The Bicyclo Ring System Is 1,5-benzodiazepine (including Hydrogenated) Patents (Class 540/517)
  • Publication number: 20150038495
    Abstract: To provide a cancer pain therapeutic and/or prophylactic agent which can be administered to a patient for a long period of time from the early stage to the final stage of the cancer pain therapy, instead of conventional non-opioid analgesic agents or opioid analgesic agents. The cancer pain therapeutic and/or prophylactic agent containing, as an active ingredient, a 1,5-benzodiazepine derivative represented by formula (1): (wherein R1 represents a C1-6 alkyl group, R2 represents a phenyl group or a cyclohexyl group, and Y represents a single bond or a C1-4 an alkylene group) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: September 24, 2014
    Publication date: February 5, 2015
    Applicant: Zeria Pharmaceutical Co., Ltd.
    Inventors: Koji YOSHINAGA, Hiroki Hamano, Takayuki Hori
  • Publication number: 20150025064
    Abstract: The present invention relates to novel benzodiazepinone compounds of Formulae (I) wherein R1, R2, R4, R6, R7, R8, R9, and R10 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, methods of use of such compounds and compositions, and methods for preparing the compounds and compositions. The compounds are Group II metabotropic glutamate antagonists or allosteric modulators and are useful for the treatment of a variety of CNS disorders.
    Type: Application
    Filed: August 29, 2012
    Publication date: January 22, 2015
    Applicant: Sanford-Burnham Medical Research Institute
    Inventors: John Howard Hutchinson, Leo Bleicher, Nick Cosford, Robert John Ardecky, Jiwen Zou
  • Patent number: 8741889
    Abstract: The present invention provides a method for treating a patient having cancer comprising administering to the patient a therapeutically effective amount of compound (1), or a pharmaceutically acceptable salt thereof, having the formula: The present invention also provides a kit containing the above compound.
    Type: Grant
    Filed: April 19, 2012
    Date of Patent: June 3, 2014
    Assignee: Hoffmann-La Roche Inc
    Inventors: John Frederick Boylan, Leopoldo Ladores Luistro, Kathryn Elizabeth Packman
  • Publication number: 20130109019
    Abstract: Embodiments of hapten conjugates including a hapten, an optional linker, and a peroxidase-activatable aryl moiety are disclosed. In some embodiments, the peroxidase-activatable aryl moiety is tyramine or a tyramine derivative. Embodiments of methods for making and using the hapten conjugates also are disclosed. In particular embodiments, the hapten conjugates are used in a signal amplification assay. In certain embodiments, the hapten is an oxazole, a pyrazole, a thiazole, a benzofurazan, a triterpene, a urea, a thiourea other than a rhodamine thiourea, a nitroaryl other than dinitrophenyl or trinitrophenyl, a rotenoid, a cyclolignan, a heterobiaryl, an azoaryl, a benzodiazepine, or 7-diethylamino-3-carboxycoumarin. The hapten is coupled to the peroxidase-activatable aryl moiety directly or indirectly via a linker. In certain embodiments, the hapten conjugates are used in multiplexed assays.
    Type: Application
    Filed: July 1, 2011
    Publication date: May 2, 2013
    Inventors: Adrian E. Murillo, Jerome W. Kosmeder, Eric May, William Day, Mark Lefever, Anne M. Pedata, Christopher Bieniarz, Phillip Miller
  • Patent number: 8314694
    Abstract: The present invention is concerned with an alarm system and a method for suppressing redundant alarms in a monitored system. The alarm system comprises a process control unit, an FDI unit, a filter, and an alarm display unit. The process control unit detects anomalies in the monitored system and generates alarms corresponding to them. The FDI unit diagnoses failures in the monitored system and generates a failure-cause-effect graph comprising a list of generated alarms, along with the alarms corresponding to the causes and effects of each listed alarm. The FDI unit dynamically updates the failure-cause-effect graph concurrently with the generation of alarms by the process control unit and the diagnosis of failures by the FDI unit. The filter receives the generated alarms and identifies redundant and not-yet-classified alarms from the received alarms, by using the failure-cause-effect graph.
    Type: Grant
    Filed: June 28, 2004
    Date of Patent: November 20, 2012
    Assignee: ABB Research Ltd
    Inventors: Martin Naedele, Christian Frei, Patrick Sager, Alexander Fay
  • Publication number: 20120283249
    Abstract: The subject matter of the present invention is novel families of compounds which are aromatic amine, imine, aminoadamantane and benzodiazepine derivatives, medicaments comprising same and the use thereof as inhibitors of the toxic effects of toxins with intracellular activity, such as, for example, ricin, and of viruses that use the internalization pathway for infecting cells.
    Type: Application
    Filed: June 17, 2009
    Publication date: November 8, 2012
    Inventors: Roman Lopez, Séverine Hebbe, Daniel Gillet, Julien Barbier
  • Patent number: 8119631
    Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1? converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-?-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-?-mediated diseases and decreasing IGIF and IFN-? production using the compounds and compositions of this invention.
    Type: Grant
    Filed: May 24, 2010
    Date of Patent: February 21, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Mark James Batchelor, David Bebbington, Guy W. Bemis, Wolf Herman Fridman, Roger John Gillespie, Julian M. C. Golec, Yong Gu, David J. Lauffer, David J. Livingston, Saroop Singh Matharu, Michael D. Mullican, Mark A. Murcko, Robert Murdoch, Philip Nyce, Andrea L. C. Robidoux, Michael Su, M. Woods Wannamaker, Keith P. Wilson, Robert E. Zelle
  • Publication number: 20120010401
    Abstract: An industrially advantageous method for producing a 1,5-benzodiazepine compound is provided. A compound (5) is obtained according to the reaction scheme shown below, and this compound is used as an intermediate.
    Type: Application
    Filed: March 29, 2010
    Publication date: January 12, 2012
    Applicant: Zeria Pharmaceutical Co., Ltd.
    Inventor: Masaru Terauchi
  • Patent number: 7994161
    Abstract: The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide derivatives, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds, and to intermediate precursors to such compounds.
    Type: Grant
    Filed: November 10, 2008
    Date of Patent: August 9, 2011
    Assignee: Sanofi-Aventis
    Inventors: Jidong Zhang, Yannick Benedetti, Alain Commerçon
  • Publication number: 20110059956
    Abstract: To provide a cancer pain therapeutic and/or prophylactic agent which can be administered to a patient for a long period of time from the early stage to the final stage of the cancer pain therapy, instead of conventional non-opioid analgesic agents or opioid analgesic agents. The cancer pain therapeutic and/or prophylactic agent containing, as an active ingredient, a 1,5-benzodiazepine derivative represented by formula (1): (wherein R1 represents a C1-6 alkyl group, R2 represents a phenyl group or a cyclohexyl group, and Y represents a single bond or a C1-4 an alkylene group) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: May 14, 2009
    Publication date: March 10, 2011
    Applicant: ZERIA PHARMACEUTICAL CO., LTD.
    Inventors: Koji Yoshinaga, Hiroki Hamano, Takayuki Horii
  • Patent number: 7842686
    Abstract: The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions.
    Type: Grant
    Filed: January 21, 2009
    Date of Patent: November 30, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Corey Don Anderson, Andreas P. Termin, Pramod Joshi, Sara S. Hadida Ruah, Daniele Bergeron, Sanghee Yoo, Jingrong Cao
  • Patent number: 7790713
    Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1? converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-?-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-?-mediated diseases and decreasing IGIF and IFN-? production using the compounds and compositions of this invention.
    Type: Grant
    Filed: January 18, 2007
    Date of Patent: September 7, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Mark James Batchelor, David Bebbington, Guy W. Bemis, Wolf Herman Fridman, Roger John Gillespie, Julian M. C. Golec, Yong Gu, David J. Lauffer, David J. Livingston, Saroop Singh Matharu, Michael D. Mullican, Mark A. Murcko, Robert Murdoch, Philip Nyce, Andrea L. C. Robidoux, Michael Su, M. Woods Wannamaker, Keith P. Wilson, Robert E. Zelle
  • Patent number: 7759346
    Abstract: This invention provides a method of treating pain in a mammal that includes administering to a mammal in need of such treatment a pain treating effective amount of a compound of the formula (I): where R1 is H, alkyl or phenylalkyl; R2 is H, alkyl, alkenyl or phenylalkyl; or R1 and R2 taken together as Z are —CH2C—H2—, —CH2C(R6)(R7)CH2— or —CH2C(R8)(R9)—C(R10)(R11)CH2—, where R6, R8 and R10 are, independently, H, alkyl or hydroxyl and R7, R9 and R11 are, independently, H or alkyl; A is alkylene or alkenylene; X is CO2R3, P(O)(OR4)(OR5), 3,5-dioxo-1,2,4-oxadiazolidin-2-yl or 5-tetrazolyl in which R3, R4 and R5 are, independently, H or alkyl, or a pharmaceutically acceptable salt thereof. The present invention also provides pharmaceutical compositions for treating pain containing a pain treating effective amount of the compound of formula (I).
    Type: Grant
    Filed: May 12, 2006
    Date of Patent: July 20, 2010
    Assignee: Wyeth LLC
    Inventors: Michael Richard Brandt, Margaret Maria Zaleska, John Allen Moyer
  • Publication number: 20100144715
    Abstract: The present invention is directed to substituted benzodiazepinones, benzoxazepinones and benzothiazepinones compounds that are sodium channel blockers useful for the treatment of chronic and neuropathic pain. The compounds of the present invention are also useful for the treatment of other conditions, including disorders of the CNS such as anxiety, depression, epilepsy, manic depression and bipolar disorder. This invention also provides pharmaceutical compositions comprising a compound of the present invention, either alone, or in combination with one or more therapeutically active compounds, and a pharmaceutically acceptable carrier. This invention further comprises methods for the treatment of acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain and disorders of the CNS including, but not limited to, epilepsy, manic depression, depression, anxiety and bipolar disorder comprising administering the compounds and pharmaceutical compositions of the present invention.
    Type: Application
    Filed: February 25, 2008
    Publication date: June 10, 2010
    Inventors: Scott B. Hoyt, Dong Ok, Hyun Ok, Clare London, Joseph I. Duffy
  • Patent number: 7718795
    Abstract: This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Grant
    Filed: April 2, 2008
    Date of Patent: May 18, 2010
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventor: Richard E. Olson
  • Publication number: 20090176771
    Abstract: The present invention relates to compounds which inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.
    Type: Application
    Filed: October 7, 2008
    Publication date: July 9, 2009
    Inventors: Paul Charifson, David Deininger, Anne-Laure Grillot, Yusheng Liao, Steven Ronkin, Dean Stamos, Emanuele Perola, Tiansheng Wang, Arnaud Le Tiran, Joseph Drumm
  • Patent number: 7528249
    Abstract: This invention relates to novel cyclic malonamides having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Grant
    Filed: June 19, 2008
    Date of Patent: May 5, 2009
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Richard E. Olson, Michael G. Yang
  • Patent number: 7511033
    Abstract: The present invention relates to compounds of formula (I), a process for the manufacture thereof, their use for the preparation of medicaments for treating CNS disorders and pharmaceutical compositions containing them. Compounds of formula (I) are represented by general formula (I) wherein R1, R2, R3 and R4 are defined as in the specification.
    Type: Grant
    Filed: April 14, 2008
    Date of Patent: March 31, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Silvia Gatti McArthur, Juergen Wichmann, Thomas Johannes Woltering
  • Publication number: 20080293692
    Abstract: This invention relates to novel lactams having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Application
    Filed: December 4, 2007
    Publication date: November 27, 2008
    Applicant: BRISTOL-MYERS SQUIBB PHARMA COMPANY
    Inventors: Richard E. Olson, Thomas P. Maduskuie, Lorin Andrew Thompson
  • Publication number: 20080261957
    Abstract: The present invention relates to compounds of formula (I), a process for the manufacture thereof, their use for the preparation of medicaments for treating CNS disorders and pharmaceutical compositions containing them. Compounds of formula (I) are represented by general formula (I) wherein R1, R2, R3 and R4 are defined as in the specification.
    Type: Application
    Filed: April 14, 2008
    Publication date: October 23, 2008
    Inventors: Silvia Gatti McArthur, Juergen Wichmann, Thomas Johannes Woltering
  • Publication number: 20080234250
    Abstract: The invention concerns compounds according to general formulae 1, wherein G1 is an amine. Compounds according to the invention are vasopressin V2 receptor agonists. Pharmaceutical compositions of the compounds are useful as antidiuretic agents.
    Type: Application
    Filed: August 18, 2005
    Publication date: September 25, 2008
    Inventor: Gary Robert William Pitt
  • Patent number: 7414049
    Abstract: The invention relates to 4-oxo-2,3,4,5-tetrahydro-benzo [b][1,4]diazepines of formula I wherein R1, R2, R3 and R4 are as defined in the description and claims, which are ?-secretase inhibitors and which may be useful in the treatment of Alzheimer's disease.
    Type: Grant
    Filed: September 14, 2007
    Date of Patent: August 19, 2008
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Flohr, Roland Jakob-Roetne, Wolfgang Wostl
  • Patent number: 7390802
    Abstract: This invention relates to novel lactams of Formula (I): having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Grant
    Filed: January 19, 2007
    Date of Patent: June 24, 2008
    Assignee: Bristol-Myers Squibb Pharma Corporation
    Inventors: Qi Han, Hong Liu, Richard E. Olson, Michael G. Yang
  • Patent number: 7390801
    Abstract: Disclosed are compounds which inhibit ?-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits ?-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: May 12, 2006
    Date of Patent: June 24, 2008
    Assignees: Athena Neurosciences, Inc., Eli Lilly and Company
    Inventors: Eugene D. Thorsett, Michael A. Pleiss, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Bruce A. Dressman, James J. Droste, Steven S. Henry, Russell D. Stucky, Warren J. Porter
  • Patent number: 7375099
    Abstract: The invention relates to malonamide derivatives of formula wherein each of the variables are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The compounds are ?-secretase inhibitors. Thus, the invention also relates to pharmaceutical compositions containing these compounds and to a method of treating Alzheimer's disease by administering the compounds of the invention.
    Type: Grant
    Filed: January 29, 2004
    Date of Patent: May 20, 2008
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Annick Goergler, Helmut Jacobsen, Eric Argirios Kitas, Jens-Uwe Peters
  • Patent number: 7304056
    Abstract: This invention relates to novel lactams having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Grant
    Filed: July 26, 2006
    Date of Patent: December 4, 2007
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Richard E. Olson, Thomas P. Maduskuie, Lorin Andrew Thompson
  • Patent number: 7166587
    Abstract: The present invention provides compounds of the general formula wherein R4 is one of the following groups ?and R1, R2, R3, R7, R8, and R9 are as defined in the specification and pharmaceutically acceptable salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. The compounds are useful for the treatment of Alzheimer's disease.
    Type: Grant
    Filed: September 27, 2004
    Date of Patent: January 23, 2007
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Flohr, Guido Galley, Roland Jakob-Roetne, Eric Argirios Kitas, Jens-Uwe Peters, Wolfgang Wostl
  • Patent number: 7160875
    Abstract: The invention relates to malonamide derivatives of formula wherein each of the variables are as defined herein and to pharmaceutically acceptable acid addition salts, optically pure enantiomers, racemates and diastereomeric mixtures thereof. These compounds are ?-secretase inhibitors and may be used for the treatment of Alzheimer's disease.
    Type: Grant
    Filed: September 2, 2004
    Date of Patent: January 9, 2007
    Assignee: Hoffmann-La Rache Inc.
    Inventors: Alexander Flohr, Guido Galley, Roland Jakob-Roetne, Eric Argirios Kitas, Jens-Uwe Peters, Wolfgang Wostl
  • Patent number: 7151098
    Abstract: The present invention is a compound of formula wherein X is an ethynediyl group, R1, R2 and R3 are as defined in the specification.
    Type: Grant
    Filed: February 27, 2006
    Date of Patent: December 19, 2006
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Geo Adam, Alexander Alanine, Erwin Goetschi, Vincent Mutel, Thomas Johannes Woltering
  • Patent number: 7112583
    Abstract: This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Grant
    Filed: December 28, 2004
    Date of Patent: September 26, 2006
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Richard E. Olson, Hong Liu, Lorin A. Thompson
  • Patent number: 7053084
    Abstract: This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Grant
    Filed: February 17, 2000
    Date of Patent: May 30, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventor: Richard E. Olson
  • Patent number: 7018998
    Abstract: The present invention is a compound of formula wherein X is an ethynediyl group, R1, R2 and R3 are as defined in the specification.
    Type: Grant
    Filed: June 7, 2005
    Date of Patent: March 28, 2006
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Geo Adam, Alexander Alanine, Erwin Goetschi, Vincent Mutel, Thomas Johannes Woltering
  • Patent number: 6962913
    Abstract: This invention relates to novel compounds of the class of succinoyl lactams, such as diazepinee of Formula (Id), or a pharmaceutically acceptable salt thereof, as described above, having drug and bio-affecting properties. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of Alzheimer's disease.
    Type: Grant
    Filed: November 1, 2002
    Date of Patent: November 8, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Richard E. Olson, Thomas P. Maduskuie, Lorin Andrew Thompson
  • Patent number: 6960578
    Abstract: The present invention is a compound of formula wherein X is an ethynediyl group, R1, R2 and R3 are as defined in the specification.
    Type: Grant
    Filed: November 20, 2002
    Date of Patent: November 1, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Geo Adam, Alexander Alanine, Erwin Goetschi, Vincent Mutel, Thomas Johannes Woltering
  • Patent number: 6949542
    Abstract: This invention relates to dihydro-benzo[b][1,4]diazepin-2-one derivatives of the formula wherein R1, R2, X and Y are as defined in the specification and R3 is a six-membered aromatic heterocycle containing 1 to 3 nitrogen atoms or a pyridine-N-oxide as further defined in the specification. The invention further relates to medicaments containing these compounds, a process for their preparation as well as their use for preparation of medicaments for the treatment or prevention of acute and/or chronic neurological disorders.
    Type: Grant
    Filed: January 24, 2003
    Date of Patent: September 27, 2005
    Assignee: Hoffman-La Roche Inc.
    Inventors: Geo Adam, Erwin Goetschi, Juergen Wichmann, Thomas Johannes Woltering
  • Patent number: 6916805
    Abstract: This invention discloses quinoxalinones which display inhibitory effects on serine proteases such as factor Xa, thrombin, and/or factor VIIa. The invention also discloses pharmaceutically acceptable salts and prodrugs of the compounds, pharmaceutically acceptable compositions comprising the compounds, their salts or prodrugs, and methods of using them as therapeutic agents for treating or preventing disease states in mammals characterized by abnormal thrombosis.
    Type: Grant
    Filed: January 4, 2002
    Date of Patent: July 12, 2005
    Assignee: Warner-Lambert Company LLC
    Inventors: Danette Andrea Dudley, Jeremy John Edmunds
  • Patent number: 6838455
    Abstract: Disclosed are compounds which inhibit ?-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits ?-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: December 23, 2002
    Date of Patent: January 4, 2005
    Assignees: Athena Neurosciences, Inc., Eli Lilly & Company
    Inventors: James E. Audia, Warren J. Porter, Richard C. Thompson, Stephen C. Wilkie, Douglas R. Stack, Qing Shi
  • Publication number: 20040198717
    Abstract: Compounds of structural formula (I) are disclosed as useful for modulating the androgen receptor (AR) in a tissue selective manner in a patient in need of such modulation, and in particular for antagonizing AR in the prostate of a male patient or in the uterus of a female patient and agonizing AR in bone and/or muscle tissue. These compounds are useful in the treating conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including: osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, female sexual dysfunction, post-menopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, prostate cancer, arthritis and joint repair, alone or in combination with other active agents.
    Type: Application
    Filed: April 16, 2004
    Publication date: October 7, 2004
    Inventors: Paul J Coleman, Lou Anne Neilson
  • Patent number: 6774125
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: October 7, 2002
    Date of Patent: August 10, 2004
    Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & Company
    Inventors: James E. Audia, Richard C. Thompson, Stephen C. Wilkie, Thomas C. Britton, Warren J. Porter, George W. Huffman, Lee H. Latimer
  • Publication number: 20040121996
    Abstract: The present invention provides compounds of Formula I 1
    Type: Application
    Filed: December 8, 2003
    Publication date: June 24, 2004
    Inventors: Nicole Barvian, Christine Nylund Kolz, Kimberly Suzanne Para, William Chester Patt, Melean Visnick
  • Patent number: 6747022
    Abstract: Provided are calcium salts of a 1,5-benzodiazepine derivative represented by the following formula (I): (wherein, R1 represents a lower alkyl group, R2 represents a phenyl or cyclohexyl group, and Y represents a single bond or a lower alkylene group); a process for preparing the salts; and drugs containing the same as the active ingredient. The compounds exhibit a potent inhibitory activity against the secretion of gastric acid and potent antagonism against gastrin and/or CCK-B receptor.
    Type: Grant
    Filed: August 15, 2002
    Date of Patent: June 8, 2004
    Assignee: Zeria Pharmaceutical Co., Ltd.
    Inventors: Katsuo Shinozaki, Masakazu Murata, Kiyoto Maeda, Hiroaki Taguchi, Nobuo Kawase, Naoyoshi Miura
  • Patent number: 6696438
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: December 12, 2002
    Date of Patent: February 24, 2004
    Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & Company
    Inventors: James E. Audia, Bruce A. Dressman, Qing Shi
  • Patent number: 6683075
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: January 6, 2003
    Date of Patent: January 27, 2004
    Assignees: Athena Neurosciences, Inc., Eli Lilly & Company
    Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
  • Publication number: 20030166639
    Abstract: This invention relates to dihydro-benzo[b][1,4]diazepin-2-one derivatives of the formula 1
    Type: Application
    Filed: January 24, 2003
    Publication date: September 4, 2003
    Inventors: Geo Adam, Erwin Goetschi, Juergen Wichmann, Thomas Johannes Woltering
  • Patent number: 6569851
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: June 22, 1999
    Date of Patent: May 27, 2003
    Assignees: Elan Pharmaceutials, Inc., Eli Lilly & Company
    Inventors: Richard C. Thompson, Stephen Wilkie, Douglas R. Stack, Eldon E. VanMeter, Qing Shi, Thomas C. Britton, James E. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, Steven S. Henry, Stacey L. McDaniel, Russell D. Stucky, Warren J. Porter
  • Publication number: 20030092677
    Abstract: The present invention is a compound of formula 1
    Type: Application
    Filed: November 20, 2002
    Publication date: May 15, 2003
    Inventors: Geo Adam, Alaxander Alanine, Erwin Goetschi, Vincent Mutel, Thomas Johannes Woltering
  • Patent number: 6548495
    Abstract: This invention is a dihydro-benzo[b][1,4]diazepin-2-one derivative of the formula wherein R1, R2, R3 and Y are as defined in the specification. The invention includes pharmaceutical compositions containing these compounds, a process for their preparation and a method of treatment or prevention of acute and/or chronic neurological disorders by administering an effective amount of the compound of formula I or a pharmaceuticall acceptable salt thereof.
    Type: Grant
    Filed: April 3, 2002
    Date of Patent: April 15, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Geo Adam, Erwin Goetschi, Vincent Mutel, Juergen Wichmann, Thomas Johannes Woltering
  • Patent number: 6544985
    Abstract: This invention is a dihydro-benzo[b][1,4]diazepin-2-one derivative of the formula wherein R1, R2, R3, X and Y are as defined in the specification. The invention includes pharmaceutical compositions containing these compounds, a process for their preparation, their use in preparation of pharmaceutical compositions and administration of an effective amount of the compounds for the treatment or prevention of acute and/or chronic neurological disorders to a patient in need of such treatment.
    Type: Grant
    Filed: April 3, 2002
    Date of Patent: April 8, 2003
    Assignee: Hoffman-La Roche Inc.
    Inventors: Geo Adam, Erwin Goetschi, Vincent Mutel, Juergen Wichmann, Thomas Johannes Woltering
  • Patent number: 6407094
    Abstract: The present invention relates to compounds of with a base structure of formula 1 The compounds of formula I are shown to have activity as metabotropic glutamate receptor antagonists.
    Type: Grant
    Filed: October 13, 2000
    Date of Patent: June 18, 2002
    Assignee: Hoffmann-la Roche Inc.
    Inventors: Geo Adam, Alexander Alanine, Erwin Goetschi, Vincent Mutel, Thomas Johannes Woltering
  • Patent number: 6344452
    Abstract: This invention relates to 1,5-benzodiazepine derivatives, which are each represented by the following formula (1): wherein R1 represents a lower alkyl group, R2 and R3 may be the same or different and represent a hydrogen atom or a lower alkyl group, R4 represents a cyclohexyl group or phenyl group, and n stands for an integer of from 1 to 3, and also to medicines containing the same. These compounds are useful as curatives or preventives for diseases in which a gastrin receptor and/or a CCK-B receptor takes part.
    Type: Grant
    Filed: December 5, 2000
    Date of Patent: February 5, 2002
    Assignee: Zeria Pharmaceuticals Co., Ltd.
    Inventors: Katsuo Shinozaki, Tomoyuki Yoneta, Masakazu Murata, Naoyoshi Miura, Kiyoto Maeda