1,2,4-thiadiazoles (including Hydrogenated) Patents (Class 548/128)
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Publication number: 20090106915Abstract: The present invention concerns coloring keratin fibers, especially human hair, with colored metal complexes.Type: ApplicationFiled: May 3, 2006Publication date: April 30, 2009Inventors: Nicole End, Kai-Uwe Schoning, Beate Frohling
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Patent number: 7524957Abstract: The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R1, R2, R3, n and m are as described in the specification, in the preparation of a medicament for the treatment or prevention of a disease condition mediated through glucokinase (GLK), such as type 2 diabetes. The invention also relates to a novel group of compounds of Formula (I) and to methods for preparing compounds of Formula (I).Type: GrantFiled: February 1, 2008Date of Patent: April 28, 2009Assignee: AstraZeneca ABInventors: Scott Boyd, Peter William Rodney Caulkett, Rodney Brian Hargreaves, Suzanne Saxon Bowker, Roger James, Clifford David Jones, Darren McKerrecher, Michael Howard Block, Craig Johnstone
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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: 20090068378Abstract: A discotic nematic material comprising a compound of R1—H1—Ar—H2—R wherein Ar represents a substituted or unsubstituted aromatic hydrocarbon ring; H1 and H2 represent an aromatic hetero ring; and R1 and R2 represent a substituent having from 1 to 30 carbon atoms. The discotic nematic material contains a discotic liquid-crystal compound having a smaller number of side branches and capable of expressing an ND phase.Type: ApplicationFiled: February 6, 2007Publication date: March 12, 2009Applicant: FUJIFILM CorporationInventor: Makoto Takahashi
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Patent number: 7498351Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR modulators to treat or inhibit the progression of, for example, dyslipidemia.Type: GrantFiled: November 15, 2005Date of Patent: March 3, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Gee-Hong Kuo, Lan Shen, Aihua Wang, Yan Zhang
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Publication number: 20090048311Abstract: Compositions and processes for controlling nematodes are described herein, e.g., nematodes that infest plants or animals. The compounds include oxazoles, oxadiazoles and thiadiazoles.Type: ApplicationFiled: August 13, 2008Publication date: February 19, 2009Inventors: Deryck J. Williams, Matt W. Dimmic, William P. Haakenson, JR., Al Wideman, Barry J. Shortt, Tim Cheeseright, Michael J. Crawford
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Publication number: 20090018056Abstract: Compounds having glucokinase activating effects and being useful as treatments for diabetes, which are represented by the following formula (I): [wherein X1 represents oxygen, etc., X2 represents oxygen, etc., R1 represents a group on Ring A such as alkylsulfonyl, etc., R2 represents C3-7 cyclic alkyl optionally substituted with a halogen, etc., R3 represents a substituent on Ring B such as lower alkyl, etc., formula (II): [Chemical Formula 1] represents 6- to 10-membered aryl, etc., and formula (III): [Formula 1] represents monocyclic or bicyclic heteroaryl optionally having on Ring B a substituent represented by R3 above, wherein the carbon atom of Ring B which is bonded to the nitrogen atom of the amide group of formula (I) forms a C?N bond with the nitrogen atom of the ring], as well as their pharmaceutically acceptable salts.Type: ApplicationFiled: September 5, 2008Publication date: January 15, 2009Inventors: Tomoharu Iino, Noriaki Hashimoto, Hiroshi Nakashima, Keiji Takahashi, Teruyuki Nishimura, Jun-ichi Eiki
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Publication number: 20080293780Abstract: The present invention comprises bicyclic aryl-sulfonic acid [1,3,4]-thiadiazol-2-yl-amides, their functional derivatives thereof as well as their physiologically acceptable salts and pharmaceutical compositions thereof that exhibit peroxisome proliferator activated receptor (PPAR) PPARdelta and PPARgamma agonist activity. The structure of the compounds of the invention are defined by Formula I below, wherein the various substituents are defined herein, including their physiologically acceptable salts. Processes for the compounds preparation are also disclosed. The compounds are suitable for the treatment of fatty acid metabolism and glucose utilization disorders, disorders relating to insulin resistance are involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: ApplicationFiled: April 4, 2008Publication date: November 27, 2008Applicant: SANOFI-AVENTISInventors: Karl SCHOENAFINGER, Stefanie KEIL, Matthias URMANN, Hans MATTER, Maike GLIEN, Wolfgang WENDLER
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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: 7442760Abstract: Electroactive polymeric arylenes and intermediates useful for making such polymers are disclosed. The present invention also provides electroactive compositions comprising the electroactive polymeric arylenes, organic electronic devices which comprise these polymers and compositions, and methods of fabricating these devices.Type: GrantFiled: March 17, 2006Date of Patent: October 28, 2008Assignee: 3M Innovative Properties CompanyInventors: Ralph R. Roberts, James G. Bentsen, Yingbo Li
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Publication number: 20080262049Abstract: A therapeutic and/or prophylactic agent for a hematopoietic tumor, which comprises a thiadiazoline derivative represented by the general formula (I), or a pharmaceutically acceptable salt thereof: [Formula 1] [wherein, n represents an integer of 1 to 3, R1 represents a hydrogen atom, R2 represents lower alkyl, or R1 and R2 are combined together to represent alkylene, R3 represents lower alkyl, R4 represents NHSO2R6 (wherein R6 represents hydroxy or the like) or the like, and R5 represents aryl or the like] and the like are provided.Type: ApplicationFiled: March 22, 2006Publication date: October 23, 2008Applicants: KYOWA HAKKO KOGYO CO., LTD., FUJIFILM CORPORATIONInventors: Ryuichiro Nakai, Seiho Okamoto, Hideaki Kusaka, Yoshinori Yamashita, Hiroyuki Ishida
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Patent number: 7439242Abstract: Modulators of PPAR? activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.Type: GrantFiled: April 15, 2002Date of Patent: October 21, 2008Assignee: Amgen Inc.Inventors: Jonathan B. Houze, Lawrence R. McGee, Steven Marc Rubenstein
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Publication number: 20080207703Abstract: The present invention provides novel heterocyclic urea compounds having useful antibacterial activity, pharmaceutical compositions comprising one or more of these compounds, methods of making the same, and methods of using the same.Type: ApplicationFiled: July 23, 2007Publication date: August 28, 2008Applicant: Replidyne, Inc.Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun
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Patent number: 7414142Abstract: Compounds of formula I, wherein R1-R9 and n are defined herein, and pharmaceutical compositions and kits containing these compounds are provided. Also provided are methods of inducing contraception, providing hormone replacement therapy, treating cycle-related symptoms, or treating or preventing benign or malignant neoplastic disease using the compounds of formula I or formula II, wherein R3-R5, R10, and R11 are defined herein.Type: GrantFiled: September 18, 2006Date of Patent: August 19, 2008Assignee: WyethInventors: Puwen Zhang, Jeffrey Curtis Kern, Eugene Anthony Terefenko, Eugene John Trybulski
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Publication number: 20080194653Abstract: A therapeutic and/or prophylactic agent for a solid tumor, which comprises a thiadiazoline derivative represented by the general formula (I), or a pharmaceutically acceptable salt thereof: [wherein, n represents an integer of 1 to 3, R1 represents a hydrogen atom, R2 represents lower alkyl, or R1 and R2 are combined together to represent alkylene, R3 represents lower alkyl, R4 represents NHSO2R6 (wherein R6 represents hydroxy or the like) or the like, and R5 represents aryl or the like] and the like are provided.Type: ApplicationFiled: March 22, 2006Publication date: August 14, 2008Applicants: KYOWA HAKKO KOGYO CO., LTD., FUJIFILM CORPORATIONInventors: Chikara Murakata, Kazuhiko Kato, Junichiro Yamamoto, Ryuichiro Nakai, Seiho Okamoto, Yoji Ino, Yushi Kitamura, Toshikazu Saitoh, Takeshi Katsuhira
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Patent number: 7407976Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: November 15, 2004Date of Patent: August 5, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Mark T. Miller, Sarah S. Hadida Ruah, Peter D. J. Grootenhuis, Matthew Hamilton
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Patent number: 7399765Abstract: Compounds of formula (I) Z-Ar1—Ar2??(I) wherein Z is a diazabicyclic amine, Ar1 is a 5- or 6-membered aromatic ring, and Ar2 is selected from the group consisting of an unsubstituted or substituted 5- or 6-membered heteroaryl ring; unsubstituted or substituted bicyclic heteroaryl ring; 3,4-(methylenedioxy)phenyl; carbazolyl; tetrahydrocarbazolyl; naphthyl; and phenyl; wherein the phenyl is substituted with 0, 1, 2, or 3 substituents in the meta- or para-positions. The compounds are useful in treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods for using such compounds and compositions.Type: GrantFiled: September 16, 2004Date of Patent: July 15, 2008Assignee: Abbott LaboratoriesInventors: William H. Bunnelle, Jianguo Ji, Tao Li, Jennifer M. Pace, Karin R. Tietje, Kathleen H. Mortell, Diana L. Nersesian, Michael R. Schrimpf
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Publication number: 20080146624Abstract: The present invention is directed to amidino heterocyclic compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.Type: ApplicationFiled: September 18, 2007Publication date: June 19, 2008Applicant: INCYTE CORPORATIONInventors: Andrew P. Combs, Eddy Wai Tsun Yue
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Publication number: 20080132479Abstract: The problem of the present invention is to provide a useful compound as a glucokinase activating agent, which is the oxime derivative of the formula [I]: wherein Ring A is aryl or heteroaryl; Q is cycloalkyl, heterocycle, alkyl or alkenyl; Ring T is heteroaryl or heterocycle; R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl or the like; R3 and R4 are independently hydrogen atom, hydroxy, oxo, halogen atom or the like; R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl or the like; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: July 10, 2006Publication date: June 5, 2008Inventors: Kazutoshi Sugawara, Tetsuji Matsudaira, Hiroshi Sugama, Masao Nawano, Rikiya Chashi
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Patent number: 7375123Abstract: The present invention is directed to novel 1,2,4-thiadiazole derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.Type: GrantFiled: February 1, 2006Date of Patent: May 20, 2008Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Magdalena Eisinger, Louis J. Fitzpatrick, Daniel H. Lee, Kevin Pan, Carlos Plata-Salaman, Allen B. Reitz, Virginia L. Smith-Swintosky, Boyu Zhao
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Patent number: 7371746Abstract: The present invention relates to a 1,2,4-thiadiazole compound of the formula (I) represented by the formula (1): wherein R1? represents C3-C7 alkynyl and X represents C4-C7 straight alkylene optionally substituted with one to four of R2?, C4-C7 straight alkenylene optionally substituted with one to four of R2?, ethylene-oxy-ethylene optionally substituted with one to four of R4?, or ethylene-thio-ethylene optionally substituted with one to four of R4?, R2? represents a halogen atom, trifluoromethyl or C1-C4 alkyl, and R4 represents a fluorine atom or C1-C3 alkyl.Type: GrantFiled: September 27, 2004Date of Patent: May 13, 2008Assignee: Sumitomo Chemical Company LimitedInventors: Hideki Ihara, Daisuke Takaoka, Hajime Mizuno
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Patent number: 7361675Abstract: 1,2,4-Thiadiazole compounds represented by the formula (1) have excellent control activities against harmful arthropods: wherein R1 represents C3-C7 alkynyl group optionally substituted one or more halogen atom(s); R2 a represents a halogen atom, a C1-C4 alkyl group, a C1-C4 haloalkyl group, a C1-C4 alkoxy group, a C1-C4 haloalkoxy group, a C1-C4 alkylthio group, a cyano group, or a nitro group, and n is an integer of 0 to 5, provided that, when n is an integer of 2 or more, respective R2s may be the same or different; A represents an oxygen atom, a sulfur atom, a single bond, a CR3R4 group, or NR5; R3 and R4 represent each independently a hydrogen atom or a C1-4 alkyl group; and R5 represent a hydrogen and the like.Type: GrantFiled: November 8, 2002Date of Patent: April 22, 2008Assignee: Sumitomo Chemical Company LimitedInventors: Hideki Ihara, Noriyasu Sakamoto
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Patent number: 7361769Abstract: The present invention discloses compounds of formula I wherein m, n, p, R1, R2 and X, are herein defined, the compounds being novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: GrantFiled: July 14, 2005Date of Patent: April 22, 2008Assignee: Schering CorporationInventors: Jing Su, Brian A. McKittrick, Haiqun Tang, Thavalakulamgara K. Sasikumar, Li Qiang
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Patent number: 7358265Abstract: Compounds formula (IA) or (IB), wherein W represents HO(C?O)—, HONH(C?O)— or H(C?O)N(OH)—; X represents —O— or —S—; and R1, R2, and R3 are as defined in the description and claims, are inhibitors of matrix metalloproteinases, in particular MMP9 and/or MMP12.Type: GrantFiled: February 20, 2003Date of Patent: April 15, 2008Assignees: Vernalis (R&D) Ltd, Laboratories Serono S.A.Inventors: Andrew Paul Ayscough, Stephen John Davies, Gilles Pain, Jean-Yves Gillon
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Patent number: 7345009Abstract: The present invention relates to novel substituted pyrazolines of the formula (I) in which R1, R2, R3 and R4 are as defined in the disclosure, to a plurality of processes for preparing these substances and their use for controlling pests, and to novel intermediates and processes for their preparation.Type: GrantFiled: January 23, 2003Date of Patent: March 18, 2008Assignee: Bayer CropScience AGInventors: Fritz Maurer, Rainer Fuchs, Angelika Lubos-Erdelen, legal representative, Jörg Konze, Peter Lösel, Andreas Turberg, Christoph Erdelen
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Patent number: 7342031Abstract: The thiadiazole compound represented by the formula (A): wherein R1 represents a C1-C7 alkyl group, a C3-C7 alkenyl group, a C3-C7 alkynyl group and the like; R2 represents a C1-C4 alkyl group substituted with a hetero ring group in which the hetero ring group may be substituted, which the hetero ring group is a five-membered ring containing only an oxygen atom(s) or a sulfur atom(s) as a hetero atom(s); has an excellent arthropod pests controlling activity.Type: GrantFiled: October 7, 2003Date of Patent: March 11, 2008Assignee: Sumitomo Chemical Company, LimitedInventor: Hideki Ihara
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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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Publication number: 20080045560Abstract: Compounds of the following structure are described: wherein R1-R6, R11, R12, m, 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
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Patent number: 7319107Abstract: The present invention is directed to novel 1,2,4-thiadiazol-2-ium derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.Type: GrantFiled: November 4, 2002Date of Patent: January 15, 2008Assignee: Johnson & Johnson Consumer Companies, Inc.Inventors: Magdalena Eisinger, Louis J. Fitzpatrick, Daniel H. Lee, Kevin Pan, Carlos Plata-Salaman, Allen B. Reitz, Virginia L. Smith-Swintosky, Boyu Zhao
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Patent number: 7316851Abstract: An electroluminescent element is disclosed, comprising an electroluminescent material and a fluorescent substance emitting light having an emission maximum at the wavelength different from that of light emitted from the electroluminescent material upon absorption of the light emitted from the electroluminescent material. A color conversion filter is also disclosed, comprising a fluorescent substance emitting light having an emission maximum at the wavelengths of 400 to 700 nm upon absorption of the light emitted from the electroluminescent material.Type: GrantFiled: September 4, 2003Date of Patent: January 8, 2008Assignee: Konica CorporationInventors: Hiroshi Kita, Yoshiyuki Suzuri, Taketoshi Yamada, Kazuaki Nakamura, Noriko Ueda, Yasushi Okubo
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Patent number: 7314875Abstract: The present invention provides compounds of the structure: wherein the constituent members are defined herein, including pharmaceutical compositions thereof and methods of treating diseases therewith.Type: GrantFiled: April 12, 2005Date of Patent: January 1, 2008Assignee: Cephalon, Inc.Inventors: Edward R. Bacon, Sankar Chatterjee, Derek Dunn, John A. Gruner, Rabindranath Tripathy
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Patent number: 7291744Abstract: The present application describes modulators of chemokine receptors of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: November 12, 2004Date of Patent: November 6, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Soo S. Ko, Douglas G. Batt, George V. Delucca, John V. Duncia, Daniel S. Gardner, Joseph B. Santella
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Patent number: 7282512Abstract: Cycloalkyl ketoamide derivatives, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such cycloalkyl ketoamide derivatives as well as methods of using the same in the treatment of disorders, including osteoporosis, associated with enhanced bone turnover which can ultimately lead to fracture.Type: GrantFiled: January 15, 2003Date of Patent: October 16, 2007Assignee: SmithKline Beecham CorporationInventors: John George Catalano, David Norman Deaton, Aaron Bayne Miller, Francis Xavier Tavares
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Patent number: 7253195Abstract: The present invention relates to compounds of the Formula wherein R3, R5, R7, U, X, Y and Z are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. This invention also relates to pharmaceutical compositions and methods of treating diseases, for example, neurodegenerative diseases, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.Type: GrantFiled: August 20, 2004Date of Patent: August 7, 2007Assignee: Pfizer IncInventor: Yuhpyng L. Chen
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Patent number: 7217706Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.Type: GrantFiled: February 14, 2002Date of Patent: May 15, 2007Assignee: Astellas Pharma Inc.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Patent number: 7173030Abstract: The present invention relates to compounds with the formula (I) and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.Type: GrantFiled: May 21, 2004Date of Patent: February 6, 2007Assignee: Biovitrum ABInventors: David Pyring, Martin Henriksson, Jan Vagberg, Meredith Williams, Cecilia Nilsson, Catrine Dreifeldt
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Patent number: 7148219Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: GrantFiled: April 29, 2005Date of Patent: December 12, 2006Assignee: Rib-X Pharmaceuticals, Inc.Inventors: Rongliang Lou, Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
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Patent number: 7115639Abstract: The present invention is related to pyrrolidine oxadiazole and thiadiazole derivatives for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such pyrrolidine oxadiazole derivatives. Said pyrrolidine derivatives are useful in the treatment and/or prevention of preterm labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including preterm labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation.Type: GrantFiled: June 14, 2002Date of Patent: October 3, 2006Assignee: Applied Research Systems ARS Holding N.V.Inventors: Matthias Schwarz, Anna Quattropani, Patrick Page, Russell J. Thomas, Vincent Pomel
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Patent number: 7105471Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I) in which X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenylalkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, Z represents hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, CKE represents one of the groups ?in which A, B, D, G and Q1 to Q6 are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.Type: GrantFiled: February 12, 2004Date of Patent: September 12, 2006Assignee: Bayer AktiengesellschaftInventors: Folker Lieb, Reiner Fischer, Alan Graff, Udo Schneider, Thomas Bretschneider, Christoph Erdelen, Wolfram Andersch, Mark-Wilhelm Drewes, Markus Dollinger, Ingo Wetcholowsky, Randy Allen Myers
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Patent number: 7098325Abstract: The invention relates to a process for the sulfurization of phosphorus-containing compounds which comprises contacting the phosphorus compound to be sulfurized with a sulfur transfer reagent of formula (I) wherein R1 is aryl which can be substituted by halo, (C1–C6) alkyl or (C1-C6) alkoxy, and R2 is (C1–C6) alkyl, which could also form a cyclic ring together with R1, in a solvent or a mixture of solvents.Type: GrantFiled: October 7, 2002Date of Patent: August 29, 2006Inventors: Pierre Martin, Francois J Natt
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Patent number: 7094902Abstract: Electroactive polymeric arylenes and intermediates useful for making such polymers are disclosed. The present invention also provides electroactive compositions comprising the electroactive polymeric arylenes, organic electronic devices which comprise these polymers and compositions, and methods of fabricating these devices.Type: GrantFiled: September 25, 2002Date of Patent: August 22, 2006Assignee: 3M Innovative Properties CompanyInventors: Ralph R. Roberts, James G. Bentsen, Yingbo Li
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Patent number: 7078403Abstract: Disclosed herein are compounds of formula II: wherein Alk, Z, X1, X2, R1, —R10 and R11 are defined herein, and their salts and pharmaceutically acceptable derivatives thereof, as well as other compounds of the general formula Het-A-Alk-W-Ar-C(X2)?NO-X2 where Het, A, W and Ar are also defined herein. These compounds are useful in treating picornavirus infections in mammals. Novel intermediates of these compounds, as well as pharmaceutical compositions and methods of use, are also disclosed herein.Type: GrantFiled: June 16, 2000Date of Patent: July 18, 2006Assignee: Biota Scientific Management Pty Ltd.Inventors: Wen-Yang Wu, Keith Watson, Darryl McConnell, Betty Jin, Guy Krippner
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Patent number: 7078424Abstract: This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.Type: GrantFiled: June 24, 2003Date of Patent: July 18, 2006Assignee: GPI NIL Holdings, Inc.Inventors: Gregory S. Hamilton, Mark H. Norman, Yong-Qian Wu
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Patent number: 7056932Abstract: The invention is concerned with novel heterocyclyl substituted 1-alkoxy acetic acid derivatives of formula (I) wherein R1 to R6 and A are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor and can be used as medicaments.Type: GrantFiled: December 10, 2004Date of Patent: June 6, 2006Assignee: Hoffman-La Roche Inc.Inventors: Luca Claudio Gobbi, Katrin Groebke Zbinden, Peter Mohr, Ulrike Obst
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Patent number: 7049331Abstract: The present invention is directed to novel 1,2,4-thiadiazole derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.Type: GrantFiled: November 4, 2002Date of Patent: May 23, 2006Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Magdalena Eisinger, Louis J. Fitzpatrick, Daniel H. Lee, Kevin Pan, Carlos Plata-Salaman, Allen B. Reitz, Virginia L. Smith-Swintosky, Boyu Zhao
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Patent number: 7015329Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR modulators to treat or inhibit the progression of, for example, dyslipidemia.Type: GrantFiled: October 28, 2004Date of Patent: March 21, 2006Assignee: Janssen Pharmaceutica N. V.Inventors: Gee-Hong Kuo, Lan Shen, Aihua Wang, Yan Zhang
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Patent number: 6987104Abstract: N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, salts or prodrugs thereof have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by PDF inhibitors, such as treatment of bacterial infections.Type: GrantFiled: June 14, 2002Date of Patent: January 17, 2006Assignee: Vicuron Pharmaceuticals Inc.Inventors: Jeffrey Jacobs, Rakesh K. Jain, Jason G. Lewis, Dinesh V. Patel, Zhengyu Yuan
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Patent number: 6974829Abstract: This invention is directed to a class of compounds (Formula I) including succinoyl amino pyrazoles, succinoyl amino thiadiazoles, succinoyl amino acid esters, succinoyl amino acid amides, succinoyl amino alcohols, succinoyl amino ketones, succinoyl amino hydantoins, succinoyl anilines, and succinoyl derivatives of privileged structures. The invention is also directed to a pharmaceutical formation comprising such compound in a pharmaceutically acceptable salt form or prodrug thereof. The invention is further directed to a method for inhibiting ?-amyloid peptide release and/or synthesis, a method for inhibiting ?-secretase activity and a method for treating neurological disorders associated with ?-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.Type: GrantFiled: May 7, 2003Date of Patent: December 13, 2005Assignee: Elan Pharmaceuticals, Inc.Inventors: Jay S. Tung, Ashley C. Guinn, Eugene D. Thorsett, Michael A. Pleiss
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Patent number: 6951945Abstract: 2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 3-position being a substituted phenyl group and at the 2-position being a methyl cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.Type: GrantFiled: July 9, 2003Date of Patent: October 4, 2005Assignee: Hoffman-La Roche Inc.Inventors: Fred Thomas Bizzarro, Wendy Lea Corbett, Joseph Francis Grippo, Nancy-Ellen Haynes, George William Holland, Robert Francis Kester, Paige Erin Mahaney, Ramakanth Sarabu
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Patent number: RE40558Abstract: The use of diaryl acid derivatives of formula (I) or pharmaceutically acceptable salts, N-oxides, hydrates or solvates thereof, wherein the variables shown are defined in the disclosure, and their pharmaceutical compositions as PPAR ligand receptor binders. The PPAR ligand receptor binders of this invention are useful as agonists or antagonists of the PPAR receptor.Type: GrantFiled: October 20, 2005Date of Patent: October 28, 2008Assignee: Sanofi-Aventis Deutschland GmbHInventors: Zaid Jayyosi, Gerard M. McGeehan, Michael F. Kelley, Richard F. Labaudiniere, Litao Zhang, Robert D. Groneberg, Daniel G. McGarry, Thomas J. Caulfield, Anne Minnich, Mark Bobko