Sulfur Attached Directly To Amino Nitrogen By Nonionic Bonding (e.g., Sulfenamides, Etc.) Patents (Class 514/608)
  • Patent number: 9006485
    Abstract: The present invention relates to compounds of the formula (I) wherein R1 and R2 independently of one another are hydrogen, C1-C10-alkyl, C1-C10-haloalkyl, C3-C10-cycloalkyl, C3-C10-halocycloalkyl, C2-C10-alkenyl, C2-C10-haloalkenyl or together represent an aliphatic chain, or the like; R3 is halogen, cyano, C1-C8-alkyl, C1-C8-haloalkyl, C3-C8-cycloalkyl, C3-C8-halocycloalkyl, C2-C8-alkenyl, C2-C8-haloalkenyl, C1-C8-alkoxy, phenyl, or the like; R4 is hydrogen, C1-C10-alkyl, C1-C10-haloalkyl, C3-C8-cycloalkyl, C3-C8-halocycloalkyl, C2-C10-alkenyl, C2-C10-haloalkenyl, phenyl, or the like; t is 0 or 1; p is 0, 1, 2, 3 or 4. The present invention also relates to a process for preparing a compound of the formula (I) which comprises reacting a compound of the formula II with a compound of the formulae III or IV: where t, p, R1 R3, R3 and R4 are as defined in any of claims 1 to 6 and where A? is an equivalent of an anion having a pKB of at least 10 (determined under standard conditions in water).
    Type: Grant
    Filed: August 10, 2012
    Date of Patent: April 14, 2015
    Assignee: BASF SE
    Inventors: Karsten Koerber, Prashant Deshmukh, Florian Kaiser, Michael Rack, Timo Frasetto, Gemma Veitch, Markus Kordes, Marco Naujok
  • Publication number: 20140213611
    Abstract: The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds; wherein R1 to R9 are as defined herein.
    Type: Application
    Filed: July 6, 2012
    Publication date: July 31, 2014
    Applicant: KalVista Pharmaceuticals Limited
    Inventors: David Michael Evans, Rebecca Louise Davie, Hannah Joy Edwards, David Philip Rooker
  • Publication number: 20140155451
    Abstract: The present invention relates to compounds of the formula (I) wherein R1 and R2 independently of one another are hydrogen, C1-C10-alkyl, C1-C10-haloalkyl, C3-C10-cycloalkyl, C3-C10-halocycloalkyl, C2-C10-alkenyl, C2-C10-haloalkenyl or together represent an aliphatic chain, or the like; R3 is halogen, cyano, C1-C8-alkyl, C1-C8-haloalkyl, C3-C8-cycloalkyl, C3-C8-halocycloalkyl, C2-C8-alkenyl, C2-C8-haloalkenyl, C1-C8-alkoxy, phenyl, or the like; R4 is hydrogen, C1-C10-alkyl, C1-C10-haloalkyl, C3-C8-cycloalkyl, C3-C8-halocycloalkyl, C2-C10-alkenyl, C2-C10-haloalkenyl, phenyl, or the like; t is 0 or 1; p is 0, 1, 2, 3 or 4. The present invention also relates to a process for preparing a compound of the formula (I) which comprises reacting a compound of the formula II with a compound of the formulae III or IV: where t, p, R1 R3, R3 and R4 are as defined in any of claims 1 to 6 and where A? is an equivalent of an anion having a pKB of at least 10 (determined under standard conditions in water).
    Type: Application
    Filed: August 10, 2012
    Publication date: June 5, 2014
    Applicant: BASF SE
    Inventors: Karsten Koerber, Prashant Deshmukh, Florian Kaiser, Michael Rack, Timo Frasetto, Gemma Veitch, Markus Kordes, Marco Naujok
  • Patent number: 8632794
    Abstract: There are provided methods for controlling microbial or biofilm growth, comprising mixing a hypochlorite oxidant and at least one nitrogen-containing compound or salt thereof selected from a particular group of nitrogen-containing compounds and salts to form a biocide, and applying the biocide. Apparatus for practicing the methods are also provided.
    Type: Grant
    Filed: January 12, 2005
    Date of Patent: January 21, 2014
    Assignee: A.Y. Laboratories Ltd.
    Inventor: Ayala Barak
  • Patent number: 8623859
    Abstract: The invention relates to compounds of formula (I) wherein R1, R1a, R1b, R2, R3 and X, X1, X2, X3 have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
    Type: Grant
    Filed: August 10, 2009
    Date of Patent: January 7, 2014
    Assignee: Evotec AG
    Inventors: James Madden, David James Hallett, Alastair Parkes, Ali Raoof, Xiaolu Wang
  • Publication number: 20130253051
    Abstract: Agents of formula: where R1 and R2 vary independently and are acyl, sulfonyl, phosphoryl, alkyl, substituted alkyl, halogen, aryl, arylalkyl, substituted aryl, heteroaryl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, heterocycle, or heteroatoms; and R3 is H or a member of a ring structure which includes R2, are provided; as are agents of formula: where R1, R2 and R3 vary independently and: R1=OH, OR?, NHR?, NR?R? (with R? R?=alkyl, aryl, heteroaryl, etc); R2=acyl, alkyl, aryl, sulfonyl, etc; R3=alkyl, aryl, substituted aryl, heteroaryl, etc; and R4 and R5 are (independently) H, methyl or alkyl, substituted alkyl, aryl, substituted aryl, etc. Methods of using the agents to treat e.g. cardiovascular disease, stroke, shock, injuries caused by hypoxia, male erectile dysfunction, and Alzheimer's are provided.
    Type: Application
    Filed: December 1, 2011
    Publication date: September 26, 2013
    Applicant: WASHINGTON STATE UNIVERSITY
    Inventors: Ming Xian, Yu Zhao
  • Publication number: 20130184238
    Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: March 8, 2013
    Publication date: July 18, 2013
    Inventors: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
  • Publication number: 20130028992
    Abstract: An herbal-based solution includes a first amount of wasabi comprising at least an allyl isothiocyanate component, and a second amount of saline solution. The saline solution and the organic material are combined to substantially dilute the wasabi in the saline solution to produce the herbal-based solution. The herbal-based solution further has anti-inflammatory, anti-microbial and anti-coagulative properties. The wasabi may include Eutrema Wasabi. The herbal-based solution is deliverable as a nasal.
    Type: Application
    Filed: July 26, 2011
    Publication date: January 31, 2013
    Inventor: Caleb James Walker
  • Patent number: 8357721
    Abstract: The invention relates to compounds of the general formula (I) wherein R1, R2, R3, R4, R5, R6, i and j have the meanings given in claim 1, and to the use thereof as caspase-10 inhibitors, especially for the treatment of diabetic retinopathy.
    Type: Grant
    Filed: April 6, 2006
    Date of Patent: January 22, 2013
    Assignee: Merck Patent GmbH
    Inventors: Claude Lardy, Marc Lecomte, Thierry Convard, Catherine Vidal
  • Publication number: 20130012555
    Abstract: Dihydroxyaryl compounds and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of IAPP or amylin fibril diseases, and the manufacture of medicaments for such treatment.
    Type: Application
    Filed: January 12, 2012
    Publication date: January 10, 2013
    Inventors: Thomas Lake, Alan D. Snow
  • Publication number: 20120252733
    Abstract: Provided herein are compositions and related methods useful for accelerating bone healing and growth. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity.
    Type: Application
    Filed: June 4, 2010
    Publication date: October 4, 2012
    Applicant: UNIVERSITY OF PITTSBURGH - OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
    Inventors: Michael W. Epperly, Abhay Sudhir Gokhale, Joel S. Greenberger, Peter Wipf, Julianne Glowacki
  • Publication number: 20120015960
    Abstract: Provided are compounds for inhibiting Snail-p53 binding and therapeutic agents for cancer including the compounds as an effective component. The Snail-p53 binding inhibitors induce expression of p53 in K-Ras mutant cell lines, thereby enabling effective treatment or prevention of K-Ras mutant cancer, such as, pancreatic cancer, lung cancer, cholangioma, and colon cancer, of which diagnosis or treatment is not easy.
    Type: Application
    Filed: November 23, 2009
    Publication date: January 19, 2012
    Applicants: The Industry & Academic Cooperation in Chungnam National University, Pusan National University Industry-University Cooperation Foundation
    Inventors: Bum Joon Park, Nam Chul Ha, Sun Hye Lee, Gyu Yong Song, Jee Hyun Lee
  • Publication number: 20110178072
    Abstract: This disclosure relates to compositions and methods of use involving compounds (e.g., drugs) containing methylsulfinyl moieties. For example, a compound may be administered in an excess of either the R- or S-epimer of the methylsulfinyl moiety based on whether the compound exhibits higher biological activity when the methylsulfinyl moiety is present in the methylsulfinyl-oxidized form or the methylsulfide-reduced form.
    Type: Application
    Filed: July 23, 2009
    Publication date: July 21, 2011
    Inventors: Vadim Gladyshev, Byung Cheon Lee
  • Publication number: 20110065717
    Abstract: The present invention relates to novel substituted sulfoximine derivatives of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation.
    Type: Application
    Filed: August 4, 2008
    Publication date: March 17, 2011
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Vrajesh B. Pandya, Pankaj Ramanbhai Patel
  • Publication number: 20110039802
    Abstract: The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): wherein R1 is lower alkyl, cycloalkyl or the like, R2 is hydrogen, lower alkyl or the like, n is 1 or 2, X is lower alkylone, lower alkenylene, arylene, cycloalkylene or the like, Y is CONR7, CSNR7, NR7CO, NR7CS or the like, Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R7 is hydrogen or lower alkyl, prodrug, pharmaceutically acceptable salt or solvate thereof
    Type: Application
    Filed: July 2, 2010
    Publication date: February 17, 2011
    Inventors: Yasuyuki KAWANISHI, Hideyuki TAKENAKA, Kohji HANASAKI, Tetsuo OKADA
  • Publication number: 20110028560
    Abstract: The invention relates to a self-emulsifiable liquid composition intended to be diluted in an aqueous intermediate solution and then incorporated into the drinking water of livestock animals, and also to the use of such a composition. The invention is characterized in that the composition comprises at least—between 1% and 12% by weight of the florfenicol active ingredient, relative to the total volume of the composition; —at least 50% by weight, relative to the total volume of the composition (p/v), of a mixture of C8-C10 saturated polyglycosylated glycerides having an HLB (hydrophilic-lipophilic balance) of less than 16; and—at least 5% by weight, relative to the total volume of the composition (p/v), of a surfactant.
    Type: Application
    Filed: December 17, 2008
    Publication date: February 3, 2011
    Applicant: VIRBAC SA
    Inventors: Guy Derrieu, Bernard Raynier
  • Publication number: 20100323978
    Abstract: The present invention relates to a delivery system for ophthalmic drugs, and more particularly, to a non aqueous oil delivery system. Low concentrations of ophthalmic drugs suspended in an oil vehicle delivery system are as therapeutically effective in man and animals as the corresponding higher concentrations of ophthalmic drugs that are commercially used in aqueous solutions. Eye drops that utilize this nonaqueous oil delivery system, when used in man, are comfortable to use and produce little ocular irritation, have a longer shelf-life, low systemic toxic potential, and only short term blurring of vision. Using this nonaqueous oil delivery system, a single drop of ophthalmic drug with a concentration that is 10 times less than the same drug used in commercially available aqueous eye drops is as effective as the commercially available aqueous ophthalmic eye drops that require many applications to be effective.
    Type: Application
    Filed: June 22, 2009
    Publication date: December 23, 2010
    Inventor: Calvin Hanna
  • Publication number: 20100098733
    Abstract: The present invention provides an oral care composition Comprising a nitric oxide releasing particle and an orally-acceptable carrier. The nitric oxide releasing particle comprises at least one nitric oxide donor. Another aspect of the present invention provides a device for oral care comprising a nitric oxide releasing particle, wherein the device is configured to expose a targeted site in an oral cavity of a subject to nitric oxide. The present invention also provides methods and uses of providing oral health benefits by using the oral care compositions or devices as described above.
    Type: Application
    Filed: October 16, 2009
    Publication date: April 22, 2010
    Inventor: Nathan Stasko
  • Publication number: 20100087505
    Abstract: The invention relates to aryl-sulphonamido compounds endowed with inhibitory activity against metallo proteases MMP, having formula (I) below wherein R, R1, R2, R3, R4, R5, n and m have the meanings reported in the specification; the invention also refers to the process for their preparation, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly in the treatment of degenerative disorders.
    Type: Application
    Filed: March 14, 2008
    Publication date: April 8, 2010
    Applicant: Bracco Imaging S.p.A.
    Inventors: Aldo Balsamo, Armando Rossello, Elisa Nuti, Elisabetta Orlandini, Tziano Tuccinardi
  • Publication number: 20100016310
    Abstract: Disclosed are methods of using soluble epoxide hydrolase (sEH) inhibitors for treating diseases related to cardiovascular disease.
    Type: Application
    Filed: August 15, 2007
    Publication date: January 21, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Richard Harold Ingraham
  • Publication number: 20090258947
    Abstract: Low dose pharmaceutical dosage form comprising nimesulide or its pharmaceutically acceptable salts, esters, solvates or hydrates thereof, along with one or more pharmaceutically acceptable excipient(s) are provided. The present invention also provides process of preparing such dosage forms and therapeutic methods of using such dosage forms. The low dose compositions 10 are designed to exhibit such bioavailability, which is effective in the treatment of NSAID indicated disorders particularly, which require long-term treatment regimens such as arthritis. Such compositions reduce the cost of therapy in diseases, which require long-term therapies, are easy to manufacture, and also result in the reduction of dose related side effects associated with nimesulide therapy.
    Type: Application
    Filed: April 23, 2007
    Publication date: October 15, 2009
    Inventors: Rajesh Jain, Kour Chand Jindal
  • Publication number: 20090215730
    Abstract: Chemical compounds derived by in silico molecular modelling, having a well defined structure suitable for the blocking of the phosphorylation event, through the specific interaction of the chemical with the Casein Kinase 2 enzyme substrate phosphorylation domain or it's neighbourhood. This invention comprises also the pharmaceutical compositions containing such compounds, and their use in the preparation of medicines or agents for the treatment of diseases or conditions related with neoplasic processes.
    Type: Application
    Filed: May 5, 2006
    Publication date: August 27, 2009
    Inventors: Rolando Eduardo Rodriguez Fernandez, Roberto Vera Alvarez, Ania De La Nuez Veulens, Yuliet Mazola Reyes, Silvio Ernesto Perea Rodriguez, Boris Ernesto Acevedo Castro, Alexis Musacchio Lasa, Raimundo Ubieta Gomez
  • Publication number: 20090118306
    Abstract: The present invention generally relates to a novel therapeutical use of liver X receptor (LXR) agonsits. More specifically, the present invention relates to the use of LXR agonist for the preparation of a medicament useful for the treatment and/or the prevention of a disease associated with beta cells degeneration, such as diabetes, and a method for increasing ex vivo viability of pancreatic islet cells, comprising contacting said islet cells with a LXR agonist.
    Type: Application
    Filed: May 10, 2006
    Publication date: May 7, 2009
    Applicant: LABORATOIRE FOURNIER S.A. French Limited Compay
    Inventors: Bernadette Husson, Pierre Broqua, Jean-Louis Junien
  • Publication number: 20090118660
    Abstract: Method for in-vivo plasmapheresis utilizing a plurality of elongated hollow microporous filter fibers periodically interrupt diffusion of blood plasma from a patient, and, for a selected time, directing backflush fluid into the fibers at a pressure and interval sufficient to cleanse the fiber pores, after which plasma diffusion is resumed. The backflush fluid, preferably a normal saline solution, may contain an anticoagulant such as heparin, citrate or NO donor in suitable concentration for systemic anti-coagulation or for treating the fiber for thromboresistance.
    Type: Application
    Filed: January 13, 2009
    Publication date: May 7, 2009
    Applicant: Transvivo Inc.
    Inventors: Reynolds G. Gorsuch, Tommy Gene Cooper, Harold H. Handley, JR., Harold W. Peters
  • Publication number: 20090018161
    Abstract: The present invention provides a more effective gastrointestinal function promoter. The present invention also provides a method for the prophylaxis or improvement of functional gastrointestinal disorders, a method for appetite regulation and the like. The present invention also provides a method for screening for a substance capable of promoting a gastrointestinal function. The present invention provides a gastrointestinal function promoter containing a T1R agonist as an active ingredient and a method for the prophylaxis or improvement of functional gastrointestinal disorders, a method for appetite regulation and the like by administering a T1R agonist. The present invention also provides a method of screening for a substance capable of promoting a gastrointestinal function which method uses a cell expressing T1R receptor.
    Type: Application
    Filed: May 2, 2008
    Publication date: January 15, 2009
    Applicant: AJINOMOTO CO. INC.
    Inventors: Tatsuro Tanaka, Hisayuki Uneyama, Shinichi Fujita, Saori Ogawa, Yusuke Amino, Seiji Shiraishi, Koichi Fujita, Tatsuhiro Yamada, Takashi Yamamoto, Takeshi Aihara, Manabu Suzuki
  • Publication number: 20090011051
    Abstract: The present invention generally relates to the modulation of hypoxia-inducible factor (HIF) using the compounds and methods disclosed herein. These compounds and methods can be applied to the prevention, pretreatment, and/or treatment of conditions or states associated with HIF, such as hypoxia- and ischemia-related conditions and the induction of stasis.
    Type: Application
    Filed: September 28, 2007
    Publication date: January 8, 2009
    Inventors: Mark B. Roth, Mark Budde
  • Publication number: 20080214393
    Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as agrochemical active ingredients and can be prepared in a manner known per se.
    Type: Application
    Filed: September 20, 2005
    Publication date: September 4, 2008
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Andre Jeanguenat, Anthony Cornelius O'Sullivan
  • Publication number: 20080146548
    Abstract: This disclosure relates to amides, aryl sulphonamides, aryl ureas, and ?,?-diketones derivatives useful as carboxylesterase esterase inhibitors. The disclosure is also directed to the use of these compounds as selective human intestinal carboxylesterase inhibitors and insect carboxylesterase inhibitors. The disclosure is also directed to pharmaceutical compositions and pesticide formulations containing these compounds, and to methods for treating or ameliorating the toxic effects following administration of drugs such as cancer therapy drugs, treating or ameliorating the effects of a drug overdose, and to the use of the compounds for increasing the effectiveness of insecticides and pesticides.
    Type: Application
    Filed: February 15, 2008
    Publication date: June 19, 2008
    Applicant: ST. JUDE CHILDREN'S RESEARCH HOSPITAL
    Inventors: Philip M. Potter, Janice L. Hyatt, Christopher L. Morton, Paul P. Beroza, Komath V. Damoradan
  • Patent number: 7105575
    Abstract: The present invention relates to new uses of S-2-(3-aminopropylamino)ethyl dihydrogen phosphorothioate, (amifostine) and other aminothiol compounds to treat and reverse toxicities caused by therapeutic agents, radiation treatment or diabetes. In particular, the invention provides a method for treating neurotoxicity and nephrotoxicity associated with the administration of chemotherapeutic agents.
    Type: Grant
    Filed: May 3, 2002
    Date of Patent: September 12, 2006
    Assignee: Medimmune Oncology Inc.
    Inventors: Martin Stogniew, David S. Alberts, Edward H. Kaplan
  • Patent number: 7105572
    Abstract: An emulsion composition containing a compound represented by the formula: wherein R, R0, Ar and n are as defined in the specification or a salt thereof or a prodrug thereof, wherein the composition is adjusted to have a pH of not more than about 6, shows improved stability of the compound, a salt thereof or a prodrug thereof, and realizes expression of superior efficacy.
    Type: Grant
    Filed: February 1, 2001
    Date of Patent: September 12, 2006
    Assignee: Takeda Pharmaceutical Company Limited
    Inventor: Jun Sato
  • Patent number: 6953806
    Abstract: The present invention provides compounds of formula (I) wherein A1, A2, A3, A4, A5, A6, A7, A8, A9, A10, U, V, W, m, n and p are as indicated in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia and hyperlipemia.
    Type: Grant
    Filed: December 10, 2002
    Date of Patent: October 11, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, Johannes Aebi, Henrietta Dehmlow, Georges Hirth, Hans-Peter Maerki, Olivier Morand
  • Patent number: 6844320
    Abstract: Preeclampsia and preterm labor in a pregnant female mammal are treated by administering thereto a combination of a progestin and a nitric oxide synthase substrate, a nitric oxide donor or both, optionally in further combination with one or more of a cyclooxygenase inhibitor, a PGI2-mimetic, a thromboxane (TXA2) inhibitor, a compound possessing TXA2-agonistic and TXA2-inhibiting properties, a compound possessing TXA2-antagonistic and PGI2-memetic activities, and a TXA2 antagonist.
    Type: Grant
    Filed: July 24, 1998
    Date of Patent: January 18, 2005
    Assignees: Board of Regents, The University of Texas System, Schering Aktiengesellschaft
    Inventors: Robert E. Garfield, Krzysztof Chwalisz, Radoslaw Bukowski, Chandra Yallampalli
  • Patent number: 6777572
    Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful for treatment of renal failure.
    Type: Grant
    Filed: November 28, 2001
    Date of Patent: August 17, 2004
    Assignee: Pharmacia Corporation (of Pfizer Inc.)
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 6762202
    Abstract: The present invention describes rapid noninvasive methods for measuring vasodilation or changes in blood flow in a patient following administration of at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one vasoactive agent. The method comprises the administration of at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one vasoactive agent to the patient followed by monitoring the temperature change of an area of interest using infrared thermography.
    Type: Grant
    Filed: May 8, 2001
    Date of Patent: July 13, 2004
    Assignee: NitroMed, Inc.
    Inventors: Przemyslaw A. Marek, Andzrej M. Trocha, Chia-En Lin, Ramani R. Ranatunga, Stewart K. Richardson
  • Patent number: 6762205
    Abstract: Phenyl sulfamate derivatives represented by the following formula or salts thereof have a powerful inhibitory effect on steroid sulfatase and are hence useful for the prophylaxis or treatment of diseases associated with steroids such as estrogens, such as breast cancer, corpus uteri cancer, endometrial hyperplasia, infertility, endometriosis, adenomyosis uteri, autoimmune disease, dementia or Alzheimer's disease. wherein R1 and R2 each independently represent a hydrogen atom or a lower alkyl group; R3 represents a hydrogen atom, a halogen atom, a lower alkyl group, —OSO2NR1R2, a lower alkanoylamino group, a nitro group or a cyano group; and A represents a substituted or unsubstituted phenyl group, a group of the formula —X—NR4R5, or the like.
    Type: Grant
    Filed: January 3, 2002
    Date of Patent: July 13, 2004
    Assignee: Teikoku Hormone Mfg. Co., Ltd.
    Inventors: Naoyuki Koizumi, Makoto Okada, Shigeki Iwashita, Shigehiro Takegawa, Takayoshi Nakagawa, Hiroo Takahashi, Tomohito Fujii
  • Patent number: 6667414
    Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension.
    Type: Grant
    Filed: November 28, 2001
    Date of Patent: December 23, 2003
    Assignee: Pharmacia Corporation
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 6586476
    Abstract: The present invention relates to new uses of S-2-(3-aminopropylamino)ethyl dihydrogen phosphorothioate, (amifostine) and other aminothiol compounds to treat and reverse toxicities caused by therapeutic agents, radiation treatment or diabetes. In particular, the invention provides a method for treating neurotoxicity and nephrotoxicity associated with the administration of chemotherapeutic agents.
    Type: Grant
    Filed: October 28, 1999
    Date of Patent: July 1, 2003
    Assignee: MedImmune Oncology, Inc.
    Inventors: Martin Stogniew, David S. Alberts, Edward H. Kaplan
  • Patent number: 6583161
    Abstract: The invention provides compounds, compositions and methods relating to novel aromatic derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.
    Type: Grant
    Filed: December 12, 2000
    Date of Patent: June 24, 2003
    Assignee: Tularik Inc.
    Inventor: Julio C. Medina
  • Patent number: 6528528
    Abstract: The present invention provides compounds of Formula I shown below. The present invention also provides methods of treating or preventing 3 inflammation or atherosclerosis, and a pharmaceutical composition that contains a compound of Formula I.
    Type: Grant
    Filed: May 15, 2001
    Date of Patent: March 4, 2003
    Assignee: Warner-Lambert Company
    Inventors: David Thomas Connor, William Howard Roark, Karen Elaine Sexton, Roderick Joseph Sorenson
  • Patent number: 6524624
    Abstract: A two-part disinfecting systems, as well as disinfecting compositions and methods for making and using the same. The two-part disinfecting system contains a first part and a second part adapted to be mixed to yield an aqueous disinfecting composition, wherein the first part comprises a chlorite and the second part comprises an acid and an optional oxidizable colorant, and wherein the first part, the second part, or both the first and second parts comprise an alpha olefin sulfonate.
    Type: Grant
    Filed: May 16, 2001
    Date of Patent: February 25, 2003
    Assignee: Alcide Corporation
    Inventors: Joseph Morelli, C. Cayce Warf, Jr., Maura Aldrich, Cecilia Moser Morse, Jean Wiley
  • Patent number: 6479551
    Abstract: The invention is directed to pharmaceutical compositions useful in the treatment of migraine. The compositions contain metoclopramide and one or more NSAIDs in unit dosage form. By selecting NSAIDs that are non-acidic or segregating the metoclopramide and NSAID, the storage life of the compositions has been increased. Also disclosed are coordinated dosage forms for the sequential release of drugs. The invention encompasses methods of treating migraine using any of these dosage forms.
    Type: Grant
    Filed: March 3, 2000
    Date of Patent: November 12, 2002
    Assignee: Pozen Inc.
    Inventors: John R. Plachetka, Zakauddin T. Chowhan
  • Patent number: 6479550
    Abstract: &agr;-Sulfenimino acid derivatives of formula I including the optical isomers thereof and mixtures of such isomers, wherein A is cycloalkyl, cycloalkenyl, aryl or heteroaryl, each optionally substituted, B is a direct bond or optionally substituted alkylene, E is hydrogen or optionally substituted aryl, R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl, each optionally substituted, and T is NH or oxygen, have been found to be useful for controlling or preventing the infestation of plants by phytopathogenic microorganisms, especially fungi. The invention relates the novel compounds and also to the preparation thereof and to the use of the compounds for plant protection, and to compositions suitable for applying the novel compounds in agricultural techniques.
    Type: Grant
    Filed: July 16, 2001
    Date of Patent: November 12, 2002
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: André Jeanguenat, Martin Zeller, Hugo Ziegler
  • Patent number: 6410591
    Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma a therapeutically effective amount of a 3, 7 or 3 and 7 thia or oxa prostanoic acid derivative.
    Type: Grant
    Filed: May 8, 2001
    Date of Patent: June 25, 2002
    Assignee: Allergan Sales, Inc.
    Inventors: Robert M. Burk, Mark Holoboski, Mari F. Posner
  • Patent number: 6403600
    Abstract: The invention relates to novel methoximinophenylacetamides, to a process for their preparation and to their use as fungicides.
    Type: Grant
    Filed: April 5, 2001
    Date of Patent: June 11, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Fritz Maurer, Herbert Gayer, Peter Gerdes, Ulrich Heinemann, Bernd-Wieland Krüger, Robert Markert, Klaus Stenzel, Gerd Hänssler, Astrid Mauler-Machnik
  • Patent number: 6387954
    Abstract: The present invention provides certain alkenyl sulphonamide derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.
    Type: Grant
    Filed: January 23, 2001
    Date of Patent: May 14, 2002
    Assignee: Eli Lilly and Company
    Inventors: Winton Dennis Jones, Paul Leslie Ornstein, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
  • Patent number: 6380182
    Abstract: The invention relates to a method to inhibit bacteria from adhering to a submergible surface. The method contacts the submergible surface with an effective amount of at least one sulfamic acid or salt thereof to inhibit bacterial adhesion to the submergible surface. The invention also relates to a method for controlling biofouling of an aqueous system. This method adds an effective amount of at least one sulfamic acid or salt thereof to inhibit bacteria from adhering to a submerged surface within the aqueous system. This method effectively controls biofouling without substantially killing the fouling organisms. The sulfamic acid used in the method of the invention has the formula R1R2NS(O)2(OH). In this formula, R1 and R2 are independently a hydrogen, a C4-C20 alkyl group or a cyclohexyl group. However, R1 and R 2 are not both hydrogen.
    Type: Grant
    Filed: June 12, 2000
    Date of Patent: April 30, 2002
    Inventors: Thomas E. McNeel, Marilyn S. Whittemore, Stephen D. Bryant, Graciela H. Vunk
  • Patent number: 6342624
    Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful for treatment of a disorder mediated by inhibiting plasma renin activity.
    Type: Grant
    Filed: January 6, 2000
    Date of Patent: January 29, 2002
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 6194463
    Abstract: &agr;-Amino acid amides of formula (I) wherein the substituents are defined as follows: n is a number zero or one; R1 to R7 are as defined herein; R8 is C1-C6alkyl, C3-C6alkenyl or C3-C6alkynyl; R9 is C3-C8cycloalkyl; a C1-C6alkyl, C3-C6alkenyl or C3-C6alkynyl group substituted by one or more halogen atoms; or a group (a) wherein p and q are identical or different and are each independently of the other a number zero or one; and R13, R14, R15 and R16 are identical or different and are each independently of the others hydrogen or C1-C4alkyl; X is hydrogen, in which case p and q must have the value zero; phenyl, unsubstituted or mono- or poly-substituted by halogen, nitro, cyano, carboxy, C2-C6alkenyl, C2-C6alkenyl, C1-C6haloalkyl, C3-C6alkenyloxy, C3-C6alkynyloxy, C3-C7cycloalkyl, C1-C6haloalkoxy, C1-C6alkylthio, C1-C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl, C3-C6alkynyloxycarbonyl, C1-C6or by C1-C6alkoxy, cyano, —COOR17; —COR18 or a group (b) wherein R17 and R21 are each independently of the other
    Type: Grant
    Filed: August 24, 1999
    Date of Patent: February 27, 2001
    Assignee: Novartis Crop Protection, Inc.
    Inventor: Martin Zeller
  • Patent number: 6191170
    Abstract: The invention provides compounds, compositions and methods relating to novel aromatic derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.
    Type: Grant
    Filed: January 7, 1999
    Date of Patent: February 20, 2001
    Assignee: Tularik Inc.
    Inventor: Julio C. Medina
  • Patent number: 6174923
    Abstract: Compounds characterized generally as ethynyl alanine amino diol derivatives are useful to treat disorders mediated by plasma renin activity.
    Type: Grant
    Filed: January 28, 1999
    Date of Patent: January 16, 2001
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran