Chalcogen In The Hetero Ring Patents (Class 540/488)
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Patent number: 7772224Abstract: The present invention is directed to compounds of Formula I: and Formula II: (where variables R1, R2, R3, R4, A, B, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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: GrantFiled: April 3, 2009Date of Patent: August 10, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Daniel V. Paone, Anthony W. Shaw
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Patent number: 7732435Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them.Type: GrantFiled: December 5, 2006Date of Patent: June 8, 2010Assignee: Novartis AGInventors: Andrew James Culshaw, Christopher Thomas Brain, Edward Karol Dziadulewicz, Lee Edwards, Terance William Hart, Timothy John Ritchie
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Patent number: 7671195Abstract: A dibenzothiazepine compound is suitably prepared by subjecting a 2-amino-2?-carboxy-diphenylsulfide compound to dehydration-condensation reaction in the presence of an acidic catalyst; the 2-amino-2?-carboxy-diphenylsulfide compound is suitably prepared by reducing a 2-nitro-2?-carboxy-diphenylsulfide compound in a lower aliphatic ester solvent; and the 2-nitro-2?-carboxy-diphenylsulfide compound is suitably prepared by reacting a nitrobenzene compound with a thiosalicylic acid compound in a mixture of a lower aliphatic alcohol and water.Type: GrantFiled: February 21, 2007Date of Patent: March 2, 2010Assignees: AstraZeneca UK Limited, UBE Industries, Ltd.Inventors: Paul Michael Murray, Luis-Manuel Vaz, Debra Ainge, Katsumasa Harada, Shigeyoshi Nishino, Kiyotaka Yoshii
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Publication number: 20100041637Abstract: This invention relates to novel compounds of the Formula (I), (I*), (I**), I, Ia, Ib, Ic, Id, Ie, If, Ig, Il1-3, Im1-3, In1-3, or Io1-2, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.Type: ApplicationFiled: August 11, 2009Publication date: February 18, 2010Applicant: Vitae Pharmaceuticals, Inc.Inventors: David A. Claremon, Linghang Zhuang, Colin M. Tice, Suresh B. Singh, Yuanjie Ye, Wei Zhao, Katerina Leftheris
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Publication number: 20100034813Abstract: Disclosed are new substituted pyrazole and triazole compounds of Formula (I) and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses thereof:Type: ApplicationFiled: November 8, 2007Publication date: February 11, 2010Inventors: Yi Xia, Kris G. Mendenhall, Paul A. Barsanti, Annette O. Walter, David Duhl, Paul A. Renhowe
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Patent number: 7659300Abstract: The present invention is directed to compounds of Formula I: I (where A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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: GrantFiled: September 6, 2005Date of Patent: February 9, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Craig A. Stump
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Publication number: 20100022509Abstract: The present invention utilizes three families of bacterial enzymes, which play a key role in mycothiol biosynthesis. The three families are bacterial cysteine:glucosaminyl inositol ligases (MshC) with catalytic ligase activity for ligation of glucosaminyl inositol and cysteine, bacterial acetyl-CoA:Cys-GlcN-Ins acetyltransferases (MshD) with catalytic activity for addition of an acetyl group to Cys-GlcN-Ins and bacterial MshA glycosyltransferase with catalytic activity for production of GlcNAc-Ins. The invention provides methods for using the mycothiol biosynthesis ligases, acetyltransferases or glycosyltransferases in drug screening assays to determine compounds that inhibit activity. The invention also provides inhibitors of the production or activity of the enzymes of mycothiol biosynthesis, and use of the inhibitors for treating microbial infection.Type: ApplicationFiled: June 7, 2007Publication date: January 28, 2010Inventors: Robert C. Fahey, Gerald L. Newton, Philong V. Ta, Nancy Buchmeier
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Publication number: 20090318412Abstract: The present invention provides a tricyclic heterocyclic compound having a serotonin 5-HT2C receptor activation action and the like. A 5-HT2C receptor activator containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.Type: ApplicationFiled: July 10, 2007Publication date: December 24, 2009Inventors: Takahiro Matsumoto, Izumi Kamo, Izumi Nomura
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Publication number: 20090298806Abstract: The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.Type: ApplicationFiled: January 5, 2009Publication date: December 3, 2009Inventors: Bing-Yan Zhu, Shawn M. Bauer, Zhaozhong J. Jia, Gary D. Probst, Yanchen Zhang, Robert M. Scarborough
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Patent number: 7615549Abstract: The present invention relates to new substituted pyrrolidinones of general formula wherein A, X, B and R1 to R9 are as defined above, or a tautomer or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.Type: GrantFiled: December 16, 2005Date of Patent: November 10, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Kai Gerlach, Henning Priepke, Roland Pfau, Wolfgang Wienen, Annette Schuler-Metz, Herbert Nar, Peter Kuehn, Georg Dahmann
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Patent number: 7569561Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R6, X and Y are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or anomalous cell proliferation, as well as the use thereof for preparing a pharmaceutical composition with the above-mentioned properties.Type: GrantFiled: February 16, 2007Date of Patent: August 4, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Heinz Stadtmueller, Anke Baum, Guido Boehmelt, Harald Engelhardt, Jens Juergen Quant, Flavio Solca, Martin Steegmaier, Stephan Karl Zahn
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Publication number: 20090192139Abstract: The present invention is directed to compounds of Formula I: and Formula II: (where variables R1, R2, R3, R4, A, B, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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: April 3, 2009Publication date: July 30, 2009Inventors: Daniel V. Paone, Anthony W. Shaw
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Patent number: 7566778Abstract: The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I wherein R1, R2 and R3 are independently H or (C1-4)alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, CF3, halogen, nitro, cyano, NR4R5, NR4COR6, and CONR4R5; R4 and R5 are independently H or (C1-4-)alkyl; or R4 and R5 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR6; R6 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 1, 2008Date of Patent: July 28, 2009Assignee: N.V. OrganonInventors: Simon James Anthony Grove, Julia Adam-Worrall, Mingqiang Zhang, Robert Gilfillan
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Patent number: 7550453Abstract: The invention relates particularly to 2-alkoxy-3,4,5-trihydroxy-alkylamides, preparation thereof, compositions containing them and use thereof as a medicament, particularly as anti-cancer agents.Type: GrantFiled: May 24, 2007Date of Patent: June 23, 2009Assignee: Aventis Pharma SAInventors: Jidong Zhang, Neerja Bhatnagar, Jean-Marie Ruxer
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Publication number: 20090054399Abstract: Tricyclic compounds of Formula (I) are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: May 5, 2006Publication date: February 26, 2009Inventors: Joseph P. Vacca, John S. Wai, Linda S. Payne, Richard C.A. Isaacs, Wei Han, Melissa Egbertson, Richard Pracitto
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Patent number: 7491713Abstract: Compounds of Formula I: and Formula II: (where variables R1, R2, R3, R4, A, B, D, G, J, Q, T, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, pharmaceutical compositions comprising these compounds, use of these compounds and compositions to prevent or treat diseases involving CGRP.Type: GrantFiled: January 25, 2005Date of Patent: February 17, 2009Assignee: Merck + Co., Inc.Inventors: Christopher S. Burgey, Daniel V. Paone, Anthony W Shaw, Craig A. Stump, Theresa M. Williams
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Publication number: 20080306041Abstract: The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one heterocyclic nitric oxide donor group, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension and (n) treating ophthalmic disorders. The cardiovascular compounds are preferably ?-adrenergic antagonists, angiotensin-converting enzyme (ACE) inhibitors, anti-hyperlipidemic compounds, and antithrombotic and vasodilator compounds.Type: ApplicationFiled: January 23, 2006Publication date: December 11, 2008Inventor: David S. Garvey
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Publication number: 20080293678Abstract: The invention describes compositions and kits comprising at least qrie organic nitric oxide enhancing salt of an angiotensin converting enzyme inhibitor, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; Q) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension; (n) treating ophthalmic disorders; (o) treating metabolic syndrome; and (p) treating hyperlipidemia.Type: ApplicationFiled: March 17, 2006Publication date: November 27, 2008Applicant: NitroMed, Inc.Inventor: David S. Garvey
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Publication number: 20080262221Abstract: The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I wherein R1, R2 and R3 are independently H or (C1-4)alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, CF3, halogen, nitro, cyano, NR4R5, NR4COR6, and CONR4R5; R4 and R5 are independently H or (C1-4-)alkyl; or R4 and R5 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR6; R6 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: February 1, 2008Publication date: October 23, 2008Applicant: N.V. OrganonInventors: Simon James Anthony Grove, Julia Adam-Worall, Mingqiang Zhang, Robert Gilfillan
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Publication number: 20080207590Abstract: This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I) wherein Q, J, L and Z are as defined in the specification.Type: ApplicationFiled: October 26, 2007Publication date: August 28, 2008Applicant: METHYLGENE INC.Inventors: Robert Deziel, Silvana Leit, Patrick Beaulieu, Yves Andre Chantigny, John Mancuso, Pierre Tessier, Gideon Shapiro, Richard Chesworth, David Smil
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Publication number: 20080146539Abstract: The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.Type: ApplicationFiled: December 19, 2007Publication date: June 19, 2008Applicant: Boehringer Ingelheim International GmbHInventors: Henning PRIEPKE, Kai Gerlach, Roland Pfau, Norbert Hauel, Iris Kauffmann-Hefner, Georg Dahmann, Herbert Nar, Sandra Handschuh, Wolfgang Wienen, Annette Schuler-Metz
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Publication number: 20080132482Abstract: This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.Type: ApplicationFiled: February 1, 2008Publication date: June 5, 2008Applicant: Bristol-Myers Squibb Pharma CompanyInventors: Richard E. Olson, Hong Liu, Lorin A. Thompson
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Patent number: 7361648Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S or NR5, and the other substituents are as defined in the specification; and prodrugs, individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.Type: GrantFiled: August 22, 2006Date of Patent: April 22, 2008Assignee: Roche Palo Alto LLCInventors: Charles Alois Dvorak, Lawrence Emerson Fisher, Keena Lynn Green, Ralph New Harris, III, Hans Maag, Anthony Prince, David Bruce Repke, Russell Stephen Stabler
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Patent number: 7314930Abstract: A process for preparing a dibenzothiazepine derivative such as dibenzo[b,f][1,4]thiazepin-11-one employable as a starting material for the preparation of 11-[4-(2-(2-hydroxyethoxy)ethyl)]-1-piperadinyldibenzothiazepine derivative which is known to be effective as an antipsychotic pharmaceutical, has the steps of reacting a nitrobenzene derivative with a thiosalicylic acid derivative, reducing the obtained 2-nitro-2?-carboxy-diphenylsulfide derivative, and subjecting the obtained 2-amino-2?-carboxy-diphenylsulfide derivative to dehydration-condensation reaction.Type: GrantFiled: March 30, 2006Date of Patent: January 1, 2008Assignees: UBE Industries, Ltd., Astrazeneca UK, Ltd.Inventors: Katsumasa Harada, Shigeyoshi Nishino, Kiyotaka Yoshii
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Patent number: 7307073Abstract: The present invention relates to benzoxazepine derivative having the general formula I, wherein X represents CO or SO2; R1, R2, R3 and R4 are independently selected from H, (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, halogen, nitro, cyano, NR8R9, NR8COR10, and CONR8R9, R5, R6 and R7 are independently H or (C1-4)alkyl; R8 and R9 are independently H or (C1-4)alkyl; or R8 and R9 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR11; R10 is (C1-4)alkyl; R11 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 5, 2002Date of Patent: December 11, 2007Assignee: N.V. OrganonInventors: Simon James Anthony Grove, Mingqiang Zhang, Mohammad Shahid
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Patent number: 7294622Abstract: Compounds having the formula (I) pharmaceutical compositions containing them and their methods of use for the treatment of neurological disorders related to amyloid ? protein production and neurological disorders such as Alzheimer's disease. These compounds inhibit ? secretase and thereby inhibit the production of amyloid ? protein, thereby acting to prevent the formation of neurological deposits of amyloid protein.Type: GrantFiled: October 2, 2003Date of Patent: November 13, 2007Assignee: Astrazeneca ABInventors: Christopher Becker, Bruce Dembofsky, Robert Jacobs, James Kang, Cyrus Ohnmacht, James Rosamond, Ashokkumar Bhikkappa Shenvi, Thomas Simpson, James Woods
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Patent number: 7279582Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: GrantFiled: October 25, 2002Date of Patent: October 9, 2007Assignee: Abbott LaboratoriesInventors: Eric J. Stoner, Arthur J. Cooper, Lawrence Kolaczkowski, Ketan M. Patel, Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Daniel A. Dickman, Patricia A. Oliver, Jien-Heh J. Tien
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Patent number: 7229984Abstract: Compounds of the Formula I: wherein m, n, k, A, X, Y, Z, Ar, R1, R2, R3, and R4 are as defined herein. The compounds are useful as 5-HT6 receptor antagonists. Also provided are compositions comprising, methods of using, and methods of making the subject compounds.Type: GrantFiled: December 9, 2005Date of Patent: June 12, 2007Assignee: Roche Palo Alto LLCInventors: Ralph New Harris, III, James M. Kress, David Bruce Repke, Russell Stephen Stabler
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Patent number: 7214793Abstract: Disclosed is a method of preparing 10H-dibenzo[b,f][1,4]thiazepin-11-one, including reacting dithiosalicylic acid with 1-chloro-2-nitrobenzene in a basic aqueous solution in the presence or absence of a reducing agent, to prepare 2-(2-nitrophenylsulfuryl)benzoic acid; subjecting the 2-(2-nitrophenylsulfuryl)benzoic acid to nitro group reduction in the presence of hydrogen, a solvent and a heterogeneous metal catalyst, to prepare 2-(2-aminophenylsulfuryl)benzoic acid; and directly cyclizing the 2-(2-aminophenylsulfuryl)benzoic acid in an organic solvent in the presence or absence of an acid catalyst. The method according to the present invention is economical due to the use of the inexpensive starting material, and also environmentally friendly and efficient by minimizing the use of the organic solvent and performing direct cyclization without the activation of carboxylic acid.Type: GrantFiled: November 26, 2003Date of Patent: May 8, 2007Assignee: SK CorporationInventors: Byong-Sung Kwak, Ki-Nam Chung, Ki-Ho Koh, Hee-Jun Hwang
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Patent number: 7208487Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.Type: GrantFiled: December 12, 2003Date of Patent: April 24, 2007Assignee: Cytokinetics, IncorporatedInventors: Gustave Bergnes, Dashyant Dhanak, Steven David Knight, Pu Ping Lu, David J. Morgans, Jr., Kenneth Allen Newlander
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Patent number: 7205292Abstract: The present invention is directed to compounds of Formula I and Formula II: (where variables R1, R2, R3, R4, R6, A, B, G, J, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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: GrantFiled: April 9, 2004Date of Patent: April 17, 2007Assignee: Merck & Co., Inc.Inventors: Christopher S. Burgey, Daniel V. Paone, Anthony W. Shaw, Theresa M. Williams
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Patent number: 7157442Abstract: The present invention relates to a compound of formula (I) (wherein R1 and R2 represent an aryl group, a heterocyclic group, an alkyl group, an alkenyl group and the like which are optionally substituted, R3 represents a hydrogen atom or a hydroxyl group, and X1 and X2 represent an oxygen atom or a sulfur atom, or a nitrogen atom which may be substituted), a pharmaceutically acceptable derivative thereof or a salt thereof. The present invention also relates to a pharmaceutical composition comprising a compound described above as an active ingredient for the prevention or treatment of bacterial infections. The present invention includes the use of a compound described above in order to prepare a medicament effective in the prevention or treatment of bacterial infections.Type: GrantFiled: February 19, 2002Date of Patent: January 2, 2007Assignee: Sankyo Company, LimitedInventors: Hitoshi Hotoda, Masakatsu Kaneko, Masatoshi Inukai, Yasunori Muramatsu, Yukio Utsui, Satoshi Ohya
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Patent number: 7109233Abstract: This invention relates in general to certain substituted substituted 1,1,4-1l6-trioxo[1,2]thiazepan-4-ylamides of formula I as defined herein which are protease inhibitors.Type: GrantFiled: May 21, 2003Date of Patent: September 19, 2006Assignee: SMithKline Beecham CorporationInventors: Jae U. Jeong, Dennis S. Yamashita
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Patent number: 7045621Abstract: A process for preparing a dibenzothiazepine derivative such as dibenzo[b,f] [1,4]thiazepin-11-one employable as a starting material for the preparation of 11-[4-(2-(2-hydroxyethoxy)ethyl)]-1-piperadinyldibenzothiazepine derivative which is known to be effective as an antipsychotic pharmaceutical, has the steps of reacting a nitrobenzene derivative with a thiosalicylic acid derivative, reducing the obtained 2-nitro-2?-carboxy-diphenylsulfide derivative, and subjecting the obtained 2-amino-2?-carboxy-diphenylsulfide derivative to dehydration-condensation reaction.Type: GrantFiled: July 9, 1999Date of Patent: May 16, 2006Assignees: Ube Industries, Ltd., AstraZeneca, UK, Ltd.Inventors: Katsumasa Harada, Shigeyoshi Nishino, Kiyotaka Yoshii
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Patent number: 7015212Abstract: The present invention discloses non-catechol compounds, such as thiazolothiazepines, and analogs and derivatives thereof, which are anti-integrase inhibitors. The compounds, which are useful as treatments for HIV disease, include compounds (I), (II), (III), or pharmaceutically acceptable salts thereof wherein A is thiazole, benzene, naphthalene, pyridine, pyrimidine, pyrazine, or quinoline; R is one or more of H, halogen, lower alkyl, lower alkoxy, NO2, lower ester or carboxylic acid; X—Y is CH2—S, S—CH2, CH2—O, CH2—S(O). S(O)—CH2, CH2—CH2, CH2—CH2—CH2, or CH2—CH2—CH2—CH2; R4 is H or hydroxy; R5 is H, phenyl, or alkylamine; W is S or O; and R6 is H, substituted or unsubstituted alkyl or amine; and Z is S, O, CH2, CH2CH2, or C?O.Type: GrantFiled: May 10, 2000Date of Patent: March 21, 2006Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Nouri Neamati, Yves Pommier, Antonio Garofalo, Vito Nacci
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Ethane-1,2-diaminium bis[(2R)-2-bromo-3-phenylpropanoate], processes for its preparation and its use
Patent number: 7009047Abstract: The present invention relates to ethane-1,2-diaminium bis[(2R)-2-bromo-3-phenyl-propanoate], the preparation of ethane-1,2-diaminium bis[(2R)-2-bromo-3-phenyl-propanoate] from (2R)-2-bromo-3-phenylpropionic acid and ethylenediamine in 2-propanol, and the use of ethane-1,2-diaminium bis[(2R)-2-bromo-3-phenyl-propanoate] for the preparation of ACE/NEP inhibitors.Type: GrantFiled: March 17, 2003Date of Patent: March 7, 2006Assignee: Sanofi-Aventis Deutschland GmbHInventors: Javier Manero, Tobias Metzenthin, Rainer Gauler -
Patent number: 6974872Abstract: The present invention discloses processes for preparing piperidine derivative compounds of the formulae: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.Type: GrantFiled: August 5, 2002Date of Patent: December 13, 2005Assignee: AMR Technology, Inc.Inventors: Thomas E. D'Ambra, Garry M. Pilling
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Patent number: 6967198Abstract: Protein kinase, such as CHK-1, inhibiting tricyclic compounds of the following formula (wherein R2, R3 and R4 are as defined in the specification) pharmaceutical compositions containing effective amounts of said compounds or their salts are useful as a single agent or in combination with an anti-neoplastic agent or therapeutic radiation having an anti-neoplastic effect for treating diseases or conditions such as cancers.Type: GrantFiled: January 9, 2004Date of Patent: November 22, 2005Assignee: Agouron Pharmaceuticals Inc.Inventors: Suzanne Benedict, Michael Bennett, Sacha Ninkovic, Min Teng, Yuanjin Rui, Fen Wang, Yong Wang, Jinjiang Zhu
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Patent number: 6949538Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.Type: GrantFiled: July 17, 2003Date of Patent: September 27, 2005Assignees: Cytokinetics, Inc., Smithkline Beecham CorporationInventors: Andrew McDonald, Gustave Bergnes, David J. Morgans, Jr., Dashyant Dhanak, Steven David Knight
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Patent number: 6924277Abstract: Compounds having the general formula wherein R1a, R1b, R1c, X1, X2, R2, R3, R4, R5, R6, n, Y and Z are as defined in the specification, methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.Type: GrantFiled: September 27, 2001Date of Patent: August 2, 2005Assignee: AstraZeneca ABInventor: Peter Bernstein
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Patent number: 6921759Abstract: Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: October 10, 2001Date of Patent: July 26, 2005Assignee: Merck & Co., Inc.Inventors: Neville J. Anthony, Robert P. Gomez, Steven D. Young, Melissa Egbertson, John S. Wai, Linghang Zhuang, Mark Embrey, Jeffrey Y. Melamed, H. Marie Langford, James P. Guare, Thorsten E. Fisher, Samson M. Jolly, Michelle S. Kuo, Debra S. Perlow, Jennifer J. Bennett, Timothy W. Funk
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Patent number: 6919328Abstract: The present invention provides novel tricyclic compounds, compositions comprising these compounds and methods of using these compounds as neuroprotectants. In particular, the compounds of the invention are useful for treating stroke.Type: GrantFiled: October 8, 2002Date of Patent: July 19, 2005Assignee: Neuraxon Inc.Inventors: Suman Rakhit, Jailall Ramnauth, Svetoslav Bratovanov, Shawn Maddaford
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Patent number: 6919458Abstract: The present invention relates to a process for preparing piperidine derivative compounds of the formulae: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents, The process comprises providing a regiosomer of the following formula: wherein Z is —CG1G2G3, m is an integer from 1 to 6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; G1, G2, and G3 are the same or different and are selected from the group consisting of OR8, SR8, and NR8R9; R6 and R7 are the same or different and are selected from the group consisting of hydrType: GrantFiled: August 5, 2002Date of Patent: July 19, 2005Assignee: AMR Technology, Inc.Inventors: Thomas E. D'Ambra, Garry M. Pilling
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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: 6864250Abstract: Compounds of structural Formula (I) where A is a lipophilic group including an aliphatic bridging group, B is a lipophilic group, D is a group having at least one amino or substituted amino group and R is hydrogen, alkyl or cycloalkyl, and pharmaceutically acceptable salts and individual isomers thereof, which have growth hormone releasing activity in humans or animalsType: GrantFiled: August 20, 1998Date of Patent: March 8, 2005Assignees: Kaken Pharmaceutical Co., Ltd., Molecular Research InstituteInventors: Hidenori Funamizu, Nobuo Ishiyama, Satoru Ikegami, Tadashi Okuno, Kiyoshi Inoguchi, Ping Huang, Gilda Loew
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Patent number: 6852713Abstract: Lactam derivatives of the general formula are disclosed. Pharmaceutical compositions containing the compounds and methods for their use are also disclosed.Type: GrantFiled: April 16, 2003Date of Patent: February 8, 2005Assignee: Adolor CorporationInventors: Roland E. Dolle, Paul Anson Tuthill
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Patent number: 6846814Abstract: Compounds having the general formula wherein R1a, R1b, R1c, R2, R3, R4, R5, R6, R7, R8, X1, X2, Y, Z and n are as defined in the specification, methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.Type: GrantFiled: April 5, 2001Date of Patent: January 25, 2005Assignee: Astra Zeneca ABInventors: Jeffrey Scott Albert, Peter Bernstein, Cyrus Ohnmacht, Jr., Keith Russell, Ashokkumar Bhikkappa Shenvi
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Publication number: 20040254159Abstract: Compounds having the formula 1Type: ApplicationFiled: February 25, 2004Publication date: December 16, 2004Inventors: Lisa A. Hasvold, Laura Hexamer, Gaoquan Li, Nan-Horng Lin, Hing Sham, Gerard M. Sullivan, Le Wang, Ping Xia
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Patent number: 6828439Abstract: Disclosed are novel compounds, compositions, and methods that are particularly useful in photodynamic therapy. In particular, the inventive compounds, compositions, and methods relate to the formation of cytotoxic radical species in the presence of light. Significantly, the compounds, compositions, and methods of the present invention do not require the presence of oxygen in the photodynamic therapy and, as such, rely on a unimolecular mechanism for producing the radicals. The inventive compounds, compositions, and methods can be used, for example, in the treatment of cancers as well as infections caused by microorganisms such as protozoa, fungi, bacteria, and viruses.Type: GrantFiled: August 20, 2001Date of Patent: December 7, 2004Assignee: Advanced Research and Technology Institute, Inc.Inventors: Jeffrey M. Zaleski, Diwan Singh Rawat
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Publication number: 20040229861Abstract: The present invention is directed to compounds of Formula I: 1Type: ApplicationFiled: May 4, 2004Publication date: November 18, 2004Inventors: Christopher S. Burgey, Zhengwu J. Deng, Diem N. Nguyen, Daniel V. Paone, Anthony W. Shaw, Theresa M. Williams