The Additional Hetero Ring Is Five-membered Consisting Of Carbon And Plural Nitrogens As The Only Ring Members Patents (Class 514/266.23)
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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
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Patent number: 7112590Abstract: The invention relates to compounds that are heterocyclic derivatives of dipeptides and dipeptides mimetics and pharmaceutically acceptable salts thereof.Type: GrantFiled: May 4, 2001Date of Patent: September 26, 2006Assignees: LEK Pharmaceuticals d.d., University of Ljubljana, Faculty of PharmacyInventors: Danijel Kikelj, Lucija Peterlin, Petra Marinko, Matej Breznik, Mojca Stregnar, Bakija Alenka Trampuz, Marjana Fortuna
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Patent number: 7105669Abstract: A compound of formula (I) or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2 or NR10 where R10 is hydrogen or C1-6 alkyl, and R1, R2, R3, R4, R5, R6, R7, R8 and R9 are various specified organic groups. These compounds are inhibitors of aurora 2 kinase, and are useful in the treatment of cancer.Type: GrantFiled: September 18, 2000Date of Patent: September 12, 2006Assignee: AstraZeneca ABInventors: Andrew Austen Mortlock, Nicholas John Keen
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Patent number: 7098330Abstract: This invention describes novel pyrazole compounds of formula III: wherein 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 taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5–8 membered carbocyclo ring; and R2 and R2? are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: GrantFiled: September 14, 2001Date of Patent: August 29, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Hayley Binch, Ronald Knegtel, Julian M. C. Golec, Sanjay Patel, Jean-Damien Charrier, David Kay, Robert J. Davies
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Patent number: 7074801Abstract: The present invention discloses compounds and compositions of formula (I): having inhibitory activity on activation of STAT6, wherein X represents quinoline, isoquinoline, quinazoline or imidazopyridine; Y represents phenyl, piperazine, pyridine, thiophene, thiazole, oxathiazole or oxathiadiazole; and variables Z, n, R1, R2, R3 and R4 are as defined in the claims.Type: GrantFiled: April 25, 2002Date of Patent: July 11, 2006Assignee: Eisai Co., Ltd.Inventors: Ichiro Yoshida, Naoki Yoneda, Yoshiaki Ohashi, Shuichi Suzuki, Mitsuaki Miyamoto, Futoshi Miyazaki, Hidenori Seshimo, Junichi Kamata, Yasutaka Takase, Manabu Shirato, Daiya Shimokubo, Yoshinori Sakuma, Hiromitsu Yokohama
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Patent number: 7074800Abstract: The invention relates to the use of compounds of formula (I), wherein ring C is an 8, 9, 10, 12 or 13-membered bicyclic or tricyclic moiety which optionally may contain 1–3 heteroatoms selected independently from O, N and S; Z is —O—, —NH—, —S—, —CH2— or a direct bond; n is 0–5; m is 0–3; R2 represents hydrogen, hydroxy, halogeno, cyano, nitro, trifluoromethyl, C1-3alkyl, C1-3alkoxy, C1-3alkylsulphanyl, —NR3R4 (wherein R3 and R4, which may be the same or different, each represents hydrogen or C1-3alkyl), or R5X1— (wherein X1 and R5 are as defined herein; R1 represents hydrogen, oxo, halogeno, hydroxy, C1-4alkoxy, C1-4alkyl, C1-4alkoxymethyl, C1-4alkanoyl, C1-4haloalkyl, cyano, amino, C2-5alkenyl, C2-5alkynyl, C1-3alkanoyloxy, nitro, C1-4alkanoylamino, C1-4alkoxycarbonyl, C1-4alkylsulphanyl, C1-4alkylsulphinyl, C1-4alkylsulphonyl, carbamoyl, N—C1-4alkylcarbamoyl, N,N-di(C1-4alkylcarbamoyl, aminosulphonyl, N—C1-4alkylaminosulphonyl, N,N-di(C1-4alkyl)aminosulphonyl, N—(C1-4alkylsulphonyl)amino, N—(C1-4alkylsulphType: GrantFiled: February 8, 2000Date of Patent: July 11, 2006Assignee: AstraZeneca ABInventors: Elaine S E Stokes, Darren Mckerrecher, Laurent F A Hennequin, Patrick Ple
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Patent number: 7053215Abstract: Compounds are provided that have the formula: where X, A4, Ra, R1, R2, R3, R4, R14, L and Q are as described herein. These compounds are useful, for example, as modulators of a chemokine receptor and for treatment of inflammatory and immunoregulatory disorders and diseases. Pharmaceutical compositions and methods of using these compounds for the treatment of inflammatory and immunoregulatory disorders and diseases, such as multiple sclerosis, rheumatoid arthritis and type I diabetes, are also provided.Type: GrantFiled: August 29, 2002Date of Patent: May 30, 2006Assignee: Amgen SF, LLCInventors: Julio C. Medina, Michael G. Johnson, An-Rong Li, Jiwen Liu, Alan Xi Huang, Liusheng Zhu, Andrew P. Marcus
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Patent number: 6989385Abstract: This invention describes novel pyrazole compounds of formula IIc: wherein R1 is T-Ring D, wherein 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 taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-7 membered ring having 0-3 heteroatoms; and R2 and R2? are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: GrantFiled: December 19, 2001Date of Patent: January 24, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Jean-Damien Charrier, Robert Davies, Simon Everitt, David Kay, Ronald Knegtel, Sanjay Patel
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Patent number: 6962922Abstract: A compound selected from those of formula (I): wherein W1 represents O, S, or —NR3 in which R3 represents hydrogen, alkyl, OH or CN; W2 represents a group selected from hydrogen, CF3, NH2, monoalkylamino, dialkylamino, alkyl, alkenyl, alkynyl, aryl, arylalkyl, cycloalkylalkyl, heterocycle, these groups being optionally substituted, or W1 and W2 form together a group of formula —N?X4—W3— as defined in the description, X1, X2 and X3 represent N or C optionally substituted, n is 0 to 8, Z represents —CR12R13, wherein R12 and R13 are as defined in the description, A represents a ring system, the groups R2 represent hydrogen or various chemical groups as defined in the description, q is 0 to 7; R1 represents hydrogen, alkyl, alkenyl, alkynyl, or a ring system, and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix metalloprotease.Type: GrantFiled: October 11, 2002Date of Patent: November 8, 2005Assignee: Warner-Lambert Company LLCInventors: Bernard Gaudilliere, Henri Jacobelli, Joseph Armand Picard, Michael William Wilson
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Patent number: 6949550Abstract: The present application describes substituted-aminomethyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.Type: GrantFiled: November 26, 2002Date of Patent: September 27, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Mimi L. Quan, Ruth R. Wexler
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Patent number: 6949535Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K? plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.Type: GrantFiled: October 30, 2003Date of Patent: September 27, 2005Assignee: ICOS CorporationInventors: Chanchal Sadhu, Ken Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
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Patent number: 6919331Abstract: The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides heterocyclic substituted 2-methylbenzimidazole derivatives for the treatment of respiratory syncytial virus infection.Type: GrantFiled: December 4, 2002Date of Patent: July 19, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Kuo-Long Yu, Xiangdong Wang, Yaxiong Sun, Christopher Cianci, Jan Willem Thuring, Keith Combrink, Nicholas Meanwell, Yi Zhang, Rita L. Civiello
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Patent number: 6919338Abstract: The use of a compound of formula (I) or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, or NR6 where R6 is hydrogen or C1-6alkyl; R5 is an optionally substituted 5-membered heteroaromatic ring, R1, R2, R3, R4 are independently selected from various specified moieties, in the preparation of a medicament for use in the inhibition of aurora 2 kinase. Certain compounds are novel and these, together with pharmaceutical compositions containing them are also described and claimed.Type: GrantFiled: June 21, 2001Date of Patent: July 19, 2005Assignee: AstraZeneca ABInventors: Andrew Mortlock, Frederic Jung
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Patent number: 6911446Abstract: The present invention is directed in part towards methods of modulating the function of serine/threonine protein kinases with quinazoline-based compounds. The methods incorporate cells that express a serine/threonine protein kinase, such as RAF. In addition, the invention describes methods of preventing and treating serine/threonine protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to quinazoline compounds and pharmaceutical compositions comprising these compounds.Type: GrantFiled: January 26, 2001Date of Patent: June 28, 2005Assignee: Sugen, Inc.Inventors: Peng C. Tang, Gerald McMahon, Heinz Weinberger, Bernhard Kutscher, Harald App
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Patent number: 6906070Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings D-E represent guanidine mimics, which are useful as inhibitors of factor Xa.Type: GrantFiled: August 8, 2001Date of Patent: June 14, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Patrick Y. Lam, Charles G. Clark, Celia Dominguez, John M. Fevig, Qi Han, Renhua Li, Donald J. P. Pinto, James R. Pruitt, Mimi L. Quan
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Patent number: 6897214Abstract: The invention concerns quinazoline derivatives of the formula I wherein X1 is a direct link or a group such as CO, C(R2)2 and CH(OR2); wherein Q1 is phenyl, naphthyl or a 5- or 6-membered heteroaryl moiety and Q1 optionally bears up to 3 substituents; wherein m is 1 or 2 and each R1 may be a group such as hydrogen, halogeno and trifluoromethyl; and wherein Q2 may be phenyl or a 9- or 10-membered bicyclic heterocyclic moiety and Q2 optionally bears up to 3 substituents; or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and the use of their receptor tyrosine kinase inhibitory properties in the treatment of proliferative disease such as cancer.Type: GrantFiled: May 2, 2002Date of Patent: May 24, 2005Assignee: Zeneca LimitedInventors: Andrew John Barker, Craig Johnstone
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Patent number: 6890924Abstract: The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R3, R4, R5, R11, m and p are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.Type: GrantFiled: June 18, 2001Date of Patent: May 10, 2005Assignee: Pfizer IncInventors: John Charles Kath, Joel Morris, Samit Kumar Bhattacharya
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Patent number: 6869945Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N?(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; -G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems reType: GrantFiled: November 20, 2002Date of Patent: March 22, 2005Assignee: Pfizer IncInventors: Anthony Marfat, Michael William McKechney
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Patent number: 6800620Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K&dgr;) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K&dgr; plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K&dgr;, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K&dgr; activity, including compounds that selectively inhibit PI3K&dgr; activity. Methods of using PI3K&dgr; inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K&dgr; inhibitory compounds to inhibit PI3K&dgr;-mediated processes in vitro and in vivo.Type: GrantFiled: January 6, 2003Date of Patent: October 5, 2004Assignee: ICOSInventors: Chanchal Sadhu, Ken Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
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Patent number: 6794389Abstract: There is provided an excellent novel analgesic having an analgesic effect which is effective widely against a pain including a chronic pain or an allodynia accompanied with herpes zoster by acting on a nociceptin receptor. The present invention relates to a compound represented by the following formula: or a salt thereof.Type: GrantFiled: September 25, 2002Date of Patent: September 21, 2004Assignee: Nippon Shinyaku Co., Ltd.Inventors: Masahiko Okana, Kazuya Mori
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Patent number: 6759410Abstract: The present invention relates to 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolines of formula (1), or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.Type: GrantFiled: May 10, 2002Date of Patent: July 6, 2004Assignee: SmithLine Beecham CorporationInventors: Jerry L. Adams, Michael J. Bower, Ralph Hall, Don Edgar Griswold, David C. Underwood
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Publication number: 20040092515Abstract: Compounds of the formula I: 1Type: ApplicationFiled: August 27, 2003Publication date: May 13, 2004Inventors: Torbjjorn Lundstedt, Anneli Hallgren, Per Andersson, Anders Hallberg, Malin Graffner Nordberg
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Publication number: 20040082542Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, &bgr;-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.Type: ApplicationFiled: March 5, 2003Publication date: April 29, 2004Inventors: Adnan M.M. Mjalli, Robert C. Andrews, Ramesh Gopalaswamy, Anitha Hari, Kwasi S. Avor, Ghassan Qabaja, Xiao-Chuan Guo, Suparna Gupta, David R. Jones, Xin Chen
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Publication number: 20040077668Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.Type: ApplicationFiled: May 8, 2003Publication date: April 22, 2004Applicants: Cytokinetics, Inc., SmithKline BeechamInventors: Bainian Feng, Gustave Bergnes, David J. Morgans, Dashyant Dhanak, Steven David Knight, Michael Gerard Darcy
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Publication number: 20040053948Abstract: Quinazolinedione derivatives useful for treating cellular proliferative disorders and disorders associated with Kif15 kinesin activity are described.Type: ApplicationFiled: May 8, 2003Publication date: March 18, 2004Applicant: Cytokinetics, Inc.Inventors: Andrew McDonald, Gustave Bergnes, David J. Morgans
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Patent number: 6699861Abstract: Dihydroquinazoline derivatives of the formula where R3 is —(CH2)p—A where p is from 1 to 4 and A is a 5- or 6-membered N-containing heterocyclic ring attached via the N atom or A is —NA′A″ wherein A′ and A″ are the same or different and are each a C1-C4 alkyl group or their pharmaceutically acceptable salts possessing anti-cancer activity.Type: GrantFiled: October 19, 2001Date of Patent: March 2, 2004Assignee: Cancer Research Technology LimitedInventors: Lorraine Skelton, Vassilis Bavetsias, Ann Jackman
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Patent number: 6696452Abstract: This invention describes novel pyrazole compounds of formula II: wherein Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, and R2, R2′, Rx, and Ry are as described in the specification. Ring C has an ortho substituent and is optionally substituted in the non-ortho positions. R2 and R2′ are optionally taken together with their intervening atoms to form a fused ring system, such as an indazole ring; and Rx and Ry are optionally taken together with their intervening atoms to form a fused ring system, such as a quinazoline ring. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3, for treating diseases such as diabetes and Alzheimer's disease.Type: GrantFiled: September 14, 2001Date of Patent: February 24, 2004Assignee: Vertex Pharmaceuticals IncorporatedInventors: Robert Davies, David Bebbington, Ronald Knegtel, Marion Wannamaker, Pan Li, Cornelia Forster, Albert Pierce
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Patent number: 6696437Abstract: The present invention relates to novel benzimidazoles, their preparation and their use as inhibitors of the enzyme poly(ADP-ribose) polymerase or PARP (EC 2.4.2.30) for producing drugs.Type: GrantFiled: March 25, 2002Date of Patent: February 24, 2004Assignee: Abbott GmbH & Co. KGInventors: Wilfried Lubisch, Michael Kock, Thomas Hoeger, Roland Grandel, Uta Holzenkamp, Sabine Schult, Reinhold Mueller
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Publication number: 20040009981Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: March 14, 2003Publication date: January 15, 2004Inventors: David Bebbington, Hayley Binch, Jean-Damien Charrier, Simon Everitt, Julian M.C. Golec, David Kay, Ronald Knegtel, Andrew Miller, Francoise Pierard
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Patent number: 6667300Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K&dgr;) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K&dgr; plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K&dgr;, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K&dgr; activity, including compounds that selectively inhibit PI3K&dgr; activity. Methods of using PI3K&dgr; inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K&dgr; inhibitory compounds to inhibit PI3K&dgr;-mediated processes in vitro and in vivo.Type: GrantFiled: October 19, 2001Date of Patent: December 23, 2003Assignee: ICOS CorporationInventors: Chanchal Sadhu, Ken Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
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Publication number: 20030232817Abstract: Compounds of the formula I 1Type: ApplicationFiled: February 24, 2003Publication date: December 18, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventor: Roman Wolfgang Fleck
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Publication number: 20030229087Abstract: Novel active compound combinations of compounds of the formula (I) 1Type: ApplicationFiled: November 6, 2002Publication date: December 11, 2003Inventors: Astrid Mauler-Machnik, Ulrike Wachendorff-Neumann, Herbert Gayer
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Publication number: 20030225089Abstract: The present invention relates to novel pharmaceutical compositions based on anticholinergics and p38 kinase inhibitors, processes for preparing them and their use in the treatment of respiratory diseases.Type: ApplicationFiled: April 7, 2003Publication date: December 4, 2003Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Birgit Jung, Michel Pairet, Michael P. Pieper, Hans Clemens Reiser
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Publication number: 20030225053Abstract: Disclosed are amide compounds of formula(I): 1Type: ApplicationFiled: April 10, 2003Publication date: December 4, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Donghong Amy Gao, Daniel R. Goldberg, Abdelhakim Hammach, Ming-Hong Hao, Victor Marc Kamhi, Neil Moss, Kevin Chungeng Qian, Gregory Paul Roth, Christopher Ronald Sarko, Alan David Swinamer, Zhaoming Xiong
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Publication number: 20030220357Abstract: A process for the preparation of various quinazoline compounds which are useful as Rho-Kinase inhibitors, and thus having utility in the treatment of hypertension and other indications.Type: ApplicationFiled: September 24, 2002Publication date: November 27, 2003Inventors: Donald Bankston, Dhanaphalan Nagarathnam, Davoud Asgari, Jianxing Shao, Xiao-Gao Liu, Uday Khire, Chunguang Wang, Barry Hart, Stephen Boyer, Olaf Weber, Mark Lynch
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Patent number: 6653300Abstract: This invention describes novel pyrazole compounds of formula I′: wherein Q′ is —O—, —C(R6′)2—, 1,2-cyclopropanediyl, 1,2-cyclobutanediyl, or 1,3-cyclopropanediyl, and R1 is T-Ring D, wherein 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 L—Z—R3, or Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-7 membered ring having 0-3 heteroatoms; and R2 and R2′ are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: GrantFiled: December 19, 2001Date of Patent: November 25, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Jeremy Green, David Kay, Ronald Knegtel, Andrew Miller, Ronald Tomlison, Pan Li
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Patent number: 6645971Abstract: A compound given by general formula (1): [wherein T represents oxygen or sulfur atom, Y represents alkyl, cycloalkyl group, etc., ring W represents benzene ring, etc., R1 and R2 represent independently hydrogen atom, lower alkyl group, etc., and R3 represents hydrogen atom, alkyl group, etc. Z represents a group given by formula: {wherein A1 and A2 represent independently hydrogen atom, alkyl group, etc. and G represents straight chain alkylene having 1-6 of the carbon number, etc.} or a group given by formula: {wherein n represents 0, 1 or 2, ring E represents 4-8 membered saturated heterocyclic ring containing nitrogen atom(s), and A3 represents hydrogen atom, alkyl group, etc.}], its prodrug or pharmaceutically acceptable salt thereof is an antagonist against muscarinic receptor that is useful as anticholinergic medicaments, and therefore it is useful as pollakiuria or urinary incontinence remedy.Type: GrantFiled: April 10, 2001Date of Patent: November 11, 2003Assignee: Sumitomo Pharmaceuticals Company LimitedInventors: Masami Muraoka, Kazuki Matsui, Koji Morishita, Naohito Ohashi
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Publication number: 20030207868Abstract: The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides heterocyclic substituted 2-methylbenzimidazole derivatives for the treatment of respiratory syncytial virus infection.Type: ApplicationFiled: December 4, 2002Publication date: November 6, 2003Inventors: Kuo-Long Yu, Xiangdong Wang, Yaxiong Sun, Christopher Cianci, Jan Willem Thuring, Keith Combrink, Nicholas Meanwell, Yi Zhang, Rita L. Civiello
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Publication number: 20030199530Abstract: A compound selected from those of formula (I): 1Type: ApplicationFiled: March 18, 2003Publication date: October 23, 2003Inventors: Solo Goldstein, Alain Dhainaut, Andre Tizot, Jean-Luc Fauchere, Nathalie Kucharczyk, John Hickman, Alain Pierre, Gordon Tucker, Laurence Kraus-Berthier
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Publication number: 20030191139Abstract: The invention relates to compounds of formula I D—CO—B—A-Het and pharmaceutically acceptable salts thereof where substituents in description have the specified meanings. The compounds are used as thrombin inhibitors.Type: ApplicationFiled: January 31, 2003Publication date: October 9, 2003Inventors: Danijel Kikelj, Lucija Peterlin, Petra Marinko, Matej Breznik, Mojca Stregnar, Bakija Alenka Trampuz, Marjana Fortuna
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Publication number: 20030191116Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors.Type: ApplicationFiled: April 10, 2003Publication date: October 9, 2003Inventors: Sarkis Barret Kalindjian, Ildiko Maria Buck, Caroline Minli Rachel Low, Matthew John Tozer
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Publication number: 20030187002Abstract: The use of a compound of formula (I) 1Type: ApplicationFiled: December 16, 2002Publication date: October 2, 2003Applicant: AstraZeneca ABInventors: Andrew Mortlock, Frederic Jung
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Patent number: 6627634Abstract: Bicyclic heterocycles of general formula wherein: Ra to Rd, A to C and X are as defined herein, the tautomers, the stereoisomers and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases, diseases of the lungs and respiratory tract, and the preparation thereof.Type: GrantFiled: March 23, 2001Date of Patent: September 30, 2003Assignee: Boehringer Ingelheim Pharma KGInventors: Frank Himmelsbach, Elke Langkopf, Birgit Jung, Stefan Blech, Flavio Solca
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Publication number: 20030181472Abstract: Compounds, compositions and methods that are useful in the treatment of inflammatory, immunoregulatory, metabolic and cell proliferative conditions or diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in inflammation, metabolism and cell proliferation. The subject compounds contain quinoline or quinazoline rings.Type: ApplicationFiled: December 4, 2002Publication date: September 25, 2003Applicant: Tularik Inc.Inventors: David L. Clark, Timothy D. Cushing, Michael R. DeGraffenreid, Xiaolin Hao, Xiao He, Juan C. Jaen, Marc Labelle, Jay Powers, Marie-Louise Smith, Craig S. Tomooka, Nigel P.C. Walker, Adrian L. Gill, Francisco X. Talamas, Sharada Labadie
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Publication number: 20030176421Abstract: Stasis is treated or prevented in all or any part or parts of the stomach of a patient, especially a human patient, in need of such treatment, where said stasis results from hypomotility in the stomach, particularly gastric hypomotility with delayed emptying of the liquid and/or solid contents of the stomach. Gastric or gastrointestinal disorders are also treated which are characterized by one or more symptoms selected from pain, nausea, vomiting, heartburn, postprandial discomfort, indigestion and gastroesophageal reflux. Such treatment or prevention is achieved by administering to the patient a therapeutically effective amount of an inhibitor of phosphodiesterase-4 (PDE4), including isozyme subtypes thereof, sufficient to treat or prevent such hypomotility or gastric or gastrointestinal disorder in said patient.Type: ApplicationFiled: December 30, 1999Publication date: September 18, 2003Inventors: JOHN W. WATSON, PAUL L. R. ANDREWS, ANTHONY J. WOODS
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Patent number: 6610678Abstract: This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R1 is C1-6alkyl, NR6R7, OR6 or SR7; R2 is hydrogen, C1-6alkyl, C1-6alkyloxy or C1-6alkylthio; R3 is Ar1 or Het1; R4 and R5 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, cyano, nitro, amino, and mono- or di(C1-6alkyl)amino; R6 is hydrogen, C1-6alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R7 is hydrogen, C1-8alkyl, mono- or di(C3-6cyclo-alkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxy-C1-6alkyl or C1-6alkyloxyC1-6alkyl; R6 is C1-8alkyl, mono- or di(C3-6cycloalkyl)-methyl, Ar2CH2, C1-6alkyloxyC1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl; or R6 and R7 taken together with the nitrogen atom to which they are attached maType: GrantFiled: October 8, 2002Date of Patent: August 26, 2003Inventors: Charles Huang, Keith M. Wilcoxen, Chen Chen, Mustapha Haddach, James R. McCarthy
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Publication number: 20030158189Abstract: Therapeutically active compositions of matter are described which are useful for treating or preventing diseases and conditions comprising inflammatory diseases including joint inflammation, Crohn's disease, and inflammatory bowel disease; respiratory diseases such as chronic obstructive pulmonary disease (COPD) including asthma, chronic bronchitis, and pulmonary emphysema; infectious diseases including endotoxic shock and toxic shock syndrome; immune diseases including systemic lupus erythematosis and psoriasis; and other diseases including bone resorption diseases and reperfusion injury; wherein said composition of matter comprises a compound which is an inhibitor of phosphodiesterase isozyme 4 (PDE4) and wherein an indazole is one essential component of said compound's overall chemical structure, and wherein said indazole constitutes a bioisosteric replacement of a catechol component or functional derivative thereof in a known compound having the same said therapeutic activity and the same remaining said cType: ApplicationFiled: December 12, 2002Publication date: August 21, 2003Inventor: Anthony Marfat
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Publication number: 20030149043Abstract: NHE-1 inhibitors, methods of using such NHE-1 inhibitors and pharmaceutical compositions containing such NHE-1 inhibitors. The NHE-1 inhibitors are useful for the reduction of tissue damage resulting from tissue ischemia.Type: ApplicationFiled: December 9, 2002Publication date: August 7, 2003Applicant: Pfizer Inc.Inventors: Ernest S. Hamanaka, Angel Guzman-Perez, Christian J. Mularski, Roger B. Ruggeri, Ronald T. Wester
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Publication number: 20030144308Abstract: The present invention relates to certain quinazoline compounds which have utility in the treatment of diabetes mellitus, hypercholesterolemia, hyperlipidemia, diabetic complications and cancer. The invention also relates to pharmaceutical compositions and kits comprising such quinazoline compounds and to methods of using such compounds in the treatment of diabetes mellitus, hypercholesterolemia, hyperlipidemia, diabetic complications and cancer.Type: ApplicationFiled: September 20, 2002Publication date: July 31, 2003Inventors: Paul H. Bauer, Stephen W. Wright, Rodney C. Schnur
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Publication number: 20030125344Abstract: Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds of the present invention are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease.Type: ApplicationFiled: March 22, 2002Publication date: July 3, 2003Applicant: BAYER CORPORATIONInventors: Dhanaphalan Nagarathnam, Davoud Asgari, Jianxing Shao, Xiao-Gao Liu, Uday Khire, Chunguang Wang, Barry Hart, Stephen Boyer, Olaf Weber, Mark Lynch