Nitrogen Of The Hetero Ring Is Shared By An Additional Cyclo Of The Polycyclo Ring System Patents (Class 540/579)
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Publication number: 20110251178Abstract: Bicyclic pyridinylpyrazoles of the formula (I) in which the symbols have the meanings given in the description and agrochemically active salts thereof and their use for controlling unwanted microorganisms in crop protection and the protection of materials and for reducing mycotoxins in plants and plant parts, and also processes for preparing compounds of the formula (I).Type: ApplicationFiled: April 5, 2011Publication date: October 13, 2011Applicant: Bayer CropScience AGInventors: Amos MATTES, Hendrik HELMKE, Stefan HILLEBRAND, Gorka PERIS, Alexander SUDAU, Lars RODEFELD, Stefan GAUGER, Jürgen BENTING, Peter DAHMEN, Ruth MEISSNER, Ulrike WACHENDORFF-NEUMANN, Hiroyuki HADANO
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Publication number: 20110213143Abstract: Provided are compounds having superior TAFIa inhibitory activity.Type: ApplicationFiled: October 28, 2009Publication date: September 1, 2011Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Hideaki Amada, Daisuke Matsuda, Masahiro Bohno, Shiuji Saito, Ayako Bohno
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Publication number: 20110158989Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.Type: ApplicationFiled: March 4, 2011Publication date: June 30, 2011Applicant: Takeda Pharmaceutical Company LimitedInventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
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Patent number: 7968553Abstract: Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds of Formula A: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein n is an integer equal to zero, 1, 2 or 3, and R1, R3, R4, R12, R14, R16, R30, R32, R34 and R36 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: March 12, 2008Date of Patent: June 28, 2011Assignee: Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.p.A.Inventors: Benedetta Crescenzi, Olaf Kinzel, Ester Muraglia, Federica Orvieto, Giovanna Pescatore, Michael Rowley, Vincenzo Summa
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Publication number: 20110152248Abstract: The present application relates to indole and indoline derivatives of formula (I), formula (II), formula (III), or formula (IV) wherein a, R2, R3, h, k, m, n, L, Q, X, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions.Type: ApplicationFiled: December 14, 2010Publication date: June 23, 2011Applicant: ABBOTT LABORATORIESInventors: Lei Shi, William H. Bunnelle, Tao Li, Marc J. Scanio, Michael R. Schrimpf, Chih-Hing Lee
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Publication number: 20110144092Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein X, R1, R2, R3, R4, and m are defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates thereof and their use in therapeutics.Type: ApplicationFiled: December 15, 2010Publication date: June 16, 2011Applicants: SANOFI-AVENTIS, MITSUBISHI TANABE PHARMA CORPORATIONInventors: Aude FAYOL, Alistair LOCHEAD, Mourad SAADY, Julien VACHE, Philippe YAICHE
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Publication number: 20110144091Abstract: This invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof; as well as a method for treating obesity, a method for treating diabetes, and a pharmaceutical composition.Type: ApplicationFiled: December 7, 2010Publication date: June 16, 2011Applicant: ELI LILLY AND COMPANYInventors: Macklin Brian Arnold, Thomas James Beauchamp, Emily Jane Canada, Erik James Hembre, Jianliang Lu, John Robert Rizzo, John Mehnert Schaus, Qing Shi
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Publication number: 20110077395Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein G, L, Q, Z, R6, R7, and R8 are defined herein.Type: ApplicationFiled: December 2, 2010Publication date: March 31, 2011Inventors: James J. Li, Lawrence G. Hamann, Zheming Ruan, Christopher B. Cooper, Shung C. Wu, Ligaya M. Simpkins, Haixia Wang, Akbar Nayeem, Stanley R. Krystek
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Publication number: 20110034440Abstract: The invention provides a homocysteine synthase inhibitor useful for the prophylaxis or treatment of diseases involving homocysteine synthase. The homocysteine synthase inhibitor is a compound of the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof.Type: ApplicationFiled: April 10, 2009Publication date: February 10, 2011Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Akira Nakao, Hiroko Suzuki, Ryo Tatsumi, Maki Seki, Minoru Tanaka, Tomofumi Setsuta, Hiroshi Iwasaki
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Publication number: 20110020276Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.Type: ApplicationFiled: March 25, 2009Publication date: January 27, 2011Inventors: Zhong Yang, John A. Bender, John F. Kadow
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Publication number: 20110009389Abstract: There is provided an imidazole derivative useful as a thrombosis treating agent, which is represented by the formula (I): wherein R represents an optionally substituted cyclic hydrocarbon group or an optionally substituted heterocyclic group, W represents a bond or an optionally substituted divalent linear hydrocarbon group, X represents an optionally substituted divalent hydrocarbon group, Y represents —CO—, —S(O)—, —S(O)2— or a bond, ring A represents an optionally substituted pyrrolidine ring, an optionally substituted piperidine ring or an optionally substituted perhydroazepine ring, Z1 and Z3 independently represent a bond or an optionally substituted divalent linear hydrocarbon group, Z2 represents —N(R1)—, —O—, —S(O)—, —S(O)2—, —CO—, —CH(R1)— or a bond, ring B represents an optionally substituted imidazole ring, wherein a substituent which the optionally substituted imidazole ring represented by ring B may have may be taken together with R1 to form an optionally substituted ring, and a represents 0Type: ApplicationFiled: September 10, 2010Publication date: January 13, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Keiji KUBO, Takanobu KUROITA, Yasuhiro IMAEDA, Masaki KAWAMURA
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Publication number: 20110003738Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: July 1, 2010Publication date: January 6, 2011Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Peter R. GUZZO, Matthew David SURMAN, Alan John HENDERSON, May Xiaowu JIANG
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Publication number: 20100273775Abstract: Disclosed are compounds of Formulae 1 and 1a, N-oxides, and salts thereof, wherein R1, R1a, Y, and J are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention. Further disclosed is a method for preparing compounds of Formula 1 from compounds of Formula 1a.Type: ApplicationFiled: December 10, 2008Publication date: October 28, 2010Applicant: E.I. Du pont de Nemours and CompanyInventors: John Joseph Bisaha, Alvin Donald Crews, JR., Michael Henry Howard, JR., Paula Louise Sharpe, Thomas Martin Stevenson, Andrew Edmund Taggi
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Publication number: 20100273767Abstract: The present application relates to 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2 -a][1,4]benzodiazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,5]benzodiazepine, 2,3,4,4a,5,6,7,11b-octahydro-1H-pyrido[3,4-d][2]benzazepine, 1,2,3,4,4a,5,6,7 -octahydropyrazino[1,2-a][1]benzazepine, 1,2,3,4,4a,5-hexahydro-7H-pyrazino[1,2 -a][4,1]benzoxazepine, and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[2,1-d][1,5]benzoxazepine, and 5,6,7,7a,8,9,10,11-octahydropyrazino[1,2-d]pyrido[3,2-b][1,4]diazepine derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X1, X2, X3, X4, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.Type: ApplicationFiled: April 22, 2010Publication date: October 28, 2010Applicant: ABBOTT LABORATORIESInventors: Ying Wang, Jason T. Brewer, Irini Akritopoulou-Zanze, Stevan W. Djuric, Bhadra Shelat, Frauke Pohlki, Wilfried Braje, Ana-Lucia Relo
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Publication number: 20100255117Abstract: The instant invention provides methods and compositions for the treatment of cancer.Type: ApplicationFiled: April 6, 2008Publication date: October 7, 2010Applicant: The Johns Hopkins UniversityInventors: Shyam Biswal, Anju Singh, Deepti Malhotra
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Publication number: 20100249105Abstract: The present application relates to indole and indoline derivatives of formula (I), (II), (III), (IV), (V), or (VI) wherein a, R1, R2, R3, R4, R5, U, V, W, X, Y, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.Type: ApplicationFiled: March 19, 2010Publication date: September 30, 2010Applicant: ABBOTT LABORATORIESInventors: Michael R. Schrimpf, Chih-Hung Lee, Tao Li, Gregory A. Gfesser, Kathleen H. Mortell, Ramin Faghih, Diana L. Nersesian, Kevin B. Sippy, William H. Bunnelle, Marc Scanio, Lei Shi, Murali Gopalakrishnan, Diana L. Donnelly-Roberts, Min Hu
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Publication number: 20100216988Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R1; R2; R3; R4; J1; J2; J3; J4 and G have the meanings indicated in the claims. The present invention provides a direct metal, e.g. palladium or copper, catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.Type: ApplicationFiled: December 22, 2009Publication date: August 26, 2010Applicant: SANOFI-AVENTISInventors: Jorge ALONSO, Andreas LINDENSCHMIDT, Marc NAZARE, Omar RKYEK, Matthias URMANN, Nis HALLAND
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Publication number: 20100173892Abstract: This invention relates to a process for the hydrogenation of a ketooxime to selectively form an aminoalcohol stereoisomer, and, in particular, to a process for the hydrogenation of 4,5-dihydro-imidazo[4,5,1-jk][1]benzazepin-2,6,7[1H]-trione-6-oxime or a salt thereof to selectively form a stereoisomer of 6-amino-7-hydroxy-4,5,6, 7-tetrahydro-imidazo[4,5,1-jk][1]-benzazepin-2[1H]-one or a salt thereof. This invention also relates to the use of the 6-amino-7-hydroxy-4,5,6,7-tetrahydro-imidazo[4,5,1-jk][1]-benzazepin-2[1H]-one hydrogenation product or a salt thereof to selectively make a stereoisomer of zilpaterol or a salt thereof, as well as the use of such a zilpaterol stereoisomer or salt in methods of treatment and medicaments for animals.Type: ApplicationFiled: January 31, 2008Publication date: July 8, 2010Inventors: Juan Jose Almena-Perea, Monika Brink, Gerhard Geiss, Renat Kadyrov, Thorsten Meyer
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Patent number: 7732438Abstract: Compounds of Formula (I) and Formula (II) (where variables R1, R2, R4, A, B, W, X, Y and Z are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: October 12, 2005Date of Patent: June 8, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Daniel V. Paone, Anthony W. Shaw, Craig M. Potteiger
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Patent number: 7732437Abstract: The invention concerns a novel histamine receptor antagonist and the use of an histamine receptor antagonist for the reduction of intracranial pressure (ICP), in particular for the prevention and treatment of elevated intracranial pressure and/or secondary ischaemida, in particular caused by brain injury, more in particular caused by traumatic (TBI) and non-traumatic brain injury. The novel compounds comprise compounds according to the general Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof. In particular, the preferred compound is 3-[2-[4-(11,12-dihydro-6H-benzimidazo[2,1-b][3]benzazepin-6-yl)-2-(phenyl-methyl)-1-piperidinyl]ethyl]-2,10-dimethyl pyrimido[1,2-?]benzimidazol-4(10H)-one, the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof.Type: GrantFiled: November 22, 2002Date of Patent: June 8, 2010Assignee: Janssen Pharmaceutica, NV.Inventors: Frank Tegtmeier, Frans Eduard Janssens, Joseph Elisabeth Leenaerts, Koenraad Arthur van Rossem, Manuel Jesús Alcázar-Vaca, Pedro Martínez-Jiménez, José Manuel Bartolomé-Nebreda, Antonio Gómez-Sánchez, Francisco Javier Fernández-Gadea, Jozef Leo Henri Van Reempts
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Publication number: 20100121050Abstract: This invention generally relates to processes for making zilpaterol and salts thereof, as well as processes for making intermediates that, inter alia, may be used to make zilpaterol and salts thereof. The zilpaterol and salts prepared in accordance with this invention can be used to increase the rate of weight gain, improve feed efficiency, and/or increase carcass leanness in livestock, poultry, and fish.Type: ApplicationFiled: March 28, 2008Publication date: May 13, 2010Inventor: Stephane Dubuis
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Publication number: 20100087419Abstract: Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein X1, X2, Y, R1A, R1B, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Processes for making compounds of Formula I and intermediates thereof are also described.Type: ApplicationFiled: October 2, 2009Publication date: April 8, 2010Inventors: Richard C. A. Isaacs, Wayne J. Thompson, Peter D. Williams, Dai-Shi Su, Shankar Venkatraman, Mark W. Embrey, Thorsten E. Fisher, John S. Wai, David C. Dubost, Richard G. Ball, Eric J. Choi, Tao Pei, Sarah L. Trice, Neil Campbell, Matthew Maddess, Peter E. Maligres, Michael Shevlin, Zhiguo Jake Song, Dietrich P. Steinhuebel, Neil A. Strotman, Jingjun Yin
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Publication number: 20100022490Abstract: This invention is directed generally to zilpaterol enantiomer compositions and, in particular, to compositions comprising the 6R,7R zilpaterol enantiomer. This invention is also directed to processes for making such compositions; methods for using such compositions to, for example, increase the rate of weight gain, improve feed efficiency, and/or increase carcass leanness in livestock, poultry, and/or fish; and uses of such compositions to make medicaments. This invention is further directed to methods for determining the absolute configurations of zilpaterol enantiomers.Type: ApplicationFiled: July 10, 2007Publication date: January 28, 2010Applicant: Intervet International B.V.Inventors: Christian Miculka, Thorsten Meyer, Christopher Kern, Serge Francois Droux
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Publication number: 20100009959Abstract: The present invention relates to pentacyclic indole derivatives of formula (I): wherein A, Ar, R1, R2, W, X, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.Type: ApplicationFiled: May 4, 2007Publication date: January 14, 2010Applicant: Instituto di Ricerche di Biologia Molecolare P. Angeletti SPAInventors: Elena Capito, Joerg Habermann, Frank Narjes, Maria del Rosario Rico Ferreira, Ian Stansfield
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Publication number: 20090318421Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.Type: ApplicationFiled: April 28, 2006Publication date: December 24, 2009Inventors: Brian Alvin Johns, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
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Publication number: 20090253677Abstract: The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: ApplicationFiled: March 18, 2009Publication date: October 8, 2009Inventors: Francis Beaulieu, Carl Ouellet, B. Narasimhulu Naidu, Manoj Patel, Yasutsugu Ueda, Timothy P. Connolly, Jonathan R. Weiss, Michael A. Walker, Nicholas A. Meanwell, Kevin M. Peese, Margaret E. Sorenson
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Publication number: 20090181942Abstract: The present invention relates to tricyclic compounds each represented by the following formula (I): (wherein, R1, R2, R2?, R3, R4, X, Y and Z have the same meanings as defined in the specification); and a drug containing the compound. Since the compounds according to the present invention exhibit an excellent squalene synthetase inhibitory effect and cholesterol synthesis inhibitory effect so that they are useful as a drug such as preventive and/or remedy for diseases in mammals including humans such as hyperlipemia, e.g., hypercholesterolemia, hypertriglyceridemia, and low HDL cholesterolemia and/or arteriosclerosis.Type: ApplicationFiled: October 23, 2006Publication date: July 16, 2009Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Kazuyuki Sugita, Masami Otsuka, Hitoshi Oki, Noriyasu Haginoya, Masanori Ichikawa, Masao Itoh
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Patent number: 7550588Abstract: Disclosed are novel homotropane compounds with CNS activity. These compounds can be used for alleviating symptoms of CNS disorders.Type: GrantFiled: March 12, 2007Date of Patent: June 23, 2009Assignee: The Research Foundation of State University of New YorkInventor: Huw M. L. Davies
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Patent number: 7538104Abstract: Compounds of the formula I R7?N—R6 RS—C,N—R4 H C, R?/I R, 3 R 2 (I) in which R, is an aromatic or heteroaromatic radical which is capable of absorbing light in the wave-length range from 200 nm to 650 nm and which is unsubstituted or substituted one or more times by C,—C,8alkyl, C2-C,ealkenyl, C2-C,8alkynyl, C,—C,ehaloalkyl, NO2, NR,OR, CN, OR,2, SR,2, C(O)R,3, C(O)OR,4, halogen or a radical of the formula II R˜—N? R6 1 R5-C,N.Type: GrantFiled: October 8, 2002Date of Patent: May 26, 2009Assignee: Ciba Specialty Chemicals CorporationInventors: Gisèle Baudin, Kurt Dietliker, Tunja Jung
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Publication number: 20090099153Abstract: This invention relates to novel 8,10-diaza-bicyclo[4.3.1]decane derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: May 21, 2007Publication date: April 16, 2009Inventors: Dan Peters, Gunnar M. Olsen, Elsebet Ostergaard Nielsen, Daniel B. Timmermann, Steven Charles Loechel, Jeppe Kejser Christensen, Tino Dyhring
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Publication number: 20090093630Abstract: The present invention relates to improved methods of resolution and recrystallization for synthesizing compounds useful as 5HT2C agonists or partial agonists, including intermediates thereto.Type: ApplicationFiled: September 19, 2008Publication date: April 9, 2009Applicant: WyethInventors: Sreenivasulu Megati, Shilpa Bhansali, Christoph Dehnhardt, Subodh Deshmukh, Peter Fung, Michael MacEwan, Robert J. Tinder
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Publication number: 20090069294Abstract: The present disclosure relates to XIAP inhibitor compounds of the formula I.Type: ApplicationFiled: June 6, 2006Publication date: March 12, 2009Inventors: Zhuoliang Chen, Mark G. Palermo, Sushil K. Sharma, Troy Smith, Christopher S. Straub, Run-Ming D. Wang, Yaping Wang, Leigh Zawel
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Publication number: 20090036427Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: Wherein Y, Z, R1, R2, R3, R4, R5, R6, R7, n, m, and o are as described herein. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3?, such as Alzheimer disease.Type: ApplicationFiled: May 16, 2008Publication date: February 5, 2009Applicants: SANOFI-AVENTIS, MITSUBISHI TANABE PHARMA CORPORATIONInventors: Nathalie CHEREZE, Alistair LOCHEAD, Mourad SAADY, Franck SLOWINSKI, Philippe YAICHE
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Patent number: 7476662Abstract: The invention concerns novel substituted tetracyclic imidazole derivatives useful for the treatment of elevated intracranial pressure (ICP) and/or secondary ischaemia, in particular caused by brain injury, more in particular caused by traumatic (TBI) and non-traumatic brain injury, processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine. The novel compounds comprise compounds according to the general Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof. In particular, the preferred compound is 3-[2-[4-(11,12-dihydro-6H-benzimidazo[2,1-b][3]benzazepin-6-yl)-2-(phenyl-l-methyl)-1-piperidinyl]ethyl]-2,10-dimethyl pyrimido[1,2-?]benzimidazol-4(10H)-one, the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof.Type: GrantFiled: June 11, 2002Date of Patent: January 13, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Frans Eduard Janssens, Joseph Elisabeth Leenaerts, Koenraad Arthur Van Rossem, Manuel Jesús Alcázar-Vaca, Pedro Martínez-Jiménez, José Manuel Bartolomé-Nebreda, Antonio Gómez-Sánchez, Francisco Javier Fernández-Gadea, Jos Van Reempts
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Publication number: 20080305075Abstract: The present invention relates to vinca alkaloid and analog N-oxides having activity for treating hyperproliferative disorders. Further, the invention relates to pharmaceutical compositions and methods of using vinca alkaloid and analog N-oxides, alone or in combination with one or more other active agents or treatments, to treat hyperproliferative disorders.Type: ApplicationFiled: April 29, 2008Publication date: December 11, 2008Inventors: John G. Curd, John F.W. Keana, Alshad S. Lalani, Paul B. Westberg, Bradford Goodwin, W. David Henner
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Publication number: 20080267942Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof are agonists at the beta-2 adrenoceptor. They are useful as feed additives for livestock animals.Type: ApplicationFiled: April 11, 2008Publication date: October 30, 2008Applicant: Pfizer LimitedInventors: Jessica Boyle, Ashley Edward Fenwick, David Morris Gethin, Catherine Frances McCusker
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Publication number: 20080206191Abstract: The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.Type: ApplicationFiled: February 15, 2008Publication date: August 28, 2008Inventors: Andrew Nickel, John F. Kadow
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Patent number: 7414045Abstract: Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds of Formula (A): are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein n is an integer equal to zero, 1, 2 or 3, and R1, R3, R4, R12, R14, R16, R30, R32, R34 and R36 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: December 18, 2003Date of Patent: August 19, 2008Assignee: Istituto di Ricerche di Biologia Molecolare P. Angeletti S.p.A.Inventors: Benedetta Crescenzi, Olaf Kinzel, Ester Muraglia, Federica Orvieto, Giovanna Pescatore, Michael Rowley, Vincenzo Summa
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Publication number: 20080161288Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof are agonists at the beta-2 adrenoceptor. They are useful as feed additives for livestock animals.Type: ApplicationFiled: November 21, 2007Publication date: July 3, 2008Inventors: Jessica Boyle, Ashley Edward Fenwick, David Morris Gethin, Catherine Frances McCusker
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Publication number: 20080153806Abstract: This invention relates to novel diazabicyclic aryl derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: October 18, 2005Publication date: June 26, 2008Inventors: Dan Peters, Daniel B. Timmermann, Gunnar M. Olsen, Elsebet Ostergaard Nielsen, Tino Dyhring Jorgensen
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Publication number: 20080146537Abstract: The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.Type: ApplicationFiled: November 19, 2007Publication date: June 19, 2008Inventors: John A. Bender, Min Ding, Robert G. Gentles, Piyasena Hewawasam
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Patent number: 7365196Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.Type: GrantFiled: March 15, 2001Date of Patent: April 29, 2008Assignees: Merck Sharp & Dohme Ltd., Merck Frosst Canada & Co.Inventors: Patrice Charles Belanger, Ian James Collins, Joanne Claire Hannam, Timothy Harrison, Stephen John Lewis, Andrew Madin, Edward Giles McIver, Alan John Nadin, Joseph George Neduvelil, Mark Steven Shearman, Adrian Leonard Smith, Timothy Jason Sparey, Graeme Irvine Stevenson, Martin Richard Teall
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Publication number: 20080045512Abstract: The present invention provides a benzoate salt of Formula I: Formula I is also known as 4-(5-methyloxazolo[4,5-b]pyridine-2-yl)-1,4-diazabicyclo[3.2.2]nonane. The benzoate salt of the invention is useful in the treatment of schizophrenia and Alzheimer's Disease. It is particularly of use in the treatment of cognitive deficits associated with schizophrenia, cognitive and attention deficit symptoms of Alzheimer's Disease, and neurodegeneration associated with Alzheimer's Disease.Type: ApplicationFiled: August 9, 2006Publication date: February 21, 2008Inventors: Allen J. Duplantier, Kenneth George Kraus, Bruce Nelsen Rogers
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Publication number: 20070287694Abstract: The invention encompasses compounds as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.Type: ApplicationFiled: May 31, 2007Publication date: December 13, 2007Inventors: Kap-Sun Yeung, Katharine A. Grant-Young, Min Ding, Robert G. Gentles, John F. Kadow
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Publication number: 20070275930Abstract: The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.Type: ApplicationFiled: May 23, 2007Publication date: November 29, 2007Inventors: Robert G. Gentles, Min Ding, Piyasena Hewawasam
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Publication number: 20070275947Abstract: The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.Type: ApplicationFiled: May 24, 2007Publication date: November 29, 2007Inventor: Carl P. Bergstrom
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Publication number: 20070270405Abstract: The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.Type: ApplicationFiled: May 3, 2007Publication date: November 22, 2007Inventors: John A. Bender, Min Ding, Robert G. Gentles, Piyasena Hewawasam
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Patent number: 7268127Abstract: Described herein are compounds with affinity for the 5-HT6 receptor, which have the general formula I: Wherein A, B, D, E, R1 to R3 and n are described herein. Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT6 receptor is implicated, such as schizophrenia.Type: GrantFiled: June 24, 2005Date of Patent: September 11, 2007Assignee: NPS Allelix CorpInventors: Louise Edwards, Abdelmalik Slassi, Ashok Tehim, Tao Xin
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Patent number: 7202238Abstract: The present invention relates to a group of unique diazabicyclo alkane derivatives having interesting neurokinin-NK1 receptor antagonistic activity represented by the general formula (1) wherein: R1 represents phenyl, 2-indolyl, 3-indolyl, 3-indazolyl or benzo[b]thiophen-3-yl, which groups may be substituted with halogen or alkyl (1–3C), R2 and R3 independently represent halogen, H, OCH3, CH3 and CF3, R4, R5 and R6 independently represent H, OH, O-alkyl(1–4C), CH2OH, NH2, dialkyl(1–3C)N, pyrrolidin-1-yl, piperidin-1-yl, morpholin-4-yl or morpholin-4-yl substituted with one or two methyl or methoxymethyl groups, morpholin-4-ylamino, morpholin-4-ylmethyl, imidazol-1-yl, thiomorpholin-4-yl, 1,1-dioxothiomorpholin-4-yl or 3-oxa-8-azabicyclo[3.2.Type: GrantFiled: April 2, 2003Date of Patent: April 10, 2007Assignee: Solvay Pharmaceuticals B.V.Inventors: Dirk de Boer, Hein K. A. C. Coolen, Mayke B. Hesselink, Wouter I. Iwema Bakker, Gijsbert D. Kuil, Jan H. van Maarseveen, Andrew C. McCreary, Gustaaf J. M. van Scharrenburg
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Patent number: 7173022Abstract: The invention encompasses a series cyclic bicyclic heterocyclic compounds of Formula I which are inhibitors of HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS.Type: GrantFiled: May 26, 2005Date of Patent: February 6, 2007Assignee: Bristol-Myers Squibb CompanyInventors: B. Narasimhulu Naidu, Jacques Banville, John D. Matiskella, Serge Plamondon, Yasutsugu Ueda