Nitrogen Attached Indirectly To The Thiazole Ring By Nonionic Bonding Patents (Class 548/205)
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Publication number: 20100029588Abstract: The present invention relates to oxime ether-, hydrazone- or azomethine-substituted phenylamidines of the general formula (I), to a process for their preparation, to the use of the amidines according to the invention for controlling unwanted microorganisms and also to a composition for this purpose, comprising the amidines according to the invention. Furthermore, the invention relates to a method for controlling unwanted microorganisms by applying the compounds according to the invention to the microorganisms and/or their habitat.Type: ApplicationFiled: March 8, 2008Publication date: February 4, 2010Applicant: BAYER CROPSCIENCE AGInventors: Thomas Seitz, Klaus Kunz, Wahed Ahmed Moradi, Jörg Nico Greul, Darren James Mansfield, Urlich Heinemann, Amos Mattes, Oswald Ort, Jean-Pierre Vors, Peter Dahem, Ulrike Wachendorff-Neumann, Arnd Voerste
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Publication number: 20100029689Abstract: PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: wherein R1, R2, R3, and R4 are as defined herein.Type: ApplicationFiled: July 2, 2009Publication date: February 4, 2010Applicants: MEMORY PHARMACEUTICALS CORPORATION, ROCHE PALO ALTO LLCInventors: Allen T. HOPPER, Joan Marie CAROON, Elbert CHIN, Robert F. DUNN, Sharada Shenvi LABADIE, Jim LI, Richard Allen SCHUMACHER, Francisco Xavier TALAMAS
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Publication number: 20100016260Abstract: The invention provides compounds of formula I and formula II, their preparation, and their use as pharmaceutically active immunosuppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as other disorders modulated by lymphopenia or SIP receptors.Type: ApplicationFiled: August 1, 2007Publication date: January 21, 2010Applicant: PRAECIS PHARMACEUTICALS INCORPORATEDInventors: Hongfeng Deng, Ghotas Evindar, Sylvie Bernier, Gang Yao, Aaron Coffin, Hongfang Yang, Raksha A. Acharya
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Patent number: 7649006Abstract: The present invention provides compounds of formula (I): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).Type: GrantFiled: May 9, 2003Date of Patent: January 19, 2010Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Samuel J. Danishefsky, Alexey Rivkin, Yoshimura Fumikiko, Ting-Chao Chou, Ana E. Gabarda, Huajin Dong
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Publication number: 20100009936Abstract: The invention provides compounds formula I, their preparation, and their use as pharmaceutically active immuno-suppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as other disorders modulated by lymphopenia or SIP receptors.Type: ApplicationFiled: August 1, 2007Publication date: January 14, 2010Applicant: PRAECIS PHARMACEUTICALS INCORPORATEDInventors: Ghotas Evindar, Hongfeng Deng, Sylvie Bernier, Gang Yao, Aaron Coffin, Hongfang Yang
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Patent number: 7638637Abstract: The present invention relates to S1P analogs that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds have the general structure (I) wherein R11 is C5-C18 alkyl or C5-C18 alkenyl; Q is selected from the group consisting of C3-C6 optionally substituted cycloalkyl, C3-C6 optionally substituted heterocyclic, C3-C6 optionally substituted aryl C3-C6 optionally substituted heteroaryl and; R2 is selected from the group consisting of H, C1-C4 alkyl, (C1-C4 alkyl)OH and (C1-C4 alkyl)NH2; R23 is H or C1-C4 alkyl, and R15 is a phosphonate ester or a phosphate ester or a pharmaceutically acceptable salt or tautomer thereof.Type: GrantFiled: November 3, 2004Date of Patent: December 29, 2009Assignee: University of Virginia Patent FoundationInventors: Kevin R. Lynch, Timothy L. Macdonald
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Publication number: 20090318389Abstract: The invention provides compounds formulae I-III, their preparation, and their use as pharmaceutically active immunosuppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as other disorders modulated by lymphopenia or SIP receptors.Type: ApplicationFiled: August 2, 2007Publication date: December 24, 2009Applicant: PRAECIS PHARMACEUTICALS INCORPORATEDInventors: Ghotas Evindar, Hongfeng Deng
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Publication number: 20090299073Abstract: Disclosed is a process for the manufacture of a Compound of formula (I) wherein Hal represents fluoro or chloro, and R1 and R2 represent, independently from one another, hydrogen or Hal; in which process a Compound of formula (II) is converted to a corresponding alkyl, fluoroalkyl or aryl sulfonic acid ester, which is then reacted with an alkali metal nitrite in the presence of a suitable crown ester in a polar non-nucleophilic solvent at a temperature of ?10 to 50° C. to give the Compound of formula (I).Type: ApplicationFiled: November 29, 2006Publication date: December 3, 2009Inventors: Marc Muller, Lin Xu
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Patent number: 7615569Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides heterocyclic aryl sulfonamides, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel.Type: GrantFiled: August 11, 2006Date of Patent: November 10, 2009Assignee: Icagen, Inc.Inventors: Alan Fulp, Brian Marron, Mark J. Suto, Xiaodong Wang
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Publication number: 20090253656Abstract: The present invention is directed to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. The BCRP inhibitor contains, as an active ingredient, an acrylonitrile derivative represented by formula (1): wherein one of R1 and R2 represents a cyano group and the other represents a hydrogen atom; Ar1 represents a group selected from among the groups represented by formulas (2) to (4): and Ar2 represents an aromatic hydrocarbon group having a condensed ring which may be substituted by a halogen atom, or a group selected from among the groups represented by the following formulas (5) to (15): or a salt thereof.Type: ApplicationFiled: March 29, 2006Publication date: October 8, 2009Applicant: Kabushiki Kaisha Yakult HonshaInventors: Ryuta Yamazaki, Yukiko Nishiyama, Tomio Furuta, Takeshi Matsuzaki, Hiroshi Hatano, Oh Yoshida, Masato Nagaoka, Ritsuo Aiyama, Shusuke Hashimoto, Yoshikazu Sugimoto
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Patent number: 7598280Abstract: Heterocyclic compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of inflammatory and autoimmune diseases and disorders are disclosed.Type: GrantFiled: February 28, 2008Date of Patent: October 6, 2009Assignee: Lexicon Pharmaceuticals, Inc.Inventors: David J. Augeri, Jeffrey Bagdanoff, Simon D. P. Baugh, Kenneth G. Carson, Theodore C. Jessop, James E. Tarver
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Publication number: 20090211038Abstract: The present disclosure relates to a novel dye composition for the dyeing and/or lightening of keratin materials, such dye comprising a hemicyanin styryl chromophore thiol or disulfide dye of formula (I) or (II): the organic or mineral acid salts thereof, optical isomers and geometric isomers thereof, and the solvates thereof such as hydrates. The present disclosure further relates to a dyeing process with a lightening effect on keratin materials, in particular keratin fibers, including human keratin fibers such as the hair, using said composition. This composition makes it possible to obtain a coloring with a lightening effect which is particularly resistant and visible on dark keratin fibers.Type: ApplicationFiled: September 19, 2008Publication date: August 27, 2009Inventors: Andrew GREAVES, Nicolas DAUBRESSE
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Patent number: 7579477Abstract: Disclosed are novel NO-donating compounds, designed such that when NO is released from the compound a residue which is a naturally occurring metabolite is formed, and thus a development of tolerance to the compounds upon repetitive administration is prevented or decreased. Also disclosed are methods of preparing such NO-donating compounds, pharmaceutical compositions and medical devices containing such compounds and methods utilizing such compounds in the treatment of various medical conditions.Type: GrantFiled: November 4, 2005Date of Patent: August 25, 2009Assignee: Renopharm Ltd.Inventors: Peter Assaf, Elham Gazaleen-Mariee, Michael Naveh
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Patent number: 7560462Abstract: Substituted urea compounds useful in the treatment of diseases and C1-3alkyleneOR3 conditions related to DNA damage or lesions in DNA replication are disclosed formula (I), wherein X1 is null, —O—, —S—, —CH2—, or —N(R1)—; X2 is —O—, . -£>. -, or —N(R1)—,—. . Y xs 0 or S; or =y represents two hydrogen atoms attached to a common carbon atom, —W is selected from the group consisting of heteroaryl, aryl, heterocycloalkyl, cycloalkyl, and C1-6alkyl substituted with a heteroaryl. or aryl group; R6 is —C?C—R7 or heteroaryl; R8, R9, and R10, independently, are selected from the group consisting of halo, optionally substituted C1-6alkyl, C2-6alkenyl, C2-6alkynyl, OCP3, CF3, NO2, CN, NC, N(R3)2, OR3, CO2R3, C(O)N (R3)2, C(O)R3, N(R1)COR3, N(R1)C(O)OR3, N(R8)C(O)OR3, N(R1)C(O)C1-3alkyleneC(O)R3, N(R1)C(O)C1 -3alkyleneC(O)OR3, N(R1)C(O)C1-3alkyleneOR3, N(R1)C(O)C1-3alkyleneNHC(O)OR3, N(R1)C(O)C1-3alkyleneSO2.Type: GrantFiled: July 1, 2005Date of Patent: July 14, 2009Assignee: ICOS CorporationInventors: John Joseph Gaudino, Adam Wade Cook
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Publication number: 20090176846Abstract: Disclosed is an N-Hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy} benzamidine 2 methansulfonic acid salt, which has excellent bioavailability. Also disclosed are a method of preparing the compound and a pharmaceutical composition comprising the compound.Type: ApplicationFiled: November 22, 2005Publication date: July 9, 2009Inventors: Jei Man Ryu, Jin Soo Lee, Dong Hyuk Shin, Seung Kyoo Seong, Soon Ki Cho, Chan Seok Jeon, Young Goo Jin, Ki Young Lee, Se Hyun Jung, Eun Hee Cho, Seok Hoon Ahn
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Patent number: 7553976Abstract: The invention relates to new derivatives of 2-(iminomethyl)amino-phenyl which are NO synthase inhibitors and can trap reactive oxygen species. These compounds can notably be used for the treatment of stroke, of neurodegenerative diseases and of ischemic or hemorragic cardiac of cerebral infarctions.Type: GrantFiled: January 22, 2008Date of Patent: June 30, 2009Assignee: Societe de Conseils de Recherches et d'Applications (S.C.R.A.S.)Inventors: Pierre Etienne Chabrier De Lassauniere, Serge Auvin, Dennis Bigg, Michel Auquet, Jeremiah Harnett
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Patent number: 7547701Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.Type: GrantFiled: September 17, 2004Date of Patent: June 16, 2009Assignee: Virobay, Inc.Inventors: John O. Link, Craig J. Mossman, Soon H. Woo, Sheila M. Zipfel
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Patent number: 7511149Abstract: Insecticidal sulfoximines are produced efficiently and in high yield by the oxidation of the corresponding sulfilimine with ruthenium tetraoxide or an alkali metal permanganate.Type: GrantFiled: February 9, 2007Date of Patent: March 31, 2009Assignee: Dow AgroSciences LLCInventors: Kim E. Arndt, Douglas C. Bland, David E. Podhorez, James R. McConnell
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Publication number: 20090082390Abstract: This invention relates to N-aroyl cyclic amine derivatives and their use as pharmaceuticals, specifically as orexin receptor antagonists.Type: ApplicationFiled: July 8, 2008Publication date: March 26, 2009Inventors: Wai Ngor CHAN, Amanda Johns, Christopher Norbert Johnson, Riccardo Novelli, Roderick Alan Porter
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Patent number: 7504420Abstract: The present invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating Alzheimer's disease.Type: GrantFiled: August 9, 2006Date of Patent: March 17, 2009Assignees: CoMentis, Inc., The Board of Trustees of the University of Illinois, Oklahoma Medical Research Foundation, Purdue Research FoundationInventors: Arun K. Ghosh, Nagaswamy Kumaragurubaran, Chunfeng Liu, Thippeswamy Devasamudram, Hui Lei, Lisa M. Swanson, Sudha V. Ankala, Jordan J. N. Tang, Geoffrey M. Bilcer
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Patent number: 7498445Abstract: Disclosed are novel NO-donating compounds, designed such that when NO is released from the compound a residue which is a naturally occurring metabolite is formed, and thus a development of tolerance to the compounds upon repetitive administration is prevented or decreased. Also disclosed are methods of preparing such NO-donating compounds, pharmaceutical compositions and medical devices containing such compounds and methods utilizing such compounds in the treatment of various medical conditions.Type: GrantFiled: November 4, 2005Date of Patent: March 3, 2009Assignee: Renopharm Ltd.Inventors: Peter Assaf, Elham Gazaleen-Mariee, Michael Naveh
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Publication number: 20090054642Abstract: The present invention relates to a novel benzamidine derivative, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The benzamidine derivative of the present invention effectively inhibits osteoclast differentiation at an extremely low concentration, and greatly increases the trabecular bone volume, and thus it can be advantageously used for the prevention and treatment of osteoporosis.Type: ApplicationFiled: January 31, 2007Publication date: February 26, 2009Applicant: DONGWHA PHARMACEUTICAL IND. CO., LTD.Inventors: Jei Man Ryu, Jin Soo Lee, Young Goo Jin, Ki Young Lee, Jae Hoon Park, Yun Ha Hwang, Sae Kwang Ku
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Publication number: 20090030050Abstract: Heterocyclic compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of inflammatory and autoimmune diseases and disorders are disclosed.Type: ApplicationFiled: February 28, 2008Publication date: January 29, 2009Inventors: David J. Augeri, Jeffrey Bagdanoff, Simon D.P. Baugh, Kenneth G. Carson, Theodore C. Jessop, James E. Tarver
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Publication number: 20080312282Abstract: The present invention relates to compounds of formula (I): wherein Q, G1, G2, and G3, are defined herein. Pharmaceutical compositions and methods for treating DGAT-1 related diseases or conditions are also disclosed.Type: ApplicationFiled: April 30, 2008Publication date: December 18, 2008Applicant: ABBOTT LABORATORIESInventors: Andrew S. Judd, Mathew M. Mulhern, Rajesh R. Iyengar, Philip R. Kym, Andrew J. Souers
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Publication number: 20080312297Abstract: The present application relates to new substituted oxyguanidines of structure (I) a method for their preparation and their use for the control of animal pests, mainly arthropods, in particular insects.Type: ApplicationFiled: November 12, 2005Publication date: December 18, 2008Applicant: Bayer Cropscience AGInventors: Peter Jeschke, Peter Losel, Ralf Nauen, Peter Marczok, Christian Arnold, Erich Sanwald
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Publication number: 20080287509Abstract: Disclosed herein is a composition for the treatment bone fracture comprising N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxyl-benzamidine, 4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}-benzamidine or pharmaceutically acceptable salts thereof as a medicinally effective ingredient. The composition of the present invention can significantly reduce the volume of bony callus, and increase bony density and strength of bony callus, and decrease the contents of connective tissue and cartilage tissue in bony callus, and thus promote loss and ossification of the bony callus formed during the fracture healing process. Therefore, the composition of the present invention is useful for the treatment of bone fracture.Type: ApplicationFiled: July 5, 2005Publication date: November 20, 2008Applicant: DONG WHA PHARMACEUTICAL IND. CO., LTD.Inventors: Jei Man Ryu, Jin Soo Lee, Sae Kwang Ku, Jung Woo Lee, Hee Bog Yang
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Patent number: 7452874Abstract: Invented are non-peptide TPO mimetics. Also invented are novel processes and intermediates used in the preparation of the presently invented compounds. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative.Type: GrantFiled: January 8, 2007Date of Patent: November 18, 2008Assignee: SmithKline Beecham Corp.Inventors: Kevin J. Duffy, Juan I. Luengo, Antony N. Shaw, Kenneth Wiggall
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Publication number: 20080280875Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is (4-12)-membered heterocyclyl; Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).Type: ApplicationFiled: May 9, 2007Publication date: November 13, 2008Inventors: Hao Bai, Simon Bailey, Dilip Ramakant Bhumralkar, Feng C. Bi, Fengli Guo, Mingying He, Paul Stuart Humphries, Anthony Lai Ling, Jihong Lou, Seiji Nukul, Ru Zhou
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Publication number: 20080280915Abstract: N-Substituted (heteroaryl)alkyl sulfilimines are effective at controlling insects.Type: ApplicationFiled: February 9, 2007Publication date: November 13, 2008Inventors: Michael R. Loso, Benjamin M. Nugent, Yuanming Zhu, Richard B. Rogers, Jim X. Huang, James M. Renga, Zoltan L. Benko, Gregory T. Whiteker, John F. Daeuble
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Patent number: 7429581Abstract: The present invention is directed to a compound of formula I, in which R0; R1; R2; R3; R4; Q; V, G and M have the meanings indicated below. The compound of formula I is a pharmacologically active compound. It exhibits a strong anti-thrombotic effect and is suitable, for example, for the therapy and prophylaxis of a cardio-vascular disorder like a thromboembolic disease or restenosis. It is a reversible inhibitor of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore is directed to a process for the preparation of the compound of formula I, and pharmaceutical preparation comprising it.Type: GrantFiled: December 23, 2003Date of Patent: September 30, 2008Assignee: Sanofi-Aventis Deutschland GmbHInventors: Marc Nazare, Volkmar Wehner, David W. Will, Hans Matter
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Publication number: 20080233163Abstract: Disclosed are novel NO-donating compounds, designed such that when NO is released from the compound a residue which is a naturally occurring metabolite is formed, and thus a development of tolerance to the compounds upon repetitive administration is prevented or decreased. Also disclosed are methods of preparing such NO-donating compounds, pharmaceutical compositions and medical devices containing such compounds and methods utilizing such compounds in the treatment of various medical conditions.Type: ApplicationFiled: March 24, 2008Publication date: September 25, 2008Applicant: Renopharm Ltd.Inventor: Peter Assaf
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Patent number: 7407959Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: GrantFiled: November 18, 2005Date of Patent: August 5, 2008Assignee: Merck Frosst Canada & Co.Inventors: Jacques Yves Gauthier, Chun Sing Li, Christophe Mellon
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Publication number: 20080125470Abstract: The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.Type: ApplicationFiled: September 18, 2007Publication date: May 29, 2008Applicant: INCYTE CORPORATIONInventors: Andrew P. Combs, Brian M. Glass, Richard B. Sparks, Eddy Wai Tsun Yue
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Patent number: 7371770Abstract: Compounds of formula (I) as defined herein: inhibit the formation of the ?-amyloid peptide (?-A4) and are, therefore, useful in the treatment of pathologies in which a ?-amyloid peptide (?-A4) formation inhibitor provides a therapeutic benefit. Particular such pathologies are senile dementia, Alzheimer's disease, Down's syndrome, Parkinson's disease, amyloid angiopathy, cerebrovascular disorders, frontotemporal dementias and Pick's disease, post-traumatic dementias, pathologies linked to neuroinflammatory processes, Huntington's disease and Korsakov's syndrome.Type: GrantFiled: July 14, 2006Date of Patent: May 13, 2008Assignee: SanofiaventisInventors: Sylvie Baltzer, Marc Pascal, Viviane Van Dorsselaer
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Patent number: 7368577Abstract: Disclosed are novel NO-donating compounds, designed such that when NO is released from the compound a residue which is a naturally occurring metabolite is formed, and thus a development of tolerance to the compounds upon repetitive administration is prevented or decreased. Also disclosed are methods of preparing such NO-donating compounds, pharmaceutical compositions and medical devices containing such compounds and methods utilizing such compounds in the treatment of various medical conditions.Type: GrantFiled: November 4, 2005Date of Patent: May 6, 2008Assignee: Renopharm Ltd.Inventors: Peter Assaf, Elham Gazaleen-Mariee, Michael Naveh
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Publication number: 20080058390Abstract: N-Substituted (heteroaryl)cycloalkyl sulfoximines are effective at controlling insects.Type: ApplicationFiled: February 9, 2007Publication date: March 6, 2008Inventors: Michael R. Loso, Benjamin M. Nugent, Jim X. Huang
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Publication number: 20080058394Abstract: N-Substituted (2-substituted-1,3-thiazol)alkyl sulfoximines are effective at controlling insects.Type: ApplicationFiled: August 30, 2007Publication date: March 6, 2008Applicant: Dow AgroSciences LLCInventors: Michael R. Loso, Benjamin M. Nugent, Yuanming Zhu, Thomas L. Siddall, Francis E. Tisdell, Jim X. Huang, Zoltan L. Benko
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Publication number: 20080045556Abstract: Compounds of the following structure are described: wherein R1, R2, R5, R6, V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.Type: ApplicationFiled: August 13, 2007Publication date: February 21, 2008Applicant: WyethInventors: Thomas Joseph Commons, Andrew Fensome, Gavin David Heffernan, Casey Cameron McComas, Richard Page Woodworth, Michael Byron Webb, Michael Anthony Marella, Edward George Melenski, Ronald Charles Bernotas
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Patent number: 7332513Abstract: Disclosed are novel NO-donating compounds, designed such that when NO is released from the compound a residue which is a naturally occurring metabolite is formed, and thus a development of tolerance to the compounds upon repetitive administration is prevented or decreased. Also disclosed are methods of preparing such NO-donating compounds, pharmaceutical compositions and medical devices containing such compounds and methods utilizing such compounds in the treatment of various medical conditions.Type: GrantFiled: November 4, 2005Date of Patent: February 19, 2008Assignee: Renopharm Ltd.Inventors: Peter Assaf, Elham Gazaleen-Mariee, Michael Naveh
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Patent number: 7326812Abstract: Arylsulfonamidobenzyl alcohols, amines and sulfonamides are provided which are useful in treating lipid disorders, metabolic diseases and cell-proliferative diseases.Type: GrantFiled: January 17, 2006Date of Patent: February 5, 2008Assignee: Amgen Inc.Inventors: Xian Yun Jiao, Frank Kayser, Sharon McKendry, Derek E. Piper, Andrew K. Shiau
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Patent number: 7294640Abstract: The present invention relates to substituted thiazole derivatives that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin and MCAK activity, and for inhibiting KSP kinesin and MCAK. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: January 21, 2005Date of Patent: November 13, 2007Assignee: Merck & Co., Inc.Inventors: Paul J. Coleman, Robert M. Garbaccio, Lou Anne Neilson
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Patent number: 7259157Abstract: Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.Type: GrantFiled: April 2, 2002Date of Patent: August 21, 2007Assignee: Merck & Co., Inc.Inventors: Nigel J. Liverton, John W. Butcher, Charles McIntyre, Christopher F. Claiborne, David A. Claremon, John A. McCauley, Joseph J. Romano, Wayne Thompson, Peter M. Munson
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Patent number: 7241801Abstract: A compound, represented by formula (I): wherein A, B, R1, R2, R3, R5, R6, R7, R9, and R10 are as defined herein, or an enantiomer, diastereoisomer or tautomer thereof, including a salt, ester or derivative thereof, as an inhibitor of HCV NS5B polymerase.Type: GrantFiled: July 15, 2005Date of Patent: July 10, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Pierre Beaulieu, Christian Brochu, Stephen Kawai, Jean Rancourt, Timothy A. Stammers, Bounkham Thavonekham, Youla S. Tsantrizos
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Patent number: 7179823Abstract: A compound of formula (I) F wherein R1 represents a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; x represents a bond, an oxygen atom, a sulfur atom, or a group of the formula: —CO—, —CS—, —CR4(OR5)— or —NR6— wherein each of R4 and R6 represents a hydrogen atom or a hydrocarbon group which may be stubstituted, R5 represents a hydrogen atom or a protective group for a hydroxyl group; m represents an integer of 0 to 3; Y represents an oxygen atom, a sulfur atom, or a group of the formula: —SO—, —SO2—, —NR7—, —CONR7— or —NR7CO— wherein R7 represents a hydrogen atom or a hydrocarbon group which may be substituted; ring A represents an aromatic ring which may further have 1 to 3 substituents; n represents an integer of 1 to 8; ring B represents a nitrogen-containing 5-membered hetero ring which may further be substituted by an alkyl group.Type: GrantFiled: November 9, 2000Date of Patent: February 20, 2007Assignee: Takeda Pharmaceutical Company LimitedInventors: Yu Momose, Tsuyoshi Maekawa, Hiroyuki Odaka, Hiroyuki Kimura
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Patent number: 7141672Abstract: This invention provides compounds of Formula I having the structure or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.Type: GrantFiled: January 8, 2004Date of Patent: November 28, 2006Assignee: WyethInventor: Michael S. Malamas
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Patent number: 7122547Abstract: The invention relates to anthranilic acid amides and the use thereof as medicaments for the treatment of diseases that are triggered by persistent angiogenesis, in addition to intermediate products in the production of anthranilic acid amides.Type: GrantFiled: November 9, 1999Date of Patent: October 17, 2006Assignees: Schering AG, Novartis AGInventors: Andreas Huth, Dieter Seidelmann, Karl-Heinz Thierauch, Guido Bold, Paul William Manley, Pascal Furet, Jeanette Marjorie Wood, Jürgen Mestan, Jose Brüggen, Stefano Ferrari, Martin Krüger, Eckhard Ottow, Andreas Menrad, Michael Schirner
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Patent number: 7071220Abstract: The present invention relates to an N-substituted benzothiophenesulfonamide derivative or a pharmaceutically acceptable salt thereof and applications thereof. Furthermore, it provides an agent for preventing or treating cardiac or circulatory disease and so on caused by abnormal increase of production of angiotensin II or endothelin I based on chymase activity, or by activation of mast cell, and an agent for preventing adhesion after surgery, wherein the agent has a selective inhibitory action on chymase.Type: GrantFiled: March 13, 2003Date of Patent: July 4, 2006Assignee: Toa Eiyo Ltd.Inventors: Shoji Satoh, Akira Tatsui, Takeshi Hasegawa, Hideki Yamada, Shin-ichi Kazayama, Takahiro Morita, Hidekazu Masaki, Atsuo Takahashi, Fumiya Yoneyama, Tetsuo Kuze, Yusuke Mizuno, Mizuo Miyazaki, Shinji Takai
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Patent number: 7071358Abstract: Arylsulfonamidobenzyl alcohols, amines and sulfonamides are provided which are useful in treating lipid disorders, metabolic diseases and cell-proliferative diseases.Type: GrantFiled: January 29, 2003Date of Patent: July 4, 2006Assignee: Amgen Inc.Inventors: Xian Yun Jiao, Frank Kayser, Sharon McKendry, Derek E. Piper, Andrew K. Shiau
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Patent number: 7030239Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII) useful in treating Alzheimer's disease and other similar diseases.Type: GrantFiled: May 18, 2004Date of Patent: April 18, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Roy Hom, Shumeye S. Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Y. Fang
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Patent number: 7019019Abstract: The present invention provides matriptase inhibitors and compositions thereof useful for treating cancer. Martripase is a trypsin-like serine protease active in the development of cancerous conditions, such as tumors and metastasis of cancer.Type: GrantFiled: December 18, 2003Date of Patent: March 28, 2006Assignee: Dendreon CorporationInventors: David F. Duncan, L. Josue Alfaro-Lopez, Mallareddy Komandla, Odile Esther Levy, Ofir Moreno, Joseph E. Semple, Amir P. Tamiz