Polycyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos (e.g., Maytansinoids, Etc.) Patents (Class 514/229.5)
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Patent number: 7560457Abstract: The present invention provides compounds of the following structure, wherein R1, R2, R4, R4?, R6, R7, and R15 are defined above: These compounds are useful in treating neurological disorders or complications due to stroke or head injury; benign or malignant neoplastic disease, carcinomas and adenocarcinomas; proliferative disorders; and inflammatory disorders. The compounds are therefore useful as neuroprotective and neuroregenerative, anti-proliferative, and anti-inflammatory agents.Type: GrantFiled: January 26, 2007Date of Patent: July 14, 2009Assignee: WyethInventors: Edmund Idris Graziani, Kevin Pong, Jerauld Skotnicki
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Patent number: 7547692Abstract: The present invention features rifamycin analogs and methods of using these compounds to treat a variety of microbial infections.Type: GrantFiled: December 14, 2006Date of Patent: June 16, 2009Assignee: ActivBiotics Pharma, LLCInventors: John H. van Duzer, Arthur F. Michaelis, William B. Geiss, Douglas G. Stafford, Joseph Raker, Xiang Y. Yu, James M. Siedlecki, Yingfei Yang
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Publication number: 20090149453Abstract: The invention features methods and compositions for treating bacterial infections.Type: ApplicationFiled: December 31, 2008Publication date: June 11, 2009Applicant: ACTIVBIOTICS PHARMA LLCInventor: Chalom B. Sayada
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Publication number: 20090143373Abstract: The compounds include substituted rifamycin derivatives in which a quinolone carboxylic acid pharmacophore is covalently bonded to a benzoxazinorifamycin or a spiropiperidinorifamycin. The rifamycin derivatives are useful as antimicrobial agents and are effective against a number of human and veterinary Gram positive and Gram negative pathogens. The advantage of the inventive compounds is that both the rifamycin and quinolone antibacterial pharmacophores are co-delivered with matched pharmacokinetics to the targeted pathogens of interests. Delivery of multiple antibacterial pharmacophores simultaneously to the targeted pathogens has the maximum chance of achieving synergy and minimizing the development of resistance to the antibiotics given.Type: ApplicationFiled: November 12, 2008Publication date: June 4, 2009Applicant: Cumbre Pharmaceuticals Inc.Inventors: Charles Z. Ding, Yafei Jin, Keith Combrink, In Ho Kim
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Publication number: 20090137575Abstract: In its many embodiments, the present invention provides tetracyclic compounds of formula I or formula II (wherein the various moieties are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.Type: ApplicationFiled: December 17, 2008Publication date: May 28, 2009Inventors: Duane A. Burnett, Wen-Lian Wu
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Publication number: 20090105233Abstract: The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. Molecules of the invention can modulate casein kinase (CK) activity and/or poly(ADP-ribose)polymerase (PARP) activity. The invention also relates in part to methods for using such molecules.Type: ApplicationFiled: August 31, 2007Publication date: April 23, 2009Inventors: Peter C. CHUA, Fabrice Pierre, Jeffrey P. Whitten
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Patent number: 7514427Abstract: HIV inhibitory compounds of formula: salts and stereoisomers thereof, wherein R1 and R2 are hydrogen or optionally substituted C1-10alkyl; R3 is n is 1, 2 or 3; R3a is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, hydroxycarbonyl, aminocarbonyl, C 1-4alkyloxycarbonyl, mono- or di(C1-4alkyl)aminocarbonyl, C1-4alkylcarbonyl, methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy-methanimidamidyl or Het; or R3 is a monocyclic or bicyclic aromatic heterocyclic ring system, wherein one, two, three or four ring members are nitrogen, oxygen and sulfur, and wherein the remaining ring members are carbon atoms; and wherein each of said heterocyclic ring systems may optionally be substituted; X is —NR7—, —O— or —S—; pharmaceutical compositions containing these compounds, methods for preparing these compounds and compositions.Type: GrantFiled: January 10, 2006Date of Patent: April 7, 2009Assignee: Tibotec Pharmaceuticals, Ltd.Inventors: Bart Rudolf Romanie Kesteleyn, Pierre Jean-Marie Raboisson, Wim Van De Vreken, Maxime Francis Jean-Marie Ghislain Canard
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Publication number: 20090088423Abstract: The invention features methods and compositions for treating bacterial infections.Type: ApplicationFiled: October 21, 2008Publication date: April 2, 2009Applicant: ACTIVBIOTICS PHARMA LLCInventor: Chalom B. Sayada
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Patent number: 7494991Abstract: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3?-hydroxy analogs, and/or various fused ring systems with the benzene ring at the 4?,5? or 5?,6? positions.Type: GrantFiled: May 17, 2007Date of Patent: February 24, 2009Assignee: ActivBiotics Pharma, LLCInventors: John H. van Duzer, Arthur F. Michaelis, William B. Geiss, Douglas G. Stafford, Xiang Y. Yu, James M. Siedlecki, Yingfei Yang
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Patent number: 7488726Abstract: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3?-hydroxy analogs, 5?-halo and/or alkoxy analogs, and various 4?- and/or 6?-substituents that incorporate a cyclic amine moiety.Type: GrantFiled: November 2, 2006Date of Patent: February 10, 2009Assignee: ActivBiotics Pharma, LLCInventors: John H. Van Duzer, James M. Siedlecki, Xiang Y. Yu
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Publication number: 20090012071Abstract: The present invention provides compounds of the formula that possess antimicrobial activity. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity. Particular compounds provided herein are also potent and/or selective inhibitors of microbial DNA synthesis and reproduction. The invention provides anti-microbial compositions, including pharmaceutical compositions, containing a compound of the invention and one or more or more carriers. The invention provides pharmaceutical compositions containing a 4-substituted-1H-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2H,9H)-dione or related compound as the only active agent or in combination with one or more other active agents.Type: ApplicationFiled: April 23, 2008Publication date: January 8, 2009Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Barton James Bradbury, Milind Deshpande, Akihiro Hashimoto, Ha Young Kim, Edlaine Lucien, Godwin Pais, Michael John Pucci, Qiuping Wang, Jason Allan Wiles
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Publication number: 20090005371Abstract: Fused [1,2]imidazo[4,5-c] ring compounds, e.g., fused [1,2]imidazo[4,5-c]quinolines and [1,2]imidazo[4,5-c]naphthyridines, with a substituent, e.g., a substituted 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 10, 2006Publication date: January 1, 2009Inventors: Michael J. Rice, Bryon A. Merrill, Philip D. Heppner
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Patent number: 7470682Abstract: Compounds of the following structure, wherein R1, R2, R4, R4?, R6, R7, and R15 are defined above, are provided: These compounds are useful in treating neurological disorders or complications due to stroke or head injury. The compounds are therefore useful as neuroprotective and neuroregenerative agents.Type: GrantFiled: August 14, 2007Date of Patent: December 30, 2008Assignee: WyethInventors: Edmund Idris Graziani, Kevin Pong, Jerauld Skotnicki
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Publication number: 20080318938Abstract: The invention relates in part to methods for inhibiting proliferation of cancer cells and treating one or more cell proliferative conditions using compounds described herein.Type: ApplicationFiled: June 20, 2008Publication date: December 25, 2008Inventors: David M. RYCKMAN, Denis Drygin, Jeffrey P. Whitten, Kenna Anderes, Katy Trent, Levan Darjania, Mustapha Haddach, Sean O'Brien, William G. Rice
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Publication number: 20080318939Abstract: The invention relates in part to methods for treating ophthalmic conditions using compounds described herein. The conditions to be treated include various ocular cancers. The compositions employed include a polycyclic quinolinone derivative or related heteroaromatic analog thereof.Type: ApplicationFiled: June 20, 2008Publication date: December 25, 2008Inventors: Jeffrey P. WHITTEN, Sean O'Brien
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Publication number: 20080312218Abstract: In its many embodiments, the present invention provides tetracyclic compounds of formula I or formula II (wherein the various moieties are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimers disease.Type: ApplicationFiled: September 21, 2006Publication date: December 18, 2008Inventors: Duane A. Burnett, Wen-Lian Wu
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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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Patent number: 7456177Abstract: The present invention provides a compound having the structure of formula I: wherein R1 is hydrogen, (C1–C6) alkyl, unconjugated (C3–C6) alkenyl, benzyl, YC(?O)(C1–C6) alkyl or —CH2CH2—O—(C1–C4) alkyl; X is CH2 or CH2CH2; Y is (C2–C6) alkylene; Z is (CH2)m, CF2, or C(?O), where m is 0, 1 or 2; R2 and R3 are selected independently from hydrogen, halogen, —(C1–C6) alkyl optionally substituted with from 1 to 7 halogen atoms, and —O(C1–C6) alkyl optionally substituted with from 1 to 7 halogen atoms, or R2 and R3 each together with the atom to which it is connected independently form C(?O), S?O, S(?O)2, or N?O; and is a 5- to 7-membered monocyclic heteroaryl group selected from pyridinyl, pyridone, pyridazinyl, imidazolyl, pyrimidinyl, pyrazolyl, triazolyl, pyrazinyl, furyl, thienyl, isoxazolyl, thiazolyl, oxazolyl, isothiazolyl, pyrrolyl, cinnolinyl, triazinyl, oxadiazolyl, thiadiazolyl and furazanyl groups.Type: GrantFiled: July 12, 2004Date of Patent: November 25, 2008Assignee: Pfizer Inc.Inventors: Martin P. Allen, Jotham W. Coe, Spiros Liras, Christopher J. O'Donnell, Brian T. O'Neill
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Publication number: 20080269192Abstract: Fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines) with a —CH(—X1—R1)-group in the fused ring at the 1-position of the imidazo ring, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, 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: December 29, 2005Publication date: October 30, 2008Applicant: Coley Pharmaceutical Group, Inc.Inventors: George W. Griesgraber, Tushar A. Kshirsagar, Azim A. Celebi, Sarah J. Slania, Michael E. Danielson, Michael J. Rice, Joshua R. Wurst
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Publication number: 20080261962Abstract: The invention is directed to a method for alleviating respiratory depression in a subject as a result of disease of pharmacological agents such as opiates, opioids or barbiturates. The invention also discloses pharmaceutical compositions for use with the method, the composition containing in combination, an analgesic, anaesthetic, or a sedative and a positive allosteric AMPA receptor modulator in an amount sufficient to reduce or inhibit respiratory depression caused by the analgesic, anaesthetic, or sedative.Type: ApplicationFiled: August 30, 2007Publication date: October 23, 2008Applicant: The Governors of the University of AlbertaInventor: John Greer
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Publication number: 20080261963Abstract: The present invention relates to quinobenzoxazines analogs having the general formula: and pharmaceutically acceptable salts, esters and prodrugs thereof; wherein A, U, V, W, X and Z are substituents. The present invention also relates to methods for using such compounds.Type: ApplicationFiled: January 14, 2008Publication date: October 23, 2008Inventors: Jeffrey P. Whitten, Michael Schwaebe, Adam Siddiqui-Jain, Terence Moran
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Publication number: 20080249085Abstract: Ansamycin analogs, including maytansinoid analogs, and their use in treating cell proliferative diseases and conditions, and in particular, for use as antitumor agents.Type: ApplicationFiled: April 4, 2005Publication date: October 9, 2008Applicant: THE OHIO STATE UNIVERSITY RESEARCH FOUNDATIONInventors: John M. Cassady, Heinz G. Floss
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Patent number: 7427615Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof having inhibitory activity against tau protein kinase 1: wherein R1 represents a C1-C12 alkyl group which may be substituted; R represents, for example, a group represented by the following formula (II): wherein R2 and R3 independently represent a hydrogen atom or a C1-C8 alkyl group; R4 represents a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.Type: GrantFiled: September 20, 2002Date of Patent: September 23, 2008Assignees: Mitsubishi Pharma Corporation, Sanofi-SynthelaboInventors: Fumiaki Uehara, Keiichi Aritomo, Aya Shoda, Shinsuke Hiki, Masahiro Okuyama, Yoshihiro Usui, Mitsuru Ooizumi, Kazutoshi Watanabe, Koichi Yamakoshi
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Patent number: 7402579Abstract: The present invention relates to quinobenzoxazines analogs having the general formula: and pharmaceutically acceptable salts, esters and prodrugs thereof; wherein A, U, W, X, Z, B, L, R1, R3, R4 and R5 are substituents. The present invention also relates to methods for using such compounds.Type: GrantFiled: April 14, 2006Date of Patent: July 22, 2008Assignee: Cylene Pharmaceuticals, Inc.Inventors: Jeffrey P. Whitten, Fabrice Pierre, Michael Schwaebe
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Publication number: 20080167296Abstract: HIV inhibitory compounds of formula: salts and stereoisomers thereof, wherein R1 and R2 are hydrogen or optionally substituted C1-10alkyl; R3 is n is 1, 2 or 3; R3a is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, hydroxycarbonyl, aminocarbonyl, CI 4alkyloxycarbonyl, mono- or di(C1-4alkyl)aminocarbonyl, C1-4alkylcarbonyl, methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy-methanimidamidyl or Het; or R3 is a monocyclic or bicyclic aromatic heterocyclic ring system, wherein one, two, three or four ring members are nitrogen, oxygen and sulfur, and wherein the remaining ring members are carbon atoms; and wherein each of said heterocyclic ring systems may optionally be substituted; X is —NR7—, —0— or —S—; pharmaceutical compositions containing these compounds, methods for preparing these compounds and compositions.Type: ApplicationFiled: January 10, 2006Publication date: July 10, 2008Inventors: Bart Rudolf Romanie Kesteleyn, Pierre Jean-Marie Raboisson, Wim Van De Vreken, Maxime Francis Jean-Marie Ghislain Canard
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Publication number: 20080139472Abstract: This invention provides methods of preserving, improving, or restoring cognitive function in mammal having one or more mutations in the FMR1 gene (e.g. at risk for or having fragile x syndrome), where the methods involve the brain derived neurotrophic factor (BDNF) level or activity in the brain of said mammal. In certain embodiments the methods involve administering one or more AMPA potentiators (e.g., ampakines) to the mammal in an amount sufficient to increase BDNF levels in the brain of the mammal.Type: ApplicationFiled: October 5, 2007Publication date: June 12, 2008Inventors: JULIE LAUTERBORN, GARY LYNCH, CHRISTINE GALL, CHRISTOPHER REX
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Patent number: 7381720Abstract: The present invention relates to methods for ameliorating a cell proliferative disorder using quinobenzoxazines analogs having the general formula: and pharmaceutically acceptable salts, esters and prodrugs thereof; wherein A, U, V, W, X and Z are substituents.Type: GrantFiled: May 10, 2006Date of Patent: June 3, 2008Assignee: Cylene Pharmaceuticals, Inc.Inventors: Jeffrey P. Whitten, Michael Schwaebe, Adam Siddiqui-Jain, Terrance Moran
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Patent number: 7371745Abstract: A molecule for labeling a target material is provided including two transition-metal chelates and a detectable group. The molecule has the general structural formula (I): wherein: (a) Y and Y? are each a transition metal, (b) R1 and R1? are each independently CH(COO?), CH(COOH), or absent; (c) R2 and R2? are linkers each having a length of from about 3.0 to about 20 ?; and (d) X is a detectable group. The linkers may be linear or branched, may contain aromatic moieties, and may optionally be further substituted. Methods of using the molecules of the invention as probes in detecting and analyzing target materials as well as kits including the molecule of the invention are also provided.Type: GrantFiled: September 21, 2004Date of Patent: May 13, 2008Assignee: Rutgers, The State University of New JerseyInventors: Richard H. Ebright, Yon W. Ebright
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Patent number: 7354916Abstract: The present invention relates to quinobenzoxazines analogs having the general formula: and pharmaceutically acceptable salts, esters and prodrugs thereof; wherein A, U, V, W, X and Z are substituents. The present invention also relates to methods for using such compounds.Type: GrantFiled: July 30, 2004Date of Patent: April 8, 2008Assignee: Cylene PharmaceuticalsInventors: Jeffrey P. Whitten, Michael Schwaebe, Adam Siddiqui-Jain, Terence Moran
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Patent number: 7342011Abstract: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3?-hydroxy analogs, 4?- and/or 6? halo and/or alkoxy analogs, and various 5? substituents that incorporate a cyclic amine moiety.Type: GrantFiled: August 11, 2004Date of Patent: March 11, 2008Assignee: ActivBiotics, Inc.Inventors: John H. van Duzer, Arthur F. Michaelis, William B. Geiss, Douglas G. Stafford, Joseph Raker
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Patent number: 7326702Abstract: The present invention relates to quinobenzoxazines analogs having the general formula: and pharmaceutically acceptable salts, esters and prodrugs thereof; wherein A, U, V, W, X and Z are substituents. The present invention also relates to methods for using such compounds.Type: GrantFiled: March 28, 2006Date of Patent: February 5, 2008Assignee: Cylene Pharmaceuticals, Inc.Inventors: Jeffrey P. Whitten, Michael Schwaebe, Adam Siddiqui-Jain, Terence Moran
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Patent number: 7312213Abstract: A compound selected from those of formula (I): wherein: W1, with the carbon atoms to which it is bonded, represents phenyl or pyridyl, Z represents a group selected from hydrogen, halogen, linear or branched (C1-C6)alkyl, aryl, aryl-(C1-C6)alkyl, aryloxy, aryl-(C1-C6)alkoxy, hydroxy and linear or branched (C1-C6)alkoxy, R1 is as defined in the description, R2 represents hydrogen or —CH2CH2O—R8, R3 and R4 each represents hydrogen, linear or branched (C1-C6)alkyl, aryl or aryl-(C1-C6)alkyl, n represents an integer of from 1 to 6 inclusive, its isomers, and addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same which are useful in the treatment of cancer.Type: GrantFiled: October 17, 2003Date of Patent: December 25, 2007Assignee: Les Laboratories ServierInventors: Gérard Coudert, Franck Lepifre, Daniel-Henri Caignard, Pierre Renard, John Hickman, Alain Pierre, Laurence Kraus-Berthier
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Publication number: 20070232595Abstract: A method for accelerating cutaneous barrier recovery and a method for preventing epidermal hyperplasia by inhibiting production of Nitric Oxide by an epidermal cell are provided.Type: ApplicationFiled: March 27, 2007Publication date: October 4, 2007Applicant: Shiseido Company, Ltd.Inventors: Kazuyuki Ikeyama, Shigeyoshi Fuziwara, Mitsuhiro Denda
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Patent number: 7276498Abstract: The present invention provides compounds of the following structure, wherein R1, R2, R4, R4?, R6, R7, and R15 are defined above: These compounds are useful in treating neurological disorders or complications due to stroke or head injury; benign or malignant neoplastic disease, carcinomas and adenocarcinomas; proliferative disorders; and inflammatory disorders. The compounds are therefore useful as neuroprotective and neuroregenerative, anti-proliferative, and anti-inflammatory agents.Type: GrantFiled: December 15, 2005Date of Patent: October 2, 2007Assignee: WyethInventors: Edmund Idris Graziani, Kevin Pong, Jerauld Skotnicki
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Patent number: 7276497Abstract: New thiol and disulfide-containing maytansinoids bearing a mono or di-alkyl substitution on the ?-carbon atom bearing the sulfur atom are disclosed. Also disclosed are methods for the synthesis of these new maytansinoids and methods for the linkage of these new maytansinoids to cell-binding agents. The maytansinoid-cell-binding agent conjugates are useful as therapeutic agents, which are delivered specifically to target cells and are cytotoxic. These conjugates display vastly improved therapeutic efficacy in animal tumor models compared to the previously described agents.Type: GrantFiled: May 20, 2004Date of Patent: October 2, 2007Inventors: Ravi V. J. Chari, Wayne C. Widdison
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Patent number: 7271165Abstract: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3?-hydroxy analogs, 4?- and/or 6? halo and/or alkoxy analogs, and various 5? substituents that incorporate a cyclic amine moiety.Type: GrantFiled: December 22, 2004Date of Patent: September 18, 2007Assignee: ActivBiotics, Inc.Inventors: John H. van Duzer, Arthur F. Michaelis, William B. Geiss, Douglas G. Stafford, Joseph Raker, Xiang Y. Yu, James M. Siedlecki, Yingfei Yang
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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: 7265107Abstract: The current invention relates to a series of rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms, specifically, the 3,4-cyclo-rifamycin derivatives having an oxime group at the C-11 position.Type: GrantFiled: March 9, 2005Date of Patent: September 4, 2007Assignee: Cumbre Pharmaceuticals Inc.Inventors: Jing Li, Zhenkun Ma
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Patent number: 7259167Abstract: Disclosed herein is a pharmacophore model for antimalarial activity and methods of making and using thereof. The pharmacophore comprises two hydrogen bond acceptor (lipid) functions and two hydrophobic (aromatic) functions. The pharmacophore model was made using a test set of tryptanthrin compounds which exhibit antimalarial activity. Also disclosed are tryptanthrin compounds having greater solubility and bioactivity as compared to prior art tryptanthrin compounds and methods of making and using thereof. Also disclosed are methods of treating malaria in a subject.Type: GrantFiled: February 7, 2003Date of Patent: August 21, 2007Assignee: United States of America as Represented by the Secretary of the ArmyInventors: Daniel A. Nichols, Rickey P. Hicks, Apurba K. Bhattacharjee
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Patent number: 7238690Abstract: The present invention is directed to compounds useful for treating addictive behavior and sleep disorders represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The compounds used in the method of treatment of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including addictive behavior and sleep disorders.Type: GrantFiled: March 15, 2006Date of Patent: July 3, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Wenting Chen, Christopher D. McClung, Emilie J. Calvello, David M. Zawrotny
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Patent number: 7220738Abstract: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3?-hydroxy analogs, and/or various fused ring systems with the benzene ring at the 4?,5? or 5?,6? positions.Type: GrantFiled: December 9, 2004Date of Patent: May 22, 2007Assignee: ActivBiotics, Inc.Inventors: John H. van Duzer, Arthur F. Michaelis, William B. Geiss, Douglas G. Stafford, Xiang Y. Yu, James M. Siedlecki, Yingfei Yang
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Patent number: 7214701Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) specified agonists or antagonists of nicotinic acetylcholine receptors.Type: GrantFiled: June 25, 2004Date of Patent: May 8, 2007Assignee: Bayer CropScience AGInventors: Reiner Fischer, Christoph Erdelen
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Patent number: 7141565Abstract: The present invention relates to quinobenzoxazines analogs having the general formula: and pharmaceutically acceptable salts, esters and prodrugs thereof; wherein A, U, V, W, X and Z are substituents. The present invention also relates to methods for using such compounds.Type: GrantFiled: April 7, 2004Date of Patent: November 28, 2006Assignee: Cylene Pharmaceuticals, Inc.Inventors: Jeffrey P. Whitten, Michael Schwaebe, Adam Siddiqui-Jain, Terrance Moran
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Patent number: 7078399Abstract: The invention features sulfhydryl rifamycin compositions, methods of making these compositions, and methods for treating disease using these compositions.Type: GrantFiled: December 12, 2002Date of Patent: July 18, 2006Assignee: ActivBiotics, Inc.Inventors: Arthur F. Michaelis, Hawkins V. Maulding, Chalom Sayada, Barry Eisenstein, William B. Geiss, Joseph Raker
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Patent number: 6984641Abstract: Selective inhibitors of cGMP-specific PDE, and use of the compounds and salts and solvates thereof as therapeutic agents, are disclosed.Type: GrantFiled: May 2, 2002Date of Patent: January 10, 2006Assignee: Lilly Icos LLC.Inventors: Mark W. Orme, Jason S. Sawyer, Alain C. Daugan, Agnes Bombrun, Françoise Gellibert, Lisa M. Schultze, Raymond F. Brown, Romain L. Gosmini
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Patent number: 6936726Abstract: The present invention refers to new products generated by the conjugation of flavanols with molecules that contain the thiol group. New molecules are obtained from polyphenolic plant extracts rich in oligomeric and polymeric procyanidines and prodelfinidins. In this way, new products are generated with antioxidant properties for application as protective agents for the organism against disorders such as cancer, cardiovascular diseases and premature aging. The invention also refers to obtaining these new agents from waste material generated by the agroalimentary industry. Since these waste materials are highly complex mixtures a simple and effective method is described to isolate and purify these, based on the physico-chemical characteristics of the new molecules.Type: GrantFiled: December 14, 2001Date of Patent: August 30, 2005Assignee: Consejo Superior de Investigaciones CientificasInventor: José Luis Torres Simón
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Patent number: 6930105Abstract: The present invention provides compounds of Formula (I): wherein R1, R2, R3, R4, R5, and R6, have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula (I). The compounds are 5-HT ligands and are useful for treating diseases wherein modulation of 5-HT2C activity is desired.Type: GrantFiled: October 15, 2002Date of Patent: August 16, 2005Assignee: Pharmacia & Upjohn CompanyInventor: Jian-Min Fu
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Patent number: 6919333Abstract: A molecule for labeling a target material is provided including two transition-metal chelates and a detectable group. The molecule has the general structural formula (I): wherein: (a) Y and Y? are each a transition metal, (b) R1 and R1? are each independently CH(COO?), CH(COOH), or absent; (c) R2 and R2? are linkers each having a length of from about 3.0 to about 20 ?; and (d) X is a detectable group. The linkers may be linear or branched, may contain aromatic moieties, and may optionally be further substituted. Methods of using the molecules of the invention as probes in detecting and analyzing target materials as well as kits including the molecule of the invention are also provided.Type: GrantFiled: September 17, 2003Date of Patent: July 19, 2005Assignee: Rutgers, The State University of New JerseyInventors: Richard H. Ebright, Yon W. Ebright
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Patent number: 6900204Abstract: The invention features compounds that act as antimicrobial agents and/or antimicrobial enhancer agents, compositions that include the antimicrobial enhancer agents of the invention, and methods for treating microbial infections using those compositions.Type: GrantFiled: September 6, 2002Date of Patent: May 31, 2005Assignee: ActivBiotics, Inc.Inventors: Arthur F. Michaelis, Hawkins V. Maulding
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Patent number: 6884800Abstract: Imidazole compounds of the formula I in which R1 and R2, independently of one another, each denote A1, OA1, SA1 or Hal, A1 denotes H, A, alkenyl, cycloalkyl or alkylenecycloalkyl, A denotes alkyl having 1-10 carbon atoms, Hal denotes F, Cl, Br or I, and X denotes O, S, SO or SO2, and their physiologically acceptable salts and/or solvates, as phosphodiesterase VII inhibitors, and their use for the preparation of a medicament.Type: GrantFiled: October 31, 2000Date of Patent: April 26, 2005Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Hans-Michael Eggenweiler, Rochus Jonas, Michael Wolf, Michael Gassen, Thomas Welge