Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 546/284.1)
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Publication number: 20090054650Abstract: The present invention relates to a new method of cross-coupling aryl moieties comprising reacting an arylhalide with an arylboronic acid in the presence of a palladium compound and a compound comprising a di-alkylphosphine moiety.Type: ApplicationFiled: October 3, 2008Publication date: February 26, 2009Inventor: Alex Sergey IONKIN
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Publication number: 20090036492Abstract: The present invention relates to a novel cercosporamide derivative, a pharmacologically acceptable salt thereof or an ester thereof which has an excellent hypoglycemic effect and is useful as a therapeutic and/or prophylactic agent for diabetes.Type: ApplicationFiled: August 8, 2006Publication date: February 5, 2009Inventors: Akihiro Furukawa, Jun Ohsumi, Tsuyoshi Arita, Takehiro Fukuzaki, Kazushi Araki, Makoto Mori, Takayuki Momose, Takeshi Honda, Masanori Kuroha, Ryo Okuyama, Susumu Satoh
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Publication number: 20090023783Abstract: The invention relates to novel benzofuran derivatives, processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative disordersType: ApplicationFiled: August 29, 2008Publication date: January 22, 2009Inventors: Chengzhi Zhang, Jacques Dumas, Gaetan H. Ladouceur, Qian Zhao, Martin Hentemann, Sharad K. Verma, Qingming Zhu, Rico C. Lavoie, Jianmei Fan, Barton Phillips
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Publication number: 20080286204Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: May 9, 2008Publication date: November 20, 2008Inventors: Sara S. Hadida-Ruah, Mark Miller, Brian Bear, Jinglan Zhou, Jason McCartney, Peter Grootenhuis
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Publication number: 20080280875Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is (4-12)-membered heterocyclyl; Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).Type: ApplicationFiled: May 9, 2007Publication date: November 13, 2008Inventors: Hao Bai, Simon Bailey, Dilip Ramakant Bhumralkar, Feng C. Bi, Fengli Guo, Mingying He, Paul Stuart Humphries, Anthony Lai Ling, Jihong Lou, Seiji Nukul, Ru Zhou
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Patent number: 7442712Abstract: A compound represented by the structural formula and pharmaceutically acceptable salts and solvents thereof is disclosed, wherein: the single-dashed line between the ring carbons to which R10 and R34 are attached represents either a single bond or a double bond; the double-dashed line between X and the carbon to which Y is attached represents either a single bond or an absent bond; X is —O— or —NR6— when the double-dashed line represents a single bond; X is H, —OH or —NHR20 when the double-dashed line represents an absent bond; and other parameters are as defined herein. Also disclosed are pharmaceutical compositions and combinations containing said compounds and their uses as thrombin receptor antagonists and binders to cannabinoid receptors.Type: GrantFiled: May 25, 2005Date of Patent: October 28, 2008Assignee: Schering CorporationInventors: Mariappan V. Chelliah, Samuel Chackalamannil, Yan Xia, Martin C. Clasby, William J. Greenlee, Yuguang Wang, Enrico P. Veltri, Wenxue Wu, Michael P. Graziano, Teddy Kosoglou, Madhu Chintala
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Patent number: 7439368Abstract: The present invention provides a process of preparing a compound of the formula [I]: wherein X is a group of the formula: —N? or —CH?; R1 is a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a cyano group or an amino group optionally substituted by a lower alkyl group; Ring A is a nitrogen-containing heterocyclic group; Ring B is an optionally substituted benzene ring or an optionally substituted pyridine ring; and R3 is a hydrogen atom or a lower alkyl group, or a pharmaceutically acceptable salt thereof, which is useful as an inhibitor of activated blood coagulation factor X.Type: GrantFiled: June 29, 2004Date of Patent: October 21, 2008Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Masahiko Seki, Shin-ichi Yoshida, Nobuhiro Yagi, Masanori Hatsuda, Mayumi Kimura, Kazuhiko Kondo
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Patent number: 7419986Abstract: Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as premenstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.Type: GrantFiled: August 31, 2006Date of Patent: September 2, 2008Assignee: WyethInventors: Dahui Zhou, Gary Paul Stack
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Publication number: 20080194638Abstract: The present invention relates to bioavailable pharmaceutical formulations of heterocyclic compounds, such as such as N-(3,5-dichloropyrid-4-yl)-4-difluoromethoxy-8-methanesulfonamido-dibenzo[b,d]furan-1-carboxamide (oglemilast) and pharmaceutically acceptable salts thereof, to processes for their preparation and to methods of treatment using the same. The present invention also relates to substantially pure amorphous forms of heterocyclic compounds, such as oglemilast. The invention is particularly directed to bioavailable pharmaceutical oral dosage forms containing amorphous oglemilast.Type: ApplicationFiled: February 8, 2008Publication date: August 14, 2008Applicant: Forest Laboratories Holdings LimitedInventors: Mahendra G. DEDHIYA, Rahul Surana, Suneel K. Rastogi, Anil Chhetrry
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Publication number: 20080146810Abstract: The present invention relates to novel tricyclic compounds useful for the treatment of inflammatory conditions, diseases of the central nervous and insulin resistant diabetes.Type: ApplicationFiled: June 27, 2007Publication date: June 19, 2008Applicant: GLENMARK PHARMACEUTICALS S.A.Inventors: Gopalan Balasubramanian, Laxmikant A. Gharat, Aftab D. Lakdawala, Raghu R. Anupindi
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Patent number: 7368477Abstract: Compounds of formula I or pharmaceutically acceptable salts thereof are provided: wherein each of R1, R1?, R2, R3, R4, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.Type: GrantFiled: April 21, 2006Date of Patent: May 6, 2008Assignee: WyethInventors: Jonathan Laird Gross, Gary Paul Stack, Dahui Zhou, Hong Gao
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Patent number: 7368476Abstract: The present invention is directed to certain hydroxamate derivatives that are inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: GrantFiled: April 7, 2005Date of Patent: May 6, 2008Assignee: Pharmacyclics, Inc.Inventor: Eduardo L. Setti
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Patent number: 7335666Abstract: Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.Type: GrantFiled: August 31, 2006Date of Patent: February 26, 2008Assignee: WyethInventors: Dahui Zhou, Gary Paul Stack
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Publication number: 20080004318Abstract: Substituted bicyclic and tricyclic modified himbacine derivative of the formula: or a pharmaceutically acceptable salt or solvate of said compound wherein represents an optional double bond and wherein En, Fn, Gn, Zn, Jn, X, R3, R9, R10, R11, R32, R33, B and Het are herein defined are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other agents is also claimed.Type: ApplicationFiled: June 27, 2007Publication date: January 3, 2008Inventors: Mariappan V. Chelliah, Samuel Chackalamannil, Yan Xia
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Patent number: 7304078Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt thereof, wherein: the dotted line represents an optional single bond; represents an optional double bond; n is 0–2; Q is cycloalkyl, optionally substituted by R13 and R14; R13 and R14 are independently selected from (C1–C6)alkyl, (C3–C8)cycloalkyl, —OH, (C1–C6)alkoxy, R27-aryl(C1–C6)alkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, halogen and haloalkyl; or R13 and R14 together form a spirocyclic or a heterospirocyclic ring of 3–6 atoms; Het is a mono- or bi-cyclic optionally substituted heteroaryl group; and B is a bond, alkylene, or optionally substituted alkenylene or alkynylene, wherein the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administeringType: GrantFiled: April 14, 2003Date of Patent: December 4, 2007Assignee: Schering CorporationInventors: Samuel Chackalamannil, William J. Greenlee, Yuguang Wang, Wenxue Wu, Enrico P. Veltri, Yan Xia
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Patent number: 7291580Abstract: 4-Aminopicolinic acids having (1,1-difluoroalkyl) substituents in the 6-position and their amine and acid derivatives are potent herbicides demonstrating a broad spectrum of weed control.Type: GrantFiled: August 4, 2004Date of Patent: November 6, 2007Assignee: Dow AgroSciences LLCInventors: Terry William Balko, Stephen Craig Fields, Nicholas Martin Irvine, Christian Thomas Lowe, Paul Richard Schmitzer
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Patent number: 7250518Abstract: Compounds of the formula: useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils.Type: GrantFiled: February 17, 2004Date of Patent: July 31, 2007Assignee: Pfizer Inc.Inventors: Thomas V. Magee, Anthony Marfat, Robert J. Chambers
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Patent number: 7241795Abstract: The present invention relates to novel 2,5-bis{[alkyl (or aryl) imino]aminophenyl}furans and thiophenes of the general formula in which R1, R2, R3 and R4 are each independently selected from the group consisting of H, alkyl, alkoxy, halide, and alkylhalide groups; R5 is H, alkyl or aryl; R6 is H, alkyl, aryl, or NR7R8, in which R7 and R8 are each independently selected from the group consisting of H, alkyl and aryl; and X is O, S or NR9, in which R9 is H or alkyl, and to the use of such compounds.Type: GrantFiled: March 2, 2004Date of Patent: July 10, 2007Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc., Duke UniversityInventors: David W. Boykin, Richard R. Tidwell, W. David Wilson, John R. Perfect, Chad F. Stephens
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Patent number: 7235568Abstract: The invention provides compounds of the formula: wherein (a) is a single or double bond; W is CH, CH2, CHCH3, C(CH3)2, C(CH2)2 or C(CH2)3; X is N; and Y is H or F, and salts, hydrates, tautomers, pure enantiomers, and enantiomeric mixtures; and a method of treating schizophrenia comprising administering same.Type: GrantFiled: July 28, 2006Date of Patent: June 26, 2007Assignee: Pierre Fabre MedicamentInventors: Bernard Vacher, Stéphane Cuisiat, Wouter Koek, Francis Colpaert
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Patent number: 7205305Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: July 17, 2003Date of Patent: April 17, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Guy W Bemis, Francesco G Salituro, John P Duffy, John E Cochran, Edmund M Harrington, Mark A Murcko, Keith P Wilson, Michael Su, Vincent P Galullo
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Patent number: 7189758Abstract: A compound of Formula (I) wherein R1, R2, R3, R4, R5, and R6 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.Type: GrantFiled: October 5, 2005Date of Patent: March 13, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Rajashekhar Betageri, David Thomson, Yan Zhang, Renee Michele Zindell
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Patent number: 7183293Abstract: This application is directed to compounds of the formula wherein j is 1; k is 0 or 1; m is 1, 2 or 3; n is 1 or 2; W1 and W2 are independently —O— or —S(?O)t—, where t is 0, 1, or 2; Y is ?C(R1a)—, where R1a is a member selected from the group consisting of H; F; Cl; CN; NO2; —(C1–C4)alkyl; —(C2–C4)alkynyl; fluorinated-(C1–C3)alkyl; fluorinated-(C1–C3)alkoxy; —OR16; and —C(?O)NR22aR22b; R22a and R22b are defined as set forth in the specification; —RA and RB are each a member independently selected from the group consisting of H; F; CF3; —(C1–C4)alkyl; —(C3–C7)cycloalkyl; phenyl; and benzyl; wherein said cycloalkyl, phenyl, and benzyl moieties are each independently substituted with 0 to 3 substituents R10, which is defined as set forth in the specification; R16 and R17 are defined as set forth in the specification; —RC and RD have the same meaning as defined above for RA and RB except that one of them must be —H, and they are selected independently of each other and of RA and RB; R1 and R2 are each a membType: GrantFiled: August 13, 2004Date of Patent: February 27, 2007Assignees: Pfizer Inc., Pfizer Products Inc.Inventors: Anthony Marfat, Robert J. Chambers, Thomas V. Magee
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Patent number: 7153871Abstract: PDE4 inhibition is achieved by novel compounds, e.g., aminoindazole and aminobenzofuran analogs. The compounds of the present invention are of Formulas I and II: wherein R1, R2, R3, R4, R7 and R8 are as defined herein.Type: GrantFiled: July 18, 2003Date of Patent: December 26, 2006Assignee: Memory Pharmaceuticals CorporationInventors: Richard A. Schumacher, Allen T. Hopper, Ashok Tehim
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Patent number: 7144885Abstract: This invention relates to a novel fused tricyclic heterocycle of the formula (Ia, Ib) and its use for the treatment of hyper-proliferative disordersType: GrantFiled: February 21, 2003Date of Patent: December 5, 2006Assignee: Bayer Pharmaceuticals CorporationInventors: Chengzhi Zhang, Michael Burke, Zhi Chen, Jacques Dumas, Dongping Fan, Benjamin D. Jones, Gaetan Ladouceur, Wendy Lee, Barton Phillips, Scott M. Wilhelm, Qian Zhao
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Patent number: 7145021Abstract: The subject invention provides compounds having the structure: wherein R1 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R2 is H, OH, a photoactivatable moiety, a fluorescent-moiety, or a radioactive moiety; R3 is H or OH; R4 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; and wherein at least one of R1, R2, R3, or R4 is a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety, or an optically pure enantiomer of the compound or wherein R1 is H or OH; R2 is H, OH, halogen, unsubstituted or substituted, straight or branched (C1–C5) alkyl group, (C2–C5) alkenyl, or a (C2–C5) alkynyl, (C1–C5) alkoxy, (C2–C5) alkenyloxy, or (C2–C5) alkynyloxy, —N3, —COR5, —CONR5R6, —CO2R5, —OCOR5, —NH(OH), —NR5R6, —NHCOR5, —N(OH)COR5, —CH2OR5, —OCH2CO2R5, —CH2SR5, —CH2NR5R6, —SR5, —OSR5, or —NR5SO2R6, where R5 and R6 are each independently hydrogen, substituted or unsubstituted (C1–C5) alkyl, (C2–C5) alkenyl, or (C2–C5) alkynyl, or a cycloType: GrantFiled: March 28, 2003Date of Patent: December 5, 2006Assignee: The Trustees of Columbia University in the City of New YorkInventors: Kristian Stromgaard, Makiko Suehiro, Koji Nakanishi, Stine B. Vogensen
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Patent number: 7135479Abstract: Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.Type: GrantFiled: September 10, 2003Date of Patent: November 14, 2006Assignee: WyethInventors: Dahui Zhou, Gary Paul Stack
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Patent number: 7045545Abstract: The present invention provides serotonergic aminoalkylbenzofurans of Formula (I): where R, R1, R2, R3, R4, R4?, R5, R5?, and R12 are as described in the specification.Type: GrantFiled: January 19, 2000Date of Patent: May 16, 2006Assignee: Eli Lilly and CompanyInventors: Karin Briner, Joseph Paul Burkhart, Timothy Paul Burkholder, Matthew Joseph Fisher, William Harlan Gritton, Daniel Timothy Kohlman, Sidney Xi Liang, Shawn Christopher Miller, Jeffrey Thomas Mullaney, Yao-Chang Xu, Yanping Xu
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Patent number: 7037920Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salts thereof, wherein: n1 and n2 are independently 0-2; Het is an optionally substituted mono-, bi- or tricyclic heteroaromatic group; B is alkyl or optionally substituted alkenyl; R22 is —COR23 or a carboxy, sulfinyl, sulfonyl, sulfonamide or amino acid derivative; R23 is haloalkyl; alkenyl; haloalkenyl; alkynyl; optionally substituted cycloalkyl; cycloalkyl-alkyl; aryl; arylalkyl; heteroaryl; heterocycloalkyl; or —COOH and/or —SO3H substituted alkyl; R1, R2, R3, R9, R10 and R11 are as defined in the specification; are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds.Type: GrantFiled: October 16, 2002Date of Patent: May 2, 2006Assignee: Schering CorporationInventors: Samuel Chackalamannil, Mariappan V. Chelliah, Martin C. Clasby, Yan Xia
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Patent number: 7022718Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and X are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.Type: GrantFiled: January 18, 2005Date of Patent: April 4, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Markus Boehringer, Bernd Michael Loeffler, Jens-Uwe Peters, Matthias Steger, Peter Weiss
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Patent number: 6989398Abstract: Benzanilides are provided which are voltage-dependent potassium channel openers. Methods of using the benzanilides of the invention are also provided.Type: GrantFiled: February 2, 2004Date of Patent: January 24, 2006Assignee: ICAgen, Inc.Inventors: Grant A. McNaughton-Smith, Michael F. Gross, Alan D. Wickenden
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Patent number: 6943182Abstract: The invention relates to cyclopentabenzofuran derivatives, process for their preparation, the use of cyclopentabenzofuran derivatives for the production of a medicament for the therapy of NF-?B-dependent diseases and medicaments which contain the cyclopentabenzofuran derivatives.Type: GrantFiled: May 30, 2002Date of Patent: September 13, 2005Assignee: Bayer AktiengesellschaftInventors: Walter Guarnieri, Thomas Jaetsch, Andreas Schoop, Jörg Baumgarten, Axel Kretschmer, Horst-Peter Antonicek
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Patent number: 6894065Abstract: Heterocyclic-substituted compounds of the formula or a pharmaceutically acceptable salt thereof, are disclosed, wherein: Z is —(CH2)n—; ?wherein R10 is absent; or ?wherein R3 is absent; the single dotted line represents an optional double bond; the double dotted line represents an optional single bond; n is 0-2; Het is an optionally substituted mono-, bi- or tricyclic heteroaromatic group; B is —(CH2)n3—, wherein n3 is 0-5, —CH2—O—, —CH2S—, —CH2—NR6—, —C(O)NR6—, —NR6C(O)—, ?optionally substituted alkenyl or optionally substituted alkynyl; X is —O— or —NR6— when the double dotted line represents a single bond, or X is H, —OH or —NHR20 when the bond is absent; Y is ?O, ?S, (H, H), (H, OH) or (H, C1-C6 alkoxy) when the double dotted line represents a single bond, or when the bond is absent, Y is ?O, ?NOR17, (H, H), (H, OH), (H, SH), (H, C1-C6 alkoxy) or (H, substituted-amino); R22 and R23 are independently —OH, —OC(O)R30, OC(O)NR30R31, or optionally substituted alkyl, alkenyl, alkynyl, heterocType: GrantFiled: June 9, 2003Date of Patent: May 17, 2005Assignee: Schering CorporationInventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yan Xia
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Patent number: 6881733Abstract: The present invention provides serotonergic benzofurans of Formula (I): where A, R, R1, R2, R3, and R4 are as described in the specification.Type: GrantFiled: July 21, 2000Date of Patent: April 19, 2005Assignee: Eli Lilly and CompanyInventors: Karin Briner, Joseph Paul Burkhart, Timothy Paul Burkholder, Brian Eugene Cunningham, Matthew Joseph Fisher, William Harlan Gritton, Cynthia Darshini Jesudason, Shawn Christopher Miller, Jeffrey Thomas Mullaney, Matthew Robert Reinhard, Roger Ryan Rothhaar, Freddie Craig Stevens, Leonard Larry Winneroski, Yanping Xu, Yao-Chang Xu
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Patent number: 6881743Abstract: Selective MMP-13 inhibitors are pyridine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: R1 and R2 independently are hydrogen, halo, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, NO2, NR4R5, CN, or CF3, E is independently O or S; A and B independently are OR4 or NR4R5; R4 and R5 independently are H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted, n is an integer of from 0 to 6.Type: GrantFiled: February 8, 2002Date of Patent: April 19, 2005Assignee: Warner-Lambert CompanyInventors: Nicole Chantel Barvian, David Thomas Connor, Patrick Michael O'Brien, Daniel Fred Ortwine, William Chester Patt, Kevon Ray Shuler, Michael William Wilson
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Patent number: 6858632Abstract: Novel derivatives of isosorbide mononitrate and its pharmaceutically acceptable salts, which have vasodilating activity with a reduced effect of tolerance, of the general formula (I) in which A and B independently represent any of the groups —ONO2 and —Z—CO—R, wherein Z is an oxygen atom or sulphur atom and R is an alkyl C1-C4 group, an aryl group or an aralkyl group, eventually substituted, or the group in which R1 is hydrogen, or an alkyl C1-C4 group, an aryl group or an aralkyl group, eventually substituted, with the proviso that one of A or B is always —ONO2, but never both of them at the same time, when Z is an sulphur atom R is an alkyl C1-C4 group, an aryl group or an aralkyl group, eventually substituted, and when Z is an oxygen atom R is the groupType: GrantFiled: April 28, 2003Date of Patent: February 22, 2005Assignee: Lacer, S.A.Inventors: Jose Repolles Moliner, Francisco Pubill Coy, Lydia Cabeza Llorente, Marcel.li Carbo Banus, Cristina Negrie Rofes, Juan Antonio Cerda Riudavets, Alicia Ferrer Siso, Marek W. Radomski, Eduardo Perez-Rasilla, Juan Martinez Bonnin
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Patent number: 6855822Abstract: Benzo[b]furan dimers and processes for their preparation are provided. The invention provides a synthetic process for the preparation of benzo[b]furan dimer using mild reaction conditions, which provides a high substituent tolerance and is appropriate for use in solid phase syntheses for producing a library of benzo[b]furan dimers for biological screening.Type: GrantFiled: June 23, 2003Date of Patent: February 15, 2005Assignee: VivoQuest, Inc.Inventors: Yun Liao, Reza Fathi, Zhen Yang
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Patent number: 6846819Abstract: Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.Type: GrantFiled: October 6, 2000Date of Patent: January 25, 2005Assignee: Affinium Pharmaceuticals, Inc.Inventors: William H. Miller, Kenneth A. Newlander, Mark A. Seefeld, Irene N. Uzinskas, Walter E. DeWolf, Jr., Dalia R. Jakas
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Patent number: 6846817Abstract: The invention provides nicotine receptor agonists of formula I: wherein R1, x, y, and n have any of the values given in the specification, or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions comprising such a compound or salt, methods for preparing such a compound or salt, and methods for modulating (e.g. antagonizing or activating) nicotine receptors with such a compound or salt.Type: GrantFiled: November 30, 2001Date of Patent: January 25, 2005Assignee: Regents of the University of MinnesotaInventor: S. Mbua Ngale Efange
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Patent number: 6828333Abstract: This application is directed to compounds of the formula wherein j is 1; k is 0 or 1; m is 1, 2 or 3; n is 1 or 2; W1 and W2 are independently —O— or —S(═O)t—, where t is 0, 1, or 2; Y is ═C(R1a)—, where R1a is a member selected from the group consisting of H; F; Cl; CN; NO2; —(C1-C4) alkyl; —(C2-C4) alkynyl; fluorinated-(C1-C3) alkyl; fluorinated-(C1-C3) alkoxy; —OR16; and —C(═O)NR22aR22b; R22a and R22b are defined as set forth in the specification; —RA and RB are each a member independently selected from the group consisting of H; F; CF3; —(C1-C4) alkyl; —(C3-C7) cycloalkyl; phenyl; and benzyl; wherein said cycloalkyl, phenyl, and benzyl moieties are each independently substituted with 0 to 3 substituents R10, which is defined as set forth in the specification; R16 and R17 are defined as set forth in the specification; —RC and RD have the same meaning as defined above for RA and RB except that oneType: GrantFiled: January 31, 2002Date of Patent: December 7, 2004Assignee: Pfizer Inc.Inventors: Anthony Marfat, Robert J. Chambers, Thomas V. Magee
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Publication number: 20040235852Abstract: Compounds of Formula I are useful for inhibiting serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein and have improved pharmacokinetic properties. These compounds may be used in methods of preventing and/or treating clotting disorders.Type: ApplicationFiled: May 19, 2004Publication date: November 25, 2004Inventors: Alan G. Olivero, Daniel P. Sutherlin
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Patent number: 6794392Abstract: The novel benzamide derivative represented by formula (1) and the novel anilide derivative represented by formula (13) of this invention has differentiation-inducing effect, and are, therefore, useful a therapeutic or improving agent for malignant tumors, autoimmune diseases, dermatologic diseases and parasitism. In particular, they are highly effective as an anticancer drug, specifically to a hematologic malignancy and a solid carcinoma.Type: GrantFiled: October 13, 1999Date of Patent: September 21, 2004Assignee: Schering AktiengesellschaftInventors: Tsuneji Suzuki, Tomoyuki Ando, Katsutoshi Tsuchiya, Osamu Nakanishi, Akiko Saito, Takashi Yamashita, Yoshinori Shiraishi, Eishi Tanaka
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Publication number: 20040176418Abstract: A crystalline polymorph of a bislulfate salt of a thrombin receptor antagonist compound, which exhibits a powder x-ray diffraction profile substantially the same as that shown in FIG. 1, or which exhibits a differential scanning calorimtery profile substantially the same as that shown in FIG.Type: ApplicationFiled: January 9, 2004Publication date: September 9, 2004Applicant: Schering CorporationInventors: Tiruvettipuram K. Thiruvengadam, Wenxue Wu, Tao Wang, John S. Chiu, Susan Bogdanowich-Knipp, Anastasia Pavlovsky, William J. Greenlee, Michael P. Graziano, Teddy Kosoglou, Madhu Chintala, Samuel Chackalamannil
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Publication number: 20040162318Abstract: The present invention relates to novel benzofuran derivatives and analogs, as well as compositions containing the same and to the use thereof for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the hepatitis C virus.Type: ApplicationFiled: October 31, 2003Publication date: August 19, 2004Inventors: Ashis K. Saha, Christopher J. Burns, Alfred M. Del Vecchio, Thomas R. Bailey, Jason A. Reinhardt, Bheemashankar A. Kulkarni, Thomas H. Faitg, Hao Feng, Susan R. Rippin, Charles W. Blackledge, David J. Rys, Thomas A. Lessen, John Swestock, Yijun Deng, Theodore J. Nitz
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Publication number: 20040152902Abstract: PDE4 inhibition is achieved by novel nitroxide compounds, e.g., N-substituted aniline and diphenylamine analogs.Type: ApplicationFiled: November 19, 2003Publication date: August 5, 2004Inventors: Richard A. Schumacher, Elizabeth Doorly Graham, Allen T. Hopper, Ashok Tehim
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Publication number: 20040138265Abstract: The invention concerns novel carboxamides of formula (I) wherein A is (A1), (A2), (A3), (A4), (A5); Q is (Q1), (Q2), (Q3), (Q4), (Q5), (Q6); R1 is CH2 R2, CH2CH═CHR2, CH═C═CHR2 or COR3; R2 is hydrogen, C1-C6alkyl, C1-C6haloalkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C7cycloalkyl, COOC1-C4alkyl, COOC3-C6alkenyl, COOC3-C6alkynyl or CN; R3 is C1-C6alkyl, C1-C6alkyl substituted by halogen, C1-C6alkoxy or C1-C6haloalkoxy; or is C1-C6alkylthio, C1-C6haloalkylthio, C1-C6alkoxy, C1-C6haloalkoxy; C3-C6alkenyloxy or C3-C6haloalkenyloxy; C3-C6haloalkenyloxy; C3-C6alkynyloxy or C3-C6haloalkynyloxy; R4 is methyl, CF2Cl, CF3, CF2H, CFH2, Cl or Br, R5 is methyl, CF3, CH2OCH3 or CH2OCF3; R6 is hydrogen, fluoro, CF3 or methyl; R7 is hydrogen, methyl or halogen; and Z is phenyl, halophenyl, C5-C7cycloalkyl, C5-C7acycloalkyl substituted by C1-C3alkyl, C1C3haloalkyl or halogen, or a group of the form —CHR8—CH2—CHR9R10 wherein R8, R9 and R10 are independently of each other C1-C3alkyl.Type: ApplicationFiled: January 12, 2004Publication date: July 15, 2004Inventors: Harald Walter, Stephan Trah
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Publication number: 20040110949Abstract: Benzo[b]furan dimers and processes for their preparation are provided. The invention provides a synthetic process for the preparation of benzo[b]furan dimer using mild reaction conditions, which provides a high substituent tolerance and is appropriate for use in solid phase syntheses for producing a library of benzo[b]furan dimers for biological screening.Type: ApplicationFiled: June 23, 2003Publication date: June 10, 2004Inventors: Yun Liao, Reza Fathi, Zhen Yang
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Publication number: 20040102480Abstract: This invention provides compounds of Formula I having the structure 1Type: ApplicationFiled: November 21, 2002Publication date: May 27, 2004Applicant: WyethInventors: Michael S. Malamas, Jay E. Wrobel, Arlene J. Dietrich, Zenan Li, Iwan Gunawan
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Publication number: 20040087625Abstract: The invention relates to triamide MTP/ApoB inhibitors of the formula 1 1Type: ApplicationFiled: August 13, 2003Publication date: May 6, 2004Applicant: Pfizer IncInventors: Peter Bertinato, Brian S. Bronk, Alan E. Blize, Hengmiao Cheng, Jin Li, Hiep Huatan, Clive Mason
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Patent number: 6720423Abstract: Compounds of the formula where the variables have the meaning defined in the specification, are specific or selective agonists of RXR retinoid receptors.Type: GrantFiled: April 30, 2002Date of Patent: April 13, 2004Assignee: Allergan, Inc.Inventors: Jayasree Vasudevan, Dehua Huang, Vidyasagar Vuligonda, Roshanta S. Chandraratna
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Patent number: 6706882Abstract: A process for the preparation of (pyridinylidene)-phthalides starting from 3-oxo-1,3-dihydro-isobenzofuran-1-carboxylic acids and pyridinecarbaldehydes, is described.Type: GrantFiled: October 16, 2001Date of Patent: March 16, 2004Assignee: Zambon Group S.p.A.Inventor: Mauro Napoletano