At Least One Of The Ring Hetero Atoms Is Chalcogen Patents (Class 546/83)
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Patent number: 7557211Abstract: The present invention provides for thiazolopyridine-based tricyclic compounds having the formula (I), wherein R1, R2, R5 and R6 are as described herein. The present invention further provides pharmaceutical compositions comprising such compounds, as well as the use of such compounds for treating inflammatory and immune diseases.Type: GrantFiled: November 10, 2005Date of Patent: July 7, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Jagabandhu Das, James Kempson, William J. Pitts, Steven H. Spergel
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Publication number: 20090134784Abstract: Carbazole-containing compounds are provided. In particular, the compounds are oligocarbazole-containing compounds having an unsymmetrical structure. The compounds may be useful in organic light emitting devices, in particular as hosts in the emissive layer of such devices.Type: ApplicationFiled: November 21, 2008Publication date: May 28, 2009Applicant: Universal Display CorporationInventors: Chun Lin, Alexey Dyatkin, Zeinab Elshenawy
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Publication number: 20090117040Abstract: The present invention relates to pharmaceutical and diagnostic compositions as well as to the use of the active substances contained therein for preparing a pharmaceutical or a diagnostic composition for the treatment or diagnosis of neurodegenerative disorders or amyloid diseases.Type: ApplicationFiled: February 11, 2005Publication date: May 7, 2009Applicant: Max-Delbrug-Centrum Fur Molekulare MedizinInventors: Erich Wanker, Sabine Engemann, Susanne Rautenberg, Annett Boeddrich, Phoebe Markovic, Dagmar Ehrnhofer, Martin Herbst, Jacqueline Walther
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Publication number: 20090093465Abstract: The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, and modulating protein kinase activity. Molecules of the invention can modulate casein kinase (CK) activity. The invention also relates in part to methods for using such molecules.Type: ApplicationFiled: August 29, 2008Publication date: April 9, 2009Applicant: Cylene Pharmaceuticals, Inc.Inventors: Fabrice PIERRE, Mustapha HADDACH
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Publication number: 20090035810Abstract: Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.Type: ApplicationFiled: May 29, 2008Publication date: February 5, 2009Applicant: INVITROGEN CORPORATIONInventors: Wai-Yee Leung, Ching-Ying Cheung, Stephen Yue
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Publication number: 20090035809Abstract: Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.Type: ApplicationFiled: May 29, 2008Publication date: February 5, 2009Applicant: INVITROGEN CORPORATIONInventors: Wai-Yee Leung, Ching-Ying Cheung, Stephen Yue
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Publication number: 20090012077Abstract: The present invention relates to compounds and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases, including cathepsins B, K, C, F, H, L, O, S, W and X. Of particular interest are diseases associated with Cathepsin K.Type: ApplicationFiled: June 25, 2008Publication date: January 8, 2009Inventors: Alexander Graham Dossetter, Nicola Murdoch Heron
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Publication number: 20080318998Abstract: Thiazoloquinolines and thiazolonaphthyridines with an alkoxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.Type: ApplicationFiled: February 8, 2006Publication date: December 25, 2008Applicant: COLEY PHARMACEUTICAL GROUP, INC.Inventors: Ryan B. Prince, Bryon A. Merrill, Philip D. Heppner, Tushar M. Kshirsagar, Joshua R. Wurst, Karl J. Manske, Michael J. Rice
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Patent number: 7465742Abstract: This application relates to novel fused tricyclic thienopyridines of Formulas I and II, which useful for treating Hepatitis B infection and other diseases. This application also relates to pharmaceutical compositions comprising thienopyridines and to the use of such compositions to treat Hepatitis B and other diseases.Type: GrantFiled: February 3, 2006Date of Patent: December 16, 2008Inventors: Huanming Chen, Robert Tam, Anneke K. Raney
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Patent number: 7465741Abstract: The invention concerns substituted tricyclic isoxazoline derivatives according to Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisoxazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on the phenylpart of the tricyclic moiety with at least one radical that is attached to the phenyl radical by a carbon-carbon bond as well as processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for treating depression, anxiety, movement disorders, psychosis, Parkinson's disease and body weight disorders including anorexia nervosa and bulimia, wherin all variables are defined in claim 1.Type: GrantFiled: August 12, 2003Date of Patent: December 16, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: José Ignacio Andrés-Gil, José Manuel Bartolomé-Nebreda, Rosa Maria Alvarez-Escobar, Margaretha Henrica Maria Bakker, Antonius Adrianus Hendrikus Petrus Megens
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Patent number: 7462717Abstract: The invention concerns substituted tricyclic isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisoxazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on at least one of the C6- and C9-positions of the phenylpart of the tricyclic moiety with a selected radical, according to Formula (I) wherein X=CH2, N—R7, S or O, R1, R2, R14 and R15 are certain specific substituents, with the proviso that at least one of R14 and R15 is not hydrogen, Pir is preferably an optionally substituted piperidinyl or piperazinyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S; a process for their preparation, pharmaceutical compositions comprising themType: GrantFiled: August 19, 2003Date of Patent: December 9, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, Maria Encarnacion Matesanz-Ballesteros, Margaretha Henrica Maria Bakker, Antonius Adrianus Hendrikus Petrus Megens
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Publication number: 20080287432Abstract: The invention provides a novel class of compounds of formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the AbI, Bcr-AbI, Aurora-A, SGK, Tie-2, Trk-B, FGFR3, c-kit, b-RAF, c-RAF, DYRK2, Fms, Fyn and PDGFRalpha and PDGFR&bgr; kinases.Type: ApplicationFiled: August 15, 2006Publication date: November 20, 2008Applicants: IRM LLC, The Scripps Research InstituteInventors: Barun Okram, Pingda Ren, Nathanael S. Gray
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Patent number: 7439253Abstract: The invention relates to novel heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a method for preparing these compounds, and to their use as medicaments, in particular as antibacterials and ?-lactamase inhibitors.Type: GrantFiled: December 4, 2003Date of Patent: October 21, 2008Assignee: NovexelInventors: Maxime Lampilas, Branislav Musicki, Michel Klich, David Alan Rowlands
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Publication number: 20080114020Abstract: The invention provides compounds of the formula (I) in which the substituents and symbols are as defined in the description. The compounds inhibit the secretion of gastric acid.Type: ApplicationFiled: October 13, 2005Publication date: May 15, 2008Applicant: Altana Pharma AGInventors: Wilm Buhr, Peter Jan Zimmermann, Christof Brehm, Adreas Palmer, M.Vittoria Chiesa, Wolfgang-Alexander Simon, Stefan Postius, Wolfgang Kromer, Georg Rast, Udo Doelling
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Publication number: 20080090834Abstract: The invention pertains to heteroaromatic compounds of the formula I, as defined herein, that serve as effective phosphodiesterase (PDE) inhibitors. In particular, the invention relates to said compounds which are selective inhibitors of PDE10. The invention also relates to pharmaceutical compositions comprising said compounds; and the use of said compounds in a method for treating certain central nervous system (CNS) or other disorders.Type: ApplicationFiled: June 29, 2007Publication date: April 17, 2008Inventors: Dennis J. Hoover, Kevin G. Witter
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Patent number: 7326784Abstract: The invention relates to compounds of the formula 1, in which R1, R2, R3, Arom and PG have the meanings as indicated in the description. These compounds are valuable intermediates for the preparation of pharmaceutically active compounds.Type: GrantFiled: December 17, 2004Date of Patent: February 5, 2008Assignee: Altana Pharma AGInventors: Andreas Palmer, Ulrike Nettekoven
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Patent number: 7291733Abstract: Disclosed are substituted tricyclic heterocycle compounds of the formulas (I), (II) and (III) shown below, wherein R1, R2, R3 and R4 are described herein, which are active as anti-inflammatory agents.Type: GrantFiled: October 7, 2004Date of Patent: November 6, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Charles Lawrence Cywin, Roman Wolfgang Fleck, Eugene Richard Hickey, Weimin Liu, Tina Marie Morwick, John Robert Proudfoot, Denice M. Spero
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Patent number: 7288543Abstract: A compound of the formula (I) (I) wherein the variables X1 to X6, Ra, Rb, R1 to R7 including R3?, E, p, j, y, z, A, B and C are as described or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosedType: GrantFiled: March 8, 2005Date of Patent: October 30, 2007Assignee: Eli Lilly and CompanyInventors: Howard Barff Broughton, Nuria Diaz Buezo, Charles Howard Mitch, Concepcion Pedregal-Tercero
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Patent number: 7288549Abstract: The invention relates to new heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a process for the preparation of these compounds, as well as their use as medicaments, in particular as anti-bacterial agents.Type: GrantFiled: June 4, 2002Date of Patent: October 30, 2007Assignee: Aventis Pharma S.A.Inventors: Joseph Aszodi, Maxime Lampilas, Branislav Musicki, David Alan Rowlands, Pascal Colette
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Patent number: 7265103Abstract: The invention concerns substituted amino isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisozazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on the phenylpart of the tricyclic moiety with primary, secondary and/or tertiary amino groups, according to Formula (I) wherein X=CH2, N—R7, S or O, R1, R2 and R3 are certain specific substituents, with the proviso that at least one of R1 and R2 is an amino radical of formula N—R10R11 wherein R10 and R11 are each a variety of radicals, Pir is an optionally substituted piperidyl or piperazyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S; a process for their preparation, pharmaceutiType: GrantFiled: March 27, 2003Date of Patent: September 4, 2007Assignee: Janssen Pharmaceutica NV.Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, Margaretha Henrica Maria Bakker, Ana Isabel De Lucas Olivares
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Patent number: 7199128Abstract: The invention provides compounds and salts of Formula I and Formula II: which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A1, A8, R2, R3, R5, R6, R7, and R9 are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of compounds of Formula I and/or Formula II and one or more other active agents. The invention also provides methods for treating microbial and protozoal infections in animals.Type: GrantFiled: February 1, 2006Date of Patent: April 3, 2007Assignee: Achillion Pharmaceuticals, Inc.Inventors: Barton J. Bradbury, Jason Allan Wiles, Milind Deshpande, Qiuping Wang, Akihiro Hashimoto, Edlaine Lucien
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Patent number: 7189736Abstract: Compounds of formula 1, in which the substituents have the meanings mentioned in the description are suitable for the prevention and treatment of gastrointestinal diseases.Type: GrantFiled: April 19, 2004Date of Patent: March 13, 2007Assignee: Altana Pharma AGInventors: Jörg Senn-Bilfinger, Wilm Buhr
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Patent number: 7176214Abstract: The present invention provides for pyrazolopurine-based tricyclic compounds having the formula (I), wherein R1, R2, R3, R4, R5 and R6 are as described herein. The present invention further provides pharmaceutical compositions comprising such compounds, as well as the use of such compounds for treating inflammatory and immune diseases.Type: GrantFiled: May 18, 2004Date of Patent: February 13, 2007Assignee: Bristol-Myers Squibb CompanyInventors: William J. Pitts, Makonen Belema, Patrice Gill, James Kempson, Yuping Qiu, Claude A. Quesnelle, Steven H. Spergel, Fred Christopher Zusi
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Patent number: 7169786Abstract: The invention concerns substituted isoxazolines derivatives according to Formula (I): wherein X=CH?2#191, N—R7, S or O, R1, R2 and R3 are certain specific substituents, Pir is an optionally substituted piperidyl or piperazyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S; a process for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for the treatment of depression and/of anxiety and disorders of body weight. The compounds according to the invention have surprisingly been shown to have a serotonine (5-HT) reuptake inhibitor activity in combination with additional ?2-adrenoceptor antagonist activity and show a strong anti-depressant activity without being sedative.Type: GrantFiled: February 13, 2002Date of Patent: January 30, 2007Inventors: José Ignacio Andrés-Gil, Francisco Javier Fernández-Gadea, Manuel Jesús Alcázar-Vaca, José Maria Cid-Nuñez, Joaquin Pastor-Fernandez, Antonius Adrianus Hendrikus Petrus Megens, Godelieve Irma Christine Maria Heylen, Xavier Jean Michel Langlois, Margaretha Henrica Maria Bakker, Thomas Horst Wolfgang Steckler
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Patent number: 7169926Abstract: Compounds are provided which may be used to inhibit DPP-IV comprising the formula: wherein the substituents are as described in the specification and claims.Type: GrantFiled: August 12, 2004Date of Patent: January 30, 2007Assignees: Takeda Pharmaceutical Company Limited, Array BioPharma Inc.Inventors: Laurence E. Burgess, Scott D. Cowen, Stephen L. Gwaltney, II, Jeongboeb Seo, Jeffrey A. Stafford
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Patent number: 7148232Abstract: Thiazolo-, oxazolo- and selenazolo[4,5-c]quinolin-4-amines and analogs thereof are described including methods of manufacture and the use of novel intermediates. The compounds are immunomodulators and induce cytokine biosynthesis, including interferon and/or tumor biosynthesis, necrosis factor, and inhibit the T-helper-type 2 immune response. The compounds are further useful in the treatment of viral and neoplastic diseases.Type: GrantFiled: August 25, 2004Date of Patent: December 12, 2006Assignee: 3M Innovative Properties CompanyInventors: John F. Gerster, Kyle J. Lindstrom, Gregory J. Marszalek
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Patent number: 7144885Abstract: This invention relates to a novel fused tricyclic heterocycle of the formula (Ia, Ib) and its use for the treatment of hyper-proliferative disordersType: GrantFiled: February 21, 2003Date of Patent: December 5, 2006Assignee: Bayer Pharmaceuticals CorporationInventors: Chengzhi Zhang, Michael Burke, Zhi Chen, Jacques Dumas, Dongping Fan, Benjamin D. Jones, Gaetan Ladouceur, Wendy Lee, Barton Phillips, Scott M. Wilhelm, Qian Zhao
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Patent number: 7141578Abstract: Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.Type: GrantFiled: October 25, 2004Date of Patent: November 28, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Mark E. Salvati, James Aaron Balog, Dacia A. Pickering, Sören Giese, Aberra Fura, Wenying Li, Ramesh N. Patel, Ronald L. Hanson, Toomas Mitt, Jacques Y. Roberge, James R. Corte, Steven H. Spergel, Richard A. Rampulla, Raj N. Misra, Hai-Yun Xiao
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Patent number: 7101891Abstract: The present invention relates to a compound of formula (I), which are useful for inhibiting resistant neoplasms where the resistance is conferred in part or in total by MRP1Type: GrantFiled: March 27, 2002Date of Patent: September 5, 2006Assignee: Eli Lilly and CompanyInventors: Jeffrey Daniel Cohen, Louis Nickolaus Jungheim, Brian Stephen Muehl, Kenneth Jeff Thrasher
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Patent number: 7064131Abstract: The present invention relates to a compound of formula (I) which are useful for inhibiting resistant neoplasms where the resistance is conferred in part or in total by MRP1.Type: GrantFiled: March 27, 2002Date of Patent: June 20, 2006Assignee: Eli Lilly and CompanyInventors: Peter Ambrose Lander, Mark Christopher Lohman
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Patent number: 7037921Abstract: The present invention relates to a compound of Formula (I), which are useful for inhibiting resistant neoplasms where the resistance is conferred in part or in total by MRP1.Type: GrantFiled: March 28, 2002Date of Patent: May 2, 2006Assignee: Eli Lilly and CompanyInventors: Rosanne Bonjouklian, Louis Nickolaus Jungheim, Kenneth Jeff Thrasher
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Patent number: 7018840Abstract: The present invention is directed, in part, to fluorescent metal sensors for detecting metal ions, and methods of making and using the same.Type: GrantFiled: April 17, 2002Date of Patent: March 28, 2006Assignee: Massachusetts Institute of TechnologyInventors: Stephen J. Lippard, Shawn Burdette
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Patent number: 6949648Abstract: Novel pharmaceutical compositions for inhibiting Th2-selective immune response and pharmaceutical compositions for inhibiting cyclooxygenase comprising condensed pyrazole derivatives represented by the general formula (I): or salts thereof.Type: GrantFiled: March 27, 2001Date of Patent: September 27, 2005Assignee: Takeda Pharmaceutical Company LimitedInventors: Osamu Uchikawa, Keita Mitsui, Akiko Asakawa, Shigeru Morimoto, Masataka Yamamoto, Hiroyuki Kimura, Takeo Moriya, Masahiro Mizuno
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Patent number: 6936623Abstract: Compounds of the formula (I), in which the substituents have the meanings mentioned in the description, are suitable for the prevention and treatment of gastrointestinal diseases.Type: GrantFiled: April 1, 2004Date of Patent: August 30, 2005Assignee: Altana Pharma AGInventors: Jörg Senn-Bilfinger, Wilm Buhr
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Patent number: 6927292Abstract: The invention relates to compounds of Formula (1), in which the substituents and symbols have the meanings indicated in the description. The compounds are valuable intermediates for the preparation of pharmaceutical active compounds.Type: GrantFiled: July 31, 2002Date of Patent: August 9, 2005Assignee: Altana Pharma AGInventors: Jörg Senn-Bilfinger, Peter Jan Zimmermann
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Patent number: 6916925Abstract: Dye labeled imidazonaphthyridine, imidazopyridine and imidazoquinoline compounds having immune response modulating activity are disclosed. The compounds arc useful, inter alia, for determining the binding and/or receptor sites of the molecules.Type: GrantFiled: July 22, 2003Date of Patent: July 12, 2005Assignee: 3M Innovative Properties Co.Inventors: Michael J. Rice, Mark A. Tomai, Ai-Ping Wei
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Patent number: 6906063Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 2, 2001Date of Patent: June 14, 2005Assignee: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Wolin Huang, Charles K. Marlowe, Kim A. Kane-MaGuire
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Patent number: 6869949Abstract: The invention relates to imidazopyridines of a certain formula 1, in which the substituents and symbols have the meanings indicated in the description. The compounds have gastric secretion-inhibiting properties.Type: GrantFiled: October 23, 2001Date of Patent: March 22, 2005Assignee: Altana Pharma AGInventors: Jörg Senn-Bilfinger, Wilm Buhr, Peter Zimmermann, Bernhard Kohl
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Patent number: 6858621Abstract: The present invention is directed to novel 2-(quinolonyl)-fused heterocyclyl derivatives of the general formula (I) wherein R1, R2, R3, R3a, R4, R5, R6 and R7 are as herein defined, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: GrantFiled: April 11, 2003Date of Patent: February 22, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: James C. Lanter, Zhihua Sui, James J. Fiordeliso
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Patent number: 6833374Abstract: The present invention provides a compound of formula I and the use thereof for the immunotherapeutic treatment of transplant rejection, autoimmune disease or graft vs. host disease.Type: GrantFiled: July 28, 2003Date of Patent: December 21, 2004Assignee: WyethInventors: Neal Jeffrey Green, Lihren Chen, Steve Yikkai Tam
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Publication number: 20040235880Abstract: The present invention relates to a compound of formula (I) which are useful for inhibiting resistant neoplasms where the resistance is conferred in part or in total by MRP1.Type: ApplicationFiled: June 25, 2004Publication date: November 25, 2004Inventors: Peter Ambrose Lander, Mark Christopher Lohman
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Patent number: 6821982Abstract: The present invention relates to a method for the preparation for camptothecin and camptothecin-like compounds and to novel intermediates used in this preparation. In particular, the invention provides a process for the preparation of the camptothecin derivative of formula (I′) known by the chemical name “7-(4-methylpiperazino-methylene)-10,11-ethylenedioxy-20(R,S)-camptothecin”, which comprises cyclising the compound of formula (II′), wherein X is halogen, particularly chloro, bromo, or iodo; and when the compound of formula (I′) is obtained as a mixture of enantiomers optionally resolving the mixture to obtain the desired enantiomer; and/or if desired, converting the resulting compound of formula (I′) or a salt thereof into a physiologically acceptable salt or solvate thereof.Type: GrantFiled: March 24, 2003Date of Patent: November 23, 2004Assignee: OSI Pharmaceuticals, Inc.Inventors: Francis Gerard Fang, Edward McDonald Huie, Shiping Xie, Daniel L. Comins
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Patent number: 6812247Abstract: A metal complex and its use for binding or cleaving a nucleic acid. The metal complex has the formula: M is Pt, Pd, Ni, Co, or Cu; X is aryl, heteroaryl, cyclyl, or heterocyclyl; Y is halogen, tosylate, mesylate, triflate, pyrophosphate, or carboxylate; each of A1 and A2, independently, is N or C; each of A3 and A4, independently, is N, S, or O, wherein A1, A2, A3, and A4 taken together have one positive charge; and each of R1 and R2, independently, is alkyl, aryl, heteroaryl, alkoxyl, aryloxyl, heteroaryloxyl, alkoxylcarbonyl, aryloxylcarbonyl, or heteroaryloxylcarbonyl.Type: GrantFiled: September 30, 2002Date of Patent: November 2, 2004Assignee: Academia SinicaInventors: Kuang-Lieh Lu, Jih-Ru Hwu, Shwu-Chen Tsay, Sheng-Fa Yu, Jui-Te Hung, Jiann-Jyh Huang
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Publication number: 20040180920Abstract: Compounds of the formula (I), in which the substituents have the meanings mentioned in the description, are suitable for the prevention and treatment of gastrointestinal diseases.Type: ApplicationFiled: April 1, 2004Publication date: September 16, 2004Applicant: ALTANA PHARMA AGInventors: Jorg Senn-Bilfinger, Wilm Buhr
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Publication number: 20040176405Abstract: The present invention further relates to a method of inhibiting MRP1 in a mammal which comprises administering to a mammal in need thereof an effective amount of a compound of formula (I).Type: ApplicationFiled: March 10, 2004Publication date: September 9, 2004Inventors: Julian Kroin, Bryan Hurst Norman, Jeremy Schulenburg York
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Publication number: 20040176595Abstract: The present invention provides non-steroidal compounds of formula I which are selective modulators (i.e., agonist and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compositions containing these compounds and methods for using these compounds to treat animals requiring glucocorticoid receptor agonist or antagonist therapy. Glucocorticoid receptor modulators are useful to treat diseases, such as obesity, diabetes, inflammation and others as described below. The present invention also provides intermediates and processes for preparing these compounds.Type: ApplicationFiled: November 25, 2003Publication date: September 9, 2004Applicant: Pfizer, Inc.Inventors: Robert L. Dow, Kevin K. Liu, Bradley P. Morgan, Andrew G. Swick
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Patent number: 6780872Abstract: Compounds of formula I are useful in treating diseases prevented by or ameliorated with potassium channel openers. Also disclosed are potassium channel opening compositions and a method of opening potassium channels in a mammal.Type: GrantFiled: January 22, 2003Date of Patent: August 24, 2004Assignee: Abbott LaboratoriesInventors: Irene Drizin, Robert J. Altenbach, William A. Carroll
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Patent number: 6765011Abstract: The present invention is directed to novel 7-heterocyclyl quinoline and thieno[2,3-b]pyridine derivatives of the general formula (I) or (II) wherein all variables are as herein defined, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions associated with gonadotropin releasing hormone (GnRH). The compounds of the invention are antagonists of GnRH, useful in the treatment of the infertility, prostate cancer, benign prostate hyperplasia (BPH) and as contraceptives.Type: GrantFiled: April 3, 2003Date of Patent: July 20, 2004Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Zhihua Sui, Mark Macielag, James C. Lanter
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Publication number: 20040138222Abstract: Compounds of the formula: 1Type: ApplicationFiled: September 10, 2003Publication date: July 15, 2004Inventors: Gary Paul Stack, Michael Byron Webb, Deborah Ann Evrard, Dahui Zhou
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Publication number: 20040116460Abstract: The present invention relates to a compound of formula (I), which are useful for inhibiting resistant neoplasms where the resistance is conferred in part or in total by MRP1.Type: ApplicationFiled: September 25, 2003Publication date: June 17, 2004Inventors: Jeffrey Daniel Cohen, Louis Nickolaus Jungheim, Brian Stephen Muehl, Kenneth Jeff Thrasher