Polycyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/455)
-
Patent number: 8003659Abstract: Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.Type: GrantFiled: February 3, 2009Date of Patent: August 23, 2011Assignee: Indenix Pharmaceuticals, Inc.Inventors: Christophe Claude Parsy, Francois-Rene Alexandre, Dominique Surleraux, Michel Derock, Frederic Leroy
-
Publication number: 20110189129Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof: Q-G-A-L-B—W??(I), which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: January 25, 2011Publication date: August 4, 2011Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Hui Cao, Yat Sun Or
-
Publication number: 20110152279Abstract: Inhibitors of HCV replication of formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein Y, R1, R2, R4 and n have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.Type: ApplicationFiled: August 14, 2009Publication date: June 23, 2011Applicant: TIBOTEC PHARMACEUTICALSInventors: David Craig MC GOWAN, Sandrine Marie Helene VENDEVILLE, Pierre Jean-Marie Bernard RABOISSON, Abdellah TAHRI
-
Publication number: 20110150835Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.Type: ApplicationFiled: October 31, 2007Publication date: June 23, 2011Inventors: Srikanth Venkatraman, F. George Njoroge, Wanli Wu, Viyyoor M. Girijavallabhan, Brian A. McKittrick, Jing Su, Francisco Velazquez, Patrick A. Pinto
-
Publication number: 20110105550Abstract: The present invention relates to Rifaximin polymorphic, salt, hydrate, and amorphous forms, to their use in medicinal preparations and to therapeutic methods using them.Type: ApplicationFiled: August 25, 2010Publication date: May 5, 2011Applicant: SALIX PHARMACEUTICALS, LTD.Inventors: Karen S. Gushurst, Dongali Yang, Melanie Roe, Nathan Schultheiss
-
Publication number: 20110046161Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.Type: ApplicationFiled: April 16, 2009Publication date: February 24, 2011Inventors: Nigel J. Liverton, John A. McCauley, John W. Butcher, Kevin F. Gilbert, Charles J. McIntyre, Michael T. Rudd
-
Publication number: 20110028450Abstract: The invention relates to ring-annulated dihydropyrrolo[2,1-a]isoquinoline compounds according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: ApplicationFiled: July 27, 2010Publication date: February 3, 2011Applicant: N.V. OrganonInventors: Cornelis Marius Timmers, Hubert Jan Jozef Loozen, Herman Thijs Stock
-
Publication number: 20100317623Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.Type: ApplicationFiled: October 19, 2007Publication date: December 16, 2010Inventors: Nigel J. Liverton, Vincenzo Summa, Joseph P. Vacca
-
Patent number: 7851439Abstract: Organic compounds that are useful for the treatment, prevention and/or amelioration of diseases are described.Type: GrantFiled: May 30, 2007Date of Patent: December 14, 2010Assignee: Novartis AGInventors: Simon Bushell, Matthew LaMarche, Michael J. Patane, Lewis Whitehead
-
Publication number: 20100311757Abstract: Salarines and Tulearins isolated from Fascaplysinopsis sp. sponge and synthetic derivatives thereof are provided.Type: ApplicationFiled: September 25, 2008Publication date: December 9, 2010Applicants: RAMOT AT TEL-AVIV UNIVERSITY LTD., Université De La RéunionInventors: Yoel Kashman, Maurice Aknin, Amira Rudi, Ashgan Bishara, Drorit Neumann, Nathalie Ben Califa
-
Publication number: 20100292179Abstract: We describe the functional cloning and the use of a non-fungal inositol phosphoryceraminde synthase (IPC synthase) in a screening assay for the identification of agents that target and antagonize the activity of IPC synthase.Type: ApplicationFiled: January 19, 2007Publication date: November 18, 2010Applicant: The University of DurhamInventors: Paul William Denny, Ralph Thomas Schwarz, Hosam Shams-Eldin
-
Publication number: 20100280238Abstract: The Huisgen 1,3-dipolar cycloaddition is a ‘click’ reaction that results from the ligation of azides and alkynes to give a triazole moiety. This reaction has been shown to be effective in the formation of a variety of macrocyclic rings. A key point of interest is the regioselectivity and specificity of the cycloaddition. Disclosed herein are specific, selective, and high-yielding methods of azide-alkyne macrocyclization to form 1,4- and 1,5-triazoles and libraries thereof.Type: ApplicationFiled: April 29, 2010Publication date: November 4, 2010Inventors: Lisa A. Marcaurelle, Ann R. Kelly, Sarathy Kesavan, Jingqiang Wei, Damian W. Young
-
Publication number: 20100267654Abstract: Disclosed are rifamycin derivatives having antibacterial activities, wherein the compounds have the following general formula: wherein: R is hydrogen or acetyl; R1 and R2 are independently selected from the group consisting of hydrogen, (C1-4)alkyl, benzyloxy, mono- and di-(C1-3)alkylamino-(C1-4)alkyl, (C1-3)alkoxy, (C1-4)alkyl, hydroxy-methyl, hydroxy-(C2-4)-alkyl, and nitro or R1 and R2 taken together with two consecutive carbon atoms of the pyridine nucleus form a benzene ring optionally substituted by one or two methyl or ethyl groups and R3 is hydroxyalkyl(C1-4). In addition, processes to obtain these compounds are described.Type: ApplicationFiled: May 27, 2009Publication date: October 21, 2010Applicant: ALFA WASSERMAN, S.P.A.Inventors: Giuseppe C. VISCOMI, Manuela CAMPANA, Mahena FOLEGATTI, Paolo RIGHI, Vincenzo CANNATA, Goffredo ROSINI
-
Publication number: 20100266507Abstract: Luminescent reporter compounds that are rotaxanes having the structure where B—Z—C is a reporter molecule based on a cyanine, squaric acid, or other reporter, and K is a macrocycle that encircles and interlocks with the reporter molecule. Applications of the reporter compounds are provided, as well as reactive intermediates used to synthesize the reporter compounds, and methods of synthesizing the reporter compounds.Type: ApplicationFiled: July 30, 2009Publication date: October 21, 2010Inventors: Ewald A. Terpetschnig, Leonid D. Patsenker, Oleksii Klochko, Yuliia Kudriavtseva, Anatoliy L. Tatarets, Inna G. Yermolenko, Yevgen A. Povrozin
-
Publication number: 20100240638Abstract: The present application describes macrocyclic compounds of formula (I) with NS3 protease inhibitory activity for treating hepatitis C virus infection.Type: ApplicationFiled: February 19, 2008Publication date: September 23, 2010Inventors: Shawn D. Britt, Jiping Fu, David Thomas Parker, Michiael Patane, Parkash Raman, Branko Radetich, Mohindra Seepersaud, Aregahegn Yifru, Rui Zheng, Trixi Brand, Sylvain Cottens, Claus Ehrhardt, Stefan Andreas Randl, Pascal Rigollier, Nikolaus Schiering, Oliver Simic
-
Publication number: 20100204159Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.Type: ApplicationFiled: September 11, 2007Publication date: August 12, 2010Inventors: Trixl Brandl, Sylvain Cottens, Claus Ehrhardt, Jiping Fu, Subramanian Karur, David Thomas Parker, Michael A. Patane, Prakash Raman, Stefan Andreas Randl, Pascal Rigollier, Mohindra Seepersaud, Oliver Simic
-
Patent number: 7737134Abstract: Provided herein are compositions, all related stereoisomers as well as pharmaceutically acceptable salts provided as simplified analogs of pateamine A, in which the analogs generally are devoid of the C3-amino and C5-methyl groups, also referred to as desmethyl, desamino-pateamine A. Suitable analogs provide anticancer and antiproliferative effects in vivo and in vitro by a novel drug mechanism of action described herein for pateamine A, including inhibition of eIF4A-dependent translation initiation. As with pateamine A, as described herein, suitable analogs cause cell cycle arrest or induce apoptosis in transformed cells. However, toxicity of such compounds to slow growing normal cells is low. In addition, such analogs, like pateamine A, target translation initiation factors and are useful as anticancer and antiproliferative agents in subjects in need thereof.Type: GrantFiled: October 6, 2006Date of Patent: June 15, 2010Assignees: The Texas A & M University System, The Johns Hopkins UniversityInventors: Daniel Romo, Jun Liu, Nam Song Choi, Zonggao Shi, Woon-Kai Low, Yongjun Dang, Tilman Schneider-Poetsch
-
Publication number: 20100113770Abstract: A medicament having inhibitory activity against NF-?B activation which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in a main chain is 2 to 5 (said connecting group may be substituted), “A” represents an acyl group which may be substituted, (provided that unsubstituted acetyl group and unsubstituted acryloyl group are excluded,) or a C1 to C6 alkyl group which may be substituted, or A may bind to connecting group X to form a cyclic structure which may be substituted, “E” represents an aryl group which may be substituted or a heteroaryl group which may be substituted, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group rType: ApplicationFiled: October 14, 2009Publication date: May 6, 2010Applicant: INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC.Inventors: Susumu MUTO, Akiko ITAI
-
Publication number: 20100113504Abstract: The present invention relates to a compound of Formula (I), its geometrical isomers, in an optically active form as enantiomers, diastereomers, as well as in the form of racemate, as well as pharmaceutically acceptable salts thereof, wherein R is selected from CONHOH, CONHCH2SH, CONHCH2SCOCH3, SH, SCOCH3, SCH3, N(OH)COH, COCONHCH3 and CF3 for the preparation of a medicament, in particular for selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells, for inducing differentiation of tumor cells in a tumor, for inhibiting the activity of histone deacetylase and for the treatment of primary cancer or secondary cancer.Type: ApplicationFiled: March 12, 2008Publication date: May 6, 2010Applicant: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A.Inventors: Stephan Hanessian, Luciana Auzzas, Giuseppe Giannini, Claudio Pisano, Loredana Vesci, Walter Cabri
-
Publication number: 20100093720Abstract: The present invention provides conformationally-defined macrocyclic compounds that bind to and/or are functional modulators of the motilin receptor including subtypes, isoforms and/or variants thereof. These macrocyclic compounds, at a minimum, possess adequate pharmacological properties to be useful as therapeutics for a range of disease indications. In particular, these compounds are useful for treatment and prevention of disorders characterized by hypermotilinemia and/or gastrointestinal hypermotility, including, but not limited to, diarrhea, cancer treatment-related diarrhea, cancer-induced diarrhea, chemotherapy-induced diarrhea, radiation enteritis, radiation-induced diarrhea, stress-induced diarrhea, chronic diarrhea, AIDS-related diarrhea, C.Type: ApplicationFiled: September 11, 2007Publication date: April 15, 2010Inventors: Eric Marsault, Graeme L. Fraser, Kamel Benakli, Carl St-Louis, Alain Rouillard, Helmut Thomas
-
Patent number: 7691859Abstract: A family of imidazole compounds useful for inhibiting the activity of prenyl transferases. The compounds are covered by the following formula: wherein X is (CHR11)n3(CH2)n4Z(CH2)n5 where Z is O, N(R12), S, or a bond; Y is CO, CH2, CS, or a bond; R1 is or N(R24R25); and the remaining substituents are as defined in the disclosure.Type: GrantFiled: October 30, 2007Date of Patent: April 6, 2010Assignee: Ipsen Pharma S.A.S.Inventors: Thomas D. Gordon, Barry A. Morgan
-
Patent number: 7678783Abstract: The present invention is directed to macrocyclic tertiary amine compounds represented by general formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: GrantFiled: November 14, 2005Date of Patent: March 16, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Philippe G. Nantermet, Hemaka A. Rajapakse, Harold G. Selnick, Stacey Lindsley, Keith P. Moore, Shawn J. Stachel
-
Publication number: 20090312540Abstract: Novel spatially-defined macrocyclic compounds incorporating peptide bond surrogates are disclosed. Libraries of these macrocycles are then used to select one or more macrocycle species that exhibit a specific interaction with a particular biological target, in particular, compounds according to the invention are disclosed as agonists or antagonists of a mammalian motilin receptor and a mammalian ghrelin receptor.Type: ApplicationFiled: May 26, 2009Publication date: December 17, 2009Inventors: Pierre Deslongchamps, Yves Dory, Luc Ouellet, Gerald Villeneuve, Mahesh Ramaseshan, Daniel Fortin, Mark L. Peterson, Hamid R. Hoveyda, Sylvie Beaubien, Eric Marsault, Graeme L. Fraser
-
Publication number: 20090275648Abstract: The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and/or variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as antagonists or inverse agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, cardiovascular disorders, obesity and obesity-associated disorders, gastrointestinal disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.Type: ApplicationFiled: April 26, 2006Publication date: November 5, 2009Inventors: Graeme L. Fraser, Hamid R. Hoveyda
-
Publication number: 20090221689Abstract: The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.Type: ApplicationFiled: January 9, 2009Publication date: September 3, 2009Inventors: Eric Marsault, Carl St-Louis
-
Publication number: 20090198050Abstract: The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.Type: ApplicationFiled: October 31, 2008Publication date: August 6, 2009Inventors: Eric Marsault, Luc Ouellet, Carl St-Louis, Sylvie Beaubien, Kamel Benakli, Hamid R. Hoveyda, Mark L. Peterson, Shridhar Bhat
-
Patent number: 7566719Abstract: The present invention relates to compounds of Formula I or II, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: March 6, 2008Date of Patent: July 28, 2009Assignee: Enanta Pharmaceuticals, Inc.Inventors: Suanne Nakajima, Zhenwei Miao, Ying Sun, Datong Tang, Guoyou Xu, Brian Porter, Yat Sun Or, Zhe Wang
-
Publication number: 20090137467Abstract: The invention provides a compound having a structural formula (I): X-?-Y, wherein X is an moiety that binds to the Rif pocket of a bacterial RNA polymerase, Y is a moiety that binds to the secondary channel of a bacterial RNA polymerase, and ? is a linker. The compound can act as an inhibitor of bacterial RNA polymerase. The invention has applications in control of bacterial gene expression, control of bacterial growth, antibacterial chemistry, and antibacterial therapy.Type: ApplicationFiled: November 4, 2006Publication date: May 28, 2009Inventors: Richard H. Ebright, Dongye Wang
-
Patent number: 7470664Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.Type: GrantFiled: July 12, 2006Date of Patent: December 30, 2008Assignee: Merck & Co., Inc.Inventors: M. Katharine Holloway, Nigel J. Liverton, Steven W. Ludmerer, John A. McCauley, David B. Olsen, Michael T. Rudd, Joseph P. Vacca, Charles J. McIntyre
-
Patent number: 7429565Abstract: The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: GrantFiled: April 26, 2004Date of Patent: September 30, 2008Assignee: Gilead Sciences, Inc.Inventors: Constantine G. Boojamra, Carina Cannizzaro, James M. Chen, Xiaowu Chen, Aesop Cho, Lee S. Chong, Maria Fardis, Haolun Jin, Ralph F. Hirschmann, Alan X. Huang, Choung U. Kim, Thorsten Kirschberg, Christopher P. Lee, William A. Lee, Richard L. Mackman, David Y. Markevitch, David A. Oare, Vidya K. Prasad, Hyung-Jung Pyun, Adrian S. Ray, Rosemarie Sherlock, Sundaramoorthi Swaminathan, William J. Watkins, Jennifer R. Zhang
-
Publication number: 20080221142Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases.Type: ApplicationFiled: May 30, 2007Publication date: September 11, 2008Inventors: Matthew J. LaMarche, Simon Bushell, Michael A. Patane, Lewis Whitehead
-
Publication number: 20080194672Abstract: The present invention provides novel conformationally-defined macrocyclic compounds that can function as selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, bone disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.Type: ApplicationFiled: February 8, 2008Publication date: August 14, 2008Inventors: Hamid Hoveyda, Graeme L. Fraser, Kamel Benakli, Sophie Beauchemin, Martin Brassard, David Drutz, Eric Marsault, Luc Ouellet, Mark L. Peterson, Zhigang Wang
-
Publication number: 20080176835Abstract: A family of imidazole compounds useful for inhibiting the activity of prenyl transferases. The compounds are covered by the following formula: wherein X is (CHR11)n3(CH2)n4Z(CH2)n5 where Z is O, N(R12), S, or a bond; Y is CO, CH2, CS, or a bond; R1 is or N(R24R25); and the remaining substituents are as defined in the disclosure.Type: ApplicationFiled: October 30, 2007Publication date: July 24, 2008Inventors: Thomas D. Gordon, Barry A. Morgan
-
Publication number: 20080161555Abstract: The invention relates to a process for the purification of tacrolimus comprising contacting crude tacrolimus with a silver salt dissolved in a water/organic solvent mixture and with a carrier of vegetable origin, separating the mixture from the carrier and recovering purified tacrolimus.Type: ApplicationFiled: July 10, 2006Publication date: July 3, 2008Applicant: ANTIBIOTICOS S.p.A.Inventors: Luca Morra, Jacopo Roletto, Giovanni Lazzari, Walter Cabri, Paolo Paissoni
-
Publication number: 20080146796Abstract: A process for preparing an o-alkylated rapamycin derivative represented by the following general formula (1) is provided. The process includes the steps of reacting rapamycin with an alkyl triflate, purifying the resulting reaction product with a normal phase chromatograph and further purifying a purified product, which has been purified with the normal phase chromatograph, with a reverse phase chromatography wherein R represents an alkyl, arylalkyl, hydroxyalkyl, alkoxyalkyl, acyloxyalkyl, aminoalkyl, alkylaminoalkyl, alkoxycarbonylaminoalkyl, acylaminoalkyl, or aryl.Type: ApplicationFiled: November 26, 2007Publication date: June 19, 2008Applicant: Terumo Kabushiki KaishaInventors: Tetsuro Kawanishi, Masashi Isozaki
-
Publication number: 20080139601Abstract: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR12—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O—; X2 represents a direct bond, —NR11—C1-2alkyl-, —NR11—CH2—, —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen, hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R3 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R10 represents hydrogen; R11 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R12 represents Het14-C1-4alkyl, in particular morpholinyl-C1-4alkyl; Het2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferabType: ApplicationFiled: December 15, 2004Publication date: June 12, 2008Inventors: Eddy Jean Edgard Freyne, Peter Jacobus Johannes Antonius Buijnsters, Kristof Van Emelen, Werner Constant Johan Embrechts, Timothy Pietro Suren Perera
-
Publication number: 20080132500Abstract: Certain water-soluble thiazolyl peptides are antibiotic capable of treating serious bacterial infections in mammals, and particularly, in humans. Some of the analogs can also be employed as versatile intermediates for the preparation of new derivatives with useful antibacterial activity.Type: ApplicationFiled: October 19, 2007Publication date: June 5, 2008Inventors: Kun Liu, Peter T. Meinke, James F. Dropinski, Libo Xu
-
Publication number: 20080132477Abstract: The invention relates to novel macrocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, the number of ring atoms included in the macrocyclic ring being 14, 15, 16 or 17, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.Type: ApplicationFiled: January 13, 2006Publication date: June 5, 2008Inventors: Claudia Betschart, Andreas Lerchner, Rainer Machauer, Heinrich Rueger, Marina Tintelnot-Blomley, Siem Jacob Veenstra
-
Patent number: 7381743Abstract: The present invention relates to new macrocycles of the general formula (I) as well as their use for the treatment of cancer diseasesType: GrantFiled: November 26, 2004Date of Patent: June 3, 2008Assignee: Leibniz-Institut Fuer Pflanzenbiochemie (IPB)Inventors: Ludger A. Wessjohann, Uwe Eichelberger, Thao Tran Thi Phuong
-
Patent number: 7323455Abstract: This invention provides progesterone receptor modulators having the structure: wherein R1 to R7, X, and Q are as defined in the specification; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 22, 2005Date of Patent: January 29, 2008Assignee: WyethInventors: Puwen Zhang, Jay Edward Wrobel, Eugene Anthony Terefenko, Jeffrey Curtis Kern
-
Publication number: 20070281884Abstract: The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: August 11, 2006Publication date: December 6, 2007Inventors: Ying Sun, Deqiang Niu, Guoyou Xu, Yat Sun Or, Zhe Wang
-
Patent number: 7244594Abstract: A microbial method for the preparation of an epothilone containing a terminal hydroxyalkyl group, comprising contacting at least one epothilone having a terminal alkyl group with an enzyme or microorganism capable of catalyzing the selective hydroxylation of said alkyl group to a hydroxyalkyl group, and effecting said hydroxylation.Type: GrantFiled: March 23, 2004Date of Patent: July 17, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Wenying Li, James A. Matson, Xiaohua Huang, Kin Sing Lam, Grace A. McClure
-
Patent number: 7176208Abstract: The present invention relates to compounds of Formula I or II, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: April 16, 2004Date of Patent: February 13, 2007Assignee: Enanta Pharmaceuticals, Inc.Inventors: Suanne Nakajima, Zhenwei Miao, Ying Sun, Datong Tang, Guoyou Xu, Brian Porter, Yat Sun Or, Zhe Wang
-
Patent number: 7122662Abstract: This invention relates to tricyclic compounds having spiro union represented by the following formula (I) or its salt which is useful as a drug, and in particular, as an inhibitor for activated blood coagulation factor X, which can be administered orally and which exhibits strong anticoagulation action. The invention also relates to a pharmacophore which was derived from the compound and is useful in molecular designing of the FXa inhibitor.Type: GrantFiled: December 16, 2004Date of Patent: October 17, 2006Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Hidemitsu Nishida, Fumihiko Saitoh, Kousuke Harada, Ikuya Shiromizu, Takafumi Mukaihira
-
Patent number: 7074961Abstract: Methods and compositions of antidepressants and analogs thereof for inducing local long-lasting anesthesia and analgesia are provided. The methods and compositions are useful for alleviating acute and chronic pain, particularly useful for treating a localized pain.Type: GrantFiled: April 4, 2002Date of Patent: July 11, 2006Assignee: The Brigham and Women's Hospital, Inc.Inventors: Ging Kuo Wang, Peter Gerner, Donald K. Verrecchia
-
Patent number: 7030107Abstract: A novel fused bicyclic pyridine derivative or a salt thereof that acts as a tachykinin receptor antagonist, in particular as an NK1 receptor antagonist, is represented by the following general formula (1): wherein the rings A and B are each a benzene ring which may have 1 to 3 substituents (any adjacent two of which may be bound to one another to form a ring); the ring C is a nitrogen-containing ring having a hydrogen atom substituted with a nitrogen atom; R1 and R2 are each independently a hydrogen atom, a C1 to C6 alkyl group, a C1 to C6 alkylsulfonyl group, a C1 to C6 alkylcarbonyl group, or a C1 to C6 alkoxycarbonyl group, or R1 and R2 are bound to one another to form the ring D; m is 1 or 2; n is 2 or 3; and q is an integer from 1 to 4.Type: GrantFiled: December 6, 2002Date of Patent: April 18, 2006Assignee: Kyorin Pharmaceutical.Co., Ltd.Inventors: Shigeki Seto, Asao Tanioka, Makoto Ikeda, Shigeru Izawa
-
Patent number: 7012140Abstract: The present invention is directed, in general, to a contrast agent comprising a tetraazacyclododecane ligand and comprising a macrocyclic ring and a paramagnetic metal ion coordinated to the tetraazacyclododecane ligand. Pendent arms R, R?, R? and R?? attached to a ring nitrogen. The pendent arms have the general formula: ?C?HR1R2 and for three or more of the pendant arms a chirality of the carbon atoms C? are identical for each of three or more of the pendant arms. The R1 group is larger than hydrogen and R2 is selected from the group consisting of: an alcohol, amides, a carboxylate, phosphinates and a phosphonate. One or more substituents R6 is a group larger than a methyl group and is located on one or more ring carbons.Type: GrantFiled: July 14, 2003Date of Patent: March 14, 2006Assignees: Board of Regents, The University of Texas System, MacrocyclicsInventors: A. Dean Sherry, Mark Woods, Zoltan Kovacs
-
Patent number: 6995153Abstract: A novel fused bicyclic pyrimidine derivative or a salt thereof that acts as a tachykinin receptor antagonist and, in particular, as an NK1 receptor antagonist is represented by the following general formula (1): wherein the rings A and B are each a benzene ring having 1 to 3 substituents (any adjacent two of which may be bound to one another to form a ring); the ring C is a nitrogen-containing ring; m is 1 or 2; and n is 2 or 3.Type: GrantFiled: January 15, 2003Date of Patent: February 7, 2006Assignee: Kyorin Pharmaceutical. Co., Ltd.Inventors: Shigeki Seto, Asao Tanioka, Makoto Ikeda, Shigeru Izawa
-
Patent number: RE41911Abstract: The present invention relates to epothilone derivatives, having the following formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1-R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.Type: GrantFiled: August 11, 2009Date of Patent: November 2, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Gregory D. Vite, Soong-Hoon Kim, Robert M. Borzilleri
-
Patent number: RE42375Abstract: The present invention relates to compounds of Formula I or II, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: February 11, 2008Date of Patent: May 17, 2011Assignee: Enanta Pharmaceuticals, Inc.Inventors: Suanne Nakajima, Zhenwei Miao, Ying Sun, Datong Tang, Guoyou Xu, Brian Porter, Yat Sun Or, Zhe Wang