Bicyclo Ring System Having The Hetero Ring As One Of The Cyclos (e.g., Methylenedioxyphenyl Group, Etc.) Patents (Class 514/464)
  • Patent number: 6136836
    Abstract: A composition and method for controlling warm-blooded animal parasites comprising 1-[3-chloro-4-(1,1,2-trifluoro-2-trifluoromethoxyethoxy)phenyl]-3-(2,6,dif luorobenzoyl)urea.
    Type: Grant
    Filed: July 30, 1999
    Date of Patent: October 24, 2000
    Assignee: Isagro S.p.A.
    Inventors: Franco Bettarini, Paolo Piccardi
  • Patent number: 6133263
    Abstract: Novel nonpeptide endothelin antagonists with ether-linked groups are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating atherosclerosis, restenosis, Raynaud's phenomenon, mild or severe congestive heart failure, cerebral ischemia, cerebral infarction, embolic stroke, cerebral vasospasm, subarachnoid hemorrhage, hemorrhagic stroke, diabetes, gastric ulceration and mucosal damage, ischemnic bowel disease, Chrohn's disease, essential or malignant hypertension, pulmonary hypertension, pulmonary hypertension after bypass, acute respiratory distress syndrome, chronic obstructive pulmonary diseases, male penile erectile dysfunction, cancer, especially malignant hemangicendothelioma or prostate cancer, myocardial infarction or ischemia, acute or chronic renal failure, renal ischemia, radiocontrast-induced nepbrotoxicity, endotoxic, septic, hemorrhagic shock, angina, preeclampsia, asthma, arhythmias, benign prostatic hyperplasia, and elevated lev
    Type: Grant
    Filed: August 3, 1998
    Date of Patent: October 17, 2000
    Assignee: Warner-Lambert Company
    Inventors: Xue-Min Cheng, Annette Marian Doherty, William Chester Patt, Joseph Thomas Repine
  • Patent number: 6130251
    Abstract: The invention relates to new alkoximinoacetic acid amides, a process for their preparation and their use as agents for combating pests.
    Type: Grant
    Filed: July 23, 1997
    Date of Patent: October 10, 2000
    Assignee: Bayer Aktiengesellschaft
    Inventors: Thomas Seitz, Gerd Hanssler, Klaus Stenzel
  • Patent number: 6107334
    Abstract: The present invention is directed towards the control of inflammation. More specifically there are provided herein dietary fatty acid regimens that may be used to inhibit the increase of serum arachidonic acid when GLA is provided as a dietary supplement.
    Type: Grant
    Filed: February 23, 1998
    Date of Patent: August 22, 2000
    Assignee: Wake Forest University
    Inventor: Floyd H. Chilton
  • Patent number: 6107339
    Abstract: The derivatives of esters of carboxylic acids represented by the general formula I: ##STR1## wherein: R.sub.1 is an alkyl group having a chain or branched chain of 1 to 4 carbon atoms; andR.sub.2 is a group represented by the following general formulae II, III or IV; ##STR2## wherein: R.sub.3 is a hydrogen atom or a methyl group;X is an oxygen atom or a methylidene group;R.sub.4 is an hydrogen atom or an ethynyl group;R.sub.5 and R.sub.6 are alike or differently selected from the group consisting of hydrogen, fluorine, chlorine atoms or methyl group;R.sub.7 is a hydrogen atom or a trifluoromethyl group;R.sub.8 is selected from the group consisting of propargyl, methoxymethyl or methylthio groups; orR.sub.7 and R.sub.8 may combine with each other to form a methylenedioxy chain; and the process for manufacturing the same, and the insecticides and the insect proofing agents containing the same as an active ingredient.
    Type: Grant
    Filed: November 1, 1996
    Date of Patent: August 22, 2000
    Assignee: Dainihon Jochugiku Co., Ltd.
    Inventors: Yoshio Katsuda, Koji Nakayama, Yoshihiro Minamite
  • Patent number: 6087402
    Abstract: The present invention relates to a foam composition for killing dust mites comprising an acaricidal agent, polymer, ether solvent, perfume, surfactant and water.
    Type: Grant
    Filed: September 26, 1997
    Date of Patent: July 11, 2000
    Assignee: Colgate Palmolive Company
    Inventors: Germaine Zocchi, Pierre Fonsny
  • Patent number: 6080792
    Abstract: The present invention relates to a foam composition for killing dust mites comprising an acaricidal agent, polymer, ether solvent, perfume, surfactant and water.
    Type: Grant
    Filed: September 25, 1997
    Date of Patent: June 27, 2000
    Assignee: Colgate Palmolive Company
    Inventors: Germaine Zocchi, Pierre Fonsny
  • Patent number: 6046232
    Abstract: Disclosed are novel .alpha.-aryl-N-alkylnitrone compounds and pharmaceutical compositions containing such compounds. The disclosed compositions are useful as therapeutics for preventing and/or treating neurodegenerative, autoimmune and inflammatory conditions in mammals and as analytical reagents for detecting free radicals.
    Type: Grant
    Filed: October 15, 1998
    Date of Patent: April 4, 2000
    Assignee: Centaur Pharmaceuticals, Inc.
    Inventors: Judith A. Kelleher, Kirk R. Maples, Alina Dykman, Yong-Kang Zhang, Allan L. Wilcox, Julian Levell
  • Patent number: 6040339
    Abstract: Compounds of formula (I): ##STR1## wherein: R.sup.1 is alkyl; R.sup.2a, R.sup.2b, R.sup.2c and R.sup.2d are the same or different and each is hydrogen, optionally substituted alkyl or various other organic groups; R.sup.3 is alkyl; R.sup.4 is a group of formula (II), (III), (IV), (V), (VI), (VII), (VIII) or (IX): ##STR2## wherein: A.sup.1 is a single bond, alkylene or alkenylene; A.sup.2 is or alkenylene; A.sup.3 is a single bond, alkyleneor alkenylene; R.sup.5a and R.sup.5b are the same or different and each is hydrogen, alkyl or various other groups; R.sup.6 is alkyl or phenyl; R.sup.7 is hydrogen or alkyl; R.sup.8 is alkyl or various other groups; and n is 0 and pharmaceutically acceptable salts thereof have valuable inhibitory activity against acyl-CoA: cholesterol acyl transferase.
    Type: Grant
    Filed: May 28, 1998
    Date of Patent: March 21, 2000
    Assignee: Sankyo Company, Limited
    Inventors: Akira Yoshida, Kozo Oda, Takashi Kasai, Kousei Shimada, Hiroshi Kogen, Ichiro Hayakawa, Sadao Ishihara, Teiichiro Koga, Eiichi Kitazawa, Taro Tokui
  • Patent number: 6017916
    Abstract: Novel nonpeptide antagonists of endothelin I are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, myocardial ischemia, cerebral vasospasm, cerebral ischemia, cerebral infarction, cirrhosis, septic shock, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, stroke, benign prosthatic hyperplasia (BPH), and diabetes.
    Type: Grant
    Filed: January 22, 1997
    Date of Patent: January 25, 2000
    Assignee: Warner-Lambert Company
    Inventors: Kent Alan Berryman, Annette Marian Doherty, Jeremy John Edmunds, William Chester Patt, Mark Stephen Plummer, Joseph Thomas Repine
  • Patent number: 6017951
    Abstract: Novel nonpeptides characterized as having a carbamic group which are antagonists of endothelin I are described, as well as methods for their preparation and pharmaceutical compositions containing the same. The compounds are useful in treating elevated levels of endothelin and are therefore useful in the treatment of hypertension, myocardial infarction, diabetes, cerebral vasospasm, cirrhosis, septic shock, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythminas, asthma, chronic and acute renal failure, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, stroke, head injury, and ischemic bowel syndrome.
    Type: Grant
    Filed: February 10, 1999
    Date of Patent: January 25, 2000
    Assignee: Warner-Lambert Company
    Inventors: William C. Patt, Bill R. Reisdorph, Joseph T. Repine
  • Patent number: 6013836
    Abstract: This invention relates to N'-substituted-N,N'-disubstitutedhydrazines of formula I ##STR1## wherein X and X' are independently O, S, or NR; A' and B' are independently substituted or unsubstituted aryl or aromatic heterocycle; wherein F is alkyl, alkenyl, or aralkyl; and wherein E is a tertiary carbon containing organic radical having a total of at least four carbon and halogen atoms but not more than six halogen atoms, or a non-tertiary carbon containing non-haloalkyl organic or organometallic radical having at least five atoms other than hydrogen, oxygen and halogen which are useful as insecticides, compositions containing those compounds, methods of producing the compounds, and methods of their use. More particularly, the invention relates to insect growth regulating compounds and compositions, and methods of using such compounds and compositions. Compounds of the present invention are particularly suitable for controlling plant-destructive insects in crops of cultivated plants, ornamentals and forestry.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: January 11, 2000
    Assignee: Rohm and Haas Company
    Inventors: Adam Chi-Tung Hsu, Harold Ernest Aller, Dat Phat Le, Donald Wesley Hamp, Barry Weinstein, Raymond August Murphy
  • Patent number: 6004957
    Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
    Type: Grant
    Filed: July 22, 1998
    Date of Patent: December 21, 1999
    Assignee: Vertex Pharmaceuticals, Incorporated
    Inventors: Roger D. Tung, Mark A. Murcko, Govinda R. Bhisetti
  • Patent number: 6004988
    Abstract: Carboxylic acid derivatives of the formula I ##STR1## here R.sup.1 is a tetrazole [sic], nitrile [sic], a group COOH or a radical which can be hydrolyzed to COOH, and the other substituents have the meaning explained in the description.
    Type: Grant
    Filed: February 24, 1998
    Date of Patent: December 21, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Wilhelm Amberg, Andreas Kling, Dagmar Klinge, Hartmut Riechers, Liliane Unger, Manfred Raschack, Stefan Hergenroder, Bernd Elger, Sabine Schult
  • Patent number: 5998408
    Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.
    Type: Grant
    Filed: October 8, 1997
    Date of Patent: December 7, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Robert K. Baker, Frank Kayser, Jianming Bao, Andrew Kotliar, William H. Parsons, Kathleen M. Rupprecht
  • Patent number: 5994270
    Abstract: Plant disease caused by soil-borne fungus Gaeumannonyces graminis (Gg) is controlled by applying to the seed or the soil a fungicide which has the following general formula: ##STR1##
    Type: Grant
    Filed: September 11, 1996
    Date of Patent: November 30, 1999
    Assignee: Monsanto Company
    Inventors: Dennis Paul Phillion, Matthew James Graneto, John Kennedy Pratt, Sai Chi Wong
  • Patent number: 5990157
    Abstract: The present invention relates to a foam composition for killing dust mites comprising an acaricidal agent, polymer, ether solvent, perfume, surfactant and water.
    Type: Grant
    Filed: July 2, 1998
    Date of Patent: November 23, 1999
    Assignee: Colgate Palmolive Company
    Inventors: Germaine Zocchi, Pierre Fonsny
  • Patent number: 5985870
    Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
    Type: Grant
    Filed: December 19, 1997
    Date of Patent: November 16, 1999
    Assignee: G.D. Searle & Co.
    Inventors: Daniel P Getman, Gary A. Decrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, Joseph J. McDonald
  • Patent number: 5973011
    Abstract: The present invention describes the use of nitric-oxide-liberating or transferring compounds, stimulators of endogenous NO formation, as well as stimulators of guanylate cyclase, for prevention, treatment and elimination of endothelial dysfunctions and the diseases accompanying these dysfunctions or caused by them, as well as the use of said compounds to produce pharmaceutical products for the cited areas of application.
    Type: Grant
    Filed: September 27, 1996
    Date of Patent: October 26, 1999
    Assignee: ISIS PHARMA GmbH
    Inventors: Eike Albrecht Noack, Georg Kojda
  • Patent number: 5962515
    Abstract: Process for isolation of 1-(3,4-methylenedioxy-phenyl)-1E-tetradecene from Piper longum. Processes for synthesis of 1-(3,4-methylenedioxy-phenyl)-1E-tetradecene; its stereoisomers and analogues are disclosed. The compounds isolated and synthesized according to this invention have immunomodulatory properties and can be used to treat tumors and infections.
    Type: Grant
    Filed: May 29, 1997
    Date of Patent: October 5, 1999
    Assignee: National Institute of Immunology
    Inventors: Shakti N. Upadhyay, Ram A. Vishwakarma, Sabari Ghosal, Supriya Shukla, Chanda Bose, Anita Kamra
  • Patent number: 5955491
    Abstract: The present invention provides a cathepsin L inhibitor containing a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or an arylalkyl, heterocyclic-alkyl or lower alkyl group which may be substituted; R.sup.2 and R.sup.3 independently are a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.4 is an alkanoyl, sulfonyl, carbonyloxy, carbamoyl or thiocarbamoyl group which may be substituted; X is formula: --CHO or --CH.sub.2 OB (wherein B is a hydrogen atom or a protecting group of hydroxyl group); m and n independently are an integer of 0 or 1; provided that R.sup.4 is an alkanoyl group substituted by aryl, a sulfonyl group substituted by aryl having more than 9 carbon atoms or by lower alkyl, or a carbamoyl or thiocarbamoyl group which may be substituted when R.sup.1 is an unsubstituted lower alkyl, arylalkyl on methylthioethyl group, R.sup.2 and R.sup.3 independently are a lower alkyl or arylalkyl, X is --CHO, m is 1 and n is 0 or 1, or a salt thereof.
    Type: Grant
    Filed: June 27, 1995
    Date of Patent: September 21, 1999
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Sohda, Yukio Fujisawa, Tsuneo Yasuma, Junji Mizoguchi, Masakuni Kori, Masayuki Takizawa
  • Patent number: 5952386
    Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.
    Type: Grant
    Filed: September 24, 1997
    Date of Patent: September 14, 1999
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Sanshiro Matsuo, Taro Hirose, Keiichi Izumi, Masaya Suzuki, Noriyasu Sakamoto, Kazunori Tsushima, Shigeru Saito, Hirotaka Takano
  • Patent number: 5939430
    Abstract: The combination of compounds of formula I and II can be used for the treatment of retroviraI infections. The combination can be used to treat AIDS and ARC and other diseases caused by the retrovirus HTV or other related viruses.
    Type: Grant
    Filed: July 20, 1995
    Date of Patent: August 17, 1999
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: A. Stanley Tyms, Debra L. Taylor
  • Patent number: 5929114
    Abstract: Arylthiol and dithiobisarylamide antibacterial and antiviral agents have the general formula ##STR1## where A is monocyclic or bicyclic aryl which can contain up to 3 heteroatoms selected from O, S, and N,R.sup.1 and R.sup.2 are substituent groups, X is ##STR2## or SO.sub.2 NR.sup.4 Z, Y is H or SZ when n is 1, a single bond when n is 2; R.sup.4 and Z can be hydrogen or alkyl.
    Type: Grant
    Filed: May 15, 1997
    Date of Patent: July 27, 1999
    Assignee: Warner-Lambert Company
    Inventors: John Michael Domagala, Edward Faith Elslager, Rocco Dean Gogliotti
  • Patent number: 5922759
    Abstract: Novel nonpeptides characterized as having a carbarimic group which are antagonists of endothelin I are described, as well as methods for their preparation and pharmaceutical compositions containing the same. The compounds as useful in treating elevated levels of endothelin and are therefore used in the treatment of hypertension, myocardial infarction, diabetes, cerebral vasospasm, cirrhosis, septic shock, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, chronic and acute renal failure, preeclamnpsia, atherosclerotic disorders including Raynaud's disease and restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, stroke, head injury, and ischemic bowel syndrome.
    Type: Grant
    Filed: December 15, 1997
    Date of Patent: July 13, 1999
    Assignee: Warner-Lambert Company
    Inventors: William C. Patt, Bill R. Reisdorph, Joseph T. Repine
  • Patent number: 5906992
    Abstract: The present invention relates to a foam composition for killing dust mites comprising an acaricidal agent, polymer, ether solvent, perfume, surfactant and water.
    Type: Grant
    Filed: November 21, 1996
    Date of Patent: May 25, 1999
    Assignee: Colgate Palmolive Company
    Inventors: Pierre Fonsny, Germaine Zocchi
  • Patent number: 5902587
    Abstract: Camomile oil having a high cis- and trans-spiroether content is produced in a process which includes steam distillation or aqueous distillation of fresh camomile or an extraction residue of camomile.
    Type: Grant
    Filed: July 1, 1992
    Date of Patent: May 11, 1999
    Assignee: ASTA Medica Aktiengesellschaft
    Inventors: Reinhold Carle, Otto Isaac
  • Patent number: 5898036
    Abstract: The method of this invention is directed to a treatment of depression in men and women and to a treatment of pre-menstrual syndrome (PMS) in women by administering to a patient a therapeutically effective amount of chromium in a pharmaceutically acceptable form either alone or in conjunction with the administration of a standard antidepressant composition, such as a selective serotonin reuptake inhibitor composition. Chromium, preferably in the form of chromium picolinate, is administered to the patient at dosages in a preferred range of about 200 to about 500 micrograms chromium.
    Type: Grant
    Filed: February 19, 1998
    Date of Patent: April 27, 1999
    Inventor: Malcolm N. McLeod
  • Patent number: 5889046
    Abstract: The present invention discloses a preventive or ameliorant of hypertension or medical symptoms caused by it and a food or beverage that prevents or ameliorates hypertension or medical symptoms caused by it that contain for its active ingredient dioxabicyclo?3.3.0!octane derivative represented by the formula (2). ##STR1## wherein, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are respectively and independently a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, or R.sup.1 and R.sup.2 and/or R.sup.4 and R.sup.5 collectively represent a methylene group or ethylene group, and n, m and L represent 0 or 1.
    Type: Grant
    Filed: February 1, 1996
    Date of Patent: March 30, 1999
    Assignee: Suntory Limited
    Inventors: Kengo Akimoto, Shiro Morimoto, Yasuo Matsumura, Hajime Yoshizumi, Tetsuo Murakami
  • Patent number: 5880147
    Abstract: Compounds of formula (I): ##STR1## wherein: R.sup.1 is alkyl; R.sup.2a, R.sup.2b, R.sup.2c and R.sup.2d are the same or different and each is hydrogen, optionally substituted alkyl, --(C.dbd.O)--B.sup.1 (wherein B.sup.1 is hydrogen or alkyl), nitro, --NR.sup.c R.sup.d (wherein R.sup.c is hydrogen or alkyl and Rd is alkyl), hydroxy, protected hydroxy group, alkoxy, cyano, alkylthio, alkylsulfinyl, alkylsulfonyl or halogen;R.sup.3 is alkyl; R.sup.4 is a group of the formula (II) ##STR2## wherein A.sup.1 is a single bond, alkylene or alkenylene; R.sup.5a and R.sup.5b are the same or different and each is hydrogen, alkyl or --A.sup.4 R.sup.5.sub.c wherein A is a single bond, alkylene or alkenylene and R.sup.5.sub.c is alkoxy; and n is 0, and pharmaceutically acceptable salts thereof. Such compounds have valuable inhibitory activity against acyl-CoA (cholesterol acyl transferase).
    Type: Grant
    Filed: September 18, 1996
    Date of Patent: March 9, 1999
    Assignee: Sankyo Company, Limited
    Inventors: Akira Yoshida, Kozo Oda, Takashi Kasai, Kousei Shimada, Hiroshi Kogen, Ichiro Hayakawa, Sadao Ishihara, Teiichiro Koga, Eiichi Kitazawa, Taro Tokui
  • Patent number: 5866609
    Abstract: Disclosed herein are substituted vinylurea derivatives represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.3 are independently a phenyl group which may be substituted, R.sup.2 is a phenyl group which may be substituted, or a cycloalkyl group, and wave lines mean that the bonding state may be either E or Z, with the proviso that the cases where R.sup.1, R.sup.2 and R.sup.3 are unsubstituted phenyl groups, and where R.sup.1 and R.sup.2 are unsubstituted phenyl groups and R.sup.3 is a 4-ethoxyphenyl group are excluded, or salt thereof, and medicines comprising such a derivative as an active ingredient as well as a method of preventing and treating arteriosclerosis with such a medicine. The derivatives or salts thereof selectively and strongly inhibit ACAT in macrophages and are hence useful as prophylactic and therapeutic agents for arteriosclerosis.
    Type: Grant
    Filed: July 24, 1997
    Date of Patent: February 2, 1999
    Assignee: SS Pharmaceutical Co., Ltd.
    Inventors: Yoshihiko Kanamaru, Hiroyuki Hirota, Akihiro Shibata, Teruo Komoto, Hiroyuki Naito, Koichi Tachibana, Mari Ohtsuka, Fumio Ishii, Susumu Sato
  • Patent number: 5852052
    Abstract: The invention refers to the treatment and prevention of lyso paf-mediated disorders with an effective amount of at least one antagonists against lyso paf receptors. Lyso paf or paf receptor antagonists were administered with or without an antagonist against production of ether phospholipids. Lyso paf antagonists are Ginkgoloides which are administered, for example, by food or topically.
    Type: Grant
    Filed: December 9, 1996
    Date of Patent: December 22, 1998
    Assignee: Ruth Korth
    Inventor: Ruth Korth
  • Patent number: 5840753
    Abstract: The present invention relates to the derivatives of formula: ##STR1## and to their use in therapeutics, especially as drugs with anti-inflammatory and analgesic properties.
    Type: Grant
    Filed: March 24, 1997
    Date of Patent: November 24, 1998
    Assignee: Laboratories UPSA
    Inventors: Eric Nicolai, Jean-Marie Teulon
  • Patent number: 5824665
    Abstract: A method of reducing hair growth in a mammal includes applying, to an area of skin from which reduced hair growth is desired, a dermatologically acceptable composition containing a suppressor of the metabolic pathway for the conversion of glucose to acetyl-CoA.
    Type: Grant
    Filed: April 23, 1997
    Date of Patent: October 20, 1998
    Inventors: James Henry, Gurpreet Ahluwalia, Douglas Shander
  • Patent number: 5817693
    Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.
    Type: Grant
    Filed: November 9, 1994
    Date of Patent: October 6, 1998
    Inventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
  • Patent number: 5814657
    Abstract: Compounds of the formula ##STR1## wherein the variables are defined as in the specification, are capable of lowering introaocular pressure in the eye of a mammal.
    Type: Grant
    Filed: November 21, 1997
    Date of Patent: September 29, 1998
    Assignee: Allergan
    Inventors: Robert M. Burk, David F. Woodward
  • Patent number: 5783701
    Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
    Type: Grant
    Filed: February 23, 1995
    Date of Patent: July 21, 1998
    Assignee: Vertex Pharmaceuticals, Incorporated
    Inventors: Roger D. Tung, Mark A. Murcko, Govinda Rao Bhisetti
  • Patent number: 5780592
    Abstract: A composition comprising lipoproteins and a compound of the formula I ##STR1## stereoisomeric form or salt thereof, suitable for the treatment of immunological disorders, cancer or in transplantation.
    Type: Grant
    Filed: December 10, 1996
    Date of Patent: July 14, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Stefan Mullner, Axel Hofmann, Karin Saar, Hans-Ulrich Schorlemmer, Robert Bartlett
  • Patent number: 5767154
    Abstract: The invention relates to the use of derivatives of F-type prostaglandins as ocular hypotensives. The PGF derivatives used in accordance with the invention are encompassed by the following structure formula I: ##STR1## wherein wavy line attachments indicate either the alpha (a) or beta (b) configuration; hatched lines indicate a configuration, solid triangles are used to indicate b configuration, dashed bonds represent a double bond, or a single bond; n is 0, or an integer of from 1 to 3; X is NH.sub.2 or OR; R is hydrogen, R.sub.4 or a --(CO)R.sub.4 group; R.sub.1, R.sub.2, and R.sub.3 independently are hydroxyl, or --O(CO)R.sub.5 groups, wherein R.sub.4 and R.sub.5 independently stand for saturated or unsaturated acyclic hydrocarbon having from 1 to 20 carbon atoms, or --(CH.sub.2).sub.m R.sub.6 where m is 0-10 and R.sub.6 is an aliphatic, aromatic or heteroaromatic ring, R.sub.7 and R.sub.8 together are .dbd.
    Type: Grant
    Filed: March 24, 1997
    Date of Patent: June 16, 1998
    Assignee: Allergan
    Inventors: David A. Woodward, Ming F. Chan
  • Patent number: 5756510
    Abstract: A range of 3-oxybenzamide compounds and related quinazolinone compounds are disclosed which can act as potent inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase or PARP enzyme (EC 2.4.2.30), and which thereby can provide useful therapeutic compounds for use in conjunction with DNA-damaging cytotoxic drugs or radiotherapy to potentiate the effects of the latter. The compounds disclosed include 3-benzyloxybenzamides, 3-oxybenzamides in which a chain of 5 or more methylene groups terminate in a halogen atom or in a purin-9-yl moiety, certain benzoxazole-4-carboxamide compounds and certain quinazolinone compounds. In formula X and Y together may form a bride --X--Y-- that represents the grouping (a), (b) or (c )wherein R.sup.5 is H, alkyl, aryl or aralkyl.
    Type: Grant
    Filed: August 30, 1996
    Date of Patent: May 26, 1998
    Assignee: Newcastle University Ventures Limited
    Inventors: Roger John Griffin, Alan Hilary Calvert, Nicola Jane Curtin, David Richard Newell, Bernard Thomas Golding
  • Patent number: 5753660
    Abstract: Selected sulfonylalkanoylamino hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
    Type: Grant
    Filed: November 13, 1996
    Date of Patent: May 19, 1998
    Assignee: G. D. Searle & Co.
    Inventors: James A. Sikorski, Daniel P. Getman, Gary A. DeCrescenzo, Balekudru Devadas, John N. Freskos, Hwang-Fun Lu, Joseph J. McDonald
  • Patent number: 5744494
    Abstract: The anthelmintic efficacy in animals and humans of a benzimidazole such as fenbendazole, albendazole, oxfendazole or trichlabendazole is potentiated by use with piperonyl butoxide or other methylenedioxyphenyl synergist.
    Type: Grant
    Filed: July 25, 1995
    Date of Patent: April 28, 1998
    Assignee: British Technology Group Limited
    Inventors: Quintin Archibald McKellar, Hafid Abdelaali Benchaoui
  • Patent number: 5741483
    Abstract: An industrial preservative antifungal composition containing and underwater antifouling composition comprising 4,5-dichloro-2-n-octyl-4-isothiazoline-3-one and/or 2-n-octyl-4-isothiazoline-3-one or salts thereof and 5-?2-(2-butoxyethoxy)ethoxymethyl!-6-propyl-1,3-benzodioxole and/or octachlorodipropyl ether as supplementary agent(s).
    Type: Grant
    Filed: May 3, 1996
    Date of Patent: April 21, 1998
    Assignee: Rohm and Haas Company
    Inventor: Shozo Okawa
  • Patent number: 5739166
    Abstract: A class of terphenyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: ##STR1## wherein each of R.sup.2 and R.sup.3 is independently selected from hydrido and halo; or wherein R.sup.2 and R.sup.3 together form --OCH.sub.2 O--; wherein each of R.sup.6 through R.sup.8 is independently selected from hydrido, lower alkyl, halo, lower alkoxy, lower haloalkyl, and lower dialkylamino; or wherein R.sup.6 and R.sup.7 together form --OCH.sub.2 O; and wherein R.sup.12 is selected from lower alkylsulfonyl and aminosulfonyl; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: November 29, 1994
    Date of Patent: April 14, 1998
    Assignee: G.D. Searle & Co.
    Inventors: David B. Reitz, Jinglin Li, Monica B. Norton
  • Patent number: 5726195
    Abstract: Certain novel aminoacyl adenylate mimics are described. An exemplary compound of this invention is ?S-(R*,R*)!-3,6-anhydro-1,2-dideoxy-1-?5-?4-?(5-nitro-2-thienyl)ethynyl!ph enyl!-2H-tetrazol-2-yl!-D-allo-heptitol 7-(2-amino-3-methyl-1-oxopentyl)sulfamate. These compounds inhibit isoleucyl-tRNA synthetases and are useful as antimicrobial and antiparasitic agents.
    Type: Grant
    Filed: July 16, 1996
    Date of Patent: March 10, 1998
    Assignee: Cubist Pharmaceuticals, Inc.
    Inventors: Jason M. Hill, Guixue Yu, Youe-Kong Shue, Thomas M. Zydowsky, Julius Rebek
  • Patent number: 5719182
    Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.
    Type: Grant
    Filed: May 16, 1995
    Date of Patent: February 17, 1998
    Assignee: SmithKline Beecham Corporation
    Inventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
  • Patent number: 5719183
    Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: February 17, 1998
    Assignee: SmithKline Beecham Corporation
    Inventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
  • Patent number: 5716985
    Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.
    Type: Grant
    Filed: May 23, 1995
    Date of Patent: February 10, 1998
    Assignee: SmithKline Beecham Corporation
    Inventors: John Duncan Elliott, Maria Amparo Lago
  • Patent number: 5716984
    Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.
    Type: Grant
    Filed: May 16, 1995
    Date of Patent: February 10, 1998
    Assignee: SmithKline Beecham Corporation
    Inventors: Russell Donovan Cousins, John Duncan Elliott
  • Patent number: 5705500
    Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: January 6, 1998
    Assignee: G.D. Searle & Co.
    Inventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, Joseph J. McDonald