Nitrogen Bonded Directly To The Hetero Ring Patents (Class 540/527)
  • Patent number: 10835575
    Abstract: The invention provides compositions and methods for reducing one or more symptoms of disease by administering compositions comprising SipA. The invention's compositions and methods are particularly advantageous in reducing symptoms of diseases that are associated with overexpression of P-gp and/or p53. The invention's compositions and methods are useful in reducing cancer symptom and/or cancer multidrug resistance (MDR). The invention provides a method for reducing one or more symptoms of cancer in a mammalian subject in need thereof, comprising administering to said subject a composition comprising purified SipA. In one embodiment, said SipA is operably conjugated to a nanoparticle. In another embodiment, said cancer comprises cancer cells resistant to at least one cytotoxin.
    Type: Grant
    Filed: December 20, 2018
    Date of Patent: November 17, 2020
    Assignee: University of Massachusetts
    Inventors: Beth McCormick, Regino Mecado-Lubo
  • Patent number: 10201589
    Abstract: The invention provides compositions and methods for reducing one or more symptoms of disease by administering compositions comprising SipA. The invention's compositions and methods are particularly advantageous in reducing symptoms of diseases that are associated with overexpression of P-gp and/or p53. The invention's compositions and methods are useful in reducing cancer symptom and/or cancer multidrug resistance (MDR). The invention provides a method for reducing one or more symptoms of cancer in a mammalian subject in need thereof, comprising administering to said subject a composition comprising purified SipA. In one embodiment, said SipA is operably conjugated to a nanoparticle. In another embodiment, said cancer comprises cancer cells resistant to at least one cytotoxin.
    Type: Grant
    Filed: December 11, 2014
    Date of Patent: February 12, 2019
    Assignee: University of Massachusetts
    Inventors: Beth McCormick, Regino Mercado-Lubo
  • Patent number: 8853200
    Abstract: The invention relates to 3-(2?,2?-dimethylpropanoylamino)-tetrahydropyridin-2-one, and its pharmaceutical compositions and its use for preparing a medicament intended to prevent or treat inflammatory disorders.
    Type: Grant
    Filed: August 1, 2008
    Date of Patent: October 7, 2014
    Assignee: Cambridge Enterprise Limited
    Inventors: David John Grainger, David Fox
  • Publication number: 20140005175
    Abstract: Compounds of formula II are described: wherein D, n, Ra, Rb, and Rc are as herein defined, along with pharmaceutical compositions and methods of using compounds of formula II for treating or reducing the risk of peritoneal carcinomatosis in a patient.
    Type: Application
    Filed: August 26, 2013
    Publication date: January 2, 2014
    Applicants: Cephalon, Inc., University of Utah Research Foundation, University of Hawaii
    Inventors: Bruce D. Dorsey, Scott K. Kuwada, Jay P. Theroff, Craig A. Zificsak
  • Publication number: 20130203734
    Abstract: Disclosed herein are methods of preventing or treating inflammatory diseases using sulfonamide analogs of 3-aminolactam compounds, each with aromatic “tail groups”. Compounds as defined by formulae (I) and (I?), and the medical uses of the compounds, are described herein.
    Type: Application
    Filed: June 8, 2011
    Publication date: August 8, 2013
    Inventors: David John Grainger, David John Fox
  • Patent number: 8497261
    Abstract: The invention provides compounds, compositions and uses of compounds of general formula (I) or pharmaceutically acceptable salts thereof, which are 3-aminocaprolactam derivatives, for the preparation of a medicament intended to treat an inflammatory disorder: wherein X is —CO—Y—(R1)n or SO2—Y—(R1)n; and Y is a cycloalkyl or polycycloalkyl group (such as an adamantyl, adamantanemethyl, bicyclooctyl, cyclohexyl, cyclopropyl group); or is a cycloalkenyl or polycycloalkenyl group.
    Type: Grant
    Filed: March 17, 2010
    Date of Patent: July 30, 2013
    Assignee: Cambridge Enterprise Limited
    Inventors: David J. Grainger, David John Fox
  • Publication number: 20130172318
    Abstract: Disclosed herein are methods of preventing or treating inflammatory diseases using 3-aminolactam compounds, each with aromatic “tail groups”. Compounds as defined by formulae (I) and (I?), and the medical uses of the compounds, are described herein.
    Type: Application
    Filed: June 8, 2011
    Publication date: July 4, 2013
    Inventors: David John Grainger, David John Fox
  • Publication number: 20130172319
    Abstract: The invention relates to the generation of a library of compounds enriched in agonist and antagonists for members of the G-protein coupled class of receptors (GPCRs). The library contains compounds of general formula (II) wherein: y is any integer from 1 to 8; X is —CO—R1 or —SO2—R1; each R1 is independently selected from an alkyl, haloalkyl, alkenyl, alkynyl, alkylaminoalkyl, alkylaminodialkyl, or charged alkylaminotrialkyl, radical of 1 to 20 carbon atoms; or each R1 is independently selected from oxyalkyl, aminoalkyl, aminodialkyl, or charged aminotrialkyl radical; and wherein the R1 radical has a “key” carbon next to the carbonyl of the carbon amide or the sulfonyl group of the sulfonamide which is di-substituted with the same or different groups selected from: alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl and alkylamino radicals.
    Type: Application
    Filed: February 26, 2013
    Publication date: July 4, 2013
    Applicants: CAMBRIDGE ENTERPRISE LIMITED
    Inventors: Cambridge Enterprise Limited, David J. Grainger, David John Fox
  • Patent number: 8188069
    Abstract: Compounds of formula (I), pharmaceutical compositions comprising them, and methods for their use are described.
    Type: Grant
    Filed: August 4, 2008
    Date of Patent: May 29, 2012
    Assignee: Eli Lilly and Company
    Inventors: Melinda Joy Hope Miller, Warren Jaye Porter, Jon Kevin Reel, Almudena Rubio-Esteban
  • Publication number: 20110282053
    Abstract: A process for preparing compounds of formula I or a solvate or hydrate thereof, where R, R1, R2, R3 and R5 have the meanings as indicated in the specification. Such compounds are useful in the treatment of a number of conditions associated with substance P and neurokinin.
    Type: Application
    Filed: July 22, 2011
    Publication date: November 17, 2011
    Applicant: Novartis AG
    Inventor: Robert PORTMANN
  • Publication number: 20110212920
    Abstract: Disclosed are N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. In Formula (I), R1, R2, R3, R4, R3?, R10 and R11 are as described herein. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of treating cognitive disorders using compounds of Formula (I).
    Type: Application
    Filed: May 9, 2011
    Publication date: September 1, 2011
    Inventors: Martin Neitzel, Michael S. Dappen, Jennifer Marugg
  • Patent number: 8008479
    Abstract: A process for preparing compounds of formula (I) or a solvate or hydrate thereof, where R, R1, R2, R3 and R5 have the meanings as indicated in the specification. Such compounds are useful in the treatment of a number of conditions associated with substance P and neurokinin.
    Type: Grant
    Filed: April 11, 2007
    Date of Patent: August 30, 2011
    Assignee: Novartis AG
    Inventor: Robert Portman
  • Patent number: 7989441
    Abstract: The present disclosure relates to XIAP inhibitor compounds of the formula I.
    Type: Grant
    Filed: June 6, 2006
    Date of Patent: August 2, 2011
    Assignee: Novartis AG
    Inventors: Zhuoliang Chen, Mark G. Palermo, Sushil K. Sharma, Troy Smith, Christopher S. Straub, Run-Ming D. Wang, Yaping Wang, Leigh Zawel
  • Patent number: 7968592
    Abstract: 3-aminopyrrolidone compounds and pharmaceutically acceptable salts thereof that are active as sodium and/or calcium channel modulators and therefore useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to cardiovascular, inflammatory, ophthalmic, urologic, metabolic and gastrointestinal diseases.
    Type: Grant
    Filed: November 16, 2004
    Date of Patent: June 28, 2011
    Assignee: Newron Pharmaceuticals S.p.A.
    Inventors: Florian Thaler, Cibele Maria Sabido David, Sara Maestroni, Luca Francesco Raveglia, Patricia Salvati
  • Publication number: 20110150873
    Abstract: The invention relates to the use of Broad-Spectrum Chemokine Inhibitors (BSCIs), and in particular members of the acylaminolactam class of pharmaceutical agents, for the prevention, prophylaxis, treatment or amelioration of symptoms of inflammatory diseases. In particular, improved compositions consisting of BSCI agents combined with one or more additional active pharmaceutical agents in order to achieve improved anti-inflammatory efficacy with a reduced side-effect profile are described and claimed.
    Type: Application
    Filed: December 10, 2008
    Publication date: June 23, 2011
    Applicant: CAMBRIDGE ENTERPRISE LIMITED
    Inventor: David John Grainger
  • Patent number: 7803793
    Abstract: This invention provides novel heterocyclic derived matrix metalloprotease inhibitors of the formula: and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing matrix metalloproteases. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.
    Type: Grant
    Filed: September 21, 2007
    Date of Patent: September 28, 2010
    Assignee: Janssen Pharmaceutica NV
    Inventors: Yue-Mei Zhang, Bangping Xiang, Shyh-Ming Yang, Kenneth Rhodes, Robert Scannevin, Paul Jackson, Davraj Chakravarty, Xiaodong Fan, Lawrence J. Wilson, Prabha Karnachi
  • Publication number: 20100197660
    Abstract: Compounds of formula (I), pharmaceutical compositions comprising them, and methods for their use are described.
    Type: Application
    Filed: August 4, 2008
    Publication date: August 5, 2010
    Applicant: ELI LILLY AND COMPANY
    Inventors: Melinda Joy Hope Miller, Warren Jaye Porter, Jon Kevin Reel, Almudena Rubio-Esteban
  • Publication number: 20100190688
    Abstract: Compounds, compositions and methods for treatment of hyperproliferative diseases, such as cancer are provided.
    Type: Application
    Filed: July 12, 2005
    Publication date: July 29, 2010
    Inventors: Bin Chao, Thomas L. Deckwerth, Paul S. Furth, Steven D. Linton, Alfred P. Spada, Brett R. Ullman, Michael I. Weinhouse
  • Publication number: 20100190753
    Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-+related disease.
    Type: Application
    Filed: August 27, 2009
    Publication date: July 29, 2010
    Applicant: BELLUS Health (International) Limited
    Inventors: Xianqi KONG, Walter A. Szarek, Francine Gervais
  • Patent number: 7718796
    Abstract: An efficient syntheses for the preparation of (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one.
    Type: Grant
    Filed: April 6, 2007
    Date of Patent: May 18, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael Palucki, Ian Davies, Dietrich Steinhuebel, Jonathan Rosen
  • Patent number: 7691845
    Abstract: The invention provides compounds, compositions and uses of compounds of general formula (I) or (I?), or pharmaceutically acceptable salts thereof, which are 3-aminocaprolactam derivatives, for the preparation of a medicament intended to treat an inflammatory disorder.
    Type: Grant
    Filed: August 10, 2005
    Date of Patent: April 6, 2010
    Assignee: Cambridge Enterprise Limited
    Inventors: David J. Grainger, David John Fox
  • Publication number: 20100016286
    Abstract: The invention provides compounds, pharmaceutical compositions and uses of compounds and salts thereof of general formula (I), for the preparation of a medicament for treatment of an inflammatory disorder, but excluding (S)-3-(r-methylcyclohexyl-carbonylamino)-caprolactam: wherein z is 1, 2, 3 or 4; A is —CO— or —SO2-; Q is linear or branched alkyl, alkenyl, alkynyl, alkoxy, oxyalkyl, aminoalkyl, alkylamino, alkylaminoalkyl, haloalkyl, aryl or substituted aryl; T1 and T2 together constitute a cycloalkyl, cycloalkenyl or polycycloalkyl radical composed of n additional carbon atoms, where n is between 2 and 7; and each hydrogen atom bonded to the carbon atoms in the ring generated by T1 and T2 may be independently be substituted by a group R1, where R1 is independently selected from an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl or alkylamino radical of 1 to 20 carbon atoms; or each R1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl or aminodialkyl radi
    Type: Application
    Filed: June 14, 2006
    Publication date: January 21, 2010
    Inventors: David J. Grainger, David John Fox
  • Publication number: 20100009965
    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: Application
    Filed: September 2, 2009
    Publication date: January 14, 2010
    Applicant: BRISTOL-MYERS SQIBB PHARMA COMPANY
    Inventors: Richard E. Olson, Michael G. Yang
  • Patent number: 7585855
    Abstract: The invention relates to the preparation of substituted caprolactams, a method for the preparation thereof, compositions containing them and the use thereof as a medicament, particularly as anticancer agents.
    Type: Grant
    Filed: August 19, 2008
    Date of Patent: September 8, 2009
    Assignee: Aventis Pharma SA
    Inventors: Jidong Zhang, Neerja Bhatnagar
  • Publication number: 20090137797
    Abstract: A process for preparing compounds of formula (I) or a solvate or hydrate thereof, where R, R1, R2, R3 and R5 have the meanings as indicated in the specification. Such compounds are useful in the treatment of a number of conditions associated with substance P and neurokinin.
    Type: Application
    Filed: April 11, 2007
    Publication date: May 28, 2009
    Inventor: Robert Portman
  • Publication number: 20090075977
    Abstract: The present application describes deuterium-enriched MK-0974, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: September 11, 2008
    Publication date: March 19, 2009
    Applicant: PROTIA, LLC
    Inventor: Anthony W. Czarnik
  • Patent number: 7501406
    Abstract: The invention relates to compounds of general formula wherein R1, R2, R3/R3?, R4/R4? and R5/R5? are as defined in the specification and to pharmaceutically acceptable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. The compounds are ?-secretase inhibitors which can be useful in the treatment of Alzheimer's disease or common cancers including, but not limited to, cervical carcinomas and breast carcinomas and malignancies of the hematopoietic system.
    Type: Grant
    Filed: August 8, 2006
    Date of Patent: March 10, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Flohr, Guido Galley, Roland Jakob-Roetne, Eric Argirios Kitas, Wolfgang Wostl
  • Publication number: 20090042858
    Abstract: The present invention discloses novel methods and compositions for viral inhibition, particularly inhibition of HCV and SARS. The invention also provides compositions including novel oxoazepanylacetamide derivatives useful for viral inhibition.
    Type: Application
    Filed: June 16, 2006
    Publication date: February 12, 2009
    Inventors: Paul Barsanti, Nathan Brammier, Bryan Chang, Zhi-Jie Ni, Weibo Wang, Amy Weiner
  • Publication number: 20080318928
    Abstract: The invention relates to the preparation of substituted caprolactams, a method for the preparation thereof, compositions containing them and the use thereof as a medicament, particularly as anticancer agents.
    Type: Application
    Filed: August 19, 2008
    Publication date: December 25, 2008
    Applicant: AVENTIS PHARMA S.A.
    Inventors: Jidong ZHANG, Neerja Bhatnagar
  • 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: 20080275024
    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: Application
    Filed: June 19, 2008
    Publication date: November 6, 2008
    Applicant: BRISTOL-MYERS SQUIBB PHARMA COMPANY
    Inventors: Richard E. Olson, Michael G. Yang
  • Publication number: 20080194541
    Abstract: The invention provides compounds, compositions and uses of compounds of general formula (I) or pharmaceutically acceptable salts thereof, which are 3-aminocaprolactam derivatives, for the preparation of a medicament intended to treat an inflammatory disorder wherein X is —CO—Y—(R1)n or SO2—Y—(R1)n; and Y is 0 cycloalkyl or polycyloalkyl group (such as an adamantyl, adamantanemethyl, bicyclooctyl, cyclohexyl, cyclopropyl group); or is 0 cycloalkenyl or polycycloalkenyl group.
    Type: Application
    Filed: August 10, 2005
    Publication date: August 14, 2008
    Applicant: CAMBRIDGE ENTERPRISE LIMITED
    Inventors: David J. Grainger, David John Fox
  • Patent number: 7378410
    Abstract: This invention relates to certain substituted lactam compounds of the formula (I), particularly caprolactam compounds, which are useful for the treatment of cancer
    Type: Grant
    Filed: July 23, 2004
    Date of Patent: May 27, 2008
    Assignee: Novartis AG
    Inventors: Kenneth Walter Bair, Frederick Ray Kinder, Jr., Richard William Versace
  • Patent number: 7348318
    Abstract: There are disclosed a novel ?-amino-N-(diaminophosphinyl)lactam derivative represented by general formula (1): wherein, for example, A is a hydrogen atom or a substituent such as a lower alkyl group or the like; W, X, Y and Z are independently a hydrogen atom or a substituent such as a lower alkyl group, aryl group, arylacyl group, arylaminocarbonyl group or the like; and Q is —(CH2)n— wherein n is 0 to 3, or its salt, and a therapeutic agent and a prophylactic agent for myelosuppression, a therapeutic agent for infectious diseases, an agent for increasing the number of leukocytes and a dipeptidyl peptidase IV inhibitor which comprise the above-mentioned derivative or salt thereof as an active ingredient.
    Type: Grant
    Filed: March 24, 2003
    Date of Patent: March 25, 2008
    Assignees: Nippon Kayaku Kabushiki Kaisha, Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Masatoshi Abe, Masashi Nagai, Keiichirou Yamamoto, Chihiro Nishimura
  • Patent number: 7342007
    Abstract: This invention relates to novel compounds having formula (I) to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit secretase and thereby inhibit the production of amyloid ? protein, thereby acting to prevent the formation of neurological deposits of amyloid protein.
    Type: Grant
    Filed: March 10, 2004
    Date of Patent: March 11, 2008
    Assignee: AstraZeneca AB
    Inventors: Keith John Herzog, Robert Jacobs, Jianxing Kang, Thomas Richard Simpson, James M Woods
  • Patent number: 7294622
    Abstract: Compounds having the formula (I) pharmaceutical compositions containing them and their methods of use for the treatment of neurological disorders related to amyloid ? protein production and neurological disorders such as Alzheimer's disease. These compounds inhibit ? secretase and thereby inhibit the production of amyloid ? protein, thereby acting to prevent the formation of neurological deposits of amyloid protein.
    Type: Grant
    Filed: October 2, 2003
    Date of Patent: November 13, 2007
    Assignee: Astrazeneca AB
    Inventors: Christopher Becker, Bruce Dembofsky, Robert Jacobs, James Kang, Cyrus Ohnmacht, James Rosamond, Ashokkumar Bhikkappa Shenvi, Thomas Simpson, James Woods
  • Patent number: 7253158
    Abstract: The invention relates to compounds of the general formula in which R1, R2, R3, R4, R2?, R3?, R4?, R5, and X is —CHR— are as defined in the specification. The invention also provides pharmaceutically acceptable acid addition salts, optically pure enantiomers, racemates and diastereomeric mixtures of such compounds. The invention further provides methods for the treatment of Alzheimer's disease or common cancers.
    Type: Grant
    Filed: July 12, 2005
    Date of Patent: August 7, 2007
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Eric Argirios Kitas, Roland Jakob-Roetne
  • Patent number: 7208488
    Abstract: Disclosed are N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. In Formula (I), R1, R2, R3, R4, R3?, R10 and R11 are as described herein. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of treating cognitive disorders using compounds of Formula (I).
    Type: Grant
    Filed: October 29, 2004
    Date of Patent: April 24, 2007
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Martin Neitzel, Michael S. Dappen, Jennifer Marugg
  • Patent number: 7153846
    Abstract: The present invention relates to bengamide derivatives which are formed, during fermentation, by the microorganism Myxococcus virescens ST200611 (DSM 15898), to their use for treating cancer diseases, to pharmaceuticals which comprise bengamide derivatives, to a process for preparing bengamides of the formula (V) and to the microorganism Myxococcus virescens ST200611 (DSM 15898)
    Type: Grant
    Filed: October 22, 2004
    Date of Patent: December 26, 2006
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Holger Hoffmann, Sabine Haag-Richter, Michael Kurz, Heiko Tietgen
  • Patent number: 7001899
    Abstract: The present invention relates to novel compounds, compositions comprising said compounds, and uses thereof, said compounds having the formula: wherein each X is independently selected from: i) —C(W)2—; ii) —C(O)—; iii) —NR2—; iv) —S—; v) —S(O)—; vi) —S(O)2—; vii) two units, one from each adjacent X unit, can be taken together to form a substituted or unsubstituted double bond having the formula —CW?CW—; wherein each W is hydrogen of a unit having the formula —(L2)j—R2, the index j is 0 or 1; R is a carbocyclic or heterocyclic aryl ring; R1 is a cysteine trap; each R2 is independently a suitable substituent; and L, L1, and L2 are linking units.
    Type: Grant
    Filed: June 9, 2003
    Date of Patent: February 21, 2006
    Assignee: The Procter & Gamble Company
    Inventors: John August Wos, Yili Wang, Kofi Abeka Oppong, Steven Victor O'Neil, Michael Christopher Laufersweiler, David Lindsey Soper, Biswanath De, Thomas Prosser Demuth, Jr.
  • Patent number: 6960576
    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: November 4, 2002
    Date of Patent: November 1, 2005
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Richard E. Olson, Hong Liu, Lorin A. Thompson
  • Patent number: 6958329
    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: November 4, 2002
    Date of Patent: October 25, 2005
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventor: Richard E. Olson
  • Patent number: 6953788
    Abstract: The present invention relates to certain novel 3-mercaptoacetylamino-1,5-substituted-2-oxo-azepan derivatives useful as inhibitors of matrix metalloproteinase. Pharmaceutical compositions containing said compounds as well as methods of treating various disease states responding to inhibition of matrix metalloproteinase are also claimed herein.
    Type: Grant
    Filed: December 19, 1997
    Date of Patent: October 11, 2005
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Alan M. Warshawsky, Joseph T. Tsay, Michael J. Janusz, Jian Shen, Gary A. Flynn, Ramalinga M. Dharanipragada, Joseph P. Burkhart, Douglas W. Beight, Meena V. Patel
  • Patent number: 6953789
    Abstract: The present invention provides a compound represented by Formula: wherein ring A and ring B may be same or different and each is an optionally substituted homocyclic or heterocyclic ring and the like, each R1 may be same or different and is a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group, an optionally substituted heterocyclic group or SR2, etc., X1 is a bond, an optionally substituted divalent C1-3 aliphatic hydrocarbon group or —NR3—, etc, X2 is a bond, an optionally substituted divalent C1-3 aliphatic hydrocarbon group, —NR4—, —O— or —S(O)p— (wherein p is 0, 1 or 2), each Y may be same or different and is a hydrogen atom, an optionally substituted hydrocarbon group, a halogen atom, a carboxyl group, an acyl group, an optionally substituted hydroxy group, an optionally substituted amino group, SR5, an oxo group, a thioxo group, an optionally substituted imino group, a nitro group, a cyano group, etc.
    Type: Grant
    Filed: January 13, 2004
    Date of Patent: October 11, 2005
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Toshiro Yamashita, Hiroshi Nara, Masayuki Takizawa, Koji Yoshimura
  • Patent number: 6906056
    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 that include 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: March 20, 2003
    Date of Patent: June 14, 2005
    Assignees: Elan Pharmaceuticals, 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
  • Patent number: 6900213
    Abstract: The invention relates to bisaryl derivatives of the formula I, wherein (R,R) is selected from (H,H), O, (H,CH3), (H,OH) and (H,CN); Ar is substituted phenyl and A is a group of formula II, III, IV or V: An example is (3S,6S)-1-N-(7-phenylheptyl)-3-(4-(3,4,5-trimethoxyphenyl)benzyl)-4-N-methyl-6-methyl-2,5-dioxo-1,4-piperazine: The compounds of the invention have FSH receptor modulatory activity and can be used for the control of fertility, for contraception or for treatment of hormone-dependent disorders.
    Type: Grant
    Filed: July 21, 2003
    Date of Patent: May 31, 2005
    Assignee: Pharmacopeia Drug Discovery, Inc.
    Inventors: Tao Guo, Koc-Kan Ho, Edward McDonald, Roland Ellwood Dolle, Kurt W. Saionz, Steven G. Kultgen, Ruiyan Liu, Guizhen Dong, Peng Geng, Anton Egbert Peter Adang, Nicole Corine Renee Van Straten
  • Patent number: 6794381
    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&bgr;-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 &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Grant
    Filed: February 17, 2000
    Date of Patent: September 21, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: Richard E. Olson, Thomas P. Maduskuie, Lorin Andrew Thompson
  • Patent number: 6777550
    Abstract: N-formyl hydroxylamines are provided which have the structure wherein R is H, alkyl, alkenyl, aryl-(CH2)p—, heteroaryl-(CH2)p— or cycloheteroalkyl-(CH2)p— R1 is H or COR2 where R2 is alkyl, aryl-(CH2)p—, cycloheteroalkyl-(CH2)p—, heteroaryl-(CH2)p—, alkoxy or cycloalkyl-(CH2)p—, p is 0 to 8, and A is a dipeptide derived from an amino acid or is a conformationally restricted dipeptide mimic. The above compounds are useful in treating hypertension congestive heart failure, renal failure, and hepatic cirrhosis.
    Type: Grant
    Filed: April 4, 1997
    Date of Patent: August 17, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventor: Jeffrey A. Robl
  • Patent number: 6770640
    Abstract: The present invention relates to certain novel 1-carboxymethyl-2-oxo-azepan derivatives of the formula useful as inhibitors of matrix metalloproteinases (MMPs). The compounds of formula (1) are especially useful as selective inhibitors of MMP-12. Pharmaceutical compositions containing said compounds as well as methods of treating various disease states responding to inhibition of matrix metalloproteinase are also claimed herein.
    Type: Grant
    Filed: December 17, 1999
    Date of Patent: August 3, 2004
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Alan M. Warshawsky, Michael J. Janusz
  • Publication number: 20040138201
    Abstract: This invention relates to novel lactams of Formula (I): 1
    Type: Application
    Filed: October 14, 2003
    Publication date: July 15, 2004
    Inventors: Qi Han, Hong Liu, Richard E. Olson, Michael G. Yang