At Least Three Cyclos In The Polycyclo Ring System Patents (Class 514/224.5)
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Publication number: 20110190278Abstract: The present invention relates to a compound of the following formula (I) or a pharmaceutically acceptable salt thereof, being useful as a renin inhibitor. [wherein R1a is halogen, etc.; R1m is H, etc.; G1 is —N(R1b)—, etc.; G2 is —CO—, etc.; G3 is —C(R1c)(R1d)—, etc.; G4 is oxygen, etc.; R1b is optionally substituted C1-6 alkyl, etc.; R1c and R1d are independently the same or different, H, etc.; R3 is H, optionally substituted C1-6 alkyl, etc.; R3a, R3b, R3c and R3d are independently the same or different, and a group: -A-B (said A is single bond, etc., and said B is H, etc.), etc.; and n is 1, etc.Type: ApplicationFiled: December 19, 2008Publication date: August 4, 2011Inventors: Hiroyuki Nakahira, Yohei Ikuma, Nobuhisa Fukuda, Kozo Yoshida, Hidenori Kimura, Satoshi Suetsugu, Akira Fusano, Kiyoto Sawamura, Junya Ikeda, Yoshio Nakai
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Publication number: 20110158989Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.Type: ApplicationFiled: March 4, 2011Publication date: June 30, 2011Applicant: Takeda Pharmaceutical Company LimitedInventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
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Publication number: 20110152253Abstract: A compound represented by the general formula (I): or a pharmaceutically acceptable salt thereof, has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.Type: ApplicationFiled: July 24, 2009Publication date: June 23, 2011Applicant: Eisai R&D Management Co., LtdInventors: Takafumi Motoki, Toshihiko Kaneko, Noboru Yamamoto, Afzal Khan
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Publication number: 20110136790Abstract: The present invention relates to novel Tricyclic Heterocycle Derivatives, pharmaceutical compositions comprising the Tricyclic Heterocycle Derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. R1 is formula (Ia), (Ib) or (Ic); R2 is alkvl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl. any of which can be optionally substituted with R11; M1 is —CH—. —C(halo)- or —N—; Y is —C(O)—, —S—. —S(O)—, —S(O)2—, —CH2— or —O—, such that Y is not —O— when an adjacent atom is N.Type: ApplicationFiled: July 21, 2009Publication date: June 9, 2011Inventors: Manuel De Lera Ruiz, MIchael Y Berlin, Junying Zheng, Robert G. Aslanian, Kenvin D. McCormick, Qingbel Zeng
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BENZENESULFONYL-CHROMANE, THIOCHROMANE, TETRAHYDRONAPHTHALENE AND RELATED GAMMA SECRETASE INHIBITORS
Publication number: 20110110948Abstract: Disclosed are novel gamma secretase inhibitors of the formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, wherein L1, n, X, Ar, Y, Z, Q, and Q1 are as defined herein. Also disclosed are methods for inhibiting gamma secretase, methods for treating Alzheimer's disease, methods of treating one or more neurodegenerative diseases, and methods of inhibiting the deposition of amyloid protein (e.g., amyloid beta protein) in, on or around neurological tissue (e.g., the brain) using the compounds of formula 1.0.Type: ApplicationFiled: July 15, 2008Publication date: May 12, 2011Applicant: SCHERING CORPORATIONInventors: Thavalakulamgara K. Sasikumar, Duane A. Burnett, Theodros Asberom, Wen-Lian Wu, Hongmei Li, Ruo Xu, Hubert B. Josien -
Patent number: 7923445Abstract: The present invention relates to inhibiting proliferation and inducing apoptosis in activated lymphocytes, including T cells and B cells. The invention also provides compositions and methods for inhibiting proliferation and inducing apoptosis in activated lymphocytes, as well methods for treating diseases associated with activated lymphocytes by administering 5-HT receptor antagonists.Type: GrantFiled: August 31, 2007Date of Patent: April 12, 2011Assignee: Immune Control, Inc.Inventors: Stephen Roth, Clayton Buck, Christopher Self, Gary Olson
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Publication number: 20110065687Abstract: This application relates to certain novel polycyclic compounds that interact with quadruplex-forming regions of polynucleotides and thereby inhibit translation of genetic information into polypeptides. These compounds can thus provide anticancer and antibacterial and antiviral effects. The invention includes novel compounds and pharmaceutical compositions, and methods of using them to treat cancer and other conditions.Type: ApplicationFiled: April 17, 2008Publication date: March 17, 2011Inventors: Michael Schwaebe, Johnny Yasuo Nagasawa, Mustapha Haddach
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Publication number: 20110034446Abstract: The invention features derivatives of R(?)-2-methoxy-11-hydroxyaporphines and methods of treating Parkinson's disease, sexual dysfunction, and depressive disorders therewith.Type: ApplicationFiled: July 10, 2008Publication date: February 10, 2011Applicant: THE MCLEAN HOSPITAL CORPORATIONInventors: John L. Neumeyer, Yu-Gui Si
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Publication number: 20110015134Abstract: This patent describes a method and materials to treat cancer diagnosed at an early stage, particularly breast cancer. It considers that metastatic breast cancer growth includes periods of dormancy, that surgery to remove a primary tumor can induce metastatic growth, and that women with Down Syndrome rarely get breast cancer. It elevates the level of an antiangiogenic drug produced by chromosome 21 preferably Endostatin in plasma preferably at least one day prior to surgery and kept at that high level preferably indefinitely. In one embodiment, the therapy specifically excludes drugs that significantly inhibit the VEGF pathway since that is important for wound healing. This method will prevent results of surgery from stimulating tumor growth and angiogenesis of micrometastatic disease that is much easier to prevent than control after the fact. This can be done indefinitely since there is no acquired resistance that develops, as happens in most cancer therapies.Type: ApplicationFiled: September 22, 2010Publication date: January 20, 2011Inventor: Michael W. Retsky
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Patent number: 7846923Abstract: The invention provides a novel class of compounds, 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 Abl, Bcr-Abl, Bcr-Abl(T315I), ALK, BLK, BMX, BRK, C-kit, c-RAF, CSK, c-SRC, EGFR, Fes, FGFR3, Flt3, Fms, Fyn, IGF-1R, IR, JAK(2), JAK(3), KDR, Lck, NLK, p70S6K, PDGFR?, Ros, SAPK2?, SGK, SIK, Syk, Tie2 and TrkB kinases.Type: GrantFiled: May 11, 2007Date of Patent: December 7, 2010Assignee: IRM LLCInventors: Pingda Ren, Baogen Wu, Guobao Zhang, Yongping Xie, Barun Okram, Victor Nikulin, Xia Wang, Ha-Soon Choi
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Patent number: 7842686Abstract: The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions.Type: GrantFiled: January 21, 2009Date of Patent: November 30, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Corey Don Anderson, Andreas P. Termin, Pramod Joshi, Sara S. Hadida Ruah, Daniele Bergeron, Sanghee Yoo, Jingrong Cao
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Publication number: 20100285087Abstract: Enantomerically purified phenothiazines are provided as active ingredients of medicaments to limit activity of bone resorbing cells so as to reduce bone loss. Novel phenothiazine derivatives are provided. A method of synthesizing enantiomerically pure phenothiazine derivatives is provided that avoids post-synthetic enantiomeric resolution.Type: ApplicationFiled: February 1, 2010Publication date: November 11, 2010Applicant: The University Of TexasInventors: Joseph McDonough, Stanton Furst McHardy
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Patent number: 7820652Abstract: The invention features an ascending dose regimen for the administration of rifamycin-class antibiotics. The dosing regimen can be used to treat bacterial infections and diseases related to infection.Type: GrantFiled: September 23, 2004Date of Patent: October 26, 2010Assignee: ActivBiotics Pharma, LLCInventors: Arthur F. Michaelis, Bernard E. Cabana
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Publication number: 20100234363Abstract: Disclosed is a compound which is useful as an 11?-hydroxysteroid dehydrogenase type 1 inhibitor.Type: ApplicationFiled: September 17, 2008Publication date: September 16, 2010Applicants: INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC., SHIONOGI & CO., LTD.Inventors: Akiko Itai, Susumu Muto, Ryuko Tokuyama, Hiroshi Fukasawa, Takeshi Yanase
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Patent number: 7772225Abstract: The present invention relates to novel N-sulfamoyl-piperidineamides of Formula I and their physiologically acceptable acid addition salts, to pharmaceutical compositions comprising them, processes for their preparation, and their use for the treatment of obesity and its concomitant and/or secondary diseases and related or other conditions.Type: GrantFiled: December 8, 2006Date of Patent: August 10, 2010Assignee: Solvay Pharmaceuticals GmbHInventors: Jochen Antel, Michael Firnges, Uwe Schoen, Harald Waldeck, Michael Wurl, Dania Reiche, Peter-Colin Gregory
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Patent number: 7772227Abstract: The invention relates to tricyclic 1-[(indol-3-yl)carbonyl]piperazine derivative having the general Formula (I) wherein X is CH2, O or S; R represents 1-3 substituents independently selected from H, (C1-4)alkyl, (C1-4)alkyloxy and halogen; R1 is (C5-8)cycloalkyl; R2 is H or (C1-4)alkyl; R3, R3?, R4? R4?, R5, R5? and R6? are independently hydrogen or (C1-4)-alkyl, optionally substituted with (C1-4)alkyloxy, OH or halogen; R6 is hydrogen or (C1-4)alkyl, optionally substituted with (C1-4)alkyloxy, OH or halogen; or R6 forms together with R7 a 4-7 membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O and S; R7 forms together with R6 a 4-7 membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O and S; or R7 is H, (C1-4)alkyl or (C3-5)cycloalkyl, the alkyl groups being optionally substituted with OH, halogen or (C1-4)alkyloxy; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 13, 2004Date of Patent: August 10, 2010Assignee: N.V. OrganonInventor: Julia Adam-Worrall
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Publication number: 20100190763Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.Type: ApplicationFiled: January 21, 2010Publication date: July 29, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
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Publication number: 20100144610Abstract: An aspect of the present invention provides for a medicament including a solution containing pleconaril or a pharmaceutically acceptable salt thereof, wherein at least one solvent including the solution is a pleconaril-dissolving hydrofluorocarbon.Type: ApplicationFiled: February 17, 2010Publication date: June 10, 2010Inventors: Saeed M. Chaudhry, Julianne Berry, Joel A. Sequeira
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Publication number: 20100119622Abstract: The present invention relates to new 3H-benzooxazol-2-one modulators of D2 receptors and/or 5-HT1A receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: September 15, 2009Publication date: May 13, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100069374Abstract: This invention relates to benzopyran derivatives of formula (I) or (II), or pharmaceutically acceptable salts thereof wherein R1 and R2 are independently of each other hydrogen atom, C1-6alkyl group or C6-14aryl group, R3 is hydrogen atom or C1-6alkylcarbonyloxy group, or together with R4 forms a bond, R4 is hydrogen atom, or together with R3 forms a bond, m is an integer of 0 to 4, n is an integer of 0 to 4, V is a single bond, CR7R8, NR9, O, S, SO or SO2, R5 is hydrogen atom or C1-6alkyl group, R6 is hydrogen atom, C1-6alkyl group, C3-8cycloalkyl group, C3-8cycloalkenyl group, amino group, C1-6alkylamino group, di-C1-6alkylamino group, C6-14arylamino group, C2-9heteroarylamino group, C6-14aryl group, C2-9heteroaryl group or C2-9heterocyclyl group, A is 5-, 6- or 7-member ring fused with benzene ring, as constituent atom of the ring, oxygen atom, nitrogen atom or sulfur atom may be contained in the number of 1 to 3 alone or in a combination thereof, the number of unsaturated bond in the ring is 1, 2 or 3Type: ApplicationFiled: November 17, 2009Publication date: March 18, 2010Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Kazuhiko Ohrai, Yukohiro Shigeta, Osamu Uesugi, Takumi Okada, Tomoyuki Matsuda
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Publication number: 20090215736Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.Type: ApplicationFiled: September 23, 2008Publication date: August 27, 2009Applicant: Vertex Pharmaceuticals, IncorporatedInventors: Michael Mortimore, Andrew Miller, John Studley, Jean-Damien Charrier
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Patent number: 7579343Abstract: 1H-Pyrrolo-1,4-thiazines and a process for the preparation thereof are described. These compounds are useful as enzyme inhibitors in cells, particularly for medical uses.Type: GrantFiled: September 6, 2006Date of Patent: August 25, 2009Assignee: Board of Trustees of Michigan State UniversityInventors: Rawle Hollingsworth, Li Gao
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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: 20090099159Abstract: A method of treating or preventing of a disease or condition associated with an increased level of isoforms of amyloid ? peptides (A?) and/or with a changed ratio of levels of A? isoforms and/or with the formation of plaques containing amyloid ? peptide (A?) isoforms in a mammal comprising administering to said mammal an therapeutically effective amount of a compound selected from the formulas Ia, Ib wherein V, W, Y, R2, R3, R5, R6, L1 and i are defined as in claim 1.Type: ApplicationFiled: December 17, 2008Publication date: April 16, 2009Applicants: BOEHRINGER INGELHEIM INTERNATIONAL GMBH, BOEHRINGER INGELHEIM PHARMACEUTICALS, INC.Inventors: Klaus BORNEMANN, Guenter TRUMMLITZ, Bernd BECK, Frank SAMS-DODD, Dagmar KUGLER, Klaus KLINDER, Cornelia DORNER-CIOSSEK, Marcus KOSTKA
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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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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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Publication number: 20090042868Abstract: Inhibitors of indoleamine 2,3-dioxygenase (IDO) are provided as are pharmaceutical compositions containing such inhibitors as well as the use of such inhibitors and compositions for the treatment of a condition in a mammalian subject characterized by pathology of the IDO-mediated tryptophan metabolic pathway. Such conditions may involve suppression of T-cell mediated immune response or may directly result from depletion of tryptophan or accumulation of a product of tryptophan degradation. Specific disease conditions include cataracts, age-related yellowing in the eye, neurodegenerative disorders, mood disorders, cancer and various bacterial/viral infections. IDO inhibitors of this invention are substituted naphthalene and anthracene diones. Novel compounds of this invention include the following taurine-substituted naphthaquinone structure.Type: ApplicationFiled: July 13, 2005Publication date: February 12, 2009Applicant: THE UNIVERSITY OF BRITISH COLUMBIAInventors: Raymond J. ANDERSEN, Alban PEREIRA, Xin-Hui HUANG, Grant MAUK, Eduardo VOTTERO, Michel ROBERGE, Aruna BALGI
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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: 20080305082Abstract: Disclosed are compounds having Formula I: and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, A, and B are as defined herein, for use in methods for treating, preventing or ameliorating hyperproliferative disorders, such as cancer and other diseases and conditions. The invention also relates to pharmaceutical compositions and formulations comprising a compound having Formula I, and in combination with one or more other active agents and/or treatments.Type: ApplicationFiled: September 14, 2005Publication date: December 11, 2008Inventors: John G. Curd, Robert L. Capizzi, John F.W. Keana
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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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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: 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: 7262190Abstract: The invention relates to compounds of formula (I): wherein: R1 represents hydrogen, alkyl or cycloalkyl, R2 represents hydrogen, halogen or hydroxy, A represents CR3R4 or NR3 wherein R3 and R4 are as defined in the description, Y represents an alkylene chain as described in the description, X represents NR5R6, S(O)nR7, OR8, C(O)R9, amidino or a heterocycle, their isomers, and addition salts thereof; and medicinal products containing the same which are useful in the prevention or treatment of diseases associated with AMPA flux.Type: GrantFiled: December 8, 2005Date of Patent: August 28, 2007Assignee: Les Laboratoires ServierInventors: Patrice Desos, Alexis Cordi, Pierre Lestage, Laurence Danober
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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: 7141566Abstract: The invention relates to compounds of formula (I), the tautomeric and isomeric forms and salts thereof, in addition to a method for production and use thereof in medicaments.Type: GrantFiled: August 23, 2000Date of Patent: November 28, 2006Assignee: Schering AktiengesellschaftInventors: Peter Hölscher, Hartmut Rehwinkel, Stefan Jaroch, Detlev Sülzle, Margrit Hillmann, Gerardine Anne Burton, Fiona Mcdougall McDonald
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Patent number: 7135468Abstract: Bacterial protein synthesis-inhibiting compounds having formula (I) and salts, prodrugs, salts of prodrugs, and metabolites thereof, processes for making the compounds and intermediates in the processes, compositions containing the compounds, and methods of using the compounds are disclosed.Type: GrantFiled: February 4, 2005Date of Patent: November 14, 2006Assignee: Abbott LaboratoriesInventors: Mira M. Hinman, Teresa A. Rosenberg, Rolf Wagner
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Patent number: 7018999Abstract: Novel methods for the treatment and/or prevention of pain are presented. The methods may comprise administering to a subject in need thereof an effective amount of a stress-activated protein kinase inhibitor. Preferred compounds for use in the methods include fused pyrrolocarbazole compounds.Type: GrantFiled: May 15, 2002Date of Patent: March 28, 2006Assignee: Cephalon, Inc.Inventors: Lisa D. Aimone, Robert L. Hudkins, Matthew S. Miller
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Publication number: 20040266758Abstract: Novel non-steroidal compounds are provided which are glucocorticoid receptor modulators which are useful in treating diseases requiring glucocorticoid receptor agonist or antagonist therapy such as obesity, diabetes, inflammatory and immune disorders, and have the structure 1Type: ApplicationFiled: June 10, 2004Publication date: December 30, 2004Inventors: Sara Sabine Hadida-Ruah, Xiaohui He, Johnny Yasuo Nagasawa
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Patent number: 6800623Abstract: A method for treating schizophrenia which comprises administering a compound of general formula (I)Type: GrantFiled: January 6, 2003Date of Patent: October 5, 2004Assignee: Boehringer Ingelheim Pharma KGInventors: Karin Winter, Thomas Weiser, Stefan M. Blech, Angelo Ceci
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Publication number: 20040170654Abstract: A method for systemic administration of a hydrophobic dopamine agonist to a mammal is disclosed. The method involves delivering the hydrophobic dopamine agonist to the dermis of the mammal whereby improved systemic absorption is obtained compared to absorption produced upon delivering the substance subcutaneously by bolus administration.Type: ApplicationFiled: December 15, 2003Publication date: September 2, 2004Inventor: Thomas C. Pinkerton
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Publication number: 20040171600Abstract: This invention concerns antimicrobial compositions that are useful for industrial applications.Type: ApplicationFiled: September 4, 2003Publication date: September 2, 2004Inventors: Toshimasa Ohnishi, Ikuya Tanaka
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Publication number: 20040167124Abstract: Tricyclic compounds according to the structure below, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed.Type: ApplicationFiled: October 16, 2003Publication date: August 26, 2004Applicant: GILEAD SCIENCES, INC.Inventors: James M. Chen, Xiaowu Chen, Maria Fardis, Haolun Jin, Choung U. Kim, Laura N. Schacherer
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Publication number: 20040157835Abstract: The present invention is related to a type of thienothiazine compounds having molecular structure of formula (1) and their pharmaceutically acceptable salts or solvates. The present invention is also related to the method of producing the formula (1) compound, an anti-inflammatory and analgesic pharmaceutical composition containing the formula (1) compound, and the method of using the formula (1) compound to prepare anti-inflammatory and analgesic medicine.Type: ApplicationFiled: December 24, 2003Publication date: August 12, 2004Inventor: Jing Li
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Publication number: 20040157831Abstract: The present invention provides compounds of Formula (I): 1Type: ApplicationFiled: February 3, 2004Publication date: August 12, 2004Applicant: Pharmacia & Upjohn CompanyInventor: William W. McWhorter
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Publication number: 20040147504Abstract: The invention relates to the use of compound of Formula I in treating patients for inflammatory or neuropathic pain as well as various symptoms of multiple sclerosis.Type: ApplicationFiled: December 16, 2003Publication date: July 29, 2004Applicant: Aventis Pharmaceuticals Inc.Inventors: Bin Zhu, Joseph Wettstein, Margaret A. Petty
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Publication number: 20040138200Abstract: A pharmaceutical composition comprising a salt, preferably a crystalline salt, of an organic acid of low water solubility and a compound of formula (I) is provided. The salts are useful in treating Parkinson's disease. Also provided are methods of treatment using the salts and methods of making crystalline forms of the salts.Type: ApplicationFiled: October 2, 2003Publication date: July 15, 2004Inventors: Michael Hawley, Michael S. Bergren, Phillip R. Nixon, Gordon W. Halstead, Robert S. Chao, Tzu-chi R. Ju
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Publication number: 20040132725Abstract: A preparation of a tyrphostin including a compound of a general formula: 1Type: ApplicationFiled: November 19, 2003Publication date: July 8, 2004Inventors: Alexander Levitzki, Aviv Gazit, Shmuel Banai, David S. Gertz, Gershon Golomb, Frank D. Boehmer, Johannes Waltenberger
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Publication number: 20040127493Abstract: Compounds of the formula: 1Type: ApplicationFiled: September 10, 2003Publication date: July 1, 2004Inventors: Hong Gao, Gary Paul Stack
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Patent number: RE39300Abstract: Nontoxic substances that block the N-methyl-D-aspartate (NMDA) receptor, e.g., a morphinan such as dextromethorphan or dextrorphan, or that block a major intracellular consequence of NMDA-receptor activation, e.g., a ganglioside such as GM1 or GT1b, a phenothiazine such as trifluoperazine or a naphthalenesulfonamide such as N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide, inhibit the development of tolerance to and/or dependence on addictive drugs, e.g., narcotic analgesics such as morphine, codeine, etc.Type: GrantFiled: June 15, 2001Date of Patent: September 19, 2006Assignee: Virginia Commonwealth University Medical College of VirginiaInventors: David J. Mayer, Jianren Mao
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Patent number: RE39679Abstract: The present invention is directed to certain novel compounds 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 invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: February 16, 2006Date of Patent: June 5, 2007Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Michael Guang Yang, Simon Haydar, Wenting Chen, Christopher D. McClung, Emile J. B. Calvello, David M. Zawrotny, Parthasarathl Rajagopalan