The Halogen Is Fluorine Patents (Class 564/54)
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Patent number: 9029401Abstract: The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.Type: GrantFiled: February 14, 2012Date of Patent: May 12, 2015Assignee: The Regents of the University of CaliforniaInventors: Bruce D. Hammock, Sung Hee Hwang, Aaron T. Wecksler, Christophe Morisseau
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Patent number: 8993780Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.Type: GrantFiled: December 10, 2013Date of Patent: March 31, 2015Assignee: Allergan, Inc.Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
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Patent number: 8940935Abstract: The disclosure provides curable inks including a bis-urea gelator having the structure of Formula I. wherein R and R? each, independently of the other, is a saturated aliphatic hydrocarbon group selected from the group consisting of (1) linear aliphatic groups, (2) branched aliphatic groups, (3) cyclic aliphatic groups, (4) aliphatic groups containing both cyclic and acyclic portions, any carbon atom of the saturated aliphatic hydrocarbon group may be optionally substituted with an alkyl group (cyclic or acyclic), wherein (1) and (2) groups have a carbon number of from about 1 to about 22 carbons, and wherein (3) and (4) groups have a carbon number of from about 4 to about 10 carbons; and X is selected from the group consisting of: (i) an alkylene group, (ii) an arylene group, (iii) an arylalkylene group, and (iv) an alkylarylene group.Type: GrantFiled: January 28, 2013Date of Patent: January 27, 2015Assignee: Xerox CorporationInventors: Naveen Chopra, Michelle N. Chretien, Barkev Keoshkerian, Jenny Eliyahu, Daryl W. Vanbesien, Adela Goredema
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Publication number: 20140329860Abstract: Methods of treating or suppressing oxidative stress diseases including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2-substituted-p-quinone derivatives as disclosed herein.Type: ApplicationFiled: March 24, 2014Publication date: November 6, 2014Applicant: Edison Pharmaceuticals, Inc.Inventors: Andrew W. Hinman, Kieron E. Wesson, Orion D. Jankowski, Paul Mollard, William D. Shrader, Christopher R. Cornell
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Patent number: 8816076Abstract: The present invention relates to novel aryl urea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.Type: GrantFiled: August 14, 2013Date of Patent: August 26, 2014Assignee: Allergan, Inc.Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
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Publication number: 20140094614Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.Type: ApplicationFiled: December 10, 2013Publication date: April 3, 2014Applicant: Allergan, Inc.Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
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Publication number: 20140088156Abstract: The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.Type: ApplicationFiled: February 14, 2012Publication date: March 27, 2014Applicant: The Regents of the University of CaliforniaInventors: Bruce D. Hammock, Sung Hee Hwang, Aaron T. Wecksler, Christophe Morisseau
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Publication number: 20130331570Abstract: The present invention relates to novel aryl urea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.Type: ApplicationFiled: August 14, 2013Publication date: December 12, 2013Applicant: Allergan, Inc.Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
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Patent number: 8541577Abstract: The present invention relates to novel aryl urea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.Type: GrantFiled: November 5, 2012Date of Patent: September 24, 2013Assignee: Allergan, Inc.Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
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Publication number: 20100311980Abstract: There is provided a process for preparing sorafenib or a salt thereof comprising the use of a compound of formula (A) wherein R? is selected from the group consisting of hydrogen, —C(O)OA, —C(O)CX3, —C(O)NH2, —C(O)—NHOH or There is also provided intermediate compounds of general formula (A), N-methyl-4-(4-ureidophenoxy)picolinamide, 4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenylcarbamate derivative and N-methyl-4-(4-(2,2,2-trihaloacetamido)phenoxy)picolinamide, processes for their preparation and their use in the preparation of sorafenib.Type: ApplicationFiled: September 10, 2008Publication date: December 9, 2010Applicant: CIPLA LIMITEDInventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Maruti Ghagare, Sandip Chikhalikar
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Publication number: 20100240613Abstract: The present invention relates to a pyrimidine compound or a pharmaceutically acceptable salt thereof represented by the following formula [I] wherein each symbol is as defined in the specification and a method of therapeutically or prophylactically treating an undesirable cell proliferation, comprising administering such a compound. The compound of the present invention has superior activity in suppressing undesirable cell proliferation, particularly, an antitumor activity, and is useful as an antitumor agent for the prophylaxis or treatment of cancer, rheumatism, and the like. In addition, the compound of the present invention can be a more effective antitumor agent when used in combination with other antitumor agents such as an alkylating agent or metabolism antagonist.Type: ApplicationFiled: November 25, 2009Publication date: September 23, 2010Applicant: Japan Tobacco Inc.Inventors: Hisashi Kawasaki, Hiroyuki Abe, Kazuhide Hayakawa, Tetsuya Iida, Shinichi Kikuchi, Takayuki Yamaguchi, Toyomichi Nanayama, Hironori Kurachi, Masahiro Tamaru, Yoshikazu Hori, Mitsuru Takahashi, Takayuki Yoshida, Toshiyuki Sakai
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Patent number: 7696249Abstract: The invention relates to novel specifically trifluoromethyl and halogen substituted 1,3-diphenyl ureas and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects like the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as anti-infectives.Type: GrantFiled: December 8, 2006Date of Patent: April 13, 2010Assignee: ARPIDA AGInventors: Ralf Loewe, Sergio Lociuro, Stephen Hawser, Laurent Schmitt
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Patent number: 7645903Abstract: The present invention relates to an IgG-binding compound, which more specifically has affinity for human IgGs of ?-type and functional derivatives thereof. More specifically, the compound according to the invention comprises an N,N-alkylated urea moiety located between an aromatic part and another part, which is a linear or cyclic substituted or unsubstituted aliphatic group. The compound binds to a pocket-shaped binding site present on all human IgG ?-Fabs, which site is located between the two domains (CH1 and CL) of its constant part. Accordingly, the compound according to the invention is a ligand for human IgGs of ?-type, and consequently, the invention also relates to a separation matrix for affinity chromatography, which matrix comprises said compound, as well as to other uses of the compound.Type: GrantFiled: September 12, 2003Date of Patent: January 12, 2010Assignee: GE Healthcare Bio-Sciences ABInventors: Andreas Axén, Herbert Baumann, Enrique Carredano, Anna Grönberg, Elles Steensma
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Publication number: 20090192192Abstract: The present invention relates to the use of compounds as broad spectrum inhibitors of bacterial biofilm formation. In particular the invention refers to a family of compounds that block the quorum sensing system of Gram-negative and Gram-positive bacteria, a process for their manufacture, pharmaceutical compositions containing them and to their use for the treatment and prevention of bacterial damages and diseases, in particular for diseases where there is an advantage in inhibiting quorum sensing regulated phenotypes of pathogens.Type: ApplicationFiled: December 17, 2008Publication date: July 30, 2009Inventors: Aldo Ammendola, Tanja Wieber, Andreas Wuzik, Martin Lang
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Publication number: 20090082423Abstract: Disclosed are amide, thioamide, urea and thiourea compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, and diabetic-related diseases.Type: ApplicationFiled: September 10, 2008Publication date: March 26, 2009Inventors: Sampath-Kumar Anandan, Richard D. Gless, JR.
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Publication number: 20090023813Abstract: The invention relates to novel specifically trifluoromethyl and halogen substituted 1,3-diphenyl ureas and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects like the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as anti-infectives.Type: ApplicationFiled: December 8, 2006Publication date: January 22, 2009Applicant: Arpida AGInventors: Ralf Loewe, Sergio Lociuro, Stephen Hawser, Laurent Schmitt
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Publication number: 20090005452Abstract: The invention relates to novel specifically trifluoromethyl and halogen substituted 1,3-diphenyl ureas and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects like the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as anti-infectives.Type: ApplicationFiled: December 8, 2006Publication date: January 1, 2009Applicant: ARIPIDA AGInventors: Ralf Loewe, Sergio Lociuro, Stephen Hawser, Laurent Schmitt
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Publication number: 20080096943Abstract: Compounds of formula I in free or salt form, wherein T, X, R1, R2, Ra, R3, R4, R5 and U have the meanings as indicated in the specification, are useful for treating a condition mediated by CCR-3, particularly an inflammatory or allergic condition such as an inflammatory or obstructive airways disease. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: August 9, 2005Publication date: April 24, 2008Inventors: Gurdip Bhalay, Andrew Dunstan, Angela Glen, Trevor John Howe, Clive McCarthy
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Patent number: 7241923Abstract: The present invention relates to certain phenalkyloxy-phenyl derivatives of formula (I) and analogs, to a process for preparing such compounds, having the utility in clinical conditions associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: GrantFiled: May 30, 2003Date of Patent: July 10, 2007Assignee: Astrazeneca ABInventors: Jonas Fagerhad, Lanna Li, Lindstedt Alstermark Eva-Lotte
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Patent number: 7235576Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.Type: GrantFiled: January 11, 2002Date of Patent: June 26, 2007Assignee: Bayer Pharmaceuticals CorporationInventors: Bernd Riedl, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, Mary-Katherine Monahan, Reina Natero, Joel Renick, Robert N. Sibley
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Patent number: 7105567Abstract: The present invention relates to a urea derivative of the formula (1) wherein each symbol is as described in the specification, a pharmaceutically acceptable salt thereof and pharmaceutical use thereof. The compound of the present invention has a C5a receptor antagonistic action and is useful as an agent for the prophylaxis or treatment of diseases or syndromes due to inflammation caused by C5a [e.g., autoimmune diseases such as rheumatism, systemic lupus erythematosus and the like, sepsis, adult respiratory distress syndrome, chronic obstructive pulmonary disease, allergic diseases such as asthma and the like, atherosclerosis, cardiac infarction, brain infarction, psoriasis, Alzheimer's disease and serious organ injury (e.g., pneumonia, nephritis, hepatitis, pancreatitis and the like) due to activation of leukocytes caused by ischemia, trauma, burn, surgical invasion and the like].Type: GrantFiled: August 10, 2001Date of Patent: September 12, 2006Assignee: Mitsubishi Pharma CorporationInventors: Seigo Ishibuchi, Hiroshi Sumichika, Katsuhiko Itoh, Yoichi Naka
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Patent number: 6962945Abstract: The present invention provides N-aryloxypropanolyl-N?-phenethyl-urea derivatives of formula 3, method for their preparation and use thereof as potent appetite suppressants for treatment of obesity wherein R is selected from the group consisting of H, 2, 3 or 4-trifluoromethyl, 2, 3, or 4-chloro, 2, 3, or 4-bromo, 4-acetyl, 4-propionyl, 4-acetamido, 2,3 or 4 methoxy, 4 nitrile, 2,3 or 4-methyl, and 4 formyl and X is S or O.Type: GrantFiled: March 26, 2004Date of Patent: November 8, 2005Assignee: Council of Scientific and Industrial ResearchInventors: Kalpana Bhandari, Shipra Srivastava, Chandeshwar Nath
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Patent number: 6699904Abstract: PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.Type: GrantFiled: February 14, 2002Date of Patent: March 2, 2004Assignee: Pfizer Inc.Inventors: Cheryl M. Hayward, David A. Perry
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Patent number: 6686394Abstract: Described herein are novel 1-aryl-3-(2-chloroalkanylureas derivatives. These derivatives are useful anticaner agents having excellent specifilty towards cell targets and potent antineoplastic activity without systemic toxicity derivatives mutagenicity. More specifically, the invention is directed to novel derivatives of the following formula: wherein R1 is C1-C6 alkyl, C3-C7 cycloalkyl, C1-C6 alkoxy, C1-C6 hydroxy alkyl, or C1-C6 halide; R2 is H, C1-C6 alky, C3-C7 cycloalkyl, C1-C6 I alkoxy, C1-C6 hydroxy alkyl or C1-C6 halide, di-halide or tri-halide; R1 and R2 may also be part of cyclic structures.Type: GrantFiled: December 6, 2001Date of Patent: February 3, 2004Assignee: Sovar, Societe en CommanditeInventor: René C. -Gaudreault
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Patent number: 6214880Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: September 21, 1999Date of Patent: April 10, 2001Assignee: Tularik Inc.Inventor: Jonathan B. Houze
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Patent number: 5639887Abstract: Compounds of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are herein described, A is a straight or branched (C.sub.2 -C.sub.12)alkyl or a phenyl moiety and B is a moiety of the formula: ##STR2## The compounds are effective in potentiating the activity of chemotherapeutic anti-cancer agents by increasing the sensitivity of multi-drug resistant cells to such chemotherapeutic agents.Type: GrantFiled: May 25, 1995Date of Patent: June 17, 1997Assignee: American Cyanamid CompanyInventors: Dennis Powell, Rolf Paul, William A. Hallett, Dan M. Berger, Minu D. Dutia
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Patent number: 5621010Abstract: Urea derivatives of formula (I) ##STR1## wherein the valuable groups are as defined in the specification, which possess both an ACAT inhibitory activity and an antioxidative activity. Those derivatives are useful in the prophylaxis and treatment of hypercholesterolemia and atherosclerosis.Type: GrantFiled: May 18, 1994Date of Patent: April 15, 1997Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Noriyoshi Sueda, Kazuhiko Yamada, Makoto Yanai, Katsutoshi Miura, Masato Horigome, Norio Oshida, Shigeru Hiramoto, Koichi Katsuyama, Fumihisa Nakata, Nobuhiro Kinoshita, Yoko Tsukada
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Patent number: 5441984Abstract: The present invention provides novel urea, thiourea and guanidine derivatives, pharmaceutical formulations thereof and a method of using same to prevent diabetic complications.Type: GrantFiled: November 14, 1994Date of Patent: August 15, 1995Assignee: Eli Lilly and CompanyInventors: William F. Heath, Jr., Jill A. Panetta, John K. Shadle
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Patent number: 5420348Abstract: Urea derivatives of the general formula (I) ##STR1## and salts thereof, pharmaceutical compositions containing the same, and methods for producing the same are-disclosed.The urea derivatives of the general formula (I) and salts thereof are novel compounds having the acyl-CoA cholesterol acyltransferase (ACAT) inhibiting activity.Type: GrantFiled: July 2, 1993Date of Patent: May 30, 1995Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Noriki Ito, Koyo Matsuda, Kiyoshi Iwaoka, Yuichi Iizumi
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Patent number: 5414111Abstract: Polyfluoro organic compound having at least one urea linkage derived from: (1) at least one polyisocyanate containing at least three isocyanate groups, (2) at least one fluorochemical compound which contains per molecule (a) a single functional group having one or more Zerewitinoff hydrogen atoms and (b) at least two carbon atoms each of which contains at least two fluorine atoms, and (3) water in an amount sufficient to to react with from about 5% to about 60% of the isocyanate groups.Type: GrantFiled: February 2, 1994Date of Patent: May 9, 1995Assignee: E. I. Du Pont de Nemours and CompanyInventor: Jack R. Kirchner
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Patent number: 5410073Abstract: Process comprising (I) reacting (a) at least one polyisocyanate or mixture of polyisocyanates which contains at least three isocyanate groups per molecule with (b) a stoichiometric deficiency of at least one fluorochemical compound which contains per molecule (i) a single functional group having one or more Zerewitinoff hydrogen atoms and (ii) at least two carbon atoms each of which contains at least two fluorine atoms, and (II) thereafter forming one or more urea linkages per mol of said polyisocyanate by reacting the remaining isocyanate groups with water in an amount sufficient to to react with from about 5% to about 60% of the isocyanate groups in said polyisocyanate.Type: GrantFiled: February 4, 1994Date of Patent: April 25, 1995Assignee: E. I. Du Pont de Nemours and CompanyInventor: Jack R. Kirchner
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Patent number: 5407959Abstract: Compounds of structure ##STR1## where W is selected from the group consisting of ##STR2## where Q is oxygen or sulfur, R.sup.7 and R.sup.8 are independently selected from hydrogen and alkyl, or R.sup.7 and R.sup.8, together with the nitrogen atoms to which they are attached, define a radical of formula ##STR3## L.sup.1 and L.sup.2 are independently selected from a valence bond, alkylene, propenylene, and propynylene; R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently selected from alkyl, alkoxy, haloalkyl, halogen, cyano, amino, alkoxycarbonyl, and dialkylaminocarbonyl; Y is oxygen, >NR.sup.11, where R.sup.11 is hydrogen or alkyl, or ##STR4## where n=0, 1, or 2; and R.sup.5 and R.sup.6 are alkyl, inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.Type: GrantFiled: November 12, 1993Date of Patent: April 18, 1995Assignee: Abbott LaboratoriesInventors: Joseph F. Dellaria, Anwer Basha, Lawrence A. Black, Linda J. Chernesky, Wendy Lee
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Patent number: 5389682Abstract: The invention concerns a series of novel bis-urea derivatives, nonpeptides, which show good binding affinity for the CCK-B receptor. The compounds, compositions containing them, methods of preparation, and utilities including anxiety, gastric acid secretion inhibition, and psychoses are included.Type: GrantFiled: September 13, 1993Date of Patent: February 14, 1995Assignee: Warner-Lambert CompanyInventors: Bradley D. Tait, Michael W. Wilson
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Patent number: 5384425Abstract: Diurea derivatives are provided which can be represented by the following general formula and salts thereof: ##STR1## wherein, R.sup.1 and R.sup.2 are the same or different, and each represents C.sup.1 -10 alkyl group, a C.sup.3 -18 cycloalkyl group, or a lower alkyl group substituted by cycloalkyl radical(s);R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different, and each represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, hydrocarbyl aralkyl group, a pyridyl group, or an unsubstituted or substituted phenyl group, the substituents of the phenyl group being selected from a group consisting of lower alkyl radical, halogen atom-substituted lower alkyl radical, halogen atom, nitro radical, amino radical, mono- or di-lower alkylamino radical, lower acylamino radical, hydroxyl radical, lower alkoxy radical and lower acyloxy radical;X represents an oxygen atom or a sulfur atom, and n.sup.1 and n.sup.2 represent an integer of 1 to 6; and wherein at least one of R.sup.3 -R.sup.Type: GrantFiled: October 7, 1993Date of Patent: January 24, 1995Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Noriki Ito, Tomoyuki Yasunaga, Yuichi Iizumi, Tomio Araki
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Patent number: 5380941Abstract: A process for preparing ureas of the formula ##STR1## where the ring A can be substituted and benzo-fused andn is 0 or 2,R.sup.4 and R.sup.5 are hydrogen, C.sub.1 -C.sub.4 -alkyl or phenyl,L is unsubstituted or substituted C.sub.2 -C.sub.4 -alkylene, or NR.sup.5 and L are together the radical of the formula ##STR2## and Z is hydroxyl or a radical which can be eliminated under alkaline reaction conditions,by reacting a phenylurea of the formula ##STR3## where R.sup.4 and the ring A each have the abovementioned meanings, with an amine of the formula ##STR4## where n, R.sup.5, L and Z each have the abovementioned meanings, at from 80.degree. to 180.degree. C. in the presence or absence of an inert diluent is described.Type: GrantFiled: October 1, 1993Date of Patent: January 10, 1995Assignee: BASF AktiengesellschaftInventors: Bernd Siegel, Manfred Patsch
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Patent number: 5283362Abstract: Process for the preparation of very pure ureas of the formula phenyl--(NH--CO--NR.sub.1 R.sub.2).sub.n in which phenyl represents an unsubstituted or substituted phenyl or phenylene group and R.sub.1 and R.sub.2 are either identical and each represent an alkyl group, or are different, in which case R.sub.1 represents a hydrogen atom and R.sub.2 represents an alkyl or phenyl group, or R.sub.1 and R.sub.2, together with the nitrogen atom, represent an aliphatic heterocyclic ring and n is the number 1 or 2, by reacting a phenylurea of the formula phenyl--(NH--CO--NH.sub.2).sub.n with an amine of the formula NR.sub.1 R.sub.2 H at temperatures from 100 to 200.degree. C. in a diluent which is inert under the reaction conditions, the reaction being interrupted before by-products are formed, and the urea which is formed being removed from the starting compounds, and the unreacted starting compounds being returned to the process if appropriate.Type: GrantFiled: July 31, 1992Date of Patent: February 1, 1994Assignee: Chemie Linz Gesellschaft m.b.H.Inventors: Kurt A. Hackl, Heinz Falk
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Patent number: 5264441Abstract: The invention provides new ureas and thioureas derivatives of general formula (I) ##STR1## and pharmaceutically acceptable salts thereof, which are useful as therapeutic agents such as for the prevention of coronary heart disease and as antidyslipidaemic agents.Type: GrantFiled: February 18, 1992Date of Patent: November 23, 1993Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Paolo Cozzi, Danielle Fancelli, Dino Severino, Augusto Chiari, Giancarlo Ghiselli
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Patent number: 5258405Abstract: Urea derivatives of the general formula (I) ##STR1## and salts thereof, pharmaceutical compositions containing the same, and methods for producing the same are disclosed.The urea derivatives of the general formula (I) and salts thereof are novel compounds having the acyl-CoA cholesterol acyltransferase (ACAT) inhibiting activity.Type: GrantFiled: September 29, 1992Date of Patent: November 2, 1993Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Noriki Ito, Koyo Matsuda, Kiyoshi Iwaoka
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Patent number: 5231216Abstract: There are described novel trans-2-acylaminocyclohexyloxyacyldipeptides of formula I ##STR1## wherein R.sub.1 represents --CO--R.sub.6, --SO.sub.2 --R.sub.7 or ##STR2## R.sub.6 is C.sub.1 -C.sub.18 alkyl or C.sub.1 -C.sub.18 alkoxy, R.sub.7 is C.sub.1 -C.sub.18 alkyl or an optionally substituted phenyl group,Y is .dbd.O, .dbd.S or .dbd.NH;R.sub.2 =R.sub.3 and represent --H or C.sub.1 -C.sub.12 alkyl,R.sub.4 represents --OR.sub.8 or --NHR.sub.9,R.sub.8 is --H, C.sub.1 -C.sub.8 alkyl or benzyl,R.sub.9 is --H, a straight or branched chain C.sub.1 -C.sub.18 alkyl group or benzyl group;R.sub.5 represents --OR.sub.9 or --NHR.sub.9,and novel (1R,2R)- and (1S,2S)-trans-2-acylaminocyclohexyloxyacetyldipeptides of the formulas Ia and Ib ##STR3## wherein R.sub.1 is --CO--R.sub.6, R.sub.6 is C.sub.1 -C.sub.18 alkyl,R.sub.2 is --H,R.sub.3 is --H or C.sub.1 -C.sub.12 alkyl,R.sub.4 is --OR.sub.8 or --NHR.sub.9,R.sub.8 is --H, C.sub.1 -C.sub.8 alkyl or benzyl,R.sub.9 is --H, C.sub.1 -C.sub.18 alkyl or benzyl,R.sub.5 is --OR.Type: GrantFiled: August 19, 1991Date of Patent: July 27, 1993Assignee: Univerza Edvarda Kardelja v LjubljanaInventors: Slavko Pecar, Danijel Kikelj, Uros Urleb, Marija Sollner, Gasper Marc, Ales Krbavcic, Vlado Kotnik, Branka Wraber-Herzog, Sasa Simcie, Alojz Than, Lidija Klamfer, Lucka Povsic, Zdravko Kopitar, Anton Stalc
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Patent number: 5227492Abstract: Diurea derivatives are provided which can be represented by the following general formula and salts thereof: ##STR1## Illustrative derivatives include 1,3-bis[[1-cycloheptyl-3-(3-pyridyl)ureido]-methyl]benzene, 1,3-bis[[1-cycloheptyl-3-(2-pyridyl)ureido]-methyl]benzene, and 1,3-bis[[1-cycloheptyl-3-(4-pyridyl)ureido]-methyl]benzene.The above compounds inhibit acyl-coenzyme A cholesterol acyltransferase (ACAT enzyme), and thereby control the accumulation of cholesterol ester to the smooth muscle of arterial wall in the blood vessel.Type: GrantFiled: June 30, 1992Date of Patent: July 13, 1993Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Noriki Ito, Tomoyuki Yasunaga, Yuichi Iizumi, Tomio Araki
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Patent number: 5198582Abstract: A process for preparing N,N'-disubstituted urea derivatives of the following formula (I) ##STR1## wherein Ar represents an unsubstituted aromatic radical or an aromatic radical substituted with a halogen atom, an alkyl group, or an alkoxy group, which comprises reacting an aromatic mono-nitro compound, an aromatic primary amine, and synthesis gas in the presence of a catalyst consisting essentially of a divalent palladium compound as a main catalyst component and an ammonium or a phosphonium salt containing halogen atom as a co-catalyst component, and a non-polar solvent.Type: GrantFiled: October 22, 1991Date of Patent: March 30, 1993Assignee: Lucky Ltd.Inventors: Jae S. Oh, Sang M. Lee
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Patent number: 5166429Abstract: Diurea Derivatives represented by the following general formula and salts thereof: ##STR1## The above compounds inhibit acyl-coenzyme A chloresterol acyl-transferase (ACAT enzyme), and thereby control the accumulation of cholesterol ester to the smooth muscle of arterial wall in the blood vessel.Type: GrantFiled: September 24, 1991Date of Patent: November 24, 1992Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Noriki Ito, Tomoyuki Yasunaga, Yuichi Iizumi, Tomio Araki
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Patent number: 5126483Abstract: Novel 1-phenylakyl-3-phenylurea derivatives represented by the following formula (I): ##STR1## wherein R.sup.1 is an alkyl group of 1 to 8 carbon atoms, an alkoxy group of 1 to 5 carbon atoms or a halogen atom, R.sup.2 is an alkyl group of 1 to 15 carbon atoms, each of R.sup.3 and R.sup.4 is independently an alkyl group of 1 to 5 carbon atoms, m is an integer of 1 to 3, and n is 0 or 1, are provided.The compounds are potent in reducing the cholesterol level in serum, and useful for treating hyperlipemia and atherosclerosis.Type: GrantFiled: August 3, 1990Date of Patent: June 30, 1992Assignee: Mitsubishi Kasei CorporationInventors: Tetsuo Sekiya, Shinya Inoue, Chiaki Hyodo, Hiromi Okushima, Kohei Umezu, Kazuo Suzuki
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Patent number: 5106873Abstract: This invention relates to novel compounds which are ACAT inhibitors rendering them useful in lowering blood cholesterol levels. The compounds contain two urea or thiourea, amide, or amine moieties or combinations of said moieties and have the following general formula: ##STR1## wherein m and n are zero or one, W and YNH and ##STR2## form the urea, thiourea, amide or amine moieties; and R.sub.1 and R .sub.2 are hydrogen or a hydrocarbon radical.Type: GrantFiled: June 26, 1990Date of Patent: April 21, 1992Assignee: Warner-Lambert CompanyInventors: Patrick M. O'Brien, Drago R. Sliskovic, Michael W. Wilson
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Patent number: 5099021Abstract: Process for the preparation of pure, unsymmetrically disubstituted ureas of the general formula ##STR1## in which R denotes a phenyl radical which is unsubstituted, or monosubstituted or polysubstituted by halogen atoms or alkyl, alkoxy, aryloxy or trifluoromethyl groups, an oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, benzoxazolyl or benzothiazolyl radical which is unsubstituted, or monosubstituted or polysubstituted by halogen atoms or alkyl, alkoxy or trifluoromethyl groups and R.sub.1 and R.sub.2 independently of one another denote a hydrogen atom or an alkyl group, where R.sub.1 and R.sub.2 are not simultaneously hydrogen or R.sub.1 and R.sub.2 together denote a butylene or pentylene group, by reaction of an N-alkyl- or N,N-dialkylurea with an unsubstituted or substituted arylamine or a heterocyclic amine in the presence of that amine which is already present in the starting material, the respective N-alkyl- or N,N-dialkylurea.Type: GrantFiled: October 30, 1990Date of Patent: March 24, 1992Assignee: Agrolinz Agrarchemikalien Gesellschaft m.b.H.Inventors: Rudolf H. Worther, Horst Korntner, Egmont Auer, Kurt Thonhofer
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Patent number: 5091419Abstract: Diurea derivatives are provided which are represented by the following general formula and salts thereof: ##STR1## The above compounds inhibit acyl-coenzyme A cholesterol acyl-transferase (ACAT enzyme), and thereby control the accumulation of cholesterol ester on the smooth muscle of arterial wall in the blood vessels.Type: GrantFiled: October 2, 1990Date of Patent: February 25, 1992Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Noriki Ito, Tomoyuki Yasunaga, Yuichi Iizumi, Tomio Araki
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Patent number: 5063247Abstract: Novel diphenylurea derivatives represented by the following formula (I): ##STR1## wherein R.sub.1 is an alkyl group of 5 to 18 carbon atoms, each of R.sub.2 and R.sub.3 is independently an alkyl group of 1 to 5 carbon atoms, an alkoxy group of 1 to 5 carbon atoms or a halogen atom, R.sub.4 is hydrogen atom, an alkyl group of 1 to 5 carbon atoms, an alkoxy group of 1 to 5 carbon atoms or a halogen atom, and X is oxygen atom or sulfur atom, are provided.The compounds are potent in reducing the cholesterol level in serum, and useful for treating hyperlipemia and atherosclerosis.Type: GrantFiled: June 13, 1990Date of Patent: November 5, 1991Assignee: Mitsubishi Kasei CorporationInventors: Tetsuo Sekiya, Shinya Inoue, Masao Taniguchi, Kohei Umezu, Kazuo Suzuki
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Patent number: 5055582Abstract: This invention relates to a process for preparing useful thromboxane A.sub.2 inhibiting (.+-.)7-[3.alpha.-[1-[[(phenylamino)thioxomethyl]hydrazono]ethyl]-1.alpha. ,4.alpha.-bicyclo[2.2.1]hept-2.beta.-yl]-heptenoic acids and useful derivatives thereof from (.+-.)octahydro-1.alpha.-methyl-3a.alpha.,7a.alpha.-4.alpha.,7.alpha.-meth ano-2H-inden-2-ones.Type: GrantFiled: December 13, 1988Date of Patent: October 8, 1991Assignee: National Research Development CorporationInventors: Robert B. Garland, Masateru Miyano
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Patent number: 5015762Abstract: Aralkylphenylureas of the formula ##STR1## where R.sup.1 and R.sup.2 are hydrogen, alkoxy or unsubstituted or substituted alkyl, cycloalkyl, alkenyl or alkynyl, or R.sup.1 and R.sup.2 together are unsubstituted or substituted alkylene which may or may not be interrupted by oxygen or sulfur, Y is hydrogen, alkyl, halogen, alkoxy or haloalkyl, A is unsubstituted or substituted alkylene, Z is hydrogen, alkyl, haloalkyl, alkoxyalkyl, cycloalkyl, aralkyl, aryl, aryloxy, halogen, a C.sub.4 H.sub.4 chain which is fused to the benzene ring to give a substituted or unsubstituted naphthyl ring, alkoxy, haloalkoxy, alkylthio, thiocyanato, cyano, ##STR2## R' and R" being hydrogen, alkyl, alkoxy, alkylthio, cycloalkyl or unsubstituted or substituted phenyl and n is 1, 2, 3 or 4, and herbicides containing these ureas.Type: GrantFiled: May 28, 1981Date of Patent: May 14, 1991Assignee: BASF AktiengesellschaftInventors: Ulrich Schirmer, Wolfgang Rohr, Bruno Wuerzer
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Patent number: 5015644Abstract: Certain substituted urea, thiourea, carbamate, and thiocarbamate compounds are potent inhibitors of the enzyme acyl-CoA: cholesterol acyltransferase and are thus useful agents for inhibiting the intestinal absorption of cholesterol, and for lowering blood plasma cholesterol.Type: GrantFiled: June 1, 1989Date of Patent: May 14, 1991Assignee: Warner-Lambert CompanyInventors: Bruce D. Roth, Bharat K. Trivedi