.sub.1 wherein R.sub.1, R.sub.2 and R.sub.3 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.1 is not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.1 or --NR.sub.2 COOR.sub.1, or R.sub.1 and R.sub.3 may together with N form a 5 to 7 momoered heterocyclic group; and the pharmaceutically acceptable salts thereof. These compounds exhibit .beta.-adrenergic blocking activity and are also useful in the treatment of glaucoma.
Abstract: A method for the treatment of glaucoma or lowering intraocular pressure in a mammal, involving topically administering to the eye of such mammal a selectively metabolized beta-blocking compound of the formula ##STR1## wherein R may be lower alkyl, lower alkynyl aryl, or aralkyl; A may be a direct bond, lower alkylenyl, or lower alkenyl; x may be an integer from 1 to 3; Ar may be substituted or unsubstituted aromatic; R.sub.1 may be lower alkyl, lower hydroxy alkyl, lower alkenyl, lower alkynyl, or aralkyl; and pharmaceutically accepted salts thereof. Because of a relatively long duration of action of such compounds in ocular fluids and a relatively short duration of action in the systemic circulation, such compounds are useful for the treatment of excessive intraocular pressure without substantial systemic side effects.
Abstract: New compositions using particular .beta..sub.2 agonists and vehicle materials have been prepared and are useful for producing a topical anti-inflammatory effect in mammals. The selected .beta..sub.2 agonists have previously not been known to exhibit topical anti-inflammatory activity. The compositions can be for example in the form of sprays, ointments, creams, gels, lotions, and suppositories, all of which are to be applied to the mammal topically, as opposed to systemically.
Abstract: Amidino compounds represented by the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful anti-trypsine, anti-plasmin, anti-kallikrein and anti-thrombin agents. Having strong anti-Cl (Clr, Cls) activities and an anticomplement activity, they are also useful as anticomplement agents. These amidino compounds are prepared by usual esterification of carboxylic acid compounds represented by the formula (II)R.sub.1 --COOH (II)with amidinophenol compound (III) and, if necessary, can be transformed into pharmaceutically acceptable acid addition salts thereof.
Abstract: Amidino compounds represented by the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful antitrypsine, antiplasmin, antikallikrein and antithrombin agents. Having strong anti-C1 (C1r, C1s) activities and an anticomplement activity, they are also useful as anticomplement agents. These amidino compounds are prepared by usual esterification of carboxylic acid compounds represented by the formula ##STR2## with 6-amidino-2-naphthol and, if necessary, can be transformed into pharmaceutically acceptable acid addition salts thereof.