The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 544/361)
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Publication number: 20100286163Abstract: Disclosed herein are indolo[3,2-c]quinoline compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein R and m are given the definitions as set forth in the Specification and Claims. These compounds can be used to inhibit both growth of cancer cells and activity of telomerase.Type: ApplicationFiled: August 31, 2009Publication date: November 11, 2010Applicant: Kaohsiung Medical UniveristyInventors: Cherng-Chyi Tzeng, Yeh-Long Chen, Jing-Jer Lin, Chih-Ming Lu
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Patent number: 7829567Abstract: Disclosed herein are novel imino-indeno[1,2-c]quinoline derivatives of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein each of the substituents is given the definition as set forth in the Specification and Claims. Also disclosed are the preparation processes of these derivatives, their synthetic precursors and their uses in the manufacture of pharmaceutical compositions for use in the treatment of cancers.Type: GrantFiled: October 31, 2007Date of Patent: November 9, 2010Assignee: Kaohsiung Medical UniversityInventors: Cherng-Chyi Tzeng, Yeh-Long Chen, Chih-Hua Tseng, Pei-Jung Lu
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Publication number: 20100280001Abstract: The present invention provides compounds of formula (I) wherein Ra, R1, R2, R3, X1, Y1, Z1, A, n and m 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: ApplicationFiled: May 6, 2008Publication date: November 4, 2010Inventors: Roger Victor Bonnert, Thomas McInally, Stephen Thom, Hiroki Wada
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Patent number: 7816406Abstract: The present invention provides quinolone analogs which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing quinolone analogs, and methods of using the same.Type: GrantFiled: September 16, 2005Date of Patent: October 19, 2010Assignee: Cylene Pharmaceuticals, Inc.Inventors: Jeffrey P. Whitten, Fabrice Pierre, Collin Regan, Michael Schwaebe, Johnny Y. Nagasawa, Peter Chua
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Publication number: 20100261901Abstract: The present invention is directed to novel process for the preparation of regioselective perylenediimides derivatives, specifically mono and dibrominated derivatives.Type: ApplicationFiled: May 6, 2008Publication date: October 14, 2010Inventors: Boris Rybtchinski, Paramasivan Rajasingh, Elijah Shirman
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Publication number: 20100261706Abstract: Provided herein are tetracyclic 1H-indeno[1,2-b]pyridine-2(5H)-one analogs and derivatives, compositions comprising an effective amount of a tetracyclic 1H-indeno[1,2-b]pyridine-2(5H)-one analog and/or derivative and methods for treating or preventing an inflammatory disease, a reperfusion injury, diabetes mellitus, a diabetic complication, a reoxygenation injury resulting from organ transplantation, an ischemic condition, a neurodegenerative disease, renal failure, a vascular disease, a cardiovascular disease, an ocular or opthalmologic disease, cancer, a complication of prematurity, cardiomyopathy, retinopathy, nephropathy, contrast induced nephropathy, neuropathy, erectile dysfunction or urinary incontinence, comprising administering to a subject in need thereof an effective amount of a tetracyclic 1H-indeno[1,2-b]pyridine-2(5H)-one analog or derivative.Type: ApplicationFiled: December 8, 2009Publication date: October 14, 2010Applicant: INOTEK PHARMACEUTICALS CORPORATIONInventors: Prakash JAGTAP, Duy-Phong Pham-Huu, Frederick COHEN, Huiyong HU, Xiaojing WANG
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Publication number: 20100256112Abstract: Disclosed herein are hydroxylthienoquinolones and related compounds and their pharmaceutically acceptable salts useful as antiviral agents and having the general formula in which the variables R2, R6, and R7 are defined herein. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity and are particularly efficacious for the treatment of MRSA infections. The invention also provides pharmaceutical compositions, pharmaceutical compositions containing a hydroxylthienoquinolone in combination with one or more other active agent, and methods of treating microbial infections in animals by administering an effective amount of a hydroxylthienoquinolone or related compound to an animal suffering from a microbial infection.Type: ApplicationFiled: April 5, 2010Publication date: October 7, 2010Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Barton James BRADBURY, Milind DESHPANDE, Akihiro HASHIMOTO, Ha Young KIM, Edlaine LUCIEN, Godwin PAIS, Michael PUCCI, Qiuping WANG, Jason Allan WILES, Avinash PHADKE
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Publication number: 20100222321Abstract: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: June 7, 2006Publication date: September 2, 2010Inventors: Donna J. Armstrong, Essa H. Hu, Michael J. Kelly, III, Mark E. Layton, Yiwei Li, Jun Liang, Kevin J. Rodzinak, Michael A. Rossi, Philip E. Sanderson, Jiabing Wang
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Publication number: 20100222316Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions that are mediated by excessive glucocorticoid action.Type: ApplicationFiled: March 17, 2010Publication date: September 2, 2010Applicant: ABBOTT LABORATORIESInventors: Marina A. Pliushchev, Dariusz Wodka, Bryan K. Sorensen, James T. Link
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Publication number: 20100216786Abstract: The present invention relates to the adenosine A3 receptor ligands of the general formula (I), within them favourably to the antagonists, to their salts, solvates, N-oxides and isomers, to the pharmaceutical compositions containing the compounds of the general formula (I), their salts, solvates, N-oxides and isomers, to the use of the compounds of the general formula (I), their salts, solvates, N-oxides and isomers, to the preparation of the compounds of the general formula (I), their salts, solvates, N-oxides and isomers, as well as to the new intermediates of the general formula (II), (VI), (XI), (XII) and (XV), and to the preparation thereof.Type: ApplicationFiled: December 4, 2009Publication date: August 26, 2010Applicant: SANOFI-AVENTISInventors: Edit SUSAN, Kinga BOER, Zoltan KAPUI, Geza TIMARI, Sandor BATORI, Endre MIKUS, Judit VARGANE SZEREDI, Michel FINET, Katalin URBAN-SZABO, Tibor SZABO
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Publication number: 20100216807Abstract: Novel heterocyclic compounds of formula I: A-B-D??Formula I or a pharmaceutically acceptable salt thereof, wherein: A is selected from the group consisting of a moiety having general Formula II and a moiety having general Formula III: B is a moiety selected from the group consisting of: D is a moiety selected from the group consisting of: which exhibit a dopamine receptor (preferably a D4 receptor) and/or a serotonine receptor (preferably 5HTA1 agonistic activity), processes of preparing same, pharmaceutical compositions containing same and uses thereof in the treatment of medical conditions associated with the dopaminergic and/or serotonergic systems (e.g., sexual disorders, dyskinesia, anxiety) are disclosed.Type: ApplicationFiled: September 24, 2007Publication date: August 26, 2010Applicant: ATIR Holding S.AInventor: Vladimir Kogan
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Publication number: 20100210629Abstract: The present invention provides for tricyclic compounds having the formula (I), wherein R1, R2, R5, R6, R7, and R8 are as described herein. The present invention further provides pharmaceutical compositions comprising such compounds, as well as the use of such compounds for treating inflammatory and immune diseases.Type: ApplicationFiled: April 23, 2010Publication date: August 19, 2010Inventors: William J. Pitts, James Kempson, Junqing Guo, Jagabandhu Das, Charles M. Langevine, Steven H. Spergel, Scott Hunter Watterson
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Patent number: 7772227Abstract: The invention relates to tricyclic 1-[(indol-3-yl)carbonyl]piperazine derivative having the general Formula (I) wherein X is CH2, O or S; R represents 1-3 substituents independently selected from H, (C1-4)alkyl, (C1-4)alkyloxy and halogen; R1 is (C5-8)cycloalkyl; R2 is H or (C1-4)alkyl; R3, R3?, R4? R4?, R5, R5? and R6? are independently hydrogen or (C1-4)-alkyl, optionally substituted with (C1-4)alkyloxy, OH or halogen; R6 is hydrogen or (C1-4)alkyl, optionally substituted with (C1-4)alkyloxy, OH or halogen; or R6 forms together with R7 a 4-7 membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O and S; R7 forms together with R6 a 4-7 membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O and S; or R7 is H, (C1-4)alkyl or (C3-5)cycloalkyl, the alkyl groups being optionally substituted with OH, halogen or (C1-4)alkyloxy; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 13, 2004Date of Patent: August 10, 2010Assignee: N.V. OrganonInventor: Julia Adam-Worrall
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Publication number: 20100197634Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.Type: ApplicationFiled: September 8, 2008Publication date: August 5, 2010Inventors: Tony Siu, Jonathan Young, Michael Altman, Alan Northrup, Matthew Katcher, Ellalahewage Sathyajith Kumarasinghe, Ekaterina Kozina, Scott Peterson, Matthew Childers
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Publication number: 20100197910Abstract: The present invention provides a novel process for the preparation of the prulifloxacin intermediate, 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-[1,3] thiazeto[3,2-a]quinoline-3-carboxylic acid, thereby producing prulifloxacin and its pharmaceutical acceptable acid addition salts thereof in high purity and in high yield using novel intermediates in lesser reaction time. Thus, for example, ethyl 6,7-difluoro-1-methyl-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate is reacted with boric acid in the presence of acetic anhydride and acetic acid to give a borane compound, which is then condensed with piperazine in the presence of acetonitrile and dimethylsulfoxide, followed by treatment with potassium hydroxide solution to give 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-[1,3] thiazeto [3,2-a]quinoline-3-carboxylic acid.Type: ApplicationFiled: November 17, 2006Publication date: August 5, 2010Applicant: HETERO DRUGS LIMITEDInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy
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Patent number: 7763634Abstract: The instant invention provides for tetracyclic compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.Type: GrantFiled: June 5, 2007Date of Patent: July 27, 2010Assignees: Merck & Co., Inc., Merck Sharp & Dohme Corp.Inventors: Jonathan R. Young, Andrew Haidle, Paul Tempest, Michelle Machacek
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Patent number: 7763633Abstract: Indolo[3,2-c]quinoline compounds of formula (I) shown below. Each variable in this formula is defined herein. These compounds can be used to inhibit both growth of cancer cells and activity of telomerase.Type: GrantFiled: April 9, 2009Date of Patent: July 27, 2010Assignee: Kaohsiung Medical UniversityInventors: Cherng-Chyi Tzeng, Yeh-Long Chen, Jing-Jer Lin, Chih-Ming Lu
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Publication number: 20100184758Abstract: Beta-carboline derivatives of structural formula I are selective antagonists of the somatostatin subtype receptor 3 (SSTR3) and are useful for the treatment of Type 2 diabetes mellitus and of conditions that are often associated with this disease, including hyperglycemia, insulin resistance, obesity, lipid disorders, and hypertension. The compounds are also useful for the treatment of depression and anxiety.Type: ApplicationFiled: July 15, 2008Publication date: July 22, 2010Inventors: Peter H. Dobbelaar, Wu Du, Liangqin Guo, William K. Hagmann, Shuwen He, Tianying Jian, Jian Liu, Ravi P. Nargund, Alexander Pasternak, Shrenik K. Shah, Quang T. Truong, Zhixiong Ye, James Deliureficio, Raman Bakshi
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Publication number: 20100168417Abstract: 2-indolyl imidazo[4,5-d]phenanthroline compounds of Formula I that are capable of intracellular chelation of transition metals and of exerting antiproliferative effects in cancer cells, that are cytostatic and/or cytotoxic, are provided. Compounds of Formula I can also induce apoptosis in cancer cells and are thus capable of exerting a cytotoxic effect on cancer cells. The compounds of Formula I are also capable of selectively inhibiting the proliferation of one or more of prostate cancer cells, colon cancer cells, non-small lung cancer cells and leukemia cells. The compounds of Formula I are also capable of increasing the expression of the zinc-regulated tumour suppressor, KLF4 and thus are useful in inhibiting the proliferation of cancer cells in which KLF4 functions as a tumour-suppressor, including, but not limited to, bladder cancer, cancers of the gastrointestinal tract and various leukemias.Type: ApplicationFiled: May 25, 2006Publication date: July 1, 2010Inventors: Mario Huesca, Aiping H. Young, Yoon Lee, Aye Aye Khine, Jim A. Wright, Lisa Lock, Raed Al-Qawasmeh
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Publication number: 20100158858Abstract: In accordance with the present invention, compounds are provided which are useful in a method or in the manufacture of a medicament for post-transcriptionally inhibiting the expression of VEGF in a subject in need thereof comprising inhibiting VEGF mRNA translation by orally administering said medicament once, twice or thrice daily to the subject.Type: ApplicationFiled: April 12, 2008Publication date: June 24, 2010Inventors: Liangxian Cao, Samit Hirawat, Langdon Miller, Gary Elfring, Thomas Davis, Marla L. Weetall
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Publication number: 20100152183Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: December 4, 2009Publication date: June 17, 2010Applicant: ABBOTT LABORATORIESInventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura Hexamer, Aaron Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt
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Publication number: 20100120817Abstract: An azonafide-based compound of Formula I, a composition comprising the compound, and a method of using the compound to deliver a cytotoxic azonafide derivative to a cell, as well as related compounds and methods for the use thereof to pre-pare an azonafide-based compound of Formula I.Type: ApplicationFiled: September 12, 2007Publication date: May 13, 2010Applicant: Office of Technology Transfer, NIHInventors: Nadya I. Tarasova, Marcin Dyba, Christopher J. Michejda, Maria Michejda
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Publication number: 20100120717Abstract: Compounds are provided for use with kinases that comprise a compound selected from the group consisting of formula (I) wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture in comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: October 8, 2007Publication date: May 13, 2010Inventors: Jason W. Brown, Qing Dong, Bheema R. Paraselli, Jeffrey A. Stafford, Michael B. Wallace, Hasanthi Wijesekera
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Publication number: 20100121049Abstract: The present invention relates to Indenoisoquinolinone Analogs, compositions comprising an effective amount of an Indenoisoquinolinone Analog and methods for treating or preventing an inflammatory disease, a reperfusion injury, diabetes mellitus, a diabetic complication, reoxygenation injury resulting from organ transplantation, an ischemic condition, a neurodegenerative disease, renal failure, a vascular disease, a cardiovascular disease, cancer, a complication of prematurity, cardiomyopathy, retinopathy, nephropathy, neuropathy, erectile dysfunction or urinary incontinence, comprising administering to a subject in need thereof an effective amount of an Indenoisoquinolinone Analog.Type: ApplicationFiled: February 28, 2008Publication date: May 13, 2010Applicant: INOTEK PHARMACEUTICALS CORPORATIONInventors: Prakash Jagtap, Duy-Phong Pham-Huu, Frederick Cohen, Xiaojing Wang
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Publication number: 20100113783Abstract: The present invention relates to processes for the preparation of Type I, Type II and Type III crystals of prulifloxacin.Type: ApplicationFiled: March 14, 2008Publication date: May 6, 2010Applicant: RANBAXY LABORATORIES LIMITEDInventors: Tarun Kant Sharma, Sandeep T. Kanawade
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Selected CGRP antagonists, processes for preparing them and their use as pharmaceutical compositions
Publication number: 20100113411Abstract: The present invention relates to CGRP antagonists of general formula wherein A, U, V, W, X and R1 to R3 are defined as in claim 1, the tautomers, diastereomers, enantiomers, hydrates, mixtures thereof and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them.Type: ApplicationFiled: August 6, 2009Publication date: May 6, 2010Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KGInventors: Klaus RUDOLF, Stephan Georg MUELLER, Dirk STENKAMP, Philipp LUSTENBERGER, Alexander DREYER, Eckhart BAUER, Marcus SCHINDLER, Kirsten ARNDT, Henri DOODS -
Publication number: 20100099871Abstract: Compounds having anti-psychotic activity are disclosed herein. In some embodiments, the compounds are atypical anti-psychotics. In some embodiments, the compounds are selective for the 5-HT2A receptor over the D2 receptor. Pharmaceutical derivatives and pharmaceutical compositions including the compounds are disclosed herein. Methods for treating a psychotic condition that include administering the compounds, a pharmaceutical derivative thereof, or a pharmaceutical composition thereof are also disclosed herein.Type: ApplicationFiled: August 17, 2009Publication date: April 22, 2010Inventors: Dwight W. Miller, Neil C. Mitchell, Bill W. Massey
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Publication number: 20100068181Abstract: The present invention provides compounds of Formula I (wherein R, R1, R3, R4, X, and ring Y are as defined herein). The present invention also provides compositions comprising these compounds that are useful for treating cellular proliferative diseases or disorders associated with KSP kinesin activity and for inhibiting KSP kinesin activity.Type: ApplicationFiled: December 19, 2007Publication date: March 18, 2010Inventors: Sunil Paliwal, Hon-Chung Tsui, Jose S. Duca, Charles A. Lesburg, Ronald J. Doll, Neng-Yang Shih
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Publication number: 20100069360Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein the groups R1, R2, R3, R7 and X are as defined in the specification.Type: ApplicationFiled: August 28, 2007Publication date: March 18, 2010Inventors: Laszlo Revesz, Achim Schlapbach, Rudolf Walchli
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Publication number: 20100063046Abstract: The present invention provides tetracyclic imidazole analogs which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing these compounds, and methods of using the same.Type: ApplicationFiled: May 17, 2007Publication date: March 11, 2010Inventors: Jeffrey P. Whitten, Michael Schwaebe
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Publication number: 20100056558Abstract: The invention relates to novel organic compounds of formula (I) processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment of an inflammatory or obstructive airway disease, such as asthma, disorders commonly occurring in connection with transplantation, or a proliferative disease, such as a tumor disease.Type: ApplicationFiled: October 12, 2009Publication date: March 4, 2010Inventors: Carlos Garcia-Echeverria, Frédéric Stauffer, Pascal Furet
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Publication number: 20100048552Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, Bcr-Abl(T315I), ALK, BLK, BMX, BRK, C-kit, c-RAF, CSK, c-SRC, EGFR, Fes, FGFR3, Flt3, Fms, Fyn, IGF-1R, IR, JAK(2), JAK(3), KDR, Lck, NLK, p70S6K, PDGFR?, Ros, SAPK2?, SGK, SIK, Syk, Tie2 and TrkB kinases.Type: ApplicationFiled: May 11, 2007Publication date: February 25, 2010Applicant: IRM LLCInventors: Pingda Ren, Baogen Wu, Guobao Zhang, Yongping Xie, Barun Okram, Victor Nikulin, Xia Wang, Ha-Soon Choi
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Patent number: 7666877Abstract: Disclosed are ergoline derivatives, Formula (I), wherein either each of R1 and R2, independently, is H; optionally R10 and/or R11-substituted-phenyl or -phenyl-C1-4alkyl; optionally R10 and/or R11-substituted-heteroaryl or -heteroaryl-C1-4alkyl; optionally R10 and/or R11-substituted heteroaryl N-oxide; optionally R10-substituted C1-C8 alkyl; optionally R10-substituted C2-C8 alkenyl, optionally R10-substituted C2-C8 alkynyl; optionally R10-substituted C3-C8 cycloalkyl, or optionally R10-substituted C4-C8 cycloalkenyl; or R1 and R2 form together with the nitrogen atom to which they are attached an optionally R10-substituted 3-8 membered ring containing in addition to the nitrogen atom up to 2 heteroatoms selected independently from N, O and S; R3 is H; OR1; CH2R1R2; (CH2)1-2NR1R2; CH2—CH2—OR1; CH2—CO—NR1R2; or CO—CH2R1R2; R4 is F; Cl; Br; I; OR1; NR1R2 or has one of the significances given for R1; and R5 has one of the significances given for R1, in free form or in salt form for preventing or treating disordersType: GrantFiled: May 29, 2006Date of Patent: February 23, 2010Assignee: Novartis AGInventors: Rolf Baenteli, Fraser Glickman, Jiri Kovarik, Ian Lewis, Markus Streiff, Gebhard Thoma, Hans-Günter Zerwes
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Patent number: 7667039Abstract: The invention relates to novel organic compounds of formula (I) processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment of an inflammatory or obstructive airway disease, such as asthma, disorders commonly occurring in connection with transplantation, or a proliferative disease, such as a tumor disease.Type: GrantFiled: May 18, 2006Date of Patent: February 23, 2010Assignee: Novartis AGInventors: Carlos Garcia-Echeverria, Frédéric Stauffer, Pascal Furet
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Publication number: 20100035826Abstract: A method of providing a patient with controlled release of a phenolic opioid using a prodrug capable, upon enzymatic activation, of releasing the phenolic opioid through intra-molecular cyclization leading to formation of a cyclic urea, carbamate or thiocarbamate.Type: ApplicationFiled: May 24, 2007Publication date: February 11, 2010Applicant: Phamacofoce, Inc.Inventors: Thomas E. Jenkins, Aleksandr Kolesnikov
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Publication number: 20100035279Abstract: The present invention relates to compounds of the general structure: wherein Y is O, X is O, bond ? is absent and bond ? is present, or Y is H, X is CH, bond ? is present, and bond ? is absent; atom Z is a carbon and bonds ?, ? and ? are present, or is a nitrogen and bonds ?, ? and ? are absent; R1 is —H, —OH, —O—R7, —N(H)—R8, —N(H)—(CH2)n—NH2, —N(R9)(R10), or a piperazine cation; R2 is either covalently bound to R9, or is —H, or is covalently bound to R3 so as to form a substituted or unsubstituted pyrrole or R2 is covalently bound to R9 or R8 or R7; or R1 and R2 are covalently joined to form an aromatic ring; R3 is either covalently bound to R2 so as to form a pyrrole, or is, inter alia, —H, —OH, alkyl, or when Z is nitrogen R3 is ?O; R4 is, inter alia, —H, —OH, or —R11NH2; R5 is, inter alia, —H, —OH, or —R12NH2, and R6 is either is covalently bound to R10 or is —H, or R6 is covalently bound to R10 or R8 or R7.Type: ApplicationFiled: July 27, 2007Publication date: February 11, 2010Inventors: Niko Gert Gubernator, Dalibor Sames, David Sulzer, Paul Vadola
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Publication number: 20100029635Abstract: This invention concerns the compounds the N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein X is NR2, O, S, SO, SO2; R1 is hydrogen, cyano, halo, substituted carbonyl, methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, Het1 or Het2; n is 1, 2 or 3; R2 is hydrogen, aryl substituted with a radical —COOR4; or R2 is substituted C1-10alkyl, C2-10alkenyl or C3-7cycloalkyl; or R2 is a radical of formula: —CpH2p—CH(OR14)—CqH2q—R15 (b-3); —CH2—CH2—(O—CH2—CH2)m—OR14 (b-4); —CH2—CH2—(O—CH2—CH2)m—NR5aR5b(b-5) -a1=a2-a3=a4- is —CH?CH—CH?CH—; —N?CH—CH?CH—; —CH?N—CH?CH—; —CH?CH—N?CH—; —CH?CH—CH?N— (c-5); wherein one of the hydrogen atoms in (c-1)-(c-5) is replaced by particular radicals; R3 is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, hydroxycarbonyl, substituted carbonyl, methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy-methanimidamidyl or Het1.Type: ApplicationFiled: October 9, 2009Publication date: February 4, 2010Inventors: Bart Rudolf Romanie Kesteleyn, Sandrine Marie Helene Vendeville, Natalie Maria Francisca Kindermans, Dominique Louis Nestor Ghislai Surleraux, Pierre Jean-Marie Bernard Raboisson, Piet Tom Bert Paul Wigerinck, Annick Ann Peeters
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Publication number: 20100029616Abstract: The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters and prodrugs thereof, pharmaceutical compositions containing compounds of formula (I) and the use of said compounds and compositions as urotensin II receptor antagonists.Type: ApplicationFiled: July 31, 2009Publication date: February 4, 2010Inventors: William A. Kinney, Diane K. Luci, Bruce E. Maryanoff, Shyamali Ghosh, Edward C. Lawson
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Patent number: 7652028Abstract: The present invention relates to Indenoisoquinolinone Analogs, compositions comprising an effective amount of an Indenoisoquinolinone Analog and methods for treating or preventing an inflammatory disease, a reperfusion injury, diabetes mellitus, a diabetic complication, reoxygenation injury resulting from organ transplantation, an ischemic condition, a neurodegenerative disease, renal failure, a vascular disease, a cardiovascular disease, cancer, a complication of prematurity, cardiomyopathy, retinopathy, nephropathy, neuropathy, erectile dysfunction or urinary incontinence, comprising administering to a subject in need thereof an effective amount of an Indenoisoquinolinone Analog.Type: GrantFiled: August 23, 2006Date of Patent: January 26, 2010Assignee: Inotek Pharmaceuticals CorporationInventors: Prakash Jagtap, Duy-Phong Pham-Huu
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Publication number: 20100009971Abstract: A novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound or its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound of the present disclosure is also useful in the treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.Type: ApplicationFiled: August 19, 2009Publication date: January 14, 2010Inventors: Takahiro Ishii, Takashi Sugane, Jun Maeda, Fumie Narazaki, Akio Kakefuda, Kentaro Sato, Tatsuhisa Takahashi, Takatoshi Kanayama, Chikashi Saitoh, Jotaro Suzuki, Chisato Kanai
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Publication number: 20090306071Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.Type: ApplicationFiled: June 5, 2007Publication date: December 10, 2009Inventors: Jonathan R. Young, Andrew Haidle, Paul Tempest, Michelle Machacek
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Patent number: 7629338Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, m, n, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: May 7, 2007Date of Patent: December 8, 2009Assignee: Merck & Co., Inc.Inventors: Michael R. Wood, Steven N. Gallicchio, Harold G. Selnick, C. Blair Zartman, Ian M. Bell, Craig A. Stump
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Publication number: 20090298846Abstract: Indolo[3,2-c]quinoline compounds of formula (I) shown below. Each variable in this formula is defined herein. These compounds can be used to inhibit both growth of cancer cells and activity of telomerase.Type: ApplicationFiled: April 9, 2009Publication date: December 3, 2009Applicant: KAOHSIUNG MEDICAL UNIVERSITYInventors: CHERNG-CHYI TZENG, YEH-LONG CHEN, JING-JER LIN, CHIH-MING LU
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Publication number: 20090291963Abstract: Substituted indoles of the formula (I) and physiologically acceptable derivatives and salts thereof, in which R1, D, E, R12, p, X1, E, G, X2 and Z are as defined in claim 1, exhibit particular actions on the central nervous system, especially 5HT reuptake-inhibiting and 5 HTx-agonistic and/or -antagonistic actions and in particular serotonin-agonistic and -antagonistic properties and can be employed as antipsychotics, neuroleptics, antidepressants, anxiolytics and/or antihypertonics.Type: ApplicationFiled: July 29, 2009Publication date: November 26, 2009Inventors: Oliver SCHADT, Henning Böttcher, Joachim Leibrock, Kai Schiemann, Timo Heinrich, Günter Hölzemann, Christoph van Amsterdam, Gerd Bartoszyk, Christoph Seyfried
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Publication number: 20090291921Abstract: Tricyclic compounds, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed.Type: ApplicationFiled: November 19, 2008Publication date: November 26, 2009Applicant: Gilead Sciences, Inc.Inventors: Salman Y. Jabri, Haolun Jin, Choung U. Kim, Jiayao Li, Samuel E. Metobo, Michael R. Mish
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Publication number: 20090281081Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.Type: ApplicationFiled: May 6, 2009Publication date: November 12, 2009Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima, Geraldine C. B. Harriman, Kenneth G. Carson, Shomir Ghosh, Amy M. Elder, Karen M. Mattia
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Patent number: 7612205Abstract: A main object is to provide a crystal of 6-fluoro-1-methyl-7-[4-(5-methyl-2-oxo-1,3-dioxolen-4-yl)-methyl-1-piperazinyl]-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid acetonitrile solvate (Compound B) which is an intermediate for producing preferentially the type III crystal of 6-fluoro-1-methyl-7-[4-(5-methyl-2-oxo-1,3-dioxolen-4-yl)methyl-1-piperazinyl]-4-oxo-4H-[1,3]-thiazeto[3,2-a]quinoline-3-carboxylic acid (Compound A). A crystal of Compound B can be preferentially precipitated by controlling the supersaturation concentration in crystalization using acetonitrile as a solvent. Subsequently, the type III crystal of Compound A can be produced by performing desolvation of the crystal.Type: GrantFiled: April 28, 2004Date of Patent: November 3, 2009Assignee: Nippon Shinyaku Co., Ltd.Inventors: Jun Akai, Hiroshi Nishida
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Publication number: 20090270411Abstract: The present invention relates to new phenanthridine derivatives of formula (I), wherein the variables are as defined in the specification, to processes for producing the same, to pharmacological compositions containing the same and to their use in therapy or prevention of painful and inflammatory processes.Type: ApplicationFiled: December 19, 2006Publication date: October 29, 2009Inventors: Gyula Beke, Eva Bozo, Gabor Czira, Janos Eles, Sandor Farkas, Katalin Hornok, Eva Schmidt, Eva Szentirmay, Istvan Vago, Monika Vastag
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Publication number: 20090253695Abstract: Certain imidazonaphthyridines with a hydroxymethyl or hydroxyethyl substituent at the 2-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for preferentially inducing IFN-? biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.Type: ApplicationFiled: February 22, 2006Publication date: October 8, 2009Applicant: Coley Pharmaceutical Group, Inc,Inventors: Tushar A. Kshirsagar, Scott E. Langer, Shri Niwas, George W. Griesgraber, Philip D. Heppner, Kyle J. Lindstrom
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Patent number: RE41150Abstract: This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.Type: GrantFiled: January 10, 2008Date of Patent: February 23, 2010Assignee: Eisai Corporation of North AmericaInventors: Dana V. Ferraris, Jia-He Li