Bicyclo Ring System Having The Hetero Ring As One Of The Cyclos (e.g., Methylenedioxyphenyl Group, Etc.) Patents (Class 514/464)
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Patent number: 6136836Abstract: 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: GrantFiled: July 30, 1999Date of Patent: October 24, 2000Assignee: Isagro S.p.A.Inventors: Franco Bettarini, Paolo Piccardi
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Patent number: 6133263Abstract: 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 levType: GrantFiled: August 3, 1998Date of Patent: October 17, 2000Assignee: Warner-Lambert CompanyInventors: Xue-Min Cheng, Annette Marian Doherty, William Chester Patt, Joseph Thomas Repine
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Patent number: 6130251Abstract: The invention relates to new alkoximinoacetic acid amides, a process for their preparation and their use as agents for combating pests.Type: GrantFiled: July 23, 1997Date of Patent: October 10, 2000Assignee: Bayer AktiengesellschaftInventors: Thomas Seitz, Gerd Hanssler, Klaus Stenzel
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Patent number: 6107334Abstract: 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: GrantFiled: February 23, 1998Date of Patent: August 22, 2000Assignee: Wake Forest UniversityInventor: Floyd H. Chilton
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Patent number: 6107339Abstract: 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: GrantFiled: November 1, 1996Date of Patent: August 22, 2000Assignee: Dainihon Jochugiku Co., Ltd.Inventors: Yoshio Katsuda, Koji Nakayama, Yoshihiro Minamite
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Patent number: 6087402Abstract: The present invention relates to a foam composition for killing dust mites comprising an acaricidal agent, polymer, ether solvent, perfume, surfactant and water.Type: GrantFiled: September 26, 1997Date of Patent: July 11, 2000Assignee: Colgate Palmolive CompanyInventors: Germaine Zocchi, Pierre Fonsny
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Patent number: 6080792Abstract: The present invention relates to a foam composition for killing dust mites comprising an acaricidal agent, polymer, ether solvent, perfume, surfactant and water.Type: GrantFiled: September 25, 1997Date of Patent: June 27, 2000Assignee: Colgate Palmolive CompanyInventors: Germaine Zocchi, Pierre Fonsny
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Patent number: 6046232Abstract: 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: GrantFiled: October 15, 1998Date of Patent: April 4, 2000Assignee: Centaur Pharmaceuticals, Inc.Inventors: Judith A. Kelleher, Kirk R. Maples, Alina Dykman, Yong-Kang Zhang, Allan L. Wilcox, Julian Levell
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Patent number: 6040339Abstract: 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: GrantFiled: May 28, 1998Date of Patent: March 21, 2000Assignee: Sankyo Company, LimitedInventors: Akira Yoshida, Kozo Oda, Takashi Kasai, Kousei Shimada, Hiroshi Kogen, Ichiro Hayakawa, Sadao Ishihara, Teiichiro Koga, Eiichi Kitazawa, Taro Tokui
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Patent number: 6017916Abstract: 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: GrantFiled: January 22, 1997Date of Patent: January 25, 2000Assignee: Warner-Lambert CompanyInventors: Kent Alan Berryman, Annette Marian Doherty, Jeremy John Edmunds, William Chester Patt, Mark Stephen Plummer, Joseph Thomas Repine
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Patent number: 6017951Abstract: 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: GrantFiled: February 10, 1999Date of Patent: January 25, 2000Assignee: Warner-Lambert CompanyInventors: William C. Patt, Bill R. Reisdorph, Joseph T. Repine
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Patent number: 6013836Abstract: 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: GrantFiled: May 22, 1995Date of Patent: January 11, 2000Assignee: Rohm and Haas CompanyInventors: Adam Chi-Tung Hsu, Harold Ernest Aller, Dat Phat Le, Donald Wesley Hamp, Barry Weinstein, Raymond August Murphy
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Patent number: 6004957Abstract: 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: GrantFiled: July 22, 1998Date of Patent: December 21, 1999Assignee: Vertex Pharmaceuticals, IncorporatedInventors: Roger D. Tung, Mark A. Murcko, Govinda R. Bhisetti
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Patent number: 6004988Abstract: 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: GrantFiled: February 24, 1998Date of Patent: December 21, 1999Assignee: BASF AktiengesellschaftInventors: Wilhelm Amberg, Andreas Kling, Dagmar Klinge, Hartmut Riechers, Liliane Unger, Manfred Raschack, Stefan Hergenroder, Bernd Elger, Sabine Schult
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Patent number: 5998408Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.Type: GrantFiled: October 8, 1997Date of Patent: December 7, 1999Assignee: Merck & Co., Inc.Inventors: Robert K. Baker, Frank Kayser, Jianming Bao, Andrew Kotliar, William H. Parsons, Kathleen M. Rupprecht
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Patent number: 5994270Abstract: 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: GrantFiled: September 11, 1996Date of Patent: November 30, 1999Assignee: Monsanto CompanyInventors: Dennis Paul Phillion, Matthew James Graneto, John Kennedy Pratt, Sai Chi Wong
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Patent number: 5990157Abstract: The present invention relates to a foam composition for killing dust mites comprising an acaricidal agent, polymer, ether solvent, perfume, surfactant and water.Type: GrantFiled: July 2, 1998Date of Patent: November 23, 1999Assignee: Colgate Palmolive CompanyInventors: Germaine Zocchi, Pierre Fonsny
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Patent number: 5985870Abstract: 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: GrantFiled: December 19, 1997Date of Patent: November 16, 1999Assignee: 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
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Patent number: 5973011Abstract: 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: GrantFiled: September 27, 1996Date of Patent: October 26, 1999Assignee: ISIS PHARMA GmbHInventors: Eike Albrecht Noack, Georg Kojda
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Patent number: 5962515Abstract: 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: GrantFiled: May 29, 1997Date of Patent: October 5, 1999Assignee: National Institute of ImmunologyInventors: Shakti N. Upadhyay, Ram A. Vishwakarma, Sabari Ghosal, Supriya Shukla, Chanda Bose, Anita Kamra
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Patent number: 5955491Abstract: 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: GrantFiled: June 27, 1995Date of Patent: September 21, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Yukio Fujisawa, Tsuneo Yasuma, Junji Mizoguchi, Masakuni Kori, Masayuki Takizawa
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Patent number: 5952386Abstract: 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: GrantFiled: September 24, 1997Date of Patent: September 14, 1999Assignee: Sumitomo Chemical Company, LimitedInventors: Sanshiro Matsuo, Taro Hirose, Keiichi Izumi, Masaya Suzuki, Noriyasu Sakamoto, Kazunori Tsushima, Shigeru Saito, Hirotaka Takano
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Patent number: 5939430Abstract: 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: GrantFiled: July 20, 1995Date of Patent: August 17, 1999Assignee: Merrell Pharmaceuticals Inc.Inventors: A. Stanley Tyms, Debra L. Taylor
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Patent number: 5929114Abstract: 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: GrantFiled: May 15, 1997Date of Patent: July 27, 1999Assignee: Warner-Lambert CompanyInventors: John Michael Domagala, Edward Faith Elslager, Rocco Dean Gogliotti
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Patent number: 5922759Abstract: 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: GrantFiled: December 15, 1997Date of Patent: July 13, 1999Assignee: Warner-Lambert CompanyInventors: William C. Patt, Bill R. Reisdorph, Joseph T. Repine
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Patent number: 5906992Abstract: The present invention relates to a foam composition for killing dust mites comprising an acaricidal agent, polymer, ether solvent, perfume, surfactant and water.Type: GrantFiled: November 21, 1996Date of Patent: May 25, 1999Assignee: Colgate Palmolive CompanyInventors: Pierre Fonsny, Germaine Zocchi
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Patent number: 5902587Abstract: 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: GrantFiled: July 1, 1992Date of Patent: May 11, 1999Assignee: ASTA Medica AktiengesellschaftInventors: Reinhold Carle, Otto Isaac
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Patent number: 5898036Abstract: 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: GrantFiled: February 19, 1998Date of Patent: April 27, 1999Inventor: Malcolm N. McLeod
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Patent number: 5889046Abstract: 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: GrantFiled: February 1, 1996Date of Patent: March 30, 1999Assignee: Suntory LimitedInventors: Kengo Akimoto, Shiro Morimoto, Yasuo Matsumura, Hajime Yoshizumi, Tetsuo Murakami
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Patent number: 5880147Abstract: 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: GrantFiled: September 18, 1996Date of Patent: March 9, 1999Assignee: Sankyo Company, LimitedInventors: Akira Yoshida, Kozo Oda, Takashi Kasai, Kousei Shimada, Hiroshi Kogen, Ichiro Hayakawa, Sadao Ishihara, Teiichiro Koga, Eiichi Kitazawa, Taro Tokui
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Patent number: 5866609Abstract: 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: GrantFiled: July 24, 1997Date of Patent: February 2, 1999Assignee: SS Pharmaceutical Co., Ltd.Inventors: Yoshihiko Kanamaru, Hiroyuki Hirota, Akihiro Shibata, Teruo Komoto, Hiroyuki Naito, Koichi Tachibana, Mari Ohtsuka, Fumio Ishii, Susumu Sato
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Patent number: 5852052Abstract: 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: GrantFiled: December 9, 1996Date of Patent: December 22, 1998Assignee: Ruth KorthInventor: Ruth Korth
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Patent number: 5840753Abstract: 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: GrantFiled: March 24, 1997Date of Patent: November 24, 1998Assignee: Laboratories UPSAInventors: Eric Nicolai, Jean-Marie Teulon
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Patent number: 5824665Abstract: 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: GrantFiled: April 23, 1997Date of Patent: October 20, 1998Inventors: James Henry, Gurpreet Ahluwalia, Douglas Shander
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Patent number: 5817693Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: November 9, 1994Date of Patent: October 6, 1998Inventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
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Patent number: 5814657Abstract: 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: GrantFiled: November 21, 1997Date of Patent: September 29, 1998Assignee: AllerganInventors: Robert M. Burk, David F. Woodward
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Patent number: 5783701Abstract: 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: GrantFiled: February 23, 1995Date of Patent: July 21, 1998Assignee: Vertex Pharmaceuticals, IncorporatedInventors: Roger D. Tung, Mark A. Murcko, Govinda Rao Bhisetti
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Patent number: 5780592Abstract: 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: GrantFiled: December 10, 1996Date of Patent: July 14, 1998Assignee: Hoechst AktiengesellschaftInventors: Stefan Mullner, Axel Hofmann, Karin Saar, Hans-Ulrich Schorlemmer, Robert Bartlett
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Patent number: 5767154Abstract: 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: GrantFiled: March 24, 1997Date of Patent: June 16, 1998Assignee: AllerganInventors: David A. Woodward, Ming F. Chan
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Patent number: 5756510Abstract: 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: GrantFiled: August 30, 1996Date of Patent: May 26, 1998Assignee: Newcastle University Ventures LimitedInventors: Roger John Griffin, Alan Hilary Calvert, Nicola Jane Curtin, David Richard Newell, Bernard Thomas Golding
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Patent number: 5753660Abstract: 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: GrantFiled: November 13, 1996Date of Patent: May 19, 1998Assignee: 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
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Patent number: 5744494Abstract: 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: GrantFiled: July 25, 1995Date of Patent: April 28, 1998Assignee: British Technology Group LimitedInventors: Quintin Archibald McKellar, Hafid Abdelaali Benchaoui
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Patent number: 5741483Abstract: 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: GrantFiled: May 3, 1996Date of Patent: April 21, 1998Assignee: Rohm and Haas CompanyInventor: Shozo Okawa
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Patent number: 5739166Abstract: 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: GrantFiled: November 29, 1994Date of Patent: April 14, 1998Assignee: G.D. Searle & Co.Inventors: David B. Reitz, Jinglin Li, Monica B. Norton
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Patent number: 5726195Abstract: 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: GrantFiled: July 16, 1996Date of Patent: March 10, 1998Assignee: Cubist Pharmaceuticals, Inc.Inventors: Jason M. Hill, Guixue Yu, Youe-Kong Shue, Thomas M. Zydowsky, Julius Rebek
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Patent number: 5719182Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: May 16, 1995Date of Patent: February 17, 1998Assignee: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
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Patent number: 5719183Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: June 2, 1995Date of Patent: February 17, 1998Assignee: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
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Patent number: 5716985Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: May 23, 1995Date of Patent: February 10, 1998Assignee: SmithKline Beecham CorporationInventors: John Duncan Elliott, Maria Amparo Lago
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Patent number: 5716984Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: May 16, 1995Date of Patent: February 10, 1998Assignee: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, John Duncan Elliott
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Patent number: 5705500Abstract: 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: GrantFiled: June 7, 1995Date of Patent: January 6, 1998Assignee: 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