Benzene Ring Bonded Directly To Urea Nitrogen (i.e., Anilides) Patents (Class 564/48)
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Patent number: 6391917Abstract: Dialkyl urea compounds are described which act as calcitonin mimetics. These compounds are useful in the treatment of diseases which are associated with bone resorption. The calcitonin mimetics of the present invention are also useful in assays for the determination of calcitonin receptor activity.Type: GrantFiled: April 19, 2001Date of Patent: May 21, 2002Assignee: ZymoGenetics, Inc.Inventors: Charles R. Petrie, Patricia A. McKernan, Emma E. Moore, John M. Ostresh, Jean-Philippe Meyer, Richard A. Houghten, Clemencia Pinilla
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Publication number: 20020052417Abstract: The present invention relates to compounds of the formula I, 1Type: ApplicationFiled: June 6, 2001Publication date: May 2, 2002Inventors: Otmar Klingler, Manfred Schudok, Hans-Peter Nestler, Hans Matter, Herman Schreuder
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Patent number: 6380392Abstract: The present invention includes array of new chiral ligands that are optically active or racemic. These ligands are bidentate, tridentate, tetradentate or pentadentate ligands which include P-P, P-N, N-N, mixed P-N, Schiff base or carbene sites. The present invention further includes a catalyst prepared by a process, which includes contacting a transition metal salt, or a complex thereof, and a ligand according to the present invention. The present invention still further includes a process for preparation of an asymmetric compound. In this process, a substrate capable of forming an asymmetric product by an asymmetric reaction and a catalyst according to the present invention are contacted to produce an asymmetric product. Transition metal complexes with these ligands are effective catalysts for asymmetric reactions.Type: GrantFiled: June 29, 2000Date of Patent: April 30, 2002Assignee: The Penn State Research FoundationInventor: Xumu Zhang
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Publication number: 20020049352Abstract: The present invention relates to a scaleable process for the oxidation of carbon-boron bonds with Oxone®.Type: ApplicationFiled: June 25, 2001Publication date: April 25, 2002Inventors: Weiling Cai, David H. Ripin
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Patent number: 6372933Abstract: This invention relates to a process for making certain phenyl urea compounds by using a Lewis acid to effect the ring opening of a benzoxazolinone by an amine.Type: GrantFiled: February 27, 2001Date of Patent: April 16, 2002Assignee: SmithKline Beecham CorporationInventors: Neil H. Baine, Ann Marie Eldridge, Marvin Sungwhan Yu
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Publication number: 20020038025Abstract: The present invention relates to compounds of formula (I) 1Type: ApplicationFiled: July 16, 2001Publication date: March 28, 2002Inventors: Jean Ackermann, Johannes Aebi, Alexander Chucholowski, Henrietta Dehmlow, Olivier Morand, Sabine Wallbaum, Thomas Weller
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Patent number: 6362229Abstract: The present invention relates generally to the fields of bacteriology and mycology. More particularly, the present invention provides novel inhibitors of multidrug transport proteins that may be used in combination with existing antibacterial agent and/or antifungal agents to increase the toxic effects of the antimicrobial agents. More specifically, the present invention provides methods and compositions for enhancing the antibacterial action of fluoroquinolones by administering fluoroquinolones in combination with an inhibitor of multidrug transporters and of enhancing the antifungal action of azole antifungal agents by administering an azole antifungal agent in combination with an inhibitor of multidrug transporters. Compositions comprising indole, urea, quinoline or aromatic amide based inhibitors also are disclosed.Type: GrantFiled: August 17, 2000Date of Patent: March 26, 2002Assignee: Influx, Inc.Inventors: Penelope N. Markham, Debbie C. Mulhearn, Alexander A. Neyfakh, David Crich, Mohamad-Rami Jaber, Michael E. Johnson
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Patent number: 6333432Abstract: Fungicidal compositions and methods comprising acylated aminosalicylamides (AASA) described herein. Novel amines and 3-nitrosalicylamides, and their use as pesticides and in the preparation of the antifungal AASA compounds are also disclosed.Type: GrantFiled: May 1, 2000Date of Patent: December 25, 2001Inventors: Gina M. Fitzpatrick, Ann B. Orth, Maurice C. H. Yap, Richard B. Rogers, Todd L. Werk, George E. Davis
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Patent number: 6294694Abstract: Peptoid compounds of Formula I and Formula II are disclosed The compounds are useful in the treatment of matrix metalloproteinase-mediated disorders.Type: GrantFiled: June 4, 1999Date of Patent: September 25, 2001Assignee: Wisconsin Alumni Research FoundationInventors: Donald T. Witiak, Paul J. Bertics, Yingsheng Zhang
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Patent number: 6255351Abstract: Dialkyl urea compounds are described which act as calcitonin mimetics. These compounds are useful in the treatment of diseases which are associated with bone resorption. The calcitonin mimetics of the present invention are also useful in assays for the determination of calcitonin receptor activity.Type: GrantFiled: September 30, 1999Date of Patent: July 3, 2001Assignee: ZymoGenetics, Inc.Inventors: Charles R. Petrie, Patricia A. McKernan, Emma E. Moore, John M. Ostresh, Jean-Philippe Meyer, Richard A. Houghten, Clemencia Pinilla
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Patent number: 6221913Abstract: Dialkyl urea compounds are described which act as calcitonin mimetics. These compounds are useful in the treatment of diseases which are associated with bone resorption. The calcitonin mimetics of the present invention are also useful in assays for the determination of calcitonin receptor activity.Type: GrantFiled: January 20, 1999Date of Patent: April 24, 2001Assignee: ZymoGenetics, Inc.Inventors: Charles R. Petrie, Patricia A. McKernan, Emma E. Moore, John M. Ostresh, Jean-Philippe Meyer, Richard A. Houghten, Clemencia Pinilla
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Patent number: 6218389Abstract: The invention provides compounds of formula as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.Type: GrantFiled: July 31, 1998Date of Patent: April 17, 2001Assignee: The Procter & Gamble Co.Inventors: Neil Gregory Almstead, Roger Gunnard Bookland, Yetunde Olabisi Taiwo, Rimma Sandler Bradley, Rodney Dean Bush, Biswanath De, Michael George Natchus, Stanislaw Pikul
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Patent number: 6214881Abstract: The present invention relates to the novel use of phenyl ureas in the treatment of disease states mediated by the chemokine, Interleukin-8 (I-8).Type: GrantFiled: February 9, 1999Date of Patent: April 10, 2001Assignee: SmithKline Beecham CorporationInventor: Jia-Ning Xiang
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Patent number: 6197798Abstract: Compounds of the formula I wherein R2—C, R3—C, R4—C or R5—C may be replaced by N; and wherein n is 1, 2 or 3; R1 is aryl, cycloalkyl or heterocyclyl; R2, R3, R4 and R5 are independently hydrogen, optionally substituted alkyl, halo, amino, substituted amino, trifluoromethyl, cyano, carboxyl, alkoxycarbonyl, aralkoxycarbonyl, (alkyl, aryl or aralkyl)-thio, (alkyl, aryl or aralkyl)-oxy, acyloxy, (alkyl, aryl or aralkyl)-aminocarbonyloxy; or any two of R2, R3, R4 and R5 at adjacent positions are alkylenedioxy; R6 is hydrogen, optionally substituted alkyl, amino, substituted amino, acylamino, wherein Ra is hydrogen or optionally substituted alkyl, Rb and Rc are independently hydrogen, optionally substituted alkyl, cycloalkyl, aryl or heterocyclyl; or Rb and Rc together represent lower alkylene or lower alkylene interrupted by O, S, or N—(H, alkyl or aralkyl); Rd is optionally substituted alkyl, cycloalkyl, aryl or heterocyclyl; and Re is opType: GrantFiled: July 20, 1999Date of Patent: March 6, 2001Assignee: Novartis AGInventors: Cynthia A. Fink, Gary M. Ksander, Paivi J. Kukkola, Eli M. Wallace, Mahavir Prashad
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Patent number: 6180676Abstract: This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More particularly, the invention relates to aromatic guanylhydrazone (more properly termed amidinohydrazone) compositions and their use to inhibit the uptake of arginine by macrophages and/or its conversion to urea. These compositions and methods are also useful in preventing the generation of nitric oxide (NO) by cells, and so to prevent NO-mediated inflammation and other responses in persons in need of same. In another embodiment, the compounds can be used to inhibit arginine uptake in arginine-dependent tumors and infections.Type: GrantFiled: June 6, 1995Date of Patent: January 30, 2001Assignee: The Picower Institute for Medical ResearchInventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
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Patent number: 6166064Abstract: A compound of formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are as defined in the description, R.sup.2 being an aromatic group, useful in the treatment and condition selected from the group consisting of the group meningitis and salpingitis, septic shock, disseminated intravascular coagulation, and/or adult respiratory distress syndrome, acute or chronic inflammation, arthritis, cholangitis, colitis, encephalitis, endocarditis, glomerulonephritis, hepatitis, myocarditis, pancreatitis, pericarditis, reperfusion injury, vasculitis, acute and delayed hypersensitivity, graft rejection, and graft-versus-host disease, auto-immune diseases including Type 1 diabetes mellitus and multiple sclerosis, periodonate diseases, interstitial pulmonary fibrosis, cirrhosis, systemic sclerosis, keloid formation tumors which produce IL-1 as an autocrine growth factor, cachexia, Alzeimer's disease, percussion injury, depression, atherosclerosis, osteoporosis in a mammal, including human.Type: GrantFiled: July 16, 1999Date of Patent: December 26, 2000Assignee: Pfizer IncInventors: Mark Anthony Dombroski, James Frederick Eggler
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Patent number: 6156899Abstract: Novel N-aryl-2-hydroxyalkylamido compounds having the formula (I): ##STR1## are well suited for inducing/stimulating hair growth and/or retarding hair loss and/or for therapeutically treating hyperseborrhea and/or acne.Type: GrantFiled: November 13, 1998Date of Patent: December 5, 2000Assignee: Societe L'Oreal S.A.Inventors: Jean-Baptiste Galey, Odile Destree, Lionel Breton
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Patent number: 6093742Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved in cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: June 27, 1997Date of Patent: July 25, 2000Assignee: Vertex Pharmaceuticals, Inc.Inventors: Francesco Gerald Salituro, Guy W. Bemis, Jeremy Green, James L. Kofron
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Patent number: 6063819Abstract: Neuroprotective drugs are disclosed with at least 3 branches extending outwardly from a center atom or group, each branch having a guanidino group at its terminus. All branches preferably should be identical, and distributed around the center atom or group in a radial manner. Three branches can be bonded to a nitrogen atom, or four branches can be coupled to a carbon atom; other center groups include stable aromatic, cycloalkyl, heterocyclic, or bicyclic structures. Starting reagents are disclosed with a center atom or group, and with reactive groups (such as primary amines or hydroxyl groups) at the ends of short "spacer chains" bonded to the center atom or group. Reagents derived from arginine (an amino acid having a terminal guanidino group) can be bonded to these center components, using protective groups on the arginyl reagents to ensure desired final products with accessible guanidino groups at the ends of spacer chains.Type: GrantFiled: February 18, 1998Date of Patent: May 16, 2000Assignee: Cypros Pharmaceutical Corp.Inventors: Paul J. Marangos, Brian W. Sullivan, Torsten Wiemann, Anne M. Danks, Marina Sragovicz, Lewis R. Makings
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Patent number: 6015921Abstract: A method for preparing carbamoylmethylurea derivatives of the formula (I): ##STR1## characterized by reacting a compound of the formula (II): ##STR2## with a compound of the formula (III): ##STR3##Type: GrantFiled: February 3, 1998Date of Patent: January 18, 2000Assignee: Shionogi & Co., Ltd.Inventors: Haruo Koike, Yasufumi Ueda, Koji Matsuda, Mikio Kabaki
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Patent number: 6005008Abstract: This invention relates to the novel use of phenyl ureas in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: GrantFiled: August 15, 1997Date of Patent: December 21, 1999Assignee: SmithKline Beecham CorporationInventors: Katherine Louisa Widdowson, Daniel Frank Veber, Anthony Joseph Jurewicz, Robert Philip Hertzberg, Melvin Clarence Rutledge, Jr.
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Patent number: 5985881Abstract: The invention relates to new compounds of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein A, B, Z, R.sup.1, R.sup.2, R.sup.3 and m are defined as in the specification, processes for preparing them and pharmaceutical compositions containing these compounds. The compounds are valuable neurokinin (tachykinin) antagonists.Type: GrantFiled: August 2, 1997Date of Patent: November 16, 1999Assignee: Boehringer Ingelheim KGInventors: Horst Dollinger, Gerd Schnorrenberg, Hans Briem, Birgit Jung, Georg Speck
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Patent number: 5925762Type: GrantFiled: September 15, 1997Date of Patent: July 20, 1999Assignee: Boehringer Ingelheim (Canada) Ltd.Inventor: Bounkham Thavonekham
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Patent number: 5919824Abstract: Aminophenol derivatives represented by the following formula (1): ##STR1## wherein X is O or S; A is alkylene, R.sup.1 is phenyl, etc., R.sup.2 and R.sup.3 are H or alkyl; R.sup.4 is substituted carbamoylalkyl, etc.; R.sup.5 is substituted amino, etc.; their salts, and optical isomers of the derivatives and salts. Also disclosed are gastrin receptor antagonists, cholecystokinin receptor antagonists, and medicines for digestive diseases. The compounds have strong binding inhibition against gastrin receptor or CCK-A receptor and also they have higher selectivity to either group of CCK-A receptor or gastrin receptor, and therefore, the compounds are useful for preventing and treating gastrointestinal diseases including peptic ulcers as well as central nervous system diseases.Type: GrantFiled: September 12, 1997Date of Patent: July 6, 1999Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Shuichi Yokohama, Keiichi Kawagoe, Yasuyuki Takeda, Yoshihiro Yokomizo, Aki Yokomizo
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Patent number: 5902899Abstract: Process for preparing 1,3-disubstituted urea of the formula: ##STR1## wherein R.sup.5 is the same as or different from R.sup.6, and each of R.sup.5 and R.sup.6 is independently linear or branched, alkyl of 1-20 carbon atoms, alkenyl group having 2 to 20 carbon atoms or alkynyl group having 2 to 20 carbon atoms, which may have phenoxy, alkoxy of 1-13 carbon atoms, monocycloalkyl of 3-8 carbon atoms, bicycloalkyl of 6-12 carbon atoms, aryl of 6-13 carbon atoms, furyl, pyridyl, or aralkyl of 7-20 carbon atoms, comprising reacting cyclic carbonic acid ester with an amine using alkali metal alkoxide or trialkylamine as base, in safety and high yield.Type: GrantFiled: December 4, 1997Date of Patent: May 11, 1999Assignee: Sumika Fine Chemicals Co., Ltd.Inventors: Taketo Hayashi, Junichi Yasuoka
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Patent number: 5892100Abstract: The present invention provides a method for producing N-acyl carbamate in high yield. The method of the present invention comprises the step of reacting an unsaturated acid halide with a carbamate in the presence of a hindered amine. Another method of the present invention comprises the step of reacting a N,N-diacyl carbamate with an active hydrogen compound.Type: GrantFiled: September 9, 1997Date of Patent: April 6, 1999Assignee: Nippon Paint Co., Ltd.Inventors: Eiji Yamanaka, Masami Yabuta, Satoshi Urano
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Patent number: 5892111Abstract: A cure-accelerator for an epoxy resin, which comprises a compound of the formula (I),R.sub.1 R.sub.2 NCONH--Ar--NECONR.sub.3 R.sub.4 (I)wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are C.sub.1 -C.sub.3 lower alkyl groups which may be the same or different, and Ar is a substituted tolylene group of the formula (II) ##STR1## (wherein R.sub.5 and R.sub.6 are C.sub.1 -C.sub.4 lower alkyl groups which may be the same or different) or a 1,5-naphthylene group.Type: GrantFiled: September 8, 1997Date of Patent: April 6, 1999Assignee: Hodogaya Chemical Co., Ltd.Inventor: Susumu Jinbo
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Patent number: 5872115Abstract: This invention is concerned with 2-ureido-benzamide compounds of the formula (1) ##STR1## in which R.sup.1 is H, halogen atom, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy or (C.sub.1 -C.sub.4)dialkylamino and R.sup.2 is H, halogen atom, hydroxy, nitro, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, (C.sub.3 -C.sub.6) cycloalkylmethoxy, (C.sub.1 -C.sub.4) alkylthio, (C.sub.1 -C.sub.4) alkylsulfinyl, (C.sub.1 -C.sub.4)alkylsulfonyl or ##STR2## wherein j is an integer of from 0 to 2 and R.sup.3 and R.sup.4 are each independently H, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkanoyl, (C.sub.1 -C.sub.4)alkylsulfonyl or (C.sub.1 -C.sub.4)alkylcarbamoyl, NR.sup.3 R.sup.4 can to form a pyrrolidine, piperidine, morpholine, imidazole or pyrazole ring;X is a (C.sub.3 -C.sub.15)alkyl, (C.sub.3 -C.sub.6) cycloalkyl, (C.sub.3 -C.sub.6) cycloalkylmethyl, .omega.-(C.sub.1 -C.sub.4) alkoxy-(C.sub.1 -C.sub.4) alkyl group or ##STR3## wherein k is an integer of from 1 to 4 and R.sup.5 and R.sup.Type: GrantFiled: December 30, 1996Date of Patent: February 16, 1999Assignees: Grelan Pharmaceutical Co. Ltd., Laboratoires Fournier S.C.A.Inventors: Jean Binet, Christian Guffroy, Hirotaka Kasai, Nagatoshi Wagatsuma
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Patent number: 5866609Abstract: Disclosed herein are substituted vinylurea derivatives represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.3 are independently a phenyl group which may be substituted, R.sup.2 is a phenyl group which may be substituted, or a cycloalkyl group, and wave lines mean that the bonding state may be either E or Z, with the proviso that the cases where R.sup.1, R.sup.2 and R.sup.3 are unsubstituted phenyl groups, and where R.sup.1 and R.sup.2 are unsubstituted phenyl groups and R.sup.3 is a 4-ethoxyphenyl group are excluded, or salt thereof, and medicines comprising such a derivative as an active ingredient as well as a method of preventing and treating arteriosclerosis with such a medicine. The derivatives or salts thereof selectively and strongly inhibit ACAT in macrophages and are hence useful as prophylactic and therapeutic agents for arteriosclerosis.Type: GrantFiled: July 24, 1997Date of Patent: February 2, 1999Assignee: SS Pharmaceutical Co., Ltd.Inventors: Yoshihiko Kanamaru, Hiroyuki Hirota, Akihiro Shibata, Teruo Komoto, Hiroyuki Naito, Koichi Tachibana, Mari Ohtsuka, Fumio Ishii, Susumu Sato
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Patent number: 5849732Abstract: Disclosed are a phenol compound represented by the formula (1): ##STR1## wherein R.sup.0 represents H, alkyl or alkyloxy; R.sup.1 represents alkyl; R.sup.2 represents alkyl or alkyloxy; OR.sup.3 represents OH; R.sup.4 represents H, lower alkyl or acyl, each of the above substituents may be substituted; W represents O, S or NR.sup.7 ; where R.sup.7 represents H, alkyl, aryl, OH or alkyloxy, a group of the formula (2): ##STR2## represents an amino which may be mono- or di-substituted or heterocyclic group containing N atom,or a pharmaceutically acceptable salt thereof, and a process for preparing the same.Type: GrantFiled: February 14, 1997Date of Patent: December 15, 1998Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Toshikazu Suzuki, Hiroshi Ohmizu, Yoshimasa Hashimura, Hitoshi Kubota, Keiko Tanaka
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Patent number: 5808151Abstract: There is provided novel biphenylamido derivatives of the formula ##STR1## wherein Z is ##STR2## and Y is H or Z is H and Y is ##STR3## n is 0 or 1; R is C.sub.1-6 alkyl;R.sup.1 is C.sub.1-3 alkyl, C.sub.3-6 cycloalkyl, C.sub.1-4 alkoxymethyl, or NHR.sup.2 ; andR.sup.2 is C.sub.1-3 alkyl or cyclopropylwhich are melatonergic agents and are useful in the treatment of circadian rhythm-related disorders and other conditions affected by melatonin activity.Type: GrantFiled: April 8, 1997Date of Patent: September 15, 1998Assignee: Bristol-Myers Squibb CompanyInventors: James R. Epperson, Joseph P. Yevich
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Patent number: 5753684Abstract: This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More particularly, the invention relates to aromatic guanylhydrazone (more properly termed amidinohydrazone) compositions and their use to inhibit the uptake of arginine by macrophages and/or its conversion to urea. These compositions and methods are also useful in preventing the generation of nitric oxide (NO) by cells, and so to prevent NO-mediated inflammation and other responses in persons in need of same. In another embodiment, the compounds can be used to inhibit arginine uptake in arginine-dependent tumors and infections.Type: GrantFiled: June 6, 1995Date of Patent: May 19, 1998Assignee: The Picower Institute for Medical ResearchInventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
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Patent number: 5750573Abstract: This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More particularly, the invention relates to aromatic guanylhydrazone (more properly termed amidinohydrazone) compositions and their use to inhibit the uptake of arginine by macrophages and/or its conversion to urea. These compositions and methods are also useful in preventing the generation of nitric oxide (NO) by cells, and so to prevent NO-mediated inflammation and other responses in persons in need of same. In another embodiment, the compounds can be used to inhibit arginine uptake in arginine-dependent tumors and infections.Type: GrantFiled: June 5, 1995Date of Patent: May 12, 1998Assignee: The Picower Institute for Medical ResearchInventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
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Patent number: 5739162Abstract: A compound of the formula (I): ##STR1## wherein R.sub.1 is a hydrogen atom or lower alkyl; R.sub.2 is a lower alkoxy, lower alkylamino, lower cycloalkyl, optionally substituted phenyl or optionally substituted heterocyclic group; R.sub.3 is an optionally substituted phenyl; R.sub.4 is an optionally substituted phenyl, optionally substituted cycloalkyl, optionally substituted alkyl or optionally substituted heterocyclic group, or a pharmaceutically acceptable salt thereof, which has a high affinity for gastrin receptors and/or CCK-B receptors but not for CCK-A receptors, and is useful for treating diseases associated with gastrin receptors and/or CCK-B receptors without inducing the side effects associated with CCK-A receptors.Type: GrantFiled: August 9, 1996Date of Patent: April 14, 1998Assignee: Shionogi & Co., Ltd.Inventors: Sanji Hagishita, Susumu Kamata, Yasushi Murakami, Nobuhiro Haga, Yasunobu Ishihara, Toshiro Konoike
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Patent number: 5739398Abstract: A process for preparing N-alkenylureas of the general formula I ##STR1## where R.sup.1 and R.sup.2 are hydrogen, C.sub.1 - to C.sub.40 -alkyl, C.sub.2 - to C.sub.40 -alkenyl, C.sub.3 - to C.sub.20 -cycloalkyl, C.sub.4 - to C.sub.20 -alkylcyc1oalkyl, C.sub.4 - to C.sub.20 -cycloalkylalkyl, aryl, C.sub.7 - to C.sub.20 -alkylaryl or C.sub.7 - to C.sub.20 -aralkyl, or aryl, C.sub.7 - to C.sub.20 -alkylaryl or C.sub.7 - to C.sub.20 -aralkyl which are mono- to pentasubstituted by C.sub.1 - to C.sub.8 -alkyl, C.sub.1 - to C.sub.8 -alkoxy or halogen, together are a C.sub.2 - to C.sub.10 -alkylene chain which is unsubstituted or mono- to hexasubstituted by C.sub.1 - to C.sub.8 -alkyl, andR.sup.3 and R.sup.4 are hydrogen or C.sub.1 - to C.sub.8 -alkyl,by reaction of ureas of the general formula II ##STR2## where R.sup.1 and R.sup.2 have the abovementioned meanings, with an alkenyl carboxylate of the general formula III ##STR3## where R.sup.3 and R.sup.4 have the abovementioned meanings and R.sup.5 is hydrogen, C.sub.Type: GrantFiled: July 3, 1996Date of Patent: April 14, 1998Assignee: BASF AktiengesellschaftInventors: Jochem Henkelmann, Marc Heider, Thomas Ruhl
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Patent number: 5733931Abstract: The present invention provides a cyclohexanediurea derivative, inclusive of its salt, represented by the following formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and they each represent a straight-chain or branched alkyl group having at least 3 carbons, a cycloalkyl group, a cycloalkyl group having a bridge head, a furyl group, a furyl lower alkyl group or an aralkyl group, A.sub.1 and A.sub.2 are the same or different and they each represent a phenyl, pyridyl, quinolyl, isoquinolyl or indolyl group which may have substituents; a process for production thereof; an intermediate thereof; pharmaceutical use, a method for treatment and use thereof.Type: GrantFiled: March 8, 1996Date of Patent: March 31, 1998Assignee: Nissin Food Products Co., Ltd.Inventors: Toshihiro Yamada, Yoichi Nobuhara, Ichinari Takagi, Shiho Furumoto, Kazuhiro Kobayashi, Kiyohito Ikemoto
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Patent number: 5719320Abstract: A cure-accelerator for an epoxy resin, which comprises a compound of the formula (I),R.sub.1 R.sub.2 NCONH--Ar--NHCONR.sub.3 R.sub.4 (I)wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are C.sub.1 -C.sub.3 lower alkyl groups which may be the same or different, and Ar is a substituted tolylene group of the formula (II) ##STR1## wherein R.sub.5 and R.sub.6 are C.sub.1 -C.sub.4 lower alkyl groups which may be the same or different) or a 1,5-naphthylene group.Type: GrantFiled: April 8, 1996Date of Patent: February 17, 1998Assignee: Hodogaya Chemical Co., Ltd.Inventor: Susumu Jinbo
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Patent number: 5712312Abstract: The invention relates to a compound selected from these of formula (I): ##STR1## in which R.sub.7, R.sub.8, Y, n and A are as defined in the description, and medicinal product containing the same useful for treating a disorder of the melatoninergic system.Type: GrantFiled: April 12, 1996Date of Patent: January 27, 1998Assignee: Adir et CompagnieInventors: Michel Langlois, Monique Mathe-Allainmat, Philippe Delagrange, Pierre Renard, Beatrice Guardiola
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Patent number: 5696123Abstract: The invention relates to new compounds of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein A, B, Z, R.sup.1, R.sup.2, R.sup.3 and m are defined as in the specification, processes for preparing them and pharmaceutical compositions containing these compounds. The compounds are valuable neurokinin (tachykinin) antagonists.Type: GrantFiled: June 7, 1995Date of Patent: December 9, 1997Assignee: Boehringer Ingelheim KGInventors: Horst Dollinger, Gerd Schorrenberg, Hans Briem, Birgit Jung, Georg Speck
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Patent number: 5668136Abstract: A benzene, pyridine or pyrimidine derivative having the below shown formula is novel and useful as an anti-arteriosclerotic agent. ##STR1## wherein R.sup.1 stands for a lower alkyl group, an amino group which may be substituted, or the like; R.sup.2 stands for a group represented by the formula: ##STR2## (wherein R.sup.16 stands for an alkyl group having 1 to 6 carbon atoms, or the like) or the like; R.sup.3 stands for a group represented by the formula: --O--(CH.sub.2).sub.m --Y (Y stands for an imidazolyl or piperazinyl group, or the like and m is 1 to 6) or the like; R.sup.5 stands for a hydrogen atom, a lower alkyl group, or the like; A stands for a group represented by the formula: ##STR3## (wherein R.sup.6 stands for a hydrogen atom, a lower alkyl group, or the like), --N.dbd., or the like; and B stands for a group represented by the formula: ##STR4## (wherein R.sup.4 stands for a hydrogen or the like), --N.dbd., or the like.Type: GrantFiled: September 11, 1991Date of Patent: September 16, 1997Assignee: Eisai Co., Ltd.Inventors: Teiji Kimura, Nobuhisa Watanabe, Yasutaka Takase, Kenji Hayashi, Makoto Matsui, Hironori Ikuta, Youji Yamagishi, Kozo Akasaka, Hiroshi Tanaka, Issei Ohtsuka, Takao Saeki, Motoji Kogushi, Tohru Fujimori, Isao Saito
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Patent number: 5658944Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein Ar is a mono- or bicyclic aromatic group optionally containing one or two heteroatoms independently selected from nitrogen, oxygen and sulphur, said group being optionally substituted by one or more atoms or groups independently selected from halogen, nitro, amino, --NRR.sup.1 where R and R.sup.1 are independently selected from hydrogen, C.sub.1-8 alkyl and C.sub.1-8 alkanoyl, cyano, carboxyalkoxy, alkoxycarbonylalkoxy, C.sub.1-8 alkyl (including cycloalkyl and cycloalkylalkyl), C.sub.1-8 alkoxy (including cycloalkoxy and cycloalkylalkoxy), C.sub.Type: GrantFiled: April 14, 1995Date of Patent: August 19, 1997Assignee: The University of South CarolinaInventors: James Mood Chapman, Jr., Roy Lee Hawke, Karl Witold Franzmann, Kevin Julian O'Connor
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Patent number: 5639768Abstract: The invention relates to the compounds of formula (I) wherein the C(.dbd.NH)--NHR.sub.3 group may be in tautomeric or isomeric form, and pharmaceutically acceptable salts thereof, in which: R.sub.1 is amino which is mono- or disubstituted by a substituent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical, an aromatic radical, and a cycloaliphatic hydrocarbon radical or is amino which is disubstituted by a divalent aliphatic hydrocarbon radical or a said radical interrupted by oxygen; R.sub.2 is hydroxy which is etherified by an aliphatic alcohol which is substituted by carboxy, by esterified carboxy or by amidated carboxy; R.sub.3 is hydrogen or an acyl radical which is derived from an organic carbonic acid, an organic carboxylic acid, a sulfonic acid, or a carbamic acid; X.sub.1 and X.sub.3, independently of one another, are oxygen (--O--) or sulphur (--S--); and X.sub.2 is a divalent aliphatic hydrocarbon radical which may be interrupted by an aromatic radical.Type: GrantFiled: July 25, 1995Date of Patent: June 17, 1997Assignee: Ciba-Geigy CorporationInventors: Michael M. Morrissey, Hongsuk Suh
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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: 5614550Abstract: Compounds of formula (I) are provided: ##STR1## wherein: R.sup.1 represents an alkyl group; or a group of formula (II), (III), (IV) or (V): ##STR2## and wherein the groups R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen or various organic groups; and pharmaceutically acceptable salts thereof; as well as methods for the preparation of such compounds and their use in the treatment and prophylaxis of hypercholesteremia and arteriosclerosis.Type: GrantFiled: February 27, 1996Date of Patent: March 25, 1997Assignee: Sankyo Company, LimitedInventors: Akira Yoshida, Koza Oda, Sadao Ishihara, Fujio Saito, Hiroyuki Koike, Teiichiro Koga, Eiichi Kitazawa, Hiroshi Kogen, Ichiro Hayakawa
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Patent number: 5606096Abstract: The present invention provides a process for producing a variety of unsaturated carbamic acid derivatives from corresponding unsaturated carbamates by substitution reaction. The present invention provides a process for producing unsaturated carbamic acid derivatives, comprising reacting an unsaturated carbamate represented by ##STR1## wherein R represents a hydrogen atom or an alkyl group having 1 to 8 carbon atoms, R.sup.1 represents a residue of an alcohol from which an OH group is removed,with an alcohol, a primary or secondary amine or an oxime at a temperature of 80.degree. to 150.degree. C. to substitute the --OR.sup.1 group in the formula (A).Type: GrantFiled: April 3, 1995Date of Patent: February 25, 1997Assignee: Nippon Paint Co., Ltd.Inventors: Eiji Yamanaka, Noriyuki Tsuboniwa, Takao Morimoto, Masamichi Furukawa, Satoshi Urano
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Patent number: 5599984Abstract: This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More particularly, the invention relates to aromatic guanylhydrazone (more properly termed amidinohydrazone) compositions and their use to inhibit the uptake of arginine by macrophages and/or its conversion to urea. These compositions and methods are also useful in preventing the generation of nitric oxide (NO) by cells, and so to prevent NO-mediated inflammation and other responses in persons in need of same. In another embodiment, the compounds can be used to inhibit arginine uptake in arginine-dependent tumors and infections.Type: GrantFiled: September 29, 1994Date of Patent: February 4, 1997Assignee: The Picower Institute For Medical ResearchInventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
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Patent number: 5576410Abstract: A diaminourea compound having the formula (I); ##STR1## wherein R.sub.1 and R.sub.2 are independently a straight or branched alkylene group having 2 to 8 carbon atoms, an alicyclic alkylene group having 6 to 15 carbon atoms, a phenylene group, a C.sub.1 -C.sub.4 alkyl-substituted phenylene group, a C.sub.1 -C.sub.4 mono- or di-alkylene substituted phenylene group, or a methanediphenylene group, and a production process thereof as well as a high heat resistant polyurethaneurea derived therefrom and a production process thereof.Type: GrantFiled: January 25, 1995Date of Patent: November 19, 1996Assignee: Asahi Kasei Kogyo Kabushiki KaishaInventors: Akihiko Yosizato, Satoshi Furubeppu
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Patent number: 5534529Abstract: Compounds of formula (I) are provided: ##STR1## wherein: R.sup.1 represents an alkyl group; or a group of formula (II), (III), (IV) or (V): ##STR2## and wherein the groups R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen or various organic groups; and pharmaceutically acceptable salts thereof; as well as methods for the preparation of such compounds and their use in the treatment and prophylaxis of hypercholesteremia and arteriosclerosis.Type: GrantFiled: June 28, 1994Date of Patent: July 9, 1996Assignee: Sankyo Company, LimitedInventors: Akira Yoshida, Koza Oda, Sadao Ishihara, Takashi Kasai, Fujio Saito, Hiroyuki Koike, Teiichiro Koga, Eiichi Kitazawa, Hiroshi Kogen, Ichiro Hayakawa
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Patent number: 5530026Abstract: The present invention is concerned with novel anticancer agents having potent antineoplastic activity without systemic toxicity and mutagenicity. The novel anticancer agents of the present invention are derivatives of formula I: ##STR1## wherein: A is O or NH; andB is an aryl group selected from the group consisting of phenyl, indane, fluorene, indazole, indole, and pyridine, the aryl group being substituted with at least one substituent selected from the group consisting of hydrogen, C.sub.1-16 alkyl optionally substituted with one or more OH or SH, lower alkoxy, C.sub.3-6 cycloalkyl, lower alkylthio, nitro, cyano, lower alkene, lower alkyne, OH, SH, carboxy lower alkyl, carboxy lower alkyl esters, amino, N-lower alkyl, N,N-dilower alkyl and halogen;or a prodrug thereof, with the provisos that when A is NH and B is phenyl:a) B is substituted with at least one substituent other than hydrogen;b) B is not:1) mono-substituted in the 4 position with C.sub.1-2 alkyl, tert-butyl or n-butyl, halogen, OH, carboxy C.Type: GrantFiled: January 6, 1995Date of Patent: June 25, 1996Assignee: Universite LavalInventors: Rene C. Gaudreault, Patrick Poyet
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Patent number: 5510432Abstract: Isocyanate prepolymers based on an aromatic diisocyanate and a polyether polyol in which at least 95% of the isocyanate groups are blocked by blocking agents selected fromA) about 50 to about 97 equivalent % of a phenol or substituted phenol,B) about 30 to about 50 equivalent % of a pyrazole or a substituted pyrazole andC) 0 to about 10 equivalent % of a blocking agent different from A) and B).These blocked isocyanate prepolymers are particularly useful for the production of flexible epoxy resin systems.Type: GrantFiled: May 31, 1995Date of Patent: April 23, 1996Assignee: Bayer AktiengesellschaftInventors: Lutz Schmalstieg, Rainer Rettig, Eberhard Konig