Additional Hetero Ring Attached Directly Or Indirectly To The Purine Ring System By Nonionic Bonding Patents (Class 514/263.2)
-
Publication number: 20080214580Abstract: The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.Type: ApplicationFiled: October 4, 2007Publication date: September 4, 2008Applicant: PHARMACOPEIA, INC.Inventors: Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Nasrin Ansari
-
Publication number: 20080214581Abstract: A compound of formula (I): wherein R1-R3 are as defined in the specification, and compositions, combinations, and methods of manufacture, and methods of treatment of inflammatory diseases, using the same.Type: ApplicationFiled: July 17, 2006Publication date: September 4, 2008Inventors: David George Allen, Michael David Barker, Richard Peter Charles Cousins
-
Publication number: 20080207647Abstract: Compounds of the formula (I), in which R, X, R1, R2, R3 and R4 have the meanings indicated in Claim (1), are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: July 24, 2006Publication date: August 28, 2008Applicant: Merck Patent GmbHInventors: Guenter Hoelzemann, Helene Crassier, Wilfried Rautenberg
-
Publication number: 20080200456Abstract: The present invention provides compounds and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.Type: ApplicationFiled: December 14, 2007Publication date: August 21, 2008Inventors: Guoquan Wang, Jayson M. Rieger, Robert D. Thompson
-
Publication number: 20080194593Abstract: Disclosed are methods for treating asthma, inflammatory gastrointestinal tract disorders, cancer, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis using A2B adenosine receptor antagonists having the structure of Formula I or Formula II:Type: ApplicationFiled: January 11, 2008Publication date: August 14, 2008Inventors: Rao Kalla, Thao Perry, Elfatih Elzein, Xiaofen Li, Jeff Zablocki, Dewan Zeng, Dengming Xiao, Vaibhav Varkhedkar, Prabha Ibrahim, Venkata Palle, Hongyan Zhong
-
Patent number: 7407955Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are defined as in claims 1 to 16, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: August 12, 2003Date of Patent: August 5, 2008Assignee: Boehringer Ingelheim Pharma GmbH & Co., KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Michael Mark, Roland Maier, Ralf R. H. Lotz, Mohammad Tadayyon
-
Publication number: 20080176872Abstract: This invention relates to novel compounds having the formula (I); and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.Type: ApplicationFiled: February 15, 2006Publication date: July 24, 2008Applicant: ASTRAZENECA ABInventors: Michelle Lamb, Tao Wang, Dingwei Yu, Peter Mohr, Bin Wang
-
Publication number: 20080176840Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.Type: ApplicationFiled: May 25, 2007Publication date: July 24, 2008Inventors: Lijun Sun, Weiwen Ying, Junghyun Chae, Teresa Przewloka, Shijie Zhang, Dinesh U. Chimmanamada, Kevin Foley, Zhenjian Du, Hao Li, David James, Howard P. Ng, Zachary Demko, Dan Zhou, Shuzhen Qin
-
Publication number: 20080153856Abstract: Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.Type: ApplicationFiled: December 3, 2007Publication date: June 26, 2008Inventors: Rao Kalla, Thao Perry, Elfatih Elzein, Vaibhav Varkhedkar, Xiaofen Li, Prabha Ibrahim, Venkata Palle, Dengming Xiao, Jeff Zablocki
-
Patent number: 7388002Abstract: Compounds represented by the formula: A is (CH2)nR2, —CH?CH2, CH2—CH?CH2, O(CH2)nR2, CH(OH)CH3, CH(OH)CH2OH, CH2—CH(OH)CH3, CH2CH(OH)CH2OH, or CH(OH)CH(OH)CH3, R,R1 individually is H, NH2OH, Cl, Br, I, aryl, substituted aryl, heterocycle, NR3R4, OR3 or SR3, R2 is H, OH, F, N3, NH2, CO2H, SH, alkyl, substituted alkyl, S-alkyl, O-acyl, CONH2, or CONH-alkyl, n is 1-3, y is O, S or NH, W is O or S, Z, Z? individually is OR3, OR4, O(CH2)m—O—(CH2)xCH3, NH—CH(alkyl)CO2R3, alkyl, substituted alkyl, OCH2CH2S—C(O)CH3, OCH2CH2S—C(O)CH(CH3)2, OCH2CH2S—C(O)C(CH3)3, OCH2CH2—SC(O)aryl, OCH2CH2—S—S—OCH2CH2OH, OCH2OC(O)C(CH3)3, OCH2—O—C(O)OCH(CH3)2, or OCH2—O—C(O)CH(CH3)2 R3, R4 individually is H, alkyl, substituted alkyl, aryl, or substituted aryl; Both R3 and R4 can form a monocyclic ring of 4-7 atoms with N or optionally a further heteroatom in the ring; m is 1-3, x is 0-19; and pharmaceutically acceptable salts thereof and prodrugs thereof are provided.Type: GrantFiled: November 9, 2005Date of Patent: June 17, 2008Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, Pooran Chand, Yahya El-Kattan, Minwan Wu
-
Publication number: 20080108636Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.Type: ApplicationFiled: December 28, 2006Publication date: May 8, 2008Applicant: PHARMACYCLICS, INC.Inventors: Lee Honigberg, Erik Verner, Zhengying Pan
-
Patent number: 7358235Abstract: Analogs or derivatives of nitrobenzylthioinosine compounds. The use of these new analogs of nitrobenzylthioinosine and methods for the treatment of pain and various other indications using these analogs of nitrobenzylthioinosine as well as pharmaceutical compositions including analogs of nitrobenzylthioinosine.Type: GrantFiled: October 6, 2004Date of Patent: April 15, 2008Assignees: Gruenenthal GmbH, Leiden UniversityInventors: Claudia Puetz, Corinna Sundermann, Bernd Sundermann, Adriaan Pieter Ijzerman, Reynier Tromp, Jacobien Von Frijtag Drabbe Kuenzel
-
Publication number: 20080085909Abstract: A chemical genus of purinones and 1H-imidazopyridinones, which are useful as PKC? inhibitors, and their methods of use are disclosed.Type: ApplicationFiled: February 2, 2007Publication date: April 10, 2008Applicant: Pharmacopeia Drug Discovery, Inc.Inventors: Andrew Roughton, Yajing Rong, Koc Kan Ho, Michael Ohlmeyer, David Diller
-
Patent number: 7342006Abstract: Selective antagonists of A2B adenosine receptors like those of formula I are provide. The compounds and compositions are useful as pharmaceutical agents.Type: GrantFiled: August 20, 2004Date of Patent: March 11, 2008Assignee: Adenosine Therapeutics, LLCInventors: Guoquan Wang, Jayson M. Rieger, Robert D. Thompson
-
Patent number: 7335655Abstract: The present invention relates generally to compounds of formula (I): wherein X is a five or six-membered heteroaromatic ring, containing one to four heteroatoms, selected from nitrogen, oxygen, or sulfur, provided that at least one heteroatom is nitrogen; and G1 and G2 are independently CH or N. The present invention also relates to the preparation of the compounds, pharmaceutical formulations thereof, and their use in medicine as potent or selective A2B adenosine receptor antagonists and their uses for treating asthma, autoimmune diseases and retinal vascular diseases.Type: GrantFiled: February 22, 2006Date of Patent: February 26, 2008Assignee: King Pharmaceuticals Research and Development, Inc.Inventors: Pier Giovanni Baraldi, Pier A. Borea
-
Patent number: 7335654Abstract: PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein.Type: GrantFiled: August 8, 2003Date of Patent: February 26, 2008Assignee: Memory Pharmaceuticals CorporationInventors: Allen T. Hopper, Ruiping Liu
-
Publication number: 20080045549Abstract: The present invention provides compounds of the formula which are adenosine A2B receptor antagonists and, thus, may be employed for the treatment of conditions and diseases mediated by the adenosine A2B receptor activity. Such conditions include, but are not limited to, chronic and acute inflammatory diseases involving degranulation of mast cells, e.g., asthma, allergic rhinitis and allergic dermatitis; impaired sensitivity to insulin, e.g., type 2 diabetes, non-insulin dependent diabetes, pre-diabetic state, and impaired glucose tolerance; diseases in which angiogenesis is a key component of pathogenesis, e.g., solid tumors and angiogenic retinopathies; apnea of preterm infants; myocardial reperfusion injury; inflammatory bowel disease; autoimmune diseases, such as rheumatoid arthritis, multiple sclerosis, and lupus erythematosis; diseases involving microvascular abnormalities of the retina that are mediated by adenosine A2B receptors, e.g.Type: ApplicationFiled: June 25, 2007Publication date: February 21, 2008Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Allan Moorman, Mojgan Aghazadeh Tabrizi
-
Patent number: 7317017Abstract: Disclosed are novel A2B adenosine receptor antagonists having the structure of Formula I or Formula II The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract disorders, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis.Type: GrantFiled: July 25, 2005Date of Patent: January 8, 2008Assignee: CV Therapeutics, Inc.Inventors: Rao Kalla, Thao Perry, Elfatih Elzein, Vaibhav Varkhedkar, Xiaofen Li, Prabha Ibrahim, Venkata Palle, Dengming Xiao, Jeff Zablocki
-
Patent number: 7304070Abstract: Disclosed are novel A2B adenosine receptor antagonists having the structure of Formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract disorders, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis.Type: GrantFiled: September 16, 2004Date of Patent: December 4, 2007Assignee: CV Therapeutics, Inc.Inventors: Rao Kalla, Thao Perry, Elfatih Elzein, Vaibhav Varkhedkar, Xiaofen Li, Prabha Ibrahim, Venkata Palle, Dengming Xiao, Jeff Zablocki
-
Publication number: 20070270440Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.Type: ApplicationFiled: May 18, 2007Publication date: November 22, 2007Applicant: WyethInventors: Derek Cecil Cole, Magda Asselin, Joseph Raymond Stock, Jin-In Kim
-
Patent number: 7262176Abstract: Disclosed are novel compounds that are A3 adenosine receptor agonists, useful for treating various disease states, including cancer, cardiac ischemia, leukopenia, and neutropennia.Type: GrantFiled: November 25, 2003Date of Patent: August 28, 2007Assignee: CV Therapeutics, Inc.Inventors: Elfatih Elzein, Venkata Palle, Vaibhav Varkhedkar, Jeff Zablocki
-
Patent number: 7259159Abstract: The present invention relates to acylguanidino derivatives of formula (I), in which R1, R2, R3, A, B, X, Y and n have the meanings indicated in claim 1, their physiologically tolerable salts and their prodrugs. The compounds of the formula (I) are valuable pharmaceutically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion and bone resorption by osteoclasts. This renders them suitable, for example, for the therapy and prophylaxis of illness which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or proliferation of cells of the vascular smooth muscles.Type: GrantFiled: July 23, 2001Date of Patent: August 21, 2007Assignees: Sanofi-Aventis Deutschland GmbH, Genentech Inc.Inventors: Anuschirwan Peyman, David Will, Thomas R Gadek, Robert McDowell, Jean Francois Gourvest, Jean-Marie Ruxer, Jochen Knolle
-
Patent number: 7253176Abstract: The invention relates to a novel use of 8-substituted xanthine derivatives for the manufacture of a medicament for the treatment of auto-immuno disorders.Type: GrantFiled: May 4, 2000Date of Patent: August 7, 2007Assignee: K.U. Leuven Research & DevelopmentInventors: Mark Jozef Albert Waer, Piet André´ M. M. Herdewijn, Wolfgang Eugen Pfleiderer
-
Patent number: 7247639Abstract: The present invention provides novel adenosine receptor antagonists, more particularly, A1 adenosine receptor antagonists of formula (I). Pharmaceutical compositions comprising an A1 adenosine receptor antagonist of formula (I) and a pharmaceutically acceptable carrier are further provided. Compositions also include diagnostic assay-type probes comprising a novel A1 adenosine receptor antagonist of formula (I) that is labeled or conjugated with radioactive or non-radioactive material. Methods for treating A1 adenosine receptor related disorders comprising administering an A1 adenosine receptor antagonist of formula (I) are also disclosed. The novel A1 adenosine receptor antagonist compositions of formula (I) find further use in diagnostic and imaging methods. wherein R3 is Alk14ArR16, and wherein Alk14 is C1-8 straight or branched alkylene or alkenylene.Type: GrantFiled: June 4, 2004Date of Patent: July 24, 2007Assignee: Endacea, Inc.Inventors: Constance N. Wilson, John J. Partridge
-
Patent number: 7235538Abstract: The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV, which are of formula I wherein each n is one or two independently and R1, R2, R3, R6, R7, R9, and R10 are defined herein. The present invention also relates to pharmaceutical compositions comprising the compounds of formula I and the use of the compounds for treating diseases that are associated with proteins that are subject to inactivation by DPP-IV, such as type-2 diabetes and obesity.Type: GrantFiled: July 17, 2003Date of Patent: June 26, 2007Assignee: Novo Nordisk A/SInventors: Anders Bendtz Kanstrup, Lise Brown Christiansen, Jane Marie Lundbeck, Christian K. Sams, Marit Kristiansen
-
Patent number: 7217702Abstract: Selective antagonists of A2A adenosine receptors like those of formula I are provided, wherein Y forms a ring. The novel A2A blockers are useful for the treatment of Parkinsons disease and other diseases.Type: GrantFiled: April 4, 2005Date of Patent: May 15, 2007Assignee: Adenosine Therapeutics, LLCInventors: Anthony Beauglehole, Jayson M. Rieger, Robert D. Thompson
-
Patent number: 7217716Abstract: Compounds represented by Formula (I): (I) or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving painType: GrantFiled: February 20, 2002Date of Patent: May 15, 2007Assignee: Merck & Co., Inc.Inventors: Christopher F. Claiborne, David A. Claremon, Brian E. Libby, John W. Butcher, John A. McCauley, Nigel J. Liverton, Peter M. Munson, Kevin T. Nguyen, Brian Phillips, Wayne Thompson
-
Patent number: 7202252Abstract: Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described.Type: GrantFiled: February 17, 2004Date of Patent: April 10, 2007Assignee: Endacea, Inc.Inventors: Constance Neely Wilson, John J. Partridge
-
Patent number: 7192952Abstract: The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV of formula I, pharmaceutical compositions comprising the compounds and the use of such compounds for and the manufacture of medicaments for treating diseases that are associated with proteins that are subject to inactivation by DPP-IV, such as type 2 diabetes and obesityType: GrantFiled: March 2, 2005Date of Patent: March 20, 2007Assignee: Novo Nordisk, A/SInventors: Anders Bendtz Kanstrup, Christian Klarner Sams, Jane Marie Lundbeck, Lise Brown Christiansen, Marit Kristiansen
-
Patent number: 7157465Abstract: This invention relates to an adenine derivative, a tautomer thereof, or a pharmaceutically acceptable salt thereof represented by general formula (I): wherein X represents NR3 (wherein R3 represents a hydrogen atom or C1-3 alkyl) or the like; R1 represents substituted or unsubstituted alkyl or the like; R2 represents hydroxyl or the like; and Y represents a substituted or unsubstituted aromatic hetero ring or the like. Also, the present invention relates to pharmaceuticals such as an interferon inducer, antiviral agent, anticancer agent, type 2 helper T cell selective immune response inhibitor, antiallergic agent, and immune response modulator comprising the above derivative as an active ingredient.Type: GrantFiled: April 15, 2002Date of Patent: January 2, 2007Assignee: Dainippon Simitomo Pharma Co., Ltd.Inventors: Yoshiaki Isobe, Haruhisa Ogita, Masanori Tobe, Haruo Takaku, Tetsuhiro Ogino, Ayumu Kurimoto, Hajime Kawakami
-
Patent number: 7148229Abstract: The present invention is a sulfonamide substituted xanthine derivative of formula I: or a pharmaceutically acceptable salt thereof, wherein R1 is lower alkyl, lower alkyl substituted by phenyl, or lower alkyl substituted by halogen substituted phenyl; R2 is lower alkyl or lower alkyl substituted by lower cycloalkyl; and R3 is: Compounds of formula I and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.Type: GrantFiled: February 11, 2004Date of Patent: December 12, 2006Assignee: Hoffman-La Roche Inc.Inventors: Peter W. Dunten, Louise H. Foley, Nicholas J. S. Huby, Sherrie L. Pietranico-Cole, Weiya Yun
-
Patent number: 7135475Abstract: The present invention is a 1,3,8 substituted xanthine derivative of formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are as defined in the specification. Compounds of formula I and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.Type: GrantFiled: June 12, 2003Date of Patent: November 14, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Peter W. Dunten, Louise H. Foley, Nicholas J. S. Huby, Sherrie L. Pietranico-Cole, Weiya Yun
-
Patent number: 7129239Abstract: Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein. wherein A is an optionally substituted aryl or an optionally substituted heteroaryl; B is an optionally substituted aryl or an optionally substituted heteroaryl; R1 is hydrogen, (C1–C4)alkyl, halo-substituted (C1–C4)alkyl, or (C1–C4)alkoxy; and R4 is as described herein.Type: GrantFiled: October 20, 2003Date of Patent: October 31, 2006Assignee: Pfizer Inc.Inventor: David A. Griffith
-
Patent number: 7115739Abstract: This invention describes novel triazole compounds of formula IX: wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least one of Z1 and Z2 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from —R1; Ring D is a 5–7 membered monocyclic ring or 8–10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or Rx and Ry are taken together with their intervening atoms to form a fused ring; R1, R3, and T are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3 and Aurora, for treating diseases such as diabetes, cancer, and Alzheimer's disease.Type: GrantFiled: September 14, 2001Date of Patent: October 3, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Ronald Knegtel, Hayley Binch, Julian M. C. Golec, Pan Li, Jean-Damien Charier
-
Patent number: 7074798Abstract: The present invention provides novel compounds exhibiting an excellent DPPIV inhibition effect. The compounds are represented by the formula: wherein, m is 0 or 1; n is 0; R31, R32, R33, R34, R35, R36, R37, R38, R39, R40, R41, and R42 each represent a hydrogen atom; X represents an alkynyl group, an aryl group, and such, which group may be substituted; and, R1 and R2 each independently represents a hydrogen atom, an alkyl group, an alkoxyl group, or such, or salts or hydrates thereof.Type: GrantFiled: February 24, 2003Date of Patent: July 11, 2006Assignee: Eisai Co., LtdInventors: Seiji Yoshikawa, Eita Emori, Fumiyoshi Matsuura, Richard Clark, Hironori Ikuta, Nobuyuki Yasuda, Tadashi Nagakura, Kazuto Yamazaki, Mika Aoki
-
Patent number: 7053096Abstract: Disclosed are compounds having selective hydrolytic potential. The disclosed compounds are useful as compounds having selective stability and are capable of undergoing programmed hydrolysis in biologic systems.Type: GrantFiled: May 5, 2004Date of Patent: May 30, 2006Assignee: Cell Therapeutics Inc.Inventors: David Porubek, Anil M. Kumar, Charles R. Bredl, J. Peter Klein
-
Patent number: 7037918Abstract: New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.Type: GrantFiled: December 3, 2002Date of Patent: May 2, 2006Assignee: Chiron CorporationInventors: John M. Nuss, Stephen D. Harrison, David B. Ring, Rustum S. Boyce, Sean P. Brown, Dane A. Goff, Kirk W. Johnson, Keith B. Pfister, Savithri Ramurthy, Paul A. Renhowe, Lynn Seely, Sharadha Subramanian, Allan S. Wagman, Xiaohui A. Zhou
-
Patent number: 7022710Abstract: Disclosed are novel methods of antagonizing the A1 adenosine receptor in a mammal, comprising administering to a mammal in need thereof a therapeutically effective dose of a compound of the formula: wherein R1 is optionally substituted C1-14 alkyl; Y is C1-14 alkylene; and Z is phenyl that is optionally substituted with halo, hydroxy, amino, cyano, or optionally substituted C1-4 alkyl or a pharmaceutically acceptable salt, ester, or prodrug thereof. The A1 adenosine receptors are antagonized in order to treat a disease state is chosen from renal failure, renal dysfunction, nephritis, hypertension, edema, Alzheimers disease, stress, depression, cardiac arrhythmia, restoration of cardiac function, congestive heart failure, diabetes, asthma, respiratory disorders, ischemia-induced injury of the brain, heart and kidney, and diarrhea.Type: GrantFiled: July 22, 2004Date of Patent: April 4, 2006Assignee: CV Therapeutics, Inc.Inventors: Jeff Zablocki, Rao Kalla, Dewan Zeng
-
Patent number: 7005425Abstract: Methods are provided for treating arrhythmia in a manner that minimizes undesirable side effects, comprising administration of a therapeutically effective minimal dose of an A1 adenosine receptor agonist with a therapeutically effective minimal dose of a beta blocker, calcium channel blocker, or a cardiac glycoside.Type: GrantFiled: April 18, 2003Date of Patent: February 28, 2006Assignee: CV Therapeutics, Inc.Inventors: Luiz Belardinelli, Arvinder Dhalla
-
Patent number: 7001910Abstract: The present invention refers to compounds of the general formula (I), to their possible pharmaceutically acceptable salts and tautomeric forms. The present invention also refers to a process for their production and to their use as antidiabetic and *hypoglycemic agents, alone or in combination with other antidiabetic agents, such as sulfonilureas or biguanides, as well as for the treatment of complications associated to the resistance to the insulin, such as hypertension, hyperuricemia or other cardiovascular, metabolic, endocrine conditions, or other conditions related with diabetes.Type: GrantFiled: November 15, 2000Date of Patent: February 21, 2006Assignee: Vita-Invest S.A.Inventors: Marisabel Mourelle Mancini, Juan Carlos Del Castillo Nieto, Elisabet De Ramon Amat
-
Patent number: 6969720Abstract: The compounds of the present invention are 2,6,9-trisubstituted purine derivatives which are inhibitors of cyclin/cdk complexes. The compounds of the current invention also are potent inhibitors of human cellular proliferation. As such, the compounds of the present invention constitute pharmaceutical compositions with a pharmaceutically acceptable carrier. Such compounds are useful in treating a disorder mediated by elevated levels of cell proliferation in a mammal compared to a healthy mammal by administering to such mammal an effective amount of the compound. Examples of the compounds of the present invention are represented by the following chemical structures: wherein: X=N; V=NH; O; S; or CH2; A=CH2; (CH2)2; (CH2)3; OCH2CH2; or CHCH3; and Y, R1, R2, R3, R4, and n1 are defined herein.Type: GrantFiled: September 11, 2001Date of Patent: November 29, 2005Assignee: AMR Technology, Inc.Inventor: Michael Peter Trova
-
Patent number: 6949559Abstract: The compounds of the present invention are 2,6,9-trisubstituted purine derivatives which are inhibitors of cyclin/cdk complexes. The compounds of the current invention also are potent inhibitors of human cellular proliferation. As such, the compounds of the present invention constitute pharmaceutical compositions with a pharmaceutically acceptable carrier. Such compounds are useful in treating a disorder mediated by elevated levels of cell proliferation in a mammal compared to a healthy mammal by administering to such mammal an effective amount of the compound. Examples of the compounds of the present invention are represented by the following chemical structures: with X, Y, D, Q, V, A, R1, R2, R3, R4, and n1 defined herein.Type: GrantFiled: October 7, 2003Date of Patent: September 27, 2005Assignee: AMR Technology, Inc.Inventor: Michael Peter Trova
-
Patent number: 6936618Abstract: The use of a type V cyclic nucleotide phosphodiesterase inhibitor for the preparation of a medicament for the treatment of cystic fibrosis.Type: GrantFiled: March 24, 2003Date of Patent: August 30, 2005Assignee: University of Wales College of MedicineInventors: Robert Leslie Dormer, Margaret Ann McPherson
-
Patent number: 6926763Abstract: The invention features compounds of the formula: or a pharmaceutically acceptable salt thereof, wherein A is CR2 and B is N; wherein n is 0-3; wherein R1 is (CH2)m—{(G)o—(CH2)p}q—L, in which G is CH2, CH?CH, C?C, CO, O, S, or NR5, where R5 is H or C1-6 alkyl, CHR6, where R6 is OH or C1-6 alkyl, CH(CR7R8), where each of R7 and R8 is, independently, H, halo, or C1-6 alkyl, OCO, CONR9, NR10CO, where each of R9 and R10 is, independently, H or C1-6 alkyl, SO2NH, or NHSO2; in which m is 1-4, o is 0-4, p is 0-4, and q is 0-4. The compounds disclosed herein have potent anti-microbial, e.g., both Gram-positive and Gram-negative anti-bacterial properties. The compounds inhibit DNA polymerase IIIC and DNA polymerase IIIE enzymes and thus act therapeutically by inhibiting the growth of a broad array of bacteria. The compounds can be administered to prevent or to treat Gram-positive or Gram-negative bacterial infections, e.g., in eukaryotic cell cultures, animals, or humans.Type: GrantFiled: February 10, 2003Date of Patent: August 9, 2005Assignee: GLSynthesis, Inc.Inventors: George E. Wright, Wei-Chu Xu, Neal C. Brown
-
Patent number: 6900315Abstract: The present invention relates to novel compounds, compositions and methods for inhibiting the growth, elaboration and/or replication of HIV in human patients and to the prevention and treatment of human acquired immunodeficiency syndrome (AIDS) and other diseases caused by retroviral infection. More particularly, in preferred aspects, the present invention provides a method for the use of novel prodrug forms of 9-(2,3-Dideoxy-?-D-glycero-pent-2-enofuranosyl) guanine (d4G) for the prevention and treatment of both wild type and drug-resistant Human Immunodeficiency Virus (HIV), the causative pathogen of AIDS. Compounds according to the present invention are based upon the chemical formula: where X is OCH3, N3, NHCH3, N(CH3)2 or an aminocyclopropyl group; R1 is H or a C1 to C20 acyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group; and R2 is H or a C1 to C20 acyl or alkyl group.Type: GrantFiled: February 5, 2002Date of Patent: May 31, 2005Assignees: Yale University, University of Georgia Research Foundation, Inc.Inventors: Karen S. Anderson, Adrian Staffin Ray, Chung K. Chu, Yang Zhenjun
-
Patent number: 6894021Abstract: This invention concerns methods for identifying A2B adenosine receptor agonists and antagonists as well as methods for using A2B adenosine receptor antagonists to treat cell proliferation orders mediated by the A2B adenosine receptor.Type: GrantFiled: February 16, 2001Date of Patent: May 17, 2005Assignees: CV Therapeutics, Inc., University of Florida Research FoundationInventors: Luiz Belardinelli, Maria B. Grant
-
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
-
Patent number: 6894054Abstract: Compounds, compositions, and methods for inhibiting the glycine transporter 2 and for inhibiting glycine transporter mediated neuronal activity. These compounds are particularly useful for treating diseases of the nerve and muscle, including psychoses, pain, epilepsy, neurodegenerative diseases, stroke, head trauma, multiple sclerosis and the like, and of muscle disorders, including diseases or conditions associated with increased muscle contraction, such as spasticity and myoclonus. In addition, the compounds may be used to discover other agents with improved activity in assays in which the compounds of the invention are active.Type: GrantFiled: February 5, 2002Date of Patent: May 17, 2005Assignee: Telik, Inc.Inventors: Edgardo Laborde, Hugo O. Villar
-
Patent number: 6894045Abstract: Compounds provided herein are novel substituted tetrahydropurinones of Formula (I): wherein R3 is aryl substituted with 0-5 XAr or heteroaryl substituted with 0-4 XhAr. Such compounds are particularly useful as CRF receptor ligands, and hence, in the treatment of various neurologically-related disorders such as affective disorder, anxiety and depression.Type: GrantFiled: July 10, 2002Date of Patent: May 17, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventor: Richard A. Hartz
-
Patent number: RE39112Abstract: The present invention provides a preventive or therapeutic agent of a new type for diabetes mellitus and diabetic complications on the basis of an adenosine A2 receptor antagonist action. A purine compound represented by the formula (I), its pharmacologically acceptable salt or hydrates thereof has an adenosine A2 receptor antagonistic action and is useful for prevention or therapy of diabetes mellitus and diabetic complications. In addition, adenosine A2 receptor antagonists having different structures from those of the compounds described above, for example KW6002, are also effective for prevention or therapy of diabetes mellitus and diabetic complications. In the formula, W is —CH2CH2—, or —CH?CH— or —C?C—; R1 is: (in the formula, X is hydrogen atom, hydroxyl group, a lower alkyl group, a lower alkoxy group, etc.; and R5 and R6 are the same as or different from each other and each represents hydrogen atom, a lower alkyl group, a cycloalkyl group, etc.) and the like; R2 is an amino group, etc.Type: GrantFiled: December 24, 1998Date of Patent: May 30, 2006Assignee: Eisai Co., Ltd.Inventors: Osamu Asano, Hitoshi Harada, Yorihisa Hoshino, Seiji Yoshikawa, Takashi Inoue, Tatsuo Horizoe, Nobuyuki Yasuda, Kaya Ohashi, Junsaku Nagaoka, Manabu Murakami, Seiichi Kobayashi