Abstract: A compound represented by the general formula (I) shown below ##STR1## or a pharmaceutically acceptable salt thereof can be used as the active ingredient in a pharmaceutical preparation. The pharmaceutical preparation is desirable for its anti-ulcer activity, for therapeutic use against tumors sustained by gastrin and other bioactive polypeptides correlated therewith, for therapeutic use in treating disorders of the gastrointestinal tract, for the treatment of pathological conditions of the central nervous system linked to imbalances in the neural physiological levels of gastrin or other bioactive polypeptides correlated therewith, for use in the treatment and prevention of pathological eye conditions caused by surgical treatment of cataracts or chronic ocular inflammation, and for the prevention of diseases of other sensory organs.
Type:
Grant
Filed:
December 29, 1997
Date of Patent:
July 13, 1999
Assignee:
Rotta Research Laboratorium S.p.A.
Inventors:
Francesco Makovec, Walter Peris, Lucio C. Rovati, Luigi A. Rovati
Abstract: The dihalopropene compounds of the general formula ?I! have excellent insecticidal/acaricidal activity, so that they are satisfactorily effective for the control of noxious insects, mites and ticks.
Abstract: The present invention relates to novel substituted N-methyl-N-(4-(4-(1H-benzimidazol-2-yl-amino)piperidin-1-yl)-2-(aryl)butyl )benzamide derivatives of the formula: ##STR1## stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonists. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.
Type:
Grant
Filed:
January 6, 1997
Date of Patent:
July 13, 1999
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
George Daniel Maynard, John Michael Kane, Braulio Santiago, Elizabeth Mary Kudlacz, Larry Don Bratton, Christopher Robin Dalton
Abstract: The present invention is directed to aminoquinolines of Formula I: ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.
Abstract: The invention relates to compound of general formula (I): ##STR1## wherein: Z represents O or CH.sub.2n is from 0 to 4R, X and Y are as defined in the description, andA represents ##STR2## wherein R.sup.1, R.sup.2, R.sup.6, R.sup.7 and T' are as defined in the description,and medicinal products containing the same are useful in treating or in preventing melatoninergic disorders.
Type:
Grant
Filed:
April 24, 1998
Date of Patent:
July 6, 1999
Assignee:
Adir et Compagnie
Inventors:
Gerald Guillaumet, Isabelle Charton, Ahmed Mamai, Pierre Renard, Bruno Pfeiffer, Philippe Delagrange, Beatrice Guardiola
Abstract: The present invention is concerned with a novel process for the manufacture of quinargine ##STR1## (N-(2-quinolylcarbonyl)-asparagine) based on the reaction of the succinimide ester ##STR2## with asparagine or asparagine salts in an aqueous reaction medium at a neutral pH value.
Abstract: A halogenated compound (I) containing one or more >C.dbd.O, olefinic and/or aromatic >C.dbd.C< groups is hydrogenated for producing a halogenated compound (II) having no or a decreased level of >C.dbd.O, olefinic and/or aromatic >C.dbd.C< groups. In the hydrogenation process a liquid feed stream comprising one or more of these compounds (I) is contacted with a hydrogen-rich gaseous stream and a liquid recycle stream comprising one or more of these compounds (II) in the presence of a catalyst.
Abstract: Novel process for the preparation of quinolone carboxylic acid derivatives of general formula I, and intermediates thereof as illustrated in Scheme 1 wherein the key intermediate is a compound of formula IX.
Type:
Grant
Filed:
March 11, 1998
Date of Patent:
June 22, 1999
Assignee:
Apotex, Inc.
Inventors:
Ian Egle, Regis C.S.H. Leung-Toung, Bo Lei, Tim Fat Tam, Tao Xin, Khashayar Karimian
Abstract: A method form forming a dielectric film on a substrate includes the steps of placing the substrate in a process chamber wherein said substrate is isolated from an external environment, depositing the dielectric film on the substrate in the process chamber, and annealing the dielectric film in said process chamber. In particular, the dielectric film can be formed from Ta.sub.2 O.sub.5. Systems for forming the dielectric film are also disclosed.
Type:
Grant
Filed:
September 12, 1996
Date of Patent:
June 8, 1999
Assignee:
Samsung Electronics Co., Ltd.
Inventors:
Young-wook Park, Moon-yong Lee, Kyung-hun Kim, In-sung Park
Abstract: This invention encompasses compounds of formula (I), and pharmaceutically acceptable non-toxic salts thereof wherein X and Y are the same or different and represent oxygen or H.sub.2 with the proviso that not both X and Y are H.sub.2 ; W represents phenyl, thienyl, or pyridyl, each of which may be unsubstituted or mono or disubstituted with organic or inorganic substituents; and R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are variables representing organic and inorganic substituents. These compounds are highly selective agonists, antagonists or inverse agonists for GABAs brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.
Abstract: The present invention relates particularly to novel preorganized hexadentate ligands that are suitable for completing with a radionuclide, and are useful as general imaging agents for diagnostic purposes.
Type:
Grant
Filed:
December 14, 1990
Date of Patent:
June 1, 1999
Assignee:
Mallinckrodt Inc.
Inventors:
Raghavan Rajagopalan, William L. Neumann, Dennis L. Nosco
Abstract: Compounds having anti-inflammatory and anti-oxidant activity are disclosed. The compounds are useful in preventing and treating inflammatory disorders through several mechanisms. Methods of treatment employing these properties of the compounds and corresponding pharmaceutical compositions are disclosed.
Type:
Grant
Filed:
February 13, 1998
Date of Patent:
June 1, 1999
Assignee:
Alcon Laboratories, Inc.
Inventors:
Mark Hellberg, Pete Delgado, Jon C. Nixon
Abstract: A process for the preparation of optically pure (-)-1,2,3,4-tetrahydroquinoline-3-carboxylic acid by reaction of L-phenylalanine with formaldehyde in aqueous solution or paraformaldehyde in the presence of hydroiodic acid is described.
Abstract: The present invention relates to novel quinoline derivatives of the formula ##STR1## which inhibit exogenously or endogenously stimulated gastric acid secretion and thus can be used in the prevention and treatment of gastrointestinal inflammatory diseases.
Abstract: Compounds of formula (I), wherein R.sub.1 is (a), (b), (c) or (d); n is 0, 1 or 2; A, B, C and D are each independently nitrogen or carbon; R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each independently hydrogen, C.sub.1 to C.sub.6 alkyl, aryl, C.sub.1 to C.sub.3 alkyl-aryl, halogen (e.g. fluorine, chlorine, bromine or iodine), cyano, nitro, --(CH.sub.2).sub.m NR.sub.14 R.sub.15, --(CH.sub.2).sub.m OR.sub.9, --SR.sub.9, --SO.sub.2 NR.sub.14 R.sub.15, --(CH.sub.2).sub.m NR.sub.14 SO.sub.2 R.sub.15 --(CH.sub.2).sub.m NR.sub.14 CO.sub.2 R.sub.9, --(CH.sub.2).sub.m NR.sub.14 COR.sub.9, --(CH.sub.2).sub.m NR.sub.14 CONHR.sub.9, --CONR.sub.14 R.sub.15, or --CO.sub.2 R.sub.9 ; R.sub.2 and R.sub.3, R.sub.3 and R.sub.4, or R.sub.4 and R.sub.
Abstract: The subject invention provides for novel synergistic compositions useful for inactivating viruses or inducing apoptosis in tumor cells and for treating cancer or retroviral infections. Generally, the compositions comprise one or a plurality of ligands that oxidatively attack a zinc finger of pADPRT in combination with one or a plurality of agents selected from the group consisting of: agents that decrease cellular levels of glutathione and ligands that non-covalently bind to the nicotinamide site of pADPRT but do not effect zinc ejection from a zinc finger of pADPRT.
Type:
Grant
Filed:
January 13, 1995
Date of Patent:
March 2, 1999
Assignee:
Octamer, Inc.
Inventors:
Ernest Kun, Jerome Mendeleyev, Eva Kirsten
Abstract: Cyclic amides are inhibitors of tumor necrosis factor and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is 3-phenyl-3-(1-oxoisoindolin-2-yl)propionamide.
Abstract: The present invention is directed to a new 5HT.sub.2 antagonist, (+)-.alpha.-(2,3-dimethoxyphenyl)-1-?2-(4-fluorophenyl)ethyl!-4-piperidine methanol, and its use in the treatment of a number of disease states.
Type:
Grant
Filed:
October 2, 1997
Date of Patent:
February 23, 1999
Assignee:
Merrell Pharmaceutical, Inc.
Inventors:
Albert A. Carr, John M. Kane, David A. Hay, Christopher J. Schmidt
Abstract: The present invention is concerned with novel benzoate derivatives having the formula ##STR1## the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 is halo or C.sub.1-6 alkylsulfonylamino; either R.sup.2 is hydrogen and R.sup.3 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl; or R.sup.2 and R.sup.3 taken together form a bivalent radical of formula --CH.dbd.CH-- (a), --(CH.sub.2).sub.2 -- (b), or --(CH.sub.2).sub.3 -- (c); in the bivalent radicals of formula (a), (b) or (c) one or two hydrogen atoms may be replaced by C.sub.1-6 alkyl; Alk is C.sub.1-6 alkanediyl; R.sup.4 is hydrogen or C.sub.1-6 alkyloxy; R.sup.5, R.sup.6 and R.sup.7 each independently are hydrogen, halo, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy; or R.sup.5 and R.sup.6 taken together may also form a bivalent radical of formula: --NR.sup.8 C(O)NR.sup.9 --, --NH--C(NHR.sup.10).dbd.N--, --O--(CH.sub.2).sub.m --O--; R.sup.8 and R.sup.
Type:
Grant
Filed:
March 24, 1997
Date of Patent:
February 16, 1999
Assignee:
Janssen Pharmaceutica, N.V.
Inventors:
Marie-Louise Hendrickx, Kurt Godfried Cornelius Emile Van Daele, Peter Jules Victor Van Daele, Glenn Kurt Ludo Van Daele, Jean-Paul Rene Marie Andre Bosmans, Marc Gustaaf Celine Verdonck
Abstract: A process for preparing an N-oxide of pyridine or a halopyridine, said process comprising reacting a reaction mixture of said pyridine, or said halopyridine, and hydrogen peroxide in a reaction conducted at an elevated temperature in the presence of a catalytically effective amount of a heterogeneous catalyst, said heterogeneous catalyst being insoluble in said reactants, to form said 2-halopyridine-N-oxide or pyridine-N-oxide.