Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/243)
  • METHODS OF TREATMENT FOR MRSA INFECTIONS
    Publication number: 20110251162
    Abstract: The present subject matter relates to pathogenesis of MRSA. Specifically, the present disclosures identifies the pro-inflammatory properties of PVL as the cause of MRSA. Viewed from this new perspective, the present subject matter achieves novel methods and apparatus for treating MRSA infection in a subject involving the administration of an anti-inflammatory drug to the subject. Furthermore the present subject matter teaches methods and apparatus for treating a Panton-Valetine leukocidin associated infection in a subject involving the administration of an anti-inflammatory drug to the subject.
    Type: Application
    Filed: September 25, 2009
    Publication date: October 13, 2011
    Applicant: CEDARS-SINAI MEDICAL CENTER
    Inventors: George Y. Liu, Ching Wen Tseng
  • METHOD FOR TREATING A PULMONARY HYPERTENSION CONDITION
    Publication number: 20110245253
    Abstract: A method for treating a pulmonary hypertension condition such as pulmonary arterial hypertension (PAH) in a subject comprises administering to the subject a therapeutically effective amount of ambrisentan, wherein, at baseline, time from first diagnosis of the condition in the subject is not greater than about 2 years.
    Type: Application
    Filed: June 16, 2011
    Publication date: October 6, 2011
    Inventors: Michael J. Gerber, Christopher Dufton
  • USE OF A COMPOUND CAPABLE OF REDUCING THE URIC ACID LEVEL FOR THE PREVENTION AND/OR THE TREATMENT OF LUNG INFLAMMATION AND FIBROSIS
    Publication number: 20110243911
    Abstract: The present invention is directed to the use of a compound capable of reducing the uric acid level in a mammal for the prevention and/or the treatment of IL-1? driven lung pathology, particularly to treat lung inflammation such as chronic fibrosis, COPD and interstitial fibrosis and other IL-1? driven lung pathologies including those of autoimmune origin. Preferred compounds capable of reducing the uric acid level are selected from the group consisting of xanthine oxidase inhibitors, such as allopurinol, recombinant enzyme uricase and uricosuric compound capable of enhancing uric acid excretion, such as probenecid. The invention further relates to a method for identifying in vitro whether a patient presents an IL-1? driven lung pathology or is at risk to develop an IL-1? driven lung pathology, or for the screening of a compound for treating an IL-1? driven lung pathology.
    Type: Application
    Filed: September 18, 2009
    Publication date: October 6, 2011
    Inventors: Bernhard Ryffel, Isabelle Couillin
  • METHODS AND COMPOSITIONS FOR THE TREATMENT OF OCULAR DISORDERS
    Publication number: 20110243999
    Abstract: The invention provides methods and compositions for the delivery of lipophilic drugs that are useful for the treatment of various ophthalmological diseases, disorders, and pathologies, including the treatment of age-related macular degeneration, diabetic retinopathy, diabetic macular edema, cancer, and glaucoma.
    Type: Application
    Filed: April 4, 2011
    Publication date: October 6, 2011
    Inventors: Luis A. DELLAMARY, Arek TABAK, Shiyin YEE
  • PYRROLOTRIAZINE KINASE INHIBITORS
    Publication number: 20110245252
    Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of Trk receptors such as TrkA, TrkB, TrkC or Flt-3 thereby making them useful as anticancer agents.
    Type: Application
    Filed: June 14, 2011
    Publication date: October 6, 2011
    Inventors: Brian E. Fink, Ping Chen
  • FAST DISSOLVING DRUG DELIVERY SYSTEMS
    Publication number: 20110237563
    Abstract: The present invention related to the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for treating illnesses of patient with critical buccal condition, leading to difficulties in swallowing oral medicine forms and thus difficulties in treating said illnesses. Particularly, the present invention discloses the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for treating illnesses of patient with dysphagia and/or odynophagia and/or aspiration risk. Another aspect of the present invention is the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for the treatment of dysphagia and/or odynophagia and/or aspiration risk.
    Type: Application
    Filed: March 23, 2010
    Publication date: September 29, 2011
    Inventor: Dominique Costantini
  • HETEROCYCLIC COMPOUNDS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
    Publication number: 20110224195
    Abstract: The present invention is directed to substituted six-membered heterocyclic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as obesity and diabetes, particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.
    Type: Application
    Filed: August 18, 2008
    Publication date: September 15, 2011
    Inventors: Tesfaye Biftu, Danqing Feng, Ann E. Weber, Jason M. Cox, Xiaoxia Qian, Jinyou Xu
  • AZOLOTRIAZINONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS
    Publication number: 20110218185
    Abstract: The present application provides compounds that are useful as MCHR1 antagonists, especially for the treatment of obesity, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein the variables are defined herein.
    Type: Application
    Filed: October 8, 2009
    Publication date: September 8, 2011
    Inventors: Pratik Devasthale, William N. Washburn, Kishore V. Renduchintala, Radhakrishnan Sridhar
  • Fused Bicyclic mTOR Inhibitors
    Publication number: 20110218183
    Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
    Type: Application
    Filed: May 13, 2011
    Publication date: September 8, 2011
    Inventors: Xin Chen, Heather Coate, Andrew Philip Crew, Han-Qing Dong, Ayako Honda, Mark Joseph Mulvihill, Paula A.R. Tavares, Jing Wang, Douglas S. Werner, Kristen Michelle Mulvihill, Kem W. Siu, Bijoy Panicker, Apoorba Bharadwaj, Lee D. Arnold, Meizhong Jin, Brian Volk, Qinghua Weng, James David Beard
  • CHEMICAL MODULATORS OF PRO-APOPTOTIC BAX AND BCL-2 POLYPEPTIDES
    Publication number: 20110218155
    Abstract: The invention provides a method for identifying a compound which modulates the activity of a BCL-2 family polypeptide, the method comprising: a) contacting said BCL-2 family polypeptide with a compound under conditions suitable for modulation of the activity of said BCL-2 family polypeptide; and b) detecting modulation of the activity of said BCL-2 family polypeptide by the compound, wherein the compound interacts with a binding site comprising one or more of an ?1 helix, ?2 helix, a loop between ?1-?2, ?.6 helix, and select residues of ?4, ?.5, and ?.8 helices in said BCL-2 family polypeptide; wherein the interaction of the compound with the binding site occurs at a horizontal hydrophobic groove with or without a perimeter of charged and hydrophilic residues, a superior juxta-loop, an inferior juxta-loop, or combination thereof.
    Type: Application
    Filed: October 9, 2009
    Publication date: September 8, 2011
    Applicant: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Loren D. Walensky, Evripidis Gavathiotis
  • IMIDAZO[1,2-B][1,2,4]TRIAZINES AS C-MET INHIBITORS
    Publication number: 20110212967
    Abstract: The present invention relates to imidazo[1,2-b][1,2,4]triazines that are inhibitors of c-Met and are useful in the treatment of c-Met associated diseases including cancer.
    Type: Application
    Filed: February 2, 2011
    Publication date: September 1, 2011
    Applicant: INCYTE CORPORATION
    Inventors: Jincong Zhuo, Chunhong He, Wenqing Yao
  • USE OF MULTI-PHARMACOPHORE COMPOUNDS TO TREAT NASAL DISORDERS
    Publication number: 20110195962
    Abstract: Compositions and methods for treating nasal disorders associated with nasal inflammation using a multipharmacophoric agent (MPA) that can prevent the production and/or release of at least one or more pro-inflammatory cytokines (for instance IL-1 and TNF?) and inhibit p38 MAP kinase or at least one matrix metalloproteinases (MMP-1 and MMP-9) are disclosed.
    Type: Application
    Filed: April 18, 2011
    Publication date: August 11, 2011
    Applicant: ALCON RESEARCH, LTD.
    Inventors: Najam A. Sharif, Martin B. Wax
  • Tricyclic 1,2,4-triazine oxides and compositions for therapeutic use in cancer treatments
    Patent number: 7989451
    Abstract: The invention relates to novel tricyclic 1,2,4-triazine-1-oxides and novel tricyclic 1,2,4-triazine-1,4-dioxides of formula I and to related analogues, to their preparation, and to their use as hypoxia-selective drugs and radiosensitizers for cancer therapy, both alone or in combination with radiation and/or other anticancer drugs.
    Type: Grant
    Filed: March 31, 2006
    Date of Patent: August 2, 2011
    Assignee: Auckland Uniservices Limited
    Inventors: Michael Patrick Hay, Adrian Blaser, William Alexander Denny, Kevin Owen Hicks, Ho Huat Lee, Karin Pchalek, Frederik Bastiaan Pruijn, Bronwyn Gae Siim, William Robert Wilson, Shangjin Yang
  • AROMATIC RING FUSED TRIAZINE DERIVATIVES AND USES THEREOF
    Publication number: 20110183972
    Abstract: The invention belongs to pharmaceutical field. The invention relates to the compounds according to Formula I, including their optically active forms, pharmaceutically acceptable salts or hydrates, and the pharmaceutical composition comprising thereof as active ingredient; uses in the preparation of vascular endothelial growth factor receptor tyrosine kinase inhibitors, and uses in the preparation of medicament for the treatment and/or prevention of cancer.
    Type: Application
    Filed: February 10, 2009
    Publication date: July 28, 2011
    Applicant: SHENYANG PHARMACEUTICAL UNIVERSITY
    Inventors: Linxiang Zhao, Jinling Lv, Rui Wang, Dan Liu, Yongkui Jing
  • HETEROCYCLIC COMPOUND AS PROTEIN KINASE INHIBITOR
    Publication number: 20110183983
    Abstract: Provided are novel heterocyclic compounds useful as anti-cancer drugs by suppressing protein kinase activities of growth factor receptors such as c-Met, pharmaceutical compositions containing the same, and methods for using the compound.
    Type: Application
    Filed: August 28, 2009
    Publication date: July 28, 2011
    Applicant: NEOPHARM CO., LTD.
    Inventors: Tae-Seong Kim, Eunkyung Lee, Doyoung Kim, Bu-mahn Park, Jiyeon Park, JungJe Joo
  • Pyrrolotriazine kinase inhibitors
    Patent number: 7982033
    Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of Trk receptors such as TrkA, TrkB, TrkC or Flt-3 thereby making them useful as anticancer agents.
    Type: Grant
    Filed: November 2, 2007
    Date of Patent: July 19, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Brian E. Fink, Ping Chen
  • Tetracyclic fused heterocyclic compound and use thereof as HCV polymerase inhibitor
    Patent number: 7977331
    Abstract: The present invention relates to a tetracyclic fused heterocyclic compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: July 12, 2011
    Assignee: Japan Tobacco Inc.
    Inventors: Takahiro Oka, Kazutaka Ikegashira, Shintaro Hirashima, Hiroshi Yamanaka, Satoru Noji, Yasushi Niwa, Yoko Matsumoto, Toshihiro Sato, Izuru Ando, Yukihiro Nomura
  • Polymorphic forms of vardenafil
    Patent number: 7977478
    Abstract: Crystalline polymorphic forms of vardenafil and vardenafil hydrochloride, and processes for preparing them.
    Type: Grant
    Filed: September 27, 2006
    Date of Patent: July 12, 2011
    Assignees: Dr. Reddy's Laboratories Limited, Dr. Reddy's Laboratories, Inc.
    Inventors: Eswaraiah Sajja, Ravindar Reddy Koppera, Satyanarayana Revu, Venkata Reddy Vajrala, Vijayapal Reddy Kanumathi
  • PIPERIDINE DERIVATIVES AS JAK3 INHIBITORS
    Publication number: 20110165183
    Abstract: The invention provides a compound of formula (I): wherein W is a bicyclic heteroaromatic group; or a salt thereof. The compounds and salts thereof have beneficial therapeutic properties (e.g. immunosuppressant properties).
    Type: Application
    Filed: July 31, 2009
    Publication date: July 7, 2011
    Applicant: BioCryst Pharmaceuticals, Inc.
    Inventors: Yarlagadda S. Babu, Pooran Chand, Pravin L. Kotian, V. Satish Kumar
  • Pyrimidotriazinediones and Pyrimidopyrimidinediones and Methods of Using the Same
    Publication number: 20110166144
    Abstract: The present disclosure is directed to pyrimidotriazinediones and pyrimidopyrimidinediones having a formula (I), (II), or (III), or a mixture or pharmaceutically acceptable salt or hydrate thereof, and to methods of treating cancer comprising administering the same.
    Type: Application
    Filed: July 30, 2009
    Publication date: July 7, 2011
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: H.D. H. Showalter, Anjanette J. Turbiak, Eric R. Fearon, Guido T. Bommer
  • DRUGS TO PREVENT HPV INFECTION
    Publication number: 20110165220
    Abstract: A method of inhibiting HPV virus infection is disclosed. In one embodiment, the method involves exposing a papillomavirus to an effective amount of a compound selected from the group consisting of Compound 13, Compound 14, and analogs of Compounds 13 and 14. In another embodiment, the method involves administering an inhibitor selected from the group consisting of Compound 13, Compound 14, and analogs of Compounds 13 and 14 to a susceptible tissue or cell.
    Type: Application
    Filed: May 29, 2009
    Publication date: July 7, 2011
    Inventors: Paul F. Lambert, Paul G. Ahlquist, Dohun Pyeon, Hao Shun Huang
  • HETEROCYCLIC AMIDE COMPOUNDS USEFUL AS KINASE INHIBITORS
    Publication number: 20110160207
    Abstract: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.
    Type: Application
    Filed: March 2, 2011
    Publication date: June 30, 2011
    Inventors: Stephen T. Wrobleski, Jagabandhu Das, T.G. Murali Dhar, Alaric J. Dyckman, John Hynes, Katerina Leftheris, James Lin, Shuqun Lin
  • NOVEL THIENOPYRROLE COMPOUNDS
    Publication number: 20110152243
    Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Application
    Filed: December 21, 2010
    Publication date: June 23, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: Neil Wishart, Theresa Dunstan, Jeremy J. Edmunds, Anna M. Ericsson, Catherine R. Ferenz, Adrian D. Hobson, David C. Ihle, Kent D. Stewart, Lei Wang, Lu Wang
  • TRIAZOLOTRIAZINES AS KINASE INHIBITORS
    Publication number: 20110144113
    Abstract: The present invention is directed to [1,2,4]triazolo[4,3-b][1,2,4]triazines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.
    Type: Application
    Filed: February 24, 2011
    Publication date: June 16, 2011
    Inventors: Jincong Zhuo, Colin Zhang, Meizhong Xu, Ding-Quan Qian, Wenqing Yao, Ravi Kumar Jalluri
  • IMIDAZOTRIAZINES AND IMIDAZOPYRIMIDINES AS KINASE INHIBITORS
    Publication number: 20110136781
    Abstract: The present invention is directed to imidazo[1,2-b][1,2,4]triazines and imidazo[1,2-a]pyrimidines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.
    Type: Application
    Filed: June 10, 2010
    Publication date: June 9, 2011
    Applicant: Incyte Corporation
    Inventors: Jincong ZHUO, Meizhong XU, Chunhong HE, Colin ZHANG, Ding-Quan QIAN, David M. BURNS, Yun-Long LI, Brian METCALF, Wenqing YAO
  • Agent for repairing corneal sensitivity containing amide compound
    Patent number: 7956072
    Abstract: The amide compound of the formula (I) [each symbol is as defined in the description] has a promoting action on neuritogenesis of trigeminal nerve cells, and the compound is useful as a corneal neuritogenesis promoter, an agent for recovering corneal sensitivity by promotion of corneal neuritogenesis, and an agent for treating dry eye.
    Type: Grant
    Filed: November 3, 2008
    Date of Patent: June 7, 2011
    Assignees: Senju Pharmaceutical Co., Ltd., Mitsubishi Tanabe Pharma Corporation
    Inventors: Yoshiko Takayama, Yoshikuni Nakamura, Jun Inoue, Mitsuyoshi Azuma
  • FUSED HETEROCYCLIC COMPOUNDS USEFUL AS KINASE MODULATORS
    Publication number: 20110124640
    Abstract: Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are useful as kinase modulators, including Btk modulation, wherein R1, R2, R3, R4, Q, A and B are as defined herein.
    Type: Application
    Filed: July 23, 2009
    Publication date: May 26, 2011
    Inventors: Chunjian Liu, Katerina Leftheris, Andrew J. Tebben
  • PYRROLOTRIAZINE KINASE INHIBITORS
    Publication number: 20110124623
    Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.
    Type: Application
    Filed: January 28, 2011
    Publication date: May 26, 2011
    Inventors: Mark D. Wittman, Harold Mastalerz, Kurt Zimmermann, Mark G. Saulnier, Upender Velaparthi, Dolatrai M. Vyas, Guifen Zhang, Walter Lewis Johnson, David B. Frennesson, Xiaopeng Sang, Peiying Liu, David R. Langley
  • Fused bicyclic mTOR inhibitors
    Patent number: 7943767
    Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
    Type: Grant
    Filed: November 20, 2009
    Date of Patent: May 17, 2011
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Xin Chen, Heather Coate, Andrew Philip Crew, Han-Qing Dong, Ayako Honda, Mark Joseph Mulvihill, Paula A. R. Tavares, Jing Wang, Douglas S. Werner, Kristen Michelle Mulvihill, Kam W. Siu, Bijoy Panicker, Apoorba Bharadwaj, Lee D. Arnold, Meizhong Jin, Brian Volk, Quinghua Weng, James David Beard
  • FXA INHIBITORS WITH CYCLIC AMIDOXIME OR CYCLIC AMIDRAZONE AS P4 SUBUNIT, PROCESSES FOR THEIR PREPARATIONS, AND PHARMACEUTICAL COMPOSITIONS AND DERIVATIVES THEREOF
    Publication number: 20110112083
    Abstract: The present invention relates to novel oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone group, pharmaceutically acceptable salts thereof, methods for preparing the same and pharmaceutical compositions comprising the same. The oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone group or the pharmaceutically acceptable salts thereof can be effectively used for the treatment of thromboembolism and tumor as an anticoagulant based on the inhibition of factor Xa.
    Type: Application
    Filed: June 5, 2009
    Publication date: May 12, 2011
    Applicant: LEGOCHEM BIOSCIENCE LTD.
    Inventors: Ho Young Song, Young Lag Cho, Dae Yon Lee, Hee Sock Park, Sung Yoon Baek, Sang Eun Chae, Sang Hui Jo, Yeon Ok Kim, Hyang Sook Lee, Ju Hyun Park, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim
  • COMPOSITIONS AND METHODS RELATING TO HIV PROTEASE INHIBITION
    Publication number: 20110105477
    Abstract: The present invention relates to HIV protease, and methods for inhibiting the function of HIV protease. In particular, present invention provides compounds that inhibit or block the biological activity of HIVp, thereby causing the replication of the HIV virus to be inhibited or to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS. The compounds and formulations also find use in diagnostic and research settings.
    Type: Application
    Filed: September 12, 2008
    Publication date: May 5, 2011
    Applicant: The Regents of the University of Michigan
    Inventors: Heather A. Carlson, Kelly L. Damm, Kristen L. Meagher
  • Crystalline forms of [(1R), 2S]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy]-1-methylethyl ester
    Patent number: 7932383
    Abstract: Crystalline form, Form N-1, of [(1R),2S]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy]-1-methylethyl ester (Compound I) is provided. Also provided are a pharmaceutical composition and an oral dosage form comprising the Form N-1 of Compound I as well as a method of using the Form N-1 of Compound I in the treatment of cancer and other proliferative diseases.
    Type: Grant
    Filed: June 8, 2009
    Date of Patent: April 26, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventor: John E. Thornton
  • Reverse-turn mimetics and method relating thereto
    Patent number: 7932384
    Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.
    Type: Grant
    Filed: July 27, 2009
    Date of Patent: April 26, 2011
    Assignee: Choongwae Pharma Corporation
    Inventors: Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen, Soo Jin Lee
  • ALPHA HELIX MIMETICS AND METHODS RELATING THERETO
    Publication number: 20110092459
    Abstract: Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a compound relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.
    Type: Application
    Filed: June 5, 2009
    Publication date: April 21, 2011
    Applicant: PRISM Biolab Corporation
    Inventors: Takenao Odagami, Yuji Kogami, Hiroyuki Kouji
  • RADIOSENSITIZATION OF TUMORS WITH INDAZOLPYRROLOTRIAZINES FOR RADIOTHERAPY
    Publication number: 20110086850
    Abstract: Provided herein is a method of radiosensitizing a tumor in a subject, which comprises administering to the subject a radiosensitizing amount of an indazolpyrrolotriazine of Formula I. Also provided herein is a method of treating a tumor in a subject, which comprises the steps of administering to the subject a radiosensitizing amount of an indazolpyrrolotriazine of Formula I, and a therapeutically effective fraction of radiation.
    Type: Application
    Filed: April 10, 2009
    Publication date: April 14, 2011
    Applicant: Board of Regents, The University of Texas System
    Inventors: Kie-Kian Ang, Luka Milas
  • Fused bicyclic mTor inhibitors
    Patent number: 7923555
    Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
    Type: Grant
    Filed: December 2, 2008
    Date of Patent: April 12, 2011
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Xin Chen, Heather Coate, Andrew Philip Crew, Hanqing Dong, Ayako Honda, Mark Joseph Mulvihill, Paula A. R. Tavares, Jing Wang, Douglas S. Werner, Kristen Michelle Mulvihill, Kam W. Siu, Bijoy Panicker, Apoorba Bharadwaj, Lee D. Arnold, Meizhong Jin, Brian Volk, Quinghua Weng, James David Beard
  • SUBSTITUTED IMIDAZOTRIAZINES
    Publication number: 20110082147
    Abstract: This invention relates to novel substituted imidazotriazines and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a compound showing partial-agonist activity at the GABA ?2, ?3 and ?5 subtype receptors, and antagonist activity at the al subtype receptor.
    Type: Application
    Filed: July 23, 2010
    Publication date: April 7, 2011
    Applicant: CoNCERT Pharmaceuticals, Inc.
    Inventors: Scott L. Harbeson, Roger D. Tung, Julie F. Liu
  • Peptide deformylase inhibitors
    Patent number: 7919528
    Abstract: Novel PDF inhibitors and novel methods for their use are provided.
    Type: Grant
    Filed: May 30, 2003
    Date of Patent: April 5, 2011
    Assignee: GlaxoSmithKline LLC
    Inventors: Kelly M. Aubart, Andrew B. Benowitz, Siegfried B. Christensen, IV, Joseph M. Karpinski, Jinhwa Lee, Domingos J. Silva
  • Triazolotriazines as kinase inhibitors
    Patent number: 7915408
    Abstract: The present invention is directed to [1,2,4]triazolo[4,3-b][1,2,4]triazines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.
    Type: Grant
    Filed: January 28, 2010
    Date of Patent: March 29, 2011
    Assignee: Incyte Corporation
    Inventors: Jincong Zhuo, Colin Zhang, Meizhong Xu, Ding-Quan Qian, Wenqing Yao, Ravi Kumar Jalluri
  • HETEROCYCLIC OXIME COMPOUNDS
    Publication number: 20110065708
    Abstract: The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).
    Type: Application
    Filed: August 19, 2010
    Publication date: March 17, 2011
    Applicant: NOVARTIS AG
    Inventors: Miao DAI, Xingnian FU, Feng HE, Lei JIANG, Yue LI, Fang LIANG, Lei LIU, Yuan MI, Yao-chang XU, Guoliang XUN, Xiaoxia YAN, Zhengtian YU, Ji Yue ZHANG
  • AURORA KINASE MODULATORS AND METHOD OF USE
    Publication number: 20110065709
    Abstract: The present invention relates to chemical compounds having a general formula I wherein A1-5 and 7-8, D?, L1, L2, R1, R3, R6-8, n and o are defined herein, and synthetic intermediates, which are capable of modulating the activity of Aurora kinase proteins and, thereby, influencing various disease states and conditions related to the activities of Aurora kinases. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.
    Type: Application
    Filed: March 19, 2009
    Publication date: March 17, 2011
    Applicant: Amgen Inc.
    Inventors: Ryan White, Jason Human
  • Insecticidal N-substituted sulfoximines
    Patent number: 7897782
    Abstract: N-Substituted sulfoximines are effective at controlling insects.
    Type: Grant
    Filed: November 11, 2009
    Date of Patent: March 1, 2011
    Assignee: Dow AgroSciences LLC
    Inventors: Yuanming Zhu, Richard B. Rogers, Jim X. Huang
  • USE OF PDE5 INHIBITORS FOR TREATING CIRCADIAN RHYTHM DISORDERS
    Publication number: 20110046141
    Abstract: A method of altering circadian rhythm in a mammal is provided. In certain embodiments, the method comprising: administering to the mammal a PDE5 inhibitor, e.g., sildenafil, vardenafil, tadalafil or zaprinast. The method may be employed to prevent a circadian rhythm disorders including, but not limited to transmeridian flight disorder (i.e., “jet-lag”), shiftwork-related disorder, seasonal affected disorder and insomnia by phase delay or phase advance.
    Type: Application
    Filed: May 29, 2008
    Publication date: February 24, 2011
    Applicants: CONSEJO NACIONAL DE INVESTIGACIONES CIENTIFICAS Y TECNICAS (CONICET), UNIVERSIDAD NACIONAL DE QUILMES
    Inventors: Diego Andrés Golombek, Patricia Verónica Agostino, Santiago Andrés Plano, Gabriela Alejandra Ferreyra
  • METHODS FOR THE PRODUCTION OF FUNCTIONAL PROTEIN FROM DNA HAVING A NONSENSE MUTATION AND THE TREATMENT OF DISORDERS ASSOCICATED THEREWITH
    Publication number: 20110046136
    Abstract: The present invention relates to functional proteins encoded by nucleic acid sequences comprising a nonsense mutation. The present invention also relates to methods for the production of functional proteins encoded by nucleic acid sequences comprising a nonsense mutation and the use of such proteins for prevention, management and/or treatment of diseases associated with a nonsense mutation(s) in a gene.
    Type: Application
    Filed: March 29, 2007
    Publication date: February 24, 2011
    Applicant: THERAPEUTICS, INC.
    Inventors: Neil G. Almstead, Guangming Chen, Hirawat Samit, Peter Seongwoo Hwang, Gary M. Karp, Langdon Miller, Young-Choon Moon, Hongyu Ren, James J. Takasugi, Ellen M. Welch, Richard G. Wilde, Paul Kennedy
  • Tetrahydrocyclopenta[b]indole Androgen Receptor Modulators
    Publication number: 20110039855
    Abstract: The present invention provides a compound of the Formula (I), or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating or preventing physiological disorders, particularly reduced bone mass, osteoporosis, osteopenia, reduced muscle mass or strength, or erectile dysfunction comprising administering a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: May 14, 2009
    Publication date: February 17, 2011
    Applicant: ELI LILLY AND COMPANY
    Inventors: Prabhakar Kondaji Jadhav, Venkatesh Krishnan, Euibong Jemes Kim
  • PYRROLOTRIAZINE COMPOUNDS AS KINASE INHIBITORS
    Publication number: 20110039838
    Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
    Type: Application
    Filed: October 25, 2010
    Publication date: February 17, 2011
    Inventors: Brian E. Fink, Ashvinikumar V. Gavai, Gregory D. Vite, Ping Chen, Harold Mastalerz, Derek J. Norris, John S. Tokarski, Yufen Zhao, Wen-Ching Han
  • NON-BASIC MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS
    Publication number: 20110034375
    Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I. where R1, R1a, R1b, A, R3, R4, R5, R5b and R6 are as defined herein.
    Type: Application
    Filed: October 19, 2010
    Publication date: February 10, 2011
    Inventors: William N. Washburn, Saleem Ahmad, Andres S. Hernandez
  • ORODISPERSABLE FORMULATIONS OF PHOSPHODIESTERASE-5 (PDE-5) INHIBITORS
    Publication number: 20110028480
    Abstract: Orodisperable formulations of phosphodiesterase-5 (PDE-5) inhibitors and methods of manufacturing such are provided. Further, an improved dosage form and method of treating sexual dysfunction are provided.
    Type: Application
    Filed: April 1, 2008
    Publication date: February 3, 2011
    Applicant: Ocean 1 806, LLC
    Inventors: Adriana Rendon, Esther Rendon
  • SUBSTITUTED PYRROLOTRIAZINES AND THEIR USE
    Publication number: 20110028479
    Abstract: The present application relates to new, substituted pyrrolo[2,1-f][1,2,4]triazine derivatives of the formula (I) as prostacyclin (PGI2) IP receptor activators for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: October 16, 2008
    Publication date: February 3, 2011
    Inventors: Thomas Lampe, Raimund Kast, Friederike Stoll, Joachim Schuhmacher
  • Pyrrolotriazine kinase inhibitors
    Patent number: 7879855
    Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.
    Type: Grant
    Filed: March 26, 2009
    Date of Patent: February 1, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mark D. Wittman, Harold Mastalerz, Kurt Zimmermann, Mark G. Saulnier, Upender Velaparthi, Dolatrai M. Vyas, Guifen Zhang, Walter Lewis Johnson, David B. Frennesson, Xiaopeng Sang, Peiying Liu, David R. Langley