1,3-diazole Ring (including Hydrogenated) Patents (Class 544/370)
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Patent number: 7091219Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.Type: GrantFiled: April 17, 2003Date of Patent: August 15, 2006Assignee: G. D. Searle & Co.Inventors: John N. Freskos, Daniel P. Getman, John J. Talley, James A. Sikorski
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Patent number: 7067513Abstract: The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as aggression, anxiety disorders, autism, vertigo, depression, disturbances of cognition, disturbances of memory, Parkinson's disease, schizophrenia, and psychotic disorders. The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0–2; R5 and R6 are independently H or alkyl (1–3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3–5, and R7 is alkyl (1–3C), alkoxy (1–3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2–4, and salts thereof.Type: GrantFiled: August 22, 2000Date of Patent: June 27, 2006Assignee: Solvay Pharmaceuticals B.V.Inventors: Roelof Van Hes, Johannes A. M. Van der Heijden, Cornelis G Kruse, Jacobus Tipker, Martinus T. M Tulp, Gerben M Visser, Bernard J Van Vliet
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Patent number: 7056918Abstract: The present invention relates to novel triazolo-pyridines of the formula I wherein Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from nitrogen, sulfur and oxygen wherein at least one of said heteroatoms atoms must be nitrogen; R2 is selected from the group consisting of hydrogen, (C1–C6)alkyl or other suitable substituents; R3 is selected from the group consisting of hydrogen, (C1–C6)alkyl or other suitable substituents; s is an integer from 0–5; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.Type: GrantFiled: March 11, 2002Date of Patent: June 6, 2006Assignee: Pfizer, Inc.Inventors: Mark A. Dombroski, Michael A. Letavic, Kim F. McClure
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Patent number: 7057042Abstract: The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction, wherein A, L, D and B1 are as described in the specification.Type: GrantFiled: May 23, 2003Date of Patent: June 6, 2006Assignee: Abbott LaboratoriesInventors: Marlon D. Cowart, Steven P. Latshaw, Sherry L. Nelson, Andrew O. Stewart
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Patent number: 7045625Abstract: An asymmetric synthesis of diarylmethylpiperazines is described. The synthetic route enables preparation of a variety of enatiomerically pure amines with different N-alkyl groups. The invention includes an asymmetric addition of organometallic compounds to chiral sulfinimine to give adducts in predominantly one diastereomer can subsequently be transferred into pure enantiomers of by cleavage of the chiral auxilliary which is followed by synthesis of the piperazine ring by alkylation procedures.Type: GrantFiled: March 5, 2002Date of Patent: May 16, 2006Assignee: AstraZeneca ABInventors: William Brown, Niklas Plobeck
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Patent number: 7034029Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptorType: GrantFiled: January 16, 2004Date of Patent: April 25, 2006Assignee: WyethInventors: Michael Gerard Kelly, Derek Cecil Cole
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Patent number: 7030113Abstract: The present invention discloses compounds of formula I wherein Ar, Z, m, n, p, R1 and R8 are herein defined, said compounds being novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: GrantFiled: September 30, 2004Date of Patent: April 18, 2006Assignee: Schering CorporationInventors: Thavalakulamgara K. Sasikumar, Duane A. Burnett
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Patent number: 7030150Abstract: The present invention relates to novel benzimidazole compounds that have useful antiviral activity. More specifically, the invention encompasses benzimidazole compounds that inhibit membrane fusion associated events such as viral transmission, reduce viral load or otherwise treat viral infections. The invention also encompasses the use of benzimidazole compounds as inhibitors of membrane fusion associated events, such as viral transmission. In another embodiment, the invention encompasses processes for making benzimidazole compounds, methods of using the benzimidazole compounds and compositions comprising the benzimidazole compounds. Finally, the invention provides methods for treating, preventing or ameliorating symptoms associated with respiratory infection, particularly that caused by Respiratory Syncytial Virus utilizing the novel benzimidazole compounds of the invention.Type: GrantFiled: May 9, 2002Date of Patent: April 18, 2006Assignee: Trimeris, Inc.Inventors: John William Lackey, Daniel S Kinder, Nicolai A Tvermoes
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Patent number: 7026314Abstract: Provided herein is a compound of the formula (I) wherein said compound is useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating, disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT1B antagonists. Also provided herein are processes for making compounds of Formula (I) and intermediate compounds.Type: GrantFiled: January 15, 2002Date of Patent: April 11, 2006Assignee: AstraZeneca ABInventors: Marc Chapdelaine, Timothy Davenport, Markus Haeberlein, Carey Horchler, John McCauley, Edward Pierson, Daniel Sohn
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Patent number: 6984642Abstract: The present invention relates to substituted phenylcyclohexanecaboxamides of the formula (I), to processes for their preparation and to their use in medicaments, in particular for treating cardiovascular disorders.Type: GrantFiled: May 16, 2000Date of Patent: January 10, 2006Assignee: Bayer AktiengesellschaftInventors: Erwin Bischoff, Stephan Lensky, Stephan-Nicholas Müller, Holger Paulsen, Jörg Keldenich, Thomas Krahn, Joachim Schuhmacher, Jan Jänichen, Wolfgang Thielemann, Henning Steinhagen
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Patent number: 6982264Abstract: The invention relates to substituted alcohol compounds of the formula (I): wherein X, R1, R2, R3, RN, R20 and RC are defined herein. The compounds are useful in the treatment or prevention of Alzheimer's disease and more specifically to compounds that are capable of inhibiting beta-secretase, an enzyme that cleaves amyloid precursor protein to produce amyloid beta peptide (A-beta), a major component of the amyloid plaques found in the brains of Alzheimer's sufferers.Type: GrantFiled: June 27, 2002Date of Patent: January 3, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Varghese John, Roy Hom, John Tucker
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Patent number: 6972289Abstract: The present invention relates to a cell division inhibitor comprising various dehydrodiketopiperazines such as dehydrophenylahistin, or analogs thereof as an active ingredient, and a dehydrogenase and a method for producing the same inhibitor.Type: GrantFiled: September 29, 2000Date of Patent: December 6, 2005Assignee: Nereus Pharmaceuticals, Inc.Inventors: Hiroshi Kanzaki, Kaneo Kanoh, Satohiro Yanagisawa, Teruhiko Nitoda, Kazumi Akazawa
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Patent number: 6969711Abstract: The present invention offers novel cyclic diamine compounds and a pharmaceutical composition containing the same. The present invention relates to a compound represented by the formula (I) or salt(s) or solvate(s) thereof. (In the formula, is an optionally substituted divalent residue of benzene, pyridine, cyclohexane or naphthalene or is a vinylene group where Ar is an optionally substituted aryl group; X is —NH—, oxygen atom or sulfur atom; Y is —NR1—, oxygen atom, sulfur atom, sulfoxide or sulfone; Z is a single bond or —NR2—; R1 is hydrogen atom, optionally substituted lower alkyl group, optionally substituted aryl group or optionally substituted silyl lower alkyl group; R2 is hydrogen atom, optionally substituted lower alkyl group, optionally substituted aryl group or optionally substituted silyl lower alkyl group; l is an integer of from 0 to 15; m is an integer of 2 or 3; and n is an integer of from 0 to 3).Type: GrantFiled: February 20, 2003Date of Patent: November 29, 2005Assignee: Kowa Company, Ltd.Inventors: Kimiyuki Shibuya, Katsumi Kawamine, Yukihiro Sato, Toru Miura, Chiyoka Ozaki, Toshiyuki Edano, Mitsuteru Hirata, Tadaaki Ohgiya
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Patent number: 6969713Abstract: The invention provides piperidine and piperazine derivatives of general formula (I), processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapyType: GrantFiled: December 18, 2000Date of Patent: November 29, 2005Assignee: AstraZeneca ABInventors: Premji Meghani, Colin Bennion
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Patent number: 6960582Abstract: Compounds having the general structure II are provided: A is selected from the group consisting of C or CH and X and Y are independently selected from the group consisting of CH2, N, C?O, C?S, (CR6R7)n, S?O, SO2, O, NR9, S, C(?O)—(CR6R7)n, and C(?S)—(CR6R7)n where n is 1, 2, or 3. W is selected from the group consisting of and Z1, Z2, and Z3 are independently selected from the group consisting of substituted carbon and nitrogen. L is selected from the group consisting of N, O, S, S?O, SO2, C(O), NC(O), NC(S), OC(O), OC(S), C(NR10), C(NOR10), and a covalent bond. Compounds of formula II are agonists of the melanocortin-4 receptor (“MC4-R”) and therefore may have useful properties for controlling diseases related to MC4-R action in humans, such as obesity and type II diabetes.Type: GrantFiled: April 30, 2003Date of Patent: November 1, 2005Assignee: Chiron CorporationInventors: Rustum Boyce, David Duhl
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Patent number: 6936611Abstract: Compounds of formula (I) in which R2, X, Y, Cy, L and Lp(D)n have the meanings given in the specification, are inhibitors of the serine protease, Factor Xa and are useful in the treatment of cardiovascular disorders.Type: GrantFiled: January 12, 2004Date of Patent: August 30, 2005Assignee: Eli Lilly and CompanyInventors: John Walter Liebeschuetz, Christopher William Murray, Stephen Clinton Young, Nicholas Paul Camp, Stuart Donald Jones, William Alexander Wylie, John Joseph Masters, Michael Robert Wiley, Scott Martin Sheehan, David Birenbaum Engel, Brian Morgan Watson, Peter Robert Guzzo, Michael John Mayer
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Patent number: 6936613Abstract: The present invention relates to novel benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for inducing and maintaining anesthesia, sedation and muscle relaxation, as well as for combating febrile convulsions in children. The compounds of the invention may also be used by veterinarians.Type: GrantFiled: July 15, 2003Date of Patent: August 30, 2005Assignee: Neurosearch A/SInventors: Lene Teuber, Frank Watjen
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Patent number: 6921760Abstract: The present invention relates to compounds of the formula Orosco wherein R1, R2, R3, X, Y and the dashed line are defined as in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. These compounds are useful as psychotherapeutic agents.Type: GrantFiled: November 6, 2001Date of Patent: July 26, 2005Assignee: Pfizer Inc.Inventor: Harry Ralph Howard
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Patent number: 6916813Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts thereof, are useful for modulating mitochondrial F1F0 ATPase activity and treating ischemic conditions including myocardial infarction, congestive heart failure, and cardiac arrhythmias.Type: GrantFiled: December 10, 2002Date of Patent: July 12, 2005Assignee: Bristol-Myers Squibb Co.Inventors: Karnail S. Atwal, Gary J. Grover, Charles Z. Ding, Philip D. Stein, John Lloyd, Saleem Ahmad, Lawrnce G. Hamann, David Green, Francis N. Ferrara
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Patent number: 6916812Abstract: Novel piperazine and homopiperazine derivatives are agonists of melanocortin receptor(s) and are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of the melanocortin receptors. The compounds of the present invention are therefore useful for treatment or prevention of diseases and disorders such as obesity, diabetes, and sexual dysfunction.Type: GrantFiled: October 4, 2002Date of Patent: July 12, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Graham S. Poindexter, Guanglin Luo, Ling Chen
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Patent number: 6908922Abstract: Compound of formula (I): wherein: V represents a single bond or an alkylene chain, M represents a single bond or an alkylene chain, A and E each represents nitrogen or CH, but at least one of the two groups A or E represents nitrogen, W represents a group of formula (i), (ii) or (iii): Medicinal products containing the same which are useful in the treatment of diseases or pathological conditions ins which endothelial dysfunction is known.Type: GrantFiled: November 12, 2002Date of Patent: June 21, 2005Assignee: Les Laboratoires ServierInventors: Jean-Louis Peglion, Christophe Poitevin, Jean-Paul Vilaine, Nicole Villeneuve, Marie-Pierre Bourguignon, Catherine Thollon
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Patent number: 6906075Abstract: Melanin concentrating hormone receptor ligands (especially substituted benzoimidazole analogues), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).Type: GrantFiled: January 9, 2003Date of Patent: June 14, 2005Assignee: Neurogen Corp.Inventors: Robert W. DeSimone, Cheryl Steenstra, Linda Gustavson, Rajagopal Bakthavatchalam, Alan Hutchison
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Patent number: 6906090Abstract: The invention provides the use of certain isatin and oxindole derivatives in the preparation of a medicament for use in the treatment of mycobacterial disease.Type: GrantFiled: March 4, 1999Date of Patent: June 14, 2005Assignee: AstraZeneca ABInventor: Ramachandran Janakiraman
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Patent number: 6900206Abstract: This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with sulfonylureido piperazine derivatives of Formula I. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS. wherein: Z is Q is selected from the group consisting of: —W— is — represents a carbon-carbon bond or does not exist; and A is NR13R14.Type: GrantFiled: June 9, 2003Date of Patent: May 31, 2005Assignee: Bristol-Myers Squibb CompanyInventors: John F. Kadow, Alicia Regueiro-Ren, Qiufen May Xue
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Patent number: 6894041Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; —G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems recitType: GrantFiled: November 20, 2002Date of Patent: May 17, 2005Assignee: Pfizer IncInventors: Anthony Marfat, Michael William McKechney
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Patent number: 6884803Abstract: Disclosed are substituted phenylalkynes of formula (I), wherein R1, R2, R3, R4, R5 and n are as defined, compositions containing them, and methods of making and using them to treat histamine-mediated conditions.Type: GrantFiled: December 2, 2002Date of Patent: April 26, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Richard Apodaca, Wei Xiao, Jill A. Jablonowski
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Patent number: 6869945Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N?(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; -G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems reType: GrantFiled: November 20, 2002Date of Patent: March 22, 2005Assignee: Pfizer IncInventors: Anthony Marfat, Michael William McKechney
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Patent number: 6864260Abstract: The invention is directed to methods to inhibit p38-? kinase using compounds which contain a phenyl group linked through a piperazine ring to a substituted indole.Type: GrantFiled: May 28, 2002Date of Patent: March 8, 2005Assignee: Scios, Inc.Inventors: Babu J. Mavunkel, Sarvajit Chakravarty, John J. Perumattam, Sundeep Dugar, Qing Lu, Xi Liang
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Patent number: 6861434Abstract: Compounds of the formula: useful for treatment of disorders of the dopaminergic system, such as schizophrenia, schizoaffective disorder, bipolar disorder, Parkinson's disease, L-DOPA induced pychoses and dyskinesias, Tourette's syndrome and hyperprolactinemia and in the treatment of drug addiction such as the addiction to ethanol, nicotine or cocaine and related illnesses.Type: GrantFiled: April 23, 2002Date of Patent: March 1, 2005Assignee: WyethInventor: Gary P. Stack
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Patent number: 6861432Abstract: This invention relates to new piperazine derivatives of general formula I, in which V, W, n, R, R?, i, j, Y and Z have the meaning that is indicated in the description. The compounds according to the invention are distinguished by a diazacycloalkane substituent. They have at their disposal a special action with respect to the action that destabilizes the androgen receptor and can be used, for example, for treating prostrate cancer.Type: GrantFiled: November 22, 2002Date of Patent: March 1, 2005Assignee: Schering AktiengesellschaftInventors: Arwed Cleve, Christoph Huwe, Volker Schulze, Helmut Morack, Dieter Zopf, Jens Hoffmann, Andreas Reichel
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Patent number: 6855713Abstract: The invention concerns benzimidazole derivatives of the general formula (I) in which the radicals R1, R2, R3, X1 and A can have the meanings assigned to them in the specification, their prodrugs, processes for their production as well as the use of the benzimidazole derivatives as medicines, especially as medicines that have trypsin-inhibiting action.Type: GrantFiled: September 9, 2002Date of Patent: February 15, 2005Assignee: Boehringer Ingelheim Pharma KGInventors: Pascale Pouzet, Christoph Hoenke, Claudia Heine, Ralf Anderskewitz, Horst Dollinger, Herbert Nar, Hans Michael Jennewein, Bernd Disse
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Patent number: 6855714Abstract: The invention relates to novel benzimidazole derivatives with general formula I, whereby radicals R1, R2, R3, A, B and Y have the meanings that are indicated in the description and the claims, the use of these compounds for the production of a pharmaceutical agent for treating and for preventing diseases that are associated with microglia activation, as well as pharmaceutical preparations that contain these compounds.Type: GrantFiled: July 5, 2002Date of Patent: February 15, 2005Assignee: Schering AktiengesellschaftInventors: Thorsten Blume, Wolfgang Halfbrodt, Joachim Kuhnke, Ursula Moenning, Herbert Schneider, Bernd Elger
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Patent number: 6852718Abstract: A class of phenylsulphonyl derivatives wherein the sulphonyl moiety is also attached to an N-arylalkyl-substituted piperazine ring are selective antagonists of the human 5-HT2A receptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse conditions of the central nervous system, including schizophrenia and other psychotic disorders.Type: GrantFiled: March 30, 2001Date of Patent: February 8, 2005Assignee: Merck Sharp & Dohme LtdInventors: Frank Burkamp, Susan Koon-Fung Cheng, Stephen Robert Fletcher
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Patent number: 6838461Abstract: Compounds of the formula I in which R1, R2, R4 and R5 have the meanings indicated in claim 1, are potent 5-HT2A antagonists and are suitable for the treatment of psychoses, schizophrenia, depression, neurological disorders, memory disorders, Parkingson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, eating disorders such as bulimia, nervous anorexia, premenstrual syndrome and/or for positively affecting compulsive behavior (obsessive-compulsive disorder, OCD).Type: GrantFiled: July 7, 2000Date of Patent: January 4, 2005Assignee: Merck Patent GmbHInventors: Henning Boettcher, Christoph Seyfried
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Publication number: 20040267017Abstract: The invention provides novel thiazoles bearing 3-pyridyl or 4-isoquinilinyl substituents, and pharmaceutical compositions thereof. The invention also provides methods of using compounds of the invention and pharmaceutical compositions thereof as inhibitors of lyases, e.g., the 17a-hydroxylase-C17,20 enzyme. The invention further provides methods for treating cancer in a subject, comprising administering to the subject a compound of the invention or a pharmaceutical composition thereof. The cancer can be, e.g., prostate cancer or breast cancer.Type: ApplicationFiled: March 26, 2004Publication date: December 30, 2004Inventors: Donald E Bierer, Jeffrey Johnson, Gaetan Ladouceur, William J Scott, Andrea C McClure, Wenlang Fu, Furahi Achebe, Michael Burke, Chen Bi, Barry P Hart
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Publication number: 20040266759Abstract: The invention relates to heterocyclic derivatives of formula (I), or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect.Type: ApplicationFiled: April 6, 2004Publication date: December 30, 2004Applicant: AstraZeneca ABInventors: Peter W.R. Caulkett, Roger James, Stuart E. Pearson, Anthony M. Slater, Rolf P. Walker
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Publication number: 20040259884Abstract: The present invention provides compounds according to formula I 1Type: ApplicationFiled: June 14, 2004Publication date: December 23, 2004Inventors: Gregory Jay Haley, Norman Kong, Emily Aijun Liu, Klaus B. Simonsen, Binh Thanh Vu, Stephen Evan Webber
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Publication number: 20040259867Abstract: The present invention provides compounds according to formula I and pharmaceutically acceptable salts and esters thereof, having the designations provided herein and which inhibit the interaction of MDM2 protein with a p53-like peptide and have antiproliferative activity.Type: ApplicationFiled: June 15, 2004Publication date: December 23, 2004Inventors: Nader Fotouhi, Emily Aijun Liu, Binh Thanh Vu
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Publication number: 20040254179Abstract: The present invention relates to imidazole derivatives of the general formula 1Type: ApplicationFiled: June 12, 2004Publication date: December 16, 2004Inventors: Bernd Buettelmann, Simona Maria Ceccarelli, Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira
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Publication number: 20040254180Abstract: The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, isoxazolidine compounds which have been designed to include esters within the structure of the compounds are provided. This invention is also drawn to methods of treating disorders, such as diabetes, comprising the administration of therapeutically effective compositions comprising compounds which have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the isoxazolidine compounds are also taught.Type: ApplicationFiled: June 15, 2004Publication date: December 16, 2004Applicant: ARYx TherapeuticsInventors: Pascal Druzgala, Peter G. Milner
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Patent number: 6821967Abstract: The present invention relates to substituted piperazine derivatives of general formula wherein Ra, Rb, Rc, Rf, Rg, X, m and n are defined as in claim 1, the isomers and salts thereof, particularly the physiologically acceptable salts thereof, which are valuable inhibitors of the microsomal triglyceride-transfer protein (MTP), medicaments containing these compounds and their use, as well as the preparation thereof.Type: GrantFiled: October 9, 2002Date of Patent: November 23, 2004Assignee: Boehringer Ingelheim Pharma KGInventors: Thorsten Lehmann-Lintz, Armin Heckel, Leo Thomas, Michael Mark
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Patent number: 6818662Abstract: The present invention provides a pharmaceutical composition comprising N-(3-chloro-4-morpholin-4-yl)phenyl-N′-hydroxyimidoformamidine and sulfobutyl ether &bgr;-cyclodextrin or a salt thereof, wherein sulfobutyl ether &bgr;-cyclodextrin increases the solubility of N-(3-chloro-4-morpholin-4-yl)phenyl-N′-hydroxyimidoformamidine and improves the photostability.Type: GrantFiled: August 14, 2002Date of Patent: November 16, 2004Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Shusei Ito, Akio Miwa, Mari Nakano
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Publication number: 20040220402Abstract: Compounds of Formula 1 1Type: ApplicationFiled: May 14, 2003Publication date: November 4, 2004Inventors: Ken Chow, Todd Heidelbaugh, Daniel Gil, Michael Garst, Larry A. Wheeler, Phong X. Nguyen, Dario G. Gomez
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Publication number: 20040214816Abstract: This invention relates to substituted imidazoles of Formula I 1Type: ApplicationFiled: October 17, 2001Publication date: October 28, 2004Inventors: Scott Beers, Michael P. Wachter
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Publication number: 20040209874Abstract: The present application describes novel hydantoin derivatives of formula (I): 1Type: ApplicationFiled: May 12, 2004Publication date: October 21, 2004Inventors: James E. Sheppeck, Jingwu Duan, Chu-Biao Xue, Zelda Wasserman
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Publication number: 20040204410Abstract: The present invention provides compounds according to formula I and formula II and pharmaceutically acceptable salts and esters thereof, having the designations provided herein and which inhibit the interaction of MDM2 protein with a p53-like peptide and have antiproliferative activity.Type: ApplicationFiled: April 28, 2004Publication date: October 14, 2004Inventors: Norman Kong, Emily Aijun Liu, Binh Thanh Vu
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Patent number: 6803368Abstract: Compounds of the formula useful for treatment of disorders of the dopaminergic system, such as schizophrenia, schizoaffective disorder, bipolar disorder, Parkinson's disease, L-DOPA induced pychoses and dyskinesias, Tourette's syndrome and hyperprolactinemia and in the treatment of drug addiction such as the addiction to ethanol, nicotine or cocaine and related illnesses.Type: GrantFiled: April 23, 2002Date of Patent: October 12, 2004Assignee: WyethInventors: Gary P. Stack, James A. Nelson
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Patent number: 6800636Abstract: Disclosed are compounds of the formula: wherein R8 represents a cyclic moiety to which is bound an imodazolylalkyl group; R9 represents a carbamate, urea, amide or sulfonamide group; and the remaining substituents are as defined herein. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.Type: GrantFiled: December 20, 2001Date of Patent: October 5, 2004Assignee: Schering CorporationInventors: Timothy Guzi, Dinanath F. Rane, Alan K. Mallams, Alan B. Cooper, Ronald J. Doll, Viyyoor M. Girijavallabhan, Arthur G. Taveras, Corey Strickland, Joseph M. Kelly, Jianping Chao
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Patent number: 6797824Abstract: Disclosed are compounds of the formula: wherein R1 represents optionally substituted aryl, heteroaryl, arylalkyl, or cycloalkyl groups; X, Z, and Y are optionally substituted nitrogen or carbon atoms; R3 and R4 are organic or inorganic substitutents which may together form ring structutes; m is zero, one or two; and R5 and R6 are are organic or inorganic substituents; and the pharmaceutically acceptable addition salts thereof, which compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.Type: GrantFiled: March 18, 2002Date of Patent: September 28, 2004Assignee: Neurogen CorporationInventors: Andrew Thurkauf, Raymond F. Horvath, Jun Yuan, John M. Peterson
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Publication number: 20040180887Abstract: This invention relates to N-aroyl cyclic amine derivatives of formula (1), wherein X represents a bond, oxygen, NR3 or a group (CH2), wherein n represents 1, 2 or 3; Y represents CH2, CO, CH(OH), or CH2CH(OH); Het is an optionally substituted bicyclic heteroaryl group containing up to 4 heteroatoms selected from N, O and S; Ar2 represents an optionally substituted phenyl or a 5- or 6-membered heterocyclyl group containing up to 3 heteroatoms selected from N, O and S and their use as pharmaceuticals, specifically as orexin receptor antagonists.Type: ApplicationFiled: April 26, 2004Publication date: September 16, 2004Inventors: Clive Leslie Branch, Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, David John Nash, Riccardo Novelli, Jean-Pierre Pilleux, Roderick Porter, Rachel Elizabeth Anne Stead, Geoffrey Stemp