Plural Ring Chalcogens In The Hetero Ring Patents (Class 514/360)
-
Patent number: 6288092Abstract: (4-oxy-3-(aryl)phenyl)pyridine compounds, in free or acid addition salt form, are useful as pharmaceuticals for treatment and prophylaxis of inflammation, particularly inflammatory or obstructive diseases of the airways, e.g. for asthma therapy. Preferred compounds are novel biphenyl pyridines, biphenyl benzamides and biphenyl phenylcarboxy compounds. The compounds are selective inhibitors of PDE 4 isoenzyme activity and also act to down regulate or inhibit TNF-&agr; release.Type: GrantFiled: September 6, 2000Date of Patent: September 11, 2001Assignee: Novartis AGInventor: Paul W. Manley
-
Patent number: 6225330Abstract: This invention is directed to tricyclic compounds which are selective antagonists for NPY (Y5) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.Type: GrantFiled: June 30, 1999Date of Patent: May 1, 2001Assignees: Synaptic Pharmaceutical Corporation, Novartis AGInventors: Mohammad R. Marzabadi, Wai C. Wong, Walter Schilling, Stewart A. Noble
-
Patent number: 6207690Abstract: The present invention is directed toward the use of the drug Troglitazone and related thiazolidinedione compounds in the treatment of the climacteric and cancer. This use is based on the novel discovery that Troglitazone inhibits steroidogenesis in granulosa cell cultures. This activity is believed to result from the ability of thiazolidinedione derivatives to act as a ligand for the orphan steroid receptor peroxisome proliferator-activated receptor gamma (PPAR&ggr;). Troglitazone and related compounds can therefore be used to prevent excessive uterine bleeding during. Further, enhanced translocation of this orphan nuclear receptor into the nucleus of cells will block transcription in rapidly proliferating cancer cells that express PPAR&ggr;, resulting in loss of cell viability.Type: GrantFiled: September 3, 1999Date of Patent: March 27, 2001Assignee: Board of Regents, The University Texas SystemInventors: Randall J. Urban, Allan Green
-
Patent number: 6199607Abstract: A dry powder composition comprising formoterol and a carrier substance, both of which are in finely divided form, wherein the formulation has a poured bulk density of from 0.28 to 0.38 g/ml is useful in the treatment of respiratory disorders.Type: GrantFiled: September 22, 1999Date of Patent: March 13, 2001Assignee: Astra AktiebolagInventor: Jan Trofast
-
Patent number: 6200997Abstract: The present invention relates to heterocyclyl-substituted phenyl compounds of the formula I, where the substituents have the following meanings: Y is halogen, C1-C4-alkyl, C1-C4-haloalkyl or C1-C4-alkoxy; n is 0, 1 or 2, where the radicals Y may be different if n=2; E is a group A or B, where # denotes the bond to the phenyl ring, and G R&agr;, R&bgr;, Y, n, T and Z are each as defined in the description.Type: GrantFiled: January 25, 1999Date of Patent: March 13, 2001Assignee: BASF AktiengesellschaftInventors: Andreas Gypser, Hubert Sauter, Herbert Bayer, Markus Gewehr, Wassilios Grammenos, Thomas Grote, Roland Götz, Bernd Müller, Arne Ptock, Franz Röhl, Volker Harries, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
-
Patent number: 6197799Abstract: The invention relates to novel dithiazole dioxides, to processes for their preparation and to their use in crop protection and in the protection of materials.Type: GrantFiled: June 2, 1998Date of Patent: March 6, 2001Assignee: Bayer AktiengesellschaftInventors: Hermann Uhr, Klaus Stenzel, Martin Kugler, Heinrich Schrage
-
Patent number: 6191159Abstract: The present application describes disubstituted pyrazolines and triazolines of formulae I and II: or pharmaceutically acceptable salt forms thereof, wherein one of M1 and M2 maybe N and D may be a variety of N-containing groups, which are useful as inhibitors of factor Xa.Type: GrantFiled: March 26, 1999Date of Patent: February 20, 2001Assignee: Dupont Pharmaceuticals CompanyInventor: Donald J. P. Pinto
-
Patent number: 6136829Abstract: 1,3-diazolino and 1,3-diazolidino heterocycle derivatives useful as nitric oxide synthase inhibitors.Type: GrantFiled: July 19, 1999Date of Patent: October 24, 2000Assignee: G.D. Searle & Co.Inventors: Donald W. Hansen, Jr., Ariia A. Bergmanis, Timothy J. Hagen, E. Ann Hallinan, Steven W. Kramer, Suzanne Metz, Karen B. Peterson, Barnett S. Pitzele, Foe S. Tjoeng, Mihaly V. Toth, Mahima Trivedi, R. Keith Webber, Sofya Tsymbalov, Rolando E. Gapud
-
Patent number: 6129782Abstract: The invention provides a means of inhibiting bacterial growth particularly on a coated substrate. It comprises a method of forming a substantially dry powder coating containing a biocide, applying the powder coating composition to form a coating on the substrate, the biocide being capable of retaining effective biocidal activity in the coating.Type: GrantFiled: October 4, 1999Date of Patent: October 10, 2000Inventors: Harold Brodie, Rainer Clover
-
Patent number: 6124328Abstract: The present invention relates to methods and pharmaceutical compositions for stimulating the growth of neutering in nerve cells. The compositions comprise a neurotrophic amount of a compound which binds to the FK-506 binding protein (FKBP) and a neurotrophic factor, such as nerve growth factor NGF. The methods comprise treating nerve cells with the above-described compositions or compositions comprising the FKBP binding compound without a neurotrophic factor. The methods of this invention can be used to promote repair of neuronal damage caused by disease or physical trauma.Type: GrantFiled: February 28, 1997Date of Patent: September 26, 2000Assignee: Vertex Pharmaceuticals IncorporatedInventor: David M. Armistead
-
Patent number: 6013663Abstract: A compound of formula (I): ##STR1## wherein one of m and n represents 0, and the other represents 0, 1 or 2; k represents 0 or 1 to 12; R.sup.1 is hydrogen, an aryl, a heterocyclic, an alkyl, a hydroxy or --OR.sup.7, wherein R.sup.7 is an alkyl, an alkenyl or an aralkyl; A is --CON(R.sup.2)SO.sub.2--, wherein R.sup.2 is hydrogen, an alkyl or an aralkyl; B is a single bond; and pharmaceutically acceptable salts thereof. The compounds have the ability to enhance the activity of glutathione reductase and can therefore be used for the treatment and prevention of a variety of diseases including cataracts.Type: GrantFiled: March 31, 1998Date of Patent: January 11, 2000Assignee: Sankyo Company, LimitedInventors: Takashi Fujita, Tomihisa Yokoyama
-
Patent number: 5983956Abstract: A dry powder composition comprising formoterol and a carrier substance, both of which are in finely divided form, wherein the formulation has a poured bulk density of from 0.28 to 0.38 g/ml is useful in the treatment of respiratory disorders.Type: GrantFiled: January 9, 1998Date of Patent: November 16, 1999Assignee: Astra AktiebolagInventor: Jan Trofast
-
Patent number: 5980620Abstract: The invention provides a means of inhibiting bacterial growth particularly on a coated substrate. It comprises a method of forming a substantially dry powder coating containing a biocide, applying the powder coating composition to form a coating on the substrate, the biocide being capable of retaining effective biocidal activity in the coating.Type: GrantFiled: November 30, 1998Date of Patent: November 9, 1999Inventors: Harold Brodie, Rainer Clover
-
Patent number: 5981556Abstract: 1,3-diazolino and 1,3-diazolidino heterocycle derivatives useful as nitric oxide synthase inhibitors.Type: GrantFiled: July 22, 1997Date of Patent: November 9, 1999Assignee: G.D. Searle & Co.Inventors: Donald W. Hansen, Jr., Arija A. Bergmanis, Timothy J. Hagen, E. Ann Hallinan, Steven W. Kramer, Suzanne Metz, Karen B. Peterson, Barnett S. Pitzele, Foe S. Tjoeng, Mihaly V. Toth, Mahima Trivedi, R. Keith Webber, Sofya Tsymbalov, Rolando E. Gapud
-
Use of thiazolidinedione derivatives in the treatment of anovulation, hyperandrogenism and hirsutism
Patent number: 5972944Abstract: The present invention provides methods of using thiazolidinone derivatives to treat anovulation, hyperandrogenism and hirsutism.Type: GrantFiled: July 29, 1998Date of Patent: October 26, 1999Assignee: Warner-Lambert CompanyInventors: Tammy Antonucci, Dean Lockwood, Rebecca Norris -
1,2,4-oxa diazolino and 1,24-oxa diazolidion heterocycles as useful nitric oxide synthase inhibitors
Patent number: 5958958Abstract: 1,2,4-oxa-diazolino and 1,2,4-oxa-diazolidino heterocycle derivatives useful as nitric oxide synthase inhibitors.Type: GrantFiled: January 14, 1999Date of Patent: September 28, 1999Assignee: G.D. Searle & Co.Inventors: Donald W. Hansen, Jr., Arija A. Bergmanis, Timothy J. Hagen, E. Ann Hallinan, Steven W. Kramer, Suzanne Metz, Karen B. Peterson, Barnett S. Pitzele, Foe S. Tjoeng, Mihaly V. Toth, Mahima Trivedi, R. Keith Webber, Sofya Tsymbalov, Rolando E. Gapud -
Patent number: 5955451Abstract: Disclosed are compositions comprising non-steroid anti-inflammatory drugs (NSAID'S) complexed with zwitterionic, neutral phospholipids, or both, having reduced gastrointestinal irritating effects and enhanced antipyretic, analgesic, and antiinflammatory activity. Also disclosed are improved methods of using the complexes for treating fever, inflammation, and preventing platelet aggregation. In some embodiments, the anti-pyretic activity of sub-therapeutically used amounts of NSAID's are enhanced to elicit anti-pyretic activity in vivo when associated (noncovalently) with zwitterionic phospholipids, such as dipalmitoyl phosphatidyl choline. Methods and compositions useful for enhancing the therapeutic activity of non-steroidal anti-inflammatory agents in the presence of anti-secretory agents are also discussed.Type: GrantFiled: September 24, 1996Date of Patent: September 21, 1999Assignee: The University of Texas System Board of RegentsInventors: Lenard Lichtenberger, Bruce D Butler
-
Patent number: 5948800Abstract: The present invention is directed to a drug for preventing or remedying Alzheimer's disease. The drug contains as the active ingredient 2-phenyl-1,2-benzisoselenazol-3(2H)-one (referred as compound (A)), whose effect is based on the action of reducing neuron toxicity induced by .beta.-amyloid protein.Type: GrantFiled: August 4, 1997Date of Patent: September 7, 1999Assignee: A. Nattermann & Cie. GmbHInventors: Ikuro Maruyama, Kazuhiro Abeyama, Hiroyuki Masayasu
-
Patent number: 5938825Abstract: This invention is directed to stabilized antimicrobial compositions which have been stabilized using mixture of at least one halopropynyl compound, and particularly a halopropynyl carbamate fungicide such as IPBC and an effective UV absorber.Type: GrantFiled: May 21, 1998Date of Patent: August 17, 1999Assignee: Troy Technology Corporation Inc.Inventors: Kamlesh D. Gaglani, Meihua Yang
-
Patent number: 5925367Abstract: A composition for controlling harmful insects and representatives of the order Acarina, containing as biologically active components a) a substance that modifies the behavior of the pests and b) at least one pesticidally active compound, wherein the biologically active components are contained in a flowable or viscous non-hardening matrix that is resistant to water and weather, is protected against light and is suitable for distribution in the form of droplets or droplet-like units or spots that adhere to a substrate, by means of which matrix the behavior-modifying substance is protected against UV radiation and from which it is slowly released in a biologically effective amount over a prolonged period, and wherein the pesticidally active compound can be taken up in a pesticidally effective amount from the surface of the droplets or droplet-like units or spots by the pests to be controlled; as well as a method of controlling the said pests, especially plant-destructive insects.Type: GrantFiled: January 19, 1995Date of Patent: July 20, 1999Assignee: Ciba-Geigy CorporationInventors: Max Angst, Fran.cedilla.ois Gugumus, Gunther Rist, Manfred Vogt, Jean Rody
-
Patent number: 5885984Abstract: Aminocyclohexylester compounds, including thioesters, are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the blockade of ion channels and the treatment of arrhythmias.Type: GrantFiled: February 27, 1997Date of Patent: March 23, 1999Assignee: University of British ColumbiaInventors: Bernard A. MacLeod, Michael J. A. Walker, Richard A. Wall
-
Patent number: 5846993Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.Type: GrantFiled: June 7, 1995Date of Patent: December 8, 1998Assignee: Agouron Pharmaceuticals, Inc.Inventors: Bruce A. Dressman, James E. Fritz, Stephen W. Kaldor, Vincent J. Kalish, Siegfried Heinz Reich, John H. Tatlock, Michael J. Rodriguez
-
Patent number: 5824677Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocyle. R.sub.3 may be either hydrogen or C.sub.13. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.Type: GrantFiled: June 7, 1995Date of Patent: October 20, 1998Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
-
Patent number: 5817677Abstract: 5-Membered heterocyclic compounds, of which the following compounds are exemplary:(a) 4-??trans-4-(2-carboxyethyl)cyclohexyl!aminocarbonyl!-1-(4-piperidyl)imida zole,(b) 5-??trans-4-(2-carboxyethyl)cyclohexyl!aminocarbonyl!-4-methyl-2-(4-piperi dyl)-1,3-thiazole,(c) 5-??4-(carboxymethoxy)phenyl!aminocarbonyl!-4-methyl-2-(4-piperidyl)-1,3-t hiazole,(d) 5-??trans-4-(2-carboxyethyl)cyclohexyl!aminocarbonyl!-2-(4-piperidyl)-1,3, 4-thiadiazole,(e) 5-??4-(carboxymethoxy)phenyl!aminocarbonyl!-2-(4-piperidyl)-1,3,4-thiadiaz ole,(f) 5-??trans-4-(carboxymethoxy)cyclohexyl!aminocarbonyl!-2-(4-piperidyl)-1,3- thiazole,(g) 5-??4-(carboxymethoxy)phenyl!aminocarbonyl!-2-(4-piperidyl)-1,3-thiazole,(h) 5-??trans-4-(2-carboxyethyl)cyclohexyl!aminocarbonyl!-2-(4-piperidyl)-1,3- thiazole, and(i) 4-??trans-4-carboxycyclohexyl!aminocarbonyl!-1-?2-(4-piperidyl)ethyl!imida zole.Type: GrantFiled: October 18, 1996Date of Patent: October 6, 1998Assignee: Dr. Karl Thomae GmbHInventors: Gunter Linz, Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Brian Guth, Johannes Weisenberger
-
Patent number: 5814647Abstract: The present invention is directed toward the use of the drug Troglitazone and related thiazolidinedione compounds in the treatment of the climacteric and cancer. This use is based on the novel discovery that Troglitazone inhibits steroidogenesis in granulosa cell cultures. This activity is believed to result from the ability of thiazolidinedione derivatives to act as a ligand for the orphan steroid receptor peroxisome proliferator-activated receptor gamma (PPAR.gamma.). Troglitazone and related compounds can therefore be used to prevent excessive uterine bleeding during. Further, enhanced translocation of this orphan nuclear receptor into the nucleus of cells will block transcription in rapidly proliferating cancer cells that express PPAR.gamma., resulting in loss of cell viability.Type: GrantFiled: March 4, 1997Date of Patent: September 29, 1998Assignee: Board of Regents, The University of Texas SystemInventors: Randall J. Urban, Allan Green
-
Patent number: 5780497Abstract: The present invention relates to new 2-Phenyl-1-?4-(amino-1-yl-alk-1-ynyl)benzyl!-1H-indol-5-ol compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structure below.Type: GrantFiled: April 14, 1997Date of Patent: July 14, 1998Assignee: American Home Products CorporationInventors: Chris P. Miller, Michael D. Collini, Bach D. Tran
-
Patent number: 5767137Abstract: A description is given of novel and know 1,3,2-benzodithiazole 1-oxides of the formula (I) ##STR1## and of their preparation and use for protecting industrial materials against infestation by microorganisms.Type: GrantFiled: August 1, 1996Date of Patent: June 16, 1998Assignee: Bayer AktiengesellschaftInventors: Hermann Uhr, Franz Kunisch, Peter Wachtler, Martin Kugler, Joachim Mittendorf
-
Patent number: 5731002Abstract: A stable, oral pharmaceutical composition comprising a proton pump inhibitor and a gelling agent designed for the treatment of gastric acid related diseases in animals, the process for preparation of the composition and the use thereof.Type: GrantFiled: April 29, 1994Date of Patent: March 24, 1998Assignee: Astra AktiebolagInventors: Stig-Goran Arthur Olovson, .ANG.ke Gunnar Pilbrant
-
Patent number: 5728719Abstract: The present invention is a method for controlling ectoparasites. More particularly, the invention relates to a method of treatment in which the warm blooded animal is dosed with an ovicidally effective amount of a heterocyclic nitrogen compound selected from the group represented by the formula: ##STR1## wherein R.sub.1, is either one of the following groups: ##STR2## in which R.sub.7, R.sub.8, R.sub.9, R.sub.10, R.sub.11, R.sub.12, R.sub.13, R.sub.14, R.sub.15, R.sub.16, and R.sub.17 are, the same or different, each a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkoxy group, a C.sub.1 -C.sub.4 alkylthio group, a trifluoro methyl group or a vitro group, R.sub.18, R.sub.19, R.sub.20 and R.sub.21 are, the same or different, each a hydrogen atom or a methyl group, k is an integer of 0 to 1 and 1 is an integer of 0 to 3; R.sub.2 and R.sub.3 are, the same or different, each a hydrogen atom, a halogen atom or a methyl group; R.sub.4 is a halogen atom or a methyl group; R.sub.5 and R.sub.Type: GrantFiled: March 14, 1995Date of Patent: March 17, 1998Assignee: Virbac, Inc.Inventor: Thomas A. Miller
-
Patent number: 5719170Abstract: Cyclohexanol esters of the formula I ##STR1## are described in which the radicals have the given meaning. The compounds are pharmacologically active and may therefore be used as pharmaceuticals, in particular for treating diabetes and other diseases which are characterized by an elevated secretion of glucose from the liver or by an elevated activity of the glucose-6-phosphatase system.Type: GrantFiled: December 11, 1996Date of Patent: February 17, 1998Assignee: Hoechst AktiengesellschaftInventors: Horst Hemmerle, Gerrit Schubert, Peter Below, Andreas Herling, Hans-Jorg Burger
-
Patent number: 5688744Abstract: A method of inhibiting the growth of bacteria and algae in industrial loci using a compound of formula I or II: ##STR1## is disclosed. Antimicrobial compounds useful in inhibiting the growth of bacteria and algae in industrial loci and compositions containing the antimicrobial compounds are also disclosed.Type: GrantFiled: October 11, 1996Date of Patent: November 18, 1997Assignee: Rohm and Haas CompanyInventors: Rhoda Weber Joseph, Diane Lynn Antes, Peter Osei-Gyimah
-
Patent number: 5670529Abstract: Compositions comprising optionally substituted 3-isothiazolone derivative compounds, a metal nitrate, cupric (Cu.sup.2+) ion in ppm amounts in the form of an inorganic copper salt and water are described for preventing the formation of unsightly precipitations in these compositions during storage.Type: GrantFiled: June 5, 1996Date of Patent: September 23, 1997Assignee: Rohm and Haas CompanyInventor: Philippa Clarke
-
Patent number: 5641796Abstract: Antihyperglycemic compounds selected from the group consisting of C-substituted pentacycloazoles and N-alkyl-substituted pentacycloazoles.Type: GrantFiled: November 1, 1994Date of Patent: June 24, 1997Assignee: Eli Lilly and CompanyInventors: Samuel J. Dominianni, Lora L. Fitch, Klaus K. Schmiegel
-
Patent number: 5641783Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocycle. R.sub.3 may be either hydrogen or C.sub.1-3. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.Type: GrantFiled: September 8, 1994Date of Patent: June 24, 1997Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
-
Patent number: 5602133Abstract: Novel methods of using thiazolidinone derivatives and related antihyperglycemic agents to treat populations at risk for developing noninsulin-dependent diabetes mellitus (NIDDM) and complications arising therefrom are disclosed. In one embodiment, the compounds of the invention are used to treat polycystic ovary syndrome in order to prevent or delay the onset of noninsulin-dependent diabetes mellitus. In another embodiment, the compounds of the invention are used to treat gestational diabetes in order to prevent or delay the onset of noninsulin-dependent diabetes mellitus.Type: GrantFiled: June 6, 1995Date of Patent: February 11, 1997Assignee: Warner-Lambert CompanyInventors: Tammy Antonucci, Dean Lockwood, Rebecca Norris
-
Patent number: 5580896Abstract: This invention relates to the treatment of pain and inhibiting the growth of colorectal cancer with dipeptoids of .alpha.-substituted Trp-Phe derivatives.Type: GrantFiled: May 22, 1995Date of Patent: December 3, 1996Assignee: Warner-Lambert CompanyInventors: David C. Horwell, Martyn C. Pritchard, Edward Roberts, Reginald S. Richardson, Julian Aranda
-
Patent number: 5565455Abstract: A method for relief or prevention of a withdrawal syndrome resulting from addiction to a drug or substance of abuse and/or for the suppression of dependence on drugs or substances of abuse which comprises administering to a patient in need thereof an effective amount of a bisphenylalkylpiperazinde derivative, wherein said withdrawal syndrome comprises at least one of the symptoms selected from the group consisting of sleep disturbance, mood disturbance, and craving for the drug or substance of abuse.Type: GrantFiled: November 30, 1994Date of Patent: October 15, 1996Assignee: Pharmacia ABInventors: Anders Bjork, Gunnar Andersson
-
Patent number: 5554633Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q is optionally substituted phenyl or benzhydryl; X and Y are each H or together form a group=O; Z is O, S or NR.sup.9, where R.sup.9 is H or C.sub.1-6 alkyl; R.sup.1 represents H or C.sub.1-6 alkyl; R.sup.2 represents C.sub.1-6 alkyl substituted by CONR.sup.7 (CH.sub.2).sub.p R.sup.8 (where R.sup.7 is H or C.sub.1-6 alkyl, R.sup.8 is optionally substituted heteroaryl and p is 0, 1, 2, 3, 4, 5 or 6); R.sup.3 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkynyl; R.sup.4 represents H, C.sub.1-6 alkyl or optionally substitute phenyl; R.sup.5 represents optionally substituted phenyl; R.sup.6 is H or C.sub.1-6 alkyl; and q is 0, 1, 2 or 3; are tachykinin antagonists useful in therapy.Type: GrantFiled: January 27, 1995Date of Patent: September 10, 1996Assignee: Merck, Sharp & Dohme, Ltd.Inventor: Martin R. Teall
-
Patent number: 5543433Abstract: Compounds of the formula I ##STR1## where X is hydrogen, halogen, alkyl, alkoxy, trifluoromethyl, cyano or nitro,Y is an amino, methylamino or dimethylamino group,Z is a group CHCH.sub.3, CHOCH.sub.3 or NOCH.sub.3,R is hydrogen or alkyl,A is hydrogen, alkyl, haloalkyl or cycloalkyl,B is unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl or the group ##STR2## where W is hydrogen, alkyl, alkoxy, alkylthio, alkylamino or dialkylamino, unsubstituted or substituted aryl or heteroaryl, unsubstituted or substituted aryloxy, arylthio, arylamino or aryl-N-(C.sub.1 -C.sub.6 -alkyl)amino, heteroaryloxy, heteroarylthio, heteroarylamino or heteroaryl-N-(alkyl)amino orA and B, together with the C atom whose substituents they are, are an isocyclic or heterocyclic ring which can also be quinonoid,and fungicides containing these compounds.Type: GrantFiled: June 3, 1994Date of Patent: August 6, 1996Assignee: BASF AktiengesellschaftInventors: Reinhard Doetzer, Hubert Sauter, Herbert Bayer, Franz Roehl, Gisela Lorenz, Eberhard Ammermann, Horst Wingert
-
Patent number: 5504095Abstract: Aminobenzosultam derivatives, which are inhibitors of lipoxygenase, having the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein Ar is cycloalkyl having five to seven carbon atoms, tetrahydropyranyl, pyridyl, oxazolyl, phenyl or substituted phenyl wherein said substituent is methyl, methoxy, fluoro, chloro or trifluoromethyl; n is an integer of 1 to 3; X is hydrogen, methyl, methoxy, fluoro, chloro or trifluoromethyl; Z is --NH--, --O--, or --CH.sub.2 --; and R.sup.1 is hydrogen or alkyl having one to three carbon atoms.Type: GrantFiled: December 20, 1994Date of Patent: April 2, 1996Assignee: Pfizer Inc.Inventors: Masami Nakane, Kunio Satake, Kazuo Ando, Hiroaki Wakabayashi
-
Patent number: 5502066Abstract: The invention relates to the use of 1,2,4-dithiazolium salts, some of which are known, of the general formula (I) ##STR1## in which the substituents have the meaning given in the description, to a process for their preparation and to their use as chemotherapeutics, in particular as TNF inhibitors.Type: GrantFiled: June 10, 1994Date of Patent: March 26, 1996Assignee: Bayer AktiengesellschaftInventors: Ulrich Heinemann, Ralf Tiemann, Klaus Stu/ nkel
-
Patent number: 5498610Abstract: The present invention is directed to a method of blocking N-methyl-D-aspartic (NMDA) acid receptor sites in a mammal in need thereof with an effective NMDA blocking (neuroprotective and antiischemic) amount of 5-(1-hydroxy-2-piperidino)-propyl-2(1H,3H)-indolone analogs and the pharmaceutically acceptable salts thereof; methods of using these compounds in the treatment of stroke, head trauma, spinal cord trauma, traumatic brain injury, multiinfarct dementia, CNS degenerative diseases such as Alzheimer's disease, senile dementia of the Alzheimer's type, Huntington's disease, Parkinson's disease, epilepsy, amyotrophic lateral sclerosis, pain, AIDS dementia, psychotic conditions, drug addictions, migraine, hypoglycemia, anxiolytic conditions, urinary incontinence and an ischemic event arising from CNS surgery, open heart surgery or any procedure during which the function of the cardiovascular system is compromised.Type: GrantFiled: February 1, 1994Date of Patent: March 12, 1996Assignee: Pfizer Inc.Inventor: Bertrand L. Chenard
-
Patent number: 5482962Abstract: This invention relates to N,N'-disubstituted-N,N'-diacylhydrazines which are useful as insecticides, compositions containing those compounds and methods of their use. This invention also relates to the production of intermediates useful in the production of such compounds.The compounds of this invention may be represented by the formula ##STR1## wherein R.sup.1 is cyano or H,R.sup.2 is branched alkyl,B is aryl or substituted aryl,R.sup.a is H or a variety of substituents, andZ forms a fused 5-member heterocyclic ring.Type: GrantFiled: July 22, 1994Date of Patent: January 9, 1996Assignee: Rohm and Haas CompanyInventor: Robert E. Hormann
-
Patent number: 5478852Abstract: Novel methods of using thiazolidinone derivatives and related antihyperglycemic agents to treat populations experiencing impaired glucose intolerance in order to prevent or delay the onset of noninsulin-dependent diabetes mellitus (NIDDM) and complications arising therefrom are disclosed.Type: GrantFiled: August 23, 1994Date of Patent: December 26, 1995Assignee: Sankyo Company, LimitedInventors: Jerrold Olefsky, Tammy Antonucci, Dean Lockwood, Rebecca Norris
-
Patent number: 5457109Abstract: Novel methods of using thiazolidinone derivatives and related antihyperglycemic agents to treat populations at risk for developing noninsulin-dependent diabetes mellitus (NIDDM) and complications arising therefrom are disclosed. In one embodiment, the compounds of the invention are used to treat polycystic ovary syndrome in order to prevent or delay the onset of noninsulin-dependent diabetes mellitus. In another embodiment, the compounds of the invention are used to treat gestational diabetes in order to prevent or delay the onset of noninsulin-dependent diabetes mellitus.Type: GrantFiled: August 23, 1994Date of Patent: October 10, 1995Assignee: Warner-Lambert CompanyInventors: Tammy Antonucci, Dean Lockwood, Rebecca Norris
-
Patent number: 5432175Abstract: Pyridine and pyridine N-oxide derivatives of diaryl methyl piperidines or piperazines and pharmaceutically acceptable salts thereof are disclosed, which possess anti-allergic and anti-inflammatory activity. Pharmaceutical compositions containing and methods of using the compounds are also described.Type: GrantFiled: April 1, 1993Date of Patent: July 11, 1995Assignee: Schering CorporationInventors: John J. Piwinski, Jesse Wong, Michael J. Green, Vera Seidl, Richard Friary
-
Patent number: 5393775Abstract: A compound selected from those of formula (I): ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9 and n are as defined in the description, its optical isomers, and its addition salts thereof with a pharmaceutically-acceptable acid or base,and medicinal product containing the same for treating a mammal afflicted with a disorder connected with peroxydation processes and biosynthesis of eicosanoids.Type: GrantFiled: September 7, 1993Date of Patent: February 28, 1995Assignee: Adir et CompagnieInventors: Guillaume Le Baut, Jean-Paul Babingui, Sylvie Robert-Piessard, Pierre Renard, Daniel-henri Caignard, jean-Francois Renaud de la Faverle, Gerard Adam
-
Patent number: 5360803Abstract: A pharmaceutical composition for treatment of cancer comprises:(A) a therapeutically effective amount of at least one compound selected from the group consisting of compounds represented by the General Formula (I) ##STR1## wherein X.sub.1 and X.sub.2, which may be the same or different, each represents O, S, Se, --CH.dbd.CH--, ##STR2## Y.sub.1 represents O, S, Se, or ##STR3## R.sub.1 and R.sub.3, which may be the same or different, each represents an alkyl group;R.sub.2 represents an alkyl group, an aryl group or a heterocyclic group;Z.sub.1 and Z.sub.2, which may be the same or different, each represents an atomic group necessary to form a 5- or 6-membered ring;L.sub.1 represents a methine group or L.sub.1 and R.sub.3 may combine and form a 5- or 6-membered ring;R.sub.4 and R.sub.5, which may be the same or different, each represents a alkyl group;R.sub.6 and R.sub.Type: GrantFiled: November 6, 1992Date of Patent: November 1, 1994Assignees: Dan Farber Cancer Institute, Fuji Photo Film Co., Ltd.Inventors: Tadao Shishido, Lan B. Chen
-
Patent number: 5360804Abstract: Multicomponent agent or kit for preparing the sulpho-conjugated form of pyridino, pyrimidino or triazino N-oxide compounds and method of use.The present invention relates to a multicomponent agent or kit for preparing the sulpho-conjugated form of pyridino, pyrimidino or triazino N-oxide compounds,comprising at least one compound of the pyridino, pyrimidino or triazino N-oxide type, on the one hand,and a sulphating agent, on the other hand.Type: GrantFiled: December 12, 1991Date of Patent: November 1, 1994Assignee: L'OrealInventors: Quintino Gaetani, Andre Rougier, Albert Duranton, Michel Hocquaux
-
Patent number: 5348968Abstract: The invention relates to a compound of formula (I): ##STR1## in which: R.sub.1 represents hydrogen or halogen, alkyl, alkoxy, cyano or aminocarbonyl or any one of the following: ##STR2## in which: m is equal to 1, 2 or 3,n is equal to 0, 1 or 2,T represents a CO or SO.sub.2,R.sub.4 or R.sub.5, which are identical or different, represent hydrogen or alkyl or phenyl,R.sub.2 represents hydrogen or alkyl, phenyl or acyl,R.sub.3 represents hydrogen, alkyl (optionally substituted by hydroxyl or phenyl) or alkoxycarbonyl,--X--Y.dbd. represents --N--C.dbd., --N--N.dbd.or else ##STR3## represents --O--N.dbd.; to its enantiomers, diastereoisomers and epimers and to its addition salts with a pharmaceutically acceptable acid.Type: GrantFiled: February 1, 1994Date of Patent: September 20, 1994Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Philippe Maillos, Olivier Muller, Michel Laubie, Tony Verbeuren, Jean-Jacques Descombes