Acyclic Carbon Bonded Directly To The -c(=x)- (e.g., N-oleoylpyrrolidine, Etc.) Patents (Class 548/540)
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Publication number: 20090163547Abstract: The present invention makes reference to new indene derivatives with general formula (I), as well as to their preparation procedures, their application as medicament and the pharmaceutical compositions containing them. The new compounds of formula (I) show affinity for 5-HT6 receptors and are, therefore, effective for treating diseases mediated by these receptors.Type: ApplicationFiled: November 7, 2006Publication date: June 25, 2009Inventors: Maria De Las Ermitas Alcalde-Pais, Jordi Frigola-Constansa, Joerg Holenz, Ramon Merce-Vidal, Maria De Les Neus Mesquida-Estevez, Sara Lopez-Perez
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Publication number: 20090149509Abstract: N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, salts or prodrugs thereof have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by PDF inhibitors, such as treatment of bacterial infections.Type: ApplicationFiled: December 3, 2008Publication date: June 11, 2009Applicant: VICURON PHARMACEUTICALS INC.Inventors: Jeffrey JACOBS, Rakesh K. JAIN, Jason G. LEWIS, Dinesh V. PATEL, Zhengyu YUAN
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Publication number: 20090137658Abstract: Besylate salts of trans-4-({2-[(2S)-2-cyano-pyrrolidinyl]-2-oxoethyl}amino)-N,N-dimethylcyclohexanecarboxamide are described as well as methods of using the same in the treatment of disorders characterized by hyperglycemia.Type: ApplicationFiled: November 9, 2007Publication date: May 28, 2009Inventors: Masataka HIKOTA, Toru Iijima, Michael S. McClure
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Publication number: 20090124559Abstract: The invention provides compounds and methods for inhibiting proteases. One aspect of the invention features pro-soft inhibitors which react with an activating protease to release an active inhibitor moiety in proximity to a target protease. In certain instances, compounds inhibit proteasomes and/or post-proline cleaving enzymes (PPCE), such as dipeptidyl peptidase IV. The compounds of the invention provide a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.Type: ApplicationFiled: December 15, 2006Publication date: May 14, 2009Applicant: Trustees of Tufts College Office of Technology and Industry CollaborationInventors: William W. Bachovchin, Hung-Sen Lai, Wengen Wu
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Patent number: 7524844Abstract: The present invention relates to novel compounds useful as dipeptidyl peptidase IV (DPP-IV) inhibitors of the formula: wherein X, Y, a, R1, and R2 are as defined herein.Type: GrantFiled: February 15, 2007Date of Patent: April 28, 2009Assignee: Glenmark Pharmaceuticals S.A.Inventors: Abraham Thomas, Balasubramanian Gopalan, V.S. Prasada Rao Lingam, Daisy Manish Shah
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Patent number: 7514571Abstract: A novel bicyclo derivative represented by the following general formula (1), or a pharmaceutically acceptable salt thereof, acts as an effective DPP-IV inhibitor: One example is (2S,4S)-1-[[N-(4-methylbicyclo[2,2,2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile).Type: GrantFiled: February 22, 2005Date of Patent: April 7, 2009Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Kazuya Yokota, Koji Murakami, Tomohiro Ide
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Publication number: 20090082420Abstract: The present application describes deuterium-enriched vildagliptin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 18, 2008Publication date: March 26, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090076284Abstract: A process for continuously removing a target product X in the form of fine crystals from a liquid phase P comprising the target product X and constituents other than the target product X by cooling suspension crystallization in the secondary chamber, into which the liquid phase P flows continuously, of an indirect heat exchanger with simultaneous continuous flow of a coolant through the primary chamber of the indirect heat exchanger and continuous withdrawal of a crystal suspension S having a degree of crystallization Y from the secondary chamber, in which the degree of crystallization Y is adjusted on the basis of a heat balance conducted continuously with the aid of a process computer.Type: ApplicationFiled: September 12, 2008Publication date: March 19, 2009Applicant: BASF SEInventors: Joerg Heilek, Peter Schlemmer, Ulrich Hammon, Klaus Joachim Mueller-Engel
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Patent number: 7488725Abstract: Compounds are provided having the formula: wherein R1, R2, R2?, R3, R3?, R4, R4?, R5, X, Y and Z are as defined herein.Type: GrantFiled: October 30, 2006Date of Patent: February 10, 2009Assignee: Bristol-Myers Squibb Co.Inventors: Stephen P. O'Connor, Lawrence G. Hamann
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Publication number: 20090036436Abstract: Compounds of Formulas 1 and 2 where the variables have the meaning disclosed in the specification, have analgesic and in some cases immunostimulant activity.Type: ApplicationFiled: January 25, 2006Publication date: February 5, 2009Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello
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Patent number: 7462641Abstract: The present invention includes anhydrous crystalline forms of (2S,4S)-4-fluoro-1-[4-fluoro-?-(4-fluorophenyl)-L-phenylalanyl]-2-pyrrolidinecarbonitrile p-toluenesulfonic acid salt.Type: GrantFiled: July 19, 2004Date of Patent: December 9, 2008Assignee: SmithKline Beecham CorporationInventors: David H Igo, Paul R Johnson, Daniel E Patterson, Amarjit Sab Randhawa
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Publication number: 20080299190Abstract: This invention relates to tablets especially tablets formed by direct compression of a dipeptidylpeptidase IV (DPP-IV) inhibitor compound, a process for the preparation thereof; to new pharmaceutical formulations, and new tableting powders comprising DPP-IV inhibitor formulations capable of being directly compressed into tablets. The invention relates further to a process for preparing the tablets by blending the active ingredient and specific excipients into the new formulations and then directly compressing the formulations into the direct compression tablets. The invention also relates to vildagliptin particle size distribution and a new crystal form of vildagliptin particularly adapted for the preparation of improved tablets and other pharmaceutical compositions.Type: ApplicationFiled: January 17, 2006Publication date: December 4, 2008Applicant: NOVARTIS AGInventors: Sabine Pfeffer, Frank Schaefer, Ricardo Schneeberger, Paul Allen Sutton, Martin Friedrich Trueby, Wolfgang Wirth
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Publication number: 20080300192Abstract: Auristatin-type peptides are disclosed which are highly cytotoxic, synthetically accessible, and can be conjugated to antibodies and other ligands.Type: ApplicationFiled: November 14, 2005Publication date: December 4, 2008Applicant: Seattle Genetics, Inc.Inventors: Svetlana o. Doronina, Brian A. Mendelsohn
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Publication number: 20080286219Abstract: Skin brightening compositions based on hydroquinone derivatives and methods of making and using the composition. The hydroquinone derivatives are 2-thio-hydroquinone derivatives.Type: ApplicationFiled: May 17, 2007Publication date: November 20, 2008Inventors: Michael Fitzpatrick Wempe, Jeffrey M. Clauson
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Publication number: 20080287687Abstract: The present invention relates to a production method of a compound represented by the formula (3), which includes reacting a compound represented by the formula (2) with a diphenylmethyl halide compound represented by the formula (1) in the presence of alkali metal alkoxide. According to the method of the present invention, compound (3) can be produced at a high purity and in a high yield. wherein each symbol is as defined in the specification, *1 and *2 each show an asymmetric carbon atom, and the configuration of the asymmetric carbon atom of *1 and *2 is (S,S) or (R,R).Type: ApplicationFiled: October 31, 2007Publication date: November 20, 2008Applicant: AJINOMOTO CO. INCInventors: Takayuki Hamada, Kunisuke Izawa, Vadim A. Soloshonok
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Publication number: 20080255126Abstract: Novel compounds that are inhibitors of one or most post-proline cleaving proteases, e.g. dipeptidyl peptidase IV, according to general formula (1). R1 is H or CN, X1 is O, S, CH2, CHF, CF2, CH(CH3), C(CH3)2 or CH(CN), and b is 1 or 2. G1 is H or a group according to the formula —CH2—X2—(CH2)a-G3 and G2 is H or a group according to the formula —CH2—(CH29a-G3, provided that one of G1 and G2 is H and the other is not H. X2 is O, S, or CH2, and a is 0, 1 or 2, provided that when a is 1 then X2 is CH2. G3 is a group according to one of general formulae 2-4, where the variables have meaning given in the description. The compounds are useful in the treatment of i.a. type 2 diabetes and impaired glucose tolerance.Type: ApplicationFiled: December 20, 2007Publication date: October 16, 2008Inventors: David M. Evans, Doreen M. Ashworth
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Publication number: 20080242658Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula IType: ApplicationFiled: April 6, 2005Publication date: October 2, 2008Inventors: Mark G Palermo, Sushil Kumar Sharma, Christopher Straub, Run-Ming Wang, Leigh Zawel, Yanlin Zhang, Zhuoliang Chen, Yaping Wang, Fan Yang, Wojciech Wrona, Gang Liu, Mark G. Charest, Feng He
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Publication number: 20080234292Abstract: The present invention relates to a series of novel compounds having the formula (I) wherein: X is NR3 or O; n is 1 or 2; A is a bicyclic carbocycle and R1 and R2 are as described herein. The compounds are useful as DPP-IV inhibitors, such as for the treatment of diabetes.Type: ApplicationFiled: July 21, 2005Publication date: September 25, 2008Inventors: Susan Marie Royalty, James Ford Burns, Jan Jozef Scicinski, Gunnar Erik Jagdmann, Jr., Robert James Foglesong, Kellee Griffin Ring, Tatyana Dyakonov, David Middlemiss
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Publication number: 20080200466Abstract: Compounds of formula (I) in free or pharmaceutically acceptable salt form, where R1, R2, R3, R4, R5, R6, R7, m, n, w, X, and Y have the meanings as indicated in the specification, are useful for treating conditions mediated by the CRTh2 receptor, especially inflammatory or obstructive airways diseases.Type: ApplicationFiled: May 22, 2006Publication date: August 21, 2008Inventors: Jake Axford, Urs Baettig, Brian Cox, Kamlesh Jagdis Bala, Catherine Leblanc, David Andrew Sandham
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Publication number: 20080182888Abstract: The present invention relates to a novel crystalline form of zofenopril calcium of formula (I), chemically known as (4S)-1-[(2S)-3-(benzoylthio)-2-methylpropionyl]-4-(phenylthio)-L-proline calcium salt. The present invention further relates to a process for the preparation of the new crystalline form of zofenopril calcium and its use in pharmaceutical preparations.Type: ApplicationFiled: December 20, 2007Publication date: July 31, 2008Inventors: Vinayak G. Gore, Ashok D. Pehere, Avinash C. Gaikwad, Priyesh S. Vijaykar
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Publication number: 20080146818Abstract: Novel bicycloester derivatives and pharmaceutically acceptable salts thereof have high DPP-IV inhibitory activity. SOLVING MEANS The novel bicycloester derivatives are represented by the general formula (1): Pharmaceutically acceptable salts thereof are also included (Example: (2S,4S)-1-[[N-(4-ethoxycarbonylbicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile)).Type: ApplicationFiled: February 1, 2005Publication date: June 19, 2008Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Kohei Ohata, Kazuya Yokota, Koji Murakami, Toshiyuki Matsui
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Publication number: 20080145335Abstract: Embodiments of this invention include novel analogs of Glycyl-Prolyl-Glutamate (GPE) and compositions containing such analogs of GPE. Of these, certain analogs have modified proline residues. Other embodiments of this invention include uses of analogs of GPE to protect neural cells from degeneration and/or death in response to injury or disease. Disorders treatable with compounds and compositions of this invention include hypoxia/ischemia, toxic injury, and chronic neurodegenerative disorders including Parkinson's disease.Type: ApplicationFiled: November 20, 2007Publication date: June 19, 2008Applicant: Neuren Pharmaceuticals LimitedInventors: Margaret Anne Brimble, Paul William Richard Harris, Frank Sieg
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Patent number: 7375238Abstract: The present invention relates to a process for the preparation of a N-(N?-substituted glycyl)-2-cyanopyrrolidine comprising at least (a) reacting, in the presence of dimethylformamide, a compound of formula (V) ?wherein, independently of each other, X1 and X3 are halogen; X2 is halogen, OH, O—C(?O)—CH2X3, —O—SO2—(C1-8)alkyl or 13 O—SO2-(aryl), ?with L-prolinamide, followed by (b) reacting the resultant compound without isolation with a dehydration agent, optionally followed by (c) reacting, in the presence of a base, the resultant compound without isolation with an appropriate amine and (d) recovering the resultant compound in free form or in acid addition salt form.Type: GrantFiled: April 15, 2004Date of Patent: May 20, 2008Assignee: Novartis AGInventors: Frank Schaefer, Gottfried Sedelmeier
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Patent number: 7361663Abstract: This invention is directed to N-acylpyrrolidin-2-ylalkylbenzamidine derivatives which useful for inhibiting the activity of Factor Xa, by contacting said derivatives with a composition containing Factor Xa. The present invention is also directed to compositions containing said derivatives, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.Type: GrantFiled: October 16, 2003Date of Patent: April 22, 2008Assignee: Aventis Pharmaceuticals Inc.Inventors: Mark Czekaj, Scott I. Klein, Heinz W. Pauls
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Patent number: 7335677Abstract: Novel compounds that are inhibitors of one or most post-proline cleaving proteases, e.g. dipeptidyl peptidase IV, according to general formula (1). R1 is H or CN, X1 is O, S, CH2, CHF, CF2, CH(CH3), C(CH3)2 or CH(CN), and b is 1 or 2. G1 is H or a group according to the formula —CH2—X2—(CH2)a-G3 and G2 is H or a group according to the formula —CH2—(CH29a-G3, provided that one of G1 and G2 is H and the other is not H. X2 is O, S, or CH2, and a is 0, 1 or 2, provided that when a is 1 then X2 is CH2. G3 is a group according to one of general formulae 2-4, where the variables have meaning given in the description. The compounds are useful in the treatment of i.a.Type: GrantFiled: October 23, 2002Date of Patent: February 26, 2008Assignee: Ferring B.V.Inventors: David M. Evans, Doreen M. Ashworth
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Patent number: 7329762Abstract: The present invention relates to phosphate ester prodrugs of dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: June 8, 2004Date of Patent: February 12, 2008Assignee: Merck & Co., Inc.Inventors: Mark E. Fraley, Robert M. Garbaccio, George D. Hartman, William F. Hoffman
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Patent number: 7309714Abstract: The present invention is directed to phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: November 26, 2003Date of Patent: December 18, 2007Assignee: Merck & Co., Inc.Inventors: Joseph L. Duffy, Robert J. Mathvink, Ann E. Weber, Jinyou Xu
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Patent number: 7304166Abstract: A benzenesulfonate salt of (2S,4S)-2-cyano-4-fluoro-1-[(2-hydroxy-1,1-dimethyl)ethylamino]acetylpyrrolidine that has an excellent DPPIV inhibition activity as well as physical properties (e.g., stability) required for pharmaceutical preparations. The present invention allows easy obtaining of the compound in high-purity uniform crystal form with excellent solid-state stability.Type: GrantFiled: August 27, 2003Date of Patent: December 4, 2007Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Hiroshi Fukushima, Akira Hiratate, Masato Takahashi, Kazuya Kameo
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Patent number: 7241902Abstract: Compounds which are the reaction product of allicin and ACE-inhibiting compounds are useful in treating hypertension, elevated triglycerides, and elevated insulin.Type: GrantFiled: May 30, 2002Date of Patent: July 10, 2007Assignee: Yeda Research and Development Co. Ltd.Inventors: Talia Miron, Aharon Rabinkov, David Mirelman, Meir Wilchek
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Patent number: 7238683Abstract: The present invention is directed to fused phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-RV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: October 29, 2004Date of Patent: July 3, 2007Assignee: Merck & Co., Inc.Inventors: Wallace T. Ashton, Hong Dong, Jinyou Xu
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Patent number: 7199150Abstract: Amino alcohol compounds and phosphonic acid compounds having excellent immunosuppressive activity, pharmacologically acceptable salts thereof and pharmacologically acceptable esters thereof, and pharmaceutical compositions comprising such compounds, the compounds having the following formula: wherein R1 and R2 each represent hydrogen, or a protecting group of the amino group; R3 represents hydrogen, or a protecting group of the hydroxyl group; R4 represents a lower alkyl group; n is 1 to 6; X represents oxygen or nitrogen, which is unsubstituted or substituted with a lower alkyl group; Y represents ethylene; Z represents a C1–C10 alkylene; R5 represents an aryl group; and R6 and R7 each represents hydrogen; provided that when R5 represents hydrogen, then Z represents a group other than a single bond or a straight chain C1–C10 alkylene group.Type: GrantFiled: July 12, 2004Date of Patent: April 3, 2007Assignee: Sankyo Company, LimitedInventors: Takahide Nishi, Takaichi Shimozato, Futoshi Nara, Shojiro Miyazaki
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Patent number: 7196201Abstract: The present invention relates to novel compounds, their use for inhibiting serine proteases, such as dipeptidyl peptidases, such as dipeptidyl peptidase IV (DPP-IV) and to methods for their production and their therapeutic utilityType: GrantFiled: June 26, 2002Date of Patent: March 27, 2007Assignee: SmithKline Beecham CorporationInventors: Curt Dale Haffner, Darryl Lynn McDougald, Amarjit Sab Randhawa, Steven Michael Reister, David N Deaton
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Patent number: 7183290Abstract: The present invention relates to novel compounds, their use for inhibiting post prolin/analine-cleaving proteases, such as serine proteases, such as dipeptidyl peptidases, such as dipeptidyl peptidase IV (DPP-IV), and to methods for their production and their therapeutic utility.Type: GrantFiled: June 26, 2002Date of Patent: February 27, 2007Assignee: SmithKline Beecham CorporationInventors: Curt Dale Haffner, Darryl Lynn McDougald, James Martin Lenhard
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Patent number: 7179918Abstract: Compounds of the formula: where the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with the HIV virus. Intermediates and synthetic methods for preparing such compounds are also described.Type: GrantFiled: June 11, 2002Date of Patent: February 20, 2007Assignee: Agouron Pharmaceuticals, Inc.Inventors: Stacie S. Canan Koch, Therese N. Alexander, Benjamin J. Burke, Tanya M. Jewell, David J. Kucera, Maria Angelica Linton, Lennert J. Mitchell, Jr., Siegfried H. Reich, Donald J. Skalitzky, John H. Tatlock, Michael D. Varney, Scott C. Virgil, Stephen E. Webber, Stephen T. Worland, Mark Barvian, Gary Bolton, Frederick Earl Boyer, Jr., Jeffrey J. Machak, Tod Holler, Sean T. Murphy, Michael Melnick, Vara Prasad Josyula
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Patent number: 7169806Abstract: Compounds which are 1-(2?-aminoacyl)-2-cyanopyrrolidine derivatives according to general formula (1) are DP-IV inhibitors for treatment of impaired glucose tolerance or type 2 diabetes; wherein A is selected from groups (2, 3 and 4); X is selected from aminoacyl groups corresponding to the natural amino acids, acyl groups R3CO, groups R4COOC(R5)(R6)OCO, methoxycarbonyl, ethoxycarbonyl and benzyloxycarbonyl; R1 is selected from H, C1–C6alkyl residues, (CH2)aNHW1, (CH2)bCOW2, (CH2)cOW3, CH(Me)OW4, (CH2)d—C6H4—W5 and (CH2)eSW6, where a is 2–5, b is 1–4, c is 1–2, d is 1–2, e is 1–3, W1 is COW6, CO2W6 or SO2W6, W2 is OH, NH2, OW6 or NHW6, W3 is H or W6, W4 is H or W6, W5 is H, OH or OMe, and W6 is C1–C6 alkyl, optionally substituted phenyl, optionally substituted heteroaryl or benzyl and R2 is selected from H and (CH2)n—C5H3N—Y, where n is 2–4 and Y is H, F, Cl, NO2 or CN, or R1 and R2 together are —(CH2)p— where p is 3 or 4; R3 is selected from H, C1–C6 alkyl and phenyl; R4 is selected from H, C1–C6 alkyl, benzyType: GrantFiled: April 15, 2005Date of Patent: January 30, 2007Assignee: Ferring BVInventor: David Michael Evans
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Patent number: 7157454Abstract: The invention relates to compounds of formula: These compounds show affinity for the bradykinin receptors with selectivity towards the B1 receptors; they may be used for the preparation of medicinal products intended for treating or preventing inflammation pathologies and persistent or chronic inflammatory diseases.Type: GrantFiled: March 27, 2002Date of Patent: January 2, 2007Assignee: Sanofi-AventisInventors: Bernard Ferrari, Jean Gougat, Yvette Muneaux, Pierre Perreaut, Lionel Sarran
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Patent number: 7132539Abstract: The present invention relates to compounds which comprise a nitrogen-containing ring scaffold substituted by an R1 alkyl units selected from the group consisting of C1–C12 linear or branched alkyl, C3–C8 cyclic alkyl, C2–C12 linear or branched alkenyl, or haloalkyl, for example, the 2-keto-3-alkylpiperazines having the formula: wherein R is selected from the group consisting of phenyl, 3-fluorophenyl, 4-fluorophenyl, 3,5-difluorophenyl, and 4-chlorophenyl; R1 is selected from the group consisting of methyl, ethyl, propyl, iso-propyl, butyl, iso-butyl, sec-butyl, tert-butyl, cyclopropyl, cyclopropylmethyl, cyclopentyl, cyclopentylmethyl, cyclohexyl, cyclohexylmethyl, benzyl, allyl, 1-methylallyl, 2-methylallyl, but-2-enyl, and propargyll; R7a is selected from the group consisting of hydrogen, —CO2H, —CONH2, —CONHCH3, and —CON(CH3)2; R8 is benzyl, substituted benzyl, or naphthalen-2-ylmethyl.Type: GrantFiled: October 20, 2003Date of Patent: November 7, 2006Assignee: The Procter & Gamble CompanyInventors: Frank Hallock Ebetino, Xinrong Tian, Wieslaw Adam Mazur, Anny-Odile Colson
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Patent number: 7132443Abstract: The present invention relates to novel compounds, their use for inhibiting serine proteases, such as dipeptidyl peptidases, such as dipeptidyl peptidase IV (DPP-IV) and to methods for their production and their therapeutic utility.Type: GrantFiled: June 26, 2002Date of Patent: November 7, 2006Assignee: SmithKlineBeecham CorporationInventors: Curt Dale Haffner, Darryl Lynn McDougald, Amarjit Sab Randhawa, Steven Michael Reister, James Martin Lenhard
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Patent number: 7087759Abstract: Disclosed are MC-3/MC-4 receptor ligands, the ligands having the following formula: wherein A is a conformationally restricted ring system selected from the group consisting of: a) non-aromatic carbocyclic rings; b) aromatic carbocyclic rings; c) non-aromatic heterocyclic rings; d) aromatic heterocyclic rings; wherein said rings comprises from 5 to 8 atoms; and W is a unit which preferable comprises D-1-fluorophenyalanine, Y comprises a heteroatom, and Z comprises an aromatic carbocyclic ring. Also disclosed are pharmaceutical compositions comprising the ligands of the invention as well as methods of treating diseases mediated through MC-3/MC-4 receptors.Type: GrantFiled: May 28, 2004Date of Patent: August 8, 2006Assignee: The Procter & Gamble CompanyInventors: Wieslaw Adam Mazur, Xinrong Tian, Xiufeng Eric Hu, Frank Hallock Ebetino
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Patent number: 7045532Abstract: ACE-2 inhibitors for the treatment of body weight and related disorders are disclosed. ACE-2 inhibitors include peptides and small molecules. Examples of small molecule ACE-2 inhibitors include compounds of formula (I): Z-???(I) Wherein Z is a zinc coordinating moiety and ? is an amino-acid mimicking moiety, and pharmaceutically acceptabale salts thereof. Methods of using the inhibitors and pharmaceutical compositions containing the inhibitors to treat a body weight disorder, to decrease appetite, to increase muscle mass, to decrease body fat, to treat diabetes and to treat a state associated with altered lipid metabolism, are also described.Type: GrantFiled: October 31, 2001Date of Patent: May 16, 2006Assignee: Millennium Pharmaceuticals, Inc.Inventors: Susan L. Acton, Timothy D. Ocain, Alexandra E. Gould, Natalie A. Dales, Bing Guan, James A. Brown, Michael Patane, Vivek J. Kadambi, Michael Solomon, Alain Stricker-Krongrad
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Patent number: 7041831Abstract: Disclosed is a method of preparing a composition comprising a compound represented Structural Formula (I): The method comprises the step of reacting an aldehyde compound R10CHO with an isonitrile compound represented by Structural Formula (II):Type: GrantFiled: November 23, 2004Date of Patent: May 9, 2006Assignee: Genzyme CorporationInventor: Bradford H. Hirth
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Patent number: 7026316Abstract: The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: March 22, 2002Date of Patent: April 11, 2006Assignee: Merck & Co., Inc.Inventors: Wallace T. Ashton, Charles G. Caldwell, Hyun O. Ok, Emma R. Parmee, Ann E. Weber
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Patent number: 6987123Abstract: The present invention relates to compounds of the general formula (I), there derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates, wherein all variables are as defined in the specification.Type: GrantFiled: August 10, 2001Date of Patent: January 17, 2006Assignee: Cadila Healthcare LimitedInventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Vijay Kumar Gajubhai Barot
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Patent number: 6943269Abstract: The present invention provides basic ionic contrast agents that have anticoagulant activity. The contrast media incorporate a lysine or arginine group or derivative, and have a free amino or guanidino group. Methods of using the contrast media are also disclosed.Type: GrantFiled: June 20, 2003Date of Patent: September 13, 2005Assignee: University of North Carolina - Chapel HillInventors: Don A. Gabriel, Laura J. Melton
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Patent number: 6911467Abstract: Compounds which are 1-(2?-aminoacyl)-2-cyanopyrrolidine derivatives according to general formula (1) are DP-IV inhibitors for treatment of impaired glucose tolerance or type 2 diabetes; wherein A is selected from groups (2, 3 and 4); X is selected from aminoacyl groups corresponding to the natural amino acids, acyl groups R3CO, groups R4COOC(R5)(R6)OCO, methoxycarbonyl, ethoxycarbonyl and benzyloxycarbonyl; R1 is selected from H, C1-C6 alkyl residues, (CH2)aNHW1, (CH2)bCOW2, (CH2)cOW3, CH(Me)OW4, (CH2)d—C6H4—W5 and (CH2)eSW6, where a is 2-5, b is 1-4, c is 1-2, d is 1-2, e is 1-3, W1 is COW6, CO2W6 or SO2W6, W2 is OH, NH2, OW6 or NHW6, W3 is H or W6, W4 is H or W6, W5 is H, OH or OMe, and W6 is C1-C6 alkyl, optionally substituted phenyl, optionally substituted heteroaryl or benzyl and R2 is selected from H and (CH2)n—C5H3N—Y, where n is 2-4 and Y is H, F, Cl, NO2 or CN, or R1 and R2 together are —(CH2)p— where p is 3 or 4; R3 is selected from H, C1-C6 alkyl and phenyl; R4 is selected from H, C1-C6 alkyl, benzType: GrantFiled: November 30, 2000Date of Patent: June 28, 2005Assignee: Ferring BVInventor: David Michael Evans
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Patent number: 6887866Abstract: The invention provides compounds compositions and methods useful for inducing or maintaining general anesthesia or sedation in mammals.Type: GrantFiled: January 24, 2003Date of Patent: May 3, 2005Assignee: Theravance, Inc.Inventors: Thomas E. Jenkins, Sabine Axt, Jennifer Bolton
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Patent number: 6867310Abstract: The present invention provides transition-metal-catalyst-based methods for the arylation and vinylation of activated methyl, methylene, and methine carbons with aryl halides, vinyl halides, and the like. The methods of the invention provide several improvements over existing methods, including the ability to synthesize efficiently and under mild conditions ?-aryl and ?-vinyl products from a wide range of starting materials, including ketones, esters, hydrazones, and imines. Furthermore, the methods of the invention may be used in an asymmetric sense, i.e. to produce enantiomerically-enriched chiral ?-aryl and ?-vinyl products.Type: GrantFiled: January 27, 1999Date of Patent: March 15, 2005Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, John P. Wolfe, Jens Ahman, Malisa Troutman, Michael Palucki, Ken Kamikawa, Andre Chieffi
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Patent number: 6855706Abstract: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to ? 4 integrin. They are used as therapeutic agents for various diseases concerning ? 4 integrin.Type: GrantFiled: May 20, 2002Date of Patent: February 15, 2005Assignee: Ajinomoto Co., Inc.Inventors: Yasuhiro Tanaka, Toshihiko Yoshimura, Hiroyuki Izawa, Chieko Ejima, Mitsuhiko Kojima, Yuko Satake, Eiji Nakanishi, Nobuyasu Suzuki, Shingo Makino, Manabu Suzuki, Masahiro Murata
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Patent number: 6812350Abstract: The present invention relates to a method of making novel dipeptidyl peptidase-IV (“DPP-IV’) inhibitor compounds useful for treating, inter alia, diseases that are associated with proteins that are subject to processing by DPP-IV, such as Type 2 diabetes mellitus, metabolic syndrome (Syndrome X or insulin resistance syndrome), hyperglycemia, impaired glucose tolerance, glucosuria, metabolic acidosis, cataracts, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic cardiomyopathy, Type 1 diabetes, obesity, hypertension, hyperlipidemia, atherosclerosis, osteoporosis, osteopenia, frailty, bone loss, bone fracture, acute coronary syndrome, infertility due to polycystic ovary syndrome, short bowel syndrome and to prevent disease progression in Type 2 diabetes. The invention also relates to a method of making 3,3,4,4-tetrafluoropyrrolidine, a starting material utilized in the afore-mentioned method for preparing DPP-IV compounds.Type: GrantFiled: June 3, 2003Date of Patent: November 2, 2004Assignee: Pfizer Inc.Inventor: Bernard Hulin
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Patent number: RE38947Abstract: A chiral catalyst is disclosed together with methods of using it for enantioselective syntheses. The chiral catalyst includes a nucleus with two metal atoms that has four bridging ligands oriented radially to the axis of the nucleus. Each of these ligands includes a two complexing atoms each complexed to one of the metal atoms. At least one of the bridging ligands includes a chiral center which is bonded to one of the complexing atoms. Preferably, all four of the bridging ligands include a chiral center bonded to one of the complexing atoms. The catalyst of the invention has been found to be useful in catalyzing carbenoid transformation reactions such as cyclopropanation.Type: GrantFiled: February 14, 1996Date of Patent: January 24, 2006Assignee: Research Corporation Technologies, Inc.Inventor: Michael P. Doyle