Aldehyde Or Ketone Group In Acid Moiety Patents (Class 560/51)
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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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Publication number: 20020087025Abstract: An improved method is described for making 9-deoxy-PGF1-type compounds. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds.Type: ApplicationFiled: February 15, 2002Publication date: July 4, 2002Applicant: UNITED THERAPEUTICS CORPORATIONInventors: Robert M. Moriarty, Raju Penmasta, Liang Guo, Munagala S. Rao, James P. Staszewski
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Patent number: 6380249Abstract: Certain six-membered aromatic and heteroaromatic-dioxobutyric acid derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: June 1, 1999Date of Patent: April 30, 2002Assignees: Merck & Co., Inc., Tularik Inc.Inventors: Steven D. Young, Melissa Egbertson, Linda S. Payne, John S. Wai, Thorsten E. Fisher, James P. Guare, Jr., Mark W. Embrey, Lekhanh Tran, Linghang Zhuang, Joseph P. Vacca, H. Marie Langford, Jeffrey Melamed, Juan C. Jaen, David L. Clark, Julio C. Medina
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Patent number: 6376546Abstract: Compounds represented by general formula I or salts thereof, wherein n is an integer of 2 or 3; R represents a straight-chain or branched saturated alkyl group having 4 or 4 carbon atoms, a cyclopentyl group, a cyclohexyl group or the like, Y represents a hydroxyl or amino group, A represents a hydrogen atom, a hydroxyl, methoxy, nitro group or the like, Q represents a hydrogen atom or a hydroxyl or methoxy group. They can be formulated to give pharmaceutical compositions that are effective as prophylactic or therapeutic agents for allergic diseases associated with IgE production inhibitors or IgE antibodies.Type: GrantFiled: June 8, 2000Date of Patent: April 23, 2002Assignee: Asahi Kasei Kabushiki KaishaInventors: Motoshi Shoda, Hiromichi Itoh
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Patent number: 6369194Abstract: The invention relates to compounds of formula where R is a structural diversity element selected from the group consisting of alkyl, cycloalkyl, aryl, heteroaryl, peptidyl, heteroatom-substituted alkyl, cycloalkyl, and amines; and Nu is a structural diversity element derived from a nucleophile, NuH, selected from the group consisting of amines, amino acids, peptide, water, hydrogen sulfide, alcohols, and thiols. The invention also relates to arrays and combinatorial libraries of such compounds, and to a method of preparing such compounds.Type: GrantFiled: November 9, 1998Date of Patent: April 9, 2002Assignee: Yale UniversityInventor: Harry H. Wasserman
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Publication number: 20020037923Abstract: The invention provides a resorcinol derivative and a method of using the resorcinol derivative to attenuate the growth of a neoplasm.Type: ApplicationFiled: August 13, 2001Publication date: March 28, 2002Inventor: Craig R. Travis
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Patent number: 6346546Abstract: Biaromatic compounds connected by a propynylene or ailenylene bond, corresponding to the formula (I).Type: GrantFiled: May 25, 2000Date of Patent: February 12, 2002Assignee: Galderma Research & DevelopmentInventors: Jean-Michel Bernardon, Simon Trouille
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Publication number: 20020016492Abstract: Processes are disclosed for preparing 3-hydroxymethylcyclopentanone compounds, which are useful as intermediates in the preparation of HIV chemokine CCR-5 receptor antagonists. A process is described in which the compounds are prepared by opening the cyclopropyl ring of a (1-alkoxycarbonyl-2-oxo)-trans-bicyclo[3.1.0]hexane compound by addition of a nucleophile to the cyclopropyl ring, and then decarboxylating the resulting 2-alkoxycarbonyl-3-(Nu-methyl)-cyclopentanone (Nu=the added nucleophilic group) via base solvolysis. Also described is a process for preparing the bicyclo[3.1.0]hexane precursors by the catalyzed cyclopropanation of a suitable alpha-diazo-beta-ketoester. The preparation of the alpha-diazo-beta-ketoesters and precursors thereto are also disclosed.Type: ApplicationFiled: April 20, 2001Publication date: February 7, 2002Inventors: Nobuyoshi Yasuda, Michael Palucki, Joann M. Um, David Alan Conlon, Barry M. Trost
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Patent number: 6329377Abstract: The present invention is directed to novel ketomethylene group-containing inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.Type: GrantFiled: January 18, 2000Date of Patent: December 11, 2001Assignee: Cephalon, Inc.Inventor: Sankar Chatterjee
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Patent number: 6329547Abstract: The present invention provides compounds represented by the following general formula [I] and salts thereof, which are useful as therapeutic agents for glaucoma, wherein R1 is H, lower alkyl or phenyl, and the phenyl can be substituted by lower alkyl, hydroxy, lower alkoxy, halogen, nitro or phenyl; R2 and R3, being the same or different, are H, halogen or lower alkyl; R4 and R5, being the same or different, are H, lower alkyl or carboxyl or ester thereof; and R6 is carboxyl or phosphono or ester thereof.Type: GrantFiled: November 22, 2000Date of Patent: December 11, 2001Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Eiichi Shirasawa, Koji Konomi, Masaki Ichikawa, Hiroshi Suhara
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Patent number: 6313340Abstract: The present invention describes a process for the direct preparation of methyl p-vinylbenzoate from methyl p-formylbenzoate using ketene in the presence of potassium acetate. The chief products obtained from the process are about a five to two ratio of methyl p-vinylbenzoate to p-carbomethoxycinnamic acid. The latter may be thermally decarboxylated, especially in the presence of copper powder, to produce additional quantities of methyl p-vinylbenzoate. Methyl p-vinylbenzoate may further undergo hydrolysis to form p-vinyl benzoic acid. Both methyl p-vinyl benzoate and p-vinyl benzoic acid may be polymerized with ethylenically unsaturated monomers to form useful latex compositions of the present invention.Type: GrantFiled: July 22, 1999Date of Patent: November 6, 2001Assignee: Eastman Chemical CorporationInventors: Philip Conrad Heidt, Matthew Lynn Elliott, Mahendra Kumar Sharma
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Patent number: 6313344Abstract: Compounds of formula (I), wherein either X is CH or N, Y is OR1 and Z is O, or X is N, Y is NHR8 and Z is O, S or S(═O); R1, R2 and R3 are as defined according to the specification; m is 0, 1 or 2; R5 is, for example, halogen, C1-C6alkyl, halo-C1-C6alkyl or C3-C6cycloalkyl; n is 0, 1, 2, 3 or 4; R9 is methyl, fluoromethyl or difluoromethyl; A and R7 are as defined according to the specification; D is O, S, —S(═O) or S(═O)2; G is C1-C6aalkylene; T—R6 is R6, —C(═N—O—A1—R77)—R6; —SiR14(R15)—R6; —C(═O)—R6; —C(R16)═C(R17)—R6, —C≡C—R6 or —D—R6; R6 is C1-C4alkyl or unsubstituted or substituted aryl or heteroaryl; A1 and R77 are as defined above for A and R7; L is U—R18, P(OR)vR11R12, P(S)wR11R12 or N(aryl)R13; v and w are 0 or 1; U—R18 is —C(═O)—C(═O)—R18; —C(OH)—C(OH)—R18; —C(═N&mdType: GrantFiled: May 27, 1998Date of Patent: November 6, 2001Assignee: Bayer AktiengesellschaftInventors: Stephan Trah, Henry Szczepanski, Ottmar Franz Hüter, Roger Graham Hall, Saleem Farooq, Alfons Pascual
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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: 6291702Abstract: The present invention relates to chromotropic nitrone spin trapping agents, methods of making these agents, compositions comprising same, and methods of their use. In particular, azulenyl nitrones of the present invention are effective agents for trapping free radical species and find use as efficient antioxidants in physicochemical and biological systems. Accordingly, the invention also relates to spin adducts formed from the combination of azulenyl nitrones with free radicals. The compounds of the present invention are readily prepared from available starting materials and find further use in assays and in a number of diagnostic, prophylactic and therapeutic applications, including but not limited to the alleviation, modulation and inhibition of the negative effects of carbon-centered or oxygen-centered radical species and other products of oxidation. Moreover, the combination adducts may be colorimetrically detected and, optionally, isolated and characterized to obtain valuable information (e.g.Type: GrantFiled: February 8, 2000Date of Patent: September 18, 2001Assignee: Florida International UniversityInventor: David Alan Becker
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Patent number: 6288265Abstract: A series of phloroglucide derivatives are synthesized, which possess potent antibacterial activities. They include unsymmetrical phloroglucide analogs, phloroglucides attached to cephalosporins at the C-3′ position, and 7-(phloroglucidamido)cephalosporins.Type: GrantFiled: September 20, 1999Date of Patent: September 11, 2001Assignee: National Science CouncilInventors: Jih Ru Hwu, Shwu-Chen Tsay, Gholam H. Hakimelahi, Chun Chieh Lin, Wen Nan Tseng, Ali A. Moshfegh, Abdolmajid Azaripour, Hasan Mottaghian
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Patent number: 6258977Abstract: An alkyl 3-oxoalkanoate, a process for preparation and use for the synthesis of fatty hydroxylated amino acids, fatty amino alcohols and ceramides.Type: GrantFiled: July 6, 1999Date of Patent: July 10, 2001Assignee: L'OrealInventors: Michel Philippe, Bernadette Luppi, Didier Semeria, Claude Mahieu
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Patent number: 6258843Abstract: (4-oxy-3-(aryl)phenyl)pyridine compounds, in free or acid addition salt form, are useful as pharmaceuticals for treatment and prophylaxis of inflammation, particularly inflammatory or obstructive diseases of the airways, e.g. for asthma therapy. Preferred compounds are novel biphenyl pyridines, biphenyl benzamides and biphenyl phenylcarboxy compounds. The compounds are selective inhibitors of PDE 4 isoenzyme activity and also act to down regulate or inhibit TNF-&agr; release.Type: GrantFiled: April 27, 2000Date of Patent: July 10, 2001Assignee: Novartis AGInventor: Paul W. Manley
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Patent number: 6228848Abstract: Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity.Type: GrantFiled: November 22, 1999Date of Patent: May 8, 2001Assignee: Allergan, Inc.Inventors: Elliott S. Klein, Alan T. Johnson, Andrew M. Standeven, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Sunil Nagpal, Vidyasagar Vuligonda, Min Teng, Roshantha A. Chandraratna
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Publication number: 20010000038Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula 1Type: ApplicationFiled: December 1, 2000Publication date: March 15, 2001Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
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Patent number: 6191171Abstract: para-Aminomethylaryl carboxamides of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.Type: GrantFiled: November 13, 1998Date of Patent: February 20, 2001Assignee: Merck & Co., Inc.Inventors: Stephen E. DeLaszlo, William K. Hagmann
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Patent number: 6180816Abstract: The present invention provides compounds which inhibit an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.Type: GrantFiled: April 10, 2000Date of Patent: January 30, 2001Assignee: Eli Lilly and CompanyInventors: Scott C. Mauldin, John E. Munroe
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Patent number: 6175034Abstract: The present invention provides compounds which inhibit an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.Type: GrantFiled: April 10, 2000Date of Patent: January 16, 2001Assignee: Eli Lilly and CompanyInventors: Scott C. Mauldin, John E. Munroe
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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: 6133303Abstract: The present invention provides compounds of Formula (I). The present invention also provides a method of treating cancer and treating or preventing restenosis or atherosclerosis. Also provided by the present invention is a pharmaceutically acceptable composition containing a compound of Formula (I).Type: GrantFiled: August 2, 1999Date of Patent: October 17, 2000Assignee: Warner-Lambert CompanyInventors: Jack Bikker, Ellen Myra Dobrusin, Annette Marian Doherty, Matthew Drowns, James Stanley Kaltenbronn, Juergen Kleinschroth, Dennis Joseph McNamara, John Quin, III, Joseph Thomas Repine, Marcin Stasiak
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Patent number: 6118017Abstract: This invention relates to ketones, alcohols and amines and acids represented by the likes of 3-(3-cyclopentyloxy-4-methoxyphenyl)-3-phenylcyanoclobutan-1-one. They are useful as PDE 4 antngionists.Type: GrantFiled: April 8, 1999Date of Patent: September 12, 2000Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Cornelia J. Forster
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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: 6090168Abstract: The present application relates to a series of novel sulfonic acid metal cation salts of the formula ##STR1## which are useful intermediates to prepare antifolate 5-substituted pyrrolo[2,3-d]pyrimidines. The present invention also relates to a novel process for preparing the sulfonic acid metal cation salts and to a novel process for preparing aldehydes of the formula ##STR2## from the corresponding sulfonic acid metal cation salts.Type: GrantFiled: October 6, 1999Date of Patent: July 18, 2000Assignee: Eli Lilly and CompanyInventors: Douglas Patton Kjell, Brian James Slattery, Charles Jackson Barnett
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Patent number: 6090974Abstract: This invention includes an alkyl 3-oxoalkanoate, and processes for its preparation and use for the synthesis of fatty hydroxylated amino acids, fatty amino alcohols and ceramides.Type: GrantFiled: October 15, 1996Date of Patent: July 18, 2000Assignee: L'Oreal SAInventors: Michel Philippe, Bernadette Luppi, Didier Semeria, Claude Mahieu
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Patent number: 6075154Abstract: A novel phosphine compound usable as a catalyst in various asymmetric synthetic reactions is disclosed. The compound is a 2,2'-bis(diarylphosphino)-6,6'-bis(trifluoromethyl)-1,1'-biphenyl of (1): ##STR1## where R is a phenyl group or a phenyl group substituted by lower alkyl group, lower alkoxy group, halogen atom, or lower haloalkyl group.Type: GrantFiled: July 30, 1998Date of Patent: June 13, 2000Assignee: Takasago International CorporationInventors: Yoshiharu Gonda, Yoji Hori, Akio Yamaguchi, Toshimitsu Hagiwara
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Patent number: 6057474Abstract: Preparation process for .alpha.,.beta.-dicarbonylated compounds of formula (I) ##STR1## in which R.sub.2 =alkyl, phenyl or benzyl being able to be substituted in various ways on the cycle, or carboxylic ester, and R.sub.3 =alkyl or alkoxy or carboxylic ester in which a compound of formula (II) ##STR2## in which R.sub.1 =alkyl, or alkyl .alpha.-ketocarboxylate or carboxylic ester, and R.sub.2 and R.sub.3 have the same meanings as previously is reacted in a nitrile type solvent, with molecular oxygen in the presence of copper.sup.II nitrate or ferric chloride as catalyst, and use for obtaining ethyl .alpha.-ketobutyrate, ethyl phenyl pyruvate, ethyl pyruvate, ethyl phenylglyoxylate, butane-2,3-dione or diethyl mesoxalate.Type: GrantFiled: December 22, 1998Date of Patent: May 2, 2000Assignee: Clariant S.A.Inventors: Jean-Claude Vallejos, Nicolas Capelle, Henri Arzoumanian
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Patent number: 6054457Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc.,R.sup.3 is hydrogen, etc.,R.sup.4 is lower alkoxy, etc.,R.sup.5 is hydrogen, etc.,A is NH, etc.,E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, andY is CH or N,and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.Type: GrantFiled: December 9, 1997Date of Patent: April 25, 2000Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroyuki Setoi, Takehiko Ohkawa, Tatsuya Zenkoh, Hitoshi Sawada, Kentaro Sato, Hirokazu Tanaka
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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: 6046220Abstract: The invention relates to novel propynyl or dienyl biaromatic compounds which have the general formula (I) ##STR1## as well as to the use of these compounds in pharmaceutical compositions intended for use in human or veterinary medicine (dermatological, rheumatic, respiratory, cardiovascular and ophthalmological complaints in particular), or alternatively in cosmetic compositions.Type: GrantFiled: January 26, 1998Date of Patent: April 4, 2000Assignee: Centre International de Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 6020502Abstract: A method for the fluorination of 1,3-diketones and 1,3-ketoesters is disclosed.Type: GrantFiled: February 21, 1997Date of Patent: February 1, 2000Assignee: BNFL Fluorochemicals Ltd.Inventors: Richard D. Chambers, John Hutchinson, Martin P. Greenhall, John S. Moilliet, Julie Thomson
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Patent number: 6017471Abstract: A light-stable colored composition which includes a colorant and a radiation transorber. The colorant, in the presence of the radiation transorber, is adapted, upon exposure of the transorber to specific, narrow bandwidth radiation, to be mutable. The radiation transorber also imparts light-stability to the colorant so that the colorant does not fade when exposed to sunlight or artificial light.Type: GrantFiled: April 23, 1997Date of Patent: January 25, 2000Assignee: Kimberly-Clark Worldwide, Inc.Inventors: John Gavin MacDonald, Ronald Sinclair Nohr
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Patent number: 6008204Abstract: Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity.Type: GrantFiled: December 30, 1998Date of Patent: December 28, 1999Assignee: Allergan Sales, Inc.Inventors: Elliott S. Klein, Alan T. Johnson, Andrew M. Standeven, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Sunil Nagpal, Vidyasagar Vuligonda, Min Teng, Roshantha A. Chandraratna
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Patent number: 6004992Abstract: The present invention relates to novel fluorobutenyl aminocarboxylates of the formula (I)R--CO--O--CH.sub.2 --CH.sub.2 --CX.dbd.CF.sub.2 (I)in whichX represents hydrogen or halogen andR represents one of the groups ##STR1## (b) R.sup.3 --A--CO--NR.sup.4 --CR.sup.5 R.sup.6 -- or ##STR2## in which A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each as defined in the description, to processes for their preparation and to their use for controlling animal pests.Type: GrantFiled: May 22, 1998Date of Patent: December 21, 1999Assignee: Bayer AktiengesellschaftInventors: Udo Kraatz, Wolfram Andersch, Andreas Turberg, Norbert Mencke
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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: 5977400Abstract: A method for the preparation and purification of compounds using a novel support, a tetrabenzo[a,c,g,i]fluorene group (Tbf) comprising reacting a building block (A) containing a Tbf group (Tbf-A), with a second building block (B), to afford an intermediate compound (Tbg-A-B) followed by purifying the intermediate compound by adsorption on a carbon support, removing the intermediate compound from the support with a solvent and repeating the previous reactions using the required number of building blocks to synthesize the compounds followed by removal of the Tbf group to afford the desired compounds.Type: GrantFiled: March 25, 1998Date of Patent: November 2, 1999Assignee: Warner-Lambert CompanyInventors: Sheila Helen DeWitt, Robert Ramage, Alasdair Arthur MacDonald
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Patent number: 5973190Abstract: The present invention provides a process for the preparation of pesticidal fluoroolefin compounds having the structural formula I ##STR1## The present invention also provides intermediate compounds which are utilized in the process of this invention.Type: GrantFiled: June 18, 1998Date of Patent: October 26, 1999Assignee: American Cyanamid CompanyInventors: Brian Lee Buckwalter, Timothy Claude Barden
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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: 5951841Abstract: Salts of aromatic hydroxy compounds are used as brighteners in acidic electroplating baths. Furthermore, acidic electroplating baths for the electrolytic deposition of metallic layers onto shaped articles comprise, as brighteners, at least one novel salt of an aromatic hydroxy compound. Finally, shaped articles are electroplated by a process using the novel acidic electroplating baths.Type: GrantFiled: October 6, 1997Date of Patent: September 14, 1999Assignee: BASF AktiengesellschaftInventors: Thomas Wehlage, Ulrich Schroder, Alfred Oftring
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Patent number: 5952386Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.Type: GrantFiled: September 24, 1997Date of Patent: September 14, 1999Assignee: Sumitomo Chemical Company, LimitedInventors: Sanshiro Matsuo, Taro Hirose, Keiichi Izumi, Masaya Suzuki, Noriyasu Sakamoto, Kazunori Tsushima, Shigeru Saito, Hirotaka Takano
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Patent number: 5945561Abstract: Certain novel substituted (5,6)-dihydroanthracenyl compounds of the general formula ##STR1## wherein A, n, p, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are as defined in the specification exhibit retinoid-like properties and are particularly useful in the prevention of post-surgical adhesions.Type: GrantFiled: April 24, 1998Date of Patent: August 31, 1999Assignee: Bristol-Myers Squibb CompanyInventors: John E. Starrett, Jr., Kenneth M. Tramposch, Xina Nair, Peter R. Reczek, Anna Ericsson, Anne Marinier, Alain Martel, Fred C. Zusi
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Patent number: 5945559Abstract: A novel process for producing 3-oxocarboxylic acid esters, which are useful as intermediates in the synthesis of ceramides to be used as a humectant, biodegradable polymers, drugs, etc., at a high purity and a high yield without requiring any troublesome procedure, is disclosed. The process comprises reacting an acetoacetic ester with a calcium compound, a barium compound or a strontium compound in the presence of an organic solvent at a temperature of 10 to 120.degree. C., further reacting the obtained product with a carboxylic acid chloride to thereby acylate it, and then adding thereto an alcohol in an amount 1 to 5 times by mol as much as the calcium compound, barium compound or strontium compound to thereby deacetylate the same.Type: GrantFiled: May 23, 1997Date of Patent: August 31, 1999Assignee: Takasago International CorporationInventors: Tsukasa Sotoguchi, Yoshifumi Yuasa, Akio Tachikawa, Shunichi Harada
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Patent number: 5910596Abstract: Processes for preparing substituted 3-aryl-5-haloalkyl-pyrazoles and, specifically, for preparing C.sub.1-5 alkyl esters of 5- ?1-(C.sub.1-5 alkyl) -4-halo-5-(C.sub.1-3 haloalkyl) -1H-pyrazole-3-yl!-2,4-dihalo-benzoic acids such as isopropyl 5-?4-bromo-1-methyl-5-(trifluoromethyl)-1H-pyrazole-3-yl!-2-chloro-4-fluor obenzoate, are presented. The described processes include novel approaches for forming phenyl-diketones, forming and alkylating pyrazoles, brominating heterocyclic compounds, oxidizing alkyl-substituted benzene compounds, and esterifying carboxylic acids. These processes may be combined to prepare 3-aryl-5-haloalkyl pyrazoles, or alternatively, used in subcombinations or individually to prepare intermediates or other useful compounds.Type: GrantFiled: October 3, 1997Date of Patent: June 8, 1999Assignee: Monsanto CompanyInventor: Michael K. Mao
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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: 5883263Abstract: Processes for preparing substituted 3-aryl-5-haloalkyl-pyrazoles and, specifically, for preparing C.sub.1-5 alkyl esters of 5-?1-(C.sub.1-5 alkyl)-4-halo-5-(C.sub.1-3 haloalkyl)-1H-pyrazole-3-yl!-2,4-dihalo-benzoic acids such as isopropyl 5-?4-bromo-1-methyl-5-(trifluoromethyl)-1H-pyrazole-3-yl!-2-chloro-4-fluor obenzoate, are presented. The described processes include novel approaches for forming phenyldiketones, forming and alkylating pyrazoles, brominating heterocyclic compounds, oxidizing alkyl-substituted benzene compounds, and esterifying carboxylic acids. These processes may be combined to prepare 3-aryl-5-haloalkyl pyrazoles, or alternatively, used in subcombinations or individually to prepare intermediates or other useful compounds.Type: GrantFiled: October 3, 1997Date of Patent: March 16, 1999Assignee: Monsanto CompanyInventors: Bruce C. Hamper, Michael K. Mao, Wendell Gary Phillips