Carbocyclic Ring Containing Patents (Class 544/321)
  • Patent number: 6156772
    Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
    Type: Grant
    Filed: May 14, 1999
    Date of Patent: December 5, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Mark Goulet, Thomas F. Walsh, Feroze Ujjainwalla, Matthew J. Wyvratt, Jr.
  • Patent number: 6153619
    Abstract: There are provided compositions and methods comprising compounds of formula I: ##STR1## wherein R.sup.1, A, B, X, Y and Z have the meaning given in claim 1, for the control of insect and acarid pests.
    Type: Grant
    Filed: March 22, 1999
    Date of Patent: November 28, 2000
    Assignee: American Cyanamid Company
    Inventors: William Wakefield Wood, Linda Fleming, Salvatore John Cuccia
  • Patent number: 6136971
    Abstract: The present invention provides a process for preparing 1,2-diheteroethylene sulfonamide of the formula: ##STR1## by reacting a pyrimidine monohalide of the formula: ##STR2## with a mono-protected 1,2-diheteroethylene anion of the formula M.sub.1 XCH.sub.2 CH.sub.2 YR.sub.5 and removing the protecting group, wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, Z, X, Y, M, M.sub.1 and W are defined herein.
    Type: Grant
    Filed: July 15, 1999
    Date of Patent: October 24, 2000
    Assignee: Roche Colorado Corporation
    Inventors: Peter J. Harrington, Hiralal N. Khatri, Bradley S. Dehoff
  • Patent number: 6111102
    Abstract: Compounds of the formula I or salts thereof, in whichX is oxygen, --O--NR.sup.2 -- or --SO.sub.2 --NR.sup.2 --, and Y is N or CH,R.sup.1 is (C.sub.1 -C.sub.6)alkyl, (C.sub.2 -C.sub.6)alkenyl or (C.sub.2 -C.sub.6)alkynyl, which are in each case optionally substituted, or, in the case where X=oxygen, also (subst.) phenyl,R.sup.2 is H, (C.sub.1 -C.sub.6)alkyl, (C.sub.2 -C.sub.6)alkenyl or -alkynyl or (C.sub.3 -C.sub.6)cycloalkyl,R.sup.3 and R.sup.4 are H, (subst.) (C.sub.1 -C.sub.4)alkyl or (subst.) (C.sub.1 -C.sub.4)alkoxy or halogen, (C.sub.1 -C.sub.4)alkylthio, (C.sub.1 -C.sub.4)-alkylamino or di[(C.sub.1 -C.sub.4)alkyl]-amino,R.sup.5 is H or (C.sub.1 -C.sub.4)alkyl and R.sup.6 is hydrogen,may be prepared by reacting compounds of the formula II,R.sup.1 --X--R.sup.7 (II)with compounds of the formulae III, IV and VR.sup.8 --OCN (III)SO.sub.2 Cl.sub.2 (IV) ##STR1## where R.sup.7 and R.sup.8 are H, a quarternary ammonium ion or one equivalent of a metal cation.
    Type: Grant
    Filed: March 2, 1999
    Date of Patent: August 29, 2000
    Assignee: Hoechst Aktiengesellschaft
    Inventor: Gunter Schlegel
  • Patent number: 6110925
    Abstract: The present invention is directed to anti-bacterial and anti-tumor agents and the synthesis thereof.
    Type: Grant
    Filed: August 6, 1998
    Date of Patent: August 29, 2000
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Robert M. Williams, Chenguang Yuan
  • Patent number: 6096753
    Abstract: Selected novel substituted pyrimidinone and pyridone compounds are effective for prophylaxis and treatment of diseases, such as TNF-.alpha., IL-1.beta., IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: December 4, 1997
    Date of Patent: August 1, 2000
    Assignee: Amgen Inc.
    Inventors: Ulrike D. Spohr, Michael J. Malone, Nathan B. Mantlo
  • Patent number: 6093718
    Abstract: This invention concerns heterocyclic derivatives which are useful in inhibiting oxido-squalene cyclase, processes for their preparation and pharmaceutical compositions containing them. The present invention is also concerned with heterocyclic derivatives capable of inhibiting cholesterol biosynthesis and hence in lowering cholesterol levels in blood plasma. The present invention also relates to methods of using such heterocyclic derivatives in diseases and medical conditions such as hypercholesterolemia and atherosclerosis.
    Type: Grant
    Filed: February 12, 1999
    Date of Patent: July 25, 2000
    Assignee: Zeneca Limited
    Inventors: David Waterson, Elaine Sophie Elizabeth Stokes, George Robert Brown, Nicholas John Newcombe
  • Patent number: 6057325
    Abstract: This invention concerns the compounds of formula ##STR1## the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Alk is C.sub.1-6 alkanediyl; R.sup.1 is hydrogen, C.sub.1-6 alkyl, aryl or aryl C.sub.1-6 alkyl; R.sup.2, R.sup.3 and R.sup.4 are each independently selected from hydrogen, halo, hydroxy, nitro, cyano, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, trifluoromethyl, C.sub.1-6 alkylthio, mercapto, amino, mono- and di(C.sub.1-6 alkyl)amino, carboxyl, C.sub.1-6 alkyloxycarbonyl or C.sub.1-6 alkylcarbonyl; R.sup.5 is hydrogen, C.sub.1-6 alkyl, phenyl or phenylC.sub.1-6 alkyl; R.sup.6 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylthio, or a radical of formula --NR.sup.8 R.sup.9, wherein R.sup.8 and R.sup.9 are each independently selected from hydrogen, C.sub.1-6 alkyl, phenyl or phenylC.sub.1-6 alkyl; R.sup.7 is hydrogen or C.sub.1-6 alkyl; or R.sup.6 and R.sup.7 taken together may form a bivalent radical of formula --R.sup.6 --R.sup.
    Type: Grant
    Filed: November 9, 1998
    Date of Patent: May 2, 2000
    Assignee: Janssen Pharmaceutia, N.V.
    Inventors: Ludo Edmond Josephine Kennis, Josephus Carolus Mertens
  • Patent number: 6048866
    Abstract: Compounds of formula (1) are described: ##STR1## and the salts, solvates, hydrates and N-oxides thereof, in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 have the meanings given in claim 1. The compounds are selective inhibitors of protein kinases, especially src-family protein kinases and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to have a role.
    Type: Grant
    Filed: March 13, 1998
    Date of Patent: April 11, 2000
    Assignee: Celltech Therapeutics, Limited
    Inventors: Martin Clive Hutchings, Peter David Davis, David Festus Charles Moffat
  • Patent number: 6040315
    Abstract: Herein is disclosed how to make and to use a nonmetallic antacid composition which is the product of the co-polymerization of guanidine and polyethylenimine. The resultant polymer is useful as an antacid.
    Type: Grant
    Filed: October 29, 1998
    Date of Patent: March 21, 2000
    Inventor: Charles E. Day
  • Patent number: 6028073
    Abstract: N-substitued 3-azabicyclo[3.2.0]heptane derivatives of formula (I) ##STR1## in which R.sup.1, R.sup.2, A, X, Y and Z have the meanings given in the description, their method of preparation and their use as pharmacological agents.
    Type: Grant
    Filed: September 18, 1998
    Date of Patent: February 22, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Gerd Steiner, Rainer Munschauer, Thomas Hoger, Liliane Unger, Hans-Jurgen Teschendorf
  • Patent number: 6013651
    Abstract: The present invention is directed to compounds of the formula ##STR1## and pharmaceutically acceptable salts and isomers thereof.
    Type: Grant
    Filed: March 4, 1998
    Date of Patent: January 11, 2000
    Assignee: G. D. Searle & Co.
    Inventors: Thomas E. Rogers, Peter G. Ruminski
  • Patent number: 6008351
    Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
    Type: Grant
    Filed: December 18, 1995
    Date of Patent: December 28, 1999
    Assignee: Corvas International, Inc.
    Inventors: Susan Yoshiko Tamura, Joseph Edward Semple, William Charles Ripka, Robert John Ardecky, Yu Ge, Stephen H. Carpenter, Terence K. Brunck, Marguerita S. L. Lim-Wilby, Ruth F. Nutt, Matthew M. Abelman
  • Patent number: 5972949
    Abstract: There are disclosed novel ether compounds of the general formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are each hydrogen or the like; A is a group of the general formula: ##STR2## B is a group of the general formula: ##STR3## and X is oxygen or sulfur; and harmful-organism controlling agents containing them as active ingredients.
    Type: Grant
    Filed: October 16, 1998
    Date of Patent: October 26, 1999
    Assignee: Sumito Chemical Co., Ltd.
    Inventors: Akira Shuto, Hirosi Kisida, Toru Tsuchiya, Yoji Takada, Hiroaki Fujimoto
  • Patent number: 5958934
    Abstract: The aryl pyrimidine derivatives and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, including utility as selective 5HT.sub.2B -antagonists. The 5-HT.sub.2B antagonist is a compound of the formula: ##STR1## wherein: R.sup.1 is hydrogen, alkyl, lower alkoxy, hydroxyalkyl, cycloalkyl, cycloalkyl lower alkyl, alkenyl, lower thioalkoxy, halo, fluoroalkyl, --NR.sup.6 R.sup.7, --CO.sub.2 R.sup.8, --O(CH.sub.2).sub.n R.sup.9, or lower alkyl optionally substituted with hydroxy, alkoxy, halo, or aryl; in whichn is 1, 2, or 3;R.sup.6 and R.sup.7 are hydrogen or lower alkyl;R.sup.8 is hydrogen or lower alkyl; andR.sup.9 is hydrogen, lower alkyl, hydroxy, hydroxy lower alkyl, lower alkenyl, or lower alkoxy;R.sup.2 is hydrogen, lower alkyl, lower alkoxy, halo, or lower fluoroalkyl;R.sup.3 is optionally substituted aryl other than pyridyl, thienyl, or furanyl;R.sup.4 is hydrogen, lower alkyl, cycloalkyl, alkenyl, acyl, amino, amido, aryl, --(CH.sub.2).sub.m NR.sup.10 R.sup.
    Type: Grant
    Filed: November 21, 1997
    Date of Patent: September 28, 1999
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jacob Berger, Lee Allen Flippin, Robert Greenhouse, Saul Jaime-Figueroa, Yanzhou Liu, Aubry Kern Miller, David George Putman, Klaus Kurt Weinhardt, Shu-Hai Zhao
  • Patent number: 5945427
    Abstract: The present invention is directed to derivatives of 5-thia- and 5-selenopyrimidinone are useful as inhibitors of the enzyme glycimide ribonucleotide formyl transferase (GARFT) and amino imidozole carboxamide ribonucleotide formyl transferase (AICARFT), pharmaceutical compositions containing these derivatives, and methods of using these derivatives. The present invention is also directed to intermediates useful for preparing these derivatives and methods of preparing these intermediates.
    Type: Grant
    Filed: January 6, 1998
    Date of Patent: August 31, 1999
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Michael D. Varney, William H. Romines, Cynthia L. Palmer, Judith G. Deal
  • Patent number: 5945426
    Abstract: A pharmaceutical composition comprising a compound of the following general formula ?I! or its salt. ##STR1## wherein R.sup.1 represents aryl or a heteroaromatic group. R.sup.2 represents hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, hydroxyalkyl, haloalkyl, alkoxy, alkylthio, amino, monoalkylamino, dialkylamino, or phenyl. R.sup.3 and R.sup.4 independently represent hydrogen or alkyl or R.sup.3 and R.sup.4 taken together with the adjacent N atom represent a 5- through 7-membered cyclic amino group. A represents C.sub.2-10 alkylene. W represents O, S, or (CH).sub.n (where CH may be substituted by alkyl; n is an integer of 1 or 2). X, Y, and Z may be the same or different and each represents CH (which may be substituted by alkyl), or N. Provided, however, that the case in which X, Y, and Z concurrently represent CH is excluded. The compound of the invention has excellent neuronal death inhibitory activity and is useful as a therapeutic drug for cerebrovascular diseases.
    Type: Grant
    Filed: March 7, 1997
    Date of Patent: August 31, 1999
    Assignee: Nippon Shinyaku Co., Ltd.
    Inventors: Shoichi Chokai, Yojiro Ukai, Tomiyoshi Aoki, Kyoichi Ideguchi
  • Patent number: 5936085
    Abstract: Disclosed and claimed is a process for the preparation of a carbamate (IV)Ar--O--CO--NR--B (IV)by reaction of a saltM.sup..sym. .crclbar.NR--B (II-S)with a diaryl carbonate(ArO).sub.2 CO (III).The carbamate can be reacted, without any necessity of intermediate isolation, with a sulfonamide A--SO.sub.2 NH.sub.2 (V) to give a sulfonylurea (I) or salts thereofA--SO.sub.2 --NH--CO--NR--B (I).And thus, disclosed and claimed too is a process for the preparation of sulfonylurea (I) by (i) contacting a salt (II-S) with a diaryl carbonate (III) to form a carbamate (IV), and (ii) contacting carbamate (IV) from step (i) with or without intermediate isolation, with a sulfonamide (V). These processes avoid the use of alkali metal hydrides as a base. And, these processes can additionally include the preparation of salt (II-S) from a compound H--NR--B (II) and base M.sup..sym. Base.sup..crclbar..
    Type: Grant
    Filed: July 11, 1996
    Date of Patent: August 10, 1999
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Gerhard Schnabel, Harald Knorr, Klemens Minn, Jan Vermehren
  • Patent number: 5935973
    Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R.sub.1 is an optional substituent; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents CO.HET, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.
    Type: Grant
    Filed: January 5, 1998
    Date of Patent: August 10, 1999
    Assignee: Knoll Aktiengesellschaft
    Inventors: Alan Martin Birch, David John Heal, Frank Kerrigan, Keith Frank Martin, Patricia Lesley Needham, Bruce Jeremy Sargent
  • Patent number: 5922646
    Abstract: Acylated aminophenylsulfonylureas, processes for their preparation and their use as herbicides and plant growth regulators. Compounds of the formula (I) and salts thereof ##STR1## in which W.sup.1, W.sup.2, R, n, R.sup.1, R.sup.2, R.sup.4, X, Y and Z are as defined in claim 1 and R.sup.3 is an acyl radical, are suitable as herbicides and plant growth regulators. The herbicides can be prepared by the process variants from claim 5, the novel intermediate products (II), (IV), (VI) and (VIII)* of claims 9 and 10 being employed.
    Type: Grant
    Filed: August 4, 1997
    Date of Patent: July 13, 1999
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer
  • Patent number: 5922645
    Abstract: Compounds of the formula (I) and salts thereof ##STR1## in which R.sup.1 to R.sup.6, W, X, Y and Z are defined as in claim 1, have herbicidal or plant growth-regulatory properties.They can be prepared by processes analogous to known processes (cf. claim 5), in some cases via novel intermediate products (cf.
    Type: Grant
    Filed: November 22, 1995
    Date of Patent: July 13, 1999
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Heinz Kehne, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
  • Patent number: 5919792
    Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.
    Type: Grant
    Filed: October 28, 1997
    Date of Patent: July 6, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, George D. Hartman, William F. Hoffman, Nathan C. Ihle
  • Patent number: 5912350
    Abstract: Disclosed are compounds of the formula: ##STR1## where S and V are various organic or inorganic substituents;G and K are the same or different and represent N or CR' where R' is an organic or inorganic substituent;R is hydrogen or an alkyl group;R.sub.1, X, Y, Z and T are organic or inorganic substituents; andR.sub.2 and R.sub.3 represent hydrogen or organic substituents; orNR.sub.2 R.sub.3 together represents a heterocyclic ring system;and the pharmaceutically acceptable salts thereof; which are highly selective partial agonists or antagonists at brain dopamine receptor subtypes and, thus, are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
    Type: Grant
    Filed: October 8, 1997
    Date of Patent: June 15, 1999
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Andrew Thurkauf
  • Patent number: 5912252
    Abstract: The subject invention concerns compounds of formula (I): whereinn=1 or 2;R.sup.1 is H, NH.sub.2 or halogen;R.sup.2 is H or NH.sub.2 ;R.sup.3 represents the group CR.sup.6 R.sup.7 R.sup.8 where R.sup.6, R.sup.7 and R.sup.8 are the same or different and are each H, C.sub.1-6 alkyl or C.sub.1-6 haloalkyl;R.sup.4 and R.sup.5 are the same or different and are selected from the group consisting of H, CO.sub.2 H, CO.sub.2 C.sub.1-6, NHSO.sub.2 CF.sub.3, tetrazole and (CR.sup.9 R.sup.10).sub.p (Y).sub.q (CR.sup.9 R.sup.10).sub.t Z where (CR.sup.9 R.sup.10), or (CR.sup.9 R.sup.10).sub.t is straight or branched chain bearing the substituents R.sup.9 and R.sup.10 when p or t>1;R.sup.9 and R.sup.10 are the same or different and are each C.sub.0-6 alkyl-Z;p=1-3;q=0 or 1;t=0-4, provided that t>0 when q=1;Y=O, NH or S(O).sub.m where m=0-2; andZ is selected from a group consisting of H, CN, CO.sub.2 H, CO.sub.2 C.sub.1-6 alkyl, NHSO.sub.2 CF.sub.3 tetrazole, triazole, CONH.sub.2, CON(C.sub.1-6 alkyl).sub.2, CONH(C.sub.
    Type: Grant
    Filed: May 19, 1997
    Date of Patent: June 15, 1999
    Assignee: Darwin Discovery Limited
    Inventors: Steven Colin Beasley, John Gary Montana
  • Patent number: 5908844
    Abstract: Compounds of the formula I ##STR1## where B, R.sup.1, R.sup.2, n, R.sup.3, A, X, Y and Z have the meanings stated in the description, and their preparation are described. The novel ompounds are suitable for controlling diseases.
    Type: Grant
    Filed: May 6, 1996
    Date of Patent: June 1, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Gerd Steiner, Rainer Munschauer, Liliane Unger, Hans-Jurgen Teschendorf, Thomas Hoger
  • Patent number: 5886176
    Abstract: The invention relates to a novel process for preparing herbicidal sulphonylurea salts of the formula (I) ##STR1## in which M.sup.+ represents an alkali metal ion or an alkaline earth metal ion equivalent,Z represents N, CH or C-halogen,R.sup.1 represents in each case optionally substituted aryl, aralkyl or heteroaryl,(where R.sup.2, X and Y have the meanings given in the description).
    Type: Grant
    Filed: March 1, 1993
    Date of Patent: March 23, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventor: Klaus-Helmut Muller
  • Patent number: 5883092
    Abstract: The present invention is directed to a pyrimidine derivative of the following formula (1) or a salt of the derivative: ##STR1## ?wherein R.sup.1 represents a hydroxyl group, a lower alkoxy group, a phenyloxy group which may have a substituent, an aralkyloxy group which may have a substituent, or --NR.sup.2 R.sup.3 ; X represents an oxygen atom or N--R.sup.4 ; m is 2 or 3; and n is 1 or 2 (wherein each of R.sup.2 and R.sup.3, which are identical to or different from each other, represents a hydrogen atom, a hydroxyl group, a lower alkyl group which may have a substituent, a phenyl group which may have a substituent, an aralkyl group which may have a substituent, or a heterocyclic group which may have a substituent; R.sup.4 represents a lower alkyl group, a phenyl group, a formyl group, or a lower alkoxycarbonyl group)!, as well as to a medicine containing the derivative or salt as the active ingredient.
    Type: Grant
    Filed: March 4, 1998
    Date of Patent: March 16, 1999
    Assignee: Kowa Co., Ltd.
    Inventors: Mitsuteru Hirata, Takeo Deushi, Yoshio Takahashi, Masahiro Tamura, Takeshi Ohshima, Toshiaki Oda, Tetsuya Ishikawa, Hiroyuki Sonoki, Masami Shiratsuchi
  • Patent number: 5869428
    Abstract: A pyridonesulfonylurea compound of the formula (I) or its salt: ##STR1## wherein Q is ##STR2## for use as a herbicide, wherein the variables are hereinbelow defined.
    Type: Grant
    Filed: March 4, 1996
    Date of Patent: February 9, 1999
    Assignee: Ishihara Sangyo Kaisha Ltd.
    Inventors: Yasuo Morishima, Shigeo Murai, Yoshiyuki Aoyama, Hiroshi Sasaki, Hiroshi Kikugawa, Soichiro Nagayama, Makiko Mitani
  • Patent number: 5863924
    Abstract: The disclosed pyrimidine derivatives, and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, in particular use as selective 5HT.sub.2B -antagonists. The invention is also directed to formulations and methods for treatment.
    Type: Grant
    Filed: May 20, 1997
    Date of Patent: January 26, 1999
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jacob Berger, Lee Allen Flippin, Robert Greenhouse, Saul Jaime-Figueroa, Yanzhou Liu, Aubry Kern Miller, David George Putman, Klaus Kurt Weinhardt, Shu-Hai Zhao
  • Patent number: 5863923
    Abstract: Method of treating 5-HT.sub.3 -mediated disorders, which comprises systemic administration of an effective amount of a compound of formula (I) ##STR1## the pharmaceutically acceptable acid addition salt forms and the stereochemically isomeric forms thereof, wherein R.sup.1 and R.sup.2 represent hydrogen, or R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd.CH-- (a), --CH.dbd.C(Cl)--CH.dbd.CH--(b) or --CH.dbd.CH--C(Cl)=CH-- (c); n represents 2, 3 or 4; R.sup.3 represents hydrogen or methoxy; m represents 1 or 2; R.sup.4 represents hydrogen, amino or C.sub.1-3 -alkylcarbonylamino; and R.sup.5 represents hydrogen or halo; novel compounds; compositions; processes for preparing novel compounds and intermediates.
    Type: Grant
    Filed: May 1, 1997
    Date of Patent: January 26, 1999
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Georges Henri Paul Van Daele, Jean-Paul Rene Marie Andre Bosmans, Willy Joannes Carolus Van Laerhoven
  • Patent number: 5859020
    Abstract: The invention relates to substituted 4-alkoxypyrimidines of the formula ##STR1## in which R.sup.1 is hydrogen, halogen, alkyl or cycloalkyl, R.sup.2 is hydrogen, optionally substituted alkyl, optionally substituted alkoxy, optionally substituted alkylthio, alkylamino or dialkylamino, R.sup.3 is hydrogen, alkyl, alkoxy, haloalkoxy, halogen, alkylthio, amino, alkylamino or dialkylamino, and R.sup.4 is hydrogen, alkyl, cycloalkyl or haloalkyl, where R.sup.2 and R.sup.3 together with the carbon atoms to which they are attached can also form a ring, and Q is as defined in the description.The invention furthermore relates to a process for their preparation, to agents containing them, and to their use as pesticides.
    Type: Grant
    Filed: January 15, 1997
    Date of Patent: January 12, 1999
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Rainer Preuss, Gerhard Salbeck, deceased, Wolfgang Schaper, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lummen
  • Patent number: 5854179
    Abstract: Sulfur-substituted phenylsulfonylureas; processes for their preparation and their use as herbicides and plant growth regulatorsCompounds of the formula (I) and salts thereof ##STR1## in which R*, R.sup.1, R.sup.2, R.sup.3, X, Y, Z, W, n and m are defined as in claim 1, and specifically R* is a formyl equivalent of the formula CHO, --CH.dbd.NR or CH(X.sup.1 R')(X.sup.2 R"), are suitable as herbicides and plant growth regulators. They are prepared analogously to known methods, in some cases using novel intermediate products of the formula (XVII) ##STR2## in which U*.dbd.NH.sub.2, Cl or (substituted) amino.
    Type: Grant
    Filed: November 3, 1995
    Date of Patent: December 29, 1998
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
  • Patent number: 5852019
    Abstract: The present invention provides a novel compound which is represented by formula (I): ##STR1## wherein preferable examples of R.sup.1 to R.sup.6 are as follows; R.sup.1 and R.sup.2 are each an alkyl group optionally substituted by a halogen atom, an amino group, a hydroxyl group, an alkoxyl group or a thiol group, a hydrogen atom, a halogen atom or an alkoxyl group; R.sup.3 is a hydrogen atom; R.sup.4 is a methyl group; R.sup.5 is a hydrogen atom or an alkyl group; and R.sup.6 is a group of the formula: ##STR2## wherein Z is a phenyl group; and has an antitumor effect.
    Type: Grant
    Filed: February 4, 1998
    Date of Patent: December 22, 1998
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Akio Ejima, Masamichi Sugimori, Ikuo Mitsui
  • Patent number: 5849666
    Abstract: N-substituted hydrazinophenylsulfonylureas, processes for their preparation and their use as herbicides and plant growth regulatorsCompounds of the formula (I) or salts thereof ##STR1## in which R.sup.1 to R.sup.6, W, Q, X, Y and Z are defined as in formula (I) as claimed in claim 1, are suitable as herbicides and plant growth regulators.The compounds (I) are prepared by processes analogous to known processes (cf.
    Type: Grant
    Filed: November 22, 1995
    Date of Patent: December 15, 1998
    Assignee: Hoechst Schering Agrevo GmbH
    Inventors: Heinz Kehne, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
  • Patent number: 5824624
    Abstract: New herbicidal pyridine and pyrimidine derivatives of general formula (I), ##STR1## wherein Z represents a nitrogen atom or a C--H group; A represents an optionally substituted aryl group or an optionally substituted 5- or 6-membered nitrogen-containing heteroaromatic group; n represents an integer from 0 to 2 and R.sup.1 or each R.sup.1 independently represents a hydrogen atom or an optionally substituted alkyl, alkoxy, alkylthio or dialkylamino group; m represents an integer from 0 to 5 and R.sup.2 or each R.sup.2 independently represents a hydrogen or a halogen atom or an optionally substituted alkyl, haloalkyl, haloalkoxy, alkoxy, alkylthio group or a nitro, cyano or a halosulphonyl group; and X represents an oxygen or sulphur atom.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: October 20, 1998
    Assignee: American Cyanamid Company
    Inventors: Axel Kleeman, Helmut Siegfried Baltruschat, Thelka Hulsen
  • Patent number: 5807863
    Abstract: This invention relates to novel 2-(4-pyrazolyloxy-pyrimidin-5-yl) acetic acid derivatives of formula I ##STR1## wherein R.sub.1 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, C.sub.3-6 cycloalkyl, or di-C.sub.1-4 alkylamino,R.sub.2 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, or di-C.sub.1-4 alkyl-amino,R.sub.3 is hydrogen or methyl,R.sub.4 is aryl, aryl-C.sub.1-4 alkyl, heteroaryl, or heteroaryl-C.sub.1-4 alkyl, wherein each of the aromatic rings may be optionally substituted; andX is CH or nitrogen;the use of such compounds for the control of phytopathogens, compositions for facilitating such use, and the preparation of the compounds of formula I.
    Type: Grant
    Filed: September 19, 1996
    Date of Patent: September 15, 1998
    Assignee: Novartis Corporation
    Inventors: Martin Eberle, Clemens Lamberth, Fritz Schaub
  • Patent number: 5783576
    Abstract: New compounds of general formula (I) are provided: ##STR1## which are explained in the specification can be prepared by a variety of methods. The compounds may be used in pharmaceutical compositions.
    Type: Grant
    Filed: August 9, 1996
    Date of Patent: July 21, 1998
    Assignee: Boehringer Ingelheim KG
    Inventors: Otto Roos, Georg Speck, Walter Losel, Dietrich Arndts, Wolf-Dietrich Bechtel
  • Patent number: 5780473
    Abstract: Compounds of the formula ##STR1## inhibit the activity of endothelin.
    Type: Grant
    Filed: July 25, 1996
    Date of Patent: July 14, 1998
    Assignee: Bristol-Myers Squibb Company
    Inventors: Natesan Murugesan, Joel C. Barrish, Philip D. Stein
  • Patent number: 5760038
    Abstract: Compounds of the formula ##STR1## in which the symbols are as defined herein, inhibit the activity of endothelin.
    Type: Grant
    Filed: February 6, 1995
    Date of Patent: June 2, 1998
    Assignee: Bristol-Myers Squibb Company
    Inventors: Natesan Murugesan, Joel C. Barrish, Philip D. Stein
  • Patent number: 5753668
    Abstract: The present invention provides certain novel nitro or nitroso substituted benzyloxy pyrimidines useful as AGT inactivators. An example of such a pyrimidine is a compound of the formula ##STR1## wherein R.sub.1, is NO.sub.2 or NO, and R.sub.2 is hydrogen, halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 hydroxyalkyl, thiol, C.sub.1 -C.sub.4 alkythio, trifluoromethoxy, oxymethanesulfonyl, oxytrifluoromethanesulfonyl, or C.sub.1 -C.sub.4 oxyacyl. The present invention further provides pharmaceutical compositions comprising these compounds, and a method of enhancing the chemotherapeutic treatment of tumor cells in a mammal with an antineoplastic alkylating agent which causes cytotoxic lesions at the O.sup.6 -position of guanine.
    Type: Grant
    Filed: June 11, 1996
    Date of Patent: May 19, 1998
    Assignees: The United States of America as represented by the Department of Health and Human Services, Penn State Research Foundation, Arch Development Corporation
    Inventors: Robert C. Moschel, Anthony E. Pegg, M. Eileen Dolan, Mi-Young Chae
  • Patent number: 5747421
    Abstract: Formylaminophenylsulfonylureas; processes for their preparation, and their use as herbicides and plant growth regulatorsCompounds of the formula (I) ##STR1## in which R.sup.1 is H, a substituted or unsubstituted hydrocarbon radical or an unsubstituted or substituted heterocyclic radical,R.sup.2 is H, (C.sub.1 -C.sub.6)-alkyl or (C.sub.1 -C.sub.6)-alkoxy,R.sup.3 is halogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.1 -C.sub.6)-alkoxy, (C.sub.1 -C.sub.6)-haloalkyl, (C.sub.1 -C.sub.6)-haloalkoxy, NO.sub.2, CN, NH.sub.2, (C.sub.1 -C.sub.4) -mono- or dialkylamino, each independently of other radicals R.sup.3 if n is 2 or 3,n is 0, 1, 2 or 3,W is an oxygen atom or a sulfur atom,X and Y independently of one another are halogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.1 -C.sub.6)-alkoxy or (C.sub.1 -C.sub.6)-alkylthio, each of the three last-mentioned radicals being unsubstituted or substituted by one or more radicals selected from the group consisting of halogen, (C.sub.1 -C.sub.4)-alkoxy and (C.sub.1 -C.sub.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: May 5, 1998
    Assignee: Hoechst Schering Agrevo GmbH
    Inventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
  • Patent number: 5739134
    Abstract: N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system.
    Type: Grant
    Filed: April 13, 1995
    Date of Patent: April 14, 1998
    Assignee: Janssen Pharmacetuica N.V.
    Inventors: Georges H.P. Van Daele, deceased, Frans M.A. Van den Keybus, Marie L. Hendrickx, heiress, Kurt G.C.E. Van Daele, heir, Peter J.V. Van Daele, heir, Glenn K.L. Van Daele, heir
  • Patent number: 5728706
    Abstract: A benzenesulfonamide derivative of the formula ?I!: ##STR1## wherein Ring A and Ring B are the same or different and each substituted or unsubstituted benzene ring, Q is a single bond or a group of the formula: --O--, --S--, --SO--, --SO.sub.2 -- or --CH.sub.2 --, Y is a group of the formula: --O--, --S-- or --NH--, Alk is lower alkylene group or lower alkenylene group, Z is a single bond or a group of the formula: --O-- or --NH--, R is a substituted or unsubstituted aromatic heterocyclic or aryl group, R.sup.
    Type: Grant
    Filed: April 24, 1996
    Date of Patent: March 17, 1998
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Koichiro Yamada, Kosuke Yasuda, Kohei Kikkawa, Rikako Kohno
  • Patent number: 5726312
    Abstract: Intermediates for preparing derivatives of 5-thia- and 5-selenopyrimidinone, ##STR1## which are useful as inhibitors of the enzymes glycinamide ribonucleotide formyl transferase (GARFT) and amino imidazole carboxamide ribonucleotide formyl transferase (AICARFT). The present invention is also directed to methods of preparing these intermediates.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: March 10, 1998
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Michael D. Varney, William H. Romines, Cynthia L. Palmer, Judith G. Deal
  • Patent number: 5723473
    Abstract: A fungicidal compound of formula (I): ##STR1## wherein A is hydrogen, halogen, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; and one of R.sup.1 and R.sup.2 is optionally substituted isoquinoline while the other is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, halogen or cyano.
    Type: Grant
    Filed: April 11, 1995
    Date of Patent: March 3, 1998
    Assignee: Zeneca Limited
    Inventor: Brian Leslie Pilkington
  • Patent number: 5723409
    Abstract: The compounds of the formula (I) ##STR1## in which R.sup.1 -R.sup.4, W, X, Y and Z are as defined in claim 1 are suitable for controlling harmful plants in crops.
    Type: Grant
    Filed: April 28, 1995
    Date of Patent: March 3, 1998
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer
  • Patent number: 5721192
    Abstract: Aminosulfonyl ureas having general formula (I): ##STR1## The aminosulfonyl ureas having general formula (I) have a high herbicidal activity.
    Type: Grant
    Filed: October 16, 1996
    Date of Patent: February 24, 1998
    Assignee: Isagro Ricerca S.r.l.
    Inventors: Giovanni Meazza, Giampaolo Zanardi, Sergio Massimini, Piero La Porta, Ernesto Signorini
  • Patent number: 5716993
    Abstract: The present invention provides an anthranilic acid derivative having a cGMP-PDE inhibitory activity.An anthranilic acid derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof: ##STR1## ?wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent the same or different from each other, a hydrogen atom, a halogen atom, a hydroxy group, an optionally halogenated lower alkyl group, an optionally halogenated lower alkoxy group, a nitro group, a hydroxyalkyl group, a cyano group or the like; R.sup.5 and R.sup.6 represent the same or different from each other, a hydrogen atom, a halogen atom, a hydroxy group, a cyano group, an optionally halogenated lower alkyl group, an optionally halogenated lower alkoxy group or the like;W represents a group of the formula: --N.dbd. or --CH.dbd.; R.sup.7 and R.sup.
    Type: Grant
    Filed: September 14, 1995
    Date of Patent: February 10, 1998
    Assignee: Eisai Co., Ltd.
    Inventors: Fumihiro Ozaki, Keiji Ishibashi, Hironori Ikuta, Hiroki Ishihara, Shigeru Souda
  • Patent number: 5712393
    Abstract: The present invention provides a compound of formula (1) ##STR1## in which: R.sub.4 represents a hydrogen atom, a halogen atom or a nitro group;R.sub.6 represents a hydrogen atom or a straight or branched (C.sub.1 -C.sub.6) alkyl group;R.sub.7 represents a chlorine atom or a hydroxyl group; andZ represents: a phenyl group optionally substituted with one or more halogen atoms, straight or branched (C.sub.1 -C.sub.4)alkyl groups, straight or branched (C.sub.1 -C.sub.4)alkoxy groups, or trifluoromethyl, formyl, --CH.sub.2 OR, --CH.sub.2 OCOR, --CH.sub.2 CONRR', --CH.sub.2 ONCOR, --COOR, nitro, --NHR, --NRR' or --NHCOR groups, wherein R and R' are each, independently, a hydrogen atom or a (C.sub.1 -C.sub.7) alkyl group; a heterocyclic group optionally substituted as defined above for phenyl; or a cyclo(C.sub.5 -C.sub.8)alkyl group; additionally, when R.sub.
    Type: Grant
    Filed: November 24, 1995
    Date of Patent: January 27, 1998
    Assignee: Synthelabo
    Inventors: Jean Michel Altenburger, Gilbert Lassalle
  • Patent number: 5696053
    Abstract: Salts of the formula (I) ##STR1## in which n is 0, 1, 2 or 3,R is halogen, alkyl or alkoxy, mainly in each case independently of other substituents R in the event that n is greater than 1,R.sup.1 is a substituted or unsubstituted hydrocarbon radical or a substituted or unsubstituted heterocyclic radical,R.sup.2 is an acyl radical,R.sup.3 is hydrogen or C.sub.1 -C.sub.5 -alkyl,M.sym. is a metal or ammonium ion,X and Y independently of one another are halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy or C.sub.1 -C.sub.6 -alkylthio, each of the three last-mentioned radicals being unsubstituted or substituted by one or more radicals selected from the group consisting of halogen, C.sub.1 -C.sub.4 -alkoxy and C.sub.1 -C.sub.4 -alkylthio, or are C.sub.3 -C.sub.6 -cycloalkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, C.sub.3 -C.sub.6 -alkenyloxy, C.sub.2 -C.sub.6 -alkynyloxy, mono- or di(C.sub.1 -C.sub.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: December 9, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer