The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 544/125)
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Publication number: 20110027226Abstract: Compounds of a certain formula I, in which R1, R2, R3 and R4 have the meanings indicated in the description, are effective Eg5-inhibiting compounds with anti-proliferative and/or apoptosis inducing activity.Type: ApplicationFiled: August 22, 2007Publication date: February 3, 2011Applicant: 4SC AGInventors: Matthias Vennemann, Juergen Braugner, Petra Gimmnich, Thomas Baer
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Publication number: 20110009628Abstract: The present technology relates to compounds of Formulas I-VI and methods of making and using such compounds. Methods of use include prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, and metabolic syndrome. Compounds disclosed herein also increase HDL-C, lower total cholesterol, LDL-cholesterol, and triglycerides and increase hepatic LDL receptor expression, inhibit PCSK9 expression, and activate AMP-activated protein kinase.Type: ApplicationFiled: July 8, 2010Publication date: January 13, 2011Inventors: Haiyan Liu, Gaoping Li, Junbo Wang, Jingwen Liu
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Patent number: 7855201Abstract: The present invention is directed to morpholine carboxamide compounds which are antagonists of prokineticin receptors, in particular antagonists of prokineticin 2 receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which prokineticin receptors are involved. 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 prokineticin receptors are involved.Type: GrantFiled: December 4, 2006Date of Patent: December 21, 2010Assignee: Merck Sharp & Dohme. Corp.Inventors: Wayne J. Thompson, Jeffrey Y. Melamed
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Publication number: 20100311739Abstract: The invention relates to novel compounds which are naphthalene diimides of general formula (I). The compounds are used in therapy, particularly in cancer treatment.Type: ApplicationFiled: November 28, 2008Publication date: December 9, 2010Inventors: Mekala Gunaratnam, Francisco Cuenca, Stephen Neidle
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Publication number: 20100292231Abstract: Compounds of formula (I) or formula (Ia) and a method of treating a patient suffering from certain inflammatory disorders, demyelinating disorders, FLT3-mediated disorders, CSF-1R-mediated disorders, cancers and leukemias, comprising administering to said patient a therapeutically effective amount of a compound of formula (I) or formula (Ia) or a pharmaceutically acceptable salt thereof. Definitions for the variables are provided herein.Type: ApplicationFiled: February 2, 2010Publication date: November 18, 2010Inventors: Alfred M. Ajami, Kenneth Duncan
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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: 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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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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Publication number: 20100179140Abstract: 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: December 11, 2009Publication date: July 15, 2010Applicant: Inotek Pharmaceuticals CorporationInventors: Prakash JAGTAP, Duy-Phong Pham-Huu
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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: 20100099667Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic [4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: March 24, 2009Publication date: April 22, 2010Inventors: David T. Hung, Andrew Asher Protter, Sarjavit Chakravarty, Rajendra Parasmal Jain
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Publication number: 20100093698Abstract: Provided herein are Heteroaryl Compounds of formula (I): wherein R1 and R2 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing inflammatory conditions or cancer, and conditions treatable or preventable by inhibition of a kinase or a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a subject in need thereof.Type: ApplicationFiled: September 8, 2009Publication date: April 15, 2010Inventors: Sogole Bahmanyar, R.J. Bates, Kate Blease, Andrew Antony Calabrese, Thomas Oran Daniel, Mercedes Delgado, Jan Elsner, Paul Erdman, Bruce Fahr, Gregory Ferguson, Branden Lee, Lisa Nadolny, Garrick Packard, Patrick Papa, Veronique Plantevin-Krenitsky, Jennifer Riggs, Patricia Rohane, Sabita Sankar, John Sapienza, Yoshitaka Satoh, Victor Sloan, Randall Stevens, Lida Tehrani, Jayashree Tikhe, Eduardo Torres, Andrew Wallace, Brandon Wade Whitefield, Jingjing Zhao
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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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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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Patent number: 7652024Abstract: Certain novel N-acylated spiropiperidine derivatives are ligands of the human melanocortin receptor(s) and, in particular, are selective ligands of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of MC-4R, such as obesity, diabetes, nicotine addiction, alcoholism, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: October 13, 2006Date of Patent: January 26, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Raman K. Bakshi, James P. Dellureficio, Peter H. Dobbelaar, Liangqin Guo, Shuwen He, Qingmei Hong, Ravi P. Nargund, Zhixiong Ye
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Patent number: 7645753Abstract: This invention is concerned with compounds of the formula wherein A, B1, B2, R1, R2 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.Type: GrantFiled: March 2, 2006Date of Patent: January 12, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Alfred Binggeli, Andreas Dominik Christ, Luke Gideon Granville Green, Wolfgang Guba, Hans-Peter Maerki, Rainer Eugen Martin, Peter Mohr
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Publication number: 20100004220Abstract: 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: January 7, 2010Inventors: Prakash JAGTAP, Duy-Phong PHAM-HUU, Frederick COHEN, Xiaojing WANG
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Publication number: 20090325948Abstract: The present invention relates to compounds that are selective and/or potent inhibitors of UPPS. In addition to compounds which inhibit UPPS, the invention also provides pharmaceutical compositions comprising these compounds and methods of using these compounds for treating bacterial disease, such as bacterial infection.Type: ApplicationFiled: July 25, 2007Publication date: December 31, 2009Inventors: Timothy Brian Hurley, Kwangho Lee, Stefan Peukert, Sompong Wattanasin
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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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Publication number: 20090291940Abstract: Disclosed is an aminopyrrolidine compound represented by the formula [I] or a pharmaceutically acceptable salt thereof. The compound or the salt is useful as a prophylactic/therapeutic agent for mode disorder such as depression, anxiety disorder, anorexia, cachexia, pain and drug dependence, whose action relies on the MC4 receptor antagonistic effect.Type: ApplicationFiled: March 30, 2007Publication date: November 26, 2009Applicants: Taisho Pharmaceutical Co., Ltd., Nissan Chemical Industries, Ltd.Inventors: Taketoshi Okubo, Toshihito Kumagai, Takaaki Ishii, Toshio Nakamura, Kumi Abe, Yuri Amada, Tomoko Ishizaka, Xiang-Min Sun, Yoshinori Sekiguchi, Shigetada Sasako, Takanori Shimizu, Takayuki Nagatsuka
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Publication number: 20090246169Abstract: Compounds of a certain formula I, in which R1, R2, R3, R4, R5 and R6 have the meanings indicated in the description, are effective compounds with anti-proliferative and/or apoptosis inducing activity.Type: ApplicationFiled: February 21, 2007Publication date: October 1, 2009Inventors: Matthias Vennemann, Thomas Bar, Jürgen Braunger, Astrid Zimmermann, Volker Gekeler
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Publication number: 20090215766Abstract: The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.Type: ApplicationFiled: August 6, 2008Publication date: August 27, 2009Inventors: James D. Rodgers, Darius J. Robinson, Argyrios G. Arvanitis, Thomas P. Maduskuie, JR., Stacey Shepard, Louis Storace, Haisheng Wang, Maria Rafalski, Ravi Kumar Jalluri, Andrew P. Combs, Matthew L. Crawley
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Patent number: 7531550Abstract: Pseudobase benzo[c]phenanthridines and the pharmaceutically acceptable salts thereof of Formula I are provided herein. The variables R, R1, R2, R3, and R4 are defined herein. Certain pseudobase benzo[c]phenanthridines provided herein act as prodrugs, targeting the parent benzo[c]phenanthridinium alkaloid to hydrophilic or hydrophobic regions in the body. Pharmaceutical compositions comprising a pseudobase benzo[c]phenanthridine and a carrier, excipient, or diluent are provided herein. Methods of treating or preventing microbial, fungal and or viral infections and methods of treating diseases and disorders responsive to protein kinase C modulation, topoisomerase I, and/or topoisomerase II modulation are also provided.Type: GrantFiled: July 31, 2007Date of Patent: May 12, 2009Assignee: Yale UniversityInventors: Kenneth Shaw, Mingbao Zhang
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Publication number: 20090068577Abstract: The present invention provides a naphthalenetetracarboxylic acid diimide derivative represented by the following general formula (1): wherein R1 and R2, which are identical or different, each represent a substituted or non-substituted alkyl group or a substituted or non-substituted aromatic hydrocarbon group; R3 represents an alkyl group having 1 to 8 carbon atoms or an aromatic hydrocarbon group; R4, R5, R6 and R7, which are identical or different, each represent a hydrogen atom, a substituted or non-substituted alkyl group, or a substituted or non-substituted aromatic hydrocarbon group; and R1 and R2 may be linked to form a substituted or non-substituted heterocyclic group including a nitrogen atom; with compounds where all of R1, R2 and R3 are a methyl group, and compounds where both of R1 and R2 are a methyl group and R3 is a 1-octyl group being excluded.Type: ApplicationFiled: September 5, 2008Publication date: March 12, 2009Applicant: RICOH COMPANY, LTD.Inventors: Masafumi OHTA, Tomoyuki SHIMADA, Yuuji TANAKA, Eiji KURIMOTO, Keisuke SHIMOYAMA
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Patent number: 7501435Abstract: The instant invention provides for compounds which comprise substituted triazoloquinazolinones that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.Type: GrantFiled: April 24, 2007Date of Patent: March 10, 2009Assignee: Merck & Co., Inc.Inventors: Kenneth L. Arrington, Edward J. Brnardic, Vadim Y. Dudkin, Mark E. Fraley, Shaei Y. Huang, Cheng Wang
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Publication number: 20090048246Abstract: Compositions comprising extracts or isolated or purified compounds from plants of the genus Corydalis provide prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, and metabolic syndrome. Corydalis compounds and their derivatives of natural and synthetic origins lower total cholesterol, LDL-cholesterol, and triglycerides and increase hepatic LDL receptor expression and activate AMP-activated protein kinase. Specific stereoisomers of Corydalis compounds with lipid lowering activity include 14R-(+)-corypalmine, 14R,13S-(+)-corydaline, 14R-(+)-tetrahydropalmatin, (+)-corlumidin, d-(+)-bicuculline, and (+)-egenine.Type: ApplicationFiled: June 20, 2008Publication date: February 19, 2009Inventors: Haiyan Liu, Junbo Wang, Rui Zhang, Nicholas Cairns, Jingwen Liu
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Patent number: 7479557Abstract: The invention is directed to a compound having the general formula (I): wherein each of La and Lb is an independently selected from a linking moiety comprising 0 to 10 main chain atoms, optionally substituted; each of Za and Zb is an independently selected complexing moiety comprising at least one nitrogen atom; either both or one of Za and/or Zb is coordinatively bonded to a respective transition metal complex MaVa and MbVb through said nitrogen atom, wherein each of Ma and Mb is an independently selected transition metal, and each of Va and Vb is an independently selected valence group.Type: GrantFiled: June 10, 2004Date of Patent: January 20, 2009Assignee: Agency for Science, Technology +ResearchInventors: Zhiqiang Gao, Fang Xie
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Publication number: 20090018127Abstract: 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: ApplicationFiled: May 29, 2006Publication date: January 15, 2009Inventors: Rolf Baenteli, Fraser Glickman, Jiri Kovarik, Ian Lewis, Markus Streiff, Gebhard Thoma, Hans-Gunter Zerwes
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Publication number: 20090001354Abstract: A thin film transistor comprises a layer of organic semiconductor material comprising a tetracarboxylic diimide naphthalene-based compound having, attached to one or both of the imide nitrogen atoms, a substituted or unsubstituted heterocycloalkyl ring system. Such transistors can further comprise spaced apart first and second contacts or electrodes in contact with said material. Further disclosed is a process for fabricating an organic thin-film transistor device, preferably by sublimation deposition onto a substrate, wherein the substrate temperature is no more than 200° C.Type: ApplicationFiled: June 29, 2007Publication date: January 1, 2009Inventors: Deepak Shukla, Thomas R. Welter, Wendy G. Ahearn
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Patent number: 7446110Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner.Type: GrantFiled: September 2, 2004Date of Patent: November 4, 2008Assignee: Merck & Co., Inc.Inventors: Mildred L. Kaufman, Robert S. Meissner, Helen J. Mitchell
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Patent number: 7442710Abstract: The present invention relates to compounds of general formula IA or IB wherein X1 and X2 are each independently N or C—R? and R1, R2,R3, R4, R5, and R6 are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The compounds can be used for the treatment of diseases related to the glycine transporter inhibitor, such as schizophrenia and Alzheimer's disease.Type: GrantFiled: January 24, 2006Date of Patent: October 28, 2008Assignee: Hoffman-La Roche Inc.Inventors: Synese Jolidon, Robert Narquizian, Roger David Norcross, Emmanuel Pinard
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Patent number: 7435726Abstract: This invention relates to compositions comprising thalidomide and another anti-cancer drug which can be used in the treatment or prevention of cancer. Preferred anti-cancer drugs are topoisomerase inhibitors. A particular composition comprises thalidomide, or a pharmaceutically acceptable salt, solvate, or clathrate thereof, and irinotecan. The invention also relates to methods of treating or preventing cancer which comprise the administration of a thalidomide and another anti-cancer drug to a patient in need of such treatment or prevention. The invention further relates to methods of reducing or avoiding adverse side effects associated with the administration of chemotherapy or radiation therapy which comprise the administration of thalidomide to a patient in need of such reduction or avoidance.Type: GrantFiled: May 14, 2001Date of Patent: October 14, 2008Assignee: Celgene CorporationInventors: Jerome B. Zeldis, Andrew L. Zeitlin, Sol Barer
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Patent number: 7432276Abstract: The present invention provides compounds useful for increasing cellular ATP binding cassette transporter ABCA1 production in mammals, and to methods of using such compounds in the treatment of coronary artery diseases, dyslipidiemias and metabolic syndrome. The invention also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.Type: GrantFiled: December 27, 2006Date of Patent: October 7, 2008Assignee: CV Therapeutics, Inc.Inventors: Matthew Abelman, Robert Jiang, Jeff Zablocki, Dmitry Koltun, Melanie Boze
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Patent number: 7423045Abstract: The present invention provides compounds useful for increasing cellular ATP binding cassette transporter ABCA1 production in mammals, and to methods of using such compounds in the treatment of coronary artery diseases, dyslipidiemias and metabolic syndrome. The invention also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.Type: GrantFiled: June 28, 2006Date of Patent: September 9, 2008Assignee: CV Therapeutics, Inc.Inventors: Matthew Abelman, Robert Jiang, Jeff Zablocki, Dmitry Koltun
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Publication number: 20080214537Abstract: Bridged phenanthridine compounds having the structure of formula I or of formula II are provided: These compounds are useful as cannabinoid receptor ligands and can be prepared as pharmaceutical compositions for the prophylaxis or treatment of a variety of diseases, disorders and conditions including inflammatory pain, visceral pain, postoperative pain, cancer pain, neuropathic pain, musculoskeletal pain, dysmenorrhea, menstrual pain, migraine, headache as well as inflammatory diseases such as rheumatoid arthritis, systemic lupus erythematosus, Crohn's disease, psoriasis, eczema, multiple sclerosis, diabetes and thyroiditis. The compounds can also be used in the treatment of skin disorders, lung disorders, ophthalmic disorders, gastrointestinal disorders, cardiovascular disorders, as well as neurodegenerative, neuroinflammatory and certain psychiatric disorders.Type: ApplicationFiled: February 29, 2008Publication date: September 4, 2008Applicant: CARA THERAPEUTICS, INC.Inventors: Janet L. Ralbovsky, R. Paul Beckett
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1-Heterocyclylalkyl-3-sulfonylazaindole or -azaindazole derivatives as 5-hydroxytryptamine-6 ligands
Patent number: 7411064Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptorType: GrantFiled: February 15, 2006Date of Patent: August 12, 2008Assignee: WyethInventors: Ronald Charles Bernotas, Steven Edward Lenicek, Hassan Mahmoud Elokdah, David Zenan Li -
Patent number: 7405211Abstract: Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). PI 3-kinase generates 3-phosphorylated PI second messengers which stimulate platelet adhesion under blood-flow conditions. Because platelet adhesion is a necessary step in the formation of a thrombus, inhibition by these compounds of PI 3-kinase under such conditions inhibits or prevents thrombus formation.Type: GrantFiled: October 12, 2004Date of Patent: July 29, 2008Assignee: AstraZeneca ABInventors: Alan D. Robertson, Shaun Jackson, Vijaya Kenche, Cindy Yaip, Hishani Parbaharan, Phil Thompson
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Patent number: 7393955Abstract: The invention provides novel classes of Isoquinoline Derivatives. Pharmaceutical compositions and methods of making and using the compounds, are also described.Type: GrantFiled: July 8, 2005Date of Patent: July 1, 2008Assignee: Inotek Pharmaceuticals CorporationInventors: Prakash Jagtap, Aloka Roy, William Williams
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Patent number: 7388016Abstract: The present invention relates to Dibenzonaphthyridine Derivatives, compositions comprising an effective amount of a Dibenzonaphthyridine Derivative and methods for treating or preventing a proliferative disorder, comprising administering to a subject in need thereof an effective amount of a Dibenzonaphthyridine Derivative.Type: GrantFiled: December 6, 2006Date of Patent: June 17, 2008Assignee: WyethInventors: Ariamala Gopalsamy, Mengxiao Shi, Kristina Kutterer, Kim Timothy Arndt
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Patent number: 7381722Abstract: The present invention relates to Tetracyclic Amino Compounds and Tetracyclic Carboxamido Compounds, compositions comprising an effective amount of a Tetracyclic Amino Compound or a Tetracyclic Carboxamido Compound and methods for treating or preventing an inflammatory disease, a reperfusion injury, diabetes, a diabetic complication, reoxygenation injury resulting from organ transplantation, an ischemic condition, Parkinson's disease, renal failure, a vascular disease, a cardiovascular disease, or cancer, comprising administering to a subject in need thereof an effective amount of a Tetracyclic Amino Compound or a Tetracyclic Carboxamido Compound.Type: GrantFiled: February 15, 2006Date of Patent: June 3, 2008Assignee: Inotek Pharmaceuticals CorporationInventors: Prakash Jagtap, Csaba Szabo
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Patent number: 7354918Abstract: The invention relates to novel derivatives of 14,15-dihydro 20,21-dinoreburnamenin-14-ol, having formula (I) in which R represents a radical —AR? wherein A represents a heteroatom and R? represents a group selected from the group comprising linear or branched C1-C6 alkyl radicals, C2-C6 alkenyls, C2-C6 alkynyls, arylalkyls; esters comprising the formula —R1— CO—O—R2; amides comprising the formula —R3—CO—NZY, wherein Y and Z together can form a cycloalkyl radical or a heterocyclic radical, optionally substituted by one or more alkyl radicals; a radical selected from the group comprising alkyl radicals, alkenyls or alkynyls, substituted by at least one amine with formula —NZY; or one of the pharmaceutically-acceptable salts thereof, including the isomers, enantiomers and diastereoisomers thereof and mixtures thereof.Type: GrantFiled: October 13, 2006Date of Patent: April 8, 2008Assignee: BiocortechInventors: Paola Ciapetti, Laurence Deyon, Camille-Georges Wermuth, Jean-François Pujol, Dinah Weissmann
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Patent number: 7351830Abstract: Selective phosphorylation of phenpanstatin (3a) with tetrabutylammonium dihydrogen phosphate and dicyclohexyl-carbodiimide in pyridine followed by cation exchange chromatographic procedures was found to provide an efficient mute to a new series (3b-3d) of promising 3,4-O-cyclic phosphate prodrugs designated phenpanstatin phosphates. Application of analogous reaction conditions to pancratistatin (1a) led to a mixture of monophosphate derivatives where sodium paancratistatin 4-O-phosphate (4a) was isolated and the structure confirmed by x-ray craxtallography. Modification of the reaction conditions allowed direct phosphorylation of pancratistatin followed by cation exchange chromatography to afford sodium pancratistatin 3,4-O-cyclic phosphate (5b) which was selected for preclinical development.Type: GrantFiled: June 18, 2004Date of Patent: April 1, 2008Assignee: Arizona Board of Regents, a body corporate of the State of Arizona, acting for and on behalf of Arizona State UniversityInventors: George R. Pettit, Noeleen Melody
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Patent number: 7320984Abstract: The invention provides a morphinan derivative of the Formula (I): wherein R1 is methyl, cyclopropylmethyl or the like; R2 and R3 are hydroxy, methoxy, acetoxy or the like; both Y and Z are valence bonds, —C(?O)— or the like; X is C2-C5 carbon chain (one of the carbon atoms may be substituted by oxygen, sulfur or nitrogen) constituting a part of the ring structure, or the like; (R4)k is substituted or non-substituted benzene fused ring, carbonyl group or the like; R9 is hydrogen or the like; R10 and R11 are bound to represent —O—, or the like, and R6 is hydrogen or the like or a pharmaceutically acceptable acid addition salt thereof. The invention also provides a therapeutic or prophylactic agent for urinary frequency or urinary incontinence, comprising as an effective ingredient the morphinan derivative or the pharmaceutically acceptable acid addition salt thereof; a method for therapy or prophylaxis of the diseases.Type: GrantFiled: October 8, 2003Date of Patent: January 22, 2008Assignee: Toray Industries, Inc.Inventors: Naoki Izumimoto, Koji Kawai, Kuniaki Kawamura, Morihiro Fujimura, Toshikazu Komagata
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Patent number: 7273865Abstract: The present invention relates to compounds of formula I wherein R1 and R2 are described hereinbelow. These compounds have high affinity to A2A receptors and good selectivity to A1 and A3 receptors. These compounds are useful, inter alia, in the treatment of Alzheimer's disease, depression, Parkinson's disease and ADHD.Type: GrantFiled: September 15, 2004Date of Patent: September 25, 2007Assignee: Hoffmann-La Roche Inc.Inventor: Roger David Norcross
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Patent number: 7268143Abstract: The invention provides novel classes of Isoquinoline Derivatives. Pharmaceutical compositions and methods of making and using the compounds, are also described.Type: GrantFiled: October 12, 2004Date of Patent: September 11, 2007Assignee: Inotek Pharmaceuticals CorporationInventors: Prakash Jagtap, Csaba Szabo, Andrew L. Salzman, Aloka Roy, William Williams
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Patent number: 7217709Abstract: The invention relates to Tetracyclic Benzamide Derivatives; compositions comprising a Tetracyclic Benzamide Derivative; and methods for treating or preventing an inflammatory disease, a reperfusion disease, an ischemic condition, renal failure, diabetes, a diabetic complication, a vascular disease, or cancer, comprising administering to a subject in need thereof an effective amount of a Tetracyclic Benzamide Derivative.Type: GrantFiled: February 26, 2004Date of Patent: May 15, 2007Assignee: Inotek Pharmaceuticals CorporationInventors: Prakash Jagtap, Csaba Szabo
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Patent number: 7115619Abstract: The present invention pertains to certain N8,N13-disubstituted quino[4,3,2-kl]acridinium salts of formula (Q?) which inhibit telomerase wherein: p is an integer from 0 to 4; q is an integer from 0 to 3; r is an integer from 0 to 4; each RA is —H or a ring substituent; each RB is —H or a ring substituent; each RC is —H or a ring substituent; RN8 is a nitrogen substituent; RN13 is a nitrogen substituent; and, Q is an anion. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit telomerase, to regulate cell proliferation, and in the treatment of proliferative conditions, such as cancer.Type: GrantFiled: October 12, 2001Date of Patent: October 3, 2006Assignee: Cancer Research Technology LimitedInventors: Malcolm F. G. Stevens, Lloyd R Kelland, Robert A Heald
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Patent number: 7064202Abstract: The present invention relates to novel intermediates and prodrugs of camptothecin and related analogs.Type: GrantFiled: May 12, 2004Date of Patent: June 20, 2006Assignees: University of Kentucky Research Foundation, University of PittsburghInventors: Thomas G. Burke, deceased, Dennis P. Curran, Wu Du
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Patent number: 7064124Abstract: A NF-?B inhibitor represented by the following formula (I) is provided: ?Type: GrantFiled: March 27, 2002Date of Patent: June 20, 2006Assignees: Daiichi Suntory Pharma Co., Ltd., Daiichi Suntory Biomedical Research Co., Ltd.Inventors: Kenji Suzuki, Yoichi Nunokawa, Naohisa Ogou
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1-heterocyclylalkyl-3-sulfonylazaindole or -azaindazole derivatives as 5-hydroxytryptamine-6 ligands
Patent number: 7057039Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.Type: GrantFiled: July 17, 2003Date of Patent: June 6, 2006Assignee: WyethInventors: Ronald Charles Bernotas, Steven Edward Lenicek, Hassan Mahmoud Elokdah, David Zenan Li