Tricyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/479)
  • Publication number: 20150119553
    Abstract: Compounds are disclosed that are useful for noninvasive imaging in the near-infrared spectral range.
    Type: Application
    Filed: November 24, 2014
    Publication date: April 30, 2015
    Inventors: Xinshe Xu, Daniel R. Draney, Lael Cheung
  • Patent number: 8912322
    Abstract: Convenient methods of preparing aza-dibenzocyclooctynes are disclosed herein. Aza-dibenzocyclooctynes attached to a surface are also disclosed herein. Aza-dibenzocyclooctynes can be reacted with azides to form heterocyclic compounds. Such reactions can be useful in a wide variety of applications including, for example, labeling surfaces.
    Type: Grant
    Filed: July 21, 2011
    Date of Patent: December 16, 2014
    Assignee: University of Georgia Research Foundation, Inc.
    Inventors: Vladimir V. Popik, Alexander Kuzmin, Andrei Polukhtine
  • Patent number: 8901115
    Abstract: The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Grant
    Filed: August 6, 2012
    Date of Patent: December 2, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Patrick Y. S. Lam, Charles G. Clark, James R. Corte, William R. Ewing, Paul J. Gilligan, Yoon Jeon, Wu Yang, Leon M. Smith, II, Yufeng Wang
  • Publication number: 20140286899
    Abstract: A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV.
    Type: Application
    Filed: November 18, 2013
    Publication date: September 25, 2014
    Applicant: Presidio Pharmaceuticals, Inc.
    Inventors: Min Zhong, Leping Li
  • Publication number: 20140213782
    Abstract: A pharmaceutical intermediate including a first indole moiety which is associated with an optionally carboxylated hexahydroazepino moiety, an optionally carboxylated azonane moiety, or a second, optionally carboxylated indole moiety, having an alkyl, allyl, phenylallyl, cinnamyl, alkenyl, and/or alkyl-alkenyl substituent pendant from a nitrogen atom of the same.
    Type: Application
    Filed: March 28, 2014
    Publication date: July 31, 2014
    Inventor: William Allen Boulanger
  • Publication number: 20140213783
    Abstract: A pharmaceutical intermediate including a first indole moiety which is associated with an optionally carboxylated hexahydroazepino moiety, an optionally carboxylated azonane moiety, or a second, optionally carboxylated indole moiety, having an alkyl, allyl, phenylallyl, cinnamyl, alkenyl, and/or alkyl-alkenyl substituent pendant from a nitrogen atom of the same.
    Type: Application
    Filed: March 28, 2014
    Publication date: July 31, 2014
    Inventor: William Allen Boulanger
  • Publication number: 20130281656
    Abstract: Methods for derivatizing the surface of a substrate having a plurality of thiol groups thereon are disclosed herein. The method can include reacting the thiol groups with an o-quinone methide, which can optionally be generated by irradiating an o-quinone methide precursor compound. In some embodiments, the method can advantageously be reversible. Exemplary o-quinone methides having a cyclic alkyne attached thereto, and precursor compounds for generating such compounds, are also disclosed herein.
    Type: Application
    Filed: April 16, 2013
    Publication date: October 24, 2013
    Applicant: University of Georgia Research Foundation, Inc. Boyd Graduate Studies Research Center
    Inventor: University of Georgia Research Foundation, Inc. Boyd Graduate Studies Research Center
  • Patent number: 8541625
    Abstract: Cyclic alkynes (e.g., cyclooctynes such as dibenzocyclooctynes) can be photochemically generated from cyclopropenones as disclosed herein. The cyclic alkynes can be reacted (e.g., in situ) with materials having alkyne-reactive groups (e.g., azide groups in a “click” reaction). In preferred embodiments, the generation and reaction of the cyclic alkyne can proceed in the absence of a catalyst (e.g., Cu(I)). These reactions can be useful, for example, for the selective labeling of living cells that are metabolically modified with azido-containing surface monosaccharides, or for light-directed surface patterning.
    Type: Grant
    Filed: August 6, 2012
    Date of Patent: September 24, 2013
    Assignee: University of Georgia Research Foundation, Inc.
    Inventors: Vladimir V. Popik, Andrei A. Poloukhtine, Geert-Jan Boons, Margaretha Wolfert
  • Publication number: 20130189287
    Abstract: The present application relates to methods for the functionalization of immunoglobulins, in particular with drugs.
    Type: Application
    Filed: December 21, 2012
    Publication date: July 25, 2013
    Applicants: Innate Pharma
    Inventors: Innate Pharma, Paul Scherrer Institut
  • Publication number: 20130178618
    Abstract: A pharmaceutical intermediate including a first indole moiety which is associated with an optionally carboxylated hexahydroazepino moiety, an optionally carboxylated azonane moiety, or a second, optionally carboxylated indole moiety, having an alkyl, allyl, phenylallyl, cinnamyl, alkenyl, and/or alkyl-alkenyl substituent pendant from a nitrogen atom of the same.
    Type: Application
    Filed: January 10, 2012
    Publication date: July 11, 2013
    Inventor: William Allen Boulanger
  • Patent number: 8481524
    Abstract: The present invention relates to compounds of formula I useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative disorders.
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: July 9, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Lauffer, Pan Li, Nathan Waal, Kira Mcginty, Qing Tang, Steven Ronkin, Luc Farmer, Dean Shannon, Dylan Jacobs
  • Publication number: 20130039860
    Abstract: Compounds and methods are disclosed that are useful for noninvasive imaging in the near-infrared spectral range. The cyanine compounds of Formula I are presented: wherein Q is a portion of a polymethine bridge: Also included are bioconjugates of the compounds of Formula I, methods of labeling biomolecules with the compounds, and methods of imaging.
    Type: Application
    Filed: August 31, 2012
    Publication date: February 14, 2013
    Applicant: LI-COR, INC.
    Inventor: Lael Cheung
  • Publication number: 20120197012
    Abstract: Convenient methods of preparing aza-dibenzocyclooctynes are disclosed herein. Aza-dibenzocyclooctynes attached to a surface are also disclosed herein. Aza-dibenzocyclooctynes can be reacted with azides to form heterocyclic compounds. Such reactions can be useful in a wide variety of applications including, for example, labeling surfaces.
    Type: Application
    Filed: July 21, 2011
    Publication date: August 2, 2012
    Inventors: VLADIMIR V. POPIK, Alexander Kuzmin, Andrei Polukhtine
  • Patent number: 8188306
    Abstract: Novel compounds useful for inhibiting the 90kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.
    Type: Grant
    Filed: September 30, 2009
    Date of Patent: May 29, 2012
    Assignee: University of Kansas
    Inventors: Brian S. J. Blagg, Gang Shen
  • Patent number: 8143304
    Abstract: The present invention relates to (3-amino-1,2,3,4-tetrahydro-9H-carbazol-9-yl)-acetic acid derivatives of Formula (I) wherein R1, R2, R3, R4, R5 and R6 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.
    Type: Grant
    Filed: August 2, 2007
    Date of Patent: March 27, 2012
    Assignee: Actelion Pharmaceutical Ltd.
    Inventors: Heinz Fretz, Julien Pothier, Philippe Risch
  • Publication number: 20120029186
    Abstract: Convenient methods of preparing aza-dibenzocyclooctynes are disclosed herein. Aza-dibenzocyclooctynes attached to a surface are also disclosed herein. Aza-dibenzocyclooctynes can be reacted with azides to form heterocyclic compounds. Such reactions can be useful in a wide variety of applications including, for example, labeling surfaces.
    Type: Application
    Filed: July 21, 2011
    Publication date: February 2, 2012
    Inventors: VLADIMIR V. POPIK, Alexander Kuzmin, Andrei Polukhtine
  • Publication number: 20120015907
    Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: April 19, 2011
    Publication date: January 19, 2012
    Applicant: NOVARTIS AG
    Inventors: David BARNES, Rajiv CHOPRA, Scott Louis COHEN, Jiping FU, Mitsunori Kato, Peichao LU, Mohindra SEEPERSAUD, Wei ZHANG
  • Publication number: 20110275798
    Abstract: The present disclosure provides solution to the problems involved in determining the crystallinity of sirolimus. More particularly, the instant disclosure is successful in providing a method to determine crystallinity of sirolimus or its analogues using Near-Infrared [NIR] spectroscopy. Also, the instant disclosure provides a method for crystallization of sirolimus or its analogues.
    Type: Application
    Filed: March 6, 2009
    Publication date: November 10, 2011
    Inventors: Rakesh Bhaiyyaram Mendhe, Onkar Prakash Santan, Amit Anantrao Phatale, Nitin Sopanrao Patil
  • Patent number: 8039474
    Abstract: The invention relates to novel tetrahydro-1H-carbazole derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and methods of treatment comprising administration of said compounds to patients.
    Type: Grant
    Filed: December 22, 2005
    Date of Patent: October 18, 2011
    Assignee: Actelion Pharmaceutical Ltd.
    Inventors: Anja Fecher, Heinz Fretz, Markus Riederer
  • Publication number: 20110152310
    Abstract: The present invention relates to substituted tricyclic triazole compounds and compositions comprising substituted tricyclic triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a compound of the invention, or a composition comprising such a compound.
    Type: Application
    Filed: May 15, 2009
    Publication date: June 23, 2011
    Inventors: Joseph A. Burlison, Weiwen Ying
  • Patent number: 7964722
    Abstract: Compounds of Formula (1) are disclosed. Cb is a carbocyclic or heterocyclic group having an atom within the cyclic structure selected from C, N, Si, and Cr and singly bound to A. A is CR, COR, CSR, CNR2, CCN, CCONR2, CNO2, CNNAr, CX1, or N. Cr is a chromophore having a substantially planar cyclic structure. The compounds function as nanometer-scale rotary molecular motors powered and controlled by light energy. The design of the molecular motor devices is flexible so that the rotary direction, drive light wavelength, and other physical characteristics can be varied. The compounds can be chemically functionalized to allow it to be integrated into or attached to a variety of structures. The device can be used in applications where mechanical power, positional control, and information encoding are to be generated at the size scale of individual molecules.
    Type: Grant
    Filed: June 24, 2004
    Date of Patent: June 21, 2011
    Assignee: Board of Regents of the Nevada System of Higher Education, on behalf of the University of Nevada, Reno
    Inventors: Thomas W. Bell, Joseph I. Cline, Christine R. Cremo, Stephen L. Gillett, John H. Frederick
  • Patent number: 7854999
    Abstract: Provided are a cyclopentaphenanthrene-based compound and an organoelectroluminescent device employing the same. The cyclopentaphenanthrene-based compound is easy to prepare and excellent in solubility, color purity, color stability, and thermal stability. The cyclopentaphenanthrene-based compound is useful as a material for forming an organic layer, in particular, an emitting layer, in an organoelectroluminescent device, and as an organic dye or an electronic material such as a nonlinear optical material.
    Type: Grant
    Filed: July 18, 2007
    Date of Patent: December 21, 2010
    Assignee: Samsung Mobile Display Co., Ltd.
    Inventors: Sang-Hoon Park, Yu-Jin Kim, Jhun-Mo Son
  • Publication number: 20100216988
    Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R1; R2; R3; R4; J1; J2; J3; J4 and G have the meanings indicated in the claims. The present invention provides a direct metal, e.g. palladium or copper, catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.
    Type: Application
    Filed: December 22, 2009
    Publication date: August 26, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Jorge ALONSO, Andreas LINDENSCHMIDT, Marc NAZARE, Omar RKYEK, Matthias URMANN, Nis HALLAND
  • Patent number: 7763691
    Abstract: Norbornene monomers with fluorene group and polymer material thereof are disclosed. The norbornene monomers with fluorene group are prepared by Diels-Alder reation. The Norbornene monomers containing fluorene groups are highly active for ring-opening-metathesis polymerization (ROMP), and the molecular weight and PDI value of the obtained polymers are controllable.
    Type: Grant
    Filed: October 5, 2007
    Date of Patent: July 27, 2010
    Assignee: National Taiwan University of Science & Technology
    Inventor: Der-Jang Liaw
  • Patent number: 7741315
    Abstract: Tricyclic compounds of Formula (I) are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: May 5, 2006
    Date of Patent: June 22, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joseph P. Vacca, John S. Wai, Linda S. Payne, Richard C. A. Isaacs, Richard Pracitto
  • Publication number: 20100015092
    Abstract: The present invention relates to compounds of Formula I or II, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: July 20, 2009
    Publication date: January 21, 2010
    Inventors: Suanne Nakajima, Zhenwei Miao, Ying Sun, Datong Tang, Guoyou Xu, Brian Porter, Yat Sun Or, Zhe Wang
  • Publication number: 20090270414
    Abstract: The invention relates to novel tetrahydro-1H-carbazole derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and methods of treatment comprising administration of said compounds to patients.
    Type: Application
    Filed: December 22, 2005
    Publication date: October 29, 2009
    Applicant: Actelion Pharmaceuticals Ltd.
    Inventors: Anja Fecher, Heinz Fretz, Markus Riederer
  • Patent number: 7605288
    Abstract: Novel compounds useful for inhibiting the 90 kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.
    Type: Grant
    Filed: March 26, 2007
    Date of Patent: October 20, 2009
    Assignee: University of Kansas
    Inventors: Brian Blagg, Gang Shen, Randell C. Clevenger
  • Patent number: 7241745
    Abstract: The invention relates to a new pyridyl alkene and pyridyl alkine acid amides according to the general formula (I) as well as methods for their production, medicaments containing these compounds as well as their medical use, especially in the treatment of tumors or for immunosuppression.
    Type: Grant
    Filed: August 5, 2002
    Date of Patent: July 10, 2007
    Assignee: Astellas Pharma GmbH
    Inventors: Elfi Biedermann, Max Hasmann, Roland Löser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt
  • Patent number: 7238802
    Abstract: An intermediate for vinblastine synthesis represented by general formula A. general formula A. (in the formula, R1, R2, R3 and R4 are the group selected independently from the group consisting of H, lower alkyl group, lower alkoxy group, halogen, lower perfluoroalkyl group, lower alkylthio group, hydroxy group, amino group, mono- or di-alkyl or acylamino group, lower alkyl or arylsulfonyloxy group. R5 is H, or a lower alkyl group or a substituted or non-substituted aryl group, R6 is an alkyl group of carbon number 4 or less, R7 is a substituted or non-substituted aryl group, R8 is a substituted or non-substituted aryl group or lower alkyl group and R9 is an acyl group or trialkylsilyl group.
    Type: Grant
    Filed: August 9, 2002
    Date of Patent: July 3, 2007
    Assignee: Japan Science Technology Agency
    Inventors: Tohru Fukuyama, Hidetoshi Tokuyama, Satoshi Yokoshima
  • Patent number: 7208630
    Abstract: Novel compounds useful for inhibiting the 90 kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.
    Type: Grant
    Filed: October 27, 2004
    Date of Patent: April 24, 2007
    Assignee: University of Kansas
    Inventors: Brian Blagg, Gang Shen, Randell C. Clevenger
  • Patent number: 7122534
    Abstract: The present invention relates to compounds of formula (I) and their pharmaceutically acceptable salts, wherein R1, R2, R3 and Z are as defined herein, intermediates in the synthesis of such compounds, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of neurological and psychological disorders.
    Type: Grant
    Filed: January 23, 2004
    Date of Patent: October 17, 2006
    Assignee: Pfizer Inc
    Inventor: Jotham Wadsworth Coe
  • Patent number: 6887838
    Abstract: Formulation components such as bleach boosting compounds selected from the group consisting of bleach boosters comprising quaternary imine cations, zwitterions, polyions having a net charge of from about +3 to about 3 and mixtures thereof, bleaching species comprising oxariridinium cations, zwitterions, polyions having a net charge of from about +3 to about ?3 and mixtures thereof, and mixtures thereof are disclosed. The bleach boosting compounds increase bleaching effectiveness even in lower temperature solutions and provides improved stability toward unwanted boosting compound decomposition. The bleach boosting compounds are ideally suited for inclusion into bleaching compositions including those with detersive surfactants and enzymes. Also provided is a method for laundering a fabric employing the bleach compounds, a laundry additive product employing the bleach boosting compounds.
    Type: Grant
    Filed: May 26, 2004
    Date of Patent: May 3, 2005
    Assignee: Procter & Gamble Company
    Inventors: Robert Richard Dykstra, Gregory Scot Miracle
  • Patent number: 6867198
    Abstract: The present invention provides selective kinase inhibitors of formula (I)
    Type: Grant
    Filed: December 18, 2000
    Date of Patent: March 15, 2005
    Assignee: Eli Lilly and Company
    Inventors: Rima Salim Al-Awar, Kyle Andrew Hecker, James Edward Ray, Jianping Huang, Sajan Joseph, Tiechao Li, Michael Paal, Radhakrishnan Rathnachalam, Chuan Shih, Philip Parker Waid, Xun Zhou, Guoxin Zhu
  • Patent number: 6858624
    Abstract: This invention is directed to compounds of the formula (I): and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of nicotine addiction/withdrawal and CNS disorders.
    Type: Grant
    Filed: November 27, 2002
    Date of Patent: February 22, 2005
    Assignees: Pfizer, Inc., Pfizer Products, Inc.
    Inventors: Anne E. Hagen, R. Scott Obach
  • Patent number: 6800656
    Abstract: The present invention provides a compound of the formula and pharmaceutically acceptable salts having useful antiviral activity against viruses of the herpes family. Wherein: X=O, (CH2)m, S, SO, SO2, NH, NR8; Y=O, (CH2)m, S, SO, SO2, NH, NR8 or a chemical bond; Z=NH, O, NR8, S, SO, SO2; The remaining substituents are described in the specification.
    Type: Grant
    Filed: July 5, 2002
    Date of Patent: October 5, 2004
    Assignee: Warner Lambert Company
    Inventors: Richard John Booth, Vara Prasad Venkata Nagendra Josyula, Annette Lynn Meyer, Bruce Allan Steinbaugh
  • Publication number: 20040186286
    Abstract: An intermediate for vinblastine synthesis represented by general formula A.
    Type: Application
    Filed: February 10, 2004
    Publication date: September 23, 2004
    Inventors: Tohru Fukuyama, Hidetoshi Tokuyama, Satoshi Yokoshima
  • Patent number: 6670371
    Abstract: Disclosed are compounds of the formula: wherein Ar is optionally substituted aryl or heteroaryl R1 is hydrogen or alkyl; R7 is hydrogen or alkyl; R2 is hydrogen, halogen, alkyl or alkoxy; or R1 and R2 taken together with the ring to which they are attached form a 5-9 membered saturated or aromatic ring optionally having a hetero atom selected from oxygen, sulfur or nitrogen; R3 and R4 are independently hydrogen, alkyl, cycloalkyl, aryl or heteroaryl groups; or R3 and R4 together with the nitrogen atom to which they are attached form a 5-8 membered ring; and R5 is hydrogen, halogen, straight or branched chain lower alkyl having 1-6 carbon atoms, or straight or branched chain lower alkoxy or thioalkoxy having 1-6 carbon atoms, which compounds are highly selective partial agonists or antagonists at human Corticotropin-Releasing Factor 1 (CRF1) receptors and are useful in the diagnosis and treatment of treating stress related disorders such as post trumatic stress disorder (PTSD) as wel
    Type: Grant
    Filed: March 12, 2002
    Date of Patent: December 30, 2003
    Assignee: Neurogen Corporation
    Inventors: Raymond F. Horvath, Alan Hutchison
  • Publication number: 20030149041
    Abstract: Compounds that selectively inhibit inappropriate kinase activities and methods for their preparation are disclosed.
    Type: Application
    Filed: June 28, 2002
    Publication date: August 7, 2003
    Applicant: Pharmacopeia, Inc.
    Inventors: Shawn David Erickson, James Inglese, Jeffrey John Letourneau, Christopher Mark Riviello
  • Patent number: 6462035
    Abstract: The present invention relates to compounds of formula (I) and their pharmaceutically acceptable salts, wherein R1, R2, R3 and Z are as defined herein, intermediates in the synthesis of such compounds, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of neurological and psychological disorders.
    Type: Grant
    Filed: August 7, 2000
    Date of Patent: October 8, 2002
    Assignee: Pfizer Inc.
    Inventor: Jotham Wadsworth Coe
  • Patent number: 6359130
    Abstract: The present invention is directed to novel fused aryl and heteroaryl bridged indenopyrrolocarbazoles which are useful, inter alia, as therapeutic agents. The invention is also directed to methods for making and using the bridged indenopyrrolocarbazoles.
    Type: Grant
    Filed: May 17, 2000
    Date of Patent: March 19, 2002
    Assignee: Cephalon, Inc.
    Inventors: Jasbir Singh, Robert L. Hudkins, John P. Mallamo, Theodore L. Underiner, Rabindranath Tripathy
  • Patent number: 6355651
    Abstract: Disclosed are compounds of the formula: wherein Ar is optionally substituted aryl or heteroaryl R1 is hydrogen or alkyl; R7 is hydrogen or alkyl; R2 is hydrogen, halogen, alkyl or alkoxy; or R1 and R2 taken together with the ring to which they are attached form a 5-9 membered saturated or aromatic ring optionally having a hetero atom selected from oxygen, sulfur or nitrogen; R3 and R4 are independently hydrogen, alkyl, cycloalkyl, aryl or heteroaryl groups; or R3 and R4 together with the nitrogen atom to which they are attached form a 5-8 membered ring; and R5 is hydrogen, halogen, straight or branched chain lower alkyl having 1-6 carbon atoms, or straight or branched chain lower alkoxy or thioalkoxy having 1-6 carbon atoms, which compounds are highly selective partial agonists or antagonists at human Corticotropin-Releasing Factor 1 (CRF1) receptors and are useful in the diagnosis and treatment of treating stress related disorders such as post trumatic stress disorder (PTSD) as wel
    Type: Grant
    Filed: September 6, 2000
    Date of Patent: March 12, 2002
    Assignee: Neurogen Corporation
    Inventors: Raymond F. Horvath, Alan Hutchison
  • Patent number: 6225306
    Abstract: A biphenyl derivative represented by the following general formula (1) and a pharmaceutically acceptable salt thereof: [In the formula (1), A represents a single bond, —CH2—, —CO—, —CS— or —SO2—; B represents a single bond or —CH2—; R1 represents a hydrogen atom, —OH, —NR11R12 (wherein R11 and R12 each independently represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms), —OCOCH3, or a halogen atom; R2 represents a hydrogen atom or R1 and R2 form a group ═O together; R3 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms; provided that in the formula, the absolute configuration of the position a may be either R or S]. The compound of the present invention has considerably high safety and efficacy and is useful as, in particular, a vasopressin receptor antagonist.
    Type: Grant
    Filed: September 30, 1999
    Date of Patent: May 1, 2001
    Assignee: Wakamoto Pharmaceutical Co., Ltd.
    Inventors: Yasuhiro Ohtake, Akira Naito, Kenji Naito, Hidehiko Matsukawa, Yoshiaki Saito, Hatsunori Toyofuku
  • Patent number: 6214816
    Abstract: The compounds are N-substituted azaheterocyclic compounds of formula I wherein R1 and R2 independently are hydrogen, halogen, trifluoromethyl, hydroxy, C1-6-alkyl or C1-6-alkoxy; and Y is >N—CH2— wherein only the underscored atom participates in the ring system; and X is —C(R6R7)—, —CH2CH2—, —CH═CH—CH2—, —CH2—CH═CH—, —CH2—(C═O)—, —(C═O)—CH2—, —CH2CH2CH2—, —CH═CH—, CH(R10)CH2—, —CH2CH(R10) or —(C═O)— wherein R6 and R7 independently are hydrogen or C1-6-alkyl and wherein R10 is C1-6-alkyl or phenyl; and r is 0, 1 or 2; and Z is selected from wherein A is —CH2—, —O—, —S— or —N(R5)— wherein R5 is H or C1-6-alkyl; and R3 is —(CH2)pCOR4 wherein p is 1, 2, 3 or 4 and R4 is OH, NH2, NHOH or C1-6-alkoxy; or a pharmaceutically acceptable salt th
    Type: Grant
    Filed: March 10, 1999
    Date of Patent: April 10, 2001
    Assignee: Novo Nordisk A/S
    Inventors: Rolf Hohlweg, Tine Krogh Jørgensen, Knud Erik Andersen, Uffe Bang Olsen, Zdenék Polivka, Karel Sindelar
  • Patent number: 6172058
    Abstract: A pharmaceutical compound of the formula in which R1 is C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-10 cycloalkyl, C3-10 cycloalkyl-C1-10 alkyl, C3-10 cycloalkyl-C2-10 alkenyl, C3-10 cycloalky-C2-10 alkynyl, optionally substituted phenyl-C1-10 alkyl, optionally substituted phenyl-C2-10 alkenyl, optionally substituted phenyl-C2-10 alkynyl, optionally substituted naphthyl, optionally substituted naphthyl-C1-10 alkyl, C1-10 alkoxy-C1-10 alkyl, C3-10 cycloalkoxy-C1-10 alkyl, optionally substituted heterocyclyl, optionally substituted heterocyclyl-C1-10 alkyl, optionally substituted phenyl fused to C5-10 cycloalkyl, optionally substituted tricyclic, optionally substituted tricyclic-C1-10 alkyl, or [optionally substituted phenyl(CH2)n]2-C1-10 alkyl, where n is 0 or 1 to 4, and R2 is hydrogen or one of the values for R1; or a salt or ester thereof.
    Type: Grant
    Filed: April 3, 1998
    Date of Patent: January 9, 2001
    Assignee: Lilly, SA
    Inventors: Concepci{acute over (o)}n Pedregal Tercero, Ivan Collado Cano, Angel Maz{acute over (o)}n Ruiz
  • Patent number: 6133282
    Abstract: Disclosed are compounds of the formula: ##STR1## wherein Ar is optionally substituted aryl or heteroarylR.sub.1 is hydrogen or alkyl;R.sub.7 is hydrogen or alkyl;R.sub.2 is hydrogen, halogen, alkyl or alkoxy; orR.sub.1 and R.sub.2 taken together with the ring to which they are attached form a 5-9 membered saturated or aromatic ring optionally having a hetero atom selected from oxygen, sulfur or nitrogen;R.sub.3 and R.sub.4 are independently hydrogen, alkyl, cycloalkyl, aryl or heteroaryl groups; orR.sub.3 and R.sub.4 together with the nitrogen atom to which they are attached form a 5-8 membered ring; andR.sub.
    Type: Grant
    Filed: August 5, 1999
    Date of Patent: October 17, 2000
    Assignee: Neurogen Corporation
    Inventors: Raymond F. Horvath, Alan Hutchison
  • Patent number: 6066632
    Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the present description, or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.
    Type: Grant
    Filed: August 17, 1999
    Date of Patent: May 23, 2000
    Assignee: Novo Nordisk A/S
    Inventors: Knud Erik Andersen, Tine Krogh J.o slashed.rgensen, Rolf Hohlweg, Erik Fischer, Uffe Bang Olsen, Zdenek Polivka, Karel Sindelar, Vladimir Valenta
  • Patent number: 6011041
    Abstract: The present invention is particularly directed to the use of a derivative of vinblastine, 3',4'-anhydrovinblastine (AHVB), which differs from vinblastine in that it possesses a double bond at the 3',4' position of the caranthine nucleus rather than the hydroxyl group that is present in the parent structure, as an antineoplastic agent in the therapeutic treatment of cancer. Specifically, the treatment of lymphoma with 3',4'-anhydrovinblastine is disclosed.
    Type: Grant
    Filed: July 26, 1996
    Date of Patent: January 4, 2000
    Assignee: University of British Columbia
    Inventors: Bruce Schmidt, James Kutney, Lawrence Mayer
  • Patent number: 5998405
    Abstract: The present invention discloses compounds of the formula, or any of its enantiomers or any mixture thereof, a pharmaceutically acceptable addition salt thereof or the N-oxide thereofwhereinX and Y together forms .dbd.O, .dbd.S, .dbd.NOR.sup.2, .dbd.CR.sup.3 R.sup.4, .dbd.N--CN, .dbd.N--NR.sup.7 R.sup.8, --(CH.sub.2).sub.m --, or--W'--(CH.sub.2).sub.p --W"--, or one of X and Y is hydrogen and the other is --OR.sup.5, --SR.sup.5, or --NR.sup.5 R.sup.6Z is hydrogen, --COOR.sup.9 ;R.sup.3 and R.sup.4 are independently hydrogen, halogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, aryl, arylalkyl, or --(CH.sub.2).sub.q --COOR.sup.2 ;R.sup.2, R.sup.5 and R.sup.6 are independently hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, aryl, or arylalkyl, --CO-alkyl, or --SO.sub.2 -alkyl;R.sup.7 and R.sup.8 are independently hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, aryl, or arylalkyl;R.sup.9 is alkyl, alkenyl or alkynyl;R.sup.
    Type: Grant
    Filed: June 4, 1998
    Date of Patent: December 7, 1999
    Assignee: NeuroSearch A/S
    Inventors: J.o slashed.rgen Scheel-Kruger, Gunnar M. Olsen, Elsbet .O slashed.stergaard Nielsen, Bjarne Hugo Dahl, Leif Helth Jensen
  • Patent number: RE37449
    Abstract: The present invention relates to the synthesis of dimer alkaloid compounds, particularly those of the Catharantus (Vinca) family, from an indole unit, such as cantharanthine, and a dihydroindole unit, such as vindoline. A multi-step process is disclosed including the steps of (1) of 1,4-reduction of a first dimeric iminium intermediate to an enamine compound by reaction with a 1,4-dihydropyridine compound; (2) oxidative transformation of the resulting enamine to a second iminium intermediate under controlled aeration; (3) reduction of the second iminium intermediate to form the target dimer alkaloid compounds. The entire process can be conducted in a one-pot operation to obtain the target compounds without isolation of the intermediates.
    Type: Grant
    Filed: November 10, 1999
    Date of Patent: November 13, 2001
    Assignee: University of British Columbia
    Inventors: James P. Kutney, Lewis S. L. Choi, Jun Nakano, Hiroki Tsukamoto, Camille A. Boulet, Michael McHugh