Bicyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/362)
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Patent number: 7595343Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: GrantFiled: September 12, 2002Date of Patent: September 29, 2009Assignee: MethylGene, Inc.Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg, Oscar Moradei, Silvana Leit, Stephane Raeppel, Sylvie Frechette, Giliane Bouchain
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Patent number: 7595327Abstract: This invention provides compounds of Formula I, having the structure: that are useful in treating diseases or disorders mediated by TNF-?, such as arthritis (rheumatoid arthritis (RA), juvenile RA, psoriatic arthritis, osteoarthritis etc), tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection, ankylosing spondylitis, psoriasis, sepsis, multiple sclerosis, Crohn's disease, degenerative cartilage loss, asthma, idiopathic pulmonary fibrosis, vasculitis, systemic lupus erythematosus, irritable bowel syndrome, acute coronary syndrome, hepatitis C, cachexia, COPD, stroke or type 2 diabetes, and for alleviation of symptoms thereof. The invention further provides methods for use of the compounds.Type: GrantFiled: March 16, 2006Date of Patent: September 29, 2009Assignee: WyethInventors: Jeremy I. Levin, Zhong Li, George Diamantidis, Frank E. Lovering, Weiheng Wang, Jeffrey S. Condon, Yang-I Lin, Jerauld S. Skotnicki, Kaapjoo Park
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Patent number: 7566787Abstract: Cyclin D1 ablative agents and methods of using these agents in the treatment of cancers, and particularly breast cancer. Also provided are methods of treating cancer, the method comprising administering a therapeutically effective amount of one of the cyclin D1 ablative agents described herein to a subject in need of such treatment. Also provided are methods of treating cancers comprising using the cyclin D1 ablative agents described herein in combination therapies with existing chemotherapeutic agents.Type: GrantFiled: December 22, 2005Date of Patent: July 28, 2009Assignee: The Ohio State UniversityInventor: Ching-Shih Chen
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Patent number: 7553848Abstract: bis-Bicyclic amides and derivatives thereof and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration,Type: GrantFiled: January 21, 2005Date of Patent: June 30, 2009Assignee: Amgen Inc.Inventors: Christopher Hulme, Mqhele Vellah Ncube, Mark H. Norman, Vassil I. Ognyanov, Liping H. Pettus, Jiawang Zhu
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Publication number: 20090118323Abstract: The present invention provides antitumor compounds of the formula (I); and antitumor methods.Type: ApplicationFiled: September 11, 2007Publication date: May 7, 2009Inventors: Mary Margaret Mader, Luisa Maria Martin-Cabrejas, Michael Enrico Richett
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Publication number: 20090111183Abstract: This invention relates to a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. The ligands comprise a class of ketones.Type: ApplicationFiled: October 9, 2007Publication date: April 30, 2009Inventors: Colin M. Tice, Enrique L. Michelotti, Robert E. Hormann
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Patent number: 7491748Abstract: A carboxylic acid derivative of formula (I): wherein R1 is —COOH, —COOR6, etc.; A is a single bond, alkylene, etc.; R2 is alkyl, alkoxy, etc.; B is a carbocyclic ring or a heterocyclic ring; Q is alkylnene-Cyc2, etc.; D is a linking chain; and R3 is alkyl, a carbocyclic ring or a heterocyclic ring, or a non-toxic salt thereof. The compound of formula (I) binds to PGE2 receptor, especially subtypes EP3 and/or EP4 and show the antagonizing activity, are useful for the prevention and/or treatment of diseases induced pain, itch, urticaria, allergy, urinary frequency, urinary disturbance, Alzheimer's disease, cancer, dysmenorrhea, endometriosis, etc.Type: GrantFiled: August 8, 2002Date of Patent: February 17, 2009Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kousuke Tani, Masaki Asada, Kaoru Kobayashi, Masami Narita, Mikio Ogawa
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Publication number: 20090042973Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: ApplicationFiled: July 2, 2008Publication date: February 12, 2009Inventors: Michael R. Hale, Christopher T. Baker, Timothy A. Stammers, Ronald George Sherrill, Andrew Spaltenstein, Eric Steven Furfine, Francois Maltais, Clarence Webster Andrews, III, John Franklin Miller, Vicente Samano
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Publication number: 20090030038Abstract: The present invention relates to new compounds of formula I. (I) wherein R1 to R12, X, Q and n are as defined as in formula I, or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.Type: ApplicationFiled: May 22, 2006Publication date: January 29, 2009Applicant: ASTRAZENECA ABInventors: Chester Chu, Andrew Lister, Gunnar Nordvall, Carl Petersson, Didier Rotticci, Daniel Sohn, Stefan Von Berg
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Patent number: 7476690Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein Ar, Y, R1 and q are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness, promotion of wakefulness, treatment of Parkinson's disease, cerebral ischemia, stroke, sleep apneas, eating disorders, stimulation of appetite and weight gain, treatment of attention deficit hyperactivity disorder (“ADHD”), enhancing function in disorders associated with hypofunctionality of the cerebral cortex, including, but not limited to, depression, schizophrenia, fatigue, in particular, fatigue associated with neurologic disease, such as multiple sclerosis, chronic fatigue syndrome, and improvement of cognitive dysfunction.Type: GrantFiled: June 21, 2006Date of Patent: January 13, 2009Assignee: Cephalon FranceInventors: Brigitte Lesur, Christophe Yue, Sophie Chasset, Olivier Renault
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Patent number: 7470722Abstract: Disclosed herein are carbonyl compounds of Formula I as described herein. Methods and compositions are disclosed for treating disease states including, but not limited to cancers, autoimmune diseases, tissue damage, central nervous system disorders, neurodegenerative disorders, fibrosis, bone disorders, polyglutamine-repeat disorders, anemias, thalassemias, inflammatory conditions, cardiovascular conditions, and disorders in which angiogenesis play a role in pathogenesis, using the compounds of the invention. In addition, methods of modulating the activity of histone deacetylase (HDAC) are also disclosed.Type: GrantFiled: June 9, 2005Date of Patent: December 30, 2008Assignee: Kalypsys, Inc.Inventors: James William Malecha, Stewart Alwyn Noble, Christian Andreus Hassig, Paul L. Wash, Brandon M. Wiley, Charles Maxwell Lawrence, Timothy Z. Hoffman
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Publication number: 20080300243Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: February 24, 2006Publication date: December 4, 2008Inventors: Michael G. Kelly, John Kincaid, Matthew Duncton, Kiran Sahasrabudhe, Satyanarayana Janagani, Ravindra B. Upasani, Guoxian Wu, YunFeng Fang, Zhi-Liang Wei, Carl Kaub, Jianhua He
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Publication number: 20080226983Abstract: The invention provides a non-aqueous electrolyte including: at least one kind selected from the compounds represented by Chemical formula 1: wherein R1 and R2 each represent a hydrogen group, a hydrocarbon group or an alkylsilyl group, or any of these groups part or all of the hydrogen atoms of which is/are substituted with a halogen, R1 and R2 may be bonded to each other, and n is an integer of 1 or larger.Type: ApplicationFiled: March 14, 2008Publication date: September 18, 2008Applicant: SONY CORPORATIONInventors: Toru Odani, Tadahiko Kubota
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Publication number: 20080125465Abstract: This invention relates to a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. The ligands comprise a class of ketones.Type: ApplicationFiled: August 17, 2007Publication date: May 29, 2008Applicant: Intrexon CorporationInventors: Colin M. Tice, Enrique L. Michelotti, Robert E. Hormann
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Publication number: 20080119511Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables and A are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.Type: ApplicationFiled: September 6, 2007Publication date: May 22, 2008Applicant: Amgen Inc.Inventors: Sean P. Brown, Paul Dransfield, Jonathan B. Houze, Jinqian Liu, Jiwen Liu, Zhihua Ma, Julio C. Medina, Vatee Pattaropong, Michael J. Schmitt, Rajiv Sharma, Yingcai Wang
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Patent number: 7307088Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: July 8, 2003Date of Patent: December 11, 2007Assignee: Amgen Inc.Inventors: Qi Huang, Guoqing Chen, Aiwen Li, Babak Riahi, Andrew Tasker, Kevin Yang, Chester Chenguang Yuan
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Patent number: 7265130Abstract: The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): wherein R1 is lower alkyl, cycloalkyl or the like, R2 is hydrogen, lower alkyl or the like, n is 1 or 2, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, Y is CONR7, CSNR7, NR7CO, NR7CS or the like, Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R7 is hydrogen or lower alkyl, prodrug, pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: December 30, 2003Date of Patent: September 4, 2007Assignee: Shionogi & Co., Ltd.Inventors: Yasuyuki Kawanishi, Hideyuki Takenaka, Kohji Hanasaki, Tetsuo Okada
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Patent number: 7220523Abstract: Improved organophotoreceptor comprises an electrically conductive substrate and a photoconductive element on the electrically conductive substrate, the photoconductive element comprising: (a) a charge transport material having the formula where R1, R2, R3, R4, R5, and R6 comprise, each independently, H, an alkyl group, an alkenyl group, an alkynyl group, an aromatic group, or a heterocyclic group; X1 and X2 are, each independently, a —(CH2)n— group, where n is an integer between 1 and 10, inclusive; X3 is linking group; and Q1, Q2, Q3, Q4, Q5, and Q6 are, each independently, O, S, NR, NC(?O)R? where R and R? are, each independently, H, an alkyl group, an alkenyl group, an alkynyl group, a heterocyclic group, or an aromatic group; and (b) a charge generating compound. Corresponding electrophotographic apparatuses and imaging methods are described.Type: GrantFiled: June 10, 2004Date of Patent: May 22, 2007Assignee: Samsung Electronics Co., Ltd.Inventors: Zbigniew Tokarski, Nusrallah Jubran, Ramunas Lygaitis, Juozas V. Grazulevicius, Edmundas Montrimas, Jonas Sidaravicius
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Patent number: 7119049Abstract: This invention relates to novel oxathiinecarboxamides of the formula (I) in which R, R1 and m are as defined in the disclosure, to a plurality of processes for preparing these substances and to their use for controlling unwanted micro-organisms.Type: GrantFiled: May 15, 2003Date of Patent: October 10, 2006Assignee: Bayer Cropscience AGInventors: Heiko Rieck, Ralf Dunkel, Hans-Ludwig Elbe, Ulrike Wachendorff-Neumann, Astrid Mauler-Machnik, Karl-Heinz Kuck
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Patent number: 7045514Abstract: Provided herein is a compound having the formula (I): Wherein said compounds are useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT1B and 5HT1D antagonists.Type: GrantFiled: July 12, 2004Date of Patent: May 16, 2006Assignee: AstraZeneca ABInventors: Edward Pierson, Daniel Sohn, Markus Haeberlein, Timothy Davenport, Marc Chapdelaine, Carey Horchler, John P. McCauley
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Patent number: 7033401Abstract: The 3-aminophenol derivatives of formula (I), or the physiologically compatible, water-soluble salts thereof: wherein R1 represents a group of formula (II) or a group of formula (III): are useful as couplers in hair colorants. Agents for dyeing keratin fibers, especially hair, based on a developer-coupler combination containing these compounds and methods of dyeing using these agents are described.Type: GrantFiled: January 8, 2003Date of Patent: April 25, 2006Assignee: Wella AGInventors: Gisela Umbricht, Franco Jose Rosato, Hans-Juergen Braun
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Patent number: 7022732Abstract: This invention relates to a medicament containing as an active ingredient, a novel propanolamine having a 1,4-benzodioxane ring or a pharmaceutically acceptable salt thereof: The present compound is represented by the above formula wherein R1-3 may be the same or different and each represents a hydrogen atom, a halogen atom, a hydroxy group, a (C1–C6)alkyl group, a (C1–C6)alkoxy group, a (C1–C6)alkylsulfonamido group, or a phenyl group; R4-5 each represents a hydrogen atom or a (C1–C6)alkyl group; and A represents any of a benzene ring, a pyridine ring and a pyrimidine ring. This compound is useful as a prophylactic or therapeutic agent for diabetes, obesity, hyperlipemia, depression, a respiratory disease, or a gastrointestinal disease.Type: GrantFiled: September 13, 2001Date of Patent: April 4, 2006Assignees: Nisshin Pharma Inc., Kyorin Pharmaceutical Co., Ltd.Inventors: Masahiro Ueno, Koji Kawamura, Makoto Yanai, Toshihiro Takahashi, Nobuhiro Kinoshita, Koichi Katsuyama, Satoko Fuchizawa, Shigeru Hiramoto
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Patent number: 7019003Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: March 1, 2002Date of Patent: March 28, 2006Assignee: Smithkline Beecham CorporationInventors: Jia-Ning Xiang, Siegfried B. Christensen, IV, Jinhwa Lee, Daniel J. Mercer
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Patent number: 7015339Abstract: The invention provides compositions and methods for isolating phenolic compounds, particularly isoflavones, from aqueous extracts of plant materials that contain such compounds. The process comprising: (a) providing an aqueous plant extract at a first pH less than 10, the aqueous plant extract comprising a plurality of phenolic compounds; (b) extracting the aqueous plant extract with a first organic solvent to yield a first organic extract; (c) extracting the first organic extract with an aqueous phase of pH greater than 10 to yield a phenol rich aqueous phase; (d) adjusting the pH of the phenol rich aqueous phase to a pH of less than 9; and (e) isolating the phenolic compounds from the phenol rich aqueous phase.Type: GrantFiled: July 23, 2002Date of Patent: March 21, 2006Assignee: Cargill, IncorporatedInventors: Anil Bhagwan Khare, Brent Howard Hilbert
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Patent number: 6916844Abstract: The present invention provides hydroxy pyranone derivatives and a method for preparing the hydroxy pyranone derivatives. The hydroxy pyranone derivatives of the present invention are significantly effective in promoting the biosynthesis of collagen and in inhibiting the activity of collagenase, i.e. an enzyme for decomposing collagen, to have anti-wrinkle efficacy, and can be incorporated into medicines or external applications for lessening skin-wrinkles.Type: GrantFiled: May 9, 2003Date of Patent: July 12, 2005Assignee: Amorepacific CorporationInventors: Ho Sik Roh, Su Nam Kim, Bae Hwan Kim, Hae Kwang Lee, Duck Hee Kim, Ih Seop Chang, Ok Sub Lee
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Patent number: 6878700Abstract: The present invention relates to novel cinnamide compounds that are useful for treating inflammatory and immunune diseases, to pharmaceutical compositions containing these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.Type: GrantFiled: March 31, 2000Date of Patent: April 12, 2005Assignee: Abbott LaboratoriesInventors: James Link, Gang Liu, ZhongHua Pei, Tom von Geldern, Martin Winn, Zhili Xin, Steven A. Boyd, Gui-Dong Zhu, Jennifer C. Freeman, Indrani W. Gunawardana, Michael A. Staeger, Hwan-Soo Jae, John K. Lynch, Sheldon Wang
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Patent number: 6867203Abstract: The present invention relates to novel cinnamide compounds that are useful for treating inflammatory and immune diseases and cerebral vasospasm, to pharmaceutical compositions containing these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.Type: GrantFiled: December 1, 2003Date of Patent: March 15, 2005Assignee: Abbott LaboratoriesInventor: Indrani W. Gunawardana
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Patent number: 6828446Abstract: The present invention is directed to selective LXR modulators, small molecule compounds corresponding to Formula I and is further directed to a process of treating a condition in a mammal that is modulated by LXR using a therapeutically effective dose of a compound of Formula I.Type: GrantFiled: December 23, 2002Date of Patent: December 7, 2004Assignee: Pharmacia CorporationInventors: Nizal S. Chandrakumar, Christopher R. Dalton, James W. Malecha, Michael B. Tollefson, Jennifer Ann Van Camp, Phillip B. Cox
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Publication number: 20040235921Abstract: This invention relates to a medicament containing as an active ingredient, a novel propanolamine having a 1,4-benzodioxane ring or a pharmaceutically acceptable salt thereof: 1Type: ApplicationFiled: April 21, 2004Publication date: November 25, 2004Inventors: Masahiro Ueno, Koji Kawamura, Makoto Yanai, Toshihiro Takahashi, Nobuhiro Kinoshita, Koichi Katsuyama, Satoko Fuchizawa, Shigeru Hiramoto
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Patent number: 6812225Abstract: Provided herein is a compound having the formula (I): Wherein said compounds are useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT1B and 5HT1D antagonists.Type: GrantFiled: January 16, 2002Date of Patent: November 2, 2004Assignee: AstraZeneca ABInventors: Edward Pierson, Daniel Sohn, Markus Haeberlein, Timothy Davenport, Marc Chapdelaine, Carey Horchler, John P. McCauley
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Patent number: 6784299Abstract: This invention relates to a series of substituted aromatic ethers of the formula I wherein ring A and X and Y are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.Type: GrantFiled: April 16, 2003Date of Patent: August 31, 2004Assignee: Pfizer Inc.Inventor: John A. Lowe, III
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Publication number: 20040110967Abstract: Plastic additives which are useful as nucleating agents and which are especially useful for improving the optical properties of polymeric materials are provided. More particularly, this invention relates to certain alkyl (or alkoxy) substituted fluoro-benzylidene sorbitol acetals and polymer compositions thereof which may be utilized within, as merely examples, food or cosmetic containers and packaging. These inventive fluorinated and alkylated benzylidene sorbitol acetals are also useful as gelling agents for water and organic solvents, particularly those used in the preparation of antiperspirant gel sticks.Type: ApplicationFiled: November 19, 2003Publication date: June 10, 2004Inventors: John D. Anderson, Nathan A. Mehl
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Patent number: 6734182Abstract: This invention is directed to novel aryl sulfonamide and sulfamide compounds which bind selectively to and inhibit the activity of the human Y5 receptor. This invention is also related to uses of these compounds for the treatment of feeding disorders such as obesity, anorexia nervosa, bulimia nervosa, and abnormal conditions such as sexual/reproductive disorders, depression, epileptic seizure, hypertension, cerebral hemorrhage, congestive heart failure or sleep disturbances and for the treatment of any disease in which antagonism of a Y5 receptor may be useful.Type: GrantFiled: April 2, 2002Date of Patent: May 11, 2004Assignee: Synaptic Pharmaceutical CorporationInventors: Imadul Islam, Daljit S. Dhanoa, John M. Finn, Ping Du, Charles Gluchowski, Yoon T. Jeon
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Patent number: 6710089Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-fused-phenyl-N-benzyl aminoalcohols.Type: GrantFiled: May 23, 2002Date of Patent: March 23, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20040054197Abstract: The present invention provides a compound represented by general formula (I): 1Type: ApplicationFiled: July 25, 2003Publication date: March 18, 2004Inventors: Arata Yanagisawa, Shin-ichiro Mohri, Masashi Yanase
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Publication number: 20040044226Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynacomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.Type: ApplicationFiled: April 15, 2003Publication date: March 4, 2004Inventors: Frank P. DiNinno, Seongkon Kim, Jane Y. Wu
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Patent number: 6699900Abstract: Hydrophilic and lipophilic silibinin pro-forms and pharmaceutical compositions thereof, and methods of using compositions of silibinin pro-forms for topical or oral administration for treatment of disorders of cell proliferation, oxidative stress, sebaceous gland activity, and cardiovascular activity.Type: GrantFiled: April 5, 2002Date of Patent: March 2, 2004Inventor: Jan E. Zielinski
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Publication number: 20030236299Abstract: The present invention provides hydroxy pyranone derivatives and a method for preparing the hydroxy pyranone derivatives. The hydroxy pyranone derivatives of the present invention are significantly effective in promoting the biosynthesis of collagen and in inhibiting the activity of collagenase, i.e. an enzyme for decomposing collagen, to have anti-wrinkle efficacy, and can be incorporated into medicines or external applications for lessening skin-wrinkles.Type: ApplicationFiled: May 9, 2003Publication date: December 25, 2003Inventors: Ho Sik Roh, Su Nam Kim, Bae Hwan Kim, Hae Kwang Lee, Duck Hee Kim, Ih Seop Chang, Ok Sub Lee
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Patent number: 6635437Abstract: Novel heterocyclic compounds which generate chemiluminescence on reaction with a phosphatase enzyme are provided as well as a process for their preparation and intermediates useful therein. The compounds comprise a nitrogen, oxygen or sulfur-containing heterocyclic ring system bearing an exocyclic carbon—carbon double bond. The double bond is further substituted at the distal carbon with a phosphate group and an oxygen or sulfur atom-containing group. Novel compositions further comprising a cationic aromatic compound (CAC) in addition to the heterocyclic phosphate compound are provided. The addition of the CAC in the composition greatly increases the production of chemiluminescence and provides improved detection sensitivity. Compositions further comprising an anionic surfactant and a non-ionic surfactant provide additional improvements in detection sensitivity.Type: GrantFiled: January 22, 2002Date of Patent: October 21, 2003Assignee: Lumigen, Inc.Inventors: Hashem Akhavan-Tafti, Zahra Arghavani, Renuka DeSilva
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Publication number: 20030130342Abstract: This invention relates to certain bicyclic compounds having a nucleus formed of two fused six membered rings, for example, benzopyran, isoquinoline, isoquinolone, tetrahydronaphthalene, dihydronaphthalene, or tetralone, substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.Type: ApplicationFiled: September 9, 2002Publication date: July 10, 2003Inventors: Matthew J. Fisher, Anne Marie Happ, Joseph A. Jakubowski, Michael Dean Kinnick, Allen D. Kline, Michael John Martinelli, John Michael Morin, Michael Paal, Gerd Ruhter, Kenneth James Ruterbories, Daniel J. Sall, Theo Schotten, Marshall A. Skelton, Wolfgang Stenzel, Robert Theodore Vasileff
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Publication number: 20030100772Abstract: The present invention relates to oxygen-containing heterocyclic compounds represented by the following formula (I): 1Type: ApplicationFiled: August 28, 2002Publication date: May 29, 2003Inventors: Etsuo Ohshima, Koji Yanagawa, Haruhiko Manabe, Ichiro Miki, Yoshiaki Masuda
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Patent number: 6555695Abstract: The present invention relates to an improved process for the preparation of ethyl 2,3-dihydrobenzo[1,4]dioxin-2-carboxylate. More particularly the present invention provides a process for the preparation of ethyl 2,3-dihydrobenzo[1,4]dioxin-2-carboxylate in hydrocarbon solvent in the presence of a base and catalytic amount of a phase transfer catalyst.Type: GrantFiled: February 14, 2002Date of Patent: April 29, 2003Assignee: Council of Scientific & Industrial ResearchInventors: Malladi Pardhasaradhi, Gullapalli Kumaraswamy, Arun Kanti Das, Nivedita Jena, Chembumkulam Kamalakshyamma Snehalatha Nair
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Patent number: 6555028Abstract: Described are polymeric matrix compatibilized naphthopyran compounds, examples of which are certain 2H-naphtho[1,2-b]pyrans, 3H-naphtho[2,1-b]pyrans and indeno[2,1-f]naphtho[1,2-b]pyrans each having at least one substituent containing terminal and/or pendant groups selected from hydroxyl, carboxyl, sulfo, sulfono, (meth)acryloxy, 2-(methacryloxy)ethylcarbamyl, epoxy or a mixture thereof. Specific substituents are also present on the naphtho, indeno and/or pyrano portions of the compounds. These compounds may be represented by the following graphic formulae: Also described are various substrates that contain or that are coated with such compounds. Optically clear articles such as contact lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, are also described.Type: GrantFiled: April 6, 2001Date of Patent: April 29, 2003Assignee: Transitions Optical, Inc.Inventors: Robert W. Walters, Barry Van Gemert
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Publication number: 20030069302Abstract: Hydrophilic and lipophilic silibinin pro-forms and pharmaceutical compositions thereof, and methods of using compositions of silibinin pro-forms for topical or oral administration for treatment of disorders of cell proliferation, oxidative stress, sebaceous gland activity, and cardiovascular activity.Type: ApplicationFiled: April 5, 2002Publication date: April 10, 2003Inventor: Jan E. Zielinski
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Publication number: 20020193424Abstract: Silibinin derivatives useful in investigation of cancer control and prophylaxis and in the treatment and prophylaxis of cancers in humans.Type: ApplicationFiled: May 24, 2002Publication date: December 19, 2002Inventor: Thomas J. Slaga
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Patent number: 6469028Abstract: Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity.Type: GrantFiled: March 28, 2001Date of Patent: October 22, 2002Assignee: Allergan, Inc.Inventors: Elliott S. Klein, Alan T. Johnson, Andrew M. Standeven, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Sunil Nagpal, Vidyasagar Vuligonda, Min Teng, Roshantha A. Chandraratna
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Patent number: 6448260Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: July 10, 2001Date of Patent: September 10, 2002Assignee: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
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Patent number: 6448295Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-fused-phenyl-N-benzyl aminoalcohols.Type: GrantFiled: November 14, 2001Date of Patent: September 10, 2002Assignee: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: RE39197Abstract: The present invention relates to novel cinnamide compounds that are useful for treating inflammatory and immune diseases, to pharmaceutical compositions comprising these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.Type: GrantFiled: August 29, 2002Date of Patent: July 18, 2006Assignee: Abbott LaboratoriesInventors: James T. Link, Gang Liu, Zhonghua Pei, Tom von Geldern, Martin Winn, Zhili Xin
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Patent number: RE39593Abstract: 1-phenyl-3-dimethylaminopropane compounds corresponding to the formula I a method of preparing them, and the use of these substances as analgesic active ingredients in pharmaceutical compositions.Type: GrantFiled: June 17, 2003Date of Patent: April 24, 2007Assignee: Gruenenthal GmbHInventors: Helmut Buschmann, Wolfgang Strassburger, Elmar Friderichs