Nitrogen Attached Directly Or Indirectly To The Purine Ring System By Nonionic Bonding Patents (Class 544/276)
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Publication number: 20120245140Abstract: N-containing heteroaryl derivatives of formula I or II, wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as JAK, particularly JAK3, kinase inhibitors.Type: ApplicationFiled: October 29, 2010Publication date: September 27, 2012Inventors: Carmen Almansa Rosales, Jorge Salas Solana, Robert Soliva Soliva, Sergio Rodríguez Escrich, Maria Cristina Sicre Gonzåles
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Publication number: 20120232073Abstract: The present invention relates to Fused Bicyclic Pyrimidine Derivatives, compositions comprising a Fused Bicyclic Pyrimidine Derivative, and methods of using the Fused Bicyclic Pyrimidine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) in a patient.Type: ApplicationFiled: November 16, 2010Publication date: September 13, 2012Inventors: Santhosh Francis Neelamkavil, Dipshikha Biswas, Samuel Chackalamannil, Bernard R. Neustadt, Andrew Stamford, Hong Liu
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Publication number: 20120232077Abstract: The invention features compounds of formula (I): The compounds are useful as antibacterial agents, especially again Clostridium difficile-associated diseases.Type: ApplicationFiled: September 10, 2010Publication date: September 13, 2012Inventors: George E. Wright, Wei-Chu Xu
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Publication number: 20120220586Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphoType: ApplicationFiled: May 10, 2012Publication date: August 30, 2012Applicant: Amgen Inc.Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer Seganish, Youngsook Shin, Dawei Zhang
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Patent number: 8252805Abstract: The present invention provides novel polymorphs of lapatinib ditosylate, processes for preparing them, and pharmaceutical compositions comprising one or more of these polymorphs.Type: GrantFiled: May 7, 2009Date of Patent: August 28, 2012Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Leonid Metsger, Ariel Mittelman, Slavik Yurkovski
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Publication number: 20120213758Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.Type: ApplicationFiled: April 27, 2012Publication date: August 23, 2012Applicant: DeCODE Genetics enfInventors: Jasbir SINGH, Mark E. GURNEY, Alex BURGIN, Alexander KISELYOV, Munagala RAO, Timothy HAGEN
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Publication number: 20120202998Abstract: Disclosed are a novel, high-yield method for preparing entecavir and intermediates used therein.Type: ApplicationFiled: September 15, 2010Publication date: August 9, 2012Applicant: HANMI HOLDINGS CO., LTD.Inventors: Jae Heon Lee, Gha Seung Park, Jin Hee Kim, Tae Jin Choi, Ji Eun Lee, Jung Hee Han, Hyo Jeong Bang, Sun Young Jung, Young Kil Chang, Gwan Sun Lee, Maeng Sup Kim
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Publication number: 20120190850Abstract: The present invention provides a novel process for the preparation of pure valganciclovir hydrochloride.Type: ApplicationFiled: August 12, 2010Publication date: July 26, 2012Applicant: RANBAXY LABORATORIES LIMITEDInventors: Mohammed Salman Hashmi, Mukesh Kumar Sharma, Chandra Has Khanduri
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Publication number: 20120190697Abstract: HIV replication inhibitors of formula wherein -a1=a2-a3=a4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; -b1=b2-b3=b4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; n and m is 0-4, R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; polyhalomethyl; polyhalomethylthio; —S(?O)pR6; C(?NH)R6; R2a is CN; amino; substituted amino; C1-6alkyl; halo; C1-6alkyloxy; carbonyl; —CH?N—NH—C(?O)—R16; C1-6alkyloxyC1-6alkyl; C2-6alkenyl or C2-6alkynyl; —C(?N—O—R8)—C1-4alkyl; R7 or —X—R7; R3 is CN; amino; C1-6alkyl; halo; C1-6alkyloxy; substituted carbonyl; —CH?N—NH—C(?O)—R16; substituted C1-6alkyl; C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(?N—O—R8)—C1-4alkyl; R7; —X—R7; R4 is halo; OH; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; CN; nitro; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; substitutedType: ApplicationFiled: March 2, 2012Publication date: July 26, 2012Inventors: Jerôme Emile Georges GUILLEMONT, Mikaël Paugam, Bruno Francois Marie Delest, Jan Heeres, Paulus Joannes Lewi, Frank Xavier Jozef Herwig Arts
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Publication number: 20120184516Abstract: Compounds of Formula I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.Type: ApplicationFiled: June 30, 2011Publication date: July 19, 2012Inventors: Charles Kim, Takashi Nakai, Thomas Wai-Ho Lee, Joel Moore, Nicholas Robert Perl, Jason Rohde, Rajesh R. Iyengar, Ara Mermerian
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Patent number: 8222263Abstract: The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.Type: GrantFiled: March 14, 2008Date of Patent: July 17, 2012Assignee: Exelixis Patent Company LLCInventors: Suleyman Bahceci, William Bajjalieh, Jeff Chen, Sergey Epshteyn, Timothy Patrick Forsyth, Tai Phat Huynh, Byung Gyu Kim, James W. Leahy, Matthew Sangyup Lee, Gary L. Lewis, Morrison B. Mac, Grace Mann, Charles K. Marlowe, Brian Hugh Ridgway, Joan C. Sangalang, Xian Shi, Craig Stacy Takeuchi, Yong Wang
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Patent number: 8222257Abstract: Compounds and compositions are provided for treatment, prevention, or amelioration of a variety of medical disorders associated with viral infections and/or cell proliferation. The compounds provided herein are 5-phosphono-pent-2-en-1-yl nucleosides and esters thereof.Type: GrantFiled: March 30, 2006Date of Patent: July 17, 2012Assignee: The Regents of the University of CaliforniaInventors: Karl Y. Hostetler, James R. Beadle, Hyunah Choo
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Publication number: 20120178743Abstract: An antiallergic agent for topical administration containing an adenine compound of general formula (1): [wherein ring A represents a 6 to 10 membered, mono or bicyclic, aromatic hydrocarbon or a 5 to 10 membered, mono or bicyclic, aromatic heterocycle containing one to three heteroatoms selected among 0 to 2 nitrogen atoms, 0 or 1 oxygen atom, and 0 or 1 sulfur atom; n is an integer of 0 to 2; m is an integer of 0 to 2; R represents halogeno, (un)substituted alkyl, etc.; X1 represents oxygen, sulfur, NR1 (R1 represents hydrogen or alkyl), or a single bond; Y1 represents a single bond, alkylene, etc.; Y2 represents a single bond, alkylene, etc.; Z represents alkylene; and at least one of Q1 and Q2 represents —COOR10 (wherein R10 represents (un)substituted alkyl, etc.), etc.] or a pharmaceutically acceptable salt of the compound.Type: ApplicationFiled: February 22, 2012Publication date: July 12, 2012Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Yoshiaki ISOBE, Haruo Takaku, Haruhisa Ogita, Masanori Tobe, Ayumu Kurimoto, Tetsuhiro Ogino, Hitoshi Fujita
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Patent number: 8217050Abstract: The invention provides a compound which is (a) an amino acid derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate or solvate thereof: wherein R1, R2, L1, Het, A, x, y and W are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.Type: GrantFiled: November 5, 2007Date of Patent: July 10, 2012Assignee: Chroma Therapeutics LimitedInventors: David Festus Charles Moffat, Simon Christopher Hirst, Stuart Thomas Onions
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Publication number: 20120172591Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K? plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.Type: ApplicationFiled: February 17, 2012Publication date: July 5, 2012Applicant: ICOS CORPORATIONInventors: Chanchal Sadhu, Ken Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
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Publication number: 20120164172Abstract: An agent that stimulates antiviral immunity may be used, for the treatment of cancer. A product comprising an immunostimulant and a vector comprising a transgene that promotes death of neoplastic cells, may also be used for simultaneous, sequential or separate administration in the treatment of cancer.Type: ApplicationFiled: September 23, 2010Publication date: June 28, 2012Inventors: Timothy Farries, David Eckland
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Publication number: 20120148660Abstract: The invention provides TLR agonists and conjugates thereof useful in vaccines and to prevent, inhibit or treat a variety of disorders including pathogen infection and asthma.Type: ApplicationFiled: February 7, 2008Publication date: June 14, 2012Applicant: Regents of the University of California, San Diego UCSD Technology Transfer OfficeInventors: Dennis A. Carson, Howard B. Cottam, Wolfgang Wrasidlo, Christina C.N. Wu, Gregory A. Daniels
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Patent number: 8193182Abstract: Chemical entities of Formula I: that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with P13 kinase activity are described herein.Type: GrantFiled: July 15, 2009Date of Patent: June 5, 2012Assignee: Intellikine, Inc.Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan, Christian Rommel
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Publication number: 20120129800Abstract: The present invention concerns an agent for prevention and treatment of pityriasis. The agent according to the present invention comprises at least one transaminase inhibitor effectively inhibiting the transamination process which is of pathogenetic relevance for the disease, prevents a recurrence of the disease and which protects the human skin flora. Upon release into the environment, no resistances are induced in other fungi.Type: ApplicationFiled: January 14, 2010Publication date: May 24, 2012Applicant: Justus-Liebig-Universitat GiessenInventor: Peter Mayser
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Patent number: 8183238Abstract: Compounds of Formula X: wherein A, X, Y, Z, R5, R6a, and R6b are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other neurodegenerative and/or neurological disorders in mammals, including humans.Type: GrantFiled: June 16, 2010Date of Patent: May 22, 2012Assignee: Pfizer Inc.Inventors: Michelle M. Claffey, Amy B. Dounay, Matthew M. Hayward, Suobao Rong, Patrick R. Verhoest, Jamison B. Tuttle, Xinmin Gan
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Publication number: 20120123119Abstract: Methods and novel intermediates for the preparation of and the treatment with acyclic nucleoside derivatives of the formula: where one of R1 and R2 is an amino acid acyl group and the other of R1 and R2 is a —C(O)C3—C21 saturated or monounsaturated, optionally substituted alkyl and R3 is OH or H.Type: ApplicationFiled: January 20, 2012Publication date: May 17, 2012Applicant: Medivir ABInventors: Per ENGELHARDT, Marita Hogberg, Xiao-Xiong Zhou, Nils-Gunnar Johansson, Bjorn Lindborg
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Publication number: 20120115864Abstract: The present invention discloses substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases.Type: ApplicationFiled: March 12, 2010Publication date: May 10, 2012Inventors: Venkata Palle, Vidya Ramdas, Dinesh Barawkar, Sujay Basu, Summon Koul, Yogesh Waman, Meena Patel, Anil Panmand
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Patent number: 8163479Abstract: The invention relates to substrates for O6-alkylguanine-DNA alkyltransferases (AGT) of formula R1-A-X—CH2—R3—R4-L1, wherein A is a group recognized by AGT as a substrate, X is oxygen or sulfur, R1 is a group —R2-L2 or a group R5, R2 and R4 are, independently of each other, a linker, R3 is an aromatic or a heteroaromatic group, or an optionally substituted unsaturated alkyl, cycloalkyl or heterocyclyl group with the double bond connected to CH2, R5 is arylmethyl or heteroarylmethyl or an optionally substituted cycloalkyl, cycloalkenyl or heterocyclyl group, L1 is a label, a plurality of same or different labels, a bond connecting R4 to A forming a cyclic substrate, or a further group —R3—CH2—X-A-R1, and L2 is a label or a plurality of same or different labels. The invention further relates to methods of transferring a label from these substrates to O6-alkylguanine-DNA alkyltransferases (AGT) and AGT fusion proteins.Type: GrantFiled: March 1, 2005Date of Patent: April 24, 2012Assignee: Ecole Polytechnique Federale de LausanneInventors: Hughes Jaccard, Kai Johnsson, Maik Kindermann, India Christina Sielaff
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Publication number: 20120095077Abstract: Disclosed are compositions and methods related to modified nucleobases. Also disclosed are compositions and methods related to modified interfering RNAs. Also disclosed are compositions and methods related to modified guanine bases for controlling off-target effects in RNA interference.Type: ApplicationFiled: March 23, 2010Publication date: April 19, 2012Applicant: UNIVERSITY OF UTAH RESEARCH FOUNDATIONInventors: Cynthia J. Burrows, Arunkumar Kannan, Peter A. Beal
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Publication number: 20120088765Abstract: Disclosed are: a novel purine derivative, a composition thereof, a method for treating tumor using the purine derivative, and an antitumor agent using the purine derivative. Specifically disclosed is a compound represented by formula (I), or a pharmaceutically acceptable salt, solvate or hydrate thereof, or a prodrug thereof.Type: ApplicationFiled: April 28, 2010Publication date: April 12, 2012Applicant: Zenyaku Kogyo KabushikikaishaInventors: Toshiaki Suzuki, Hideki Satoh, Toshiyuki Matsuno, Kenichi Saitoh, Soichi Ohta, Manami Masuda, Shinichi Yaguchi, Ichiro Koshimizu, Yuriko Watanabe, Yoshie Minowa, Masayuki Takahashi, Tomoyoshi Kayou
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Publication number: 20120083500Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.Type: ApplicationFiled: December 8, 2011Publication date: April 5, 2012Inventors: Li CHEN, Michael Patrick DILLON, Lichun FENG, Minmin YANG
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Patent number: 8148371Abstract: A drug for topically administration which is effective as an antiallergic agent. The drug for topically administration contains as an active ingredient an adenine compound represented by the general formula (1): [wherein ring A represents a 6 to 10 membered, mono or bicyclic, aromatic hydrocarbon or a 5 to 10 membered, mono or bicyclic, aromatic heterocycle containing one to three heteroatoms selected among 0 to 2 nitrogen atoms, 0 or 1 oxygen atom, and 0 or 1 sulfur atom; n is an integer of 0 to 2; m is an integer of 0 to 2; R represents halogeno, (un)substituted alkyl, etc.; X1 represents oxygen, sulfur, NR1 (R1 represents hydrogen or alkyl), or a single bond; Y1 represents a single bond, alkylene, etc.; Y2 represents a single bond, alkylene, etc.; Z represents alkylene; and at least one of Q1 and Q2 represents —COOR10 (wherein R10 represents (un)substituted alkyl, etc.), etc.] or a pharmaceutically acceptable salt of the compound.Type: GrantFiled: June 3, 2010Date of Patent: April 3, 2012Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Yoshiaki Isobe, Haruo Takaku, Haruhisa Ogita, Masanori Tobe, Ayumu Kurimoto, Tetsuhiro Ogino, Hitoshi Fujita
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Patent number: 8138172Abstract: The present invention provides 8-oxoadenine derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The 8-oxoadenine derivatives act as modulators of Toll-like Receptor (TLR) 7 and thus may be used in the treatment of asthma, hepatitis, allergic diseases, viral and bacterial infection as well as cancer.Type: GrantFiled: July 3, 2007Date of Patent: March 20, 2012Assignees: AstraZeneca AB, Dainippon Sumitomo Pharma Co Ltd.Inventors: Anthony Cook, Tom McInally, Stephen Thom, Hiroki Wada
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Patent number: 8124417Abstract: A method is herein presented for analyzing nucleobases on a single molecular basis (a single molecule detection), which comprises scanning a molecular tip chemically modified with the complementary nucleobase on the nucleobases, and measuring the tunneling currents between the scanned nucleobases and the molecular tips with scanning tunneling microscopy.Type: GrantFiled: December 28, 2005Date of Patent: February 28, 2012Assignee: Japan Science and Technology AgencyInventors: Yoshio Umezawa, Takahito Ohshiro
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Publication number: 20120040982Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R4 are as defined herein, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: October 25, 2011Publication date: February 16, 2012Applicant: BOEHRINGER INGELHEIM PHARMA & CO. KGInventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf LOTZ
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Publication number: 20120040918Abstract: The present invention provides a novel class of peptide nucleic acid derivatives, which show good cell penetration and strong binding affinity for nucleic acid.Type: ApplicationFiled: March 13, 2009Publication date: February 16, 2012Applicant: CTI BIOInventors: Jong-Ook Lee, Shin Chung, Heui-Yeon Kim, Hyun-Jin Park, Mi-Ran Kim
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Publication number: 20120010408Abstract: Preparation of acyclovir 2/3 hydrate comprises mixing acyclovir with water at weight ratio of 1:5˜50, dissolving at 50˜100° C., filtering, cooling filtrate at 0˜30° C. to precipitate crystal, collecting the crystal by filtration, and drying the crystal at 0˜150° C. for 0.5˜24 hours to obtain acyclovir 2/3 hydrate. The preparation process is simple and suitable for industrial production. The prepared product has good and stable crystal form.Type: ApplicationFiled: March 17, 2010Publication date: January 12, 2012Applicant: Zhejiang Charioteer Pharmaceutical CO., LTDInventors: Tong Pu, Yi Fan, Tian Chen, Ming Lei, Naixing Wang, Zhen Yang
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Publication number: 20120004212Abstract: A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.Type: ApplicationFiled: August 26, 2011Publication date: January 5, 2012Inventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
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Publication number: 20110319394Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia. The compound is represented by the formula (I): wherein the symbols are defined in the specification.Type: ApplicationFiled: June 22, 2011Publication date: December 29, 2011Inventors: Takahiko TANIGUCHI, Masato YOSHIKAWA, Kasei MIURA, Tomoaki HASUI, Eiji HONDA, Keisuke IMAMURA, Makoto KAMATA, Haruhi KAMISAKI, John F. QUINN, Joseph RAKER, Fatoumata CAMARA, Yi WANG
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Publication number: 20110306610Abstract: The present invention provides an 8-oxoadenine compound having immunemodulating activities such as an interferon inducing activity and useful as an antiviral agent and antiallergic agent, which is represented by the following formula (1): [wherein the ring A represents a 6-10 membered aromatic carbocyclic ring and the like, R represents a halogen atom, an alkyl group and the like, n represents an integer of 0-2, Z1 represents alkylene, X2 represents oxygen atom, sulfur atom, SO2, NR5, CO, CONR5, NR5CO and the like, Y1, Y2 and Y3 represent independently a single bond or an alkylene group, X1 represents oxygen atom, sulfur atom, NR4 (R4 is hydrogen atom or an alkyl group) or a single bond, R2 represents a substituted or unsubstituted alkyl group, R1 represents hydrogen atom, hydroxy group, an alkoxy group, an alkoxycarbonyl group or a haloalkyl group] or its pharmaceutically acceptable salt.Type: ApplicationFiled: July 20, 2011Publication date: December 15, 2011Applicants: AstraZeneca Aktiebolag, Dainippon Sumitomo Pharma Co., Ltd.Inventors: Ayumu KURIMOTO, Kazuki Hashimoto, Yoshiaki Isobe, Stephen Brough, Ian Millichip, Hiroki Wada, Roger Bonnert, Thomas Mcinally
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Patent number: 8071609Abstract: This invention relates to compounds of the general formula: in which Q is an ethynyl or ethenyl moiety; Ring A is an aryl, heteroaryl or heterocyclic ring or ring system; and the remaining variable groups are as defined herein, and to their preparation and use.Type: GrantFiled: August 11, 2006Date of Patent: December 6, 2011Assignee: ARIAD Pharmaceuticals, Inc.Inventors: Yihan Wang, Wei-Sheng Huang, Rajeswari Sundaramoorthi, Xiaotian Zhu, R. Mathew Thomas, William C. Shakespeare, David C. Dalgarno, Tomi K. Sawyer
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Patent number: 8067411Abstract: The present invention provides compounds of formula wherein R1, Y1, X1, Z1, X2, Y2, A, n and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: December 13, 2007Date of Patent: November 29, 2011Assignees: AstraZeneca AB, Dainippon Sumitomo Pharma Co., Ltd.Inventors: Roger Victor Bonnert, Thomas McInally, Tobias Mochel, Stephen Thom
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Patent number: 8067426Abstract: Compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.Type: GrantFiled: August 7, 2009Date of Patent: November 29, 2011Assignee: GlaxoSmithKline LLCInventors: Keith Biggadike, Diane Mary Coe, Xiao Qing Lewell, Charlotte Jane Mitchell, Stephen Allan Smith, Naimisha Trivedi
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Patent number: 8067413Abstract: The present invention provides compounds of formula (I) wherein R1, Y1, X1, L and R2 are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: March 19, 2008Date of Patent: November 29, 2011Assignees: AstraZeneca AB, Dainippon Sumitomo Pharma Co., Ltd.Inventors: Roger Victor Bonnert, Thomas McInally, Stephen Thom
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Patent number: 8063051Abstract: The present invention provides compounds of formula where n, R1, R2, A, X1, Y1, Z1, X2 and Y2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: March 19, 2008Date of Patent: November 22, 2011Assignees: AstraZeneca AB, Dainippon Sumitomo Pharma Co., Ltd.Inventors: Roger Victor Bonnert, Thomas McInally, Stephen Thom
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Publication number: 20110275590Abstract: The present invention relates to conjugates of a drug and an amino acid or an amino acid derivative or analog, pharmaceutical compositions that include the conjugates and methods of use thereof. In particular, the present invention relates to conjugates of anti-proliferative drugs and asparagine and glutamine and analogs thereof as compositions for treatment of cancer, and conjugates of imaging agent carriers and amino acids for the diagnosis of tumors and metastases.Type: ApplicationFiled: June 20, 2011Publication date: November 10, 2011Inventors: Stela Gengrinovitch, Esther Izakovich
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Publication number: 20110275652Abstract: Compounds which are active against viruses have the following formulas: wherein B is a purine or pyrimidine heterocyclic ring or base. In a preferred embodiment, the purine include 6-aminopurine (adenine), 6-hydroxypurine (hypoxanthine), 2-amino-6-hydroxypurine (guanine), 2,6-diamino-purine, 2-amino-6-azidopurine, 2-amino-6-halo substituted purines such as 2-amino-6-chloropurine, 2-amino-6-fluoropurine, 2-amino-6-alkoxypurines such as 2-amino-6-methoxypurine, 2-amino-6-cyclopropylaminopurine, 2-amino-6-alkylamino or 2-amino-6-dialkylamino substituted purines, 2-amino-6-thiopurine, 2-amino-6-alkylthio substituted purines, 3-deazapurines, 7-deazapurines and 8-azapurines. The pyrimidine incorporates cytosine, uracil and thymine, 5-halo substituted cytosines and uracils, 5-alkyl substituted cytosines and uracils including derivatives with a saturated or unsaturated alkyl group and 6-azapyrimidines.Type: ApplicationFiled: July 15, 2011Publication date: November 10, 2011Inventors: Jiri Zemlicka, Shaoman Zhou, John C. Drach
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Publication number: 20110269780Abstract: Disclosed are small molecule inhibitors of the formula (I): and the pharmaceutical compositions thereof and processes of making the same. The compounds are useful in treating various diseases and conditions involving chymase.Type: ApplicationFiled: August 25, 2009Publication date: November 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Michel Jose Emmanuel, Xin Guo, Jin Mi Kim, Ho Yin Lo, Peter Allen Nemoto, Kevin Chungeng Qian
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Publication number: 20110262661Abstract: An optical performance humidity dependency improving agent for cellulose acylate film, which contains a compound having a nucleic acid base skeleton, is capable of preventing the fluctuation of Re and Rth of the film against the humidity change in usage environments.Type: ApplicationFiled: April 21, 2011Publication date: October 27, 2011Applicant: FUJIFILM CorporationInventors: Masato Nagura, Aiko Yoshida, Naoyuki Nishikawa
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Patent number: 8044056Abstract: A novel adenine compound represented by the formula (1): [wherein R1 is substituted or unsubstituted alkyl, etc., X is oxygen, etc., A1 is 4- to 8-membered substituted or unsubstituted saturated nitrogen-containing heterocycle containing 1 to 2 hetero atom(s) selected from 1 to 2 nitrogen(s), 0 to 1 oxygen and 0 to 1 sulfur, etc., A2 is substituted or unsubstituted 6- to 10-membered aryl, etc., L1 and L2 are independently a straight chain or branched chain alkylene, etc.], or a pharmaceutically acceptable salt thereof, which is useful as a medicament.Type: GrantFiled: March 19, 2008Date of Patent: October 25, 2011Assignees: Dainippon Sumitomo Pharma Co., Ltd., AstraZeneca AktiebolagInventors: Yoshiaki Isobe, Tomoaki Nakamura
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Publication number: 20110251387Abstract: The present invention relates to a novel, high-yield and low-cost method for preparing entecavir, [1-S-(1?,3?,4?)]-2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-6H-purin-6-one, an antiviral agent, and novel intermediates used therein.Type: ApplicationFiled: December 24, 2009Publication date: October 13, 2011Applicant: HANMI HOLDINGS CO., LTD.Inventors: Jaeheon Lee, Gha-Seung Park, Jin Hee Kim, Ji Eun Lee, Chul Hyun Park, Tae Jin Choi, Eun-Ju Park, Cheol Kyung Kim, Eun Jung Lim, Young-Kil Chang, Gwan Sun Lee
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Publication number: 20110245458Abstract: Disclosed is a peptide nucleic acid monomer as well as a corresponding peptide nucleic acid molecule. The monomer comprises a terminal amino group and a terminal group A. The terminal amino group and the terminal group A are connected by an aliphatic moiety. The main chain of this aliphatic moiety is free of groups that are charged under physiological conditions. The terminal group A is one of —COOH, —COOR3, —COX, —COSR3, —CN, —CONH2, —CONHR3, —CONR3, R4, with R3 and R4 being H or an aliphatic, alicyclic, aromatic, arylaliphatic or arylalicyclic group, and X being a halogen atom. The terminal amino group is substituted by an aliphatic group with a main chain of at least two carbon atoms and optionally 0 to a bout 2 heteroatoms selected from the group N, O, S, Se and Si. The main chain has a polar head group Z.Type: ApplicationFiled: September 3, 2008Publication date: October 6, 2011Applicant: NANYANG TECHONOLOGICAL UNIVERSITYInventors: Chuan Fa Liu, Yun Zeng, Xiao Wei Lu
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Publication number: 20110236952Abstract: The invention relates to compounds of formula (I?): in which A, L2, M and B are as defined in the description.Type: ApplicationFiled: September 22, 2009Publication date: September 29, 2011Applicant: CIS BIO InternationalInventors: Emmanuel Bourrier, Michel Laget, Laurent Lamarque, Norbet Tinel, Eric Trinquet, Hervé Bazin
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Patent number: 8026245Abstract: The present invention relates to the use of a compound of formula (I) for the manufacture of a medicament for the prevention or the treatment of HIV infection wherein the compound of formula (I) is a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein A and B each represents a radical of formula and wherein —C-D- represents a bivalent radical of formula —N?CH—NR17—??(c-1); or —NR17—CH?N—??(c-2); provided that when A represents a radical of formula (a) then B represents a radical of formula (b) and when A represents a radical of formula (b) then B represents a radical of formula (a).Type: GrantFiled: September 21, 2004Date of Patent: September 27, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts, legal representative, Paulus Joannes Lewi, Marc René de Jonge, Lucien Maria Henricus Koymans, Frederik Frans Desiré Daeyaert, Jan Heeres, Hendrik Maarten Vinkers, Ruben Gerardus George Leenders, Dirk Alfons Leo Vandenput
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Publication number: 20110230659Abstract: Provided is a compound having at least one selected from the group consisting of cell growth promoting activity, angiogenesis promoting activity, lumen formation promoting activity, cell migration promoting activity, and neurocyte growth promoting activity, which is a chemically stable low-molecular-weight substance that has high absorbability and can be supplied stably at a low cost because of its low molecular weight. A cyclobutyl purine derivative, a tautomer or stereoisomer thereof, or a salt, solvate, or hydrate thereof according to the present invention is a cyclobutyl purine derivative represented by the following general formula (1), a tautomer or stereoisomer thereof, or a salt, solvate, or hydrate thereof.Type: ApplicationFiled: November 27, 2009Publication date: September 22, 2011Applicant: NATIONAL UNIVERSITY CORPORATION KAGAWA UNIVERSITYInventors: Ikuko Tsukamoto, Ryoji Konishi, Masaaki Tokuda, Yasuo Kubota, Tokumi Maruyama, Hiroaki Kosaka, Junsuke Igarashi