Three Or More Hetero Atoms In The Hetero Ring Patents (Class 514/435)
  • Publication number: 20150126437
    Abstract: The disclosure provides compounds useful as insect repellents, compositions comprising such repellents, and methods of repelling an arthropod using such compounds and compositions. The disclosure further provides insect traps and method for identifying ligands and cognates for biological molecules.
    Type: Application
    Filed: October 17, 2012
    Publication date: May 7, 2015
    Applicant: The Regents of the University of California
    Inventors: Anandasankar Ray, Sean Michael Boyle
  • Patent number: 8951992
    Abstract: The present invention is directed to methods and compounds for inhibiting bacterial growth and treating a bacterial infection in a subject. These methods involve providing an inhibitor of intrabacterial pH homeostasis, including inhibitors of the Mycobacterium tuberculosis Rv3671c gene encoded membrane protease. Methods for identifying novel compounds that disrupt intrabacterial pH homeostasis and their use for inhibiting bacterial growth and treating a bacterial infection in a subject are also disclosed.
    Type: Grant
    Filed: July 20, 2009
    Date of Patent: February 10, 2015
    Assignee: Cornell University
    Inventors: Carl Nathan, Sabine Ehrt, Omar Vandal, Crystal Darby
  • Patent number: 8901170
    Abstract: Compounds of formula (I) wherein the symbols have the meaning given in the specification, as well as processes for preparing the compounds (I), pesticidal compositions and synergistic mixtures comprising compounds (I), methods for the control of insects, acarids or nematodes by contacting the pests or their food supply, habitat or breeding grounds with a pesticidally effective amount of compounds formula (I), and a method for treating, controlling, preventing or protecting animals against infestation or infection by parasites which comprises orally, topically or parenterally administering or applying to the animals a parasiticidally effective amount of compounds of formula (I).
    Type: Grant
    Filed: June 22, 2007
    Date of Patent: December 2, 2014
    Assignee: BASF SE
    Inventors: Matthias Pohlman, Michael Hofmann, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Hassan Oloumi-Sadeghi, Takeo Hokama, Christopher Palmer
  • Patent number: 8815936
    Abstract: Described is a composition for preventing or treating an oxidative stress related disease or condition in a subject. The disease or condition is characterized by the presence of excess oxidative compounds in the subject, and the composition includes a synergistic combination of therapeutically effective amounts of resveratrol to promote NAD+ synthesis in the subject; a chelating agent to reduce production of additional oxidative compounds in the subject; and an antioxidant to minimize the oxidative activity in the subject.
    Type: Grant
    Filed: March 3, 2009
    Date of Patent: August 26, 2014
    Assignee: Nad Life Pty Ltd
    Inventors: Ross Stewart Grant, Nady Braidy, Gilles Guillemin, George Smythe
  • Patent number: 8476233
    Abstract: The subject invention pertains to materials and methods for the prevention and treatment of disease conditions associated with oxidative stress or a compromised reducing environment, including inflammatory bowel diseases such as ulcerative colitis. Another aspect of the subject invention concerns compositions formulated for administration as an enema. The subject invention also concerns compositions formulated for oral administration. Methods of the invention include administration of compounds or compositions of the invention. In one embodiment, compounds or compositions of the invention are rectally instilled in a patient. In another embodiment, compounds or compositions are orally administered.
    Type: Grant
    Filed: June 13, 2008
    Date of Patent: July 2, 2013
    Assignee: Therapeutic Research, LLC
    Inventor: Jay Pravda
  • Publication number: 20120208850
    Abstract: The invention relates to methods, compounds, and compositions for delivering 1,3-propanedisulfonic acid (1,3PDS) in a subject, preferably a human subject. The invention encompasses compounds that will yield or generate 1,3PDS, either in vitro or in vivo. The invention also relates to sulfonate ester prodrugs of 1,3PDS as well as Gemini dimmers and oligomers of 1,3PDS for the prevention or treatment of associated diseases and conditions.
    Type: Application
    Filed: August 6, 2010
    Publication date: August 16, 2012
    Applicant: BELLUS HEALTH INC.
    Inventors: Xianqi Kong, Nigel Levens, Abderrahim Bouzide, Stephane Ciblat, Richard Frenette, Johanne Renaud
  • Patent number: 8026274
    Abstract: The subject invention provides a method of treating burn-induced weight loss in a burn patient which comprises administering a therapeutically effective amount of an oxandrolone to the patient. The invention also provides a method of treating a wound in a patient suffering from a wound which comprises administering a therapeutically effective amount of an oxandrolone to the patient. The subject invention further provides a method of treating burn-induced weight loss in a burn patient which comprises administering a therapeutically effective amount of an oxandrolone in conjunction with a protein supplement to the patient.
    Type: Grant
    Filed: March 12, 2004
    Date of Patent: September 27, 2011
    Assignee: Savient Pharmaceuticals, Inc.
    Inventor: Don Fishbein
  • Publication number: 20100215777
    Abstract: Compounds of formula (I) wherein the symbols have the meaning given in the specification, as well as processes for preparing the compounds (I), pesticidal compositions and synergistic mixtures comprising compounds (I), methods for the control of insects, acarids or nematodes by contacting the pests or their food supply, habitat or breeding grounds with a pesticidally effective amount of compounds formula (I), and a method for treating, controlling, preventing or protecting animals against infestation or infection by parasites which comprises orally, topically or parenterally administering or applying to the animals a parasiticidally effective amount of compounds of formula (I).
    Type: Application
    Filed: June 22, 2007
    Publication date: August 26, 2010
    Applicant: BASF SE
    Inventors: Matthias Pohlman, Michael Hofmann, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Hassan Oloumi-Sadeghi, Takeo Hokama, Christopher Palmer
  • Patent number: 7144985
    Abstract: The invention relates to methods of determining islet cell activity by detecting the level of Archipelin or a fragment thereof and comparing the level to a baseline level or range associated with a known islet cell activity. Such methods are useful in diagnosing and studying the development of diabetes.
    Type: Grant
    Filed: December 2, 2002
    Date of Patent: December 5, 2006
    Assignee: Metabolex, Inc.
    Inventors: Jeffrey D. Johnson, John E. Blume, John F. Palma, Yun-Ping Zhou
  • Patent number: 6825226
    Abstract: The invention relates to the discovery that specific adamantyl or adamantyl group derivatives containing retinoid-related compounds induce apoptosis of cancer cells and therefore may be used for the treatment of cancer, including advanced cancer. Also, the present invention relates to novel adamantyl or adamantyl group derivatives containing retinoid compounds and their usage for treatment and/or prevention of cancer, keratinization disorders, dermatological conditions, and other therapies More specifically, it has been shown that such adamantyl compounds, e.g., 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoicacid, 2-[3-(1-adamantyl)-4-methoxyphenyl]-5-benzimidazole carboxylic acid, and 6-[3-(1-adamantyl)-4,5-methylenedioxyphenyl]-2-naphthoic acid, can be used to treat or prevent cervical cancers and precancers such as cervical dysplasias, including high grade and low grade dysplasias.
    Type: Grant
    Filed: June 24, 2002
    Date of Patent: November 30, 2004
    Assignee: Galderma Research & Development, S.N.C.
    Inventors: Magnus Pfahl, Xian-Ping Lu, Darryl Rideout, Hongyue Zhang
  • Patent number: 6727258
    Abstract: The present invention relates to compounds of formula (IA): the preparation thereof, pharmaceutical formulations thereof, and their use in medicine as allosteric adenosine receptor modulators for uses including protection against hypoxia and ischemia induced injury and treatment of adenosine-sensitive cardiac arrhythmias.
    Type: Grant
    Filed: March 19, 2001
    Date of Patent: April 27, 2004
    Assignee: King Pharmaceutical Research & Development, Inc.
    Inventor: Pier Giovanni Baraldi
  • Patent number: 6620782
    Abstract: The present invention is directed to novel 2-aminobenzamide thereof, represented by the general Formula I: where R1-R3, X, and A—D are defined herein. The present invention also relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.
    Type: Grant
    Filed: March 16, 2000
    Date of Patent: September 16, 2003
    Assignee: Cytovia, Inc.
    Inventors: Sui Xiong Cai, Yan Wang
  • Patent number: 6548534
    Abstract: This invention describes the new, nonsteroidal gestagens of general formula I in which A, B, Ar1, R1, R2 and R3 have the meanings that are indicated in more detail in the description. The new compounds show a very great affinity to the gestagen receptor. They can be used alone or in combination with estrogens in contraceptive preparations. In addition, they can be used for treating endometriosis. Together with estrogens, they can also be used in preparations for treating gynecological disorders, for treating premenstrual symptoms and for substitution therapy. Based on the androgenic action, they can also be used for male birth control, male HRT and hormone therapy and for treating andrological disease agents.
    Type: Grant
    Filed: July 27, 2001
    Date of Patent: April 15, 2003
    Assignee: Schering Aktiengesellschaft
    Inventors: Manfred Lehmann, Klaus Schoellkopf, Peter Strehlke, Nikolaus Heinrich, Karl-Heinrich Fritzemeier, Rolf Krattenmacher, Hans-Peter Muhn
  • Patent number: 6541506
    Abstract: The invention features enediynes and methods for their production and use. The enediynes of the invention have the formula: wherein R1 is a hydroxyl group or a moiety that can be replaced by a hydroxyl group in a hydrolysis reaction; each R2 is, independently, H or a monovalent hydrocarbon moiety containing between 1 and 4 carbon atoms, inclusive; R3 is a pyrrole, furan, or thiophene ring; and X is an integer between 4 and 10, inclusive.
    Type: Grant
    Filed: October 5, 2000
    Date of Patent: April 1, 2003
    Assignee: Phytera Incorporated
    Inventors: Baoliang Cui, James Bruce McAlpine, Maureen Kelly Talbot, Shu-Wei Yang, Catherine Heintz, Angela Stafford
  • Patent number: 6462064
    Abstract: The invention relates to the discovery that specific adamantyl or adamantyl group derivatives containing retinoid-related compounds induce apoptosis of cancer cells and therefore may be used for the treatment of cancer, including advanced cancer. Also, the present invention relates to novel adamantyl or adamantyl group derivatives containing retinoid compounds and their usage for treatment and/or prevention of cancer, keratinization disorders, dermatological conditions, and other therapies More specifically, it has been shown that such adamantyl compounds, e.g., 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid, 2-[3-(1-adamantyl)-4-methoxyphenyl]-5-benzimidazole carboxylic acid, and 6-[3-(1-adamantyl)-4,5-methylenedioxyphenyl]-2-naphthoic acid, can be used to treat or prevent cervical cancers and precancers such as cervical dysplasias, including high grade and low grade dysplasias.
    Type: Grant
    Filed: February 4, 2000
    Date of Patent: October 8, 2002
    Assignee: Galderma Research & Development S.N.C.
    Inventors: Magnus Pfahl, Xian-Ping Lu, Darryl Rideout, Hongyue Zhang
  • Patent number: 6221896
    Abstract: This invention relates to an insecticidal and miticidal composition which contains as active ingredients chlorfenapyr in combination with one or more compounds selected from the group consisting of benzoepin, nereistoxin-type insecticidal agents and diafenthiuron.
    Type: Grant
    Filed: May 24, 1999
    Date of Patent: April 24, 2001
    Assignee: American Cyanamid Co.
    Inventor: Toshiki Fukuchi
  • Patent number: 6127415
    Abstract: The present invention relates to specific adamantyl or adamantyl group derivative containing retinoid compounds induce apoptosis of cancer cells. These adamantyl retinoid derivatives are useful for the treatment of many cancers and solid tumors, especially androgen-independent prostate cancer, skin cancer, pancreatic carcinomas, colon cancer, melanoma, ovarian cancer, liver cancer, small cell lung carcinoma, non-small cell lung carcinoma, cervical carcinoma, brain cancer, bladder cancer, breast cancer, neuroblastoma/glioblastoma, and leukemia. Also, the invention relates to novel adamantyl or adamantyl group derivative compounds which are useful as active agents for the treatment or prevention of keratinization disorders and other dermatological conditions, and other diseases.
    Type: Grant
    Filed: April 14, 1999
    Date of Patent: October 3, 2000
    Assignee: Galderma Research & Development, S.N.C.
    Inventors: Magnus Pfahl, Xian-Ping Lu, Darryl Rideout, Hongyue Zhang
  • Patent number: 5869520
    Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.
    Type: Grant
    Filed: January 8, 1997
    Date of Patent: February 9, 1999
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Raymond W. Kosley, Jr., Robert Joseph Cherill, Gerard O'Malley
  • Patent number: 5856323
    Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: January 5, 1999
    Assignee: CytoMed, Inc.
    Inventors: Xiong Cai, Sajjat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
  • Patent number: 5827876
    Abstract: This invention relates to 3-(4-acrylamidobenzoyl)benzo?b! thiophenes, to the process for their preparation, to pharmaceutical compositions and to their use for modifying the balance between bone resorption and bone production in a mammal. The compounds useful in this invention are represented by the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl containing 1-8 carbon atoms, or R.sup.1 and R.sup.2 together with the interposed nitrogen forms a 5-7 membered ring optionally containing an additional heteroatom selected from nitrogen, sulfur or oxygen.
    Type: Grant
    Filed: April 8, 1997
    Date of Patent: October 27, 1998
    Assignee: American Home Products Corporation
    Inventor: Joseph Peter Sabatucci
  • Patent number: 5646175
    Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: July 8, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Raymond W. Kosley, Jr., Robert Joseph Cherill, Gerard O'Malley
  • Patent number: 5543427
    Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.
    Type: Grant
    Filed: August 24, 1994
    Date of Patent: August 6, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Robert J. Cherill, Gerard O'Malley
  • Patent number: 5374650
    Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.
    Type: Grant
    Filed: March 25, 1993
    Date of Patent: December 20, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Raymond W. Kosley, Jr., Robert J. Cherill, Gerard O'Malley
  • Patent number: 5356925
    Abstract: Novel N-(mercaptoalkyl)urea or carbamates of the formulae I and II ##STR1## wherein A is a monocyclic or bicyclic arylene or heteroarylene;Q is hydrogen or R.sub.9 CO--;Y is --O--,--S-- or --NR.sub.8 --;R.sub.1 is lower alkyl, cyclolower alkyl, aryl or heteroaryl;R.sub.2 and R.sub.8 are independently hydrogen; lower alkyl; cyclolower alkyl; substituted lower alkyl; aryl; or heteroaryl;R.sup.3 is --OR.sub.5 or --NR.sub.5 R.sub.6 ;R.sub.4 is --(CH.sub.2).sub.q R.sub.7 ; or R.sub.2 and R.sub.4 and the carbons to which they are attached complete a ring;R.sub.5 and R.sub.6 are hydrogen, lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl or aryl lower alkyl, or R.sub.5 and R.sub.
    Type: Grant
    Filed: February 11, 1993
    Date of Patent: October 18, 1994
    Assignee: Schering Corporation
    Inventors: Bernard R. Neustadt, Alan Bronnenkant
  • Patent number: 5140039
    Abstract: The present invention includes compounds represented by the formula: ##STR1## wherein X is O or S; R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, hydroxy, halo, loweralkoxy, thioalkoxy and loweralkyl; or R.sub.1 and R.sub.2 taken together can form a methylenedioxy or ethylenedioxy bridge;R.sub.3 is loweralkyl;R.sub.4 is selected from ##STR2## wherein Y is O or S, R.sub.6 is hydrogen, methoxy or halo and m is 0 or 1; R.sub.5 is hydrogen, loweralkyl, phenyl or substituted phenyl wherein the phenyl ring is substituted with one, two or three substituents independently selected from loweralkyl, halo, hydroxy, loweralkoxy, amino and thioalkoxy; andR.sub.8 hydrogen or R.sub.3 and R.sub.8 taken together form a pyrrolidine ring; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 31, 1991
    Date of Patent: August 18, 1992
    Assignee: Abbott Laboratories
    Inventors: John F. DeBernardis, David L. Arendsen, Robert E. Zelle
  • Patent number: 5045562
    Abstract: 1,3,5-trithiane derivatives represented by the formula (I) ##STR1## wherein the substituents are defined herein, are disclosed. The trithiane derivatives and their compositions are useful as anti-arteriosclerotic or anti-hyperlipemic agents.
    Type: Grant
    Filed: October 17, 1988
    Date of Patent: September 3, 1991
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Masashi Nagamine, Kunikazu Hiraga, Atsushi Sakai, Matazaemon Uchida
  • Patent number: 4942161
    Abstract: The invention relates to the use of beta blockers for the treatment of the progression of infantile axial myopia.
    Type: Grant
    Filed: February 24, 1989
    Date of Patent: July 17, 1990
    Inventor: Heinfried Tiburtius
  • Patent number: 4816475
    Abstract: An anti-arteriosclerotic or anti-hyperlipemic 1,3,5-trithiane derivative according to the formula (I): ##STR1## a pharmaceutical composition containing the same, and a process for producing the same.
    Type: Grant
    Filed: July 14, 1987
    Date of Patent: March 28, 1989
    Assignee: Nihon Nohyaku Co. Ltd.
    Inventors: Masashi Nagamine, Kunikazu Hiraga, Atsushi Sakai, Matazaemon Uchida
  • Patent number: 4804677
    Abstract: Novel compounds of the general formula ##STR1## wherein R.sub.1 is lower alkyl, lower cycloalkyl, lower alkenyl, lower alkynyl, lower alkyl carboxymethyl, aryl carboxymethyl, aryl, or aralkyl; A is a direct bond, lower alkylene, or lower alkenylene; x is 1 or 2, provided that when x is greater than 1, different occurrences of the ##STR2## group may be the same or different; Ar is heterocyclic unsubstituted aromatic or aromatic substituted with lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy, halogen, acetamido, amino, nitro, lower alkylamino, hydroxy, lower hydroxyalkyl or cyano; W is alkylene containing from 1 to about 10 carbon atoms; and B is --NR.sub.2 COR.sub.3, --NR.sub.2 CONR.sub.3 R.sub.4, --NR.sub.2 SO.sub.2 R.sub.3, --NR.sub.2 SO.sub.2 NR.sub.3 R.sub.4, or --NR.sub.2 COOR.sub.5, wherein R.sub.2, R.sub.3, R.sub.4 and R.sub.5 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, alkoxyaryl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.3 and R.
    Type: Grant
    Filed: September 8, 1987
    Date of Patent: February 14, 1989
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Paul W. Erhardt, William L. Matier
  • Patent number: 4725591
    Abstract: Compounds having one or two substituents at the 3-position, represented by the general formula ##STR1## wherein R.sub.1 is an optionally acylated or protected amino group and X is hydrogen atom or methoxy group, or a pharmaceutically acceptable salt thereof; when used either alone or in combination with a .beta.-lactam antibiotic, show excellent .beta.-lactamase inhibitory activity and can be used as drugs for use in humans and domestic animals.
    Type: Grant
    Filed: February 3, 1984
    Date of Patent: February 16, 1988
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Taisuke Matsuo, Mitsuzo Kuno, Kenji Okonogi
  • Patent number: 4551472
    Abstract: Unsymmetrical N-substituted bis-carbamoyl sulfide compounds exhibit exceptional broad spectrum pesticidal activity coupled with extremely low mammalian toxicity and phytotoxicity.
    Type: Grant
    Filed: January 9, 1984
    Date of Patent: November 5, 1985
    Assignee: Union Carbide Corporation
    Inventor: Themistocles D. J. D'Silva