Polycyclo Ring System Patents (Class 562/466)
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Patent number: 6869967Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? suptype.Type: GrantFiled: July 18, 2002Date of Patent: March 22, 2005Assignee: Novo Nordisk A/SInventors: Lone Jeppesen, Paul Stanley Bury, John Patrick Mogensen, Ingrid Pettersson, Per Sauerberg
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Patent number: 6867320Abstract: A compound represented by the formula (I) or a salt thereof: wherein n represents an integer of 1 to 3, R represents an alkyl group having 3 to 8 carbon atoms, a group represented by the following formula: R1(CH2)k— (wherein k represents 0 or an integer of 1 to 3; R1 represents a saturated cyclic alkyl group having 3 to 7 carbon atoms or a saturated condensed cyclic alkyl group having 6 to 8 carbon atoms, and the group R1 may be substituted with a lower alkyl group having 1 to 4 carbon atoms) and the like, and Ar represents a condensed bicyclic group such as naphthalen-1-yl group, which has suppressing action on prostaglandin and leukotriene production and is useful for prophylactic and/or therapeutic treatment of various inflammatory diseases and the like caused by these lipid mediators.Type: GrantFiled: February 20, 2003Date of Patent: March 15, 2005Assignee: Asahi Kasei Pharma CorporationInventors: Motoshi Shoda, Hiroshi Kuriyama
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Patent number: 6825233Abstract: There are provided compounds represented by the formula I or a nontoxic pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof, wherein the various substituents are as defined. Also included are methods for preventing and/or treating tumors, arthritis, and non-malignant skin disorders comprising administering a compound of formula I to a mammal. Further provided are pharmaceutical formulations comprising a compound of formula I in admixture with one or more pharmaceutically acceptable excipients.Type: GrantFiled: February 13, 2002Date of Patent: November 30, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Anna Ericsson, Anne Marinier, Fred C. Zusi
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Publication number: 20040198825Abstract: Compounds of the formula 1Type: ApplicationFiled: April 3, 2003Publication date: October 7, 2004Inventors: Richard L. Beard, Haiqing Yuan, Roshantha A. Chandratratna
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Patent number: 6777418Abstract: The current invention provide novel retinoid compounds and methods for their synthesis, methods of treating or preventing emphysema, cancer and dermatological disorders and pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders.Type: GrantFiled: October 1, 2001Date of Patent: August 17, 2004Assignee: Syntex (U.S.A.) LLCInventors: Jean-Marc Lapierre, David Mark Rotstein, Eric Brian Sjogren
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Publication number: 20040147611Abstract: Diabetic mammals are treated with compounds that are significantly more efficacious as agonists of RXR&bgr; retinoid receptors than as agonists of RXR&agr; or RXR&ggr; retinoid receptors. The treatment reduces serum glucose and triglyceride levels of the mammals without the undesirable side effects of reducing serum thyroxine levels and a transient increase in serum triglyceride levels Compounds suitable for use in the methods of treatments of the present invention are selected by testing and identifying compounds of selective or specific efficacy as agonists of RXR&bgr; retinoid receptors in preference over RXR&agr; and/or RXR&ggr; retinoid receptors. Novel compounds used in the methods of the invention have Formula 1 where the variables are defined as disclosed in the specification.Type: ApplicationFiled: December 17, 2003Publication date: July 29, 2004Inventors: Yang-Dar Yuan, Richard L. Beard, Roshantha A. Chandraratna
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Patent number: 6759547Abstract: Compounds of the formula where the variables have the meaning defined in the specification are capable of reducing serum glucose levels in diabetic mammals without the undesirable side effect of reducing serum thyroxine levels.Type: GrantFiled: January 14, 2003Date of Patent: July 6, 2004Assignee: Allergan, Inc.Inventors: Richard L. Beard, Haiqing Yuan, Yang-Dar Yuan, Roshantha A. Chandraratna
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Publication number: 20040110951Abstract: The invention provides thiazolidinedione, oxadiazolidinedione, and triazolone compounds of Formula (I) which compounds are thyroid receptor ligands.Type: ApplicationFiled: July 11, 2003Publication date: June 10, 2004Inventor: Yuan-Ching P. Chiang
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Publication number: 20040092748Abstract: Derivatives of C2-substituted indan-1-ol compounds of formula I: 1Type: ApplicationFiled: October 27, 2003Publication date: May 13, 2004Applicant: Aventis Pharma Deutschland GmBHInventors: Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
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Publication number: 20040092749Abstract: Polysubstituted indan-1-ol compounds, methods for their preparation; and methods for their use are disclosed herein.Type: ApplicationFiled: October 27, 2003Publication date: May 13, 2004Applicant: Aventis Pharma Deutschland GmBHInventors: Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
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Publication number: 20040063963Abstract: The present invention provides a binaphthol compound represented by formula [1]: 1Type: ApplicationFiled: July 1, 2003Publication date: April 1, 2004Inventors: Ryuzo Ueno, Masaya Kitayama, Kenji Minami, Hiroyuki Wakamori
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Publication number: 20040042981Abstract: The present invention relates to novel compounds, termed serpentemycins, of the formula (I) 1Type: ApplicationFiled: June 27, 2003Publication date: March 4, 2004Applicant: Aventis Pharma Deutschland GmbHInventors: Laszlo Vertesy, Michael Kurz, Joachim Wink
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Patent number: 6686386Abstract: The present invention relates to pharmaceutical and cosmetic compositions comprising at least one agonist ligand, which is specific for receptors of the RAR-&ggr; type, which are characterized as inducers of apoptosis in at least one cell population in which apoptosis can be induced by activating receptors of the RAR-&ggr; type. In one aspect of the present invention, there is provided a method of combating photoinduced or chronological ageing of skin, said method comprising administering an effective amount of at least one agonist ligand which is specific for receptors of the RAR-&ggr; type to combat photoinduced or chronological aging of skin, wherein the agonist ligand has a ratio R which is equal to or greater than 10.Type: GrantFiled: November 2, 1999Date of Patent: February 3, 2004Assignee: Galderma Research & Development S.N.C.Inventors: Laszlo Fesus, Zsuzsa Szondy, Uwe Reichert
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Patent number: 6683111Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).Type: GrantFiled: October 25, 2001Date of Patent: January 27, 2004Assignees: Novo Nordisk A/S, Dr. Reddy's Research FoundationInventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Publication number: 20030220315Abstract: Alkenyldiarylmethane (ADAM) compounds have been found effective as anti-HIV agents. Novel ADAM compounds, their pharmaceutical formulations and a method of using same to treat viral infections are described.Type: ApplicationFiled: May 27, 2003Publication date: November 27, 2003Inventors: Mark S. Cushman, Agustin Casimiro-Garcia, William G. Rice
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Publication number: 20030212293Abstract: A method for transferring amino acid into ketone acid (ester) may obtain ketone acid (ester) at low cost. The method uses sodium hypochlorous acid as oxidizing agent and proceeds oxidation reaction with amino acid or its derivatives so as to obtain ketone acid and its derivatives. The sodium hypochlorous acid is easily to get with low cost and the conditions of the reaction are mild so that the method meets the needs of the industry.Type: ApplicationFiled: May 10, 2002Publication date: November 13, 2003Inventor: Chung-Jang Chang
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Patent number: 6632963Abstract: Novel pharmaceutically/cosmetically-active bicyclic aromatic compounds have the structural formula (I): in which Ar1 is a radical having one of the structural formulae (a)-(c): Ar2 is a radical having one of the following formulae (d)-(h): and X is a radical having one of the following formulae (i)-(l): and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: March 29, 1999Date of Patent: October 14, 2003Assignee: Galderma Research & Development S.N.C.Inventor: Jean-Michel Bernardon
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Publication number: 20030176506Abstract: 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: ApplicationFiled: December 2, 2002Publication date: September 18, 2003Inventors: Marcia J. Dawson, Joseph A. Fontana, Xiao-kun Zhang, Mark Leid, Ling Jong, Peter D. Hobbs
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Patent number: 6610883Abstract: Compounds, compositions, and methods for modulating processes mediated by Retinoid X Receptors using retinoid-like compounds which have activity selective for members of the subclass of Retinoid X Receptors (RXRs), in preference to members of the subclass of Retinoic Acid Receptors (RARs). Examples of such compounds are bicyclic benzyl, pyridinyl, thiophene, furanyl, pyrrole, and polyenoic acid derivatives including carbocyclic polyenoic acids. The disclosed methods employ compounds for modulating processes selectively mediated by Retinoid X Receptors.Type: GrantFiled: July 13, 1998Date of Patent: August 26, 2003Assignee: Ligand Pharmaceuticals, Inc.Inventors: Marcus F. Boehm, Richard A. Heyman, Lin Zhi, Chan Kou (Jack) Hwang, Steve White, Alex Nadzan
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Patent number: 6610877Abstract: Compounds of the formula wherein R1 is a residue of the formula and R2-R10 have the significance given in the specification can be used as pharmaceuticals, particularly for the repair of photodamaged skin, other dermatological conditions, and oncological indications.Type: GrantFiled: August 1, 1997Date of Patent: August 26, 2003Assignee: Hoffman-La Roche Inc.Inventors: Michael Klaus, Peter Mohr
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Patent number: 6603012Abstract: New compounds containing bicyclic fused rings, one of which being a phenyl moiety connected by an aliphatic chain to a cycloalkyl or aryl moiety, and pharmaceutically active salts thereof are useful as RAR selective retinoid agonists. Furthermore, such retinoic acid receptor agonists, particularly retinoic acid receptor &ggr; (RAR&ggr;) selective agonists, are useful for the treatment of emphysema and associated pulmonary diseases, as well as for the therapy and prophylaxis of dermatological disorders, for the therapy and prophylaxis of malignant and premalignant epithelial lesions, tumors and precancerous changes of the mucous membrane in the mouth, tongue, larynx, esophagus, bladder, cervix and colon.Type: GrantFiled: April 23, 2001Date of Patent: August 5, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Paula Nanette Belloni, Synese Jolidon, Michael Klaus, Jean-Marc Lapierre
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Patent number: 6603040Abstract: Compounds useful as surface coating agents, including compounds of the formula: wherein X1 comprises a first photoreactive species; X2 comprises a second photoreactive species; Y comprises a nonpolymeric core molecule comprising an aromatic group; and Z comprises at least one charged group. The Y core can include an aromatic group such as a benzene radical, the charged groups Z can be independently selected from the organic acids that include sulfonic acid, carboxylic acid, and phosphoric acid, and the photoreactive species of X1 and X2 can independently be aryl ketones, such as those selected from the group acetophenone, benzophenone, anthraquinone, anthrone, and anthrone-like heterocycles, and their substituted derivatives.Type: GrantFiled: June 25, 2001Date of Patent: August 5, 2003Assignee: SurModics, Inc.Inventor: Dale G. Swan
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Publication number: 20030139473Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR&dgr; suptype.Type: ApplicationFiled: July 19, 2002Publication date: July 24, 2003Inventors: Lone Jeppesen, Paul Stanley Bury, John Patrick Mogensen, Ingrid Pettersson, Per Sauerberg
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Patent number: 6586463Abstract: Compounds having the general structure: which are useful for the treatment of a variety of diseases and conditions, such as bone disorders.Type: GrantFiled: September 4, 2001Date of Patent: July 1, 2003Assignee: The Procter & Gamble CompanyInventors: Mitchell Anthony deLong, David Lindsey Soper, John August Wos, Biswanath De
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Patent number: 6562998Abstract: Granular product of 2-hydroxynaphthalene-3-carboxylic acid with well-suppressed dusting tendency, and process for preparing the same is provided. Granular product of 2-hydroxynaphthalene-3-carboxylic acid having an average particle size of 150 &mgr;m or more and a hardness of 70-3000 g, and a process for preparing the same comprising the steps of dry compressing powdery 2-hydroxynaphthalene-3-carboxylic acid to give compressed material and pulverizing and classifying the same.Type: GrantFiled: June 26, 2001Date of Patent: May 13, 2003Assignee: Kabushiki Kaisha Ueno Seiyako Oyo KenkyujoInventors: Ryuzo Ueno, Masaya Kitayama, Nobutaka Izumichi, Syungo Nara, Masaharu Kittaka
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Patent number: 6555704Abstract: A method is provided for the preparation of alpha-aryl-propionic acids such as ibuprofen by carbonylating the corresponding 1-arylethyl halide in an acidic aqueous medium containing a palladium catalyst. In the preparation of ibuprofen, 1-(4′-isobutylphenyl)ethyl halide is reacted with carbon monoxide in an acidic aqueous medium containing a palladium catalyst.Type: GrantFiled: May 22, 1995Date of Patent: April 29, 2003Assignee: BASF CorporationInventor: Varadaraj Elango
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Patent number: 6555577Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).Type: GrantFiled: January 26, 2001Date of Patent: April 29, 2003Assignee: Novo Nordisk A/SInventors: John Patrick Mogensen, Per Sauerberg, Paul Stanley Bury, Lone Jeppesen, Ingrid Pettersson
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Patent number: 6521646Abstract: Compounds of the formula (I) and their physiologically acceptable salts and solvates are useful as integrin-inhibiting substances. They are especially useful in the prophylaxis and treatment of cardiovascular disorders, of thrombosis, cardiac infarction, coronary heart diseases, arteriosclerosis, osteoporosis, in pathological conditions that are caused or propagated by angiogenesis and in tumor therapy.Type: GrantFiled: October 15, 2001Date of Patent: February 18, 2003Assignee: Merck Patent GmbHInventors: Wolfgang Stähle, Rudolf Gottschlich, Simon Goodman
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Publication number: 20030018207Abstract: The present invention relates to certain phenalkyloxy-phenyl derivatives of formula (I) and analogs, to a process for preparing such compounds, having the utility in clinical conditions associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: June 3, 2002Publication date: January 23, 2003Inventors: Jonas Fagerhag, Lanna Li, Eva-Lotte Linstedt Alstermark
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Publication number: 20030008882Abstract: The present invention relates to compounds and pharmaceutical compositions which are proteomimetic and to methods for inhibiting the interaction of an alpha-helical protein with another protein or binding site. Methods for treating diseases or conditions which are modulated through interactions between alpha helical proteins and their binding sites are other aspects of the invention.Type: ApplicationFiled: May 8, 2002Publication date: January 9, 2003Inventors: Andrew D. Hamilton, Justin Ernst, Brendan P. Orner
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Patent number: 6495546Abstract: Propanolamine derivatives represented by the following formula (I): These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.Type: GrantFiled: November 22, 2000Date of Patent: December 17, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Patent number: 6479549Abstract: A novel carnosic acid derivative for promoting the synthesis of nerve growth factor (NGF), a composition comprising the carnosic acid derivative as an effective ingredient, as well as, a method of promoting the synthesis of NGF comprising administering an effective amount of the carnosic acid derivative as an effective ingredient to a subject requiring such promotion. The carnosic acid derivative, composition and method according to the present invention can safely and efficiently promote the production of NGF in the living body, without being accompanied by a side effect such as a loss of a quantitative balance of hormones in the living body.Type: GrantFiled: February 28, 2001Date of Patent: November 12, 2002Assignee: Nagase & Company, Ltd.Inventors: Kunio Kosaka, Toshitsugu Miyazaki, Toshio Yokoi
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Publication number: 20020151720Abstract: Novel naphthol derivatives, and various azo compounds and metal complexes prepared by using the derivatives are provided.Type: ApplicationFiled: January 16, 2002Publication date: October 17, 2002Inventors: Ryuzo Ueno, Masaya Kitayama, Kenji Minami, Hiroyuki Wakamori
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Publication number: 20020120153Abstract: A method of producing a compound of the formula: 1Type: ApplicationFiled: February 15, 2001Publication date: August 29, 2002Inventor: M. Mahmun Hossain
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Patent number: 6433021Abstract: Indane compounds of general formulae (1) to (4) and their pharmaceutical use, particularly to achieve mast cell stabilising activity and/or anti-inflammatory activity are described.Type: GrantFiled: December 3, 1999Date of Patent: August 13, 2002Assignee: Venantius LimitedInventors: Neil Frankish, Helen Sheridan, John Walsh, Michael Jordan
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Patent number: 6403638Abstract: Compounds having the formulas below, where R is H, lower alkyl, or a pharmaceutically acceptable salt, and where R1 represents i-propyl, t-butyl or n-butyl groups, have selective RXR retionoid agonist activity.Type: GrantFiled: March 21, 2000Date of Patent: June 11, 2002Assignee: Allergan Sales, Inc.Inventors: Vidyasagar Vuligonda, Kwok Yin Tsang, Jayasree Vasudevan, Roshantha A. Chandraratna
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Patent number: 6387951Abstract: Compounds having Formulas 5 and 6 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.Type: GrantFiled: August 29, 2000Date of Patent: May 14, 2002Assignee: Allergan Sales, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Dehua Huang, Roshantha A. Chandraratna
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Publication number: 20020002290Abstract: 1Type: ApplicationFiled: June 14, 2001Publication date: January 3, 2002Applicant: Secretary of State for Defence in her Britannic Majesty's Government of the United KingdomInventors: Graeme P. Nicholson, Mark J. Kan, Gareth Williams, Michael G. Drew, Paul D. Beer
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Patent number: 6326369Abstract: A compound of the formula: wherein R1 and R2 each represents a lower alkyl, or R1 and R2 may be bonded together to form a ring; X represents a spacer of which the number of atoms constituting the principal chain is 1 to 15; Y represents an acyl, or a hydroxy, an amino or an aromatic group, each of which may be substituted; and ring A represents a 5- to 8-membered ring which may be further substituted apart from —X—Y, or a salt thereof is useful as a pharmaceutical composition for preventing or treating disease related to mitochondrial dysfunction.Type: GrantFiled: July 6, 1999Date of Patent: December 4, 2001Assignee: Takeda Chemicals Industries, Ltd.Inventors: Kaneyoshi Kato, Taiichi Ohra, Masaomi Miyamoto
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Patent number: 6316009Abstract: “Biphenyl derivatives substituted with an aromatic or heteroaromatic radical, and pharmaceutical and cosmetic compositions containing them” in which: Ar represents an aromatic or a heteroaromatic radical optionally substituted, in particular, with an alkyl or a carboxyl group, R2 and R3 represent, in particular, H or alkyl, or R2 and R3, taken together, form a 5- or 6-membered ring, R4 and R5 represent, in particular, H or halogen, R6 represents, in particular, H or lower alkyl, and the salts of the compounds of formula (I). These compounds can be used in particular in the treatment of dermatological complaints associated with a keratinization disorder, and for combating ageing of the skin.Type: GrantFiled: April 6, 1999Date of Patent: November 13, 2001Assignee: Galderma Research & DevelopmentInventors: Jean-Michel Bernardon, Philippe Nedoncelle
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Patent number: 6306899Abstract: This invention relates to anti-viral drugs such as Helioxanthin and its analogs. The present compounds may be used alone or in combination with other drugs for the treatment of Hepatitis B virus (HBV), Hepatitis C virus (HCV), Yellow Fever, Dengue Virus, Japanese Encephalitis, West Nile virus and related flaviviruses. In addition, compounds according to the present invention can be used to prevent hepatoma secondary to virus infection as well as other infections or disease states which are secondary to the virus infection.Type: GrantFiled: August 23, 1999Date of Patent: October 23, 2001Assignees: Yale University, N. Y. Mu, N.T.U., V.G.HInventors: Yung-Chi Cheng, Chen-Kung Chou, Lei Fu, Yueh-Hsiung Kuo, Sheau-Farn Yeh, Juliang Zhu, Yonglian Zhu
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Patent number: 6248781Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, Ar, X, Q, A, Y and Z are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).Type: GrantFiled: October 19, 1999Date of Patent: June 19, 2001Assignees: Novo Nordisk A/S, Dr. Reddy's Research FoundationInventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Patent number: 6242635Abstract: A process for producing a 2-aralkyl-3-hydroxypropionic acid (or its ester), comprising the steps of: reacting a 3-hydroxy-2-methylene-3-arylpropionic acid ester, easily obtained by the reaction of an arylaldehyde with an acrylic acid ester, with an acid anhydride to form a 2-aralkylidene-3-acyloxypropionic acid ester; subjecting the same to hydrolysis or alcoholysis; and reducing the resulting 2-aralkylidene-3-hydroxypropionic acid or its ester. The reduction step may be conducted in the presence of a base.Type: GrantFiled: September 18, 1998Date of Patent: June 5, 2001Assignee: Ajinomoto Co., Inc.Inventors: Takayuki Suzuki, Takayuki Hamada, Kunisuke Izawa
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Patent number: 6242493Abstract: Compounds of formula I: as well as pharmaceutically acceptable salts, hydrates and esters thereof, are disclosed. The compounds are useful for treating or preventing prostaglandin mediated diseases. Pharmaceutical compositions containing such compounds and methods of treatment are also included.Type: GrantFiled: March 10, 1999Date of Patent: June 5, 2001Assignee: Merck Frosst Canada & Co.Inventors: Yves Gareau, Marc LaBelle, Helene Juteau, Michel Gallant, Nicolas LaChance, Michel Belley
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Patent number: 6201019Abstract: Bi-aromatic compounds linked via a heteroethynylene radical are provided along with pharmaceutical and cosmetic compositions containing these compounds and methods for their use.Type: GrantFiled: April 8, 1999Date of Patent: March 13, 2001Assignee: Galderma Research & DevelopmentInventors: Jean-Michel Bernardon, Philippe Diaz
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Patent number: 6187933Abstract: Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.Type: GrantFiled: January 27, 2000Date of Patent: February 13, 2001Assignee: Allergan Sales, Inc.Inventors: Vidyasagar Vuligonda, Min Teng, Richard L. Beard, Alan T. Johnson, Yuan Lin, Roshantha A. Chandraratna
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Patent number: 6160175Abstract: A class of novel naphthyl acetamide compounds is disclosed together with the use of such compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.Type: GrantFiled: June 9, 1998Date of Patent: December 12, 2000Assignee: Eli Lilly and CompanyInventors: Theodore Goodson, Jr., Richard W. Harper, David K. Herron
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Patent number: 6147224Abstract: Compounds of Formula 1, Formula 2 or Formula 3 where X is O, S, or (CR.sub.1 R.sub.1).sub.n where n is 0, 1 or 2; Y is a bivalent radical having Formula 4 or Formula 5 where o is an integer from 1 to 4 ##STR1## or Y is a bivalent aryl or 5 or 6 membered heteroaryl radical having 1 to 3 heteroatoms selected from N, S and O, said aryl or heteroaryl groups being unsubstituted, or substituted with 1 to 3 C.sub.1-6 alkyl or with 1 to 3 C.sub.1-6 fluoroalkyl groups; and the remaining symbols have the meaning described in the specification, have RXR selective retinoid agonist-like activity.Type: GrantFiled: October 1, 1998Date of Patent: November 14, 2000Assignee: Allergan Sales, Inc.Inventors: Vidyasagar Vuligonda, Kwok Yin Tsang, Jayasree Vasudevan, Roshantha A. Chandraratna
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Patent number: 6136852Abstract: The present invention relates to 3,4-disubstituted phenylethanolaminotetralincarboxylic acid derivatives represented by the general formula: ##STR1## [wherein Q represents a vinylene group or a group represented by the general formula:-A-(CH.sub.2).sub.m --(wherein A represents an oxygen atom or a methylene group; and m is an integer of from 1 to 6); R represents a hydrogen atom or a lower alkyl group; n is an integer of 1 or 2; the carbon atom marked with * represents a carbon atom in R configuration, S configuration or a mixture thereof; and the carbon atom marked with (S) represents a carbon atom in S configuration] and pharmaceutically acceptable salts thereof, which have a selective .beta..sub.2 -adrenergic receptor stimulating effect with relieved burdens on the heart such as tachycardia and are useful as an agent for the prevention of threatened abortion and premature labor, a bronchodilator and an agent for pain remission and promoting stone removal in urolithiasis.Type: GrantFiled: March 8, 1999Date of Patent: October 24, 2000Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Makio Kitazawa, Kosuke Okazaki, Tetsuro Tamai, Masaru Saito, Nobuyuki Tanaka, Hiroaki Kobayashi, Ken Kikuchi, Hideyuki Muranaka
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Patent number: 6096920Abstract: Palladium-catalyzed arylation of an olefin (e.g., ethylene) with an aromatic halide (e.g., 2-bromo-6-methoxynaphthalene, m-bromobenzophenone, or 4-isobutyl-1-bromobenzene) is conducted in specified media. After a special acid or base phase separation procedure, palladium-catalyzed carbonylation of the olefinically-substituted aromatic intermediate is conducted in specified media using CO and water or an alcohol to form arylalkylcarboxylic acid or ester or substituted arylalkylcarboxylic acid or ester (e.g., racemic 2-(6-methoxy-2-naphthyl)propionic acid, 2-(3-benzoylphenyl)propionic acid, or 2-(4-isobutylphenyl)propionic acid). Catalyst recovery procedures enabling recycle of catalyst residues and efficient recovery of amine hydrogen halide scavenger and solvent used in the arylation reaction are described, as well as novel, highly efficient methods of conducting the carbonylation reaction.Type: GrantFiled: July 8, 1998Date of Patent: August 1, 2000Assignee: Albemarle CorporationInventors: Robert H. Allen, R. Carl Herndon, Jr., Kannappan C. Chockalingam, W. Dirk Klobucar, Gary D. Focht, Tse-Chong Wu, Gary D. Heidebrecht, Joseph D. McLean, Yaping Zhong, Thorsten W. Brockmann, Ronny W. Lin, William J. Layman, Jr., Ranjit K. Roy