Benzene Ring Bonded Directly To Urea Nitrogen (i.e., Anilides) Patents (Class 564/48)
  • Patent number: 6391917
    Abstract: 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: Grant
    Filed: April 19, 2001
    Date of Patent: May 21, 2002
    Assignee: ZymoGenetics, Inc.
    Inventors: Charles R. Petrie, Patricia A. McKernan, Emma E. Moore, John M. Ostresh, Jean-Philippe Meyer, Richard A. Houghten, Clemencia Pinilla
  • Publication number: 20020052417
    Abstract: The present invention relates to compounds of the formula I, 1
    Type: Application
    Filed: June 6, 2001
    Publication date: May 2, 2002
    Inventors: Otmar Klingler, Manfred Schudok, Hans-Peter Nestler, Hans Matter, Herman Schreuder
  • Patent number: 6380392
    Abstract: 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: Grant
    Filed: June 29, 2000
    Date of Patent: April 30, 2002
    Assignee: The Penn State Research Foundation
    Inventor: Xumu Zhang
  • Publication number: 20020049352
    Abstract: The present invention relates to a scaleable process for the oxidation of carbon-boron bonds with Oxone®.
    Type: Application
    Filed: June 25, 2001
    Publication date: April 25, 2002
    Inventors: Weiling Cai, David H. Ripin
  • Patent number: 6372933
    Abstract: 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: Grant
    Filed: February 27, 2001
    Date of Patent: April 16, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: Neil H. Baine, Ann Marie Eldridge, Marvin Sungwhan Yu
  • Publication number: 20020038025
    Abstract: The present invention relates to compounds of formula (I) 1
    Type: Application
    Filed: July 16, 2001
    Publication date: March 28, 2002
    Inventors: Jean Ackermann, Johannes Aebi, Alexander Chucholowski, Henrietta Dehmlow, Olivier Morand, Sabine Wallbaum, Thomas Weller
  • Patent number: 6362229
    Abstract: 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: Grant
    Filed: August 17, 2000
    Date of Patent: March 26, 2002
    Assignee: Influx, Inc.
    Inventors: Penelope N. Markham, Debbie C. Mulhearn, Alexander A. Neyfakh, David Crich, Mohamad-Rami Jaber, Michael E. Johnson
  • Patent number: 6333432
    Abstract: 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: Grant
    Filed: May 1, 2000
    Date of Patent: December 25, 2001
    Inventors: Gina M. Fitzpatrick, Ann B. Orth, Maurice C. H. Yap, Richard B. Rogers, Todd L. Werk, George E. Davis
  • Patent number: 6294694
    Abstract: Peptoid compounds of Formula I and Formula II are disclosed The compounds are useful in the treatment of matrix metalloproteinase-mediated disorders.
    Type: Grant
    Filed: June 4, 1999
    Date of Patent: September 25, 2001
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Donald T. Witiak, Paul J. Bertics, Yingsheng Zhang
  • Patent number: 6255351
    Abstract: 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: Grant
    Filed: September 30, 1999
    Date of Patent: July 3, 2001
    Assignee: ZymoGenetics, Inc.
    Inventors: Charles R. Petrie, Patricia A. McKernan, Emma E. Moore, John M. Ostresh, Jean-Philippe Meyer, Richard A. Houghten, Clemencia Pinilla
  • Patent number: 6221913
    Abstract: 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: Grant
    Filed: January 20, 1999
    Date of Patent: April 24, 2001
    Assignee: ZymoGenetics, Inc.
    Inventors: Charles R. Petrie, Patricia A. McKernan, Emma E. Moore, John M. Ostresh, Jean-Philippe Meyer, Richard A. Houghten, Clemencia Pinilla
  • Patent number: 6218389
    Abstract: 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: Grant
    Filed: July 31, 1998
    Date of Patent: April 17, 2001
    Assignee: 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
  • Patent number: 6214881
    Abstract: 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: Grant
    Filed: February 9, 1999
    Date of Patent: April 10, 2001
    Assignee: SmithKline Beecham Corporation
    Inventor: Jia-Ning Xiang
  • Patent number: 6197798
    Abstract: 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 op
    Type: Grant
    Filed: July 20, 1999
    Date of Patent: March 6, 2001
    Assignee: Novartis AG
    Inventors: Cynthia A. Fink, Gary M. Ksander, Paivi J. Kukkola, Eli M. Wallace, Mahavir Prashad
  • Patent number: 6180676
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: January 30, 2001
    Assignee: The Picower Institute for Medical Research
    Inventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
  • Patent number: 6166064
    Abstract: 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: Grant
    Filed: July 16, 1999
    Date of Patent: December 26, 2000
    Assignee: Pfizer Inc
    Inventors: Mark Anthony Dombroski, James Frederick Eggler
  • Patent number: 6156899
    Abstract: 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: Grant
    Filed: November 13, 1998
    Date of Patent: December 5, 2000
    Assignee: Societe L'Oreal S.A.
    Inventors: Jean-Baptiste Galey, Odile Destree, Lionel Breton
  • Patent number: 6093742
    Abstract: 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: Grant
    Filed: June 27, 1997
    Date of Patent: July 25, 2000
    Assignee: Vertex Pharmaceuticals, Inc.
    Inventors: Francesco Gerald Salituro, Guy W. Bemis, Jeremy Green, James L. Kofron
  • Patent number: 6063819
    Abstract: 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: Grant
    Filed: February 18, 1998
    Date of Patent: May 16, 2000
    Assignee: Cypros Pharmaceutical Corp.
    Inventors: Paul J. Marangos, Brian W. Sullivan, Torsten Wiemann, Anne M. Danks, Marina Sragovicz, Lewis R. Makings
  • Patent number: 6015921
    Abstract: 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: Grant
    Filed: February 3, 1998
    Date of Patent: January 18, 2000
    Assignee: Shionogi & Co., Ltd.
    Inventors: Haruo Koike, Yasufumi Ueda, Koji Matsuda, Mikio Kabaki
  • Patent number: 6005008
    Abstract: 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: Grant
    Filed: August 15, 1997
    Date of Patent: December 21, 1999
    Assignee: SmithKline Beecham Corporation
    Inventors: Katherine Louisa Widdowson, Daniel Frank Veber, Anthony Joseph Jurewicz, Robert Philip Hertzberg, Melvin Clarence Rutledge, Jr.
  • Patent number: 5985881
    Abstract: 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: Grant
    Filed: August 2, 1997
    Date of Patent: November 16, 1999
    Assignee: Boehringer Ingelheim KG
    Inventors: Horst Dollinger, Gerd Schnorrenberg, Hans Briem, Birgit Jung, Georg Speck
  • Patent number: 5925762
    Type: Grant
    Filed: September 15, 1997
    Date of Patent: July 20, 1999
    Assignee: Boehringer Ingelheim (Canada) Ltd.
    Inventor: Bounkham Thavonekham
  • Patent number: 5919824
    Abstract: 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: Grant
    Filed: September 12, 1997
    Date of Patent: July 6, 1999
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Shuichi Yokohama, Keiichi Kawagoe, Yasuyuki Takeda, Yoshihiro Yokomizo, Aki Yokomizo
  • Patent number: 5902899
    Abstract: 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: Grant
    Filed: December 4, 1997
    Date of Patent: May 11, 1999
    Assignee: Sumika Fine Chemicals Co., Ltd.
    Inventors: Taketo Hayashi, Junichi Yasuoka
  • Patent number: 5892100
    Abstract: 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: Grant
    Filed: September 9, 1997
    Date of Patent: April 6, 1999
    Assignee: Nippon Paint Co., Ltd.
    Inventors: Eiji Yamanaka, Masami Yabuta, Satoshi Urano
  • Patent number: 5892111
    Abstract: 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: Grant
    Filed: September 8, 1997
    Date of Patent: April 6, 1999
    Assignee: Hodogaya Chemical Co., Ltd.
    Inventor: Susumu Jinbo
  • Patent number: 5872115
    Abstract: 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: Grant
    Filed: December 30, 1996
    Date of Patent: February 16, 1999
    Assignees: Grelan Pharmaceutical Co. Ltd., Laboratoires Fournier S.C.A.
    Inventors: Jean Binet, Christian Guffroy, Hirotaka Kasai, Nagatoshi Wagatsuma
  • Patent number: 5866609
    Abstract: 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: Grant
    Filed: July 24, 1997
    Date of Patent: February 2, 1999
    Assignee: SS Pharmaceutical Co., Ltd.
    Inventors: Yoshihiko Kanamaru, Hiroyuki Hirota, Akihiro Shibata, Teruo Komoto, Hiroyuki Naito, Koichi Tachibana, Mari Ohtsuka, Fumio Ishii, Susumu Sato
  • Patent number: 5849732
    Abstract: 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: Grant
    Filed: February 14, 1997
    Date of Patent: December 15, 1998
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Toshikazu Suzuki, Hiroshi Ohmizu, Yoshimasa Hashimura, Hitoshi Kubota, Keiko Tanaka
  • Patent number: 5808151
    Abstract: 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: Grant
    Filed: April 8, 1997
    Date of Patent: September 15, 1998
    Assignee: Bristol-Myers Squibb Company
    Inventors: James R. Epperson, Joseph P. Yevich
  • Patent number: 5753684
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: May 19, 1998
    Assignee: The Picower Institute for Medical Research
    Inventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
  • Patent number: 5750573
    Abstract: 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: Grant
    Filed: June 5, 1995
    Date of Patent: May 12, 1998
    Assignee: The Picower Institute for Medical Research
    Inventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
  • Patent number: 5739162
    Abstract: 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: Grant
    Filed: August 9, 1996
    Date of Patent: April 14, 1998
    Assignee: Shionogi & Co., Ltd.
    Inventors: Sanji Hagishita, Susumu Kamata, Yasushi Murakami, Nobuhiro Haga, Yasunobu Ishihara, Toshiro Konoike
  • Patent number: 5739398
    Abstract: 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: Grant
    Filed: July 3, 1996
    Date of Patent: April 14, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Jochem Henkelmann, Marc Heider, Thomas Ruhl
  • Patent number: 5733931
    Abstract: 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: Grant
    Filed: March 8, 1996
    Date of Patent: March 31, 1998
    Assignee: Nissin Food Products Co., Ltd.
    Inventors: Toshihiro Yamada, Yoichi Nobuhara, Ichinari Takagi, Shiho Furumoto, Kazuhiro Kobayashi, Kiyohito Ikemoto
  • Patent number: 5719320
    Abstract: 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: Grant
    Filed: April 8, 1996
    Date of Patent: February 17, 1998
    Assignee: Hodogaya Chemical Co., Ltd.
    Inventor: Susumu Jinbo
  • Patent number: 5712312
    Abstract: 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: Grant
    Filed: April 12, 1996
    Date of Patent: January 27, 1998
    Assignee: Adir et Compagnie
    Inventors: Michel Langlois, Monique Mathe-Allainmat, Philippe Delagrange, Pierre Renard, Beatrice Guardiola
  • Patent number: 5696123
    Abstract: 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: Grant
    Filed: June 7, 1995
    Date of Patent: December 9, 1997
    Assignee: Boehringer Ingelheim KG
    Inventors: Horst Dollinger, Gerd Schorrenberg, Hans Briem, Birgit Jung, Georg Speck
  • Patent number: 5668136
    Abstract: 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: Grant
    Filed: September 11, 1991
    Date of Patent: September 16, 1997
    Assignee: 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
  • Patent number: 5658944
    Abstract: 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: Grant
    Filed: April 14, 1995
    Date of Patent: August 19, 1997
    Assignee: The University of South Carolina
    Inventors: James Mood Chapman, Jr., Roy Lee Hawke, Karl Witold Franzmann, Kevin Julian O'Connor
  • Patent number: 5639768
    Abstract: 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: Grant
    Filed: July 25, 1995
    Date of Patent: June 17, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: Michael M. Morrissey, Hongsuk Suh
  • Patent number: 5621010
    Abstract: 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: Grant
    Filed: May 18, 1994
    Date of Patent: April 15, 1997
    Assignee: 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
  • Patent number: 5614550
    Abstract: 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: Grant
    Filed: February 27, 1996
    Date of Patent: March 25, 1997
    Assignee: Sankyo Company, Limited
    Inventors: Akira Yoshida, Koza Oda, Sadao Ishihara, Fujio Saito, Hiroyuki Koike, Teiichiro Koga, Eiichi Kitazawa, Hiroshi Kogen, Ichiro Hayakawa
  • Patent number: 5606096
    Abstract: 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: Grant
    Filed: April 3, 1995
    Date of Patent: February 25, 1997
    Assignee: Nippon Paint Co., Ltd.
    Inventors: Eiji Yamanaka, Noriyuki Tsuboniwa, Takao Morimoto, Masamichi Furukawa, Satoshi Urano
  • Patent number: 5599984
    Abstract: 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: Grant
    Filed: September 29, 1994
    Date of Patent: February 4, 1997
    Assignee: The Picower Institute For Medical Research
    Inventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
  • Patent number: 5576410
    Abstract: 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: Grant
    Filed: January 25, 1995
    Date of Patent: November 19, 1996
    Assignee: Asahi Kasei Kogyo Kabushiki Kaisha
    Inventors: Akihiko Yosizato, Satoshi Furubeppu
  • Patent number: 5534529
    Abstract: 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: Grant
    Filed: June 28, 1994
    Date of Patent: July 9, 1996
    Assignee: Sankyo Company, Limited
    Inventors: Akira Yoshida, Koza Oda, Sadao Ishihara, Takashi Kasai, Fujio Saito, Hiroyuki Koike, Teiichiro Koga, Eiichi Kitazawa, Hiroshi Kogen, Ichiro Hayakawa
  • Patent number: 5530026
    Abstract: 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: Grant
    Filed: January 6, 1995
    Date of Patent: June 25, 1996
    Assignee: Universite Laval
    Inventors: Rene C. Gaudreault, Patrick Poyet
  • Patent number: 5510432
    Abstract: 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: Grant
    Filed: May 31, 1995
    Date of Patent: April 23, 1996
    Assignee: Bayer Aktiengesellschaft
    Inventors: Lutz Schmalstieg, Rainer Rettig, Eberhard Konig