1,2,4-thiadiazoles (including Hydrogenated) Patents (Class 548/128)
-
Patent number: 6894041Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; —G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems recitType: GrantFiled: November 20, 2002Date of Patent: May 17, 2005Assignee: Pfizer IncInventors: Anthony Marfat, Michael William McKechney
-
Patent number: 6872737Abstract: Compounds of general formula (I): where A, E, G, X, Y and the bond - - - take various meanings are of use in the preparation of a pharmaceutical formulation, for example in the treatment of a disease in which GSK-3 is involved, including Alzheimer's disease or the non-dependent insulin diabetes mellitus, or hyperproliferative disease such as cancer, displasias or metaplasias of tissue, psoriasis, arteriosclerosis or restenosis.Type: GrantFiled: November 8, 2002Date of Patent: March 29, 2005Assignee: Consejo Superior de Investigaciones CientificasInventors: Ana Martinez Gil, Ana Castro Morera, Maria Concepcion Martin Perez, Mercedes Alonso Cascon, Isabel Dorronsoro Diaz, Francisco Jose Moreno Munoz, Francisco Wandosell Jurado
-
Patent number: 6861106Abstract: Dichroic dyes, dichroic dye compositions, and liquid crystal composition and liquid crystal display element containing the dichroic dyes. The dichroic dye has increased solubility and stability.Type: GrantFiled: May 23, 2003Date of Patent: March 1, 2005Assignee: Industrial Technology Research InstituteInventors: Shih-Hsien Liu, Yang-Chu Lin, Woan-Shiow Tzeng, Jie-Hwa Ma, Kung-Lung Cheng, Long-Li Lai
-
Patent number: 6794518Abstract: The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention also provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention also provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety.Type: GrantFiled: December 17, 1999Date of Patent: September 21, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Milind Rajopadhye, Thomas D. Harris, Edward H. Cheesman
-
Publication number: 20040167188Abstract: The present invention is directed to compounds of formula (I), 1Type: ApplicationFiled: February 14, 2003Publication date: August 26, 2004Inventors: Zhili Xin, Gang Liu, Zhonghua Pei, Bruce G. Szczepankiewicz, Michael D. Serby, Hongyu Zhao
-
Publication number: 20040147755Abstract: This invention provides compounds of Formula I having the structure 1Type: ApplicationFiled: January 8, 2004Publication date: July 29, 2004Applicant: WyethInventor: Michael S. Malamas
-
Patent number: 6767918Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed 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: December 9, 2002Date of Patent: July 27, 2004Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: Jing Wu, Eugene D. Thorsett, Jeffrey S. Nissen, Thomas E. Mabry, Lee H. Latimer, Varghese John, Lawrence Y. Fang, James E. Audia
-
Publication number: 20040138464Abstract: Novel compounds of the formula I 1Type: ApplicationFiled: December 2, 2003Publication date: July 15, 2004Inventors: Teresa Mujica-Fernaud, Herwig Buchholz, Christophe Carola, Wilfried Rautenberg, Christian Sirrenberg
-
Publication number: 20040135117Abstract: Dichroic dyes, dichroic dye compositions, and liquid crystal composition and liquid crystal display element containing the dichroic dyes. The dichroic dye has increased solubility and stability.Type: ApplicationFiled: May 23, 2003Publication date: July 15, 2004Applicant: INDUSTRIAL TECHNOLOGY RESEARCH INSTITUTEInventors: Shih-Hsien Liu, Yang-Chu Lin, Woan-Shiow Tzeng, Jie-Hwa Ma, Kung-Lung Cheng, Long-Li Lai
-
Patent number: 6743817Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.Type: GrantFiled: September 6, 2001Date of Patent: June 1, 2004Assignee: Neurogen CorporationInventors: George Maynard, LingHong Xie, Stanislaw Rachwal
-
Publication number: 20040097564Abstract: Provided, among things, is a method of decreasing intraocular pressure in an animal, including a human, comprising administering an intraocular pressure decreasing amount of a compound of the formula I: 1Type: ApplicationFiled: September 25, 2003Publication date: May 20, 2004Inventor: Martin Gall
-
Publication number: 20040092559Abstract: The invention provides compounds of the formula I 1Type: ApplicationFiled: October 14, 2003Publication date: May 13, 2004Inventors: Lawrence Hamann, David Augeri
-
Publication number: 20040087633Abstract: A methylidene oxazolidinone compound represented by formula (1) or a pharmaceutically acceptable salt thereof, and a preparation method thereof, showing superior antimicrobial activities against gram-positive germs including resistant strains such as methicillic-resistant staphylococcus aureus and vancomycin-resistant enterococcus: 1Type: ApplicationFiled: October 29, 2003Publication date: May 6, 2004Applicant: Korea Institute of Science and TechnologyInventors: Hun Yeong Koh, Yong Seo Cho, Ae Nim Pae, Joo Hwan Cha, Hye Yeon Kim, Jae Seok Lee, Hak Soo Kim, Sanghee Kim
-
Publication number: 20040077874Abstract: The invention is directed to polymerizable vinyl compounds having halogenated aromatic groups and to a method of synthesizing such compounds. In particular, the invention is directed to polymerizable aromatic vinyl compounds wherein, except for the vinylic hydrogen atoms, aromatic C—H bonds are replaced by C—X bonds, where X is a halogen or other selected substituent having a de minimus number, if any, of C—H bonds; for example, without limitation, highly fluorinated fluoroalkanes. In addition, the compounds of the invention have a de minimus number, if any, of N—H and O—H bonds.Type: ApplicationFiled: September 22, 2003Publication date: April 22, 2004Inventors: Olivier Arnoud, Marc Moroni, Stephane Roux
-
Publication number: 20040072881Abstract: Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.Type: ApplicationFiled: October 28, 2002Publication date: April 15, 2004Inventors: Jeffrey A. Robl, Joseph A. Tino, Andres S. Hernandez, Jun Li
-
Patent number: 6713498Abstract: Provided, among things, is a method of decreasing intraocular pressure in an animal, including a human, comprising administering an intraocular pressure decreasing amount of a compound of the formula I:Type: GrantFiled: May 30, 2002Date of Patent: March 30, 2004Assignee: Alteon IncorporatedInventor: Martin Gall
-
Patent number: 6686363Abstract: This invention relates to new oxazolidinones having a cyclopropyl moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and enterococci, Bacteroides spp., Clostridia spp. species, as well as acid-fast organisms such as Mycobacterium tuberculosis and other mycobacterial species. The compounds are represented by structural formula I: its enantiomer, diastereomer, or pharmaceutically acceptable salt or ester thereof.Type: GrantFiled: November 27, 2002Date of Patent: February 3, 2004Assignee: Kyorin Pharmaceutical Co., Ltd.Inventor: Yasumichi Fukuda
-
Patent number: 6673820Abstract: The invention relates to novel compounds of the general formula: in which R1 is hydrogen, halogen, C1-C6alkyl, C1-C6alkoxy, C1-C6haloalkyl or unsubstituted or mono- to pentasubstituted phenyl, where the substituents are selected from the group consisting of C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, aryloxy, halogen, cyano and nitro, where, if the number of substituents exceeds 1, the substituents can be identical or different; R2 is hydrogen, C1-C6alkyl, (C1-C6alkylene)phenyl, pyridyl, COOR6, CONR7R8, COR6, allyl or CH2—O—R6; R3 is unsubstituted or substituted heterocyclyl, where the substituents are in each case selected from the group consisting of unsubstituted or substituted phenyl, where the substituents are selected from the group consisting of C1-C6alkyl, C1-C6alkoxy, halogen, cyano and nitro, where, if the number of substituents exceeds 1, the substituents can be identical or different, benzyl, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, aryloxy, halogen, cyano, hydroxyl, amiType: GrantFiled: May 31, 2002Date of Patent: January 6, 2004Assignee: Novartis Animal Health US, Inc.Inventors: Pierre Ducray, Jacques Bouvier, Maurizio Schwarzenbach
-
Patent number: 6656911Abstract: The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.Type: GrantFiled: April 18, 2002Date of Patent: December 2, 2003Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W Spruce
-
Patent number: 6656910Abstract: The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.Type: GrantFiled: August 10, 2001Date of Patent: December 2, 2003Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
-
Patent number: 6635634Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.Type: GrantFiled: February 14, 2002Date of Patent: October 21, 2003Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
-
Patent number: 6630506Abstract: Acyl guanidines are provided which are sodium/proton exchange (NHE) inhibitors which have the structure wherein n is 0 to 4; X is a bond, O, S, SO, SO2, CO, or NR7; Y is a bond, O, S, SO, SO2, CO, or NR7′ wherein at least one of X and Y is other than a bond; and R1, R2, R3, R4, R5, R6, R7 and Ra, Rb, Rc, Rd are as defined herein, and are useful as antianginal, cardioprotective agents, antiischemic agents, and agents for peripheral vascular disease including intermittent claudication. In addition, a method is provided for preventing or treating angina pectoris, cardiac dysfunction, myocardial necrosis, arrhythmia, peripheral vascular diseases (PVD), including peripheral atherosclerotic disease (PAD), including intermittent claudication, Raynaud's diseases, and LeRiches Syndrome, pain, parethesia or discomfort in the lower limb and gluteal regions produced by vascular (e.g.Type: GrantFiled: April 21, 2000Date of Patent: October 7, 2003Assignee: Bristol-Myers Squibb Co.Inventors: Sundeep Dugar, Steven V. O'Neil
-
Patent number: 6620767Abstract: The invention relates to compounds of the general formula wherein R1 is hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-haloalkyl or unsubstituted or mono- to penta-substituted phenyl, whereby the substituents are selected from the group comprising C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, aryloxy, halogen, cyano and nitro, whereby if the number of substituents is greater than 1, the substituents may be identical or different; R2 is hydrogen, C1-C6-alkyl, (C1-C6-alkylene)phenyl, pyridyl, COOR6, CONR7R8COR6, allyl or CH2—O—R6; R3 is C1-C6-alkyl; R4 is unsubstituted or substituted phenyl, unsubstituted or substituted benzyl or unsubstituted or substituted heterocyclyl, whereby each of the substituents, independently of each other, is selected from the group comprising C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, aryloxy, halogen, cyano, hydroxy, amino and nitro, whereby if the number of substituents is greater than 1, the substituents may be identical or different; R6 is C1-C6Type: GrantFiled: May 28, 2002Date of Patent: September 16, 2003Assignee: Novartis Animal Health US, Inc.Inventors: Pierre Ducray, Jacques Bouvier
-
Publication number: 20030162819Abstract: The present invention is directed to novel 1,2,4-thiadiazol-2-ium derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.Type: ApplicationFiled: November 4, 2002Publication date: August 28, 2003Inventors: Magdalena Eisinger, Louis J. Fitzpatrick, Daniel H. Lee, Kevin Pan, Carlos Plata-Salaman, Allen B. Reitz, Virginia L. Smith-Swintosky, Boyu Zhao
-
Patent number: 6610707Abstract: Compounds of the formula: wherein R1, Y, W, A and R2 are as defined above are inhibitors of rotamase enzymes in particular FKBP-12 and FKBP-52. The compounds therefore moderate neuronal regeneration and outgrowth and can be used for treating neurological disorders arising from neurodegenerative diseases and nerve damage.Type: GrantFiled: September 1, 1999Date of Patent: August 26, 2003Assignee: Pfizer Inc.Inventors: David John Bull, Robert John Maguire, Michael John Palmer, Martin James Wythes
-
Patent number: 6608175Abstract: Certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of serine proteases, are prepared in various embodiments using Grignard reagents and alkyllithium reagents and various aldehydes to make oxadiazole, thiadiazole and triazole peptoid alcohols, which are then oxidized to the desired keto products.Type: GrantFiled: November 16, 2001Date of Patent: August 19, 2003Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
-
Patent number: 6605630Abstract: The invention concerns a compound of the formula (I): wherein, for example: T is of the formula (IA), (IB), or (IC); R1 is of the formula —NHC(═O)Rb wherein Rb is (1-4C)alkyl; R2 and R3 are hydrogen or fluoro; >A—B— is >C═CH— (but not when T is (IA)) or >CH—CH2—; wherein when T is of the formula (IA) or (IB); R6 is, for example, (1-4C)alkyl; R5 is hydrogen, R10CO—, R10SO2— or R10CS— wherein R10 is, for example, optionally substituted phenyl, or (1-10C)alkyl, or when T is of the formula (IA), (IB); or (IC): R5 and R6 are linked to give a 5- or 6-membered ring which is fused to the ring shown in (IA), (IB), or (IC) so as to give an optionally substituted bicyclic ring; and pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them, and their use as antibacterial agents.Type: GrantFiled: February 18, 2000Date of Patent: August 12, 2003Assignee: Syngenta LimitedInventor: Michael Barry Gravestock
-
Publication number: 20030143422Abstract: Organic materials based on [5] helicenes or dibenzofluorenes are shown to have excellent properties for use in electroluminescent devices, including high stability and efficiency and low excimer formation. The materials may advantageously be adapted to have hole transport or electron transport capabilities in addition to emissive properties.Type: ApplicationFiled: December 12, 2001Publication date: July 31, 2003Inventor: Jian Ping Chen
-
Patent number: 6589914Abstract: The dihalopropene compounds of the general formula (I) have excellent insecticidal/acaricidal activity, so that they are satisfactorily effective for the control of noxious insects, mites and ticks.Type: GrantFiled: March 4, 2002Date of Patent: July 8, 2003Assignee: Sumitomo Chemical Company, LimitedInventors: Noriyasu Sakamoto, Sanshiro Matsuo, Masaya Suzuki, Taro Hirose, Kazunori Tsushima, Kimitoshi Umeda
-
Publication number: 20030105071Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various mammalian cellular receptors, including G-protein coupled receptors. A third aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for mammalian dopamine, muscarinic or serotonin receptors or transporters. Another aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for mammalian dopamine, muscarinic or serotonin receptors.Type: ApplicationFiled: April 12, 2002Publication date: June 5, 2003Inventors: Gregory D. Cuny, James R. Hauske, Michele L.R. Heffernan, Joanne M. Holland, Paul E. Persons, Heike Radeke
-
Patent number: 6569876Abstract: The present invention is directed to novel inhibitors and methods for inhibiting serine elastases. These compounds and methods achieve a novel approach to enzyme inhibition; namely, balanced inhibition of a plurality of serine elastases. Balanced inhibition of a plurality of elastases offers a novel approach to therapeutic treatment of diseases that involve abnormal activities of a plurality of elastases resulting in pathological changes such as occur in inflammatory and vascular conditions. These pathological changes are not limited to the breakdown of elastin but may include the processing of other proteins by serine elastases which in turn results in adverse effects. The opportunity of targeting a plurality of enzymes using single inhibitor offers therapeutic advantages over administering multiple therapeutic against where each agent has a single specificity for an individual target enzyme.Type: GrantFiled: June 19, 2000Date of Patent: May 27, 2003Inventor: John C. Cheronis
-
Patent number: 6559100Abstract: Substituted 2-benzoylcyclohexane-1,3-diones of the formula I where: R1 and R2 are each hydrogen, mercapto, nitro, halogen, cyano, thiocyanato, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C2-C6-alkenyl, C2-C6-alkynyl, —OR3, —OCOR3, —OSO2R3, —S(O)nR3, —SO2OR3, —SO2N(R3)2, —NR3SO2R3 or —NR3COR3; R3 is hydrogen, C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, phenyl or phenyl-C1-C6-alkyl; where the abovementioned alkyl radicals may be partially or fully halogenated and/or may carry one to three of the following groups: hydroxyl, mercapto, amino, cyano, R3, —OR3, —SR3, —N(R3)2, ═NOR3, —OCOR3, —SCOR3, —NR3COR3, —CO2R3, —COSR3, —CON(R3)2, C1-C4-alkyliminooxy, C1-C4-alkoxyamino, C1-C4-alkylcarbonyl, C1-C4-alkoxy-C2-C6-alkoxycarbonyl, C1-C4-alkylsulfonyl, heterocyclyl, heterocyclyloxy, phenyl, benzyl, hetaryl, phenoxy, benzyloxy and hetaryloxy, where the eight last mentioned radicType: GrantFiled: February 7, 2000Date of Patent: May 6, 2003Assignee: BASF AktiengesellschaftInventors: Stefan Engel, Joachim Rheinheimer, Ernst Baumann, Wolfgang von Deyn, Regina Luise Hill, Guido Mayer, Ulf Misslitz, Oliver Wagner, Matthias Witschel, Martina Otten, Helmut Walter, Karl-Otto Westphalen
-
Patent number: 6525086Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, X, T, Q, Z, U, Y, Ar, p and n are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).Type: GrantFiled: March 14, 2001Date of Patent: February 25, 2003Assignee: Novo Nordisk A/SInventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
-
Patent number: 6500950Abstract: Benzylidenepyrazolones of the formula I, where the substituents and the index n have the following meanings: R1 is unsubstituted or substituted C1-C6-alkyl; R2 is unsubstituted or substituted C1-C6-alkyl, unsubstituted or substituted C1-C6-alkoxy, halogen, nitro, cyano; R3 is hydrogen, halogen, nitro, cyano, a group NR5R6, OCOR5, NR5COR6, CO2R5, —COSR5, —CONR5R6, C1-C4-alkoxyiminoalkyl, C1-C6-alkylcarbonyl, unsubstituted or substituted C1-C6-alkyl, unsubstituted or substituted C1-C6-alkoxy, unsubstituted or substituted C1-C6-alkylthio, unsubstituted or substituted C2-C6-alkenyl, unsubstituted or substituted C2-C6-alkynyl, unsubstituted or substituted phenyl, unsubstituted or substituted phenoxy, an unsubstituted or substituted 5- or 6-membered saturated or unsaturated heterocycle which may contain up to 4 nitrogen atoms and/or up to 2 oxygen or sulfur atoms as ring members; R4 is C1-C6-alkyl, C1-C4-haloalkyl; R3 and R4 form an optionally substituted saturated or unsaturatedType: GrantFiled: January 22, 2001Date of Patent: December 31, 2002Assignee: BASF AktiengesellschaftInventors: Joachim Rheinheimer, Matthias Witschel, Stefan Engel, Ernst Baumann, Wolfgang von Deyn, Regina Luise Hill, Guido Mayer, Ulf Misslitz, Oliver Wagner, Martina Otten, Karl-Otto Westphalen, Helmut Walter
-
Patent number: 6495546Abstract: Propanolamine derivatives represented by the following formula (I): These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.Type: GrantFiled: November 22, 2000Date of Patent: December 17, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
-
Publication number: 20020165255Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.Type: ApplicationFiled: October 19, 2001Publication date: November 7, 2002Inventors: Kimberly O. Cameron, Bruce A. Lefker, Robert L. Rosati
-
Patent number: 6468977Abstract: Novel 1,2,4-thiadiazole compounds are provided, which are effective as inhibitors of cysteine activity-dependent enzymes and in particular of cysteine proteases. The compounds are useful in treating acne by inhibition of transglutaminase, common cold by inhibition of human rhinovirus 3C protease and inflammatory joint disease by inhibition of cathepsins. The compounds of the present invention are 3,5-disubstituted 1,2,4-thiadazole of the general formula (I): where Z is a nitrogen containing group with recognition sequence for the enzyme and Y is a substituent that tunes the reactivity of the inhibitor towards the thiol group of the cysteine activity-dependent enzyme. The Y group may also serve in recognition.Type: GrantFiled: May 23, 2000Date of Patent: October 22, 2002Assignee: Apotex Inc.Inventors: Khashayar Karimian, Tim Fat Tam, Regis C. S. H. Leung-Toung, Wanren Li, Steve Patrick Bryson, Jolanta Maria Wodzinska
-
Patent number: 6448201Abstract: Benzoylcyclohexanediones and benzoylpyrazoles, their preparation and their use as herbicides and plant growth regulators. There are described benzoyl compounds of the formula (I), their preparation and their use as herbicides and plant growth regulators. In this formula (I), R1, R2, R3 and R4 are various radicals, X is an alkylene chain which may contain a hetero atom and Het is a heterocycle or heteroaromatic ring.Type: GrantFiled: November 2, 2000Date of Patent: September 10, 2002Assignee: Aventis CropScience GmbHInventors: Thomas Seitz, Lothar Willms, Thomas Auler, Hermann Bieringer, Felix Thürwächter
-
Color-developing agent, silver halide photographic light-sensitive material and image-forming method
Publication number: 20020102489Abstract: There is disclosed a novel color-developing agent of a 1,2,4-thiadiazol-5-yl hydrazine type. There is also disclosed a silver halide photographic light-sensitive material which gives sufficient color formation by development and forms an image excellent in image quality and image storability, by using the color-developing agent. Further, there is disclosed an image-forming method using the light-sensitive material.Type: ApplicationFiled: June 25, 2001Publication date: August 1, 2002Inventors: Osamu Uchida, Yasuhiro Ishiwata, Kiyoshi Takeuchi, Taiji Katsumata, Takashi Nakamura -
Publication number: 20020082267Abstract: The invention provides fungicidal compounds of formula I and salts thereof: 1Type: ApplicationFiled: August 6, 2001Publication date: June 27, 2002Applicant: Aventis CropScience S.A.Inventors: Vincent Gerusz, Darren James Mansfield, Joseph Perez, Jean-Pierre Vors
-
Patent number: 6403622Abstract: Novel phenylacetic acid heterocyclyl amides of the formula in which R1, R2, R3, R4, A, X and n are as defined in the description, a process for preparing these novel compounds and their use for controlling undesirable microorganisms and animal pests. Novel intermediates of the formula and a plurality of processes for their preparation.Type: GrantFiled: April 27, 2001Date of Patent: June 11, 2002Assignee: Bayer AktiengesellschaftInventors: Markus Heil, Hans-Christian Militzer, Thomas Bretschneider, Bernd Alig, Astrid Mauler-Machnik, Klaus Stenzel, Ulrike Wachendorff-Neumann
-
Patent number: 6392052Abstract: 3-[N′-(benzoyl)thioureido]-5-substituted-1,2,4-thiadiazoles are debenzoylated in an aqueous KOH solution. This process provides the 5-substituted-3-thioureido-1,2,4-thiadiazoles in unexpectedly high yield and purity as compared to similar processes employing NaOH.Type: GrantFiled: February 27, 2001Date of Patent: May 21, 2002Assignee: The Procter & Gamble CompanyInventor: Joseph Kofi Agyin
-
Publication number: 20020052510Abstract: This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.Type: ApplicationFiled: December 3, 1998Publication date: May 2, 2002Inventors: GREGORY S. HAMILTON, MARK H. NORMAN, YONG-QIAN WU
-
Patent number: 6358980Abstract: Compounds of the formula: useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.Type: GrantFiled: January 27, 2000Date of Patent: March 19, 2002Assignee: American Cyanamid CompanyInventors: Jeremy I. Levin, Aranapakam M. Venkatesan, James M. Chen, Arie Zask, Vincent P. Sandanayaka, Mila T. Du, Jannie L. Baker
-
Publication number: 20020016471Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: ApplicationFiled: March 16, 2001Publication date: February 7, 2002Inventors: Francesco Salituro, Guy Bemis, John Cochran
-
Publication number: 20020002193Abstract: Disclosed is a novel class of thiazole, thiadiazole, and oxadiazole compounds which are substituted at their nuclear carbons by aromatic moieties. These compounds exhibit antifungal activity against a variety of fungi including strains which have proven to be resistant to treatment with known antifungal agents such as Fluconazole.Type: ApplicationFiled: December 5, 2000Publication date: January 3, 2002Inventors: Dingwei Tim Yu, Orest Taras Macina, Ila Sircar, Jagadish Chandra Sircar, Christopher Mark Riviello
-
Patent number: 6331537Abstract: This invention relates to novel N-heteorocyclic carboxylic acids and carboxylic acid isosteres, their preparation and use for treating neurological disorders including physically damaged nerves and neurodengenerative diseases, for treating alopecia and promoting hair growth, for treating vision disorders and/or improving vision, and for treating memory impairment and/or enhancing memory performance by administering such compounds.Type: GrantFiled: December 2, 1999Date of Patent: December 18, 2001Assignee: GPI Nil Holdings, Inc.Inventors: Gregory S. Hamilton, Mark H. Norman, Yong-Qian Wu
-
Patent number: 6329373Abstract: A compound of formula (I) wherein X is a —CONHOH group and the R groups are defined in the claims. The compounds are inhibitors of matrix metalloproteinases involved in tissue degradation and inhibitors of the release of tumour necrosis factor from cells.Type: GrantFiled: January 7, 2000Date of Patent: December 11, 2001Assignee: British Biotech Pharmaceuticals, Ltd.Inventors: Fionna Mitchell Martin, Christopher Norman Lewis, Mark Whittaker
-
Patent number: 6329421Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: February 25, 1997Date of Patent: December 11, 2001Assignee: Merck Frosst Canada & Co.Inventors: Petpiboon Prasit, Daniel Guay, Zhaoyin Wang, Serge Leger, Michel Therien
-
Patent number: 6323227Abstract: This invention relates to compounds of formula which inhibit Factor Xa, to pharmaceutical compositions containing the compounds, and to the use of the compounds for the treatment of patients suffering from conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.Type: GrantFiled: February 26, 1999Date of Patent: November 27, 2001Assignee: Aventis Pharmaceuticals Products Inc.Inventors: Scott I. Klein, Kevin R. Guertin, Alfred P. Spada, Heinz W. Pauls, Yong Gong, Daniel G. McGarry