Benzene Ring Is Part Of A Substituent Which Contains Oxygen Patents (Class 514/598)
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Publication number: 20080274884Abstract: A method for preventing a plant such as vegetables, corn, cotton, rice, sugar beet or soybean from damage by insect pest after germination of the plant which comprises steps of treating seeds of the plant with a composition containing a (N?-methyl)benzoylurea compound represented by the formula (I): wherein R1 denotes a hydrogen atom or the like, R2 denotes a halogen atom or the like, R3 denotes a halogen atom, an optionally halogenated C1-C4 alkyl group, or the like, and sowing the treated seeds, followed by cultivation.Type: ApplicationFiled: April 18, 2008Publication date: November 6, 2008Inventors: Norihisa Sakamoto, Masato Konobe
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Publication number: 20080275047Abstract: This invention relates to tetrahydro-naphthalene derivatives and salts thereof which are useful as an active ingredient of pharmaceutical preparations. The tethrahydro-naphthalene derivatives of the present invention have excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, urge urinary incontienence, chronic pain, neuropathic pain, post-operative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.Type: ApplicationFiled: April 15, 2008Publication date: November 6, 2008Inventors: Masaomi Tajimi, Toshio Kokubo, Masahiro Shiroo, Yasuhiro Tsukimi, Takeshi Yura, Klaus Urbahns, Noriyuki Yamamoto, Muneto Mogi, Hiroshi Fujishima, Tsutomu Masuda, Nagahiro Yoshida, Toshiya Moriwaki
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Publication number: 20080269265Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: June 25, 2008Publication date: October 30, 2008Inventors: Scott Miller, Martin Osterhout, Jacques Dumas, Uday Khire, Timothy B. Lowinger, Bernd Riedl, William J. Scott, Roger A. Smith, Jill E. Wood, David Gunn, Martha Rodriguez, Ming Wang, Tiffany Turner, Catherine Brennan
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Patent number: 7423175Abstract: This invention relates to hydroxy-tetrahydro-naphthalenylurea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The hydroxy-tetrahydro-naphthalenylurea derivatives of the present invention have an excellent activity as VR1 antagonist and are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.Type: GrantFiled: February 5, 2004Date of Patent: September 9, 2008Assignee: Bayer Healthcare AGInventors: Takeshi Yura, Muneto Mogi, Hiroshi Fujishima, Klaus Urbahns, Tsutomu Masuda, Yasuhiro Tsukimi, Masaomi Tajimi, Noriyuki Yamamoto, Nagahiro Yoshida, Toshiya Moriwaki
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Publication number: 20080171783Abstract: The present disclosure provides amide-based, non-nucleoside compounds having an inhibitory activity against endogenous polymerases, such as polymerase alpha and polymerase gamma. This disclosure further provides uses of treating hyperproliferative diseases or disorders, such as benign or malignant neoplasms, and more specifically cancers that are sensitive to inhibition of polymerase alpha and polymerase gamma.Type: ApplicationFiled: December 28, 2007Publication date: July 17, 2008Applicant: Migenix Inc.Inventors: Dale Russell Cameron, Maria Marta Guarna, Luba Metlitskaia
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Publication number: 20080125424Abstract: The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.Type: ApplicationFiled: July 10, 2007Publication date: May 29, 2008Inventors: Pierre DePrez, Sarah E. Lively, Taoues Temal
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Publication number: 20080085936Abstract: The invention relates to compounds of formula (I), wherein R, R1, R2, X and n are as defined in the description, and their use for the preparation of pharmaceutical compositions for the treatment of inflammatory states.Type: ApplicationFiled: June 16, 2005Publication date: April 10, 2008Inventors: Pier Giovanni BARALDI, Pier Andrea BOREA, Pierangelo GEPPETTI
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Publication number: 20080058377Abstract: This invention relates to bicyclic amide, carbamate or urea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The bicyclic amide, carbamate or urea derivative of the present invention has vanilloid receptor (VR1) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor oeractivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pulmonary (or airways) disease (COPD).Type: ApplicationFiled: October 26, 2004Publication date: March 6, 2008Applicant: Bayer HealthCare AGInventors: Muneto Mogi, Hiroshi Fujishima, Masaomi Tajimi, Noriyuki Yamamoto, Klaus Urbahns, Fumihiko Hayashi, Yasuhiro Tsukimi, Jang Gupta, Hiroaki Yuasa
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Patent number: 7115664Abstract: One aspect of the present invention relates to novel peptidomimetic compounds. A second aspect of the present invention relates to the use of the novel peptidomimetic compounds as ligands—agonists or antagonists—for various cellular receptors, e.g., G-protein-coupled receptors and opioid receptors, and various cellular ion channels, e.g., sodium and calcium. In certain embodiments, compounds of the present invention preferentially or selectively inhibit sodium or calcium ion channels. In certain embodiments, compounds of the present invention preferentially or selectively agonize or antagonize $gm opioid receptors.Type: GrantFiled: February 27, 2001Date of Patent: October 3, 2006Assignee: Sepracor Inc.Inventors: Paul E. Persons, Joanne M. Holland, James Hauske
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Patent number: 7109243Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme (e.g., cathespin K). The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.Type: GrantFiled: March 23, 2004Date of Patent: September 19, 2006Assignee: IRM LLCInventors: Hong Liu, David Tully, Robert Epple, Badry Bursulaya, Jennifer Williams, Arnab Chatterjee, Jennifer Leslie Harris, Jun Li
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Patent number: 7105567Abstract: The present invention relates to a urea derivative of the formula (1) wherein each symbol is as described in the specification, a pharmaceutically acceptable salt thereof and pharmaceutical use thereof. The compound of the present invention has a C5a receptor antagonistic action and is useful as an agent for the prophylaxis or treatment of diseases or syndromes due to inflammation caused by C5a [e.g., autoimmune diseases such as rheumatism, systemic lupus erythematosus and the like, sepsis, adult respiratory distress syndrome, chronic obstructive pulmonary disease, allergic diseases such as asthma and the like, atherosclerosis, cardiac infarction, brain infarction, psoriasis, Alzheimer's disease and serious organ injury (e.g., pneumonia, nephritis, hepatitis, pancreatitis and the like) due to activation of leukocytes caused by ischemia, trauma, burn, surgical invasion and the like].Type: GrantFiled: August 10, 2001Date of Patent: September 12, 2006Assignee: Mitsubishi Pharma CorporationInventors: Seigo Ishibuchi, Hiroshi Sumichika, Katsuhiko Itoh, Yoichi Naka
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Patent number: 6992106Abstract: The present invention provides composition having as active ingredients a stilbene derivative and a platinum coordination compound which is highly efficacious and highly safe for treating tumors, particularly for the treatment of solid or malignant tumors and thus methods of cancer and tumor treatment using the composition are also provided.Type: GrantFiled: June 12, 2002Date of Patent: January 31, 2006Assignee: Ajinomoto Co., Inc.Inventors: Yoshihiro Morinaga, Yukio Nihei, Yasuyo Suga, Manabu Suzuki, Kazuo Ohishi, Akira Okano
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Patent number: 6933320Abstract: An antitumor combination comprising a stilbene derivative and an anticancer compound selected from the group consisting of taxanes, alkylating agents, antimetabolites, vinca alkaloids, platinum compounds, epidophylloptoxins, and antibiotics as the active ingredients is provided. Methods of using these pharmaceutical preparations for the treatment of solid carcinomas and the like are also provided.Type: GrantFiled: March 15, 2002Date of Patent: August 23, 2005Assignee: Aventis Pharma S. A.Inventor: Marie-Christine Bissery
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Patent number: 6864380Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of inflammatory diseases such as asthma and other allergic diseases.Type: GrantFiled: July 3, 2003Date of Patent: March 8, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Dean A Wacker, John V Duncia, Joseph B Santella, III, Daniel S Gardner
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Patent number: 6852738Abstract: A class of acyl sulfamides comprises compounds that are potent ligands for PPAR gamma and generally have antagonist or partial agonist activity. The compounds may be useful in the treatment, control or prevention of obesity, non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, inflammation, and other PPAR gamma mediated diseases, disorders and conditions.Type: GrantFiled: January 25, 2002Date of Patent: February 8, 2005Assignee: Merck & Co., Inc.Inventors: A. Brian Jones, John J. Acton, III
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Patent number: 6838472Abstract: The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cancer and dermatological disorders.Type: GrantFiled: September 17, 2002Date of Patent: January 4, 2005Assignee: Syntex (U.S.A.) LLCInventors: Michael Klaus, Jean-Marc Lapierre
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Patent number: 6822001Abstract: Combination therapies are provided for the treatment of proliferative disorders which use a pentafluorobenzenesulfonamide of formula I and an antineoplastic agent such as gemcitabine or paclitaxel.Type: GrantFiled: November 2, 2001Date of Patent: November 23, 2004Assignee: Tularik Inc.Inventors: Susan Schwendner, Pieter Timmermans, Jacqueline Walling
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Patent number: 6815556Abstract: A compound according to formula one that is useful as a fungicide is provided. Additionally, processes to make and use same are provided.Type: GrantFiled: June 9, 2003Date of Patent: November 9, 2004Assignee: Dow AgroSciences LLCInventors: Carla Jean Rasmussen Klittich, Jeannie Rachel Cetusic, Marilene Tenguan Iamauti, Irene Mae Morrison, Michael Thomas Sullenberger, William Chi-Leung Lo, Ann Marie Buysse, Brent Jeffrey Rieder, John Todd Mathieson, Monica Britt Olson, Michael John Ricks
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Patent number: 6777561Abstract: Compounds of general formula I are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.Type: GrantFiled: June 1, 2000Date of Patent: August 17, 2004Assignee: AstraZeneca Canada Inc.Inventors: Daniel Delorme, Vlad Gregor, Edward Roberts, Eric Sun
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Publication number: 20040082625Abstract: The compounds of the invention are represented by the following general structure 1Type: ApplicationFiled: May 22, 2003Publication date: April 29, 2004Inventors: Michael G. Kelly, Shimin Xu, Ning Xi, Philip Miller, John F. Kincaid, Chiara Ghiron, Thomas Coulter
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Publication number: 20040082661Abstract: The invention relates to novel compounds having Vanilloid Receptor (VR1) antagonist activity, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders.Type: ApplicationFiled: September 8, 2003Publication date: April 29, 2004Inventors: Harshad Kantilal Rami, Mervyn Thompson, Paul Adrian Wyman
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Patent number: 6696487Abstract: The invention relates to compounds of formula (I), and also to salts thereof, which have fungicidal activities: in which the various radicals and substituents are as defined in the description, and also to the fungicidal compositions containing them and to methods for combating the phytopathogenic fungi of crops using these compounds and compositions.Type: GrantFiled: August 6, 2001Date of Patent: February 24, 2004Assignee: Bayer Cropscience S.A.Inventors: Vincent Gerusz, Darren James Mansfield, José Perez, David Tickle, Jean-Pierre Vors, Derek Baldwin, Thomas Lawley Hough, Dale Robert Mitchell
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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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Patent number: 6664259Abstract: This invention relates to novel compounds of Formula (I) to (VII), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: GrantFiled: September 6, 2002Date of Patent: December 16, 2003Assignee: SmithKline Beecham CorporationInventors: Katherine Louisa Widdowson, Qi Jin
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Patent number: 6624117Abstract: A heat sensitive recording material, comprising a) at least one colour forming compound, and b) at least one developer of the formula wherein R1 is unsubstituted or substituted phenyl, naphthyl or C1-C20alkyl, X is a group of the formula A is unsubstituted or substituted phenylene, naphthylene or C1-C12alkylene, or is an unsubstituted or substituted heterocyclic group, B is a linking group of formula —O—SO2—, —SO2—O—, —NH—SO2—, —SO2—NH—, —S—SO2—, —O—CO—, —O—CO—NH—, —NH—CO—, —NH—CO—O—, —S—CO—NH—, —S—CS—NH—, —CO—NH—SO2—, —O—CO—NH—SO2—, —NH═CH—, —CO—NH—CO—, —S—, —CO—, —O—, —SO2—NH—CO—, —O&mType: GrantFiled: October 1, 2001Date of Patent: September 23, 2003Assignee: Ciba Specialty Chemicals CorporationInventors: Michael Heneghan, Roy Alan Kirk, James Philip Taylor, John Whitworth, Robert Montgomery O'Neil, John Barry Henshall
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Patent number: 6608052Abstract: Disclosed are novel aromatic compounds of the formula(I) wherein G, E, W, Ar, X, Y and Z. The compounds are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.Type: GrantFiled: April 13, 2001Date of Patent: August 19, 2003Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Steffen Breitfelder, Pier F. Cirillo, John R. Regan
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Patent number: 6608227Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of inflammatory diseases such as asthma and other allergic diseases.Type: GrantFiled: October 13, 2000Date of Patent: August 19, 2003Assignee: Bristol-Myers Squibb PharmaInventors: Dean A Wacker, John V Duncia, Joseph B Santella, III, Daniel S Gardner
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Publication number: 20030125383Abstract: The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cancer and dermatological disorders.Type: ApplicationFiled: September 17, 2002Publication date: July 3, 2003Applicant: Roche Bioscience, a division of Syntex (U.S.A.) LLCInventors: Michael Klaus, Jean-Marc Lapierre
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Patent number: 6569895Abstract: Tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. It has been determined that 5-lipoxygenase activity, oral availability, and stability in vivo (for example, glucuronidation rate) can vary significantly among the optical isomers of the disclosed compounds.Type: GrantFiled: September 8, 1999Date of Patent: May 27, 2003Assignee: Millennium Pharmaceuticals, Inc.Inventors: Xiong Cai, Aberra Fura, Changgeng Qian
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Patent number: 6566304Abstract: The invention relates to use of (a) compounds of phosphorus containing at least partly lipophilic organic radicals together with (b) urea and/or urea derivatives in selected quantity ratios of (a) to (b) as a soil additive for biologically controlling plant-parasitic soil nematodes by strengthening the correspondingly antagonistic soil potential, more particularly by strengthening the growth of antagonistic and/or nematicidal rhizosphere bacteria and/or corresponding mycorrhiza strains—and at the same time strengthening the growth of cultivated plants in soil. The multicomponent mixtures which strengthen bacterial growth are preferably introduced into the region of the plant roots in the form of an aqueous preparation using plant-compatible emulsifiers before and/or during plant growth. Components (a) and (b) are used in such quantity ratios that the ratio by weight of C to N is no higher than 6:1 and preferably no higher than 5:1.Type: GrantFiled: February 6, 2001Date of Patent: May 20, 2003Assignee: Cognis Deutschland GmbHInventors: Doris Bell, Bettina Kopp-Holtwiesche, Stephan Von Tapavicza
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Patent number: 6525091Abstract: Substituted diarylureas, pharmaceutical compositions containing them, and their use for stimulating Fas-mediated apoptosis. The compounds, as single stereoisomers or mixtures of stereoisomers, their pharmaceutically acceptable salts, and pharmaceutical compositions containing them, are useful in methods of treating autoimmune diseases, infectious diseases, and malignancies.Type: GrantFiled: February 22, 2002Date of Patent: February 25, 2003Assignee: Telik, Inc.Inventors: Louise Robinson, Hugo O. Villar
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Patent number: 6515021Abstract: The invention relates to novel bicyclic aromatic compounds which have the general formula (I): as well as to the use of these compounds in pharmaceutical compositions intended for use in human or veterinary medicine (dermatological, rheumatic, respiratory, cardiovascular and ophthalmological complaints in particular), or alternatively in cosmetic compositions.Type: GrantFiled: September 12, 2000Date of Patent: February 4, 2003Assignee: Centre International de Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 6492419Abstract: A topically acceptable aqueous pour-on formulation adapted for localized external application to an animal, which format includes an effective amount of a water insoluble insect growth regulator (IGR), a suspending agent, a surfactant or mixture of surfactants, and an aqueous carrier.Type: GrantFiled: August 15, 2000Date of Patent: December 10, 2002Assignee: Schering-Plough Animal Health Corp.Inventor: Stanley Shepherd
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Patent number: 6492428Abstract: There are disclosed methods of use and pharmaceutical compositions for two related genera of low molecular weight compounds comprising optionally substituted iminoquinone or orthoquinone ring systems. The compounds have MIF (macrophage migration inhibitory factor) antagonist activity and find utility as such. For example, the compounds are useful for treating a variety of diseases involving inflammatory activity or pro-inflammatory cytokine responses, such as autoimmune diseases (including rheumatiod arthritis, insulin-dependent diabetes, multiple sclerosis, graft versus host disease, lupus syndromes), asthma, arthritis, EAE, ARDS, psoriasis, interleukin-2 toxicity, proliferative vascular disease, and various forms of sepsis and septic shock, and other conditions characterized by underlying MIF responses including, for instance, tumor growth and neovascularization (angiogenesis).Type: GrantFiled: July 26, 2000Date of Patent: December 10, 2002Assignee: The Picower Institute for Medical ResearchInventors: Yousef Al-Abed, Richard J. Bucala, Robert A. Mitchell, Peter Senter
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Patent number: 6479519Abstract: The invention is directed to physiologically active compounds of formula (I): wherein: R1 is hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy; X1, X2 and X6 independently represent N or CR10; and one of X3, X4 and X5 represents CR11 and the others independently represents N or CR10; where R10 is hydrogen, amino, halogen, hydroxy, lower alkyl, lower alkoxy, lower alkylthio, lower alkylsulphinyl, lower alkylsulphonyl, nitro or trifluoromethyl; and R11 represents a group —L1—Ar1—L2—Y; and the corresponding N-oxides, and their prodrugs; and pharmaceutically acceptable salts and solvates of such compounds and their N-oxides and prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (&agr;4&bgr;1).Type: GrantFiled: April 26, 2000Date of Patent: November 12, 2002Assignee: Aventis Pharma LimitedInventors: Peter Charles Astles, David Edward Clark, Alan John Collis, Paul Joseph Cox, Paul Robert Eastwood, Neil Victor Harris, Justine Yeun Quai Lai, Andrew David Morley, Barry Porter
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Patent number: 6462087Abstract: The present invention provides composition having as active ingredients a stilbene derivative and a platinum coordination compound which is highly efficacious and highly safe for treating tumors, particularly for the treatment of solid or malignant tumors and thus methods of cancer and tumor treatment using the composition are also provided.Type: GrantFiled: October 3, 2000Date of Patent: October 8, 2002Assignee: Ajinomoto Co., Inc.Inventors: Yoshihiro Morinaga, Yukio Nihei, Yasuyo Suga, Manabu Suzuki, Kazuo Ohishi, Akira Okano
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Patent number: 6423854Abstract: Use of at least one aminophenol derivative of formula (I) below: in which: R represents a hydrogen atom or a radical —COR2, wherein R2 represents a saturated or unsaturated, linear, cyclic or branched, optionally hydroxylated, C1 to C30 hydrocarbon or alkoxy radical; R1 is a radical of formula (a), (b) or (c) below: (a) —CO—NR3R4 (b) —CO—O—R5 (c) —SO2—R5 wherein R3 represents a hydrogen atom or a linear or branched, saturated or unsaturated, optionally hydroxylated, C1 to C6 hydrocarbon radical, R4 represents a hydrogen atom or a saturated or unsaturated, linear, cyclic or branched, optionally hydroxylated, C1 to C30 hydrocarbon radical, and R5 represents a saturated or unsaturated, linear, cyclic or branched, optionally hydroxylated, C1 to C30 hydrocarbon radical, in a depigmenting and/or bleaching cosmetic composition for human skin, body hairs or head hair; compositions comprising the derivatives of formula (I) and a process forType: GrantFiled: June 21, 1999Date of Patent: July 23, 2002Assignee: L'OrealInventors: Michel Philippe, Remy Tuloup, Christian Blaise
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Patent number: 6387906Abstract: The present invention concerns novel compounds of formula a N-oxide form, a pharmaceutically acceptable acid addition salt or a stereochemically isomeric form thereof, wherein n is zero, 1, 2 or 3; X is N or CH; each R1 independently is halo, nitro, cyano, amino, hydroxy, C1-4alkyl, C1-4alkyloxy or trifluoromethyl; R2 is hydrogen; C3-7alkenyl; C3-7alkynyl, aryl; C3-7cycloalkyl; optionally substituted C1-6alkyl R3 and R4 each independently are hydrogen, C1-6alkyl, C3-7cycloalkyl or aryl; or R3 and R4 taken together form a bivalent radical —R3—R4— of formula: wherein R5a, R5b, R5c, R5d each independently are hydrogen, C1-6alkyl or aryl; and aryl is optionally substituted phenyl; as antifungals; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: January 7, 2000Date of Patent: May 14, 2002Inventors: Lieven Meerpoel, Jan Heeres, Frank Christopher Odds, Hugo Florent Adolf Vanden Bossche, Louis Jozef Elisabeth Van der Veken
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Publication number: 20020026068Abstract: Composition containing at least one aminophenol derivative and a solubilizing compound which is not in the form of vesicles, chosen from: (a) oxyalkylenated fatty acid esters of sorbitan, (b) oxyalkylenated hydrogenated castor oils, and/or (c) oxyalkylenated fatty alcohols. The invention also relates to a process for dissolving at least one aminophenol derivative by mixing it with a solubilizing agent as defined above.Type: ApplicationFiled: December 20, 2000Publication date: February 28, 2002Applicant: L'OREALInventors: Veronique Chevalier, Melanie Quest
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Publication number: 20020016367Abstract: Modulation of the activity of the insulin receptor, enhancement of glucose uptake by cells, and other effects significant in the control and management of diabetes are accomplished using compounds of the formula 1Type: ApplicationFiled: September 21, 2001Publication date: February 7, 2002Inventors: Richard Sportsman, Hugo O. Villar, Lawrence M. Kauvar, Apparao Satyam
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Patent number: 6329431Abstract: Modulation of the activity of the insulin receptor, enhancement of glucose uptake by cells, and other effects significant in the control and management of diabetes are accomplished using compounds of the formula wherein each A is independently a proton-accepting substituent; each R is independently a noninterfering substituent; m is 0 or 1; n is 0, 1, or 2; and each linker is independently —NHCNHNH—, —NHCOO—, OCOO—,—CH═CH—, —CH═N—, —CH2CH2—, —NHCH2—, —OCO— or —COO—. Compounds in the genus of Formula (1) can also be used for structure activity studies to identify features responsible for the relevant activities.Type: GrantFiled: August 21, 1997Date of Patent: December 11, 2001Assignee: Telik, Inc.Inventors: Richard Sportsman, Hugo O. Villar, Lawrence M. Kauvar, Apparao Satyam
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Patent number: 6316478Abstract: This invention relates to novel spiro compound derivatives of benzoisothiazolyl-urea and -thiourea and compositions thereof. These compounds are useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: GrantFiled: March 3, 2000Date of Patent: November 13, 2001Assignee: SmithKline Beecham CorporationInventors: Katherine L. Widdowson, Hong Nie
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Patent number: 6310074Abstract: The invention relates to compound of formula (I): A—G1—Cy—G2—Cy′—G3—B (I) wherein: A represents a grouping NR1C(Q)R2, C(Q)NR2R3 or NR1C(Q)NR2R3, B represents a grouping NR1C(Q)R2, NR1C(Q)NR2R3, C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 or NR2R3, G1 and G3 represent an optionally substituted alkylene chain, Cy and Cy′, which are different, represent a ring structure or G2 represents a chain and medicinal products containing the same are useful in treating or in preventing melatoninergic disorders.Type: GrantFiled: May 18, 2000Date of Patent: October 30, 2001Assignee: Adir et CompagnieInventors: Patrick Depreux, Said Yous, Gwenael Cheve, Gérald Guillaumet, Marie-Claude Viaud, Carlos Larraya, Caroline Bennejean, Philippe Delagrange, Pierre Renard, Carole Descamps-Francois
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Patent number: 6150415Abstract: Biologically stable inhibitors of soluble epoxide hydrolases are provided. The inhibitors can be used, for example, to selectively inhibit epoxide hydrolase in therapeutic applications such as treating inflammation, for use in affinity separations of the epoxide hydrolases, and in agricultural applications. A preferred class of compounds for practicing the invention have the structure shown by Formula 1 ##STR1## wherein X and Y is each independently nitrogen, oxygen, or sulfur, and X can further be carbon, at least one of R.sub.1 -R.sub.4 is hydrogen, R.sub.2 is hydrogen when X is nitrogen but is not present when X is sulfur or oxygen, R.sub.4 is hydrogen when Y is nitrogen but is not present when Y is sulfur or oxygen, R.sub.1 and R.sub.3 are each independently a substituted or unsubstituted alkyl, haloalkyl, cycloalkyl, aryl, acyl, or heterocyclic, or being a metabolite or degradation product thereof.Type: GrantFiled: February 18, 1999Date of Patent: November 21, 2000Assignee: The Regents of the University of CaliforniaInventors: Bruce D. Hammock, Christophe H. Morisseau, Jiang Zheng, Marvin H. Goodrow, Tonya Severson, James Sanborn
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Patent number: 6147255Abstract: The invention relates to novel bicyclic aromatic compounds which have the general formula (I): ##STR1## as well as to the use of these compounds in pharmaceutical compositions intended for use in human or veterinary medicine (dermatological, rheumatic, respiratory, cardiovascular and ophthalmological complaints in particular), or alternatively in cosmetic compositions.Type: GrantFiled: January 26, 1998Date of Patent: November 14, 2000Assignee: Centre International de Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 6147116Abstract: The present invention relates to polyaromatic compounds having useful antiviral activity against viruses of the herpes family, to a composition containing them, and to a method of using them for the treatment of herpes viruses infections.Type: GrantFiled: May 11, 1999Date of Patent: November 14, 2000Assignee: Pharmacia & Upjohn CompanyInventors: Michael Robert Barbachyn, Fred L. Homa, Antonio Monge, Esteban Santiago, Juan J. Martinez-Irujo, Maria Font
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Patent number: 6133319Abstract: This invention relates to the use of phenyl ureas of formulas (I) and (II) in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8). The variables of (I) and (II) are defined herein.Type: GrantFiled: August 19, 1999Date of Patent: October 17, 2000Assignee: SmithKline Beecham CorporationInventor: Katherine L. Widdowson
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Patent number: 6103761Abstract: The invention concerns a series of novel bis-urea derivatives, nonpeptides, which show good binding affinity for the CCK-B receptor. The compounds, compositions containing them, methods of preparation, and utilities including anxiety, gastric acid secretion inhibition, and psychoses are included.Type: GrantFiled: October 19, 1994Date of Patent: August 15, 2000Assignee: Warner-Lambert CompanyInventors: Bradley Dean Tait, Michael William Wilson
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Patent number: RE38915Abstract: Modulation of the activity of the insulin receptor, enhancement of glucose uptake by cells, and other effects significant in the control and management of diabetes are accomplished using compounds of the formula wherein each A is independently a proton-accepting substituent; each R is independently a noninterfering substituent; n is 0, 1, or 2; and each linker is independently an isostere of —NHCONH— or of —N?N— or of —NHCO—. Compounds in the genus of Formula (1) can also be used for structure activity studies to identify features responsible for the relevant activities.Type: GrantFiled: December 21, 2000Date of Patent: December 6, 2005Assignee: Telik, Inc.Inventors: Richard Sportsman, Hugo O. Villar, Lawrence M. Kauvar, Wayne R. Spevak
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Patent number: RE39866Abstract: Modulation of the activity of the insulin receptor, enhancement of glucose uptake by cells, and other effects significant in the control and management of diabetes are accomplished using compounds of the formula wherein each A is independently a proton-accepting substituent; each R is independently a noninterfering substituent; n is 0, 1, or 2; and each linker is independently an isostere of —NHCONH— or of —N?N— or of —NHCO—. Compounds in the genus of Formula (1) can also be used for structure activity studies to identify features responsible for the relevant activities.Type: GrantFiled: June 23, 2005Date of Patent: October 2, 2007Assignee: Telik, Inc.Inventors: Richard Sportsman, Hugo O. Villar, Lawrence M Kauvar, Wayne R Spevak