Nitrogen Containing Hetero Ring In The Nitrogen Containing Substituent (e.g., Oxazole, Etc.) Patents (Class 544/42)
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Patent number: 10035795Abstract: The present invention provides a phenothiazine derivative or a pharmaceutically acceptable salt thereof, a method of preparing a compound selected therefrom and a pharmaceutical composition containing the compound as an active ingredient. The phenothiazine derivative according to the present invention has an effect of inhibiting calmodulin (CaM; calcium-modulated protein) and thus helps cell death by maintaining the intracellular level of calcium in lung cancer cells at high concentration. Accordingly, the phenothiazine derivative according to the present invention can be usefully used to prevent or treat malignant tumors such as lung cancer.Type: GrantFiled: April 6, 2017Date of Patent: July 31, 2018Assignee: Korea Institute of Science and TechnologyInventors: Eun Joo Roh, Bo Ra Mi Jeon, Chang Joon Lee, Jin Pyo Hong, Joo Yeon Jeong, Sang Soo Kang
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Patent number: 9040173Abstract: The present invention relates to a triphenylene-based compound represented by the following Formula 1 and an organic electroluminescent device including the same, and the compound of the present invention has excellent hole injection and/or transporting ability, electron transporting ability, and/or light emitting ability, and particularly, green and red light emitting ability, and thus in an organic electroluminescent device containing the same as a light emitting host material, characteristics such as luminous efficiency, luminance, thermal stability, driving voltage, service life and the like may be improved. In the formula, each of A, L, X and R1 to R19 is the same as those as defined in Detailed Description.Type: GrantFiled: December 29, 2010Date of Patent: May 26, 2015Assignee: DOOSAN CORPORATIONInventors: Jin-Seok Hong, Chang-Ju Shin, Tae-Hyung Kim, Kyoung-Soo Kim
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Publication number: 20150041784Abstract: A compound represented by the general formula (1) is useful as a light-emitting material. In the general formula (1), Ar1 to Ar3 represent an aryl group, provided that at least one thereof represents an aryl group substituted by a group represented by the general formula (2). In the general formula (2), R1 to R8 represent a hydrogen atom or a substituent; Z represents O, S, O?C or Ar4—N; and Ar4 represents an aryl group.Type: ApplicationFiled: May 10, 2013Publication date: February 12, 2015Inventors: Katsuyuki Shizu, Hiroyuki Tanaka, Hajime Nakanotani, Chihaya Adachi
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Publication number: 20140294994Abstract: The preset invention relates to use of antipsychotic phenothiazine derivative for eliminating cancer stem cells (CSCs) and/or preventing a cancer. The invention also provides a pharmaceutical composition for treating a cancer, and/or preventing or delaying cancer recurrence comprising trifluoperazine and an anti-cancer drug, such as gefitinib or cisplatin.Type: ApplicationFiled: October 29, 2012Publication date: October 2, 2014Inventor: Ch-Ying Huang
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Publication number: 20140288060Abstract: The invention relates to a compound for use in treating a cancer, wherein the cancer depends on the proteolytic activity of the MALT1 protease, and wherein the compound has the general formula (I) wherein X is N or C; Y is S, O, SO2, SO, NH, CO, CH2, CH?CH, CH2?CH2; ( )z is a C1-C5 linear or branched alkyl chain; A is NR3R4, or OR5, or HET; R1 and R2 in each occurrence are independently selected from —H, —CH3, —OH, —OCH3, —SCH3, —F, —Cl, —CF3, —NH2, and —COOH; R3, R4, and R5 are H, or C1-C5 linear or branched alkyl groups, and HET is a heterocyclic ring of 5, 6, or 7 members, wherein the ring atoms can be C, O, N, or S, the ring can be saturated or aromatic, and the ring can be substituted with H or C1-C5 linear or branched alkyl groups; or a pharmaceutically acceptable salt, prodrug, enantiomer, diastereomer, racemic mixture, crystalline form, amorphous form, unsolvated form or solvate of said compound. The compound of the invention may further be used in the treatment of MALT1-dependent immune diseases.Type: ApplicationFiled: August 1, 2012Publication date: September 25, 2014Applicant: Helmholtz Zentrum München, Deutsches Forschungszentrum für Gesundheit and Umwelt GmbH)Inventors: Daniel Krappmann, Daniel Nagel, Dolores Schendel, Stefani Spranger
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Patent number: 8754074Abstract: The present invention relates to the use of the vinyl quinuclidine enantiomer (R) of the following formula 2 as a synthesis intermediate in the preparation of (R)-mequitazine.Type: GrantFiled: January 10, 2012Date of Patent: June 17, 2014Assignees: Pierre Fabre Medicament, Commissariat a l'Energie Atomique et aux Energies AlternativesInventors: Marc Nicolas, Laurent Larquetoux, Sébastien Leroux, Eric Doris
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Publication number: 20130310348Abstract: This disclosure provides a new class of compounds referred to as “reversed chloroquines” (RCQs), which are highly effective against CQR and CQS malaria parasites. RCQs are hybrid molecules, which include an antimalarial quinoline analog (such as chloroquine) moiety and a CQR reversal moiety. Exemplary RCQ chemical structures are provided. Also provided are pharmaceutical compositions including the disclosed RCQ compounds, and methods of using such compounds and compositions for the treatment of malaria and inhibition of CQR or CQS Plasmodium sp. (such as P. falciparum).Type: ApplicationFiled: July 25, 2013Publication date: November 21, 2013Applicants: State UniversityInventors: David H. Peyton, Steven Burgess
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Publication number: 20130126856Abstract: An organic compound with excellent characteristics excelling in hole-injecting/transporting performance and having electron blocking ability, high stability in a thin-film state and high luminous efficiency is provided as material for an organic electroluminescent device. The compound of a general formula (1) having an indenocarbazole ring structure is used as a constituent material of at least one organic layer in the organic electroluminescent device that includes a pair of electrodes and one or more organic layers sandwiched between the pair of electrodes.Type: ApplicationFiled: July 29, 2011Publication date: May 23, 2013Applicant: HODOGAYA CHEMICAL CO., LTD.Inventors: Norimasa Yokoyama, Makoto Nagaoka, Kazunori Togashi, Kouki Kase, Eiji Takahashi
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Chemically modified mutant serine hydrolases show improved catalytic activity and chiral selectivity
Patent number: 8357524Abstract: This invention provides novel chemically modified mutant serine hydrolases that catalyze a transamidation and/or a transpeptidation and/or a transesterification reaction. The modified serine hydrolases have one or more amino acid residues in a subsite replaced with a cysteine, wherein the cysteine is modified by replacing the thiol hydrogen in the cysteine with a substituent group providing a thiol side chain comprising a moiety selected from the group consisting of a polar aromatic substituent, an alkyl amino group with a positive charge, and a glycoside. In particularly preferred embodiments, the substitutents include an oxazolidinone, a C1 to C15 alkyl amino group with a positive charge, or a glycoside.Type: GrantFiled: July 30, 2012Date of Patent: January 22, 2013Assignee: Danisco US Inc.Inventors: John Bryan Jones, Michael Dickman, Richard C. Lloyd -
Publication number: 20130009136Abstract: The present invention relates to a triphenylene-based compound represented by the following Formula 1 and an organic electroluminescent device including the same, and the compound of the present invention has excellent hole injection and/or transporting ability, electron transporting ability, and/or light emitting ability, and particularly, green and red light emitting ability, and thus in an organic electroluminescent device containing the same as a light emitting host material, characteristics such as luminous efficiency, luminance, thermal stability, driving voltage, service life and the like may be improved. In the formula, each of A, L, X and R1 to R19 is the same as those as defined in Detailed Description.Type: ApplicationFiled: December 29, 2010Publication date: January 10, 2013Applicant: DOOSAN CORPORATIONInventors: Jin-Seok Hong, Chang-Ju Shin, Tae-Hyung Kim, Kyoung-Soo Kim
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Publication number: 20120261650Abstract: An organic electroluminescent device comprising: a pair of electrodes comprising an anode and a cathode, and one or more layers arranged between the anode and the cathode; wherein at least one of the one or more layers is a light emitting layer and wherein the one or more layers, comprises an organic compound represented by a substituted 2,2?-biimidazole.Type: ApplicationFiled: October 21, 2011Publication date: October 18, 2012Applicant: Commonwealth Scientific and Industrial Research OrganisationInventors: James Matthew MacDonald, Mark Bown, Kazunori Ueno, Karl Peter Weber, Jenny Lee O'Connell, Tadahiko Hirai
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Publication number: 20120217485Abstract: Provided are novel organic electroluminescent compounds and organic electroluminescent devices using the same. Since the organic electroluminescent compound exhibits good luminous efficiency and excellent life property compared to the existing material, it may be used to manufacture OLED devices having superior operation life and consuming less power due to improved power efficiency.Type: ApplicationFiled: July 30, 2010Publication date: August 30, 2012Applicant: ROHM AND HAAS ELECTRONIC MATERIALS KOREA LTD.Inventors: Hyo Jung Lee, Young Jun Cho, Sung Jin Eum, Hyuck Joo Kwon, Bong Ok Kim, Sung Min Kim, Seung Soo Yoon
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Chemically modified mutant serine hydrolases show improved catalytic activity and chiral selectivity
Patent number: 8148128Abstract: This invention provides novel chemically modified mutant serine hydrolases that catalyze a transamidation and/or a transpeptidation and/or a transesterification reaction. The modified serine hydrolases have one or more amino acid residues in a subsite replaced with a cysteine, wherein the cysteine is modified by replacing the thiol hydrogen in the cysteine with a substituent group providing a thiol side chain comprising a moiety selected from the group consisting of a polar aromatic substituent, an alkyl amino group with a positive charge, and a glycoside. In particularly preferred embodiments, the substitutents include an oxazolidinone, a C1 to C15 alkyl amino group with a positive charge, or a glycoside.Type: GrantFiled: September 19, 2008Date of Patent: April 3, 2012Assignee: The Governing Council of the University of TorontoInventors: John Bryan Jones, Michael Dickman, Richard C. Lloyd -
Patent number: 8143245Abstract: This invention relates to the use of 10-[(3R)-1-azabicyclo[2.2.2]oct-3-ylmethyl]-10H-phenothiazine as well as its pharmaceutically acceptable salts for the preparation of a drug having the particularity of treating or preventing urinary incontinence, by local and/or oral route.Type: GrantFiled: December 26, 2007Date of Patent: March 27, 2012Assignee: Pierre Fabre MedicamentInventors: Thierry Clerc, Jacky Tisne-Versailles, Christophe Przybylski
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Publication number: 20120035161Abstract: The invention includes compositions and methods for inhibiting proliferation and inducing apoptosis in activated lymphocytes, treating diseases associated with activated lymphocytes, or treating PAH.Type: ApplicationFiled: July 18, 2011Publication date: February 9, 2012Inventors: Stephen Roth, Bruce Tomczuk
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Publication number: 20110223221Abstract: The present invention relates to processes of stabilization of cation radicals from one or more phenothiazinic compounds or derivatived compounds thereof. Another embodiment of the present invention relates to cosmeceutical formulations comprising one or more phenothiazinic compounds or derivatived compounds thereof, in combination with cosmeceutically acceptable excipients. The invention also relates to uses of one or more phenothiazinic compounds or derivatived compounds thereof, i the preparation of cosmeceutical formulations for the prevention of skin diseases and disturbances. Methods for prevention of skin diseases and disturbances are also disclosed by the present invention. Particularly, the embodiments of the present invention employ the cited one or more phenothiazinic compounds o derivatived compounds thereof in the form of their stabilized cation radicals.Type: ApplicationFiled: May 12, 2009Publication date: September 15, 2011Inventors: Iseli Lourenco Nantes, Tiago Rodrigues, Carolina Gregorutti Dos Santos
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Patent number: 7981885Abstract: The present invention relates to inhibiting proliferation and inducing apoptosis in activated lymphocytes, including T cells and B cells. The invention also provides compositions and methods for inhibiting proliferation and inducing apoptosis in activated lymphocytes, as well methods for treating diseases associated with activated lymphocytes by administering 5-HT receptor antagonists.Type: GrantFiled: August 31, 2007Date of Patent: July 19, 2011Assignee: Immune Control Inc.Inventors: Stephen Roth, Clayton Buck, Christopher Self, Gary Olson
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Patent number: 7790298Abstract: Organic electronic devices comprising a phthalimide compound. The phthalimide compounds disclosed herein are electron transporters with large HOMO-LUMO gaps, high triplet energies, large reduction potentials, and/or thermal and chemical stability. As such, these phthalimide compounds are suitable for use in any of various organic electronic devices, such as OLEDs and solar cells. In an OLED, the phthalimide compounds may serve various functions, such as a host in the emissive layer, as a hole blocking material, or as an electron transport material. In a solar cell, the phthalimide compounds may serve various functions, such as an exciton blocking material. Various examples of phthalimide compounds which may be suitable for use in the present invention are disclosed.Type: GrantFiled: April 12, 2007Date of Patent: September 7, 2010Assignee: The University of Southern CaliforniaInventors: Azad M. Hassan, Mark E. Thompson
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Publication number: 20100093709Abstract: The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic ?-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.Type: ApplicationFiled: November 20, 2009Publication date: April 15, 2010Inventors: Steven J. Coats, Scott L. Dax, Bart DeCorte, Li Liu, Mark McDonnell, James J. McNally
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Patent number: 7652005Abstract: The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic ?-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.Type: GrantFiled: October 9, 2008Date of Patent: January 26, 2010Assignee: Janssen Pharmaceutica N.V.Inventors: Steve Coats, Scott L. Dax, Bart DeCorte, Li Liu, Mark McDonnell, James J. McNally
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Publication number: 20090275557Abstract: The present invention relates to inhibiting proliferation and inducing apoptosis in activated lymphocytes, including T cells and B cells. The invention also provides compositions and methods for inhibiting proliferation and inducing apoptosis in activated lymphocytes, as well methods for treating diseases associated with activated lymphocytes by administering 5-HT receptor antagonists.Type: ApplicationFiled: February 26, 2009Publication date: November 5, 2009Applicant: Immune Control, Inc.Inventors: Stephen Roth, Clayton Buck, Christopher Self, Gary Olson, Nallaganchu Rao
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Publication number: 20090192146Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.Type: ApplicationFiled: February 9, 2009Publication date: July 30, 2009Applicant: ACEA BIOSCIENCES, INC.Inventors: Xiao XU, Haoyun An, Xiaobo Wang
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Patent number: 7432257Abstract: The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic ?-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.Type: GrantFiled: January 5, 2006Date of Patent: October 7, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: Steve J. Coats, Scott L. Dax, Bart DeCorte, Li Liu, Mark McDonnell, James J. McNally
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Patent number: 7414128Abstract: The present invention relates to crystalline R-guanidines of (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate, its preparations and its use as therapeutic agents. More specifically the present invention relates to crystalline Arginine (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate, preferably (L)-Arginine (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate, its preparation and its use as therapeutic agent.Type: GrantFiled: March 14, 2005Date of Patent: August 19, 2008Assignees: Dr. Reddy's Laboratories, Limited, Dr. Reddy's Laboratories, Inc.Inventors: Søren Ebdrup, Petra Christine Lugstein
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Patent number: 7189483Abstract: An improved organophotoreceptor includes an electrically conductive substrate and a photoconductive element on the electrically conductive substrate where the photoconductive element comprises: a) a charge transport material having the following formula: where X is a linking group; Y1 and Y2 are, each independently, a phenothiazine group, a phenoxazine group, or a phenazine group; R1, R2, R3, and R4 are, each independently, an alkyl group, an alkenyl group, a heterocyclic group, or an aromatic group; and R5 and R6 are, each independently, a hydrogen, an alkyl group, an alkenyl group, a heterocyclic group, or an aromatic group; and (b) a charge generating compound. Corresponding electrophotographic apparatuses and imaging methods are described.Type: GrantFiled: February 27, 2004Date of Patent: March 13, 2007Assignee: Samsung Electronics Co., Ltd.Inventors: Almantas Danilevicius, Gintaras Buika, Ramunas Lygaitis, Juozas V. Grazulevicius, Robertas Maldzius, Edmundas Montrimas, Zbigniew Tokarski, Nusrallah Jubran
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Patent number: 7169521Abstract: Improved organophotoreceptor comprises an electrically conductive substrate and a photoconductive element on the electrically conductive substrate, the photoconductive element comprising: (a) a charge transport material having the formula ?where R1 and R2 are, each independently, an alkyl group, an alkenyl group, an alkynyl group, an aromatic group, or a heterocyclic group; R3 and R4 are, each independently, H, an alkyl group, an alkenyl group, an alkynyl group, an aromatic group, or a heterocyclic group; X1 and X2 are, each independently, a linking group; Y1 and Y2, each independently, comprise an arylamine group; and Z is a bridging group; and (b) a charge generating compound. Corresponding electrophotographic apparatuses and imaging methods are described.Type: GrantFiled: April 30, 2004Date of Patent: January 30, 2007Assignee: Samsung Electronics Co., Ltd.Inventors: Zbigniew Tokarski, Nusrallah Jubran, Vytautas Getautis, Jonas Sidaravicius, Edmundas Montrimas, Maryte Daskeviciene, Valentas Gaidelis, Vygintas Jankauskas, Albina Stanisauskaite
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Patent number: 6992082Abstract: Phenothiazine derivatives of formula (I) are disclosed. The compounds are inhibitors of the mitotic kinesin KSP and are useful in the treatment of cellular proliferative diseases, such as cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders and inflammation.Type: GrantFiled: January 18, 2002Date of Patent: January 31, 2006Assignee: Cytokinetics, Inc.Inventors: Jeffrey T. Finer, John C. Chabala
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Patent number: 6919351Abstract: Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: October 9, 2001Date of Patent: July 19, 2005Assignee: Merck & Co., Inc.Inventors: Neville J. Anthony, Robert P. Gomez, Steven D. Young, Melissa S. Egbertson, John S. Wai, Jennifer J. Bennett
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Publication number: 20040248885Abstract: The invention concerns compounds of general formula (I), wherein: A represents one of the radicals in which R5 represents independently a hydrogen atom, or alkyl; R6, R7 and R8 independently represent a hydrogen atom, alkyl, cycloalkyl, hydroxy or alkoxy; R11 represents a hydrogen atom of alkyl; and R9, R10 and R12 independently represent a hydrogen atom, alkyl, hydroxy or alkoxy: B represents a hydrogen atom or alkyl; n represents an integer from 0 to 5; R1 and R2 independently represent a hydrogen atom, alkyl or cycloalkyl; R3 and R4 independently represent a hydrogen atom or an alkyl radical, or R3 and R4 together form with the nitrogen atom which bears them a heterocycle optionally substituted comprising in all 1 to 2 heteroatoms and 5 to 7 members. Said compounds can be used for preparing a medicine for protecting mitochondria, and in particular a medicine for preventing or treating cirrhosis.Type: ApplicationFiled: January 13, 2004Publication date: December 9, 2004Inventors: Michel Auguet, Pierre-Etienne Chabrier De Lassauniere, Jeremiah Harnett
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Publication number: 20040242570Abstract: Novel chemical conjugates of psychotropic drugs and organic acids, uses thereof in the treatment of psychotic and/or proliferative disorders and diseases and as chemosensitizing agents, and their syntheses are disclosed. The organic acids are selected to reduce side effects induced by the psychotropic drugs and/or to exert an anti-proliferative activity.Type: ApplicationFiled: March 25, 2004Publication date: December 2, 2004Inventors: Abraham Nudelman, Ada Rephaeli, Irit Gil-Ad, Abraham Weizman
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Publication number: 20040241563Abstract: An improved organophotoreceptor includes an electrically conductive substrate and a photoconductive element on the electrically conductive substrate where the photoconductive element comprises:Type: ApplicationFiled: February 27, 2004Publication date: December 2, 2004Inventors: Almantas Danilevicius, Gintaras Buika, Ramunas Lygaitis, Juozas V. Grazulevicius, Robertas Maldzius, Edmundas Montrimas, Zbigniew Tokarski, Nusrallah Jubran
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Publication number: 20040092515Abstract: Compounds of the formula I: 1Type: ApplicationFiled: August 27, 2003Publication date: May 13, 2004Inventors: Torbjjorn Lundstedt, Anneli Hallgren, Per Andersson, Anders Hallberg, Malin Graffner Nordberg
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Publication number: 20040053923Abstract: This invention relates to compounds represented by the general formula [I] 1Type: ApplicationFiled: April 8, 2003Publication date: March 18, 2004Applicant: Banyu Pharmaceutical Co., Ltd.Inventors: Toshio Nagase, Tomoharu Iino, Yoshiyuki Sato, Teruyuki Nishimura, Jun-Ichi Eiki
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Patent number: 6703401Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by clear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).Type: GrantFiled: November 27, 2001Date of Patent: March 9, 2004Assignees: Novo Nordisk A/S, Dr. Reddy's Research FoundationInventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Patent number: 6608194Abstract: A compound of Formula (Ih) The compounds may be used, inter alia, for preparing beta aryl-alpha-oxy substituted alkylcarboxylic acids.Type: GrantFiled: May 10, 2001Date of Patent: August 19, 2003Assignee: Dr. Reddy's Laboratories LimitedInventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Ashok Channaveerappa Bajji, Shivaramayya Kalchar, Rao Bheema Paraselli, Ranga Madhavan Gurram
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Patent number: 6583138Abstract: The invention provides a novel heterocyclic ring condensed benzothiazine compound which is effective for prevention or remedy of disease, in which histamine, leukotriene and the like participate. The heterocyclic ring condensed benzothiazine compound of the present invention or a pharmacologically acceptable salt thereof is effective for prevention or remedy of disease, in which a chemical mediator, such as histamine, leukotriene and the like, participate, for example, asthma, allergic coryza, atopic dermatitis, hives, hay fever, gastrointestinal allergy, food allergy and the like.Type: GrantFiled: January 4, 2001Date of Patent: June 24, 2003Assignee: Eisai Co., Ltd.Inventors: Mitsuaki Miyamoto, Tatsuya Yoshiuchi, Keizo Sato, Motohiro Soejima, Takashi Sato, Koichi Kikuchi, Hiroyuki Yoshimura, Katsuhiro Moriya, Yoshinori Sakuma, Shigeru Akasofu, Koji Yamada
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Patent number: 6548666Abstract: A compound of Formula (Ig) The compounds may be used, inter alia, for preparing beta aryl-alpha-oxy substituted alkylcarboxylic acids.Type: GrantFiled: May 10, 2001Date of Patent: April 15, 2003Assignees: Dr. Reddy's Research Foundation, Reddy-Cheminor, Inc.Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Ashok Channaveerappa Bajji, Shivaramayya Kalchar, Rao Bheema Paraselli, Ranga Madhavan Gurram
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Publication number: 20030032801Abstract: A compound having the structural formula 1Type: ApplicationFiled: May 7, 2001Publication date: February 13, 2003Inventors: Ai J. Lin, Jian Guan, Dennis E. Kyle, Wilbur K. Milhous
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Patent number: 6444811Abstract: Compounds represented by formula I: as well as pharmaceutically acceptable salts, esters, N-oxides and hydrates thereof are disclosed. Pharmaceutical compositions and methods of use are also included. The compounds are active against the caspase-3 enzyme, and thus are useful to treat fin caspase-3 mediated diseases and conditions.Type: GrantFiled: July 19, 2000Date of Patent: September 3, 2002Assignee: Merck Frosst Canada & Co.Inventors: Yongxin Han, Andre Giroux, Robert Zamboni, Daniel J. McKay, Christopher I. Bayly, Erich L. Grimm, John Colucci
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Patent number: 6440961Abstract: A compound of formula (1) it derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts, or its pharmaceutically acceptable solvates, processes for its preparation and methods of use thereof.Type: GrantFiled: February 24, 1999Date of Patent: August 27, 2002Assignees: Dr. Reddy's Research Foundation, Reddy-Cheminor, Inc.Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Ashok Channaveerappa Bajji, Shivaramayya Kalchar, Rao Bheema Paraselli, Ranga Madhavan Gurram, Rajagopalan Ramanujam, Ranjan Chakrabarti
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Patent number: 6333322Abstract: A phenothiazine, acridan, acridone oxime, acridone hydrazone and dibenzodiazepine derivative represented by formula (I) effective against diseases in which histamine, leukotrienes, etc. participate and effective in preventing or treating diseases in which chemical mediators such as histamine and leukotrienes participate, for example, asthma, allergic rhinitis, atopic dermatitis, urticaria, hay fever, gastrointestinal allergy and food allergy.Type: GrantFiled: September 21, 1998Date of Patent: December 25, 2001Assignee: Eisai Co., Ltd.Inventors: Mitsuaki Miyamoto, Tatsuya Yoshiuchi, Keizo Sato, Makoto Kaino, Masayuki Tanaka, Motohiro Soejima, Katsuhiro Moriya, Yoshinori Sakuma, Koji Yamada, Kokichi Harada, Yukio Nishizawa, Seiichi Kobayashi, Makoto Okita, Koichi Katayama
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Patent number: 6159966Abstract: A compound of formula (I) ##STR1## its tautomeric forms, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates, wherein R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are the same or different; R.sup.1 and R.sup.2 together represent along with carbon atoms to which they are attached an aromatic cyclic structure containing 5-6 ring atoms which may optionally be substituted; X represents a heteroatom selected from oxygen or sulfur; R.sup.7 represents hydrogen atom, hydroxy, alkoxy, halogen, lower alkyl group or optionally substituted aralkyl group or forms a bond together with R.sup.8 ; R.sup.8 represents hydrogen atom, hydroxy, alkoxy, halogen, lower alkyl group or optionally substituted aralkyl or R.sup.8 forms a bond together with R.sup.Type: GrantFiled: August 14, 1998Date of Patent: December 12, 2000Assignees: Reddy-Cheminor Inc., Dr. Reddy's Research FoundationInventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Ashok Chennaveerappa Bajji, Shivaramayya Kalchar, Sekar Reddy Alla, Rajagopalan Ramanujam, Reeba Kannimel Vikramadithyan
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Patent number: 6139876Abstract: A gelatin with increased oxygen content for pharmaceutical, cosmetic and/or veterinary use. The gelatin comprises a gelling agent and a solvent, furthermore oxygen in a substantially even distribution with a pressure exceeding normal atmospheric pressure, wherein the surface tension of the gelatin is sufficiently high to retain at least a portion of the overpressure of the oxygen throughout a predetermined period of time after having been exposed ton atmospheric environment. Glucose and bactericide and/or fungicide agents can be added to facilitate cellular metabolism and decrease the danger of local infections. The solvent can be distilled water or a physiologic saline solution.Type: GrantFiled: October 27, 1997Date of Patent: October 31, 2000Assignees: Jozsef Ladanyi, Mihaly LantosInventor: Peter Kolta
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Patent number: 6054453Abstract: Novel .beta.-aryl-.alpha.-oxysubstituted alkylcarboxylic acids of the formula (I) and compositions containing them. ##STR1## The compounds have hypolipidemic, antihyperglycemic uses.Type: GrantFiled: January 23, 1998Date of Patent: April 25, 2000Assignees: Redd's Research Foundation, Reddy-Cheminor, Inc.Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Ashok Channaveerappa Bajji, Shivaramayya Kalchar, Rajagopalan Ramanujam, Ranjan Chakrabarti
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Patent number: 5597819Abstract: New benzothiazine derivatives corresponding to the general formula I: ##STR1## in which: X represents halogen,n represents 0, 1, or 2,B represents the following formula: ##STR2## in which: R.sub.1 & R.sub.2 together with the carbons to which they are attached form a 6-carbon-atom aromatic ring which is optionally substituted by a group X' representing halogen, andY represents the radical --(SO.sub.2).sub.x --Alk--Z, x, Alk, and Z are as defined in the specification;as well as their possible stereoisomers, epimers, N-oxides and pharmaceutically-acceptable acid or base addition salts; and medicinal products containing the same, useful in the treatment of inflammatory disorders requiring an inhibitor of cytokines.Type: GrantFiled: February 13, 1995Date of Patent: January 28, 1997Assignee: Adir Et CompagnieInventors: Jean-Daniel Brion, Anne-Marie Chollet, Luc Demuynck, Lucy De Montarby, Yves Rolland, Jacqueline Bonnet, Pietro Ghezzi, Armel Fradin
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Patent number: 5321026Abstract: New phenothiazine derivatives of general formula (I) in whichR represents 4- to 6-membered cycloalkyl, or represents --CH.sub.2 R" in which R" is hydrogen, alkyl containing 1 to 5 carbon atoms, alkenyl or alkynyl containing 2 to 4 carbon atoms, cycloalkyl (3- to 6-membered), phenyl, optionally substituted (with 1 or 2 halogen atoms or with a hydroxyl, alkyl, alkyloxy, trifluoromethyl or nitro radical) or heterocyclic selected from furyl, thienyl or pyridyl, andR' either represents a radical of general formula (IIa) in which R.sub.1 and R.sub.2, which may be identical or different, are alkyl, cycloalkylalkyl, hydroxyalkyl or acetyloxyalkyl or, together with the nitrogen atom to which they are attached, form a saturated or partially unsaturated 4- to 7-membered heterocycle optionally substituted with 1 or 2 alkyl, hydroxyalkyl or acetyloxyalkyl radicals, andR.sub.Type: GrantFiled: January 27, 1992Date of Patent: June 14, 1994Assignee: Rhone-Poulenc Rorer S.A.Inventors: Claude Garret, Claude Guyon, Bernard Plau, Gerard Taurand
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Patent number: 5219879Abstract: The present invention relates to novel substituted 15-oxa-, 15-thia-, and 15-aza- dihydrolanosterols, to pharmaceutical compositions containing such compounds, and to methods of using these compounds to suppress the activity of 3-hydroxy-3- methylglutaryl coenzyme A reductase (HMGR), an enzyme which is important in cholesterol biosynthesis. The overall effect of these heterocyclic lanosterol analogs is to decrease cholesterol formation, thereby resulting in lower serum cholesterol levels in mammals, and impaired ergosterol synthesis in fungi.Type: GrantFiled: March 1, 1991Date of Patent: June 15, 1993Assignee: Du Pont Merck Pharmaceutical CompanyInventors: Soo S. Ko, James M. Trzaskos
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Patent number: 5049669Abstract: Phenothiazine derivatives of general formula (I), in which R is a linear or branched (1 to 6 C) alkyl radical and R.sub.1 and R.sub.2, which may be identical or different, are linear or branched (1 to 4 C) alkyl radicals or form, with the nitrogen atom to which they are attached, a 4- to 7-membered heterocycle, their isomeric forms and mixtures thereof as well as their addition salts with acids, possess analgesic and diuretic activity.Type: GrantFiled: June 12, 1989Date of Patent: September 17, 1991Assignee: Rhone-Poulenc SanteInventors: Claude Garret, Claude Guyon, Bernard Plau, Gerard Taurand
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Patent number: 5024774Abstract: This invention describes compositions containing nitrogen, sulfur and optionally oxygen which are useful as antioxidants for lubricants.Type: GrantFiled: August 10, 1989Date of Patent: June 18, 1991Assignee: The Lubrizol CorporationInventor: Mary F. Salomon
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Patent number: 4985419Abstract: Phenothiazine derivatives of formula: ##STR1## in which Y is hydrogen or halogen, R.sub.1 and R.sub.2, which may be identical or different, denote alkyl, cycloalkyl-alkyl, hydroxyalkyl or acetyloxyalkyl radicals or form, together with the nitrogen atom to which they are attached, an optionally substituted, saturated or partially unsaturated 4- to 7-membered heterocycle; and either X is oxygen, sulphur or: N-R.sub.4, R is cycloalkyl, phenyl or --CH.sub.2 R.sub.3, R.sub.3 is H, alkyl (1 to 5 C), alkenyl or alkynyl (2 to 4 C), cycloalkyl (3 to 6 C), phenyl, substituted phenyl or a heterocyclic radical, R.sub.4 is H or --CN, except that X is not oxygen if, simultaneously, R.sub.3 is H or alkyl, R.sub.1 and R.sub.2 are alkyl or NR.sub.1 R.sub.2 forms an unsubstituted heterocycle, and Y is H; or X is: N-R.sub.4 and R.sub.Type: GrantFiled: June 12, 1989Date of Patent: January 15, 1991Assignee: Rhone-Poulenc SanteInventors: Claude Garret, Claude Guyon, Bernard Plau, Gerard Taurand