Nitrogen Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/316)
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Publication number: 20100240653Abstract: The present invention relates to certain biphenyl sulfonamide derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the histamine H3-receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders, such as, cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness such as narcolepsy, shift-work syndrome, drowsiness as a side effect from a medication, maintenance of vigilance to aid in completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, dementia, Alzheimer's disease and the like.Type: ApplicationFiled: October 16, 2007Publication date: September 23, 2010Inventors: Vincent J. Santora, Ryan M. Hart, Jason B. Ibarra, Douglas M. Park, Albert S. Ren, Graeme Semple, Jeffrey A. Schultz, Brian M. Smith, Jeffrey Smith
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Patent number: 7799914Abstract: The present invention provides a process for the preparation of a compound of formula (I): wherein X is halogen; Y is ZR1; Z is oxygen or sulphur; and R1 is C1-6 alkyl, C1-6 haloalkyl or C3-7 cycloalkyl; the process comprising either: a. hydrogenating a compound of formula (II): with a suitable transition metal catalyst in a C1-6 aliphatic alcohol, an ether, an ester or a hydrocarbon as solvent; or, b. conducting a one-pot hydrogenation of a compound of formula (III): wherein R2 is phenyl optionally substituted by chloro, C1-6 alkyl, C1-6 alkoxy or (C1-6 alkyl)2N; i. firstly at about 20° C. to form a compound of formula (IV): ii. and then at about 40° C.; both steps (i) and (ii) being carried out in the presence of a suitable catalyst and in the presence of a suitable solvent.Type: GrantFiled: March 29, 2005Date of Patent: September 21, 2010Assignee: AstraZeneca ABInventors: Ulf Larsson, Kajsa Radevik
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Publication number: 20100233116Abstract: The present invention provides heterocyclic derivatives hat modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: August 13, 2007Publication date: September 16, 2010Inventors: Natalie Dales, Julia Fonarev, Jianmin Fu, Rajender Kamboj, Vishnumurthy Kodumuru, Shifeng Liu, Natalia Pokrovskaia, Vandna Raina, Shaoyi Sun, Zaihui Zhang
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Publication number: 20100234346Abstract: The invention relates to novel pyrimidine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.Type: ApplicationFiled: October 31, 2008Publication date: September 16, 2010Inventors: Martin Bolli, Cyrille Lescop, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner
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Patent number: 7786132Abstract: The invention relates to aminopyrimidine compounds useful for treating diseases mediated by polo-like kinase 1 (Plk1). The invention also relates to the therapeutic use of such aminopyrimidine compounds and compositions thereof in treating disease states associated with abnormal cell growth and unwanted cell proliferation.Type: GrantFiled: December 16, 2005Date of Patent: August 31, 2010Assignee: Amgen Inc.Inventors: Adrian Leonard Smith, Paul Edward Brennan, Frenel Fils DeMorin, Gang Liu, Nick A. Paras, Daniel Martin Retz, Elizabeth Rainbeau
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Publication number: 20100216758Abstract: An active ingredient is a compound represented by the general formula [I]: [wherein R1 and R2 represent a lower alkyl group, a C3-6 cycloalkyl group or the like, X1 and X2 represent methine, an Ar—Y1—Y2—Y3-substituted methine or the like, however either of them is an Ar—Y1—Y2—Y3-substituted methine, X3 to X8 represent methine, —N— or the like, Y1 and Y3 represent a single bond, —O— or the like, Y2 represent a single bond, a lower alkylene group or the like, W represent —(O)—(CH2)n-(O)— or the like, n represents an integer of 1 to 4, L and Z2 represent a single bond or a methylene group, Z1 represents a single bond, a C1-4 alkylene group or the like, and Ar represents an aromatic carbocyclic group or the like]. The compound acts as a melanin-concentrating hormone receptor antagonist and useful as a therapeutic agent for obesity or the like.Type: ApplicationFiled: August 3, 2006Publication date: August 26, 2010Inventors: Makoto Ando, Etsuko Sekino, Yuji Haga, Norikazu Otake, Minoru Moriya
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Publication number: 20100210637Abstract: Provided are compounds of a formula (I) and their pharmaceutically-acceptable salts: wherein X1, X2 and X3 each independently represent N or CH; W represents the following formula (II): or the following formula (III): Y represents a group of a formula (IV): The compounds have a histamine-H3 receptor antagonistic or inverse-agonistic activity and are useful for remedy and/or prevention of obesity, diabetes, hormone secretion disorders, sleep disorders, etc.Type: ApplicationFiled: August 13, 2009Publication date: August 19, 2010Inventors: Norikazu Ohtake, Akira Naya, Yuji Haga, Makoto Jitsuoka, Takuya Suga, Ryo Yoshimoto, Shigeru Tokita, Akio Kanatani
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Publication number: 20100204245Abstract: The present invention provides an amino-pyridine compound of formula I The present invention also provides methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tangles.Type: ApplicationFiled: April 20, 2010Publication date: August 12, 2010Applicant: Wyeth LLCInventors: Michael Sotirios Malamas, William Floyd Fobare, William Ronald Solvibile, JR., Frank Eldridge Lovering, Jeffrey Scott Condon, Albert Jean Robichaud
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Publication number: 20100197711Abstract: The present invention relates to benzothiazole compounds that mimic the activity of BH3 only proteins and are capable of binding to and neutralizing pro survival Bcl 2 proteins. The invention also relates to the use of such compounds in the regulation of cell death or cell survival and the treatment and/or prophylaxis of diseases or conditions associated with the deregulation of cell death or cell survival.Type: ApplicationFiled: September 27, 2007Publication date: August 5, 2010Inventors: Keith Geoffrey Watson, Guillaume Laurent Lessene, Jonathan Bayldon Baell, David Ching Siang Huang, Ian Philip Street, Jerry McKee Adams, Peter Malcolm Colman, Brad Edmund Sleebs, Brian John Smith, Peter Edward Czabotar
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Publication number: 20100197917Abstract: Novel compounds composition capable of inhibiting TNF? and having antiimmunionflammatory and autoimmune properties useful in a pharmaceutical composition, such as for a drug containing this as an active ingredient; and a therapeutic method with the use of these novel compounds.Type: ApplicationFiled: March 18, 2010Publication date: August 5, 2010Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Jie Fei Cheng, Thomas Arrhenius, David Wallace, Mi Chen, Sovouthy Tith, Hirotaka Kashiwagi, Yoshiyuki Ono, Yoshiaki Watanabe
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Patent number: 7767670Abstract: The invention provides methods and compositions for treating conditions mediated by various kinases wherein substituted 3-carboxamido isoxazoles compounds are employed. The invention also provides methods of using the compounds and/or compositions in the treatment of a variety of diseases and unwanted conditions in subjects.Type: GrantFiled: November 15, 2004Date of Patent: August 3, 2010Assignee: Ambit Biosciences CorporationInventors: Shamal A. Mehta, Robert M. Grotzfeld, Zdravko V. Milanov, Andiliy G. Lai, Hitesh K. Patel, David J. Lockhart
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Patent number: 7767672Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: GrantFiled: November 3, 2006Date of Patent: August 3, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Michael Mortimore, Chris Davis, Dean Boyall, Simon Everitt, Daniel Robinson, Sharn Ramaya, Damien Fraysse, John Studley, Andrew Miller, Michael O'Donnell, Alistair Rutherford, Joanne Pinder
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Publication number: 20100184767Abstract: The invention relates to novel substituted oxazolidinones, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders.Type: ApplicationFiled: June 7, 2008Publication date: July 22, 2010Inventor: Susanne Rohrig
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Publication number: 20100184788Abstract: The invention relates to novel heterocyclic derivatives of the general formula (I), 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: ApplicationFiled: December 8, 2009Publication date: July 22, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Heike GIELEN-HAERTWIG, Barbara Albrecht, Jörg Keldenich, Volkhart Li, Josef Pernerstorfer, Karl-Heinz Schlemmer, Leila Telan
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Publication number: 20100178710Abstract: A mass label for labelling and detecting a biological molecule by mass spectroscopy, which label comprises the following structure: X-L-M wherein X is a mass marker moiety comprising the following group: formula (I), wherein the cyclic unit is aromatic or aliphatic and comprises from 0-3 double bonds independently between any two adjacent atoms; each Z is independently N, N(R1), C(R1), CO, CO(R1), C(R1)2, O or S; X is N, C or C(R1); each R1 is independently H, a substituted or unsubstituted straight or branched C1-C6 alkyl group, a substituted or unsubstituted aliphatic cyclic group, a substituted or unsubstituted aromatic group or a substituted or unsubstituted heterocyclic group; and y is an integer from 0-10, L is a cleavable linker comprising an amide bond and M is a mass normalization moiety.Type: ApplicationFiled: July 26, 2006Publication date: July 15, 2010Applicant: Electrophoretics LimitedInventors: Christian Hamon, Josef Schwarz, Wolfgang Becker, Stefan Kienle, Karsten Kuhn, Juergen Schaefer
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Publication number: 20100174076Abstract: Novel compounds composition capable of inhibiting TNF? and having antiimmunionflammatory and autoimmune properties useful in a pharmaceutical composition, such as for a drug containing this as an active ingredient; and a therapeutic method with the use of these novel compounds.Type: ApplicationFiled: March 18, 2010Publication date: July 8, 2010Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Jie Fei Cheng, Thomas Arrhenius, David Wallace, Mi Chen, Sovouthy Tith, Hirotaka Kashiwagi, Yoshiyuki Ono, Yoshiaki Watanabe
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Publication number: 20100168102Abstract: The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula (I) or (II) or a stereoisomer tautomer, racemic, metabolite, pro- or predrug, salt, hydrate, or solvate thereof, wherein Ar1, Ar2, R1, R3, p and n have the meaning defined in the claims In particular, the present invention relates to more specifically AGC kinases inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease.Type: ApplicationFiled: July 11, 2006Publication date: July 1, 2010Applicant: Devgen NVInventors: Olivier Raynald Defert, Gert De Wilde, Petra Blom, Dirk Casimir Maria Leysen, Thomas Brown, Nadzeya Kaval
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Publication number: 20100168088Abstract: The present invention relates to a compound of formula I wherein Ar1, Ar2, R1, R2, R3, n, o, and p are as described herein or to a pharmaceutically active salt, to all stereoisomeric forms, including individual diastereoisomers and enantiomers as well as to racemic and non-racemic mixtures thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: October 2, 2009Publication date: July 1, 2010Inventors: Caterina Bissantz, Philippe Jablonski, Henner Knust, Matthias Nettekoven, Angélique Patiny-Adam, Hasane Ratni, Claus Riemer
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Publication number: 20100160629Abstract: The present invention provides a cyclic amide derivative useful as a drug for treating thrombosis, which is represented by the formula (I): wherein R1 represents an optionally substituted cyclic hydrocarbon group or an optionally substituted heterocyclic group, W represents a bond or an optionally substituted divalent chain hydrocarbon group, a represents 0, 1, or 2, X1 represents an optionally substituted lower alkylene or an optionally substituted lower alkenylene, Y1 represents —C(O)—, —S(O)— or —S(O)2—, A represents a piperazine ring which may be further substituted or a piperidine ring which may be further substituted, X2 represents a bond or an optionally substituted lower alkylene, Y2 represents —C(O)—, —S(O)—, —S(O)2— or —C(?NR7)—, X3 represents an optionally substituted C1-4 alkylene or an optionally substituted C2-4 alkenylene, Z3 represents —N(R4)—, —O— or a bond, Z1 represents —C(R2)(R2?)—, —N(R2)—, etc., and Z2 represents —C(R3)(R3?)—, —N(R3)—, etc., or a salt thereof.Type: ApplicationFiled: March 2, 2010Publication date: June 24, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Keiji KUBO, Yasuhiro Imaeda
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Publication number: 20100152207Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure, wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: ApplicationFiled: April 4, 2008Publication date: June 17, 2010Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Willy Moree, Martin Rowbottom, Warren Wade, Liren Zhao, Richard Lowe, Nicole Smith, Neil Ashweek, Yun-Fei Zhu
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Publication number: 20100144701Abstract: Compounds of formula (I) suppress the normal signalling activity CB1 receptors, and are thus useful in the treatment of diseases or conditions which are mediated by CB1 receptor signalling activity, such as treatment of obesity and overweight, prevention of weigh gain, treatment of diseases and conditions directly or indirectly associated with obesity and overweight: wherein A1 is hydrogen, —COOH,or tetrazolyl; p and q are independently 0 or 1; A3 is phenyl or cycloalkyl, either of which is optionally substituted with R4 and/or R5; R4 and R5 are independently —R9, —CN, —F, —Cl, —Br, —OR9, —NR7R8, —NR7COR6, —NR7SO2R6, —COR6, —SR9, —SOR9, or —SO2R6; R6 is C1-C4 alkyl, cycloalkyl, —CF3 or —NR7R8; R7 and R8 are independently hydrogen, C1-C4 alkyl or cycloalkyl; R9 is hydrogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkoxy(C1-C4 alkyl)-, cycloalkyl, or fully or partially fluorinated C1-C4 alkyl; R1 (i) a bond; (ii) a divalent radical of formula —(CH2)aB1(CH2)b wherein a and b are independently O, 1, 2 or 3 provided thatType: ApplicationFiled: December 17, 2007Publication date: June 10, 2010Applicant: 7TM PHARMA A/SInventors: Martin Cooper, Jean-Marie Receveur, Thomas Hoegberg, Peter Aadal Nielsen, Jean-Michel Linget, Pia Marina Noeregaard, Anthony Murray, Emelie Bjurling
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Publication number: 20100144770Abstract: A compound having Formula I: or a pharmaceutically acceptable salt thereof, wherein X, R, R and R are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof. The compounds of Formula I are inhibitors of Casein kinase II (CK2) pathways.Type: ApplicationFiled: April 24, 2008Publication date: June 10, 2010Applicant: EXELIXIS, INC.Inventors: Elena S. Koltun, Patrick Kearney, Naing Aay, Arlyn Arcalas, Wai Ki Vicky Chan, Jeffry Kimo Curtis, Hongwang Du, Ping Huang, Brian Kane, Moon Hwan Kim, Michael Pack, Amy L. Tsuhako, Wei Xu, Cristiana A. Zaharia, Peiwen Zhou
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Publication number: 20100135954Abstract: A compound having Formula I or II (Formula I) or (Formula II), or a pharmaceutically acceptable salt thereof, wherein X, Z, R1, R2, R11 and R12 are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.Type: ApplicationFiled: April 25, 2008Publication date: June 3, 2010Applicant: EXELIXIS, INC.Inventors: Amy L. Tsuhako, Naing Aay, S. David Brown, Wai Ki Vicky Chan, Hongwang Du, Ping Huang, Brian Kane, Patrick Kearney, Moon Hwan Kim, Elena S. Koltun, Michael Pack, Wei Xu, Peiwen Zhou
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Publication number: 20100137303Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.Type: ApplicationFiled: June 2, 2009Publication date: June 3, 2010Inventors: Sandeep Raghunath Ghorpade, Manoj Ganpat Kale, Shahul Hameed Peer Mohamed, Anand Kumar Venkobachar Raichurkar, David Charles McKinney
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Publication number: 20100137336Abstract: 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: July 10, 2008Publication date: June 3, 2010Inventor: Christelle Boléa
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Publication number: 20100130739Abstract: Provided is a compound that has the ability to promote axonal outgrowth in combination with the ability to promote angiogenesis and can therefore be used to reduce central nerve injuries such as head injury and spinal cord injury, cerebral infarction, ischemic heart diseases such as myocardial infarction and organic angina, peripheral arterial occlusive diseases such as critical limb ischemia, or after-effects of these diseases. Specifically, the compound is represented by the following formula (I): in which Nx group is preferably a 6-membered aromatic ring containing two nitrogen atoms; R0, R1 and R2 are each independently a hydrogen atom, an alkyl group, an amino group or the like; E is an oxygen atom or an —NR8 group (wherein R8 is an alkyl group or the like); n is an integer of 0 to 5; X and Y are each a connecting bond, a cycloalkyl group, —CO— or the like; and Q is a hydrogen atom or a phenyl group.Type: ApplicationFiled: April 25, 2008Publication date: May 27, 2010Applicant: ASUBIO PHARMA CO., LTD.Inventors: Naohiro Takemoto, Kenji Murata, Norihito Murayama, Chikaomi Yamada
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Publication number: 20100120806Abstract: Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including, but not limited to, malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, and diseases caused by PDGFR-? kinase, PDGFR-? kinase, c-KIT kinase, cFMS kinase, c-MET kinase, and oncogenic forms, aberrant fusion proteins and polymorphs of any of the foregoing kinases.Type: ApplicationFiled: October 29, 2009Publication date: May 13, 2010Inventors: Daniel L. Flynn, Peter A. Petillo, Michael D. Kaufman
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Publication number: 20100121051Abstract: Compounds of the formula (I) wherein R1, R2, R3, R4, R5, R6, W, and Y are as described herein, or a tautomer, prodrug, solvate, or salt thereof. These compounds are useful as inhibitors of Urotensin II and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the interaction of Urotensin II with its receptor, including cardiovascular diseases. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds, and intermediates useful in these processes.Type: ApplicationFiled: May 12, 2008Publication date: May 13, 2010Applicant: Boehringer Ingelheim International GmbHInventors: Brian Nicholas Cook, Anne Bettina Eldrup, Ingo Andreas Mugge, Fariba Soleymanzadeh, Sanxing Sun, Yunlong Zhang
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Patent number: 7713961Abstract: The present invention relates to substituted 1,2-ethylenediamines of general formula (I) wherein the groups R1 to R15, A, B, L, i as well as X1—X4 are defined as in the specification and claims and the use thereof for the treatment of Alzheimer's disease (AD) and similar diseases.Type: GrantFiled: March 30, 2006Date of Patent: May 11, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Christian Eickmeier, Stefan Peters, Klaus Fuchs, Niklas Heine, Sandra Handschuh, Cornelia Dorner-Ciossek, Klaus Klinder, Marcus Kostka
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Publication number: 20100113359Abstract: The present invention relates to new dimethylphenoxy inhibitors of viral protease or parasitic enzymes, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: November 5, 2009Publication date: May 6, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100113491Abstract: A novel series of BPU analogues were synthesized and evaluated for antitumor activity. In particular, BPU sulfur analogues 6n and 7d were shown to possess up to 10-fold increased potency, when compared to compound 1, against cancer cell lines. 6n was more effective than compound 1 in causing apoptosis of MCF-7 cells. When compared to other drugs with a similar mechanism of action, 6n retained significant ability to inhibit tubulin assembly, with an IC50 of 2.1 ?M.Type: ApplicationFiled: May 26, 2009Publication date: May 6, 2010Inventors: Saeed R. Khan, Gurulingappa Hallur, Manuel Hidalgo, Antonio Jimeno
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Patent number: 7709475Abstract: The present invention relates to a compound represented by Formula [I]: wherein X is O, S, NH or CH2; Y1, Y2, Y3, Y4 and Y5, which may be identical or different, are each CH or N; however, at least one of Y1, Y2, Y3, Y4 and Y5 is N; Z1 and Z2, which may be identical or different, are each CH or N; n is an integer from 1 to 3; R1 is a C3-C8 cycloalkyl group, a C6-C10 aryl group, an aliphatic heterocyclic ring or an aromatic heterocyclic ring, or a bicyclic aliphatic saturated hydrocarbon group; R2 and R3, which may be identical or different, are each a hydrogen atom, a lower alkyl group, a lower alkenyl group, a C3-C8 cycloalkyl group, a C6-C10 aryl group, an aromatic heterocyclic ring, or the like; and R4 is a hydrogen atom, a lower alkyl group, a C3-C6 cycloalkyl group or the like, or a pharmaceutically acceptable salt or ester thereof, and a selective inhibitor against Cdk4 and/or Cdk6 or an anticancer agent containing the compound or a pharmaceutically acceptable salt or ester thereof.Type: GrantFiled: May 19, 2005Date of Patent: May 4, 2010Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yoshikazu Iwasawa, Jun Shibata, Tadashi Shimamura, Hideki Kurihara, Takashi Mita, Nobuhiko Kawanishi, Takashi Hashihayata, Mikako Kawamura, Takeshi Sagara, Sachie Arai, Hiroshi Hirai
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Publication number: 20100105904Abstract: Disclosed is a compound represented by the formula (I) below or a pharmacologically acceptable salt thereof. Also disclosed is a use of the compound or salt as a pharmaceutical product. (In the formula, Ar1 represents an imidazolyl group which may be substituted with a C1-6 alkyl group; Ar2 represents a phenyl group which may be substituted with a C1-6 alkoxy group; X1 represents a single bond; R1 and R2 respectively represent a C1-6 alkyl group or the like which may be substituted with a substituent such as a 5- to 14-membered aromatic heterocyclic group; and R3 represents a hydrogen atom or the like.Type: ApplicationFiled: May 18, 2007Publication date: April 29, 2010Inventors: Teiji Kimura, Koki Kawano, Eriko Doi, Noritaka Kitazawa, Takehiko Miyagawa, Nobuaki Sato, Toshihiko Kaneko, Kogyoku Shin, Koichi Ito, Mamoru Takaishi, Takeo Sasaki, Hiroaki Hagiwara
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Patent number: 7705008Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof is disclosed herein. A, X, J, E, and Z are as described herein. These compounds are useful for treating diseases.Type: GrantFiled: August 14, 2008Date of Patent: April 27, 2010Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh
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Publication number: 20100081673Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions that include the compounds described herein, and methods of using such antagonists of PGD2 receptors, alone or in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: September 28, 2009Publication date: April 1, 2010Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard HUTCHINSON, Nicholas Simon STOCK, Jeffrey Roger ROPPE, Jill Melissa SCOTT, Brian Andrew STEARNS, Yen Pham TRUONG, Deborah VOLKOTS, Timothy PARR
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Patent number: 7687500Abstract: Oxetane-containing nucleosides, particularly non-reducing psiconucleoside oxetanes are described herein. Therapeutic application of these oxetane compounds toward the treatment of nucleoside analog related disorders such as disorders involving cellular proliferation and infection are also described.Type: GrantFiled: January 24, 2008Date of Patent: March 30, 2010Assignee: The University of ConnecticutInventors: Amy R. Howell, Rosa C. Taboada, Stewart K. Richardson
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Patent number: 7683097Abstract: The present invention provides compounds that are effective against inhibiting topoisomerase (i.e., topoisomerase I and/or topoisomerase II). These compounds are used for treating cell-proliferative disorders. In some instances, these compounds have anticancer activity, e.g., against multi-drug resistant cancers.Type: GrantFiled: May 25, 2005Date of Patent: March 23, 2010Assignee: Propharmacon Inc.Inventors: Martin A. Murphy, John Robert Schullek, John S. Ward, Gary C. Look, Brian Siesel
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Publication number: 20100069416Abstract: The present invention relates to certain azabicyclo compounds of formula (I)?: wherein the various groups are defined herein and that are modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.Type: ApplicationFiled: March 30, 2007Publication date: March 18, 2010Inventors: Barbara Bertani, Anna Checchia, Romano Di Fabio, Gabriella Gentile, Alessandra Pasquarello, Silvia Terreni
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Publication number: 20100064450Abstract: The invention relates to an agent for dying fibers comprising keratin, particularly human hair, the agent comprising at least one compound of the formula: together with at least one CH-acidic compound. The invention also relates to methods for shading oxidation dyed fibers, methods for freshening up fibers, methods for making an agent for dyeing fibers and to various compositions.Type: ApplicationFiled: November 20, 2007Publication date: March 18, 2010Applicant: HENKEL AG & CO. KGAAInventors: Wibke Gross, Doris Oberkobusch, Ralph Nemitz
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Patent number: 7674789Abstract: The present invention is directed to compounds of formula (I), (Ia),(Ic) and (Id), compositions, and uses thereof as an inhibitor of the p38 kinase, and wherein, inter alia R1 is C(Z)N(R10?)(CR10R20)vRb, C(Z)O(CR10R20)vRb, N(R10?)C(Z)(CR10R20)vRb; N(R10?)C(Z)N(R10?)(CR10R20)vRb; or N(R10?)OC(Z)(CR10R20)vRb; R3 is C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-10 alkyl, aryl, arylC1-10 alkyl, heteroarylC1-10 alkyl, or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties may be optionally substituted; X is R2, OR2?, S(O)mR2?, (CH2)n?N(R10?)S(O)mR2?, (CH2)n?N(R10?)C(O)R2?, (CH2)n?NR4R14, (CH2)n?N(R2 ?)(R2?), or N(R10?)—Rh—NH—C(?N—CN)NRqRq?; and R2 is hydrogen, C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic, or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties, excluding hydrogen, may be optionally substituted; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 24, 2006Date of Patent: March 9, 2010Assignee: Glaxo Group LimitedInventors: James F. Callahan, Zehong Wan, Hongxing Yan, Xichen Lin
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Patent number: 7674795Abstract: This invention relates to derivatives of 4-(benzimidazol-2-yl)fluorene and 4-(azabenzimidazol-2-yl)fluorene, to pharmaceutical compositions comprising such derivatives, and to methods of treatment of disorders related to Hsp90 protein activity, comprising administering such derivatives.Type: GrantFiled: November 14, 2007Date of Patent: March 9, 2010Assignee: Aventis Pharma SAInventors: Patrick Mailliet, Luc Bertin, Fabienne Thompson, Jean-Marie Ruxer, Fabienne Pilorge, Didier Benard, Hervé Minoux, Chantal Carrez, Hélène Goulaouic, Thierry Gouyon
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Publication number: 20100048548Abstract: The present invention relates to novel iminooxazolidines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular thromboembolic disorders.Type: ApplicationFiled: April 8, 2006Publication date: February 25, 2010Applicant: Bayer HealthCare AGInventors: Susanne Röhrig, Jens Pohlmann, Elisabeth Perzborn, Christoph Gerdes, Karl-Heinz Schlemmer
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Publication number: 20100041653Abstract: The present disclosure provides compounds having the general structure A or pharmaceutically acceptable salts thereof: R—X??(A) wherein R is an alkyl or aryl moiety comprising heterocyclic structures; and X is a metal-chelatin group selected from: This disclosure further provides a focused library of compounds for use in the discovery and design of metallo-enzyme inhibitors. This fragment-based approach provides an assembly of a library of low molecular weight compounds (MW<300 Da) containing a variety of potential metal-chelating groups. The identification of the inhibitory scaffolds among these compounds provides the initial hit fragments that may be optimized for affinity against a particular target using common medicinal chemistry, structure-based or NMR-based approaches.Type: ApplicationFiled: August 14, 2009Publication date: February 18, 2010Applicants: BURNHAM INSTITUTE FOR MEDICAL RESEARCH, THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Maurizio Pellecchia, Seth M. Cohen
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Patent number: 7659272Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: GrantFiled: October 16, 2007Date of Patent: February 9, 2010Assignee: Millennium Pharmaceuticals, Inc.Inventors: Paul Fleming, Geraldine C. B. Harriman, Zhan Shi, Chen Shaowu
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Publication number: 20100029612Abstract: The present invention provides a combinatorial approach to a library of novel compounds having four diversity points. The compounds provide for the mapping of urotensin II and somatostatin 5 receptors by differential binding of said receptors. The present invention further relates to a method of treating diseases for which modulation of the urotensin II receptor produces a physiologically beneficial response in said disease, such as those associated with CNS function and cardiovascular diseases. The present invention further relates to pharmaceutical compositions comprising these agents for the treatment of these diseases adapted to modulate the urotensin II receptor.Type: ApplicationFiled: February 18, 2004Publication date: February 4, 2010Inventor: Roger Olsson
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Publication number: 20100022529Abstract: The present invention provides amidophenoxyindazole compounds useful in the treatment of cancer.Type: ApplicationFiled: July 15, 2009Publication date: January 28, 2010Inventors: Tiechao LI, Mark Andrew POBANZ, Chuan SHIH, Zhipei WU, Wei Jennifer YANG, Boyu ZHONG
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Patent number: 7652010Abstract: Azabicyclo pyridazinyl compounds including azabicyclooctyl-pyridazinyl-oxy compounds, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile, the compounds may be used for the treatment of various diseases or disorders, including those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: GrantFiled: October 14, 2005Date of Patent: January 26, 2010Assignee: Neurosearch A/SInventors: Dan Peters, Daniel B. Timmermann, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Tino Dyhring Jørgensen
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Publication number: 20100016338Abstract: The present invention relates to compounds of formula I, processes and intermediates for their production and their use as anti-inflammatory agents.Type: ApplicationFiled: July 20, 2009Publication date: January 21, 2010Applicants: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT, ASTRAZENECA ABInventors: Markus Berger, Hartmut Rehwinkel, Ekkehard May, Heike Schäcke
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Patent number: 7648992Abstract: The invention provides compounds of formula (I), wherein R1 and R2 are as defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.Type: GrantFiled: July 4, 2005Date of Patent: January 19, 2010Assignee: AstraZeneca ABInventors: Balint Gabos, Lena Ripa, Kristina Stenvall
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Publication number: 20100010024Abstract: The present application relates to the use of 1,4-diaryldihydropyrimidin-2-one derivatives of the formula (I) for the treatment and/or prophylaxis of pulmonary arterial hypertension and other types of pulmonary hypertension, and to the use thereof for the manufacture of medicaments for the treatment and/or prophylaxis of pulmonary arterial hypertension and other types of pulmonary hypertension.Type: ApplicationFiled: June 25, 2007Publication date: January 14, 2010Applicant: Bayer Healthcare AGInventors: Franz Von Nussbaum, Heike Gielen-Haertwig, Martin Klein, Volkhart Min-Jian Li, Daniel Meibom, Peter Sandner, Klemens Lustig, Stefan Schäfer