Halogen Attached Directly To The 1,2-diazine Ring By Nonionic Bonding Patents (Class 544/241)
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Patent number: 11690377Abstract: Described are herbicidal compositions that contain mesotrione and pyridate, as well as related method to control weeds in crops, such as of maize, sweet corn, oilseed rape, cereals, rice, peanuts, vegetables wheat, barley, rye, rice, maize, sugar beet, cotton and soybeans.Type: GrantFiled: July 12, 2018Date of Patent: July 4, 2023Assignee: Belchim Crop Protection NVInventors: Christian Stratmann, James R. Whitehead, Felix Thurwächter
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Patent number: 9029295Abstract: The present invention relates to a pyridazinone compound of the formula (I): wherein R1 represents hydrogen, a C1-6 alkyl group, and the like, R2 represents halogen, a cyano group, a nitro group, a C1-6 alkoxy group, and the like, G represents hydrogen, and the like, Z represents halogen, a cyano group, a nitro group, a C1-6 alkyl group, and the like, and n represents an integer of 1-5 useful as an active ingredient in a herbicide and a noxious arthropod controlling agent.Type: GrantFiled: December 26, 2011Date of Patent: May 12, 2015Assignee: Sumitomo Chemical Company, LimitedInventors: Takashi Kuragano, Shin-ichiro Souma, Yoshinobu Jin, Tomohiro Araki
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Patent number: 8961937Abstract: The present invention relates to a composition for detecting beta amyloid aggregates and a composition for diagnosing beta amyloid aggregation disease, comprising a 2-styrilpyridizine-3(2H)-one derivative or its pharmaceutically acceptable salt, to a diagnostic kit for diagnosing beta amyloid aggregation disease comprising said composition and to a method for detecting beta amyloid aggregates using said compositions to provide information for beta amyloid aggregation disease diagnosis.Type: GrantFiled: March 13, 2013Date of Patent: February 24, 2015Assignee: Korea Atomic Energy Research InstituteInventors: Yong Dae Park, Jeong Hoon Park, Yong Jin Yoon, Seung Tae Yang, Min Goo Hur
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Patent number: 8927549Abstract: Embodiments of the present invention provide adamantyl benzamide derivatives and pharmaceutical compositions comprising adamantyl benzamide derivatives. Methods of use of such compounds and compositions to modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) in a subject are also provided.Type: GrantFiled: November 17, 2009Date of Patent: January 6, 2015Assignee: High Point Pharmaceuticals, LLCInventors: Dharma Rao Polisetti, Suparna Gupta, Soren Ebdrup
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Publication number: 20140364606Abstract: Phosphodiesterase 4 inhibitors without vomiting of the present invention are compounds or prodrugs or solvates represented by formula (I) wherein R1 is an independent methoxy, bromine and substituted aryl; X is an optionally substituted six-membered heterocyclic ring; Y is —(CH2)n—, —NH(CH2)n—, and —NH(CH2)n—O—, wherein n is any value among 0, 1, 2 and 3; Z is an optionally substituted aromatic ring or an optionally substituted heteroaromatic ring. Phosphodiesterase 4 inhibitor without vomiting of the present invention are novel biphenyl series PDE4D inhibitors, and can be applied to treat depression and Alzheimer's disease, improve cognitive ability and avoid vomiting.Type: ApplicationFiled: August 25, 2012Publication date: December 11, 2014Applicant: Ningo Tiangsheg Patent AttorneysInventors: Jiangping Xu, Zhongzhen Zhou
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Patent number: 8765762Abstract: Compounds, compositions and methods for the treatment of retinal degenerative diseases, such as retinitis pigmentosa, Leber's congenital Amaurosis, Syndromic retinal degenerations, age-related macular degeneration and Usher Syndrome, and hearing loss associated with Usher Syndrome are described herein.Type: GrantFiled: March 8, 2013Date of Patent: July 1, 2014Assignee: Usher III, Initiative, Inc.Inventors: Roland Werner Bürli, William Rameshchandra Krishna Esmieu, Christopher James Lock, Karine Fabienne Malagu, Andrew Pate Owens, William E. Harte
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Publication number: 20140134109Abstract: The present invention relates to a composition for detecting beta amyloid aggregates and a composition for diagnosing beta amyloid aggregation disease, comprising a 2-styrilpyridizine-3(2H)-one derivative or its pharmaceutically acceptable salt, to a diagnostic kit for diagnosing beta amyloid aggregation disease comprising said composition and to a method for detecting beta amyloid aggregates using said compositions to provide information for beta amyloid aggregation disease diagnosis.Type: ApplicationFiled: March 13, 2013Publication date: May 15, 2014Inventors: Yong Dae PARK, Jeong Hoon PARK, Yong Jin YOON, Seung Tae YANG, Min Goo HUR
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Patent number: 8658644Abstract: The present invention relates to novel pyridazine derivatives of formula (I) wherein R1 is methyl or ethyl; R2 is H or chloro; R3 is fluoro or chloro; R4 is fluoro or methoxy; and R5 is chloro or methoxy or an agrochemically usable salt from thereof, as active ingredients which have microbiodidal activity, in particular fungicidal activity.Type: GrantFiled: February 1, 2011Date of Patent: February 25, 2014Assignee: Syngenta Crop Protection, LLCInventors: Stephan Trah, Clemens Lamberth
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Publication number: 20130227798Abstract: Tanned leather, skin or pelt is produced by non-metal tanning, comprising the step of tanning a bated hide, skin or pelt with a tanning agent (A), the tanning agent (A) being a sulpho-group— containing dichloro-diazine selected from compounds of formula (I) of formula (II) and of formula (III) and mixtures of two or more thereof, wherein R1 signifies hydrogen, methyl, methoxy, benzoyl, naphthoyl, mono- or di(C1-4-alkyl)aminocarbonyl, C1-8-alkoxy-carbonyl or oxy-mono- or oligo-(C2-3-alkyleneoxy)-carbonyl R2-(SO3M)n signifies a radical of formula R3 signifies hydrogen, C1-8-alkyl or C1-8-alkoxy, m is 1 or 2, n is 1 or 2 and M signifies hydrogen or an alkali metal cation or an ammonium cation, the ammonium cation being a protonated tertiary amine or a quaternary ammonium cation, in a tanning bath, the tanning bath having a pH of from 6 to 10 at the beginning of tanning step.Type: ApplicationFiled: October 25, 2011Publication date: September 5, 2013Applicant: CLARIANT FINANCE (BVI) LIMITEDInventors: Claus Reineking, Roberta Gamarino, Licia Trimarco, Maurizio Quaglierini, Markus Gisler, Rainer Nusser
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Patent number: 8481537Abstract: The present invention relates to a pyridazinone derivative which can be used as a caspase inhibitor, process for the preparation thereof, and pharmaceutical composition for inhibiting caspase comprising the same.Type: GrantFiled: July 27, 2007Date of Patent: July 9, 2013Assignee: LG Life Sciences Ltd.Inventors: Hye Kyung Chang, Yeong Soo Oh, Yong Jin Jang
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Publication number: 20130131062Abstract: The present invention is directed to pyridazinone compounds of formula (I) and furan compounds of formula (II), pharmaceutical compositions of compounds of formula (I) and (II), kits containing these compounds, methods of syntheses, and a method of treatment of a proliferative disease in a subject by administration of a therapeutically effective amount of a compound of formulae (I) or (II). Both classes of compounds were identified through screening of a collection of small molecule libraries.Type: ApplicationFiled: December 21, 2007Publication date: May 23, 2013Inventors: Hakim Djaballah, Harold E. Varmus, David Shum, Romel Somwar, Alexander Chucholowski, Mohan Santhanam Thiruvazhi
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Publication number: 20130059848Abstract: The present specification discloses cannabinoid-2 agonists, compositions comprising such cannabinoid-2 agonists, and methods of treating an individual suffering from a disease by administering compositions comprising such cannabinoid-2 agonists.Type: ApplicationFiled: February 7, 2011Publication date: March 7, 2013Applicant: ALLERGAN, INCInventors: June Chen, Simon Pettit, Hans Flirl
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Patent number: 8269000Abstract: Substituted pyrimidine and triazine compounds corresponding to formula I wherein R1, R2, R3, R4a, R4b, R5a, R5b, R7, R8, R9a, R9b, R10, R11, A, a, b, s, t, V, W1, W2 and W3 have defined meanings, pharmaceutical compositions comprising such compounds, a process for preparing such compounds, and the use of such compounds and compositions to treat or inhibit pain and/or other disorders or disease states.Type: GrantFiled: October 23, 2009Date of Patent: September 18, 2012Assignee: Gruenenthal GmbHInventors: Stefan Schunk, Melanie Reich, Kamila Hennig, Michael Engels, Tieno Germann, Ruth Jostock, Sabine Hees
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Patent number: 8129388Abstract: The present invention discloses compounds of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Phenylene Compound”); compositions comprising an effective amount of a Phenylene Compound; and methods for treating pain and other conditions in an animal comprising administering to an animal in need thereof an effective amount of a Phenylene Compound.Type: GrantFiled: June 10, 2011Date of Patent: March 6, 2012Assignee: Purde Pharma L.P.Inventor: Qun Sun
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Patent number: 8080551Abstract: HIV replication inhibitors having formula (I) defined herein are disclosed. Pharmaceutical compositions containing the HIV replication inhibitors; the use of the HIV replication inhibitors in the treatment of HIV; and processes for preparing the HIV replication inhibitors are also disclosed.Type: GrantFiled: June 26, 2006Date of Patent: December 20, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: Jérôme Emile Georges Guillemont, Patrice Palandijian, Marc René De Jonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desiré Daeyaert, Jan Heeres, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts, legal representative
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Patent number: 8076477Abstract: Use of an affinity adsorbent for the separation, removal, isolation, purification, characterisation, identification or quantification of a proteinaceous material, wherein the affinity adsorbent is a compound of formula (III), wherein R1 is H, alkyl, aryl, hydroxyalkyl, cyciohexyl, amino or a heterocyclic group which is optionally substituted with one or more of alkyl, aryl, alkoxy, aryloxy, acyloxy, acylamino, amino, OH, CO2H, sulphonyl, carbamoyl, sulphamoyl, alkylsuiphonyl and halogen; one X is N and the other is N, C—Cl or C—CN; Y is O, S or NR2; Z is O, S or NR3; R2 and R3 are each H, alkyl, hydroxyalkyl, benzyl or ?-phenylethyl; Q is benzene, naphthalene, benzthiazole, benzoxazole, 1-phenylpyrazole, indazoie or benzimidazoie; R4, R5 and R6 are each H, OH, alkyl, aryl, heterocyclic, alkoxy, aryloxy, amino, acyloxy, acylamino, CO2H, sulphonic acid, carbamoyl, suiphamoyl, alkylsulphonyl or halogen, or two or more of R4, R5 and R6 are linked to form a cyclic structure; U and V are the same or different C1-10Type: GrantFiled: March 2, 2007Date of Patent: December 13, 2011Assignee: ProMetic BioSciences Ltd.Inventors: Jason Richard Betley, Helen Tatton, Kelly Le Riche, Matthew Webb
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Publication number: 20110224244Abstract: Embodiments of the present invention provide adamantyl benzamide derivtives and pharmaceutical compositions comprising adamantyl benzamide derivatives. Methods of use of such compounds and compositions to modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) in a subject are also provided.Type: ApplicationFiled: November 17, 2009Publication date: September 15, 2011Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Dharma Rao Polisetti, Suparna Gupta, Soren Ebdrup
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Publication number: 20110183981Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, W, X and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: March 30, 2011Publication date: July 28, 2011Applicant: ARRAY BIOPHARMA INC.Inventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, James Blake
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Patent number: 7968711Abstract: The present invention provides a method of treating glaucoma or ocular hypertension which comprises applying to the eye of a person in need thereof an amount sufficient to treat glaucoma or ocular hypertension of a compound of formula I wherein Y, Q, Z, R, R1 and R2 are as defined in the specification. The present invention further comprises pharmaceutical compositions, e.g. ophthalmic compositions, including said compound.Type: GrantFiled: April 24, 2007Date of Patent: June 28, 2011Assignee: Allergan, Inc.Inventors: June Chen, Simon N. Pettit, Hans G. Fliri
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Publication number: 20110082153Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).Type: ApplicationFiled: September 4, 2008Publication date: April 7, 2011Inventors: Robert G. Aslanian, Xianhai Huang, Anandan Palani, JUn Qin, Wei Zhou, Xiaohong Zhu, Robert Mazzola, Pawan Dhondi, William J. Greenlee
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Publication number: 20100286390Abstract: Novel pyridazinone compounds of formula (I), which inhibit the purinergic P2X7 receptor and are useful for prevention, therapy and improvement of inflammatory and immunological diseases.Type: ApplicationFiled: October 30, 2008Publication date: November 11, 2010Inventors: Yukihiro Shigeta, Yutaka Hirokawa, Hiroshi Nagai, Kei Nagae, Tsuneo Watanabe, Megumi Io, Yusuke Shintani, Junji Kamon, Masato Horikawa, Kazuya Takeuchi
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Patent number: 7825119Abstract: A subject of the invention is the compounds of formula (I): in which R1, R2, R3, R4 and R have the meanings indicated in the description, their preparation process, their use as medicaments having an antagonist activity on the vitronectin receptor and the pharmaceutical compositions containing them.Type: GrantFiled: May 13, 2005Date of Patent: November 2, 2010Assignee: Galapagos SASInventors: Jean-Michel Lefrancois, Bertrand Heckmann
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Publication number: 20100210649Abstract: The present invention is directed to pyridazinone compounds of formula (I) and furan compounds of formula (II), pharmaceutical compositions of compounds of formula (I) and (II), kits containing these compounds, methods of syntheses, and a method of treatment of a proliferative disease in a subject by administration of a therapeutically effective amount of a compound of formulae (I) or (II). Both classes of compounds were identified through screening of a collection of small molecule libraries.Type: ApplicationFiled: December 21, 2007Publication date: August 19, 2010Applicant: Sloan-Kettering Institute for Cancer ResearchInventors: Hakim Djaballah, Harold E. Varmus, David Shum, Romel Somwar, Alexander Chucholowski, Mohan Santhanam Thiruvazhi
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Patent number: 7723362Abstract: The invention relates to compounds of formula wherein Het, A1, A2, A3, A4, D, W, T, Q, Y, X1, X2, R1, R2, R3, R4, k and m are as defined hereinabove, and, where applicable, to possible E/Z isomers, mixtures of E/Z isomers and/or tautomers thereof, in each case in free form or in salt form, to a process for the preparation of and to the use of those compounds, E/Z isomers, mixtures of E/Z isomers and/or tautomers, to pesticidal compositions in which the active ingredient has been selected from those compounds, E/Z isomers, mixtures of E/Z isomers and/or tautomers, in each case in free form or in agrochemically usable salt form, to a process for the preparation of and to the use of those compositions, to plant propagation material treated with those compositions, to a method of controlling pests, to intermediates and, where applicable, to possible E/Z isomers, mixtures of E/Z isomers and/or tautomers thereof, in each case in free form or in salt form, for the preparation of those compounds, E/Z isomers, mType: GrantFiled: January 7, 2005Date of Patent: May 25, 2010Assignee: Syngenta Crop Protection, Inc.Inventors: Roger Graham Hall, Stephan Trah, Werner Zambach, Juraj Tuleja
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Publication number: 20100113457Abstract: The present invention relates to novel pyridazine derivatives of formula (I) as active ingredients which have microbiocidal activity, in particular fungicidal activity: wherein R1 is hydrogen, C1-C6alkyl, C1-C6haloalkyl or C3-C6cycloalkyl; R2 is halogen, nitro, cyano, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy, C1-C4alkylthio or C1-C4haloalkylthio; R3 is an optionally substituted aryl; R4 is fluoro, cyano, C1-C6haloalkyl, C3-C6cycloalkyl, C1-C6haloalkoxy, C1-C6alkylthio or C1-C6haloalkylthio; and n is a whole number from 1 to 4; or an agrochemically usable salt form thereof.Type: ApplicationFiled: October 23, 2007Publication date: May 6, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Stephan Trah, Clemens Lamberth, Sebastian Wendeborn
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Patent number: 7642303Abstract: Thermoplastic composition and articles containing UV absorbers that protect the articles contents from harmful UV radiation are disclosed as well as methods for making the thermoplastic articles and methods for using the articles to contain and protect materials sensitive to UV radiation. The UV absorbers contain oxazolone and/or azine functional groups that absorb UV radiation and prevent its transmission into the article. Many of the compounds are novel compositions of matter. The generally clear thermoplastic articles of this disclosure are particularly useful for containing a variety of UV sensitive consumer products that would otherwise have to be packaged in opaque containers.Type: GrantFiled: October 13, 2005Date of Patent: January 5, 2010Inventors: Thomas L. Shakely, James John Krutak
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Patent number: 7511149Abstract: Insecticidal sulfoximines are produced efficiently and in high yield by the oxidation of the corresponding sulfilimine with ruthenium tetraoxide or an alkali metal permanganate.Type: GrantFiled: February 9, 2007Date of Patent: March 31, 2009Assignee: Dow AgroSciences LLCInventors: Kim E. Arndt, Douglas C. Bland, David E. Podhorez, James R. McConnell
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Patent number: 7465736Abstract: An azole derivative of formula (I) a medicament that contains the azole derivative of formula (I), a method of treating a disease with the azole derivative of formula (I), and a method of preparing the azole derivative of formula (I).Type: GrantFiled: June 13, 2003Date of Patent: December 16, 2008Assignee: Laboratoires Serono S.A.Inventors: Pascale Gaillard, Jean-Pierre Gotteland, Isabelle Jeanclaude-Etter, Matthias Schwarz, Russel J. Thomas
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Publication number: 20080287434Abstract: The invention relates to a compound of the general formula (I), as defined herein which is useful for the treatment of a pathology in a patient wherein a CCR3 receptor plays a role in the development of the pathology, and pharmaceutical preparations containing such compound. The invention is also directed to a process for preparing the compound of the general formula (I), and intermediate useful in the preparation.Type: ApplicationFiled: March 19, 2008Publication date: November 20, 2008Applicant: SANOFI-AVENTISInventors: Agnes PAPPNE BEHR, Zoltan KAPUI, Peter ARANYI, Sandor BATORI, Veronika BARTANE BODOR, Lajos T. NAGY, Mihalyne T. Santa, Marton VARGA, Gyorgy FERENCZY, Endre MIKUS, Katalin URBAN-SZABO, Judit VARGANE SZEREDI, Erzsebet WALCZ, Edit SUSAN
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Publication number: 20080167461Abstract: A process for preparing 3,6-dichloropyridazine-1-oxide which comprises reacting 3,6-dichloropyridazine with an acid anhydride and hydrogen peroxide of a concentration of 60% or less or a urea hydrogen peroxide addition compound.Type: ApplicationFiled: March 20, 2006Publication date: July 10, 2008Applicant: SANKYO AGRO COMPANY, LIMITEDInventors: Yoshihisa Tsukamoto, Noriaki Kudo, Toshio Kaneko, Hiroyuki Komai
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Patent number: 7115591Abstract: The present invention describes pyridazinone compounds of formula I which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX-2), COX-2 is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1) which is an important “housekeeping” enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectivity of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with currently markered non-steroidal anti-inflammatory drugs (NSAIDs).Type: GrantFiled: June 19, 2003Date of Patent: October 3, 2006Assignee: Abbott LaboratoriesInventors: Lawrence A. Black, Anwer Basha, Teodozyj Kolasa, Michael E. Kort, Huaqing Liu, Catherine M. McCarty, Meena Patel, Jeffrey J. Rohde, Michael J. Coghlan, Andrew O. Stewart
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Patent number: 7026307Abstract: The present invention relates to a process for the preparation of compounds of the formula (I) by reacting compounds of the formula (II) in which R1, R2, R4 and Het are as defined in the description, with anhydrous hydrogen halide in the presence of a nitrile.Type: GrantFiled: April 24, 2002Date of Patent: April 11, 2006Assignee: Bayer CropScience AGInventors: Jörn Stölting, Kai van Laak, Wolfram Sirges, Armin Heyn, Torsten Taschner
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Patent number: 7012041Abstract: The invention relates to novel phenylpyridazinones of the general formula (I) in which R1, R2, R3, R4, R5 and R6 are each as defined in the description, to processes for their preparation, to their use as herbicides and to novel intermediates and processes for preparing them.Type: GrantFiled: September 30, 2002Date of Patent: March 14, 2006Assignee: Bayer AGInventors: Karl-Heinz Linker, Kurt Findeisen, Wilhelm Haas, Markus Dollinger, Hans-Joachim Santel
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Patent number: 6995261Abstract: Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: wherein R1 is a halogen, or an oxygen linked leaving group including an aromatic ether, an alkyl sulfonate, an aryl sulfonate, an alkyl phosphonate, an aryl phosphonate, an alkyl phosphate or aryl phosphate; R2 is COOR5, C(?O)NH(CHR5)m—COOR5, NH(CHR5)mCON(R5)R6, C(?O)N(R5)R6 or NH(CHR5)mOH; R3 is H or alkyl; R4 is H, substituted or unsubstituted aryl, heteroaryl or alkyl; R5 and R6 are independently H, lower alkyl, aryl, hydroxy alkyl, amino alkyl, heteroaryl, lower alkylene-aryl, lower alkylene-heteroaryl or lower cycloalkyl; and m=0–6; pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1? protease activity in a mammal utilizing the compounds and compositions.Type: GrantFiled: September 22, 2003Date of Patent: February 7, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: Roland E. Dolle, Denton W. Hoyer, Tina Morgan Ross, James M. Rinker, Stanley J. Schmidt, Mark A. Ator
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Patent number: 6828276Abstract: There are described benzoylcyclohexanediones of the formula I, their preparation, and their use as herbicides and plant growth regulators. In this formula (I), C1, C2, C3 are cyclic radicals, X1 is a hetero atom, X2 is a chain of carbon atoms, L is a chain-like element, R1, R2, R3, R4, R5 are various radicals, and Y and Z are monoatomic bridge elements.Type: GrantFiled: August 30, 2001Date of Patent: December 7, 2004Assignee: Aventis CropScience GmbHInventors: Thomas Seitz, Andreas van Almsick, Lothar Willms, Hermann Bieringer, Thomas Auler, Hubert Menne
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Patent number: 6800758Abstract: The invention relates to novel processes for the preparation of 5-chloro-4-{3-[N-[2-(3,4-dimethoxyphenyl)-ethyl]-N-methylamino]-propylamino-3(2H) pyridazinone of formula (I) and the pharmaceutically acceptable acid addition salts thereof. An important feature of the invention is using 3,4,5-trichloropyridazone as starting substance of the synthesis.Type: GrantFiled: February 9, 2001Date of Patent: October 5, 2004Assignee: Egis Gyogyszergyar Rt.Inventors: Peter Kótay Nagy, Gyula Simig, József Barkóczy, Ilona Sztruhár, László Balázs, Imre Domán, Zoltán Greff, Zoltán Rátkai, Peter Seres, Támas Karancsi
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Patent number: 6653321Abstract: Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptable salts, are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.Type: GrantFiled: July 28, 2000Date of Patent: November 25, 2003Assignee: Telik, Inc.Inventors: Wayne R. Spevak, Songyuan Shi, Prasad V. V. S. V. Manchem, Michael R. Kozlowski, Steven R. Schow, Robert T. Lum, Louise Robinson, Jeong Weon Park
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Publication number: 20030171309Abstract: The present invention is related to new substituted pyrrolidine derivatives of formula (I). Said compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula (I) are useful in the treatment and/or prevention of neurodegenerative disorders, diseases associated with polygultamine tracts, epilepsy, ischemia, infertility, cardiovascular disorders renal hypoxia, hepatitis and AIDS. Said pyrrolidine derivatives display a modulatory and most notably a down-regulating-up to an inhibitory-activity with respect to the cellular death agonist Bax and/or the activation pathways leading to Bax and allows therefore to block the release of cytochrome (c).Type: ApplicationFiled: April 28, 2003Publication date: September 11, 2003Inventors: Serge Halazy, Anna Quattropani, Agnes Bombrun, Mattias Schwarz, Russel Thomas, Anthony Baxter
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Patent number: 6551963Abstract: The invention relates to novel phenylpyridazinones of the general formula (I) in which R1, R2, R3, R4, R5 and R6 are each as defined in the description, to processes for their preparation, to their use as herbicides and to novel intermediates and processes for preparing them.Type: GrantFiled: November 26, 1997Date of Patent: April 22, 2003Assignee: Bayer AktiengesellschaftInventors: Karl-Heinz Linker, Kurt Findeisen, Wilhelm Haas, Markus Dollinger, Hans-Joachim Santel
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Patent number: 6538135Abstract: In a process for preparing 4-amino-5-chloro-1-phenylpyridazin-6-one by reacting 4,5-dichloro-1-phenylpyridazin-6-one with aqueous ammonia in the presence of a catalyst, the catalyst used is soluble in the aqueous alkaline reaction medium but is essentially insoluble in the reaction medium which has been acidified after removal of the 4-amino-5-chloro-1-phenylpyridazin-6-one. The process of the present invention makes it possible for the catalyst to be recovered and reused in a simple manner.Type: GrantFiled: September 28, 2001Date of Patent: March 25, 2003Assignee: BASF AktiengesellschaftInventors: Hans Rupert Merkle, Klaus Herbig, Erich Fretschner, Helmut Fröhlich
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Patent number: 6525053Abstract: The present invention describes pyridazione compounds having the formula (I), which are cyclooxygenase (COX) inhibitors The compounds are selective inhibitors of cyclooxygenase-2-(COX-2), which is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1), which is an important “housekeeping” enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectivity of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with currently marketed non-steroidal anti-inflammatory drugs (NSAIDS).Type: GrantFiled: August 20, 1998Date of Patent: February 25, 2003Assignee: Abbott LaboratoriesInventor: Lawrence A. Black
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Patent number: 6492363Abstract: Phenylamino benzoic acid, benzamides, and benzyl alcohol derivatives of the formula where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, and Z is COOR7, tetrazolyl, CONR6R7, or CH2OR7, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as inflammation, psoriasis and restenosis, as well as stroke, heart failure, and immunodeficiency disorders.Type: GrantFiled: August 16, 2001Date of Patent: December 10, 2002Assignee: Warner-Lambert CompanyInventors: Stephen Douglas Barrett, Alexander James Bridges, Donna Reynolds Cody, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Mel Conrad Schroeder, Haile Tecle
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Patent number: 6475955Abstract: This invention provides pyridazinone derivatives encompassed by the following the formula: wherein, R1, R2, R3, R4, R5 and R7 represent a hydrogen atom and the like, and R6 represents a C1-C3 alkyl and the like. The pyridazinone derivatives have excellent herbicidal activity, therefore, they can be used as an active ingredient for herbicidal compositions and can be utilized in herbicidal method, which are also described.Type: GrantFiled: December 11, 2000Date of Patent: November 5, 2002Assignee: Sumitomo Chemical Company, LimitedInventor: Takashi Komori
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Patent number: 6399774Abstract: Compounds having Formula 1 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.Type: GrantFiled: April 9, 2001Date of Patent: June 4, 2002Assignee: Allergen Sales, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Dehua Huang, Roshantha A. Chandraratna
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Patent number: 6376492Abstract: The present invention is directed to compounds, compositions and methods of inhibiting and treating HIV and related viruses, and methods for cocrystallizing reverse transcriptase in vitro, inhibition of the replication of HIV and related viruses thereof.Type: GrantFiled: May 9, 2000Date of Patent: April 23, 2002Assignee: Medivir ABInventors: Peter Thomas Lind, Rolf Noréen, John Michael Morin, Robert John Ternansky
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Patent number: 6307047Abstract: The present invention describes pyridazinone compounds of formula I which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX-2). COX-2 is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1) which is an important “housekeeping” enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectivity of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with currently marketed non-steroidal anti-inflammatory drugs (NSAIDs).Type: GrantFiled: October 27, 1999Date of Patent: October 23, 2001Assignee: Abbott LaboratoriesInventors: Lawrence A. Black, Anwer Basha, Teodozyj Kolasa, Michael E. Kort, Huaqing Liu, Catherine M. McCarty, Meena Patel, Jeffrey J. Rohde, Michael J. Coghlan, Andrew O. Stewart
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Publication number: 20010007867Abstract: This invention relates to compounds of the formula 1Type: ApplicationFiled: December 13, 1999Publication date: July 12, 2001Inventor: YUHPYNG L. CHEN
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Patent number: 6258751Abstract: The present invention relates to novel heterocyclic compounds and their agronomically suitable salts, methods for the use of these compounds in controlling unwanted plant species, and the use of herbicidal compositions containing these compounds. In particular, the present invention pertains to substituted and unsubstituted triazoles, imidazoles and pyrazoles linked to a heterocyclic substituted benzene group. Such compounds are useful as pre-emergent and post-emergent herbicides.Type: GrantFiled: June 13, 2000Date of Patent: July 10, 2001Assignee: Rohm and Haas CompanyInventors: Richard Martin Jacobson, Mark Joseph Mulvihill, Changling Liu, Xiaonan Liu
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Patent number: 6194575Abstract: The present invention relates to a process for the preparation of compounds of the formula (I) by reacting compounds of the formula (II) in which Het, R1, R2 and R4 are as defined in the description, with urea.Type: GrantFiled: September 21, 1999Date of Patent: February 27, 2001Assignee: Bayer AktiengesellschaftInventors: Detlef Wollweber, Wolfgang Krämer, Eric Rivadeneira
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Patent number: 6191149Abstract: A pharmaceutical composition comprising a compound of the following general formula [I] or its salt. wherein R1 represents aryl or a heteroaromatic group. R2 represents hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, hydroxyalkyl, haloalkyl, alkoxy, alkylthio, amino, monoalkylamino, dialkylamino, or phenyl. R3 and R4 independently represent hydrogen or alkyl or R3 and R4 taken together with the adjacent N atom represent a 5- through 7-membered cyclic amino group. A represents a single bond C2-10 alkylene. W represents O, S, or (CH2)n (where CH may be substituted by alkyl; n is an integer of 1 or 2). X, Y, and Z may be the same or different and each represents CH (which may be substituted by alkyl), or N. Provided, however, that the case in which X, Y, and Z concurrently represent CH is excluded. The compound of the invention has excellent neuronal death inhibitory activity and is useful as a therapeutic drug for cerebrovascular diseases.Type: GrantFiled: June 16, 1999Date of Patent: February 20, 2001Assignee: Nippon Shinyaku, Co., Ltd.Inventors: Shoichi Chokai, Yojiro Ukai, Tomiyoshi Aoki, Kyoichi Ideguchi