Chalcogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/370.4)
  • Patent number: 8969589
    Abstract: The present invention provides a compound that is represented by the following general formula wherein R1, R2, R4, R5, R6, R7, X, W, X and Y are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, TP and/or EP4 receptor mediated diseases or conditions.
    Type: Grant
    Filed: December 19, 2012
    Date of Patent: March 3, 2015
    Assignee: Allergan, Inc.
    Inventors: Jussi J. Kangasmetsa, William R. Carling, Jose L. Martos, Jenny W. Wang, David F. Woodward
  • Patent number: 8889727
    Abstract: An anti-fungal agent for tinea comprising as active ingredient a compound having the skeleton of 2-(1H-pyrazol-1-yl)phenol represented by the following formula (I) or (II) or a salt thereof is provided
    Type: Grant
    Filed: January 30, 2012
    Date of Patent: November 18, 2014
    Assignee: Meiji Seika Pharma Co., Ltd.
    Inventors: Makoto Ohyama, Yuji Tabata, Maiko Iida, Kaori Kaneda, Sho Takahata
  • Patent number: 8754115
    Abstract: Disclosed are compounds of Formula 1 and Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein Q1, Q2, R1, R2, R4, R5 and X are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 or Formula 1A and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: June 17, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: Jeffrey Keith Long, Paula Louise Sharpe, Amy X Ding
  • Publication number: 20140105839
    Abstract: The present invention relates to a compound of the following formula (I): as well as its process of preparation, pharmaceutical and cosmetics composition comprising it and use thereof, notably as an inhibitor of the sodium-dependent glucose co-transporter, such as SGLT1, SGLT2 and SGLT3, in particular in the treatment or prevention of diabetes, and more particularly type-II diabetes, diabetes-related complications, such as arthritis of the lower extremities, cardiac infarction, renal insufficiency, neuropathy or blindness, hyperglycemia, hyperinsulinemia, obesity, hypertriglyceridemia, X syndrome and arteriosclerosis, as well as for its use as an anticancer, anti-infective, anti-viral, anti-thrombotic or anti-inflammatory drug, or for lightening, bleaching, depigmenting the skin, removing blemishes from the skin, particularly age spots and freckles, or preventing pigmentation of the skin.
    Type: Application
    Filed: May 29, 2012
    Publication date: April 17, 2014
    Applicant: TF-CHEM
    Inventors: Geraldine Deliencourt-Godefroy, Lenaig Lopes
  • Patent number: 8598078
    Abstract: 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: Grant
    Filed: August 21, 2008
    Date of Patent: December 3, 2013
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Olivier Loiseleur, Roger Graham Hall, André Denis Stoller, Gerald Wayne Craig, André Jeanguenat, Andrew Edmunds
  • Publication number: 20130317074
    Abstract: An anti-fungal agent for tinea comprising as active ingredient a compound having the skeleton of 2-(1H-pyrazol-1-yl)phenol represented by the following formula (I) or (II) or a salt thereof is provided
    Type: Application
    Filed: January 30, 2012
    Publication date: November 28, 2013
    Inventors: Makoto Ohyama, Yuji Tabata, Maiko Iida, Kaori Kaneda, Sho Takahata
  • Publication number: 20130165665
    Abstract: The present invention provides a compound that is represented by the following general formula wherein R1, R2, R4, R5, R6, R7, X, W, X and Y are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, TP and/or EP4 receptor mediated diseases or conditions.
    Type: Application
    Filed: December 19, 2012
    Publication date: June 27, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Patent number: 8466089
    Abstract: The present invention provides a novel herbicide showing excellent herbicidal effects, which has a wide application range including agricultural fields and non-agricultural fields and various application methods including soil treatment and foliage treatment. A pyrazole compound represented by the formula (I) or its salt: wherein R1 is alkyl, R2 is a hydrogen atom or alkyl, R3 is alkyl, R4 is alkyl, R5 is alkyl substituted by one alkoxy, alkoxy substituted by one alkoxy, or alkoxycarbonyl, R6 is alkylsulfonyl, A is alkylene substituted by at least one alkyl; a process for its production; a herbicide containing it as an active ingredient; and a method for controlling undesired plants or inhibiting their growth, which comprises applying a herbicidally effective amount thereof to the undesired plants or to a place where they grow.
    Type: Grant
    Filed: May 19, 2009
    Date of Patent: June 18, 2013
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Masamitsu Tsukamoto, Hiroshi Kikugawa, Souichiro Nagayama, Tatsuya Okita, Hiroshi Hata
  • Publication number: 20130143940
    Abstract: Disclosed are compounds of Formula 1 and Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein Q1, Q2, R1, R2, R4, R5 and X are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 or Formula 1A and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: August 31, 2011
    Publication date: June 6, 2013
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: Jeffrey Keith Long, Mary Ann Hanagan, Eric Allen Marshall, Paula Louise Sharpe, Amy X. Ding
  • Patent number: 8378118
    Abstract: The present invention discloses a novel thyroid like compounds of formula (I), wherein R1 R2, R3, R4 and Z are as defined in the specification, method for its preparation, composition containing such compounds and use of such compounds and composition as medicament. Further, compounds of formula (I) has significantly low binding affinity to thyroid receptors and thus considerably devoid of thyrotoxic effects. The invention also relates to the use of the compound of formula (I) for the preparation of a medicament for treating various disease conditions such as obesity, dyslipidemia, metabolic syndrome and co-morbidities associated with metabolic syndrome.
    Type: Grant
    Filed: January 10, 2012
    Date of Patent: February 19, 2013
    Assignee: Torrent Pharmaceuticals Ltd.
    Inventors: Laxmikant Chhipa, Shitalkumar Pukharaj Zambad, Ramesh Gupta, Davinder Tuli, Ashok Kasundra, Siralee Munshi, M. Amir Siddiqui, Subrat Kumar Bhattamisra, C. Dutt, Vijay Chauthaiwale
  • Publication number: 20120238581
    Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt, prodrug, salt of a prodrug, or a combination thereof. Pharmaceutical compositions of formula (I) and related methods for treating or preventing metabolic diseases or conditions.
    Type: Application
    Filed: May 31, 2012
    Publication date: September 20, 2012
    Inventors: Andrew J. Souers, Ju Gao, Todd M. Hasen, Rajesh R. Iyengar, Philip R. Kym, Bo Liu, Zhonghua Pei, Vince S. Yeh, Gang Zhao, Zhili Xin
  • Publication number: 20120202816
    Abstract: The present invention discloses a novel thyroid like compounds of formula (I), wherein R1 R2, R3, R4 and Z are as defined in the specification, method for its preparation, composition containing such compounds and use of such compounds and composition as medicament. Further, compounds of formula (I) has significantly low binding affinity to thyroid receptors and thus considerably devoid of thyrotoxic effects. The invention also relates to the use of the compound of formula (I) for the preparation of a medicament for treating various disease conditions such as obesity, dyslipidemia, metabolic syndrome and co-morbidities associated with metabolic syndrome.
    Type: Application
    Filed: January 10, 2012
    Publication date: August 9, 2012
    Applicant: Torrent Pharmaceuticals, Ltd.
    Inventors: Laxmikant Chhipa, Shitalkumar Pukharaj Zambad, Ramesh Gupta, Davinder Tuli, Ashok Kasundra, Siralee Munshi, M. Amir Siddiqui, Subrat Kumar Bhattamisra, C. Dutt, Vijay Chauthaiwale
  • Publication number: 20120122780
    Abstract: Described herein are compounds useful in the reduction of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: May 20, 2010
    Publication date: May 17, 2012
    Applicant: Ardea Biosciences Inc.
    Inventors: Martha De La Rosa, Jean-Luc Girardet
  • Patent number: 8143424
    Abstract: A novel thyroid like compounds of formula (I), wherein R1, R2, R3, R4 and Z are as defined in the specification, method for its preparation, composition and use thereof. Further, compounds of formula (I) has significantly low binding affinity to thyroid receptors and thus considerably devoid of thyrotoxic effects. The invention also relates to the use of the compound of formula (I) for the preparation of a medicament for treating various disease conditions including obesity, dyslipidemia, metabolic syndrome and co-morbidities associated with metabolic syndrome.
    Type: Grant
    Filed: June 2, 2008
    Date of Patent: March 27, 2012
    Assignee: Torrent Pharmaceuticals Ltd.
    Inventors: Laxmikant Chhipa, Shitalkumar Pukharaj Zambad, Ramesh Gupta, Davinder Tuli, Ashok Kasundra, Siralee Munshi, M. Amir Siddiqui, Subrat Kumar Bhattamisra, Chaitanya Dutt, Vijay Chauthaiwale
  • Publication number: 20120029192
    Abstract: This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivatives thereof, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such, the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).
    Type: Application
    Filed: October 7, 2011
    Publication date: February 2, 2012
    Inventors: Lyn Howard Jones, Charles Eric Mowbray, David Anthony Price, Matthew Duncan Selby, Paul Anthony Stupple
  • Patent number: 8093282
    Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein J1, U1, U2, B, Y, and A are as described. Methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: May 1, 2009
    Date of Patent: January 10, 2012
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Danny T. Dinh
  • Patent number: 8063044
    Abstract: This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereofs, wherein R1 to R4 are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodeficiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).
    Type: Grant
    Filed: August 25, 2008
    Date of Patent: November 22, 2011
    Assignee: Pfizer Inc.
    Inventors: Lyn Howard Jones, Charles Eric Mowbray, David Anthony Price, Matthew Duncan Selby, Paul Anthony Stupple
  • Publication number: 20110178149
    Abstract: The invention relates to ether compounds with nitrogen-containing 5-member heterocycle, represented by formula (I): The groups are as defined as specification. The compounds of the present invention have broad-spectrum insecticidal activities, and they are very effective to lepidopterous pests, including Ostrinia nubilalis, sugarcane borer, summer fruit tortrix moth, Grapholitha inopinata, Lymantria dispar, Cnaphalocrocis medialis, Pyrausta nubilalis, Heliothis assulta, Grapholitha molesta, Plutella xylostella, Laphygma exigua, Prodenialitura and the like, especially more effective to Plutella xylostella and Laphygma exigua, and can have very good effects at very low doses. And the compounds of present invention have high activities to homopteran pests such as aphid. At the same time, some compounds of present invention have very good fungicidal activities, and can be used for preventing wheat powdery mildew, cucumber downy mildew, vegetable grey mould and the like.
    Type: Application
    Filed: November 25, 2009
    Publication date: July 21, 2011
    Inventors: Changling Liu, Miao Li, Junfeng Wang, Jinbo Zhang
  • Publication number: 20110160062
    Abstract: The present invention provides a novel herbicide showing excellent herbicidal effects, which has a wide application range including agricultural fields and non-agricultural fields and various application methods including soil treatment and foliage treatment. A pyrazole compound represented by the formula (I) or its salt: wherein R1 is alkyl, R2 is a hydrogen atom or alkyl, R3 is alkyl, R4 is alkyl, R5 is alkyl substituted by one alkoxy, alkoxy substituted by one alkoxy, or alkoxycarbonyl, R6 is alkylsulfonyl, A is alkylene substituted by at least one alkyl; a process for its production; a herbicide containing it as an active ingredient; and a method for controlling undesired plants or inhibiting their growth, which comprises applying a herbicidally effective amount thereof to the undesired plants or to a place where they grow.
    Type: Application
    Filed: May 19, 2009
    Publication date: June 30, 2011
    Applicant: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Masamitsu Tsukamoto, Hiroshi Kikugawa, Souichiro Nagayama, Tatsuya Okita, Hiroshi Hata
  • Publication number: 20110152532
    Abstract: The present invention relates to a process for the preparation of 1-alkyl- or 1-aryl-substituted 5-pyrazolecarboxylic acid derivatives comprising the reaction of substituted 1,3-dioxolanes and 1,4-dioxanes with alkyl- or arylhydrazines to give 1-alkyl- or 1-aryl-substituted dihydro-1H-pyrazoles, and their further reaction to give 1-alkyl- or 1-aryl-substituted 5-pyrazolecarboxylic acid derivatives, which can be used as valuable intermediates for producing insecticidally effective anthranilamides.
    Type: Application
    Filed: December 15, 2010
    Publication date: June 23, 2011
    Applicant: Bayer CropScience AG
    Inventors: Sergii PAZENOK, Norbert Lui, Igor Gerus
  • Patent number: 7863312
    Abstract: The invention provides substituted pyrazolidinone compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing preterm labor, dysmenorrhea, asthma, hypertension, infertility or fertility disorder, undesired blood clotting, preeclampsia or eclampsia, an eosinophil disorder, sexual dysfunction, osteoporosis and other destructive bone disease or disorder, and other diseases and disorders associated with the prostaglandin EP2 and/or EP4 receptors.
    Type: Grant
    Filed: May 14, 2008
    Date of Patent: January 4, 2011
    Assignee: Merck Serono SA
    Inventors: Gian Luca Araldi, Yihua Liao, Adulla P. Reddy, Zhong Zhao
  • Publication number: 20100324091
    Abstract: A pyrazolone derivative represented by formula (I) below: wherein R1 to R3 are the same as defined in claims; or an optical isomer, a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof is provided. The novel pyrazolone derivative according to the present invention has a PAI-1 production inhibitory activity, a tissue fibrosis inhibitory activity, and a fibrolytic activity, and is effective for preventing and/or treating tissue fibrotic diseases (lung fibrosis, kidney fibrosis, etc.) and diseases of which a pathological thrombus becomes the cause, such as ischemic cardiac diseases (cardiac infarction and angina pectoris), atrial thrombus, lung embolism, deep thrombophlebitis, disseminated intravascular clotting, ischemic brain diseases (brain infarction, brain hemorrhage), and arterial sclerosis.
    Type: Application
    Filed: June 23, 2008
    Publication date: December 23, 2010
    Applicant: Kowa Company, Ltd.
    Inventors: Noriaki Gomi, Shinji Ina, Kenjirou Yamana, Yoshio Kaneko
  • Patent number: 7812175
    Abstract: The present invention relates to a process for producing a 5-alkoxy-4-hydroxymethylpyrazole compound represented by the general formula (3) which comprises reacting a pyrazole compound represented by the general formula (1) (wherein R1 is a substituent such as alkyl group, substituted or unsubstituted group or the like, and R2 is an electron withdrawing group) with a compound represented by the general formula (2) L-R3??(2) (wherein L is a leaving group and R3 is a substituent such as substituted or unsubstituted alkyl group or the like) in the presence of a base and formaldehyde.
    Type: Grant
    Filed: February 8, 2007
    Date of Patent: October 12, 2010
    Assignee: Ihara Chemical Industry Co., Ltd.
    Inventors: Yukio Uchida, Naoya Atsumi
  • Publication number: 20100189648
    Abstract: A hydrophobic binding pocket on ubiquitin-protein ligase E3 is described, and used in designing the inhibitors disrupting ubiquitin conjugating enzyme E2 and E3 interaction. Four types of inhibitors designed by using the binding pocket are provided, which can be used for cancer treatment.
    Type: Application
    Filed: November 1, 2007
    Publication date: July 29, 2010
    Inventors: Lan Huang, Li Xing
  • Publication number: 20100168110
    Abstract: The present invention discloses a novel thyroid like compounds of formula (I), wherein R1 R2, R3, R4 and Z are as defined in the specification, method for its preparation, composition containing such compounds and use of such compounds and composition as medicament. Further, compounds of formula (I) has significantly low binding affinity to thyroid receptors and thus considerably devoid of thyrotoxic effects. The invention also relates to the use of the compound of formula (I) for the preparation of a medicament for treating various disease conditions such as obesity, dyslipidemia, metabolic syndrome and co-morbidities associated with metabolic syndrome.
    Type: Application
    Filed: June 2, 2008
    Publication date: July 1, 2010
    Applicant: TORRENT PHARMACEUTICALS LTD.
    Inventors: Laxmikant Chhipa, Shitalkumar Zambad, Ramesh Gupta, Davinder Tuli, Ashok Kasundra, Siralee Munshi, M. Amir Siddiqui, Subrat Kumar Bhattamisra, C. Dutt, Vijay Chauthaiwale
  • Patent number: 7713974
    Abstract: The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A1, A2, A3 or A4 and R1, R2, R3, R4a, R4b, R5, R6, Ar, X1, X2, X4, X4 and X5 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.
    Type: Grant
    Filed: August 15, 2007
    Date of Patent: May 11, 2010
    Assignee: Roche Palo Alto LLC
    Inventors: Joshua Kennedy-Smith, Wylie Solang Palmer, Zachary Kevin Sweeney
  • Publication number: 20100093822
    Abstract: The present invention relates to a process for the sulfinylation of a pyrazole derivative, characterized in that 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-1H-pyrazole-3-carbonitrile (II) is reacted with a sulfinylating agent S in the presence of at least one amine acid complex wherein the amine(s) are selected from cyclic secondary amines and the acid(s) are selected from sulfonic acid derivatives, and with the addition of a halogenating agent, wherein S is [CF3S(O)]2O; or CF3S(O)X wherein X means fluoro, chloro, bromo, iodo, a hydroxy group, or an alkaline or alkaline earth metal salt of the hydroxy group; or mixtures thereof.
    Type: Application
    Filed: November 5, 2007
    Publication date: April 15, 2010
    Applicant: BASF SE
    Inventors: Martin Sukopp, Oliver Kuhn, Carsten Gröning, Michael Keil, Jon J. Longlet
  • Publication number: 20090163560
    Abstract: A compound having a structure and therapeutic methods, compositions, and medicaments related thereto are disclosed herein.
    Type: Application
    Filed: February 17, 2009
    Publication date: June 25, 2009
    Inventors: David W. Old, Danny T. Dinh
  • Patent number: 7511149
    Abstract: 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: Grant
    Filed: February 9, 2007
    Date of Patent: March 31, 2009
    Assignee: Dow AgroSciences LLC
    Inventors: Kim E. Arndt, Douglas C. Bland, David E. Podhorez, James R. McConnell
  • Publication number: 20090036688
    Abstract: The present invention relates to a process for producing a 5-alkoxy-4-hydroxymethylpyrazole compound represented by the general formula (3) which comprises reacting a pyrazole compound represented by the general formula (1) (wherein R1 is a substituent such as alkyl group, substituted or unsubstituted group or the like, and R2 is an electron withdrawing group) with a compound represented by the general formula (2) L-R3??(2) (wherein L is a leaving group and R3 is a substituent such as substituted or unsubstituted alkyl group or the like) in the presence of a base and formaldehyde.
    Type: Application
    Filed: February 8, 2007
    Publication date: February 5, 2009
    Applicant: IHARA CHEMICAL INDUSTRY CO., LTD
    Inventors: Yukio Uchida, Naoya Atsumi
  • Publication number: 20080234346
    Abstract: The invention provides substituted pyrazolidinone compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing preterm labor, dysmenorrhea, asthma, hypertension, infertility or fertility disorder, undesired blood clotting, preeclampsia or eclampsia, an eosinophil disorder, sexual dysfunction, osteporosis and other destructive bone disease or disorder, and other diseases and disorders associated with the prostaglandin EP2 and/or EP4 receptors.
    Type: Application
    Filed: May 14, 2008
    Publication date: September 25, 2008
    Applicant: LABORATOIRES SERONO S.A.
    Inventors: Gian Luca ARALDI, Yihua Liao, Adulla P. Reddy, Zhong Zhao
  • Publication number: 20080194405
    Abstract: The present invention relates to novel 5-hydroxypyrazolines of the formula I in which the substituents are as defined below: B is phenyl, naphthyl or 5- or 6-membered hetaryl which contains one to four heteroatoms from the group consisting of O, N and S; A is C?O, C?S or SO2; R1 is alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl or haloalkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, phenyl, 5- or 6-membered heterocyclyl or hetaryl which contains one to four heteroatoms from the group consisting of O, N and S; R2 is alkyl, haloalkyl, alkenyl, haloalkyl, alkynyl, haloalkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, phenyl, 5- or 6-membered hetaryl or heterocyclyl which contains one to four heteroatoms from the group consisting of O, N and S; R3 is hydrogen, nitro, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, haloalkenyl, alkynyl, haloalkynyl or NR?2, where R? independently of one another are hydrogen or alkyl; R4 is hydrogen, halogen, nitro, cyano, NR?2, alkyl, haloalkyl, COOR? or 5- or 6-memb
    Type: Application
    Filed: May 24, 2006
    Publication date: August 14, 2008
    Applicant: BASF Atkiengesellschaft
    Inventors: Markus Gewehr, Jochen Dietz, Thomas Grote, Andreas Gypser, Matthias Niedenbruck
  • Publication number: 20080090875
    Abstract: A 1,2,4-triazole derivative of formula 1 or a non-toxic salt thereof, a preparation method thereof, and a pharmaceutical composition containing the derivative or the salt as an active ingredient are provided.
    Type: Application
    Filed: November 25, 2003
    Publication date: April 17, 2008
    Applicant: CJC Corporation
    Inventors: Il Hwan Cho, Myeong Yun Chae, Young Hoon, Kyu Jeong Yeon, Chun Seon Lyu, Jong Hoon Kim, Sung Hak Jung, Sang Wook Park, Hyung Chul Ryu, Ji Young Noh, Hyun Jung Park, Jie Eun Park, Young Mee Chung
  • Patent number: 7183296
    Abstract: The present invention comprises novel and known pyrazole derivatives having anti-HIV activity, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds of formula I are inhibitors of the human immunodeficiency virus reverse transcriptase enzyme which is involved in viral replication. Consequently the compounds of this invention may be advantageously used as therapeutic agents for HIV infection.
    Type: Grant
    Filed: January 27, 2004
    Date of Patent: February 27, 2007
    Assignee: Roche Palo Alto LLC
    Inventors: Brian William Dymock, Philip Stephen Jones, John Herbert Merrett, Martin John Parratt
  • Patent number: 7109228
    Abstract: This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivatives thereof, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such, the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).
    Type: Grant
    Filed: April 5, 2002
    Date of Patent: September 19, 2006
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Lyn Howard Jones, Charles Eric Mowbray, David Anthony Price, Matthew Duncan Selby, Paul Anthony Stupple
  • Patent number: 6750230
    Abstract: This invention relates to the use of pyrazole derivatives of the formula and pharmaceutically acceptable salts and solvates thereof, in the manufacture of a reverse transcriptase inhibitor or modulator, to certain novel such pyrazole derivatives and to processes for the preparation of and compositions containing such novel derivatives.
    Type: Grant
    Filed: July 5, 2001
    Date of Patent: June 15, 2004
    Assignee: Pfizer, Inc.
    Inventors: Romuald Gaston Corbau, Charles Eric Mowbray, Manoussos Perros, Paul Anthony Stupple, Anthony Wood
  • Patent number: 6750222
    Abstract: The present invention relates to compounds of the formula (I) and/or salts thereof where R1, R2, A, B, X and Y are as defined in claim 1. The compounds according to the invention are suitable for use as herbicides and plant growth regulators.
    Type: Grant
    Filed: December 13, 2002
    Date of Patent: June 15, 2004
    Assignee: Bayer CropScience GmbH
    Inventors: Hendrik Helmke, Michael Gerhard Hoffmann, Klaus Haaf, Lothar Willms, Thomas Auler, Hermann Bieringer, Hubert Menne
  • Patent number: 6699991
    Abstract: A “one-pot” process is described herein for the production of pyrazole compounds of general formula (II) comprising the steps of reacting a compound of general formula (III) with an acylating agent in the presence of a base and an optional activating agent followed by the addition of a hydrazine compound in situ.
    Type: Grant
    Filed: January 17, 2003
    Date of Patent: March 2, 2004
    Assignee: Pfizer Inc.
    Inventors: Harris Laurence James, Levett Philip Charles
  • Patent number: 6538015
    Abstract: The invention is concerned with novel pyrazole derivatives, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds of formula I are inhibitors of the human immunodeficiency virus reverse transcriptase enzyme which is involved in viral replication. Consequently the compounds of this invention may be advantageously used as therapeutic agents for HIV mediated process.
    Type: Grant
    Filed: May 24, 2002
    Date of Patent: March 25, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Brian William Dymock, Adrian Liam Gill, Philip Stephen Jones, Kevin Edward Burdon Parkes, Martin John Parratt
  • Patent number: 6518266
    Abstract: The present invention is directed to novel pyrazole derivatives and their use as pesticidal agents. The pyrazole derivatives have Formula I: or a salt thereof, where R1 represents R5O, R5SO2, R5SO or R5S in which R5 is as defined herein; X is halo, cyano, C1-6 alkoxycarbonyl, C2-6 alkynyl, optionally substituted C6-14 aryl or an optionally substituted 5- to 7-membered heteroaromatic ring linked to thiazole via a carbon-carbon bond; R2 is hydrogen, amino, chloro, bromo, iodo, cyano, C1-6 alkoxy, C1-6 alkyl or C6-10 aryl; and R3-R7 each represent hydrogen, halogen, straight- or branched-chain C1-4 alkyl or C1-4 alkoxy, either of which is unsubstituted or substituted by one or more halogen atoms, straight- or branched-chain C1-4 alkylthio or C1-4 alkylsulphinyl, either of which is substituted by one or more halogen atoms, nitro, cyano, or straight- or branched-chain C1-4 alkylsulphonyl group which is unsubstituted or substituted by one or more halogen atoms.
    Type: Grant
    Filed: July 21, 2000
    Date of Patent: February 11, 2003
    Assignees: 3-Dimensional Pharmaceuticals, Heska Corporation
    Inventors: Daljit S. Dhanoa, Dario Doller, Sanath Meegalla, Richard M. Soll, Nancy Wisnewski, Gary Silver, Dan T. Stinchcomb, R. Lee Seward, Dimitris Agrafiotis, Deyou Sha
  • Patent number: 6506784
    Abstract: The present invention is directed to inhibiting pest GABA receptors by contacting said receptors with a compound of Formula I: The invention is also directed to methods of controlling pests, especially insects and arachnids such as fleas and ticks, and to novel compounds within the scope of Formula I.
    Type: Grant
    Filed: June 29, 2000
    Date of Patent: January 14, 2003
    Assignees: 3-Dimensional Pharmaceuticals, Inc., Heska Corporation
    Inventors: Daljit S. Dhanoa, Dario Doller, Sanath Meegalla, Richard M. Soll, Dimitris Agrafiotis, Nancy Wisnewski, Gary M. Silver, Dan T. Stinchcomb, R. Lee Seward
  • Patent number: 6472538
    Abstract: A process for preparing compounds of the formula I in which R1 is hydrogen, an aliphatic group having 1-8 carbon atoms, C1-C6-alkoxycarbonyl, C1-C6-alkylthiocarbonyl or a cyclic ring system having 3-14 ring atoms, and R2 is hydrogen, an aliphatic group having 1-8 carbon atoms, or R1 and R2 together with the carbon atom to which they are bound form a cyclic or bicyclic ring system having 3-14 ring atoms, comprises the preparation of compounds of the formula II  in which R3 and R4 are readily detachable groups and R1 and R2 are as defined above, as starting materials or intermediates and the cyclization of these under suitable reaction conditions to give compounds of the formula I.
    Type: Grant
    Filed: April 25, 2001
    Date of Patent: October 29, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Norbert Götz, Roland Götz, Michael Rack
  • Patent number: 6410533
    Abstract: The present invention provides compounds having useful antibacterial activity and pharmaceutical compositions comprising one or more of these compounds. The invention further relates to a method of treating a bacterial infection in a patient, comprising administering to the patient an effective mount of one or more of the antibacterial compounds of the invention.
    Type: Grant
    Filed: February 10, 2000
    Date of Patent: June 25, 2002
    Assignee: Genzyme Corporation
    Inventors: Bradford H. Hirth, Andrew Janjigian, Fred Vinick
  • Patent number: 6407259
    Abstract: A “one-pot” process is described herein for the production of pyrazole compounds of general formula (II) comprising the steps of reacting a compound of general formula (III) with an acylating agent in the presence of a base and an optional activating agent followed by the addition of a hydrazine compound in situ.
    Type: Grant
    Filed: July 6, 2001
    Date of Patent: June 18, 2002
    Assignee: Pfizer Inc.
    Inventors: Laurence James Harris, Philip Charles Levett
  • Patent number: 6392058
    Abstract: The invention relates to a process for preparing 1-substituted 5- and/or 3-hydroxypyrazoles of the formulae I and II in which R1 is C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C6-cycloalkyl or C1-C4-alkoxy, where these groups may be substituted by halogen, C1-C4-alkoxy, phenoxy, C1-C6-alkoxycarbonyl, C1-C6-alkylthiocarbonyl or by a cyclic ring system having 3-14 ring atoms, which comprises reacting an alkyl 3-alkoxyacrylate of the formula III in which R2, R3 independently of one another are C1-C6-alkyl or C3-C6-cycloalkyl with a hydrazine of the formula IV in which R1 is as defined above a) at a pH of 6-11 to give 5-hydroxypyrazoles of the formula I or b) at a pH of 11-14 to give 3-hydroxypyrazoles of the formula II.
    Type: Grant
    Filed: May 17, 2001
    Date of Patent: May 21, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Volker Maywald, Adrian Steinmetz, Michael Rack, Norbert Götz, Roland Götz, Jochem Henkelmann, Heike Becker, Juan Jose Aiscar Bayeto
  • Patent number: 6329530
    Abstract: The invention relates to a method for the production of 1-substituted 5-hydroxypyrazoles of formula (I) wherein R1 is C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkinyl, C3-C6-cycloalkyl or C1-C4-alkoxy, whereby these groups can be substituted by halogen, C1-C4-alkoxy, phenoxy, C1-C6-alkoxycarbonyl, C1-C6-alkylthiocarbonyl or a cyclic ring system with 3-14 ring atoms, by reacting a) an alkylvinylether of general formula (III) wherein R2 is C1-C6-alkyl or C3-C6-cycloalkyl, with phosgene (IVa), “diphosgene” (IVb) or “triphosgene” (IVc) to form acid chlorides of formula (V), b) transforming said acid chlorides by eliminating hydrogen chloride into the corresponding 3-alkoxyacrylic acid chloride of formula (VI) and c) reacting said acid chloride with hydrazines of formula (VII) wherein R1 has the above cited meaning, to form 5-hydroxypyrazoles of formula (I).
    Type: Grant
    Filed: May 3, 2001
    Date of Patent: December 11, 2001
    Assignee: BASF Aktiengesellschaft
    Inventors: Volker Maywald, Adrian Steinmetz, Michael Rack, Norbert Götz, Roland Götz, Jochem Henkelmann, Heike Becker, Juan Jose Aiscar Bayeto
  • Patent number: 6303569
    Abstract: The present invention is directed to double prodrugs containing polymeric-based transport forms.
    Type: Grant
    Filed: August 21, 1998
    Date of Patent: October 16, 2001
    Assignee: Enzon, Inc.
    Inventors: Richard B. Greenwald, Yun H. Choe, Annapurna Pendri