Only Two Ring Oxygens In The Hetero Ring Which Is Not A Polycyclo Ring System (e.g., Dioxolane, Etc.) Patents (Class 514/467)
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Publication number: 20030181517Abstract: This invention provides a method of treating obesity, generalized anxiety disorder, post-traumatic stress disorder, late luteal phase dysphoric disorder (premenstrual syndrome), attention deficit disorder, with and without hyperactivity, Gilles de la Tourette syndrome, bulimia nervosa or Shy Drager Syndrome in a mammal by administering to the mammal an effective amount of a hydroxycycloalkanephenethyl amine of the following structural formula: 1Type: ApplicationFiled: March 25, 2003Publication date: September 25, 2003Applicant: WyethInventors: Richard L. Rudolph, Albert T. Derivan, Eric A. Muth, G. Virginia Upton
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Publication number: 20030166650Abstract: There is provided novel cinnamide derivatives of Formula I 1Type: ApplicationFiled: May 31, 2002Publication date: September 4, 2003Inventors: Yong-Jin Wu, Li-Quang Sun, Jie Chen, Huan He, Alexandre L'Heureux, Pierre Dextraze, Jean-Paul Daris, Gene G. Kinney, Steven I. Dworetzky, Piyasena Hewawasam
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Publication number: 20030158252Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: 1Type: ApplicationFiled: February 6, 2003Publication date: August 21, 2003Applicant: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan, Thomas P. Stagnaro
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Patent number: 6608061Abstract: A medicament for treatment of cancer comprising a compound represented by the following general formula (I) or a physiologically acceptable salt thereof: Ar1—S—R1—S—Ar2 wherein R1 represents a nonmetal bridging group; Ar1 and Ar2 independently represent a group selected from the group consisting of an aryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group and said aryl group may have one to three substituents other than hydroxyl group on its ring; and a heteroaryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group, and said heteroaryl group may have one to three substituents other than hydroxyl group on its ring.Type: GrantFiled: February 14, 2000Date of Patent: August 19, 2003Assignees: Kyoma Hakko Kogyo Co., Ltd., Fuji Photo Film Co., Ltd.Inventors: Yoshiyuki Yonetani, Takeshi Takahashi, Yuko Kanda, Tamio Mizukami, Tatsuya Tamaoki, Shun-ichi Ikeda, Masanobu Takashima, Naoki Asanuma, Tadashi Inaba, Hiroshi Takeuchi, Hiroshi Kawamoto, Yoshihisa Tsukada, Masato Satomura, Hiroshi Kitaguchi
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Publication number: 20030144217Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.Type: ApplicationFiled: August 21, 2002Publication date: July 31, 2003Applicant: Vertex Pharmaceuticals IncorporatedInventors: Roger D. Tung, Michael R. Hale, Christopher T. Baker, Andrew Spaltenstein, Eric S. Furfine, Istvan Kaldor, Wieslaw M. Kazmierski
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Patent number: 6586465Abstract: The present invention deals with the certain novel esters derived from specific cyclic ether containing alcohols. These products have surprising hydroalcoholic solubility and a very desirable skin feel, making them ideal candidates for use in products like after shave preparations.Type: GrantFiled: May 30, 2002Date of Patent: July 1, 2003Inventors: John Imperante, Anthony J. O'Lenick, Jr.
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Patent number: 6552089Abstract: The present application discloses a method of treating alopecia which is based on the use of a tellurium compound such as ammonium trichloro(dioxoethylene-O,O-tellurate).Type: GrantFiled: November 29, 1996Date of Patent: April 22, 2003Inventors: Benjamin Sredni, Michael Albeck
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Patent number: 6521661Abstract: The novel compositions and methods of the subject invention can be used in antifugal applications. The antifugal agents of the subject invention can be used in the treatment of an animal or human having a fugal infection. In a further embodiment the compounds can be used to treat plant fugal infections, disinfect surfaces, and prevent spoilage of organic compositions such as food and cosmetics.Type: GrantFiled: July 20, 2001Date of Patent: February 18, 2003Assignees: Harbor Branch Oceanographic Institution, Inc., Mycologics, Inc.Inventors: Ying Chen, Katherine Chilson, Keith Brian Killday, Dedra Harmody, Peter J. McCarthy, Shirley A. Pomponi, Rebecca Schimoler, Claude Selitrennikoff, Amy E. Wright
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Patent number: 6518310Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: March 16, 2001Date of Patent: February 11, 2003Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L Fedde, Carl R Illig, Thomas P. Markotan, Thomas P Stagnaro
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Publication number: 20030013757Abstract: Compounds of formula I 1Type: ApplicationFiled: June 11, 2002Publication date: January 16, 2003Inventors: Ulrike Leser-Reiff, Tim Sattelkau, Gerd Zimmermann
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Publication number: 20030013660Abstract: Dioxolane analogs of the following formula: 1Type: ApplicationFiled: October 15, 2001Publication date: January 16, 2003Applicant: Shire BioChem Inc.Inventors: Giorgio Attardo, Boulos Zacharie, Rabindra Rej, Jean-Francois Lavallee, Louis Vaillancourt, Real Denis, Sophie Levesque
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Patent number: 6486200Abstract: A methods of treating an infection comprises administering a therapeutically effective amount of a compound described by the Formula (I): wherein: X may be O, S, or NR′ wherein R′ is H or loweralkyl; R1 and R2 may be independently selected from the group consisting of H, loweralkyl, oxyalkyl, alkoxyalkyl, cycloalkyl, aryl, hydroxyalkyl, aminoalkyl, and alkylaminoalkyl; R3 and R4 are each independently selected from the group consisting of H, loweralkyl, halogen, oxyalkyl, oxyaryl, and oxyarylalkyl; R5 is represented by a formula selected from the group consisting of: wherein: X1, X2, and X3 are independently selected from O and S; and R6 and R7 are independently selected from the group consisting of loweralkyl, aryl, alkylaryl, oxyaryl, an ester-containing substituent, and oxyalkyl; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 7, 2000Date of Patent: November 26, 2002Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc.Inventors: David W. Boykin, M. Syed Rahmathullah, Richard R. Tidwell, James E. Hall
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Patent number: 6458827Abstract: A method of modifying or altering the structure of a 1&agr;-hydroxylated vitamin D compound to increase its biological activity by altering the conformational equilibrium of the A-ring to favor a chair conformation that presents the 1&agr;-hydroxyl in the axial orientation. This is accomplished by either locking the A-ring chair conformation in a geometry having an axially orientated 1&agr;-hydroxyl, or by the addition of one or more substituents to the A-ring which interact with other substituents in the molecule or on the A-ring to provide a driving force to the A-ring to adopt a chair conformation which presents the 1&agr;-hydroxyl in the axial orientation.Type: GrantFiled: July 20, 2001Date of Patent: October 1, 2002Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Rafal R. Sicinski
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Publication number: 20020068075Abstract: The present invention provides a citral acetal capable of sustaining a lemon aroma unique to citral and a perfume composition comprising the citral acetal, as well as an LDH inhibitor and a deodorant, cosmetics and a skin agent for external application, comprising the LDH inhibitor.Type: ApplicationFiled: October 10, 2001Publication date: June 6, 2002Applicant: Kao CorporationInventors: Sakuya Tanaka, Shigeyoshi Tanaka, Shunichi Akiba, Katsutoshi Ara, Hirohiko Ishida
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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: 6353014Abstract: A method of treating glaucoma or ocular hypertension in a patient, which comprises administering to the patient a pharmaceutically effective amount of a compound of formula I:Type: GrantFiled: June 2, 1999Date of Patent: March 5, 2002Assignee: Alcon Laboratories, Inc.Inventors: Verney L. Sallee, Mark R. Hellberg, Peter G. Klimko
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Patent number: 6316496Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: February 1, 2000Date of Patent: November 13, 2001Assignee: G. D. Searle & Co.Inventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, David L Brown, Joseph J McDonald
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Patent number: 6310080Abstract: Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically inhibiting retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: December 1, 1999Date of Patent: October 30, 2001Assignee: G. D. Searle & Co.Inventors: Daniel P Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L. Brown, Joseph J. McDonald
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Patent number: 6306901Abstract: A pharmaceutical agent comprising an ascorbic acid, a derivative thereof or a salt thereof (ascorbic acids) as an active ingredient, for selectively inducing apoptosis of unnecessary or pathogenic cells to thereby prevent and/or treat diseases caused by said cells; a method for the prophylaxis and/or treatment of diseases caused by unnecessary or pathogenic cells, comprising selectively inducing apoptosis of said cells by the use of ascorbic acids; and use of ascorbic acids for the production of a pharmaceutical agent for selectively inducing apoptosis of unnecessary or pathogenic cells to thereby prevent and/or treat diseases caused by said cells. The ascorbic acids are low toxic and selectively induce apoptosis of unnecessary or pathogenic cells. Therefore, they are useful for the prophylaxis and/or treatment of the diseases caused by said cells.Type: GrantFiled: November 5, 1998Date of Patent: October 23, 2001Inventor: Seiichi Tanuma
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Patent number: 6306899Abstract: This invention relates to anti-viral drugs such as Helioxanthin and its analogs. The present compounds may be used alone or in combination with other drugs for the treatment of Hepatitis B virus (HBV), Hepatitis C virus (HCV), Yellow Fever, Dengue Virus, Japanese Encephalitis, West Nile virus and related flaviviruses. In addition, compounds according to the present invention can be used to prevent hepatoma secondary to virus infection as well as other infections or disease states which are secondary to the virus infection.Type: GrantFiled: August 23, 1999Date of Patent: October 23, 2001Assignees: Yale University, N. Y. Mu, N.T.U., V.G.HInventors: Yung-Chi Cheng, Chen-Kung Chou, Lei Fu, Yueh-Hsiung Kuo, Sheau-Farn Yeh, Juliang Zhu, Yonglian Zhu
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Patent number: 6284793Abstract: A process for preventing the transfer of harmful organisms of zooplankton including the epifauna thereof and of phytoplankton including its resting stages, which are taken up with the ballast water of ships and transferred to another locality on discharge. The organisms are substantially destroyed by the addition of an agent containing a water-soluble percarboxylic acid with 1 to 6 carbon atoms, particularly an aqueous solution containing peracetic acid and/or performic acid and hydrogen peroxide, in a quantity of 0.1 to 200 mg of percarboxylic acid per liter of ballast water and allowing it to react before discharge. In a preferred embodiment, cyanide is also added to the ballast water.Type: GrantFiled: December 6, 1999Date of Patent: September 4, 2001Assignee: Degussa-Huls AGInventors: Rainer Fuchs, Michael Huss, Peter Werle
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Patent number: 6251937Abstract: The invention relates to cleavable surfactants of formula: in which R′ and R, which may be identical or different, represent a hydrogen atom or a linear or branched, saturated or unsaturated alkyl radical, the sum of the carbon atoms of R′ and R being between 5 and 42. The invention also relates to the corresponding derivatives obtained by alkaline hydrolysis or amidation. The invention furthermore relates to the preparation of these surfactants from glucono-1(5)-lactone and a compound of formula R—CO—R′ in the presence of an acid catalyst, R and R′ having the meaning given above. The surfactants are used in particular in emulsion polymerization and in the field of cosmetics.Type: GrantFiled: April 13, 1998Date of Patent: June 26, 2001Assignee: CECA S.A.Inventors: Serge Petit, Stephane Fouquay
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Patent number: 6235753Abstract: Inhibitors of the Production of s-CD23 and the secretion of TNF are provided.Type: GrantFiled: January 21, 1999Date of Patent: May 22, 2001Assignee: SmithKline Beecham p.l.c.Inventors: Stuart Bailey, Andrew Faller, David Glynn Smith, Derek Richard Buckle
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Patent number: 6235778Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R114 R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and mare set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: November 26, 1997Date of Patent: May 22, 2001Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan, Thomas P. Stagnaro
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Patent number: 6211201Abstract: A quaternary ammonium cholinergic agent is complexed with a multivalent anion, or with multiple monovalent anions. The complex may be administered orally to a patient to treat pain, or for some other purpose. Numerous modifications are contemplated, including modifications to the ring structure of the compound, substitution and functionalization of the ring. Other contemplated modifications include the use of different anions, including various monovalent and polyvalent anions, and both organic and inorganic anions. The compounds have utility as cholinergic agents, and especially in the treatment of mysasthenia gravis, chest pain, and carpal tunnel syndrome.Type: GrantFiled: June 29, 1999Date of Patent: April 3, 2001Assignee: ICN Pharmaceuticals, Inc.Inventors: Colin Granger, Robert Orr, Kandasamy Ramasamy
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Patent number: 6201017Abstract: An ectoparasite-controlling agent for animals comprising 0.1 to 20% by weight of the neonocotinoid compounds defined in the specification and 10 to 95% by weight of a glycol or glycol monoalkyl ether has an excellent effectiveness by the application methods such as spot-on and pour-on application.Type: GrantFiled: September 21, 1999Date of Patent: March 13, 2001Assignee: Sumitomo Chemical Co., Ltd.Inventors: Satoshi Sembo, Mitsuyasu Makita
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Patent number: 6197817Abstract: Disclosed are compounds of the formula: R represents hydrogen or is a C-3 to C-6 cycloalkyl or C-4 to C-10 straight or branched carbon chain alkyl-cycloalkyl or a group —B—D, where B is C-2 to C-10 straight or branched carbon chain alkyl and D is hydroxy or alkyloxy or 2,3-dihydroxypropyl or 2,3-dialkyloxypropyl or 2,2-dialkyl-1,3-dioxolane-5-methyl, where alkyl is C-1 to C-10 straight or branched carbon chain; W represents CH(CH3)CH2—, C(CH3)2CH2—; Z represents hydrogen, —NHCOR2, —NHCONR2R3 or —NHSO2R2 or —NHSO2NR2R3 or —NHCOOR4 wherein R4 is alkyl of from 1 to about 6 carbon atoms, alkoxyalkyl wherein the alkyl groups may be the same or different and contain from 1 to about 6 carbon atoms, alkoxyaryl, cycloalkyl of from 3 to about 8 carbon atoms.Type: GrantFiled: January 22, 1999Date of Patent: March 6, 2001Assignee: Selectus Pharmaceuticals, Inc.Inventors: William L. Matier, Shyam Patil
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Patent number: 6177576Abstract: A novel composition for supplementing the human diet having a polyol-derived pyruvate (2-keto-propionic-acid) moeity as a component.Type: GrantFiled: August 5, 1998Date of Patent: January 23, 2001Inventor: Michael J. Arnold
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Patent number: 6166017Abstract: A method for the medical treatment of diabetes mellitus type II and for counteracting the risk factors forming part of the Metabolic syndrome (also known as the "deadly quartet" or "syndrome X" or the Insulin Resistance Syndrome) in a patient having increased cortisol activity, which method of treatment comprises decreasing said increased cortisol activity in said patient by the steps of providing an inhibitor of cortisol synthesis.Type: GrantFiled: December 14, 1998Date of Patent: December 26, 2000Assignee: Cortendo, ABInventor: Per Marin
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Patent number: 6147077Abstract: A method of treating fungal infections with a mixture of isomers of 2R,4S-hydroxyitraconazole and their sulfate and phosphate derivatives is disclosed. Pharmaceutical compositions containing these compounds are also disclosed.Type: GrantFiled: April 29, 1999Date of Patent: November 14, 2000Assignee: Sepracor Inc.Inventors: Patrick Koch, Richard F. Rossi, Jr., Chris Hugh Senanayake, Stephen Alan Wald
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Patent number: 6143788Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: January 21, 1998Date of Patent: November 7, 2000Assignee: G.D. Searle & Co.Inventors: Daniel P. Getman, Gary A. Decrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Belekudru Devadas, Srinivasan RAJ Nagarajan, David L. Brown, Joseph J. McDonald
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Patent number: 6143790Abstract: There is disclosed a novel amino glycol derivatives of L-N.sup.6 -(1-iminoethyl)lysine, pharmaceutical compositions containing these novel compounds, and to their use in therapy, in particular their use as nitric oxide synthase inhibitors.Type: GrantFiled: September 6, 1996Date of Patent: November 7, 2000Assignee: G.D. Searle & Co.Inventors: E. Ann Hallinan, Foe S. Tjoeng, Kam F. Fok, Timothy J. Hagen, Mihaly V. Toth, Sofya Tsymbalov, Barnett S. Pitzele
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Patent number: 6136836Abstract: A composition and method for controlling warm-blooded animal parasites comprising 1-[3-chloro-4-(1,1,2-trifluoro-2-trifluoromethoxyethoxy)phenyl]-3-(2,6,dif luorobenzoyl)urea.Type: GrantFiled: July 30, 1999Date of Patent: October 24, 2000Assignee: Isagro S.p.A.Inventors: Franco Bettarini, Paolo Piccardi
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Patent number: 6127407Abstract: The present invention provides substituted 3,3-diphenyl indanone, indane and indole compounds, as well as analogues thereof, which are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.Type: GrantFiled: November 20, 1997Date of Patent: October 3, 2000Assignees: Ion Pharmaceuticals, Inc., President and Fellows of Harvard College, Children's Medical Center CorporationInventors: Carlo Brugnara, Jose Halperin, Rudolf Fluckiger, Emile M. Bellott, Jr., Richard John Lombardy, John J. Clifford, Ying-Duo Gao, Reem M. Haidar, Eugene W. Kelleher, Adel M. Moussa, Yesh P. Sachdeva, Minghua Sun, Heather N. Taft
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Patent number: 6096773Abstract: A method for the inhibition of the binding of .alpha..sub.4 .beta..sub.1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of diseases states in which .alpha..sub.4 .beta..sub.1 is involved.Type: GrantFiled: April 15, 1999Date of Patent: August 1, 2000Assignee: Texas Biotechnology Corporation, Inc.Inventors: Ian L. Scott, Bore G. Raju, Ronald J. Biediger, Vanessa O. Grabbe, Jamal Kassir, Karin M. Keller, Timothy P. Kogan, deceased, Shuqun Lin, Robert V. Market
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Patent number: 6090852Abstract: Compounds of formula (I): ##STR1## where the substituents are as defined herein, and salts thereof, are matrix metalloprotease inhibitors.Type: GrantFiled: January 20, 1999Date of Patent: July 18, 2000Assignee: Pfizer IncInventors: Kevin Neil Dack, Gavin Alistair Whitlock
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Patent number: 6054476Abstract: Iminoacetamides of the formula (I) ##STR1## in which A represents a single bond or optionally substituted alkylene,Q represents oxygen or sulphur,R.sup.1 represents respectively optionally substituted cycloalkyl, cycloalkenyl, aryl or heterocyclyl,R.sup.2 represents respectively optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, aryl or heterocyclyl,R.sup.3 represents hydrogen or respectively optionally substituted alkyl, alkenyl, alkinyl or cycloalkyl,R.sup.4 represents respectively optionally substituted cycloalkyl, cycloalkenyl, aryl or heterocyclcyla process for their preparation, pesticidal compositions containing them, and their use for controlling pests.Type: GrantFiled: April 15, 1998Date of Patent: April 25, 2000Assignee: Bayer AktiengesellschaftInventors: Thomas Seitz, Klaus Stenzel
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Patent number: 6043389Abstract: 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-dedendent patients, treating cystic fibrosis patients, inhibiting telomerase activity, treating virus-associated tumors, especially EBV-associated tumors, augmenting expression of tumor suppressor genes, inducing tolerance to antigens, or treating, preventing or ameliorating protozoan infection or inhibiting histone deacetylase in cells. The compositions of the invention are to and the methods of the invention use hydroxy and ether-containing oxyalkylene esters.Type: GrantFiled: March 11, 1997Date of Patent: March 28, 2000Assignees: Mor Research Applications, Ltd., Beacon Laboratories, Inc., Bar-Ilan UniversityInventors: Abraham Nudelman, Ada Rephaeli
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Patent number: 6043272Abstract: The present invention provides substituted 3,3-diphenyl indanone, indane and indole compounds, as well as analogues thereof, which are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.Type: GrantFiled: November 20, 1997Date of Patent: March 28, 2000Assignees: Ion Pharmaceuticals, Inc., President and Fellows of Harvard College, Children's Medical Center CorporationInventors: Carlo Brugnara, Jose Halperin, Rudolf Fluckiger, Emile M. Bellott, Jr., Richard John Lombardy, John J. Clifford, Ying-Duo Gao, Reem M. Haidar, Eugene W. Kelleher, Adel M. Moussa, Yesh P. Sachdeva, Minghua Sun, Heather N. Taft
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Patent number: 5990158Abstract: New therapeutic agents of carboxylic acid derivatives are disclosed, which are represented by the compounds of the following formula (I) or its pharmaceutically acceptable salts, ##STR1## These compounds are useful as a matrix metalloproteinases (MMPs) inhibitors.Type: GrantFiled: November 3, 1997Date of Patent: November 23, 1999Assignee: Kotobuki Seiyaku Co., Ltd.Inventors: Tsuyoshi Tomiyama, Akira Tomiyama, Takashi Yanagisawa, Atsushi Noda, Yoshinori Kobayashi
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Patent number: 5981511Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.Type: GrantFiled: March 5, 1997Date of Patent: November 9, 1999Assignee: G.D. Searle & Co.Inventors: Rolando E. Gapud, Timothy J. Hagen, Ann E. Hallinan, Donald W. Hansen, Jr., Robert E. Manning, Suzanne Metz, Barnett S. Pitzele, Foe S. Tjoeng, Mihaly V. Toth, R. Keith Webber
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Patent number: 5977166Abstract: A method is disclosed for enhancing flavors in low moisture consumable items, including chewing gum, using menthone ketals. Chewing gum, oral compositions, pharmaceuticals, and low moisture foods containing menthone ketals are provided.Type: GrantFiled: March 24, 1993Date of Patent: November 2, 1999Assignee: WM. Wrigley Jr. CompanyInventor: Michael J. Greenberg
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Patent number: 5968919Abstract: Topical alcoholic or aqueous alcoholic gels containing testosterone, progesterone, estradiol or other hormones have enhanced penetration through skin by including in the formulation 2-n-nonyl-1,3-dioxolane or other hydrocarbyl derivative of 1,3-dioxolane or 1,3-dioxane or acetal, as skin penetration enhancing compound.Type: GrantFiled: October 16, 1997Date of Patent: October 19, 1999Assignee: MacroChem CorporationInventors: Carlos M. Samour, Scott F. Krauser, Robert J. Gyurik
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Patent number: 5955498Abstract: A pharmaceutical agent comprising an ascorbic acid, a derivative thereof or a salt thereof (ascorbic acids) as an active ingredient, for selectively inducing apoptosis of unnecessary or pathogenic cells to thereby prevent and/or treat diseases caused by said cells; a method for the prophylaxis and/or treatment of diseases caused by unnecessary or pathogenic cells, comprising selectively inducing apoptosis of said cells by the use of ascorbic acids; and use of ascorbic acids for the production of a pharmaceutical agent for selectively inducing apoptosis of unnecessary or pathogenic cells to thereby prevent and/or treat diseases caused by said cells. The ascorbic acids are low toxic and selectively induce apoptosis of unnecessary or pathogenic cells. Therefore, they are useful for the prophylaxis and/or treatment of the diseases caused by said cells.Type: GrantFiled: December 23, 1996Date of Patent: September 21, 1999Inventor: Sei-ichi Tanuma
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Patent number: 5928645Abstract: The present invention provides a extracted substance from a mixture of a non-fat starch from Ricini semen and a root of coptis Sp. This substance is suitable for use in the therapeutic applications of AIDS.Type: GrantFiled: September 13, 1995Date of Patent: July 27, 1999Assignee: Young Bok Han & Korean Assoc. of Creation ResearchInventors: Young Bok Han, Jeong Jo Mun, Hong Ki Kyung, Jong Bae Kim, Kyung Tae Kim, Hae Ri Kim, Jeong Han Kim, Hyun Gil Shin, Kyung Rae Kim, Eun Kyung Hong, Choon Won Kim
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Patent number: 5917056Abstract: The present invention relates to novel 10-deacetyl-14.beta.-hydroxybaccatine III derivatives. The novel derivatives, having cytotoxic and antitumour activity, are prepared from this synton after functionalization of the hydroxyls at 1-, 14- as thiocarbonate, iminocarbonate and sulfite and possible oxidation of the hydroxyl at C.sub.10. These derivatives are subjected to a subsequent esterification at position 13- with a variously substituted isoserine chain. The products of the invention can be administered by the injective or oral route, when suitably formulated.Type: GrantFiled: August 5, 1997Date of Patent: June 29, 1999Assignee: INDENA S.p.A.Inventor: Ezio Bombardelli
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Patent number: 5852027Abstract: This invention includes the compounds 2'-deoxy-5-fluoro-3'-oxacytidine, (-)-2'-deoxy-5-fluoro-3'-oxacytidine, and (+)-2'-deoxy-5-fluoro-3+-oxacytidine, and pharmaceutically acceptable salts thereof for use in medical therapy, for example for the treatment or prophylaxis of an HIV infection.Type: GrantFiled: November 9, 1993Date of Patent: December 22, 1998Assignee: Emory UniversityInventors: Dennis C. Liotta, Raymond F. Schinazi, Woo-Baeg Choi
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Patent number: 5849740Abstract: The present invention is a method of using ketoconazole or molecules resembling ketoconazole with comparable biological activity for the manufacture of drugs and for medical treatment of diabetes mellitus type II as well as for counteracting the other risk factors associated with the Metabolic Syndrome.Type: GrantFiled: February 6, 1997Date of Patent: December 15, 1998Assignee: Cortendo ABInventor: Per Marin
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Patent number: 5837725Abstract: Bridged bicyclic aromatic compounds are provided having the structure ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and n are as defined herein. The novel compounds are useful for modulating gene expression of retinoic acid receptors, vitamin D receptors and thyroid receptors. Pharmaceutical compositions and methods for modulating gene expression are provided as well.Type: GrantFiled: May 24, 1995Date of Patent: November 17, 1998Assignees: SRI International, La Jolla Cancer Research FoundationInventors: Marcia I. Dawson, James F. Cameron, Peter D. Hobbs, Ling Jong, Magnus Pfahl, Xiao-kun Zhang, Jurgen M. Lehmann
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Patent number: 5786379Abstract: Novel pharmaceutically/cosmetically-active adamantyl-substituted biaromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a')-(f'): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular, bone and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: December 2, 1996Date of Patent: July 28, 1998Assignee: Centre International de Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon