Bicyclo Ring System Having The Diazine Ring As One Of The Cyclos Patents (Class 544/349)
  • Publication number: 20080081803
    Abstract: The present invention is directed to compounds of the formula I: Wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X, n and the broken lines are as defined herein which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
    Type: Application
    Filed: October 15, 2004
    Publication date: April 3, 2008
    Inventors: Gabor Butora, Stephen D. Goble, Alexander Pastemak, Lihu Yang, Changyou Zhou, Christopher R. Moyes
  • Patent number: 7345038
    Abstract: An aminomethylpyridyloxymethyl/benzisoxazole substituted azabicyclic compound of formula I, pharmaceutical composition comprising same, and a method of treating one or more CNS or other disorders, including concurrent treatment of disorders such as schizophrenia and depression, wherein formula I is or a pharmaceutically acceptable salt or thereof, wherein Z is wherein Y is methylene; X is oxygen; n is 0; R1 and R2 are each hydrogen or halogen; and R3 and R4 together with the nitrogen atom to which they are attached form i) a saturated non-aromatic 3 to 7 membered monocyclic ring, said ring i) being unsubstituted or substituted or substituted with one or more (C1–C4)alkyl, (C1–C4)alkoxy(C1–C4)alkyl, or hydroxy groups.
    Type: Grant
    Filed: March 12, 2004
    Date of Patent: March 18, 2008
    Assignee: Pfizer, Inc
    Inventors: Gene Michael Bright, Michael A. Brodney, Bishop Wlodecki
  • Patent number: 7335657
    Abstract: Disclosed are compounds of formula (I) Where Ar1, X, Y, Q, W, R3, R4, R5, R6 and Ry are defined herein. The compounds of the invention inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. The compounds are also useful for treating diseases or conditions related to oncology and anticoagulant or fibrinolytic therapy. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: June 27, 2006
    Date of Patent: February 26, 2008
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Pier Francesco Cirillo, Donghong Amy Gao, Daniel R. Goldberg, Abdelhakim Hammach, Ming-Hong Hao, Victor Marc Kamhi, Neil Moss, Matthew Russell Netherton, Kevin Chungeng Qian, Mark Stephen Ralph, Lifen Wu, Zhaoming Xiong, Ronald A. Aungst, Jr.
  • Patent number: 7304064
    Abstract: The present invention relates to 1-[(indol-3-yl)carbonyl]piperazine derivative according to the general formula I or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said 1-[(indol-3-yl)carbonyl]piperazine derivatives, and to the use of these derivatives in the treatment of pain, such as peri-operative pain, chronic pain neuropathic pain, cancer pain, and pain and spasticity associated with multiple sclerosis.
    Type: Grant
    Filed: June 13, 2003
    Date of Patent: December 4, 2007
    Assignee: N.V. Organon
    Inventors: Phillip Martin Cowley, Wilson Caulfield, Jason Tierney, James Cairns, Julia Adam-Worrall, Mark York
  • Patent number: 7300933
    Abstract: This invention relates to novel diazabicyclic biaryl 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: Grant
    Filed: May 6, 2003
    Date of Patent: November 27, 2007
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Tino Dyhring Jørgensen, Philip K. Ahring
  • Patent number: 7288545
    Abstract: This invention relates to a method for treating an angiogenesis-related disease. The method includes administering to a subject in need thereof an effective amount of a piperazinedione compound having the formula: In the above formula, each of and , independently, is a single bond or a double bond; A is H or CH(RaRb) when is a single bond, or C(RaRb) when is a double bond; Z is CH(RcRd) when is a single bond, or C(RcRd) when is a double bond; each of R1 and R2, independently, is H, C(O)Re, C(O)ORe, C(O)NReRf, or SO2Re; and each of Ra, Rb, Rc, Rd, Re, and Rf, independently, is H, C1-C6 alkyl, aryl, heteroaryl, C3-C8 cycloalkyl, or C3-C8 heterocycloalkyl; or Ra and Rb taken together are C3-C8 cycloalkyl, C3-C8 heterocycloalkyl, aryl, or heteroaryl; or R1 and Ra or R1 and Rb taken together are C3-C8 cycloalkyl, C3-C8 heterocycloalkyl, aryl, or heteroaryl; provided that one of Rc and Rd is aryl or heteroaryl.
    Type: Grant
    Filed: October 20, 2003
    Date of Patent: October 30, 2007
    Assignee: AngioRx Corporation
    Inventors: Che-Ming Teng, Hui-Po Wang, Eric I. C. Li, On Lee, Jih-Hwa Guh, Huei-Ting Chen, Ya-Bing Fan, Ya-Lan Chen
  • Patent number: 7268127
    Abstract: 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: Grant
    Filed: June 24, 2005
    Date of Patent: September 11, 2007
    Assignee: NPS Allelix Corp
    Inventors: Louise Edwards, Abdelmalik Slassi, Ashok Tehim, Tao Xin
  • Patent number: 7256287
    Abstract: The present invention is directed to small molecule inhibitors of the IgE response to allergens, which are useful in the treatment of allergy and/or asthma or any diseases where IgE is pathogenic. This invention also relates to phenyl-aza-benzimidazole molecules that are cellular proliferation inhibitors and thus are useful as anticancer agents. This invention further relates to small molecules which suppress cytokines and leukocytes.
    Type: Grant
    Filed: September 12, 2003
    Date of Patent: August 14, 2007
    Assignee: Avanir Pharmaceuticals
    Inventors: Jagadish C. Sircar, Richard J. Thomas, Mark L. Richards, Anjana Sinha
  • Patent number: 7253168
    Abstract: Compounds of Formula I are provided, in which variables are as described herein: Such compounds may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).
    Type: Grant
    Filed: April 6, 2005
    Date of Patent: August 7, 2007
    Assignee: Neurogen Corporation
    Inventors: Alan J. Hutchison, Bertrand L. Chenard, James G. Tarrant, Guiying Li, Manuka Ghosh, George P. Luke, John M. Peterson, Wallace C. Pringle, Mary-Margaret E. O'Donnell, Kyungae Lee, Linda M. Gustavson, Dario Doller
  • Patent number: 7244734
    Abstract: The invention relates to hexahydro-pyrido[1,2-a]pyrazine derivatives having interesting neurokinin-NK1 receptor antagonistic activity. The invention also relates to methods for the preparation of these compounds, to pharmaceutical compositions containing a pharmacologically active amount of at least one of these compounds as an active ingredient, as well as to the use of these compositions for the treatment of disorders in which neurokinin receptors are involved. The invention relates to compounds represented by the general formula (1) wherein the symbols have the meanings as given in the description.
    Type: Grant
    Filed: September 22, 2004
    Date of Patent: July 17, 2007
    Assignee: Solvay Pharmaceuticals B.V.
    Inventors: Wouter I. Iwema Bakker, Gustaaf J. M. Van Scharrenburg, Adrianus Van Den Hoogenband, Andrew C. McCreary
  • Patent number: 7223753
    Abstract: This invention relates to novel diazabicyclic biaryl 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: Grant
    Filed: November 10, 2003
    Date of Patent: May 29, 2007
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Gunnar M. Olsen, Elsebet Oestergaard Nielsen, Tino Dyhring Joergensen, Philip K. Ahring
  • Patent number: 7220741
    Abstract: This invention relates to novel 1,4-diazabicycloalkane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention 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: Grant
    Filed: September 29, 2003
    Date of Patent: May 22, 2007
    Assignee: NeuroSearch A/S
    Inventors: Dan Peters, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Tino Dyhring Jørgensen, Philip K. Ahring
  • Patent number: 7211572
    Abstract: The present invention relates to a nitrogen-containing fused ring compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, and an anti-HIV agent containing such compound. The compound of the present invention has an HIV integrase inhibitory activity, and is useful as an agent for the prophylaxis or treatment of AIDS, or as an anti-HIV agent. In addition, by the combined use with other anti-HIV agents such as a protease inhibitor, a reverse transcriptase inhibitor and the like, it can be a more effective anti-HIV agent. Because it shows integrase-specific high inhibitory activity, the compound can be a pharmaceutical agent safe on human body, which causes only a fewer side effects.
    Type: Grant
    Filed: October 13, 2005
    Date of Patent: May 1, 2007
    Assignee: Japan Tobacco Inc.
    Inventors: Susumu Miyazaki, Susumu Katoh, Kaoru Adachi, Hirotaka Isoshima, Satoru Kobayashi, Yuji Matsuzaki, Wataru Watanabe, Kazunobu Yamataka, Shinichi Kiyonari, Shuichi Wamaki
  • Patent number: 7202238
    Abstract: 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: Grant
    Filed: April 2, 2003
    Date of Patent: April 10, 2007
    Assignee: 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
  • Patent number: 7189713
    Abstract: The present invention relates to piperidine derivatives of formula (I): R represents halogen or C1-4 alkyl R1 represents C1-4 alkyl; R2 or R3 independently represent hydrogen or C1-4 alkyl; R4 represents trifluoromethyl, C1-4 alkyl, C1-4 alkoxy, trifluoromethoxy or halogen; R5 represents hydrogen, C1-4 alkyl or C3-7 cycloalkyl; R6 is hydrogen and R7 is a radical of formula (W): ?or R6 is a radical of formula (W) and R7 is hydrogen; X represents CH2, NR5 or O; Y represents Nitrogen and Z is CH or Y represents CH and Z is Nitrogen; A represents C(O) or S(O)q, provided that when Y is nitrogen and Z is CH, A is not S(O)q; m is zero or an integer from 1 to 3; n is an integer from 1 to 3; p and q are independently an integer from 1 to 2; and pharmaceutically acceptable salts and solvates thereof. The process for their preparation and their use in the treatment of a condition mediated by tachykinins.
    Type: Grant
    Filed: February 10, 2003
    Date of Patent: March 13, 2007
    Assignee: Glaxo Group Limited
    Inventors: Giuseppe Alvaro, Romano Di Fabio, Maria Elvira Tranquillini, Simone Spada
  • Patent number: 7186721
    Abstract: Novel substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.
    Type: Grant
    Filed: April 27, 2005
    Date of Patent: March 6, 2007
    Assignee: Novo Nordisk A/S
    Inventors: Bernd Peschke, Rolf Hohlweg
  • Patent number: 7183273
    Abstract: Heterocyclic compounds that bind chemokine receptors and inhibit the binding of their natural ligands are disclosed. The invention compounds are protective against infection by HIV and exert effects characteristic of antagonists to the CXCR4 receptor.
    Type: Grant
    Filed: April 30, 2004
    Date of Patent: February 27, 2007
    Assignee: AnorMED, Inc.
    Inventors: Gary J. Bridger, Renato Skerlj, Al Kaller, Curtis Harwig, David Bogucki, Trevor R. Wilson, Jason Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols
  • Patent number: 7176200
    Abstract: The present invention relates to new derivatives of sulphonamides, with the general formula (I), as well as to their physiologically acceptable salts, the processes for their preparation, their application as medicaments in human and/or veterinary therapy and the pharmaceutical compositions that contain them
    Type: Grant
    Filed: September 3, 2004
    Date of Patent: February 13, 2007
    Assignee: Laboratories Del Dr. Esteve, S.A.
    Inventors: Ramón Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
  • Patent number: 7160874
    Abstract: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to ?4 integrin. They are used as therapeutic agents for various diseases concerning ?4 integrin.
    Type: Grant
    Filed: November 15, 2004
    Date of Patent: January 9, 2007
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yasuhiro Tanaka, Toshihiko Yoshimura, Hiroyuki Izawa, Chieko Ejima, Mitsuhiko Kojima, Yuko Satake, Eiji Nakanishi, Nobuyasu Suzuki, Shingo Makino, Manabu Suzuki, Masahiro Murata
  • Patent number: 7160877
    Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein A represents —CH2— or —S—, R1 represents hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group or a lower-alkoxy lower alkyl group, X represents —N(R3)—, —O— or —CO—, where R3 represents hydrogen atom or a lower alkyl group, and R2 represents (1) a cyclic group which may be substituted, or (2) an amino group which may be substituted, or a pharmaceutically acceptable salt thereof, a method for preparing the above-mentioned compound and a pharmaceutical composition comprising the above-mentioned compound as an effective ingredient.
    Type: Grant
    Filed: June 22, 2004
    Date of Patent: January 9, 2007
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Kosuke Yasuda, Hiroshi Morimoto, Saburo Kawanami, Masataka Hikota, Takeshi Matsumoto, Kenji Arakawa
  • Patent number: 7148215
    Abstract: The present invention concerns compounds of general formula (I): in which the substituents are as described herein.
    Type: Grant
    Filed: March 18, 2004
    Date of Patent: December 12, 2006
    Assignee: Aventis Pharma S.A.
    Inventors: Andrew James Ratcliffe, Roger John Aitchison Walsh, Tahir Nadeem Majid, Sukanthini Thurairatnam, Shelley Amendola, David John Aldous, John Edward Souness, Conception Nemecek, Sylvie Wentzler, Corinne Venot
  • Patent number: 7148224
    Abstract: The present invention relates to a compound of the general formula (I): [Ar1 is aryl fused to the adjacent pyrazinone ring at the 5th and 6th positions, etc., X is CO, etc., Y is CH, etc., Z is CH, etc., V is CH, etc., Wn is —(CH2)n— (n is zero to four), R1, is H or optionally substituted lower alkyl, etc., R2 is H, etc., R3 and R4 are the same or different and are each H, etc., R5 and R6 are the same or different and are each H, hydroxy, etc.] or a pharmaceutically acceptable salt or ester thereof; a pharmaceutical composition, an inhibitor of Cdk4 and/or Cdk6 or an anti-cancer agent, containing the same as an active ingredient; and a process for preparing them.
    Type: Grant
    Filed: April 14, 2005
    Date of Patent: December 12, 2006
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Takashi Hayama, Nobuhiko Kawanishi, Tooru Takaki
  • Patent number: 7144883
    Abstract: The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system
    Type: Grant
    Filed: June 11, 2002
    Date of Patent: December 5, 2006
    Assignee: Biovitrum AB
    Inventors: Patrizia Caldirola, Gary Johansson, Andrew Mott, Katarina Beierlien, Markus Thor, Lars Tedenborg, Ulf Bremberg, Annika Jenmalm Jensen
  • Patent number: 7125863
    Abstract: Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV.
    Type: Grant
    Filed: April 26, 2001
    Date of Patent: October 24, 2006
    Assignee: Ferring BV
    Inventors: David Michael Evans, Gary Robert William Pitt
  • Patent number: 7125877
    Abstract: This invention provides compounds which are represented by a general formula [I] [in which X stands for hydrogen or halogen; B stands for halogen, cyano or optionally fluorine-substituted lower alkyl; D stands for a 3–10 membered aliphatic nitrogen-containing heterocyclic group; R3, R4 and R5 may be same or different, and each stands for hydrogen, lower alkyl optionally having substituent group(s) and the like; and a is 0 or 1]. These compounds exhibit high affinity to nociceptin receptors and whereby inhibit actions of nociceptin, and are useful as an analgesic, antiobestic, agent for ameliorating brain function, treating agents for Alzheimer's disease and dementia, and therapeutic agents for schizophrenia, neurodegenerative diseases, depression, diabetes insipidus, polyuria, hypotension and the like.
    Type: Grant
    Filed: May 14, 2003
    Date of Patent: October 24, 2006
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Kensuke Kobayashi, Hirobumi Takahashi, Hiroshi Kawamoto, Tetsuya Kato, Satoru Itoh, Takashi Yoshizumi, Osamu Okamoto
  • Patent number: 7115654
    Abstract: The invention provides compounds of Formula I and derivatives thereof, pharmaceutical compositions comprising a compound of Formula I, and methods of treatment utilizing such compounds and compositions: wherein: R1 is chosen from optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, and optionally substituted heteroaralkyl; L is a linker; R2 is chosen from optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, and optionally substituted heteroaralkyl; and or single stereoisomers, mixtures of stereoisomers, or the pharmaceutically acceptable salts, amides, or esters thereof.
    Type: Grant
    Filed: June 5, 2003
    Date of Patent: October 3, 2006
    Assignee: Sunesis Pharmaceuticals, Inc.
    Inventors: Darin Allen, Bruce Fahr, Johan Oslob, Brian C. Raimundo, Michael J. Romanowski
  • Patent number: 7115600
    Abstract: This invention is directed to a compound of the formula I as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by modulating histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of depression, mood disorders, schizophrenia, anxiety disorders, Alzheimer's disease, attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper and hypo motility and acidic secretion of the gastro-intestinal tract, the method comprising a
    Type: Grant
    Filed: January 28, 2005
    Date of Patent: October 3, 2006
    Assignee: Pfizer Inc.
    Inventors: Travis T. Wager, Ramalakshmi Y. Chandrasekaran
  • Patent number: 7087750
    Abstract: The invention provides 2, 3-, 4- or 5-substituted-N1-(arylsulfonyl)indole and (heteroaryl)indole compounds of the general formula (I): in which Ar, R2, R3, R4 and R5 are as defined in the specification. The compounds bind to the 5-HT6 receptor and are useful for the treatment and prophylaxis of disorders mediated by the 5-HT6 receptor, such as obesity and CNS disorders.
    Type: Grant
    Filed: October 22, 2001
    Date of Patent: August 8, 2006
    Assignee: Biovitrum AB
    Inventors: Patrizia Caldirola, Björn M. Nilsson, Gary Johansson
  • Patent number: 7074534
    Abstract: The present invention relates to polymeric charge transport compositions. The invention further relates to electronic devices in which there is at least one active layer comprising such charge transport compositions.
    Type: Grant
    Filed: July 2, 2003
    Date of Patent: July 11, 2006
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Norman Herron, Nora Sabina Radu, Eric Maurice Smith
  • Patent number: 7071180
    Abstract: The invention relates to compounds of the general formula (I): wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO2—, —NH—, (ii) a C1-4-alkyl- or C1-6-acyl-substituted nitrogen atom or (iii) a C1-8-alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is —C(R4)(R5)—, —OC(R4)(R5)—, —N(R6)C(R4)(R5)—, —N(R6)—, —O—, —S— or —SO2—; R is optionally substituted C3-8-cycloalkyl, aryl or heteroaryl; R1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ring members, which rings optionally are substituted in one or more positions, or a group —[C(R4)(R5)]xN(R2a)(R3a)]; R2a, R3a, R4, R5, R6 and x are as
    Type: Grant
    Filed: June 22, 2004
    Date of Patent: July 4, 2006
    Assignee: Biovitrum AB
    Inventors: Björn Nilsson, Jan Tejbrant, Benjamin Pelcman, Erik Ringberg, Markus Thor, Jonas Nilsson, Mattias Jönsson
  • Patent number: 7056922
    Abstract: A compound of the formula wherein D, E, F, G, L, T, W, X, Y, Z, U, A, R1, R2, R3, R4, R5, R6 R7 are as defined in the specification, pharmaceutical compositions thereof, and methods of use to treat diseases and as D3 receptor modulators.
    Type: Grant
    Filed: July 29, 2003
    Date of Patent: June 6, 2006
    Assignee: Pfizer Inc
    Inventors: Anton F. J. Fliri, Anthony R. Reinhold
  • Patent number: 7037911
    Abstract: The present invention relates generally to compounds that inhibit serine proteases. In particular it is directed to novel amino-bicyclic pyrazinone and pyridinone compounds of Formula (I): or a stereoisomer or pharmaceutically acceptable salt form thereof, which are useful as selective inhibitors of serine protease enzymes of the coagulation cascade; for example thrombin, factor Xa, factor XIa, factor IXa, and/or factor VIIa. In particular, it relates to compounds that are factor VIIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.
    Type: Grant
    Filed: June 19, 2003
    Date of Patent: May 2, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventor: Xiaojun Zhang
  • Patent number: 7026318
    Abstract: A compound represented by the general formula: wherein R20 is —CH2COOH and the like; R21 is —COCONH2 and the like; R22 is C4–C6 alkyl; and the like; R23 is —CH2—R18 wherein R18 is aryl and the like; R24 is hydrogen or C1–C6 alkyl and the like; an optical active compound, a prodrug thereof, or a pharmaceutically acceptable salt, or a solvate having type X sPLA2 inhibitory effect was found.
    Type: Grant
    Filed: June 27, 2001
    Date of Patent: April 11, 2006
    Assignee: Shionogi & Co., Ltd.
    Inventors: Tomoyuki Ogawa, Kaoru Seno, Kohji Hanasaki, Minoru Ikeda, Takashi Ono
  • Patent number: 6992085
    Abstract: A compound selected from those of formula (I): wherein: Ra represents linear or branched (C1–C6)alkylene, X represents a group selected from W1, —C(W1)—W2—, —W2—C(W1)—, —W2—C(W1)W2—, —W2—Ra— and —CH(OR1)— wherein W1, W2 and R1 are as defined in the description, when Y represents aryl or heteroaryl, or X represents a group selected from single bond, —C(W1)—, —W2—C(W1)—, —W2—Ra and —CH(OR1)— wherein W1, W2, Ra and R1 are as defined hereinbefore, when Y represents a fused bicyclic group, of formula: wherein: A represents nitrogen-containing heterocycle having from 4 to 7 ring members that is unsaturated or partially saturated and optionally contains a second hetero atom, B represents phenyl ring optionally substituted by one or more groups as defined in the description, its isomers, and addition salts thereof with a pharmaceutically acceptable acid or base, medicinal products containing the same are useful in the treatment of cognitive deficiencies.
    Type: Grant
    Filed: July 12, 2002
    Date of Patent: January 31, 2006
    Assignee: Les Laboratories Servier
    Inventors: Solo Goldstein, Guillaume Poissonnet, Jean-Gilles Parmentier, Pierre Lestage, Brian Lockhart
  • Patent number: 6969713
    Abstract: The invention provides piperidine and piperazine derivatives of general formula (I), processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy
    Type: Grant
    Filed: December 18, 2000
    Date of Patent: November 29, 2005
    Assignee: AstraZeneca AB
    Inventors: Premji Meghani, Colin Bennion
  • Patent number: 6930104
    Abstract: The object of the present invention is to provide soluble ?-amyloid precursor protein secretory stimulators, which are effective in treating neurodegenerative diseases as well as cerebrovascular disorder-induced neuronopathy. More specifically, the present invention provides a novel compound of the following Formula (I) or a salt or prodrug thereof: [wherein R1 and R2 each represent a hydrogen atom or a lower alkyl group, etc., Ar1 and the ring B each represent an optionally substituted aromatic group, the ring A represents an optionally substituted benzene ring, the ring C represents an optionally substituted 4- to 8-membered ring which may further be condensed with an optionally substituted ring, X represents CH or N, and Y represents CH or N].
    Type: Grant
    Filed: April 25, 2002
    Date of Patent: August 16, 2005
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Mitsuru Kakihana, Kaneyoshi Kato, Masaaki Mori, Toshiro Yamashita
  • Patent number: 6927214
    Abstract: Novel non-peptide GLP-1 agonists, pharmaceutical compositions comprising them, use of the non-peptide GLP-1 agonists for the preparation of pharmaceutical compositions and methods for the treatment and/or prevention of disorders and diseases wherein an activation of the human GLP-1 receptor is beneficial, especially metabolic disorders such as IGT, Type 1 diabetes, Type 2 diabetes and obesity.
    Type: Grant
    Filed: January 14, 2000
    Date of Patent: August 9, 2005
    Assignee: Novo Nordisk A/S
    Inventors: Min Teng, Larry Kenneth Truesdale, Dilip Bhumralkar, Dan Kiel, Michael D. Johnson, Christine Thomas, Anker Steen Jorgensen, Peter Madsen, Preben Houlberg Olesen, Liselotte Bjerre Knudsen, Ingrid Vivika Petterson, Johannes Cornelis de Jong, Carsten Behrens, Janos Tibor Kodra, Jesper Lau
  • Patent number: 6921759
    Abstract: Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: October 10, 2001
    Date of Patent: July 26, 2005
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Robert P. Gomez, Steven D. Young, Melissa Egbertson, John S. Wai, Linghang Zhuang, Mark Embrey, Jeffrey Y. Melamed, H. Marie Langford, James P. Guare, Thorsten E. Fisher, Samson M. Jolly, Michelle S. Kuo, Debra S. Perlow, Jennifer J. Bennett, Timothy W. Funk
  • Patent number: 6906060
    Abstract: Novel substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.
    Type: Grant
    Filed: June 3, 2003
    Date of Patent: June 14, 2005
    Assignee: Novo Nordisk A/S
    Inventors: Bernd Peschke, Rolf Hohlweg
  • Patent number: 6897215
    Abstract: Novel 6-bicyclopiperazinyl-1-arylsulfonylindole and 6-bicyclopiperidinyl-1-arylsulfonylindole compounds are disclosed which are useful as 5-HT6 receptor antagonists in the treatment of central nervous system disorders such as schizophrenia, depression, ADHD, and cognition and memory dysfunction The compounds are Formula I wherein: R1 is H or C1-4 alkyl; X is CH, —C—OR3, ?C, or —N and Y is C-R2 or N; R3 is H or —C(O)-R4; R4 is H or a labile prodrug group; n is 1 or 2; m and o are, independently, 0, 1, or 2 with the proviso that m+o is 1 or 2; and Ar is an aryl or heteroaryl group optionally substituted with 1-3 substitutents.
    Type: Grant
    Filed: November 4, 2000
    Date of Patent: May 24, 2005
    Assignee: NPS Allelix Corp.
    Inventors: Tao Xin, Methvin Isaac, Abdelmalik Slassi
  • Patent number: 6894005
    Abstract: Compounds of formula wherein the substituents have the meanings given in claim 1, and agronomically tolerable salts, isomers and enantiomer of those compounds, are suitable for use as herbicides.
    Type: Grant
    Filed: September 5, 2000
    Date of Patent: May 17, 2005
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Thomas Maetzke, André Stoller, Sebastian Wendeborn, Henry Szczepanski
  • Patent number: 6887870
    Abstract: Heterocyclic are provided which are sodium/proton exchange (NHE) inhibitors which have the structure wherein n is 1 to 5; X is N or C—R5 wherein R5 is H, halo, alkenyl, alkynyl, alkoxy, alkyl, aryl or heteroaryl; Z is a heteroaryl gorup, R1, R2, R3 and R4 are as defined herein, and where X is N. R1 is preferably aryl or heteroaryl, and are useful as antianginal and cardioprotective agents. In addition, a method is provided for preventing or treating angina pectoris, cardiac dysfunction, myocardial necrosis, and arrhythmia employing the above heterocyclic derivatives.
    Type: Grant
    Filed: September 25, 2000
    Date of Patent: May 3, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Saleem Ahmad, Shung C. Wu, Steven V. O'Neil, Khehyong Ngu, Karnail S. Atwal, David S. Weinstein
  • Patent number: 6858613
    Abstract: The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat conditions or diseases in which ?7 is known to be involved.
    Type: Grant
    Filed: February 14, 2003
    Date of Patent: February 22, 2005
    Assignee: Pfizer Inc.
    Inventors: Bruce N. Rogers, David W. Piotrowski, Daniel Patrick Walker, Eric Jon Jacobsen, Brad A. Acker, Donn G. Wishka, Vincent E. Groppi, Jr.
  • Patent number: 6858611
    Abstract: Compounds which are useful as potassium channel inhibitors and which because of their slow off-rates are especially useful for the treatment of cardiac arrhythmias are described.
    Type: Grant
    Filed: March 19, 2003
    Date of Patent: February 22, 2005
    Assignee: Icagen, Inc.
    Inventors: Aimee Dolores Reed, Michael Francis Gross, Serge Beaudoin
  • Patent number: 6858610
    Abstract: Compounds as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.
    Type: Grant
    Filed: August 2, 2002
    Date of Patent: February 22, 2005
    Assignee: ICAgen, Inc.
    Inventors: Michael Gross, Serge Beaudoin, Aimee D. Reed
  • Patent number: 6855706
    Abstract: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to ? 4 integrin. They are used as therapeutic agents for various diseases concerning ? 4 integrin.
    Type: Grant
    Filed: May 20, 2002
    Date of Patent: February 15, 2005
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yasuhiro Tanaka, Toshihiko Yoshimura, Hiroyuki Izawa, Chieko Ejima, Mitsuhiko Kojima, Yuko Satake, Eiji Nakanishi, Nobuyasu Suzuki, Shingo Makino, Manabu Suzuki, Masahiro Murata
  • Patent number: 6852712
    Abstract: This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor or p56lck tyrosine kinase activity, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.
    Type: Grant
    Filed: February 4, 2003
    Date of Patent: February 8, 2005
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Michael R. Myers, Wei He, Alfred P. Spada, Martin P. Maguire
  • Patent number: 6852721
    Abstract: The present invention relates to diazabicyclic compounds, preferably to N-aryl diazabicyclic compounds. Of particular interest are 2-pyridinyl diazabicyclic compounds, such as (1S,4S)-2-(5-(3-methoxyphenoxy)-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane. Other exemplary compounds of the present invention include (1S,4S)-2-(5-(4-methoxyphenoxy)-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane, (1S,4S)-2-(5-(3-thienyl)-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane, (1S,4S)-2-(5-(4-fluorophenoxy)-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane, and (1S,4S)-2-(5-benzoyl-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane. The present invention also relates to prodrug derivatives of the compounds of the present invention.
    Type: Grant
    Filed: May 24, 2001
    Date of Patent: February 8, 2005
    Assignee: Targacept, Inc.
    Inventors: Craig Harrison Miller, Gary Maurice Dull, Lan Miao, Dwo Lynm, Jeffrey Daniel Schmitt, Thomas Jeffrey Clark
  • Patent number: 6849634
    Abstract: Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.
    Type: Grant
    Filed: December 7, 2001
    Date of Patent: February 1, 2005
    Assignee: ICAgen
    Inventors: Serge Beaudoin, Aimee D. Reed, Michael F. Gross
  • Patent number: 6849622
    Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein A represents —CH2— or —S—, R1 represents hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group or a lower alkoxy lower alkyl group, X represents —N(R3)—, —O— or —CO—, where R3 represents hydrogen atom or a lower alkyl group, and R2 represents (1) a cyclic group which may be substituted, or (2) an amino group which may be substituted, or a pharmaceutically acceptable salt thereof, a method for preparing the above-mentioned compound and a pharmaceutical composition comprising the above-mentioned compound as an effective ingredient.
    Type: Grant
    Filed: October 5, 2001
    Date of Patent: February 1, 2005
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Kosuke Yasuda, Hiroshi Morimoto, Saburo Kawanami, Masataka Hikota, Takeshi Matsumoto, Kenji Arakawa
  • Patent number: 5125102
    Abstract: A digitally trunked radio repeater system provides substantial improvements in timeliness of channel acquisition and channel drop, and in reliability of critical control signalling. The system uses a much higher digital signalling rate than is typically found in prior art systems, and uses a control channel to convey digital channel request and assignment messages between the central site and mobile transceivers. The mobile radio transceivers transmit channel requests on the control channel (if no response is received, the mobile retries during a retry time window which increases in duration in dependence on the number of retries). The mobile transceiver switches to a working channel in response to an assignement message received on the control channel. Subaudible digital signals transmitted on the control channel and on active working channels allow late entry, shifting to higher priority calls, and other advanced functions.
    Type: Grant
    Filed: January 3, 1990
    Date of Patent: June 23, 1992
    Assignee: Ericsson GE Mobile Communications Inc.
    Inventors: Jeffrey S. Childress, Marc A. Dissosway, Gerald M. Cooper, Houston H. Hughes, III