Five-membered Hetero Ring Consisting Of One Nitrogen And Four Carbons Patents (Class 544/372)
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Patent number: 8236792Abstract: Certain substituted pyrrolidine amide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.Type: GrantFiled: May 19, 2009Date of Patent: August 7, 2012Assignee: Janssen Pharmaceutica NVInventors: Nicholas I Carruthers, Michael A. Letavic, Kiev S. Ly, Neelakandha S. Mani, Daniel J. Pippel, Chandravadan R. Shah, Akinola Soyode-Johnson, Emily M. Stocking, Lana Young
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Publication number: 20120189539Abstract: Inhibitors of Bcl-2/Bcl-xL and compositions containing the same are disclosed. Methods of using the Bcl-2/Bcl-xL inhibitors in the treatment of diseases and conditions wherein inhibition of Bcl-2/Bcl-xL provides a benefit, like cancers, also are disclosed.Type: ApplicationFiled: January 24, 2012Publication date: July 26, 2012Applicant: THE REGENTS OF UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Haibin Zhou, Jianfang Chen, Angelo Aguilar, Jennifer L. Meagher, Duxin Sun, Chao-Yie Yang, Liu Liu, Longchuan Bai, Donna McEachem, Jeanne Stuckey, Xiaoqin Li
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Publication number: 20120190689Abstract: The present invention relates to compounds of chemical formula 1 and having CCR2 (chemokine receptor 2) antagonistic effects, and salts or isomers thereof. These compounds are very useful for treating, preventing, or relieving rheumatoid arthritis, arteriosclerosis, multiple sclerosis, asthma, and various diseases related to CCR2. wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 is the same as defined in the specification.Type: ApplicationFiled: June 11, 2010Publication date: July 26, 2012Applicant: YANG JI CHEMICAL CO., LTD.Inventors: Jee Woong Lim, Jong-Hoon Kim, Min-Ho Oak, Yongho Na, Youna Oh, So-Hee Kang, Jung-Ok Lee, Jung-Duk Sohn, Seung-Woo Lee
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Patent number: 8222290Abstract: The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine ureas of formula (I). Wherein R, R1, R2, R3, R4 and R5 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-phenyl-bipyrrolidine ureas and intermediates therefor.Type: GrantFiled: March 15, 2010Date of Patent: July 17, 2012Assignee: SanofiInventors: Werngard Czechtizky, Zhongli Gao, William Joseph Hurst, Lothar Schwink, Siegfried Stengelin
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Patent number: 8183243Abstract: The present invention relates to a compound having a good agonistic activity to melanocortin receptor, or pharmaceutically acceptable salt or isomer thereof, and an agonistic composition for melanocortin receptor comprising the same as an active ingredient.Type: GrantFiled: June 13, 2011Date of Patent: May 22, 2012Assignee: LG Life Sciences Ltd.Inventors: Koo Lee, Sang Dae Lee, Sang Pil Moon, In Ae Ahn, Sung Pil Choi, Hyun Ho Lee, Dong Sup Shim, Soo Yong Chung, Hyun Min Lee
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Patent number: 8183239Abstract: The invention provides novel non-peptidic NPY Y2 receptor inhibitors useful in treating or preventing: anxiolytic disorders or depression; injured mammalian nerve tissue; conditions responsive to treatment through administration of a neurotrophic factor; neurological disorders; bone loss; substance related disorders; sleep/wake disorders; cardiovascular disease; obesity; or an obesity-related disorder. Compounds of the invention are also useful in modulating endocrine functions, particularly endocrine functions controlled by the pituitary and hypothalamic glands, and are therefore useful in the treatment or prevention of inovulation and infertility.Type: GrantFiled: October 27, 2006Date of Patent: May 22, 2012Assignee: Janssen Pharmaceutica NVInventors: Pascal Bonaventure, Nicholas I. Carruthers, Wenying Chai, Curt A. Dvorak, Jill A. Jablonowski, Dale A. Rudolph, Mark Seierstad, Chandravadan R. Shah, Devin M. Swanson, Victoria D. Wong
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Publication number: 20120122868Abstract: Derivatives of 2,5-piperazinedione of formula (I) are apoptotic peptidase activating factor 1 (Apaf-1) inhibitors, therefore they are useful as active pharmaceutical ingredients for the prophylaxis and/or treatment of a pathological and/or physiological condition associated with an increase of apoptosis.Type: ApplicationFiled: July 29, 2010Publication date: May 17, 2012Applicant: LABORATORIOS SALVAT, S.A.Inventors: Ángel Messeguer Pyepoch, Alejandra Moure Fernández, Daniel Gonzáles Pinacho, Isabel Masip Masip, Enrique Pérez Payá, Natividad García, Ester Monlleó Mas, Juanlo Catena Ruiz
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Publication number: 20120122839Abstract: The present invention provides compounds of formula (I) or (Ia) which are ligands binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility in cancer therapy and prevention. Compounds of formula (I) or (Ia) can be used as therapeutics for treating stroke, myocardial infarction, ischemia, multi-organ failure, spinal cord injury, Alzheimer's Disease, injury from ischemic events and heart valvular degenerative disease. Moreover, compounds of formula (I) or (Ia) can be used to decrease the side effects from cytotoxic cancer agents, radiation and to treat viral infections.Type: ApplicationFiled: January 17, 2012Publication date: May 17, 2012Applicant: Priaxon AGInventors: Christoph BURDACK, Cedric Kalinski, Vladimir Khazak, Gunther Ross, Lutz Weber
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Patent number: 8178528Abstract: 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: GrantFiled: March 28, 2006Date of Patent: May 15, 2012Assignee: Eli Lilly and CompanyInventors: Philip Arthur Hipskind, Takako Takakuwa, Cynthia Darshini Jesudason, Robert Alan Gadski, William Joseph Hornback, Richard Todd Pickard, Lisa Selsam Beavers
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Patent number: 8168788Abstract: The present invention relates to compounds useful as Chemokine Receptor antagonists. Compounds of general formula I are provided: or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions for the inhibition of Chemokine Receptors and also for the treatment of various diseases, conditions, or disorders, including acute or chronic inflammatory disease, cancer or osteolytic bone disorders.Type: GrantFiled: December 17, 2010Date of Patent: May 1, 2012Assignee: Millennium Pharmaceuticals, Inc.Inventors: Kenneth G. Carson, Shomir Ghosh, Prakash Raman, Francois Soucy, Qing Ye
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Patent number: 8163793Abstract: The invention relates to a compound of formula (I) wherein A, R1-R6 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: GrantFiled: April 16, 2010Date of Patent: April 24, 2012Assignee: Hoffman-La Roche Inc.Inventors: Rubén Alvarez Sánchez, David Banner, Simona M. Ceccarelli, Uwe Grether, Wolfgang Haap, Peter Hartman, Guido Hartmann, Hans Hilpert, Holger Kuehne, Harald Mauser, Jean-Marc Plancher
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Publication number: 20120083488Abstract: A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).Type: ApplicationFiled: June 9, 2010Publication date: April 5, 2012Inventors: Kazutomo Kinoshita, Kohsuke Asoh, Noriyuki Furuichi, Toshiya Ito, Hatsuo Kawada, Nobuya Ishii, Hiroshi Sakamoto, WooSang Hong, MinJeong Park, Yoshiyuki Ono, Yashuharu Kato, Kenji Morikami, Takashi Emura, Nobuhiro Oikawa
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Publication number: 20120065193Abstract: Disclosed herein is at least one cyclopropyl amide derivative, at least one pharmaceutical composition comprising at least one cyclopropyl amide derivative disclosed herein, and at least one method of using at least one cyclopropyl amide derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith.Type: ApplicationFiled: November 21, 2011Publication date: March 15, 2012Inventors: James Arnold, Andrew Todd Brugel, Scott Throner, Steven Wesolowski, Phil Edwards, Andrew Griffin, Thierry Groblewski, Denis Labrecque
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Publication number: 20120058996Abstract: Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are useful as kinase modulators, including Btk modulation.Type: ApplicationFiled: November 9, 2011Publication date: March 8, 2012Inventors: Qingjie Liu, Douglas G. Batt, George V. DeLucca, Qing Shi, Andrew J. Tebben
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Publication number: 20120058939Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: July 1, 2010Publication date: March 8, 2012Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Peter R. GUZZO, Matthew David SURMAN, Alan John HENDERSON, Mark HADDEN, Emily Elizabeth FREEMAN
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Publication number: 20120040933Abstract: piperazine compounds for use as pharmaceutically active compounds and in pharmaceutical formulations that are useful for the treatment of disorders associated with apoptosis, including neurodegenerative disorders, diseases associated with polyglutamine tracts, epilepsy, ischemia, infertility, cardiovascular disorders, renal hypoxia, hepatitis and AIDS, where the piperazine compounds are represented by formula (I) and the terms R0, R1, R2, R3, k, l, m, n, and X are defined herein:Type: ApplicationFiled: September 6, 2011Publication date: February 16, 2012Applicant: APPLIED RESEARCH SYSTEMS ARS HOLDING N.V.Inventors: Serge HALAZY, Dennis Church, Bruno Antonsson, Agnes Bombrun, Patrick Gerber, Jean-Claude Martinou
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Publication number: 20120035187Abstract: The present invention has an object to provide a novel agent for anti-neurodegenerative diseases and solves the object by providing an agent for anti-neurodegenerative diseases containing, as an effective ingredient, the compound(s) represented by the following General formula 1: wherein in General formula 1, R1 through R3 independently represent a hydrogen atom or an appropriate substituent; Z1 represents a heterocyclic ring and Z2 represents the same or different heterocyclic or aromatic ring as in Z1, wherein the heterocyclic and aromatic rings optionally have a substituent; represents an integer of 0, 1 or 2; p represents an integer of 0 or 1, with the proviso that p is 1 when o is 0 or 2, and p is 0 when o is 1; R1 and R2 do not exist when o is 0, while, when p is 0, R3 does not exist and the binding between the carbon atom to which R2 binds and Z2 is a single bond; X1? represents an appropriate counter anion and q represents an integer of 1 or 2.Type: ApplicationFiled: January 25, 2010Publication date: February 9, 2012Applicant: KABUSHIKI KAISHA HAYASHIBARA SEIBUTSU KAGAKU KENKYUJOInventors: Hitomi Ohta, Kenji Akita, Tsunetaka Ohta, Toshio Kawata, Shigeharu Fukuda
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Publication number: 20120028920Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: ApplicationFiled: October 11, 2011Publication date: February 2, 2012Inventors: Hiroshi YAMASHITA, Hideaki Kuroda, Nobuaki Ito, Shin Miyamura, Kunio Oshima, Jun Matsubara, Haruka Takahashi, Tae Fukushima, Satoshi Shimizu, Kazumi Kondo, Yohji Sakurai, Takeshi Kuroda, Shinichi Taira, Motohiro Itotani, Tatsuyoshi Tanaka
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Publication number: 20120022004Abstract: The invention provides a method of treating T-cell mediated diseases and a method of inhibiting the activation of T-cells using certain diketopiperazines. The invention also provides methods of synthesizing diketopiperazines and pharmaceutical compositions comprising certain diketopiperazines. The invention further provides methods of making improved pharmaceutical compositions of proteins and peptides by either increasing or decreasing the content of diketopiperazines in the compositions and the resultant improved pharmaceutical compositions.Type: ApplicationFiled: September 28, 2011Publication date: January 26, 2012Inventors: David Bar-Or, Raphael Bar-Or, Richard Shimonkevitz
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Publication number: 20120015957Abstract: The present invention is directed to piperidinyl and piperazinyl derivatives of formula (I) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds for the treatment and/or prevention of disorders, diseases and conditions mediated by the NPY Y2 receptor.Type: ApplicationFiled: December 17, 2008Publication date: January 19, 2012Inventors: Wenying Chai, Curt A. Dvorak, Jill A. Jablonowski, Dale A. Rudolph, Chandravadan R. Shah, Victoria D. Wong
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Patent number: 8088776Abstract: The present invention discloses novel compounds of Formula I: possessing 11 ?-HSD type 1 antagonist 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 the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11 ?-HSD type 1 activity.Type: GrantFiled: April 19, 2007Date of Patent: January 3, 2012Assignee: Eli Lilly and CompanyInventors: Thomas Daniel Aicher, Zhaogen Chen, Ronald Jay Hinklin, Gary Alan Hite, Alexei Pavlovych Krasutsky, Renhua Li, Jefferson Ray McCowan, Ashraf Saeed, Nancy June Snyder, James Lee Toth, Owen Brendan Wallace, Leonard Larry Winneroski, Jr., Yanping Xu, Jeremy Schulenburg York
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Publication number: 20110312931Abstract: The compounds of the present invention are represented by the following formula (I): wherein the substituents R1, R2, R3, R4, (R5)m, R6, A, X, and Y are as defined herein. The compounds are useful in methods of treating a disorder which is created by or is dependent upon inhibiting GlyT-1.Type: ApplicationFiled: June 2, 2011Publication date: December 22, 2011Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Christopher L. CIOFFI, Mark A. WOLF, Peter R. GUZZO, Shuang LIU, Kashinath SADALAPURE, Visweswaran PARTHASARATHY, Jun-Ho MAENG
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Publication number: 20110312996Abstract: The embodiments provide compounds of the general Formulae VI, VII, VIII, IX, X, XI, XII, XIII, XIV, and XV as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.Type: ApplicationFiled: May 16, 2011Publication date: December 22, 2011Applicant: InterMune, Inc.Inventors: Brad Buckman, John B. Nicholas, Vladimir Serebryany, Scott D. Seiwert
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Patent number: 8071787Abstract: A compound of the following formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, X, Y, and Z are as defined herein. Also disclosed is a method for inhibiting actively of fibroblast activation protein or for treating cancer or inflammation conditions with such a compound.Type: GrantFiled: February 19, 2010Date of Patent: December 6, 2011Assignee: National Health Research InstitutesInventors: Weir-Tong Jiaang, Xin Chen
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Patent number: 8071586Abstract: The invention is concerned with novel heterocyclyl compounds of formula (I) wherein A, X, Y1, Y2, Y3, R3, R4, R5, R6, R7, R8, R9, R10, m, n and p are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor and can be used as medicaments.Type: GrantFiled: July 8, 2009Date of Patent: December 6, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin, Olivier Roche
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Patent number: 8071600Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: GrantFiled: August 31, 2006Date of Patent: December 6, 2011Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hiroshi Yamashita, Hideaki Kuroda, Nobuaki Ito, Shin Miyamura, Kunio Oshima, Jun Matsubara, Haruka Takahashi, Tae Fukushima, Satoshi Shimizu, Kazumi Kondo, Yohji Sakurai, Takeshi Kuroda, Shinichi Taira, Motohiro Itotani, Tatsuyoshi Tanaka
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Publication number: 20110288104Abstract: The present invention relates to new compounds, ligands of the beta-3 adrenergic receptor, their preparation and their use in therapy or as research tools for said receptor; the invention also relates to a process for the preparation of the compounds of the invention and the use of inverse agonists of the beta-3 adrenergic receptor as medicaments.Type: ApplicationFiled: August 3, 2011Publication date: November 24, 2011Applicant: UNIVERSITA' DEGLI STUDI DI BARIInventors: Antonio Scilimati, Maria Grazia Perrone, Ernesto Santandrea
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Patent number: 8063042Abstract: The invention is concerned with novel heterocyclyl compounds of formula (I) wherein A, X, Y, R3, R4, R5, R6, R7, R8, R9, R10, m and n are as herein defined, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor and can be used as medicaments.Type: GrantFiled: July 10, 2008Date of Patent: November 22, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin
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Patent number: 8053436Abstract: The present invention is related to piperazine derivatives of carbazole of formula (I) notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such piperazine derivatives of carbazole. Said piperazine derivatives of carbazole are efficient modulators, in particular efficient inhibitors, of the Bax function and/or activation. The present invention is furthermore related to novel piperazine derivatives of carbazole as well as methods of their preparation.Type: GrantFiled: October 18, 2000Date of Patent: November 8, 2011Assignee: Merck Serono SAInventors: Serge Halazy, Dennis Church, Bruno Antonsson, Agnes Bombrun, Patrick Gerber, Jean-Claude Martinou
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Patent number: 8039474Abstract: The invention relates to novel tetrahydro-1H-carbazole derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and methods of treatment comprising administration of said compounds to patients.Type: GrantFiled: December 22, 2005Date of Patent: October 18, 2011Assignee: Actelion Pharmaceutical Ltd.Inventors: Anja Fecher, Heinz Fretz, Markus Riederer
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Patent number: 8039622Abstract: The present invention relates to a compound having a good agonistic activity to melanocortin receptor, or pharmaceutically acceptable salt or isomer thereof, and an agonistic composition for melanocortin receptor comprising the same as an active ingredient.Type: GrantFiled: November 10, 2009Date of Patent: October 18, 2011Assignee: LG Life Sciences Ltd.Inventors: Koo Lee, Sang Dae Lee, Sang Pil Moon, Dong Sup Shim, Soo Yong Chung
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Publication number: 20110245500Abstract: The present invention relates to a compound having a good agonistic activity to melanocortin receptor, or pharmaceutically acceptable salt or isomer thereof, and an agonistic composition for melanocortin receptor comprising the same as an active ingredient.Type: ApplicationFiled: June 13, 2011Publication date: October 6, 2011Inventors: Koo Lee, Sang Dae Lee, Sang Pil Moon, In Ae Ahn, Sung Pil Choi, Hyun Ho Lee, Dong Sup Shim, Soo Yong Chung, Hyun Min Lee
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Publication number: 20110237795Abstract: The present invention relates to a compound having a good agonistic activity to melanocortin receptor, or pharmaceutically acceptable salt or isomer thereof, and an agonistic composition for melanocortin receptor comprising the same as an active ingredient.Type: ApplicationFiled: June 13, 2011Publication date: September 29, 2011Inventors: Koo Lee, Sang Dae Lee, Sang Pil Moon, In Ae Ahn, Sung Pil Choi, Hyun Ho Lee, Dong Sup Shim, Soo Yong Chung, Hyun Min Lee
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Publication number: 20110237601Abstract: The present invention relates to compounds useful as Chemokine Receptor antagonists. Compounds of general formula I are provided: or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions for the inhibition of Chemokine Receptors and also for the treatment of various diseases, conditions, or disorders, including acute or chronic inflammatory disease, cancer or osteolytic bone disorders.Type: ApplicationFiled: December 17, 2010Publication date: September 29, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Kenneth G. Carson, Prakash Raman, Francois Soucy, Qing Ye, Shomir Ghosh
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Patent number: 8022064Abstract: The present invention relates to compounds of general formula (I): wherein: R1 and R2, identical or different, represent: an atom of hydrogen or halogen, CN or NO2, with R1 and R2 not representing hydrogen simultaneously, m represents: 1 or 2 n represents: 0, 1 or 2 R3 represents: phenyl substituted or not by one or more residues chosen among halogen, hydroxyl or C1-C6 alkyl; C2-C6 alkyl substituted or not by one or more residues chosen among halogen or hydroxyl; cycloalkyl; pyridine; thiophene; pyrrole substituted or not by C1-C6 alkyl; thiazole or furan; or the therapeutically-acceptable salts or solvates thereof.Type: GrantFiled: June 19, 2007Date of Patent: September 20, 2011Assignee: Pierre Fabre MedicamentInventors: Michel Perez, Marie Lamothe, Bruno Le Grand, Robert Letienne
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Patent number: 8022096Abstract: Pyrrolidine compounds described herein and methods for using them to inhibit dipeptidyl peptidase IV and treat Type II diabetes.Type: GrantFiled: February 25, 2009Date of Patent: September 20, 2011Assignee: National Health Research InstitutesInventors: Weir-Torn Jiaang, Yu-Sheng Chao, Ting-Yueh Tsai, Tsu Hsu
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Publication number: 20110224219Abstract: The present invention relates to a compound having a good agonistic activity to melanocortin receptor, or pharmaceutically acceptable salt or isomer thereof, and an agonistic composition for melanocortin receptor comprising the same as an active ingredient.Type: ApplicationFiled: November 10, 2009Publication date: September 15, 2011Applicant: LG LIFE SCIENCES LTD.Inventors: Koo Lee, Sang Dae Lee, Sang Pil Moon, In Ae Ahn, Sung Pil Choi, Hyun Ho Lee, Dong Sup Shim, Soo Yong Chung, Hyun Min Lee
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Patent number: 8017607Abstract: There are provided compounds of the formula wherein X, Y, R1, R2, R3, R3, R4, and R5 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof which are useful as anticancer agents.Type: GrantFiled: October 6, 2010Date of Patent: September 13, 2011Assignee: Hoffmann-La Roche Inc.Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Jin-Jun Liu, Tina Morgan Ross, Zhuming Zhang
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Patent number: 8008296Abstract: 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: GrantFiled: June 28, 2006Date of Patent: August 30, 2011Assignee: Eli Lilly and CompanyInventors: 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
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Patent number: 7994176Abstract: The present invention discloses novel compounds of Formula I: having 11 Beta-HSD type 1 antagonist 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 the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11 Beta-HSD type 1 activity.Type: GrantFiled: April 24, 2007Date of Patent: August 9, 2011Assignee: Eli Lilly and CompanyInventors: Renhua Li, Thomas Edward Mabry, Owen Brendan Wallace, Leonard Larry Winneroski, Jr., Yanping Xu
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Publication number: 20110182850Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.Type: ApplicationFiled: April 7, 2010Publication date: July 28, 2011Inventors: Trixi BRANDL, Prakash Raman, Pascal Rigollier, Mohindra Seepersaud, Oliver Simic
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Publication number: 20110178091Abstract: The present invention relates to novel arylpiperazine-containing pyrrole 3-carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof which is useful for preventing or treating depressive disorders. The present invention also provides a method for preparing the arylpiperazine-containing pyrrole 3-carboxamide derivatives or the pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, and a method for preventing or treating depressive disorders.Type: ApplicationFiled: September 23, 2009Publication date: July 21, 2011Applicant: GREEN CROSS CORPORATIONInventors: Jinhwa Lee, Suk Youn Kang, Eun-Jung Park, Kwang-Seop Song, Min Ju Kim, Hee Jeong Seo, Suk Ho Lee, Jeongmin Kim, Ae Nim Pae, Woo-Kyu Park
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Patent number: 7977371Abstract: Objects of the present invention are to study on the synthesis of a novel pyrrole derivative having a ureido group and an aminocarbonyl group as substituents or a salt thereof, to find a pharmacological effect of the derivative or a salt thereof, and to find a medicinal agent which has a prophylactic and/or therapeutic effect on a retinal disease or the like through oral administration. A compound represented by the general formula (1) or a salt thereof has an inhibitory activity against the production of interleukin-6 and/or an inhibitory effect on choroidal neovascularization, and is therefore useful as a prophylactic and/or therapeutic agent for a disease associated with interleukin-6, an ocular inflammatory disease and/or a retinal disease.Type: GrantFiled: February 26, 2008Date of Patent: July 12, 2011Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Kenji Kawashima, Hiroshi Enomoto, Noriko Ishizaka, Minoru Yamamoto, Kazuhiro Kudou, Masaaki Murai, Takaaki Inaba, Kazuyoshi Okamoto
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Publication number: 20110165087Abstract: The present invention relates to nitroxide imaging probes that are isotopically modified or unmodified. Such nitroxide imaging probes may be included in liposomes that encapsulate self-quenching concentrations thereof, wherein the liposomes optionally comprise a targeting ligand specific to and having affinity for targeted tissue.Type: ApplicationFiled: December 22, 2010Publication date: July 7, 2011Inventors: JOSEPH P.Y. KAO, SCOTT R. BURKS, GERALD R. ROSEN
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Patent number: 7973039Abstract: The present invention is related to derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: GrantFiled: December 19, 2005Date of Patent: July 5, 2011Assignee: Merck Serono SAInventors: Dominique Swinnen, Agnes Bombrun, Patrick Gerber, Catherine Jorand-Lebrun
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Patent number: 7968550Abstract: The invention relates to substituted N-aryl heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof. Compounds of the formula I in which the radicals have the stated meanings the N-oxides and the physiologically tolerated salts thereof and process for the preparation thereof are described. The compounds are suitable for example as anorectic agents.Type: GrantFiled: January 11, 2007Date of Patent: June 28, 2011Assignees: Aventis Pharma Deutschland GmbH, Sanofi-Aventis Deutschland GmbHInventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Thomas Boehme, Gerhard Hessler, Petra Stahl, Dirk Gretzke
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Patent number: 7964601Abstract: A melanocortin receptor-specific compound of the general formula of structure I: where X, R1, R2a, R2b, R3, R4a, R4b, R5a and R5b are as defined in the specification, which compound binds with high affinity to one or more melanocortin receptors and is optionally an agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist, and may be employed for treatment of one or melanocortin receptor-associated conditions or disorders, and methods for the use of the compounds of the invention.Type: GrantFiled: June 2, 2008Date of Patent: June 21, 2011Assignee: Palatin Technologies, Inc.Inventors: Shubh D. Sharma, Yi-Qun Shi, Ramesh Rajpurohit, Zhijun Wu, Papireddy Purma, Annette M. Shadiack, Kevin D. Burris
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Publication number: 20110144103Abstract: The present invention relates to substituted pyrrole compounds and compositions comprising substituted pyrrole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted pyrrole compound of the invention, or a pharmaceutical composition comprising such a compound.Type: ApplicationFiled: June 4, 2009Publication date: June 16, 2011Inventors: Dinesh U. Chimmanamada, Weiwen Ying
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Publication number: 20110143445Abstract: A plurality of mass differential tagging reagents is used to label amine functionality in amine-containing compounds. The labeled analytes have distinct retention times on a reversed phase column, and distinct masses. Under high energy collision, reporter groups can be generated and the intensity or the peak area detected for each reporter group can be used for quantitation. One exemplary set of reagents includes a set of three different mass differential reagents comprising tagging weights of 140 atomic mass units, 144 atomic mass units, and 148 atomic mass units, respectively, with reporter groups of 113, 117, and 121 atomic mass units, respectively. A package including each of the mass differential reagents is also provided and can include separate respective containers, for example, one for each of the different reagents. The package can also include one or more standards each comprising a respective known concentration of a respective known amine-containing compound.Type: ApplicationFiled: December 15, 2010Publication date: June 16, 2011Applicant: DH Technologies Development Pte. Ltd.Inventors: Scott DANIELS, Subhasish PURKAYASTHA
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Publication number: 20110144110Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: ApplicationFiled: August 14, 2009Publication date: June 16, 2011Applicant: N30 PHARMACEUTICALS, LLCInventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu