Chalcogen Or Nitrogen Attached Directly To Ring Carbon Of The Thiadiazole Ring By Nonionic Bonding Patents (Class 548/135)
  • Patent number: 8933441
    Abstract: An organic electronic device may include an organic semiconductor compound represented by the following Chemical Formula 1 or Chemical Formula 2. Each substituent of the above Chemical Formulas 1 and 2 may be the same as described in the detailed description.
    Type: Grant
    Filed: January 8, 2013
    Date of Patent: January 13, 2015
    Assignee: Samsung Electronics Co., Ltd.
    Inventors: Jong Won Chung, Bang Lin Lee, Jeong Il Park, Yong Wan Jin
  • Patent number: 8846727
    Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: September 30, 2014
    Assignee: Romark Laboratories, L.C.
    Inventors: Jean-Francois Rossignol, J. Edward Semple
  • Publication number: 20140057871
    Abstract: [Problem] To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogues and a prophylactic and/or therapeutic agent against diabetes, obesity, or the like. [Means of solving the problem] A compound of Formula (III): (where f is 0 to 2; g is 1 to 4; j is 0 to 3; k is 0 to 2; n is 0 to 2; p is 0 to 4; h is 0 to 3; q1 id 0 to 3; q2 is 0 or 1; r1 is 0 to 2 (with the proviso that q1+q2+r1 is 0 to 5); J1a is —CR11a—, N; J2 is —CR12aR12b—, —CR12c—; T is —CH2—, O, —S(O)i— (i is an integer of 0 to 2) or —NR7—; X is O, S, or —NR7—; ring A?? is a benzene ring, a pyridine ring; ring B? is a benzene ring, a pyridine ring, a pyrimidine ring; and R1 to R14 are specific groups), a salt of the compound, or a solvate of the salt or the compound.
    Type: Application
    Filed: April 11, 2012
    Publication date: February 27, 2014
    Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.
    Inventors: Akihiro Okano, Munetaka Ohkouchi, Muneyoshi Makabe
  • Publication number: 20130203739
    Abstract: [Problem] To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogues and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of solving the problem] A compound of Formula (1): (where n is 0 to 2; p is 0 to 4; h is 0 to 3; j is 0 to 3; k is 0 to 2; a ring B is an aryl group or a heteroaryl group; X is O, S, or —NR7—; J1 is —CR11aR11b— or —NR11c—; J2 is —CR12aR12b— or —NR12c—; and R1 to R12c are specific groups), a salt of the compound, or a solvate of the salt or the compound.
    Type: Application
    Filed: October 11, 2011
    Publication date: August 8, 2013
    Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.
    Inventors: Akihiro Okano, Munetaka Ohkouchi, Muneyoshi Makabe
  • Publication number: 20130158002
    Abstract: The present invention is directed to 5-substituted 1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxide and 1,3-dihydro[1,2,5]thiadiazolo[3,4-b]pyridine 2,2,-dioxide derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Application
    Filed: February 28, 2011
    Publication date: June 20, 2013
    Inventors: Mark E. Layton, Michael J. Kelly, Timothy J. Hartingh
  • Publication number: 20130123246
    Abstract: The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.
    Type: Application
    Filed: January 4, 2013
    Publication date: May 16, 2013
    Applicant: INCYTE CORPORATION
    Inventor: Incyte Corporation
  • Publication number: 20120227545
    Abstract: This invention relates to a process for the recovery of precious metal/s from a precious metal-containing material in an aqueous leach slurry or solution. The process includes the step of contacting the precious metal/s in the leach slurry or solution with a ligand selected from dithiooxamide (rubeanic acid), or a substituted dithiooxamide. The leaching of PGMs, gold and silver from their ores using the ligand of the present invention may take place under aqueous alkaline conditions, avoiding both corrosive acidic conditions and the use of cyanide.
    Type: Application
    Filed: July 21, 2010
    Publication date: September 13, 2012
    Applicant: ANGLO OPERATIONS LIMITED
    Inventors: Diandree Padayachee, Makhosazane Chucky Kunene, Marga Retha Burger, Noko Simon Phala
  • Patent number: 8252820
    Abstract: Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated.
    Type: Grant
    Filed: December 6, 2006
    Date of Patent: August 28, 2012
    Assignee: Novartis AG
    Inventors: David Barnes, Gary Mark Coppola, Travis Stams, Sidney Wolf Topiol
  • Publication number: 20120202750
    Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.
    Type: Application
    Filed: January 23, 2012
    Publication date: August 9, 2012
    Applicant: Genentech, Inc.
    Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
  • Publication number: 20120196906
    Abstract: The present invention provides imidazole derivatives of Formula (I-IV), methods of their preparation, pharmaceutical compositions comprising the compounds of Formula (I-IV), and their use in treating human or animal disorders. The compounds of the invention inhibit protein tyrosine phosphatase 1B and thus can be useful for the management, treatment, control, or the adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes and Type II diabetes.
    Type: Application
    Filed: March 6, 2012
    Publication date: August 2, 2012
    Applicant: TransTech Pharma, Inc.
    Inventors: Adnan M.M. Mjalli, Dharma R. Polisetti, Govindan Subramanian, James C. Quada, Ravindra R. Yarragunta, Robert C. Andrews, Rongyuan Xie
  • Publication number: 20120058893
    Abstract: Ketosultams and diketopyridines of the formula (I) and use thereof as herbicides are described. In this formula (I), G, X, Y and Z are each radicals such as hydrogen and organic radicals such as alkyl. W represents organic radicals such as alkyl. A represents a heterocycle.
    Type: Application
    Filed: August 31, 2011
    Publication date: March 8, 2012
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Stefan LEHR, Christian WALDRAFF, Elmar GATZWEILER, Isolde HÄUSER-HAHN, Ines HEINEMANN, Christopher Hugh ROSINGER
  • Patent number: 8119666
    Abstract: Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated.
    Type: Grant
    Filed: December 6, 2006
    Date of Patent: February 21, 2012
    Assignee: Novartis AG
    Inventors: David Barnes, Gregory Raymond Bebernitz, Gary Mark Coppola, Travis Stams, Sidney Wolf Topiol, Thalaththani Ralalage Vedananda, James Richard Wareing
  • Publication number: 20120015926
    Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
    Type: Application
    Filed: November 9, 2009
    Publication date: January 19, 2012
    Inventors: Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Joseph A. Kozlowski, Michael K.C. Wong, Lei Chen, Guowei Zhou, Razia K. Rizvi, Robert Feltz, Aneta Maria Kosinski, De-Yi Yang, Chaoyang Dai, Luke Fire, Vinay Girijavallabhan, Dansu Li, Janeta Popovici-Muller, Judson E. Richard, Kristen E. Rosner, M. Arshad Siddiqui, Liping Yang
  • Patent number: 8084448
    Abstract: Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated.
    Type: Grant
    Filed: March 29, 2007
    Date of Patent: December 27, 2011
    Assignee: Novartis AG
    Inventors: Alan Neubert, David Barnes, Young-Shin Kwak, Katsumasa Nakajima, Gregory Raymond Bebernitz, Gary Mark Coppola, Louise Kirman, Michael H. Serrano-Wu, Travis Stams, Sidney Wolf Topiol, Thalaththani Ralalage Vedananda, James Richard Wareing
  • Patent number: 7842758
    Abstract: The invention concerns compounds, oligomers, and polymers that contain: (I), (II), (III), or (IV) groups; where “-” indicates points of attachment.
    Type: Grant
    Filed: January 10, 2007
    Date of Patent: November 30, 2010
    Assignee: The Trustees Of The University Of Pennsylvania
    Inventors: Michael J. Therien, Kimihiro Susumu
  • Publication number: 20100298328
    Abstract: 1-Heterocyclylamino-2-hydroxy-3-amino-?-arylalkanes of formula (I) and the salts thereof have renin-inhibiting properties and can be used as antihypertensive, medicinally active ingredients.
    Type: Application
    Filed: March 30, 2007
    Publication date: November 25, 2010
    Inventors: John J. Baldwin, David A. Claremon, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wenguang Zeng
  • Patent number: 7820702
    Abstract: Compounds are provided which are useful in the treatment of androgen receptor-associated conditions, such as age-related diseases, which compounds have the structure wherein R1, R2, R3, R4, R4a, R4b, R4c, R4c1, Rd, Re, Rf, Rg, Rh, R5, R5?, R7, and R7? are defined herein; G is aryl, heterocycle or heteroaryl group, wherein said group is mono- or polycyclic, and which is optionally substituted; and n is an integer of 1 or 2, m is an integer of 1 or 2, Z is oxygen (—O—) or NR4b, a prodrug ester, all stereoisomers thereof and a pharmaceutically acceptable salt thereof. A method for treating androgen receptor-associated conditions such as age-related diseases is also provided.
    Type: Grant
    Filed: February 1, 2005
    Date of Patent: October 26, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: Lawrence G. Hamann, Yingzhi Bi, Mark C. Manfredi, Alexandra A. Nirschl, James C. Sutton
  • Publication number: 20100249198
    Abstract: The present invention relates to a novel class of (R)-4-(heteroaryl)phenylpropionic derivatives of formula (I), useful in the inhibition of the chemotactic activation induced by the fraction C5a of complement. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of autoimmune hemolytic anemia (AIHA), psoriasis, bullous pemphigoid, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.
    Type: Application
    Filed: October 17, 2008
    Publication date: September 30, 2010
    Applicant: Dompe S.p.A
    Inventors: Alessio Moriconi, Andrea Aramini
  • Patent number: 7763884
    Abstract: An organic semiconductor material represented by the following general formula (1): wherein X1 to X4 each independently represent a chalcogen atom; and at least one of R1 and R2 represents a substituent for obtaining solubility, and R1 and R2 may be connected to each other to form a ring.
    Type: Grant
    Filed: June 27, 2007
    Date of Patent: July 27, 2010
    Assignee: Sony Corporation
    Inventors: Mao Tatsuhara, Akito Ugawa
  • Patent number: 7737283
    Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.
    Type: Grant
    Filed: June 9, 2006
    Date of Patent: June 15, 2010
    Assignee: Deciphera Pharmaceuticals, LLC
    Inventors: Daniel L. Flynn, Peter A. Petillo
  • Patent number: 7700633
    Abstract: Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. The compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated.
    Type: Grant
    Filed: December 6, 2006
    Date of Patent: April 20, 2010
    Assignee: Novartis AG
    Inventors: David Barnes, Gregory Raymond Bebernitz, Gary Mark Coppola, Travis Stams, Sidney Wolf Topiol, Thalaththani Ralalage Vedananda, James Richard Wareing, Katsumasa Nakajima
  • Patent number: 7691856
    Abstract: Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, acute pain, acute and chronic inflammatory pain, and neuropathic pain using a compound of formula IA.
    Type: Grant
    Filed: January 9, 2007
    Date of Patent: April 6, 2010
    Assignees: Schering Corporation, Pharmacopeia, Inc.
    Inventors: Arthur G. Taveras, Jianhua Chao, Purakkattle J. Biju, Younong Yu, Cynthia J. Aki, J. Robert Merritt, Ge Li, John J. Baldwin, Gaifa Lai, Minglang Wu, Evan A. Hecker
  • Publication number: 20100035942
    Abstract: Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated.
    Type: Application
    Filed: December 6, 2006
    Publication date: February 11, 2010
    Inventors: David Barnes, Gary Mark Coppola, Travis Stams, Sidney Wolf Topiol
  • Publication number: 20100022525
    Abstract: The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.
    Type: Application
    Filed: October 4, 2007
    Publication date: January 28, 2010
    Inventors: Haiyan Jia, Ian Zachary, Michelle Tickner, Lili Cheng, Chris Chapman, Katie Ellard, Basil Hartzoulakis, Ashley Jarvis, Rosemary Lynch, Jamie Nally, David Selwood, Mark Stewart
  • Publication number: 20100022482
    Abstract: The present invention relates to compounds of formula wherein the residues have various meanings and their use as pharmaceuticals.
    Type: Application
    Filed: August 21, 2007
    Publication date: January 28, 2010
    Inventors: Karl Baumann, Andreas Billich, Berndt Oberhausen
  • Publication number: 20090181928
    Abstract: Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated.
    Type: Application
    Filed: March 29, 2007
    Publication date: July 16, 2009
    Inventors: Alan Neubert, David Barnes, Young-Shin Kwak, Katsumasa Nakajima, Gregory Raymond Bebernitz, Gary Mark Coppola, Louise Kirman, Michael H. Serrano-Wu, Travis Stams, Sidney Wolf Topiol, Thalaththani Ralalage Vedananda, James Richard Wareing
  • Publication number: 20090170911
    Abstract: Azole compounds represented by formula I: wherein ring A is isoxazole and the like, R1 is a substituted or unsubstituted aryl group and the like, R2 is a hydrogen atom and the like, and R3 is a substituted or unsubstituted alkyl group and the like, and pharmaceutically acceptable salts thereof inhibit the physiological activity of lysophosphatidic acid (LPA), and are useful as for the prophylaxis or treatment of diseases in which inhibition of the physiological activity of LPA is useful for the prophylaxis or treatment thereof, such as diseases involving the LPA receptor.
    Type: Application
    Filed: February 20, 2009
    Publication date: July 2, 2009
    Applicant: AJINOMOTO CO. INC
    Inventors: Takashi YAMAMOTO, Akira Chiba, Koichi Fujita, Yuka Kataba, Koji Ohsumi, Sayaka Asari, Naoyuki Fukuchi, Misato Noguchi, Itsuya Tanabe, Chiori Ijichi, Naoko Oomuta, Yuko Iida, Satoshi Iwayama
  • Publication number: 20090105230
    Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.
    Type: Application
    Filed: June 9, 2006
    Publication date: April 23, 2009
    Inventors: Daniel L. Flynn, Peter A. Petillo
  • Publication number: 20080293776
    Abstract: Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated.
    Type: Application
    Filed: December 6, 2006
    Publication date: November 27, 2008
    Inventors: David Barnes, Gregory Raymond Bebernitz, Gary Mark Coppola, Travis Stams, Sidney Wolf Topiol, Thalaththani Ralalage Vedananda, James Richard Wareing
  • Publication number: 20080293782
    Abstract: Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated.
    Type: Application
    Filed: December 6, 2006
    Publication date: November 27, 2008
    Inventors: David Barnes, Gary Mark Coppola, Robert Edson Damon, Katsumasa Nakajima, Brian Christopher Raudenbush, Travis Stams, Sidney Wolf Topiol, Thalaththani Ralalage Vedananda
  • Publication number: 20080262050
    Abstract: Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. The compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated.
    Type: Application
    Filed: December 6, 2006
    Publication date: October 23, 2008
    Inventors: David Barnes, Gregory Raymond Bebernitz, Gary Mark Coppola, Katsumasa Nakajima, Travis Stams, Sidney Wolf Topiol, Thalaththani Ralalage Vedananda, James Richard Wareing
  • 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
  • Patent number: 7432292
    Abstract: The present invention relates to novel phosphate isosteres. The invention relates to compounds having a sulfhydantoin or a reverse sulfhydantoin moiety, uses thereof, and related methods. The present invention relates to compounds of formula I or II: or pharmaceutically acceptable salts thereof; wherein Q, T, m, and X are as described herein. These compounds are inhibitors of phosphatases, particularly inhibitors of SHP-2. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing these compounds and compositions in the treatment of various phosphatase-mediated diseases.
    Type: Grant
    Filed: December 30, 2003
    Date of Patent: October 7, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jeffrey O. Saunders, Gregory F. Miknis, James F. Blake
  • Publication number: 20080182850
    Abstract: Disclosed are certain 3-(heteroaryl)alanine derivatives which bind VLA-4 and inhibit leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Application
    Filed: October 16, 2007
    Publication date: July 31, 2008
    Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu, Frank Stappenbeck
  • Publication number: 20080161366
    Abstract: The present invention is directed to aminoalkyl-substituted aryl sulfamide derivatives of formula I: or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.
    Type: Application
    Filed: December 12, 2007
    Publication date: July 3, 2008
    Applicant: Wyeth
    Inventors: Casey Cameron McComas, Stephen Todd Cohn, Matthew Lantz Crawley, Andrew Fensome, Joel Adam Goldberg, Douglas John Jenkins, Callain Younghee Kim, Paige Erin Mahaney, Charles William Mann, Michael Anthony Marella, David John O'Neill, Joseph Peter Sabatucci, Eugene Anthony Terefenko, Eugene John Trybulski, An Thien Vu, Richard Page Woodworth, Puwen Zhang
  • Patent number: 7358239
    Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is
    Type: Grant
    Filed: March 14, 2005
    Date of Patent: April 15, 2008
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
  • Patent number: 7338968
    Abstract: Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and ischemia reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.
    Type: Grant
    Filed: December 16, 2004
    Date of Patent: March 4, 2008
    Assignee: Schering Corporation
    Inventors: Purakkattle J. Biju, Arthur G. Taveras, J. Robert Merritt, John J. Baldwin, Younong Yu, Junying Zheng, Jianhua Chao, Cynthia J. Aki
  • Publication number: 20080004325
    Abstract: This invention relates to modulating (e.g., inhibiting) protein tyrosine phosphatase 1b (PTP1b).
    Type: Application
    Filed: June 29, 2007
    Publication date: January 3, 2008
    Applicant: Wyeth
    Inventors: Jinbo Lee, Zhao-Kui Wan, Douglas P. Wilson, Eva Binnun, David V. Erbe, Eddine Saiah
  • Patent number: 7291635
    Abstract: Compounds of the formula provide pharmacological agents which are inhibitors of PTPases, in particular, the compounds of formula I inhibit PTP-1B and TC PTP, and thus may be employed for the treatment of conditions associated with PTPase activity. The compounds of the present invention may also be employed for inhibition of other enzymes with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula I may be employed for prevention or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels.
    Type: Grant
    Filed: April 2, 2003
    Date of Patent: November 6, 2007
    Assignee: Novartis AG
    Inventors: Gary Mark Coppola, John William Davies, Charles Francis Jewell, Jr., Yu-Chin Li, James Richard Wareing, Donald Mark Sperbeck, Travis Mathew Stams, Sidney Wolf Topiol, Isidoros Vlattas
  • Patent number: 7160909
    Abstract: A novel class of tricyclic compounds of the following formula (I) is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.
    Type: Grant
    Filed: July 29, 2002
    Date of Patent: January 9, 2007
    Assignee: Eli Lilly and Company
    Inventors: Michael Dean Kinnick, Edward David Mihelich, John Michael Morin, Daniel Jon Sall, Jason Scott Sawyer
  • Patent number: 7125869
    Abstract: Novel polycyclic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively, into cosmetic compositions.
    Type: Grant
    Filed: June 10, 2005
    Date of Patent: October 24, 2006
    Assignee: Galderma Research & Development
    Inventors: Laurence Clary, Pascal Collette, Michel Rivier, Andre Jomard
  • Patent number: 7108948
    Abstract: An organophotoreceptor comprises an electrically conductive substrate and photoconductive element on the electrically conductive substrate, the photoconductive element having a) a charge transport composition with the formula where Y1 and Y2 are, each independently, an arylamine group; X1 and X2 are, each independently, a linking group; R1 and R2 are, each independently, a hydrogen, an alkyl group, an alkenyl group, a heterocyclic group, an aromatic group; Z is a bridging group; and n is a distribution of integers between 1 and 100,000 with an average value greater than 1; and (b) a charge generating compound. Corresponding electrophotographic apparatuses and imaging methods are described.
    Type: Grant
    Filed: February 27, 2004
    Date of Patent: September 19, 2006
    Assignee: Samsung Electronics Co., LTD
    Inventors: Zbigniew Tokarski, Nusrallah Jubran, Vytautas Getautis, Juozas V. Grazulevicius, Tadas Malinauskas, Edmundas Montrimas, Valentas Gaidelis
  • Patent number: 7105556
    Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.
    Type: Grant
    Filed: May 22, 2002
    Date of Patent: September 12, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Peter T. Cheng, Yoon Jeon, Wei Wang
  • 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
  • Publication number: 20040198778
    Abstract: Compounds of Formula (I), 1
    Type: Application
    Filed: March 26, 2004
    Publication date: October 7, 2004
    Applicant: Wyeth
    Inventors: Anthony Frank Kreft, Lynn Resnick, Scott Christian Mayer, George Diamantidis, Derek Cecil Cole, Boyd Lynn Harrison, Minsheng Zhang, Molly Hoke, Tingzhong Wang, Rocco John Galante
  • Publication number: 20040167187
    Abstract: The present invention relates to novel phosphate isosteres. The invention relates to compounds having a sulfhydantoin or a reverse sulfhydantoin moiety, uses thereof, and related methods.
    Type: Application
    Filed: December 30, 2003
    Publication date: August 26, 2004
    Inventors: Jeffrey O. Saunders, Gregory F. Miknis, James F. Blake
  • Patent number: 6720342
    Abstract: The present invention relates to therapeutically active azabicyclic compounds, a method of preparing the same and to pharmaceutical or veterinary compositions comprising the compounds. The novel compounds are useful in treating a disease in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.
    Type: Grant
    Filed: August 28, 2001
    Date of Patent: April 13, 2004
    Assignee: Novo Nordisk A/S
    Inventors: Lone Jeppesen, Per Sauerberg
  • Publication number: 20040034025
    Abstract: Heterocyclic aromatic amides having a hydroxy group adjacent to the amide functionality are useful as antifungal agents, particularly for plants.
    Type: Application
    Filed: December 2, 2002
    Publication date: February 19, 2004
    Inventors: Michael J. Ricks, William H. Dent, Richard B. Rogers, Chenglin Yao, Bassam S. Nader, John L. Miesei, Gina M. Fitzpatrick, Kevin G. Meyer, Noormohamed M. Niyaz, Irene M. Morrison, Robert P. Gajewski
  • Publication number: 20040023974
    Abstract: Compounds of the formula 1
    Type: Application
    Filed: April 2, 2003
    Publication date: February 5, 2004
    Inventors: Gary Mark Coppola, John William Davies, Charles Francis Jewell, Yu-Chin Li, James Richard Wareing, Donald Mark Sperbeck, Travis Matthew Stams, Sidney Wolf Topiol, Isidoros Vlattas
  • Publication number: 20040002525
    Abstract: Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.
    Type: Application
    Filed: October 28, 2002
    Publication date: January 1, 2004
    Inventors: Jeffrey A. Robl, Joseph A. Tino, Andres S. Hernandez, Jun Li