Plural Rings With Nitrogen Bonded Directly To At Least One Ring Patents (Class 562/457)
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Patent number: 6974595Abstract: New pharmaceutical compositions for oral use containing Diclofenac together with alkali metal bicarbonates in amounts of from 20 to 80 by weight with respect to Diclofenac are described. These compositions are entirely palatable and free from any unpleasant taste or other side effects; in particular, these formulations permit to obtain in human patients higher Cmax of the active principle and shorter Tmax together with a lower coefficient of variation.Type: GrantFiled: March 14, 2000Date of Patent: December 13, 2005Assignee: ProEthic Pharmaceuticals, Inc.Inventors: Alberto Reiner, Giorgio Reiner
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Patent number: 6951943Abstract: A process for the preparation of a class of phenylalanine enamide derivatives is described: wherein: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a linker group selected from —N(R4)— [where R4 is a hydrogen atom or an optionally substituted straight or branched C1-6alkyl group], —CON(R4)—, or —S(O)2N(R4)—; R1 is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; Rx, Ry and Rz which may be the same or different is each an atom or group -L1(Alk1)n(R3)v; and the salts, solvates, hydrates and N-oxides thereof; which comprises reacting a compound of formula (2): wherein: Qa is a group —N(R4)H; and the salts, solvates, hydrates and N-oxides thereof; with a compound Ar1W wherein W is a group selected from X1(wherein X1 is a leaving atom or group), —COX2 (wherein X2 is a halogen atom or a —OH group) or —SO2X3 (in which X3 is a halogen atom).Type: GrantFiled: July 16, 2003Date of Patent: October 4, 2005Assignee: Celltech R & D LimitedInventors: Benjamin Mark Skead, Nicholas David Tyrrell, Stephen Wilfred Jones, Michael Handforth Brookes
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Patent number: 6949575Abstract: The present invention provides compounds of Formula (I) and a method of treating Alzheimer's disease using a compound of Formula (I), wherein: R1 and R2 include alkyl and phenylalkyl; R3 is hydrogen or alkyl; and R4 and R5 include alkyl, alkoxy, carboxyl, alkoxycarbonyl, and nitro. Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of Formula (I) and a method of imaging amyloid deposits using compounds of Formula (I).Type: GrantFiled: April 25, 2001Date of Patent: September 27, 2005Assignee: Pfizer Inc.Inventors: Nancy Sue Barta, Christopher Franklin Bigge
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Patent number: 6936597Abstract: Polymeric prodrugs of the formula: wherein B is selected from the group consisting of OH, leaving groups, residues of amine-containing moieties and a residues of hydroxyl-containing moieties; Y1 is selected from the group consisting of O, S, and NR5; M is NR3, O or S; Ar is a moiety which when included in Formula I forms a multi-substituted aromatic or heteroaromatic hydrocarbon or a multi-substituted heterocyclic group; (m) is zero or a positive integer; R1-3 and R5 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy and C1-6 heteroalkoxy; and R4 is a polymeric residue; as well as methods of making and using the same are disclosed.Type: GrantFiled: March 21, 2002Date of Patent: August 30, 2005Assignee: Enzon, Inc.Inventors: Richard B. Greenwald, Yun H. Choe
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Patent number: 6831102Abstract: New thyroid receptor ligands are provided which have the general formula I: wherein R1 is halogen, trifluoromethyl, substituted or unsubstituted aryl, substituted or unsubstituted C1-6 alkyl, or substituted or unsubstituted C3-7 cycloalkyl; R2 and R3 are each independently hydrogen, halogen, substituted or unsubstituted C1-4 alkyl, or substituted or unsubstituted C3-6 cycloalkyl, wherein at least one of R2 and R3 is other than hydrogen; R4 is a carboxylic acid selected from the group consisting of (CH2)nCOOH, (CH)2COOH, NHCO(CH2)nCOOH, CONH(CH2)nCOOH and NH(CH2)mCOOH; n is an integer from 0 to 4; and m is an integer from 1 to 4. In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.Type: GrantFiled: December 6, 2002Date of Patent: December 14, 2004Assignee: Bristol-Myers Squibb CompanyInventor: Jon J. Hangeland
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Patent number: 6765021Abstract: This invention provides compounds of formula I having the structure wherein: B, D, C, and R1 as defined herein.Type: GrantFiled: August 9, 2002Date of Patent: July 20, 2004Assignee: WyethInventors: John A. Butera, Craig E. Caufield, Russell F. Graceffa, Alexander Greenfield, Eric G. Gundersen, Lisa Marie Havran, Alan H. Katz, Joseph R. Lennox, Scott C. Mayer, Robert E. McDevitt
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Patent number: 6747170Abstract: A thermosensitive recording material has a support and a thermosensitive coloring layer formed thereon containing a leuco dye and a color developer capable of inducing color formation in the leuco dye upon application of heat thereto, with the color developer including at least one compound (A) having in a molecule thereof at least two aromatic ring moieties with specific structures, selected from the group consisting of an aromatic ring moiety having at least one carboxyl group and electron-attracting functional group, an aromatic ring moiety having at least one carboxyl group and electron-donating functional group, and an aromatic ring moiety having at least one carboxyl group, free of the electron-attracting and electron-donating functional groups. An aromatic carboxylic acid compound serving as the above-mentioned compound (A) and the producing method thereof are also disclosed.Type: GrantFiled: May 23, 2002Date of Patent: June 8, 2004Assignee: Ricoh Company, Ltd.Inventors: Kunio Hayakawa, Mitsunobu Morita
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Patent number: 6743373Abstract: Process for the separation of enantiomers comprising at least one free functional group, in which process a reagent based on an enantiopure amino acid is reacted in basic medium with a mixture comprising enantiometers.Type: GrantFiled: April 14, 2000Date of Patent: June 1, 2004Assignee: Solvay (Societe Anonyme)Inventors: Thierry Delplanche, Roland Callens
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Patent number: 6727281Abstract: Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.Type: GrantFiled: July 23, 2002Date of Patent: April 27, 2004Assignee: Novartis AGInventors: Roger A. Fujimoto, Leslie W. McQuire, Benjamin B. Mugrage, John H. van Duzer
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Patent number: 6713647Abstract: Compounds having Formula 4 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.Type: GrantFiled: February 11, 2003Date of Patent: March 30, 2004Assignee: Allergan, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Roshantha A. Chandraratna
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Patent number: 6710205Abstract: An agent comprising the benzoic acid of formula (I) wherein A, B, R6, R7 are carbocyclic ring, heterocyclic ring, etc.; R1 is hydroxy etc.; R2, R3, R4 are alkyl etc.; R5, D, E are alkylene, etc.; G is oxygen etc., as active ingredient. The compound of formula (I) is considered to be useful for the treatment and/or prophylaxis of bone diseases, cancer, systemic granuloma, immunological diseases, allergy, atopy, asthma, gumboil, gingivitis, periodontitis, neurocyte death, Alzheimer's diseases, lungs injury, pulmopathy, acute hepatitis, nephritis, myocardial ischemia, Kawasaki disease, ambustion, ulcerative colitis, Crohn's disease, multiple organ failure, sleeping disorder, platelet aggregation, etc.Type: GrantFiled: August 16, 2002Date of Patent: March 23, 2004Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kousuke Tani, Kaoru Kobayashi, Takayuki Maruyama
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Patent number: 6696606Abstract: A solid phase synthetic method for preparing arylretinamides is provided. The method comprises reacting hexachloroacetone with a solvent-suspended resin-bound triphenylphosphine to provide a suspension comprising an activated chlorinating reagent; reacting retinoic acid with the activated chlorinating reagent to provide retinoyl chloride; adding pyridine and a select arylamine to the resulting mixture; and stirring the resulting mixture for a time and at a temperature sufficient for the select arylamine to react with the retinoyl chloride and provide the arylretinamide. Also provided, are select arylretinamides that can be prepared by the present method, and methods of using such arylretinamides to induce apoptosis in cancer cells.Type: GrantFiled: July 8, 2002Date of Patent: February 24, 2004Assignee: The Ohio State University Research FoundationInventors: Robert W. Curley, Jr., Serena M. Mershon
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Patent number: 6686499Abstract: The present invention relates to a method for making 2-N-phenylamino)benzoic acids by coupling a benzoic acid and an aniline using an alkaline metal hexamethyldisilazide as a base.Type: GrantFiled: August 20, 2001Date of Patent: February 3, 2004Assignee: Warner-Lambert CompanyInventors: Michael Huai Gu Chen, Javier Magano
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Patent number: 6677360Abstract: The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases. The compounds according to the invention have the formula (1) wherein R1, R2, U, V, A, B, W, R3, C and R4 have the meaning as defined in the claims.Type: GrantFiled: April 6, 2001Date of Patent: January 13, 2004Assignee: Bayer AktiengesellschaftInventors: Markus Albers, Klaus Urbahns, Andrea Vaupel, Michael Härter, Delf Schmidt, Beatrix Stelte-Ludwig, Christoph Gerdes, Elke Stahl, Jörg Keldenich, Ulf Brueggemeier, Klemens Lustig
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Patent number: 6664291Abstract: The present invention relates to novel thyroid receptor ligands and, more particularly, relates to malonamic acids and derivatives thereof of Formula I, which are useful in the treatment of obesity, overweight condition, hyperlipidemia, glaucoma, cardiac arrhythmias, skin disorders, thyroid disease, hypothyroidism, thyroid cancer and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, congestive heart failure, hypercholesteremia, depression, osteoporosis and hair loss. The present invention also provides methods, pharmaceutical compositions and kits for treating such diseases and disorders.Type: GrantFiled: March 28, 2001Date of Patent: December 16, 2003Assignee: Pfizer, Inc.Inventors: Yuan-Ching P. Chiang, Gary E. Aspnes, Kimberly G. Estep
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Patent number: 6649656Abstract: The present invention relates to an anthranilic acid derivative expressed by the following formula (1) or the following formula (2), or its pharmacologically permissible salt or solvate.Type: GrantFiled: April 4, 2001Date of Patent: November 18, 2003Assignee: Teijin LimitedInventors: Naoki Tsuchiya, Susumu Takeuchi, Takumi Takeyasu, Naoki Hase, Takao Yamori, Takashi Tsuruo
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Patent number: 6605642Abstract: The nonenzymatic glycation and crosslinking of proteins is a part of the aging process with the glycation endproducts and crosslinking of long-lived proteins increasing with age. This process is increased at elevated concentrations of reducing sugars in the blood and in the intracellular environment such as occurs with diabetes. The structural and functional integrity of the affected molecules become perturbed by these modifications and can result in severe consequences. The compounds of the present invention can be used to inhibit this process of nonenzymatic glycation and therefore to inhibit some of the ill effects caused by diabetes or by aging. The compounds are also useful for preventing premature aging, spoilage of proteins in food and can prevent discoloration of teeth.Type: GrantFiled: March 8, 2001Date of Patent: August 12, 2003Assignee: City of HopeInventors: Samuel Rahbar, Iraj Lalezari
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Patent number: 6583180Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are novel glucocorticoid receptor modulators and are useful for treating type II diabetes in a mammal.Type: GrantFiled: February 8, 2002Date of Patent: June 24, 2003Assignee: Abbott LaboratoriesInventors: James T. Link, Bryan K. Sorensen, Jyoti R. Patel, David L. Arendsen, Gaoquan Li
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Patent number: 6573252Abstract: The present invention relates to nitrate salts of compounds having therapeutic activity in bony disorders, such compounds being characterized in that they contain at least a reactive group capable of being salified with nitric acid.Type: GrantFiled: January 19, 2001Date of Patent: June 3, 2003Assignee: Nicox, S.A.Inventor: Piero Del Soldato
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Publication number: 20030055076Abstract: Novel compounds of the general formula (I), the use of these compounds as medicaments, pharmaceuticaly compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR). The compounds exert their effects by modulating the PPAR&ggr; response in a partial agonist manner.Type: ApplicationFiled: July 30, 2002Publication date: March 20, 2003Inventors: Lone Jeppesen, Paul Stanley Bury, John Patrick Mogensen, Ingrid Pettersson, Per Sauerberg
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Publication number: 20020193409Abstract: Polymeric prodrugs of the formula: 1Type: ApplicationFiled: March 21, 2002Publication date: December 19, 2002Inventors: Richard B. Greenwald, Yun H. Choe
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Patent number: 6479548Abstract: Compound of formula I activate the insulin receptor kinase. Pharmaceutical compositions comprising the compounds, and methods of treatment of hyperglycemia and other diseases involving imbalance of glucose levels, especially for the treatment of type II diabetes, by administering these compounds to mammalian hosts, and processes for their preparation, are also described.Type: GrantFiled: May 31, 2001Date of Patent: November 12, 2002Assignee: Telik, Inc.Inventors: John Patterson, Sophia Park, Robert T. Lum, Wayne R. Spevak
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Patent number: 6451858Abstract: Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.Type: GrantFiled: September 13, 2001Date of Patent: September 17, 2002Assignee: Novartis AGInventors: Roger A. Fujimoto, Leslie W. McQuire, Benjamin B. Mugrage, John H. van Duzer
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Patent number: 6437178Abstract: The invention relates to novel o-aminophenolcarboxylic acids or o-aminothiophenolcarboxylic acids of the following structure in which: A1 to A7 are—independently of one another—H, CH3, OCH3, CH2CH3 or OCH2CH3; T is O or S, and m is 0 or 1; Z is a carbocyclic or heterocyclic aromatic radical.Type: GrantFiled: July 9, 2001Date of Patent: August 20, 2002Assignee: Infineon Technologies AGInventors: Recai Sezi, Michael Keitmann
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Patent number: 6417228Abstract: 13-Aza analogs of PGF2&agr; and methods of their use in treating glaucoma and ocular hypertension are disclosed.Type: GrantFiled: October 29, 1999Date of Patent: July 9, 2002Assignee: Alcon Manufacturing, Ltd..Inventor: Peter G. Klimko
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Patent number: 6399628Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: March 12, 1999Date of Patent: June 4, 2002Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: James E. Audia, Beverly K. Folmer, Varghese John, Lee H. Latimer, Jeffrey S. Nissen, Jon K. Reel, Eugene D. Thorsett, Celia A. Whitesitt
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Patent number: 6380256Abstract: Compounds having Formula 4 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.Type: GrantFiled: August 29, 2000Date of Patent: April 30, 2002Assignee: Allergan Sales, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Roshantha A. Chandraratna
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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: 6362210Abstract: Carboxylic acid amides of general formula which inhibit telomerase and are useful for treating tumour diseases such as carcinomas, sarcomas and leukaemias. Exemplary compounds are: (1) trans-3-(naphth-2-yl)-but-2-enoic acid-N-(2-carboxy-phenyl)-amide, and, (2) trans-3-(naphth-2-yl)-but-2-enoic acid-N-(2-carboxy-4,5-dimethoxy-phenyl)-amide.Type: GrantFiled: July 18, 2000Date of Patent: March 26, 2002Assignee: Boehringer Ingelheim Pharma KGInventors: Norbert Hauel, Henning Priepke, Klaus Damm, Andreas Schnapp
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Patent number: 6358504Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.Type: GrantFiled: February 7, 1997Date of Patent: March 19, 2002Assignee: Emisphere Technologies, Inc.Inventors: Andrea Leone-Bay, Eric Wang, Donald J. Sarubbi, Harry Leipold, Koc-Kan Ho, David Gschneidner
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Patent number: 6346242Abstract: The present invention provides a compound having the formula or a salt thereof which facilitates the delivery of active agents. Compositions and dosage unit forms comprising the compound of the present invention and at least one active agent, such as a peptide, mucopolysaccharide, carbohydrate, or a lipid, are also provided. Methods of administration and preparation of the compounds and compositions of the invention are provided as well.Type: GrantFiled: February 8, 2000Date of Patent: February 12, 2002Assignee: Emishpere Technologies, Inc.Inventors: Andrea Leone-Bay, Koc-Kan Ho, Donald J. Sarubbi, Sam J. Milstein
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Publication number: 20020013369Abstract: Disclosed are the compounds of formula I 1Type: ApplicationFiled: September 13, 2001Publication date: January 31, 2002Inventors: Roger A. Fujimoto, Leslie W. McQuire, Benjamin B. Mugrage, John H. van Duzer, Daqiang Xu
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Patent number: 6310099Abstract: Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.Type: GrantFiled: November 27, 2000Date of Patent: October 30, 2001Assignee: Novartis AgInventors: Roger A. Fujimoto, Leslie W. McQuire, Benjamin B. Mugrage, John H. van Duzer, Daqiang Xu
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Patent number: 6310238Abstract: The invention relates to novel o-aminophenolcarboxylic acids or o-aminothiophenolcarboxylic acids of the following structure in which: A1 to A7 are—independently of one another—H, CH3, OCH3, CH2CH3 or OCH2CH3; T is O or S, and m is 0 or 1; Z is a carbocyclic or heterocyclic aromatic radical.Type: GrantFiled: September 24, 1998Date of Patent: October 30, 2001Assignee: Siemens AktiengesellschaftInventors: Recai Sezi, Michael Keitmann
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Publication number: 20010023257Abstract: The application discloses substituted norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics and a medicament comprising themType: ApplicationFiled: December 12, 2000Publication date: September 20, 2001Inventors: Uwe Heinelt, Hans-Jochen Lang, Heinz-Werner Kleemann, Jan-Robert Schwark, Klaus Wirth, Hans-Willi Jansen
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Patent number: 6232467Abstract: Amines and amino acids are prepared by reacting an amine, a carbonyl derivative, and an organoboron compound under mild conditions.Type: GrantFiled: June 27, 1997Date of Patent: May 15, 2001Assignee: University of Southern CaliforniaInventors: Nicos A. Petasis, Ilia A. Zavialov
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Patent number: 6229011Abstract: Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.Type: GrantFiled: August 21, 1998Date of Patent: May 8, 2001Assignee: Hoffman-La Roche Inc.Inventors: Li Chen, Robert William Guthrie, Tai-Nang Huang, Achyutharao Sidduri, Jefferson Wright Tilley, Kenneth Gregory Hull
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Patent number: 6172239Abstract: The invention relates to compounds of the formula The compounds have agreat affinity for the neurotensin receptors.Type: GrantFiled: August 16, 1999Date of Patent: January 9, 2001Assignee: SanofiInventors: Bernard Labeeuw, Danielle Gully, Francis JeanJean, Jean-Charles Molimard, Robert Boigegrain
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Patent number: 6166050Abstract: Compounds of the formula ##STR1## which inhibit leukocyte adhesion mediated by interaction of the .alpha..sub.4 .beta..sub.1 integrin (VLA-4) with its counterreceptor VCAM-1, and their use for the treatment of inflammatory and autoimmune diseases.Type: GrantFiled: December 10, 1999Date of Patent: December 26, 2000Assignee: American Home Products CorporationInventors: Louis J. Lombardo, Joan Sabalski
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Patent number: 6160009Abstract: Compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 are as defined in the specification, and non-toxic metabolically labile ester and amides thereof are useful as modulators of metabotropic glutamate receptor function.Type: GrantFiled: May 28, 1999Date of Patent: December 12, 2000Assignee: Eli Lilly and CompanyInventors: Steven Marc Massey, James Allen Monn, Matthew John Valli
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Patent number: 6156750Abstract: Novel pharmaceutically/cosmetically-active bicyclic aromatic compounds have the structural formula (I): ##STR1## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: January 13, 1999Date of Patent: December 5, 2000Assignee: Centre International de Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 6127392Abstract: Compounds of the formula: wherein: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, independently, hydrogen, COOR.sub.15, halogen, nitro, cyano, C.sub.1-10 alkoxy, C.sub.1-10 haloalkoxy, sulfonic acid, C.sub.1-10 alkylsulfonyl, C.sub.6-12 arylsulfonyl, C.sub.6-12 aralkylsulfonyl, C.sub.1-10 alkylsulfinyl, C.sub.6-12 arylsufinyl, C.sub.6-12 aralkylsulfinyl, sulfamoyl, C.sub.1-10 alkylsulfamido, C.sub.6-12 arylsulfamido, C.sub.1-10 alkanoyl, C.sub.6-12 aryloyl, C.sub.6-12 aralkanoyl, amino, C.sub.1-10 alkylamino, C.sub.2-10 dialkylamino, C.sub.6-12 aralkylamino, C.sub.6-12 arylamino, carboxamido, C.sub.1-10 alkylcarboxamido, C.sub.6-12 arylcarboxamido, C.sub.1-10 haloalkyl, C.sub.1-10 alkyl, C.sub.2-12 alkenyl, C.sub.6-12 aryl, C.sub.6-12 aralkyl; with the proviso that at least one of R.sub.4 and R.sub.5 is COOR.sub.15 ;R.sub.9 is hydrogen, C.sub.1-10 alkyl and C.sub.1-10 haloalkyl;R.sub.10 is hydrogen, C.sub.1-10 alkyl, C.sub.1-10 haloalkyl, or C.sub.2-12 alkylidene;R.sub.Type: GrantFiled: August 3, 1998Date of Patent: October 3, 2000Assignee: American Home Products CorporationInventors: Joseph Richard Lennox, Schuyler Adam Antane, John Anthony Butera
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Patent number: 6096921Abstract: The invention relates to novel o-aminophenolcarboxylic acids, and o-aminothiophenolcarboxylic acids of the following structure: ##STR1## where A.sup.1 to A.sup.7 are--independently of one another--H, F, CH.sub.3, CF.sub.3, OCH.sub.3, OCF.sub.3, CH.sub.2 CH.sub.3, CF.sub.2 CF.sub.3, OCH.sub.2 CH.sub.3 or OCF.sub.2 CF.sub.3, where at least one of the radicals A.sup.1 to A.sup.3 must be F or an F-containing group; T is O or S, and m is 0 or 1; and Z is a carbocyclic or heterocyclic aromatic radical.Type: GrantFiled: September 1, 1999Date of Patent: August 1, 2000Assignee: Siemens AktiengesellschaftInventors: Recai Sezi, Michael Keitmann
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Patent number: 6008251Abstract: The present invention relates to a compound of the formula ##STR1## wherein X is --CONH-- or --NHCO--, or a nontoxic pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof.The compounds of the present invention exhibit retinoid-like properties and are thus useful as antiinflammatory agents for chronic skin inflammatory diseases such as psoriasis and atopic dermatitis, as agents for the treatment of rheumatic diseases such as rheumatoid arthritis, as antitumor agents for the treatment of various tumors, and as agents for the treatment of non-malignant proliferative skin conditions.Type: GrantFiled: March 27, 1998Date of Patent: December 28, 1999Assignee: Bristol-Myers Squibb CompanyInventors: Fred C. Zusi, Peter R. Reczek, Jacek Ostrowski
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Patent number: 6001347Abstract: Carrier compounds, compositions, and dosage unit forms therefor which are useful in the delivery of active agents are provided. The present invention provides a compound having the formula: ##STR1## or a salt thereof, wherein the compound may be used in a composition or dosage unit form for delivery of at least one active agent, including a peptide, mucopolysaccharide, carbohydrate, or a lipid. Methods of administration and preparation of the compounds and compositions of the invention are provided as well, including oral administration. Further, the compositions of the invention may be prepared by mixing at least one active agent, at least one carrier compound, and, optionally, a dosing vehicle.Type: GrantFiled: February 6, 1997Date of Patent: December 14, 1999Assignee: Emisphere Technologies, Inc.Inventors: Andrea Leone-Bay, Koc-Kan Ho, Donald J. Sarubbi, Sam J. Milstein
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Patent number: 6001877Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, posses an antagonistic activity on leukotriene B.sub.4.Type: GrantFiled: May 20, 1998Date of Patent: December 14, 1999Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Mitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
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Patent number: 5998662Abstract: The invention relates to novel o-aminophenolcarboxylic acids, and o-aminothiophenolcarboxylic acids of the following structure: ##STR1## where A.sup.1 to A.sup.7 are--independently of one another--H, F, CH.sub.3, CF.sub.3, OCH.sub.3, OCF.sub.3, CH.sub.2 CH.sub.3, CF.sub.2 CF.sub.3, OCH.sub.2 CH.sub.3 or OCF.sub.2 CF.sub.3, where at least one of the radicals A.sup.1 to A.sup.3 must be F or an F-containing group; T is O or S, and m is 0 or 1; and Z is a carbocyclic or heterocyclic aromatic radical.Type: GrantFiled: September 25, 1998Date of Patent: December 7, 1999Assignee: Siemens AktiengesellschaftInventors: Recai Sezi, Michael Keitmann
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Patent number: 5989539Abstract: Carrier compounds, compositions, and dosage unit forms therefor which are useful in the delivery of active agents are provided. The present invention provides a compound having the formula: ##STR1## or a salt thereof, wherein the compound may be used in a composition or dosage unit form for delivery of at least one active agent, including a peptide, mucopolysaccharide, carbohydrate, or a lipid. Methods of administration and preparation of the compounds and compositions of the invention are provided as well, including oral administration. Further, the compositions of the invention may be prepared by mixing at least one active agent, at least one carrier compound, and, optionally, a dosing vehicle.Type: GrantFiled: February 6, 1997Date of Patent: November 23, 1999Assignee: Emisphere Technologies, Inc.Inventors: Andrea Leone-Bay, Koc-Kan Ho, Donald J. Sarubbi, Sam J. Milstein
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Patent number: 5985928Abstract: Novel pharmaceutically/cosmetically-active bicyclic aromatic compounds have the structural formula (I): ##STR1## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: January 9, 1998Date of Patent: November 16, 1999Assignee: Centre International De Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 5977173Abstract: The invention provides novel PGF analogs. In particular, the present invention relates to compounds having a structure according to the following formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, Y, and Z are defined below. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof.The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using theses compounds or the compositions containing them.Type: GrantFiled: September 4, 1998Date of Patent: November 2, 1999Inventors: John August Wos, Mitchell Anthony deLong, Jack S. Amburgey, Jr., Biswanath De, Haiyan George Dai, Yili Wang