Nitrogen In Y Moiety Patents (Class 514/540)
  • Patent number: 4818772
    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
  • Patent number: 4801609
    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
  • Patent number: 4788189
    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.
    Type: Grant
    Filed: February 29, 1988
    Date of Patent: November 29, 1988
    Inventor: Howard I. Glazer
  • Patent number: 4767781
    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.
    Type: Grant
    Filed: December 8, 1986
    Date of Patent: August 30, 1988
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Susumu Shinagawa, Tsuneo Kanamaru, Setsuo Harada
  • Patent number: 4730006
    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
  • Patent number: 4719231
    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
    Inventors: Hamao Umezawa, Tomio Takeuchi, Takaaki Aoyagi, Mitsugu Hachisu, Masao Hirayama, Shinjiro Murata, Shunzo Fukatsu
  • Patent number: 4649157
    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.
    Type: Grant
    Filed: March 28, 1986
    Date of Patent: March 10, 1987
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Partis, Richard A. Mueller
  • Patent number: 4595696
    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.
    Type: Grant
    Filed: September 13, 1985
    Date of Patent: June 17, 1986
    Assignee: USV Pharmaceutical Corp.
    Inventors: Bernard Loev, Wan-Kit Chan
  • Patent number: 4582855
    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.
    Type: Grant
    Filed: November 12, 1981
    Date of Patent: April 15, 1986
    Assignee: American Hospital Supply Corporation
    Inventors: Sheung T. Kam, William L. Matier
  • Patent number: 4578403
    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.
    Type: Grant
    Filed: June 11, 1984
    Date of Patent: March 25, 1986
    Assignee: American Hospital Supply Corporation
    Inventor: William L. Matier
  • Patent number: 4574129
    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.
    Type: Grant
    Filed: May 23, 1985
    Date of Patent: March 4, 1986
    Assignee: Bristol-Myers Company
    Inventors: Xina Nair, Davis L. Temple, Jr.
  • Patent number: 4570006
    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.
    Type: Grant
    Filed: October 24, 1984
    Date of Patent: February 11, 1986
    Assignee: Torii & Co. Ltd.
    Inventors: Setsuro Fujii, Takashi Yaegashi, Toyoo Nakayama, Yojiro Sakurai, Shigeki Nunomura, Toshiyuki Okutome
  • Patent number: 4532255
    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.
    Type: Grant
    Filed: January 20, 1984
    Date of Patent: July 30, 1985
    Assignee: Torii & Co., Ltd.
    Inventors: Setsuro Fujii, Toshiyuki Okutome, Toyoo Nakayama, Takashi Yaegashi, Masateru Kurumi