Two Of The Cyclos Share At Least Three Ring Members Or A Ring Carbon Is Shared By Three Of The Cyclos (e.g., Bridged, Peri-fused, Etc.) Patents (Class 540/581)
  • Patent number: 9676788
    Abstract: Disclosed is a compound of formula (I) or formula (II): (Formulas should be inserted here) wherein R1-R6 are as defined herein. Also disclosed are a pharmaceutical composition comprising such a compound and a method of treating or preventing cancer in a mammal in need thereof, comprising administering to the mammal a compound of formula (I) or formula (II).
    Type: Grant
    Filed: February 5, 2015
    Date of Patent: June 13, 2017
    Assignees: The United States of America, as represented by the Secretary of Health and Human Services, University of Hawaii
    Inventors: William J. Chain, John A. Beutler, David Fash, William D. Figg, Zhenwu Li, Cody John Peer, Joe William Ramos, Florian J. Sulzmaier
  • Patent number: 9517224
    Abstract: Disclosed is a method of activating protein kinase C theta (PKC?) in an HIV or HTLV infected animal comprising administering to the animal an effective amount of a compound of formula (I): Formula (I), or an epimer thereof; wherein Ar and R1-R6 are described herein. Examples of diseases or conditions associated with PKC? include HIV1 infection, AIDS, HTLV infection, and adult T cell leukemia/lymphoma.
    Type: Grant
    Filed: November 13, 2013
    Date of Patent: December 13, 2016
    Assignee: The United States of America as represented by the Secretary, Department of Health and Human Services
    Inventors: Leonard M. Neckers, Carole Sourbier, Jane B. Neckers, Min-Jung Lee, John A. Beutler, W. Marston Linehan, Bradley T. Scroggins, Sunmin Lee
  • Publication number: 20150087633
    Abstract: Disclosed embodiments concern polycyclic alkaloid compounds and methods for their use and synthesis. Particular embodiments concern polycyclic alkaloids having a fused, six-membered ring, while other embodiments concern polycyclic alkaloids having a fused, five-membered ring. Methods for making the polycyclic alkaloids are disclosed, as well as methods for their use as prophylactics or treatments for certain diseases. Also disclosed are pharmaceutical compositions comprising the polycyclic alkaloids and their use.
    Type: Application
    Filed: December 1, 2014
    Publication date: March 26, 2015
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Donald D. Payan, Sylvia Braselmann
  • Publication number: 20150045351
    Abstract: The present invention provides a compound having a superior serotonin 5-HT2C receptor activating action. The present invention relates to a compound represented by the formula (1) wherein ring A is an aromatic carbocycle optionally having substituent(s) or an aromatic heterocycle optionally having substituent(s), X is —N(R1)—, —O— or the like, when ring A is an aromatic carbocycle optionally having substituent(s), then R1 is a hydrogen atom, an alkyl group optionally having substituent(s), or the like, and when ring A is an aromatic heterocycle optionally having substituent(s), then R1 is a hydrogen atom, an alkyl group optionally having substituent(s), a cycloalkyl group optionally having substituent(s), or the like, is a single bond or a double bond, and n is an integer of 0, 1 or 2, or a salt thereof.
    Type: Application
    Filed: March 6, 2013
    Publication date: February 12, 2015
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Tomokazu Kusumoto, Shigekazu Sasaki, Hironobu Maezaki
  • Patent number: 8933220
    Abstract: The present invention relates to photochromic fused naphthopyrans having a benzene ring which is adjacent to the pyran oxygen and is linked to the para substituent via both meta positions, and to the use thereof in plastics of all types, in particular for ophthalmic purposes.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: January 13, 2015
    Assignee: Rodenstock GmbH
    Inventors: Manfred Melzig, Yven Rohlfing, Udo Weigand
  • Publication number: 20140343039
    Abstract: There is provided a process for preparing cephalotaxine esters corresponding to the following general formula I, which comprises the cephalotaxine backbone, and that can be written as C(R1)(R2)(XH)COO[CTX], wherein CTX represents the cephalotaxine backbone, being optionally substituted, the process consisting in bringing the corresponding cephalotaxine compound, or salts, isomers or tautomeric forms thereof, which is free or which is in the form of a metal alkoxide CTXOM, into contact with a heterocyclic side chain precursor having both a bifunctional protected (bidentate) and activated (acylating) form of an acid bearing a hydrogenated heteroatom, in the alpha (?) position with respect to the carboxyl group, and corresponding to the following general formula: in a customary aprotic solvent, preferably with a catalyst which may be a hindered tertiary amine, at a temperature of between ?80° C. and +100° C., preferably in the range 0 to 30° C.
    Type: Application
    Filed: June 6, 2014
    Publication date: November 20, 2014
    Inventors: Jean-Pierre ROBIN, Nina RADOSEVIC, Julie BLANCHARD
  • Publication number: 20140303147
    Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and relates to novel homoharringtonine acylated derivatives of formula (I) and formula (II) and a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments.
    Type: Application
    Filed: August 20, 2012
    Publication date: October 9, 2014
    Applicant: Hangzhou Bensheng Pharmaceutical Co., Ltd.
    Inventors: Rongzhen Xu, Frank Rong, Fuwen Xie, Hongxi Lai
  • Publication number: 20140206669
    Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry and specifically relates to novel aminated homoharringtonine derivatives of formula (I) and a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments.
    Type: Application
    Filed: August 20, 2012
    Publication date: July 24, 2014
    Applicant: HANGZHOU BENSHENG PHARMACEUTICAL CO., LTD.
    Inventors: Frank Rong, Rongzhen Xu, Fuwen Xie, Hongxi Lai
  • Publication number: 20140113890
    Abstract: The invention provides 4-amino-4-oxobutanoyl peptides of Formula I and the pharmaceutically salts and hydrates thereof. The variables R, R1, R6-R8, R16, R18, R19, M, n, T, Y, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. The 4-amino-4-oxobutanoyl peptides disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptides and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptides as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptides and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections.
    Type: Application
    Filed: December 23, 2013
    Publication date: April 24, 2014
    Applicant: ACHILLION PHARMACEUTICALS, INC.
    Inventors: Avinash Phadke, Dawei Chen, Venkat Gadhachanda, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Atul Agarwal, Ha Young Kim, Shuoming Li, Cuixian Liu, Suoming Zhang, Milind Deshpande
  • Patent number: 8691808
    Abstract: The present disclosure provides compounds having affinity for the M2 proton channel, useful for the treatment of viral infections such as influenza, which are of the Formula (I): wherein R1, R2, and Y are as defined herein. Methods of preparing the compounds, pharmaceutical compositions containing the compounds, and methods of using the compounds in the treatment of viral infections such as influenza are also provided.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: April 8, 2014
    Assignee: Influmedix, Inc.
    Inventors: Jizhou Wang, Xiaodong Fan, Lidia Cristian
  • Publication number: 20130317207
    Abstract: The present invention provides novel fluorescent dyes and kits containing the same, which are useful for labeling a wide variety of biomolecules, cells and microorganisms. The present invention also provides various methods of using the fluorescent dyes for research and development, forensic identification, environmental studies, diagnosis, prognosis and/or treatment of disease conditions.
    Type: Application
    Filed: November 20, 2012
    Publication date: November 28, 2013
    Applicant: PROMEGA CORPORATION
    Inventor: Promega Corporation
  • Publication number: 20130310556
    Abstract: The present invention relates to photochromic fused naphthopyrans having a benzene ring which is adjacent to the pyran oxygen and is linked to the para substituent via both meta positions, and to the use thereof in plastics of all types, in particular for ophthalmic purposes.
    Type: Application
    Filed: December 21, 2011
    Publication date: November 21, 2013
    Applicant: Rodenstock GMBH
    Inventors: Manfred Melzig, Yven Rohlfing, Udo Weigand
  • Publication number: 20130237524
    Abstract: Disclosed embodiments concern polycyclic alkaloid compounds and methods for their use and synthesis. Particular embodiments concern polycyclic alkaloids having a fused, six-membered ring, while other embodiments concern polycyclic alkaloids having a fused, five-membered ring. Methods for making the polycyclic alkaloids are disclosed, as well as methods for their use as prophylactics or treatments for certain diseases. Also disclosed are pharmaceutical compositions comprising the polycyclic alkaloids and their use.
    Type: Application
    Filed: March 7, 2013
    Publication date: September 12, 2013
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Donald G. Payan, Sylvia Braselmann
  • Publication number: 20130210806
    Abstract: The present invention is directed to tricyclic indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by endothelial lipase, for example, cardiovascular disorders.
    Type: Application
    Filed: February 14, 2013
    Publication date: August 15, 2013
    Applicant: Janssen Pharmaceutica, NV
    Inventor: Janssen Pharmaceutica, NV
  • Publication number: 20130211074
    Abstract: Provided herein are indole and benzofuran fused isoquinuclidene derivatives. Also provided herein are processes, preferably enantioselective processes, for preparing such derivatives including processes for preparing (?) and (+) noribogaine or a salt thereof, in substantially enantiomerically pure forms.
    Type: Application
    Filed: January 24, 2013
    Publication date: August 15, 2013
    Applicant: DemeRx, Inc.
    Inventor: DemeRx, Inc.
  • Patent number: 8507669
    Abstract: It is to provide a novel optically active dibenzazepine derivative having a high utility value as an asymmetric phase-transfer catalyst. It is an optically active 6,7-dihydro-5H-dibenzo[c,e]azepine derivative represented by the following formula (1?), (wherein R represents a divalent organic group for cross-linking the 1st position and the 11th position; R1 and R2 are the same or different, and represent a hydrogen atom, halogen atom, or organic group, or R1 and R2 together represent a divalent organic group; R3? and R4? are the same or different and represent a monovalent organic group, or R3? and R4? together form an organic group that forms a cyclic structure comprising an onium nitrogen atom; Ar represents a monovalent organic group; * represents optical activity, i.e., that one axially asymmetric isomer is present in excess of the other axially asymmetric isomer with respect to a bond axis that constitutes the biphenyl structure of the compound; and X? represents a counter anion).
    Type: Grant
    Filed: April 8, 2009
    Date of Patent: August 13, 2013
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Yasushi Kubota, Tsutomu Inoue
  • Patent number: 8466142
    Abstract: The present invention provides novel cephalotaxus esters, syntheses thereof, and intermediates thereto. The invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of using said compounds or compositions in the treatment of proliferative diseases (e.g., benign neoplasm, cancer, inflammatory disease, autoimmune disease, diabetic retinopathy) and infectious disease. The invention further provides methods of using said compounds or compositions in the treatment of multidrug resistant cancer.
    Type: Grant
    Filed: March 3, 2009
    Date of Patent: June 18, 2013
    Assignee: Sloan-Kettering Institute for Cancer Research
    Inventors: David Gin, Jeremy Wilmot, Hakim Djaballah
  • Patent number: 8410292
    Abstract: Disclosed are englerins and derivatives (I) thereof useful in the treatment of a number of cancers, particularly renal cancer, as well as pharmaceutical compositions and method of treating a patient with the use of these derivatives. The englerins, for example Englerin A and Englerin B, can be isolated from the plant Phyllanthus engleri or produced by synthetic methods. An example of the englerin derivative is 2?-chloroenglerin A, which has the structure (II), wherein double bond ‘a’ is E, Z, or a mixture of E and Z.
    Type: Grant
    Filed: December 30, 2008
    Date of Patent: April 2, 2013
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: John A. Beutler, Ranjala Ratnayake, David Covell, Tanya R. Johnson
  • Patent number: 8362008
    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
    Type: Grant
    Filed: December 11, 2008
    Date of Patent: January 29, 2013
    Assignee: The University Of Edinburgh
    Inventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
  • Publication number: 20120172590
    Abstract: Methods are provided for isolating alkaloids from biomaterial, preferably plant biomaterial, wherein the biomaterial is extracted with a vegetable oil, in the concomitant presence of an alkaline aqueous phase.
    Type: Application
    Filed: September 3, 2010
    Publication date: July 5, 2012
    Inventor: Thomas Kallimopoulos
  • Patent number: 8212029
    Abstract: A process for the production of extremely pure galanthamine and galanthamine derivatives is provided. Racemic bromine narwedine is debrominated under palladium catalysis. The reaction mixture is then worked-up in the presence of oxygen or peroxides so that the palladium catalyst is converted into an insoluble form that can be easily separated. Further reaction is carried out by reduction of enantiomerically pure narwedine to form enantiomerically pure galanthamine, which is then alkylated or dealkylated, so that a corresponding substitution on the ring-nitrogen atom is achieved. By further purification, such as recrystallization, residual portions of palladium of below 5 ppm are achieved. The pure galanthamine can then be directly used as a pharmaceutical raw material.
    Type: Grant
    Filed: February 14, 2008
    Date of Patent: July 3, 2012
    Assignee: Sanochemia Pharmazeutika AG
    Inventors: Stefan Welzig, Anton Gerdenitsch, Jan Rothenburger, Susanne Kolar, Alexandra Scherleithner
  • Publication number: 20120129838
    Abstract: Provided are a pharmaceutical composition, a cosmetic composition and health foods for preventing and treating alopecia disorder, which include a norgalanthamine compound as an active ingredient. Since the norgalanthamine compound has an effect on growth and proliferation of dermal papilla cells that play an important role in hair growth, the norgalanthamine compound may be used for the pharmaceutical composition, the cosmetic composition and health foods, which are useful in preventing and treating alopecia disorder.
    Type: Application
    Filed: November 27, 2009
    Publication date: May 24, 2012
    Applicant: The Industry & Academic Cooperation in Chungnam National University
    Inventors: Young-Ho Kim, Hee Kyoung Kang, Sang Cheol Kim, Jung Il Kang, Eun Sook Yoo, Ki Ho Kim, Young Heui Kim
  • Patent number: 8178524
    Abstract: The present invention is directed to methods of treating patients for pain by administering noribogaine. Noribogaine may also be used to treat patients for the symptoms associated with withdrawal from drug dependency. In the latter case, the noribogaine treatment should be supplemented with the administration of an opioid antagonist such as naloxone.
    Type: Grant
    Filed: June 8, 2010
    Date of Patent: May 15, 2012
    Assignee: Demerx, Inc.
    Inventor: Deborah C. Mash
  • Publication number: 20120046271
    Abstract: The compounds of the present invention are represented by the following 2,5-methano- and 2,5-ethano-tetrahydrobenzazepine derivatives having formula (I): where the carbon atom designated * is in the R or S configuration when n is 1 and the substituents X and R1-R7 are as defined herein.
    Type: Application
    Filed: August 17, 2011
    Publication date: February 23, 2012
    Applicants: BRISTOL-MYERS SQUIBB COMPANY, ALBANY MOLECULAR RESEARCH, INC.
    Inventors: Peter R. GUZZO, Shuang LIU, Kristen N. RYAN, Bruce F. MOLINO, Russell DEORAZIO, Richard E. OLSON, John E. MACOR
  • Publication number: 20120046272
    Abstract: The present invention describes a series of therapeutically active compounds of formula I, X—Y—Z??(I) that are useful for treating a disorder in a mammal. In the formula I, X and Z, which may be same or different, are independently selected from substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted heterocyclic group or substituted or unsubstituted heterocyclylalkyl; and Y is a linker selected from —O—, —S—, —NH—, —(CH2)n—, —CO—, —CONRa—, —NRaCO—, —NRaCOO—, —COO—, —CONRaCO—, —CONRaCOO— and —COOCOO—.
    Type: Application
    Filed: August 19, 2011
    Publication date: February 23, 2012
    Applicant: GRUNENTHAL GMBH
    Inventor: Ramesh SESHA
  • Publication number: 20120035102
    Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.
    Type: Application
    Filed: July 1, 2010
    Publication date: February 9, 2012
    Applicant: ALBANY MOLECULAR RESEARCH, INC.
    Inventors: Peter R. GUZZO, Matthew David SURMAN, Lei ZHU
  • Publication number: 20120022250
    Abstract: A process for preparing cephalotaxine esters corresponding to the following general formula I which comprises the cephalotaxine backbone: C(R1)(R2)(XH)COO[CTX] wherein CTX represents the cephalotaxine backbone, being optionally substituted and/or dehydrogenated, in which formula I, X is a heteroatom, preferably an oxygen, a sulfur or a nitrogen, R1 and R2, taken separately, may be alkyl, cycloalkyl, heteroalkyl, aryl, heteroaryl, heterocycloalkyl or aralkyl groups, said groups being optionally interrupted by ester functions, or groups that can form one or more rings or a heterocycle together, consisting in bringing the corresponding cephalotaxine compound, or salts, isomers or tautomeric forms thereof, which is free or which is in the form of a metal alkoxide corresponding to the following general formula CTXOM, wherein CTX represents the cephalotaxine backbone, being optionally substituted and/or dehydrogenated, in which M is a hydrogen atom or a metal atom, into contact with a heterocyclic side chain precur
    Type: Application
    Filed: March 11, 2010
    Publication date: January 26, 2012
    Inventors: Jean-Pierre Robin, Nina Radosevic, Julie Blanchard
  • Publication number: 20110306600
    Abstract: The invention discloses a number of therapeutic compounds and a method of treating a disorder in mammal.
    Type: Application
    Filed: June 10, 2011
    Publication date: December 15, 2011
    Applicant: Grunenthal GmbH
    Inventor: Ramesh SESHA
  • Publication number: 20110212943
    Abstract: Provided herein are novel bridged cyclic derivatives of the general formula (I), their analogs, tautomeric forms, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds can inhibit HDACs and are useful as therapeutic or ameliorating agent for diseases that are involved in cellular growth such as malignant tumors, autoimmune diseases, skin diseases, infections, inflammation, neurode-generative disorders etc.
    Type: Application
    Filed: October 14, 2009
    Publication date: September 1, 2011
    Applicant: ORCHID RESEARCH LABORATORIES LIMITED
    Inventors: Gopalan Balasubramanian, Ponpandian Thanasekaran, Sridharan Rajagopal, Bharathimohan Kuppusamy, Virendra Kachhadia, Vignesh Radhakrishnan, Sivasudar Velaiah, Shridhar Narayanan, Mandar Bhonde, Praveen Rajendran, Sriram Rajagopal
  • Publication number: 20110190262
    Abstract: The present invention relates to compounds defined by formula I wherein the groups R1 to R3, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.
    Type: Application
    Filed: November 14, 2008
    Publication date: August 4, 2011
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Matthias Eckhardt, Bradford S. Hamilton, Armin Heckel, Joerg Kley, Thorsten Lehmann-Lintz, Herbert Nar, Stefan Peters, Annette Schuler-Metz, Matthias Zentgraf
  • Patent number: 7915252
    Abstract: Sulfonyl derivatives of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome or Syndrome X, and other symptoms associated with NIDDM.
    Type: Grant
    Filed: August 3, 2005
    Date of Patent: March 29, 2011
    Assignee: Merck Sharp & Dohme
    Inventors: Sherman T. Waddell, James M. Balkovec, Gina M. Santorelli, Aaron H. Leeman, Milana Maletic, Xin Gu
  • Publication number: 20110071097
    Abstract: The present invention provides novel cephalotaxus esters, syntheses thereof, and intermediates thereto. The invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of using said compounds or compositions in the treatment of proliferative diseases (e.g., benign neoplasm, cancer, inflammatory disease, autoimmune disease, diabetic retinopathy) and infectious disease. The invention further provides methods of using said compounds or compositions in the treatment of multidrug resistant cancer.
    Type: Application
    Filed: March 3, 2009
    Publication date: March 24, 2011
    Applicant: Sloan-Kettering Institute for Cancer Research
    Inventors: David Gin, Jeremy Wilmot, Hakim Djaballah
  • Publication number: 20110028445
    Abstract: The present invention relates to compounds defined by formula (I) wherein the groups A, B, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 ?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.
    Type: Application
    Filed: February 10, 2009
    Publication date: February 3, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Matthias Eckhardt, Frank Himmelsbach, Bradford S. Hamilton, Stefan Peters
  • Publication number: 20110003739
    Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.
    Type: Application
    Filed: July 1, 2010
    Publication date: January 6, 2011
    Applicant: ALBANY MOLECULAR RESEARCH, INC.
    Inventors: Peter R. GUZZO, Matthew David SURMAN, Lei ZHU
  • Patent number: 7842687
    Abstract: The present invention concerns a new general process for asymmetric hemisynthesis of harringtonines and their analogs, that are alkaloids used in chemotherapy. This process comprises direct esterification of a natural cephalotaxine with an acylating compound constituted of a side chain precursor which backbone and functionalization are entirely preformed. The invention also concerns a natural, synthetic or semi-synthetic harringtonines including their tautomeric forms and their salts of the following formula: wherein n=2 (i.e. harringtonine) or n=3 (i.e. homoharringtonine), in which the total content of impurities, possibly including enantiomeric forms, is lower than 1%, and/or the content of the major impurity is lower than 0.9%, and/or the chromatographic assay exhibits a harringtonines content higher than 97.5%.
    Type: Grant
    Filed: May 25, 2006
    Date of Patent: November 30, 2010
    Assignee: Chemgenex Pharmaceuticals, Inc.
    Inventors: Jean-Pierre Robin, Julie Blanchard, Jean-Pierre Marie, Nina Radosevic
  • Patent number: 7820648
    Abstract: The present invention relates to a compound of the formula 1 or a pharmaceutically acceptable salt thereof, wherein Ar is a group of formula and R1, R2, R13, A, K, M, L1, L2, X, Y1, Y2, Q, salt thereof, wherein R1, R2, R13, A, K, L1, L2, W, X, Z1, Z2, Y1, Y2, Z1, Z2, M, Q, W, X, m, p and q are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. The invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: December 20, 2006
    Date of Patent: October 26, 2010
    Assignees: Pfizer Inc, Pfizer Products Inc
    Inventors: Samit Kumar Bhattacharya, Michael Joseph Luzzio, Donn Gregory Wishka, Gonghua Pan, Arthur Douglas Brosius, Joel Thomas Arcari, James Alfred Southers, Jr., Kendra Louise Nelson, Jun Xiao
  • Publication number: 20100249105
    Abstract: The present application relates to indole and indoline derivatives of formula (I), (II), (III), (IV), (V), or (VI) wherein a, R1, R2, R3, R4, R5, U, V, W, X, Y, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.
    Type: Application
    Filed: March 19, 2010
    Publication date: September 30, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: Michael R. Schrimpf, Chih-Hung Lee, Tao Li, Gregory A. Gfesser, Kathleen H. Mortell, Ramin Faghih, Diana L. Nersesian, Kevin B. Sippy, William H. Bunnelle, Marc Scanio, Lei Shi, Murali Gopalakrishnan, Diana L. Donnelly-Roberts, Min Hu
  • Publication number: 20100240887
    Abstract: A safe pharmaceutical composition for treatment of cancer contains Homoharringtonine (HHT). The new methods of process for producing HHT include culture plant tissue and semisynthesis.
    Type: Application
    Filed: March 23, 2009
    Publication date: September 23, 2010
    Inventor: Yaguang Liu
  • Publication number: 20100227851
    Abstract: Provided are novel use of an extract of Lycoris chejuensis or a compound isolated therefrom for inhibition of ?-amyloid production and/or prevention, improvement and/or treatment of a neurodegenerative disease, more specifically a ?-amyloid production inhibitor, and/or a composition for prevention or treatment of a neurodegenerative disease containing one or more kinds selected from the group consisting of an extract of Lycoris chejuensis, and/or dihydrolycoricidine, 2-methoxypancracine, lycoricidine, and/or lycoricidinol, as an active ingredient; a method for inhibiting ?-amyloid production, and/or preventing and/or treating a neurodegenerative disease using the same; and, a method for preparing the same.
    Type: Application
    Filed: October 28, 2009
    Publication date: September 9, 2010
    Applicant: Korea Institute of Science and Technology
    Inventors: Hyun-Ok Yang, Hak-Cheol Kwon, Jin-Soo Park, Sung-Kwon Chung, Myung-Soo Kim
  • Publication number: 20100197662
    Abstract: Disclosed is a compound useful as a type I 11?hydroxysteroid dehydrogenase inhibitor. A compound represented by the formula: a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkenyl or the like, One of R2 and R3 is a group of the formula: —C(?O)—Y—R4, wherein Y is —NR9— or the like, R4 is optionally substituted cycloalkyl or the like, R9 is hydrogen or optionally substituted alkyl, W is optionally substituted alkylene, The other is a group of the formula: —V—R5, wherein V is a bond, —O— or the like, R6 is hydrogen or optionally substituted alkyl, R5 is hydrogen, optionally substituted alkyl or the like, X is a bond, —S—, —SO— or the like, U is a bond or optionally substituted alkylene, R7 is hydrogen or optionally substituted alkyl, Z is —S—, —O— or —NR8—, R8 is hydrogen, optionally substituted alkyl or the like.
    Type: Application
    Filed: June 6, 2006
    Publication date: August 5, 2010
    Applicant: Shionogi & Co., Ltd.
    Inventors: Tomoyuki Ogawa, Noriyuki Kurose, Satoru Tanaka, Koichi Nishi
  • Publication number: 20090326219
    Abstract: A process for the production of extremely pure galanthamine or extremely pure galanthamine derivatives, a start is made from racemic bromine narwedine, which is debrominated under palladium catalysis. In this case, the working-up of the reaction mixture, which is carried out in the presence of oxygen or peroxides so that the palladium catalyst in an insoluble form is converted into an easily separable form, is essential. The further reaction is carried out by reduction of enantiomer-pure narwedine to form enantiomer-pure galanthamine, whereby it is then alkylated or dealkylated so that a corresponding substitution on the ring-nitrogen atom is achieved. By further purification, such as recrystallization, residual portions of palladium of below 5 ppm are achieved, so that direct use as a pharmaceutical raw material is made possible.
    Type: Application
    Filed: June 26, 2009
    Publication date: December 31, 2009
    Applicant: SANOCHEMIA PHARMAZEUTIKA AG
    Inventors: Klaus GERDES, József GUNGL, Beate KÄLZ, Jan ROTHENBURGER, Stefan WELZIG
  • Publication number: 20090118259
    Abstract: The use of substituted amides for modulating the activity of 11-hydroxysteroid dehydrogenase type 1 (11HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11HSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
    Type: Application
    Filed: November 1, 2006
    Publication date: May 7, 2009
    Inventors: John Paul Kilburn, Henrik Sune Andersen, Gita Camilla Tejlgaard Kampen, Soren Ebdrup
  • Publication number: 20090069294
    Abstract: The present disclosure relates to XIAP inhibitor compounds of the formula I.
    Type: Application
    Filed: June 6, 2006
    Publication date: March 12, 2009
    Inventors: Zhuoliang Chen, Mark G. Palermo, Sushil K. Sharma, Troy Smith, Christopher S. Straub, Run-Ming D. Wang, Yaping Wang, Leigh Zawel
  • Publication number: 20080318930
    Abstract: Sulfonyl derivatives of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome or Syndrome X, and other symptoms associated with NIDDM.
    Type: Application
    Filed: August 3, 2005
    Publication date: December 25, 2008
    Inventors: Sherman T. Waddell, James M. Balkovec, Gina M. Santorelli, Aaron H. Leeman, Milana Meletic, Xin Gu
  • Publication number: 20080306257
    Abstract: The present invention relates to a process for preparing racemic narwedine (which can be can be kinetically resolved) to yield (?)-narwedine and which is the biogenic precursor of (?)-galanthamine) and the use thereof as a starting material for producing (?)-galanthamine. The invention further includes processes for preparing (?)-galanthamine and (?)-galanthamine hydrobromide, as well as related novel compounds.
    Type: Application
    Filed: May 3, 2006
    Publication date: December 11, 2008
    Applicant: MEDICHEM, S.A.
    Inventors: Gabriel Tojo Suarez, Ernesto Duran Lopez, Jordi Bosch I Llado
  • Publication number: 20080262223
    Abstract: The subject matter of present invention relates to the process for isolation and purification of galanthamine and its derivatives produced by numerous plants.
    Type: Application
    Filed: March 17, 2006
    Publication date: October 23, 2008
    Applicant: IVAX Pharmaceuticals s.r.o.
    Inventors: Ladislav Cvak, Martin Buchta, Jiri Faustmann, Pavel Stverka, Alexandr Jegorov
  • Publication number: 20080200451
    Abstract: Compounds of the formula (I), in which W, R, R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumours.
    Type: Application
    Filed: June 2, 2006
    Publication date: August 21, 2008
    Inventors: Kai Schiemann, David Bruge, Hans-Peter Buchstaller, Ulrich Emde, Dirk Finsinger, Christiane Amendt, Frank Zenke
  • Patent number: 7365196
    Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.
    Type: Grant
    Filed: March 15, 2001
    Date of Patent: April 29, 2008
    Assignees: Merck Sharp & Dohme Ltd., Merck Frosst Canada & Co.
    Inventors: Patrice Charles Belanger, Ian James Collins, Joanne Claire Hannam, Timothy Harrison, Stephen John Lewis, Andrew Madin, Edward Giles McIver, Alan John Nadin, Joseph George Neduvelil, Mark Steven Shearman, Adrian Leonard Smith, Timothy Jason Sparey, Graeme Irvine Stevenson, Martin Richard Teall
  • Patent number: 7285546
    Abstract: The present invention concerns a compound of formula (I) wherein: W represents O or NH, Q represents an unbranched or branched, saturated or unsaturated or aromatic, cyclic or acyclic or heterocyclic hydrocarbon radical containing 1 to 30 carbon atoms including or not heteroatom(s), R1 is H, OH, or R1, R2 form together —O—, R3?R4?OMe or R3 and R4 form together —OCH2O—, R is H, C1-C30alkyl or O-protecting group and R6 represents an unbranched or branched, saturated or unsaturated or aromatic, cyclic or acyclic or heterocyclic hydrocarboned radical containing 1 to 30 carbon atoms including or not heteroatom(s), or R and R6 form together —CMe2-, n is 0 to 8, R5 is H, OH, OMe, O—(C1-C30)-alkyl, O-aryl-(C1-C30)-alkyl, O—(C2-C30)-alkenyl, O—(C3-C30)-cycloalkyl or O-aryl, the dotted line is null or forms a double bond depending on the meaning of R1. It also concerns their methods of preparation and their use in treatment of cancers, leukemias, parasites and as reversal agents of harringtonines.
    Type: Grant
    Filed: April 1, 2003
    Date of Patent: October 23, 2007
    Assignee: Stragen Pharma S.A.
    Inventors: Jean-Pierre Robin, Robert Dhal, Freddy Drouye, Jean-Pierre Marie, Nina Radosevic, Julie Robin, Karine Souchaud, Patricia Bataille
  • Patent number: 7241887
    Abstract: The subject invention relates to 3-azabicyclo[3.2.1]octane derivatives, pharmaceutical compositions comprising such derivatives and methods of using such derivatives to treat disease states, disorders and conditions mediated by opioid receptors. The subject invention also particularly relates to using such derivatives to treat certain disorders and conditions, for example irritable bowel syndrome, drug addiction, depression, anxiety, schizophrenia and eating disorders, among others.
    Type: Grant
    Filed: April 14, 2004
    Date of Patent: July 10, 2007
    Assignee: Pfizer Inc
    Inventors: Jotham W. Coe, Stanton McHardy, Crystal G. Bashore