Benzene Ring Containing Patents (Class 564/244)
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Patent number: 6319944Abstract: Compounds represented by formula I: or a pharmaceutically acceptable salt or hydrate thereof, are disclosed. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: May 4, 2000Date of Patent: November 20, 2001Assignee: Merck & Co., Inc.Inventors: Christopher F. Claiborne, Nigel J. Liverton, Brian Libby, Neil R. Curtis, Janusz Kulagowski
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Patent number: 6300342Abstract: Antithrombotic phenylalkyl derivatives of the formula Exemplary compounds are: (a) 1-[3-(4-amidino-phenyl)propionyl]-6-(4-fluoro-phenylsulphonamido)-1,2,3,4-tetrahydro-quinoline, (b) 1-[3-(4-amidino-phenyl)propionyl]-6-butylsulphonamido-1,2,3,4-tetrahydro-quinoline, (c) 1-[3-(4-amidino-phenyl)propionyl]-5-phenylsulphonamido-1,2,3,4-tetrahydro-quinoline, (d) 1-[3-(4-amidino-phenyl)propionyl]-3-methyl-6-phenylsulphonamido-1,2,3,4-tetrahydro-quinoline, and, (e) 1-[3-(4-amidino-phenyl)propionyl]-6-(5-chloro-thien-2-ylsulphonamido)-1,2,3,4-tetrahydro-quinoline.Type: GrantFiled: December 9, 1999Date of Patent: October 9, 2001Assignee: Boehringer Ingelheim Pharm KGInventors: Armin Heckel, Rainer Soyka, Wolfgang Grell, Eric Haaksma, Klaus Binder, Rainer Zimmerman
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Patent number: 6291531Abstract: The present invention relates to a new LTB4 antagonist, processes for the preparation thereof and its use as a pharmaceutical composition.Type: GrantFiled: September 15, 2000Date of Patent: September 18, 2001Assignee: Boehringer Ingelheim Pharma KGInventor: Ralf Anderskewitz
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Patent number: 6265612Abstract: The present invention relates to new benzamidine derivatives, processes for preparing them and their use in pharmaceutical compositions.Type: GrantFiled: December 1, 2000Date of Patent: July 24, 2001Assignee: Boehringer Ingelheim Pharma KGInventors: Kurt Schromm, Ralf Anderskewitz, Ernst-Otto Renth, Franz Birke, Hans Michael Jennewein, Christopher John Montague Meade
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Patent number: 6262106Abstract: The compound of the above formula wherein R1-R5 are independently selected from hydrogen, alkyl and aryl and prodrugs thereof; and pharmaceutically acceptable salts thereof; and use of the compounds in therapy, particularly for treatment of a condition generally associated with abnormalities in glutamtergic transmission.Type: GrantFiled: September 13, 2000Date of Patent: July 17, 2001Assignee: Vernalis Research LimitedInventors: Nathaniel Julius Thomas Monck, Roger John Gillespie, Andrew James Bird
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Patent number: 6242644Abstract: The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: wherein R1, E, X1 to X4 and G1 and G2 are as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.Type: GrantFiled: December 14, 1999Date of Patent: June 5, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, Leo Alig, Alexander Chucholowski, Katrin Groebke, Kurt Hilpert, Holger Kuehne, Ulrike Obst, Lutz Weber, Hans Peter Wessel
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Patent number: 6228391Abstract: Novel amidine derivatives of the formula (1); and drug carriers such as liposomes or emulsions comprising the derivatives, which can enclose genetic materials or drugs and transfer them to cells or affected sites efficiently and safely, wherein A is an aromatic ring, R1 and R2 are the same or different and independently represent an alkyl group having any one of 10 to 25 carbon atoms, and an alkenyl group having any one of 10 to 25 carbon atoms, X and Y are the same or different and independently represent —O—, —S—, —COO—, —OCO—, —CONH—, or —NHCO—, m is 0 or 1, and n is 0 or a natural number of 1 to 6.Type: GrantFiled: December 10, 1998Date of Patent: May 8, 2001Assignee: Terumo Kabushiki KaishaInventors: Kazuhiro Shimizu, Masashi Isozaki, Kazunori Koiwai
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Patent number: 6204385Abstract: A process for preparing amidines and their salts with inorganic or organic acids comprises reacting the corresponding nitrile with ammonia, C1-C6-alkylamine or hydrazine in the presence of a mercaptocarboxylic acid and in the presence or absence of an in-organic or organic ammonium salt.Type: GrantFiled: March 1, 1999Date of Patent: March 20, 2001Assignee: BASF AktiengesellschaftInventors: Bernd Schäfer, Thomas Zierke
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Patent number: 6197824Abstract: Novel benzamidines, having LTB4-antagonistic activity, of the formula methods for their preparation, their and their use as medicaments.Type: GrantFiled: June 2, 2000Date of Patent: March 6, 2001Assignee: Boehringer Ingelheim Pharma KGInventors: Kurt Schromm, Ralf Anderskewitz, Ernst-Otto Renth, Franz Birke, Hans Michael Jennewein, Christopher John Montague Meade
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Patent number: 6166088Abstract: This invention is directed to benzamidine derivatives substituted by amino acid and hydroxy acid derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: GrantFiled: September 9, 1999Date of Patent: December 26, 2000Assignee: Berlex Laboratories, Inc.Inventors: Monica Kochanny, Raju Mohan, Michael M. Morrissey, Howard P. Ng, Weiya Yun
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Patent number: 6150382Abstract: This invention is directed to monocyclic N-heterocyclics which are substituted by acyclic or cyclic thio derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: GrantFiled: May 21, 1999Date of Patent: November 21, 2000Assignee: Berlex Laboratories, Inc.Inventors: Monica J. Kochanny, Michael M. Morrissey, Howard P. Ng
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Patent number: 6133315Abstract: Amidino and benzamidino compounds, including compounds of the formula: ##STR1## wherein R.sup.1 -R.sup.4, R.sup.6 -R.sup.9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.Type: GrantFiled: March 16, 1999Date of Patent: October 17, 2000Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Carl R. Illig, Richard M. Soll
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Patent number: 6127423Abstract: The invention relates to new phenylamidine derivatives, processes for preparing them and their use as pharmaceutical compositions.Type: GrantFiled: July 31, 1998Date of Patent: October 3, 2000Assignee: Boehringer Ingelheim KGInventors: Ralf Anderskewitz, Kurt Schromm, Ernst-Otto Renth, Franz Birke, Hans Michael Jennewein, Christopher John Montague Meade, Andreas Ding
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Patent number: 6057342Abstract: The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.Type: GrantFiled: July 7, 1997Date of Patent: May 2, 2000Assignee: Dupont Pharmaceutical Co.Inventors: John Matthew Fevig, Donald Joseph Phillip Pinto, Mimi Lifen Quan, Petrus Fredericus Wilhelmus Stouten
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Patent number: 6051164Abstract: A polymeric article, such as an extruded or molded article or a biaxially oriented tape or film, and a method of stabilizing such a polymeric article to protect the article from degradation due to exposure to UV light. The article is formed by blending a polymeric material with from about 50 to about 5,000 ppm of at least one ortho hydroxy tris-aryl triazine light absorber and from about 500 ppm to about 1.25 percent of at least one oligomeric, polymeric, or high molecular weight HALS having a molecular weight of at least about 500, wherein the weight ratio of HALS to triazine light absorber is from about 3:1 to about 20:1, to form a stabilized polymeric composition, and forming an extruded or molded article or a biaxially oriented tape or film from the stabilized polymeric composition.Type: GrantFiled: April 30, 1998Date of Patent: April 18, 2000Assignee: Cytec Technology Corp.Inventor: Sari-Beth Samuels
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Patent number: 5962693Abstract: The present invention relates to processes for the conversion of nitrites to amidines in the preparation of compounds which are antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex. The compounds described herein are potent thrombolytics and useful for the inhibition of platelet aggregation in the treatment of thromboembolic disorders.Type: GrantFiled: October 5, 1998Date of Patent: October 5, 1999Assignee: DuPont Pharmaceuticals CompanyInventors: Philip Ma, Pasquale N. Confalone, Hui-Yin Li
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Patent number: 5866612Abstract: A class of acetamidine derivatives of general formula (I) ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-6 hydrocarbyl group optionally substituted by halo, halo, nitro, cyano or a group XR.sup.3 wherein X is oxygen, C(O).sub.m wherein m is 1 or 2, S(O).sub.n wherein n is 0, 1 or 2, or a group NR.sup.4 wherein R.sup.4 is hydrogen or C.sub.1-6 alkyl; and R.sup.3 is hydrogen, C.sub.1-6 alkyl, or a group NR.sup.5 R.sup.6 wherein R.sup.5 and R.sup.6 are independently hydrogen or C.sub.1-6 alkyl, provided that R.sup.3 is not NR.sup.5 R.sup.6 when X is oxygen or S(O).sub.n; R.sup.1a and R.sup.1b are independently selected from hydrogen and halo; R.sup.2 is a C.sub.1-14 hydrocarbyl group which may optionally contain one or two heteroatoms, the group R.sup.2 being optionally substituted by one or more groups independently selected from halo; N.sub.3 ; nitro; CF.sub.3 ; ZR.sup.7 wherein Z is oxygen, C(O).sub.m' wherein m' is 1 or 2, S(O).sub.n' wherein n' is 0, 1 or 2, or a group NR.sup.8 wherein R.sup.Type: GrantFiled: June 17, 1997Date of Patent: February 2, 1999Assignee: Glaxo Wellcome Inc.Inventors: Jeffrey Alan Oplinger, Edward Patrick Garvey, Eric Steven Furfine, Barry George Shearer, Jon Loren Collins
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Patent number: 5846907Abstract: Pyrazol-4-ylbenzoyl compounds of the formula I ##STR1## where Z is a 5- or 6-membered heterocyclic saturated or unsaturated radical, Q is a pyrazole ring and L and M are as defined in the specification, their use as herbicidal compounds and to processes for preparing the compounds.Type: GrantFiled: July 30, 1997Date of Patent: December 8, 1998Assignee: BASF AktiengesellschaftInventors: Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Stefan Engel, Martina Otten, Marcus Vossen, Peter Plath, Harald Rang, Albrecht Harreus, Hartmann Konig, Helmut Walter, Karl-Otto Westphalen, Ulf Misslizt
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Patent number: 5736747Abstract: Organic compounds having at least one ethylenically-unsaturated group are described, the organic compounds being suitable for use in coatable compositions as reactive diluents; compounds of the invention preferably have a divalent organic linking moiety devoid of reactive groups other than optional ethylenically-unsaturated groups, and a polar organic moiety and are particularly adept in solubilizing aminoplast resins having radiation-curable pendant groups.Type: GrantFiled: February 23, 1996Date of Patent: April 7, 1998Assignee: Minnesota Mining and Manufacturing CompanyInventors: Ernest L. Thurber, Eric G. Larson, Alan R. Kirk, Gregg D. Dahlke
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Patent number: 5731332Abstract: Compounds of formula ##STR1## and their therapeutic use, inter alia, as LTB.sub.4 -antagonists. Exemplary compounds are:(Methoxycarbonyl-imino-{4'-?2-(2-propylphenoxy)-ethoxy!-biphenyl-4-yl}-meth yl)-amine;(Benzyloxycarbonyl-imino-{4'-?2-(2-propylphenoxy)-ethoxy!-biphenyl-4-yl}-me thyl-amine;?Hydroxy-imino-(4-{3-?4-(1-methyl-1-phenylethyl)-phenoxymethyl!-benzoyloxy} phenyl)-methyl!-amine;?Ethoxycarbonyl-imino-(4-{3-?4-(1-methyl-1-phenylethyl)-phenoxymethyl!-benz oyloxy}phenyl)-methyl!-amine; and,?3'-Pyridylcarbonyl-imino-(4-{3-?4-(1-methyl-1-phenylethyl)-phenoxymethyl!- benzyloxy}phenyl)-methyl!-amine.Type: GrantFiled: March 28, 1997Date of Patent: March 24, 1998Assignee: Boehringer Ingelheim KGInventors: Ralf Anderskewitz, Kurt Schromm, Ernst-Otto Renth, Franz Birke, Armin Fugner, Hubert Heuer, Christopher Meade
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Patent number: 5723444Abstract: The invention concerns the compounds of the formulas: ##STR1## and protected forms and salts thereof which serve as starting materials in an improved method of synthesizing thrombin and kininogenase inhibitors. The invention further concerns an improved method for synthesizing the inhibitors which utilizes the compounds.Type: GrantFiled: June 6, 1995Date of Patent: March 3, 1998Assignee: Astra ABInventors: Karl Thomas Antonsson, Ruth Elvy Bylund, Nils David Gustafsson, Nils Olov Ingemar Nilsson
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Patent number: 5637621Abstract: The invention provides fungicidal compounds having the general formula:X.sub.1 -A.sub.1 -B.sub.1 -C-B.sub.2 -A.sub.2 -X.sub.2 (I)wherein X.sub.1 is an amidine, a guanidine, or an imidazole group.A.sub.1 is either a five-membered aromatic ring, a six-membered aromatic ring, a fusion of two five-membered aromatic rings, a fusion of 2 six-membered aromatic rings, or a fusion of a six-membered aromatic ring and a five-membered aromatic ring;B.sub.1 is either O (oxygen) or absent; C is a straight chain alkyl comprising 1-8 carbons; B.sub.2 is either O (oxygen) or absent; A.sub.2 is either a five-membered aromatic ring, a six-membered aromatic ring, a fusion of two five-membered aromatic rings, a fusion of 2 six-membered aromatic rings, or a fusion of a six-membered aromatic ring and a five-membered aromatic ring; and X.sub.2 is an amidine, a guanidine, or an imidazole.Type: GrantFiled: November 14, 1994Date of Patent: June 10, 1997Assignee: NZYM, Inc.Inventors: Joel Bolonick, Terrance J. Leighton, Ida K. Yu
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Patent number: 5629348Abstract: The invention provides fungicidal compounds having the general formula:X.sub.1 -A.sub.1 -B.sub.1 -C-B.sub.2 -A.sub.2 -X.sub.2 (I)wherein X.sub.1 is an amidine, a guanidine, or an imidazole group.A.sub.1 is either a five-membered aromatic ring, a six-membered aromatic ring, a fusion of two five-membered aromatic rings, a fusion of 2 six-membered aromatic rings, or a fusion of a six-membered aromatic ring and a five-membered aromatic ring;B.sub.1 is either O (oxygen) or absent; C is a straight chain alkyl comprising 1-8 carbons; B.sub.2 is either O (oxygen) or absent; A.sub.2 is either a five-membered aromatic ring, a six-membered aromatic ring, a fusion of two five-membered aromatic rings, a fusion of 2 six-membered aromatic rings, or a fusion of a six-membered aromatic ring and a five-membered aromatic ring; and X.sub.2 is an amidine, a guanidine, or an imidazole.Type: GrantFiled: November 14, 1994Date of Patent: May 13, 1997Assignee: NZYM, Inc.Inventors: Joel Bolonick, Terrance J. Leighton, Ida K. Yu
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Patent number: 5523302Abstract: This invention relates to novel compounds containing basic and acidic termini, pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.Type: GrantFiled: November 24, 1993Date of Patent: June 4, 1996Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Gary A. Cain, Charles J. Eyermann
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Patent number: 5498792Abstract: There is disclosed a process of producing an N-alkylacetamide of the general formula (III): ##STR1## wherein X.sup.1, X.sup.2 and X.sup.3 are the same or different and are independently hydrogen, lower alkyl, lower alkoxy, lower alkenyl, halogen or trifluoromethyl; R.sup.1 and R.sup.2 are the same or different and are independently lower alkyl; and represents a chemical bond of E- or Z-configuration, or a mixture of these configurations, which includes the steps of:(a) reacting an acetonitrile of the general formula (I): ##STR2## wherein X.sup.1, X.sup.2, X.sup.3, R.sup.1 and are each as defined above, with an alkylamine of the general formula (IV):R.sup.2 --NH.sub.2 (IV)wherein R.sup.2 is as defined above, to give an N-alkylacetamidine of the general formula (II): ##STR3## wherein X.sup.1, X.sup.2, X.sup.3, R.sup.1, R.sup.2 and are each as defined above; and(b) reacting the N-alkylacetamidine (II) with a nitrite derivative in the presence of an acid.Type: GrantFiled: September 16, 1994Date of Patent: March 12, 1996Assignees: Shionogi & Co., Ltd., Sumitomo Chemical Co., Ltd.Inventors: Katuhisa Masumoto, Akihiko Nakamura, Yujiro Kiyoshima, Mikio Sasaki, Asako Tanahashi
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Patent number: 5360810Abstract: There is disclosed a compound of the formula (I): ##STR1## wherein X is a hydrogen atom or 1 to 5 substituents which may be the same or different and are selected from the group consisting of a hydrogen atom, alkyl, alkenyl, alkynyl, optionally substituted phenyl, an optionally substituted heterocyclic group, alkoxy, alkenyloxy, alkynyloxy, optionally substituted phenoxy, mono-, di- or tri-substituted halogenoalkyl and a halogen atom; Y is CH or N; m is 0 or 1; A is a group of the formula: ##STR2## (wherein R.sup.1 is a hydrogen atom or alkyl; n is 0 or 1; B is O, S or NR.sup.3 ; R.sup.2 and R.sup.3 are the same or different and are a hydrogen atom, alkyl, alkenyl, alkynyl, phenyl, benzyl, acyl or phenacyl). There are also disclosed the production thereof and an agricultural fungicide containing the compound as an active component.Type: GrantFiled: March 18, 1993Date of Patent: November 1, 1994Assignee: Shionogi & Co., Ltd.Inventors: Yoshio Hayase, Hideyuki Takenaka, Norihiko Tanimoto, Michio Masuko, Toshihiko Takahashi
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Patent number: 5308869Abstract: N,N'-disubstituted-amidines, e.g., of the formula ##STR1## wherein R, R' and R" are substituted or unsubstituted hydrocarbon and/or heterocyclic groups.Methods are provided for the treatment or prophylaxis of anxiety in an animal, for treating psychosis, and for treating hypertension by administering an effective amount of an N,N'-disubstituted amidine which, preferably, has a high affinity for the sigma receptor.Type: GrantFiled: March 30, 1992Date of Patent: May 3, 1994Assignee: State of Oregon, acting by and through the Oregon State Board of Higher EducationInventors: John F. W. Keana, Eckard Weber
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Patent number: 5286752Abstract: Novel diarylamidines, and compositions and methods for treating cardiac arrhythmias in mammals utilizing the novel and related known diarylamidines of formula I, II, III and IV ##STR1##Type: GrantFiled: September 10, 1991Date of Patent: February 15, 1994Assignee: Sterling Winthrop Inc.Inventors: Robert E. Johnson, Thomas E. D'Ambra
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Patent number: 5136094Abstract: Secondary formamides having the structural formula:R.sup.1 CHR.sup.2 CH(OR.sup.3)NHCHOwhereinR.sup.1 is H, C.sub.1 -C.sub.6 alkyl or aryl;R.sup.2 is H, or C.sub.1 -C.sub.6 alkyl; andR.sup.3 is benzyl, C.sub.1 -C.sub.8 alkyl or hydroxyalkyl;are synthesized by reacting an acetal having the structural formula: R.sup.1 CHR.sup.2 CH(OR.sup.3).sub.2 wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, with formamide in the presence of a strong acid catalyst at a temperature in the range of 0.degree.-200.degree. C.Type: GrantFiled: March 10, 1988Date of Patent: August 4, 1992Assignee: Air Products and Chemicals, Inc.Inventors: Mark L. Listemann, Ronald Pierantozzi, Robert K. Pinschmidt, Jr.
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Patent number: 5041653Abstract: A method for sensitizing hypoxic tumor cells to radiation using derivatives of benzamide are disclosed. Some of the compounds useful in the method of the invention are novel.Type: GrantFiled: September 24, 1990Date of Patent: August 20, 1991Assignee: SRI InternationalInventors: William W. Lee, Edward W. Grange, J. Martin Brown
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Patent number: 4965284Abstract: This disclosure described novel derivatives of dibenzothiophene, dibenzothiophene sulfoxide, dibenzothiophene sulfone, thioxanthene, thioxanthene sulfoxide and thioxanthene sulfone which are active as modulators of the mammalian immune response system.Type: GrantFiled: April 25, 1989Date of Patent: October 23, 1990Assignee: American Cyanamid CompanyInventors: Vijay G. Nair, Ramson B. Conrow, Bosco S. Wang, V. M. Ruszala-Mallon
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Patent number: 4788130Abstract: Novel 2,3-dihydro-1H-indene derivatives and salts thereof represented by the general formula (1), ##STR1## [wherein R.sup.1 and R.sup.2 are each a hydrogen atom, a lower alkyl group, a phenyl group which may have halogen atoms and/or alkyl groups as the substituents on the phenyl ring; R.sup.3 is a halogen atom or a lower alkyl group; R.sup.4 is a hydrogen atom, a halogen atom, a phenyl-lower alkyl group, a cycloalkyl-lower alkyl group or the like; R.sup.5 is a hydroxyimino group, an alkylamino group or a group of the formula --NHR.sup.8 (wherein R.sup.8 is a hydrogen atom, a halogen-substituted lower alkanoyl group or the like); R.sup.6 is a hydrogen atom or a phenyl group; and R.sup.7 is a hydrogen atom or a lower alkyl group].Type: GrantFiled: August 29, 1985Date of Patent: November 29, 1988Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Yasuo Oshiro, Hiraki Ueda, Kazuyuki Nakagawa
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Patent number: 4661522Abstract: The present invention is dealing with cycloalkane-indene-carboximidamide derivatives having the general formula: ##STR1## wherein Rx together with either Ry.sub.1 or Ry.sub.2 represent the moiety ##STR2## (the other Ry being hydrogen), n represents the number 1, 2 or 3,R represents hydrogen or a (1-4 C)-alkyl group,R.sub.1 represents hydrogen, (1-4 C)-alkyl, hydroxyl, (1-4 C)-alkoxy or an amino group which is unsubstituted or substituted by (1-4 C)-alkyl andR.sub.2 is hydrogen, hydroxyl or (1-4 C)-alkyl,as well as the pharmaceutically acceptable salts thereof, with powerful blood platelet aggregation-inhibiting activity.Type: GrantFiled: May 15, 1985Date of Patent: April 28, 1987Assignee: Akzo N.V.Inventor: Tom Beetz
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Patent number: 4634705Abstract: Disclosed herein are adrenergic compounds represented by the formula ##STR1## wherein m is 0, 1 or 2; R.sub.1, R.sub.2, R.sub.3 and R.sub.7 are taken from the group consisting of hydrogen, hydroxy, loweralkyl, loweralkoxy, halo, amino, acetamido or NHSO.sub.2 R wherein R is taken from the group consisting of hydrogen or loweralkyl, provided that R.sub.1, R.sub.2, R.sub.3 and R.sub.7 cannot simultaneously be hydrogen or halo, and provided that when one of R.sub.1, R.sub.2, R.sub.3 and R.sub.7 is halo, the others cannot simultaneously be hydrogen and when two of R.sub.1, R.sub.2, R.sub.3 and R.sub.7 are halo, the other two cannot simultaneously be hydrogen and provided that R.sub.1 and R.sub.7 cannot simultaneously be methoxy each when R.sub.2 and R.sub.3 are hydrogen; R.sub.1 and R.sub.2 or R.sub.2 and R.sub.3 or R.sub.3 and R.sub.7 taken together can form a methylenedioxy or ethylenedioxy bridge; or R.sub.1 and R.sub.2 or R.sub.2 and R.sub.3 or R.sub.3 and R.sub.Type: GrantFiled: March 7, 1986Date of Patent: January 6, 1987Assignee: Abbott LaboratoriesInventors: John F. DeBernardis, Fatima Z. Basha
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Patent number: 4539319Abstract: Compounds of formula (I) ##STR1## and acid addition salts thereof, whereinR.sup.1 is hydrogen, hydroxy, alkoxy, aryloxy, aralkoxy, heteroaryloxy or heteroaralkoxy;andone of R.sup.2, R.sup.3 and R.sup.4 is hydrogen and the others are the same or different and each is hydrogen, alkyl, aryl, aralkyl, heteroaryl or heteroaralkyl;orR.sup.2 is hydrogen and ##STR2## is mono- or bi-cyclic amino, inhibit enterotoxin-induced secretion into the small intestine and are, therefore, useful in treating enterotoxin induced diarrhoea in humans and scours in animals.Type: GrantFiled: June 14, 1983Date of Patent: September 3, 1985Assignee: Beecham Group p.l.c.Inventors: Peter M. Newsome, Noel A. Mullan, John P. Marshall
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Patent number: 4499105Abstract: The present invention is dealing with compounds of the formula: ##STR1## and pharmaceutically acceptable salts thereof, in which n and m represent the number 1 or 2, X and Y hydrogen, alkyl (1-4 C), alkoxy (1-4 C), hydroxy, halogen, hydroxymethyl, trifluoromethyl, acyl (1-4 C), acyloxy (1-4 C) or the group NR.sub.x R.sub.y, in which R.sub.x and R.sub.y represent hydrogen, alkyl (1-4 C) or a sulphonyl group and R represents the group ##STR2## in which R.sub.1 and R.sub.2 represent hydrogen, alkyl (1-4 C), hydroxy, alkoxy (1-4 C), phenylalkoxy (7-10 C), acyloxy, amino or mono or dialkyl (1-4 C) amino, having potent platelet aggregation inhibiting properties.Type: GrantFiled: December 28, 1982Date of Patent: February 12, 1985Assignee: Akzo N.V.Inventor: Harm J. Panneman
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Patent number: 4448975Abstract: Amidines are one of the strongest organic bases and find application where this property is needed, such as in phase transfer catalysis in the form of their substituted derivatives. Their use, however, has been hampered by their expensive nature due to only mediocre yields in their preparation. The present invention provides a process for the preparation of substituted amidines in essentially quantitative yields.Type: GrantFiled: October 15, 1981Date of Patent: May 15, 1984Assignee: General Electric CompanyInventor: Victor Mark
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Patent number: 4330552Abstract: Antiinflammatory 4,5-diaryl-2-arylthioimidazoles, such as 4,5-bis(4-methoxyphenyl)-2-(4-chlorophenylthio)-1H-imidazole useful for treatment of arthritis and related diseases.Type: GrantFiled: November 6, 1980Date of Patent: May 18, 1982Assignee: E. I. Du Pont de Nemours and CompanyInventor: Saul C. Cherkofsky
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Patent number: 4321202Abstract: Amidines are one of the strongest organic bases and find application where this property is needed, such as in phase transfer catalysis in the form of their substituted derivatives. Their use, however, has been hampered by their expensive nature due to only mediocre yields in their preparation. The present invention provides a process for the preparation of substituted amidines in essentially quantitative yields.Type: GrantFiled: December 26, 1979Date of Patent: March 23, 1982Assignee: General Electric CompanyInventor: Victor Mark
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Patent number: 4277487Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2, which may be the same or different, represent a hydrogen atom, a chlorine atom, or a methyl group, with the proviso that not both R.sub.1 and R.sub.2 are hydrogen, andR represents a radical selected from the group consisting of --(CH.sub.2).sub.2 --C(CH.sub.3).dbd.CH.sub.2, --(CH.sub.2).sub.2 --CH.dbd.CH.sub.2, --O--CH.sub.2 --CH.dbd.CH.sub.2, --O--(CH.sub.2).sub.2 --CH.dbd.CH.sub.2, --O--CH.sub.2 --C(CH.sub.3).dbd.CH.sub.2, --O--CH.sub.2 --CH.dbd.CH--CH.sub.3, ##STR2## and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as bradycardiacs.Type: GrantFiled: July 17, 1979Date of Patent: July 7, 1981Assignee: Boehringer Ingelheim GmbHInventors: Helmut Stahle, Herbert Koppe, Werner Kummer, Walter Kobinger, Christian Lillie, Ludwig Pichler
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Patent number: RE37438Abstract: A class of acetamidine derivatives of general formula (I) wherein R1 is hydrogen, C1-6 hydrocarbyl group optionally substituted by halo, halo, nitro, cyano or a group XR3 wherein X is oxygen, C(O)m wherein m is 1 or 2, S(O)n wherein n is 0, 1 or 2, or a group NR4 wherein R4 is hydrogen or C1-6 alkyl; and R3 is hydrogen, C1-6 alkyl, or a group NR5R6 wherein R5 and R6 are independently hydrogen or C1-6 alkyl, provided that R3 is not NR5R6 when X is oxygen or S(O)n; R1a and R1b are independently selected from hydrogen and halo; R2 is a C1-14 hydrocarbyl group which may optionally contain one or two heteroatoms, the group R2 being optionally substituted by one or more groups independently selected from halo; N3; nitro; CF3; ZR7 wherein Z is oxygen, C(O)m′ wherein m′ is 1 or 2, S(O)n′ wherein n′ is 0, 1 or 2, or a group NR8 wherein R8 is hydrogen or C1-6 alkyl and R7 is hydrogen, C1-6 alkyl or a group NR9R10 wherein R9 and R10 are independently hydrogen or C1-6 alkyl; or RType: GrantFiled: May 4, 1999Date of Patent: November 6, 2001Assignee: Glaxo Wellcome Inc.Inventors: Jeffrey Alan Oplinger, Edward Patrick Garvey, Eric Steven Furfine, Barry George Shearer, Jon Loren Collins