Cyano Containing Patents (Class 544/163)
  • Patent number: 9340519
    Abstract: A substituted paracyclophane of formula (I) is provided wherein X1 and X2 are linking groups comprising between 2 to 4 carbon atoms, Y1 and Y2 are selected from the group consisting of hydrogen, halide, oxygen, nitrogen, alkyl, cycloalkyl, aryl or heteroaryl and Z is a substituted or unsubstituted alkyl group, aryl group or heteroaryl group. The substituted paracyclophane provides transition metal catalysts that are useful in C—C and C—N bond formation and asymmetric hydrogenation reactions.
    Type: Grant
    Filed: July 21, 2014
    Date of Patent: May 17, 2016
    Assignee: Johnson Matthey PLC
    Inventors: Jianliang Xiao, Jiwu Ruan
  • Publication number: 20140330012
    Abstract: A substituted paracyclophane of formula (I) is provided wherein X1 and X2 are linking groups comprising between 2 to 4 carbon atoms, Y1 and Y2 are selected from the group consisting of hydrogen, halide, oxygen, nitrogen, alkyl, cycloalkyl, aryl or heteroaryl and Z is a substituted or unsubstituted alkyl group, aryl group or heteroaryl group. The substituted paracyclophane provides transition metal catalysts that are useful in C—C and C—N bond formation and asymmetric hydrogenation reactions.
    Type: Application
    Filed: July 21, 2014
    Publication date: November 6, 2014
    Applicant: Johnson Matthey Public Limited Company
    Inventors: Jianliang Xiao, Jiwu Ruan
  • Patent number: 8877747
    Abstract: An indenone derivative of formula (1) is effective in enhancing the activity of osteoblastic cells and inhibiting bone resorption by osteoclastic cells, and a pharmaceutical composition comprising the indenone derivative or a pharmaceutically acceptable salt thereof is useful for preventing or treating bone diseases such as osteoporosis.
    Type: Grant
    Filed: October 21, 2009
    Date of Patent: November 4, 2014
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Jung Nyoung Heo, Myung Ae Bae, Nack Jeong Kim, Sung Youn Chang, Nam Sook Kang, Sung Eun Yoo, Eun Sook Hwang
  • Patent number: 8822680
    Abstract: A substituted paracyclophane is described of formula (I) wherein X1 and X2 are linking groups comprising between 2 to 4 carbon atoms, Y1 and Y2 are selected from the group consisting of hydrogen, halide, oxygen, nitrogen, alkyl, cycloalkyl, aryl or heteroaryl and Z is a substituted or unsubstituted alkyl group, aryl group or heteroaryl group. Preferably X1 and X2 are —(C2H4)— and Z is a substituted aryl group. The substituted paracyclophane provides transition metal catalysts that are useful in C—C and C—N bond formation and asymmetric hydrogenation reactions.
    Type: Grant
    Filed: August 21, 2008
    Date of Patent: September 2, 2014
    Assignee: Johnson Matthey PLC
    Inventors: Jianliang Xiao, Jiwu Ruan
  • Publication number: 20140107335
    Abstract: The present invention is directed to novel cyclic amines which inhibit the P2X7 receptor.
    Type: Application
    Filed: October 10, 2013
    Publication date: April 17, 2014
    Applicant: H. Lundbeck A/S
    Inventors: John Paul Kilburn, Lars Kyhn Rasmussen, Mikkel Jessing, Eman Mohammed Eldemenky, Bin Chen, Yu Jiang
  • Publication number: 20140058101
    Abstract: The invention is directed to a phosphine compound represented by general formula (1) wherein R? and R? independently are selected from alkyl, cycloalkyl and 2-furyl radicals, or R? and R? are joined together to form with the phosphorous atom a carbon-phosphorous monocycle comprising at least 3 carbon atoms or a carbon-phosphorous bicycle; the alkyl radicals, cycloalkyl radicals, and carbon-phosphorous monocycle being unsubstituted or substituted by at least one radical selected from the group of alkyl, cycloalkyl, aryl, alkoxy, and aryloxy radicals; Cps is a partially substituted or completely substituted cyclopentadien-1-yl group, including substitutions resulting in a fused ring system, and wherein a substitution at the 1-position of the cyclopentadien-1-yl group is mandatory when the cyclopentadien-1-yl group is not part of a fused ring system or is part of an indenyl group. Also claimed is the use of these phosphines as ligands in catalytic reactions and the preparation of these phosphines.
    Type: Application
    Filed: October 29, 2013
    Publication date: February 27, 2014
    Applicant: Evonik Degussa GmbH
    Inventors: Herbert Plenio, Christoph Fleckenstein, Renat Kadyrov, Juan Almena, Axel Monsees, Thomas Riermeier
  • Publication number: 20130244962
    Abstract: Several parasites responsible for mammalian diseases are dependent on cysteine protease for various life-cycle functions. Inhibition or decreasing function of these proteases can be useful in the treatment and/or prevention of these parasitic diseases including; toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, schistosomiasis, amebiasis, giardiasis, clonorchiasis, opisthorchiasis, paragonimiasis, fasciolopsiasis, lymphatic filariasis, onchocerciasis, dracunculiasis, ascariasis, trichuriasis, stronglyoidiasis, trichostrongyliasis, trichomoniasis or cestodiasis.
    Type: Application
    Filed: April 11, 2013
    Publication date: September 19, 2013
    Applicant: Merck Frosst Canada Ltd.
    Inventors: Elise ISABEL, Christopher MELLON, Christian BEAULIEU
  • Publication number: 20130217660
    Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
    Type: Application
    Filed: May 12, 2011
    Publication date: August 22, 2013
    Inventors: Dong-Ming Shen, John S. Debenham, Thomas H. Graham, Matthew J. Clements, Yong Zhang
  • Publication number: 20130203752
    Abstract: Provided herein are compounds and prodrugs and methods of preparation of compounds and prodrugs that are capable of functioning as releasers and/or uptake inhibitors of one or more monoamine neurotransmitters, including dopamine, serotonin, and norepinephrine. Also provided are pharmaceutical compositions comprising one or more of these compounds or prodrugs, which may further comprise one or more additional therapeutic agents. Also provided are methods of treatment of various conditions that may be responsive to modification of monoamine neutrotransmitter levels, such as pre-obesity, obesity, addiction, and depression.
    Type: Application
    Filed: May 20, 2011
    Publication date: August 8, 2013
    Inventors: Bruce E. Blough, Richard Rothman, Antonio Landavazo, Kevin M. Page, Ann Marie Decker
  • Publication number: 20130089624
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein. Additionally, the present invention also relates to novel processes for the production of various morpoholine based intermediates.
    Type: Application
    Filed: September 28, 2012
    Publication date: April 11, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Jean-Damien Charrier, Stephen Clinton Young, Christopher John Davis, John Studley
  • Publication number: 20130053557
    Abstract: Processes and intermediates for preparing linezolid, and pharmaceutically acceptable salts thereof, are described herein.
    Type: Application
    Filed: April 28, 2011
    Publication date: February 28, 2013
    Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
    Inventor: James R. McCarthy
  • Publication number: 20120245348
    Abstract: Disclosed herein are phosphine compounds represented by the general formula (4): and corresponding phosphonium salts represented by the general formula (4a): Also disclosed are processes for the preparation of these phosphines and phosphonium salts as well as their use as ligands in catalytic reactions.
    Type: Application
    Filed: April 2, 2012
    Publication date: September 27, 2012
    Inventors: Herbert PLENIO, Christoph FLECKENSTEIN, Renat KADYROV, Juan ALMENA, Axel MONSEES, Thomas RIERMEIER
  • Patent number: 8268996
    Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cathepsin S.
    Type: Grant
    Filed: June 16, 2011
    Date of Patent: September 18, 2012
    Assignee: IRM LLC
    Inventors: Hong Liu, David C. Tully, Arnab Chatterjee, Phillip B. Alper, David H. Woodmansee, Daniel Mutnick
  • Publication number: 20120214991
    Abstract: An indenone derivative of formula (1) is effective in enhancing the activity of osteoblastic cells and inhibiting bone resorption by osteoclastic cells, and a pharmaceutical composition comprising the indenone derivative or a pharmaceutically acceptable salt thereof is useful for preventing or treating bone diseases such as osteoporosis.
    Type: Application
    Filed: October 21, 2009
    Publication date: August 23, 2012
    Applicant: Korea Research Institute of Chemical Technology
    Inventors: Jung Nyoung Heo, Myung Ae Bae, Nack Jeong Kim, Sung Youn Chang, Nam Sook Kang, Sung Eun Yoo, Eun Sook Hwang
  • Patent number: 8168631
    Abstract: Compounds according to the formula below are disclosed herein: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: February 3, 2009
    Date of Patent: May 1, 2012
    Assignee: Allergan, Inc.
    Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello, Rong Yang, Cédric Chauvignac
  • Publication number: 20120004227
    Abstract: The present invention discloses novel cyclohexane derivatives having NPY Y5 receptor antagonistic activity. Specifically, the present invention discloses a compound represented by the formula (I), or a pharmaceutically acceptable salt or a solvate thereof: wherein A is substituted or unsubstituted aryl or heterocyclyl; a combination of X and Y is a combination selected from (X, Y)?(C(?O)N(R1), C(?O)N(R2)), (C(?O)N(R1), imidazole-1,3-diyl), (N(R1), C(?O)N(R2)), (O, C(?O)N(R2)), (C(R3)(R4), N(R2)) or (a single bond, C(?O)N(R2)); R1, R2 and R3 are independently hydrogen or substituted or unsubstituted alkyl; R5 is substituted or unsubstituted aryl or heterocyclyl; R6 is halogen, oxo, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryloxy; m is 0 or 1; and n is an integer of 0 to 5; and B is aromatic carbocycle, monocyclic heterocycle or fused bicyclic heterocycle.
    Type: Application
    Filed: March 5, 2010
    Publication date: January 5, 2012
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Hiroshi Yoshida, Keisuke Tonogaki, Masahiro Sakagami, Kenji Takaya
  • Patent number: 7989447
    Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, or chronic pain.
    Type: Grant
    Filed: April 13, 2007
    Date of Patent: August 2, 2011
    Assignee: NeurAxon, Inc.
    Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
  • Publication number: 20110172417
    Abstract: This invention relates to a heterogeneous copper nanocatalyst composed of copper nanoparticles immobilized on a boehmite support, a method of preparing the same, and the use thereof. The copper nanocatalyst composed of the copper nanoparticles supported on boehmite exhibits excellent performance in a Huisgen cycloaddition reaction and an A3 coupling reaction of aldehyde, amine and alkyne. The copper nanocatalyst is able to be prepared in a large scale and shows superior reactivity even when used in a small amount under mild conditions without an additive in an organic reaction. This heterogeneous catalyst is easy to separate and reuse after the reaction.
    Type: Application
    Filed: July 9, 2008
    Publication date: July 14, 2011
    Applicant: Postech Academy-Industry Foundation
    Inventors: Jai Wook Park, In Soo Park
  • Publication number: 20110028718
    Abstract: A substituted paracyclophane is described of formula (I) wherein X1 and X2 are linking groups comprising between 2 to 4 carbon atoms, Y1 and Y2 are selected from the group consisting of hydrogen, halide, oxygen, nitrogen, alkyl, cycloalkyl, aryl or heteroaryl and Z is a substituted or unsubstituted alkyl group, aryl group or heteroaryl group. Preferably X1 and X2 are —(C2H4)— and Z is a substituted aryl group. The substituted paracyclophane provides transition metal catalysts that are useful in C—C and C—N bond formation and asymmetric hydrogenation reactions.
    Type: Application
    Filed: August 21, 2008
    Publication date: February 3, 2011
    Applicant: Johnson Matthey Public Limited Company
    Inventors: Jianliang Xiao, Jiwu Ruan
  • Publication number: 20100311754
    Abstract: Naphthalene-based compounds having linked heterocyclic and aromatic rings capable of inhibiting P38, methods for inhibiting P38 in vivo or in vitro, diagnostics for determining activity in the treatment of P38 and/or cytokine-associated conditions and methods for treating conditions associated with P38 activity or cytokine activity; more particularly naphthalene-based compounds of Formula (I) having a morpholine heterocyclic ring, and methods of use thereof.
    Type: Application
    Filed: August 11, 2010
    Publication date: December 9, 2010
    Applicant: ARQULE, INC.
    Inventors: Mark A. Ashwell, Yanbin Liu, Syed Ali, Jason Hill, Woj Wrona
  • Publication number: 20100305056
    Abstract: Several parasites responsible for mammalian diseases are dependent on cysteine protease for various life-cycle functions. Inhibition or decreasing function of these proteases can be useful in the treatment and/or prevention of these parasitic diseases including; toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, schistosomiasis, amebiasis, giardiasis, clonorchiasis, opisthorchiasis, paragonimiasis, fasciolopsiasis, lymphatic filariasis, onchocerciasis, dracunculiasis, ascariasis, trichuriasis, strongyloidiasis, trichostrongyliasis, trichomoniasis or cestodiasis.
    Type: Application
    Filed: November 26, 2008
    Publication date: December 2, 2010
    Applicant: Merck Frosst Canada Ltd.
    Inventors: Elise Isabel, Christophe Mellon, Christian Beaulieu
  • Publication number: 20100240644
    Abstract: The present invention provides a morpholine derivative of the formula [I]; wherein R1 is a substituted alkyl group, an optionally substituted aryl group, an optionally substituted heterocyclo group, a cycloalkyl group or an alkyl group; R2 is a substituted alkyl group, an optionally substituted aryl group, an optionally substituted heterocyclo group, an optionally substituted alkylcarbonyl group, an optionally substituted arylcarbonyl group, an optionally substituted heterocyclo-substituted carbonyl group or a cycloalkylcarbonyl group; T is a methylene group or a carbonyl group; R3, R4, R5 and R6 are the same or different and a hydrogen atom, an optionally substituted carbamoyl group or an optionally substituted alkyl group; or pharmaceutically acceptable salts thereof. These compounds are useful as a renin inhibitor.
    Type: Application
    Filed: June 16, 2008
    Publication date: September 23, 2010
    Inventors: Hidenori Akatsuka, Hiroshi Sugama, Nobumasa Awai, Takayuki Kawaguchi, Yoichi Takahashi, Toru Iijima, Jingkang Shen, Guangxin Xia, Jianshu Xie
  • Patent number: 7745629
    Abstract: The present invention relates to bicyclic compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: May 12, 2006
    Date of Patent: June 29, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Andreas Termin, Nicole Zimmermann, Tara Leanne Knoll, Gabriel Martinez-Botella, Esther Martinborough
  • Patent number: 7662849
    Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
    Type: Grant
    Filed: June 4, 2004
    Date of Patent: February 16, 2010
    Assignee: ViroBay, Inc.
    Inventors: John W. Patterson, Soon H. Woo
  • Publication number: 20100010216
    Abstract: The invention provides a 2-fluorinated acyl-3-aminoacrylonitrile derivative, and a method for producing the same. A desired 2-fluorinated acyl-3-aminoacrylonitrile derivative represented by the following Formula (3) is obtained by reacting a fluorinated acyl derivative with an aminoacrylonitrile derivative. In Formula (3), Rf represents an alkyl group having 1 to 6 carbon atoms which is substituted with at least one fluorine atom, R1 and R2 each independently represent a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or the like, and R3 represents an alkyl group having 1 to 6 carbon atoms or the like.
    Type: Application
    Filed: December 18, 2007
    Publication date: January 14, 2010
    Applicant: Mitsui Chemicals Agro, INC
    Inventors: Hideki Umetani, Yoji Aoki, Takeshi Kakimoto
  • Patent number: 7632835
    Abstract: The present invention relates to morpholine and thiomorpholine derivatives or the general formula I or pharmaceutically acceptable salts thereof and their use.
    Type: Grant
    Filed: January 28, 2009
    Date of Patent: December 15, 2009
    Assignee: H. Lundbeck A/S
    Inventors: Christian Wenzel Tornoe, Mario Rottlander, Nikolay Khanzhin, Andreas Ritzen, William Patrick Watson
  • Publication number: 20090253907
    Abstract: A phosphine compound represented by general formula (1) wherein R? and R? independently are selected from alkyl, cycloalkyl and 2-furyl radicals, or R? and R? are joined together to form with the phosphorous atom a carbon-phosphorous monocycle including at least 3 carbon atoms or a carbon-phosphorous bicycle; the alkyl radicals, cycloalkyl radicals, and carbon-phosphorous monocycle being unsubstituted or substituted by at least one radical selected from the group of alkyl, cycloalkyl, aryl, alkoxy, and aryloxy radicals; Cps is a partially substituted or completely substituted cyclopentadien-1-yl group, including substitutions resulting in a fused ring system, and wherein a substitution at the 1-position of the cyclopentadien-1-yl group is mandatory when the cyclopentadien-1-yl group is not part of a fused ring system or is part of an indenyl group. These phosphines can be used as ligands in catalytic reactions.
    Type: Application
    Filed: August 14, 2007
    Publication date: October 8, 2009
    Inventors: Herbert Plenio, Christoph Fleckenstein, Renat Kadyrov, Juan Almena, Axel Monsees, Thomas Riermeier
  • Publication number: 20090082328
    Abstract: This invention relates to novel substituted phenylamino-benzene compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 9, 2008
    Publication date: March 26, 2009
    Inventors: Yingfu Li, Joachim Rudolph, Jacques P. Dumas, Daniel Auclair, Mario Lobell, Marion Hitchcock, Ingo Hartung, Marcus Koppitz, Dominic Brittain, Florian Puehler, Kirstin Petersen, Judith Guenther
  • Patent number: 7501414
    Abstract: The present invention relates to morpholine and thiomorpholine derivatives of the general formula I or pharmaceutically acceptable salts thereof and their use.
    Type: Grant
    Filed: December 21, 2005
    Date of Patent: March 10, 2009
    Assignee: H. Lundbeck A/S
    Inventors: Christian Wenzel Tornøe, Mario Rottländer, Nikolay Khanzhin, Andreas Ritzèn, William Patrick Watson
  • Patent number: 7482448
    Abstract: Novel inhibitors of cathepsin S, K, B, and L, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
    Type: Grant
    Filed: April 24, 2006
    Date of Patent: January 27, 2009
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Sukanthini Thurairatnam, David John Aldous, Vincent Leroy, Andreas Paul Timm
  • Patent number: 7452891
    Abstract: The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
    Type: Grant
    Filed: January 28, 2005
    Date of Patent: November 18, 2008
    Assignee: Schering Corporation
    Inventors: John W. Clader, Hubert B. Josien, Anandan Palani, Tin Yau Chan
  • Patent number: 7439356
    Abstract: The present invention relates to intermediates of the formula useful in the preparation of piperazinyl-substituted indan derivatives, wherein Y is CONR2 wherein R2 is H or C1-C6 alkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted with R4 and/or R5, wherein R4 and R5 are as defined in the specification; and R9 is H, C1-C6 alkyl, C3-C6 cycloalkyl, OCF3, OCHF2, OCH2F, halogen, CN, CF3, OH, C1-C6 alkoxy, C1-C6 alkoxy-C1-C6 alkyl, NR6R7, SO3CH3, SO3CF3, SO2NR6R7, an unsubstituted or substituted heterocyclic or heteroaromatic ring containing one or two heteroatoms selected from N and O, wherein the substituent(s) is(are) C1-C6 alkyl; or COR8; wherein R6, R7 and R8 are as defined in the specification. The invention further relates to a process for the preparation of the intermediates.
    Type: Grant
    Filed: October 3, 2006
    Date of Patent: October 21, 2008
    Assignee: AstraZeneca AB
    Inventors: Stefan Berg, Lennart Florvall, Svante Ross, Seth-Olov Thorberg
  • Patent number: 7300934
    Abstract: Compounds of the formula (I) wherein m, n, A, R1, R2, R3, R4, R5 and R6 are as described herein, together with methods for making the compounds and using the compounds for treatment of diseases or conditions mediated by Cathepsin K.
    Type: Grant
    Filed: June 1, 2004
    Date of Patent: November 27, 2007
    Assignee: Roche Palo Alto LLC
    Inventors: Tobias Gabriel, Nancy Elisabeth Krauss
  • Patent number: 6982263
    Abstract: Disclosed are novel nitrile compounds of formula (I) further defined herein, which compounds are useful as reversible inhibitors of cysteine proteases such as cathepsin K, S, F, L and B. These compounds are useful for treating diseases and pathological conditions exacerbated by these proteases such as, but not limited to, osteoporosis, rheumatoid arthritis, multiple sclerosis, asthma and other autoimmune diseases, Alzheimer's disease, atherosclerosis. Also disclosed are processes for making such novel compounds.
    Type: Grant
    Filed: June 4, 2002
    Date of Patent: January 3, 2006
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Eugene R. Hickey, Younes Bekkali, Usha R. Patel, Denice Mary Spero, David S. Thomson, Erick Richard Roush Young
  • Patent number: 6927218
    Abstract: Compounds, compositions and methods treating arthritic disorders such as osteoarthritis or rheumatoid arthritis, and for treating other diseases associated with altered mitochondrial function, such as cancer, psoriasis, stroke, Alzheimer's Disease and diabetes. The compounds of this invention have the following structure (I): including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein R1-5 are as defined herein. The methods of this invention are directed to administering to a warm-blooded animal in need thereof an effective amount of a compound of structure (I), typically in the form of a pharmaceutical composition.
    Type: Grant
    Filed: March 11, 2003
    Date of Patent: August 9, 2005
    Assignee: Migenix Corp.
    Inventors: Soumitra S. Ghosh, Tomas R. Szabo
  • Patent number: 6903092
    Abstract: Compounds having the general formula wherein R1, R2, R3, R4, R5, X1 and X2 are as defined in the specification, methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.
    Type: Grant
    Filed: April 5, 2001
    Date of Patent: June 7, 2005
    Inventor: Peter Bernstein
  • Patent number: 6878706
    Abstract: Compounds according to the following formula (I): wherein the variables Q and R1 to R6 are as described herein, which reversibly inhibit the cysteine proteases, such as cathepsins K, S, F, L and B; pharmaceutical compositions containing such compounds, and method of treating diseases and pathological conditions exacerbated by these cysteine proteases such as, but not limited to rheumatoid arthritis, multiple sclerosis and other autoimmune diseases, osteoporosis, asthma, Alzheimer's disease, atherosclerosis and endometriosis.
    Type: Grant
    Filed: March 27, 2003
    Date of Patent: April 12, 2005
    Assignee: Boehringer Ingelheim Pharmaceuticals Inc.
    Inventors: Thomas A. Gilmore, Eugene Richard Hickey, Weimin Liu, Peter Allen Nemoto, Denice M. Spero
  • Patent number: 6821973
    Abstract: A compound having the general formula R1R2N—CH2CH2—CHAr1—CH2—NR3—CO—R4  (I) and methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.
    Type: Grant
    Filed: June 30, 2003
    Date of Patent: November 23, 2004
    Assignee: Astrazeneca AB
    Inventor: Peter Robert Bernstein
  • Publication number: 20040209845
    Abstract: Novel styrylacrylonitrile compounds which are useful in treating a variety of cell proliferative disorders such as cancer are disclosed.
    Type: Application
    Filed: March 17, 2004
    Publication date: October 21, 2004
    Applicant: HSC Research and Development Limited Partnership
    Inventors: Chaim M. Roifman, Thomas Grunberger, Olga Rounova, Demin Peter, Nigel Sharfe
  • Publication number: 20040171829
    Abstract: The present invention relates to processes for the production of &agr;-aryl-&bgr;-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) receptor antagonists.
    Type: Application
    Filed: February 25, 2004
    Publication date: September 2, 2004
    Applicant: Bristol-Myers Squibb Pharma Company
    Inventors: Jiacheng Zhou, Lynette May Oh, Philip Ma
  • Patent number: 6747026
    Abstract: Compounds of the invention are amine oxide prodrugs showing activity on the NK1 receptor.
    Type: Grant
    Filed: January 7, 2003
    Date of Patent: June 8, 2004
    Assignee: Hoffman-La Roche Inc.
    Inventors: Torsten Hoffmann, Sonia Maria Poli, Patrick Schnider, Andrew Sleight
  • Publication number: 20040092497
    Abstract: The present invention relates to a class of compounds represented by formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of Formula (I), and methods of selectively antagonizing the &agr;&ngr;&bgr;3 and/or the &agr;&ngr;&bgr;5 integrin without significantly antagonizing the IIb/IIIa integrin.
    Type: Application
    Filed: September 5, 2003
    Publication date: May 13, 2004
    Inventors: Srinivasan Raj Nagarajan, Ish Kumar Khanna, Michael B. Tollefson, Scott B, Mohler, Barbara B. Chen, Mark Russell, Balekudru Devadas, Thomas D. Penning, Lori A. Schretzman, Dale P. Spangler, Mark L. Boys, Nizal S. Chandrakumar, Hwang-Fun Lu
  • Publication number: 20040087583
    Abstract: This invention relates generally to amino-thio-acrylonitriles of formula Ia or Ib: 1
    Type: Application
    Filed: October 30, 2003
    Publication date: May 6, 2004
    Inventor: Frank Worden Hobbs
  • Publication number: 20040072803
    Abstract: Novel styrylacrylonitrile compounds which are useful in treating a variety of cell proliferative disorders such as cancer are disclosed. The compounds are of Formula (1).
    Type: Application
    Filed: October 27, 2003
    Publication date: April 15, 2004
    Inventors: Chaim M. Roifman, Thomas Grunberger, Olga Rounova, Demin Peter, Nigel Sharfe
  • Patent number: 6720319
    Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R2, R3, R4, R5, R6, R7, R8, Het and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.
    Type: Grant
    Filed: October 1, 2002
    Date of Patent: April 13, 2004
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Weimin Liu, Denice M. Spero, David S. Thomson, Yancey D. Ward, Erick R. R. Young
  • Patent number: 6689882
    Abstract: A new improved process for synthesizing morpholinylbenzenes of the formula I by reacting morpholine of formula II with a substituted benzene of formula III, wherein morpholine is used as a reactant and as the only one solvent.
    Type: Grant
    Filed: November 12, 2002
    Date of Patent: February 10, 2004
    Assignee: AstraZeneca AB
    Inventor: Wei Tian
  • Patent number: 6680317
    Abstract: This invention relates to novel compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
    Type: Grant
    Filed: September 17, 2002
    Date of Patent: January 20, 2004
    Assignee: SmithKline Beecham Corporation
    Inventors: Michael R. Palovich, Katherine L. Widdowson, Hong Nie
  • Publication number: 20030208068
    Abstract: The present invention relates to processes for the production of &agr;-aryl-&bgr;-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) receptor antagonists.
    Type: Application
    Filed: March 13, 2003
    Publication date: November 6, 2003
    Inventors: Jiacheng Zhou, Lynette May Oh, Philip Ma
  • Patent number: 6593472
    Abstract: Compounds of the invention are amine oxide prodrugs showing activity on the NK1 receptor.
    Type: Grant
    Filed: July 12, 2001
    Date of Patent: July 15, 2003
    Assignee: Hoffman-La Roche Inc.
    Inventors: Torsten Hoffmann, Sonia Maria Poli, Patrick Schnider, Andrew Sleight
  • Patent number: 6593473
    Abstract: Improved process for the preparation of granular N-alkylammoniumacetonitrile salts I R2R3N+R1—CR4R5—CN Y−  (I) where R1 to R5 are hydrogen or organic radicals, and Y− is a sulfate or hydrogensulfate anion, from an aqueous solution of the compound II R2R3N+R1—CR4R5—CN R6O—SO2—O−  (II) where R6 is C1- to C4-alkyl, which comprises evaporating this aqueous solution at a temperature of from 80° C. to 250° C. and a pressure of from 10 mbar to 2 bar to give a melt, then allowing the melt to solidify, where, during or following the evaporation, customary carrier materials and/or auxiliaries can be added, and the resulting solidified compound I is converted into the desired granular form.
    Type: Grant
    Filed: September 25, 2001
    Date of Patent: July 15, 2003
    Assignee: BASF Aktiegesellschaft
    Inventors: Michael Schönherr, Hans-Jürgen Kinder, Klaus Mundinger, Gregor Schürmann