Thiocarboxamides, (i.e., C(=s)-n) Patents (Class 514/599)
-
Publication number: 20110177085Abstract: The present invention relates to bitter-taste receptors and their role in bitter taste transduction. The invention also relates to assays for screening molecules that modulate, e.g. suppress or block, bitter taste transduction, or enhance bitter taste response.Type: ApplicationFiled: March 25, 2011Publication date: July 21, 2011Inventors: Bernd Bufe, Thomas Hofmann, Dietmar Krautwurst, Christina Kuhn, Wolfgang Meyerhof
-
Patent number: 7939564Abstract: Disclosed herein are methods of treating a proliferative disease, such as cancer, with bis(thio-hydrazide amides) or a tautomer, pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, in combination with hyperthermia treatment. Also disclosed are methods of treating a proliferative disease, such as cancer, with bis(thio-hydrazide amides) or a tautomer, pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, in combination with radiotherapy.Type: GrantFiled: August 30, 2007Date of Patent: May 10, 2011Assignee: Synta Pharmaceuticals Corp.Inventor: Keizo Koya
-
Publication number: 20110105618Abstract: The present invention provides new tyrphostin derivatives acting as protein kinase (PK) and receptor kinase (RK) signaling modulators. The invention further provides methods of their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as chemotherapeutic agents for preventions and treatments of PK and RK related disorders such as metabolic, inflammatory, fibrotic, and cell proliferative disorders, in particular cancer.Type: ApplicationFiled: June 7, 2009Publication date: May 5, 2011Applicant: NOVOTYR THERAPEUTICS LTD.Inventors: Hadas Reuveni, Alexander Levitzki, Revital Sasson, Andre C. B. Lucassen
-
Publication number: 20110086761Abstract: The present invention relates to fungicidal compositions and their use for controlling oomycete pathogen induced disease or diseases in one or more plants.Type: ApplicationFiled: October 13, 2010Publication date: April 14, 2011Applicant: DOW AGROSCIENCES LLCInventors: Norman R. Pearson, Lei Liu, Robert J. Ehr, John M. Atkinson
-
Patent number: 7893092Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula (I) can be used as agrochemical active ingredients and can be prepared in a manner known per se.Type: GrantFiled: December 7, 2005Date of Patent: February 22, 2011Assignee: Syngenta Crop Protection, Inc.Inventors: Andre Jeanguenat, Anthony Cornelius O'Sullivan
-
Publication number: 20110003011Abstract: There are described new active compound combinations of a compound of the formula (I) with known fungicidal active compounds, and their use for the control of phytopathogenic fungi.Type: ApplicationFiled: July 8, 2010Publication date: January 6, 2011Applicant: Bayer CropScience AGInventors: Wilhelm BRANDES, Heinz-Wilhelm Dehne, Stefan Dutzmann, Karl-Heinz Kuck, Bernd-Wieland Krüger
-
Publication number: 20100324143Abstract: Disclosed are bis(thio-hydrazide amide) disalts, which are represented by Structural Formula (I): Y is a covalent bond or a substituted or unsubstituted straight chained hydrocarbyl group. R1-R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. Z is —O or —S. M+ is a pharmaceutically acceptable monovalent cation and M2+ is a pharmaceutically acceptable divalent cation. Also, disclosed are pharmaceutical compositions comprising a bis(thio-hydrazide amide) disalt described above. Further disclosed are methods of treating a subject with cancer. The methods comprise the step of administering an effective amount of a bis(thio-hydrazide amide) disalt described above.Type: ApplicationFiled: August 30, 2010Publication date: December 23, 2010Inventors: Keizo Koya, Lijun Sun, Elena Kostik, Farid Vaghefi, Shoujun Chen, Noriaki Tatsuta, Guiqing Liang, Takayo Inoue, Zhi-Qiang Xia
-
Publication number: 20100311840Abstract: Disclosed herein are oral formulations of bis(thio-hydrazide amides) compounds of the following structural formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R7, R8, Z, and Y are defined herein.Type: ApplicationFiled: November 7, 2008Publication date: December 9, 2010Inventors: Noriaki Tatsuta, Takayo Inoue, Keizo Koya
-
Publication number: 20100267738Abstract: The present invention relates to inhibitors of 11-?-hydroxysteroid dehydrogenase type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.Type: ApplicationFiled: April 20, 2010Publication date: October 21, 2010Applicant: ABBOTT LABORATORIESInventors: Sridhar Peddi, Meena V. Patel, Jeffrey J. Rohde
-
Publication number: 20100249239Abstract: Disclosed herein are compositions comprising a compound represented by structural formula (I): 2 g of which is reconstitutable in 10 mL of a water in less than 10 minutes, and methods for preparing these compositions. Also disclosed are compositions comprising a compound represented by structural formula (I) and a pharmaceutically acceptable excipient, wherein the molar ratio of said compound to said excipient is from 1:20 to 1:1, and methods for preparing these compositions.Type: ApplicationFiled: February 1, 2010Publication date: September 30, 2010Inventors: Walter J. Lunsmann, Ninad Deshpanday
-
Patent number: 7799334Abstract: The present invention relates to pyrazolecarboxamides of the formula I in which the variables are as defined below: X is trifluoromethyl; R1 is F, Cl, Br, C1-C4-alkyl or C1-C4-haloalkyl; R2 is hydrogen, halogen or C1-C4-alkyl; R3 is hydrogen, C1-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C2-C4-alkynyl or C3-C6-cycloalkyl; W is O or S; with the proviso that, if R3 is hydrogen and W is oxygen, a) R1 and R2 are not simultaneously methyl and F, respectively; b) R1 and R2 are not simultaneously trifluoromethyl and hydrogen or fluorine, respectively. to processes for preparing these compounds, to seeds and compositions comprising them and to methods for controlling harmful fungi.Type: GrantFiled: May 10, 2006Date of Patent: September 21, 2010Assignee: BASF AktiengesellschaftInventors: Markus Gewehr, Jochen Dietz, Thomas Grote, Wassilios Grammenos, Udo Hünger, Bernd Müller, Frank Schieweck, Anja Schwögler, Jan Klaas Lohmann, Joachim Rheinheimer, Jens Renner, Peter Schäfer
-
Patent number: 7795313Abstract: Disclosed are bis(thio-hydrazide amide) disalts, which are represented by Structural Formula (I): Y is a covalent bond or a substituted or unsubstituted straight chained hydrocarbyl group. R1-R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. Z is —O or —S. M+ is a pharmaceutically acceptable monovalent cation and M2+ is a pharmaceutically acceptable divalent cation. Also, disclosed are pharmaceutical compositions comprising a bis(thio-hydrazide amide) disalt described above. Further disclosed are methods of treating a subject with cancer. The methods comprise the step of administering an effective amount of a bis(thio-hydrazide amide) disalt described above.Type: GrantFiled: July 15, 2009Date of Patent: September 14, 2010Assignee: Synta Pharmaceuticals Corp.Inventors: Keizo Koya, Lijun Sun, Elena Kostik, Farid Vaghefi, Shoujun Chen, Noriaki Tatsuta, Guiqing Liang, Takayo Inoue, Zhi-Qiang Xia
-
Patent number: 7763658Abstract: One embodiment of the present invention is a method of treating a subject with a multi-drug resistant cancer. The method comprises administering to the subject an effective amount of a compound represented by Structural Formula (I): Y is a covalent bond or a substituted or unsubstituted straight chained hydrocarbyl group, or, Y, taken together with both >C?Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. R1-R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. Preferably R1 and R2 are the same and R3 and R4 are the same. R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group.Type: GrantFiled: January 15, 2004Date of Patent: July 27, 2010Assignee: Synta Pharmaceuticals Corp.Inventors: Keizo Koya, Lijun Sun, Yaming Wu, Timothy Korbut, Dan Zhou, Zhenjian Du, Shoujun Chen, Noriaki Tatsuta, Guiqing Liang, Mitsunori Ono
-
Publication number: 20100166881Abstract: Novel indoleamine 2,3-dioxygenase (IDO) inhibitors, compositions comprising the same, and methods of use thereof are disclosed.Type: ApplicationFiled: March 11, 2010Publication date: July 1, 2010Inventors: George C. Prendergast, William P. Malachowski, Alexander J. Muller, James B. DuHadaway
-
Publication number: 20100160430Abstract: There is provided an organic sulfur compound having an excellent controlling effect on harmful arthropods represented by the formula (I): wherein, R1 represents a C1-C5 haloalkyl group having at least one fluorine atom, R2 represents a C1-C4 alkyl group optionally substituted with at least one halogen atom or the like, R3 represents a hydrogen atom or the like, R4 represents a cyano group or the like, R5 represents a hydrogen atom or the like, m represents an integer of 1 to 4, and n represents 0, 1 or 2.Type: ApplicationFiled: May 16, 2008Publication date: June 24, 2010Inventor: Hiroyuki Miyazaki
-
Publication number: 20100152289Abstract: There is provided an organic sulfur compound having an excellent controlling effect on harmful arthropods which is represented by formula (I): wherein R1 represents a C3-C6 haloalkyl group having at least one fluorine atom and at least one atom selected from group consisting of a chlorine atom, a bromine atom and an iodine atom, R2 represents a cyano group and the like, R3 represents a hydrogen atom, a halogen atom or a C1-C4 alkyl group, R4 represents a C1-C5 fluoroalkyl group, and n represents 0, 1 or 2.Type: ApplicationFiled: May 18, 2008Publication date: June 17, 2010Inventor: Hiroyuki Miyazaki
-
Publication number: 20100130565Abstract: The present invention relates to novel thioamide derivatives of formula (I) and formula (Ia): wherein, R3, R4, R5, R6, R7, P, Q, T, V, W, X, Y, Z, a, m and n are as defined in the description, compositions thereof, processes for their preparation and their uses as pesticides.Type: ApplicationFiled: October 20, 2009Publication date: May 27, 2010Inventors: Loic Patrick Le Hir de Fallois, Hyoung Ik Lee, Philip Reid Timmons
-
Patent number: 7714168Abstract: Since an amide compound represented by the formula (1) is effective for controlling plant diseases, it is useful as an effective ingredient of a composition for controlling plant diseases.Type: GrantFiled: October 20, 2006Date of Patent: May 11, 2010Assignee: Sumitomo Chemical Company, LimitedInventor: Takashi Komori
-
Publication number: 20100093828Abstract: Disclosed are compounds of formula (IA), formula (IV) or formula (V), and pharmaceutical compositions containing them which are useful for treating a subject with a proliferative disorder, such as cancer. The disclosed compounds and pharmaceutical compositions are also useful for treating disorders responsive to Hsp70 induction and/or natural killer induction.Type: ApplicationFiled: August 20, 2007Publication date: April 15, 2010Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Jun Jiang
-
Publication number: 20100081635Abstract: Disclosed are compounds of formulae (I), (III), (IV), (VII), (X), (XI), (XII), (XIII) and (XIV), wherein the variabables are as defined in the claims, and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.Type: ApplicationFiled: August 20, 2007Publication date: April 1, 2010Inventors: Shoujun Chen, Keizo Koya, Zachary Demko, Lijun Sun
-
Patent number: 7678832Abstract: Disclosed herein are compositions comprising a compound represented by structural formula (I): 2 g of which is reconstitutable in 10 mL of a water in less than 10 minutes, and methods for preparing these compositions. Also disclosed are compositions comprising a compound represented by structural formula (I) and a pharmaceutically acceptable excipient, wherein the molar ratio of said compound to said excipient is from 1:20 to 1:1, and methods for preparing these compositions.Type: GrantFiled: August 10, 2006Date of Patent: March 16, 2010Assignee: Synta Pharmaceuticals Corp.Inventors: Walter J. Lunsmann, Ninad Deshpanday
-
Publication number: 20100056635Abstract: The present invention provides new tyrphostin derivatives acting as substrate competitive protein tyrosine kinase (PTK) inhibitors and receptor tyrosine kinase (RTK) inhibitors, methods of their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as chemotherapeutic agents for preventions and treatments of PTK and RTK related disorders such as metabolic, fibrotic, and cell proliferative disorders, in particular psoriasis and cancer.Type: ApplicationFiled: December 4, 2007Publication date: March 4, 2010Inventors: Hadas Reuveni, Alexander Levitzki, Lilach Steiner, Revital Sasson, Iris Ben-David, Avi Weissberg
-
Patent number: 7671092Abstract: Disclosed is a compound represented by the Structural Formula (I): Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C=Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 and R2 are independently an aryl group or a substituted aryl group, R3 and R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is ?O or ?S.Type: GrantFiled: January 18, 2008Date of Patent: March 2, 2010Assignee: Synta Pharmaceuticals Corp.Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Noriaki Tatsuta, Yaming Wu, Mitsunori Ono
-
Patent number: 7632865Abstract: To provide cytokine production inhibitors useful as preventive or therapeutic medicines for diseases accompanied by hyperactivated immune functions. A cytokine production inhibitor containing, as an active ingredient, a thioamide compound represented by the formula (I) or a salt thereof: wherein A is N, NO, C—NO2 or C—CN; Hal is a halogen; M1 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, heterocyclyl, amino, O, S, SO or SO2; M2 is amino, O, S or a single bond; R1 is a halogen, alkyl or the like; each of R2, R3, R4 and R5 is independently H, alkyl or the like; R6 is a halogen, alkyl or the like; Cy is cycloalkyl, cycloalkenyl, aryl or heterocyclyl; each of k, p and q is independently an integer of from 0 to 3; and r is an integer of from 0 to 5.Type: GrantFiled: February 16, 2005Date of Patent: December 15, 2009Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Fuminori Kato, Hirohiko Kimura, Kiyoshi Tamai, Kazuhiro Yamamoto, Mitsuo Sano, Shinya Mori, Takashi Okada, Toshihiko Ueki, Kumiko Azuma
-
Publication number: 20090291989Abstract: Provided herein are compositions of matter and pharmaceutical compositions thereof, for use in inhibiting the growth of various microbial pathogens, including bacteria, fungi, protozoa, and viral pathogens. Also provided herein are methods of treating microbial diseases/infections and cancer with the compositions. The compositions are additionally useful in wood preservation and food preservation by inhibition of microbial growth.Type: ApplicationFiled: July 6, 2007Publication date: November 26, 2009Applicant: University of Medicine and Dentistry of New JerseyInventors: Arkady Mustaev, Natalia Kurepina
-
Patent number: 7622612Abstract: The present invention relates to tricyclic colchicine derivatives represented by the formulas (I) or (II), pharmaceutically acceptable salts thereof, and a method for providing an immuno-suppressive or immuno-modulating effect, an anti-proliferative effect, an anti-inflammatory effect or a method for treating cancer comprising administering to a patient an effective amount of one or more colchicine derivatives:Type: GrantFiled: July 10, 2006Date of Patent: November 24, 2009Assignees: Chemtech Research Incorporation, KT & G CorporationInventors: Dong Jo Chang, Eun Young Yoon, Gun Bong Lee, Soon Ok Kim, Wan Joo Kim
-
Publication number: 20090281172Abstract: Disclosed are bis(thio-hydrazide amide) disalts, which are represented by Structural Formula (I): Y is a covalent bond or a substituted or unsubstituted straight chained hydrocarbyl group. R1-R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. Z is —O or —S. M+ is a pharmaceutically acceptable monovalent cation and M2+ is a pharmaceutically acceptable divalent cation. Also, disclosed are pharmaceutical compositions comprising a bis(thio-hydrazide amide) disalt described above. Further disclosed are methods of treating a subject with cancer. The methods comprise the step of administering an effective amount of a bis(thio-hydrazide amide) disalt described above.Type: ApplicationFiled: July 15, 2009Publication date: November 12, 2009Inventors: Keizo Koya, Lijun Sun, Elena Kostik, Farid Vaghefi, Shoujun Chen, Noriaki Tatsuta, Guiqing Liang, Takayo Inoue, Zhi-Qiang Xia
-
Patent number: 7598416Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR modulators to treat or inhibit the progression of, for example, dyslipidemia.Type: GrantFiled: June 23, 2008Date of Patent: October 6, 2009Assignee: Janssen Pharmaceutica N. V.Inventors: Gee-Hong Kuo, Rui Zhang, Aihua Wang, Alan DeAngelis, Keith Demarest, Patricia Pelton
-
Patent number: 7579503Abstract: Disclosed are bis(thio-hydrazide amide) disalts, which are represented by Structural Formula (I): Y is a covalent bond or a substituted or unsubstituted straight chained hydrocarbyl group. R1-R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. Z is —O or —S. M+ is a pharmaceutically acceptable monovalent cation and M2+ is a pharmaceutically acceptable divalent cation. Also, disclosed are pharmaceutical compositions comprising a bis(thio-hydrazide amide) disalt described above. Further disclosed are methods of treating a subject with cancer. The methods comprise the step of administering an effective amount of a bis(thio-hydrazide amide) disalt described above.Type: GrantFiled: April 18, 2008Date of Patent: August 25, 2009Assignee: Synta Pharmaceuticals Corp.Inventors: Keizo Koya, Lijun Sun, Elena Kostik, Farid Vaghefi, Shoujun Chen, Noriaki Tatsuta, Guiqing Liang, Takayo Inoue, Zhi-Qiang Xia
-
Publication number: 20090093538Abstract: The invention relates to a method of treating cancer in a subject, comprising administering to the subject an anti-cancer therapy and a compound that increases the oxidative stress of the cancer cells and activates p38.Type: ApplicationFiled: December 27, 2007Publication date: April 9, 2009Applicant: Synta Pharmaceuticals CorpInventors: John Bertin, Jessica R. Kirshner, Zhenjian Du
-
Publication number: 20090042991Abstract: Methods of employing bis(thio-hydrazide amides) to increase NK cell activity in a subject in need thereof, e.g., a subject with an infection or an immunodeficiency, are provided such that the disorder is not cancer, a proliferative cell disorder, a non-infective heat shock protein 70 (Hsp70) responsive disorder, or a proteasome-inhibitor responsive disorder. Typically, a subject, e.g., a human, can be in need of increased NK cell activity has an immunodeficiency or is treated for an infection (e.g., a bacterial, viral, fungal, or parasite infection, or a combination thereof). The method includes administering to the subject an effective amount of a compound represented by Structural Formula I: Y is a covalent bond or an optionally substituted straight chained hydrocarbyl group, or, Y, taken together with both >C=Z groups to which it is bonded, is an optionally substituted aromatic group.Type: ApplicationFiled: April 13, 2006Publication date: February 12, 2009Inventors: James Barsoum, Zhenjian Du
-
Patent number: 7476683Abstract: The present invention relates to glycinamide derivatives of formula (I), the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.Type: GrantFiled: July 31, 2003Date of Patent: January 13, 2009Assignee: Merck Patent GmbHInventors: Hans-Peter Buchstaller, Matthias Wiesner, Oliver Schadt, Christiane Amendt, Frank Zenke, Christian Sirrenberg, Matthias Grell
-
Publication number: 20080318881Abstract: The present invention includes a fast-drying liquid composition comprising at least one fungicide and at least one insecticide. The present invention further includes a method for treating plant propagation materials, especially cut seeds, including tubers, against pests, a method for promoting suberization in cut seeds, a method for decreasing the drying time of a liquid pesticide on cut seeds, and a method for selectively loading a pesticide onto the skin side of a cut seed.Type: ApplicationFiled: June 28, 2006Publication date: December 25, 2008Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Marlene Torrent-Parker, Kiran Shetty
-
Publication number: 20080319080Abstract: Since an amide compound represented by the formula (1) is effective for controlling plant diseases, it is useful as an effective ingredient of a composition for controlling plant diseases.Type: ApplicationFiled: October 20, 2006Publication date: December 25, 2008Inventor: Takashi Komori
-
Publication number: 20080269340Abstract: Disclosed are bis(thio-hydrazide amide) disalts, which are represented by Structural Formula (I): Y is a covalent bond or a substituted or unsubstituted straight chained hydrocarbyl group. R1-R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. Z is —O or —S. M+ is a pharmaceutically acceptable monovalent cation and M2+ is a pharmaceutically acceptable divalent cation. Also, disclosed are pharmaceutical compositions comprising a bis(thio-hydrazide amide) disalt described above. Further disclosed are methods of treating a subject with cancer. The methods comprise the step of administering an effective amount of a bis(thio-hydrazide amide) disalt described above.Type: ApplicationFiled: April 18, 2008Publication date: October 30, 2008Applicant: Synta Pharmaceuticals Corp.Inventors: Keizo Koya, Lijun Sun, Elena Kostik, Farid Vaghefi, Shoujun Chen, Noriaki Taitsuta, Guiqing Liang, Takayo Inoue, Zhi-Qiang Xia
-
Publication number: 20080242702Abstract: One embodiment of the present invention is a compound represented by the Structural Formula (I): Y is a covalent bond of a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C=Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 is an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, or a substituted non-aromatic heterocyclic group, R2-R4 are independently —H, an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, a substituted non-aromatic heterocyclic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring.Type: ApplicationFiled: March 20, 2008Publication date: October 2, 2008Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Noriaki Tatsuta, Yaming Wu, Mitsunori Ono, Zhi-Qiang Xia
-
Publication number: 20080226588Abstract: Disclosed herein are methods of treating lentigo maligna, superficial spreading malignant melanoma, acral lentiginous malignant melanoma or nodular malignant melanoma with bis(thio-hydrazide amides) represented by a formula selected from structural formulas (i)-(ix) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these bis(thio-hydrazide amides) and compositions comprising these bis(thiohydrazide)amides and one or more anti-cancer agent.Type: ApplicationFiled: August 20, 2007Publication date: September 18, 2008Inventor: Matthew McLeod
-
Patent number: 7425649Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR modulators to treat or inhibit the progression of, for example, dyslipidemia.Type: GrantFiled: September 14, 2005Date of Patent: September 16, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: Gee-Hong Kuo, Rui Zhang, Aihua Wang, Alan DeAngelis, Keith Demarest, Patricia Pelton
-
Publication number: 20080220103Abstract: Provided is a method of treating a fungal infection on an animal epidermis, nail or hair, or in an orifice of an animal. The method comprises contacting the fungus infection with a composition comprising an antifungal botanical.Type: ApplicationFiled: March 13, 2008Publication date: September 11, 2008Inventors: Jay Birnbaum, Thomas Blake, Mahmoud Ghannoum, Steven Vallespir
-
Publication number: 20080214627Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.Type: ApplicationFiled: August 13, 2007Publication date: September 4, 2008Inventors: Robert Eugene Hormann, Colin M. Tice, Orestes Chortyk, Howard Smith, Thomas Meteyer
-
Publication number: 20080176908Abstract: A method for the treatment of acne comprising the administration, to a patient afflicted therewith, of a effective amount of a squalene monooxygenase inhibitor such as tolnaftate, naftifine, terbinafine, butenafine or ciclopirox. An advantage of the present invention relates to the surprisingly speedy onset of effectiveness in relieving acne symptoms. The compound may be administered orally or topically.Type: ApplicationFiled: January 18, 2007Publication date: July 24, 2008Inventor: Weylan R. McAnally
-
Publication number: 20080176828Abstract: Disclosed herein are methods of preventing or delaying the recurrence of melanoma in a subject with bis(thio-hydrazide amides) represented by a formula selected from Structural Formulas (I)-(IX) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these bis(thio-hydrazide amides) and compositions comprising these bis(thiohydrazide)amides and one or more anti-cancer agent.Type: ApplicationFiled: August 20, 2007Publication date: July 24, 2008Inventors: Martin Williams, Matthew McLeod, Keizo Koya
-
Publication number: 20080153701Abstract: Fungicidal mixtures, comprising as active components 1) carbamate oxime ethers of the formula I, in which X is N or CH, and 2) at least one active compound II selected from the group of the azoles, strobilurins, carboxamides, heterocyclic compounds, carbamates, guanidines, antibiotics, nitrophenyl derivatives, sulfur-containing heterocyclyl compounds, organometallic compounds, organophosphorus compounds, organochlorine compounds, inorganic active compounds, cyflufenamid, cymoxanil, dimethirimol, ethirimol, furalaxyl, metrafenone and spiroxamine, in a synergistically effective amount, methods for controlling harmful fungi using mixtures of the compound I with active compounds II, the use of the compound I with active compounds II for preparing such mixtures and compositions comprising these mixtures.Type: ApplicationFiled: December 21, 2005Publication date: June 26, 2008Applicant: BASF AktiengesellschaftInventors: Markus Gewehr, Reinhard Stierl, Matthias Niedenbruck
-
Patent number: 7385084Abstract: Disclosed are bis(thio-hydrazide amide) disalts, which are represented by Structural Formula (I): Y is a covalent bond or a substituted or unsubstituted straight chained hydrocarbyl group. R1-R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. Z is —O or —S. M+ is a pharmaceutically acceptable monovalent cation and M2+ is a pharmaceutically acceptable divalent cation. Also, disclosed are pharmaceutical compositions comprising a bis(thio-hydrazide amide) disalt described above. Further disclosed are methods of treating a subject with cancer. The methods comprise the step of administering an effective amount of a bis(thio-hydrazide amide) disalt described above.Type: GrantFiled: June 20, 2005Date of Patent: June 10, 2008Assignee: Synta Pharmaceutical Corp.Inventors: Keizo Koya, Lijun Sun, Elena Kostik, Farid Vaghefi, Shoujun Chen, Noriaki Tatsuta, Guiqing Liang, Takayo Inoue, Zhi-Qiang Xia
-
Publication number: 20080118562Abstract: Disclosed herein are compositions and methods useful for the in vivo delivery bis(thiohydrazide amides), encased in a polymeric biocompatible shell.Type: ApplicationFiled: September 10, 2007Publication date: May 22, 2008Inventor: Keizo Koya
-
Publication number: 20080119440Abstract: Disclosed herein are methods of treating a proliferative disease, such as cancer, with bis(thio-hydrazide amides) or a tautomer, pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, in combination with hyperthermia treatment. Also disclosed are methods of treating a proliferative disease, such as cancer, with bis(thio-hydrazide amides) or a tautomer, pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, in combination with radiotherapy.Type: ApplicationFiled: August 30, 2007Publication date: May 22, 2008Inventor: Keizo Koya
-
Patent number: 7345094Abstract: Disclosed is a compound represented by the Structural Formula (I): Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C=Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 and R2 are independently an aryl group or a substituted aryl group, R3 and R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is ?O or ?S.Type: GrantFiled: October 5, 2005Date of Patent: March 18, 2008Assignee: Synta Pharmaceuticals Corp.Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Noriaki Tatsuta, Yaming Wu, Mitsunori Ono
-
Patent number: 7288262Abstract: Compositions, in particular cosmetic compositions, comprising a cyclohexane-based compound defined by formula (I): wherein: R, which may be identical or different, are each chosen from hydrogen atoms and linear and branched, saturated hydrocarbons comprising 1 to 6 carbon atoms; Y, which may be identical or different, are each chosen from —CO—S—R? groups, —CO—NHR? groups, NH—COR? groups and —S—COR? groups, wherein R?, which may be identical or different, are each chosen from hydrogen atoms, aryl groups, optionally substituted with at least one hydrocarbon comprising 1 to 22 carbon atoms, wherein said hydrocarbon is chosen from linear and branched, saturated and unsaturated hydrocarbons, and linear, branched and cyclic, saturated and unsaturated hydrocarbons comprising 1 to 22 carbon atoms, wherein said hydrocarbons may optionally be substituted with at least one group chosen from aryl groups, ester groups, amide groups and urethane groups; wherein said hydrocarbons may optionally comprise at least onType: GrantFiled: September 20, 2000Date of Patent: October 30, 2007Assignee: L'Oreal S.A.Inventor: Aude Livoreil
-
Patent number: 7105545Abstract: The invention relates to N-propargyloxy-phenethyl thioacetic acid amide derivatives of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein R1 is hydrogen, alkyl, cycloalkyl or optionally substituted aryl, R2 and R3 are each independently hydrogen or alkyl, R4 is alkyl, alkenyl or alkynyl, R5, R6, R7 and R8 are each independently hydrogen or alkyl, R9 is hydrogen, optionally substituted alkyl, optionally substituted alkenyl or optionally substituted alkynyl, R10 is optionally substituted aryl or optionally substituted heteroaryl, and Z is hydroxy, optionally substituted aryloxy, optionally substituted alkoxy, optionally substituted alkynyloxy, optionally substituted arylthio, optionally substituted alkylthio, optionally substituted alkynylthio, optionally substituted alkylsulfinyl, optionally substituted alkenysulfinyl, optionally substituted alkynylsulfinyl, optionally substituted alkylsulfonyl, optionally substituted alkenylsulfonyl, optionally substituted alkyType: GrantFiled: April 2, 2002Date of Patent: September 12, 2006Assignee: Syngenta Crop Protection, Inc.Inventors: Walter Kunz, Clemens Lamberth, Fredrik Cederbaum, Martin Zeller
-
Patent number: 7074952Abstract: Disclosed is a method of preparing a thiohydrazide product compound from a hydrazide starting compound. The hydrazide starting compound is represented by Structural Formula (I): The thiohydrazide product compound is represented by Structural Formula (II): In Structural Formulas (I)–(II), R1 and R2 are independently an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R2 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. When R2 is an aryl group or a substituted aryl group, then R5 is a hydrazine protecting group; and when R2 is an aliphatic or substituted aliphatic group, then R5 is —H or a hydrazine protecting group. R10 is —H or a substituted or unsubstituted alkyl group. The method comprising the step of reacting the starting compound with a thionylating reagent.Type: GrantFiled: March 24, 2004Date of Patent: July 11, 2006Assignee: Synta Pharmaceuticals, Corp.Inventors: Shoujun Chen, Lijun Sun, Zhi-Qiang Xia, Keizo Koya, Mitsunori Ono