The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/253)
-
Publication number: 20080214638Abstract: Therapeutically active anthranilic acid derivatives of Formula (I) or of Formula (Ia) wherein R, R1, R2 and Z are as defined in the specification, processes for the preparation of said derivatives, pharmaceutical formulations containing the active compounds and the use of the compounds in therapy, particularly in the treatment of diseases in which under-activation of the HM74A receptor contributes to the disease or in which activation of the receptor will be beneficial, are disclosed.Type: ApplicationFiled: February 14, 2006Publication date: September 4, 2008Inventors: Andrew McMurtrie Mason, Ivan Leo Pinto, Shahzad Sharooq Rahman
-
Publication number: 20080214830Abstract: Disclosed herein a process for producing 2-(n-butyl)-3-[[2?-(tetrazol-5-yl)biphenyl-4-yl]methyl]-1,3-diazaspiro[4.4]non-1-en-4-one of formula (I) in pure form by using selective solvent system and cost efficient raw materials and reagents.Type: ApplicationFiled: July 27, 2006Publication date: September 4, 2008Applicant: Jubilant Organosys LimitedInventors: Charugundla Kishore, Vinod Vishwanath Bandi, Rajappa Murali, Satish M.A., Manjunatha G. Sulur
-
Publication number: 20080214637Abstract: A process for the synthesis of tetrazol derivative has been developed which starts from a tetrazole derivative where acidic hydrogen atom has been replaced by a protecting group and the deprotection is performed with a catalytic amount of organic acid and can proceed in an aqueous solvent.Type: ApplicationFiled: November 11, 2005Publication date: September 4, 2008Applicant: LEK Pharmaceuticals D.D.Inventors: Ljubomir Antoncic, Johannes Ludescher
-
Publication number: 20080200527Abstract: Compounds of formula (I), are cannabinoid CB1 receptors, useful, inter alia in the treatment of obesity: wherein A1 is hydrogen, —COOH, or tetrazolyl, and A2 is hydrogen, —COOH, tetrazolyl, —CN, —CF3, —COR6, —SO2R6, —OR7, —NR7R8, —NHCOR6, and —NR7SO2R8 provided that one of A1 and A2 is either —COOH or tetrazolyl; p is 0 or 1 and A3 is phenyl or cycloalkyl, either of which is optionally substituted with R4 and/or R5; q is 0 or 1; R1 is a bond, or —(CH2)aB1(CH2)b— wherein a and b are independently 0, 1, 2 or 3 provided that a+b is not greater than 4, and B1 is —CO—, —O—, —S—, —SO—, —SO2—, —CH2—, —CHOH— or —NR7—; R2 is a bond, —CH2)aB1(CH2)b— or —[(CH2)aB1(CH2)b]n-A4-[(CH2)cB2(CH2)d]m— wherein a, b, and B1 are as defined for R1; B2 is as defined for B1, c and d are independently 0, 1, 2 or 3; with the proviso that a+b+c+d is not greater than 6, n and m are independently 0 or 1 and A4 is a monocarbocyclic or monoheterocyclic ring, having 3 to 8 ring atoms, optionally substituted with one or more of —F, —Cl, —Br,Type: ApplicationFiled: June 14, 2006Publication date: August 21, 2008Applicant: Carex SAInventors: Remi Alain Amengual, Claire Nadelene Marsol, Eric Liu Mayeux, Michael laurence Sierra, Patrick Herve Wagner
-
Publication number: 20080194660Abstract: A compound having the structure wherein R is an angiotensin receptor antagonist active group, Y is -Y1-Y2-Y3-Y4-Y5-; Y1 is C(R1R2); R1 is selected from the group consisting of hydrogen and C1-4 alkyl; R2 is selected from the group consisting of hydrogen, C1-4 alkyl, and —OC(O)C1-4 alkyl; Y2 is O or CH2; Y3 is C(O) or CH2; Y4 is O or CH2; Y5 is —(CH2)1-2—(X)0-1—(CH2)0-1— or is absent; X is —O— or —CR3R4—; and R3 and R4 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.Type: ApplicationFiled: December 11, 2007Publication date: August 14, 2008Inventors: Iyassu K. Sebhat, Michael Man-chu Lo, Ravi P. Nargund, Amjad Ali, Chris Franklin, Nicoletta Almirante, Laura Storoni, Silvia Stefanini
-
Publication number: 20080188533Abstract: The invention is directed to compounds of formula I: wherein Ar, r, R3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula I have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.Type: ApplicationFiled: January 31, 2008Publication date: August 7, 2008Inventors: Seok-Ki Choi, Paul R. Fatheree, Sharath Hegde, Ryan Hudson, Keith Jendza, Daniel Marquess, Robert M. McKinnel, Vivek Sasikumar
-
Publication number: 20080182994Abstract: A process for producing crystals of 2-ethoxy-1-[[2?-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H-benzimidazole-7-carboxylic acid (compound (I)), characterized by dissolving or suspending the compound (I) or a salt thereof in a solvent comprising an aprotic polar solvent and crystallizing it. By the process, the contaminants which are contained in the compound (I) or its salt and are difficult to remove, such as tin compounds, analogues of the compound (I), and a residual organic solvent, can be easily removed. Crystals of the compound (I) can be efficiently and easily mass-produced in high yield on an industrial scale.Type: ApplicationFiled: March 12, 2008Publication date: July 31, 2008Inventors: Hideo Hashimoto, Hideaki Maruyama
-
Patent number: 7405332Abstract: The invention provides a process for preparation of a fluorohaloalkane, preferably an [18F]fluorohaloalkane of formula (I) wherein X is halo and n is an integer of from 1 to 6; which comprises: reaction of the corresponding organosilicon compound of formula (II): wherein n is as defined for the compound of formula (I); and R?, R?, and R?? are independently selected from C1-6 alkyl and C1-6 haloalkyl; and R? may alternatively be the group: with a compound of formula (III): wherein X is as defined for the compound of formula (I) and Y is halo. Intermediates having use in such processes are also claimed.Type: GrantFiled: September 18, 2003Date of Patent: July 29, 2008Assignee: Hammersmith Imanet Ltd.Inventors: Frank Brady, Sajinder Luthra, Yongjun Zhao
-
Publication number: 20080161373Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, M and R11 are as defined herein. The compounds of Formula (I) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: ApplicationFiled: December 13, 2006Publication date: July 3, 2008Inventors: Donald J.P. Pinto, Joanne M. Smallheer, James R. Corte, Zilun Hu, Cullen L. Cavallaro, Paul J. Gilligan, Mimi L. Quan, Leon M. Smith
-
Patent number: 7390803Abstract: The present invention is directed to compounds of the formula (I) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R27, R28, R29, R30, R31, X, m, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity.Type: GrantFiled: October 24, 2003Date of Patent: June 24, 2008Assignee: Merck & Co., Inc.Inventors: Gabor Butora, Sander G. Mills, Alexander Pasternak, Kothandaraman Shankaran, Lihu Yang, Changyou Zhou, Stephen D. Goble
-
Publication number: 20080139505Abstract: The present invention provides compounds of formula (I): pharmaceutical compositions thereof, and methods of using the same, processes or preparing the same, and intermediates thereof.Type: ApplicationFiled: November 15, 2005Publication date: June 12, 2008Inventors: Thomas Daniel Aicher, Guillermo S. Cortez, Todd Michael Groendyke, Albert Khilevich, James Allen Knobelsdorf, Fredrik Pehr Marmsater, Jeffrey Michael Schkeryantz, Tony Pisal Tang, Nicholas Andrew Magnus
-
Publication number: 20080131368Abstract: The present invention provides tetra-amine chelator conjugates with biological targeting moieties, linked via a linker group and technetium complexes thereof as radiopharmaceuticals. The linker group is such that the chelator is mono-functionalised at the bridgehead position and provides both flexibility and a lack or aryl groups, to minimise lipophilicity and steric hulk. Protected versions of the chelators are provided which permit conjugation with a wide range of targeting molecules without interfering reactions with the amine nitrogens of the tetra-amine chelator. Syntheses of the functionalised chelators are described, together with bifunctional chelate precursors. Radiopharmaceutical compositions comprising the technetium metal complexes of the invention are described, together with non-radioactive kits for the preparation of such radiopharmaceuticals.Type: ApplicationFiled: July 19, 2005Publication date: June 5, 2008Applicant: GE HEALTHCARE LIMITEDInventors: Anthony Eamonn Storey, Harry John Wadsworth, Nigel Anthony Powell, Philip Duncanson
-
Publication number: 20080132548Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.Type: ApplicationFiled: August 1, 2007Publication date: June 5, 2008Inventors: Xiangping Qian, Jeffrey T. Finer, Pu-Ping Lu, Chihyuan (Grace) Chuang, Bradley P. Morgan, David J. Morgans
-
Publication number: 20080125587Abstract: The present invention provides novel methods of preparing triazole compounds which inhibit the activity of Hsp90. One embodiment of the invention is directed to methods for preparing a triazole compound represented by the following Structural Formula: or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising the steps of: a) reacting an amide represented by the following Structural Formula: with a thionation reagent to form a thioamide; b) reacting the thioamide of step a) with hydrazine to form a hydrazonamide; c) reacting the hydrazonamide of step b) with a carbonylation or a thiocarbonylation reagent. In one embodiment, the present invention is a method of synthesis of a compound of formula (IA) or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising reacting a compound of formula (IIA) with an oxidizing agent, thereby producing a compound of formula (IA).Type: ApplicationFiled: May 25, 2007Publication date: May 29, 2008Inventors: Dinesh U. Chimmanamada, Chi-Wan Lee, David James, Shijie Zhang, Weiwen Ying, Junghyun Chae, Teresa Przewloka
-
Patent number: 7378531Abstract: Provided is a process for preparing valsartan and precursors thereof.Type: GrantFiled: April 21, 2004Date of Patent: May 27, 2008Assignee: Teva Pharmaceutical Industries LtdInventors: Zvi Harel, Igor Rukhman
-
Publication number: 20080119456Abstract: Compounds of formula (I) are useful for the treatment of disease responsive to modulation of CRTH2 receptor activity, such as asthma, rhinitis, allergic airway syndrome, and allergic rhinobronchitis; wherein X1 is —S—, —O—, —N?N—. —NR7—, —CR7?CR8—, —CR7?N—, wherein R7 and R8 are independently hydrogen or C1-C3 alkyl; A is a carboxyl group —COOH, or a carboxyl bioisostere; rings Ar2 and Ar3 each independently represent a phenyl or 5- or 6-membered monocyclic heteroaryl ring, or a bicyclic ring system consisting of a 5- or 6-membered carbocyclic or heterocyclic ring which is benz-fused or fused to a 5- or 6-membered monocyclic heteroaryl ring, said ring or ring system being optionally substituted; ring B is as defined for Ar2 and Ar3, or an optionally substituted N-pyrrolidinyl, N-piperidinyl or N-azepinyl ring; s is 0 or 1; L1, L2 and L4 are linker radicals as defined in the description; Q1 and Q2 represent substituents as defined in the description.Type: ApplicationFiled: May 30, 2005Publication date: May 22, 2008Inventors: Trond Ulven, Thomas Frimurer, Oystein Rist, Evi Kostenis, Thomas Hogberg, Jean-Marie Receveur, Marie Grimstrup
-
Publication number: 20080114045Abstract: The present invention relates to novel processes for the preparation of candesartan or of a protected form of candesartan, of a candesartan salt or of a candesartan ester; compounds which can be used in processes according to the invention, processes for their preparation, their use in processes according to the invention; a novel polymorphic form of candesartan cilexetil, a process for its preparation and its use for the production of a medicament.Type: ApplicationFiled: December 15, 2005Publication date: May 15, 2008Applicant: Graf-Arco-Str. 3Inventors: Yaping Wang, Yonggang Li, Yulin Li, Guojun Zheng, Yi Li, Stefan Koecher
-
Publication number: 20080110536Abstract: A novel compound, used for example, as a gas generating fuel, is defined as a compound having the structural formula of R3-R1-R2, wherein R1 is a benzene ring with nitro substitution, R2 is a tetrazolyl group with a C—C bond to the benzene ring, and R3 is a tetrazolyl group with a C—C bond to the benzene ring. A method of making the compound is also provided. A gas generating composition containing the novel compound as a fuel, and an oxidizer is also provided. The novel compound is contained within a gas generant composition, within a gas generator. The gas generator may be contained within a gas generating system such as an airbag inflator or seat belt assembly, or more broadly within a vehicle occupant protection system.Type: ApplicationFiled: May 4, 2007Publication date: May 15, 2008Inventors: Sudhakar R. Ganta, Graylon K. Williams, Cory G. Miller
-
Publication number: 20080099111Abstract: A poly(tetrazole) is formed by a water-based method. A gas generating composition 12 containing the poly(tetrazole) is contained within an exemplary gas generator 10. A gas generating system 200 incorporates the poly(tetrazole) therein. A vehicle occupant protection system 180 incorporates the gas generating system 200.Type: ApplicationFiled: November 1, 2005Publication date: May 1, 2008Inventors: Cory G. Miller, Graylon K. Williams
-
Publication number: 20080103182Abstract: The invention is concerned with novel indazole derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used in the prevention or treatment of diseases which are modulated by L-CPT1 inhibitors.Type: ApplicationFiled: October 19, 2007Publication date: May 1, 2008Inventors: Jean Ackermann, Konrad Bleicher, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei
-
Publication number: 20080096892Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellu-lar activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Even more specifically, the invention provides compounds for modulating c-Kit kinase activity and methods of treating diseases mediated by c-Kit activity utilizing the compounds and pharmaceutical compositions thereof.Type: ApplicationFiled: August 27, 2004Publication date: April 24, 2008Applicant: Exelixis, Inc.Inventors: Wei Cheng, Erick Wang Co, Moon Hwan Kim, Rhett Ronald Klein, Donna T. Le, Amy Lew Tsuhako, John M. Nuss, Wei Xu, William Bajjalieh
-
Patent number: 7361770Abstract: Valsartan of formula (I) is prepared by hydrolysis of valsartan benzyl ester with an alkali metal hydroxide, washing with an organic solvent, acidifying with hydrochloric acid and isolating valsartan from the reaction mixtureType: GrantFiled: June 16, 2003Date of Patent: April 22, 2008Assignee: Hetero Drugs LimitedInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy
-
Publication number: 20080090885Abstract: A method for synthesis of losartan 5-carboxylic acid (EXP-3174).Type: ApplicationFiled: January 29, 2007Publication date: April 17, 2008Inventors: Liqin Chen, Jian Li, Yingzhong Shen
-
Patent number: 7354895Abstract: The present invention relates to compounds of Formula I, and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases associated with carboxypeptidase U. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds; to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above.Type: GrantFiled: May 3, 2000Date of Patent: April 8, 2008Assignee: AstraZeneca ABInventors: Marcel Linschoten, Magnus Polla
-
Patent number: 7351825Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.Type: GrantFiled: December 15, 2004Date of Patent: April 1, 2008Assignee: Japan Tobacco Inc.Inventors: Takashi Inaba, Julia Haas, Makoto Shiozaki, Nicole M. Littmann, Katsutaka Yasue, Steven W. Andrews, Atushi Sakai, Andrew M. Fryer, Takafumi Matsuo, Ellen R. Laird, Akira Suma, Yuichi Shinozaki, Yoshikazu Hori, Hiroto Imai, Tamotsu Negoro
-
Publication number: 20080076932Abstract: A process for the preparation of olmesartan medoxomil, and derivatives thereof, by use of novel phenyltetrazole intermediates.Type: ApplicationFiled: September 26, 2007Publication date: March 27, 2008Applicant: DIPHARMA FRANCIS S.R.L.Inventors: Gabriele RAZZETTI, Lino COLOMBO, Paola ROTA, Pietro ALLEGRINI
-
Patent number: 7348322Abstract: The present invention relates to compounds of formula I: wherein A, X, R1, R2 and R3 are as defined herein and pharmaceutically acceptable salts thereof. The invention also relates to methods of using the compounds of formula I and pharmaceutical compositions comprising the compounds of formula I.Type: GrantFiled: December 8, 2006Date of Patent: March 25, 2008Assignee: Roche Palo Alto LLCInventors: Leyi Gong, Counde O'Yang, Yun-chou Tan
-
Patent number: 7345009Abstract: The present invention relates to novel substituted pyrazolines of the formula (I) in which R1, R2, R3 and R4 are as defined in the disclosure, to a plurality of processes for preparing these substances and their use for controlling pests, and to novel intermediates and processes for their preparation.Type: GrantFiled: January 23, 2003Date of Patent: March 18, 2008Assignee: Bayer CropScience AGInventors: Fritz Maurer, Rainer Fuchs, Angelika Lubos-Erdelen, legal representative, Jörg Konze, Peter Lösel, Andreas Turberg, Christoph Erdelen
-
Patent number: 7335649Abstract: Invented are non-peptide TPO mimetics. Also invented are novel processes and intermediates used in the preparation of the presently invented compounds. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative.Type: GrantFiled: November 9, 2006Date of Patent: February 26, 2008Assignee: SmithKline Beecham CorporationInventors: Kevin J. Duffy, Connie Erickson-Miller, Julian Jenkins, Juan I. Luengo, Sophie Visonneau
-
Publication number: 20080039640Abstract: A process for the preparation of a compound of formula (I) or a salt thereof wherein R is an amino, nitro or —NHCOR1 group, wherein R1 is C1-C6 alkyl or phenyl optionally substituted by a —O—(CH2)n-phenyl group, wherein n is an integer of 1 to 6; comprising reacting a compound of formula (II) or a salt thereof, both as the individual isomer and as an isomeric mixture, wherein R is as defined above; with a dehydrating agent, if necessary in the presence of an organic solvent, and optionally in the presence of a basic agent; and, if desired, converting a compound of formula (I) to another compound of formula (I) or a salt thereof.Type: ApplicationFiled: August 8, 2007Publication date: February 14, 2008Applicant: DIPHARMA FRANCIS S.R.L.Inventors: Lino COLOMBO, Pietro ALLEGRINI, Alessandra AMOROSI, Gabriele RAZZETTI, Roberto ROSSI
-
Patent number: 7326732Abstract: A compound of formula (I): or a salt, solvate and chemically protected form thereof, wherein: R5 is an optionally substituted C5-20 aryl or C4-20 alkyl group; A is selected from the group consisting of: wherein X and Y are selected from the group consisting of: O and CR3; S and CR3; NH and CR3; NH and N; O and N; S and N; N and S; and N and O, and where the dotted lines indicate a double bond in the appropriate location, and where Q is either N or CH; R3 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; R4 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; R6 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; D is selected from: B is selected from the group consisting of: where RN? is selected from H and C1-4 alkyl; where one of RP3 and RP4 is —Cm alkylene-R2 and tType: GrantFiled: February 11, 2005Date of Patent: February 5, 2008Assignee: Pharmagene Laboratories LimitedInventors: Alexander William Oxford, Richard Jon Davis, Robert Alexander Coleman, Kenneth Lyle Clark, David Edward Clark, Neil Victor Harris, Garry Fenton, George Hynd, Keith Alfred James Stuttle, Jonathan Mark Sutton, Mark Richard Ashton, Edward Andrew Boyd, Shirley Ann Brunton
-
Patent number: 7314885Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds, processes for making the compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: March 22, 2006Date of Patent: January 1, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Alex Aronov, Upul K. Bandarage, David J. Lauffer, Pan Li, Ronald C. Tomlinson
-
Patent number: 7312340Abstract: Provided is a novel method of making 2-butyl-3-[[2?(1-trityl-1H-tetrazol-5-yl)biphen-4-yl]methyl]-1,3-diazaspiro[4.4]non-1-ene-4-one, which can be converted to irbesartan. Also provided are methods of making irbesartan.Type: GrantFiled: January 9, 2006Date of Patent: December 25, 2007Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Ben-Zion Dolitzky, Julia Kaftanov, Boris Pertsikov, Igor Rukhman, Gennady Nisnevich
-
Patent number: 7309792Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of the dimeric mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.Type: GrantFiled: March 1, 2005Date of Patent: December 18, 2007Assignee: Board of Regents, The University of Texas SystemInventors: Patrick G. Harran, Xiaodong Wang, Jef K. De Brabander, Lin Li, Ranny Mathew Thomas, Hidetaka Suzuki
-
Publication number: 20070270387Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: May 11, 2007Publication date: November 22, 2007Inventors: Yariv Donde, Jeremiah H. Nguyen
-
Patent number: 7291623Abstract: A method of inhibiting or effecting the activity of protein kinase activity which comprises contacting a protein kinase with a compound of formula (I) being a derivative of a furanose or pyranose form of a monosaccharide, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 5, 2003Date of Patent: November 6, 2007Assignee: Alchemia LimitedInventors: Wim Meutermans, Karl Schafer, Michael L. West, Craig Muldoon, Fiona Foley, Natalie Bouloc, Gerald Tometzki
-
Patent number: 7291744Abstract: The present application describes modulators of chemokine receptors of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: November 12, 2004Date of Patent: November 6, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Soo S. Ko, Douglas G. Batt, George V. Delucca, John V. Duncia, Daniel S. Gardner, Joseph B. Santella
-
Publication number: 20070249519Abstract: The present invention is directed to novel compositions and their application as pharmaceuticals for the treatment of disease. Methods of upregulation of GLUT4 via activation of peroxisome proliferator activated receptor delta activity in the adipose tissue of a human or animal subject are also provided, for the treatment of conditions such as diabetes, obesity, insulin resistance, metabolic syndrome, and others in which a reduction in insulin resistance, an increase in glucose utilization, a reduction in visceral fat, a reduction in triglyceride (TG) levels, or an increase in levels of high-density lipoprotein (HDL), is beneficial.Type: ApplicationFiled: April 19, 2007Publication date: October 25, 2007Applicant: KALYPSYS, INC.Inventors: Mausumee Guha, Ayman Kabakibi
-
Patent number: 7285565Abstract: Novel benzamide compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: January 14, 2005Date of Patent: October 23, 2007Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
-
Publication number: 20070219265Abstract: A compound comprising or a pharmaceutically acceptable salt thereof, or a prodrug thereof is disclosed herein. Y, A, and B are as described herein. Methods, compositions, and medicaments related to these compounds are also disclosed.Type: ApplicationFiled: March 20, 2007Publication date: September 20, 2007Inventors: David W. Old, Danny T. Dinh
-
Publication number: 20070213371Abstract: Dibenzyl amine compounds and derivatives, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.Type: ApplicationFiled: January 3, 2007Publication date: September 13, 2007Inventors: George Chang, Ravi S. Garigipati, Bruce Lefker, David A. Perry, Dongxiang Zeng
-
Publication number: 20070213302Abstract: The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and/or cardiometabolic disorders.Type: ApplicationFiled: March 9, 2007Publication date: September 13, 2007Applicant: JENRIN DISCOVERYInventors: John Francis McElroy, Robert J. Chorvat
-
Publication number: 20070213314Abstract: Dibenzyl amine compounds and derivatives, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.Type: ApplicationFiled: January 3, 2007Publication date: September 13, 2007Inventors: George Chang, Ravi S. Garigipati, Bruce Lefker, David A. Perry
-
Publication number: 20070155707Abstract: Pharmacological inhibition of fatty acid amide hydrolase (FAAH) activity leads to increased levels of fatty acid amides. Esters of alkylcarbamic acids are disclosed that are inhibitors of FAAH activity. Compounds disclosed herein inhibit FAAH activity. Described herein are processes for the preparation of esters of alkylcarbamic acid compounds, compositions that include them, and methods of use thereof.Type: ApplicationFiled: November 20, 2006Publication date: July 5, 2007Applicant: Kadmus Pharmaceuticals, Inc.Inventors: Olivier Dasse, David Putman, Timothy R. Compton
-
Patent number: 7217825Abstract: Provided are a method of making irbesartan via a Suzuki coupling reaction and a novel intermediate, 2-butyl-3-(4?-bromobenzyl)-1,3-diazaspiro[4.4]non-1-ene-4-one, for such process. The novel process includes the step of reacting such intermediate with a protected imidazolephenylboronic acid.Type: GrantFiled: February 6, 2006Date of Patent: May 15, 2007Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Gennady Nisnevich, Igor Rukhman, Boris Pertsikov, Julia Kaftanov, Ben-Zion Dolitzky
-
Patent number: 7199144Abstract: Provided are process for the preparation of valsartan and the precursors thereof.Type: GrantFiled: April 21, 2004Date of Patent: April 3, 2007Assignee: Teva Pharmaceuticals Industries, Ltd.Inventors: Igor Rukhman, Ben-Zion Dolitzky, Evgeni Flyaks
-
Patent number: 7186749Abstract: The present invention relates to pyrrolo-naphthyl compounds of the formula and methods of using them to modulate PAI-1 expression and to treat PAI-1 related disorders.Type: GrantFiled: August 22, 2005Date of Patent: March 6, 2007Assignee: WyethInventors: Thomas J. Commons, Douglas John Jenkins
-
Patent number: 7179910Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: GrantFiled: September 8, 2003Date of Patent: February 20, 2007Assignee: Agouron Pharmaceuticals, Inc.Inventors: Huiping Guan, Congxin Liang, Li Sun, Peng Cho Tang, Chung Chen Wei, Tomas Vojkovsky, Qingwu (Alan) Jin, Paul M. Herrinton, Michael A. Mauragis
-
Patent number: 7179825Abstract: The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3; R1 represents hydrogen, hydroxy, C1-6alkyl or aryl; R2 represents hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; Het1; or R1 and R2 taken together may form a bivalent radical of formula —(CH2)n— wherein n is 2, 3, 4, 5 or 6; R3 represents hydrogen, optionally substituted C1-6alkyl, aryl, Het1; R4 represents hydrogen; hydroxy; mercapto; C1-6alkyloxy; C1-6alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C1-12alkyl; optionally substituted C2-8alkenyl; optionally substituted C2-8alkynyl; optionally substituted C3-7cycloalkyl; optionally substituted C5-7cycloalkenyl; aryl; Het1; or -Alk-NR3R5 (i) or —NR3R5 (ii) wherein Alk represents C1-6alkanediyl; and R5 represents hydrogen, C1-6alkyl, aryl, Het1, (aryl or Het1)C1-6alkyl, (aryl or Het1)carbonyl or (aType: GrantFiled: March 16, 2005Date of Patent: February 20, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: Dominique Mabire, Christophe Denis Adelinet, Imré Christian Csoka, Marc Gaston Venet
-
Patent number: 7173129Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.Type: GrantFiled: June 7, 2004Date of Patent: February 6, 2007Assignee: Athero Genics, Inc.Inventors: Kimberly J. Worsencroft, Liming Ni, Zhihong Ye, Charles Q. Meng, M. David Weingarten, Jacob E. Simpson, James A. Sikorski