1,3,4-thiadiazoles (including Hydrogenated) Patents (Class 514/363)
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Patent number: 7425636Abstract: (wherein R1 and R4 are the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkynyl, substituted or unsubstituted lower alkenyl, or the like; R5 represents a substituted or unsubstituted heterocyclic group, substituted or unsubstituted aryl, or the like; R2 represents —C(?W)R6 or the like; R3 represents a hydrogen atom, —C(?WA)R6A, or the like) Antitumor agents which comprises a thiadiazoline derivative represented by the aforementioned general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient are provided.Type: GrantFiled: December 11, 2002Date of Patent: September 16, 2008Assignees: Kyowa Hakko Kogyo Co., Ltd., Fuji Photo Film Co., Ltd.Inventors: Chikara Murakata, Kazuhiko Kato, Yoshihisa Ohta, Ryuichiro Nakai, Yoshinori Yamashita, Takeshi Takahashi
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Publication number: 20080214547Abstract: This invention describes a series of methods and compositions for prevention and treatment of diseases such as cancer. One aspect of the invention describes small molecule-based drugs that can be used to bind to death receptors TRAIL-R1/DR4 and/or TRAIL-R2/DR5 and induce apoptosis in cancer cells, while sparing normal cells. The invention also describes TRAIL Death Receptor Agonists/Activators (DRAs) and their uses, such as the induction of apoptosis through caspase-8 and caspase-3 activation. The present invention also describes the methods of treating cancers, such as breast, prostate, colon, pancreatic, ovarian, lung, and brain cancers, leukemia, lymphoma, multiple myeloma, and mesothelioma, using DRAs either as single-agent treatments, or in combination with other therapies.Type: ApplicationFiled: October 2, 2007Publication date: September 4, 2008Inventors: Rakesh K. Srivastava, Sharmila Shankar
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Publication number: 20080207636Abstract: The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R1, R2, R3, n and m are as described in the specification, in the preparation of a medicament for the treatment or prevention of a disease condition mediated through glucokinase (GLK), such as type 2 diabetes. The invention also relates to a novel group of compounds of Formula (I) and to methods for preparing compounds of Formula (I).Type: ApplicationFiled: February 1, 2008Publication date: August 28, 2008Applicant: AstraZeneca ABInventors: Scott Boyd, Peter William Rodney Caulkett, Rodney Brian Hargreaves, Suzanne Saxon Bowker, Roger James, Clifford David Jones, Darren McKerrecher, Michael Howard Block, Craig Johnstone
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Publication number: 20080207706Abstract: (wherein R1 and R4 are the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkynyl, substituted or unsubstituted lower alkenyl, or the like; R5 represents a substituted or unsubstituted heterocyclic group, substituted or unsubstituted aryl, or the like; R2 represents —C(?W)R6 or the like; R3 represents a hydrogen atom, —C(?WA)R6A, or the like) Antitumor agents which comprises a thiadiazoline derivative represented by the aforementioned general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient are provided.Type: ApplicationFiled: April 7, 2008Publication date: August 28, 2008Applicants: Kyowa Hakko Kogyo Co., Ltd, Fuji Photo Film Co., Ltd.Inventors: Chikara MURAKATA, Kazuhiko Kato, Yoshihisa Ohta, Ryuichiro Nakai, Yoshinori Yamashita, Takeshi Takahashi, Tomohisa Nakano, Yoji Ino
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Publication number: 20080207705Abstract: A novel heteroaryl-imidazole compound of formula (I) or a pharmaceutically acceptable salt thereof is effective as a cannabinoid CB1 receptor inverse agonist or antagonist, which is useful for preventing or treating obesity and obesity-related metabolic disorders. The present invention also provides a method for preparing same, a pharmaceutical composition containing same, and a method for preventing or treating obesity and obesity-related metabolic disorders.Type: ApplicationFiled: February 27, 2008Publication date: August 28, 2008Applicant: Green Cross CorporationInventors: Jinhwa LEE, Jeongmin Kim, Jong Yup Kim, Hee Jeong Seo, Myung Eun Jung, Sung-Han Lee, Kwangwoo Ahn, Suk Ho Lee
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Publication number: 20080207704Abstract: A heteroaryl-imidazole compound of formula (I) or a pharmaceutically acceptable salt thereof is effective as a cannabinoid CB1 receptor inverse agonist or antagonist, which is useful for preventing or treating obesity and obesity-related metabolic disorders. The present invention also provides a method for preparing a heteroaryl-imidazole compound of formula (I), a pharmaceutical composition containing a heteroaryl-imidazole compound of formula (I), and a method for preventing or treating obesity and obesity-related metabolic disorders.Type: ApplicationFiled: February 27, 2007Publication date: August 28, 2008Applicant: THE GREEN CROSS CORPORATIONInventors: Jinhwa Lee, Jeongmin Kim, Jong Yup Kim, Hee Jeong Seo, Myung Eun Jung, Sung-Han Lee, Kwangwoo Ahn
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Publication number: 20080200371Abstract: Compounds and compositions are provided for modulating the activity of protein tyrosine phosphatases. In one embodiment, the compounds and compositions are thiazoles and thiadiazoles that inhibit the activity of protein tyrosine phosphatase 1B.Type: ApplicationFiled: March 28, 2008Publication date: August 21, 2008Inventors: Zacharia S. CHERUVALLATH, Colin J. Loweth, Ruth F. Nutt, Darryl Rideout, Joseph E. Semple, Jing Wang, Feiyue Wu, Shankari Mylvaganam, Hengyi Zhu, Jianzhong Sun
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Patent number: 7408068Abstract: The present invention relates to compounds of the Formula wherein R3, R5, R7, U, X, Y and Z are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. This invention also relates to pharmaceutical compositions and methods of treating diseases, for example, neurodegenerative diseases, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.Type: GrantFiled: July 17, 2007Date of Patent: August 5, 2008Assignee: Pfizer Inc.Inventor: Yuhpyng L. Chen
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Patent number: 7407976Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: November 15, 2004Date of Patent: August 5, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Mark T. Miller, Sarah S. Hadida Ruah, Peter D. J. Grootenhuis, Matthew Hamilton
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Publication number: 20080176899Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: August 11, 2005Publication date: July 24, 2008Inventors: Sarah Hadida Ruah, Peter Grootenhuis, Mark Miller, Matthew Hamilton
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Patent number: 7402606Abstract: Heterocycle substituted ketoamide derivatives of Formula (I), wherein the substitutes A, D, A and R are defined as in claim in, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such heterocycle substituted ketoamide derivatives as well as method of using the same in the manufacture of medicaments for the treatment of disorders, including osteoporosis, associated with an imbalance between bone resorption and formation which can ultimately lead to fracture.Type: GrantFiled: April 1, 2003Date of Patent: July 22, 2008Assignee: SmithKline Beecham CorporationInventors: David Gene Barrett, John G. Catalano, David Norman Deaton, Aaron Bayne Miller, John A. Ray, Vicente Samano
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Patent number: 7399765Abstract: Compounds of formula (I) Z-Ar1—Ar2??(I) wherein Z is a diazabicyclic amine, Ar1 is a 5- or 6-membered aromatic ring, and Ar2 is selected from the group consisting of an unsubstituted or substituted 5- or 6-membered heteroaryl ring; unsubstituted or substituted bicyclic heteroaryl ring; 3,4-(methylenedioxy)phenyl; carbazolyl; tetrahydrocarbazolyl; naphthyl; and phenyl; wherein the phenyl is substituted with 0, 1, 2, or 3 substituents in the meta- or para-positions. The compounds are useful in treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods for using such compounds and compositions.Type: GrantFiled: September 16, 2004Date of Patent: July 15, 2008Assignee: Abbott LaboratoriesInventors: William H. Bunnelle, Jianguo Ji, Tao Li, Jennifer M. Pace, Karin R. Tietje, Kathleen H. Mortell, Diana L. Nersesian, Michael R. Schrimpf
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Publication number: 20080159955Abstract: Therapeutic methods for inhibiting the growth of preneoplastic/neoplastic vertebrate cells that abnormally express MN protein are disclosed. Screening assays are provided for identifying compounds, preferably organic compounds, preferably aromatic and heterocylic sulfonamides, which inhibit the enzymatic activity of MN/CA IX and that are useful for treating patients with preneoplastic/neoplastic disease. Further, the CA IX-specific inhibitors when labeled or linked to an appropriate visualizing means can also be used diagnostically/prognostically for preneoplastic/neoplastic disease, and for imaging use, for example, to detect hypoxic precancerous cells, tumors and/or metastases, by selectively binding to activated CA IX, preferably CA IX activated under hypoxic conditions, and not to inactive CA IX. Such detection of hypoxic conditions can be helpful in determining effective treatment options, and in predicting treatment outcome and the prognosis of disease development.Type: ApplicationFiled: October 30, 2007Publication date: July 3, 2008Inventors: Claudiu Supuran, Andrea Scozzafava, Silvia Pastorekova, Jaromir Pastorek
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Patent number: 7390908Abstract: The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R1, R2, R3, n and m are as described in the specification, in the preparation of a medicament for the treatment or prevention of a disease condition mediated through glucokinase (GLK), such as type 2 diabetes. The invention also relates to a novel group of compounds of Formula (I) and to methods for preparing compounds of Formula (I).Type: GrantFiled: August 15, 2002Date of Patent: June 24, 2008Assignee: AstraZeneca ABInventors: Scott Boyd, Peter William Rodney Caulkett, Rodney Brian Hargreaves, Suzanne Saxon Bowker, Roger James, Craig Johnstone, Clifford David Jones, Darren McKerrecher, Michael Howard Block
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Publication number: 20080146445Abstract: The present invention concerns nematicidal compounds, their formulation as nematicidal composition and their use for controlling nematodes, preferably plant parasitic nematodes.Type: ApplicationFiled: December 16, 2005Publication date: June 19, 2008Applicant: Devgen NVInventors: Jan Octaaf De Kerpel, Dirk Leysen
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Publication number: 20080146625Abstract: Disclosed herein are pyrazole glucokinase activators of the formula (I): that are useful for the treatment of metabolic diseases and disorders.Type: ApplicationFiled: December 6, 2007Publication date: June 19, 2008Inventors: Steven Joseph Berthel, Robert Francis Kester, Douglas Eric Murphy, Thomas Jay Prins, Frank Ruebsam, Chinh Viet Tran, Dionisios Vourloumis
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Patent number: 7387798Abstract: The key obstacle for current resuscitation is the acutely limited time window. The major reason for the limited time window is that the brain and spinal cord are extremely vulnerable to hypoxic-ischemic insult. A method and a lymph-like fluid composition for resuscitation of cardiac arrest are provided. The method includes steps of inhibiting CSF production, removing CSF, replacing the CSF with invented lymph-like fluid composition plus conventional CPR. The lymph-like fluid composition includes polypeptides, insulin, elevated magnesium concentration and ATP in artificial CSF.Type: GrantFiled: September 26, 2005Date of Patent: June 17, 2008Inventor: Yanming Wang
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Publication number: 20080132551Abstract: The invention provides compounds of Formula I: wherein A, B, and X are described herein. These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals used to treat diseases or conditions in which ?7 nAChR is known to be involved.Type: ApplicationFiled: March 24, 2004Publication date: June 5, 2008Inventors: Bruce Nelsen Rogers, David Walter Piotrowski, Brandon J. Margolis, Jason K. Myers, Vincent Edward Groppi, Daniel G. Rudmann
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Publication number: 20080125469Abstract: The present invention relates to Thiadiazole Compounds; compositions comprising an effective dose of a Thiadiazole Compound; and methods treating or preventing a metalloproteinase-related disorder, such as, an arthritic disorder, osteoarthritis, cancer, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, atherosclerosis, age-related macular degeneration, myocardial infarction, a corneal ulceration, an ocular surface disease, hepatitis, an aortic aneurysm, tendonitis, a central nervous system disorder, abnormal wound healing, angiogenesis, restenosis, cirrhosis, multiple sclerosis, glomerulonephritis, graft versus host disease, diabetes, an inflammatory bowel disease, shock, invertebral disc degeneration, stroke, osteopenia or a periodontal disease or comprising administering an effective dose of a Thiadiazole Compound to a mammal in need thereof.Type: ApplicationFiled: June 7, 2007Publication date: May 29, 2008Applicant: WyethInventors: Matthew G. Bursavich, Sabrina Lombardi, Adam M. Gilbert
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Patent number: 7354944Abstract: The invention relates to thiadiazole compounds useful for treating diseases mediated by protein kinase B (PKB). The invention also relates to the therapeutic use of such thiadiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.Type: GrantFiled: October 18, 2005Date of Patent: April 8, 2008Assignee: Amgen Inc.Inventors: Qingping Zeng, Guomin Yao, George Erich Wohlhieter, Vellarkad N. Viswanadhan, Andrew Tasker, James Thomas Rider, Holger Monenschein, Celia Dominguez, Matthew Paul Bourbeau
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Patent number: 7348345Abstract: This invention relates to methods of treating an HIV infection with novel heterocyclic compounds of formula I wherein R1—R4, X1 and X2 are as defined in the summary and pharmaceutically acceptable salts, and methods to inhibit or modulate Human Immunodeficiency Virus (HIV) reverse transcriptase with compounds of formula I.Type: GrantFiled: February 2, 2007Date of Patent: March 25, 2008Assignee: Roche Palo Alto LLCInventors: James Patrick Dunn, Steven Swallow, Zachary Kevin Sweeney
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Patent number: 7338966Abstract: The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.Type: GrantFiled: June 9, 2005Date of Patent: March 4, 2008Assignee: SmithKline Beecham CorporationInventors: Karen Elizabeth Lackey, Edgar Raymond Wood, III
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Patent number: 7326695Abstract: Compounds of the structure I: are useful for treating bacterial growth, wherein E is selected from the group consisting of B, P, and S, T1 and T2 are each independently selected from the group consisting of O, NR, and CH2, where R=H or C1-C8 alkyl, or C1-C8 oxoalkyl, and L is selected from the group consisting of ethylene, propylene, and four to six-membered alicyclic and aromatic rings, provided that structure I does not include AI-2-borate. The compounds may be used to treat bacterial infections in human beings and to regulate biofilm formation. Pharmaceutical compositions comprising one or more such compounds are useful for treating bacterial infections in human beings.Type: GrantFiled: May 17, 2006Date of Patent: February 5, 2008Assignee: The Trustees of Princeton UniversityInventors: Stephen R. Cooper, Kraig M. Yager
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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
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Patent number: 7288567Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: GrantFiled: March 26, 2001Date of Patent: October 30, 2007Assignee: Methylgene Inc.Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg
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Patent number: 7271289Abstract: Compounds of formula (I): or pharmaceutically acceptable derivatives thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.Type: GrantFiled: April 7, 2004Date of Patent: September 18, 2007Assignee: SmithKline Beecham CorporationInventor: Nicola Mary Aston
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Patent number: 7253195Abstract: The present invention relates to compounds of the Formula wherein R3, R5, R7, U, X, Y and Z are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. This invention also relates to pharmaceutical compositions and methods of treating diseases, for example, neurodegenerative diseases, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.Type: GrantFiled: August 20, 2004Date of Patent: August 7, 2007Assignee: Pfizer IncInventor: Yuhpyng L. Chen
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Patent number: 7232820Abstract: The present invention relates to compounds of the Formula I wherein R1, R3, R5, R7, X, Y and U are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods of treating diseases and disorders, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.Type: GrantFiled: March 11, 2005Date of Patent: June 19, 2007Assignee: Pfizer IncInventor: Yuhpyng L. Chen
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Patent number: 7232929Abstract: The invention relates to new 2,2,3,3-tetramethylcyclopropane carboxamide derivative compounds, pharmaceutical compositions thereof and uses thereof for treating psychotic disorders, neurodegenerative diseases, epilepsy and pain.Type: GrantFiled: February 15, 2004Date of Patent: June 19, 2007Assignee: Yissum Research Development Company of the Hebrew University of JerusalemInventors: Meir Bialer, Boris Yagen, Eyal Sobol, Dan Kaufmann
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Patent number: 7217714Abstract: Compounds of Formula 1 [Region ?]?[Region ?]?[Region ?]?[Region ?] ??(I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treatment using these compounds.Type: GrantFiled: November 30, 1999Date of Patent: May 15, 2007Assignee: Agouron Pharmaceuticals, Inc.Inventors: Duncan Robert Armour, David Anthony Price, Blanda Luzia Christa Stammen, Anthony Wood, Manoussos Perros, Martin Paul Edwards
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Patent number: 7211592Abstract: The invention relates to substituted and unsubstituted 3H-benzo[1,2,3]oxathiazole 2,2-dioxides, 1,3-dihydrobenzo[1,2,5]thiadiazole 2,2-dioxides and 1,3-dihydro-benzo[c]isothiazole 2,2-dioxides, to their preparation and to their use in medicaments.Type: GrantFiled: September 13, 2004Date of Patent: May 1, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Stefan Petry, Karl-Heinz Baringhaus, Swen Hoelder, Guenter Mueller
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Patent number: 7208509Abstract: This invention relates to novel heterocyclic compounds of formula I wherein R1—R4, X1 and X2 are as defined in the summary and pharmaceutically acceptable salts and solvates thereof, methods to inhibit or modulate Human Immunodeficiency Virus (HIV) reverse transcriptase with compounds of formula I, pharmaceutical compositions containing of formula I admixed with at least one solvent, carrier or excipient and processes to prepare compounds of formula I.Type: GrantFiled: March 23, 2004Date of Patent: April 24, 2007Assignee: Roche Palo Alto LLCInventors: James Patrick Dunn, Steven Swallow, Zachary Kevin Sweeney
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Patent number: 7208629Abstract: Compounds of formula (I): wherein when m is 0 to 4 R1 is selected from C1–6alkyl, C3–7cycloalkyl, C2–6alkenyl, —SO2NR4R5, —CONR4R5 and —COOR4; and when m is 2 to 4 R1 is additionally selected from C1–6alkoxy, hydroxy, NR4R5, —NR4SO2R5, —NR4SOR5, —NR4COR5, and —NR4CONR4R5; R2 is selected from hydrogen, C1–6alkyl and —(CH2)n-C3–7cycloalkyl; R3 is the group —CO—NH—(CH2)p-R6; U is selected from methyl and halogen; W is selected from methyl and chlorine; V and Y are each selected independently from hydrogen, methyl and halogen; m is selected from 0, 1, 2, 3 and 4 wherein each carbon atom of the resulting carbon chain may be optionally substituted with one or two groups selected independently from C1–6alkyl; n is selected from 0, 1, 2 and 3; p and r are independently selected from 0, 1 and 2; s is selected from 0, 1 and 2; or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitorsType: GrantFiled: October 16, 2002Date of Patent: April 24, 2007Assignee: Glaxo Group LimitedInventors: Richard Martyn Angell, Nicola Mary Aston, Paul Bamborough, George Stuart Cockerill, Suzanne Joy Merrick, Kathryn Jane Smith, Ann Louise Walker
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Patent number: 7183277Abstract: Novel compounds of the formula I in which D, W, X, Y, T and R1 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours.Type: GrantFiled: March 31, 2003Date of Patent: February 27, 2007Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Werner Mederski, Johannes Gleitz, Bertram Cezanne, Christos Tsaklakidis, Christopher Barnes
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Patent number: 7183303Abstract: Compounds of formula I: inhibit gamma-secretase and hence find use in treatment of Alzheimer's disease.Type: GrantFiled: November 5, 2004Date of Patent: February 27, 2007Assignee: Merck Sharp & Dohme LimitedInventors: Jose Luis Castro Pineiro, Ian James Collins, Timothy Harrison
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Patent number: 7157470Abstract: The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: May 5, 2003Date of Patent: January 2, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Joanne M. Smallheer, Donald J. Pinto, Shuaige Wang, Jennifer X. Qiao, Wei Han, Zilun Hu
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Patent number: 7153873Abstract: Salts of a bicyclic, N-acylated imidazo-3-amine or an imidazo-5-amine of the formula: addition products thereof with acids, and methods for preparing the salts and addition products. Also disclosed are pharmaceutical compositions comprising the same and methods using the pharmaceutical compositions for the treatment or prophylaxis of pain, drug or alcohol abuse, diarrhoea, gastritis, ulcers, urinary incontinence, depression, narcolepsy, overweight, asthma, glaucoma, tinnitus, itching, hyperkinetic syndrome, epilepsy, or schizophrenia, for inducing anesthesia, and for anxiolysis.Type: GrantFiled: June 6, 2006Date of Patent: December 26, 2006Assignee: Gruenenthal GmbHInventors: Matthias Gerlach, Corinna Sundermann
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Patent number: 7148219Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: GrantFiled: April 29, 2005Date of Patent: December 12, 2006Assignee: Rib-X Pharmaceuticals, Inc.Inventors: Rongliang Lou, Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
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Patent number: 7122565Abstract: The invention provides 1,3,4-thiadiazoles and 1,3,4-oxadiazoles having the following Formula I: in which, Y is S or O, R1 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, heteroaryl or a polycyclic group, optionally substituted, R2 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl or aryl optionally substituted, R3 is X2—R?3, in which X2 is a binding group and R?3 is cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, heteroaryl, or a polycyclic group; optionally substituted, or their pharmaceutically acceptable derivatives, a compound of Formula I, for their preparation, and processes for pharmaceutical compositions containing methods of using the compounds for the treatment of disorders for which a treatment by a PDE7 inhibitor is relevant.Type: GrantFiled: October 1, 2001Date of Patent: October 17, 2006Assignee: Warner-Lambert LLCInventors: Fabrice Vergne, Pierre Ducrot, Charles Andrianjara, Patrick Bernardelli, Edwige Lorth Ois
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Patent number: 7119099Abstract: A compound of formula (I) or its enantiomers or diastereoisomers thereof: wherein: A,; X, W, R1, Y; R3; and R4 are as defined herein. The compounds of the invention may be used as inhibitors of the papilloma virus E1-E2-DNA complex. The invention further provides a method of treating or preventing human papilloma virus infection.Type: GrantFiled: February 4, 2004Date of Patent: October 10, 2006Assignee: Boehringer Ingelheim (Canada) Ltd.Inventors: Christiane Yoakim, William W. Ogilvie, Jeffrey O'Meara, Peter White, Nathalie Goudreau
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Patent number: 7115624Abstract: The present invention provides a method of inhibiting a member of a family of Protein Tyrosine Phosphatases (PTPases, PTPs) such as PTP1B, TC-PTP, CD45, SHP-1, SHP-2, PTP?, PTP?, PTP?, PTP?, PTP?, PTP?, PTP?, PTPD1, PTPD2, PTPH1, PTP-MEG1, PTP-LAR, and HePTP by exposing said Ptpase member by administration to a host or otherwise to at least one compound with certain structural, physical and spatial characteristics that allow for the interaction of said compound with specific residues of the active site of PTP1B and/or TC-PTP. These compounds are indicated in the management or treatment of a broad range of diseases such as autoimmune diseases, acute and chronic inflammation, osteoporosis, various forms of cancer and malignant diseases, and type I diabetes and type II diabetes, as well as in the isolation of PTPases and in elucidation or further elucidation of their biological function.Type: GrantFiled: September 11, 2000Date of Patent: October 3, 2006Assignee: Novo Nordisk A/SInventors: Henrik Sune Andersen, Thomas Kruse Hansen, Lars Fogh Iversen, Jesper Lau, Niels Peter Hundahl Møller, Ole Hvilsted Olsen, Frank Urban Axe, Yu Ge, Daniel Dale Holsworth, Todd Kevin Jones, Luke Milburn Judge, Wiliam Charles Ripka, Barry Zvi Shapira, Roy Teruyuki Uyeda
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Patent number: 7115658Abstract: Compounds of formula I are hepatitis C virus (HCV) RNA-dependent RNA polymerase (RdRp) inhibitors, and are useful in therapeutic and prophylactic treatment of persons infected with hepatitis C virusType: GrantFiled: May 9, 2003Date of Patent: October 3, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Allen J. Borchardt, Peter Scott Dragovich, Javier Gonzalez, Tanya Michelle Jewell, Hui Li, Maria Angelica Linton, John Howard Tatlock, Ru Zhou, Thomas Jay Prins, Melwyn A. Abreo
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Patent number: 7115639Abstract: The present invention is related to pyrrolidine oxadiazole and thiadiazole derivatives for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such pyrrolidine oxadiazole derivatives. Said pyrrolidine derivatives are useful in the treatment and/or prevention of preterm labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including preterm labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation.Type: GrantFiled: June 14, 2002Date of Patent: October 3, 2006Assignee: Applied Research Systems ARS Holding N.V.Inventors: Matthias Schwarz, Anna Quattropani, Patrick Page, Russell J. Thomas, Vincent Pomel
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Patent number: 7105556Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.Type: GrantFiled: May 22, 2002Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. Cheng, Yoon Jeon, Wei Wang
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Patent number: 7098201Abstract: A compound of the formula (I): wherein X is hydroxy, protected hydroxy or optionally substituted amino; Y is —COORA wherein RA is hydrogen or ester residue, —CONRBRC wherein RB and RC each is independently hydrogen or amide residue, optionally substituted aryl or optionally substituted heteroaryl; and A1 is optionally substituted heteroaryl; provided that a compound wherein Y and/or A1 is optionally substituted indol-3-yl is excluded, a tautomer, a prodrug, a pharmaceutically acceptable salt or a hydrate thereof has an inhibitory activity against an integrase.Type: GrantFiled: June 18, 2003Date of Patent: August 29, 2006Assignee: Shionogi & Co., Ltd.Inventors: Toshio Fujishita, Tomokazu Yoshinaga, Akihiko Sato
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Patent number: 7078403Abstract: Disclosed herein are compounds of formula II: wherein Alk, Z, X1, X2, R1, —R10 and R11 are defined herein, and their salts and pharmaceutically acceptable derivatives thereof, as well as other compounds of the general formula Het-A-Alk-W-Ar-C(X2)?NO-X2 where Het, A, W and Ar are also defined herein. These compounds are useful in treating picornavirus infections in mammals. Novel intermediates of these compounds, as well as pharmaceutical compositions and methods of use, are also disclosed herein.Type: GrantFiled: June 16, 2000Date of Patent: July 18, 2006Assignee: Biota Scientific Management Pty Ltd.Inventors: Wen-Yang Wu, Keith Watson, Darryl McConnell, Betty Jin, Guy Krippner
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Patent number: 7078424Abstract: This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.Type: GrantFiled: June 24, 2003Date of Patent: July 18, 2006Assignee: GPI NIL Holdings, Inc.Inventors: Gregory S. Hamilton, Mark H. Norman, Yong-Qian Wu
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Patent number: 7074776Abstract: Compounds of the structure I: are useful for treating bacterial growth, wherein E is selected from the group consisting of B, P, and S, T1 and T2 are each independently selected from the group consisting of O, NR, and CH2, where R?H or C1–C8 alkyl, or C1–C8 oxoalkyl, and L is selected from the group consisting of ethylene, propylene, and four to six-membered alicyclic and aromatic rings, provided that structure I does not include AI-2-borate. The compounds may be used to treat bacterial infections in human beings and to regulate biofilm formation. Pharmaceutical compositions comprising one or more such compounds are useful for treating bacterial infections in human beings.Type: GrantFiled: October 1, 2003Date of Patent: July 11, 2006Assignee: Quorex Pharmaceuticals, Inc.Inventors: Stephen R. Cooper, Kraig M. Yager
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Patent number: 7071180Abstract: The invention relates to compounds of the general formula (I): wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO2—, —NH—, (ii) a C1-4-alkyl- or C1-6-acyl-substituted nitrogen atom or (iii) a C1-8-alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is —C(R4)(R5)—, —OC(R4)(R5)—, —N(R6)C(R4)(R5)—, —N(R6)—, —O—, —S— or —SO2—; R is optionally substituted C3-8-cycloalkyl, aryl or heteroaryl; R1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ring members, which rings optionally are substituted in one or more positions, or a group —[C(R4)(R5)]xN(R2a)(R3a)]; R2a, R3a, R4, R5, R6 and x are asType: GrantFiled: June 22, 2004Date of Patent: July 4, 2006Assignee: Biovitrum ABInventors: Björn Nilsson, Jan Tejbrant, Benjamin Pelcman, Erik Ringberg, Markus Thor, Jonas Nilsson, Mattias Jönsson
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Patent number: 7071217Abstract: The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis, In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.Type: GrantFiled: August 23, 2001Date of Patent: July 4, 2006Assignee: SmithKline Beecham CorporationInventors: Scott Howard Dickerson, Robert N Hunter, Lee Frederick Kuyper, Karen Elizabeth Lackey, Michael J. Luzzio, Edgar Raymond Wood, III