Polycyclo Ring System Having A 1,3,5-triazine As One Of The Cyclos Patents (Class 514/246)
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Patent number: 6660737Abstract: Compounds having a structure according to Formula (I): are effective in a method of increasing erythropoietin and vascularization of tissue in a subject in need thereof.Type: GrantFiled: April 29, 2002Date of Patent: December 9, 2003Assignee: The Procter & Gamble CompanyInventors: Ji-In Kim Almstead, Nicholas John Izzo, David Robert Jones, Richard Masaru Kawamoto
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Publication number: 20030207880Abstract: The present invention provides a compound of formula I 1Type: ApplicationFiled: December 18, 2002Publication date: November 6, 2003Inventors: Gordon L. Bundy, Fred L. Ciske, Michael J. Genin, Steven E. Heasley, Scott D. Larsen, Byung Hyun Lee, Paul D. May, John R. Palmer, Mark E. Schnute, Valerie A. Vaillancourt, Atli Thorarensen, Allison J. Wolf, Nancy Anne Wicnienski, David Wilhite
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Publication number: 20030195210Abstract: The invention relates to novel imidazo[1,3,5]triazinones of the general formula (I), to a method for their production and to their use as medicaments, in particular as inhibitors of cyclic GMP metabolising phosphodiesterases.Type: ApplicationFiled: November 4, 2002Publication date: October 16, 2003Inventors: Ulrich Niewhner, Helmut Haning, Thomas Lampe, Mazen Es-Sayed, Gunter Schmidt, Erwin Bischoff, Klaus Dembowsky, Elisabeth Perzborn, Karl-Heinz Schlemmer
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Patent number: 6630470Abstract: Invented are G-CSF mimetics. Also invented are selected octacyclic compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds as G-CSF mimetics. Also invented are novel processes used in preparing these compounds.Type: GrantFiled: November 20, 2000Date of Patent: October 7, 2003Assignee: SmithKline Beecham CorporationInventors: Juan I Luengo, Kevin J Duffy
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Publication number: 20030170731Abstract: An in vitromethod and a kit for the diagnosis of non-ulcer dyspepsia (NUD) in a subject suspected of having NUD, comprises identifying in the subject a dysfunction of corticotropin releasing hormone (CRH) receptors characterised by the subject's response to CRH-induced adrenocorticotropic hormone (ACTH) production by estimating the level of ACTH in a sample of blood or a blood fraction obtained from said subject relative to a control. The method can be used to diagnose NUD in patients who are infected with Helicobacter pylori and those who are free of such infection.Type: ApplicationFiled: March 17, 2003Publication date: September 11, 2003Inventors: Timothy Garard Dinan, Paul William Napoleon Keeling
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Publication number: 20030162782Abstract: This invention relates to the use of cyclic guanosine 3′,5′-monophosphate phosphodiesterase type five (cGMP PDE5) inhibitors, including in particular the compound sildenafil, for the treatment of neuropathy, including in particular the treatment of diabetic neuropathy.Type: ApplicationFiled: July 26, 2002Publication date: August 28, 2003Inventors: Eric B. Grossman, Nandan P. Koppiker, Steven B. Leichter
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Publication number: 20030125330Abstract: Corticotropin releasing factor (CRF) antagonists of Formula (I): 1Type: ApplicationFiled: March 6, 2002Publication date: July 3, 2003Inventor: Paul J. Gilligan
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Publication number: 20030114458Abstract: The present invention provides compounds of Formula (I): 1Type: ApplicationFiled: May 29, 2002Publication date: June 19, 2003Inventors: Edmund Lee Ellsworth, Howard Daniel Hollis Showalter
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Patent number: 6566365Abstract: In accordance with the present invention there is provided a method for treating or preventing a Flaviviridea viral infection in a host comprising administering a therapeutically effective amount of at least one compound of formula (I) or (II) or a pharmaceutically acceptable salts thereof, wherein Ra, R, Z and Y are defined in the application.Type: GrantFiled: November 3, 2000Date of Patent: May 20, 2003Assignee: BioChem Pharma Inc.Inventor: Richard Storer
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Patent number: 6559147Abstract: This invention is directed to poly-hydroxylated monocyclic N-heterocyclic derivatives selected from the following formulae: wherein Z1, Z2, R1, R2, R3, R4, R5, R6, and R7 are defined herein. These compounds are useful as anti-coagulants.Type: GrantFiled: May 4, 2001Date of Patent: May 6, 2003Assignee: Berlex Laboratories, Inc.Inventor: Gary B. Phillips
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Publication number: 20030069247Abstract: The present invention includes a precursor compound pertaining to a 1,2,4-Triazolo[4,3-a][1,3,5] Triazine compound, particularly a 1,2,4-Triazolo[4,3-a][1,3,5] Triazine-3,5,7-Triamine, and novel fused ring structures such as triazolyl-tetrazinyl-aminotriazine compounds, and complexes and salts thereof, and other such chemical structures.Type: ApplicationFiled: July 10, 2002Publication date: April 10, 2003Inventor: Michael E Sitzmann
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Publication number: 20030027820Abstract: Provided, among things, is a method of treating or ameliorating an indication of the invention in an animal, including a human, comprising administering an effective amount of a compound of the formula IA and or IB: 1Type: ApplicationFiled: May 30, 2002Publication date: February 6, 2003Applicant: Alteon, Inc.Inventor: Martin Gall
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Patent number: 6509338Abstract: The present invention describes novel pyrazolo[1,5-a]triazines of formula: wherein R3 is an alkyl, alkenyl, alkynyl, or cycloalkyl group, or pharmaceutically acceptable salt forms thereof, which are useful as CRF antagonists.Type: GrantFiled: June 14, 1999Date of Patent: January 21, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Richard Eric Olson, William Eric Frietze
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Publication number: 20030013878Abstract: The present invention includes a precursor compound pertaining to a 1,2,4-Triazolo[4,3-a][1,3,5] Triazine compound, particularly a 1,2,4-Triazolo[4,3-a][1,3,5] Triazine-3,5,7-Triamine, and novel fused ring structures such as triazolyl-tetrazinyl-aminotriazine compounds, and complexes and salts thereof, and other such chemical structures.Type: ApplicationFiled: June 14, 2002Publication date: January 16, 2003Inventors: William M. Koppes, Michael E. Sitzmann
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Patent number: 6489333Abstract: This invention relates to novel heterocycles which are useful as antagonists of the &agr;v&bgr;3 integrin, the &agr;2b&bgr;3 integrin, and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.Type: GrantFiled: April 9, 2001Date of Patent: December 3, 2002Assignee: Bristol - Meyers Squibb Pharma CompanyInventors: William J. Pitts, Prabhakar K. Jadhav
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Patent number: 6482815Abstract: Novel organic arsenic compounds are described as cytotoxic agents with potent anti-tumor activity against cancer cells and particularly, with regard to human leukemic cells and breast cancer cells.Type: GrantFiled: November 27, 2000Date of Patent: November 19, 2002Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Xing-Ping Liu
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Patent number: 6476028Abstract: A method of treating a CCR5-mediated disease state in mammals which comprises administering to a mammal in need of such treatment, an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 8, 2000Date of Patent: November 5, 2002Assignees: SmithKline Beecham Corporation, SmithKline Beecham p.l.c.Inventors: William E. Bondinell, James Chan, Roderick A. Porter, Joseph W. Venslavsky, Steven Dabbs, David T. Davies
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Patent number: 6469006Abstract: This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with indoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.Type: GrantFiled: May 16, 2000Date of Patent: October 22, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Wade S. Blair, Milind Deshpande, Haiquan Fang, Pin-Fang Lin, Timothy P. Spicer, Owen B. Wallace, Hui Wang, Tao Wang, Zhongxing Zhang, Kap-Sun Yeung
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Patent number: 6462044Abstract: The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase inhibitor, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one phosphodiesterase inhibitor, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents.Type: GrantFiled: August 30, 2001Date of Patent: October 8, 2002Assignee: NitroMed, Inc.Inventors: David S. Garvey, Inigo Saenz de Tejada, Richard A. Earl, Subhash P. Khanapure
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Publication number: 20020143015Abstract: Use of vardenafil or a pharmaceutical composition thereof in the preparation of a medicament for the curative, palliative or prophylactic treatment of type 2 diabetes mellitus.Type: ApplicationFiled: January 30, 2002Publication date: October 3, 2002Inventors: David A. Fryburg, Earl M. Gibbs, Nandan P. Koppiker
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Patent number: 6451825Abstract: A Rho kinase inhibitor is provided as a novel pharmaceutical agent, particularly as a therapeutic agent of hypertension, a therapeutic agent of angina pectoris, a suppressive agent of cerebrovascular contraction, a therapeutic agent of asthma, a therapeutic agent of peripheral circulation disorder, a prophylactic agent of immature birth, a therapeutic agent of arteriosclerosis, an anti-cancer drug, an anti-inflammatory agent, an immunosuppressant, a therapeutic agent of autoimmune disease, an anti-AIDS drug, a contraceptive, a prophylactic agent of digestive tract infection, a therapeutic agent of osteoporosis, a therapeutic agent of retinopathy and a brain function improving drug. In addition, the Rho kinase inhibitor is provided as a reagent and a diagnostic.Type: GrantFiled: February 26, 2001Date of Patent: September 17, 2002Assignee: Mitsubishi Pharma CorporationInventors: Masayoshi Uehata, Takashi Ono, Hiroyuki Satoh, Keiji Yamagami, Toshio Kawahara
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Patent number: 6426346Abstract: The present application describes 6-membered aromatics of formula I: or pharmaceutically acceptable salt forms thereof, wherein D may be CH2NH2 or C(═NH)NH2, which are useful as inhibitors of factor Xa.Type: GrantFiled: February 15, 2000Date of Patent: July 30, 2002Assignee: Bristol - Myers Squibb Pharma CompanyInventors: James Russell Pruitt, Donald Joseph Phillip Pinto, Mimi Lifen Ouan, Ruth Richmond Wexler
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Publication number: 20020061897Abstract: Compounds of the formula 1Type: ApplicationFiled: March 28, 2001Publication date: May 23, 2002Inventors: Richard L. Elliott, Robert M. Oliver,
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Publication number: 20020049207Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke.Type: ApplicationFiled: November 27, 2001Publication date: April 25, 2002Inventor: James R. McCarthy
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Patent number: 6372743Abstract: Disclosed are compounds of the formula: where R1, R2, R3, R4, R5, R6, and X are defined herein. These compounds are selective modulators of NPY1 receptors. These compounds are useful in the treatment of a number of CNS disorders, metabolic disorders, and peripheral disorders, particularly eating disorders and hypertension. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of NPY1 receptors and as standards in assays for NPY1 receptor binding. Methods of using the compounds in receptor localization studies are given.Type: GrantFiled: September 29, 2000Date of Patent: April 16, 2002Assignees: Neurogen Corporation, Pfizer Inc.Inventors: James W. Darrow, Stephane De Lombaert, Charles Blum, Jennifer Tran, Mark Giangiordano, David Andrew Griffith, Philip Albert Carpino
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Patent number: 6365598Abstract: A chemical compound of formula (I), wherein R1 to R3 are independently selected from hydrogen and alkyl; R4 is selected from hydrogen, alkyl, alkoxy, formyl and cyano; X1 is selected from N and C—R7; X2 is selected from N and C—R8; X3 is selected from N and C—R9; X4 is selected from N and C—R10; wherein at least one of X1, X2, X3 and X4 is N; and R5 to R10 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, alkylsulfoxyl, alkylsulfonyl, arylsulfoxyl, arylsulfonyl, amino, monoalkylamino, dialkylamino, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino, and the use thereof in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardType: GrantFiled: March 1, 2001Date of Patent: April 2, 2002Assignee: Vernalis Research LimitedInventors: David Reginald Adams, Jonathan Mark Bentley, Jonathan Richard Anthony Roffey, Corinna Dagmar Bodkin, Howard Langham Mansell, Ashley Roger George, Ian Anthony Cliffe
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Patent number: 6358950Abstract: Corticotropin releasing factor (CRF) antagonists of formula I or II: and their use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.Type: GrantFiled: October 26, 2000Date of Patent: March 19, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Liqi He, Paul Gilligan, Robert Chorvat, Argyrios Georgios Arvanitis
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Publication number: 20020028799Abstract: The present invention relates to the use of neutral endopeptidase inhibitors (NEPi) and a combination of NEPi and phosphodiesterase type 5 (PDE5) inhibitor for the treatment of male sexual dysfunction, in particular MED.Type: ApplicationFiled: June 29, 2001Publication date: March 7, 2002Inventors: Alasdair Mark Naylor, Pieter Hadewijn Van Der Graaf, Christopher peter Wayman
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Publication number: 20020025960Abstract: The present invention provides a compound of formula I 1Type: ApplicationFiled: June 22, 2001Publication date: February 28, 2002Inventors: Gordon L. Bundy, Fred L. Ciske, Michael J. Genin, Steven E. Heasley, Scott D. Larsen, Byung Hyun Lee, Paul D. May, John R. Palmer, Mark E. Schnute, Valerie A. Vaillancourt, Atli Thorarensen, Allison J. Wolf, Nancy Anne Wicnienski, David Wilhite
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Patent number: 6342492Abstract: The invention relates to a family of new synthetic triamine compounds which can be used in antiviral pharmaceutical compositions.Type: GrantFiled: August 7, 1997Date of Patent: January 29, 2002Assignee: The Research Foundation of State University of New YorkInventor: Thomas W. Bell
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Publication number: 20020002145Abstract: Hepatic cirrhosis and fibrosis and fatty liver can be prevented and treated by administering to a subject in need thereof an effective amount of at least one adenosine A2A receptor antagonist or at least one adenosine uptake promotor.Type: ApplicationFiled: February 12, 2001Publication date: January 3, 2002Inventors: Bruce N. Cronstein, Edwin Chan
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Patent number: 6331543Abstract: The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase inhibitor, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one phosphodiesterase inhibitor, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents.Type: GrantFiled: September 1, 1999Date of Patent: December 18, 2001Assignee: NitroMed, Inc.Inventors: David S. Garvey, Inigo Saenz de Tejada, Richard A. Earl, Subhash P. Khanapure
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Patent number: 6313124Abstract: Corticotropin releasing factor (CRF) antagonists of formula I or II: and their use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.Type: GrantFiled: January 28, 1998Date of Patent: November 6, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: Liqi He, Paul Gilligan, Robert Chorvat, Argyrios Georgios Arvanitis
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Patent number: 6297252Abstract: Disclosed are compounds of compounds of the formula: or the pharmaceutically acceptable nontoxic salts thereof wherein: X is oxygen, H2 or sulfur Y is hydrogen, or optionally substituted alkyl, alkenyl, (substituted)arylalkyl, aryl or heteroaryl, or a carbonyl group substituted with alkyl, cycloalkyl, aryl, or amino groups; W is alkyl, arylalkyl or heteroarylalkyl, where each aryl group is optionally substituted with up to two groups; or W is aryl, thienyl, pyridyl or heteroaryl, each of which is optionally substituted; and Z1, Z2, Z3, and Z4 independently represent nitrogen or C—R1 where R1 is hydrogen, halogen, hydroxy, amino, or phenyl or pyridyl optionally mono- or independently disubstituted with halogen, hydroxy, lower alkyl, or lower alkoxy, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists or inverse agonists for GABAa brain receptors.Type: GrantFiled: July 19, 2000Date of Patent: October 2, 2001Assignee: Neurogen CorporationInventors: Paul Chen, Alan Hutchison, Guolin Cai
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Publication number: 20010025042Abstract: Corticotropin releasing factor (CRF) antagonists of Formula (I): 1Type: ApplicationFiled: February 21, 2001Publication date: September 27, 2001Inventors: Argyrios Arvanitis, Paul J. Gilligan, James P. Beck, Rajagopal Bakthavatchalam
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Patent number: 6218410Abstract: A Rho kinase inhibitor is provided as a novel pharmaceutical agent, particularly as a therapeutic agent of hypertension, a therapeutic agent of angina pectoris, a suppressive agent of cerebrovascular contraction, a therapeutic agent of asthma, a therapeutic agent of peripheral circulation disorder, a prophylactic agent of immature birth, a therapeutic agent of arteriosclerosis, an anti-cancer drug, an anti-inflammatory agent, an immunosuppressant, a therapeutic agent of autoimmune disease, an anti-AIDS drug, a contraceptive, a prophylactic agent of digestive tract infection, a therapeutic agent of osteoporosis, a therapeutic agent of retinopathy and a brain function improving drug. In addition, the Rho kinase inhibitor is provided as a reagent and a diagnostic.Type: GrantFiled: April 19, 1999Date of Patent: April 17, 2001Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Masayoshi Uehata, Takashi Ono, Hiroyuki Satoh, Keiji Yamagami, Toshio Kawahara
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Patent number: 6194410Abstract: The present invention is concerned with pyrazolopyrimidines and pyrazolotriazines of the general formula and their pharmaceutically acceptable salts. Surprisingly, these compounds evidence selective affinity to 5HT-6 receptors. They are accordingly suitable for use in the treatment and prevention of central nervous disorders such as, for example, psychoses, schizophrenia, manic depressions, depressions, neurological disorders, memory disorders, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease and Huntington's chorea.Type: GrantFiled: February 24, 1999Date of Patent: February 27, 2001Assignee: Hoffman-La Roche Inc.Inventors: Michael Bös, Claus Riemer, Heinz Stadler
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Patent number: 6191131Abstract: Corticotropin releasing factor (CRF) antagonists of formula I or II: and their use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.Type: GrantFiled: January 28, 1998Date of Patent: February 20, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: Liqi He, Paul Gilligan, Robert Chorvat, Argyrios Georgios Arvanitis
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Patent number: 6166019Abstract: Compounds of Formula I and II and their pharmaceutically acceptable, salts, esters and prodrugs thereof are selective alpha-1D adrenoceptor anatagonists and may be useful for treating disease states.Type: GrantFiled: July 9, 1999Date of Patent: December 26, 2000Assignee: Abbott LaboratoriesInventors: Michael D. Meyer, William A. Caroll
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Patent number: 6166016Abstract: The invention provides amide derivatives which are useful as analgesics, anti-inflammatory agents, antimicrobial drugs, hypoglycemic agents, hypolipidemic agents, antihypertensive agents, anti-cancer agents, etc., the derivatives being represented by the formula ##STR1## wherein ring A represents a benzene ring, a naphthalene ring, a pyridine ring or a furan ring; R.sup.4 represents a heterocyclic group selected from the group consisting of a lower alkyl-substituted thieno[3,2-d]pyrimidin-4-yl group, an optionally substituted pyrazolo[1,5-a]-1,3,5-triazin-4-yl group, a pyrazolo[3,4-d]pyrimidin-4-yl group substituted at the 6-position and a purin-6-yl group substituted at the 2-position; and R.sup.Type: GrantFiled: December 2, 1998Date of Patent: December 26, 2000Assignee: Otsuka Pharmaceutical Factory, Inc.Inventors: Takashi Okamura, Yasuo Shoji, Tadao Shibutani, Tsuneo Yasuda, Takeshi Iwamoto
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Patent number: 6159706Abstract: The present invention provides a method for targeting toxic antimetabolites to gram negative infections. It provides a means of taking advantage of a key disease resistance mechanism to activate these drugs locally, and to overcome the resistance phenotype of the microbes. The invention further provides a method for selecting for antibiotic sensitivity, since a likely mechanism by which organisms are likely to gain resistance to the prodrugs is via loss of enzyme activity, which will make the bacteria sensitive to antibiotics once again.Type: GrantFiled: December 18, 1998Date of Patent: December 12, 2000Assignee: NewBiotics, Inc.Inventor: H. Michael Shepard
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Patent number: 6156766Abstract: Benzamide compounds of the formula ##STR1## wherein each symbol is defined in the specification, isomers thereof and pharmaceutically acceptable acid addition salts thereof. Pharmaceutical compositions comprising a therapeutically effective amount of this compound and a pharamaceutically acceptable additive, and therapeutic agents for hypertension, therapeutic agents for angina pectoris, therapeutic agent for asthma, therapeutic agents for renal and peripheral circulatory disturbances and inhibitor of cerebral vasospasm, which comprise this compound. The compound of the present invention has strong smooth muscle relaxing action, and shows hypertensive action and cerebral.cndot.coronary vasodilating action like conventional calcium antagonists, as well as long-lasting renal and peripheral circulation improving action.Type: GrantFiled: February 18, 1999Date of Patent: December 5, 2000Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Masafumi Arita, Tadamasa Saitoh, Masanori Minoguchi, Keiji Yamagami, Hiroyuki Satoh
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Patent number: 6124289Abstract: Corticotropin releasing factor (CRF) antagonists of formula I or II: ##STR1## and their use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivityassociated with psychopathological disturbance andstress.Type: GrantFiled: July 23, 1997Date of Patent: September 26, 2000Assignee: Dupont Pharmaceuticals Co.Inventors: Liqi He, Paul Joseph Gilligan, Argyrios Georgios Arvanitis, Robert John Chorvat
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Patent number: 6004585Abstract: The present invention relates to dust free, easily flowable and dosable granular compositions containing triazine, having a particle size distribution of between 40 and 400.mu. and an upper limit of particle size at 2000.mu., which can be effectively mixed with feed for administration to animals.Type: GrantFiled: July 31, 1998Date of Patent: December 21, 1999Assignee: Bayer AktiengesellschaftInventors: Dorothea Grofmeyer, Christian Mundt, Christian Wegner
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Patent number: 5985925Abstract: Novel cosmetic/dermatological UV-photoprotective compositions well suited for enhanced PF photoprotection of human skin and/or hair comprise (a) an effective UV-screening amount of at least one benzylidenecamphor sunscreen compound, and/or at least one dibenzoylmethane sunscreen compound, and/or at least one triazine sunscreen compound, and (b) a PF-enhancing amount of at least one dialkyl tartrate, formulated into a topically applicable, cosmetically/dermatologically acceptable vehicle, diluent or carrier therefor.Type: GrantFiled: September 9, 1998Date of Patent: November 16, 1999Assignee: Societe L'Oreal S.A.Inventors: Martin Josso, Jean-Louis Refregier, Isabelle Hansenne
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Patent number: 5929114Abstract: Arylthiol and dithiobisarylamide antibacterial and antiviral agents have the general formula ##STR1## where A is monocyclic or bicyclic aryl which can contain up to 3 heteroatoms selected from O, S, and N,R.sup.1 and R.sup.2 are substituent groups, X is ##STR2## or SO.sub.2 NR.sup.4 Z, Y is H or SZ when n is 1, a single bond when n is 2; R.sup.4 and Z can be hydrogen or alkyl.Type: GrantFiled: May 15, 1997Date of Patent: July 27, 1999Assignee: Warner-Lambert CompanyInventors: John Michael Domagala, Edward Faith Elslager, Rocco Dean Gogliotti
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Patent number: 5886008Abstract: 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.Type: GrantFiled: April 27, 1995Date of Patent: March 23, 1999Assignee: Pfizer Inc.Inventor: John Eugene Macor
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Patent number: 5874433Abstract: Inhibitor of the use of tetrahydrobiopterin as a cofactor for nitric oxide synthase, e.g., substituted 4-phenyl(hydropyridines) such as 1-methyl-4-(3',4'-dihydroxyphenyl)-1,2,3,6-tetrahydropyridine or, 4-(3',4'-dihydroxyphenyl)-1,2,3,6-tetrahydropyridine) or tetrahydropterin analog which does not replace tetrahydrobiopterin as a substrate for nitric oxide synthase such as (6R,S)-6,7-dimethyl-tetrahydropterin or (6R,S)-tetrahydrofolic acid or 2,4-diamino-, 2,6-diamino, or 4,6-diamino mono- or disubstituted pyrimidines or the corresponding pyrimidine-3-oxides such as 2,4-diamino-6-(diethylamino)pyrimidine, 2,4-diamino-6-piperidino-pyrimidine-3-oxide, 2,4-diamino-6-hydroxypyrimidine, 4,6-diamino-2-hydroxypyrimidine or 2,5-diamino-4,6-dihydroxypyrimidine is administered to inhibit nitric oxide synthesis from arginine in vascular cells in a subject in need of such inhibition (e.g., for prophylaxis or treatment of cytokine- or endotoxin-induced hypotension (e.g., septic shock).Type: GrantFiled: December 19, 1995Date of Patent: February 23, 1999Assignee: Cornell Research Foundation, Inc.Inventor: Steven S. Gross
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Patent number: 5856331Abstract: There is disclosed a method for preventing tissue injury caused by tissue hypoxia and reoxygenation, comprising administering a compound that inhibits signal transduction by inhibiting cellular accumulation of linoleoyl phosphatidic acid (PA) through an inhibition of the enzyme LPAAT (lysophosphatidic acyltransferase).Type: GrantFiled: October 10, 1997Date of Patent: January 5, 1999Assignee: Cell Therapeutics, Inc.Inventors: Stuart L. Bursten, Jack W. Singer, Glenn C. Rice
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Patent number: 5792766Abstract: Disclosed are compounds of compounds of the formula: ##STR1## or the pharmaceutically acceptable nontoxic salts thereof wherein: X is oxygen, H.sub.2 or sulfurY is hydrogen, or optionally substituted alkyl, alkenyl, (substituted)arylalkyl, aryl or heteroaryl, or a carbonyl group substituted with alkyl, cycloalkyl, aryl, or amino groups;W is alkyl, arylalkyl or heteroarylalkyl, where each aryl group is optionally substituted with up to two groups; orW is aryl, thienyl, pyridyl or heteroaryl, each of which is optionally substituted; andZ.sub.1, Z.sub.2, Z.sub.3, and Z.sub.4 independently represent nitrogen or C-R.sub.1 whereR.sub.1 is hydrogen, halogen, hydroxy, amino, or phenyl or pyridyl optionally mono- or independently disubstituted with halogen, hydroxy, lower alkyl, or lower alkoxy,which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists or inverse agonists for GABAa brain receptors.Type: GrantFiled: March 13, 1996Date of Patent: August 11, 1998Assignee: Neurogen CorporationInventors: Paul Chen, Alan Hutchison, Guolin Cai