Polycyclo Ring System Patents (Class 562/461)
  • Patent number: 8865689
    Abstract: Methods and compositions for treating and/or preventing hyperuricemia or metabolic disorders associated with hyperuricemia comprising administering to a patient in need a therapeutically effective amount of diacerein, rhein, or a pharmaceutically acceptable salt, an analog, a prodrug, or an active metabolite thereof.
    Type: Grant
    Filed: March 7, 2012
    Date of Patent: October 21, 2014
    Assignee: TWi Biotechnology, Inc.
    Inventors: Mannching Sherry Ku, Chih-Kuang Chen, Wei-Shu Lu, I-Yin Lin
  • Patent number: 8541618
    Abstract: This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic derivatives and to methods of preparation.
    Type: Grant
    Filed: February 25, 2011
    Date of Patent: September 24, 2013
    Assignee: Bayer HealthCare LLC
    Inventors: Derek B. Lowe, Philip L. Wickens, Xin Ma, Mingbao Zhang, William H. Bullock, Philip D. G. Coish, Ingo A. Mugge, Andreas Stolle, Ming Wang, Yamin Wang, Chengzhi Zhang, Hai-Jun Zhang, Lei Zhu, Manami Tsutsumi, James N. Livingston
  • Publication number: 20120232044
    Abstract: Methods and compositions for treating and/or preventing hyperuricemia or metabolic disorders associated with hyperuricemia comprising administering to a patient in need a therapeutically effective amount of diacerein, rhein, or a pharmaceutically acceptable salt, an analog, a prodrug, or an active metabolite thereof.
    Type: Application
    Filed: March 7, 2012
    Publication date: September 13, 2012
    Applicant: TWi Biotechnology, Inc.
    Inventors: Mannching Sherry Ku, Chih-Kuang Chen, Wei-Shu Lu, I-Yin Lin
  • Publication number: 20120129929
    Abstract: A compound used to prevent diseases caused by aquaporin deficiency, which is 18?-Glycyrrhetinic acid derivative. Said compound can not only prevent diseases caused aquaporin deficiency, but be able to prevent aquaporin (AQP) production and enhance skin function. Since AQPs have many advantages in skin cells, e.g. promoting water and glycerine molecular transportation, increasing skin elasticity and cuticle moisture, increasing the cell proliferation and cell migration, aquaporin can promote skin bather function and wound cicatrization. Therefore, said compound can be applied potentially as a medicinal cosmetic in skin medicine cosmetology, or as a new medical composition to treat diseases caused by AQP abnormality, such as urine concentration defect, wound healing slow down, corneal re-epithelialization slow down and etc.
    Type: Application
    Filed: June 16, 2011
    Publication date: May 24, 2012
    Applicant: FU-JEN CATHOLIC UNIVERSITY
    Inventor: Chi-Feng Hung
  • Publication number: 20120070492
    Abstract: The invention relates to pharmaceutical compositions comprising rhein or diacerein or salts or esters or prodrugs thereof, optionally with one or more pharmaceutically acceptable excipients. The invention also relates to the methods for preparing such compositions.
    Type: Application
    Filed: September 13, 2008
    Publication date: March 22, 2012
    Inventors: Rahul Dabre, Girish Kumar Jain, Cyril Estanove, François Pruvost, Roshanlal Sandal, Prashant Mandaogade, Premchand Nakhat
  • Publication number: 20120041226
    Abstract: The present invention relates to an improved process of ozonolysis of carbon nanotubes assisted by water vapour. The improved methodology provides an eco-friendly, cheaper, practical and efficient approach to functionalize carbon nanotubes with oxygen-containing moieties for further chemical functionalization and composite dispersion.
    Type: Application
    Filed: February 27, 2010
    Publication date: February 16, 2012
    Applicant: BAYER MATERIALsCIENCE AG
    Inventors: Helmut Meyer, Stefan Bahnmüller, Julia Hitzbleck, Zhong Zhang, Lu-Qi Liu, Ke Peng, Hongchao Li
  • Publication number: 20110207705
    Abstract: Oviedomycin derivatives, method for obtaining same and use thereof. This invention relates to oviedomycin derivatives obtained by fermentation of recombinant bacterial strains. The invention also relates to the methods used to obtain the recombinant strains and to produce the oviedomycin derivatives. The invention further relates to bacterial strains that can be used to produce oviedomycin derivatives. Finally, said oviedomycin derivatives are applicable in the field of the human health, specifically to produce drugs for the treatment of tumour diseases.
    Type: Application
    Filed: March 26, 2009
    Publication date: August 25, 2011
    Applicant: UNIVERSIDAD DE OVIEDO
    Inventors: Carmen Méndez Fernández, Felipe Lombó Brugos, Alfredo A. Fernández Braña, José Antonio Salas Fernández
  • Publication number: 20110144170
    Abstract: The present invention provides compounds capable of binding to an Fc receptor and modulating Fc receptor activity comprising a core lipophilic group in the form of an Aryl zing substituted with a group rich in p-electrons. The invention further provides for a method of treating an autoimmune disease involving Fc receptor activity using such compounds. A method for obtaining a compound which modulates Fc receptor activity is also provided, the method comprising: (a) providing or designing compounds having structural characteristics to fit in the groove of the Fc?RIIa structure; and (b) screening the compounds for modulating activity on the Fc receptor.
    Type: Application
    Filed: February 18, 2011
    Publication date: June 16, 2011
    Inventors: Mark Phillip Hogarth, Geoffrey Allan Pietersz, Gerard Peter Moloney
  • Publication number: 20100249231
    Abstract: A novel Hsp90 inhibitor that disrupts protein-protein interaction in a Hsp90 superchaperone complex without blocking ATP binding and methods for treating diseases such as pancreatic cancer are disclosed.
    Type: Application
    Filed: November 10, 2008
    Publication date: September 30, 2010
    Applicant: THE OHIO STATE UNIVERSITY RESEARCH FOUNDATION
    Inventors: Duxin Sun, Tao Zhang
  • Publication number: 20100217036
    Abstract: Novel catalytic processes for the production of carnosol from carnosic acid are presented. The carnosic acid may be in pure form, in an impure form, part of a plant extract, or may be present in rosemary needles. The catalyst may be iron, iron salts, a minor amount of water, rosemary needles, or a mixture thereof.
    Type: Application
    Filed: September 30, 2008
    Publication date: August 26, 2010
    Inventor: Christof Wehrli
  • Publication number: 20100099760
    Abstract: The present invention relates to novel derivatives of glycyrrhetinic acid, compositions comprising said derivatives and their use in the treatment of conditions or diseases that benefit from an upregulation of PPAR&ggr; and/or a downregulation of the expression or activity of one or more specificity (Sp) proteins, such as cancer, diabetes and Huntington's disease.
    Type: Application
    Filed: June 27, 2007
    Publication date: April 22, 2010
    Inventors: Stephen H. Safe, Sudhakar Chintharlapalli, Alan McAlees, Robert Mccrindle
  • Publication number: 20100056615
    Abstract: The present invention refers to the use of at least one tricyclic diterpenes for the manufacture of a nutraceutical or pharmaceutical for the treatment, co-treatment or prevention of inflammatory disorders and/or joint disorders.
    Type: Application
    Filed: November 21, 2007
    Publication date: March 4, 2010
    Inventors: Daniel Raederstorff, Goede Schueler, Joseph Schwager, Christof Wehrli
  • Publication number: 20090042832
    Abstract: New salts or ion pair complexes obtained by a reaction between boswellic acids or selectively enriched 3-O-acetyl-11-keto-?-boswellic acid (AKBA) or 11-keto-?-boswellic acid (KBA) compounds obtained through a new improved process, and an organic amine, more particularly with glucosamine. These salts or ion pair complexes are useful in nutraceuticals and in food supplements for anti-inflammatory and analgesic treatment of joints and cancer prevention or cancer therapeutic agents. These salts or ion pair complexes could also be used in cosmetic or pharmaceutical composition for external treatment of body parts or organs to treat inflammatory diseases or cancer.
    Type: Application
    Filed: March 7, 2005
    Publication date: February 12, 2009
    Inventors: Ganga Raju Gokaraju, Rama Raju Gokaraju, Venkata Subbaraju Gottumukkala, Trimurtulu Golakoti, Venkateswarlu Somepalli
  • Publication number: 20090042980
    Abstract: Neurite outgrowth-promoting prostaglandins (NEPPs) and other electrophilic compounds bind to Keap1, a negative regulator of the transcription factor Nrf2, and prevent Keap1-mediated inactivation of Nrf2 and, thus, enhance Nrf2 translocation into the nucleus of neuronal cells. Therefore, neuroprotective compositions and related methods are provided that employ such neuroprotective compounds, and prodrugs of such compounds, to cause dissociation of Nrf2 from a Keap1/Nrf2 complex.
    Type: Application
    Filed: October 10, 2007
    Publication date: February 12, 2009
    Applicant: Burnham Institute for Medical Research
    Inventors: Stuart A. Lipton, Takumi Satoh
  • Publication number: 20080207758
    Abstract: The conjugates of present invention are formed by the combination of rhein or their analogues with the organic bases or amino acids in molecular force between them. The methods for preparing the conjugates and their uses for manufacturing medicines in the treatment of diabetic nephrosis, recovery of gastrointestinal function and prevention of intestinal adhesion, as well as treatment of osteoarthritis, rheumatic arthritis and rheumatoid arthritis are also described. Rhein or their analogues as the left part of general formula (I) is selected from (1) the compounds of rhein or their analogues, in which one or two substituents of R2˜R3 and R6˜R7 are COOH at least two substituents of R1˜8 are —H; or (2) the rhein-containing extract derived from plants. In general formula (I), M represents nitrogen-containing organic bases or basic amino acids.
    Type: Application
    Filed: July 10, 2006
    Publication date: August 28, 2008
    Inventor: Xiaodong Cong
  • Patent number: 7358386
    Abstract: This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic derivatives and to methods of preparation.
    Type: Grant
    Filed: May 5, 2006
    Date of Patent: April 15, 2008
    Assignee: Bayer Pharmaceuticals Corporation
    Inventors: Derek B. Lowe, Philip L. Wickens, Xin Ma, Mingbao Zhang, William H. Bullock, Philip D. G. Coish, Ingo Mugge, Andreas Stolle, Ming Wang, Yamin Wang, Chengzhi Zhang, Hai-Jun Zhang, Lei Zhu, Manami Tsutsumi, James N. Livingston
  • Patent number: 7348449
    Abstract: Novel ligand antagonists of the RAR receptors have the following structural formula (I): in which A is a CH2, CHOH, C?O or C?N—OH radical or a sulfur or selenium atom; B is a radical selected from among those of formulae (a) to (f): and Ar is a radical selected from among those of formulae (g) to (i):
    Type: Grant
    Filed: April 28, 2005
    Date of Patent: March 25, 2008
    Assignee: Galderma Research & Development
    Inventors: Philippe Diaz, Catherine Raffin, Thibaud Biadatti
  • Publication number: 20040138262
    Abstract: The present invention provides compounds of the formula 1
    Type: Application
    Filed: July 8, 2003
    Publication date: July 15, 2004
    Applicant: Pfizer Inc.
    Inventors: Yves A. Chantigny, Edward F. Kleinman, Ralph P. Robinson
  • Publication number: 20040040470
    Abstract: The present invention provides a method for the preparation of carbonaceous materials comprising a plurality of gamma-keto-carboxyl containing functional groups surface bonded thereto, and further provides several surface modified carbonaceous materials resulting therefrom.
    Type: Application
    Filed: August 28, 2002
    Publication date: March 4, 2004
    Inventor: Bollepalli Srinivas
  • Patent number: 6548546
    Abstract: The present invention relates to HIV integrase inhibitors of the formula wherein R1 and Z are as defined in the specification.
    Type: Grant
    Filed: February 28, 2002
    Date of Patent: April 15, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael A. Walker, Timothy D. Johnson, Oak K. Kim, Yunhui Zhang
  • Patent number: 6380257
    Abstract: The present invention relates to new aromatic di-keto derivatives and to their pharmaceutically acceptable salts, esters, ethers and other chemical equivalents. The derivatives are glucose-6-phosphate translocase inhibitors and can be used in the treatment of diabetes mellitus. The present invention further relates to a process for the production of the derivatives, to the use of the derivatives and their pharmaceutically acceptable salts, esters, ethers and other chemical equivalents as pharmaceuticals, in particular to their use in the treatment of diabetes mellitus, and to pharmaceutical compositions comprising the derivatives, pharmaceutically acceptable salts, esters, ethers or other chemical equivalents thereof.
    Type: Grant
    Filed: October 24, 2000
    Date of Patent: April 30, 2002
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: László Vértesy, Michael Kurz, Erich Paulus
  • Patent number: 6339082
    Abstract: A compound selected from the group consisting of a compound of the formula wherein the substituents are defined as set forth in the specification and its salts with non-toxic pharmaceutically acceptable acids and bases useful for treating loss of bone matrix.
    Type: Grant
    Filed: June 29, 2000
    Date of Patent: January 15, 2002
    Assignees: Aventis Pharma S.A., Genetech, Inc.
    Inventors: Denis Carniato, Thomas R. Gadek, Jean-Francois Gourvest, Jochen Knolle, Robert S. McDowell, Anurschirwan Peyman
  • Patent number: 6215007
    Abstract: Novel polyketides and novel methods of efficiently producing both new and known polyketides, using recombinant technology, are disclosed. In particular, a novel host-vector system is described which is used to produce polyketide synthases which in turn catalyze the production of a variety of polyketides.
    Type: Grant
    Filed: March 5, 1999
    Date of Patent: April 10, 2001
    Assignees: The Leland Stanford Junior Univ., The John Innes Institute
    Inventors: Chaitan Khosla, David A. Hopwood, Suzanne Ebert-Khosla, Robert McDaniel, Hong Fu
  • Patent number: 6180815
    Abstract: The present invention provides compounds which inhibit an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.
    Type: Grant
    Filed: April 10, 2000
    Date of Patent: January 30, 2001
    Assignee: Eli Lilly and Company
    Inventors: Scott C. Mauldin, John E. Munroe
  • Patent number: 6175034
    Abstract: The present invention provides compounds which inhibit an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.
    Type: Grant
    Filed: April 10, 2000
    Date of Patent: January 16, 2001
    Assignee: Eli Lilly and Company
    Inventors: Scott C. Mauldin, John E. Munroe
  • Patent number: 5986129
    Abstract: The following description sets forth a process for producing rhein, diacerhein and other diacyl derivatives thereof, which comprises the following steps: treatment of a diphenylketone ##STR1## in which R.sub.1 is --OR', --NR'R", --SR', where R' and R" are H, an alkyl or aromatic group; R.sub.2 is H or a protective group, R.sub.3 is --OH or C.sub.1 -C.sub.4 alkyl, with an acid or superacid to give a 1-aminoanthraquinone derivative, diazotisation, replacement of the --NH.sub.2 group by --OH, optional removal of the protective group, and acylation.
    Type: Grant
    Filed: July 31, 1997
    Date of Patent: November 16, 1999
    Assignee: Laboratoire Medidom S.A.
    Inventor: Guido Di Napoli
  • Patent number: 5936120
    Abstract: The invention provides deoxygossylic compounds having useful biological activities, and methods for the synthesis of these and related compounds. The invention further provides valuable intermediates for the synthesis of the compounds, and pharmaceutical compositions containing biologically active compounds according to the invention.
    Type: Grant
    Filed: December 10, 1997
    Date of Patent: August 10, 1999
    Assignee: University of New Mexico
    Inventors: Robert D. Royer, Lorraine M. Deck, David L. VanderJagt
  • Patent number: 5919970
    Abstract: Compounds of the formulaY.sub.3 (R.sub.4)--X--Y.sub.1 (R.sub.1 R.sub.2)--Z--Y.sub.2 (R.sub.2)--A--Bwhere the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist or retinoid inverse agonist type biological activity.
    Type: Grant
    Filed: April 24, 1997
    Date of Patent: July 6, 1999
    Assignee: Allergan Sales, Inc.
    Inventors: Tae K. Song, Min Teng, Roshantha A. Chandraratna
  • Patent number: 5552441
    Abstract: This invention provides certain 1,2,4,5 substituted benzene derivatives containing "acid" substituents derived from cyclic or heterocyclic moieties. These unique compounds are leukotriene B.sub.4 antagonists and formulations of these derivatives, and a method of using these derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
    Type: Grant
    Filed: February 14, 1994
    Date of Patent: September 3, 1996
    Assignee: Eli Lilly and Company
    Inventors: Robert D. Dillard, J. Scott Sawyer, Michael J. Sofia
  • Patent number: 5523457
    Abstract: This invention relates to a retinoid mpound of formula I ##STR1## in which Y is --CO--NH--, --CR.sup.2 .dbd.CR.sup.3 --, --CO--O--, --O--CO--, --C(.dbd.S)--NH--, --C.tbd.C--, --O--CH.sub.2 --, --CH.sub.2 --O--, or --CH.sub.2 --CH.sub.2 --;A is --(CH.sub.2).sub.t -- or a bond;Q is phenyl optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen, or --CO.sub.2 R.sup.4 ;R.sup.1 is --CO.sub.2 Z, --CONHR.sup.5, C.sub.1-6 alkyl, --CH.sub.2 OH, or --CHO;R.sup.2, R.sup.3, R.sup.4, R.sup.5, and Z are independently hydrogen or C.sub.1-6 alkyl;t is one to six.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: June 4, 1996
    Assignee: Bristol-Myers Squibb Company
    Inventors: John E. Starrett, Jr., Muzammil M. Mansuri, David R. Tortolani
  • Patent number: 5434186
    Abstract: Compounds of the formula ##STR1## wherein X is O or CH.sub.2 ; Y is O, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, or --OCH.sub.2 C.sub.6 H.sub.4 --;Z is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- or --C.tbd.C--;f, h, k, m and t, independently, are 0 or 1;n is an integer from 1 to 12;R.sup.1 is hydrogen, lower alkyl, lower alkenyl, cycloalkyl, or aralkyl; and A is B or --O--B, wherein B is a mono-, di- or tricyclic aromatic or heteroaromatic moiety substituted by the group --COR.sup.2, --(O).sub.t --(W).sub.s --COR.sup.2 or --(CH.dbd.CH).sub.p COR.sup.2 and which may also contain up to 4 additional substituents selected, independently, from the group consisting of halogen, cyano, lower alkyl, lower alkoxy, sulfonamido, alkanoyl, aroyl, --(Q).sub.k --(W).sub.s' --E or --(Q).sub.k --(W).sub.s" --C.sub.6 H.sub.4 --(W).sub.s'" --E, provided that no more than one of said substituents is --(Q).sub.k --(W).sub.s' --E or --(Q).sub.k --(W).sub.s" --C.sub.6 H.sub.4 --(W).sub.s'" --E, and wherein E is COR.sup.
    Type: Grant
    Filed: September 28, 1993
    Date of Patent: July 18, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Noal Cohen, Ferdinand K. Lee, Keith A. Yagaloff
  • Patent number: 5403952
    Abstract: Novel substituted cyclic compounds of Formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophic epidermolysis bullosa, and coronary thrombosis associated with atherosclerotic plaque rupture. The matrix metalloendoproteinases are a family of zinc-containing proteinases including but not limited to stromelysin, collagenase, and gelatinase, that are capable of degrading the major components of articular cartilage and basement membranes. The inhibitors claimed herein may also be useful in preventing the pathological sequelae following a traumatic injury that could lead to a permanent disability. These compounds may also be useful as novel birth control agents by preventing ovulation or implantation.
    Type: Grant
    Filed: October 8, 1993
    Date of Patent: April 4, 1995
    Assignee: Merck & Co., Inc.
    Inventors: William Hagmann, Charles G. Caldwell, Paul R. Gooley
  • Patent number: 5374772
    Abstract: The invention relates to compounds of the formula ##STR1## R is hydrogen, lower alkyl, --(CH.sub.2).sub.2 N(R.sub.3).sub.2 or --CH.sub.2 OOCR.sub.3 wherein R.sub.3 is lower alkyl;R.sub.1 is CH.sub.3 (CH.sub.2).sub.n --, wherein n is 0-17, or R.sub.4 (CH.sub.2).sub.p --, wherein p is 2-18 and R.sub.4 is 1- or 2-naphthyloxy, 2,3- or 3,4-dihydroxyphenyl, phenyl, phenoxy, or substituted phenyl or phenoxy wherein the substituent is selected from the group consisting of hydroxy, benzyloxy, methylsulfinyl, methylsulfonyl or phenyl;R.sub.2 is R.sub.4 (CH.sub.2).sub.p --, 1-adamantyl--CO-- or diphenylmethyl--CO--, and, when R is hydrogen, pharmaceutically acceptable salts with bases.The compounds of formula I are potent inhibitors of phospholipases A.sub.2 (PLA.sub.2 's) and are therefore useful in the treatment of diseases, such as psoriasis, inflammatory bowel disease, asthma, allergy, arthritis, dermatitis, gout, pulmonary disease, myocardial ischemia, and trauma induced inflammation, such as spinal cord injury.
    Type: Grant
    Filed: October 22, 1993
    Date of Patent: December 20, 1994
    Assignee: Hoffmann-LaRoche Inc.
    Inventors: Mathew Carson, Ru-Jen L. Han, Ronald LeMahieu, Vincent S. Madison
  • Patent number: 5338881
    Abstract: This invention concerns a process for preparing diketones and keto-acids by reacting a dicarboxylic acid and an aromatic compound in the presence of an alkylsulfonic acid such as methanesulfonic acid and a phosphorus pentoxide. The diketones and keto-acids can be used to prepare polyketones which are useful as molding plastics, coatings, films, fibers, and the like.
    Type: Grant
    Filed: July 23, 1990
    Date of Patent: August 16, 1994
    Assignee: Eastman Chemical Company
    Inventors: Theodore R. Walker, Jr., Winston J. Jackson, Jr., Jean C. Fleischer
  • Patent number: 5262565
    Abstract: Compounds of the formula: ##STR1## where R.sup.1 is a hydrogen atom or a lower alkyl group;R.sub.2 is a lower alkoxy group;R.sub.3 is a hydroxyl or lower alkoxy group;Z is represented by the formula: ##STR2## where R.sub.2 and R.sub.3 may be the same or different from each other and each stands for a hydrogen atom or a lower alkyl;Y is represented by the formula: --(CH.sub.2).sub.n -- where n is 0 or an integer of 1 to 2 or a group represented by the formula: ##STR3## where R.sup.2 and R.sup.3 may be the same or different from each other and each stands for a lower alkyl group; andR.sup.4 represents a group of the formula: ##STR4## where p is 0 or an integer of 1 to 3 and R.sup.12 is hydrogen, a halogen atom, a lower alkyl or a lower alkoxy group a hydrogen atom, R.sup.2 is a methoxy group, R.sup.3 is a hydroxy group and R.sup.4 is a benzyl group having anti-inflammatory activity.
    Type: Grant
    Filed: November 12, 1991
    Date of Patent: November 16, 1993
    Assignee: Eisai Co., Ltd.
    Inventors: Hiroyuki Yoshimura, Shinya Abe, Tetsuya Kawahara, Takashi Inoue, Hiroshi Shirota, Kenichi Chiba, Kenichi Kusube, Toru Horie, Takeshi Suzuki, Isao Yamatsu, Naoyuki Shimomura, Kazuo Okano, Richard S. J. Clark, Takashi Mori, Shuhei Miyazawa, Ryoichi Hashida, Kenzo Muramoto, Koukichi Harada
  • Patent number: 5194664
    Abstract: Compounds of the general formula I ##STR1##
    Type: Grant
    Filed: November 12, 1991
    Date of Patent: March 16, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Hans-Heiner Wuest, Bernd Janssen
  • Patent number: 5117052
    Abstract: Benastatins A and B which are novel and physiologically active substances having the formula ##STR1## wherein R represents --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--, exhibit a potent immunomodifier activity, a glutathione transferase inhibition activity and an anti-microorganism activity and are therefore extremely useful for various drugs.
    Type: Grant
    Filed: March 14, 1991
    Date of Patent: May 26, 1992
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Tomio Takeuchi, Takaaki Aoyagi, Hiroshi Naganawa, Masa Hamada, Yasuhiko Muraoka, Takayuki Aoyama
  • Patent number: 5106407
    Abstract: The present invention discloses the antimicrobial utility of certain iodonium ylide compounds. The particular iodonium ylide compounds are phenyl iodonium ylides having an ortho substituent that stabilizes the positive charge on the polyvalent iodine by a nonbonded electrostatic interaction. The polyvalent iodine is further stabilized by a cyclic 1,3-dicarbonyl anion.
    Type: Grant
    Filed: December 4, 1989
    Date of Patent: April 21, 1992
    Assignee: The Dow Chemical Company
    Inventors: Attila G. Relenyi, Gerald F. Koser, Richard W. Walter, Jr., William J. Kruper, Jr., Ravi B. Shankar, Anthony P. Zelinko
  • Patent number: 5097064
    Abstract: This invention relates to a process for preparing an optically active 2-arylpropionic acid of general formula (I), by the hydrogenation, in a heterogeneous aqueous-organic medium, of a 2-arylacrylic acid of general formula (II) in the presence of a catalyst consisting of a rhodium derivative and a water-soluble chiral ligand.
    Type: Grant
    Filed: August 30, 1990
    Date of Patent: March 17, 1992
    Assignee: Rhone-Poulenc Sante
    Inventor: Jean-Michel Grosselin
  • Patent number: 5045541
    Abstract: Fused pyridazine compounds ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and respectively hydrogen, a halogen, hydroxy, nitro, amino, cyano, trifluoromethyl, and alkyl, an alkoxy or an alkanoylamino; one of R.sub.a and R.sub.b is a group of the formula--O--Y--NR.sup.5 R.sup.6wherein R.sup.5 and R.sup.6 are the same or different and respectively hydrogen, an alkyl, a phenylalkyl or a substituted phenylalkyl or a group forming a heterocycle together with the adjacent nitrogen atom and Y stands for a straight- or branched-chain alkylene which may have hydroxy group as a substituent on the chain, and the other is hydrogen, or both of R.sub.a and R.sub.b are the same or different and respectively a group of the formula--O--Y--NR.sup.5 R.sup.6wherein R.sup.5 and R.sup.6 are of the same meanings as defined above; W is .dbd.CH-- or .dbd.N; X is CH.sub.2, S, SO, SO.sub.
    Type: Grant
    Filed: July 2, 1989
    Date of Patent: September 3, 1991
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Toru Nakao, Minoru Kawakami, Masao Hisadome, Tetsuya Tahara
  • Patent number: 5023363
    Abstract: An aromatic compound of the formula ##STR1## These compounds are useful in human and veterinary medicines and in cosmetic compositions.
    Type: Grant
    Filed: April 1, 1988
    Date of Patent: June 11, 1991
    Assignee: L'Oreal
    Inventors: Jean Maignan, Gerard Lang, Gerard Malle, Serge Restle, Braham Shroot
  • Patent number: 4999429
    Abstract: Aryl difluoromethyl sulfone adds to aldehydes under phase transfer conditions to give novel substituted alcohols of the general formulaRCH(OH)CF.sub.2 SO.sub.2 Ar (I)wherein R is an aryl, cycloaliphatic, sec- or tert-aliphatic, or heterocyclic group and Ar is an aryl group. The substituted alcohols of formula I are of particular utility as intermediates in the synthesis of a variety of useful end products. For example, the products of formula I may be utilized in desulfonylation reactions, oxidation reactions and fluorination reactions.
    Type: Grant
    Filed: November 13, 1989
    Date of Patent: March 12, 1991
    Assignee: Ethyl Corporation
    Inventor: G. Patrick Stahly
  • Patent number: 4876381
    Abstract: The invention relates to a compound of the formula (II) ##STR1## and the corresponding isomers and salts, in which formula: a and b are integers which independently of one another can assume the values 0 or 1,R.sub.1, R.sub.2, R.sub.3 and R.sub.4 represent, independently, a hydrogen atom, a linear or branched C.sub.1 -C.sub.6 -alkyl radical or a C.sub.1 -C.sub.4 -alkoxy radical,R.sub.6 represents a C.sub.1 -C.sub.6 -alkyl radical,R.sub.5 and R.sub.12 represent a hydrogen atom or a C.sub.1 -C.sub.4 -alkyl radical, with the proviso that R.sub.5 cannot represent hydrogen if a=b=0 andR.sub.11 has various meanings.These compounds have useful dermatological properties.
    Type: Grant
    Filed: August 18, 1987
    Date of Patent: October 24, 1989
    Assignee: L'Oreal
    Inventors: Gerard Lang, Jean Maignan, Serge Forestier, Serge Restle, Alain Lagrange, Braham Shroot
  • Patent number: 4777281
    Abstract: The invention relates to novel [(3,4-dichloro-6,7,8,8a,9,10-hexahydro-6-oxo-8a-substituted-2-phenanthreny l)ox yl]-alkanoic acids and -ethanimidamides and their salts. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections and various brain concussions.
    Type: Grant
    Filed: March 3, 1986
    Date of Patent: October 11, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Otto W. Woltersdorf, Jr., Edward J. Cragoe, Jr.
  • Patent number: 4731472
    Abstract: The invention relates to novel [(5,6-dichloro-3-oxo-9a-propyl-2,3,9,9a-tetrahydrofluoren-7-yl)]alkanoic acids and alkanimidamides, their derivatives and their salts. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections, various brain concussions and elevated intracranial pressure.
    Type: Grant
    Filed: March 3, 1986
    Date of Patent: March 15, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Adolph M. Pietruszkiewicz, Otto W. Woltersdorf, Jr., Edward J. Cragoe, Jr.
  • Patent number: 4731471
    Abstract: The invention relates to novel [(5,6-dichloro-3-oxo-2,3,9,9a-tetrahydrofluoren-7-yl)]alkanoic acids and alkanimidamides bearing novel functional 9a-substituents, their derivatives and their salts. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, the neurological problems caused by AIDS, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections, various brain concussions and elevated intracranial pressure.
    Type: Grant
    Filed: November 3, 1986
    Date of Patent: March 15, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr., Adolph M. Pietruszkiewicz
  • Patent number: 4731470
    Abstract: The invention relates to novel [(5,6-dichloro-3-oxo-2,9a-alkano--2,3,9,9a-tetrahydro-1H-fluoren-7-yl)oxy] alkanoic acids and alkanimidamides, their derivatives, and their salts. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections including that due to AIDS virus, various brain concussions and elevated intracranial pressure.
    Type: Grant
    Filed: November 3, 1986
    Date of Patent: March 15, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Adolph M. Pietruszkiewicz, Otto W. Woltersdorf, Jr., Edward J. Cragoe, Jr.
  • Patent number: 4704472
    Abstract: A process for direct preparation of an enantiomer of a substituted fluorenyloxyacetic acid is disclosed. The acetic acid derivative is useful for treating brain edema.
    Type: Grant
    Filed: December 18, 1985
    Date of Patent: November 3, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Robin S. E. Conn, Sandor Karady
  • Patent number: 4605761
    Abstract: An improved method for the direct preparation of an enantiomer of a substituted fluorenyloxyacetic acid including the enhancement of a chiral phase transfer alkylation step in the synthesis using a non-ionic surfactant as co-catalyst. The substituted fluorenyloxyacetic acid is useful in the treatment of brain edema.
    Type: Grant
    Filed: December 6, 1985
    Date of Patent: August 12, 1986
    Assignee: Merck & Co., Inc.
    Inventor: Ulf H. Dolling
  • Patent number: 4605760
    Abstract: A process for direct preparation of an enantiomer of a substituted fluorenyloxyacetic acid is disclosed. The acetic acid derivative is useful for treating brain edema.
    Type: Grant
    Filed: August 16, 1985
    Date of Patent: August 12, 1986
    Assignee: Merck & Co., Inc.
    Inventor: Apurba Bhattacharya