Spiro Patents (Class 544/6)
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Publication number: 20110118461Abstract: The present invention relates to a process for the preparation of Brinzolamide, or 2H-thieno[3,2-e]-1, 2-thiazin-6-sulfonamide, 4-(ethyl amino)-3, 4-dihydro-2-(3-methoxypropyl)-, 1,1-dioxide,(4R)- via intermediates 2,3-dihydro-4H-thieno[3,2-e]-1, 2-thiazin-4-ones, 1,1-dioxide. Further objects of the present invention are the intermediates mentioned above and other intermediates of the synthesis.Type: ApplicationFiled: June 15, 2009Publication date: May 19, 2011Inventors: Alessandro Falchi, Ottorino De Lucchi, Andrea Castellin
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BENZENESULFONYL-CHROMANE, THIOCHROMANE, TETRAHYDRONAPHTHALENE AND RELATED GAMMA SECRETASE INHIBITORS
Publication number: 20110110948Abstract: Disclosed are novel gamma secretase inhibitors of the formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, wherein L1, n, X, Ar, Y, Z, Q, and Q1 are as defined herein. Also disclosed are methods for inhibiting gamma secretase, methods for treating Alzheimer's disease, methods of treating one or more neurodegenerative diseases, and methods of inhibiting the deposition of amyloid protein (e.g., amyloid beta protein) in, on or around neurological tissue (e.g., the brain) using the compounds of formula 1.0.Type: ApplicationFiled: July 15, 2008Publication date: May 12, 2011Applicant: SCHERING CORPORATIONInventors: Thavalakulamgara K. Sasikumar, Duane A. Burnett, Theodros Asberom, Wen-Lian Wu, Hongmei Li, Ruo Xu, Hubert B. Josien -
Publication number: 20110105484Abstract: A compound, its pharmaceutically acceptable salt, a composition containing the same and method of treatment that can provide analgesia and/or reduce inflammation are disclosed. A contemplated compound has a structure that corresponds to Formula A, wherein G, W, Q, Z, D, E, F, K, Y, d, e, f, k, n, m, and circle B and all R groups are defined within.Type: ApplicationFiled: October 30, 2009Publication date: May 5, 2011Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
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Publication number: 20110105481Abstract: A compound or its pharmaceutically acceptable salt, optionally including both individual enantiomeric forms, a racemate, diastereomers and mixtures thereof, composition and method are disclosed that can provide analgesia and reduce inflammation. A contemplated compound has a structure that corresponds to Formula A, wherein the R group substituents, d, e, f, k, n, m, D, E, F, K, G, P, Q, W, and Z are defined within.Type: ApplicationFiled: March 8, 2010Publication date: May 5, 2011Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
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Publication number: 20110092529Abstract: The present invention relates to a class of substituted triazoles of formula (I) with activity as oxytocin antagonists, uses thereof, processes for the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction, particularly premature ejaculation (P.E.).Type: ApplicationFiled: January 6, 2006Publication date: April 21, 2011Inventors: Alan Daniel Brown, Andrew Antony Calabrese, David Ellis
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Publication number: 20110071126Abstract: The present invention is directed to a compound represented by the following structural formula or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions and method of use of the compounds are also described.Type: ApplicationFiled: March 12, 2010Publication date: March 24, 2011Inventors: Salvacion CACATIAN, David A. CLAREMON, Lawrence W. DILLARD, Klaus FUCHS, Niklas HEINE, Lanqi JIA, Katerina LEFTHERIS, Brian McKEEVER, Angel MORALES-RAMOS, Suresh B. SINGH, Shankar VENKATRAMAN, Guosheng WU, Zhongren WU, Zhenrong XU, Jing YUAN, Yajun ZHENG
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Publication number: 20110053912Abstract: A novel and excellent method for preventing and/or treating diseases related to a cannabinoid type 2 receptor, based on an agonistic action on a cannabinoid type 2 receptor. It was found that a hetero ring derivative mainly having two substituents, for example, a pyrimidine-5-carboxamide derivative having a substituent amino group at the 2-position, exhibits a potent agonistic action on a cannabinoid type 2 receptor, and can be an agent for preventing and/or treating diseases related to a cannabinoid type 2 receptor such as inflammatory diseases, pain, and the like.Type: ApplicationFiled: March 29, 2010Publication date: March 3, 2011Applicant: Astellas Pharma Inc.Inventors: Yuji Matsushima, Hirokazu Kubota, Hisao Hamaguchi, Yoshinori Okamoto, Takeshi Hondo, Fusako Nishigaki
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Publication number: 20110009624Abstract: The present invention provides a compound that has superior gastric acid secretion inhibitory action, ample long-lasting gastric acid secretion inhibitory action, and is able to maintain intragastric pH at a high level for an extended period of time, making it useful as a therapeutic or prophylactic agent for diseases or symptoms caused by gastric acid, as well as an active form of this compound (form to which the compound is converted in the body following administration thereof) in the form of a compound represented by general formula (1a) (wherein R2 represents a group represented by formula (I) or the like, and R1, R3, W1 and X? are as defined in the description).Type: ApplicationFiled: October 11, 2007Publication date: January 13, 2011Inventors: Masato Ueda, Daisuke Iida, Sachiko Kikuchi, Masaharu Gotoda
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Patent number: 7863268Abstract: Disclosed are benzothiazin derivatives of formula (I), preparation methods therefore, and treatment methods employing such compounds as antibacterial agents in treating infectious diseases of mammals caused by bacteria, especially diseases like tuberculosis and leprosy caused by mycobacteria: wherein R1, R2, R3, R4, R5, and R6, and other variables enumerated under one or more of R1, R2, R3, R4, R5, and R6 are as defined.Type: GrantFiled: May 24, 2006Date of Patent: January 4, 2011Assignee: Alere InternationalInventors: A. Vadim Makarov, Stewart T. Cole, Ute Moellmann
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Publication number: 20100311734Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, for treating diseases and conditions of the central nervous system (CNS), in particular sleep disorders.Type: ApplicationFiled: July 24, 2008Publication date: December 9, 2010Inventors: Maurizio Botta, Emiliano Castiglioni, Romano Di Fabio, Raffaella Spinosa, Andrea Togninelli
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Publication number: 20100280241Abstract: The present invention can provide new spirooxazine radical derivatives of the following general formula (1) which have chromic property enabling the distinction between the radical species and the cation species on the basis of absorption wavelength:Type: ApplicationFiled: December 20, 2007Publication date: November 4, 2010Inventor: Atsumasa Sawada
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Publication number: 20100261641Abstract: The present invention relates to a spiro-piperidine compound represented by formula (I): wherein R1 represents hydrogen, an aliphatic hydrocarbon group which may have a substituent(s) or a cyclic group which may have a substituent(s); and ring A represents a 5- to 8-membered cyclic group which may have a substituent(s), a salt thereof, an N-oxide thereof, a quaternary ammonium salt thereof or a solvate thereof, or a prodrug thereof. The compounds represented by formula (I) have chemokine antagonistic action, so that they are useful for prevention and/or treatment of various inflammatory diseases, immune diseases such as autoimmune diseases or allergic diseases, or HIV infection.Type: ApplicationFiled: December 11, 2008Publication date: October 14, 2010Applicant: Ono Pharmaceutical Co., Ltd.Inventors: Rena Nishizawa, Yoshikazu Takaoka, Hiromu Habashita, Shiro Shibayama, Masaya Kokubo
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Publication number: 20100234363Abstract: Disclosed is a compound which is useful as an 11?-hydroxysteroid dehydrogenase type 1 inhibitor.Type: ApplicationFiled: September 17, 2008Publication date: September 16, 2010Applicants: INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC., SHIONOGI & CO., LTD.Inventors: Akiko Itai, Susumu Muto, Ryuko Tokuyama, Hiroshi Fukasawa, Takeshi Yanase
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Publication number: 20100113436Abstract: A compound having the formula (I) wherein ring A represents a substituted or unsubstituted monocyclic or multicyclic ring; m=any positive integer; n=0-5; X=CH and Y=—C(O)NR1R2, —NR1R2 or —S(O)2R4, where R1, R2 and R4 are each individually selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted amine, substituted or unsubstituted carbocyclic ring, substituted or unsubstituted heterocyclic ring, or any combination thereof, or R1 and R2 are linked so as to form part of a substituted or unsubstituted heterocyclic ring, or X=N and Y=—S(O)2R3 or —C(O)R3, where R3 is selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted amine, substituted or unsubstituted carbocyclic ring, substituted or unsubstituted heterocyclic ring or any combination thereof.Type: ApplicationFiled: October 1, 2007Publication date: May 6, 2010Inventors: Richard Amewu, Paul Micheal O'Neill, Andrew Stachulski, Gemma Ellis, Stephen Andrew Ward
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Publication number: 20100056498Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, m, n, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.Type: ApplicationFiled: November 9, 2009Publication date: March 4, 2010Inventors: Michael R. Wood, Steven N. Gallicchio, Harold G. Selnick, C. Blair Zartman, Ian M. Bell, Craig A. Stump
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Publication number: 20090292120Abstract: The present invention provides a compound that has superior gastric acid secretion inhibitory action, ample long-lasting gastric acid secretion inhibitory action, and is able to maintain intragastric pH at a high level for an extended period of time, making it useful as a therapeutic or prophylactic agent for diseases or symptoms caused by gastric acid, as well as an active form of this compound (form to which the compound is converted in the body following administration thereof) in the form of a compound represented by general formula (1a) (wherein R2 represents a group represented by formula (I) or the like, and R1, R3, W1 and X? are as defined in the description).Type: ApplicationFiled: October 11, 2007Publication date: November 26, 2009Inventors: Masato Ueda, Daisuke Iida, Sachiko Kikuchi, Masaharu Gotoda
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Patent number: 7595313Abstract: The invention describes novel compositions and kits comprising at least one nitric oxide enhancing diuretic compound, or pharmaceutically acceptable salts thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating conditions resulting from excessive water and/or electrolyte retention; (b) treating cardiovascular diseases; (c) treating renovascular diseases; (d) treating diabetes; (e) treating diseases resulting from oxidative stress; (f) treating endothelial dysfunctions; (g) treating diseases caused by endothelial dysfunctions; (h) treating cirrhosis; (j) treating pre-eclampsia; (k) treating osteoporosis; (l) treating nephropathy; (m) treating peripheral vascular diseases; (n) treating portal hypertension; (o) treating central nervous system disorders; (p) treating metabolic syndrome; (q) treating sexual dysfunctions; and (r) hyperlipidemia.Type: GrantFiled: June 10, 2008Date of Patent: September 29, 2009Assignee: NicOx, S.A.Inventors: David S. Garvey, L. Gordon Letts, Richard A. Earl, Maiko Ezawa, Xinqin Fang, Ricky D. Gaston, Subhash P. Khanapure, Chia-En Lin, Ramani R. Ranatunge, Cheri A. Stevenson, Shiow-Jyi Wey
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Publication number: 20090239851Abstract: The present invention relates to novel benzothiazin derivatives and their use as antibacterial agents in infectious diseases of mammals (humans and animals) caused by bacteria, especially diseases like tuberculosis (TB) and leprosy caused by mycobacteria. The present invention aims at the generation of new compounds with activity against mycobacteria as potential new tuberculosis drugs to overcome problems concerning resistance and drug intolerance.Type: ApplicationFiled: May 24, 2006Publication date: September 24, 2009Inventors: A. Vadim Makarov, Stewart T. Cole, Ute Möllmann
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Publication number: 20090192145Abstract: Novel heterocyclic compounds of the general formula (I) and salts, preferably pharmaceutically acceptable salts, thereof, in which R, R1, R1?, Q, m and n have the meanings explained in detail in the description, a process for their preparation and the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.Type: ApplicationFiled: April 12, 2007Publication date: July 30, 2009Applicant: SPEEDEL EXPERIMENTA AGInventors: Peter Herold, Robert Mah, Vincenzo Tschinke, Aleksandar Stojanovic, Christiane Marti, Christiane Marti, Stjepan Jelakovic, Bibia Bennacer, Stefan Stutz
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Publication number: 20090186882Abstract: The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions.Type: ApplicationFiled: January 21, 2009Publication date: July 23, 2009Inventors: Corey Don Anderson, Andreas P. Termin, Pramod Joshi, Sara S. Hadida Ruah, Daniele Bergeron, Sanghee Yoo
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Publication number: 20090131418Abstract: The present invention relates to spiroazacyclic compounds as monoamine receptor modulators; compositions comprising the same; methods of inhibiting an activity of a monoamine receptor with said compounds; methods of treating a disease condition associated with a monoamine receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.Type: ApplicationFiled: January 27, 2009Publication date: May 21, 2009Applicant: ACADIA PHARAMCEUTICALS, INC.Inventor: Nathalie Schlienger
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Patent number: 7511034Abstract: Novel dialkylhydroxybenzoic acid derivatives containing metal chelating groups are disclosed. The novel compounds are used as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species and/or excess Zn ions, in particular stroke, Parkinson's disease, Alzheimer's disease. The compounds have not only low toxicity but also similar or superior LPO inhibition activity to references. They also effectively inhibit the cerebral neuronal cell death by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.Type: GrantFiled: January 11, 2006Date of Patent: March 31, 2009Assignee: Samsung Electronics Co., Ltd.Inventors: Eu-Gene Oh, Sung-Bo Ko, Kyung-Hwa Kim, In-Kyu Chang, Dennis W. Choi, Laura L. Dugan, Jae-Young Koh, In-Jae Shin, Moo-Ho Won
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Patent number: 7494990Abstract: The compounds of a certain formula (1), in which R1, R2, R3 and R9 have the meanings as given in the description, are novel effective PDE4 inhibitors.Type: GrantFiled: February 1, 2005Date of Patent: February 24, 2009Assignee: NYCOMED GmbHInventors: Wiro M. P. B. Menge, Geert Jan Sterk
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Patent number: 7482339Abstract: The formula (I): wherein each of R2 and R3 is, same or different, C2-C4 alkyl or the like; or R2 and R3 are taken together with the adjacent carbon atom to form a 5 to 8 membered non-aromatic carbocyclic ring; R4 is C1-C6 alkyl or the like; X is an oxygen atom or a sulfur atom; A is the group of the formula: wherein R1 is, same or different, alkyl or the like; W is C2-C6 alkylene which may contain an optionally substituted heteroatom(s) or the like; n is an integer of 0 to 7, a pharmaceutically acceptable salt, or a solvate thereof.Type: GrantFiled: August 24, 2004Date of Patent: January 27, 2009Assignee: Shionogi and Co., Ltd.Inventors: Hiroyuki Kai, Yasuhide Morioka, Katsumi Koike
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Publication number: 20080255101Abstract: The invention describes novel compositions and kits comprising at least one nitric oxide enhancing diuretic compound, or pharmaceutically acceptable salts thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating conditions resulting from excessive water and/or electrolyte retention; (b) treating cardiovascular diseases; (c) treating renovascular diseases; (d) treating diabetes; (e) treating diseases resulting from oxidative stress; (f) treating endothelial dysfunctions; (g) treating diseases caused by endothelial dysfunctions; (h) treating cirrhosis; (j) treating pre-eclampsia; (k) treating osteoporosis; (l) treating nephropathy; (m) treating peripheral vascular diseases; (n) treating portal hypertension; (o) treating central nervous system disorders; (p) treating metabolic syndrome; (q) treating sexual dysfunctions; and (r) hyperlipidemia.Type: ApplicationFiled: June 10, 2008Publication date: October 16, 2008Applicant: NITROMED, INC.Inventors: David S. GARVEY, L. Gordon LETTS, Richard A. EARL, Maiko EZAWA, Xinqin FANG, Ricky D. GASTON, Subhash P. KHANAPURE, Chia-En LIN, Ramani R. RANATUNGE, Cheri A. STEVENSON, Shiow-Jyi WEY
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Publication number: 20080139540Abstract: Naphthyridine and related derivatives useful in the treatment of bacterial infections, particularly humans, are disclosed herein.Type: ApplicationFiled: January 24, 2006Publication date: June 12, 2008Applicant: Glaxo Group LimitedInventors: William Henry Miller, Meagan B. Rouse, Mark Andrew Seefeld
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Publication number: 20080125411Abstract: A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites. The compounds of the invention unexpectedly provide a single-dose cure for malaria, as well as prophylactic activity against the same. The compounds are also active against schistosomiasis and cancer.Type: ApplicationFiled: October 31, 2007Publication date: May 29, 2008Applicant: MEDICINES FOR MALARIA VENTURE MMVInventors: JONATHAN L. VENNERSTROM, YUXIANG DONG, SUSAN A. CHARMAN, SERGIO WITTLIN, JACQUES CHOLLET, DARREN J. CREEK, XIAOFANG WANG, KAMARAJ SRIRAGHAVAN, LIN ZHOU, HUGUES MATILE, WILLIAM N. CHARMAN
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Patent number: 7199118Abstract: This invention relates to novel benzothiazine derivatives of Formula I useful as modulators of the AMPA sensitive glutamate receptors, pharmaceutical compositions comprising such compounds and their use in therapy.Type: GrantFiled: October 2, 2002Date of Patent: April 3, 2007Assignee: NeuroSearch A/SInventors: Alex Haahr Gouliaev, Morgens Larsen, Thomas Varming, Claus Mathiesen, Tina Holm Johansen, Karin Sandager Nielsen, Barbara Hartz, Jorgen Scheel-Kruger
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Patent number: 7122662Abstract: This invention relates to tricyclic compounds having spiro union represented by the following formula (I) or its salt which is useful as a drug, and in particular, as an inhibitor for activated blood coagulation factor X, which can be administered orally and which exhibits strong anticoagulation action. The invention also relates to a pharmacophore which was derived from the compound and is useful in molecular designing of the FXa inhibitor.Type: GrantFiled: December 16, 2004Date of Patent: October 17, 2006Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Hidemitsu Nishida, Fumihiko Saitoh, Kousuke Harada, Ikuya Shiromizu, Takafumi Mukaihira
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Patent number: 7001910Abstract: The present invention refers to compounds of the general formula (I), to their possible pharmaceutically acceptable salts and tautomeric forms. The present invention also refers to a process for their production and to their use as antidiabetic and *hypoglycemic agents, alone or in combination with other antidiabetic agents, such as sulfonilureas or biguanides, as well as for the treatment of complications associated to the resistance to the insulin, such as hypertension, hyperuricemia or other cardiovascular, metabolic, endocrine conditions, or other conditions related with diabetes.Type: GrantFiled: November 15, 2000Date of Patent: February 21, 2006Assignee: Vita-Invest S.A.Inventors: Marisabel Mourelle Mancini, Juan Carlos Del Castillo Nieto, Elisabet De Ramon Amat
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Patent number: 6916807Abstract: The present invention relates to triaryl-oxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein said ring X is a 5-7 membered heterocyclic ring, and wherein A, Y, B, G, and W are as defined in the specification; and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.Type: GrantFiled: April 25, 2003Date of Patent: July 12, 2005Assignee: Pfizer Inc.Inventors: Kevin D. Freeman-Cook, Mark C. Noe
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Patent number: 6916806Abstract: A compound of the formula (I) having a binding activity to the cannabinoid type 2 receptor: wherein R1 is optionally substituted heterocyclic group or the like; R2 and R2 each is independently hydrogen or the like; m is an integer of 0 to 2; A is optionally substituted aromatic carbocyclic group or the like.Type: GrantFiled: February 14, 2002Date of Patent: July 12, 2005Assignee: Shionogi & Co., Ltd.Inventors: Hiroyuki Kai, Takami Murashi, Minoru Tomida
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Patent number: 6900201Abstract: The present invention relates to N-substituted-heteroaryloxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein ring X is a 5-7 membered heterocyclic ring, and wherein A, Y, B, and G are as defined in the specification; and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.Type: GrantFiled: April 25, 2003Date of Patent: May 31, 2005Assignee: Pfizer Inc.Inventors: Mark C. Noe, Kevin Freeman-Cook
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Patent number: 6849732Abstract: The invention relates to compounds of the formula 1: wherein: Z is O or S; V is a divalent radical which together with C* and N forms a ring having six ring atoms, where each of said ring atoms other than C* and N independently is unsubstituted or substituted by a suitable substituent, and at least one of said other ring atoms is a heteroatom selected from O, N and S, and the remainder are carbon atoms; and Ar is an aryl or heteroaryl group; and pharmaceutically acceptable prodrugs, salts and solvates thereof. The invention further relates to pharmaceutically acceptable prodrugs, salts and solvates of these compounds. The invention also relates to methods of inhibiting the activity of metalloproteinases by administering a compound of the formula I or a prodrug, salt or solvate thereof. The invention further relates to pharmaceutical compositions comprising an effective amount of these compounds, prodrugs, salts, and solvates.Type: GrantFiled: November 18, 2002Date of Patent: February 1, 2005Assignee: Agouron Pharmaceuticals, Inc.Inventors: Scott E. Zook, Raymond Dagnino, Jr., Michael E. Deason, Steven L. Bender, Michael J. Melnick
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Patent number: 6756371Abstract: The compounds of formula (I) in which R1, R2, A, B and Ar have the meanings as given in the description are novel effective PDe4 inhibitorsType: GrantFiled: April 12, 2002Date of Patent: June 29, 2004Assignee: Altana Pharma AGInventor: Geert Jan Sterk
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Patent number: 6743798Abstract: The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which R1, R2, R3 and A are each as defined, and to processes for their preparation and to their use as medicaments, in particular as medicaments for the treatment of cardiovascular disorders.Type: GrantFiled: April 11, 2001Date of Patent: June 1, 2004Assignee: Bayer AktiengesellschaftInventors: Alexander Straub, Achim Feurer, Cristina Alonso-Alija, Johannes-Peter Stasch, Elisabeth Perzborn, Joachim Hütter, Klaus Dembowsky, Elke Stahl
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Patent number: 6683709Abstract: Photochromic pyran compounds and their use in synthetic resin objects of all types, especially for ophthalmic applications, particularly spiro compounds having a fluorene structure derived from naphthopyrans, which are known as spirofluorenopyrans. By introducing respectively only one strongly electron donating or withdrawing group at specific positions in the periphery of the pyran dye, photochromic compounds obtained which in the excited state are distinguished by an expanded color spectrum, while simulataneously offering comparably good bleaching rates and good durability.Type: GrantFiled: February 7, 2002Date of Patent: January 27, 2004Assignee: Rodenstock GmbHInventors: Claudia Mann, Udo Weigand, Manfred Melzig
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Publication number: 20040009976Abstract: This invention relates to certain novel imidazoline compounds and analogues thereof, to their use for the treatment of diabetes, diabetic complications, metabolic disorders, or related diseases where impaired glucose disposal is present, to pharmaceutical compositions comprising them, and to processes for their preparation.Type: ApplicationFiled: April 30, 2002Publication date: January 15, 2004Inventors: Kumiko Takeuchi, Michael Robert Jirousek, Michael Paal, Gerd Ruhter, Theo Schotten
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Patent number: 6667306Abstract: The invention relates to novel compounds of formula (I) containing fused heterocyclic ring systems which are effective platelet ADP receptor inhibitors: In formula (I), W is carbon or nitrogen, wherein at least one W is a carbon; and Y is nitrogen, oxygen, or sulfur. Such compounds including pharmaceutically acceptable salts are useful in various pharmaceutical compositions for the prevention and/or treatment of cardiovascular disease particularly those related to thrombosis.Type: GrantFiled: January 7, 1999Date of Patent: December 23, 2003Assignee: Millennium Pharmaceuticals, Inc.Inventors: Alan M. Laibelman, Hans-Michael Jantzen, Pamela B. Conley, Larry J. Fretto, Robert M. Scarborough
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Publication number: 20030225056Abstract: The present invention relates to triaryl-oxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula 1Type: ApplicationFiled: April 25, 2003Publication date: December 4, 2003Applicant: Pfizer Inc.Inventors: Kevin D. Freeman-Cook, Mark C. Noe
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Publication number: 20030064978Abstract: There are provided novel compounds of formula (I) wherein R1, R2, R3, R4 and R5 are as defined in the Specification and optical isomers, racemates and tautomers thereof and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme nitric oxide synthase.Type: ApplicationFiled: August 9, 2002Publication date: April 3, 2003Inventors: Christopher Walpole, Hua Yang
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Publication number: 20020198198Abstract: The invention provides compounds which are PDE7inhibitors, having the following formula (I), (II) and (III) 1Type: ApplicationFiled: March 19, 2002Publication date: December 26, 2002Inventors: Patrick Bernardelli, Pierre Ducrot, Edwige Lorthiois, Fabrice Vergne
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Patent number: 6472398Abstract: Certain novel spiropiperidine derivatives of structural formula Ia wherein the substituents are as defined herein are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: March 20, 2001Date of Patent: October 29, 2002Assignee: Merck & Co., Inc.Inventors: Brenda L. Palucki, Ravi P. Nargund
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Patent number: 6451804Abstract: The invention provides compounds represented by the formula: wherein R1, R2, R3, R4, and n are as defined in the Summary of the Invention; and individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.Type: GrantFiled: October 20, 2000Date of Patent: September 17, 2002Assignee: Syntex (U.S.A.) LLCInventors: James Patrick Dunn, Lawrence Emerson Fisher, David Michael Goldstein, William Harris, Christopher Huw Hill, Ian Edward David Smith, Teresa Rosanne Welch
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Patent number: 6444819Abstract: Disclosed are compounds of the formula: or pharmaceutically acceptable addition salts thereof wherein: Y represents oxygen or sulfur; Z is nitrogen or CH; R1, R2 and R3 independently represent organic or inorganic substituents; R4 and R4′ independently represent hydrogen, alkyl or form a ring with the atom to which they are attached; R5 represents hydrogen, alkyl, alkoxy, or alkylthio, and R6 represents hydrogen or alkyl; or R5 and R6 form a ring together with the atoms to which they are attached; and R7, R8, R9, R10, and R11 independently represent hydrogen or alkyl, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.Type: GrantFiled: October 11, 2001Date of Patent: September 3, 2002Assignee: Neurogen CorporationInventors: Renata Xavier Kover, Salva Terdjanian, Jennifer Tran, Andrew Thurkauf
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Patent number: 6407232Abstract: The invention relates an ionic metal complex represented by the general formula (1): wherein M is an element of groups 3-15 of the periodic table; Aa+ represents a metal ion, onium ion or proton; X1 represents O, S or NR5R6; each of R1 and R2 independently represents H, a halogen, a C1-C10 alkyl group or C1-C10 halogenated alkyl group; R3 represents a C1-C10 alkylene group, C1-C10 halogenated alkylene group, C4-C20 aryl group or C4-C20 halogenated aryl group; R4 represents a halogen, C1-C10 alkyl group, C1-C10 halogenated alkyl group, C4-C20 aryl group, C4-C20 halogenated aryl group or X2R7; X2 represents O, S or NR5R6; each of R5 and R6 represents H or a C1-C10 alkyl group; and R7 represents a C1-C10 alkyl group, C1-C10 halogenated alkyl group, C4-C20 aryl group or C4-C20 halogenated aryl group. The ionic metal complex can be used as a supporting electrolyte for electrochemical devices, a polymerization catalyst of polyolefins and so forth, or a catalyst for organic synthesis.Type: GrantFiled: July 25, 2000Date of Patent: June 18, 2002Assignee: Central Glass Company, LimitedInventors: Shoichi Tsujioka, Hironari Takase, Mikihiro Takahashi
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Publication number: 20020068737Abstract: This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: ApplicationFiled: December 14, 2001Publication date: June 6, 2002Applicant: Synaptic Pharamceutical CorporationInventors: Bharat Lagu, Dhanapalan Nagarathnam, Dake Tian, Charles Gluchowski
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Patent number: 6369057Abstract: Compounds of the formula I or Ia in which n and the substituents R1, R5 and x have the meaning mentioned have an antiviral activity.Type: GrantFiled: April 7, 1995Date of Patent: April 9, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Uta-Maria Billhardt, Manfred Rösner, Günther Riess, Irvin Winkler, Rudolf Bender
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Patent number: 6191127Abstract: Compounds of Formula I wherein X and R1-6, are as defined herein, tautomeric forms thereof, and isomeric forms thereof, and salts thereof, are suitable for treating diseases that are induced by the action of nitrogen monooxide at pathological concentration. Such diseases include neurodegenerative diseases, inflammatory diseases, auto-immune diseases, and cardiovascular diseases.Type: GrantFiled: November 1, 1999Date of Patent: February 20, 2001Assignee: Schering AktiengesellschaftInventors: Peter Holscher, Hartmut Rehwinkel, Detlev Suelzle, Gerardine Burton, Margrit Hillmann, Iris Pribilla, David Daniel Davey
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Patent number: 6100246Abstract: There are provided novel compounds of formula (I) ##STR1## wherein A represents a benzo ring; a six membered heterocyclic aromatic ring containing 1 to 3 nitrogen atoms; or a five membered heterocyclic aromatic ring containing 1 to 3 heteroatoms which may be the same or different and are selected from O, N and S; and R.sup.1, R.sup.2, R.sup.3 and X are as defined in the Specification and pharmaceutically acceptable salts thereof and enantiomers and tautomers thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment and prophylaxis of inflammatory disease and pain.Type: GrantFiled: May 8, 1999Date of Patent: August 8, 2000Assignee: Astra Pharmaceuticals LimitedInventors: Peter Richard Hamley, Thomas McInally, Alan Charles Tinker