Ring Nitrogen Is Shared By Two Of The Cyclos Patents (Class 514/294)
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Publication number: 20080167337Abstract: Substituted 3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-ol compounds are disclosed that are inhibitors of the vesicular monoamine transporter 2 (VMAT2). The compounds of this invention have the structure: wherein R1 is as defined herein, including stereoisomers and pharmaceutically acceptable salts and solvates thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use in a subject in need thereof.Type: ApplicationFiled: November 8, 2007Publication date: July 10, 2008Inventor: Kyle W. Gano
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Publication number: 20080161337Abstract: Chronic prostatitis (CP) is a syndrome characterized by pelvic pain in one or more areas (perineum, lower abdominal, testicular and/or penile), urinary frequency, urinary urgency, sexual dysfunction and/or ejaculatory pain. CP type IIIa is the most common type of prostatitis and is defined by having sterile EPS and a leukocyte count greater than 1000/mm2. A method of prevention of chronic prostatitis is disclosed that comprises orally administering a composition containing a therapeutically effective amount of rifaximin to a patient exhibiting symptoms of chronic prostatitis.Type: ApplicationFiled: January 3, 2007Publication date: July 3, 2008Inventor: Leonard Weinstock
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Publication number: 20080159987Abstract: Restless legs syndrome (RLS) is characterized by an urge for leg movement, often with abnormal leg sensations. Symptoms are triggered by rest, often at night, and improve temporarily with movement, especially walking. This syndrome has a prevalence ranging from 7% to 15% and significantly contributes to sleep disorders. A method of prevention of restless legs syndrome is disclosed that comprises orally administering a composition containing a therapeutically effective amount of rifaximin to a patient exhibiting symptoms of restless legs syndrome.Type: ApplicationFiled: January 3, 2007Publication date: July 3, 2008Inventor: Leonard Weinstock
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Publication number: 20080161338Abstract: The invention relates to novel pyrrolodihydroisoquinoline derivatives, which are efficacious inhibitors of PDE10.Type: ApplicationFiled: January 11, 2006Publication date: July 3, 2008Applicant: ALTANA PHARMA AGInventors: Matthias Vennemann, Thomas Bar, Jurgen Braunger, Paola Ciapetti, Jean-Marie Contreras, Camille George Wermuth
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Publication number: 20080125456Abstract: This invention relates to tacrolimus injection comprising tacrolimus as an active ingredient, macrogol 15 hydroxystearate as a surfactant and a non-aqueous solvent.Type: ApplicationFiled: November 11, 2005Publication date: May 29, 2008Applicant: Chong Kun Dang Pharmaceutical CorporationInventors: Sang Joon Lee, Hee Jong Shin, Seok Kyu Lee, Ji Hun Yun
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Publication number: 20080108645Abstract: The invention provides novel isomers of dihydrotetrabenazine, individual enantiomers and mixtures thereof wherein the dihydrotetrabenazine is a 3,11 b-cis-dihydrotetrabenazine. Also provided are methods for the preparation of the novel isomers, pharmaceutical compositions containing them and their use in treating hyperkinetic movement disorders such as Huntington's disease, hemiballismus, senile chorea, tic, tardive dyskinesia and Tourette's syndrome.Type: ApplicationFiled: February 11, 2005Publication date: May 8, 2008Applicant: CAMBRIDGE LABORATORIES, (IRELAND), LTD.Inventors: Robert Tridgett, Ian Clarke, Robert Turtle, Grant Johnston
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Publication number: 20080026081Abstract: The present invention relates to methods of treatment using the compound (+)-isopropyl 2-methoxyethyl 4-(2-chloro-3-cyano-phenyl)-1,4-dihydro-2,6-dimethyl-pyridine-3,5-dicarboxylate, as a sole active agent or in combination with other pharmacological agents.Type: ApplicationFiled: November 19, 2004Publication date: January 31, 2008Inventors: Axel Unterbeck, Michael De Vivo, Gregory M. Rose
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Patent number: 7247642Abstract: The present invention relates to optically pure S-(?)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof, substantially free of their R-(+)-isomers, to processes for preparation of the optically pure S-(?)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof substantially free of their R-(+)-isomers, and to pharmaceutical compositions comprising the S(?)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof.Type: GrantFiled: May 8, 2000Date of Patent: July 24, 2007Assignee: Wockhardt LimitedInventors: Mahesh Vithalbhai Patel, Shivkumar Agarwal, Sreenivas Kandepu, Nitin Shetty, Dilip Jatashankar Upadhyay, Nishith Chandra Chaturvedi, Abraham Thomas, Noel John De Souza, Habil Fakhruddin Khorakiwala
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Patent number: 7186709Abstract: The present invention provides novel dihydropyrancarboxamide compounds of formula (I): and collections of these compounds, and provides methods for the synthesis of these compounds; wherein R1–R6 are as defined herein. Additionally, the present invention provides pharmaceutical compositions and methods for treating disorders such as proliferative diseases, and cancer, to name a few.Type: GrantFiled: August 27, 2003Date of Patent: March 6, 2007Assignee: President and Fellows of Harvard CollegeInventors: Stuart L. Schreiber, Robert A. Stavenger, Timothy J. Mitchison, Zoltan Maliga
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Patent number: 7166744Abstract: The present invention relates to a novel retinoid derivative compound represented by the formula I: wherein X, R1, R2 and R3 are as defined herein or pharmaceutically acceptalbe salts thereof. Also, the present invention relates to processes for producing the compound of the formula I and to an anti-cancer composition comprising the compound of the formula I. The compound of the formula I according to the present invention exerts high anti-cancer effects while not causing undesirable side effects.Type: GrantFiled: May 29, 2002Date of Patent: January 23, 2007Assignee: Chebigen Co., Ltd.Inventors: Hong-Sig Sin, Soo-Jong Um, Young-Soy Rho, Si-Ho Park, Youn-Ja Kwon, Myoung-Soon Park, Hye-Sook Han, So-Mi Kim, Dong-Myoung Kim, Deok-Kun Oh, Jong-Sup Park, Tae-Sung Bae
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Patent number: 7164023Abstract: The invention relates to crystalline S-(?)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid L-arginine salt tetrahydrate, a process for its preparation and pharmaceutical formulations incorporating it as the active ingredient for use in treating microbial infections.Type: GrantFiled: December 31, 2003Date of Patent: January 16, 2007Assignee: Wockhardt LimitedInventors: Prasad K. Deshpande, Vijaya N. Desai, Ravindra D. Yeole, Shrikant V. Gupte, Mahesh V. Patel, Noel J. de Souza
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Patent number: 7144913Abstract: Dihydropyrroloindoles and tetrahydropyridoindoles are prostaglandin receptor antagonists useful for the treatment of prostaglandin-mediated diseases such as allergic rhinitis, nasal congestion and asthma.Type: GrantFiled: May 22, 2002Date of Patent: December 5, 2006Assignee: Merck Frosst Canada & Co.Inventors: Zhaoyin Wang, Christian Beaulieu, Claude Dufresne, Daniel Guay, Yves LeBlanc
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Patent number: 7135480Abstract: The present invention is directed to substituted 1-benzoyl-3-cyano-pyrrolo[1,2-?]quinolines and analogs thereof, represented by the general Formula I: wherein R1–R8, L, Q, dash line and Ar are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: GrantFiled: December 12, 2003Date of Patent: November 14, 2006Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, John A Drewe, Sungchun Jiang, Shailaja Kasibhatla, Jared Daniel Kuemmerle, Nilantha Sudath Sirisoma, Han-Zhong Zhang
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Patent number: 7122555Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3 and R4 are as indicated in the description, or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of diseases which are associated with DPP-IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.Type: GrantFiled: June 17, 2004Date of Patent: October 17, 2006Assignee: Hoffmann-la Roche Inc.Inventors: Markus Boehringer, Bernd Kuhn, Patrizio Mattei, Robert Narquizian
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Patent number: 7098219Abstract: Compounds are described which are efflux pump inhibitors of cellular efflux pumps of microbes. Also described are methods of preparing such compounds, methods of using such efflux pump inhibitor compounds and pharmaceutical compositions which include such compounds.Type: GrantFiled: July 31, 2001Date of Patent: August 29, 2006Assignee: Wockhart LimitedInventors: Noel John de Souza, Mahesh Vithalbhai Patel, Shrikant V Gupte, Dilip J Upadhyay, Milind Chintaman Shukla, Nishith C Chaturvedi, Satish B Bhawsar, Sheela Chandresekharan Nair, Mohammed A Jafri, Habil Fakhruddin Khorakiwala
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Patent number: 7034037Abstract: The present invention is directed to medical devices and pharmaceutical or agricultural compositions, and seeds, each containing a synthetic, bioabsorbable, biocompatible polymeric wax that is the reaction product of a polybasic acid or derivative thereof, a polyol and a fatty acid, the polymeric wax having a melting point less than about 70° C., as determined by differential scanning calorimetry, and an effective amount of rapamycin or an analogue thereof.Type: GrantFiled: December 18, 2002Date of Patent: April 25, 2006Assignee: Ethicon, Inc.Inventors: Steven Arnold, Aruna Nathan, Joel Rosenblatt
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Patent number: 7022729Abstract: Azabicyclic, azatricyclic and azaspirocyclic derivatives of aminocyclohexanes which are systemically-active as NMDA, 5HT3, and nicotinic receptor antagonists, pharmaceutical compositions comprising the same, method of preparation thereof, and method of treating CNS disorders which involve disturbances of glutamatergic, serotoninergic, and nicotinic transmission, treating immunomodulatory disorders, and antimalaria, antitrypanosomal, anti-Borna virus, anti-HSV and anti-Hepatitis C virus activity.Type: GrantFiled: March 21, 2003Date of Patent: April 4, 2006Assignee: Merz Pharma GmbH & Co. KGAAInventors: Christopher Graham Raphael Parsons, Markus Henrich, Wojciech Danysz, Ivars Kalvinsh, Valerjans Kauss, Aigars Jirgensons, Markus Gold, Maksims Vanejevs
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Patent number: 6962925Abstract: A fully and partially reduced benzo(c)quinolizine compound of formula (1):Type: GrantFiled: June 12, 2000Date of Patent: November 8, 2005Assignee: Applied Research Systems ARS Holding N.V.Inventors: Antonio Guarna, Mario Serio
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Patent number: 6930114Abstract: The present invention relates to pyrrolo[2.1-a]dihydroisoquinolines which are inhibitors of phosphodiesterase 10a and can be used for combating cancer.Type: GrantFiled: December 4, 2001Date of Patent: August 16, 2005Assignee: Bayer Pharmaceuticals CorporationInventors: Maria Theresia Niewöhner, Marcus Bauser, Jens-Kerim Ergüden, Dietmar Flubacher, Paul Naab, Thorsten-Oliver Repp, Jürgen Stoltefuss, Nils Burkhardt, Andrea Sewing, Michael Schauer, Karl-Heinz Schlemmer, Olaf Weber, Stephen J. Boyer, Mark Miglarese, Ulrich Niewöhner
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Patent number: 6914066Abstract: This invention concerns compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein ?X1—X2—X3— is a trivalent radical,; >Y1—Y2— is a trivalent radical; r and s are each independently 0, 1, 2, 3, 4 or 5; t is 0, 1, 2 or 3; each R1 and R2 are independently hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkylthio, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)amino, mono- or di(C1-6alkylaminoC1-6alkyloxy, aryl, arylC1-6alkyl, aryloxy or arylC1-6alkyloxy, hydroxycarbonyl, C1-6alkyloxycarbonyl; or two R1 or R2 on adjacent positions form together a bivalent radical; R3 is hydrogen, halo, C1-6alkyl, cyano, haloC1-6alkyl, hydroxyC1-6alkyl, cyanoC1-6alkyl, aminoC1-6alkyl, C1-6alkyloxyC1-6alkyl, C1-6alkylthio-C1-6alkyl, aminocarbonylC1-6alkyl, hydroxycarbonyl, hydroxycarbonylC1-6alkyl, C1-6alkyoxycarbonylC1-6alkyl, C1-6alkylcarbonylCType: GrantFiled: June 24, 2002Date of Patent: July 5, 2005Assignee: Janssen Pharmaceutica N.V.Inventors: Patrick René Angibaud, Marc Gaston Venet, Xavier Marc Bourdrez
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Patent number: 6897222Abstract: The present invention provides compounds of formula (I): wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP-IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.Type: GrantFiled: March 15, 2004Date of Patent: May 24, 2005Assignee: Hoffmann-La Roche Inc.Inventors: Luca Claudio Gobbi, Thomas Luebbers, Patrizio Mattei, Robert Narquizian, Pierre Charles Wyss
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Patent number: 6884433Abstract: Sustained release formulation containing tacrolimus or its hydrate is provided. The time (T63.2%) required for 63.2% of the maximum amount of tacrolimus or its hydrate to be dissolved is 0.7 to 15 hours. The time is measured in accordance to the Japanes Pharmacopocia, the 13-th edition, Dissolution Test, No. 2 (Puddles method, 50 rpm) using an aqueous 0.005% hydroxypropyl cellulose solution. This aqueous test solution is adjusted to pH 4.5, accordingly. The formulation further comprises a solid base which is a water-soluble or water-insoluble polymer. The formulation is in the form of a powder, fine powder, granule, tablet or capsule. The formulation is administered to a patient once a day for preventing organ or tissue rejection by transplantation or autoimmune disease. In addition, a solid dispersion composition is provided. The solid dispersion comprises tacrolimus or its hydrate in a mixture containing water-soluble or water-insoluble polymer and an excipient.Type: GrantFiled: April 14, 2003Date of Patent: April 26, 2005Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kazunari Yamashita, Eiji Hashimoto, Yukihiro Nomura, Fumio Shimojo, Shigeki Tamura, Takeo Hirose, Satoshi Ueda, Takashi Saitoh, Rinta Ibuki, Toshio Ideno
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Patent number: 6878713Abstract: This invention relates to new generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, to their optical isomers, diastereomers or enantiomers, as well as pharmaceutically acceptable salts, hydrates, prodrugs, polymorphs and pseudopolymorphs thereof, to their preparation, to their compositions and to their use.Type: GrantFiled: December 12, 2002Date of Patent: April 12, 2005Assignee: Wockhardt LimitedInventors: Noel John De Souza, Mahesh Vithalbhai Patel, Prasad Keshav Deshpande, Shiv Kumar Agarwal, Kandepu Sreenivas, Sheela Chandrasekharan Nair, Yati Chugh, Milind Chintaman Shukla
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Patent number: 6858613Abstract: The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat conditions or diseases in which ?7 is known to be involved.Type: GrantFiled: February 14, 2003Date of Patent: February 22, 2005Assignee: Pfizer Inc.Inventors: Bruce N. Rogers, David W. Piotrowski, Daniel Patrick Walker, Eric Jon Jacobsen, Brad A. Acker, Donn G. Wishka, Vincent E. Groppi, Jr.
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Patent number: 6849644Abstract: The invention relates to novel tetrahydroquinoline compounds having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of various CNS disorders.Type: GrantFiled: November 16, 2001Date of Patent: February 1, 2005Assignee: SmithKline Beecham p.l.c.Inventors: Steven Mark Bromidge, Stephen Frederick Moss
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Patent number: 6841557Abstract: The treatment of addictive disorders, psychoactive substance use disorders, intoxication disorders, inhalation disorders, alcohol addiction, tobacco addiction, and nicotine addiction using a heterocyclic amine, a phenylazacycloalkane, a cabergoline, or an aromatic bicyclic amine active agent, or a pharmaceutically acceptable derivative or salt of any said active agent is described herein.Type: GrantFiled: August 14, 2001Date of Patent: January 11, 2005Assignee: Pharmacia & UpjohnInventors: Richard W. Anderson, Sylvia S. McBrinn, David W. Robertson, Robert C. Marshall
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Patent number: 6828328Abstract: This invention relates to the combination of muscarinic agonists with narcotic analgesics, non-steroidal anti-inflammatory drugs or other analgesic drugs and to their use as antinociception (pain relief) agents. In particular, the invention relates to a combination of a specific class of M4 selective muscarinic agonists with narcotic analgesics, non-steroidal anti-inflammatory drugs or other analgesic drugs.Type: GrantFiled: March 1, 2002Date of Patent: December 7, 2004Assignee: UCB s.A.Inventors: James Ellis, Fangming Zou
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Patent number: 6815450Abstract: Regenerative growth of an adult mammalian central nervous system neuron axon subject to growth inhibition by endogenous, myelin growth repulsion factors is promoted by delivering to the axon a therapeutically effective amount of a specific inhibitor of protein kinase C, whereby regenerative growth of the axon is promoted and a resultant promotion of the regenerative growth of the axon is detected.Type: GrantFiled: March 14, 2003Date of Patent: November 9, 2004Assignee: Children's Medical Center CorporationInventors: Zhigang He, Vuk Koprivica, Rajeev Sivasankaran
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Publication number: 20040176406Abstract: The present invention provides compounds of formula (I) 1Type: ApplicationFiled: March 15, 2004Publication date: September 9, 2004Inventors: Luca Claudio Gobbi, Thomas Luebbers, Patrizio Mattei, Robert Narquizian, Pierre Charles Wyss
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Publication number: 20040142937Abstract: The present invention provides the use of heterocyclic amine-type compounds to prevent or reduce neuronal damages in patients afflicted with or susceptible to disease states or conditions known to result in or cause neuronal damage.Type: ApplicationFiled: October 21, 2003Publication date: July 22, 2004Inventors: Haiyan Wu, Jo Ann Oostveen, Vimala Hiralal Sethy, Edward Dallas Hall, Robert Bradford McCall
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Publication number: 20040138249Abstract: The present invention relates to pyrrolo[2.1-a]dihydroisoquinolines which are inhibitors of phosphodiesterase 10a and can be used for combating cancer.Type: ApplicationFiled: February 9, 2004Publication date: July 15, 2004Inventors: Ulrich Niewohner, Maria Theresia Niewohner, Marcus Bauser, Jens-Kerim Erguden, Dietmar Flubacher, Paul Nabb, Thorsten-Oliver Repp, Jurgen Stoltefuss, Nils Burkhardt, Andrea Sewing, Michael Schauer, Karl-Heinz Schlemmer, Olaf Weber, Stephen J. Boyer, Mark Miglarese
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Patent number: 6753333Abstract: The invention relates to the new arginine salt forms of S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, a process for their preparation and pharmaceutical formulations which comprise those arginine salt forms as the active ingredient for its use in treating antimicrobial infections.Type: GrantFiled: November 22, 2002Date of Patent: June 22, 2004Assignee: Wockhardt LimitedInventors: Noel J. De Souza, Shivkumar Agarwal, Mahesh V. Patel, Satish B. Bhawsar, Rupinder K. Beri, Ravindra D. Yeole, Nitin Shetty
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Patent number: 6727261Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP-IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.Type: GrantFiled: December 17, 2002Date of Patent: April 27, 2004Assignee: Hoffman-La Roche Inc.Inventors: Luca Claudio Gobbi, Thomas Luebbers, Patrizio Mattei, Robert Narquizian, Pierre Charles Wyss
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Patent number: 6696462Abstract: A compound of formula 1 wherein: X- is an anion with a single negative charge; A and B, which are identical or different, are each —O—, —S—, —NH—, —CH2—, —CH═CH—, or —N(C1-C4-alkyl)—; R is hydrogen, hydroxy, —C1-C4-alkyl, —C1-C4-alkyloxy, —C1-C4-alkylene-halogen, —0—C1-C4-alkylene-halogen, —C1-C4-alkylene-OH, —CF3, —CHF2, —C1-C4-alkylene-C1-C4-alkyloxy, —0—COC1-C4-alkyl, —0—COC1-C4-alkylene-halogen, —C1-C4-alkylene-C3-C6-cycloalkyl, —0—COCF3, or halogen; R1 and R2, which are identical or different, are each —C1-C5-alkyl, which is optionally substituted by —C3-C6-cycloalkyl, hydroxy, or halogen, or R1 and R2 together are a —C3-C5-alkylene bridge; R3, R4, R3′, and R4′, which are identical or different, are each hydrogen, C1-C4-alkyl, C1-C4-alkyloxy, hydroxy, —CF3, —CHF2, &mdasType: GrantFiled: January 16, 2003Date of Patent: February 24, 2004Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Christian Eickmeier, Sabine Germeyer, Matthias Grauert, Sabine Pestel, Michael P. Pieper, Georg Speck, Steffen Breitfelder
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Patent number: 6673781Abstract: The present invention provides a compound having sPLA2 inhibiting activity. The compound represented by the formula (I): wherein R1 is (a) C1 to C20 alkyl, C2 to C20 alkenyl, C2 to C20 alkynyl, carbocyclic groups, heterocyclic groups or the like; R2 is CONH2 or CONHNH2; one of R3 and R4 is —(L2)-(acidic group) wherein L2 is a group connecting with an acid group and the length of the connecting groups 1 to 5 atoms, and the other is a hydrogen atom; its prodrug, their pharmaceutically acceptable salt, or solvate thereof.Type: GrantFiled: February 1, 2002Date of Patent: January 6, 2004Assignee: Shionogi & Co., Ltd.Inventors: Mitsuaki Ohtani, Masahiro Fuji, Tetsuo Okada, Makoto Adachi, Tomoyuki Ogawa
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Patent number: 6664267Abstract: The invention relates to the new arginine salt forms of RS-(±)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, R-(+)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, a process for their preparation and pharmaceutical formulations which comprise those arginine salt forms as the active ingredient for its use in treating microbial infections.Type: GrantFiled: May 28, 2002Date of Patent: December 16, 2003Assignee: Wockhardt LimitedInventors: Noel J. de Souza, Prasad K Deshpande, Milind C. Shukla, Siddiqui M Jaweed Mukarram, Dilip Ganesh Kulkarni, Ansari Azizur Rahman, Ravindra D Yeole, Mahesh V Patel, Shrikant V Gupte
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Patent number: 6664266Abstract: Regenerative growth of an adult mammalian central nervous system neuron axon subject to growth inhibition by endogenous, myelin growth repulsion factors is promoted by delivering to the axon a therapeutically effective amount of a specific inhibitor of protein kinase C, whereby regenerative growth of the axon is promoted and a resultant promotion of the regenerative growth of the axon is detected.Type: GrantFiled: March 14, 2002Date of Patent: December 16, 2003Assignee: Children's Medical Center CorporationInventors: Zhigang He, Vuk Koprivica, Rajeev Sivasankaran
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Publication number: 20030207895Abstract: The invention includes pharmaceutically active compounds and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for treating or prophylaxis of undesired thrombosis.Type: ApplicationFiled: May 23, 2003Publication date: November 6, 2003Applicant: Sunol Molecular CorporationInventors: Jin-An Jiao, Lawrence K. Luepschen, Esperanza L. Nieves, Hing C. Wong, Dean P. Taylor
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Publication number: 20030207908Abstract: The present invention relates to optically pure S-(−)-benzoquinolizlne carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof, substantially free of their R-(+)-isomers, to processes for preparation of the optically pure S-(−)-benzoquinoluzie carboylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof substantlly free of their R-(+)-isomers, and to pharmaceutical compositions comprising the S(+)-benzoquinolizie carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof.Type: ApplicationFiled: May 8, 2000Publication date: November 6, 2003Inventors: Mahesh Vithalbhai Patel, Shivkumar Agarwal, Sreenivas Kandepu, Nitin Shetty, Dilip Jatashankar Upadhyay, Nishith Chandra Chaturvedi, Abraham Thomas, Noel John De Souza, Habil Fakhruddin Khorakiwala
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Publication number: 20030191150Abstract: A process for easily and industrially advantageously producing both a tricyclic fused heterocyclic derivative having acetylcholinesterase inhibitory activity and an intermediate for the derivative. The process for producing the target compounds comprises the following reaction.Type: ApplicationFiled: March 20, 2003Publication date: October 9, 2003Inventors: Tadao Kawarasaki, Hideo Hashimoto, Kiminori Tomimatsu
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Patent number: 6630482Abstract: CFTR channel activator compounds from the benzo[c]quinolizinium family or families of compounds derived therefrom, as well as pharmaceutical compositions containing said compounds, and the uses thereof, particularly for treating cystic fibrosis, are disclosed.Type: GrantFiled: March 2, 1999Date of Patent: October 7, 2003Assignee: Centre National de la Recherche ScientifiqueInventors: Frédéric Becq, Yvette Mettey, Jean-Michel Vierfond, Bernard Verrier, Maurice Gola
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Patent number: 6624159Abstract: The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.Type: GrantFiled: June 22, 2001Date of Patent: September 23, 2003Assignee: Pharmacia & Upjohn CompanyInventors: David John Anderson, Gordon L. Bundy, Fred L. Ciske, David R. Graber, Michael J. Genin, Thomas M. Judge, Malcolm Wilson Moon, Mark E. Schnute, Joseph Walter Strohbach, Suvit Thaisrivongs, Atli Thorarensen, Steven Ronald Turner, Valerie A. Vaillancourt, Allison J. Wolf
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Patent number: 6610685Abstract: The present invention is a chemical compound of formula (I) or a pharmaceutically acceptable salt, solvate and ester thereof, wherein R1 to R4 and n are as defined in the specification. A compound of formula 1 is useful as a pharmaceutical composition for the treatment or prevention of disorders of the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes, obesity and sleep apnoea.Type: GrantFiled: December 14, 2001Date of Patent: August 26, 2003Assignees: Hoffmann-La Roche Inc., Vernalis Research LimitedInventors: Jonathan Mark Bentley, Michael John Bickerdike, Paul Hebeisen, Guy Anthony Kennett, Sean Lightowler, Patrizio Mattei, Jacques Mizrahi, Timothy James Morley, Jean-Marc Plancher, Hans Richter, Stephan Roever, Sven Taylor, Steven Paul Vickers
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Patent number: 6608078Abstract: The present invention relates to optically pure 8-(substituted piperidino)-benzo[i,j]quinolizines, their isomers, derivatives, salts, pseudopolymorphs, polymorphs prodrugs and hydrates thereof, to processes for their preparation, and to pharmaceutical compositions comprising 8-(substituted piperidino)-benzo[i,j]quinolizines their isomers, derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof. These compounds and compositions possess potent activity in treating local and systemic infections, particularly infections caused by sensitive and resistant Gram-positive organism infections, Gram-negative organism infections, mycobacterial infections and nosocomial pathogens, and particularly those belonging to the staphylococcus, streptococcus and enterococcus groups. Methods for treating the diseases and disorders arising from the foregoing infections in humans and animals are described by administering the compounds of the invention to said humans and animals.Type: GrantFiled: May 7, 2001Date of Patent: August 19, 2003Assignee: Wockhardt LimitedInventors: Noel John De Souza, Mahesh Vithalbhai Patel, Shiv Kumar Agarwal, Shirkant V Gupte, Dilip J Upadhyay, Satish B Bhawsar, Mohammad A Jafri
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Publication number: 20030153561Abstract: The present invention provides a compound of formula I 1Type: ApplicationFiled: November 5, 2002Publication date: August 14, 2003Inventors: Valerie A. Vaillancourt, Sandra Staley, Audris Huang, Richard Allen Nugent, Ke Chen, Sajiv K. Nair, James A. Nieman, Joseph Walter Strohbach
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Publication number: 20030149071Abstract: The present invention provides compounds of formula (I) 1Type: ApplicationFiled: December 17, 2002Publication date: August 7, 2003Inventors: Luca Claudio Gobbi, Thomas Luebbers, Patrizio Mattei, Robert Narquizian, Pierre Charles Wyss
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Patent number: 6602868Abstract: The invention provides methods and use of heterocyclic amines, and phenylazacycloalkane compounds, and their pharmacologically acceptable salts for the treatment of Restless Legs Syndrome (RLS).Type: GrantFiled: October 29, 2001Date of Patent: August 5, 2003Assignee: Pharmacia & Upjohn CompanyInventors: Sylvia McBrinn, Richard Wayne Anderson
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Patent number: 6576259Abstract: Sustained release formulation containing tacrolimus or its hydrate is provided. The time (T63.2%) required for 63.2% of the maximum amount of tacrolimus or its hydrate to be dissolved is 0.7 to 15 hours. The time is measured in accordance to the Japanese Pharmacopoeia, the 13-th edition, Dissolution Test, No. 2 (Puddle method, 50 rpm) using an aqueous 0.005% hydroxypropyl cellulose solution. This aqueous test solution is adjusted to pH 4.5, accordingly. The formulation further comprise a solid base which is a water-soluble polymer and/or wax. The formulation is in the form of a powder, fine powder, granule, tablet or capsule. Furthermore, the formulation is administered to a patient once a day for preventing organ or tissue rejection by transplantation or autoimmune diseases.Type: GrantFiled: October 17, 2001Date of Patent: June 10, 2003Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kazunari Yamashita, Eiji Hashimoto, Yukihiro Nomura, Fumio Shimojo, Shigeki Tamura, Takeo Hirose, Satoshi Ueda, Takashi Saitoh, Rinta Ibuki, Toshio Ideno
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Patent number: 6555550Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof useful in the treatment of pain. The compounds of the present invention are azaadamantanes, azanoradamantanes and azahomoadamantanes.Type: GrantFiled: March 27, 2002Date of Patent: April 29, 2003Assignee: UCB, S. A.,Inventors: Gurmit Grewal, Anna Toy-Palmer, Xiong Cai, George Mark Latham
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Patent number: 6555549Abstract: The present invention refers to benzo[c]quinolizine derivatives of general formula (I) their pharmaceutically acceptable salts or esters, processes for their preparation and pharmaceutical compositions containing them.Type: GrantFiled: June 25, 2001Date of Patent: April 29, 2003Assignee: Applied Research Systems ARS Holding N.V.Inventors: Antonio Guarna, Mario Serio