Plural Ring Oxygens In The Tricyclo Ring System Patents (Class 546/90)
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Publication number: 20110301189Abstract: A stable pharmaceutical compositions of Rapamycin Esters, in particular Rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid that is free of antioxidants and a process of preparing the same.Type: ApplicationFiled: June 2, 2011Publication date: December 8, 2011Applicant: FRESENIUS KABI ONCOLOGY LTD.Inventors: Dhiraj Khattar, Rajesh Khanna, Poonam Singla, Abhilasha Yadav, Vinay Gupta, Rajesh Kini, Sushil Kumar Dubey
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Publication number: 20110294844Abstract: 9-aminonoscapine, prodrugs thereof, and pharmaceutically acceptable salts thereof, are disclosed. Pharmaceutical compositions including 9-aminonoscapine, and methods of preparation and use thereof are disclosed. 9-aminonoscapine is a noscapine analog that can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, by binding tubulin and inducing apoptosis selectively in tumor cells (ovarian and T-cell lymphoma) resistant to paclitaxel, vinblastine and teniposide. 9-aminonoscapine can perturb the progression of cell cycle by mitotic arrest, followed by apoptotic cell death associated with increased caspase-3 activation and appearance of TUNEL-positive cells. Thus, 9-aminonoscapine is a novel therapeutic agents for a variety of cancers, including ovarian and T-cell lymphoma cancers, even those that have become drug-resistant to currently available chemotherapeutic drugs.Type: ApplicationFiled: September 4, 2009Publication date: December 1, 2011Applicant: EMORY UNIVERSITYInventors: Harish C. Joshi, Ritu Aneja, Surya N. Vangapandu
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Publication number: 20110160198Abstract: The present invention is directed to substituted azoanthracene derivatives or pharmaceutically acceptable salts thereof that modulate the human GLP-1 receptor and that may be useful in the treatment of diseases, disorders, or conditions in which modulation of the human GLP-1 receptor is beneficial, such as diabetes mellitus type 2. The invention is also directed to pharmaceutical compositions comprising these compounds and to the use of these compounds and compositions in the treatment of such diseases, disorders, or conditions in which modulation of the human GLP-1 receptor is beneficial.Type: ApplicationFiled: June 29, 2010Publication date: June 30, 2011Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Adnan M.M. Mjalli, Christopher Behme, Daniel P. Christen, Devi Reddy Gohimukkula, Dharma Rao Polisetti, James Quada, Jennifer L.R. Freeman, Kalpathy Santhosh, Muralidhar Bondlela, Mustafa Guzel, Ravindra Reddy Yarragunta, Robert Carl Andrews, Stephen Thomas Davis, Thomas Scott Yokum
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Publication number: 20110065713Abstract: The present invention is directed to benzazole compounds that inhibit ?-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment or prevention of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which BACE is involved.Type: ApplicationFiled: November 19, 2010Publication date: March 17, 2011Applicant: High Point Pharmaceuticals, LLCInventors: Adnan M.M. Mjalli, David Jones, Devi Reddy Gohimmukkula, Guoxiang Huang, Jeff Zhu, Mohan Rao, Robert C. Andrews, Tan Ren
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Publication number: 20100292266Abstract: Certain oxazolyl piperidine compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).Type: ApplicationFiled: May 25, 2007Publication date: November 18, 2010Inventors: Richard Apodaca, James Guy Breitenbucher, Alison L. Chambers, Mark Seierstad, Wei Xiao
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Publication number: 20100249415Abstract: The present invention provides two synthetic routes for the preparation of Temsirolimus (compound 1b and analog of Temsirolimus 1a). The first route includes the synthesis of CCI-779 by directly reacting rapamycin (4b) or Prolyl-rapamycin (4a) with substituent-2,2-bis(methoxy) propionic acid anhydride(11) in the presence of an organic base, followed by deprotection to give CCI-779 or Proline CCI-779. The second route includes a process involving a reaction of rapamycin-OH-31-sily ether (4d) or Prolyl-rapamycin-OH-31-sily ether (4c) with substituent-2,2-bis(methoxy) propionic acid anhydride(11) in the presence of an organic base and followed by subsequent hydrolysis step to obtain the desired CCI-779 or Proline CCI-779. Compound 11, as described in this invention, is stable at room temperature, cost effective and ease of processing.Type: ApplicationFiled: March 29, 2010Publication date: September 30, 2010Inventors: Kwang-Chung Lee, Ting-Huei Lee, Yen-Shih Tung, Chia-Chen Kao, Tzu-Ai Lee
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Publication number: 20100249172Abstract: 9-Chloro-nos, prodrugs thereof, and pharmaceutically acceptable salts thereof, are disclosed. Pharmaceutical compositions including 9-chloro-nos, and methods of preparation and use thereof are disclosed. 9-Chloro-nos is a noscapine analog that can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, by binding tubulin and inducing apoptosis selectively in tumor cells (ovarian and T-cell lymphoma) resistant to paclitaxel, vinblastine and teniposide. 9-Chloro-nos can perturb the progression of cell cycle by mitotic arrest, followed by apoptotic cell death associated with increased caspase-3 activation and appearance of TUNEL-positive cells. Thus, 9-chloro-nos is a novel therapeutic agents for a variety of cancers, including ovarian and T-cell lymphoma cancers, even those that have become drug-resistant to currently available chemotherapeutic drugs.Type: ApplicationFiled: March 4, 2008Publication date: September 30, 2010Applicant: EMORY UNIVERSITYInventor: Ramesh Chandra
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Publication number: 20100227878Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are noscapine analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers. While the antitussive plant alkaloid, noscapine, binds tubulin, displays anticancer activity, and has a safe pharmacological profile in humans, structure-function analyses pointed to a proton at position 9 of the isoquinoline ring that can be modified without compromising tubulin binding activity. Noscapine analogs with various functional moieties at position 9 on the isoquinoline ring kill human cancer cells resistant to other anti-microtubule agents, such as vincas and taxanes. Representative analogs include the 9-nitro, 9-bromo-, 9-iodo-, and 9-fluoro-noscapines, which bind tubulin and induce apoptosis selectively in tumor cells (ovarian and T-cell lymphoma) resistant to paclitaxel, vinblastine and teniposide.Type: ApplicationFiled: March 4, 2008Publication date: September 9, 2010Applicant: EMORY UNIVERSITYInventors: Harish C. Joshi, Ritu Aneja, Surya N. Vangapandu
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Publication number: 20100184985Abstract: The present invention discloses a new strain of Streptomyces sp. BICC 7522, its variants or mutants and use of the strain for the production of macrolides, process of production and purification of macrolides.Type: ApplicationFiled: January 12, 2010Publication date: July 22, 2010Applicant: Biocon, Ltd.Inventors: Madhav Kulkarni, Surekha K. Prabhu, Madenahally Channabasappa Shivakumar, Prijyajit Sengupta, Sanjay Tiwari, Rakesh Mendhe, Nitin Patil, Laxmi Adhikary, Anand Khedkar, Ramakrishnan Melarkode, Ramavana Gururaja, Shrikumar Suryanarayan
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Patent number: 7727980Abstract: This invention relates to non-steroidal tricyclic compounds that are modulators of androgen receptors and to methods for making and using such compounds.Type: GrantFiled: January 31, 2006Date of Patent: June 1, 2010Assignee: Ligand Pharmaceuticals IncorporatedInventors: Lin Zhi, Cornelis Arjan Van Oeveren
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Publication number: 20100130498Abstract: The present invention relates to agonists of the human bitter-taste receptors hTAS2R14, hTAS2R10 and hTAS2R4 and their role in bitter taste transduction. The invention also relates to methods for identifying molecules that modulate, e.g. suppress, or enhance hTAS2R14, hTAS2R10 and hTAS2R4 bitter taste transduction or bitter taste response.Type: ApplicationFiled: March 31, 2008Publication date: May 27, 2010Applicant: Deutshes Institut Fur Ernahrungsforschung Potsdam- RehbruckeInventors: Maik Behrens, Anne Brockhoff, Christina Kuhn, Wolfgang Meyerhof, Giovanni Appendino
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Publication number: 20100081822Abstract: The invention provides a method for separating noscapine from an opium source without substantially changing the color of the noscapine.Type: ApplicationFiled: September 29, 2009Publication date: April 1, 2010Applicant: Mallinckrodt Inc.Inventors: Benjamin M. Marshall, Keith G. Tomazi
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Publication number: 20100076012Abstract: Compounds of the formula (I), in which E, R3, R4, R5, X, Y, W, Q1, Q2, Z, s and m have the meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: February 22, 2008Publication date: March 25, 2010Applicant: Merck Patent GmbHInventors: Kai Schiemann, Dirk Finsinger, Christiane Amendt, Frank Zenke
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Publication number: 20090275754Abstract: A process for purifying Narcotine to remove color and impurities to form Noscapine. The process includes forming an aqueous isopropanol solution with the Narcotine product wherein the isopropanol concentration of the solution is about 20% to about 70% by volume; and adjusting the pH of the solution with a strong base to a pH of about 10 to about 14, wherein impurities are removed from the Narcotine product.Type: ApplicationFiled: March 28, 2007Publication date: November 5, 2009Inventors: Keith G. Tomazi, Leroy Love, JR., Joseph P. Haar, JR.
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Publication number: 20090270371Abstract: Compounds of formula (I): and/or enantiomers and/or racemates and/or diastereomers and/or pharmaceutically acceptable salts thereof formed with acids or bases, to the process for their preparation, to the intermediates of the preparation process, to the pharmaceutical formulations containing these compounds and to their use in the prevention and/or treatment of mGluR5 receptor-mediated disorders.Type: ApplicationFiled: December 19, 2006Publication date: October 29, 2009Inventors: Gyorgy Keseru, Csaba Weber, Attila Bielik, Amrita Agnes Bobok, Krisztina Gal, Marta Meszlenyine Sipos, Laszlo Molnar, Monika Vastag
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Publication number: 20090270374Abstract: Bicyclic nitrogen containing compounds and their use as antibacterials.Type: ApplicationFiled: July 18, 2007Publication date: October 29, 2009Inventors: Llius Ballell, David Barros, Gerald Brooks, Julia Castro Pichel, Steven Dabbs, Robert A. Daines, David Thomas Davies, Jose Maria Fiandor Roman, Israil Pendrak, Modesto J. Remuinan Blanco, Jason Anthony Rossi, Ilaria Giordano, Alan Joseph Hennessy, James B. Hoffman, Graham Elgin Jones, Timothy James Miles, Neil David Pearson, Lihua(lily) Zhang
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Publication number: 20090209572Abstract: The present invention relates to novel 36-des(3-methoxy-4-hydroxycyclohexyl)-36-(3-hydroxycycloheptyl)rapamycin derivatives, methods for their production, and uses thereof. In a further aspect the present invention provides for the use of these 36-des(3-methoxy-4-hydroxycyclohexyl)-36-(3-hydroxycycloheptyl)rapamycin derivatives in the treatment of cancer and/or B-cell malignancies, the induction or maintenance of immunosuppression, the treatment of transplantation rejection, graft vs. host disease, autoimmune disorders, diseases of inflammation, vascular disease and fibrotic diseases, the stimulation of neuronal regeneration or the treatment of fungal infections.Type: ApplicationFiled: November 19, 2008Publication date: August 20, 2009Applicant: Biotica Technology LimitedInventors: Barrie Wilkinson, Ming-Qiang Zhang, Rose Mary Sheridan, Christoph Beckmann
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Publication number: 20090131412Abstract: A compound represented by the formula (1) or a pharmaceutically acceptable salt thereof which has a therapeutic or prophylactic effect on an SNS-related disease such as neuropathic pain. (1) wherein R1 and R2 independently represent an alkyl group having 1 to 4 carbon atoms or the like, or R1 and R2 may together form a 5- to 7-membered ring; n represents a numerical number of 1 to 3; A represents a substituted or unsubstituted aryl group or the like or a formula: —N(R5)R6 (wherein R5 and R6 independently represent a substituted or unsubstituted alkyl group or the like); and R3 and R4 independently represent a substituted or unsubstituted alkyl group or the like, or R3 and R4 may together form a substituted or unsubstituted, saturated or unsubstituted nitrogenated heterocyclic ring, provided that both of R1 and R2 are not a hydrogen atom when R3 and R4 together form a piperidine ring.Type: ApplicationFiled: June 5, 2006Publication date: May 21, 2009Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Kazuhito Ikeda, Kazuo Kumagai, Katsunori Tsuboi, Nobuhisa Fukuda
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Publication number: 20090042874Abstract: The invention provides compounds of the Formula: that are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa, bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.Type: ApplicationFiled: May 29, 2008Publication date: February 12, 2009Applicant: WYETHInventors: Amedeo A. Failli, Deborah Evrard, Yanfang Li, Nicole T. Hatzenbuhler, Juliann Mogish, Iwan S. Gunawan, Antonina Nikitenko, Ping Zhou
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Publication number: 20090042895Abstract: Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.Type: ApplicationFiled: October 20, 2008Publication date: February 12, 2009Applicant: WyethInventors: Michael Byron Webb, Gary Paul Stack, Magda Asselin, Deborah A. Evrard
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Publication number: 20090030028Abstract: Disclosed are compounds of formula (I), wherein W, R, R1, R2, R3, R4, R5, R6, and R7 have the meanings indicated in claim 1. Said compounds can be used for the treatment of tumors, among other things.Type: ApplicationFiled: June 3, 2005Publication date: January 29, 2009Inventors: Kai Schiemann, David Bruge, Hans-Peter Buchstaller, Dirk Finsinger, Wolfgang Staehle, Christiane Amendt, Ulrich Emde, Frank Zenke
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Publication number: 20090012298Abstract: Processes for the production of a 32-deoxorapamycin from a 32-iodo- or 32-hydroxyrapamycin, wherein the hydroxy group is substituted by the residue of an arylthionocarbonate or an arylthiocarbamate, in the presence of tris(trimethylsilyl)-silan and ?,??-azo-isobutyronitril in organic solvent; and 32-deoxorapamycin in the form of a crystalline solvate.Type: ApplicationFiled: January 22, 2007Publication date: January 8, 2009Inventors: Murat Acemoglu, Sabine Pfeffer
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Publication number: 20080306098Abstract: A method for modulating at least one pharmacokinetic property of a protease inhibitor upon administration to a host is provided. One administers to the host an effective amount of a bifunctional compound of less than about 5000 daltons comprising the protease inhibitor or an active derivative thereof and a pharmacokinetic modulating moiety. The pharmacokinetic modulating moiety binds to at least one intracellular protein. The bifunctional compound has at least one modulated pharmacokinetic property upon administration to the host as compared to a free drug control that comprises the protease inhibitor.Type: ApplicationFiled: May 5, 2008Publication date: December 11, 2008Inventors: Mitchell W. Mutz, Jason E. Gestwicki
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Patent number: 7449579Abstract: A “real time” method for detecting electrophilic and nucleophilic species generally by employing tunable, precursor sensor materials that mimic the physiological interaction of these agents to form highly florescent berberine-type alkaloids that can be easily and rapidly detected. These novel precursor sensor materials can be tuned for reaction with both electrophilic (chemical species, toxins) and nucleophilic (proteins and other biological molecules) species.Type: GrantFiled: May 2, 2006Date of Patent: November 11, 2008Assignee: Sandia CorporationInventors: James R. McElhanon, Timothy J. Shepodd
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Patent number: 7442710Abstract: The present invention relates to compounds of general formula IA or IB wherein X1 and X2 are each independently N or C—R? and R1, R2,R3, R4, R5, and R6 are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The compounds can be used for the treatment of diseases related to the glycine transporter inhibitor, such as schizophrenia and Alzheimer's disease.Type: GrantFiled: January 24, 2006Date of Patent: October 28, 2008Assignee: Hoffman-La Roche Inc.Inventors: Synese Jolidon, Robert Narquizian, Roger David Norcross, Emmanuel Pinard
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Publication number: 20080234309Abstract: The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the formula: wherein R1, R2, R3, R5, R6, R8, M1, M2, M3, M4, M5, M6 and M7 are each independently a member selected from the group consisting of H, C1-6 alkyl, OH and C1-6 hydroxyalkyl; R4, R7 and R9 are each independently selected from the group consisting of C1-6 alkoxy and OH; R10 is a member selected from the group consisting of H, —OH, —OP(O)Me2, —O—(CH2)n—OH and —O—(CH2)m—O—(CH2)o—CH3, wherein subscripts n and m are each independently from 2 to 8 and subscript o is from 1 to 6; each of L1 and L4 are independently selected from the group consisting of: wherein each M8 is independently a member selected from the group consisting of C1-6 alkyl, OH and C1-6 hydroxyalkyl; each of L2 and L3 are independently selected from the group consisting of: and salts, hydrates, isomers, metabolites, N-oxides and prodrugs thereof.Type: ApplicationFiled: March 11, 2008Publication date: September 25, 2008Applicant: Elixir Medical CorporationInventors: John Yan, Xiaoxia Zheng, Vinayak D. Bhat
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Publication number: 20080227982Abstract: An improved process for coating implantable medical devices utilizes a number of techniques for improving the stability of therapeutic agents contained within the coating. The stability of the therapeutic agents may be improved by creating substantially solvent-free, amorphous forms of the therapeutic agents.Type: ApplicationFiled: May 27, 2008Publication date: September 18, 2008Inventors: Cynthia A. Maryanoff, Karel Six, Roger Vandecruys
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Publication number: 20080171763Abstract: A prodrug compound of a rapamycin analog and methods for inhibiting, treating, and preventing mammalian diseases.Type: ApplicationFiled: November 30, 2006Publication date: July 17, 2008Applicant: ABBOTT LABORATORIESInventors: Karl W. Mollison, Angela M. LeCaptain, Sandra E. Burke, Keith R. Cromack, Peter J. Tarcha, Yen-Chih J. Chen, John L. Toner
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Publication number: 20080171765Abstract: New aniline or phenol N-mustards linked to DNA-affinity carriers (such as 9-anilinoacridines, acridines and quinolines), aminobenzamides or aminophenol ethers by a urea, carbamic acid, carbanic acid ester, hydrazineurea, hydrazinecarbamic acid ester, phenoxyurea, phenoxycarbamic acid ester linkage with improved chemical stability and anti-tumor therapeutic efficacy are provided.Type: ApplicationFiled: January 11, 2008Publication date: July 17, 2008Applicant: Academia SinicaInventors: Tsann-Long Su, Ting-Chao Chou
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Publication number: 20080139546Abstract: The present invention relates to a compound of the formula: or an enantiomer, diastereomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, useful as modulators of 5-HT1A receptor activity and/or serotonin reuptake. These compounds are useful in treating nervous system disorders, such as anxiety-related disorders, cognition-related disorders, depression, schizophrenia, or sexual dysfunction and related illnesses.Type: ApplicationFiled: September 28, 2007Publication date: June 12, 2008Applicant: WyethInventors: Minsheng Zhang, Charles J. Stanton, Boyd Lynn Harrison, Terrance H. Andree
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Publication number: 20080138375Abstract: The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the formula: wherein R1, R2, R3, R5, R6 and R8 are each independently a member selected from the group consisting of H, C1-6 alkyl and OH; R4, R7 and R9 are each independently selected from the group consisting of C1-6 alkoxy and OH; R10 is a member selected from the group consisting of H, —OH, —OP(O)Me2, —O—(CH2)n—OH and —O—(CH2)m—O—(CH2)o— CH3, wherein subscripts n and m are each independently from 2 to 8 and subscript o is from 1 to 6; each of L1 and L4 are independently selected from the group consisting of: each of L2 and L3 are independently selected from the group consisting of: salts, hydrates, isomers, metabolites and prodrugs thereof.Type: ApplicationFiled: September 12, 2007Publication date: June 12, 2008Applicant: Elixir Medical CorporationInventors: John Yan, Xiaoxia Zheng, Vinayak D. Bhat
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Patent number: 7365201Abstract: A process for the preparation of the boron difluoride chelate of 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolone carboxylic acid via: (a) the reaction of 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolone carboxylic acid ethyl ester with, (b) fluoroboric acid in the presence of poly(methylhydrosiloxane) or hexamethyldisiloxane.Type: GrantFiled: March 2, 2006Date of Patent: April 29, 2008Assignee: Apotex Pharmachem Inc.Inventors: Zhi-Xian Wang, Murali Kondamreddy, Joseph DiMartino, Bhaskar Reddy Guntoori
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Patent number: 7345174Abstract: The present invention provides the compound having the formula: wherein each of R1 and R2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, t-butyl, aryloxy, arylalkyloxy, or pyridine group; wherein A is an amido moiety, —O—, —S—, —NH—, or —CH2—; and wherein n is an integer from 3 to 8. The present invention also provides a method of selectively inducing growth arrest, terminal differentiation and/or apoptosis of neoplastic cells and thereby inhibiting proliferation of such cells. Moreover, the present invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically acceptable amount of the compound above.Type: GrantFiled: June 22, 2006Date of Patent: March 18, 2008Assignees: Sloan-Kettering Institute for Cancer Research, The Trustees of Columbia University in the City of New YorkInventors: Ronald Breslow, Sandro Belvedere, Leland Gershell, Thomas A. Miller, Paul A. Marks, Victoria M. Richon, Richard A. Rifkind
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Publication number: 20080033177Abstract: The present invention is directed to a process for the synthesis of substituted-1,2,3,4-tetrahydroisoquinoline derivatives, useful as intermediates in the synthesis of pharmaceutical agents.Type: ApplicationFiled: August 7, 2007Publication date: February 7, 2008Inventors: Frank J. Villani, Hua Zhong
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Patent number: 7321039Abstract: The invention relates to a new industrially useable process for preparing tropenol, optionally in the form of the acid addition salts thereof.Type: GrantFiled: January 18, 2005Date of Patent: January 22, 2008Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Rolf Banholzer, Gisela Bodenbach, Andreas Mathes, Helmut Meissner, Peter Specht
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Patent number: 7297704Abstract: The present invention provides cycloalkylfused indole, benzothiophene, benzofuran, and indene derivatives, and methods for using them to, for example, treat, prevent and/or ameliorate central nervous system diseases by antagonizing 5-HT1A receptors and modulating serotonin levels.Type: GrantFiled: February 16, 2006Date of Patent: November 20, 2007Assignee: WyethInventors: Annmarie Louise Sabb, Robert Lewis Vogel, Gary Paul Stack, Deborah Ann Evrard, Amedeo Arturo Failli, Lalitha Krishnan, Anita Wai-Yin Chan, Jianxin Ren, Charles J. Guinosso, Reinhardt Bernhard Baudy, Jean Yi-ching Sze, Yanfang Li, Charles John Stanton, III, Antonia Nikitenko
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Publication number: 20070238750Abstract: The invention provides an isolated stereoisomer of tritoqualine having the structure of FIG. 2 and FIG. 3.Type: ApplicationFiled: April 9, 2007Publication date: October 11, 2007Inventors: Michalis Nicolaou, Emile Loria, Gaetan Terrasse, Yves Trehin
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Patent number: 7053104Abstract: The present invention provides compounds, and pharmaceutical compositions containing those compounds, that are active at metabotropic glutamate receptors. The compounds are useful for treating neurological diseases and disorders. Methods of preparing the compounds also are disclosed.Type: GrantFiled: August 5, 2002Date of Patent: May 30, 2006Assignee: NPS Pharmaceuticals, Inc.Inventors: Bradford C. Van Wagenen, Scott T. Moe, Daryl L. Smith, Susan M. Sheehan, Irina Shcherbakova, Ruth Walton, Richard Trovato, Robert Barmore, Eric G. Delmar, Thomas M. Stormann
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Patent number: 7038052Abstract: Methods of preparing compounds of Formula I are provided.Type: GrantFiled: December 12, 2003Date of Patent: May 2, 2006Assignee: WyethInventors: Anita W. Chan, Timothy T. Curran, Silvio Iera, Warren Chew, John H. Sellstedt, Galina Vid, Gregg Feigelson, Zhixian Ding
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Patent number: 7012142Abstract: The present application is directed to a method of synthesis of a bicyclic or polycyclic compound of formula I or formula II: in which E, G, Y, n, m, R, R1, R2, R3, R6, R7, R8 and R9 are as defined.Type: GrantFiled: April 25, 2003Date of Patent: March 14, 2006Assignee: Monash UniversityInventors: Patrick Perlmutter, Mark Rose, Neeranat Thienthong
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Patent number: 6962942Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds having Formula I: or pharmaceutically acceptable salts thereof; wherein Q is phenyl, benzyl, pyridyl, thienyl, indolyl, quinolinyl, benzothienyl, biphenylyl, or imidazolyl; any of which can include one or more optional substituents independently selected from halo, trifluoromethyl, hydroxy, amino, nitro, cyano, C1 alkoxy, C1-3 alkyl, methylenedioxy, carboxamido, acetamido, or amidino; X is methylene, carbonyl, or sulfonyl; Z is methylene, ethylene, or propylene; M is methylene or ethylene; and R1 R2 and R3 are independently hydrogen or C1-3 alkyl.Type: GrantFiled: September 16, 2002Date of Patent: November 8, 2005Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Scott C. Miller, Juan José Marugán Sánchez, Kristin D. Haslow, Jonathan Hall
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Patent number: 6939877Abstract: Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as premenstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.Type: GrantFiled: September 10, 2003Date of Patent: September 6, 2005Assignee: WyethInventors: Michael Bryon Webb, Gary Paul Stack, Magda Asselin, Deborah A. Evrard
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Patent number: 6911445Abstract: Compounds of the formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive-compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.Type: GrantFiled: September 10, 2003Date of Patent: June 28, 2005Assignee: WyethInventors: Deborah Ann Evrard, Gary Paul Stack, Uresh Shantilal Shah
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Patent number: 6891042Abstract: The invention relates to a new industrially useable process for preparing tropenol, optionally in the form of the acid addition salts thereof.Type: GrantFiled: January 26, 2004Date of Patent: May 10, 2005Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Rolf Banholzer, Gisela Bodenbach, Andreas Mathes, Helmut Meissner, Peter Specht
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Patent number: 6875869Abstract: A process for the preparation of the compounds of general formula (I) wherein R is selected from methyl, ethyl, n-propyl, iso-propyl, n-butyl, iso-butyl, sec.Type: GrantFiled: June 12, 2003Date of Patent: April 5, 2005Assignee: Active Biotech ABInventor: Karl Jansson
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Patent number: 6872718Abstract: A compound represented by the formula: wherein Ring A is a non-aromatic 5- to 7-membered nitrogen-containing heterocyclic ring which may be further substituted, Ring B is benzene ring which is further substituted, Ring C is a dihydrofuran-ring which may be further substituted and R is hydrogen atom or an acyl group or a salt thereof has an excellent lipid peroxidation inhibitory activity and is useful as a lipid peroxidation inhibitor.Type: GrantFiled: August 18, 2000Date of Patent: March 29, 2005Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Tadatoshi Hashimoto, Tetsuya Tsukamoto
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Patent number: 6821981Abstract: Compounds of the formula useful for the treatment of disorders, such as anxiety, aggression and stress, and for the control of various physiological phenomena, such as appetite, thermoregulation, sleep and sexual behavior.Type: GrantFiled: April 25, 2002Date of Patent: November 23, 2004Assignee: WyethInventors: Gary P. Stack, Megan Tran, Jonathan L. Gross, George E. M. Husbands
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Patent number: 6800637Abstract: Compounds of the formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa, bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.Type: GrantFiled: September 10, 2003Date of Patent: October 5, 2004Assignee: WyethInventors: Gary Paul Stack, Michael Byron Webb, Deborah Ann Evrard, Dahul Zhou
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Patent number: 6747153Abstract: The invention relates to a new industrially useable process for preparing tropenol, optionally in the form of the acid addition salts thereof.Type: GrantFiled: May 29, 2003Date of Patent: June 8, 2004Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Rolf Banholzer, Gisela Bodenbach, Andreas Mathes, Helmut Meissner, Peter Specht
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Patent number: RE39762Abstract: Polyketide compounds of the formula but not including FK-506, FK-520, 18-hydroxy-FK520 and 18-hydroxy-FK-506.Type: GrantFiled: December 9, 2005Date of Patent: August 7, 2007Assignee: Kosan Biosciences, Inc.Inventors: Christopher Reeves, Daniel Chu, Chaitan Khosla, Daniel Santi, Kai Wu