Sulfur Containing Patents (Class 564/154)
  • Patent number: 7341715
    Abstract: The preparation for permanently deforming hair has a pH of 6.5 to 9.5 and contains, as keratin-reducing agent, a 2-mercaptopropion-amide of the formula (I): in which R1 and R2, independently of one another, represent H, a linear or branched alkylaminoalkyl group with 2 to 8 carbon atoms, or a morpholinoalkyl group with 2 to 3 carbon atoms in the alkyl portion of the morpholinoalkyl group, with the proviso that R1 and R2 are not simultaneously H, or that R1 and R2, together with the nitrogen atom, form a five-or six-membered heterocyclic ring, which optionally contain an additional N or O and are optionally substituted with one or two OH and/or methyl groups.
    Type: Grant
    Filed: May 21, 2001
    Date of Patent: March 11, 2008
    Assignee: Wella AG
    Inventors: Beate Dannecker, Ursus Schweizer, Guenther Lang, Regina Ortmann, Wolfgang Hanefeld
  • Patent number: 7307191
    Abstract: This present invention provides materials for use as solid or concentrated chemical precursors for the production of organic peroxy acids (peracids). Organic peroxy acids are formed using a precursor according to the invention when they are combined with hydrogen peroxide or a hydrogen peroxide precursor such as a percarbonate or a perborate in aqueous medium. Organic peroxy acids, such as peroxyacetic acid, are used currently to disinfect medical equipment such as endoscopes and related items.
    Type: Grant
    Filed: March 16, 2004
    Date of Patent: December 11, 2007
    Assignee: OH Technologies LLP
    Inventors: David W. Hobson, Danny O. Helton
  • Patent number: 7297817
    Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein Ar, X, Y, R1, R2, R3, and q are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness, promotion of wakefulness, treatment of Parkinson's disease, cerebral ischemia, stroke, sleep apneas, eating disorders, stimulation of appetite and weight gain, treatment of attention deficit hyperactivity disorder (“ADHD”), enhancing function in disorders associated with hypofunctionality of the cerebral cortex, including, but not limited to, depression, schizophrenia, fatigue, in particular, fatigue associated with neurologic disease, such as multiple sclerosis, chronic fatigue syndrome, and improvement of cognitive dysfunction.
    Type: Grant
    Filed: April 12, 2005
    Date of Patent: November 20, 2007
    Assignees: Cephalon France, Cephalon, Inc.
    Inventors: Brigitte Lesur, Philippe Louvet, Rabindranath Tripathy
  • Patent number: 7288262
    Abstract: Compositions, in particular cosmetic compositions, comprising a cyclohexane-based compound defined by formula (I): wherein: R, which may be identical or different, are each chosen from hydrogen atoms and linear and branched, saturated hydrocarbons comprising 1 to 6 carbon atoms; Y, which may be identical or different, are each chosen from —CO—S—R? groups, —CO—NHR? groups, NH—COR? groups and —S—COR? groups, wherein R?, which may be identical or different, are each chosen from hydrogen atoms, aryl groups, optionally substituted with at least one hydrocarbon comprising 1 to 22 carbon atoms, wherein said hydrocarbon is chosen from linear and branched, saturated and unsaturated hydrocarbons, and linear, branched and cyclic, saturated and unsaturated hydrocarbons comprising 1 to 22 carbon atoms, wherein said hydrocarbons may optionally be substituted with at least one group chosen from aryl groups, ester groups, amide groups and urethane groups; wherein said hydrocarbons may optionally comprise at least on
    Type: Grant
    Filed: September 20, 2000
    Date of Patent: October 30, 2007
    Assignee: L'Oreal S.A.
    Inventor: Aude Livoreil
  • Patent number: 7256192
    Abstract: The present invention relates to an aromatic diamide derivative represented by the general formula (I): [A1 is optionally substituted (C1-C8)alkylene group, (C3-C8)alkenylene group or the like, B is —O— or —N(R4)— (wherein R4 is H, (C1-C6)alkyl, halo(C1-C6)alkyl or the like), R1 is H, (C1-C6)alkyl, optionally substituted phenyl, optionally substituted heterocyclic group, or the like, R2 and R3 are each H, (C3-C6)cycloalkyl or —A2—R8 (A2 is —C(?O)—, —C(?S)— or —C(?NR9)—, R8 and R9 are each H, (C1-C6)alkyl or the like), Q1 to Q5 are each carbon or nitrogen, X and Y are each halogen, cyano, nitro, (C3-C6)cycloalkyl, optionally substituted phenyl, optionally substituted heterocyclic group, or the like, n is 0 to 4, m is 1 to 5, and Z1 and Z2 are each O or S] or a salt thereof, an agricultural and horticultural chemical, and a usage of the chemical.
    Type: Grant
    Filed: December 22, 2000
    Date of Patent: August 14, 2007
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Masanori Tohnishi, Eiji Kohno, Hayami Nakao, Tateki Nishida, Takashi Furuya, Toshiaki Shimizu, Akira Seo, Kazuyuki Sakata, Shinsuke Fujioka
  • Patent number: 7169760
    Abstract: The present invention discloses novel peptide compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
    Type: Grant
    Filed: July 19, 2001
    Date of Patent: January 30, 2007
    Assignees: Schering Corporation, Dendreon Corporation
    Inventors: Anil K. Saksena, Viyyoor Moopil Girijavallabhan, Stephane L. Bogen, Raymond G. Lovey, Edwin Jao, Frank Bennett, Jinping L. Mc Cormick, Haiyan Wang, Russell E. Pike, Yi-Tsung Liu, Tin-Yau Chan, Zhaoning Zhu, Ashok Arasappan, Kevin X. Chen, Srinkanth Venkatraman, Tejal Parekh, Patrick A. Pinto, Bama Santhanam, F. George Njoroge, Ashit K. Ganguly, Henry A. Vaccaro, Scott Jeffrey Kemp, Odile Esther Levy, Marguerita Lim-Wilby, Susan Y. Tamura
  • Patent number: 7005549
    Abstract: This disclosure describes unique chemical structures for use as solid or concentrated chemical precursors to the production of peroxy acids when combined with hydrogen peroxide or a hydrogen peroxide precursor such as percarbonates or perborates. Peroxy acids (peracids) such as peroxyacetic acid are used currently to disinfect medical equipment such as endoscopes and related items. It has been discovered that these structures are not currently listed in Chemical Abstracts and do not appear to be the subject of any prior art related to this or any other similar application. The specification for this claim includes chemical structures for each claimed precursor as well as means of synthesis that could be carried our by any skilled synthetic organic chemist. Practical uses for this invention include several antimicrobial applications of which at least one example is included.
    Type: Grant
    Filed: January 6, 2004
    Date of Patent: February 28, 2006
    Inventors: David W. Hobson, Danny O. Helton
  • Patent number: 6974836
    Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.
    Type: Grant
    Filed: December 20, 2001
    Date of Patent: December 13, 2005
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Percy Carter, Robert Cherney
  • Patent number: 6972343
    Abstract: The invention concerns drug precursors with antimalarial effect, characterised in that it consists in quaternary bis-ammonium salts of general formula (I) wherein A and A?, identical or different, are respectively either a group A1 and A?1 of formula (1) wherein n=2 to 4; R?1 is hydrogen, C1-C5 alkyl, optionally substituted by an aryl, a hydroxy, an alkoxy, wherein the alkyl comprises 1 to 5 C, or aryloxy and W is halogen or a nucleofuge group; or a group A2 which represents formyl-CHO, or acetyl-COCH3.
    Type: Grant
    Filed: July 21, 2000
    Date of Patent: December 6, 2005
    Assignee: CNRS
    Inventors: Henri Vial, Marie-Laure Ancelin, Valerie Vidal, Michele Calas, Jean-Jacques Bourguignon, Eric Rubi
  • Patent number: 6888022
    Abstract: Disclosed are compounds which inhibit ?-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 ?-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: Grant
    Filed: February 20, 2001
    Date of Patent: May 3, 2005
    Assignees: Athena Neurosciences, Inc., Eli Lilly & Company
    Inventors: James E. Audia, Thomas C. Britton, James J. Droste, Beverly K. Folmer, George W. Huffman, Varghese John, Lee H. Latimer, Thomas E. Mabry, Jeffrey S. Nissen, Warren J. Porter, Jon K. Reel, Eugene D. Thorsett, Jay S. Tung, Jing Wu, Clark Norman Eid, William Leonard Scott
  • Patent number: 6864383
    Abstract: This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.
    Type: Grant
    Filed: January 25, 2002
    Date of Patent: March 8, 2005
    Assignee: Merck & Co., Inc.
    Inventors: Maria L. Garcia, Gregory J. Kaczorowski, Ying-Duo Gao
  • Patent number: 6811833
    Abstract: A 4-membered compound is represented by the following formula (I) is disclosed (in the formula, X1 and X2 each independently represent an oxygen atom, a sulfur atom or a substituted or unsubstituted imino group, Y1 and Y2 each independently represent a single bond, an oxygen atom or a substituted or unsubstituted imino group, B1 and B2 each independently represent an optionally substituted aliphatic, aliphatic carbonyl, aromatic or aromatic carbonyl group having 1-20 carbon atoms, and A1 and A2 each independently represent a group represented by the following formula (II) (Ar1, Ar2 and Ar3 each independently represent a cyclic group having 5-14 carbon atoms, L1 and L2 each independently represent a single bond or a divalent linking group, and p represents an integer of 0-2)). There is also disclosed a birefringence medium containing a 4-membered compound represented by the formula (I) and an optical element comprising the birefringence medium.
    Type: Grant
    Filed: September 17, 2002
    Date of Patent: November 2, 2004
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Naoyuki Nishikawa, Kentaro Toyooka
  • Publication number: 20040192780
    Abstract: Compounds characterized generally as alkylaminoalkyl-terminated sulfide/sulfonyl-containing propargyl amino-diol derivatives are useful as renin inhibitors for the treatment of hypertension.
    Type: Application
    Filed: April 12, 2004
    Publication date: September 30, 2004
    Applicant: G.D. Searle & Co.
    Inventor: Gunnar J. Hanson
  • Publication number: 20040127747
    Abstract: The present invention relates to a process for direct and selective synthesis of mono-N-substituted functionalized anilines by using alkylating agents selected from the class of organic carbonates, preferably of the dialkyl, dibenzyl and diallyl types, in the presence of suitable catalysts that are chemically related to the class of aluminosilicates.
    Type: Application
    Filed: December 15, 2003
    Publication date: July 1, 2004
    Applicant: CONSORZIO INTERUNIVERSITARIO NAZIONALE "LA CHIMICA PER L'AMBIENTE"
    Inventors: Maurizio Selva, Pietro Tundo
  • Publication number: 20040054213
    Abstract: This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.
    Type: Application
    Filed: July 16, 2003
    Publication date: March 18, 2004
    Inventors: Maria L. Garcia, Gregory J. Kaczorowski, Ying-Duo Gao
  • Patent number: 6706763
    Abstract: O-anisamide compounds and their addition salts effective for the prevention and/or therapy of metabolic diseases such as hyperlipidemia and diabetes, in which peroxisome proliferator-activated receptor (PPAR) being intranuclear receptor, in particular, human PPAR participates, as agonistic drugs thereon, and processes for preparing them, wherein the o-anisamide compounds are represented by a general formula (1) [wherein R denotes a carboxyl group, carboxymethyl group or CH2CHXCOY (here X denotes a mercapto group or S(O)nMe (n=0, 1 or 2) and Y denotes an amino group or hydroxyl group)], their medicinally acceptable salts, and their hydrates.
    Type: Grant
    Filed: March 18, 2002
    Date of Patent: March 16, 2004
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Hiroya Satoh, Masakatsu Komuro, Koji Murakami, Katsuya Awano
  • Patent number: 6703379
    Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: March 12, 2001
    Date of Patent: March 9, 2004
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yukio Iino, Kohichi Fujita, Takashi Tsuji, Ariko Kodaira, Kenji Takehana, Tsuyoshi Kobayashi, Takashi Yamamoto
  • Publication number: 20040009982
    Abstract: The present invention relates to an aromatic diamide derivative represented by the general formula (I): 1
    Type: Application
    Filed: September 20, 2002
    Publication date: January 15, 2004
    Inventors: Masanori Tohnishi, Eiji Kohno, Hayami Nakao, Tateki Nishida, Takashi Furuya, Toshiaki Shimizu, Akira Seo, Kazuyuki Sakata, Shinsuke Fujioka
  • Publication number: 20030236201
    Abstract: Compounds characterized generally as alkylaminoalkyl-terminated sulfide/sulfonyl-containing propargyl amino-diol derivatives are useful as renin inhibitors for the treatment of hypertension.
    Type: Application
    Filed: June 18, 2003
    Publication date: December 25, 2003
    Applicant: G.D. Searle & Co.
    Inventor: Gunnar J. Hanson
  • Publication number: 20030187289
    Abstract: Novel biphenyl derivatives of the general formula (I), in which Y, R R1, R2, R3, R4, m, o and p are as defined in claim 1, and their physiologically acceptable salts and solvates are integrin inhibitors and can be employed for combating thrombosis, cardiac infarction, coronary heart disease, arteriosclerosis, inflammation, tumours, osteoporosis, infections aid restenosis after angioplasty or in pathological processes which are maintained or propagated by angiogenesis.
    Type: Application
    Filed: February 21, 2003
    Publication date: October 2, 2003
    Inventors: Wolfgang Stahle, Simon Goodman
  • Patent number: 6627774
    Abstract: Derivatives of N-deacetyl-thiocolchicine or of the isoster thereof of formula (I) wherein n is an integer from 0 to 8, Y is a CH2 group or, when n is 1, can also be a group of formula NH. Compounds of formula (I) have anti-proliferative activity.
    Type: Grant
    Filed: August 2, 2002
    Date of Patent: September 30, 2003
    Assignee: Indena S.p.A.
    Inventors: Ezio Bombardelli, Alessandro Pontiroli
  • Patent number: 6603044
    Abstract: The present invention provides a phthalamide derivative of the formula (I): wherein A1 is (substituted) C1-C8 alkylene, (substituted) C3-C8 alkenylene, (substituted) C3-C8 alkynylene, etc., R1 is H, (halo) C3-C6 cycloalkyl, (substituted) phenyl, (substituted) heterocycle, —A2—R4, etc., R2 and R3 are H, C3-C6 cycloalkyl, —A2—R4, etc., A2 is —C(═O)—, —C(═S)— or —C(═NR5)—, R4 is H, alkyl, (substituted) phenyl, (substituted) heterocycle, etc., X and Y are halogen, cyano, nitro, (halo) C1-C6 alkyl, (halo) C1-C6 alkoxy, etc., l is 0-4, m is 0-5, n is 0-2; and an agrohorticultural insecticide containing said compound as active ingredient and exhibiting an excellent insecticidal effect.
    Type: Grant
    Filed: November 29, 1999
    Date of Patent: August 5, 2003
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Masanori Tohnishi, Hayami Nakao, Eiji Kohno, Tateki Nishida, Takashi Furuya, Toshiaki Shimizu, Akira Seo, Kazuyuki Sakata, Shinsuke Fujioka, Hideo Kanno
  • Patent number: 6563002
    Abstract: The present invention discloses biscyclopropanecarboxamide compounds and pharmaceutically acceptable salts thereof; and also NF-kappa B activation inhibitors, Inflammatory cytokine production inhibitors, matrix metalloprotease production inhibitors, inflammatory cell adhesion molecules incidence inhibitors, antiinflammatory agents, antirheumatic agents, immunosuppressive agents, cancerous metastasis inhibitors or antiviral agents each containing such a compound as the active ingredient.
    Type: Grant
    Filed: March 1, 2002
    Date of Patent: May 13, 2003
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yukio Iino, Kohichi Fujita, Takashi Yamamoto, Kenji Takehana, Tsuyoshi Kobayashi
  • Publication number: 20030055287
    Abstract: The present invention provides a phthalic acid diamide derivative represented by the general formula (I) 1
    Type: Application
    Filed: January 4, 2002
    Publication date: March 20, 2003
    Inventors: Masanori Tohnishi, Hayami Nakao, Eiji Kohno, Tateki Nishida, Takashi Furuya, Toshiaki Shimizu, Akira Seo, Kazuyuki Sakata, Shinsuke Fujioka, Hideo Kanno
  • Patent number: 6514925
    Abstract: N,N diacyl O-substituted imide bleach activators and compositions employing them are provided. The activators have the general formula: wherein X is selected from O, NR16 and S; e is 0 or 1; f is 0 or 1; R16 is selected from H and C1-C4 linear or branched, saturated or unsaturated alkyl groups; and R1 is preferably phenyl or C7-C13 linear or branched chain, saturated or unsaturated alkyl; R2 is preferably C1-C10 branched or unbranched, saturated or unsaturated alkyl and R3 is preferably C1-C12 linear or branched chain, saturated or unsaturated alkyl. Bleach additive and bleaching compositions including the bleach activators and methods of cleaning fabrics are also provided.
    Type: Grant
    Filed: May 23, 2002
    Date of Patent: February 4, 2003
    Assignee: The Procter & Gamble Company
    Inventors: Gregory Scot Miracle, Robert Richard Dykstra
  • Publication number: 20030022935
    Abstract: The present invention relates to compounds of general formula (I), 1
    Type: Application
    Filed: February 13, 2002
    Publication date: January 30, 2003
    Inventors: Hartmut Strobel, Paulus Wohlfart
  • Patent number: 6506904
    Abstract: A method of preparing N,N-disubstituted 3,3′-dithiodipropionamide of formula (2) is provided. In the method, 3-mercaptopropi-onamide of formula (4) reacts with an aqueous solution of amine to prepare N-substituted-3-mercaptopropionamide of formula (3) and N-substituted-3-mercaptopropionamide reacts with an aqueous solution of hydrogen peroxide. In addition, a method of preparing substituted 3-isothiazolone is provided.
    Type: Grant
    Filed: May 21, 2002
    Date of Patent: January 14, 2003
    Assignee: SK Chemicals Co., Ltd.
    Inventors: Seung-Hwan Kim, Jeong-Ho Park, Jin-Man Kim, Soon-Jong Hahn, Ki-Seong Choi, Myung-Ho Cho
  • Patent number: 6500935
    Abstract: Specific novel compounds of aromatic bis-acetoamide structures are provided as intermediate compounds to forming different types of coloring agents, at least. Such compounds are useful as intermediates in the production of certain bis-acetoanilide azo dyes, pigments, and polymeric colorants. Such compounds facilitate production of such coloring agents that exhibit favorable tinctorial strength and intense color from orange to greenish yellow within and on different substrates and media. Coloring agents and methods of making such agents are encompassed within this invention as well.
    Type: Grant
    Filed: November 21, 2001
    Date of Patent: December 31, 2002
    Assignee: Milliken & Company
    Inventors: Jusong Xia, John W. Miley
  • Patent number: 6479701
    Abstract: A method of preparing N,N-disubstituted-3,3′-dithiodipropionamide of formula (2) is provided. In the method, 3-mercaptopropionamide of formula (4) reacts with an aqueous solution of amine to prepare N-substituted-3-mercaptopropionamide of formula (3) and N-substituted-3-mercaptopropionamide reacts with an aqueous solution of hydrogen peroxide. In addition, a method of preparing substituted 3-isothiazolone is provided.
    Type: Grant
    Filed: September 28, 2001
    Date of Patent: November 12, 2002
    Assignee: SK Chemicals Co., Ltd.
    Inventors: Seung-Hwan Kim, Jeong-Ho Park, Jin-Man Kim, Soon-Jong Hahn, Ki-Seung Choi, Myung-Ho Cho
  • Publication number: 20020160962
    Abstract: The present invention discloses novel peptide compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
    Type: Application
    Filed: July 19, 2001
    Publication date: October 31, 2002
    Inventors: Anil K. Saksena, Viyyoor Moopil Girijavallabhan, Stephane L. Bogen, Raymond G. Lovey, Edwin E. Jao, Frank Bennett, Jinping L. Mc Cormick, Haiyan Wang, Russell E. Pike, Yi-Tsung Liu, Tin-Yau Chan, Zhaoning Zhu, Ashok Arasappan, Kevin X. Chen, Srikanth Venkatraman, Tejal Parekh, Patrick A. Pinto, Bama Santhanam, F. George Njoroge, Ashit K. Ganguly, Henry A. Vaccaro, Scott Jeffrey Kemp, Odile Esther Levy, Marguerita Lim-Wilby, Susan Y. Tamura
  • Publication number: 20020137687
    Abstract: The present invention relates to compounds of the Formula 1
    Type: Application
    Filed: February 20, 2002
    Publication date: September 26, 2002
    Applicant: MORPHOCHEM AG
    Inventors: Lutz Weber, Thilo Fuchs, Katrin Illgen, Alexander Doemling, Michael Cappi
  • Patent number: 6455502
    Abstract: The present invention relates to novel N-cyanomethyl amides which are cysteine protease inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
    Type: Grant
    Filed: March 15, 2000
    Date of Patent: September 24, 2002
    Assignee: AXYS Pharmaceuticals, Inc.
    Inventors: Clifford M. Bryant, Barry A. Bunin, Erica A. Kraynack, John W. Patterson
  • Patent number: 6452052
    Abstract: Methods and compositions for preventing or treating allergic diseases of the eye, nose, skin, ear, gastrointestinal tract, airways or lung and preventing or treating manifestations of systemic mastocytosis are disclosed. The compositions contain a mast cell stabilizing disulfide derivative as an active ingredient.
    Type: Grant
    Filed: January 31, 2002
    Date of Patent: September 17, 2002
    Assignee: Alcon Universal Ltd.
    Inventors: Mark R. Hellberg, Zixia Feng, Steven T. Miller
  • Patent number: 6426435
    Abstract: Substantive UV-absorbing water-soluble quaternary salts of cinnamidoalkylamine of formula I. Hair, skin and fabric care compositions containing the compounds of formula I; wherein R1 represents up to four substituents, same or different, selected from H, halo, —OH, —NH2, —NO2, —OCH3, —N(CH3)2, alkyl groups containing up to 6 carbon atoms, alkoxy groups containing up to 6 carbon atoms, alkylamino or N,N-dialkylamino groups containing up to 6 carbon atoms; R2 is selected from hydrogen, alkyl group containing up to 6 carbon atoms; R3 and R4 are independently selected from benzyl, alkyl group containing up to 6 carbon atoms; n is an integer from 1 to 6; m is an integer from 1 to 10; X− is a counter anion of quaternary centres selected from halides including chloride, bromide, iodide and methane sulphonate and its derivatives such as trifluoro methane sulphonate, benzene sulphonates including its p-bromo, nitro and methyl derivative.
    Type: Grant
    Filed: July 31, 2001
    Date of Patent: July 30, 2002
    Assignee: Galaxy Surfactants Ltd.
    Inventors: Nirmal Madhukar Koshti, Arun Harchandra Jawale, Bharat Bhikaji Parab, Shubhangi Dattaram Naik, Manasi Dattatraya Moghe, Tanaji Shamrao Jadhav, Subhash Shivling Nashte
  • Patent number: 6426365
    Abstract: The present invention provides a CETP activity inhibitor comprising as an active ingredient a compound represented by the formula (I): wherein R represents a straight chain or branched alkyl group; a straight chain or branched alkenyl group; a lower haloalkyl group; a substituted or unsubstituted cycloalkyl group; a substituted or unsubstituted cycloalkenyl group; a substituted or unsubstituted cycloalkylalkyl group; a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group, X1, X2, X3, and X4 may be the same or different and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower haloalkyl group; a lower alkoxy group; a cyano group; a nitro group; an acyl group; or an aryl group, Y represents —CO— or —SO2—, and Z represents a hydrogen atom or a mercapto-protecting group, or a prodrug compound, a pharmaceutically acceptable salt, or hydrate or solvate thereof.
    Type: Grant
    Filed: December 23, 1999
    Date of Patent: July 30, 2002
    Assignee: Japan Tobacco Inc.
    Inventors: Hisashi Shinkai, Kimiya Maeda, Hiroshi Okamoto
  • Patent number: 6420427
    Abstract: An aminobutyric acid derivative of the formula (I): (wherein all symbols are as defined in the specification) and salt thereof. salt thereof. The compounds of the formula (I) possess an inhibitory activity on matrix metalloproteinase and are useful for prevention and/or treatment of diseases, for example, rheumatoid diseases, arthrosteitis, unusual bone resorption, osteoporosis, periodontitis, interstitial nephritis, arteriosclerosis, pulmonary emphysema, cirrhosis, cornea injury, metastasis of, invasion of or growth of tumor cells, autoimmune disease (e.g. Crohn's disease, Sjogren's syndrome), disease caused by vascular emigration or infiltration of leukocytes, arterialization, multiple sclerosis, aorta aneurysm, endometriosis.
    Type: Grant
    Filed: April 7, 2000
    Date of Patent: July 16, 2002
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Kanji Takahashi, Tsuneyuki Sugiura
  • Publication number: 20020082440
    Abstract: This invention relates to a method of preparing a compound type where at least one of R′ or R″ is a carboxyl group (I) by treating a compound of formula (II) with a Group I(a) or Group II(a) metal halide, with an aprotic dipolar amide-based solvent and water.
    Type: Application
    Filed: November 8, 2001
    Publication date: June 27, 2002
    Applicant: SmithKline Beecham Corporation
    Inventors: Kevin Webb, Wilford Mendelson, Jianhao Chen
  • Patent number: 6403648
    Abstract: Compounds characterized generally as alkylaminoalkyl-terminated &bgr;-alanineamide amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula wherein n is two or three; wherein x is a number selected from zero, one and two; wherein R2 is selected from hydrido, methyl, ethyl and phenyl; wherein R3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, napthylmethyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R5 is methyl; wherein R7 is cyclohexylmethyl; wherein R8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl; and wherein each of R9 and R10 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: January 17, 2001
    Date of Patent: June 11, 2002
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran, Barbara B. Chen
  • Patent number: 6365653
    Abstract: Nonblack elastomers, which have excellent stability against oxidative, light- or ozone-induced degradation, comprise as stabilizers at least one compound of formula I wherein R1 is hydrogen, C1-C12alkyl, cyclohexyl, phenyl or benzyl, R2 is hydrogen or C1-C4alkyl, and n is the number 0, 1 or 2. The compounds of formula I are excellently suitable as colour-stable and nonstaining stabilizers and antiozonants for protecting nonblack elastomers against oxidative, thermal, light- or ozone-induced degradation.
    Type: Grant
    Filed: October 27, 2000
    Date of Patent: April 2, 2002
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Hans-Rudolf Meier, Gerrit Knobloch
  • Publication number: 20020010214
    Abstract: Compounds characterized generally as alkylaminoalkyl-terminated sulfide/sulfonyl-containing propargyl amino-diol derivatives are useful as renin inhibitors for the treatment of hypertension.
    Type: Application
    Filed: August 16, 2001
    Publication date: January 24, 2002
    Applicant: G.D. Searle & Co.
    Inventor: Gunnar J. Hanson
  • Patent number: 6307101
    Abstract: Disclosed are novel inhibitors of metalloproteases, in particular matrix metalloproteases. The disclosed inhibitors are mercaptoketone and mercaptoalcohol compounds which are useful in pharmaceutical compositions and methods for treating or controlling disease states or conditions which involve tissue breakdown, for example, arthropathy, dermatological conditions, bone resorption, inflammatory diseases, and tumor invasion and in the promotion of wound healing.
    Type: Grant
    Filed: March 17, 1999
    Date of Patent: October 23, 2001
    Inventors: David A. Campbell, Dinesh V. Patel, Xiao-Yi Xiao
  • Patent number: 6291413
    Abstract: N,N diacyl O-substituted imide bleach activators and compositions employing them are provided. Bleach additive and bleaching compositions including the bleach activators and methods of cleaning fabrics are also provided.
    Type: Grant
    Filed: May 10, 2000
    Date of Patent: September 18, 2001
    Assignee: The Procter & Gamble Company
    Inventors: Gregory Scot Miracle, Robert Richard Dykstra
  • Patent number: 6258851
    Abstract: Compounds of formula (I), wherein A, B, X, R1, R2, R3, R4, R5, R6 are as defined in the specification, are matrix metalloproteinase inhibitors.
    Type: Grant
    Filed: October 8, 1999
    Date of Patent: July 10, 2001
    Assignee: British Biotech Pharmaceuticals Limited
    Inventors: Christopher David Floyd, Sanjay Ratilal Patel, Mark Whittaker
  • Patent number: 6235787
    Abstract: Hydrazine derivatives of the formula wherein Y is CO or SO2; R1 is lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl; R2 is lower alkyl, halo-lower alkyl, aryl-lower alkyl, aryl-lower alkenyl or aryl when Y is SO2 and is lower alkyl, halo-lower alkyl, lower alkoxy, lower alkoxycarbonyl, acyl, lower cycloalkyl, aryl, aryl-lower alkyl, aryl-lower alkoxy or NR5R6 when Y is CO; and R3 is hydrogen, lower alkyl optionally substituted by cyano, amino, hydroxy, lower alkoxy, lower alkoxycarbonyl, heterocyclyl or heterocyclylcarbonyl, lower alkenyl, lower alkynyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl-lower alkyl, aryl-lower alkenyl, aryl or heterocyclyl; or R2 and R3 together form the residue of a 5-, 6- or 7-membered cyclic amide, cyclic imide, cyclic sulphonamide or cyclic urethane group; R4 is lower alkyl, hydroxy-lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl or a group of the formula X-aryl, X-heteroar
    Type: Grant
    Filed: June 16, 1998
    Date of Patent: May 22, 2001
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael John Broadhurst, William Henry Johnson, Daryl Simon Walter
  • Patent number: 6218389
    Abstract: The invention provides compounds of formula as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
    Type: Grant
    Filed: July 31, 1998
    Date of Patent: April 17, 2001
    Assignee: The Procter & Gamble Co.
    Inventors: Neil Gregory Almstead, Roger Gunnard Bookland, Yetunde Olabisi Taiwo, Rimma Sandler Bradley, Rodney Dean Bush, Biswanath De, Michael George Natchus, Stanislaw Pikul
  • Patent number: 6201133
    Abstract: Disclosed are compound of formula I wherein R represents hydrogen, lower alkyl, cycloalkyl, bicycloalkyl, adamantyl, aryl, biaryl, or mono- or di-(cycloalkyl, aryl or biaryl)-lower alkyl, di-(lower alkyl or aryl-lower alkyl)amino-lower alkyl, or (piperidino, morpholino, pyrrolidino)-lower alkyl; R1 represents hydrogen, lower alkyl, cycloalkyl, aryl, biaryl, or (cycloalkyl, aryl or biaryl)-lower alkyl; R2 represents hydrogen, lower alkyl, lower alkoxy, aryl-lower alkyl, aryl-lower alkoxy, amino, mono- or di-(lower alkyl or aryl-lower alkyl)-amino, acylamino, or (lower alkyl or aryl-lower alkyl)-(thio, sulfinyl or sulfonyl); R3 represents hydrogen, lower alkyl, cycloalkyl, aryl-lower alkyl, cycloalkyl-lower alkyl, or C2-C7-alkyl interrupted by S, SO, SO2, O or N—R5; R4 represents hydrogen or acyl; R5 represents hydrogen, lower alkyl, aryl-lower alkyl, acyl, or (lower alkyl, aryl or aryl-lower alkyl)-sulfonyl; A together with the carbon to which it is attached forms a ring and repr
    Type: Grant
    Filed: November 8, 1999
    Date of Patent: March 13, 2001
    Assignee: Novartis AG
    Inventor: Cynthia A. Fink
  • Patent number: 6187812
    Abstract: Phenylacetic acid derivatives of the formula I where the substituents and the index have the following meanings: X is oxygen or sulfur; R is hydrogen or alkyl; R1 is hydrogen or alkyl; R2 is cyano, nitro, trifluoromethyl, halogen, alkyl or alkoxy; m is 0, 1 or 2, it being possible for the R2 radicals to be different if m is 2; R3 is hydrogen, cyano, nitro, hydroxyl, amino, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, alkylamino or dialkylamino; R4 is hydrogen, cyano, nitro, hydroxyl, amino, halogen, unsubstituted or substituted alkyl, alkoxy, alkylthio, alkylamino, dialkylamino, alkenyl, alkenyloxy, alkenylthio, alkenylamino, N-alkenyl-N-alkylamino, alkynyl, alkynyloxy, alkynylthio, alkynylamino, N-alkynyl-N-alkylamino; unsubstituted or substituted cycloalkyl, cycloalkoxy, cycloalkylthio, cycloalkylamino, N-cycloalkyl-N-alkylamino, cycloalkenyl, cycloalkenyloxy, cycloalkenylthio, cycloalkenylamino, N-cycloalkenyl-N-alkylamino, heterocyclyl, heterocyclyloxy, heterocycly
    Type: Grant
    Filed: February 3, 2000
    Date of Patent: February 13, 2001
    Assignee: BASF Aktiengesellschaft
    Inventors: Herbert Bayer, Hubert Sauter, Ruth Müller, Wassilios Grammenos, Albrecht Harreus, Reinhard Kirstgen, Franz Röhl, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 6184249
    Abstract: Substituted phenylalanines are provided comprising an hydantoin, urea or 2-hydroxyl, 2-methylpropionyl group, dimers thereof and alkyl, polyfluoroamido and haloarylamino derivatives thereof, as well as radiolabeled derivatives thereof. The compounds bind specifically to the androgen receptor and find use in the therapy of indications associated with the androgen receptor, such as, hirsutism, acne and androgenetic alopecia, and in the therapy and diagnosis of cell hyperplasia dependent on androgens.
    Type: Grant
    Filed: December 18, 1998
    Date of Patent: February 6, 2001
    Assignee: Biophysica, Inc.
    Inventors: Milos Sovak, Allen L. Seligson, James Gordon Douglass, III, Brian Campion, Jason W. Brown
  • Patent number: 6127414
    Abstract: There is provided pharmaceutically useful compounds of formula I, ##STR1## wherein Ar.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 have meanings given in the description, which are useful as antagonists of neuropeptide Y and in particular in the treatment of cardiovascular diseases, for example vasoconstriction.
    Type: Grant
    Filed: October 26, 1998
    Date of Patent: October 3, 2000
    Assignee: Astra Aktiebolag
    Inventors: Nils-.ANG.ke Bergman, Thomas D'Ambra, Garry M Pilling
  • Patent number: RE37873
    Abstract: Phenylacetic acid derivatives of the formula I
    Type: Grant
    Filed: April 16, 2001
    Date of Patent: October 8, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Herbert Bayer, Hubert Sauter, Ruth Müller, Wassilios Grammenos, Albrecht Harreus, Reinhard Kirstgen, Franz Röhl, Eberhard Ammermann, Gisela Lorenz