Ring Nitrogens Of The Two Nitrogen Containing Hetero Rings Are Bonded Directly To The Same Atom Or Chain, Which Chain May Include A Ring Patents (Class 548/523)
  • Patent number: 9345722
    Abstract: The present invention relate to pharmaceutical formulations that include a CPHPC component and a delivery agent compound.
    Type: Grant
    Filed: July 24, 2007
    Date of Patent: May 24, 2016
    Assignee: EMISPHERE TECHNOLOGIES, INC.
    Inventors: Ihor Shevchuk, Steven Dinh
  • Publication number: 20150141646
    Abstract: In certain aspects, compounds and uses thereof are provided. In certain aspects, compound-conjugates and uses thereof are provided.
    Type: Application
    Filed: May 14, 2013
    Publication date: May 21, 2015
    Applicant: Concortis Biosystems, Corp., a wholly owned subsidary of Sorrento Therapeutics, Inc,
    Inventors: Zhenwei Miao, Yufeng Hong, Tong Zhu
  • Patent number: 8992902
    Abstract: The invention is directed to multi-functional N-maleimidyl polymer derivatives comprising a water soluble and non-peptidic polymer backbone having a terminal carbon, such as a poly(alkylene glycol), the terminal carbon of the polymer backbone being directly bonded to the nitrogen atom of a N-maleimidyl moiety without a linking group therebetween. The invention also provides two methods of preparing such linkerless N-maleimidyl polymer derivatives.
    Type: Grant
    Filed: May 21, 2014
    Date of Patent: March 31, 2015
    Assignee: Nektar Therapeutics
    Inventor: Xiaoming Shen
  • Publication number: 20150080364
    Abstract: Provided herein are carbamate compounds which may be useful in the treatment of for example, pain, solid tumors and/or obesity.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 19, 2015
    Applicants: Abide Therapeutics, Inc., The Scripps Research Insititute
    Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Dong-Hui Wang, Olivia Weber, Benjamin F. Cravatt, Micah J. Niphakis, Armand Cognetta, Jae Won Chang
  • Publication number: 20140376082
    Abstract: A compound is disclosed. The compound has the general structure: wherein Y is selected from the group consisting of hydrocarbons, hydrocarbons including nitrogen in the carbon backbone, and hydrocarbons including oxygen in the carbon backbone; wherein R1 and R2 are each independently selected from the group consisting of hydrogen, linear hydrocarbons, branched hydrocarbons, and cyclic hydrocarbons and wherein R1 and R2 are not both hydrogen; wherein X is selected from the group consisting of CH2, O, N—R3, S, and nothing and wherein R3 is selected from the group consisting of hydrogen, branched hydrocarbons, linear hydrocarbons, and cyclic hydrocarbons; wherein m is an integer between 1 and 50, inclusive; wherein n is an integer between 1 and 10,000, inclusive; and wherein p, q, and z are each independently an integer greater than 0.
    Type: Application
    Filed: January 24, 2012
    Publication date: December 25, 2014
    Applicant: HEWLETT-PACKARD DEVELOPMENT COMPANY, L.P.
    Inventors: Zhang-Lin Zhou, Qin Liu, Gregg Combs, James R. Owen
  • Publication number: 20140356894
    Abstract: A technique is provided to visualize microtubules in live cells that does not require genetic manipulation or microinjection. Moreover, this method also avoids perturbation of the endogenous microtubule network that occurs with taxol treatment. This technique exploits tyrosination and detyrosination of tubulin, a posttranslational modification cycle specific to the C-terminus of ?-tubulin. Specifically, cells are grown in medium supplemented with a tyrosine derivative possessing a reactive functional group. The cellular enzyme tubulin tyrosine ligase attaches the unnatural amino acid to a single site on tubulin. Addition of fresh medium containing a suitably derivatized fluorophore then yields fluorescent tubulin, which incorporate into cellular microtubules. Importantly, the tubulin labeling approach demonstrated here does not detrimentally affect microtubule network or cell morphology. Thus we present a simple, robust labeling technique that allows microscopic analysis of microtubules in live cells.
    Type: Application
    Filed: June 2, 2014
    Publication date: December 4, 2014
    Applicant: The Research Foundation for The State University of New York
    Inventors: Susan Bane Tuttle, Kamalika Mukherjee
  • Publication number: 20140349918
    Abstract: The present invention relates to xanthone analogs. Such compounds may be used in the treatment of bacterial infections.
    Type: Application
    Filed: September 10, 2012
    Publication date: November 27, 2014
    Applicants: Singapore Health Services Pte Ltd., Agency for Science, Technology and Research
    Inventors: Hanxun Zou, Lakshminiarayan Rajanmani, Lei Zhou, Chang Chui Charles Tang, Jun Jie Koh, Tiang Hwee Donald Tan, Chandra Verma, Roger W. Beuerman, Shouping Liu, Saraswathi Padmanabhan
  • Publication number: 20140330010
    Abstract: Provided are novel compounds that are useful in the prevention or treatment of such diseases as dementia, Alzheimer's disease, attention-deficient hyperactivity disorder, schizophrenia, epilepsy, central convulsion, obesity, diabetes mellitus, hyperlipidemia, narcolepsy, idiopathic hypersomnia, behaviorally induced insufficient sleep syndrome, sleep apnea syndrome, circadian rhythm disorder, parasomnia, sleep related movement disorder, insomnia, and depression, or allergic rhinitis, or pharmaceutically acceptable salts of such compounds.
    Type: Application
    Filed: December 7, 2012
    Publication date: November 6, 2014
    Applicant: TAISHO PHARMACEUTICAL CO., LTD
    Inventors: Toshio Nakamura, Seiji Masuda
  • Publication number: 20140275482
    Abstract: Compounds for UV-Vis detectable incorporation of a crosslinker a hapten into a protein or macromolecules are disclosed. The compounds comprise bis heterofunctional crosslinkers or haptens containing a chromophoric group that is incorporated into the linker that is positioned between a reactive linking moiety and a biotin molecule. The incorporation of the crosslinker or hapten into a protein or other macromolecules may be detected by UV-Vis spectroscopy.
    Type: Application
    Filed: March 14, 2013
    Publication date: September 18, 2014
    Inventor: Andrei POLUKHTIN
  • Publication number: 20140187546
    Abstract: Cystine analogs that improve the solubility of L-cystine in urine for treatment of cystinuria and which have the structure: and pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein each R and R? pair are independently selected from (i) or (ii); (i) R and R? are independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alcohol, substituted or unsubstituted aryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclic, and substituted or unsubstituted heteroaryl, or (ii) R and R? together form a substituted or unsubstituted heterocyclic ring structure, or a substituted or unsubstituted heteroaryl ring structure; X is hydrogen, or an alkyl; and Y is O or S.
    Type: Application
    Filed: January 2, 2014
    Publication date: July 3, 2014
    Applicant: Rutgers, The State University of New Jersey
    Inventors: Longqin Hu, Amrik Sahota
  • Patent number: 8765111
    Abstract: The invention is directed to multi-functional N-maleimidyl polymer derivatives comprising a water soluble and non-peptidic polymer backbone having a terminal carbon, such as a poly(alkylene glycol), the terminal carbon of the polymer backbone being directly bonded to the nitrogen atom of a N-maleimidyl moiety without a linking group therebetween. The invention also provides two methods of preparing such linkerless N-maleimidyl polymer derivatives.
    Type: Grant
    Filed: May 9, 2013
    Date of Patent: July 1, 2014
    Assignee: Nektar Therapeutics
    Inventor: Xiaoming Shen
  • Patent number: 8691710
    Abstract: Metal-containing complexes with general formula (1) (R1nPyr)(R2nPyr)ML1L2; or (2) [(R8XR9)(R1nPyr)(R2nPyr)]ML1L2 are disclosed; wherein M is a Group IV metal, Pyr is pyrrolyl ligand, n=1, 2 and 3, L1 and L2 are independently selected from alkoxide, amide or alkyl, L1 and L2 can be linked together, R1 and R2 can be same or different organic groups substituted at 2,3,4-positions of the pyrrole ring and are selected from the group consisting of linear and branched C1-6 alkyls, R8 and R9 are independently selected from the linear or branched chain alkylene group having 2-6 carbon atoms, and X is CH2 or oxygen. Methods of using the metal complexes as precursors to deposit metal or metal oxide films used for various devices in semi-conductor industries are also discussed.
    Type: Grant
    Filed: January 31, 2012
    Date of Patent: April 8, 2014
    Assignee: Air Products and Chemicals, Inc.
    Inventors: Wade Hampton Bailey, III, Sergei Vladimirovich Ivanov, Xinjian Lei, Moo-Sung Kim
  • Patent number: 8648094
    Abstract: Disclosed herein is an isomer, enantiomer, diastereoisomer or tautomer of a compound represented by Formula I: or a prodrug, or a pharmaceutically acceptable salt, or labeled with a detectable label or an affinity tag thereof; wherein R1, R1a, R100, R100a, R2, R200, W, B, and W1 are defined herein. Also disclosed are methods of using compounds of Formula I to treat proliferative disorders such as cancer.
    Type: Grant
    Filed: March 21, 2012
    Date of Patent: February 11, 2014
    Assignee: Pharmascience, Inc.
    Inventors: Alain Laurent, Scott Jarvis, Patrick Bureau, Alain Boudreault, James Jaquith
  • Patent number: 8637611
    Abstract: The invention is based on the discovery that a remarkable improvement in the performance of maleimide thermosets can be achieved by incorporating amide-extended maleimides into an adhesive formulation. Amide-extended maleimides described herein can be used to toughen bismaleimide thermosetting materials without sacrificing any thermal stability. Amide-extended maleimides are readily prepared by reacting a bismaleimide with an appropriate amine via the well-known Michael addition reaction. Acylation of the resulting secondary amines provides the amide-extended maleimide. The acylating agent can also be used to introduce polymerizable functional groups into the backbones of these thermoset monomers. Amide-extended acrylate and methacrylate monomers can also be prepared.
    Type: Grant
    Filed: August 13, 2009
    Date of Patent: January 28, 2014
    Assignee: Designer Molecules, Inc.
    Inventor: Stephen M Dershem
  • Patent number: 8486183
    Abstract: An acid gas absorbent comprising an alkylamino alkyloxy (alcohol) monoalkyl ether and a process for the selective removal Of H2S from gaseous mixtures containing H2S and CO2 using an absorbent solution comprising an alkylamino alkyloxy alcohol monoalkyl ether.
    Type: Grant
    Filed: July 21, 2006
    Date of Patent: July 16, 2013
    Assignee: ExxonMobil Research and Engineering Company
    Inventors: Michael Siskin, Edmund John Mozeleski, Robert Basil Fedich, Frank Cheng-Yu Wang
  • Publication number: 20130172576
    Abstract: A branched hetero polyfunctional polyoxyalkylene compound represented by the following formula (1): wherein Z represents a hydroxyl group-removed residue of pentaerythritol or dipentaerythritol, OA1 and OA2 represent an oxyalkylene group having 2 to 4 carbon atoms, L1, L2 and L3 represent an alkylene group or an alkylene group that contains an ester bond, a urethane bond, an amide bond, an ether bond, a carbonate bond, a secondary amino group or a urea bond, X and Y are different from each other and represent a functional group capable of a chemical reaction; m and n are an average number of moles of the oxyalkylene group added, m represents 5 to 1,000, n represents 0 to 1,000, and p, q and r represent 0 or 1; and s1 is an integer of 2 or more and s1+s2=4 or 6.
    Type: Application
    Filed: October 1, 2012
    Publication date: July 4, 2013
    Applicant: NOF CORPORATION
    Inventor: NOF Corporation
  • Patent number: 8470855
    Abstract: Compounds of the general formulae (1) and (2) A-B-D-B?-A???(1) and A-B-D-E??(2) in which A and A? may be identical or different and are the residue in which X is S, O, CH2, CH2CH2, CH2O or CH2NH, and Y is H or CN, and * designates a chiral carbon atom preferably in S- or L-configuration; B and B? may be identical or different and are an O, N or S containing or non-containing, unsubstituted or substituted, unbranched or branched alkylene residue, cycloalkylene residue, aralkylene residue, heterocycloalkylene residue, heteroarylalkylene residue, arylamidoalkylene residue, heteroarylamidoalkylene residue, unsubstituted or mono- or poly-substituted arylene residue or heteroarylene residue having one or more five-, six- or seven-membered ring(s); D is —S—S— or —Se—Se—; and E is the group —CH2—CH(NH2)—R9 or —CH2—*CH(NH2)—R9 respectively in which R9 is an O, N or S containing or non-containing, unsubstituted or substituted, unbranched or branched alkyl residue, cycloalkyl residue, aralkyl residu
    Type: Grant
    Filed: November 10, 2006
    Date of Patent: June 25, 2013
    Assignee: IMTM GmbH
    Inventors: Siegfried Ansorge, Klaus Neubert, Ute Bank, Irene Reichstein, Jürgen Faust, Michael Täger, Petra Fuchs, Bianca Senns
  • Patent number: 8431721
    Abstract: The invention relates to compounds of the structure of formula I and II: where X is selected from the group consisting of O, S and NH; Y, A and B are independently selected from the group consisting of N and CH; D, E and F are independently selected from the group consisting of CH, N, O and S; the symbol represents a single or a double bond; and R1, R2 and R3 are independently selected from the group consisting of H, electron withdrawing groups and electron releasing groups. In other embodiments, the compounds are used as oxygen scavengers and in barrier compositions and articles.
    Type: Grant
    Filed: June 20, 2011
    Date of Patent: April 30, 2013
    Assignee: Constar International, Inc.
    Inventors: Girish Nilkanth Deshpande, Paul David Weipert, Michael W. Ensley
  • Patent number: 8404795
    Abstract: Polymers for photoresists and monomers for incorporation into those polymers are disclosed. The polymers comprise a photoacid generator (PAG) component and at least a second component that is photolytically stable and acid-stable. The polymers may also contain a third, acid-labile component. The photoacid generator is based on N-sulfoxyimides and related moieties that contain photolabile oxygen-heteroatom and oxygen-aromatic carbon bonds.
    Type: Grant
    Filed: August 26, 2010
    Date of Patent: March 26, 2013
    Assignee: The Research Foundation for the State University of New York
    Inventor: Robert L. Brainard
  • Publication number: 20130043137
    Abstract: Provided is a copper plating technique that enables the filling of high aspect-ratio via-holes and through-holes in semiconductor substrates such as silicon substrates, organic material substrates or ceramic substrates. The disclosed technique involves a tertiary amine compound, which is obtained by reacting a heterocyclic compound with the epoxy group of a glycidyl ether group of a compound that has three or more glycidyl ether groups, and a quaternary amine compound thereof, as well as a copper plating additive, a copper plating bath, and a copper plating method employing the compounds.
    Type: Application
    Filed: April 30, 2010
    Publication date: February 21, 2013
    Applicant: JCU CORPORATION
    Inventors: Hiroki Yasuda, Ryoichi Kimizuka, Tatsuji Takasu, Takuro Sato, Hiroshi Ishizuka, Yasuhiro Ogo, Yuto Oyama, Yu Tonooka, Mikiko Kosaka, Aya Shimomura, Yumiko Shimizu
  • Publication number: 20130035484
    Abstract: A compound of formula (I): which is substantially free of any of the corresponding compound of formula (IB): methods of making such compounds, and the further transformation of such compounds.
    Type: Application
    Filed: April 15, 2011
    Publication date: February 7, 2013
    Applicant: SPIROGEN DEVELOPMENTS SÀRL
    Inventors: Philip Wilson Howard, Luke Masterson, Arnaud Tiberghien
  • Publication number: 20120184530
    Abstract: Compounds, compositions, and methods of using such compounds to modulate apoptosis including IAP antagonists are provided herein. Compositions including mimetics of the invention and, optionally, secondary agents, may be used to treat proliferative disorders such as, cancer and autoimmune diseases.
    Type: Application
    Filed: March 27, 2012
    Publication date: July 19, 2012
    Applicant: TETRALOGIC PHARMACEUTICALS CORPORATION
    Inventor: Stephen M. CONDON
  • Publication number: 20120129828
    Abstract: The present invention relates to compounds of Formula (I) that are have activity as S1P1 receptor modulating agents, more specifically to specifically compounds that are S1P1 receptor agonists. The invention also related to the use of such compounds to treat diseases associated with inappropriate S1P1 receptor activity such as autoimmune diseases.
    Type: Application
    Filed: June 18, 2009
    Publication date: May 24, 2012
    Inventors: Victor J. Cee, Jian Lin, Xiang Y. Yu, Zhaoda Zhang
  • Patent number: 8178528
    Abstract: The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have histamine—H3 receptor antagonist or inverse agonist activity, as well as methods and intermediates for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using these compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.
    Type: Grant
    Filed: March 28, 2006
    Date of Patent: May 15, 2012
    Assignee: Eli Lilly and Company
    Inventors: Philip Arthur Hipskind, Takako Takakuwa, Cynthia Darshini Jesudason, Robert Alan Gadski, William Joseph Hornback, Richard Todd Pickard, Lisa Selsam Beavers
  • Patent number: 8092891
    Abstract: A cyanine compound is represented by: wherein, R11 and R12 each independently represent a hydrogen atom, a hydroxyl group, a halogen atom, a nitro group, a cyano group, an organic group having 1 to 30 carbon atoms, or a group represented by the following general formula (II), (II?), or (III); R13 and R14 each independently represent a hydrogen atom, an organic group having 1 to 30 carbon atoms, or a substituent represented by the following general formula (III); R11 and R12 may be connected together to form a ring structure; R19 represents a hydrogen atom or an organic group having 1 to 30 carbon atoms; R13 and R14 may be connected together to form a heterocycle; N—R13 may be connected together with a methylene group in a polymethine chain to form a heterocycle; Z00 is an organic group having 1 to 10 carbon atoms; m is 0 or 1; s is 2 to 8; Anq? represents an anion having a valence of q; q is 1 or 2; and p represents a coefficient for maintaining charge neutrality.
    Type: Grant
    Filed: July 10, 2007
    Date of Patent: January 10, 2012
    Assignee: Adeka Corporation
    Inventor: Satoshi Yanagisawa
  • Publication number: 20110306769
    Abstract: The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.
    Type: Application
    Filed: February 24, 2010
    Publication date: December 15, 2011
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Tomomi Ikemoto, Hideya Mizufune, Toshiaki Nagata, Misayo Sera, Naohiro Fukuda, Takeshi Yamasaki
  • Publication number: 20110230463
    Abstract: [Object] Provided is a compound which has an excellent S1P1 agonist action, and is useful particularly as an active ingredient for an agent for preventing and/or treating a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells. [Means for Solution] According to the present invention, a 2H-chromene compound or a derivative thereof which has an excellent S1P1 agonist action, and is useful particularly as an active ingredient of an agent for preventing and/or treating a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells can be provided. The 2H-chromene compound and a derivative thereof which are the compounds of the present invention have an S1P1 agonist action, and can be used particularly for prevention and/or treatment of a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells.
    Type: Application
    Filed: December 4, 2009
    Publication date: September 22, 2011
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Hironori Harada, Kazuyuki Hattori, Kazuya Fujita, Sunao Imada, Tatsuaki Morokata
  • Patent number: 8022096
    Abstract: Pyrrolidine compounds described herein and methods for using them to inhibit dipeptidyl peptidase IV and treat Type II diabetes.
    Type: Grant
    Filed: February 25, 2009
    Date of Patent: September 20, 2011
    Assignee: National Health Research Institutes
    Inventors: Weir-Torn Jiaang, Yu-Sheng Chao, Ting-Yueh Tsai, Tsu Hsu
  • Publication number: 20110212955
    Abstract: The present invention relates to a new class of rosamine derivatives, in one embodiment, the compounds have the structure (I) or any pharmaceutically acceptable salt or solvate thereof, wherein: R1 represents aryl, Het1 or C1-6 alkyl, which latter group is optionally substituted by aryl or Het2; R2a and R2b together form C3.8 n-alkylene, which alkylene group is optionally substituted by one or more substituents selected from halo, C1-4 alkyl, C(O)OH and C(O)O—C1-4, alkyl and which alkylene group is optionally interrupted by X1; R3a and R3b together form C3-6 /7-alkylene, which alkylene group is optionally substituted by one or more substituents selected from halo.
    Type: Application
    Filed: July 2, 2009
    Publication date: September 1, 2011
    Applicant: CANCER RESEARCH INITIATIVES FOUNDATION
    Inventors: Hong Boon Lee, Kevin Burgess, Siang Hui Lim, Liangxing Wu
  • Patent number: 8008296
    Abstract: The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases. (Formula I).
    Type: Grant
    Filed: June 28, 2006
    Date of Patent: August 30, 2011
    Assignee: Eli Lilly and Company
    Inventors: Lisa Selsam Beavers, Don Richard Finley, Robert Alan Gadski, Philip Arthur Hipskind, William Joseph Hornback, Cynthia Darshini Jesudason, Richard Todd Pickard, Takako Takakuwa, Grant Mathews Vaught
  • Publication number: 20110177060
    Abstract: IAP BIR domain binding compounds of Formula (I), (II), (III), or (IV), and the use thereof, for example, for the treatment or prevention of proliferative diseases.
    Type: Application
    Filed: September 17, 2009
    Publication date: July 21, 2011
    Applicant: AEGERA THERAPEUTICS, INC.
    Inventor: James Jaquith
  • Publication number: 20110130538
    Abstract: Polymers for photoresists and monomers for incorporation into those polymers are disclosed. The polymers comprise a photoacid generator (PAG) component and at least a second component that is photolytically stable and acid-stable. The polymers may also contain a third, acid-labile component. The photoacid generator is based on N-sulfoxyimides and related moieties that contain photolabile oxygen-heteroatom and oxygen-aromatic carbon bonds.
    Type: Application
    Filed: August 26, 2010
    Publication date: June 2, 2011
    Applicant: The Research Foundation of the State University of New York
    Inventor: Robert L. BRAINARD
  • Patent number: 7943605
    Abstract: The present invention relates to compounds of formula (I) comprising a lactam or a lactam derivative moiety, processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as pharmaceuticals.
    Type: Grant
    Filed: October 25, 2006
    Date of Patent: May 17, 2011
    Assignee: UCB Pharma S.A.
    Inventors: Sylvain Celanire, Luc Quere, Frédéric Denonne, Laurent Provins
  • Publication number: 20100249400
    Abstract: Disclosed is a compound represented by the formula (I) below as a dihydronaphthalene compound having a chemical structure which is excellent in production efficiency when compared with lasofoxifene and nafoxidine. This compound is useful as a proteasome inhibitor and/or an antitumor agent.
    Type: Application
    Filed: September 11, 2008
    Publication date: September 30, 2010
    Applicant: Tokyo University of Science Educational Foundation Administrative Organization
    Inventor: Isamu Shiina
  • Publication number: 20100173969
    Abstract: Provided are agents and methods for use in depleting serum amyloid P component (SAP) from a patient in need thereof.
    Type: Application
    Filed: March 16, 2009
    Publication date: July 8, 2010
    Inventor: Mark B. Pepys
  • Publication number: 20100160319
    Abstract: The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.
    Type: Application
    Filed: June 28, 2006
    Publication date: June 24, 2010
    Inventors: Lisa Selsam Beavers, Don Richard Finley, Robert Alan Gadski, Philip Arthur Hipskind, William Joseph Hornback, Cynthia Darshini Jesudason, Richard Todd Pickard, Takako Takakuwa, Grant Mathews Vaught
  • Publication number: 20100145070
    Abstract: Anti-cancer compounds and manufacturing methods thereof are disclosed. The anti-cancer compounds are 1,8-diamidoanthraquinone derivatives with amino compounds. The manufacturing method includes the steps of: add 1,8-bis(chloroacetamido)anthraquinone or 1,8-bis(3-chloropropionamido)-anthraquinone with amino compounds, catalysts, and dehydrated dimethylformamide (DMF) to form a mixture and react with one another. Then by purification and recrystallization, the anti-cancer compounds are obtained. The anti-cancer compounds of the present invention are compounds with whole new structure that overcome serious cardiac toxicity of the conventional anti-cancer drug-doxorubincin.
    Type: Application
    Filed: March 7, 2009
    Publication date: June 10, 2010
    Inventor: Hsu-Shan HUANG
  • Patent number: 7709503
    Abstract: Compounds of Formula (1) and their pharmaceutically acceptable salts are described: Formula (1) Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.
    Type: Grant
    Filed: September 10, 2004
    Date of Patent: May 4, 2010
    Assignee: AstraZeneca AB
    Inventors: Oluyinka Morenike Green, Kenneth Gregory Hull, Haihong Ni, Sheila Irene Hauck, George Byron Mullen, Alexander Louis Breeze, Neil James Hales, David Timms
  • Publication number: 20100056495
    Abstract: Compounds, compositions, and methods of using such compounds to modulate apoptosis including IAP antagonists are provided herein. Compositions including mimetics of the invention and, optionally, secondary agents, may be used to treat proliferative disorders such as, cancer and autoimmune diseases.
    Type: Application
    Filed: July 24, 2007
    Publication date: March 4, 2010
    Applicant: TETRALOGIC PHARMACEUTICALS CORPORATION
    Inventor: Stephen M. Condon
  • Publication number: 20090253709
    Abstract: An series of 2,7-disubstituted anthraquinone derivatives including a formula I are provided. R is a first substituted group selected from a group consisting of a hydrogen, an amino group, a nitro group, a hydroxyl group, a C1-C12 alkyl group, a C1-C12 alkyl halide group (—(CH2)nX), a C3-C12 cycloalkyl group, a benzyl group, a C1-C12 alkylamino group, a C5-C12 nitrocycloalkyl group and a heterocyclic group, n satisfies 1?n?12 and X is an atom selected from a group consisting of a fluoride (F), a chloride (Cl), a bromide (Br) and an iodine (I). The preparation method of the 2,7-disubstituted anthraquinone derivatives includes the steps of acetylating 2,7-diaminoanthraquinone to be one 2,7-disubstituted anthraquinone derivative, which can be further aminated to be another 2,7-disubstituted anthraquinone derivative.
    Type: Application
    Filed: August 15, 2008
    Publication date: October 8, 2009
    Applicant: NATIONAL DEFENSE MEDICAL CENTER
    Inventor: Hsu-Shan HUANG
  • Publication number: 20090124667
    Abstract: Compounds of the general formulae (1) and (2) A-B-D-B?-A???(1) and A-B-D-E??(2) in which A and A? may be identical or different and are the residue in which X is S, O, CH2, CH2CH2, CH2O or CH2NH, and Y is H or CN, and * designates a chiral carbon atom preferably in S- or L-configuration; B and B? may be identical or different and are an O, N or S containing or non-containing, unsubstituted or substituted, unbranched or branched alkylene residue, cycloalkylene residue, aralkylene residue, heterocycloalkylene residue, heteroarylalkylene residue, arylamidoalkylene residue, heteroarylamidoalkylene residue, unsubstituted or mono- or poly-substituted arylene residue or heteroarylene residue having one or more five-, six- or seven-membered ring(s); D is —S—S— or —Se—Se—; and E is the group —CH2—CH(NH2)—R9 or —CH2—*CH(NH2)—R9 respectively in which R9 is an O, N or S containing or non-containing, unsubstituted or substituted, unbranched or branched alkyl residue, cycloalkyl residue, aralkyl resid
    Type: Application
    Filed: November 10, 2006
    Publication date: May 14, 2009
    Applicant: IMTM GmbH
    Inventors: Siegfried Ansorge, Klaus Neubert, Ute Bank, Irene Reichstein, Jurgen Faust, Michael Tager, Petra Fuchs, Bianca Senns
  • Publication number: 20080167479
    Abstract: The present invention relates to a process for preparing vildagliptin of formula (I) with high chemical and enantiomeric purity and compositions comprising vildagliptin. In addition, the present invention relates to (2S,2?S)-1,1?-[[(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)imino]bis(1-oxo-2,1-ethanediyl)]di(2-pyrrolidinecarbonitrile) of formula (II), processes for preparing, and compositions comprising a compound for formula (II). Furthermore, the invention relates to processes for determining the purity of vildagliptin using a compound of formula (II).
    Type: Application
    Filed: January 10, 2008
    Publication date: July 10, 2008
    Applicant: Medichem, S.A.
    Inventors: Stephen Winter, Jordi Bosch, Jordi Puig Serrano, Jose Javier Soto
  • Patent number: 7378436
    Abstract: A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein R1 is H, C1-6alkyl, —C(X)Y, C3-8cycloalkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; R2 is aryl or heteroaryl, each optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; R3 is C1-6alkyl, C3-8cycloalkyl, C3-8cycloalkyl-C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-6alkyl, C1-6alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy —C1-6alkyl and C1-4alkyl-S—C1-4alkyl; X is S o
    Type: Grant
    Filed: June 17, 2004
    Date of Patent: May 27, 2008
    Assignee: Pfizer Inc.
    Inventors: Paul Vincent Fish, Michael Jonathan Fray, Alan Stobie, Florian Wakenhut, Gavin Alistair Whitlock, Mark David Andrews, Alan Daniel Brown, Mark Ian Lansdell
  • Patent number: 7253204
    Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
    Type: Grant
    Filed: March 25, 2005
    Date of Patent: August 7, 2007
    Assignee: MethylGene Inc.
    Inventors: Daniel Delorme, Arkadii Vaisburg, Oscar Moradei, Silvana Leit, Stephane Raeppel, Sylvie Frechette, Giliane Bouchain, Zhihong Zhou, Isabelle Paquin, Frederic Gaudette, Ljubomir Isakovic
  • Patent number: 7208600
    Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3–NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection and to processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.
    Type: Grant
    Filed: October 12, 2004
    Date of Patent: April 24, 2007
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Kevin M. Cottrell, Robert B. Perni, Janos Pitlik
  • Patent number: 7160902
    Abstract: Amide derivatives of the general formulae Ia and Ib: are disclosed. Pharmaceutical compositions containing these compounds, and methods for their use, inter alia, for treating and/or preventing gastrointestinal disorders, pain, and pruritus are also disclosed.
    Type: Grant
    Filed: November 14, 2003
    Date of Patent: January 9, 2007
    Assignee: Adolor Corporation
    Inventors: Roland E. Dolle, Guo-Hua Chu, Minghua Gu
  • Patent number: 7138376
    Abstract: A compound, method and composition for treating a host infected with a hepatitis C viral comprising administering an effective hepatitis C treatment amount of a described 4?-disubstituted nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.
    Type: Grant
    Filed: September 30, 2002
    Date of Patent: November 21, 2006
    Assignees: Idenix Pharmaceuticals, Inc., Centre National de la Recherche Scientifique
    Inventors: Gilles Gosselin, Jean-Louis Imbach, Jean-Pierre Sommadossi
  • Patent number: 7109343
    Abstract: Compounds having the formula: are disclosed. M1 and M2 are the same or different and are transition metal atoms or ions; Z2 and Z3, independently, are the atoms necessary to complete a 3–12 membered heterocyclic ring; Z1 is an alkylene or arylene group; Q1 and Q2 are the same or different and are electron withdrawing groups; L1 and L3, taken together, represent —O—CR13—O—; L2 and L4, taken together, represent —O—CR14—O—; and R13 and R14 are the same or different and are selected from the group consisting of alkyl groups and aryl groups or R13 and R14 represent alkylene or arylene groups that are directly or indirectly bonded to one another. Methods for making such compounds are also disclosed, as are intermediates which can be used in their preparation. Also disclosed are methods for carrying out C—H insertion reactions using bis-transition metal catalysts, such as the above compounds. Procedures for preparing d-threo methylphenidate, tolterodine, CDP-840, nominfensine, and sertraline, are described.
    Type: Grant
    Filed: April 5, 2004
    Date of Patent: September 19, 2006
    Assignee: The Research Foundation of State University of New York
    Inventor: Huw M. L. Davies
  • Patent number: RE40525
    Abstract: A racemate diastereoisomer and optical isomer of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which may be optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4—C(O)—; a carboxyl derivative of formula R4—O—C(O)—; an amide derivative of formula R4—N(R5)—C(O)—; a thioamide derivative of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5 is H or C1-6 alkyl; and Y is H or C1-6 alkyl; R3 is C1-8 alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl; R2 is C2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl or C4-10 (alkylcycloalkyl), all of which being optionally mono-, di- or tri-
    Type: Grant
    Filed: September 30, 2005
    Date of Patent: September 30, 2008
    Assignee: Boehringer Ingelheim (Canada) Ltd.
    Inventors: Montse Llinas-Brunet, Murray D. Bailey, Dale R. Cameron, Anne-Marie Faucher, Elise Ghiro, Nathalie Goudreau, Teddy Halmos, Marc-André Poupart, Jean Rancourt, Youla S. Tsantrizos, Dominik M. Wernic
  • Patent number: RE41356
    Abstract: Racemates, diastereolsomers and optical isomers of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4—C(O)—; a carboxyl of formula R4—O—C(O)—; an amide of formula R4—N(R5)—C(O)—; a thioamide of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5 is H or C1-6 alkyl; and Y is H or C1-6 alkyl; R3 is C1-8 alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl; R2 is CH2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl or C4-10 (alkylcycloalkyl), all of which being optionally mono-, di- or tri-substituted with R21, or R20 is a C6
    Type: Grant
    Filed: May 12, 2008
    Date of Patent: May 25, 2010
    Assignee: Boehringer Ingelheim Canada Ltd.
    Inventors: Montse Llinas-Brunet, Murray D. Bailey, Dale R. Cameron, Elise Ghiro, Nathalie Goudreau, Marc-Andre Poupart, Jean Rancourt, Youla S. Tsantrizos, Anne-Marie Faucher, Teddy Halmos, Dominik M. Wernic