Ketone In Z Radical Patents (Class 514/545)
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Publication number: 20090202464Abstract: A method of providing a fragrant odour to an application, comprising the addition thereto of at least one compound of the formula (I) wherein X and Y are independently selected from the group consisting of —CR1R2R3, —NR4R5 and —OR6, wherein R1 to R5 are selected from H and essentially hydrocarbon moieties that optionally comprise at least one oxygen, nitrogen or silicon atom, and R6 is selected from essentially hydrocarbon moieties that optionally comprise at least one oxygen, nitrogen or silicon atom; and A is an essentially hydrocarbon moiety that optionally comprises at least one oxygen, sulphur, nitrogen or silicon atom, with the proviso that the compound A-CHO is a fragrant aldehyde. The use of these compounds in laundry, household and personal care products confers a long-lasting freshness.Type: ApplicationFiled: June 13, 2007Publication date: August 13, 2009Inventor: Felix Flachsmann
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Patent number: 7572831Abstract: The present invention provides an MMP-inhibitory composition comprising chalcone or its derivatives. They inhibit the MMPs in collagenase subfamily as well as those in gelatinase subfamily. The MMP inhibitory activity of chalcone derivatives was similar to or greater than that of parent compound, chalcone. Chalcone or its derivatives of the present invention inhibit activity of matrix metalloproteinase, so that it can be applied to treat and prevent diseases related to matrix metalloproteinase.Type: GrantFiled: May 3, 2004Date of Patent: August 11, 2009Assignee: Angiolab, Inc.Inventors: Min-Young Kim, Byung-Young Park, Kyoung-Mi Kim, Nack-Do Sung, Pyung-Keun Myung
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Publication number: 20090170939Abstract: This invention relates to the use of fenofibrate or a derivative thereof for the manufacture of a medicament for the prevention and/or treatment of retinopathy.Type: ApplicationFiled: November 10, 2006Publication date: July 2, 2009Applicant: Laboratoires Fournier S.A.Inventors: Jean-Claude Ansquer, Anthony Keech
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Patent number: 7488757Abstract: An alcohol based hand surgical scrub, which includes cationic anti-microbial agent preservatives, cationic polymer film-forming agents and a skin emollient, and provides a long term residual, anti-microbial “invisible glove” on the skin. The composition provides an immediate reduction in bacterial microbes. The polymer system creates an invisible film on the skin following solvent evaporation. This invisible film provides a lasting anti-microbial barrier on the skin which acts to prevent microbial growth.Type: GrantFiled: March 24, 2004Date of Patent: February 10, 2009Assignee: Becton, Dickinson and CompanyInventors: Minh Quang Hoang, Donald Edward Hunt
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Publication number: 20090036371Abstract: The present invention provides compositions and methods for treating glaucoma, methods for diagnosing glaucoma, and methods for identifying agents which may be useful in the treatment of glaucoma. More specifically, the present invention describes the use of agents that modulate the expression of serum amyloid A.Type: ApplicationFiled: February 27, 2008Publication date: February 5, 2009Applicant: ALCON, INC.Inventors: Abbot F. CLARK, Wan-Heng WANG, Loretta MCNATT
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Publication number: 20080306151Abstract: The present application describes deuterium-enriched fenofibrate, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: June 11, 2007Publication date: December 11, 2008Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20080253985Abstract: The invention provides methods and compositions for treating hyperlipidemia and disorders associated with hyperlipidemia in a mammal. Compositions useful in the practice of the invention include a microsomal triglyceride transport protein inhibitor (“MTPI”) and at least two other cholesterol lowering drugs selected from the group consisting of a cholesterol absorption inhibitor (“CAI”), a HMG-CoA reductase inhibitor, a bile acid sequestrant, a fibric acid derivative, niacin, and squalene synthetase inhibitor.Type: ApplicationFiled: October 18, 2006Publication date: October 16, 2008Inventor: Gerald L. Wisler
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Publication number: 20080248070Abstract: A pharmaceutical composition including therapeutically effective amounts of at least one HMG-CoA reductase inhibitor present as a dyhydroxyacid salt and at least one additional therapeutic agent.Type: ApplicationFiled: June 20, 2008Publication date: October 9, 2008Inventor: Josefino B. Tunac
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Patent number: 7365224Abstract: A pharmaceutical composition comprising a compound of formula (1) in polymorphic crystalline Form A: together with a pharmaceutically acceptable carrier or excipient, wherein the compound of formula (1) is present in polymorphic Form A (see, e.g., FIG. 6) substantially free of other polymorphic forms.Type: GrantFiled: December 29, 2005Date of Patent: April 29, 2008Assignee: Medicinova, Inc.Inventors: Kenneth Walter Locke, David Gregory Roe
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Patent number: 7314888Abstract: A compound or a salt thereof having the atom corresponding to N3 and the two or more atoms selected from N1, N2, N4 and N5, said atoms constitute the pharmacophore represented by the following formula: and inhibits the activity of transcription factor AP-1 and is useful as an agent for preventing and treating the diseases into which over expression of AP-1 participates and as an AP-1 inhibitor.Type: GrantFiled: November 5, 1999Date of Patent: January 1, 2008Assignee: Toyama Chemical Co., Ltd.Inventors: Hisaaki Chaki, Tadakazu Takakura, Keiichi Tsuchida, Hironori Kotsubo, Yukihiko Aikawa, Shuichi Hirono, Shunichi Shiozawa
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Patent number: 7169770Abstract: The present invention relates to supplementing the diets to sows during the periods of gestation, lactation, and breeding by feeding L-carnitine and chromium. The supplementation enhances pork productivity by increasing the number of pigs born alive in the subsequent reproductive cycle. Sow diets of this invention include L-carnitine and L-carnitine salts and trivalent chromium salts, such as chromium picolinate and chromium nicotinate. L-Carnitine is generally added to the swine feed formulation in the amount of from about 20 to about 1500 ppm, and the trivalent chromium salt is generally added to the swine feed formulation in the amount of from about 20 ppb to about 1000 ppb. The invention also relates to supplemented sow diets and feed supplement formulation.Type: GrantFiled: March 1, 2002Date of Patent: January 30, 2007Assignees: Lonza Ltd., Kansas State University Research FoundationInventors: Daryl Real, Michael D. Tokach, Steve S. Dritz, Jim L. Nelssen, Robert D. Goodband, Jason Woodworth, Kevin Q. Owen
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Patent number: 7074826Abstract: The present invention concerns esters of R-enantiomers of a non-steroidal anti-inflammatory drug, which is substantially free from the S-enantiomer. The compounds of the invention may be used in treating a disease or illness in a mammal. To this end, a composition comprising a compound mentioned above, or a pharmaceutically acceptable salt thereof where salt formation occurs, is administered to the mammal in an amount sufficient to elicit a chemopreventative effect or a chemoprotective effect or a therapeutic effect or a prophylactic effect.Type: GrantFiled: October 3, 2003Date of Patent: July 11, 2006Assignee: Encore Pharmaceuticals, Inc.Inventors: William J. Wechter, Elaine Benaksas Schwartz
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Patent number: 7064146Abstract: A pharmaceutical composition, comprising: a compound of formula (1) in polymorphic crystalline Form A: together with a pharmaceutically acceptable carrier or excipient, wherein the compound of formula (1) is present in polymorphic Form A (see, e.g., FIG. 6) substantially free of other polymorphic forms.Type: GrantFiled: June 24, 2003Date of Patent: June 20, 2006Assignee: MediciNova, Inc.Inventors: Kenneth Walter Locke, David Gregory Roe
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Patent number: 6984389Abstract: The present invention relates to methods of improving a treatment outcome comprising administering a heat shock protein (HSP) preparation or an ?-2-macroglobulin (?2M) preparation with a non-vaccine treatment modality. In particular, an HSP preparation or an ?2M preparation is administered in conjunction with a non-vaccine treatment modality for the treatment of cancer or infectious diseases. In the practice of the invention, a preparation comprising HSPs such as but not limited to, hsp70, hsp90 and gp96 alone or in combination with each other, noncovalently or covalently bound to antigenic molecules or ?2M, noncovalently or covalently bound to antigenic molecules is administered in conjunction with a non-vaccine treatment modality.Type: GrantFiled: December 16, 2002Date of Patent: January 10, 2006Assignee: University of Connecticut Health CenterInventor: Zihai Li
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Patent number: 6887898Abstract: The invention provides methods for treating beta-Amyloid protein-induced disease, pharmaceutical compositions and compounds useful for the same, and the use of these compounds for the manufacture of a medicament for treating the same. More particularly, the invention relates to the use of natural product compounds isolated from turmeric, gingko biloba, and ginger, and synthetic chemical analogues thereof, for the treatment of a beta-Amyloid protein-induced disease.Type: GrantFiled: October 23, 2000Date of Patent: May 3, 2005Inventor: Darrick S. H. L. Kim
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Patent number: 6855341Abstract: Disclosed are anti-viral compositions containing at least one zinc compound and at least one phenolic antioxidant (and optionally other ingredients), and a pharmaceutical carrier. Also disclosed are methods of treating lesionous symptoms of a viral infection involving applying an effective amount of the anti-viral composition to the lesions.Type: GrantFiled: November 4, 2002Date of Patent: February 15, 2005Inventor: Jeffrey B. Smith
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Patent number: 6838083Abstract: The present invention provides a process for the preparation of antimicrobial compound ?-keto aliphatic acid ester, a novel, aliphatic, fatty acid derivative from Bacillus sp. IICT-001.Type: GrantFiled: March 18, 2002Date of Patent: January 4, 2005Assignee: Council of Scientific and Industrial ResearchInventors: Annapurna Jetty, Dattatray M. Akkewar, Kondapuram Vijaya Raghavan
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Patent number: 6838268Abstract: The present invention provides a process for the preparation of antimicrobial compound ?-keto aliphatic acid ester, a novel, aliphatic, fatty acid derivative from Bacillus sp. IICT-001.Type: GrantFiled: July 24, 2003Date of Patent: January 4, 2005Assignee: Council of Scientific and Industrial ResearchInventors: Annapurna Jetty, Dattatray M. Akkewar, Kondapuram Vijaya Raghavan
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Publication number: 20040209952Abstract: The present invention provides an MMP-inhibitory composition comprising chalcone or its derivatives. They inhibit the MMPs in collagenase subfamily as well as those in gelatinase subfamily. The MMP inhibitory activity of chalcone derivatives was similar to or greater than that of parent compound, chalcone. Chalcone or its derivatives of the present invention inhibit activity of matrix metalloproteinase, so that it can be applied to treat and prevent diseases related to matrix metalloproteinase.Type: ApplicationFiled: May 3, 2004Publication date: October 21, 2004Inventors: Min-Young Kim, Byung-Young Park, Kyoung-Mi Kim, Nack-Do Sung, Pyung-Keun Myung
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Patent number: 6777442Abstract: The present invention relates to compounds of the general formula (I) in which X represents O, S, SO, SO2, CH2, CHF, CF2 or NR8, and Z represents a group of the formula in which A represents O or S, the subscript “a” is 0 or 1, group D represents a straight-chain (C1-C4)-alkylene group, and R36 represents OR37 or NR38R39. It also relates to processes for preparation of such compounds and to their use in medicaments for the treatment of depression, goiter, cancer of the thyroid gland, arteriosclerosis, hypercholesterolaemia, dyslipidaemia, obesity, cardiac insufficiency, pulmonary emphysema, pain, migraine, Alzheimer's disease, osteoporosis, cardiac arrhythmias, hypothyroidism, skin disorders or diabetes.Type: GrantFiled: February 26, 2002Date of Patent: August 17, 2004Assignee: Bayer AktiengesellschaftInventors: Helmut Haning, Michael Woltering, Gunter Schmidt, Christiane Faeste, Hilmar Bischoff, Axel Kretschmer, Verena Vöhringer, Peter Ellinghaus
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Publication number: 20040147597Abstract: The present invention relates to compounds, compositions and methods for the prevention or treatment of mycobacterium infections. The compounds are naturally occurring and synthetic biflavonoids, flavonoids, chalcones and chalcone like compounds. The compounds were screened for anti-mycobacterium activity. Of the compounds showing anti-mycobacterium activity, eight were identified as particularly potent, exhibiting greater than 90% inhibition of the growth of Mtb at a concentration of 12.5 Πg/mL. The actual minimum inhibitory concentrations (MIC), defined as the lowest concentration inhibiting 99% of the inoculum, for the preferred compounds ranged from 6.8 to 48.3 ΠM.Type: ApplicationFiled: January 12, 2004Publication date: July 29, 2004Applicant: Advanced Life Sciences, Inc.Inventor: Yuh-Meei Lin
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Publication number: 20040097585Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.Type: ApplicationFiled: October 14, 2003Publication date: May 20, 2004Inventor: Shalini Sharma
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Patent number: 6723750Abstract: Method for treating dermal pre-melanoma conditions which include administering an effective amount of a photosensitive agent to a dermal pre-melanoma cell and activating the photosensitive agent, thereby treating a dermal pre-melanoma condition.Type: GrantFiled: March 15, 2002Date of Patent: April 20, 2004Assignee: Allergan, Inc.Inventor: Martin A. Voet
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Patent number: 6649657Abstract: Prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.Type: GrantFiled: September 26, 2002Date of Patent: November 18, 2003Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Hua Z. Ke, Bruce A. Lefker, Robert L. Rosati, David D. Thompson
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Nitrosated and nitrosylated nonsteroidal antiinflammatory compounds, compositions and methods of use
Patent number: 6593347Abstract: The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.Type: GrantFiled: August 27, 2001Date of Patent: July 15, 2003Assignee: NitroMed, Inc.Inventors: Upul K. Bandarage, Qing Dong, Xinqin Fang, David S. Garvey, Gregory J. Mercer, Stewart K. Richardson, Joseph D. Schroeder, Tiansheng Wang -
Publication number: 20030082215Abstract: The present invention relates to a pharmaceutical composition for the oral administration of fenofibrate in the form of a preconcentrate capable of forming an oil-in-water microemulsion spontaneously on contact with an aqueous medium, of the type comprising:Type: ApplicationFiled: June 19, 2002Publication date: May 1, 2003Inventors: Josiane Lemut, Pascale Blouquin, Philippe Reginault
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Publication number: 20020099091Abstract: This invention relates to novel compounds of the formula: 1Type: ApplicationFiled: March 22, 2002Publication date: July 25, 2002Inventors: Timothy A. Ayers, Paul W. Brown
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Patent number: 6384079Abstract: Uses of topical compositions comprising a 2-hydroxycarboxylic acid or related compound to alleviate or improve signs of skin, nail and hair changes associated with intrinsic or extrinsic aging are disclosed. 2-Hydroxycarboxylic acids and their related compounds include, for example, 2-hydroxyethanoic acid, hydroxypropanoic acid, 2-methyl 2-hydroxypropanoic acid, 2-phenyl 2-hydroxyethanoic acid, 2-phenyl 2-methyl 2-hydroxyethanoic acid, 2-phenyl 3-hydroxypropanoic acid, 2,2-diphenyl 2-hydroxyethanoic acid, 2-hydroxybutane-1,4-dioic acid, 2,3-hihydroxybutane-1,4-dioic acid, 2-carboxy 2-hydroxypentane-1,5-dioic acid, 2-ketopropanoic acid, methyl 2-ketopropanoate, ethyl 2-ketopropanoate, and gluconolactone.Type: GrantFiled: January 4, 1999Date of Patent: May 7, 2002Assignee: TriStrata Technology, IncorporatedInventors: Ruey J. Yu, Eugene J. Van Scott
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Patent number: 6323211Abstract: The present invention describes methods for preventing and treating sexual dysfunctions in patients by orally administering at least one &agr;-adrenergic receptor antagonist and at least one compound that elevates endogenous nitric oxide or endothelium-derived relaxing factor in vivo. The present invention also describes orally administrable compositions comprising at least one &agr;-adrenergic receptor antagonist and at least one compound that elevates endogenous nitric oxide or endothelium-derived relaxing factor in vivo. In the present invention, the &agr;-adrenergic receptor antagonist is preferably yohimbine or phentolamine, and the compound that elevates endogenous nitric oxide or endothelium-derived relaxing factor in vivo is preferably L-arginine.Type: GrantFiled: April 2, 1999Date of Patent: November 27, 2001Assignee: NitroMed, Inc.Inventors: David S. Garvey, Joseph D. Schroeder, Inigo Saenz de Tejada
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Patent number: 6307089Abstract: Biphenyl butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells.Type: GrantFiled: December 14, 2000Date of Patent: October 23, 2001Assignee: Warner-Lambert CompanyInventors: Claude Forsey Purchase, Jr., Bruce David Roth, Gerald Paul Schielke, Lary Craswell Walker, Andrew David White
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Nitrosated and nitrosylated nonsteroidal antiinflammatory compounds, compositions and methods of use
Patent number: 6297260Abstract: The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.Type: GrantFiled: October 29, 1999Date of Patent: October 2, 2001Assignee: NitroMed, Inc.Inventors: Upul K. Bandarage, Qing Dong, Xinqin Fang, David S. Garvey, Gregory J. Mercer, Stewart K. Richardson, Joseph D. Schroeder, Tiansheng Wang -
Patent number: 6215016Abstract: The present invention relates to ketone derivatives represented by the following formula and medical agents containing the ketone derivatives or pharmacologically acceptable salts thereof as an active ingredient, and in particular, relates to a hematopoietic agent; it is shown that the present invention increases blood cells, such as platelets, white blood cells, and red blood cells, and is effective in preventing and treating cytopenia caused by cancer chemotherapy, radiation therapy, and the like.Type: GrantFiled: October 19, 1999Date of Patent: April 10, 2001Assignee: Toray Industries, Inc.Inventors: Hideki Kawai, Kiyoshi Okano, Yasumoto Adachi, Tsuyoshi Matsumoto, Yuji Sugawara, Youhei Miyamoto
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Patent number: 6166082Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula(T).sub.x A--B--D--E--Gwherein A and B are aryl or heteroaryl rings; each T is a substituent group; x is 0, 1, or 2; the group D represents ##STR1## the group E represents a three carbon chain bearing one to three substituent groups which are independent or are involved in ring formation, possible structures being shown in the text and claims; and the group G represents --M, ##STR2## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12 ; andR.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids, and include pharmaceutically acceptable salts thereof.Type: GrantFiled: April 9, 1998Date of Patent: December 26, 2000Assignee: Bayer CorporationInventors: Harold Clinton Eugene Kluender, Guenter Hans Heinz Herbert Benz, David Ross Brittelli, William Harrison Bullock, Kerry Jeanne Combs, Brian Richard Dixon, Stephan Schneider, Jill Elizabeth Wood, Michael Christopher VanZandt, Donald John Wolanin, Scott M. Wilhelm
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Patent number: 6166074Abstract: Pharmaceutical compositions which are useful for the treatment of cancer or illnesses which arise due to an abnormally elevated cell proliferation comprise acyl derivatives of aromatic aldehydes, especially arylidene diesters and .alpha.-alkoxyarylidene esters of general formula (I).Type: GrantFiled: October 4, 1996Date of Patent: December 26, 2000Assignee: Norsk Hydro A.S.Inventors: Erik Olai Pettersen, Rolf Olaf Larsen, John Michael Dornish, Bernt B.o slashed.rretzen, Reidar Oftebro, Thomas Ramdahl, Vidar Moen
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Patent number: 6121321Abstract: Substituted methoxy benzylidene indenyl compounds are useful in the treatment of precancerous lesions and neoplasms.Type: GrantFiled: June 13, 1996Date of Patent: September 19, 2000Assignees: Cell Pathways, Inc., University of ArizonaInventors: Gerhard Sperl, Paul Gross, Klaus Brendel, Gary A. Piazza, Rifat Pamukcu
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Patent number: 6110955Abstract: This invention relates to compositions for and methods of treating, preventing or ameliorating cancer and other proliferative diseases as well as methods of inducing wound healing, treating cutaneous ulcers, treating gastrointestinal disorders, treating blood disorders such as anemias, immunomodulation, enhancing recombinant gene expression, treating insulin-dependent patients, treating cystic fibrosis patients, inhibiting telomerase activity, treating virus-associated tumors, especially EBV-associated tumors, modulating gene expression and particularly augmenting expression of a tumor suppressor gene, inducing tolerance to an antigen and treating, ameliorating or preventing protozoan infection. The methods of the invention use metabolically stabilized oxyalkylene esters.Type: GrantFiled: March 11, 1997Date of Patent: August 29, 2000Assignee: Beacon Laboratories, Inc.Inventors: Abraham Nudelman, Ada Rephaeli, Edward Neiss, Bernard Loev
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Patent number: 6103925Abstract: The present invention relates to dimethyl-substituted cyclohexanediene derivatives, to a process for their preparation, to their use as pharmaceuticals and to corresponding pharmaceuticals.Type: GrantFiled: September 22, 1998Date of Patent: August 15, 2000Assignee: Bayer AktiengesellschaftInventors: Klaus Urbahns, Frank Mauler
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Patent number: 6100266Abstract: For the treatment of cancer, inflammation, and other conditions associated with matrix metalloproteinases or that are mediated by TNF.alpha. or enzymes involved in the shedding of L-selectin, CD23, the TNF receptors, IL-1 receptors, or IL-6 receptors, disclosed are compounds of the general formulaB--X--(CH.sub.2).sub.m --(CR.sup.1 R.sup.2).sub.n --W--COY.Type: GrantFiled: January 29, 1999Date of Patent: August 8, 2000Assignee: Darwin Discovery LimitedInventors: John Gary Montana, Andrew Douglas Baxter, David Alan Owen
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Patent number: 6086789Abstract: A pyruvate compound suitable for cosmetically or dermatologically administering to the skin and for use in treating diabetic ketosis or other medical treatments. The compound includes a pyruvate selected from the group of pyruvate thioester, dihydroxyacetonepyruvate, and an ester of pyruvate and a sugar or a polyol.Type: GrantFiled: May 12, 1998Date of Patent: July 11, 2000Assignee: Case Western Reserve UniversityInventors: Henri Brunengraber, Catherine Bomont, France David, Peter T. Hallowell, Kevin D. Cooper, Takhar Kasoumov
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Patent number: 6063815Abstract: This invention provides compounds of Formula I having the structure ##STR1## wherein Y is ##STR2## R.sup.1 and R.sup.2 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, perfluoroalkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, thienyl, furyl, phenyl or phenyl mono-, di- or tri-substituted with trifluoromethyl, chloro, methoxy, or trifluoromethoxy;R.sup.3 and R.sup.4 are each, independently, hydrogen, carboxyl, hydroxyl, hydoxyalkyl of 1-6 carbon atoms, hydroxyalkanoyl of 1-6 carbon atoms, aryloxycarbonyl of 7-13 carbon atoms, alkoxycarbonyl of 2-7 carbon atoms, perfluoroalkoxycarbonyl of 2-7 carbon atoms, alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, aminoalkyl of 1-6 carbon atoms, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl group, tetrazolyl, mercapto, alkylsulfanyl of 1-6 carbon atoms, nitrile, nitro, amino, --NHSO.sub.2 CF.sub.Type: GrantFiled: May 10, 1999Date of Patent: May 16, 2000Assignee: American Home Products CorporationInventor: Paul J. Dollings
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Patent number: 6048896Abstract: 4-Phenyl-4-oxo-butenoic acid derivatives for use in the treatment of the human or animal body by therapy; particularly as kynurenine-3-hydroxylase inhibitors, in the prevention and/or treatment of a neurodegenerative disease wherein the inhibition of such an enzyme is needed. The present invention further comprises a selected class of the above mentioned 4-phenyl-4-oxo-butenoic acid derivatives, their pharmaceutically acceptable salts, a process for their preparation and pharmaceutical compositions containing them.Type: GrantFiled: May 4, 1998Date of Patent: April 11, 2000Assignee: Pharmacia & Upjohn S.p.A.Inventors: Antonio Giordani, Paolo Pevarello, Carmela Speciale, Mario Varasi
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Patent number: 5990172Abstract: This invention provides peptidomimetics which bind to T4 or CD4 cell receptors and are useful in inhibiting viral infectivity by viruses which bind to T4 cell receptors. More specifically, peptidomimetics of this invention can alleviate symptoms of AIDS by inhibiting binding of HIV, the virus associated with AIDS, to receptor sites in human cells susceptible to HIV infection. These peptidomimetics, in particular, inhibit binding of HIV to cells of brain membrane and the immune system. They also display substantially longer half-lives in vivo than peptide T. The compounds of this invention which bind to T4 or CD4 receptors and thereby inhibit binding of HIV, alone or in combination with one another, can be used to alleviate AIDS symptoms and ameliorate symptoms of HIV infection, especially neuronal dementias and Kaposi's sarcoma. The compounds of this invention, alone or in combination, can further be used to prevent development of AIDS in persons who might become exposed to HIV.Type: GrantFiled: February 27, 1997Date of Patent: November 23, 1999Assignee: Innapharma, Inc.Inventors: Matthew R. Pincus, Andrew S. Kende, Joseph J. Hlavka, Henry B. Abajian
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Patent number: 5968482Abstract: The invention relates to the use of .alpha.-hydroxyketoalkyl derivatives as light protection filters for cosmetic or pharmaceutical products, the .alpha.-hydroxyketoalkyl group being linked, if appropriate via a spacer, to a chromophoric group which has an absorption maximum in a wavelength range of between 280 and 400 nm and has a conjugated .pi.-electron system of at least 8 .pi.-electrons, and to new .alpha.-hydroxyalkyl derivatives, processes for their preparation and pharmaceutical and cosmetic formulations comprising these derivatives as light protection substances.Type: GrantFiled: September 20, 1996Date of Patent: October 19, 1999Assignee: Merck Patent Gesellschaft MIT Beschrankter HaftungInventors: Roland Martin, Ingeborg Stein, Ulrich Heywang, Michael Schwarz, Thekla Kurz
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Patent number: 5965592Abstract: Compounds of the formula ##STR1## and their salts, in which R.sub.1, is a C.sub.1 -C.sub.7 aliphatic hydrocarbon radical; X.sub.1 is --CO; X.sub.2 is a divalent aliphatic hydrocarbon radical which comprises an ethyl group and an alkylene of 2 to 6 carbon atoms; R.sub.2 is hydroxy, carboxy or alkoxycarbonyl in which alkoxy is from 1 to 7 carbon atoms; X.sub.3 is a divalent aliphatic hydrocarbon; R.sub.3 is carboxyl or 5-tetrazolyl; and the rings A and B independently of one another are otherwise unsubstituted; can be prepared in a known manner and may be used as active ingredients for medicaments.Type: GrantFiled: July 29, 1998Date of Patent: October 12, 1999Assignee: Novartis CorporationInventors: Peter Buhlmayer, Franz Ostermayer, Tibur Schmidlin
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Patent number: 5892098Abstract: This invention relates to derivatives of 3,3-(disubstituted)cyclohexan-1-one monomers and related compounds which are useful for treating allergic and inflammatory diseases.Type: GrantFiled: April 15, 1997Date of Patent: April 6, 1999Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Joseph M. Karpinski, M. Dominic Ryan, Paul E. Bender
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Patent number: 5886022Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each T is a substituent g roup; x is 0, 1, or 2; the group D represents ##STR2## the subscript "e" is 2 or 3; the group R.sup.14 represents a variety of possible substituent groups of the cycloalkyl ring between D and G; the subscript "k" is 0-2; and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12 ; and R.sup.13 represents any of the side chains of the 19 noncyclic occurring amino acids.Type: GrantFiled: May 30, 1997Date of Patent: March 23, 1999Assignee: Bayer CorporationInventors: Harold Clinton Eugene Kluender, William Harrison Bullock, Brian Richard Dixon, Stephan Schneider, Michael Christopher VanZandt, Scott McClelland Wilhelm, Donald John Wolanin
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Patent number: 5886043Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each T is a substituent group; x is 0, 1, or 2; the group D represents ##STR2## the group R6 represents variety of possible substituent groups on the carbon chain between D and G, and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12, and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.Type: GrantFiled: May 30, 1997Date of Patent: March 23, 1999Assignee: Bayer CorporationInventors: Harold Clinton Eugene Kluender, Brian Richard Dixon, Michael Christopher VanZandt, Scott McClelland Wilhelm, Donald John Wolanin, William Harrison Bullock
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Patent number: 5883125Abstract: Compounds with fungicidal and insecticidal properties having formula I ##STR1## wherein A is N or CH; V is O or NH; m and n are integers 0 and 1 provided that m+n is 1;X is independently selected from hydrogen, halo, (C.sub.1 -C.sub.4)alkyl, and (C.sub.1 -C.sub.4) alkoxy;R is independently selected from, (C.sub.1 -C.sub.12)alkyl, halo(C.sub.1 -C.sub.12)alkyl, (C.sub.2 -C.sub.8) alkenyl, (C.sub.2 -C.sub.8)alkynyl, (C.sub.1 -C.sub.12)alkoxy(C.sub.1 -C.sub.12)alkyl, (C.sub.3 -C.sub.7) cycloalkyl, (C.sub.3 -C.sub.7)cycloalkyl(C.sub.1 -C.sub.4)alkyl, aryl, aralkyl, and heterocyclic moieties;R is independently selected from (C.sub.1 -C.sub.12)alkyl, halo(C.sub.1 -C.sub.12)alkyl, (C.sub.2 -C.sub.8) alkenyl, (C.sub.2 -C.sub.8)alkynyl, (C.sub.1 -C.sub.12)alkoxy(C.sub.1 -C.sub.12)alkyl, (C.sub.3 -C.sub.7) cycloalkyl, (C.sub.3 -C.sub.7)cycloalkyl(C.sub.1 -C.sub.4)alkyl, aryl, aralkyl, and heterocyclic;R.sub.1 and R.sub.2 are independently selected from hydrogen, (C.sub.1 -C.sub.6)alkyl, halo(C.sub.1 -C.sub.Type: GrantFiled: June 2, 1997Date of Patent: March 16, 1999Assignee: Rohm and Haas CompanyInventors: Ronald Ross, Ted Tsutomu Fujimoto, Steven Howard Shaber
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Patent number: 5849793Abstract: There is disclosed a structural genus of compounds, defined according to coordinates in three-dimensional space, that binds amino moieties on neighboring lysine residues in a tyrosine residue 29 pocket of the matrix protein component of the HIV preintegration complex (PIC), thereby preventing the PIC from binding to karyopherin .alpha. and preventing nuclear importation and integration of the HIV viral genome into the host cell DNA, thereby preventing viral infection.Type: GrantFiled: August 15, 1997Date of Patent: December 15, 1998Assignee: The Picower Institute for Medical ResearchInventors: Senliang Pan, Michael Bukrinsky, Omar K. Haffar
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Patent number: 5792786Abstract: The present invention provides therapeutic conjugates which comprise a therapeutic compound bound to one to three acyl groups derived from fatty acids. The therapeutic compounds are preferably non.about.steroidal anti.about.inflammatory agents which include a carboxylic acid group. The compounds involve the use of tromethamine or ethanolamine derivative to link the acyl groups derived from fatty acids to the therapeutic compounds.Type: GrantFiled: April 12, 1996Date of Patent: August 11, 1998Assignee: Commonwealth Scientific and Industrial Research OrganisationInventors: Robert George Whittaker, Veronika Judith Bender, Wayne Gerrard Reilly