Plural Rings In Substituent Q Patents (Class 564/171)
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Publication number: 20100168216Abstract: The present invention relates to new prostaglandin derivatives having improved pharmacological activity and enhanced tolerability. They can be employed for the treatment of glaucoma and ocular hypertension.Type: ApplicationFiled: March 6, 2008Publication date: July 1, 2010Applicant: CTG PHARMA S.R.L.Inventors: Piero Del Soldato, Giancarlo Santus, Anna Sparatore
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Publication number: 20100105771Abstract: The present invention is directed to novel amino acid prostaglandin salts and methods of making and using them.Type: ApplicationFiled: October 29, 2008Publication date: April 29, 2010Inventors: Mitchell A. deLong, Jill Marie Sturdivant
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Publication number: 20100105775Abstract: The present invention is directed to novel amino acid prostaglandin salts and methods of making and using them.Type: ApplicationFiled: October 29, 2008Publication date: April 29, 2010Inventors: Mitchell A. DeLong, Jill Marie Sturdivant
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Patent number: 7666912Abstract: The present invention relates to compositions, such as bimatoprost, latanoprost and travoprost, and methods to reduce fat in the body of an individual, for example, by topical administration, injection, and/or implantation of such compositions.Type: GrantFiled: March 1, 2007Date of Patent: February 23, 2010Assignee: Massachusetts Eye and Ear InfirmaryInventors: Cynthia L. Grosskreutz, Louis R. Pasquale
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Publication number: 20090291988Abstract: The instant invention relates to compounds of formula I, diagrammed below, wherein R3, E, D and Y are defined in the application, which are useful as reversible inhibitors of monoamine oxidase-B and/or monoamine oxidase-A, and therefore useful to treat or prevent neurological diseases or conditions in mammals, preferably humans.Type: ApplicationFiled: June 14, 2006Publication date: November 26, 2009Inventor: Renata Oballa
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Patent number: 7605288Abstract: Novel compounds useful for inhibiting the 90 kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.Type: GrantFiled: March 26, 2007Date of Patent: October 20, 2009Assignee: University of KansasInventors: Brian Blagg, Gang Shen, Randell C. Clevenger
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Publication number: 20090259058Abstract: The present application provides intermediates for preparing prostaglandin analogues and processes for preparing prostaglandin analogues and intermediates thereof. The intermediates include: A compound of formula (6): R1 represents H, C1-C5-alkyl, or benzyl, in particular isopropyl.Type: ApplicationFiled: April 9, 2009Publication date: October 15, 2009Inventors: Julian P. Henschke, Yuanlian Liu, Yung-Fa Chen, Dechao Meng, Ting Sun
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Publication number: 20090234016Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed.Type: ApplicationFiled: March 31, 2006Publication date: September 17, 2009Applicant: WELLSTAT THERAPEUTICS CORPORATIONInventors: Shalini Sharma, Reid W. von Borstel
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Publication number: 20090163596Abstract: The invention provides a novel polymorphic form I of crystalline bimatoprost, method for preparation thereof and new crystalline intermediates in the preparation. This form I of crystalline bimatoprost is used in purification of crude bimatoprost and in storage of bimatoprost as active pharmaceutical intermediate. Use of the physical form of bimatoprost in the manufacture of a medicament is also disclosed.Type: ApplicationFiled: August 29, 2007Publication date: June 25, 2009Inventors: Arie Gutman, Igor Rukhman, Boris Tishin, Lev Yudovich, Alexander Vilensky, Boris Pertsikov, Gennady Nisnevich
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Publication number: 20090105347Abstract: Thyronamine derivatives and analogs, methods of using such compounds, and pharmaceutical compositions containing them are disclosed.Type: ApplicationFiled: November 30, 2007Publication date: April 23, 2009Applicants: The Regents of the University of California, Oregon Health & Science UniversityInventors: Thomas S. Scanlan, Matthew E. Hart, David K. Grandy, James R. Bunzow, Mononori Miyakawa, Edwin Saavedra Tan, Katherine L. Suchland
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Publication number: 20090076114Abstract: The present invention relates to cis-1,2-substituted stilbene derivatives, or their pharmaceutically acceptable salts, glucosides or solvates, a pharmaceutical composition comprising the compound, and use of said compound for preparation of a drug for treatment and/or prevention of diabetes or improvement of diabetic complications.Type: ApplicationFiled: July 20, 2005Publication date: March 19, 2009Inventors: Zhiyun Kang, Zuze Wu, Zhuangrong Sun, Zhongxiong Tang
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Publication number: 20090069592Abstract: A phenyl tin compound is synthesized by using a derivative having various functional groups and a bromo- or iodo-benzene ring as a labeling material of a radioactive ligand. On the other hand, a novel hydroxytosyl iodobenzene compound having an electron-donating group is obtained by oxidizing iodobenzene having one or more electron-donating groups and reacting it with tosylic acid. Then, a diphenyliodonium salt which is a labeling precursor is synthesized by reacting the resulting compound with various phenyl tin compounds. Finally, a 18F-labeled ligand having various functional groups and a [18F] fluorobenzene ring is synthesized by reacting the resulting diphenyliodonium salt with [18F]F?.Type: ApplicationFiled: November 29, 2006Publication date: March 12, 2009Applicant: National Institute of Radiological SciencesInventors: Kazutoshi Suzuki, Ming-Rong Zhang, Katsushi Kumata
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Publication number: 20090062296Abstract: Nitroderivatives of prostaglandin amides having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension.Type: ApplicationFiled: June 28, 2006Publication date: March 5, 2009Inventors: Francesca Benedini, Valerio Chiroli, Wesley Kwan Mung Chong, Achim Hans-Peter Krauss, Michael Ross Niesman, Ennio Ongini
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Publication number: 20090018204Abstract: A composition including a molecule of the formula: wherein y is 0 or 1, x is 0 or 1 and x and y are not both 1, Y is a radical selected from the group consisting of alkyl, halo, e.g. fluoro, chloro, etc., nitro, amino, thiol, hydroxy, alkyloxy, alkylcarboxy, halo substituted alkyl wherein the alkyl radical comprises from one to six carbon atoms, etc. and n is 0 or an integer of from 1 to 3 and R3 is ?O, —OH or —O(CO)R6 wherein R6 is as defined above or a pharmaceutically acceptable salt thereof. A method including topically applying to a dermis or hair on the dermis an amount of a composition comprising a molecule of the formula: wherein y is 0 or 1, x is 0 or 1 and x and y are not both 1, Y is a radical selected from the group consisting of alkyl, halo, e.g. fluoro, chloro, etc., nitro, amino, thiol, hydroxy, alkyloxy, alkylcarboxy, halo substituted alkyl wherein the alkyl radical comprises from one to six carbon atoms, etc.Type: ApplicationFiled: June 4, 2008Publication date: January 15, 2009Inventor: Michael C. Brinkenhoff
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Publication number: 20080234199Abstract: Triphenylethylene compounds of formula (I) are provided. The compounds are particularly useful for selective estrogen receptor modulation.Type: ApplicationFiled: November 22, 2006Publication date: September 25, 2008Inventor: Subba Reddy Katamreddy
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Patent number: 7371887Abstract: Amphiphilic oligo(p-phenylene vinylene) compounds and methods of use en route to self-assembled composites and device fabrication.Type: GrantFiled: December 6, 2004Date of Patent: May 13, 2008Assignee: Northwestern UniversityInventors: Samuel I. Stupp, James F. Hulvat, Marina Sofos, Keisuke Tajima
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Patent number: 7312368Abstract: A method for the selective reduction of an aromatic compound. The present invention provides a method for pre-venting the reduction of at least one halogen substituted aromatic ring of an aromatic compound, while allowing the reduction of at least one functional group on the aromatic compound. In the present invention at least one hydroxyl group is placed on the at least one halogen substituted aromatic ring to be protected from reduction. The aromatic compound is then reacted with at least one alkali metal in at least one nitrogen containing base and at least one alcohol at a ratio of the alcohol to the nitrogen containing base at which the aromatic ring with the hydroxyl group is protected from reduction, while the desired functional group is reduced.Type: GrantFiled: December 2, 2004Date of Patent: December 25, 2007Assignee: Mallinckrodt Inc.Inventors: Peter Xianqi Wang, Frank W. Moser
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Patent number: 7265245Abstract: The present invention provides new amyloidogenesis inhibiting compounds of formula (I): in which R1 is a —NRaRb group, where Ra and Rb, independently, are a hydrogen atom or a C1-C6 alkyl group; —ORC group, where RC is a hydrogen atom or a C1-C6 alkyl group; a glycosyl; a C1-C6 polyhydroxyalkyl; or a —NH—CH(Rd)—COORe group, where Rd is a side chain of one of the 20 natural alpha-amino acids in either of their two enantiomerically pure forms L or D, and Re is a hydrogen atom or a C1-C6 alkyl group; and R2 is a hydrogen atom, a C1-C6 alkyl group, a glycosyl; a C1-C6 polyhydroxyalkyl; —C(?O)—Rf group, where Rf is a C1-C6 alkyl group; or a —CH2—COO—Rg group, where Rg is a hydrogen atom or a C1-C6 alkyl group; and pharmaceutically acceptable salts thereof, which are useful in the treatment of neurodegenerative diseases, among others.Type: GrantFiled: October 8, 2003Date of Patent: September 4, 2007Assignee: Innovaprotean, S.LInventors: Maria Joao Mascarenhas Saraiva, Maria do Rosario Rodrigues Almeida, José Barluenga Mur, Alfredo Ballesteros Gimeno, Antoni Planas Sauter, Gemma Arsequell Ruiz, Gregorio Valencia Parera
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Patent number: 7253318Abstract: The invention relates to compounds of the formula and their pharmaceutically acceptable salts wherein R1, R2, R3, R4, R5, n, m, and o are as defined in the specification. The compounds are selective monoamine oxidase ? inhibitors and are useful for the treatment and prevention of Alzheimer's disease and senile dementia, as well as other CNS disorders. The invention also relates to processes for preparing such compounds and pharmaceutical compositions containing them.Type: GrantFiled: June 20, 2005Date of Patent: August 7, 2007Assignee: Hoffman-La Roche Inc.Inventors: Synese Jolidon, Rosa Maria Rodriguez-Sarmiento, Andrew William Thomas, Wolfgang Wostl, Rene Wyler
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Patent number: 7223888Abstract: Novel compounds and compositions including those compounds, as well as methods of using and making the compounds are herein described. The compounds are useful in therapeutic applications, including modulation of disease or disease symptoms in a subject (e.g., mammal, human, dog, cat, horse). The compounds are useful as modulators of the mu opioid receptor (MOR) through their binding affinity with that receptor.Type: GrantFiled: October 10, 2003Date of Patent: May 29, 2007Assignee: President and Fellows of Harvard CollegeInventors: Bryce A. Harrison, Tiffany M. Gierasch, Gregory L. Verdine, Zhangjie Shi
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Patent number: 7208630Abstract: Novel compounds useful for inhibiting the 90 kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.Type: GrantFiled: October 27, 2004Date of Patent: April 24, 2007Assignee: University of KansasInventors: Brian Blagg, Gang Shen, Randell C. Clevenger
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Patent number: 7196119Abstract: The present disclosure concerns a new class of selective estrogen receptor modulators (SERMs). The disclosure also includes the identification of a previously unknown membrane associated estrogen receptor. Methods for making and using the disclosed SERMs are disclosed, including pharmaceutical formulations of the disclosed novel compounds in useful compositions.Type: GrantFiled: October 20, 2004Date of Patent: March 27, 2007Assignees: The Regents of the University of California, Oregon Health & Science UniversityInventors: Thomas S. Scanlan, Martin J. Kelly, Jian Qiu, Sandra Tobias, Oline K. Ronnekleiv
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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: 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: 7045660Abstract: This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. The present invention is therefore directed to their pharmacological use for inhibiting TNF and/or cyclic AMP phosphodiesterase, pharmacological compositions comprising the compounds and methods for their preparation.Type: GrantFiled: March 3, 2004Date of Patent: May 16, 2006Assignee: Aventis Pharma LimitedInventors: Garry Fenton, Tahir Nadeem Majid, Malcolm Norman Palfreyman
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Patent number: 7038085Abstract: The present invention relates generally to the enantiomers of para-hydroxy-milnacipran or congeners thereof. Biological assays revealed that racemic para-hydroxy-milnacipran is approximately equipotent in inhibiting serotonin and norepinephrine uptake (IC50=28.6 nM for norepinephrine, IC50=21.7 nM for serotonin). Interestingly, (+)-para-hydroxy-milnacipran is a more potent inhibitor of norepinephrine uptake than serotonin uptake (IC50=10.3 nM for norepinephrine, IC50=22 nM for serotonin). In contrast, (?)-para-hydroxy-milnacipran is a more potent inhibitor of serotonin uptake compared to norepinephrin uptake (IC50=88.5 nM for norepinephrine, IC50=40.3 nM for serotonin). The invention also relates to salts and prodrug forms of the aforementioned compounds. In certain embodiments, the compounds of the present invention and a pharmaceutically acceptable excipient are combined to prepare a formulation for administration to a patient.Type: GrantFiled: October 22, 2003Date of Patent: May 2, 2006Assignee: Collegium Pharmaceutical, Inc.Inventors: Roman V. Rariy, Michael Heffernan, Stephen L. Buchwald, Timothy M. Swager
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Patent number: 6951884Abstract: The invention relates to fluorobenzamide derivatives of the formula wherein R1, R2, R3 R4, R5, R6 and R7 are as defined herein. =, The compounds of the invention are selective monoamine oxidase B inhibitors and therefore they are suitable for the treatment of diseases mediated by monoamine oxidase B, such as Alzheimer's disease or senile dementia.Type: GrantFiled: June 6, 2003Date of Patent: October 4, 2005Assignee: Hoffmann-La Roche Inc.Inventors: Synese Jolidon, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
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Patent number: 6900354Abstract: The invention relates to 3-phenyl-propionamido, 3-phenyl-acrylamido and 3-phenyl-propynamido derivatives, for example, deriviatives of the formula wherein A is selected from R1, R3, R4, R5, R6, R7, R21, R22, R23, R24, and n are as defined herein or pharmaceutically acceptable salts thereof. The invention also relates to processes for preparation of such compounds, compositions containing them, and the use of such derivatives as MAO-B inhibitors. The invention further relates to methods for treating or preventing Alzheimer's disease and senile dementia by administering compounds of the invention.Type: GrantFiled: July 3, 2003Date of Patent: May 31, 2005Assignee: Hoffman-La Roche Inc.Inventors: Synese Jolidon, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Wolfgang Wostl, Rene Wyler
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Publication number: 20040229949Abstract: Novel 3-aryl propionic acid derivatives and analogs, process and intermediate for their manufacture, pharmaceutical preparations containing them and the use of the compounds in clinical conditions associated with insulin resistance.Type: ApplicationFiled: October 2, 2003Publication date: November 18, 2004Inventors: Kjell Andersson, Maria Boije, Johan Gottfries, Tord Inghardt, Lanna Li, Eva-Lotte Lindstedt Alstermark
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Patent number: 6777442Abstract: The present invention relates to compounds of the general formula (I) in which X represents O, S, SO, SO2, CH2, CHF, CF2 or NR8, and Z represents a group of the formula in which A represents O or S, the subscript “a” is 0 or 1, group D represents a straight-chain (C1-C4)-alkylene group, and R36 represents OR37 or NR38R39. It also relates to processes for preparation of such compounds and to their use in medicaments for the treatment of depression, goiter, cancer of the thyroid gland, arteriosclerosis, hypercholesterolaemia, dyslipidaemia, obesity, cardiac insufficiency, pulmonary emphysema, pain, migraine, Alzheimer's disease, osteoporosis, cardiac arrhythmias, hypothyroidism, skin disorders or diabetes.Type: GrantFiled: February 26, 2002Date of Patent: August 17, 2004Assignee: Bayer AktiengesellschaftInventors: Helmut Haning, Michael Woltering, Gunter Schmidt, Christiane Faeste, Hilmar Bischoff, Axel Kretschmer, Verena Vöhringer, Peter Ellinghaus
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Publication number: 20040110754Abstract: The present invention provides novel arylcyclopropylcarboxylic amides and related derivatives having the general Formula I 1Type: ApplicationFiled: November 21, 2003Publication date: June 10, 2004Inventors: Yong-Jin Wu, Li-Qiang Sun, Alexandre L'Heureux
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Publication number: 20040106818Abstract: A reaction of a para-substituted aryl composition with cyclohexanone is facilitated by a metal hydride, such as NaH, KH, LiH, MgH2, CaH2, AlH3, and/or LiAlH4 to make first intermediates useful in producing a drug commonly known as Venlafaxine. Alternatively, lithium diisopropylamide (diisopropylamino lithium) may be used in place of the metal hydride. The first intermediates may be further reacted to form second intermediates in a reduction that is facilitated by Rainey nickel or a metal hydride. These reaction processes may each occur in an organic solvent, which delivers highly pure reaction products in high yield.Type: ApplicationFiled: August 11, 2003Publication date: June 3, 2004Inventors: Lan Zhiyin, Shi Kaiyun, Mo Qizhuang, Li Yulin
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Patent number: 6703421Abstract: A method for prevention or treating myocarditis, dilated cardiomyopathy and heart failure comprising administering to a patient in need of such treatment a NF-&kgr;B inhibitor in a therapeutically effective amount, wherein said NF-&kgr;B inhibitor is a benzoquinone derivative represented by the following formula (I): wherein R1, R2 and R3 are each independently a hydrogen atom, an alkyl group having 1 to 5 carbons or an alkoxy group having 1 to 5 carbons; R4 is a hydrogen atom, a hydroxymethyl group, an alkyl group, or a carboxyl group which is optionally esterified or amidated; Z is and n is an integer from 0 to 6, or its hydroquinone form, or a pharmaceutically acceptable salt thereof, is provided.Type: GrantFiled: May 17, 2001Date of Patent: March 9, 2004Assignee: Daiichi Suntory Pharma Co., Ltd.Inventors: Yoichi Nunokawa, Akira Matsumori
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Patent number: 6693208Abstract: Amino acid derivative as carrier compounds and compositions which are useful in the delivery of active agents are provided. The active agents can be a peptide, mucopolysaccharide, carbohydrate, or lipid. Methods of administration, including oral administration, and preparation are provided as well.Type: GrantFiled: July 15, 2002Date of Patent: February 17, 2004Assignee: Emisphere Technologies, Inc.Inventors: David Gscheidner, Andrea Leone-Bay, Eric Wang, John J. Freeman, Doris C. O'Toole, Lynn Shields
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Publication number: 20030225302Abstract: Aromatic amides, their preparation process and their use as pesticides 1Type: ApplicationFiled: May 2, 2003Publication date: December 4, 2003Inventors: Jacques Demassey, Robert Peek, Antonio Ugolini, John Weston
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Publication number: 20030207894Abstract: Compounds of formula I: 1Type: ApplicationFiled: January 29, 2003Publication date: November 6, 2003Inventors: George Theodoridis, Edward Barron, Daniel H. Cohen, Ellen M. Crawford, Thomas G. Cullen, Hongyan Qi, Elizabeth Rowley, Syed F. Ali, Walter H. Yeager, Christina B. Duggan
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Publication number: 20030199589Abstract: Bis(Fluorophenyl)alkylamides have been chemically synthesized which possess beneficial pharmacological properties (e.g., anticonvulsant activity) useful for the treatment of neurological diseases or disorders, such as, for example, epilepsy, convulsions, and seizure disorders. The preferred compounds of the invention also cause little sedation and have high therapeutic and protective indices in animal models of epilepsy. These compounds further possess long pharmacologic half-lives, which, in practical clinical therapeutic application, should translate into once-a-day dosing, of great benefit to patients suffering from these diseases and/or disorders. These compounds may also be of further clinical utility in the treatment of other diseases and disorders of the central and peripheral nervous systems, or diseases or disorders affected by them, including, but not limited to, spasticity, skeletal muscle spasms and pain, restless leg syndrome, anxiety and stress, and bipolar disorder.Type: ApplicationFiled: May 2, 2003Publication date: October 23, 2003Applicant: NPS Pharmaceuticals, Inc.Inventors: Manuel F. Balandrin, Bradford C. VanWagenen, Linda D. Artman, Alan L. Mueller, Daryl Smith, Scott T. Moe
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Publication number: 20030181748Abstract: The invention relates to a method for carrying out CC-coupling reactions, in particular a Heck and Suzuki reaction, in the presence of supported palladium as the catalyst and a base in a monophase or multiphase solvent mixture. According to said method, palladium detaches itself from the support in a characteristic manner, is redeposited after the reaction and the quantity of palladium not deposited after the reaction is significantly lower than 5000 ppm, in relation to the palladium used.Type: ApplicationFiled: March 6, 2003Publication date: September 25, 2003Inventors: J?uuml;rgen Krauter, J?ouml;rg Pietsch, Peter Panster, Klaus Khler, Roland Heidenreich
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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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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: 6586475Abstract: A compound of the formula: wherein Ar is an aromatic group; X and Y are a bivalent group selected from —O—, —S—, —CO—, —SO2—, —NR8—, —CONR8—, SO2NR8 and —COO— (wherein R8 is H, a hydrocarbon group or acyl), or a bivalent C1-6 aliphatic hydrocarbon group which may contain one or two above bivalent groups; R1 and R2 are H or C1-6 alkyl, or R1 and R2 may form, together with the adjacent nitrogen atom, a nitrogen-containing heterocyclic ring; and ring A is a monocyclic aromatic ring, or a salt thereof or a prodrug thereof exhibits an excellent inhibitory activity of the production and/or the secretion of amyloid-&bgr; protein.Type: GrantFiled: June 5, 2001Date of Patent: July 1, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Kaneyoshi Kato, Jun Terauchi, Hiroaki Fukumoto, Mitsuru Kakihana
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Patent number: 6576632Abstract: The present invention relates to compounds of formula I and to pharmaceutically acceptable salts, hydrates and prodrugs thereof, wherein R1, R2, R3, R4, R5, R10, R11, b, m, n, p and v are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and methods of treating hyperproliferative disorders in mammals by administering the above compounds.Type: GrantFiled: April 13, 2000Date of Patent: June 10, 2003Assignee: Pfizer IncInventors: Steven W. Goldstein, Kelly P. Longo, James F. Blake, Mohamed M. A. Awad, Kenneth P. Raiche, Kevin W. Kramer
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Patent number: 6521663Abstract: Phenyl acetamide compounds are described, including compounds of Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R3-R6, R11, B, Y and W are set forth in the specification. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as thrombin and factor Xa. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.Type: GrantFiled: October 5, 2001Date of Patent: February 18, 2003Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Wenxi Pan, Tianbao Lu, Thomas P. Markotan, Bruce E. Tomczuk
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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: 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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Publication number: 20020095042Abstract: A process for preparing 4-bromomethylbiphenyl derivatives substituted in the 2′ position of general formula (I) 1Type: ApplicationFiled: September 4, 2001Publication date: July 18, 2002Inventors: Heinrich Schneider, Margarete Schneider
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Patent number: 6403649Abstract: The present invention provides cydopentane heptanoic acid, 2-cycloalkyl or arylalkyl compounds, which may be substituted in the 1-position with amino, amido, ether or ester groups, e.g., a 1-OH cydopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) compound. The cydopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma. Moreover, the cydopentane heptanoic, 2-(cycloalkyl or arylalkyl) compounds of this invention are smooth muscle relaxants with broad application in systemic hypertensive and pulmonary diseases; smooth muscle relaxants with application in gastrointestinal disease, reproduction, fertility, incontinence, shock, etc.Type: GrantFiled: March 6, 2000Date of Patent: June 11, 2002Assignee: Allergan Sales, Inc.Inventors: David F. Woodward, Steven W. Andrews, Robert M. Burk, Michael E. Garst
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Patent number: 6395787Abstract: Compounds of Formula 1, where the symbols are as defined in the specification, are useful as ocular hypotensive agents but do not exert their activity through the FP prostaglandin receptor. In particular the compound PGF2&agr; 1-ethanolamide, having the formula was discovered to be present in mammalian tissue as a naturally occurring substance, was synthesized in a substantially pure form and was found to be effective for lowering intraocular pressure in the mammalian eye, but not acting through the FP receptor through which many ocular hypotensive prostaglandins act.Type: GrantFiled: February 8, 2000Date of Patent: May 28, 2002Assignee: Allergan Sales, Inc.Inventors: David F. Woodward, Helen H. Usansky, Steven W. Andrews, Robert M. Burk, June Chen, Achim H-P. Krauss, Cherukury Madhu
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Patent number: RE40259Abstract: The present invention relates to novel and known alpha-aminoamide compounds, to a process for their preparation, to pharmaceutical composition containing them and to their use as therapeutic agents. In particular, the compounds of the present invention are endowed with analgesic properties and are particularly useful for the treatment and alleviation of chronic and neuropathic pain.Type: GrantFiled: December 12, 1998Date of Patent: April 22, 2008Assignee: Newron Pharmaceuticals, S.p.A.Inventors: Paolo Pevarello, Mario Varasi, Patricia Salvati, Claes Post
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Patent number: RE38506Abstract: The present invention provides the compound having the structure: wherein each of R1 and R2 are independently the same as or different from each other; when R1 and R2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiozoleamino group; when R1 and R2 are different, R1=R3—N—R4, wherein each of R3 and R4 are independently the same as or different from each other and are a hydrogen atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranched alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group, or R3 and R4 bond together to form a piperidine group and R2 is a hydroxylamino, hydroxyl, amino, alkylamino, dialkylamino or alkyloxy group; and n is an integer from about 4 to about 8. The present invention also provides a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells.Type: GrantFiled: November 2, 2001Date of Patent: April 20, 2004Assignees: Sloan-Kettering Institute for Cancer Research, The Trustees of Columbia University in the City of New YorkInventors: Ronald Breslow, Paul A. Marks, Richard A. Rifkind, Branko Jursic