1,2,4-thiadiazoles (including Hydrogenated) Patents (Class 548/128)
  • Publication number: 20090106915
    Abstract: The present invention concerns coloring keratin fibers, especially human hair, with colored metal complexes.
    Type: Application
    Filed: May 3, 2006
    Publication date: April 30, 2009
    Inventors: Nicole End, Kai-Uwe Schoning, Beate Frohling
  • Patent number: 7524957
    Abstract: 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: Grant
    Filed: February 1, 2008
    Date of Patent: April 28, 2009
    Assignee: AstraZeneca AB
    Inventors: Scott Boyd, Peter William Rodney Caulkett, Rodney Brian Hargreaves, Suzanne Saxon Bowker, Roger James, Clifford David Jones, Darren McKerrecher, Michael Howard Block, Craig Johnstone
  • Patent number: 7511149
    Abstract: 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: Grant
    Filed: February 9, 2007
    Date of Patent: March 31, 2009
    Assignee: Dow AgroSciences LLC
    Inventors: Kim E. Arndt, Douglas C. Bland, David E. Podhorez, James R. McConnell
  • Publication number: 20090068378
    Abstract: 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: Application
    Filed: February 6, 2007
    Publication date: March 12, 2009
    Applicant: FUJIFILM Corporation
    Inventor: Makoto Takahashi
  • Patent number: 7498351
    Abstract: 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: Grant
    Filed: November 15, 2005
    Date of Patent: March 3, 2009
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Gee-Hong Kuo, Lan Shen, Aihua Wang, Yan Zhang
  • Publication number: 20090048311
    Abstract: 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: Application
    Filed: August 13, 2008
    Publication date: February 19, 2009
    Inventors: Deryck J. Williams, Matt W. Dimmic, William P. Haakenson, JR., Al Wideman, Barry J. Shortt, Tim Cheeseright, Michael J. Crawford
  • Publication number: 20090018056
    Abstract: 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: Application
    Filed: September 5, 2008
    Publication date: January 15, 2009
    Inventors: Tomoharu Iino, Noriaki Hashimoto, Hiroshi Nakashima, Keiji Takahashi, Teruyuki Nishimura, Jun-ichi Eiki
  • Publication number: 20080293780
    Abstract: 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: Application
    Filed: April 4, 2008
    Publication date: November 27, 2008
    Applicant: SANOFI-AVENTIS
    Inventors: Karl SCHOENAFINGER, Stefanie KEIL, Matthias URMANN, Hans MATTER, Maike GLIEN, Wolfgang WENDLER
  • Publication number: 20080280915
    Abstract: N-Substituted (heteroaryl)alkyl sulfilimines are effective at controlling insects.
    Type: Application
    Filed: February 9, 2007
    Publication date: November 13, 2008
    Inventors: 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
  • Patent number: 7442760
    Abstract: 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: Grant
    Filed: March 17, 2006
    Date of Patent: October 28, 2008
    Assignee: 3M Innovative Properties Company
    Inventors: Ralph R. Roberts, James G. Bentsen, Yingbo Li
  • Publication number: 20080262049
    Abstract: 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: Application
    Filed: March 22, 2006
    Publication date: October 23, 2008
    Applicants: KYOWA HAKKO KOGYO CO., LTD., FUJIFILM CORPORATION
    Inventors: Ryuichiro Nakai, Seiho Okamoto, Hideaki Kusaka, Yoshinori Yamashita, Hiroyuki Ishida
  • Patent number: 7439242
    Abstract: 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: Grant
    Filed: April 15, 2002
    Date of Patent: October 21, 2008
    Assignee: Amgen Inc.
    Inventors: Jonathan B. Houze, Lawrence R. McGee, Steven Marc Rubenstein
  • Publication number: 20080207703
    Abstract: 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: Application
    Filed: July 23, 2007
    Publication date: August 28, 2008
    Applicant: Replidyne, Inc.
    Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun
  • Patent number: 7414142
    Abstract: 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: Grant
    Filed: September 18, 2006
    Date of Patent: August 19, 2008
    Assignee: Wyeth
    Inventors: Puwen Zhang, Jeffrey Curtis Kern, Eugene Anthony Terefenko, Eugene John Trybulski
  • Publication number: 20080194653
    Abstract: 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: Application
    Filed: March 22, 2006
    Publication date: August 14, 2008
    Applicants: KYOWA HAKKO KOGYO CO., LTD., FUJIFILM CORPORATION
    Inventors: Chikara Murakata, Kazuhiko Kato, Junichiro Yamamoto, Ryuichiro Nakai, Seiho Okamoto, Yoji Ino, Yushi Kitamura, Toshikazu Saitoh, Takeshi Katsuhira
  • Patent number: 7407976
    Abstract: 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: Grant
    Filed: November 15, 2004
    Date of Patent: August 5, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Mark T. Miller, Sarah S. Hadida Ruah, Peter D. J. Grootenhuis, Matthew Hamilton
  • Patent number: 7399765
    Abstract: 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: Grant
    Filed: September 16, 2004
    Date of Patent: July 15, 2008
    Assignee: Abbott Laboratories
    Inventors: William H. Bunnelle, Jianguo Ji, Tao Li, Jennifer M. Pace, Karin R. Tietje, Kathleen H. Mortell, Diana L. Nersesian, Michael R. Schrimpf
  • Publication number: 20080146624
    Abstract: 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: Application
    Filed: September 18, 2007
    Publication date: June 19, 2008
    Applicant: INCYTE CORPORATION
    Inventors: Andrew P. Combs, Eddy Wai Tsun Yue
  • Publication number: 20080132479
    Abstract: 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: Application
    Filed: July 10, 2006
    Publication date: June 5, 2008
    Inventors: Kazutoshi Sugawara, Tetsuji Matsudaira, Hiroshi Sugama, Masao Nawano, Rikiya Chashi
  • Patent number: 7375123
    Abstract: 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: Grant
    Filed: February 1, 2006
    Date of Patent: May 20, 2008
    Assignee: 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
  • Patent number: 7371746
    Abstract: 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: Grant
    Filed: September 27, 2004
    Date of Patent: May 13, 2008
    Assignee: Sumitomo Chemical Company Limited
    Inventors: Hideki Ihara, Daisuke Takaoka, Hajime Mizuno
  • Patent number: 7361675
    Abstract: 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: Grant
    Filed: November 8, 2002
    Date of Patent: April 22, 2008
    Assignee: Sumitomo Chemical Company Limited
    Inventors: Hideki Ihara, Noriyasu Sakamoto
  • Patent number: 7361769
    Abstract: 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: Grant
    Filed: July 14, 2005
    Date of Patent: April 22, 2008
    Assignee: Schering Corporation
    Inventors: Jing Su, Brian A. McKittrick, Haiqun Tang, Thavalakulamgara K. Sasikumar, Li Qiang
  • Patent number: 7358265
    Abstract: 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: Grant
    Filed: February 20, 2003
    Date of Patent: April 15, 2008
    Assignees: Vernalis (R&D) Ltd, Laboratories Serono S.A.
    Inventors: Andrew Paul Ayscough, Stephen John Davies, Gilles Pain, Jean-Yves Gillon
  • Patent number: 7345009
    Abstract: 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: Grant
    Filed: January 23, 2003
    Date of Patent: March 18, 2008
    Assignee: Bayer CropScience AG
    Inventors: Fritz Maurer, Rainer Fuchs, Angelika Lubos-Erdelen, legal representative, Jörg Konze, Peter Lösel, Andreas Turberg, Christoph Erdelen
  • Patent number: 7342031
    Abstract: 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: Grant
    Filed: October 7, 2003
    Date of Patent: March 11, 2008
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Hideki Ihara
  • Publication number: 20080045556
    Abstract: 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: Application
    Filed: August 13, 2007
    Publication date: February 21, 2008
    Applicant: Wyeth
    Inventors: 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
  • Publication number: 20080045560
    Abstract: 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: Application
    Filed: August 13, 2007
    Publication date: February 21, 2008
    Applicant: Wyeth
    Inventors: Thomas Joseph Commons, Andrew Fensome, Gavin David Heffernan, Casey Cameron McComas, Richard Page Woodworth, Michael Byron Webb, Michael Anthony Marella, Edward George Melenski
  • Patent number: 7319107
    Abstract: 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: Grant
    Filed: November 4, 2002
    Date of Patent: January 15, 2008
    Assignee: 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
  • Patent number: 7316851
    Abstract: 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: Grant
    Filed: September 4, 2003
    Date of Patent: January 8, 2008
    Assignee: Konica Corporation
    Inventors: Hiroshi Kita, Yoshiyuki Suzuri, Taketoshi Yamada, Kazuaki Nakamura, Noriko Ueda, Yasushi Okubo
  • Patent number: 7314875
    Abstract: 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: Grant
    Filed: April 12, 2005
    Date of Patent: January 1, 2008
    Assignee: Cephalon, Inc.
    Inventors: Edward R. Bacon, Sankar Chatterjee, Derek Dunn, John A. Gruner, Rabindranath Tripathy
  • Patent number: 7291744
    Abstract: 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: Grant
    Filed: November 12, 2004
    Date of Patent: November 6, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: Soo S. Ko, Douglas G. Batt, George V. Delucca, John V. Duncia, Daniel S. Gardner, Joseph B. Santella
  • Patent number: 7282512
    Abstract: 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: Grant
    Filed: January 15, 2003
    Date of Patent: October 16, 2007
    Assignee: SmithKline Beecham Corporation
    Inventors: John George Catalano, David Norman Deaton, Aaron Bayne Miller, Francis Xavier Tavares
  • Patent number: 7253195
    Abstract: 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: Grant
    Filed: August 20, 2004
    Date of Patent: August 7, 2007
    Assignee: Pfizer Inc
    Inventor: Yuhpyng L. Chen
  • Patent number: 7217706
    Abstract: 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: Grant
    Filed: February 14, 2002
    Date of Patent: May 15, 2007
    Assignee: Astellas Pharma Inc.
    Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
  • Patent number: 7173030
    Abstract: 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: Grant
    Filed: May 21, 2004
    Date of Patent: February 6, 2007
    Assignee: Biovitrum AB
    Inventors: David Pyring, Martin Henriksson, Jan Vagberg, Meredith Williams, Cecilia Nilsson, Catrine Dreifeldt
  • Patent number: 7148219
    Abstract: 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: Grant
    Filed: April 29, 2005
    Date of Patent: December 12, 2006
    Assignee: 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
  • Patent number: 7115639
    Abstract: 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: Grant
    Filed: June 14, 2002
    Date of Patent: October 3, 2006
    Assignee: Applied Research Systems ARS Holding N.V.
    Inventors: Matthias Schwarz, Anna Quattropani, Patrick Page, Russell J. Thomas, Vincent Pomel
  • Patent number: 7105471
    Abstract: 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: Grant
    Filed: February 12, 2004
    Date of Patent: September 12, 2006
    Assignee: Bayer Aktiengesellschaft
    Inventors: Folker Lieb, Reiner Fischer, Alan Graff, Udo Schneider, Thomas Bretschneider, Christoph Erdelen, Wolfram Andersch, Mark-Wilhelm Drewes, Markus Dollinger, Ingo Wetcholowsky, Randy Allen Myers
  • Patent number: 7098325
    Abstract: 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: Grant
    Filed: October 7, 2002
    Date of Patent: August 29, 2006
    Inventors: Pierre Martin, Francois J Natt
  • Patent number: 7094902
    Abstract: 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: Grant
    Filed: September 25, 2002
    Date of Patent: August 22, 2006
    Assignee: 3M Innovative Properties Company
    Inventors: Ralph R. Roberts, James G. Bentsen, Yingbo Li
  • Patent number: 7078403
    Abstract: 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: Grant
    Filed: June 16, 2000
    Date of Patent: July 18, 2006
    Assignee: Biota Scientific Management Pty Ltd.
    Inventors: Wen-Yang Wu, Keith Watson, Darryl McConnell, Betty Jin, Guy Krippner
  • Patent number: 7078424
    Abstract: 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: Grant
    Filed: June 24, 2003
    Date of Patent: July 18, 2006
    Assignee: GPI NIL Holdings, Inc.
    Inventors: Gregory S. Hamilton, Mark H. Norman, Yong-Qian Wu
  • Patent number: 7056932
    Abstract: 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: Grant
    Filed: December 10, 2004
    Date of Patent: June 6, 2006
    Assignee: Hoffman-La Roche Inc.
    Inventors: Luca Claudio Gobbi, Katrin Groebke Zbinden, Peter Mohr, Ulrike Obst
  • Patent number: 7049331
    Abstract: 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: Grant
    Filed: November 4, 2002
    Date of Patent: May 23, 2006
    Assignee: 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
  • Patent number: 7015329
    Abstract: 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: Grant
    Filed: October 28, 2004
    Date of Patent: March 21, 2006
    Assignee: Janssen Pharmaceutica N. V.
    Inventors: Gee-Hong Kuo, Lan Shen, Aihua Wang, Yan Zhang
  • Patent number: 6987104
    Abstract: 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: Grant
    Filed: June 14, 2002
    Date of Patent: January 17, 2006
    Assignee: Vicuron Pharmaceuticals Inc.
    Inventors: Jeffrey Jacobs, Rakesh K. Jain, Jason G. Lewis, Dinesh V. Patel, Zhengyu Yuan
  • Patent number: 6974829
    Abstract: 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: Grant
    Filed: May 7, 2003
    Date of Patent: December 13, 2005
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Jay S. Tung, Ashley C. Guinn, Eugene D. Thorsett, Michael A. Pleiss
  • Patent number: 6951945
    Abstract: 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: Grant
    Filed: July 9, 2003
    Date of Patent: October 4, 2005
    Assignee: 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
  • Patent number: RE40558
    Abstract: 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: Grant
    Filed: October 20, 2005
    Date of Patent: October 28, 2008
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: 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