Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Ring Carbon Of The Additional Six-membered Hetero Ring (e.g., Nicotinic Acid, Etc.) Patents (Class 544/365)
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Publication number: 20130131079Abstract: The present invention is directed to a compound of formula (I) for use in a method to treat or ameliorate amyloid or tau pathologies, such as Alzheimer's disease, or symptoms thereof. The invention is also directed to new compounds of formula (I), of subformula (II), (III), (IV), or (V).Type: ApplicationFiled: May 23, 2011Publication date: May 23, 2013Applicant: FAES FARMA, S.A.Inventors: Francisco Ledo Gómez, Ana Muñoz Muñoz, Carmen Pumar Durán
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Publication number: 20130116430Abstract: An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C3-8 cycloalkyl group, an aryl group, an ar-C1-6 alkyl group or a heterocyclic group, each optionally having at least one substituent; R3 represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R4 and R5 each independently represent a hydrogen atom; and R2 and R4 may form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.Type: ApplicationFiled: December 28, 2012Publication date: May 9, 2013Applicant: FUJIFILM CORPORATIONInventors: Hideyasu FUJIWARA, Kimihiko SATO, Shinsuke MIZUMOTO, Yuichiro SATO, Hideki KURIHARA, Yohei KUBO, Hiyoku NAKATA, Yasutaka BABA, Takashi TAMURA, Hidenobu KUNIYOSHI, Shinji HAGIWARA, Mari YAMAMOTO
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Publication number: 20130102600Abstract: The present invention relates to a compound having the general formula I, optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which is useful in treating, ameliorating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.Type: ApplicationFiled: October 18, 2012Publication date: April 25, 2013Applicants: F. HOFFMANN-LA ROCHE LTD, EUROPEAN MOLECULAR BIOLOGY LABORATORY (EMBL), SAVIRA PHARMACEUTICALS GMBHInventors: F. HOFFMANN-LA ROCHE LTD, SAVIRA PHARMACEUTICALS GMBH, EUROPEAN MOLECULAR BIOLOGY LABORAT
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Patent number: 8426416Abstract: This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4 and X have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: March 15, 2011Date of Patent: April 23, 2013Assignee: Janssen Pharmaceutica, N.V.Inventors: Sven Franciscus Anna Van Brandt, Kristof Van Emelen, Patrick Rene Angibaud, Laurence Francoise Bernadette Marconnet-Decrane, Janine Arts
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Patent number: 8420639Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: GrantFiled: April 21, 2010Date of Patent: April 16, 2013Assignee: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei Ly, Jared Andrew Forrester
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Publication number: 20130085127Abstract: A heterocyclic compound useful as an antiallergic agent is provided. A compound represented by the following formula (1) or a salt thereof: wherein the ring A is a homocyclic or heterocyclic ring; the ring B is a heterocyclic ring which contains G and nitrogen atom N as constituent atoms thereof, wherein G is CH or N; R1 is a carbonyl group or an alkylene group; R2a and R2b are an alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; X is an oxygen atom or a sulfur atom; Z is a hydroxyl group, an alkoxy group, a cycloalkyloxy group, an aryloxy group, an aralkyloxy group, an amino group, or an N-substituted amino group; and n is 0 or 1; with the proviso that when the ring A is a benzene ring or when the ring B is a piperazine ring, R1 is an alkylene group which may have a substituent.Type: ApplicationFiled: May 23, 2011Publication date: April 4, 2013Applicant: ASKA Pharmaceutical Co., LtdInventors: Makoto Okada, Koichi Hasumi, Takahiro Nishimoto, Miwa Yoshida, Kouki Ishitani, Tomoji Aotsuka, Hashime Kanazawa
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Publication number: 20130079354Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): wherein W, V, x, y, R1, R2, R3, R4, R5, R6, R7, R7a, R8, R8a, R9, R9a, R10 and R10a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.Type: ApplicationFiled: September 14, 2012Publication date: March 28, 2013Applicant: Xenon Pharmaceuticals Inc.Inventors: Melwyn ABREO, Daniel F. HARVEY, Mikhail A. KONDRATENKO, Wenbao LI, Rajender KAMBOJ, Vishnumurthy KODUMURU, Michael D. WINTHER, Heinz W. GSCHWEND, Nagasree CHAKKA, Shifeng LIU, Serguei SVIRIDOV, Shaoyi SUN
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Publication number: 20130065876Abstract: The present invention relates to compounds of formula I, wherein R1 to R5 are defined in the description and claims, and to pharmaceutically acceptable salts thereof. The present invention relates also to the manufacture of said compounds, pharmaceutical compositions containing them and methods for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as dyslipidemia, atherosclerosis and cardiovascular diseases.Type: ApplicationFiled: September 11, 2012Publication date: March 14, 2013Inventors: Uwe Grether, Paul Hebeisen, Peter Mohr, Fabienne Ricklin, Stephan Roever
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Publication number: 20130040949Abstract: The present invention relates to novel compounds which are able to modulate b-raf kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.Type: ApplicationFiled: December 29, 2010Publication date: February 14, 2013Applicant: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Nathanael S. Gray, Hwan G. Choi, Xianming Deng, Jianming Zhang
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Patent number: 8367836Abstract: The present invention provides compounds that are alpha4 integrin antagonists having a structure according to the following formula: or a tautomer, mixture of tautomers, salt or solvate thereof, wherein Cy, ring A, m, n, p, R1, R2, R3, R4, R5 and R6 are defined in the specification. The invention further provides pharmaceutical compositions including the compounds of the invention as well as methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various conditions and disorders, such as Crohn's disease and ulcerative colitis.Type: GrantFiled: April 27, 2010Date of Patent: February 5, 2013Assignee: Elan Pharmaceuticals, Inc.Inventors: Ying-zi Xu, Shendong Yuan, David Wone, Andrei Konradi
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Publication number: 20130023541Abstract: The present invention relates to voltage-gated sodium channel blocker intermediates, compounds and dimers, corresponding pharmaceutical compositions, compound preparation and treatment methods for respiratory or respiratory tract diseases.Type: ApplicationFiled: January 13, 2011Publication date: January 24, 2013Inventors: Jeffrey Charles Boehm, Roderick S. Davis, Jeffrey K. Kerns, Guoliang Lin, Hong Nie
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Patent number: 8354401Abstract: Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, or a hydrate or solvate thereof.Type: GrantFiled: October 27, 2009Date of Patent: January 15, 2013Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Seigo Ishibuchi, Hidemasa Hikawa, Akiko Tarao, Jun-ichi Endoh, Kunitomo Adachi, Kazuhiro Maeda, Kaoru Tashiro
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Publication number: 20130012709Abstract: An inhibitor of the activity of stearoyl-CoA-desaturase-1 (SCD-1) enzyme for use in the treatment of prostate cancer as well as novel inhibitors of formula (IIa).Type: ApplicationFiled: September 10, 2010Publication date: January 10, 2013Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Lluis Fajas, Zohra Benfodda, Vanessa Fritz
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Publication number: 20130005974Abstract: The invention describes an improved synthesis for piperazine derivatized with nicotinic acid and a benzyl moiety. The product compounds are useful for treatment of neurological conditions.Type: ApplicationFiled: August 24, 2010Publication date: January 3, 2013Applicant: NEURALSTEM, INC.Inventors: Sripathy Venkatraman, Syed Mahmood, Bingidimi I. Mobele, Olga Lapina, Kellie Vercoe, Ying Li, Jonathan Salsbury, Mark McLaws
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Publication number: 20120302746Abstract: The present invention relates to novel piperazine derivatives; to processes for their preparation; to pharmaceutical compositions containing the derivatives; and to the use of the derivatives in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial.Type: ApplicationFiled: August 7, 2012Publication date: November 29, 2012Inventors: Paul John Beswick, Alister Campbell, Andrew Cridland, Robert James Gleave, Jag Paul Heer, Neville Hubert Nicholson, Lee William Page, Sadie Vile
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Publication number: 20120295889Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: May 16, 2012Publication date: November 22, 2012Applicant: Merck Serono S.A.Inventors: Ulrich Abel, Holger Deppe, Achim Feurer, Ulrich Grädler, Kerstin Otte, Renate Sekul, Meinolf Thiemann, Andreas Goutopoulos, Matthias Schwarz, Xuliang Jiang
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Publication number: 20120270882Abstract: Provided are compounds of Formula I which are derivatives of 3-Hydroxypyridin-4-ones. The compounds may be used in treatment of a medical condition related to a toxic concentration of iron. The compounds may be used for preparation of a medicament for treatment of a medical condition related to a toxic concentration of iron. The medical condition related to a toxic concentration of iron may be selected from the group consisting of: cancer, pulmonary disease, progressive kidney disease and Frederich's Ataxia.Type: ApplicationFiled: July 5, 2010Publication date: October 25, 2012Applicant: APOTEX TECHNOLOGIES INC.Inventors: Tim Fat Tam, Regis Leung-Toung, Yingsheng Wang, Yangqing Zhao, Tao Xin, Birenkumar Shah, Blaise N'zemba, Jolanta Maria Wodzinska, Maryna Premyslova
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Patent number: 8288388Abstract: The present invention relates to novel piperazine derivatives; to processes for their preparation; to pharmaceutical compositions containing the derivatives; and to the use of the derivatives in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial.Type: GrantFiled: July 15, 2009Date of Patent: October 16, 2012Assignee: Convergence Pharmaceuticals LimitedInventors: Paul John Beswick, Alister Campbell, Andrew Cridland, Robert James Gleave, Jag Paul Heer, Neville Hubert Nicholson, Lee William Page, Sadie Vile
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Publication number: 20120258947Abstract: Substituted 6-amino-nicotinamides, pharmaceutical compositions containing these compounds and also use of these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: ApplicationFiled: April 18, 2012Publication date: October 11, 2012Applicant: Grunenthal GmbHInventors: Sven KÜHNERT, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder, Simon Lucas
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Patent number: 8278442Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are opioid receptor modulators, e.g. mu-opioid receptor antagonists, neutral antagonists or inverse agonists, and are useful for the treatment of metabolic disorders including obesity.Type: GrantFiled: May 22, 2008Date of Patent: October 2, 2012Assignee: Prosidion LimitedInventors: Jason Bloxham, Stuart Edward Bradley, Tom Banksia Dupree, Peter Timothy Fry, Patrick Eric Hanrahan, Thomas Martin Krulle, Martin James Procter, Colin Peter Sambrook-Smith, Karen Lesley Schofield, Donald Smyth, Alan John Stewart
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Publication number: 20120232091Abstract: The invention relates to various new polymorphic forms of manidipine and pharmaceutically acceptable salts thereof. The invention also relates to processes for the preparation of the polymorphic forms of manidipine and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: August 26, 2010Publication date: September 13, 2012Applicant: CIPLA LIMITEDInventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Maruti Ganpati Ghagare
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Publication number: 20120202775Abstract: Compounds having drug and bio-affecting properties are described herein, including their properties, pharmaceutical compositions and methods of use. In particular, tricyclic aryl or heteroaryl piperazine diamide derivatives that possess unique antiviral activity are set forth. These compounds are useful for the treatment of HIV and AIDS.Type: ApplicationFiled: August 4, 2011Publication date: August 9, 2012Inventors: Tao Wang, Zhongxing Zhang, Zhiwei Yin, John F. Kadow, Nicholas A. Meanwell
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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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Patent number: 8222402Abstract: A process for preparing compounds of the formula (I) in which R1.1, R1.2, R1.3 and R2 are as defined in the description.Type: GrantFiled: August 12, 2008Date of Patent: July 17, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Kathrin Pachur, Stefan Goepper, Guenther Huchler, Michael Konrad, Kathrin Maier, Werner Rall, Uwe Joerg Ries, Andreas Zopf
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Patent number: 8207171Abstract: Cosmetic compositions comprising 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides and methods of using such compositions to impart anti-aging benefits to the skin are disclosed. The 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging.Type: GrantFiled: June 21, 2011Date of Patent: June 26, 2012Assignee: Avon Products, Inc.Inventors: Dmitri S. Ptchelintsev, Hong Hu, Gopinathan K. Menon, Kristine Schmalenberg, John W. Lyga
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Publication number: 20120142698Abstract: The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R10R11)—C(?O)—, x-C(R12R13)—C(?S)—, x-O—C(?O)—, x-O—C(?S)—, x-N(R14)—C(?O)—, x-N(R15)—C(?S)—, x-C(R16R17)—SO2— or X—N?C(R30)—, in each case x indicates the bond that is connected to R1; T is CR18 or N; Y1, Y2, Y3, and Y4 are independently CR19 or N; Q is O or S; n is 1 or 2; p is 1 or 2, providing that when n is 2, p is 1.Type: ApplicationFiled: August 6, 2010Publication date: June 7, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Sarah Sulzer-Mosse, Clemens Lamberth, Laura Quaranta, Mathias Stephan Respondek
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Publication number: 20120136002Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.Type: ApplicationFiled: May 18, 2010Publication date: May 31, 2012Inventors: Rajeev Goswami, Anil Kumar Vuppala, Ramesh Veludandi, Ramesh Sistla, Chakshusmathi Ghadiyaram, Muralidhara Ramachandra
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Publication number: 20120108566Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.Type: ApplicationFiled: November 1, 2011Publication date: May 3, 2012Applicant: Portola Pharmaceuticals, Inc.Inventors: Shawn M. Bauer, Yonghong Song, Qing Xu, Jack W. Rose, Zhaozhong J. Jia, Brian Kane, Wolin Huang, Anjali Pandey, Mukund Mehrotra
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Publication number: 20120108606Abstract: Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R4, D, E, J, T, p, q 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: January 11, 2012Publication date: May 3, 2012Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Ihab S. Darwish, Jiaxin Yu, Hui Hong, Rajinder Singh, Sambaiah Thota, Xiang Xu
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Patent number: 8168640Abstract: Cosmetic compositions comprising 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides and methods of using such compositions to impart anti-aging benefits to the skin are disclosed. The 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging.Type: GrantFiled: June 21, 2011Date of Patent: May 1, 2012Assignee: Avon Products, Inc.Inventors: Dmitri S. Ptchelintsev, Hong Hu, Gopinathan K. Menon, Kristine Schmalenberg, John W. Lyga
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Patent number: 8163907Abstract: A dihydropyridine (DHP) calcium antagonist compound and its preparation method and medical use are related to preparation methods of compounds of general formulas (I) and (II) as shown below and their pharmaceutical salts and applications for treating cardiovascular diseases, and R1 represents a substituted or unsubstituted heterocyclic, aromatic ring or aralkyl group, and the substituent may be C1-C4 alkyl, C1-C4 alkoxyl, halogen, cyano, trifluoromethyl, trifluoromethoxyl, methylthio, nitro, amino or hydroxyl group; R2 represents a C1-C8 alkyl group; R3 and R4 are the same or different, and each represents a hydrogen, halogen, cyano, trifluoromethyl, trifluoromethoxyl, methylthio, nitro or amino group or a C1-C4 alkyl, C1-C4 alkoxyl, C1-C4 alkenyl, or C1-C4 alkinyl group; R5 and R6 are the same or different, and each represents a C1-C4 alkyl group; X represents O, S or a single bond; m=0-6, n=1-6, and m and n are the same or different.Type: GrantFiled: January 5, 2009Date of Patent: April 24, 2012Assignee: Cosunter Pharmaceutical CompanyInventors: Guo-hua Chen, Li Wang
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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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Patent number: 8133894Abstract: Compounds of Formula (I) are effective in the treatment of a microbial infection.Type: GrantFiled: July 28, 2010Date of Patent: March 13, 2012Assignee: Akebia Therapeutics Inc.Inventors: Namal Chithranga Warshakoon, Rodney Dean Bush
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Publication number: 20120046268Abstract: The invention relates to novel substituted piperidines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of cardiovascular disorders and tumour disorders.Type: ApplicationFiled: March 12, 2010Publication date: February 23, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Mario Jeske, Dirk Heimbach, Susanne Röhrig, Yolanda Cancho Grande, Dirk Schneider, Ulrich Rester, Eckhard Bender, Mark Meininghaus, Katja Zimmermann, Dmitry Zubov, Anja Buchmüller, Georges Von Degenfeld, Christoph Gerdes, Michael Gerisch, Mark Jean Gnoth, Kersten Matthias Gericke
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Patent number: 8119797Abstract: The present invention relates to a process for preparing compounds of general formula I wherein R1 and R2 are defined as in claim 1, the pharmaceutically acceptable salts and the solvates thereof, which may be prepared starting from compounds of general formula II wherein R1 is defined as in claim 1.Type: GrantFiled: August 8, 2011Date of Patent: February 21, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Guenther Huchler, Werner Rall, Uwe Reis
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Patent number: 8114875Abstract: The invention relates to substituted N-heterocyclic compounds of general formula (I.A) and to the tautomers of the compounds the physiologically acceptable salts of the compounds and the physiologically acceptable salts of the tautomers of the compounds. The invention also relates to the use of these compounds and their pharmacologically acceptable salts in the production of a pharmaceutical agent for treating diseases that respond to the influence exerted by dopamine D3 receptor ligands, especially for treating diseases of the central nervous system, especially schizophrenia and/or depression.Type: GrantFiled: December 20, 2005Date of Patent: February 14, 2012Assignee: Abbott GmbH & Co. KGInventors: Herve Geneste, Daryl R. Sauer
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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: 20120020881Abstract: This invention relates to novel compounds suitable for labeling by positron emitting isotopes, such as 18F, 11C, 13N and 15O, through appropriate labeling reagents, such as 18F reagents and methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).Type: ApplicationFiled: December 4, 2009Publication date: January 26, 2012Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Lutz Lehmann, Timo Stellfeld, Keith Graham, Jessica Becaud, Linjing Mu
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Patent number: 8101616Abstract: This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and X have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: January 16, 2007Date of Patent: January 24, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Patrick René Angibaud, Laurence Françoise Bernadette Marconnet-Decrane, Janine Arts
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Publication number: 20120015958Abstract: The present invention relates to 1-(4-ureidobenzoyl)piperazine derivatives having the general Formula I (We bring to your attention that formula I is not provided on this electronic version as it is provided in the abstract of the paper copy) Wherein R1 is (C1-8)alkyl, (C3-8)cycloalkyl or (C3-8)cycloalkyl(C1-3)alkyl, each of which may be substituted by hydroxy, cyano or halogen; R2 represents 1 or 2 optional halogens; R3 is (C1-6)alkyl, (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl, each of which may be substituted by one or more halogens; A represents a heteroaryl ring system comprising 1-3 heteroatoms selected from N, O and S, which ring system is 5- or 6-membered when X is C, and 5-membered when X is N; n is 1 or 2; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same, and to the use of a these 1-(4-ureidobenzoyl)piperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterType: ApplicationFiled: August 26, 2009Publication date: January 19, 2012Inventors: Andrew John Cooke, David Jonathan Bennett, Andrew Stanley Edwards, Andrew Laird Roughton, Irina Neagu, Jui-Hsiang Chan, Koc Kan Ho, Nasrin Ansari, Michelle Lee Morris, Yajing Rong, Michael Ohlmeyer
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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: 8097624Abstract: The present invention provides an cycloalkyl derivative of 3-hydroxy-4-pyridinone which is useful for the chelation of metal ions such as iron. Its preparation and use is described. In particular, the invention concerns the removal of iron in chemical and biological systems including chelating agents having the formula I wherein R1 is X with the proviso that R2 is Y; or R1 is T with the proviso that R2 is W; or R1 is X with the proviso that R2R5N when taken together form a heterocyclic ring selected from piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl, wherein the group piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl is either unsubstituted or substituted with one to three C1 to C6 alkyl groups.Type: GrantFiled: May 9, 2008Date of Patent: January 17, 2012Assignee: Apotex Inc.Inventors: Tim Fat Tam, Michael Spino, Wanren Li, Yingsheng Wang, Yanqing Zhao, Birenkumar Hasmukhbhai Shah
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Patent number: 8093250Abstract: The present invention relates to 2-aminocarbonyl-pyridine 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.Type: GrantFiled: October 12, 2007Date of Patent: January 10, 2012Assignee: Actelion Pharmaceuticals Ltd.Inventors: Eva Caroff, Kurt Hilpert, Emmanuel Meyers
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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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Patent number: 8076488Abstract: This invention relates to novel diaryl ureas, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and angiogenesis disorders, as a sole agent or in combination with cytotoxic therapies.Type: GrantFiled: March 1, 2004Date of Patent: December 13, 2011Assignee: Bayer Healthcare LLCInventors: Jacques Dumas, Stephen Boyer, Sharad Verma, Lila Adnane, Yuanwei Chen, Wendy Lee, Barton Phillips, Roger A. Smith, William J. Scott, Jennifer Burke, Jianqing Chen, Zhi Chen, Jianmei Fan, Karl Miranda, Brian Raudenbush, Aniko Redman, Jianxing Shao, Ning Su, Gan Wang, Lin Yi, Qingming Zhu
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Publication number: 20110281871Abstract: The invention relates to a compound of formula wherein R1, R2, X, L, W, n, and o are defined herein and to pharmaceutically suitable acid addition salts thereof, with the exception of the following compounds 6-(4-methyl-piperazin-1-yl)-N-phenethyl-nicotinamide (CAS 199478-31-4), N-(3,4-dichloro-benzyl)-3-fluoro-benzamide (CAS 424815-98-5), N-(4-chloro-benzyl)-3-fluoro-benzamide (CAS 544661-83-8), N-(3-chloro-benzyl)-3-fluoro-benzamide (CAS 796051-07-5), and N-phenethyl-6-phenylamino-nicotinamide (CAS 571913-74-1). The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of CNS disorders.Type: ApplicationFiled: July 26, 2011Publication date: November 17, 2011Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Patent number: 8048898Abstract: A compound represented by formula (I) or a pharmaceutically acceptable salt thereof: (wherein Y1 represents a nitrogen atom or a group represented by CRA, Y2 represents a nitrogen atom or a group represented by CRB, Y3 represents a nitrogen atom or a group represented by CRC, RA, RB and RC, which may be the same or different, each represent a hydrogen atom, etc. (excluding the case where Y1 is CRA, Y2 is CRB and Y3 is CRC), X represents an oxygen atom, etc., R1 represents a C1-C6 alkyl group, etc., R2 represents a C1-C6 alkyl group, etc., R3 represents an optionally substituted phenyl group, etc., R4 represents a hydrogen atom, etc., and R5 represents an optionally substituted phenyl group, etc.Type: GrantFiled: August 1, 2008Date of Patent: November 1, 2011Assignee: Taisho Pharmaceutical Co., LtdInventors: Naoya Ono, Fumiyasu Shiozawa, Tetsuya Yabuuchi, Hironori Katakai
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Publication number: 20110263557Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119; such as, but not limited to, diabetes, obesity and associated metabolic disorders. Formula (I) is a compound, in which A can have up to 2 ring —CH2- group substituted with —C(O)— and can be partially unsaturated with up to 2 double bonds; Wi and W2 are independently selected from CR10 and N; wherein R10 is selected from hydrogen and C1_6alkyl; Yi is selected from NRn, O and S; wherein Rn is selected from hydrogen and C1_6alkyl; Y2 and Y3 are independently selected from CH and N; Y4 is selected from CH2, OCH2 and NR15; wherein R15 is selected from hydrogen and C1_6alkyl; or the pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 3, 2009Publication date: October 27, 2011Applicant: IRM LLCInventors: Christopher Cow, Robert Epple
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Publication number: 20110257182Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: June 25, 2011Publication date: October 20, 2011Inventor: Christelle Bolea
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Publication number: 20110237590Abstract: To provide a novel JAK3 inhibitor that is useful as a preventive and/or therapeutic agent for rejection and graft versus host disease (GvHD) in organ transplantation, rheumatoid arthritis, multiple sclerosis, systemic lupus erythematosus, Sjögren syndrome, Behcet's disease, type I diabetes mellitus, autoimmune thyroiditis, idiopathic thrombocytopenic purpura, ulcerative colitis, Crohn's disease, asthma, allergic rhinitis, atopic dermatitis, contact dermatitis, urticaria, eczema, psoriasis, allergic conjunctivitis, uveitis, cancer, leukemia and the like. The pyridine-3-carboxyamide derivative represented by the general formula (1): or its salt or a solvate thereof.Type: ApplicationFiled: November 27, 2009Publication date: September 29, 2011Inventors: Takahiro Kitamura, Hajime Yamada, Shunji Takemura, Masanori Ashikawa, Tetsuya Ishikawa, Yoshiharu Miyake, Akiyasu Kouketsu, Seiichi Sato, Hiroyuki Ishiwata, Yuichiro Tabunoki, Manabu Shibasaki, Takatoshi Ozawa, Ryota Shigemi, Takeshi Doi, Masahiro Tamura