Bicyclo Ring System Having The Hetero Ring As One Of The Cyclos (e.g., Methylenedioxyphenyl Group, Etc.) Patents (Class 514/464)
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Patent number: 6441032Abstract: Disclosed are novel &agr;-aryl-N-alkylnitrone compounds and pharmaceutical compositions containing such compounds. The disclosed compositions are useful as therapeutics for preventing and/or treating neurodegenerative, autoimmune and inflammatory conditions in mammals and as analytical reagents for detecting free radicals.Type: GrantFiled: August 9, 2000Date of Patent: August 27, 2002Assignee: Centaur Pharmaceuticals, Inc.Inventors: Judith A. Kelleher, Kirk R. Maples, Alina Dykman, Yong-Kang Zhang, Allan L. Wilcox, Julian Levell
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Patent number: 6433008Abstract: Disclosed are novel aryl-N-alkylnitrone compounds and pharmaceutical compositions containing such compounds. The disclosed compositions are useful as therapeutics for preventing and/or treating neurodegenerative, autoimmune and inflammatory conditions in mammals and as analytical reagents for detecting free radicals.Type: GrantFiled: July 18, 2000Date of Patent: August 13, 2002Assignee: Centaur Pharmaceuticals, Inc.Inventors: Judith A. Kelleher, Kirk R. Maples, Alina Dykman, Yong-Kang Zhang, Allan L. Wilcox, Julian Levell
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Patent number: 6420393Abstract: The invention relates to cyclopentabenzofuran derivatives, processes for their preparation, the use of cyclopentabenzofuran derivatives for the production of a medicament for the therapy of NF-&kgr;B-dependent diseases and medicaments which contain the cyclopentabenzofuran derivatives.Type: GrantFiled: March 26, 2001Date of Patent: July 16, 2002Assignee: Bayer AktiengesellschaftInventors: Walter Guarnieri, Thomas Jaetsch, Andreas Schoop, Jörg Baumgarten, Axel Kretschmer, Horst-Peter Antonicek
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Publication number: 20020082256Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.Type: ApplicationFiled: September 25, 2001Publication date: June 27, 2002Inventors: Rajashehar Betageri, Steffen Breitfelder, Pier F. Cirillo, Thomas A. Gilmore, Eugene R. Hickey, Thomas M. Kirrane, Monica H. Moriak, Neil Moss, Usha R. Patel, John R. Proudfoot, John R. Regan, Rajiv Sharma, Sanxing Sun, Alan D. Swinamer, Hidenori Takahashi
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Patent number: 6410567Abstract: The present invention relates to a new pesticide which is based on a photosensitizer or combination of photosensitizers of the tetrapyrrole and/or tetraazapyrrole series which may comprise a biological and/or chemical attractant for pests and to a method of controlling pests using the new pesticide.Type: GrantFiled: December 17, 1998Date of Patent: June 25, 2002Inventor: Giulio Jori
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Publication number: 20020072537Abstract: The comprehensive pharmacologic therapy for treatment of obesity is a procedure which involves the administration of a desired therapeutic range of Diethylpropion and/or Phentermine in combination with a SSRI medication and nutritional supplementation for brief and long durations which may be 12 months or more. The preferred procedure involves the administration of drugs in combination which are identified as: Citalopram (Celexa) and Phentermine; Citalopram (Celexa) and Diethylpropion; Citalopram (Celexa), Phentermine, and Diethylpropion. In addition nutritional supplementation such as a multivitamin, 5-Hydroxytryptophan, vitamin B6, vitamin C, Tyrosine, Calcium, and Lysine may be used to enhance the performance of the weight loss treatment program.Type: ApplicationFiled: August 29, 2001Publication date: June 13, 2002Inventor: Martin C. Hinz
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Patent number: 6392046Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: GrantFiled: September 30, 1999Date of Patent: May 21, 2002Assignee: Vertex Pharmaceuticals, Inc.Inventors: Roger D. Tung, Mark A. Murcko, Govinda Rao Bhisetti
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Publication number: 20020058695Abstract: Tetrahydropiperine and analogs and derivatives thereof, including dihydropiperine, are disclosed to enhance the absorption and/or bioavailablity of nutrients, drugs and other organic compounds, such as insectides.Type: ApplicationFiled: May 21, 2001Publication date: May 16, 2002Inventors: Muhammed Majeed, Vladimir Badmaev, Rajinder Kumar Bammi, Subbalakshmi Prakash, Sankaran Natarajan
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Publication number: 20020052325Abstract: Anticonvulsant derivatives useful in maintaining weight loss.Type: ApplicationFiled: December 18, 2001Publication date: May 2, 2002Inventor: Marc Kamin
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Patent number: 6380188Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: September 29, 2000Date of Patent: April 30, 2002Assignee: G. D. Searle & Co.Inventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagaraian, Joseph J. McDonald
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Patent number: 6376535Abstract: The present invention relates to oxygen-containing heterocyclic compounds represented by the following formula (I): wherein m represents an integer of 0 to 4; R1, R2, R3 and R4 independently represent a hydrogen atom, substituted or unsubstituted lower alkyl, etc.; R5 represents substituted or unsubstituted lower alkoxy etc.; R6 represents a hydrogen atom etc.; and Y represents the following formula (II): wherein R9 represents cyano etc., R10 represents a hydrogen atom etc., R11 represents carboxy etc., and R12 represents a hydrogen atom etc.; and the like; or pharmaceutically acceptable salts thereof.Type: GrantFiled: March 1, 2001Date of Patent: April 23, 2002Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Ohshima, Koji Yanagawa, Haruhiko Manabe, Ichiro Miki, Yoshiaki Masuda
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Patent number: 6369099Abstract: A method of modifying or altering the structure of a 1&agr;-hydroxylated vitamin D compound to increase its biological activity by altering the conformational equilibrium of the A-ring to favor a chair conformation that presents the 1&agr;-hydroxyl in the axial orientation. This is accomplished by either locking the A-ring chair conformation in a geometry having an axially orientated 1&agr;-hydroxyl, or by the addition of one or more substituents to the A-ring which interact with other substituents in the molecule or on the A-ring to provide a driving force to the A-ring to adopt a chair conformation which presents the 1&agr;-hydroxyl in the axial orientation.Type: GrantFiled: April 20, 2000Date of Patent: April 9, 2002Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Rafal R. Sicinski
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Publication number: 20020040027Abstract: A method for the systemic control of blood-sucking parasites in warm-blooded animals or for the prevention of reinfestation, which comprises administering systemically to the warm-blooded animal a compound of formula 1Type: ApplicationFiled: October 5, 2001Publication date: April 4, 2002Inventors: Friedrich Karrer, Thomas Gobel, Elaine Humbert-Droz
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Patent number: 6365199Abstract: A hair growth formulation. The two basic main ingredients are castor oil and a special lemon extract. The special lemon extract is made from fresh lemon peel. The peel, including the bioflavonoids membrane, is blended with purified water until it is liquidified. Then the mixture is filtered through a sanitized cloth. Other ingredients that have been found helpful include: inositol, choline (from bitartate), niacinamide or nicotinic acid, manganese in chelated form, bioflavonoids, and folic acid. Finally perfume and sodium benzoate (as a preservative) can be added.Type: GrantFiled: August 10, 2000Date of Patent: April 2, 2002Inventor: Marsha E. Olguin
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Publication number: 20020032177Abstract: The present invention relates to the use of D-chiro-inositol (DCI) as a regulator of hypothalamic gene expression and, more particularly, to the use of DCI and derivatives and metabolites thereof to treat neuroendocrine impairments such as obesity, polycystic ovarian syndrome (PCOS), impaired regulation of hormones during aging and to correct such neuroendocrine impairments and associated functions.Type: ApplicationFiled: April 30, 2001Publication date: March 14, 2002Applicant: Insmed Pharmaceuticals, Inc.Inventors: Geoffrey Allan, Charles V. Mobbs
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Patent number: 6353014Abstract: A method of treating glaucoma or ocular hypertension in a patient, which comprises administering to the patient a pharmaceutically effective amount of a compound of formula I:Type: GrantFiled: June 2, 1999Date of Patent: March 5, 2002Assignee: Alcon Laboratories, Inc.Inventors: Verney L. Sallee, Mark R. Hellberg, Peter G. Klimko
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Publication number: 20020022638Abstract: This invention provides compounds of Formula I having the structure 1Type: ApplicationFiled: July 12, 2001Publication date: February 21, 2002Applicant: American Home Products CorporationInventors: Mark A. Ashwell, William R. Solvibile
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Patent number: 6344570Abstract: Compounds of formula (II) where R1 is in the para or meta position and is (A); R2 and R3 are each independently selected from hydrogen, nitro, C1-6alkyl, C3-6cycloalkyl, C2-6alkenyl, C2-6alkynyl, C1-4alkoxyl, C1-6alkylamino, C1-6dialkylamino, C1-6akylC1-4alkoxyl, C1-6alkylaminoC1-6alkyl, amino, cyano, halogeno, trifluoromethyl, —CO2R12 and —CONR12R13, where R12 and R13 are independently selected from hydrogen or C1-6alkyl, or R2 and R3 together with the phenyl to which they are attached form a 9 or 10 membered bicyclic ring system; R4 is C1-4alkyl; R5 is selected from hydrogen and C1-4alkyl; R6 is selected from C1-6alkyl, C1-4alkyl(C4-6)cycloalkyl, C1-6alkyl(C1-6)alkoxyl, C1-6alkylS(C1-6)alkyl, C1-4alkylsulphonyl(C1-4)alkyl; (B) where q is an integer from 1 to 6 and R14 is halogeno; R7 is selected from C1-6alkyl, C1-8alkoxylcarbonyl, C2-6alkenyl, 1,3-benzodioxol-5-yl and aryl each optionally substituted by one or more substituents selected from C1-4alkoxy, C1-6alkyl, cyano, halogType: GrantFiled: July 11, 2000Date of Patent: February 5, 2002Assignee: AstraZeneca UK LimitedInventors: David R Brittain, Craig Johnstone
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Publication number: 20020010178Abstract: 1-phenyl-3-dimethylaminopropane compounds corresponding to the formula I 1Type: ApplicationFiled: April 20, 2001Publication date: January 24, 2002Applicant: Gruenenthal GmbHInventors: Helmut Buschmann, Wolfgang Strassburger, Elmar Friderichs
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Patent number: 6340704Abstract: The present invention provides a compound represented by the formula: wherein R1 is an amino group which may be substituted; R2 is a hydrogen atom or a lower alkyl group which may be substituted; X is a methyne group which may be substituted or N(O)m (m is 0 or 1); a ring A is a homo- or hetero-cycle which is substituted by a halogen atom, lower alkyl, lower alkoxy or lower alkylenedioxy; and a ring B is a homo- or hetero-cycle which may be substituted; or a salt thereof, which exhibits excellent cell differentiation-inducing action and cell differentiation-inducing factor action-enhancing action, and is useful in the treatment and prevention of various nerve diseases or bone/joint diseases.Type: GrantFiled: July 19, 1999Date of Patent: January 22, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Shogo Marui, Masatoshi Hazama, Kohei Notoya, Koki Kato
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Publication number: 20020006910Abstract: The means for allaying drunkenness, preventing and removing alcohol intoxicaiton and hangover syndrome comprises 10 to 400 mg of a component based on succinic acid, 10 to 400 mg of at least one component based on L-glutamic acid, selected from the group consisting of L-glutamic acid, sodium mono-L-glutamate, sodium di-L-glutamate, ammonium mono-L-glutamate, ammonium di-L-glutamate, potassium mono-L-glutamate and potassium di-L-glutamate, 2 to 300 mg of at least one component based on fumaric acid, selected from the group consisting of fumaric acid, sodium monofumarate, sodium difumarate, ammononium monofumarate, ammonium difumarate, potassium monofumarate, potassium difumarate, 1 to 300 mg of ascorbic acid and up to 100 mg of at least one energizer selected from the group consisting of aspartic acid, sodium aspartate, glycine, one of amino acids, sorbic acid and at least one sugar substitute selected from the group consisting of sucrose, glucose, sorbose, sorbitol, fructose, saccarine, aspartame, xylitol, sorType: ApplicationFiled: May 17, 2001Publication date: January 17, 2002Inventors: Dmitri Miasnikov, Aleksandr Kashlinsky
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Publication number: 20020002200Abstract: Novel dephenylethylene compounds that are administered orally to decrease circulating concentrations of glucose are provided. The effect on insulin resistant rats is also shown. The effects on lipid and leptin concentrations are also shown. The compounds are orally effective anti-diabetic agents that may normalize glucose and lipid metabolism in subjects with diabetes.Type: ApplicationFiled: February 5, 2001Publication date: January 3, 2002Inventors: Bishwagit Nag, Debendranath Dey, Satyanarayana Medicherla, Partha Neogi
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Publication number: 20020002177Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: ApplicationFiled: July 10, 2001Publication date: January 3, 2002Applicant: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
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Patent number: 6335358Abstract: Compounds related to lactacystin and lactacystin &bgr;-lactone, pharmaceutical compositions containing the compounds, and methods of use.Type: GrantFiled: April 12, 1995Date of Patent: January 1, 2002Assignee: President and Fellows of Harvard CollegeInventors: Gabriel Fenteany, Timothy F. Jamison, Stuart L. Schreiber, Robert F. Standaert
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Patent number: 6331531Abstract: Method for controlling harmful organisms in genetically modified cotton plants which contain a gene derived from Bacillus thuringiensis which encodes and expresses an insecticidally active protein, which comprises applying an insecticisally effective amount of one or more compounds from the following groups and a-f, described herein, to the plants, to their seeds or propagation stock and/or to the area in which they are cultivated. The method according to the invention makes it possible to reduce the application rate of crop protection agents which act synergistically with the transgenic plants, and also to increase and widen the efficacy of the transgenic plants, and therefore offers both economical and ecological advantages.Type: GrantFiled: June 3, 1999Date of Patent: December 18, 2001Assignee: Aventis CropScience GmbHInventor: Manfred Kern
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Patent number: 6319946Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: GrantFiled: February 9, 2000Date of Patent: November 20, 2001Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael R. Hale, Christopher T. Baker, Timothy A. Stammers, Ronald George Sherrill, Andrew Spaltenstein, Eric Steven Furfine, Francois Maltais, Clarence Webster Andrews, III, John Franklin Miller, Vicente Samano
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Patent number: 6316496Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: February 1, 2000Date of Patent: November 13, 2001Assignee: G. D. Searle & Co.Inventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, David L Brown, Joseph J McDonald
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Patent number: 6310080Abstract: Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically inhibiting retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: December 1, 1999Date of Patent: October 30, 2001Assignee: G. D. Searle & Co.Inventors: Daniel P Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L. Brown, Joseph J. McDonald
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Patent number: 6306873Abstract: This invention relates to compounds of general formula (I): in which Ar is a group selected from: A1, A2, B, C, D, E, Q1-Q3, R1-R9, Z1 and Z2 are as defined in the disclosure, and Y represents carboxy or an acid bioisostere. These compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmaceutical compositions comprising compounds of formula (I), their pharmaceutical use and methods for their preparation.Type: GrantFiled: July 20, 1999Date of Patent: October 23, 2001Assignee: Aventis Pharmaceuticals Products Inc.Inventors: Christopher J. Burns, Richard Labaudiniere, Stephen Condon, Robert D. Groneberg, Rose M. Mathew, Joseph M. Salvino
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Patent number: 6306899Abstract: This invention relates to anti-viral drugs such as Helioxanthin and its analogs. The present compounds may be used alone or in combination with other drugs for the treatment of Hepatitis B virus (HBV), Hepatitis C virus (HCV), Yellow Fever, Dengue Virus, Japanese Encephalitis, West Nile virus and related flaviviruses. In addition, compounds according to the present invention can be used to prevent hepatoma secondary to virus infection as well as other infections or disease states which are secondary to the virus infection.Type: GrantFiled: August 23, 1999Date of Patent: October 23, 2001Assignees: Yale University, N. Y. Mu, N.T.U., V.G.HInventors: Yung-Chi Cheng, Chen-Kung Chou, Lei Fu, Yueh-Hsiung Kuo, Sheau-Farn Yeh, Juliang Zhu, Yonglian Zhu
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Publication number: 20010031766Abstract: Compounds and methods for treating prostaglandin mediated diseases, and certain pharmaceutical compositions thereof are disclosed.Type: ApplicationFiled: February 12, 2001Publication date: October 18, 2001Applicant: Merck Frosst Canada & Co.Inventors: Michel Belley, Nicholas Lachance, Marc Labelle, Michel Gallant, Nathalie Chauret, Laird A. Trimble
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Publication number: 20010031275Abstract: Compositions comprising sesamol or a sesamol metabolite, such as pharmaceutical or therapeutic agents, dietary supplements and nutritional solutions, are described for use as anti-inflammatory agents. Methods for inhibiting inflammation are also described.Type: ApplicationFiled: January 14, 2000Publication date: October 18, 2001Inventors: R Armour Forse, Sambasiva R Chavali
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Patent number: 6300370Abstract: Camomile oil having a high cis- and trans-spiroether content is produced in a process which includes steam distillation or aqueous distillation of fresh camomile or an extraction residue of camomile.Type: GrantFiled: June 10, 1998Date of Patent: October 9, 2001Assignee: ASTA Medica AktiengesellschaftInventors: Reinhold Carle, Otto Isaac
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Patent number: 6294568Abstract: The present invention provides compounds represented by the general formula (I): and a salt thereof, and anti-inflammatory agents and antitumor agents containing the compounds as the active ingredients.Type: GrantFiled: June 26, 2000Date of Patent: September 25, 2001Assignee: Nissin Food Products Co., Ltd.Inventors: Toshihiro Yamada, Yoichi Nobuhara, Kazuhiro Kobayashi, Satoshi Hirano, Takanobu Sakurai, Hiroshi Mikami, Ayako Miyake
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Patent number: 6294560Abstract: The present invention is directed to an improved synthesis of clasto-lactacystin-&bgr;-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-&bgr;-lactones, and analogs thereof and their use as proteosome inhibitors.Type: GrantFiled: June 20, 2000Date of Patent: September 25, 2001Assignee: Millennium Pharmaceuticals, Inc..Inventors: François Soucy, Louis Plamondon, Mark Behnke, William Roush
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Patent number: 6288071Abstract: Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.Type: GrantFiled: December 10, 1998Date of Patent: September 11, 2001Assignee: Bayer AktiengesellschaftInventors: Henry Szczepanski, Martin Zeller, Ottmar Franz Hüter
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Patent number: 6274600Abstract: Compounds are useful for enhancing synaptic responses mediated by AMPA receptors are disclosed, as are methods for the preparation thereof and methods for their use for treatment of subjects suffering from impaired nervous or intellectual functioning due to deficiencies in the number of excitatory synapses or in the number of AMPA receptors. The invention compounds can also be used for the treatment of non-impaired subjects for enhancing performance in sensory-motor and cognitive tasks which depend on brain networks utilizing AMPA receptors and for improving memory encoding.Type: GrantFiled: April 5, 1999Date of Patent: August 14, 2001Assignee: The Regents of the University of CaliforniaInventors: Gary S. Lynch, Gary A. Rogers
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Patent number: 6267992Abstract: Diabetic nephropathy and microalbuminuria are treated with the herb Salviae Miltiorrhizae Radix. In one embodiment, the method includes boiling the herb to form an aqueous extract. The aqueous extract is administered to the diabetic individual to treat diabetic nepliropathy or to an individual exhibiting microalbuminuria. Alternatively the method can include administering a salt of lithospermic acid extracted from the herb. The method can include determining the level of protein in urine before, during and/or after administering the aqueous extract or a salt of lithospermic acid.Type: GrantFiled: September 21, 2000Date of Patent: July 31, 2001Assignee: Shiva Biomedical LLCInventors: Hai-Ri Li, Hyun Chul Lee, Mankil Jung, Sudhir V. Shah
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Publication number: 20010003780Abstract: Retinoid antagonist compounds have been found to be useful in the prevention and/or minimization of surgical adhesion formation.Type: ApplicationFiled: December 8, 2000Publication date: June 14, 2001Inventors: Kenneth M. Tramposch, Xina Nair, Anne Marinier, Fred Christopher Zusi
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Patent number: 6225327Abstract: Composition and methods for treating ocular allergic reactions are disclosed. In particular, the invention is directed to compounds which inhibit human conjunctival mast cell degranulation.Type: GrantFiled: October 7, 1998Date of Patent: May 1, 2001Assignees: Alcon Laboratories, Inc., Yamanouchi Pharmaceutical Co., Ltd.Inventors: Steven T. Miller, Mark R. Hellberg, John M. Yanni
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Patent number: 6214870Abstract: The present invention relates to dioxocyclopentyl hydroxamide derivatives of the formula wherein X, Z and Q are as defined in the specification, and to pharmaceutical compositions and methods of treatment thereof.Type: GrantFiled: March 28, 2000Date of Patent: April 10, 2001Assignee: Pfizer IncInventors: Kim F. McClure, Ralph P. Robinson
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Patent number: 6211197Abstract: Compounds and methods for treating prostaglandin mediated diseases, and certain pharmaceutical compositions thereof are disclosed. The compounds are represented by formula II: Ar1—W—Ar2—X—Q II The compounds of the invention are structurally different from NSAIDs and opiates, and are antagonists of the pain and inflammatory effects of E-type prostaglandins.Type: GrantFiled: October 4, 1999Date of Patent: April 3, 2001Assignee: Merck Frosst Canada & Co.Inventors: Michel Belley, Marc Labelle, Nicholas Lachance, Michel Gallant, Nathalie Chauret, Laird A. Trimble, Chun Li
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Patent number: 6180663Abstract: A therapeutic nasal inhalant for using bioflavanoids as a topical antioxidant. The therapeutic nasal inhalant includes a method for making a therapeutic nasal inhalant composition for treating nasal mucosa. The method comprises the steps of mixing together two cups of water, one teaspoon of baking soda, one teaspoon of sodium chloride, and four milligrams of vitamin C to form a mixture. Mixing a bioflavanoid with the mixture. Allowing the mixture to stand. Filtering the mixture. Allowing the mixture to stand for a second time. Filtering the mixture.Type: GrantFiled: December 3, 1999Date of Patent: January 30, 2001Inventor: Stanley Lang
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Patent number: 6172106Abstract: Methods for inhibiting &Dgr;-5-desaturase activity, for inhibiting arachidonic acid metabolism, for inhibiting PGE2 levels and for inhibiting PLA2 activity comprising administering sesamol are disclosed.Type: GrantFiled: October 28, 1999Date of Patent: January 9, 2001Inventors: R. Armour Forse, Sambasiva R. Chavali
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Patent number: 6169085Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: October 4, 1999Date of Patent: January 2, 2001Assignee: G. D. Searle & CompanyInventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, Joseph J. McDonald
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Patent number: 6159505Abstract: Compositions for the treatment and prevention of migraine or stress headaches wherein there is supplied a combination of potassium, magnesium and pyridoxine optionally in association with other nutrients and/or simple analgesics.Type: GrantFiled: January 21, 1998Date of Patent: December 12, 2000Inventor: Edwina M. Piper
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Patent number: 6153585Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: July 15, 1999Date of Patent: November 28, 2000Assignee: Tularik Inc.Inventors: Steven M. Rubenstein, Juan C. Jaen
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Patent number: 6149915Abstract: Diabetic nephropathy and microalbuminuria are treated with the herb Salviae Miltiorrhizae Radix. In one embodiment, the method includes boiling the herb to form an aqueous extract. The aqueous extract is administered to the diabetic individual to treat diabetic nephropathy or to an individual exhibiting microalbuminuria. Alternatively the method can include administering a salt of lithospermic acid extracted from the herb. The method can include determining the level of protein in urine before, during and/or after administering the aqueous extract or a salt of lithospermic acid.Type: GrantFiled: September 29, 1999Date of Patent: November 21, 2000Assignee: Shiva Biomedical, LLCInventors: Hai-Ri Li, Hyun Chul Lee, Mankil Jung, Sudhir V. Shah
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Patent number: 6143788Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: January 21, 1998Date of Patent: November 7, 2000Assignee: G.D. Searle & Co.Inventors: Daniel P. Getman, Gary A. Decrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Belekudru Devadas, Srinivasan RAJ Nagarajan, David L. Brown, Joseph J. McDonald
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Patent number: 6143787Abstract: The present invention relates to a pharmaceutical composition comprising, as active principle, a compound of formula: ##STR1## in which the groups A and B are chosen, independently of each other, from: a mono-, bi- or tricyclic aryl group having from 6 to 14 carbon atoms;a heteroaromatic group chosen from pyridyl, pyrimidyl, pyrrolyl, furyl and thienyl groups;an alkyl group having from 1 to 14 carbon atoms;a cycloalkyl group having from 5 to 8 carbon atoms;a saturated heterocyclic group chosen from tetrahydrofuryl, tetrahydropyranyl, piperidyl and pyrrolidinyl groups;to its solvate or to a salt of this acid with a pharmaceutically acceptable base.Figures: none.Type: GrantFiled: February 2, 1999Date of Patent: November 7, 2000Assignee: Merck Patent Gesellschaft MitInventors: Gerard Moinet, Liliane Doare, Micheline Kergoat, Philippe Maizeray, Didier Mesangeau