Additional Hetero Ring Containing Patents (Class 544/96)
  • Patent number: 9758513
    Abstract: The present invention provides a compound which has an effect of inhibiting amyloid ? production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid ? proteins. A compound of the formula (I): wherein X is —C(R3a)(R3b)—, —C(R3a)(R3b)—C(R3c)(R3d)— or —C(R3a)?C(R3c)—, R1 is substituted or unsubstituted alkyl or the like, R2a, R2b, R3a, R3b, R3c and R3d are each independently hydrogen, halogen or the like, R4 is hydrogen or halogen, Ring B is substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 21, 2016
    Date of Patent: September 12, 2017
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Ken-ichi Kusakabe, Syuhei Yoshida, Kenji Nakahara, Tsuyoshi Hasegawa, Genta Tadano, Kouki Fuchino
  • Patent number: 9540359
    Abstract: The present invention provides a compound which has an effect of inhibiting amyloid ? production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid ? proteins. A compound of the formula (I): wherein X is —C(R3a)(R3b)—, —C(R3a)(R3b)—C(R3c)(R3d)— or —C(R3a)?C(R3c)—, R1 is substituted or unsubstituted alkyl or the like, R2a, R2b, R3a, R3b, R3c and R3d are each independently hydrogen, halogen or the like, R4 is hydrogen or halogen, Ring B is substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 23, 2013
    Date of Patent: January 10, 2017
    Assignee: Shionogi & Co., Ltd.
    Inventors: Ken-ichi Kusakabe, Syuhei Yoshida, Kenji Nakahara, Tsuyoshi Hasegawa, Genta Tadano, Kouki Fuchino
  • Patent number: 8999980
    Abstract: The present invention provides, for example, a compound mentioned below as a medicament for treating or preventing the diseases induced by production, secretion or deposition of amyloid-? proteins. A compound of the formula (I): wherein R1, R2a, R2b, R3, R4a, R4b, ring A and the dashed lines are defined in the specification, its pharmaceutically acceptable salt or a solvate thereof.
    Type: Grant
    Filed: December 10, 2010
    Date of Patent: April 7, 2015
    Assignee: Shionogi & Co., Ltd.
    Inventors: Moriyasu Masui, Akihiro Hori
  • Publication number: 20150094306
    Abstract: The present invention relates to pyrrolopyridinone derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
    Type: Application
    Filed: April 25, 2013
    Publication date: April 2, 2015
    Inventors: Kiyoshi Kawamura, Mikio Morita, Tatsuya Yamagishi
  • Patent number: 8987255
    Abstract: The present invention provides compounds of formula (I) having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Grant
    Filed: June 4, 2012
    Date of Patent: March 24, 2015
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Thomas Woltering
  • Publication number: 20150080363
    Abstract: The present invention relates to compounds defined by formula I: wherein the variables A1, A2, Cy1 Cy2, Cy3, E, R1a, R1b, R2, R3, n, and Q are as defined herein, 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: September 26, 2014
    Publication date: March 19, 2015
    Inventors: Matthias Eckhardt, Frank Himmelsbach, Katerina Leftheris, Suresh B. Singh, Colin M. Tice, Zhenrong Xu, Yuanjie Ye, Linghang Zhuang
  • Patent number: 8969338
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein U, V, Y, R1, R2, R2?, R3, R3? and R8 are described herein. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Grant
    Filed: September 27, 2012
    Date of Patent: March 3, 2015
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Publication number: 20150031627
    Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
    Type: Application
    Filed: July 25, 2014
    Publication date: January 29, 2015
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Rene M. Lemieux, Janeta Popovici-Muller, Jeremy Travins, Zhenwei Cai, Dawei Cui, Ding Zhou
  • Publication number: 20150031690
    Abstract: The present invention provides a compound of formula (I) having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.
    Type: Application
    Filed: January 23, 2013
    Publication date: January 29, 2015
    Applicants: F. Hoffmann-La Roche AG, Siena Biotech S.P.A
    Inventors: Hans Hilpert, Roland Humm, Thomas Woltering
  • Patent number: 8933072
    Abstract: Disclosed are compounds represented by Formula (I): or pharmaceutically acceptable salts, enantiomers or diastereomers thereof. Also disclosed are pharmaceutical compositions comprising the compounds of Formula (I) or pharmaceutically acceptable salts, enantiomers or diastereomers thereof for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. Values for the variables of Formula (I) are defined herein.
    Type: Grant
    Filed: June 15, 2011
    Date of Patent: January 13, 2015
    Assignees: Vitae Pharmaceuticals, Inc., Boehringer-Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Frank Himmelsbach, Katerina Leftheris, Suresh B. Singh, Colin M. Tice, Zhenrong Xu, Yuanjie Ye, Linghang Zhuang
  • Patent number: 8927534
    Abstract: The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; ? is a radical of formula (II), R2 is a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents.
    Type: Grant
    Filed: January 31, 2007
    Date of Patent: January 6, 2015
    Assignee: Shire Orphan Therapies GmbH
    Inventors: Gunther Zischinsky, Roland Stragies, Frank Osterkamp, Dirk Scharn, Gerd Hummel, Holger Kalkhof, Grit Zahn, Doerte Vossmeyer, Claudia Christner-Albrecht, Ulrich Reineke
  • Patent number: 8927539
    Abstract: Disclosed are compounds represented by Formula (I): or pharmaceutically acceptable salts, enantiomers or diastereomers thereof. Also disclosed are pharmaceutical compositions comprising the compounds of Formula (I) or pharmaceutically acceptable salts, enantiomers or diastereomers thereof for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. Values for the variables of Formula (I) are defined herein.
    Type: Grant
    Filed: June 10, 2010
    Date of Patent: January 6, 2015
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: David A. Claremon, Katerina Leftheris, Linghang Zhuang, Colin M. Tice, Suresh B. Singh, Yuanjie Ye
  • Patent number: 8916701
    Abstract: Disclosed is a process for making diastereomeric compound of the formula (I): wherein m, n and R1 to R4 are as defined herein. The process of the invention provides the compound of formula (I) in high yield and substantially free of the corresponding diastereomers. The compounds of formula (I) prepared by the process of the invention are useful for making pharmaceutically active compounds such as 11-?-hydroxysteroid hydrogenase type 1 (11-?-HSD1) inhibitors.
    Type: Grant
    Filed: December 15, 2011
    Date of Patent: December 23, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Daniel Robert Fandrick, Zhi-Hui Lu, Diana Reeves, Jonathan Reeves, Chris Hugh Senanayake, Jinhua Jeff Song, Yongda Zhang
  • Patent number: 8906852
    Abstract: This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions and ophthalmic diseases, disorders and conditions.
    Type: Grant
    Filed: April 8, 2011
    Date of Patent: December 9, 2014
    Assignee: MethylGene Inc.
    Inventors: Stéphane Raeppel, Franck Raeppel, Stephen William Claridge, Lijie Zhan, Frédéric Gaudette, Michael Mannion, Norifumi Sato, Yohei Yuki, Masashi Kishida, Arkadii Vaisburg
  • Patent number: 8883778
    Abstract: Disclosed are compounds represented by Formula (I): or pharmaceutically acceptable salts, enantiomers or diastereomers thereof. Also disclosed are pharmaceutical compositions comprising the compounds of Formula (I) or pharmaceutically acceptable salts, enantiomers or diastereomers thereof for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. Values for the variables of Formula (I) are defined herein.
    Type: Grant
    Filed: June 30, 2010
    Date of Patent: November 11, 2014
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: David A. Claremon, Katerina Leftheris, Suresh B. Singh, Colin M. Tice, Yuanjie Ye, Wei Zhao, Linghang Zhuang
  • Patent number: 8883779
    Abstract: The present invention provides a compound of formula (I): wherein —X? is —CR7? or —N?, ring B is a substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, R1 is substituted or unsubstituted alkyl or the like, R2 a and R2 b are each independently hydrogen, substituted or unsubstituted alkyl or the like, R3 and R4 are each independently hydrogen, halogen, substituted or unsubstituted alkyl or the like, R5 is hydrogen, substituted or unsubstituted alkyl or the like, each R6 is independently halogen, hydroxy, substituted or unsubstituted alkyl or the like, R7 is hydrogen, halogen, hydroxy, substituted or unsubstituted alkyl or the like, p is an integer of 0 to 3, or a pharmaceutically acceptable salt thereof which has an effect of inhibiting amyloid ? production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid ? proteins.
    Type: Grant
    Filed: April 25, 2012
    Date of Patent: November 11, 2014
    Assignee: Shinogi & Co., Ltd.
    Inventors: Moriyasu Masui, Yasunori Mitsuoka, Syuhei Yoshida, Ken-ichi Kusakabe, Naohiro Onodera, Noriyuki Kurose
  • Patent number: 8871738
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Grant
    Filed: October 25, 2012
    Date of Patent: October 28, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Pengcheng Patrick Shao, Wanying Sun, Revathi Reddy Katipally, Petr Vachal, Feng Ye, Jian Liu, Deyou Sha
  • Patent number: 8865707
    Abstract: Compounds of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), A1 is a cyclic group, and B is a cyclic group which is attached to the heterocyclic ring directly or through a methylene group.
    Type: Grant
    Filed: December 29, 2006
    Date of Patent: October 21, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Peter J. Sinclair, Gayle E. Taylor
  • Patent number: 8846668
    Abstract: This invention relates to novel compounds of the Formula (I), (Ia1-10), (Ib1-10), (Ic1-10), (Id1-7), (Ie1-5) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Grant
    Filed: July 23, 2009
    Date of Patent: September 30, 2014
    Assignees: Vitae Pharmaceuticals, Inc., Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Matthias Eckhardt, Bradford S. Hamilton, Annette Schuler-Metz, Linghang Zhuang
  • Publication number: 20140256700
    Abstract: The present invention is directed to carbazole compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.
    Type: Application
    Filed: February 26, 2014
    Publication date: September 11, 2014
    Inventors: Michael A. Poss, David R. Tortolani, Dharmpal S. Dodd, Christopher P. Mussari, John S. Tokarski, Ashvinikumar V. Gavai, Yufen Zhao, George V. Delucca, Daniel O'Malley, Derek J. Norris, Patrice Gill, Claude A. Quesnelle, Wen-Ching Han
  • Publication number: 20140249104
    Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, each of R1 and R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III.
    Type: Application
    Filed: February 27, 2014
    Publication date: September 4, 2014
    Inventors: Ana Elena MINATTI, Jonathan D. LOW, Jennifer R. ALLEN, Jian CHEN, Ning CHEN, Yuan CHENG, Ted JUDD, Qingyian LIU, Patricia LOPEZ, Wenyuan QIAN, Shannon RUMFELT, Robert M. RZASA, Nuria A. TAMAYO, Qiufen XUE, Bryant YANG, Wenge ZHONG
  • Publication number: 20140243325
    Abstract: The present invention provides 4-(3-Amino-phenyl)-5,6-dihydro-4H-[1,3]oxazin-2-ylamines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Application
    Filed: May 2, 2014
    Publication date: August 28, 2014
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Hans Hilpert, Wolfgang Wostl
  • Patent number: 8815851
    Abstract: A composition having BACE 1 inhibitory activity containing a compound represented by the general formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a and R4b is each independently a hydrogen atom, halogen, or hydroxy etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 0 to 3; R5 is a hydrogen atom or substituted lower alkyl; its pharmaceutically acceptable salt, or a solvate thereof.
    Type: Grant
    Filed: February 15, 2013
    Date of Patent: August 26, 2014
    Assignee: Shionogi & Co., Ltd.
    Inventors: Naotake Kobayashi, Kazuo Ueda, Naohiro Itoh, Shinji Suzuki, Gaku Sakaguchi, Akira Kato, Akira Yukimasa, Akihiro Hori, Yuji Koriyama, Hidekazu Haraguchi, Ken Yasui, Yasuhiko Kanda
  • Patent number: 8785440
    Abstract: The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.
    Type: Grant
    Filed: September 3, 2010
    Date of Patent: July 22, 2014
    Assignees: Biogen Idec MA, Inc., Sunesis Pharmaceuticals, Inc.
    Inventors: Minna Bui, Patrick Conlon, Julio H. Cuervo, Daniel A. Erlanson, Junfa Fan, Bing Guan, Brian T. Hopkins, Tracy J. Jenkins, Gnanasambandam Kumaravel, Alexey A. Lugovskoy, Doug Marcotte, Noel Powell, Daniel Scott, Laura Silvian, Art Taveras, Deping Wang, Min Zhong
  • Patent number: 8785436
    Abstract: The present invention provides compounds of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Grant
    Filed: May 9, 2012
    Date of Patent: July 22, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans Hilpert, Robert Narquizian, Emmanuel Pinard, Alessandra Polara, Mark Rogers-Evans, Thomas Woltering, Wolfgang Wostl
  • Patent number: 8754075
    Abstract: The present invention provides 4-(3-Amino-phenyl)-5,6-dihydro-4H-[1,3]oxazin-2-ylamines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Grant
    Filed: April 5, 2012
    Date of Patent: June 17, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans Hilpert, Wolfgang Wostl
  • Patent number: 8754076
    Abstract: Disclosed is a compound represented by Formula (Im1): or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof. Also disclosed are pharmaceutical compositions comprising the compound of Formula (Im1) or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof and methods of inhibiting 11?-HSD1 activity comprising the step of administering to a mammal in need of such treatment an effective amount of a compound of Formula (Im1), or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof. Values for the variables in Formula (Im1) are defined herein.
    Type: Grant
    Filed: October 5, 2012
    Date of Patent: June 17, 2014
    Assignees: Vitae Pharmaceuticals, Inc./Boehringer-Ingelheim, Boehringer-Ingelheim International GmbH
    Inventors: David A. Claremon, Frank Himmelsbach, Katerina Leftheris, Suresh B. Singh, Colin M. Tice, Zhenrong Xu, Yuanjie Ye, Linghang Zhuang
  • Publication number: 20140135493
    Abstract: Disclosed is a process for making diastereomeric compound of the formula (I): wherein m, n and R1 to R4 are as defined herein. The process of the invention provides the compound of formula (I) in high yield and substantially free of the corresponding diastereomers. The compounds of formula (I) prepared by the process of the invention are useful for making pharmaceutically active compounds such as 11-?-hydroxysteroid hydrogenase type 1 (11-?-HSD1) inhibitors.
    Type: Application
    Filed: December 15, 2011
    Publication date: May 15, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Daniel Robert Fandrick, Zhi-Hui Lu, Diana Crimhilda Reeves, Jonathan Timothy Reeves, Chris Hugh Senanayake, Jinhua J. Song, Yongda Zhang
  • Publication number: 20140112867
    Abstract: The present invention provides compounds of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes. The invention further provides a radio-labelled derivative thereof.
    Type: Application
    Filed: June 4, 2012
    Publication date: April 24, 2014
    Inventors: Edilio Borroni, Luca Gobbi, Hans Hilpert, Michael Honer, Dieter Muri, Robert Narquizian, Alessandra Polara
  • Patent number: 8703765
    Abstract: This invention relates to novel compounds of the Formula (I), dependent compounds of Formula (II), (II-A), (II-B), (II-C), (II-D), (II-E), (II-F), (II-G), (II-H), (III), (III-A), (III-B), (III-C), (IV), (IV-A), (IV-B), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Grant
    Filed: June 1, 2010
    Date of Patent: April 22, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventor: Frank Himmelsbach
  • Patent number: 8680093
    Abstract: This invention relates to novel compounds of the Formula Ik, Im1, Im2, Im5, In1, In2, In5, lo1, lo2, lo5, Ip1, Ip3, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 ?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.
    Type: Grant
    Filed: April 30, 2010
    Date of Patent: March 25, 2014
    Assignees: Vitae Pharmaceuticals, Inc., Boehringer Ingelheim International GmbH
    Inventors: Martin Renz, Martin Schuehle, Zhenrong Xu
  • Publication number: 20140080819
    Abstract: The present invention provides compounds of formula (I) having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Application
    Filed: June 4, 2012
    Publication date: March 20, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Thomas Woltering
  • Patent number: 8673899
    Abstract: This invention relates to novel compounds of the Formula Ik, Im1, Im2, Im5, In1, In2, In5, Io1, Io2, Io5, Ip1, Ip3, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Grant
    Filed: January 11, 2012
    Date of Patent: March 18, 2014
    Assignees: Vitae Pharmaceuticals, Inc., Boehringer Ingelheim International GmbH
    Inventors: David A. Claremon, Linghang Zhuang, Katerina Leftheris, Colin M. Tice, Zhenrong Xu, Yuanjie Ye, Suresh B. Singh, Salvacion Cacatian, Wei Zhao
  • Publication number: 20140065095
    Abstract: The invention relates to novel pyrrolidine derivatives of formula (I): wherein R1, R2 and R3 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
    Type: Application
    Filed: June 5, 2013
    Publication date: March 6, 2014
    Inventors: Ulrich Heiser, Daniel Ramsbeck, Robert Sommer, Antje Meyer, Torsten Hoffmann, Livia Boehme, Hans-Ulrich Demuth
  • Publication number: 20140051691
    Abstract: The present invention provides a compound of formula (I): wherein —X? is —CR7? or —N?, ring B is a substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, R1 is substituted or unsubstituted alkyl or the like, R2 a and R2 b are each independently hydrogen, substituted or unsubstituted alkyl or the like, R3 and R4 are each independently hydrogen, halogen, substituted or unsubstituted alkyl or the like, R5 is hydrogen, substituted or unsubstituted alkyl or the like, each R6 is independently halogen, hydroxy, substituted or unsubstituted alkyl or the like, R7 is hydrogen, halogen, hydroxy, substituted or unsubstituted alkyl or the like, p is an integer of 0 to 3, or a pharmaceutically acceptable salt thereof which has an effect of inhibiting amyloid ? production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid ? proteins.
    Type: Application
    Filed: April 25, 2012
    Publication date: February 20, 2014
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Moriyasu Masui, Yasunori Mitsuoka, Syuhei Yoshida, Ken-ichi Kusakabe, Naohiro Onodera, Noriyuki Kurose
  • Patent number: 8653260
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Grant
    Filed: June 20, 2012
    Date of Patent: February 18, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Ding-Ming Shen, Liping Wang, Cheng Zhu
  • Patent number: 8637505
    Abstract: This invention relates to novel compounds of the Formula Formulas (I), (Ia1-20), (Ib1-20), (Ic1-20), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Grant
    Filed: February 3, 2010
    Date of Patent: January 28, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Frank Himmelsbach
  • Patent number: 8629138
    Abstract: Disclosed is a compound represented by Formula (Im1): or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof. Also disclosed are pharmaceutical compositions comprising the compound of Formula (Im1) or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof and methods of inhibiting 11?-HSD1 activity comprising the step of administering to a mammal in need of such treatment an effective amount of a compound of Formula (Im1), or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof. Values for the variables in Formula (Im1) are defined herein.
    Type: Grant
    Filed: October 5, 2012
    Date of Patent: January 14, 2014
    Assignee: Boehringer-Ingelheim International GmbH
    Inventor: Frank Himmelsbach
  • Patent number: 8618287
    Abstract: The present invention relates to derivatives of general formula I wherein: —W represents nitrogen, —R1 represents: •a hydrogen or a linear or branched C1-C5 alkyl radical or, •a C1-C3 alkyl radical substituted with groups such as trifluoromethyl, nitrile, hydroxy, C1-C3 alcoxy, C3-C6 alkoxyalkoxy, indolyl, thiophenyl, oxothiophenyl, C1-C3 N-alkylcarbamoyl groups or, •a phenyl or pyridyl or naphthyl, or thiophenyl group optionally substituted with one or more groups such as halogen atoms, nitro, nitrile, trifluoromethyl, vinyl, methylsulfanyl, linear branched C1-C4 alkyl, linear or branched C1-C3 alkoxy groups, •a C6 2-oxocycloalkyl radical—R2 represents a methyl or heptyl, -m, n are equal to 1, —V represents CH2, —X—Y represents —N— (C?O)—, —CH—O—, —Z represents a phenyl group substituted with one or more trifluoromethyl groups, halogen atoms or linear C1-C4 alkyl groups.
    Type: Grant
    Filed: July 7, 2009
    Date of Patent: December 31, 2013
    Assignee: Pierre Fabre Medicament
    Inventors: Isabelle Leroy, Elisabeth Dupont-Passelaigue, Karine Valeille, Yves Rival, Didier Junquero
  • Patent number: 8598163
    Abstract: This invention relates to novel compounds of an 11 ?-HSD1 inhibitor disclosed herein, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11/3-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.
    Type: Grant
    Filed: February 3, 2010
    Date of Patent: December 3, 2013
    Assignees: Vitae Pharmaceuticals, Inc., Boehringer Ingelheim International GmbH
    Inventors: David Claremon, Colin Tice, Suresh Singh, Yuanjie Ye, Katerina Leftheris, Linghang Zhuang
  • Publication number: 20130316999
    Abstract: The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.
    Type: Application
    Filed: August 7, 2013
    Publication date: November 28, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Alexander STRAUB, Thomas LAMPE, Jens POHLMANN, Susanne RÔHRIG, Elisabeth PERZBORN, Karl-Heinz SCHLEMMER, Joseph PERNERSTOFER
  • Patent number: 8592409
    Abstract: This invention relates to novel compounds of the Formula (I), (Ia), (Ic), (Ie), (If), (Ig), (Ih), (Ii), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Grant
    Filed: January 21, 2009
    Date of Patent: November 26, 2013
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: David A. Claremon, Linghang Zhuang, Yuanjie Ye, Suresh B. Singh, Colin M. Tice, Salvacion Cacatian
  • Patent number: 8592410
    Abstract: This invention relates to novel compounds of the Formula Il Ik, Im3, Im4, Im6-12, In3, In4, In6-12, lo3, lo4, lo6-12, Ip2, Ip4-7, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.
    Type: Grant
    Filed: April 30, 2009
    Date of Patent: November 26, 2013
    Assignees: Vitae Pharmaceuticals, Inc., Boehringer Ingelheim International GmbH
    Inventors: David A. Claremon, Linghang Zhuang, Katerina Leftheris, Colin M. Tice, Yuanjie Ye, Suresh B. Singh, Frank Himmelsbach
  • Patent number: 8575157
    Abstract: This invention relates to novel compounds of the Formula Ik, Im1, Im2, Im5, In1, In2, In5, lo1, lo2, lo5, Ip1, Ip3, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 ?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.
    Type: Grant
    Filed: April 30, 2010
    Date of Patent: November 5, 2013
    Assignees: Vitae Pharmaceuticals, Inc., Boehringer Ingelheim International, GmbH
    Inventors: Martin Renz, Martin Schuehle, Zhenrong Xu
  • Patent number: 8575156
    Abstract: Disclosed are compounds represented by Formula (I): or pharmaceutically acceptable salts, enantiomers or diastereomers thereof. Also disclosed are pharmaceutical compositions comprising the compounds of Formula (I) or pharmaceutically acceptable salts, enantiomers or diastereomers thereof and methods of inhibiting 11?-HSD1 activity comprising the step of administering to a mammal in need of such treatment an effective amount of a compound of Formula (I), or a pharmaceutically acceptable salt, enantiomer or diastereomer thereof. Values for the variables in Formula (I) are defined herein.
    Type: Grant
    Filed: July 25, 2008
    Date of Patent: November 5, 2013
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: David A. Claremon, Wei He, Gerard McGeehan, Suresh B. Singh, Colin M. Tice, Zhenrong Xu, Yuanjie Ye, Wei Zhao, Linghang Zhuang, Salvacion Cacatian, Katerina Leftheris
  • Patent number: 8569292
    Abstract: This invention relates to novel compounds of the Formula I, Ik, Iq1-21, Ir1-21, Is1-21, It1-7, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 ?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Grant
    Filed: April 30, 2009
    Date of Patent: October 29, 2013
    Assignees: Vitae Pharmaceuticals, Inc., Boehringer Ingelheim International GmbH
    Inventors: David A. Claremon, Linghang Zhuang, Katerina Leftheris, Colin M. Tice, Zhenrong Xu, Yuanjie Ye, Suresh B. Singh, Salvacion Cacatian, Frank Himmelsbach, Matthias Eckhardt, Wei Zhao
  • Publication number: 20130274464
    Abstract: The present invention relates to ethynyl compounds of formula I wherein R1, R2, R2?, R3, R3?, R4, R4?, U, V, W, Y, m, and n are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. Compounds of formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Application
    Filed: June 10, 2013
    Publication date: October 17, 2013
    Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Publication number: 20130244993
    Abstract: The present invention relates to compounds defined by formula I: wherein the variables A1, A2, Cy1 Cy2, Cy3, E, R1a, R1b, R2, R3, n, and Q are as defined herein, 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: June 15, 2011
    Publication date: September 19, 2013
    Applicants: BOEHRINGER INGELHEIM INTERNATIONAL GMBH, VITAE PHARMACEUTICALS, INC.
    Inventors: Katerina Leftheris, Linghang Zhuang, Colin M. Tice, Suresh B. Singh, Yuanjie Ye, Zhenrong Xu
  • Publication number: 20130225530
    Abstract: The present invention relates to a pharmaceutical composition for use as a medicament for the treatment or prophylaxis of cardiac hypertrophy, comprising at least one compound of formula (I), wherein: R1 is e.g. hydrogen, —CH3, R2 is e.g. hydrogen, —CH3, R4 is hydrogen, —OH, —NH2; R5 is hydrogen, —OH; R6 is hydrogen, —OH; R3 is e.g. —OCH3 or a pharmaceutically acceptable salt, and at least one pharmaceutical excipient.
    Type: Application
    Filed: July 6, 2011
    Publication date: August 29, 2013
    Applicant: DKFZ DEUTSCHES KREBSFORSCHUNGSZENTRUM
    Inventors: Min Li-Weber, H. Peter Krammer, Gernot Polier
  • Publication number: 20130203985
    Abstract: The present invention relates to a compound of formula (I) wherein R1, R2 and n are as defined herein. The invention also relates to processes for making the compounds of formula (I) and methods of using the compounds of formula (I) as reagents in organic synthesis.
    Type: Application
    Filed: May 23, 2011
    Publication date: August 8, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Zhulin Tan