Piperazine Ring Patents (Class 544/121)
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Publication number: 20120237475Abstract: Novel heterocyclic derivatives of formula (I): or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein Ra, n, R1 and R2 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5).Type: ApplicationFiled: March 16, 2012Publication date: September 20, 2012Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Daniel Ramsbeck
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Publication number: 20120232079Abstract: The invention relates to novel acylpiperazinone compounds, to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.Type: ApplicationFiled: October 20, 2010Publication date: September 13, 2012Inventors: Vincent Gerusz, Sonia Escaich, Mayalen Oxoby, Francois Moreau
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Publication number: 20120225854Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: August 23, 2011Publication date: September 6, 2012Applicant: AMGEN INC.Inventors: Kate Ashton, Michael David Bartberger, Yunxin Bo, Marian C. Bryan, Michael Croghan, Christopher Harold Fotsch, Clarence Henderson Hale, Roxanne Kay Kunz, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Lewis Dale Pennington, Steve Fong Poon, Markian Myroslaw Stec, David Joseph St. Jean, JR., Nuria A. Tamayo, Christopher Michael Tegley, Kevin Chao Yang
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Publication number: 20120225859Abstract: Phosphatidylinositol (PI) 3-kinase inhibitor compounds (I), their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases.Type: ApplicationFiled: May 14, 2012Publication date: September 6, 2012Applicant: NOVARTIS AGInventors: Matthew BURGER, Zhi-Jie NI, Sabina PECCHI, Gordana ATALLAH, Sarah BARTULIS, Kelly FRAZIER, Aaron SMITH, Joelle VERHAGEN, Yanchen ZHANG, Allan WAGMAN, Simon NG, Keith PFISTER, Daniel POON, Alicia LOUIE, Teresa PICK, Paul BARSANTI, Edwin IWANOWICZ, Wendy FANTL, Thomas HENDRICKSON, Mark KNAPP, Hanne MERRITT, Charles VOLIVA, Marion WIESMANN, Xiaohua XIN
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Publication number: 20120202809Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disase pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.Type: ApplicationFiled: April 18, 2012Publication date: August 9, 2012Inventors: Hui Li, Seiji Nukui, Stephanie Anne Scales, Min Teng, Chunfeng Yin
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Patent number: 8232274Abstract: Disclosed is a set of compounds useful as glucan synthase inhibitors having the generic structure of Formula I: wherein the various moieties A, D, R6, etc., are as defined in the specification. These compounds are useful in treating or preventing fungal infections in a patient.Type: GrantFiled: March 12, 2008Date of Patent: July 31, 2012Assignees: Albany Molecular Research, Inc., Merck Sharp & Dohme Corp.Inventors: Pauline C. Ting, Robert G. Aslanian, Jianhua Cao, David Won-Shik Kim, Rongze Kuang, Gang Zhou, Robert Jason Herr, Andrew John Zych, Jinhai Yang, Heping Wu, Nicolas Zorn
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Publication number: 20120190681Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1, R2, R3, A, B, Z, n, and m are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.Type: ApplicationFiled: January 20, 2012Publication date: July 26, 2012Applicant: ABBOTT LABORATORIESInventors: Anil Vasudevan, Thomas D. Penning, Marina Pliuschev
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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: 20120190677Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt or ester thereof, wherein R1 to R8, A1 to A3 have the are as described herein and compositions including the compounds.Type: ApplicationFiled: January 19, 2012Publication date: July 26, 2012Inventors: Lichun Feng, Mengwei Huang, Yongfu Liu, Guolong Wu, Shixiang Yan, Hongying Yun, Mingwei Zhou
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Patent number: 8202864Abstract: Compounds of formula (I) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is a group selected from 2,6-dimethyl-3-pyridyl or 4,6-dimethyl-3-pyridyl, R4 represents methyl and R5 represents hydrogen or methyl or, R4 and R5 together with the nitrogen atom to which they are attached represent morpholino and pharmaceutically acceptable derivatives thereof are described, as are for their preparation, pharmaceutical compositions containing them and their use in medicine, particularly their use as oxytocin antagonists.Type: GrantFiled: February 25, 2011Date of Patent: June 19, 2012Assignee: Glaxo Group LimitedInventors: Alan David Borthwick, Deirdre Mary Bernadette Hickey, John Liddle, Andrew McMurtrie Mason
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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: 20120114600Abstract: The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of replication of the hepatitis C virus. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat hepatitis C viral infections, and processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: November 3, 2011Publication date: May 10, 2012Applicant: THERAVANCE, INC.Inventors: Robert Murray McKINNELL, Daniel D. LONG, Lori Jean VAN ORDEN, Lan JIANG, Mandy LOO, Daisuke Roland SAITO, Shella ZIPFEL, Eric L. Stangeland, Kassandra Lepack, Gavin Ogawa
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Publication number: 20120115845Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1, R2, R3, R4 and m are as described in the specification for use in the treatment of obesity and/or diabetes.Type: ApplicationFiled: November 7, 2011Publication date: May 10, 2012Inventors: Jack McQueen ALLEN, Roger John Butlin, Clive Green, William McCoull, Graeme Richard Robb, James Matthew Wood
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Publication number: 20120115851Abstract: An objective of the present invention is to provide compounds that can effectively suppress the concentration of phosphorus in serum to effectively prevent or treat diseases induced by an increase in concentration of phosphate in serum. The compounds according to the present invention are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein A represents an optionally substituted five- to nine-membered unsaturated carbocyclic moiety or a five- to nine-membered unsaturated heterocyclic moiety, and represents a single bond or a double bond, R5 represents optionally substituted aryl or the like, Z represents —N?CHR6R7 or the like, R6 and R7 represent H, optionally substituted alkyl, optionally substituted aryl or the like, R101 and R102 together form ?O, and R103 and R104 represent H, or R101 and R104 together from a bond, and R102 and R103 together form a bond.Type: ApplicationFiled: January 18, 2012Publication date: May 10, 2012Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Nobuaki Eto, Rika Nagao, Tetsuko Kazama
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Patent number: 8173645Abstract: Compounds are provided for use with glucokinase that comprise the formula: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: GrantFiled: March 20, 2008Date of Patent: May 8, 2012Assignee: Takeda San Diego, Inc.Inventors: Zacharia Cheruvallath, Jun Feng, Prasuna Guntupalli, Stephen L. Gwaltney, Joanne Miura, Mark Sabat, Mingnam Tang
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Publication number: 20120107273Abstract: The present invention relates to a compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof and an anti-HCV agent and an HCV polymerase inhibitor containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.Type: ApplicationFiled: April 25, 2011Publication date: May 3, 2012Applicant: Japan Tobacco Inc.Inventors: Hiroyuki Abe, Masahiro Tanaka, Kazuyuki Sugimoto, Akira Suma, Masahiro Yokota, Makoto Shiozaki, Kiyosei Ilo, Kazuhito Ueyama, Dai Motoda, Toru Noguchi, Tsuyoshi Adachi, Junichiro Tsuruha, Satoki Doi
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Publication number: 20120108588Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ.Type: ApplicationFiled: January 6, 2012Publication date: May 3, 2012Applicant: Pfizer, Inc.Inventors: Iriny Botrous, Yufeng Hong, Hui Li, Kevin Kun-Chin Liu, Seiji Nukui, Min Teng, Eileen Valenzuela Tompkins, Chunfeng Yin
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Patent number: 8168784Abstract: Processes to make compounds, including N-acylsulfonamide apoptosis promoters are disclosed.Type: GrantFiled: June 17, 2009Date of Patent: May 1, 2012Assignee: Abbott LaboratoriesInventors: Thaddeus Stephan Franczyk, II, David R. Hill, Anthony Ralph Haight, Maureen Ann McLaughlin, Shashank Shekhar, Su Yu, Jianzhang Mei, Lei Wang
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Publication number: 20120101072Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole 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 triazole compound of the invention, or a pharmaceutical composition comprising such a compound.Type: ApplicationFiled: December 21, 2011Publication date: April 26, 2012Inventors: Joseph A. Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
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Publication number: 20120095000Abstract: Compositions and methods for treatment and prevention of disorders and conditions characterized by reduced TGF-? signaling are described.Type: ApplicationFiled: December 12, 2011Publication date: April 19, 2012Applicants: SRI International, The Board of Trustees of the Leland Stanford Junior UniversityInventors: Anton Wyss-Coray, Mary J. Tanga
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Publication number: 20120088754Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: December 14, 2011Publication date: April 12, 2012Inventors: Kristof Van Emelen, Janine Arts, Leo-Jacobus Jozef Backx, Hans Louis Jos De Winter, Sven Franciscus Anna Van Brandt, Marc Gustaaf Celine Verdonck, Lieven Meerpoel, Isabelle Noëlle Constance Pilatte, Virginie Sophie Poncelet, Alexey Borisovich Dyatkin, Jimmy Arnold Viviene Van heusden
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Publication number: 20120082702Abstract: Disclosed are nicotinamide compounds of Formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. Also disclosed are methods of using such compounds in the treatment of at least one Btk associated condition, such as, for example, inflammatory disease, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: June 10, 2010Publication date: April 5, 2012Inventors: George V. DeLucca, Qing Shi, Chunjian Liu, Jingwu Duan, Andrew J. Tebben
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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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Patent number: 8148367Abstract: Disclosed are compounds, pharmaceutical compositions, kits, articles of manufacture, methods of using, and methods of preparing compounds having the formula: wherein the variables are as defined herein. The disclosed compounds are inhibitors of Renin.Type: GrantFiled: January 9, 2008Date of Patent: April 3, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Lily Kwok, Betty Lam, Zhe Li, Zhiyuan Zhang
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Publication number: 20120077787Abstract: New compounds of the Formula (I): for the treatment of non-insulin-dependent diabetes mellitus.Type: ApplicationFiled: December 6, 2011Publication date: March 29, 2012Applicant: NOVARTIS AGInventors: Daniel Kaspar Baeschlin, Nils OSTERMANN, Francois GESSIER, Finton SIROCKIN, Kenji NAMOTO
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Publication number: 20120071652Abstract: Disclosed are novel piperazine derivatives that act as agonists of the ?7 nAChR. Also disclosed are pharmaceutical compositions, methods of treating inflammatory conditions, methods of treating CNS disorders, methods for inhibiting cytokine release from mammalian cells and methods for the preparation of the novel compounds.Type: ApplicationFiled: March 23, 2011Publication date: March 22, 2012Applicant: CORNERSTONE THERAPEUTICS, INC.Inventors: Roger B. Clark, Daniel Elbaum
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Publication number: 20120071653Abstract: The present invention provides compounds useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role.Type: ApplicationFiled: June 23, 2011Publication date: March 22, 2012Applicant: SYMPHONY EVOLUTION, INC.Inventors: Lynne Canne Bannen, Erick W. Co, Vasu Jammalamadaka, John M. Nuss, Moon Hwan Kim, Donna Tra Le, Amy Lew, Morrison B. Mac, Shumeye Mamo, Zhaoyang Wen, Wei Xu, Richard George Khoury
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Publication number: 20120065169Abstract: Oligonucleotide analogues comprising modified intersubunit linkages and/or modified 3? and/or 5?-end groups are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects.Type: ApplicationFiled: May 27, 2011Publication date: March 15, 2012Inventors: Gunnar J. Hanson, Alexander Charles Rudolph, Bao Zhong Cai, Ming Zhou, Dwight D. Weller
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Patent number: 8129377Abstract: A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein R1 represents a C1-C12 alkyl; R2 represents a hydrogen atom or the like; R3 represents a halogen or the like; q represents an integer of 1 to 7; R4 represents a halogen or the like; p represents 0 or an integer of 1 to 5; R5 represents a C6-C10 aryl, a heterocycle or the like; and X represents oxygen, NH, or the like, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).Type: GrantFiled: September 29, 2005Date of Patent: March 6, 2012Assignees: Mitsubishi Tanabe Pharma Corporation, Sanofi-AventisInventors: Kazutoshi Watanabe, Kenji Fukunaga, Toshiyuki Kohara, Fumiaki Uehara, Shinsuke Hiki, Satoshi Yokoshima
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Publication number: 20120053149Abstract: The present invention relates to thiazole derivatives of formula I and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.Type: ApplicationFiled: April 21, 2010Publication date: March 1, 2012Inventors: Eva Caroff, Kurt Hilpert, Francis Hubler, David Lehmann, Emmanuel Meyer, Dorte Renneberg
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Publication number: 20120053166Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.Type: ApplicationFiled: March 5, 2010Publication date: March 1, 2012Inventors: Julie Nicole Hamblin, Zoe Alicia Harrison, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Christopher James Lunniss, Nigel James Parr
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Publication number: 20120040020Abstract: The present disclosure relates to pyrazine compounds of formula I: wherein L, n, R1, and R2 are as described in the specification. These compounds are useful as inhibitors of ATR protein kinase. The disclosure also relates to pharmaceutically acceptable compositions comprising the compounds of the disclosure; methods of treating of various diseases, disorders, and conditions using the compounds of the disclosure; processes for preparing the compounds of the disclosure; intermediates for the preparation of the compounds of the disclosure; 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.Type: ApplicationFiled: October 27, 2011Publication date: February 16, 2012Applicant: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Steven John Durrant, David Kay, Michael O'Donnell, Ronald Marcellus Alphonsus Knegtel, Somhairle MacCormick, Joanne Pinder, Stephen Clinton Young, Haley Marie Binch, Thomas Cleveland, Lev Tyler Dewey Fanning, Dennis James Hurley, Pramod Joshi, Urvi Jagdishbhai Sheth, Alina Silina, Philip Michael Reaper, Anisa Nizarali Virani
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Publication number: 20120040959Abstract: The invention provides compound and salts of Formula I and II, disclosed herein, which includes compounds of Formula A and Formula B: Such compounds possess useful antimicrobial activity. The variables R2, R3, R5, R6, R7, and R9 shown in Formula A and B are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and/or selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.Type: ApplicationFiled: October 24, 2011Publication date: February 16, 2012Applicant: Achillion Pharmaceuticals, Inc.Inventors: Barton James Bradbury, Jason Allan Wiles, Qiuping Wang, Akhiro Hashimoto, Edlaine Lucien, Godwin Clarence Gilroy Pais, Milind Deshpande, Michael John Pucci, Ha Young Kim
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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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Patent number: 8114844Abstract: Linear and cyclic peptidomimetics which bind to one or more melanocortin receptors are provided, which peptidomimetics include at least one ring-constrained amino acid surrogate of formula I: where R1, R2, R3, R4, R5, R6, R7, R8, and y are as defined in the specification, together with methods for synthesizing ring-constrained amino acid surrogates of formula I and peptidomimetics incorporating the same, and methods of use of peptidomimetics in the treatment of various diseases, syndromes and conditions.Type: GrantFiled: October 3, 2008Date of Patent: February 14, 2012Assignee: Palatin Technologies, Inc.Inventors: Shubh D. Sharma, Margarita Bastos, Wei Yang
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Patent number: 8114871Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ.Type: GrantFiled: April 10, 2008Date of Patent: February 14, 2012Assignees: Pfizer Inc., Pfizer Products Inc.Inventors: Iriny Botrous, Yufeng Hong, Hui Li, Kevin Kun-Chin Liu, Seiji Nukui, Min Teng, Eileen Valenzuela Tompkins, Chunfeng Yin
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Publication number: 20120028954Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: ApplicationFiled: July 29, 2011Publication date: February 2, 2012Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
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Publication number: 20120029191Abstract: The present invention is directed to novel processes for the preparation of cyclopropyl-amide derivatives, useful for the treatment of disorders and conditions mediated by the histamine receptor.Type: ApplicationFiled: October 11, 2011Publication date: February 2, 2012Inventors: Neelakandha S. Mani, David C. Palmer, Chennagiri R. Pandit, Mayra B. Reyes, Tong Xiao, Sergio Cesco-Cancian
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Patent number: 8097629Abstract: The invention relates to novel dihydropyridinone derivatives, processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.Type: GrantFiled: February 5, 2005Date of Patent: January 17, 2012Assignee: Bayer Pharma AktiengesellschaftInventors: Heike Gielen-Haertwig, Barbara Albrecht, Marcus Bauser, Jörg Keldenich, Volkhart Li, Josef Pernerstorfer, Karl-Heinz Schlemmer, Leila Telan
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Patent number: 8097611Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: April 13, 2010Date of Patent: January 17, 2012Assignee: Janssen Pharmaceutica, N.V.Inventors: Kristof Van Emelen, Janine Arts, Leo-Jacobus Jozef Backx, Hans Louis Jos De Winter, Sven Franciscus Anna Van Brandt, Marc Gustaaf Celine Verdonck, Lieven Meerpoel, Isabelle Noëlle Constance Pilatte, Virginie Sophie Poncelet, Alexey Borisovich Dyatkin, Jimmy Arnold Viviane Van heusden
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Publication number: 20120010201Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein X, Y, A, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as therapeutics.Type: ApplicationFiled: June 29, 2011Publication date: January 12, 2012Inventors: Luca Gobbi, Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Publication number: 20120004213Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: ApplicationFiled: September 15, 2011Publication date: January 5, 2012Applicant: FOREST LABORATORIES HOLDINGS LIMITEDInventors: Kumar SUNDARESAN, Sandeep N. RAIKAR, Srinivasa Raju SAMMETA, Ganesh PRABHU, Hosahalli SUBRAMANYA, Alexander BISCHOFF
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Publication number: 20120004197Abstract: Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin.Type: ApplicationFiled: March 31, 2010Publication date: January 5, 2012Applicant: KOWA COMPANY, LTD.Inventors: Masanori Ashikawa, Junya Tagashira, Akiyasu Koketsu, Toshiharu Morimoto, Takahiro Kitamura, Syunji Takemura, Gen Watanabe, Tatsuaki Nishiyama, Satoshi Goda, Masaki Yamabi, Takeshi Doi, Hiroyuki Ishiwata
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Patent number: 8088761Abstract: Compounds of formula (I), are aurora kinase inhibitors: wherein X is —N—, —CH2-N—, —CH2-CH—, or —CH—; R1 is a radical of formula (IA) wherein Z is —CH2-, —NH—, -0-, —S(O)— —S—, —S(O)2 or a divalent monocyclic carbocyclic or heterocyclic radical having 3-7 ring atoms; Alk is an optionally substituted divalent C1-C6 alkylene radical; A is hydrogen or an optionally substituted monocyclic carbocyclic or heterocyclic ring having 5-7 ring atoms; r, s and t are independently 0 or 1, provided that when A is hydrogen then at least one of r and s is 1; R2 is halogen, —CN, —CF3, —OCH3, or cyclopropyl; and R3 is a radical of formula (IB) wherein Q is hydrogen or an optionally substituted phenyl or monocyclic heterocyclic ring with 5 or 6 ring atoms; Z&It;1> is —S—, —S(O)—, —S(O)2-, —O—, —SO2NH—, —NHSO2-, NHC(?O)NH, —NH(C?S)NH—, Or —N(R4)— wherein R4 is hydrogen, C1-C3 alkyl, cycloalkyl, or benzyl; and Alk&It;1> and Alk&It;2> are, independently, optionally substituted divalent C1-C3 alkyleType: GrantFiled: December 21, 2006Date of Patent: January 3, 2012Assignee: Cancer Research Technology LimitedInventors: Vassilios Bavetsias, Edward McDonald, Spyridon Linardopoulos
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Patent number: 8088925Abstract: The present invention relates to compounds of the formula I, which exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses.Type: GrantFiled: November 15, 2007Date of Patent: January 3, 2012Assignee: Sanofi-AventisInventors: Michael Wagner, Matthias Urmann, Volkmar Wehner, Martin Lorenz, Armin Bauer, Marc Nazare, Hans Matter
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Publication number: 20110319413Abstract: This invention relates to a piperazine compound represented by Formula (I), wherein R1 is C1-6 alkyl; R2 is hydroxy, C1-6 alkyl that may have one or more substituents, —(C?O)—N(R3)(R4), or —(C?O)—OR5; R3 and R4 are the same or different, and each represents hydrogen or C1-6 alkyl that may have one or more substituents, or R3 and R4, taken together with a nitrogen atom to which R3 and R4 are attached, may form a saturated heterocyclic group; R5 is hydrogen or C1-6 alkyl that may have one or more substituents; and n is 1 or 2; or a salt thereof.Type: ApplicationFiled: March 8, 2010Publication date: December 29, 2011Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Yoshihiro Urade, Makoto Kitade, Kazuhiko Shigeno, Keiko Yamane, Katsunao Tanaka
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Publication number: 20110312939Abstract: The present invention relates to new compounds of general formula (I), wherein the groups R1 to R3, X1, X2, X3 and L1 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof in such a treatment.Type: ApplicationFiled: September 28, 2009Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
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Publication number: 20110313151Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein X, Y, A, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as therapeutics.Type: ApplicationFiled: June 16, 2011Publication date: December 22, 2011Inventors: Luca Gobbi, Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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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