Plural 1,4-diazine Rings Attached Directly Or Indirectly To Each Other By Nonionic Bonding Patents (Class 514/252.11)
-
Patent number: 7262197Abstract: This invention is directed to heterocyclyl-substituted anilino phospholipase C inhibitor compounds useful in treating or ameliorating an inflammatory disorders and/or restenosis of the general formula (I): and enantiomers, diastereomers and pharmaceutically acceptable salts thereof. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions affected by phospholipase modulation.Type: GrantFiled: March 31, 2004Date of Patent: August 28, 2007Assignee: Janssen Pharmaceutica, N.VInventors: Bharat Lagu, Kenneth Rupert, Michael Wachter
-
Patent number: 7259162Abstract: The present invention is related to benzazole derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzazole derivatives. Said benzazole derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and/or 3. The present invention is furthermore related to novel benzazole derivatives as well as to methods of their preparation. X is O, S or NR0, with R0 being H or an unsubstituted or substituted C1-C6 alkyl; G is an unsubstituted or substituted pyrimidinyl group.Type: GrantFiled: December 20, 2000Date of Patent: August 21, 2007Assignee: Applied Research Systems Ars Holding N.V.Inventors: Serge Halazy, Dennis Church, Montserrat Camps, Pascale Gaillard, Jean-Pierre Gotteland
-
Patent number: 7253168Abstract: Compounds of Formula I are provided, in which variables are as described herein: Such compounds may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).Type: GrantFiled: April 6, 2005Date of Patent: August 7, 2007Assignee: Neurogen CorporationInventors: Alan J. Hutchison, Bertrand L. Chenard, James G. Tarrant, Guiying Li, Manuka Ghosh, George P. Luke, John M. Peterson, Wallace C. Pringle, Mary-Margaret E. O'Donnell, Kyungae Lee, Linda M. Gustavson, Dario Doller
-
Patent number: 7244722Abstract: Compounds of the general formula (I): wherein m, n, R1, R2, R3 and R4 are as described in the specification. Further included are pharmaceutical compositions comprising the compounds, processes for their preparation, as well as the use of the compounds for the preparation of a medicament for the treatment of 5-HT2A receptor-related disorders or medical conditions.Type: GrantFiled: July 17, 2003Date of Patent: July 17, 2007Assignee: Biovitrum ABInventors: Magnus Cernerud, Helena Lundström, Björn M Nilsson, Markus Thor
-
Patent number: 7238688Abstract: Disclosed are novel compounds of the formula Also disclosed are pharmaceutical compositions comprising the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I in combination with a H1 receptor antagonist.Type: GrantFiled: October 27, 2004Date of Patent: July 3, 2007Assignee: Schering CorporationInventors: Stuart B. Rosenblum, Qingbei Zeng, Mwangi Wa Mutahi, Robert G. Aslanian, Pauline C. Ting, Neng-Yang Shih, Daniel M. Solomon, Jianhua Cao, Henry A. Vaccaro, Kevin D. McCormick, John J. Baldwin, Ge Li
-
Patent number: 7238693Abstract: The present invention relates to novel compounds, the preparation and use, particularly therapeutic, thereof. More specifically, it relates to compounds derived from aryl carbamates, the preparation and use thereof, particularly in the field of human and animal health. The compounds according to the invention are preferably 5-HT4 serotoninergic receptor ligands and can therefore be used in the therapeutic or prophylactic treatment of any disorder involving a 5-HT4 receptor. The invention also relates to pharmaceutical compositions comprising such compounds, the preparation and use thereof and treatment methods using said compounds.Type: GrantFiled: February 22, 2002Date of Patent: July 3, 2007Assignees: Cerep, Centre National de la Recherche Scientifique, Institut National de la Santa et de la Recherche Medicale (inserm)Inventors: Eric Nicolai, Sophie Curtet, James Sicsic, Frank Lezoualc'h, Rodolphe Fischmeister, Michel Langlois, Magali Maillet, Michèle Launay
-
Patent number: 7226925Abstract: The invention relates to compounds of the general Formula (I): The compounds may be prepared by per se conventional methods and can be used for treating a human or animal subject suffering from a serotonin-related disorder. The invention also relates to such use as well as to pharmaceutical compositions comprising a compound of Formula (I).Type: GrantFiled: June 18, 2003Date of Patent: June 5, 2007Assignee: Biovitrum ABInventors: Björn M. Nilsson, Erik Ringberg, Birger Sjöberg, Mattias Jönsson
-
Patent number: 7202248Abstract: Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, Y and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.Type: GrantFiled: January 31, 2006Date of Patent: April 10, 2007Assignee: Avanir PharmaceuticalsInventors: Federico C. A. Gaeta, Andrew Baird, Jerry Anchin, Wenbin Ying, Robert Florkiewicz, Jagadish Sircar, Sunil Kumar K. C.
-
Patent number: 7196080Abstract: The present invention relates to a compound which is represented by the following general formula and has type 4 phosphodiesterase inhibitory action, and uses and an intermediate compound thereof. (wherein R1, R2: hydrogen, a halogen, a lower alkyl, a lower alkoxy, or the like, R3, R4: hydrogen, a (substituted) lower alkyl, a halogen, or the like, R5: hydrogen, a lower alkyl, a lower alkoxycarbonyl, or the like, and n: 0 or 1).Type: GrantFiled: June 13, 2002Date of Patent: March 27, 2007Assignee: Astellas Pharma Inc.Inventors: Masahiro Iwata, Noriyuki Kawano, Hiroyuki Kaizawa, Tomofumi Takuwa, Issei Tsukamoto, Ryushi Seo, Kiyoshi Yahiro, Miki Kobayashi, Makoto Takeuchi
-
Patent number: 7192958Abstract: The present invention relates to compounds represented by formula (I): in which at least one of R3 and R4 is a group represented by formula (A): where the structural variables are defined herein. The compounds are useful for blocking sodium channels.Type: GrantFiled: April 21, 2004Date of Patent: March 20, 2007Assignee: Parion Sciences, Inc.Inventor: Michael R. Johnson
-
Patent number: 7192961Abstract: Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, Y and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.Type: GrantFiled: May 2, 2006Date of Patent: March 20, 2007Assignee: Avanir PharmaceuticalsInventors: Federico C. A. Gaeta, Andrew Baird, Jerry Anchin, Wenbin Ying, Robert Florkiewicz, Jagadish Sircar, Sunil Kumar K. C.
-
Patent number: 7192960Abstract: The present invention relates to a compound represented by formula (I): in which at least one of R3 and R4 is a group represented by formula (A): where the structural variables are as defined herein. The compounds are useful for blocking sodium channels.Type: GrantFiled: April 21, 2004Date of Patent: March 20, 2007Assignee: Parion Sciences, Inc.Inventor: Michael R. Johnson
-
Patent number: 7189715Abstract: The invention is directed to racemic and stereomerically pure compounds of Formula 3: and to pharmaceutical compositions comprising them, methods of their use, and methods of their preparation.Type: GrantFiled: October 24, 2003Date of Patent: March 13, 2007Assignee: Sepracor Inc.Inventors: Thomas P. Jerussi, Qun K. Fang
-
Patent number: 7186715Abstract: The present invention relates to melanocortin receptor agonists of formula I, which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunctionType: GrantFiled: January 23, 2002Date of Patent: March 6, 2007Assignee: Eli Lilly and CompanyInventors: Karin Briner, Christopher William Doecke, Vincent Mancuso, Michael John Martinelli, Timothy Ivo Richardson, Roger Ryan Rothhaar, Qing Shi, Chaoyu Xie
-
Patent number: 7179807Abstract: Novel 5-substituted-2-arylpyrazine compounds are provided. Such compounds can act as selective modulators or CRF receptors. Compounds of the invention are provided by the following formula: The 5-substituted-2-arylpyrazine compounds provided herein are useful in the treatment of a number of CNS and periphercal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds provided are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.Type: GrantFiled: August 20, 2003Date of Patent: February 20, 2007Assignee: Neurogen CorporationInventors: Taeyoung Yoon, Ping Ge, Stéphane De Lombaert, Raymond F. Horvath, Dario Doller, Kevin J. Hodgetts, Lu Yan Zhang, Bernd Kaiser, Xuechun Zhang, Yasuchika Yamaguchi, Cunyu Zhang, Jim Darrow
-
Patent number: 7173034Abstract: This invention concerns the use of compounds of formula (I) wherein -a1=a2-a3=a4- is a radical of for CH?CH—, —N?CH—CH?CH—, —CH?N—CH?CH—, —CH?CH—N?CH—, —CH?CH—CH?N— wherein each hydrogen atom may optionally be substituted; Q is a radical of formulas (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), (b-8), G is a direct bond or C1-10alkanediyl; R1 is an optionally substituted monocyclic heterocycle; for the manufacture of a medicament for the treatment of viral infections, in particular RSV infections. Certain compounds of formula (I) are new.Type: GrantFiled: June 3, 2005Date of Patent: February 6, 2007Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, Kathleen Petrus Marie-José Meersman, François Maria Sommen, Jérôme Emile Georges Guillemont, Jean Fernand Armand Lacrampe, Koenraad Jozef Lodewijk Marcel Andries
-
Patent number: 7160886Abstract: Certain novel N-acylated piperazine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: February 27, 2004Date of Patent: January 9, 2007Assignee: Merck & Co., Inc.Inventors: Raman K. Bakshi, Liangqin Guo, Qingmei Hong, Ravi P. Nargund, Patrick G. Pollard, Iyassu K. Sebhat, Feroze Ujjainwalla, Zhixiong Ye
-
Patent number: 7157464Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: June 11, 2003Date of Patent: January 2, 2007Assignee: Chemocentryx, Inc.Inventors: Andrew M. K. Pennell, James B. Aggen, J.J. Kim Wright, Subrabrata Sen, Brian E. McMaster, Daniel Joseph Dairaghi
-
Patent number: 7153858Abstract: The invention relates to 5-HT receptor agonists or antagonists. Novel arylpiperazinyl sulfonamide compounds represented by Formulae I: and II, and synthesis and uses of those compounds for treating diseases including those mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include central nervous system disorders such as generalized anxiety disorder, ADD/ADHD, neural injury, stroke, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.Type: GrantFiled: January 30, 2004Date of Patent: December 26, 2006Assignee: Epix Delaware, Inc.Inventors: Dale S. Dhanoa, Dongli Chen, Oren Becker, Silvia Noiman, Srinivasa Rao Cheruku, Yael Marantz, Anurag Sharadendu, Sharon Shachem, Alexander Heifetz, Pradyumna Mohanty, Boaz Inbal, Merav Fichman, Raphael Nudelman, Shay Bar-Haim
-
Patent number: 7153856Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.Type: GrantFiled: May 26, 2005Date of Patent: December 26, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Joel C. Barrish, John Wityak, Jagabandhu Das, Ping Chen, Derek J. Norris, Gary Schieven
-
17 ?-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases
Patent number: 7138396Abstract: There are disclosed compounds of the formula (I): prodrugs thereof, or pharmaceutically acceptable salts of the compounds or of said prodrugs which are useful as inhibitors of Type 3 17?-Hydroxysteroid Dehydrogenase. Also disclosed are pharmaceutical compositions containing said compounds and their use for the treatment or prevention of androgen dependent diseases.Type: GrantFiled: January 28, 2005Date of Patent: November 21, 2006Assignee: Schering CorporationInventors: Timothy J. Guzi, Kamil Paruch, Alan K. Mallams, Jocelyn D. Rivera, Ronald J. Doll, Viyyoor M. Girijavallabhan, Jonathan A. Pachter, Yi-Tsung Liu, Anil K. Saksena -
Patent number: 7122544Abstract: Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure: wherein R1 and R6 are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to IKK inhibition. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.Type: GrantFiled: December 4, 2001Date of Patent: October 17, 2006Assignee: Signal Pharmaceuticals, LLCInventors: Adam Kois, Karen J. MacFarlane, Yoshitaka Satoh, Shripad S. Bhagwat, Jason S. Parnes, Moorthy S. S. Palanki, Paul E. Erdman
-
Patent number: 7119086Abstract: The invention relates to compounds of formula: and also to the salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, with affinity for and selectivity towards the arginine-vasopressin V1b receptors and/or for the ocytocin receptors and, furthermore, for certain compounds, affinity for the V1a receptors. The invention also relates to the process for preparing them, to the intermediate compounds of formula (IV) that are useful for preparing them, to pharmaceutical compositions containing them and to their use for preparing medicinal products.Type: GrantFiled: July 15, 2002Date of Patent: October 10, 2006Assignee: Sanofi-AventisInventors: Alain Di Malta, Georges Garcia, Richard Roux, Bruno Schoentjes, Claudine Serradeil-Le Gal, Bernard Tonnerre, Jean Wagnon
-
Patent number: 7119203Abstract: This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. Such hydroxamic acids generally correspond in structure to the following formula: (wherein A1, A2, Y, E1, E2, E3, and Rx are as defined in this specification), and further include salts of such compounds. This invention also is directed to compositions of such hydroxamic acids, intermediates for the syntheses of such hydroxamic acids, methods for making such hydroxamic acids, and methods for treating conditions (particularly pathological conditions) associated with MMP activity and/or aggrecanase activity.Type: GrantFiled: April 25, 2003Date of Patent: October 10, 2006Assignee: Pharmacia CorporationInventors: Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, David L. Brown, Jeffery N. Carroll, Yiyuan Chen, Yvette M. Fobian, John N. Freskos, Alan F. Gasiecki, Margaret L. Grapperhaus, Robert M. Heintz, Susan L. Hockerman, Darren J. Kassab, Ish K. Khanna, Stephen A. Kolodziej, Mark A. Massa, Joseph J. McDonald, Brent V. Mischke, Deborah A. Mischke, Patrick B. Mullins, Mark A. Nagy, Monica B. Norton, Joseph G. Rico, Michelle A. Schmidt, Nathan W. Stehle, John J. Talley, William F. Vernier, Clara I. Villamil, Lijuan J. Wang, Thomas A. Wynn
-
Patent number: 7105519Abstract: Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, Y and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.Type: GrantFiled: May 24, 2002Date of Patent: September 12, 2006Assignee: Avanir PharmaceuticalsInventors: Federico C. A. Gaeta, Andrew Baird, Jerry Anchin, Wenbin Ying, Robert Florkiewicz, Jagadish Sircar, Sunil Mumar K. C.
-
Patent number: 7101886Abstract: This invention relates to compounds of the formula 1 wherein R1, R3, R4, X1, and X2 are defined as in the specification, pharmaceutical compositions containing them and their use in the treatment of central nervous system and other disorders.Type: GrantFiled: November 7, 2003Date of Patent: September 5, 2006Assignee: Warner Lambert CompanyInventors: Stephen Sung Yong Cho, Jamie Marie Singer, James M. Graham, Tracy Fay Gregory, Harry Ralph Howard, Jr., Sham Shridhar Nikam, Michael Anthony Walters
-
Patent number: 7098213Abstract: Compounds of the formula or a pharmaceutically acceptable salt or isomer thereof, wherein: Q, X and Z are CH or N; R, R4–R7 and R13 are H or alkyl; R1 is H, alkyl, fluoroalkyl, R9-arylalkyl, R9-heteroarylalkyl, alkyl-SO2—, cycloalkyl-SO2—, fluoroalkyl-SO2—, R9-aryl-SO2—, R9-heteroaryl-SO2—, N(R22)(R23)—SO2—, alkyl-C(O)—, cycloalkyl-C(O)—, fluoroalkyl-C(O)—, R9-aryl-C(O)—, NH-alkyl-C(O)— or R9-aryl-NH—C(O)—; R2 is H and R3 is H, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, R9-aryl, R9-arylalkyl, R9-heteroaryl, or R9-heteroarylalkyl, and when X and Z are each CH, R3 is alkoxy, R9-aryloxy, R9-heteroaryloxy, alkylC(O)O—, alkylaminoC(O)O—, alkylC(O)NR13—, alkylOC(O)NR13— or alkylaminoC(O)NR13—; or R2 and R3 together are ?O, ?NOR10, ?N—NR11R12 or ?CH-alkyl; R8 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenymethyl, alpha-substituted benzyl or alpha-substituted heteroarylmethyl; R9–R12 are as defined; are disclosed for the treatment of HIV, solid organ transplant rejection, graType: GrantFiled: October 14, 2005Date of Patent: August 29, 2006Assignee: Schering CorporationInventor: Michael W. Miller
-
Patent number: 7094779Abstract: The present invention relates to a group of novel piperazine oxime derivatives having interesting NK-1 antagonistic activity.Type: GrantFiled: July 3, 2002Date of Patent: August 22, 2006Assignee: Solvay Pharmaceuticals B.V.Inventors: Wouter I. Iwema Bakker, Jan H. van Maarseveen, Hein K. A. C. Coolen, Martinus Th. M. Tulp, Arnoldus H. J. Herremans, Andrew C. Mccreary, Gustaaf J. M. van Scharrenburg, Adrianus van den Hoogenband
-
Patent number: 7084141Abstract: Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, Y and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.Type: GrantFiled: November 7, 2005Date of Patent: August 1, 2006Assignee: Avanir PharmaceuticalsInventors: Federico C. A. Gaeta, Andrew Baird, Jerry Anchin, Wenbin Ying, Robert Florkiewicz, Jagadish Sircar, Sunil Kumar K. C.
-
Patent number: 7071180Abstract: The invention relates to compounds of the general formula (I): wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO2—, —NH—, (ii) a C1-4-alkyl- or C1-6-acyl-substituted nitrogen atom or (iii) a C1-8-alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is —C(R4)(R5)—, —OC(R4)(R5)—, —N(R6)C(R4)(R5)—, —N(R6)—, —O—, —S— or —SO2—; R is optionally substituted C3-8-cycloalkyl, aryl or heteroaryl; R1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ring members, which rings optionally are substituted in one or more positions, or a group —[C(R4)(R5)]xN(R2a)(R3a)]; R2a, R3a, R4, R5, R6 and x are asType: GrantFiled: June 22, 2004Date of Patent: July 4, 2006Assignee: Biovitrum ABInventors: Björn Nilsson, Jan Tejbrant, Benjamin Pelcman, Erik Ringberg, Markus Thor, Jonas Nilsson, Mattias Jönsson
-
Patent number: 7030110Abstract: Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described.Type: GrantFiled: October 4, 2002Date of Patent: April 18, 2006Assignee: Ortho-McNeil Pharmaceuticals, Inc.Inventors: Aihua Wang, Bruce Edward Tomczuk, Tianbao Lu, Richard M. Soll, John Curtis Spurlino, Roger Francis Bone
-
Patent number: 7026314Abstract: Provided herein is a compound of the formula (I) wherein said compound is useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating, disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT1B antagonists. Also provided herein are processes for making compounds of Formula (I) and intermediate compounds.Type: GrantFiled: January 15, 2002Date of Patent: April 11, 2006Assignee: AstraZeneca ABInventors: Marc Chapdelaine, Timothy Davenport, Markus Haeberlein, Carey Horchler, John McCauley, Edward Pierson, Daniel Sohn
-
Patent number: 7015325Abstract: Compounds of the formula (I), in which M, A1, A2, K1 and K2 have the meanings indicated in the description are novel active tryptase inhibitors.Type: GrantFiled: December 16, 2000Date of Patent: March 21, 2006Assignee: ALTANA Pharma AGInventor: Thomas Martin
-
Patent number: 7015216Abstract: Disclosed are a series of heteroaryl-?-alanine derivatives, compositions containing them, processes for their preparation and their use in medicine.Type: GrantFiled: July 19, 2001Date of Patent: March 21, 2006Assignees: Elan Pharmaceuticals, Inc., WyethInventors: 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
-
Patent number: 7008946Abstract: Compounds of the formula or a pharmaceutically acceptable salt or isomer thereof, wherein: Q, X and Z are CH or N; R, R4–R7 and R13 are H or alkyl; R1 is H, alkyl, fluoroalkyl, R9-arylalkyl, R9-heteroarylalkyl, alkyl-SO2—, cycloalkyl-SO2—, fluoroalkyl-SO2—, R9-aryl-SO2—, R9-heteroaryl-SO2—, N(R22)(R23)—SO2—, alkyl-C(O)—, cycloalkyl-C(O)—, fluoroalkyl-C(O)—, R9-aryl-C(O)—, NH-alkyl-C(O)— or R9-aryl-NH—C(O)—; R2 is H and R3 is H, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, R9-aryl, R9-arylalkyl, R9-heteroaryl, or R9-heteroarylalkyl, and when X and Z are each CH, R3 is alkoxy, R9-aryloxy, R9-heteroaryloxy, alkylC(O)O—, alkylaminoC(O)O—, alkylC(O)NR13—, alkylOC(O)NR13— or alkylaminoC(O)NR13—; or R2 and R3 together are ?O, ?NOR10, ?N—NR11R12 or ?CH-alkyl; R8 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenymethyl, alpha-substituted benzyl or alpha-substituted heteroarylmethyl; R9–R12 are as defined; are disclosed for the treatment of HIV, solid organ transplant rejection, graType: GrantFiled: October 21, 2004Date of Patent: March 7, 2006Assignee: Schering CorporationInventor: Michael W. Miller
-
Patent number: 7008945Abstract: The invention concerns amide derivatives of Formula (Ia) wherein X is —NHCO— or —CONH—; m is 0–3; R1 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; n is 0–2; R2 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino and carboxy; R3 is hydrogen, halogeno, (1–6C)alkyl or (1–6C)alkoxy. q is 0–4; and Q is a group such as aryl, aryloxy, aryl—(1–6C)alkoxy, arylamino and N—(1–6C)alkyl-arylamino; or pharmaceutically-acceptable salts or in-vivo-cleavable caters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: GrantFiled: March 13, 2000Date of Patent: March 7, 2006Assignee: AstraZeneca ABInventor: Dearg S. Brown
-
Patent number: 6995161Abstract: Arylpyrazine compounds are provided, including arylpyrazines that can bind with high affinity and high selectivity to CRF1 receptors, including human CRF1 receptors. The invention thus includes methods for treatment of disorders and diseases associated with CRF1 receptors, including CNS-related disorders and diseases, particularly affective disorders and diseases, and acute and chronic neurological disorders and diseases.Type: GrantFiled: February 16, 2001Date of Patent: February 7, 2006Assignee: Neurogen CorporationInventors: Taeyoung Yoon, Ping Ge, Raymond F. Horvath, Stephane DeLombaert, Kevin J. Hodgetts, Dario Doller, Cunyu Zhang
-
Patent number: 6995156Abstract: Compounds of the following formula (I): where a, b, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.Type: GrantFiled: September 22, 2004Date of Patent: February 7, 2006Assignee: Schering AktiengesellschaftInventors: Judi A. Bryant, Brad O. Buckman, Imadul Islam, Raju Mohan, Michael M. Morrissey, Guo Ping Wei, Wei Xu, Shendong Yuan
-
Patent number: 6995151Abstract: Selective MMP-13 inhibitors are isophthalic acid derivatives of the formula wherein: R1, R2, and R3 independently are hydrogen, halo, hydroxy, C1–C6 alkyl, C1–C6 alkoxy, C2–C6 alkenyl, C2–C6 alkynyl, NO2, NR4R5, CN, or CF3; E is independently O or S; A and B independently are OR4 or NR4R5; each R4 and R5 independently are H, C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring, optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is 0 to 6; or a pharmaceutically acceptable salt thereof. The compounds are useful for treating diseases in a mammal that are mediated by MMP enzymes.Type: GrantFiled: February 13, 2002Date of Patent: February 7, 2006Assignee: Warner-Lambert CompanyInventors: Nicole Chantel Barvian, David Thomas Connor, Richard Dennis Dyer, Adam Richard Johnson, William Chester Patt
-
Patent number: 6992086Abstract: The present invention relates to chemical compounds, pharmaceutical compositions comprising said compounds, uses of said compounds and compositions, methods of treatment employing said compounds and compositions, and processes for preparing said compounds. Specifically, this invention relates to novel compounds which are antagonists of MCP-1 function and are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection. More specifically, the invention is related to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases.Type: GrantFiled: November 17, 2003Date of Patent: January 31, 2006Assignee: Telik, Inc.Inventors: Edgardo Laborde, Louise Robinson, Fanying Meng, Brian T. Peterson, Hugo O. Villar, Steven E. Anuskiewicz, Yoshiro Ishiwata, Shoji Yokochi, Yukiharu Matsumoto, Takuji Kakigami, Hideaki Inagaki, Takahito Jomori, Kouji Matsushima
-
Patent number: 6960580Abstract: The present invention relates to nitrogen-containing heterocyclic quinoline compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. More particularly, the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.Type: GrantFiled: March 8, 2002Date of Patent: November 1, 2005Assignee: Millennium Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Anjali Pandey
-
Patent number: 6960588Abstract: Compounds of formula (I) in which M, B1, B2, B3, B4, B5, B6, A1, A2, A3, A4, A5, A6, K1 and K2 have the meanings as indicated in the description, are novel effective tryptase inhibitors.Type: GrantFiled: September 12, 2000Date of Patent: November 1, 2005Assignee: Altana Pharma AGInventor: Thomas Martin
-
Patent number: 6958331Abstract: The invention relates to sulfonyl amine derivatives of formula IA wherein R5A, X1, X2, R9 and R10 are as defined herein, which derivatives are useful as bradykinin B1 receptor antagonists.Type: GrantFiled: June 2, 2000Date of Patent: October 25, 2005Assignee: Novartis AGInventors: Christopher Thomas Brain, William Cantrell, Andrew James Culshaw, Edward Karol Dziadulewicz, Terance William Hart, Timothy John Ritchie, Liladhar Waykole
-
Patent number: 6949552Abstract: There are provided a therapeutic preparation for anxiety neurosis or depression which comprises a MC4 receptor antagonist as an effective ingredient; and a piperazine derivative represented by Formula [1]: [wherein Ar1 is a phenyl group, a substituted phenyl group, a naphthyl group or a substituted naphthyl group; Ar2 is a naphthyl group, a substituted naphthyl group, a quinolyl group, a group represented by the formula: (wherein R4 is a hydrogen atom or a halogen atom; and X—Y is CH—NH, CH—O, CH—S or N—O) or a group represented by the formula: (wherein R5 is a hydrogen atom, a hydroxyl group or a C1-10 alkoxy group); R1 is a hydrogen atom, a C1-10 alkyl group, a C3-8 cycloalkyl group, a C3-10 alkenyl group, a phenyl group, a 1-cyanoethyl group, a pyrimidin-2-yl group or an amidyl group; R2 and R3 are the same or different, and are each a hydrogen atom or a C1-10 alkyl group; A-B is N—CH2, CH—CH2, C(OH)—CH2 or C?CH; T1 is a single bond, —N(R6)— (wherein R6 is a hydrogen atom or a C1-10 alkyl groupType: GrantFiled: June 27, 2001Date of Patent: September 27, 2005Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Shigeyuki Chaki, Taketoshi Okubo, Shin-ichi Ogawa, Takaaki Ishii
-
Patent number: 6939884Abstract: Compositions are provided, which comprise at least one nucleoside analogue inhibitor, pharmaceutically acceptable salts, solvates, or prodrugs thereof and fusaric acid, derivatives, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprising the above compositions are also provided that optionally further include another therapeutically effective compound, such as a carrier. Systemic and topical preparations comprising the above compositions are also provided as well as methods of treating viral diseases by the administration of the above antiviral agents to a patient.Type: GrantFiled: December 3, 2002Date of Patent: September 6, 2005Assignee: Novactyl, Inc.Inventors: Michael G. Douglas, Avinash N. Amin
-
Patent number: 6924287Abstract: This invention concerns the use of compounds of formula (I) wherein -a1=a2-a3=a4- is a radical of formula —CH?CH—CH?CH—, —N?CH—CH?CH—, —CH?N—CH?CH—, —CH?CH—N?CH—, —CH?CH—CH?N— wherein each hydrogen atom may optionally be replaced; Q is a radical of formulas (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), (b-8), G is a direct bond or C1-10alkanediyl; R1 is an optionally substituted monocyclic heterocycle; for the manufacture of a medicament for the treatment of viral infections, in particular RSV infections. Certain compounds of formula (I) are new.Type: GrantFiled: June 20, 2000Date of Patent: August 2, 2005Assignee: Janssen Pharmacatica, N.V.Inventors: Frans Eduard Janssens, Kathleen Petrus Marie-José Meersman, François Maria Sommen, Jérôme Emile Georges Guillemont, Jean Fernand Armand Lacrampe, Koenraad Jozef Lodewijk Marcel Andries
-
Patent number: 6916804Abstract: The subject invention provides compounds having the structure: wherein R1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R2 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; R3 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R2 and R3 are joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present R3 is oxygen; R4 and R5 are each independently substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R4NR5 together form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl mType: GrantFiled: December 20, 2002Date of Patent: July 12, 2005Assignee: OSI Pharmaceuticals, Inc.Inventors: Arlindo Castelhano, Bryan McKibben, Arno Steinig, Eric Collington
-
Patent number: 6900211Abstract: Compounds of the formula or a pharmaceutically acceptable salt or isomer thereof, wherein: Q, X and Z are CH or N; R, R4-R7 and R13 are H or alkyl; R1 is H, alkyl, fluoroalkyl, R9-arylalkyl, R9-heteroarylalkyl, alkyl-SO2—, cycloalkyl-SO2—, fluoroalkyl-SO2—, R9-aryl-SO2—, R9-heteroaryl-SO2—, N(R22)(R23)—SO2—, alkyl-C(O)—, cycloalkyl-C(O)—, fluoroalkyl-C(O)—, R9-aryl-C(O)—, NH-alkyl-C(O)— or R9-aryl-NH—C(O)—; R2 is H and R3 is H, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, R9-aryl, R9-arylalkyl, R9-heteroaryl, or R9-heteroarylalkyl, and when X and Z are each CH, R3 is alkoxy, R9-aryloxy, R9-heteroaryloxy, alkylC(O)O—, alkylaminoC(O)O—, alkylC(O)NR13—, alkylOC(O)NR13— or alkylaminoC(O)NR13—; or R2 and R3 together are ?O, ?NOR10, ?N—NR11R12 or ?CH-alkyl; R8 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenymethyl, alpha-substituted benzyl or alpha-substituted heteroarylmethyl; R9-R12 are as defined; are disclosed for the treatment of HIV, solid organ transplant rejection, graType: GrantFiled: February 6, 2004Date of Patent: May 31, 2005Assignee: Schering CorporationInventor: Michael W. Miller
-
Patent number: 6894050Abstract: Compounds of Formula (IA) that act as 5-HT receptor ligands and their uses in the treatment of diseases linked to the activation of 5-HT2 receptors in animals are described hereinType: GrantFiled: June 5, 2002Date of Patent: May 17, 2005Assignee: Pfizer Inc.Inventors: Phoebe Chiang, William A. Novomisle, Willard M. Welch, Jr., Angel Guzman-Perez, Paul A. DaSilva-Jardine, Ravi S. Garigipati, Kevin K. Liu
-
Patent number: 6861424Abstract: Compounds of the following formula (I): where a, b, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.Type: GrantFiled: June 5, 2002Date of Patent: March 1, 2005Assignee: Schering AktiengesellschaftInventors: Judi A. Bryant, Brad O. Buckman, Imadul Islam, Raju Mohan, Michael M. Morrissey, Guo Ping Wei, Wei Xu, Shendong Yuan