Chalcogen Or Nitrogen Attached Directly To Ring Carbon Of The Thiadiazole Ring By Nonionic Bonding Patents (Class 548/135)
-
Patent number: 12162848Abstract: Disclosed are compounds of Formula (I) pharmaceutically acceptable salts thereof are defined herein, and pharmaceutical compositions thereof and combinations thereof, and methods of using the same as inhibitors of protein tyrosine phosphatases (PTPN2). These compounds are useful in treating cancer and diseases susceptible to PNPT2 inhibition.Type: GrantFiled: January 30, 2023Date of Patent: December 10, 2024Assignee: Bristol-Myers Squibb CompanyInventors: Haibo Liu, Laura Akullian D'Agostino, Shoshana L. Posy, Annapurna Pendri, Swanee E. Jacutin-Porte
-
Patent number: 8933441Abstract: 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: GrantFiled: January 8, 2013Date of Patent: January 13, 2015Assignee: Samsung Electronics Co., Ltd.Inventors: Jong Won Chung, Bang Lin Lee, Jeong Il Park, Yong Wan Jin
-
Patent number: 8846727Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.Type: GrantFiled: May 11, 2010Date of Patent: September 30, 2014Assignee: Romark Laboratories, L.C.Inventors: Jean-Francois Rossignol, J. Edward Semple
-
Publication number: 20140057871Abstract: [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: ApplicationFiled: April 11, 2012Publication date: February 27, 2014Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventors: Akihiro Okano, Munetaka Ohkouchi, Muneyoshi Makabe
-
Publication number: 20130203739Abstract: [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: ApplicationFiled: October 11, 2011Publication date: August 8, 2013Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventors: Akihiro Okano, Munetaka Ohkouchi, Muneyoshi Makabe
-
Publication number: 20130158002Abstract: 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: ApplicationFiled: February 28, 2011Publication date: June 20, 2013Inventors: Mark E. Layton, Michael J. Kelly, Timothy J. Hartingh
-
Publication number: 20130123246Abstract: The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.Type: ApplicationFiled: January 4, 2013Publication date: May 16, 2013Applicant: INCYTE CORPORATIONInventor: Incyte Corporation
-
Publication number: 20120227545Abstract: 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: ApplicationFiled: July 21, 2010Publication date: September 13, 2012Applicant: ANGLO OPERATIONS LIMITEDInventors: Diandree Padayachee, Makhosazane Chucky Kunene, Marga Retha Burger, Noko Simon Phala
-
Patent number: 8252820Abstract: 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: GrantFiled: December 6, 2006Date of Patent: August 28, 2012Assignee: Novartis AGInventors: David Barnes, Gary Mark Coppola, Travis Stams, Sidney Wolf Topiol
-
Publication number: 20120202750Abstract: 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: ApplicationFiled: January 23, 2012Publication date: August 9, 2012Applicant: Genentech, Inc.Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
-
Publication number: 20120196906Abstract: 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: ApplicationFiled: March 6, 2012Publication date: August 2, 2012Applicant: 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: 20120058893Abstract: 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: ApplicationFiled: August 31, 2011Publication date: March 8, 2012Applicant: BAYER CROPSCIENCE AGInventors: Stefan LEHR, Christian WALDRAFF, Elmar GATZWEILER, Isolde HÄUSER-HAHN, Ines HEINEMANN, Christopher Hugh ROSINGER
-
Patent number: 8119666Abstract: 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: GrantFiled: December 6, 2006Date of Patent: February 21, 2012Assignee: Novartis AGInventors: David Barnes, Gregory Raymond Bebernitz, Gary Mark Coppola, Travis Stams, Sidney Wolf Topiol, Thalaththani Ralalage Vedananda, James Richard Wareing
-
Publication number: 20120015926Abstract: 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: ApplicationFiled: November 9, 2009Publication date: January 19, 2012Inventors: 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: 8084448Abstract: 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: GrantFiled: March 29, 2007Date of Patent: December 27, 2011Assignee: Novartis AGInventors: 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: 7842758Abstract: The invention concerns compounds, oligomers, and polymers that contain: (I), (II), (III), or (IV) groups; where “-” indicates points of attachment.Type: GrantFiled: January 10, 2007Date of Patent: November 30, 2010Assignee: The Trustees Of The University Of PennsylvaniaInventors: Michael J. Therien, Kimihiro Susumu
-
Publication number: 20100298328Abstract: 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: ApplicationFiled: March 30, 2007Publication date: November 25, 2010Inventors: John J. Baldwin, David A. Claremon, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wenguang Zeng
-
Patent number: 7820702Abstract: 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: GrantFiled: February 1, 2005Date of Patent: October 26, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Lawrence G. Hamann, Yingzhi Bi, Mark C. Manfredi, Alexandra A. Nirschl, James C. Sutton
-
Publication number: 20100249198Abstract: 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: ApplicationFiled: October 17, 2008Publication date: September 30, 2010Applicant: Dompe S.p.AInventors: Alessio Moriconi, Andrea Aramini
-
Patent number: 7763884Abstract: 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: GrantFiled: June 27, 2007Date of Patent: July 27, 2010Assignee: Sony CorporationInventors: Mao Tatsuhara, Akito Ugawa
-
Patent number: 7737283Abstract: 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: GrantFiled: June 9, 2006Date of Patent: June 15, 2010Assignee: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Peter A. Petillo
-
Patent number: 7700633Abstract: 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: GrantFiled: December 6, 2006Date of Patent: April 20, 2010Assignee: Novartis AGInventors: David Barnes, Gregory Raymond Bebernitz, Gary Mark Coppola, Travis Stams, Sidney Wolf Topiol, Thalaththani Ralalage Vedananda, James Richard Wareing, Katsumasa Nakajima
-
Patent number: 7691856Abstract: 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: GrantFiled: January 9, 2007Date of Patent: April 6, 2010Assignees: 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: 20100035942Abstract: 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: ApplicationFiled: December 6, 2006Publication date: February 11, 2010Inventors: David Barnes, Gary Mark Coppola, Travis Stams, Sidney Wolf Topiol
-
Publication number: 20100022525Abstract: The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.Type: ApplicationFiled: October 4, 2007Publication date: January 28, 2010Inventors: 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: 20100022482Abstract: The present invention relates to compounds of formula wherein the residues have various meanings and their use as pharmaceuticals.Type: ApplicationFiled: August 21, 2007Publication date: January 28, 2010Inventors: Karl Baumann, Andreas Billich, Berndt Oberhausen
-
Publication number: 20090181928Abstract: 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: ApplicationFiled: March 29, 2007Publication date: July 16, 2009Inventors: 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: 20090170911Abstract: 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: ApplicationFiled: February 20, 2009Publication date: July 2, 2009Applicant: AJINOMOTO CO. INCInventors: 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: 20090105230Abstract: 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: ApplicationFiled: June 9, 2006Publication date: April 23, 2009Inventors: Daniel L. Flynn, Peter A. Petillo
-
Publication number: 20080293776Abstract: 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: ApplicationFiled: December 6, 2006Publication date: November 27, 2008Inventors: David Barnes, Gregory Raymond Bebernitz, Gary Mark Coppola, Travis Stams, Sidney Wolf Topiol, Thalaththani Ralalage Vedananda, James Richard Wareing
-
Publication number: 20080293782Abstract: 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: ApplicationFiled: December 6, 2006Publication date: November 27, 2008Inventors: David Barnes, Gary Mark Coppola, Robert Edson Damon, Katsumasa Nakajima, Brian Christopher Raudenbush, Travis Stams, Sidney Wolf Topiol, Thalaththani Ralalage Vedananda
-
Publication number: 20080262050Abstract: 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: ApplicationFiled: December 6, 2006Publication date: October 23, 2008Inventors: David Barnes, Gregory Raymond Bebernitz, Gary Mark Coppola, Katsumasa Nakajima, Travis Stams, Sidney Wolf Topiol, Thalaththani Ralalage Vedananda, James Richard Wareing
-
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
-
Patent number: 7432292Abstract: 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: GrantFiled: December 30, 2003Date of Patent: October 7, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jeffrey O. Saunders, Gregory F. Miknis, James F. Blake
-
Publication number: 20080182850Abstract: 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: ApplicationFiled: October 16, 2007Publication date: July 31, 2008Inventors: 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: 20080161366Abstract: 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: ApplicationFiled: December 12, 2007Publication date: July 3, 2008Applicant: WyethInventors: 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: 7358239Abstract: 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 isType: GrantFiled: March 14, 2005Date of Patent: April 15, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
-
Patent number: 7338968Abstract: 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: GrantFiled: December 16, 2004Date of Patent: March 4, 2008Assignee: Schering CorporationInventors: Purakkattle J. Biju, Arthur G. Taveras, J. Robert Merritt, John J. Baldwin, Younong Yu, Junying Zheng, Jianhua Chao, Cynthia J. Aki
-
Publication number: 20080004325Abstract: This invention relates to modulating (e.g., inhibiting) protein tyrosine phosphatase 1b (PTP1b).Type: ApplicationFiled: June 29, 2007Publication date: January 3, 2008Applicant: WyethInventors: Jinbo Lee, Zhao-Kui Wan, Douglas P. Wilson, Eva Binnun, David V. Erbe, Eddine Saiah
-
Patent number: 7291635Abstract: 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: GrantFiled: April 2, 2003Date of Patent: November 6, 2007Assignee: Novartis AGInventors: 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: 7160909Abstract: 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: GrantFiled: July 29, 2002Date of Patent: January 9, 2007Assignee: Eli Lilly and CompanyInventors: Michael Dean Kinnick, Edward David Mihelich, John Michael Morin, Daniel Jon Sall, Jason Scott Sawyer
-
Patent number: 7125869Abstract: 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: GrantFiled: June 10, 2005Date of Patent: October 24, 2006Assignee: Galderma Research & DevelopmentInventors: Laurence Clary, Pascal Collette, Michel Rivier, Andre Jomard
-
Patent number: 7108948Abstract: 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: GrantFiled: February 27, 2004Date of Patent: September 19, 2006Assignee: Samsung Electronics Co., LTDInventors: Zbigniew Tokarski, Nusrallah Jubran, Vytautas Getautis, Juozas V. Grazulevicius, Tadas Malinauskas, Edmundas Montrimas, Valentas Gaidelis
-
Patent number: 7105556Abstract: 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: GrantFiled: May 22, 2002Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. Cheng, Yoon Jeon, Wei Wang
-
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
-
Publication number: 20040198778Abstract: Compounds of Formula (I), 1Type: ApplicationFiled: March 26, 2004Publication date: October 7, 2004Applicant: WyethInventors: 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: 20040167187Abstract: 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: ApplicationFiled: December 30, 2003Publication date: August 26, 2004Inventors: Jeffrey O. Saunders, Gregory F. Miknis, James F. Blake
-
Patent number: 6720342Abstract: 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: GrantFiled: August 28, 2001Date of Patent: April 13, 2004Assignee: Novo Nordisk A/SInventors: Lone Jeppesen, Per Sauerberg
-
Publication number: 20040034025Abstract: Heterocyclic aromatic amides having a hydroxy group adjacent to the amide functionality are useful as antifungal agents, particularly for plants.Type: ApplicationFiled: December 2, 2002Publication date: February 19, 2004Inventors: 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: 20040023974Abstract: Compounds of the formula 1Type: ApplicationFiled: April 2, 2003Publication date: February 5, 2004Inventors: 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