Plural Alicyclic Rings In R Patents (Class 514/623)
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Patent number: 7138546Abstract: Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.Type: GrantFiled: August 16, 2001Date of Patent: November 21, 2006Assignee: Emisphere Technologies, Inc.Inventor: Pingwah Tang
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Patent number: 7132457Abstract: The invention provides adamantane derivatives of formula (I), a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy. In formula (I) D represents CH2 or CH2CH2, E represents C(O)NH or NHC(O) and R3 represents a group of formula (I).Type: GrantFiled: March 31, 2004Date of Patent: November 7, 2006Assignee: AstraZeneca ABInventors: Lilian Alcaraz, Mark Furber, Michael Mortimore, Austen Pimm, Philip Thorne, Paul Willis
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Patent number: 7053071Abstract: The present invention provides compounds that are inducers or inhibitors of apoptosis or apoptosis preceded by cell-cycle arrest. In addition, the present invention provides pharmaceutical compositions and methods for treating mammals with leukemia or other forms of cancer or for treating disease conditions caused by apoptosis of cells.Type: GrantFiled: December 2, 2002Date of Patent: May 30, 2006Assignee: The Burnham InstituteInventors: Marcia Dawson, Joseph A. Fontana, Xiao-kun Zhang, Mark Leid, Ling Jong, Peter D. Hobbs
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Patent number: 7041702Abstract: The present invention relates to pharmaceutically acceptable compounds, including acylguanidine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.Type: GrantFiled: October 20, 1998Date of Patent: May 9, 2006Assignee: Scion Pharmaceuticals, Inc.Inventors: Graham J. Durant, Seetharamaiyer Padmanabhan
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Patent number: 6995285Abstract: The present invention provides compounds that elevate cellular expression of the ABCA-1 gene, promoting cholesterol efflux from cells and increasing HDL levels in the plasma of a mammal, in particular humans. The compounds are useful for treating coronary artery disease.Type: GrantFiled: June 4, 2002Date of Patent: February 7, 2006Assignee: CV Therapeutics, Inc.Inventors: Prabha N. Ibrahim, Robert Jiang, Christopher Morrison, Kevin Shenk, Jeff A. Zablocki
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Patent number: 6963010Abstract: The disclosed invention provides new polyamine analogs and derivatives containing a hydrophobic region and a polyamine region as well as methods and compositions for their use.Type: GrantFiled: January 8, 2002Date of Patent: November 8, 2005Assignee: MediQuest Therapeutics, Inc.Inventors: Mark R. Burns, Gerard F. Graminski
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Publication number: 20040152681Abstract: Steroid derivatives of this invention interact with nuclear liver X receptor (LXR) and ubiquitous receptor (UR) and can be used to treat a variety of LXR- or UR-mediated disorders.Type: ApplicationFiled: November 10, 2003Publication date: August 5, 2004Applicant: Arch Development Corporation, an Illinois corporationInventors: Shutsung Liao, Ching Song
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Patent number: 6756504Abstract: The invention relates to compounds of the general formula (I), as defined, and to pharmaceutical compositions containing them. The compounds of formula (I) are inhibitors of various lipid-related enzymes. They can be used in reducing accumulation of sphingolipids and thus in the treatment of lipid storage diseases. The compounds of formula (I) can also be used for the treatment of cancerous diseases and for killing of wild type and drug-resistant cancer cells.Type: GrantFiled: October 17, 2002Date of Patent: June 29, 2004Assignee: Yissum Research Development Company of the Hebrew University of JerusalemInventors: Arieh Dagan, Shimon Gatt
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Patent number: 6713650Abstract: The present invention provides compounds that elevate cellular expression of the ABCA-1 gene, promoting cholesterol efflux from cells and increasing HDL levels in the plasma of a mammal, in particular humans. The compounds are useful for treating coronary artery disease.Type: GrantFiled: December 5, 2001Date of Patent: March 30, 2004Inventors: Prabha N. Ibrahim, Robert Jiang, Christopher Morrison, Kevin Shenk, Jeff A. Zablocki, Richard Lawn
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Patent number: 6713463Abstract: A method of reducing or inhibiting mucositis in a patient, which includes administering an inflammatory cytokine inhibitor or a mast cell inhibitor, or a combination thereof, is disclosed.Type: GrantFiled: September 27, 2002Date of Patent: March 30, 2004Assignee: Mucosal Therapeutics, LLCInventors: Stephen T. Sonis, Edward G. Fey
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Patent number: 6710081Abstract: Therapeutic agents for erectile dysfunction containing as the active ingredient prostaglandin derivatives of formula (I) (wherein symbols have the same meanings as described in the description), nontoxic salts thereof, or cyclodextrin clathrate compounds thereof.Type: GrantFiled: April 8, 2002Date of Patent: March 23, 2004Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Masami Narita, Kouzou Yoshida
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Publication number: 20040014758Abstract: The present application describes modulators of CCR3 of formula (I): 1Type: ApplicationFiled: July 3, 2003Publication date: January 22, 2004Inventors: Dean A. Wacker, John V. Duncia, Joseph B. Santella, Daniel S. Gardner
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Publication number: 20040002493Abstract: A pharmaceutical composition, which comprises a benzoic acid derivative of formula (I) 1Type: ApplicationFiled: February 27, 2003Publication date: January 1, 2004Inventors: Kousuke Tani, Masaki Asada, Kaoru Kobayashi, Masami Narita, Mikio Ogawa
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Patent number: 6670400Abstract: Phenoxyethylamine derivatives of general formula (I) having high affinity for the 5-HT1A receptor, methods for preparing same, pharmaceutical compositions containing said derivatives, and their use, in particular as gastric acid secretion inhibitors or as antiemetics, are disclosed. In general formula (I), Ar is phenyl substituted by one or more substituents; and R is a C1-10 hydrocarbon radical selected from straight or branched alkyl, alkenyl or alkynyl radicals, saturated or unsaturated mono- or polycyclic cycloalkyl, cycloalkylalkyl or alkylcycloalkyl radicals; a pyridyl or isoquinolyl radical, phenyl optionally substituted by one or more substituents, and salts thereof.Type: GrantFiled: April 8, 2002Date of Patent: December 30, 2003Assignee: Societe de Conseils de Recherches et D'Applications Scientifiques (S.C.R.A.S.)Inventors: Dennis Bigg, Jacques Pommier, Christiane Martin, Pierre Roubert, Jean Pierre Defaux
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Publication number: 20030216287Abstract: Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.Type: ApplicationFiled: May 7, 2003Publication date: November 20, 2003Inventor: Pingwah Tang
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Patent number: 6613771Abstract: A water soluble derivative of buckministerfullerene (C60) having antiviral and virucidal properties is used to inhibit human retroviral replication and infections. The derivatized fullerene is symmetrically substituted with polar organic moieties containing 1 to 20 carbon atoms and optionally further containing oxygen or nitrogen.Type: GrantFiled: January 25, 2001Date of Patent: September 2, 2003Assignee: The Regents of the University of CaliforniaInventors: Simon H. Friedman, Raymond F. Schinazi, Fred Wudl, Craig L. Hill, Diane L. DeCamp, Rintje P. Sijbesma, George L. Kenyon
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Publication number: 20030149103Abstract: The present invention provides functionalized cyclopropane compounds that have pesticidal and/or TMOF activity. The pesticidal compounds and other compounds of the present invention are usefully employed in the control of pests, particularly insect pests such as mosquitoes, which ingest blood.Type: ApplicationFiled: December 13, 2001Publication date: August 7, 2003Inventor: Russell J. Linderman
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Publication number: 20030134874Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: ApplicationFiled: September 16, 2002Publication date: July 17, 2003Inventors: Francine S. Grant, Bradley S. Johnson, Michael A. Pleiss, Eugene D. Thorsett
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Patent number: 6593312Abstract: A compound of formula (I): wherein: represents an optionally substituted saturated carbon ring having from 4 to 8 ring members, R1 and R4, which may be identical or different, each represents hydrogen or acyl, R2 and R3, which may be identical or different, each represents hydrogen or alkyl, R5 and R6, which may be identical or different, each represents hydrogen or alkyl, or R5 and R6 together, with the nitrogen atom carrying them, form an optionally substituted nitrogen-containing heterocycle, stereoisomers thereof, and also addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful for treatment of glucose intolerance or of disorders associated with hyperglycaemia.Type: GrantFiled: June 18, 2002Date of Patent: July 15, 2003Assignee: Les Laboratoires ServierInventors: Michel Wierzbicki, Jean-Marie Fourquez, Nigel Levens, Bernadette Husson-Robert, Olivier Nosjean, Michelle Boulanger
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Patent number: 6562782Abstract: The present invention related to an oligocycloalkanoid compound comprising formula (I) wherein m, n, and o are independently an integer from 0 to 2; A1 through A10 are independently a direct link, alkylene, alkylene-O—, carbonyl, oxygen, or sulfur; X and Y are independently hydrogen, hydroxy, alkyl, or in combination an electrophilic group; and R1 through R10 are independently hydrogen, hydroxy, alkyl, alkenyl, alkynyl, substituted or unsubstituted aryl, N-, S-, or O-heterocycles, fused or multi-ring aryl with or without hetero ring members, arylalkyl, arylalkenyl, arylalkynyl, alkylphenyl, alkenylphenyl, alkynylphenyl, alkoxy, alkenyloxy, alkynyloxy, substituted or unsubstituted aryloxy, substituted or unsubstituted arylalkoxy, alkylacyl, alkenylacyl, alkynylacyl, arylacyl, aroyl, alkylaroyl, aminoaroyl, aminoalkylacyl, aminoalkyl, aminoalkenyl, aminoalkynyl, amino, alkylamino, alkenylamino, alkynylamino, arylamino, dialkylamino, dialkenylamino, dialkynylamino, arylalkylamino, arylalkType: GrantFiled: May 10, 2000Date of Patent: May 13, 2003Assignee: University of RochesterInventors: Benjamin L. Miller, Robert D. Hubbard
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Publication number: 20030073712Abstract: Cytoprotective compounds, many of which are phenolic derivatives characterized by a substituted phenol having certain conjugated bonds, are useful in the treatment of certain ischemic or inflammatory conditions, including but not limited to stroke, myocardial infarction, congestive heart failure, and skin disorders characterized by inflammation or oxidative damage. They are also useful in the manufacture of pharmaceutical and cosmetic formulations for the treatment of such conditions.Type: ApplicationFiled: July 23, 2002Publication date: April 17, 2003Inventors: Bing Wang, Yong-Kang Zhang, Jian Chen, Wei Zhang, Jiangao Song, Ughetta Del Balzo, Lesley Brown, Sekhar Boddupalli, Steven Bobzin, Sylvain Gilat, Guy Miller
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Publication number: 20030069305Abstract: Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-&agr; and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.Type: ApplicationFiled: December 11, 2001Publication date: April 10, 2003Applicant: Celltech R & D, Inc.Inventors: Randy W. Jackson, Ihab Darwish, Ted A. Baughman, J. Jeffry Howbert
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Publication number: 20030050338Abstract: Novel compounds are disclosed that have the following chemical structures, and prodrug esters and acid-addition salts thereof, that are useful as Interleukin-1 and Tumor Necrosis Factor-&agr; modulators, and thus are useful in the treatment of various diseases.Type: ApplicationFiled: March 27, 2002Publication date: March 13, 2003Inventors: Michael Palladino, Emmanuel A. Theodorakis
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Publication number: 20030045550Abstract: The invention provides therapeutic and biological uses of chemokine-receptor-binding compounds (including chemokine receptor ligands such as chemokine receptor agonists or antagonists), such as naphthoic acid derivatives, including uses in the treatment of disease states mediated by chemokines. The relevant chemokine may for example be stromal cell-derived factor (SDF)-1, and the relevant chemokine receptors may for example be corresponding chemokine receptor (CXCR-4). In other aspects, the invention provides corresponding pharamaceutical compositions and therapeutic methods. In one aspect, for example, the invention provides for the use of 3-Hydroxy-2-naphthoic acid in the treatment of disease.Type: ApplicationFiled: November 13, 2001Publication date: March 6, 2003Inventors: Geeta Saxena, Christopher R. Tudan, Ahmed Merzouk, Hassan Salari
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Publication number: 20030013704Abstract: 1Type: ApplicationFiled: June 12, 2002Publication date: January 16, 2003Inventors: Lilian Alcaraz, Moya Caffrey, Mark Furber, Timothy Luker, Michael Mortimore, Austen Pimm, Philip Thorne, Paul Willis
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Publication number: 20030008818Abstract: The invention provides a composition containing particulate composite of a polymer and a therapeutic agent. The composition also contains a complexing agent. The polymer interacts with the complexing agent in a host-guest or a guest-host interaction to form an inclusion complex. A therapeutic composition of the invention may be used to deliver the therapeutic agent and to treat various disorders. Both the polymer of the particulate composite and the complexing agent may be used to introduce functionality into the therapeutic composition. The invention also relates to a method of preparing a composition. The method combines a therapeutic agent, a polymer having host or guest functionality, and a complexing agent having guest or host functionality to form the therapeutic composition. The complexing agent forms an inclusion complex with the polymer. The invention also relates to a method of delivering a therapeutic agent.Type: ApplicationFiled: December 19, 2001Publication date: January 9, 2003Applicant: California Institute of Technology and Insert Therapeutics, IncInventors: Suzie Hwang Pun, Hector Gonzalez, Mark E. Davis, Nathalie Bellocq, Jianjun Cheng
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Patent number: 6423870Abstract: The invention concerns compounds of formula (I) in which: A forms a tricyclic system of formula A1, A2, A3 or A4; R1 represents a hydrogen atom, an alkyl, hydroxy, alkoxy or oxo group; (R2)m and (R3)m′ are such as defined in the description; n represents an integer such that 0≦n≦3; p represents an integer such as defined in the description; B represents a group (a) or (b). The invention is useful for preparing medicines.Type: GrantFiled: July 14, 2000Date of Patent: July 23, 2002Assignee: Les Laboratoires ServierInventors: Michel Langlois, Monique Mathe-Allainmat, Carole Jellimann, Jean Andrieux, Caroline Bennejean, Pierre Renard, Philippe Delagrange
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Publication number: 20020091158Abstract: Methods and compositions for treating Kaposi's sarcoma and Epstein Barr virus using a a therapeutic derivative of a triterpenoid acid and derivatives thereof are disclosed,Type: ApplicationFiled: October 15, 2001Publication date: July 11, 2002Inventor: Ornella Flore
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Publication number: 20020086815Abstract: The present invention provides illudin analogs of the general formula I: 1Type: ApplicationFiled: November 5, 2001Publication date: July 4, 2002Applicant: The Regents of the University of CaliforniaInventors: Trevor C. McMorris, Michael J. Kelner
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Publication number: 20020013371Abstract: The invention relates to the use of arsenic compounds to treat a variety of leukemia, lymphoma and solid tumors. Further, the arsenic compounds may be used in combination with other therapeutic agents, such as a retinoid. The invention also provides a process for producing arsenic trioxide formulations.Type: ApplicationFiled: November 10, 1998Publication date: January 31, 2002Inventors: RAYMOND P. WARRELL, PIER PAOLO PANDOLFI, JANICE L. GABRILOVE
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Publication number: 20020004512Abstract: Certain novel compounds and derivatives thereof are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: ApplicationFiled: May 29, 2001Publication date: January 10, 2002Inventors: Raman Kumar Bakshi, Ravi P. Nargund, Zhixiong Ye
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Patent number: 6294585Abstract: Disclosed are methods for increasing the differentiation of mammalian neuronal cells for purposes of treating neurodegenerative diseases or nerve damage by administration of various compounds including alcohols, diols and/or triols and their analogues.Type: GrantFiled: September 18, 1997Date of Patent: September 25, 2001Assignee: Applied Genetics Incorporated DermaticsInventor: David A. Brown
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Patent number: 6262091Abstract: Compositions for controlling harmful fungi, containing in a solid or liquid carrier a) at least one p-hydroxyaniline derivative of the formula I b) at least one amide compound of the formula II A—CO—NR8—R9 (II) where the substituents have the meanings indicated in the description; and methods of controlling harmful fungi using compositions of this type are described.Type: GrantFiled: October 21, 1998Date of Patent: July 17, 2001Assignee: BASF AktiengesellschaftInventors: Oliver Wagner, Karl Eicken, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Harald Köhle, Günter Retzlaff
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Patent number: 6242470Abstract: The invention provides adamantane derivatives, a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.Type: GrantFiled: January 26, 1999Date of Patent: June 5, 2001Assignee: AstraZeneca ABInventors: Andrew Baxter, Stephen Brough, Thomas McInally, Michael Mortimore
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Patent number: 6235780Abstract: (wherein R1 is OH etc.; X is Cl, F; R2 is H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl which may be substituted; n is 0-4.), non-toxic salts thereof or cyclodextrin clathrates thereof can strongly bind on EP2 subtype receptor. Therefore, they are useful for the prevention and/or treatment of immunological diseases (autoimmune diseases, post-transplantation graft rejection etc.), asthma, abnormal bone formation, neuronal cell death, hepatopathy, abortion, premature birth or retina neuropathy (e.g. glaucoma) etc.Type: GrantFiled: July 19, 1999Date of Patent: May 22, 2001Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Shuichi Ohuchida, Kousuke Tani
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Patent number: 6225353Abstract: A composition and method of preventing or inhibiting tumor growth, and of treating malignant melanoma, without toxic side effects are disclosed. Betulinic acid or a betulinic acid derivative is the active compound of the composition, which is topically applied to the situs of tumor.Type: GrantFiled: November 10, 1998Date of Patent: May 1, 2001Assignee: The Board of Trustees of the University of IllinoisInventors: John M. Pezzuto, Tapas K. DasGupta, Darrick S. H. L. Kim
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Patent number: 6214869Abstract: There is provided a novel series of cis cyclopropane compounds of Formula I wherein R1, R2, R3, R4, X, Y, Z and m are as defined herein which bind to the human melatonin receptor and therefore are useful as melatonergic agents.Type: GrantFiled: May 25, 1999Date of Patent: April 10, 2001Assignee: Bristol-Myers SquibbInventors: Jie Chen, Pierre Dextraze, Marco Dodier, Katherine S. Takaki
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Patent number: 6096784Abstract: Inhibitors of oleamide hydrolase, responsible for the hydrolysis of an endogenous sleep-inducing lipid (1, cis-9-octadecenamide) were designed and synthesized. The most potent inhibitors possess an electrophilic carbonyl group capable of reversibly forming a (thio) hemiacetal or (thio) hemiketal to mimic the transition state of a serine or cysteine protease catalyzed reaction. In particular, the tight binding .alpha.-keto ethyl ester 8 (1.4 nM) and the trifluoromethyl ketone inhibitor 12 (1.2 nM) were found to have exceptional inhibitory activity. In addition to the inhibitory activity, some of the inhibitors displayed agonist activity which resulted in the induction of sleep in laboratory animals.Type: GrantFiled: January 5, 1999Date of Patent: August 1, 2000Assignee: The Scripps Research InstituteInventors: Richard A. Lerner, Chi-Huey Wong, Dale L. Boger, Steven J. Henriksen
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Patent number: 6090853Abstract: Carboxamides of the formula I ##STR1## where the substituents have the following meanings: R.sup.1 is unsubstituted or substituted bicycloalkyl, tricycloalkyl or bicycloalkenyl;R.sup.2,R.sup.3 and R.sup.4 are each, independently of one another, hydrogen, or unsubstituted or substituted: alkyl, cycloalkyl, cycloalkenyl or heterocyclyl;Ar is unsubstituted or substituted aryl or hetaryl,but excluding 2-cyano-N-[1-(1-naphthyl)ethyl]-3-phenyl-bicyclo[2.2.1]hept-5-ene-2-carbox amide, a process for their preparation, compositions comprising compounds I and the use of compounds I for preparing the compositions, and further a process for controlling harmful fungi and the use of the compounds I for this purpose.Type: GrantFiled: September 21, 1998Date of Patent: July 18, 2000Assignee: BASF AktiengesellschaftInventors: Frank Wetterich, Oliver Wagner, Karl Eicken, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, John-Bryan Speakman
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Patent number: 6060509Abstract: A pine root (Deutero mycetes) fungal metabolite and analogs thereof having antifungal activity.Type: GrantFiled: December 31, 1998Date of Patent: May 9, 2000Assignee: Millennium Pharmaceuticals, Inc.Inventor: Zhi-Dong Jiang
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Patent number: 6048877Abstract: Tetralone derivatives of the formula ##STR1## where R.sup.1 is halo, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, (aryl)alkenyl, (aryl)alkynyl, alkoxy, O-alkenyl, O-aryl, O-alkyl(heterocyclo), COO-alkyl,alkanoyl, CO-amino, CO-substituted amino, alkyl-CO-amino, alkyl-CO-substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-alkyl(heterocyclo), N(alkyl)CO-alkyl, N(alkyl)CO-aryl, N(alkyl)CO-heterocyclo, N(alkyl)CO-alkyl(heterocyclo);R.sup.2 is hydrogen, alkyl, halo, aryl, alkoxy, amino, substituted amino;R.sup.3 is oxo, hydroxy, alkoxy, O--COalkyl, --O--COaryl, --O--COheterocyclo, NOH, NO-alkyl, N-amino, N-substituted amino, N-NHCONHalkyl, N-NHSO.sub.2 alkyl, N-NHSO.sub.2 aryl, amino, substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-heterocyclo, spiroheterocyclo;R.sup.4 is hydrogen, alkyl, alkyl(COalkyl), alkyl(COOalkyl); orR.sup.3 and R.sup.4 taken together with the atoms to which they are attached form a five- to seven-membered ring which can contain up to three heteroatoms selected from oxygen, nitrogen and sulfur;R.sup.Type: GrantFiled: January 20, 1998Date of Patent: April 11, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Saleem Ahmad, Philip D. Stein, Francis N. Ferrara, Karnail S. Atwal
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Patent number: 5929119Abstract: A composition which is suitable for controlling fungal pests, comprising conventional additives and an effective amount of a p-hydroxyaniline derivative of the general formula I ##STR1## where the substituents have the following meanings: R.sup.1 is hydrogen, unsubstituted or substituted alkyl, unsubstituted or substituted bicycloalkyl, unsubstituted or substituted bicycloalkenyl;R.sup.2 and R.sup.3 independently of one another are halogen, alkyl, haloalkyl, alkoxy or haloalkoxy,and a liquid or solid carrier, its use, the use of the compounds I for controlling fungal pests, and the use of the compounds I for the preparation of the compositions.Type: GrantFiled: August 11, 1997Date of Patent: July 27, 1999Assignee: BASF AktiengesellschaftInventors: Oliver Wagner, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5925674Abstract: This invention relates to cycloalkylcarboxanilides of the formula ##STR1## which are used to combat pests.Type: GrantFiled: October 26, 1995Date of Patent: July 20, 1999Assignee: Bayer AktiengesellschaftInventors: Bernd-Wieland Krueger, Klaus Sasse, Thomas Schenke, Michael Negele, Heinz-Wilhelm Dehne
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Patent number: 5880160Abstract: The present invention relates to novel colchicine derivatives having antiproliferative, antineoplastic, antiinflammatory and muscle relaxant activities; said derivatives include novel colchine nitrogen amides for use either as such or after derivatization of the hydroxyl at C.sub.3 of the aromatic ring and at C.sub.10 of the tropolone ring. These novel compounds have a cytotoxicity on human tumoral cell lines comparable with colchicine but, in comparison with the latter, they are much more active on cells resistant to the usual antiblastics. The compounds can be included in pharmaceutical formulations useful for the intravenous, oral and topical administrations.Type: GrantFiled: June 27, 1996Date of Patent: March 9, 1999Assignee: Indena S.p.A.Inventors: Ezio Bombardelli, Bruno Gabetta
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Patent number: 5827891Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.Type: GrantFiled: June 7, 1995Date of Patent: October 27, 1998Assignee: Agouron Pharmaceuticals, Inc.Inventors: Bruce A. Dressman, James E. Fritz, Marlys Hammond, William J. Hornback, Stephen W. Kaldor, Vincent J. Kalish, John E. Munroe, Siegfried Heinz Reich, John H. Tatlock, Timothy A. Shepherd, Michael J. Rodriguez
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Patent number: 5780512Abstract: The invention relates to a compounds selected from these of formula (I): ##STR1## in which: R.sub.1, R.sub.2, R.sub.3 and A are as defined in the description, and a medicinal product containing the same useful for treating a melatoninergic disorder.Type: GrantFiled: March 26, 1997Date of Patent: July 14, 1998Assignee: Adir et CompagnieInventors: Daniel Lesieur, Eric Fourmaintraux, Patrick Depreux, Philippe Delagrange, Pierre Renard, Beatrice Guardiola-Lemaitre
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Patent number: 5760023Abstract: Anti-pruritic pharmaceutical formulations containing kappa agonist compounds and methods of prevention or treatment of pruritus in a mammal with the anti-pruritic formulations.Type: GrantFiled: July 14, 1997Date of Patent: June 2, 1998Assignee: Adolor CorporationInventors: John J. Farrar, An-Chih Chang, Virendra Kumar, Wei Yuan Zhang, Alan Cowan
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Patent number: 5703129Abstract: A series of 5-amino-6-cyclohexyl-4-hydroxy-hexanamide derivatives of Formula I have been synthesized. ##STR1## As inhibitors of the production of .beta.-amyloid protein from .beta.-amyloid precursor protein, these compounds are expected to be effective in treating patients suffering from or susceptible to conditions or disorders linked to brain accumulation of .beta.-amyloid protein; e.g., Alzheimer's Disease and Down's Syndrome.Type: GrantFiled: September 30, 1996Date of Patent: December 30, 1997Assignee: Bristol-Myers Squibb CompanyInventors: Kevin Felsenstein, David W. Smith, Michael A. Poss, Prasad Chaturvedula, Charles P. Sloan
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Patent number: 5693630Abstract: Compounds of the general formula ##STR1## or pharmaceutically acceptable salts thereof, wherein Z is a saturated or unsaturated 3 to 6 carbon chain,m is 2 or 3,R.sub.1 is a hydrogen atom, or a straight or branched C.sub.1-4 alkyl group,R.sub.2, R.sub.3 and R.sub.13 are situated in the ortho, meta, or para position of the phenyl ring and are the same or different and selected from the following groups: H, OH, OR.sub.14, halogen, CO.sub.2 R.sub.9, CN, CF.sub.3, NO.sub.2, NH.sub.2, COCH.sub.3,OSO.sub.2 CF.sub.3,OSO.sub.2 CH.sub.3,CONR.sub.10 R.sub.11, OCOR.sub.12, whereinR.sub.9, R.sub.12 and R.sub.14 is a straight or branched C.sub.1-4 alkyl group,R.sub.10 and R.sub.11 are the same or different and represents hydrogen or a straight or branched C.sub.1-6 alkyl group,R is 1) ##STR2## processes for their preparation, pharmaceutical preparations containing them and the use of the compounds in the treatment psychiatric disorders.Type: GrantFiled: October 26, 1994Date of Patent: December 2, 1997Assignee: Astra AktiebolagInventors: Stefan Bengtsson, Sven Hellberg, Nina Mohell, Lian Zhang, Gerd Hallnemo, David Jackson, Bengt Ulff
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Patent number: 5684049Abstract: A compound for use as a medicine having the formula ##STR1## a pharmaceutically acceptable acid addition salt form or a stereochemically isomeric form thereof, wherein R.sup.1 and R.sup.2 each independently are hydrogen, C.sub.1-6 alkyl or C.sub.3-6 cyclo-alkyl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom bearing said R.sup.1 and R.sup.2 may form a pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl or 4-C.sub.1-4 alkylpiperazinyl group; X is O or S; R.sup.3 is hydrogen or C.sub.1-6 alkyl; R.sup.4, R.sup.5 and R.sup.6 each independently are hydrogen, halo, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, nitro, trifluoromethyl, cyano, aminomethyl, carboxyl, C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkyl-carbonyl, aminocarbonyl, or hydroxy; R.sup.7 is hydrogen or halo; and R.sup.8, R.sup.9 and R.sup.10 each independently are hydrogen, halo, C.sub.1-6 alkyl, C.sub.Type: GrantFiled: March 27, 1995Date of Patent: November 4, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Georges Henri Van Daele, Marc Gustaaf Verdonck, Jean-Paul Rene Bosmans, Paul Adriaan Janssen