Two Double Bonds Between Ring Members Of The Five-membered Hetero Ring (e.g., Pyrrole, Etc.) Patents (Class 514/427)
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Patent number: 7186825Abstract: Novel conformationally restricted polyamine analogs are provided, as well as compositions comprising these novel polyamine analogs. Methods of using the novel polyamine analogs in treatment of diseases such as cancer are also provided. Also provided is a method of delivering these analogs specifically to tumor cells by covalently attaching polyamine analogs to porphyrin compounds, along with novel polyamine-porphyrin covalent conjugates.Type: GrantFiled: June 21, 2004Date of Patent: March 6, 2007Assignee: Cellgate, Inc.Inventors: Benjamin Frydman, Laurence J. Marton, Venodhar K. Reddy, Aldonia L. Valasinas, Andrei V. Blokhin, Hirak S. Basu
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Patent number: 7186749Abstract: The present invention relates to pyrrolo-naphthyl compounds of the formula and methods of using them to modulate PAI-1 expression and to treat PAI-1 related disorders.Type: GrantFiled: August 22, 2005Date of Patent: March 6, 2007Assignee: WyethInventors: Thomas J. Commons, Douglas John Jenkins
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Patent number: 7179825Abstract: The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3; R1 represents hydrogen, hydroxy, C1-6alkyl or aryl; R2 represents hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; Het1; or R1 and R2 taken together may form a bivalent radical of formula —(CH2)n— wherein n is 2, 3, 4, 5 or 6; R3 represents hydrogen, optionally substituted C1-6alkyl, aryl, Het1; R4 represents hydrogen; hydroxy; mercapto; C1-6alkyloxy; C1-6alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C1-12alkyl; optionally substituted C2-8alkenyl; optionally substituted C2-8alkynyl; optionally substituted C3-7cycloalkyl; optionally substituted C5-7cycloalkenyl; aryl; Het1; or -Alk-NR3R5 (i) or —NR3R5 (ii) wherein Alk represents C1-6alkanediyl; and R5 represents hydrogen, C1-6alkyl, aryl, Het1, (aryl or Het1)C1-6alkyl, (aryl or Het1)carbonyl or (aType: GrantFiled: March 16, 2005Date of Patent: February 20, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: Dominique Mabire, Christophe Denis Adelinet, Imré Christian Csoka, Marc Gaston Venet
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Patent number: 7173055Abstract: Novel pyraole derivatives of formula (I), wherein: X is oxygen or sufu, R1 is C1–C3alkyl, C1–C3haloalkyl, C1–C3alkoxy-C1–C3alkyl or C1–C3haloalkoxy-C1–C3alkyl; R2 is C1–C3haloalkyl; and R3 is halogen. The novel compounds have plant-protective properties and are suitable for protecting plants against infestations by phytopathogenic microorganisms.Type: GrantFiled: November 11, 2000Date of Patent: February 6, 2007Assignee: Syngenta Crop Protection, Inc.Inventor: Harald Walter
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Patent number: 7160916Abstract: This invention features a method for enhancing bone growth or inhibiting bone resportion. The method includes administering to a subject in need thereof a compound of the following formula: A is H, R, or each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, or pyrrolyl; each of R1, R2, R3, R4, R5, and R6, independently, is H, halogen, R, C(O)OH, C(O)OR, C(O)SH, C(O)SR, C(O)NH2, C(O)NHR, C(O)NRR?, ROH, ROR?, RSH, RSR?, NHR, NRR?, RNHR?, or RNR?R?; or R1 and R2 together, R3 and R4 together, or R5 and R6 together are ORO; wherein each of R, R?, and R?, independently is C1˜C6 alkyl; and n is 1, 2, or 3.Type: GrantFiled: September 1, 2004Date of Patent: January 9, 2007Assignee: Yung Shin Pharmaceutical Ind. Co., Ltd.Inventors: Wen-Mei Fu, Chih-Hsin Tang, Rong-Sen Yang, Che-Ming Teng, Sheng-Chu Kuo, Fang-Yu Lee
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Patent number: 7153881Abstract: The present invention provides novel compounds and use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: Wherein X and Y are independently chosen from O, N, S and (CH2)n, where n is 0, 1, 2, 3, 4, or 5, or a combination of these and may contain carbon-carbon multiple bonds and branched chains as well as alicyclic and heterocyclic groups; Q is H or OH; R1 and R2 can be either the same or different and are chosen from hydrogen or the residue of an aromatic group as listed in Scheme 1 and the pharmacologically active salts thereofType: GrantFiled: August 7, 2001Date of Patent: December 26, 2006Assignee: Acure Pharma ABInventors: Torbjörn Lundstedt, Anna Skottner, Arne Boman, Per Andersson, Victor Andrianov, Ivars Kalvins
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Patent number: 7122572Abstract: The present invention provides calixpyrrole, calixpyridinopyrrole, and calixpyridine macrocycles, having 4, 5, 6, 7, or 8 heterocyclic rings, as well as syntheses, derivatives, conjugates, multimers, and solid supports thereof. Such macrocycles have proved to be effective and selective ion- and neutral molecule-binding agents forming supramolecular ensembles, and ion- and neutral molecule-separation agents. The macrocycles are fully meso-non-hydrogen-substituted porphyrinogens, a few molecules of which were previously known but not recognized as possessing anion- or molecule-binding properties. The binding mode is noncovalent, primarily that of hydrogen-bonding, thereby providing a new mode for liquid chromatography, that of Hydrogen Bonding Liquid Chromatography. Further useful applications of the macrocycles provided herein include environmental remediation by removal of undesired ions or neutral molecules, and removal of phosphate for kidney dialysis.Type: GrantFiled: April 20, 2001Date of Patent: October 17, 2006Assignee: Board of Regents, University of Texas SystemInventors: Philip A. Gale, Jonathan L. Sessler, Vladimír A. Král, Andrei Andrievsky, Vincent Lynch, Petra I. Sansom, William E. Allen, Christopher T. Brown, Andreas Gebauer
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Patent number: 7122569Abstract: New compounds useful in photodynamic therapy are of the formula and their 1,4-diene isomers and the metallated and/or labeled and/or conjugated forms thereof wherein each R1 is independently alkyl (1–6C); each n is independently an integer of 0–6; and R2 is vinyl or a derivative form thereof.Type: GrantFiled: April 14, 2004Date of Patent: October 17, 2006Assignees: QLT, Inc. and, University of British ColumbiaInventors: Ethan D. Sternberg, David Dolphin, Julia G. Levy, Anna M. Richter, David W. C. Hunt, Ashok Jain, Elizabeth M. Waterfield, Ronald E. Boch, Andrew Norman Tovey
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Patent number: 7112606Abstract: Heterocyclic arylsulfonamidobenzylic compounds are provided which are useful in treating lipid disorders, metabolic disorders and cell-proliferative diseases.Type: GrantFiled: January 29, 2003Date of Patent: September 26, 2006Assignee: Amgen Inc.Inventors: Xian Yun Jiao, Frank Kayser, David J. Kopecky, Sharon McKendry, Derek E. Piper, Andrew K. Shiau
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Patent number: 7105564Abstract: The present invention provides novel compounds having a dual antagonistic activity against thromboxane A2 receptor and prostaglandin D2 receptor and pharmaceutical compositions comprising them. A compound of the formula (I): wherein R1 is —CH2—CH?CH—CH2—CH2—CH2—COOR2 or —CH?CH—CH2—CH2—CH2—COOR2; R2 is hydrogen or alkyl; m is 0 or 1; p is 0 or 1; X1 and X3 each is independently optionally substituted aryl or optionally substituted heteroaryl; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(?O)—, or the like, have a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor.Type: GrantFiled: March 2, 2000Date of Patent: September 12, 2006Assignee: Shionogi & Co., Ltd.Inventors: Tsunetoshi Honma, Yoshiharu Hiramatsu, Akinori Arimura
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Patent number: 7094431Abstract: This invention pertains to therapeutic antibacterial/antifungal-wound healing compositions comprising a therapeutically effective amount of antibacterial agents and/or antifungal agents and/or wound healing composition alone. In one embodiment, the wound healing composition comprises (a) zinc oxide; (b) calcium channel blocker, and (c) fat-soluble vitamins admixed with antibacterial and antifungal agents. The therapeutic antibacterial/antifungal-wound healing compositions may be utilized in a wide variety of pharmaceutical products and administered orally or topically.Type: GrantFiled: September 30, 2003Date of Patent: August 22, 2006Inventor: Mickey L. Peshoff
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Patent number: 7078400Abstract: The present invention relates to an inhibitor for production of 20-hydroxyeicosatetraenoic acid, comprising, as an effective ingredient, specific hydroxyformamidine derivatives or pharmaceutically-acceptable salts thereof. The inhibitors according to the present invention are useful as therapeutic agents for kidney diseases, cerebrovascular diseases, or circulatory diseases. In addition, the present invention also provides novel hydroxyformamidine derivatives or pharmaceutically-acceptable salts thereof.Type: GrantFiled: July 1, 2003Date of Patent: July 18, 2006Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
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Patent number: 7071358Abstract: Arylsulfonamidobenzyl alcohols, amines and sulfonamides are provided which are useful in treating lipid disorders, metabolic diseases and cell-proliferative diseases.Type: GrantFiled: January 29, 2003Date of Patent: July 4, 2006Assignee: Amgen Inc.Inventors: Xian Yun Jiao, Frank Kayser, Sharon McKendry, Derek E. Piper, Andrew K. Shiau
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Patent number: 7056938Abstract: Upon exposure to UVB, the epidermal component trans-urocanic acid is not only photoisomerized into cis-urocanic acid, but will also, at least in part, be photooxidized into urocanic acid oxidation products. We hypothesized that urocanic acid oxidation products can mimic UV-induced systemic immunosuppression comparable to the suppressive properties already established for cis-urocanic acid. A crude mixture of urocanic acid oxidation products showed a significant suppression of the sensitization phase of the systemic contact hypersensitivity response to picryl chloride. Three of the urocanic acid oxidation products were selected for this study: imidazole-4-carboxylic acid, imidazole-4-carboxaldehyde and imidazole-4-acetic acid. Effects on the sensitization-, elicitation- and post-elicitation phase of contact hypersensitivity to picryl chloride in BALB/c mice were studied and compared to the effects of cis-urocanic acid.Type: GrantFiled: June 23, 2000Date of Patent: June 6, 2006Assignee: Academisch Ziekenhuis Bij De Univ.Inventors: Arthur Kammeijer, Joannes Dositheus Bos
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Patent number: 7049334Abstract: A method for enhancing learning and memory or treating amnesia. The method includes administrating to a subject in need thereof a compound of the formula (I): A is H, R, or ?each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, or pyrrolyl; each of R1, R2, R3, R4, R5, and R6, independently, is H, nitro, halogen, R, OH, OR, C(O)OH, C(O)OR, C(O)SH, C(O)SR, C(O)NH2, C(O)NHR, C(O)NRR?, ROH, ROR?, RSH, RSR?, ROC(O)R?OH, NHR, NRR?, RNHR?, or RNR?R?; or R1 and R2 together, R3 and R4 together, or R5 and R6 together are ORO; wherein each of R, R?, and R?, independently is C1˜C6 alkyl; and n is 1, 2, or 3. The compound is in an effective amount for enhancing learning and memory or treating amnesia.Type: GrantFiled: September 13, 2002Date of Patent: May 23, 2006Assignee: Carlsbad Technology, Inc.Inventors: Wen-Mei Fu, Keng-Chen Liang, Wei-Lin Chien, Sheng-Chu Kuo, Fang-Yuan Lee, Che-Ming Teng
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Patent number: 7034018Abstract: The invention relates to substituted pyrrole Mannich bases of general formula (I), wherein R1=H, a C1-10-alkyl-, aryl, a heteroaryl- or an aryl, heteroaryl-, CN, Br—, Cl or OH radical bound by a C1-6 alkylene group, R2=CH(R4)N(R5)(R6), R3, R3?, R3? identically or individually represent H, F, Cl, Br, CF3, CN, NO2, SO2NH2, NHR7, SR8, OR9, CO(OR10), CH2CO(OR11), COR15, a C1-10-alkyl-, aryl-, heteroaryl-aryl radical or a heteroalkyl radical bound by a C1-6 alkylene group, R4=an unsubstituted phenyl radical or a phenyl radical substituted at least with C1-4 alkyl, C1-3-alkoxy-, halogen-, a method for the production of the above-mentioned compounds, medicaments containing said compounds, and the use of said compounds in the production of medicaments.Type: GrantFiled: December 20, 2000Date of Patent: April 25, 2006Assignee: Gruenenthal GmbHInventors: Matthias Gerlach, Corinna Maul
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Patent number: 7008932Abstract: An orally administered soft gelatin formulation preparation of low molecular weight Hyaluronic Acid (HA) for use as a nutritional supplement to provide the primary benefit of internally causing the softening of the human skin.Type: GrantFiled: July 8, 2004Date of Patent: March 7, 2006Assignee: Soft Gel Technologies, Inc.Inventors: Ronald G. Udell, Yousry M. A. Naguib
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Patent number: 7001918Abstract: A compound of Formula (I): wherein variables R, R1, R2, R3 and A are as defined in theType: GrantFiled: June 1, 2004Date of Patent: February 21, 2006Assignee: Paratek Pharmaceuticals, Inc.Inventors: Sophie Huss, Jose M. Bueno, Jose M. Fiandor, Roger Frechette
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Patent number: 6992081Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formulas (XII) (XIII), and (XIV) useful in treating Alzheimer's disease and other similar diseases.Type: GrantFiled: September 21, 2001Date of Patent: January 31, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Roy Hom, Shumeye Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Fang
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Patent number: 6987123Abstract: The present invention relates to compounds of the general formula (I), there derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates, wherein all variables are as defined in the specification.Type: GrantFiled: August 10, 2001Date of Patent: January 17, 2006Assignee: Cadila Healthcare LimitedInventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Vijay Kumar Gajubhai Barot
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Patent number: 6972287Abstract: The present invention provides a method of treating Alzheimer's disease using a compound of Formula (I). Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of the Formula (I) and a method of imaging amyloid deposits, as well as new compounds of Formula (I).Type: GrantFiled: May 31, 2000Date of Patent: December 6, 2005Assignee: Pfizer Inc.Inventors: Corinne Elizabeth Augelli-Szafran, Mark Robert Barvian, Christopher Franklin Bigge, Shelly Ann Glase, Shunichiro Hachiya, John Steven Kiely, Takenori Kimura, Yingjie Lai, Annette Theresa Sakkab, Mark James Suto, Larry Craswell Walker, Tomoyuki Yasunaga, Nian Zhuang
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Patent number: 6949536Abstract: This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl; halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring. R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 or 4.Type: GrantFiled: February 3, 2004Date of Patent: September 27, 2005Assignee: Pfizer, Inc.Inventors: Kazuo Ando, Tomoki Kato, Akiyoshi Kawai, Tomomi Nonomura
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Patent number: 6943187Abstract: This invention relates to pharmaceutical compositions and methods for treating alopecia and promoting hair growth using pyrrolidine derivatives.Type: GrantFiled: May 20, 2002Date of Patent: September 13, 2005Assignee: GPI Nil Holdings, Inc.Inventors: Joseph P. Steiner, Gregory S. Hamilton
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Patent number: 6936719Abstract: Compounds of formula (I) are useful as inhibitors of trypsin like serine protease enzymes such as thrombin, factor VIIa, factor Xa, TF/FVIIa, and trypsin. These compounds could be useful to treat and/or prevent clotting disorders, and as anticoagulating agents.Type: GrantFiled: December 18, 2003Date of Patent: August 30, 2005Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, R. Scott Rowland, Pooran Chand, Pravin L. Kotian, Yahya El-Kattan, Shri Niwas
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Patent number: 6919368Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: February 6, 2003Date of Patent: July 19, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Soo S. Ko, George V. Delucca, John V. Duncia, Ui Tae Kim, Dean A. Wacker, Changsheng Zheng
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Patent number: 6916846Abstract: Coumermycin analogs of general formula I: wherein X, a linking group, is selected from the group consisting of alkyl, aryl, diaryl, substituted alkyl, substituted aryl, alkyl with hereroatoms in the chain, heteroaryl, cyclic and bicyclic alkyl, and a combination of alkyl, aryl and heteroaryl substituents. The compounds are suitable for use as chemical dimerizers of chimeric proteins.Type: GrantFiled: April 23, 2001Date of Patent: July 12, 2005Assignee: Merck & Co. Inc.Inventors: Michael A. Farrar, Steven H. Olson, Roger M. Perlmutter, Llnon H. Slossberg
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Patent number: 6911468Abstract: A compound of the formula (I): wherein X1 and X2 are the same or different and each is a bond or a spacer having 1 to 20 atom(s) in the main chain; one of R1 and R2 is a cycle group having substituent(s) selected from 1) an optionally substituted carboxy-C1-6 alkoxy group and 2) an optionally substituted carboxy-C1-6 aliphatic hydrocarbon group, wherein the cycle group optionally has additional substituent(s), and the other is an optionally substituted cycle group or a hydrogen atom; and R3, R4 and R5 are the same or different and each is a hydrogen atom or a substituent, or R4 may link together with R3 or R5 to form an optionally substituted ring; provided that when R3 is a hydrogen atom, R4 is a hydrogen atom and R5 is methyl, X2—R2 is not 4-cyclohexylphenyl; when R3 is 4-methoxyphenyl, R4 is a hydrogen atom and R5 is methyl, X2—R2 is not 4-methoxyphenyl; and when R1 or R2 is a hydrogen atom, the adjacent X1 or X2 is not a C1-7 alkylene; or a salt thereof exhibits a protein tyrosine phosphatase inhibiType: GrantFiled: May 21, 2001Date of Patent: June 28, 2005Assignee: Takeda Chemical Industries, Ltd.Inventors: Takahiro Matsumoto, Nozomi Katayama, Hiroshi Mabuchi
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Patent number: 6887893Abstract: Certain cyclooxygenase-2 inhibitors are useful for the treatment and prevention of tumors and tumor-related disorders and cachexia.Type: GrantFiled: December 16, 1998Date of Patent: May 3, 2005Assignee: Sankyo Company, LimitedInventors: Shinichi Kurakata, Masaharu Hanai, Saori Kanai, Tomio Kimura
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Patent number: 6884754Abstract: An aqueous composition suitable for applying fungicides to plant propagation materials is provided, comprising water and a blend of the following components, by weight: a) 2-10% of a surface-active agent comprising a1) at least one anionic surfactant; b) 0.5-10% of at least one polymer selected from water-dispersible polymers and water-soluble film-forming polymers; c) 4-20% of at least one inorganic solid carrier; and d) 3-20% of at least one antifreeze agent. In one embodiment, the composition comprises a fungicidally effective amount of at least one fungicidally active compound. The inventive composition is storage stable, ready-to-apply (RTA), ecologically and toxicologically favorable and has good fungicidal efficacy.Type: GrantFiled: September 27, 2002Date of Patent: April 26, 2005Assignee: Syngenta Crop Protection, Inc.Inventors: Christian Schlatter, Ravi Ramachandran
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Patent number: 6864276Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) agonists or antagonists of nicotinic acetylcholine receptors.Type: GrantFiled: May 7, 2001Date of Patent: March 8, 2005Assignee: Bayer Cropscience AGInventors: Reiner Fischer, Christoph Erdelen
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Patent number: 6864254Abstract: An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular diseases, or circulatory diseases. The novel hydroxyformamidine derivative or pharmacologically acceptable salt thereof is also provided.Type: GrantFiled: November 1, 2000Date of Patent: March 8, 2005Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
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Patent number: 6858637Abstract: Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: GrantFiled: March 27, 2003Date of Patent: February 22, 2005Assignee: Neurogen CorporationInventors: Yang Gao, Alan J. Hutchison, Wallace C. Pringle, Andrew Thurkauf, Taeyoung Yoon, He Zhao
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Patent number: 6821989Abstract: The present invention provides methods of treating cancer of the liver, ovarian cancer, a desmoid tumor, glioma, pancreatic cancer, or renal cell carcinoma using an estrogen agonist/antagonist. The present invention also provides kits that contain an estrogen agonist/antagonist for treating cancer of the liver, ovarian cancer, a desmoid tumor, glioma, pancreatic cancer, or renal cell carcinoma.Type: GrantFiled: January 23, 2002Date of Patent: November 23, 2004Assignee: Pfizer Inc.Inventor: Robert L. Rosati
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Patent number: 6806259Abstract: An orally administered soft gelatin formulation preparation of low molecular weight Hyaluronic Acid (HA) for use as a nutritional supplement to provide the primary benefit of internally causing the softening of the human skin.Type: GrantFiled: December 21, 2001Date of Patent: October 19, 2004Assignee: Soft Gel Technologies, Inc.Inventors: Ronald G. Udell, Yousry M. A. Naguib
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Patent number: 6797694Abstract: The present invention relates to chemical compounds having inhibitory activity on an intermediate conductance Ca2+ activated potassium channel (IKCa), and the use of such compounds for the treatment or alleviation of diseases or conditions relating to immune dysfunction.Type: GrantFiled: November 9, 2001Date of Patent: September 28, 2004Assignee: Poseidon Pharmaceuticals A/SInventors: Bo Skaaning Jensen, Soren Peter Olsen, Palle Christophersen
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Patent number: 6777572Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful for treatment of renal failure.Type: GrantFiled: November 28, 2001Date of Patent: August 17, 2004Assignee: Pharmacia Corporation (of Pfizer Inc.)Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 6777418Abstract: The current invention provide novel retinoid compounds and methods for their synthesis, methods of treating or preventing emphysema, cancer and dermatological disorders and pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders.Type: GrantFiled: October 1, 2001Date of Patent: August 17, 2004Assignee: Syntex (U.S.A.) LLCInventors: Jean-Marc Lapierre, David Mark Rotstein, Eric Brian Sjogren
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Patent number: 6759427Abstract: A tetrahydroindolone derivative or analogue comprises a 9-atom bicyclic moiety, moiety A, linked through a linker L to a moiety B, where B is a carboxylic acid, a carboxylic acid ester, or a moiety of the structure N(Y1)-D, where Y1 can be one of a variety of substituents, including hydrogen or alkyl, and D is a moiety that enhances the pharmacological effects, promotes absorption or blood-brain barrier penetration of the derivative or analogue. The moiety A has a six-membered ring fused to a five-membered ring. The moiety A can have one, two, or three nitrogen atoms in the five membered ring. The moiety A can be a tetrahydroindolone moiety. The moiety B can be one of a variety of moieties, including moieties having nootropic activity or other biological or physiological activity.Type: GrantFiled: April 20, 2001Date of Patent: July 6, 2004Assignee: Spectrum Pharmaceuticals, Inc.Inventors: David B. Fick, Mark M. Foreman, Alvin J. Glasky
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Patent number: 6737423Abstract: Substituted heterocyclo-norbornylaminoderivatives having: a) an exo-configuration nitrogen and an endo-fused five-membered ring or six-membered ring of the formula (I) or b) an exo-configuration nitrogen and an exo-fused five-membered ring or six-membered ring of the formula (I a), wherein Rn, Het, A, B and T have the meanings given in the claims. These compounds have a variety of uses. They can be used as antihypertensives, for the reduction or prevention of is chemically induced damage, as pharmaceuticals for surgical interventions, for the treatment of ischemia of the nervous system, including stroke and cerebral edema, for the treatment of ischemia due to shock and disturbed respiratory drive, for the treatment of snoring, as a laxative, as an agent against ectoparasites, for the prevention of gallstone formation, as an antiatherosclerotic, as an agent against diabetic late complications, cancers, fibrotic disorders, endothelial dysfunction, organ hypertrophy, and organ hyperplasia.Type: GrantFiled: December 18, 2001Date of Patent: May 18, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Uwe Heinelt, Hans-Jochen Lang, Klaus Wirth, Hans-Willi Jansen
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Patent number: 6727238Abstract: This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo,, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring; R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 oType: GrantFiled: June 18, 2003Date of Patent: April 27, 2004Assignee: Pfizer Inc.Inventors: Kazuo Ando, Tomoki Kato, Akiyoshi Kawai, Tomomi Nonomura
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Patent number: 6723753Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-benzyl-N-phenyl aminoalcohols.Type: GrantFiled: February 7, 2002Date of Patent: April 20, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6677341Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral heteroaryl aminoalcohols.Type: GrantFiled: December 12, 2001Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6677368Abstract: The present invention relates to 4-arylindolinones, as well as pharmaceutical compositions thereof, capable of modulating protein kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation. The present invention also relates to methods for treating protein kinase related disorders.Type: GrantFiled: December 20, 2001Date of Patent: January 13, 2004Assignee: Sugen, Inc.Inventors: Jingrong Cui, Ruofei Zhang, Hong Shen, Ji Yu Chu, Fang-Jie Zhang, Marcel Koenig, Steven Huy Do, Xiaoyuan Li, Chung Chen Wei, Peng Cho Tang
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Patent number: 6677353Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.Type: GrantFiled: May 23, 2002Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6667414Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension.Type: GrantFiled: November 28, 2001Date of Patent: December 23, 2003Assignee: Pharmacia CorporationInventors: Gunnar J. Hanson, John S. Baran
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Patent number: 6649646Abstract: The invention relates to an insecticidal and miticidal composition which contains as active ingredients chlorfenapyr in combination with one or more organophosphoric acid ester-type compounds and to a method for controlling insecticidal or miticidal pests which have acquired resistance to commercial insecticidal and miticidal agents.Type: GrantFiled: September 28, 2001Date of Patent: November 18, 2003Assignee: BASF AktiengesellschaftInventor: Toshiki Fukuchi
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Patent number: 6646009Abstract: N-(Aryl)-2-arylethenesulfonamides and pharmaceutically acceptable salts and compositions thereof are useful as antiproliferative agents, including, for example, anticancer agents. They are also useful as radioprotective agents.Type: GrantFiled: February 28, 2002Date of Patent: November 11, 2003Assignees: Temple University — Of Commonwealth System of Higher Education, Onconova Therapeutics, Inc.Inventors: E. Premkumar Reddy, M.V. Ramana Reddy, Stanley C. Bell
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Patent number: 6642392Abstract: Compounds of Formula I are disclosed which are useful as fungicides wherein X is —O—, —CH(R11)— or ═C(R11)—; R1 is H or C1-C2 alkyl; R2 is H; C1-C6 alkyl; C3-C6 cycloalkyl; or phenyl optionally substituted with halogen, cyano, C1-C2 alkyl or C1-C2 alkoxy; and R3-R11 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula I and a method for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound of Formula I.Type: GrantFiled: March 2, 2001Date of Patent: November 4, 2003Assignee: Board of Trustees of the University of ArkansasInventors: Gregory Steven Basarab, Douglas Brian Jordan, Thomas Arend Lessen, Stephen L. Hansen
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Patent number: 6632840Abstract: Monoacyl-substituted guanidines of formula III, or a salt or acid thereof, and their use as medicine or diagnostic aid: in which X(2) isType: GrantFiled: March 24, 2000Date of Patent: October 14, 2003Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Peter Crause, Wolfgang Scholz, Udo Albus, Jan-Robert Schwark
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Patent number: RE39420Abstract: Compounds of formula (I) and (II): [wherein R is hydrogen, halogen or alkyl; R1 is alkyl, amino or substituted amino; R2 is optionally substituted phenyl; R3 is hydrogen, halogen or optionally substituted alkyl; R4 is hydrogen, optionally substituted alkyl, cycloalkyl, aryl, or aralkyl] have valuable analgesic, anti-inflammatory, anti-pyretic and anti-allergic activities and have the ability to inhibit the production of leukotrienes and to inhibit bone resorption. They are relatively free from the side effects which generally result from the administration of compounds having these kinds of activities.Type: GrantFiled: September 29, 2000Date of Patent: December 5, 2006Assignee: Sankyo Company, LimitedInventors: Tomio Kimura, Yasuo Noguchi, Akira Nakao, Keisuke Suzuki, Shigeru Ushiyama, Akihiro Kawara, Masaaki Miyamoto