Tricyclo Ring System Having The Seven-mmbered Hetero Ring As One Of The Cyclos Patents (Class 514/211.11)
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Patent number: 10864176Abstract: The present invention relates to pharmaceutical compositions and methods of manufacturing the same, comprising a eutectic of Cyclobenzaprine HCl and mannitol or Amitriptyline HCl and mannitol.Type: GrantFiled: September 24, 2018Date of Patent: December 15, 2020Assignee: Tonix Pharma Holdings LimitedInventors: Marino Nebuloni, Patrizia Colombo
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Patent number: 10864175Abstract: The present invention relates to pharmaceutical compositions and methods of manufacturing the same, comprising a eutectic of Cyclobenzaprine HCl and mannitol or Amitriptyline HCl and mannitol.Type: GrantFiled: September 24, 2018Date of Patent: December 15, 2020Assignee: Tonix Pharma Holdings LimitedInventors: Marino Nebuloni, Patrizia Colombo
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Patent number: 10364255Abstract: The present invention encompasses compounds of the formula (I) wherein the groups A and B are defined herein, which are suitable for the treatment of diseases related to Vanin, and processes for making these compounds, pharmaceutical preparations containing these compounds, and their methods of use.Type: GrantFiled: June 8, 2018Date of Patent: July 30, 2019Assignee: Boehringer Ingleheim International GmbHInventors: Todd Bosanac, Michael J. Burke, Brian Nicholas Cook, Darren Todd Disalvo, Thomas Martin Kirrane, Jr., Yue Shen
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Patent number: 10125113Abstract: The present disclosure provides dibenzazepine derivatives having Formula I or I(A): and the pharmaceutically acceptable salts and solvates thereof, wherein R3a, R3b, R6, V1, V2, Z1, Z2, Z3, and G are defined as set forth in the specification. The present disclosure is also directed to the use of the compounds of Formula I or I(A), and the pharmaceutically acceptable salts or solvates thereof, to treat a disorder responsive to the blockade of one or more sodium channels. In one embodiment, the compounds of the present disclosure are useful for treating pain.Type: GrantFiled: June 14, 2017Date of Patent: November 13, 2018Assignee: Purdue Pharma L.P.Inventors: Stephen M. Lynch, Laykea Tafesse
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Patent number: 10117936Abstract: The present invention relates to pharmaceutical compositions and methods of manufacturing the same, comprising a eutectic of Cyclobenzaprine HCl and mannitol or Amitriptyline HCl and mannitol.Type: GrantFiled: March 14, 2014Date of Patent: November 6, 2018Assignee: TONIX PHARMA HOLDINGS LIMITEDInventors: Marino Nebuloni, Patrizia Colombo
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Patent number: 9475805Abstract: The invention provides a method of activating PPAR ? and a method of treating or preventing a disease associated with PPAR ? by administering a tricyclic compound having a PPAR ? agonist activity, which is represented by the formula (I) wherein Z represents a single bond or the like, Y represents a hydrogen atom, lower alkyl optionally having substituent(s) or the like, X represents a hydrogen atom or the like, A represents aryl or the like, B and C are the same or different and each represents an aromatic carbocycle or the like, R4-R9 are the same or different and each represents hydrogen or the like, V represents a single bond or the like, R10 and R11 are the same or different and each represents hydrogen or the like, or a pharmaceutically acceptable salt thereof or the like:Type: GrantFiled: May 26, 2015Date of Patent: October 25, 2016Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Arata Yanagisawa, Keiji Uehara, Masahiro Matsubara, Kimihisa Ueno, Michihiko Suzuki, Takeshi Kuboyama, Keisuke Yamamoto, Tomohiro Tamura
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Patent number: 9006223Abstract: Therapeutic compositions and methods for treatment of late-onset Gaucher disease are described herein. The compositions comprise compounds having activity as pharmacological chaperones for mutant forms of the beta-glucocerebrosidase. Methods of treatment involve providing therapeutically effective amounts of such compositions to subjects in need thereof.Type: GrantFiled: February 25, 2013Date of Patent: April 14, 2015Assignees: The Hospital for Sick Children, McMaster UniversityInventors: Don J Mahuran, Michael B Tropak, Justin D Buttner, Jan E Blanchard, Eric D Brown
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Publication number: 20150080325Abstract: This disclosure relates to compounds for the inhibition of histone deacetylase and treatment of a cognitive disorder or deficit. More particularly, the disclosure provides for compounds of formula (I) wherein (I), Q, J, L and Z are as defined in the specification.Type: ApplicationFiled: April 1, 2014Publication date: March 19, 2015Applicant: EnVivo Pharmaceuticals, Inc.Inventors: Kathryn Rogers, Holger Patzke
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Patent number: 8951994Abstract: Therapeutic compositions and methods for treatment of late-onset Gaucher disease are described herein. The compositions comprise compounds having activity as pharmacological chaperones for mutant forms of the beta-glucocerebrosidase. Methods of treatment involve providing therapeutically effective amounts of such compositions to subjects in need thereof.Type: GrantFiled: November 14, 2012Date of Patent: February 10, 2015Assignees: The Hospital for Sick Children, McMaster UniversityInventors: Don J Mahuran, Michael B Tropak, Justin D Buttner, Jan E Blanchard, Eric D Brown
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Patent number: 8937059Abstract: Therapeutic compositions and methods for treatment of late-onset Gaucher disease are described herein. The compositions comprise compounds having activity as pharmacological chaperones for mutant forms of the beta-glucocerebrosidase. Methods of treatment involve providing therapeutically effective amounts of such compositions to subjects in need thereof.Type: GrantFiled: April 17, 2014Date of Patent: January 20, 2015Assignees: The Hospital for Sick Children, McMaster UniversityInventors: Don J Mahuran, Michael B Tropak, Justin D Buttner, Jan E Blanchard, Eric D Brown
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Patent number: 8809319Abstract: Nitromethylene analogues of imidacloprid and divalent and oxabridged heterocyclic neonicotinoid compounds constructed by dialdehydes, preparation methods and uses thereof are disclosed. Compounds represented by formula (A) or (B), their optical isomers or agrochemically acceptable salts are provided. Agrochemical compositions comprising the said compounds, their optical isomers or agrochemically acceptable salts, the uses of the said agrochemical compositions and the preparation methods of the said compounds, their optical isomers or agrochemically acceptable salts are also disclosed. The compounds and their derivatives have high insecticidal activities to several farming and forestry pests including homoptera and lepidoptera pests, such as aphis, fulgorid, whitefly, leafhopper, common thrips, cotton bollworm, cabbage caterpillar, cabbage moth, cotton leafworm and armyworm.Type: GrantFiled: December 9, 2010Date of Patent: August 19, 2014Assignee: East China University of Science and TechnologyInventors: Xuhong Qian, Zhong Li, Xusheng Shao, Xiaoyong Xu, Zhiping Xu, Gonghua Song
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Publication number: 20140179678Abstract: The present invention provides targeted treatment to subjects suffering from Frontotemporal lobar degeneration through use of FTLD targeted agents, as described in the present invention. In particular, the FTLD targeted agents provided herein demonstrate high brain penetration, which decreases risk issues associated with peripheral administration. Furthermore, the FTLD targeted agents of the present invention, when administered to a subject selected for treatment based on the results of a FTLD diagnostic assay, offer targeted treatment of FTLD.Type: ApplicationFiled: March 26, 2012Publication date: June 26, 2014Inventors: Holger Patzke, Gerhard Koenig, Jean-Francois Blain
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Patent number: 8461145Abstract: The present invention is related to novel tricyclic compounds of formula (I) having TRPA1 receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use as pharmacological tools, or as irritant incapacitants, or in the treatment of diseases linked to the modulation of the TRPA1 receptors in animals, in particular humans.Type: GrantFiled: December 4, 2008Date of Patent: June 11, 2013Assignee: Janssen Pharmaceutica NVInventors: Henricus Jacobus Maria Gijsen, Marc Hubert Mercken
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Patent number: 8404668Abstract: Therapeutic compositions and methods for treatment of late-onset Gaucher disease are described herein. The compositions comprise compounds having activity as pharmacological chaperones for mutant forms of the beta-glucocerebrosidase. Methods of treatment involve providing therapeutically effective amounts of such compositions to subjects in need thereof.Type: GrantFiled: September 29, 2011Date of Patent: March 26, 2013Assignees: The Hospital for Sick Children, McMaster UniversityInventors: Don J. Mahuran, Michael B. Tropak, Justin D. Buttner, Jan E. Blanchard, Eric D. Brown
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Publication number: 20130053365Abstract: Provided are inhibitors of poly(ADP-ribose)polymerase according to Formula (M): where A, B, Y, Z, D, E, R1, R2, R3, and R4 are as defined herein. Also described are pharmaceutical compositions, methods of preparing, and methods of using a compound of Formula M to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.Type: ApplicationFiled: August 29, 2012Publication date: February 28, 2013Applicant: BioMarin Pharmaceutical, Inc.Inventors: Bing Wang, Daniel Chu
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Patent number: 8367656Abstract: Disclosed herein are novel polymorphs of 7-[(3-chloro-6,11-dihydro-6-methyldibenzo[c,f][1,2]thiazepin-11-yl)amino]heptanoic acid S,S-dioxide. Also described herein are novel pharmaceutical compositions comprising one or more 7-[(3-chloro-6,11-dihydro-6-methyldibenzo[c,f][1,2]thiazepin-11-yl)amino]heptanoic acid S,S-dioxide polymorphs, methods of making, and related methods of treatment.Type: GrantFiled: March 4, 2008Date of Patent: February 5, 2013Assignee: Janssen Biotech, Inc.Inventor: Matthew Sansone
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Patent number: 8288372Abstract: Loxapine, amoxapine, or salts or prodrugs of either, is effective in alleviating pain, particularly headache pain such as migraine, cluster headaches and tension headaches. Preferably the loxapine or amoxapine is administered systemically, most preferably by inhalation.Type: GrantFiled: November 20, 2003Date of Patent: October 16, 2012Assignee: Alexza Pharmaceuticals, Inc.Inventors: Ron L. Hale, Patrik Munzar, Joshua D. Rabinowitz
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Patent number: 8242151Abstract: The present invention provides a PPAR ? agonist comprising, as an active ingredient, a tricyclic compound represented by the formula (I) (wherein R1 represents lower alkyl optionally having substituent(s) or the like, R2 and R3 are the same or different and each represents lower alkyl optionally having substituent(s) or the like, R4 and R5 are the same or different and each represents a hydrogen atom or the like, Q1-Q2-Q3 represents CH?CH—CH?CH or the like, Y represents a single bond or the like, Z1-Z2 represents C?CR13 (wherein R13 represents a hydrogen atom or the like), or the like, and A represents —COOH or the like), or a pharmaceutically acceptable salt thereof and the like.Type: GrantFiled: February 7, 2008Date of Patent: August 14, 2012Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Arata Yanagisawa, Takeshi Kuboyama, Seiji Aratake, Kazuki Hemmi, Kimihisa Ueno, Michihiko Suzuki, Masahiro Matsubara, Kozo Yao, Akinori Hamaguchi, Yukihito Tsukumo
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Patent number: 8183234Abstract: Guanidine derivatives having a condensed tricyclic ring of formula 1: are disclosed, wherein U is C(O), CRaRb, O, NRa or S(O)m; V is CRaRb or NRa; W is S(O)m; wherein Ra is H, alkyl, cycloalkyl, alkenyl or aralkyl; Rb is H, alkyl, OH, ORa or OCORa, and m is the integer 0, 1 or 2; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein with the proviso that at least one of R1, R2, R3, R4, R5, R6, R7 or R8 is guanidino or guanidinocarbonyl. These derivatives are sodium-proton exchange inhibitors and are useful as medicaments for the treatment of, for example, organ disorders associated with ischemia and reperfusion, cardiac arrhythmia, cardiac hypertrophy, hypertension, cell proliferative disorders and diabetes.Type: GrantFiled: June 30, 2010Date of Patent: May 22, 2012Assignee: Piramal Life Sciences LimitedInventors: Bansi Lal, Swati Bal-Tembe, Usha Ghosh, Arun Kumar Jain, Tulsidas More, Anil Ghate, Jacqueline Trivedi, Sapna Parikh
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Publication number: 20120101082Abstract: The present invention concerns compounds inter alia according to general formula 1a. Compounds according to the invention are vasopressin V1a receptor antagonists. Pharmaceutical compositions of the compounds are useful as treatment of dysmenorrhoea.Type: ApplicationFiled: December 19, 2011Publication date: April 26, 2012Inventors: ANDRZEJ ROMAN BATT, MARTIN LEE STOCKLEY, MICHAEL BRYAN ROE, CELINE Marguerite Simone HEENEY, ANDREW JOHN BAXTER, PETER HUDSON, RACHEL HANDY
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Patent number: 8124597Abstract: Therapeutic compositions and methods for treatment of late-onset Gaucher disease are described herein. The compositions comprise compounds having activity as pharmacological chaperones for mutant forms of the beta-glucocerebrosidase. Methods of treatment involve providing therapeutically effective amounts of such compositions to subjects in need thereof.Type: GrantFiled: August 22, 2008Date of Patent: February 28, 2012Assignees: The Hospital for Sick Children, McMaster UniversityInventors: Don J. Mahuran, Michael B. Tropak, Justin D. Buttner, Jan E. Blanchard, Eric D. Brown
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Patent number: 8088789Abstract: A method of treating an ophthalmic condition or disease by administering a compound disclosed herein is provided. The compound can be administered systemically or locally and in a variety of ways, such as via a temporary device, an implant, an injection or an eye drop. The compound can also be administered with an additional therapeutic agent.Type: GrantFiled: March 11, 2008Date of Patent: January 3, 2012Assignee: Elixir Medical CorporationInventors: John Yan, Xiaoxia Zheng, Vinayak D. Bhat
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Publication number: 20110288070Abstract: This disclosure relates to compounds for the inhibition of histone deacetylase and treatment of a cognitive disorder or deficit. More particularly, the disclosure provides for compounds of formula (I) wherein (I), Q, J, L and Z are as defined in the specification.Type: ApplicationFiled: May 5, 2009Publication date: November 24, 2011Inventors: Kathryn Rogers, Holger Patzke
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Patent number: 8063038Abstract: The invention concerns compounds according to general formulae 1, wherein G1 is an amine. Compounds according to the invention are vasopressin V2 receptor agonists. Pharmaceutical compositions of the compounds are useful as antidiuretic agents.Type: GrantFiled: August 18, 2005Date of Patent: November 22, 2011Assignee: Vantia LimitedInventor: Gary Robert William Pitt
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Publication number: 20110195950Abstract: The invention relates to compound of the formula I in which R1 represents an optionally substituted aryl group or an optionally substituted heteroaryl group; R2 represents hydrogen or a substituent different from hydrogen; R3 represents an optionally substituted aryl group, cycloalkyl group, heteroaryl group, heterocyclyl group; X1 represents O, S, NR4, CR42; X2 represents O, S, NR4, CR42; X3 represents O, S, NR4, CR42; X4 represents O, S, NR4, CR42; R4 represents hydrogen or a substituent different from hydrogen; R5 represents hydrogen or alkyl; Y represents O or S; m represents 0, 1, 2 or 3; n represents 0, 1, 2 or 3 in free base form or in acid addition salt form; to its preparation, to its use as medicament and to medicaments comprising it.Type: ApplicationFiled: August 12, 2008Publication date: August 11, 2011Inventors: Samuel Hintermann, Konstanze Hurth, Marina Tintelnot-Blomley
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Publication number: 20110136782Abstract: The present invention provides a nitrogen-containing heterocyclic compound represented by formula (I) and salt thereof (wherein, R1 to R6 each independently represents a hydrogen atom, unsubstituted or substituted C1-20 alkyl group and the like, R1 and R2, R3 and R4, or R5 and R6 may together form an unsubstituted or substituted 5- to 8-membered ring, A-B, in which A represents a carbon atom and B represents a nitrogen atom, represents the formula: C?N and the like, Y represents an oxygen atom and the like, X and X? each independently represent an unsubstituted or substituted C1-20 alkyl group and the like, m represents an integer of 0 to 2, and n represents an integer of 0 to 4), and a fungicide for agricultural and horticultural use that contains at least one of these compounds as an active ingredient thereof, demonstrates reliable effects and can be used safely.Type: ApplicationFiled: August 10, 2009Publication date: June 9, 2011Applicant: Nippon Soda Co., LtdInventors: Akira Mitani, Jun Inagaki, Raito Kuwahara, Masahiro Yokoyama, Kotaro Shibayama, Motoaki Sato
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Publication number: 20110136784Abstract: A method of treating at least one symptom or condition associated with but not limited to: Anxiety Disorders including but not limited to Panic Disorder Without Agoraphobia, Panic Disorder With Agoraphobia, Agoraphobia Without History of Panic Disorder, Specific Phobia, Social Phobia, Obsessive-Compulsive Disorder, Postaumatic Stress Disorder, Acute Stress Disorder, Generalized Anxiety Disorder and Generalized Anxiety Disorder Due to a General Medical Condition comprising administering an effective amount of Formula I or its pharmaceutically acceptable salt. In another aspect of the invention a pharmaceutical composition is provided comprising an effective amount of Formula I or its pharmaceutically acceptable salt and at least one pharmaceutically acceptable carrier or diluent.Type: ApplicationFiled: November 8, 2010Publication date: June 9, 2011Applicant: AstraZeneca ABInventors: Patricia C. Davis, Jeffrey M. Goldstein, Scott W. Grimm, Helen R. Winter, Raymond F. Suckow
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Publication number: 20110112069Abstract: The specification describes the use of selected purine derivatives for the treatment of hyperproliferative diseases.Type: ApplicationFiled: August 15, 2008Publication date: May 12, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank Himmelsbach, Michael Mark, Mohammad Tadayyon, Leo Thomas
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Publication number: 20110092483Abstract: A kit and a method for identifying compounds having anti-prion activity are provided. The kit comprises a yeast of phenotype [PSI+]; an antibiogram; and a prion curing agent in a sub-effective dose, wherein the yeast has the adel-14 allele of the ADE1 gene and an inactivated ERG6 gene. Compounds and pharmaceutical compositions having anti-prion activity are also provided, which are useful for treating various neurodegenerative diseases, including polyglutamines expansion associated diseases; Huntington's disease; Kennedy disease; amyotrophic lateral sclerosis; cerebellous autosomic ataxies; dentalorubral-pallidoluysian atrophy; and spino-bulbar amyotrophy.Type: ApplicationFiled: August 17, 2010Publication date: April 21, 2011Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), UNIVERSITE VICTOR SEGALEN BORDEAUX 2, UNIVERSITE DE POITIERSInventors: MARC BLONDEL, CHRISTOPHE CULLIN, JEAN MICHEL VIERFOND, ANNE BERTOLOTTI, STÉPHANE BACH, NICOLAS TALAREK, YVETTE METTEY
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Patent number: 7867988Abstract: A method of inhibiting smooth muscle cell proliferation or cytokine production in a subject, comprising administering a compound disclosed herein to the subject, is provided. The compound can be administered systemically, locally, or a combination thereof. For example, the compound can be locally delivered from a temporary device or an implant, such as a vascular prosthesis.Type: GrantFiled: September 12, 2007Date of Patent: January 11, 2011Assignee: Elixir Medical CorporationInventors: John Yan, Xiaoxia Zheng, Vinayak D. Bhat
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Publication number: 20100305094Abstract: Compounds of formula 1: are disclosed, wherein V is CH2; W is S(O)m; m is the integer 0, 1 or 2; U is O, C(O), CR13R14 or NR15; where R13 is H, alkyl; R14 is H, OH, OR13 or OCOR13; R15 is H, alkyl, cycloalkyl, alkenyl, C(O)R13, C(O)OR13 or alkylaminocarbonyl; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. These compounds are inhibitors of tumor necrosis factor-alpha (TNF-?) and are useful as medicaments for the treatment and prevention of disorders caused by increased TNF-? activity, in particular inflammations.Type: ApplicationFiled: August 11, 2010Publication date: December 2, 2010Applicant: Piramal Life Sciences LimitedInventors: Bansi Lal, Somesh Sharma, Usha Ghosh, Swati Bal-Tembe, Tulsidas More, Asha Kulkarni-Almeida, Sapna Parikh, Radha Panicker, Anagha Damre, Ravindra Gupte
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Patent number: 7834001Abstract: Guanidine derivatives having a condensed tricyclic ring of formula 1: are disclosed, wherein U is C(O), CRaRb, O, NRa or S(O)m; V is CRaRb or NRa; W is S(O)m; wherein Ra is H, alkyl, cycloalkyl, alkenyl or aralkyl; Rb is H, alkyl, OH, ORa or OCORa, and m is the integer 0, 1 or 2; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein with the proviso that at least one of R1, R2, R3, R4, R5, R6, R7 or R8 is guanidino or guanidino carbonyl. These derivatives are sodium-proton exchange inhibitors and are useful as medicaments for the treatment of, for example, organ disorders associated with ischemia and reperfusion, cardiac arrhythmia, cardiac hypertrophy, hypertension, cell proliferative disorders and diabetes.Type: GrantFiled: November 8, 2005Date of Patent: November 16, 2010Assignee: Piramal Life Sciences LimitedInventors: Bansi Lal, Swati Bal-Tembe, Usha Ghosh, Arun Kumar Jain, Tulsidas More
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Publication number: 20100273773Abstract: The present invention is related to novel tricyclic compounds of formula (I) having TRPA1 receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use as pharmacological tools, or as irritant incapacitants, or in the treatment of diseases linked to the modulation of the TRPA1 receptors in animals, in particular humans.Type: ApplicationFiled: December 4, 2008Publication date: October 28, 2010Inventors: Henricus Jacobus Maria Gijsen, Marc Hubert Mercken
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Publication number: 20100266711Abstract: The present invention relates to new thienobenzodiazepine modulators of D1 receptors, D2 receptors, and/or 5-HT2 receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: September 24, 2009Publication date: October 21, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100267690Abstract: Guanidine derivatives having a condensed tricyclic ring of formula 1: are disclosed, wherein U is C(O), CRaRb, O, NRa or S(O)m; V is CRaRb or NRa; W is S(O)m; wherein Ra is H, alkyl, cycloalkyl, alkenyl or aralkyl; Rb is H, alkyl, OH, ORa or OCORa, and m is the integer 0, 1 or 2; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein with the proviso that at least one of R1, R2, R3, R4, R5, R6, R7 or R8 is guanidino or guanidino carbonyl. These derivatives are sodium-proton exchange inhibitors and are useful as medicaments for the treatment of, for example, organ disorders associated with ischemia and reperfusion, cardiac arrhythmia, cardiac hypertrophy, hypertension, cell proliferative disorders and diabetes.Type: ApplicationFiled: June 30, 2010Publication date: October 21, 2010Applicant: Piramal Life Sciences LimitedInventors: Bansi LAL, Swati Bal-Tembe, Usha Ghosh, Arun Kumar Jain, Tulsidas More, Anil Ghate, Jacqueline Trivedi, Sapna Parikh
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Patent number: 7807663Abstract: A pharmaceutical composition for preventing and/or treating diabetes, diabetic complication, hyperinsulinemia, disorders of glucose metabolism or obesity, comprising a combination of the following compound, analogues or pharmaceutically acceptable salts thereof with a hypoglycemic agent.Type: GrantFiled: August 8, 2005Date of Patent: October 5, 2010Assignee: Ajinomoto Co., Inc.Inventors: Takao Ikenoue, Yoko Kageyama, Yukio Iino, Nobuo Kondo
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Publication number: 20100227850Abstract: The current invention is based, inter alia, on the finding that the transcription factor MarA, and homologues of MarA, e.g., Rob and SoxS, are virulence factors. Accordingly, the invention discloses methods for screening compounds for their ability to modulate these virulence factors. The invention further describes methods for treating and preventing bacterial infections by modulating the expression and/or activity of transcription factors. In addition, the invention provides a method for identifying other virulence factors.Type: ApplicationFiled: November 24, 2009Publication date: September 9, 2010Applicant: PARATEK PHARMACEUTICALS, INC.Inventors: MICHAEL N. ALEKSHUN, STUART B. LEVY
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Publication number: 20100216769Abstract: The present invention relates to new substituted glycinamides of general formula (I) wherein D, M, R3, R4 and R5 are defined as in the specification, the tautomers, enantiomers, diastereomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.Type: ApplicationFiled: June 28, 2006Publication date: August 26, 2010Inventors: Henning Priepke, Georg Dahmann, Kai Gerlach, Roland Pfau, Wolfgang Wienen, Annette Schuler-Metz, Sandra Handschuh, Herbert Nar
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Publication number: 20100144703Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: February 17, 2010Publication date: June 10, 2010Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank HIMMELSBACH, Elke LANGKOPF, Matthias ECKHARDT, Roland MAIER, Michael MARK, Mohammad TADAYYON, Ralf R. H. LOTZ
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Publication number: 20090298809Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: May 28, 2009Publication date: December 3, 2009Applicant: Albany Molecular Research, Inc.Inventors: David D. Manning, Christopher Lawrence Cioffi
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Patent number: 7625888Abstract: The present invention is directed to novel fused triazole derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and 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: GrantFiled: August 19, 2005Date of Patent: December 1, 2009Assignee: Merck & Co., Inc.Inventors: Ann E. Weber, Wallace T. Ashton
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Publication number: 20090258856Abstract: The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: June 23, 2009Publication date: October 15, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias ECKHARDT, Norbert HAUEL, Elke LANGKOPF, Frank HIMMELSBACH, Iris KAUFFMANN-HEFNER, Mohammad TADAYYON, Michael MARK
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Publication number: 20090221552Abstract: The invention features methods, compositions, and kits for the treatment of attention deficit hyperactivity disorder and related behavioral disorders by administering an organic cation 3 (hOCT3) inhibitor.Type: ApplicationFiled: February 27, 2007Publication date: September 3, 2009Applicant: The McLean Hospital CorporationInventors: Martin Teicher, Susan L. Andersen, Jacqueline A. Samson
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Patent number: 7566707Abstract: The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: June 10, 2004Date of Patent: July 28, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Eckhardt, Norbert Hauel, Elke Langkopf, Frank Himmelsbach, Iris Kauffmann-Hefner, Mohammad Tadayyon, Michael Mark
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Publication number: 20090131401Abstract: Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.Type: ApplicationFiled: February 12, 2008Publication date: May 21, 2009Applicant: Paratek Pharmaceuticals, Inc.Inventors: Stuart B. Levy, Michael N. Alekshun, Brent L. Podlogar, Kwasi Ohemeng, Atul K. Verma, Tadeusz Warchol, Beena Bhatia, Todd Bowser, Mark Grier
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Publication number: 20090075960Abstract: Therapeutic compositions and methods for treatment of late-onset Gaucher disease are described herein. The compositions comprise compounds having activity as pharmacological chaperones for mutant forms of the beta-glucocerebrosidase. Methods of treatment involve providing therapeutically effective amounts of such compositions to subjects in need thereof.Type: ApplicationFiled: August 22, 2008Publication date: March 19, 2009Applicants: THE HOSPITAL FOR SICK CHILDREN, McMASTER UNIVERSITYInventors: Don J. Mahuran, Michael B. Tropak, Justin D. Buttner, Jan E. Blanchard, Eric D. Brown
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Patent number: 7482337Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: October 28, 2003Date of Patent: January 27, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Roland Maier, Michael Mark, Mohammad Tadayyon, Ralf R. H. Lotz
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Publication number: 20080299118Abstract: Provided are certain methods of treating maligancies with farnesoid X receptor agonists.Type: ApplicationFiled: May 30, 2008Publication date: December 4, 2008Applicant: WyethInventors: Helen B. Hartman, Mark J. Evans
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Publication number: 20080275023Abstract: New N-hydroxyamides of n-alkyl carboxylic acids omega substituted with suitable tricyclic systems characterised by a central 7-membered ring, having activity as inhibitors of histone deacetylase (HDAC).Type: ApplicationFiled: March 13, 2006Publication date: November 6, 2008Inventors: Antonio Guidi, Tula Dimoulas, Danilo Giannotti, Nicholas Harmat
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Publication number: 20080261951Abstract: This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V1 and V2 are both H, OMe or F, or one of V1 and V2 is Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N3, NH2, NHBn or NH-acyl and the other is H, or V1 and V2 together are ?O, —O(CH2)pO— or —S(CH2)S—; W1 is either O or S; X1 and X2 are both H, or together are ?O or ?S; Y is OR5 or NR6R7; R1, R2, R3 and R4 are independently selected from H, lower alkyl, lower alkyloxy, F, Cl and Br; R5 is selected from H and lower alkyl; R6 and R7 are independently selected from H and lower alkyl, or together are —(CH2)n—; n=3, 4, 5, 6; and p is 2 or 3. The compounds are agonists at the vasopressin V2 receptor and are useful as antidiuretics and procoagulants. The invention further comprises pharmaceutical compositions incorporating these vasopressin agonists, which compositions are particularly useful in the treatment of central diabetes insipidus, nocturnal enuresis and nocturia.Type: ApplicationFiled: June 23, 2008Publication date: October 23, 2008Inventors: Doreen Mary Ashworth, Gary Robert William Pitt, Peter Hudson, Christopher Martyn Yea, Richard Jeremy Franklin