Plural Rings In Acid Moiety With Nitrogen Bonded Directly To At Least One Of The Rings Patents (Class 560/48)
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Patent number: 5783593Abstract: The present invention provides a compound of the formula ##STR1## which inhibit squalene synthetase and cholesterol biosynthesis and are useful in the treatment of e.g., hyperlipidaemia, atherosclerosis, or fungal infections, processes for the preparation of the compounds of the invention, intermediates useful in these processes, and pharmaceutical compositions containing the compounds.Type: GrantFiled: April 29, 1996Date of Patent: July 21, 1998Assignee: Abbott LaboratoriesInventors: William R. Baker, Saul H. Rosenberg, Anthony K. L. Fung, Todd W. Rockway, Stephen A. Fakhoury, David S. Garvey, B. Gregory Donner, Stephen J. O'Connor, Rajnandan N. Prasad, Wang Shen, David M. Stout, Gerard M. Sullivan
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Patent number: 5783723Abstract: Dialkyl succinylsuccinates are prepared in a pure form and in high yield by reacting an alkali metal alcoholate with an excess of dialkyl succinate under anhydrous conditions followed by isolation of the di(alkali metal) salt of the dialkyl succinylsuccinate and then neutralization of the salt with acid. The resulting dialkyl succinylsuccinate is isolated or used without isolation as an intermediate in the production of quinacridone pigments. The disclosed process provides for high yields and reduced organic waste compared with known processes.Type: GrantFiled: September 24, 1996Date of Patent: July 21, 1998Assignee: Ciba Specialty Chemicals CorporationInventors: Colin Dennis Campbell, Damien Thurber Cole, Harold Raymond Taylor, III
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Patent number: 5776951Abstract: The present invention is concerned with diaryl compounds of formula (l) and their use in medical therapy, particularly in the prophylaxis or treatment of a clinical condition for which an ACAT inhibitor is indicated, such as hyperlipidaema or atherosclerosis. The invention also relates to pharmaceutical compositions and processes for the preparation of compounds according to the invention.Type: GrantFiled: April 11, 1996Date of Patent: July 7, 1998Assignee: Glaxo Wellcome Inc.Inventors: Richard James Arrowsmith, John Gordon Dann, Karl Witold Franzmann, Simon Teanby Hodgson, Peter John Wates
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Patent number: 5773646Abstract: The present invention relates to a class of compounds represented by the Formula I ##STR1## or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the .alpha..sub.v .beta..sub.3 integrin.Type: GrantFiled: March 27, 1997Date of Patent: June 30, 1998Assignee: G. D. Searle & Co.Inventors: Nizal Chandrakumar, Barbara B. Chen, Helen Y. Chen, Michael Clare, Alan F. Gasiecki, Richard A. Haack, James W. Malecha, Peter G. Ruminski, Mark A. Russell
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Patent number: 5763635Abstract: Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.Type: GrantFiled: June 21, 1996Date of Patent: June 9, 1998Assignee: ALLERGANInventors: Vidyasagar Vuligonda, Min Teng, Richard L. Beard, Alan T. Johnson, Tien T. Duong, Yuan Lin, Roshantha A. Chandraratna
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Patent number: 5739374Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: February 14, 1997Date of Patent: April 14, 1998Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5739131Abstract: A benzene derivative of the formula (I): ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -haloalkyl, --NH.sub.2, --NHR.sup.21 ; R.sup.2 is hydroxyl, --OR.sup.22, three- to seven-membered saturated cycloaliphatic amino optionally interrupted by one or more nitrogen, oxygen or sulfur atoms, --NHR.sup.23, --N(R.sup.24).sub.2, --NH.sub.2 ; R.sup.4 is hydrogen, C.sub.1-6 -alkyl, or --C(.dbd.O)R.sup.25 ; R.sup.7 is --CO--, --SO.sub.2 --; R.sup.8 is --CO--, single bond; R.sup.12 is --R.sup.11 --R.sup.5 ; R.sup.11 is --N(R.sup.5)--, --NH--, --O--, --N(R.sup.26)--, --N(C(.dbd.O)R.sup.27)--, --N(C(.dbd.O)NH.sub.2)--, --N(C(.dbd.O)NHR.sup.28)--; R.sup.13 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -haloalkyl, --NHC(.dbd.O)(CH.sub.2).sub.m C.sub.6 H.sub.5, --NHC(.dbd.O)R.sup.29, --NHC(.dbd.O)CH(C.sub.6 H.sub.5).sub.2, --NH.sub.2, --NHR.sup.30, --(CH.sub.2).sub.n C.sub.6 H.sub.5 ; Z is C, CH, N; A is CH, N; R.sup.5 is hydrogen, --CH.sub.2 C.sub.6 H.sub.4 COOH, --CH.sub.2 C.sub.6 H.sub.4 COOR.sup.31, --CH.Type: GrantFiled: April 30, 1997Date of Patent: April 14, 1998Assignee: Kureha Chemical Industry Co., Ltd.Inventors: Mikiro Yanaka, Fuyuhiko Nishijima, Hiroyuki Enari, Toshikazu Dewa, Toru Yamazaki, Michihito Ise
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Patent number: 5709719Abstract: A poly(oxyalkylene) ester of a substituted polyphenylether having the formula: ##STR1## wherein A is amino, aminomethyl, cyano, nitro, N-alkylamino or N-alkylaminomethyl wherein the alkyl group contains about 1 to about 6 carbon atoms, or N,N-dialkylamino or N,N-dialkylaminomethyl wherein each alkyl group independently contains about 1 to about 6 carbon atoms; R.sub.1 and R.sub.2 are independently hydrogen or lower alkyl having about 1 to about 6 carbon atoms and each R.sub.1 and R.sub.3 is independently selected in each --O--CHR.sub.1 -CHR.sub.2 - unit; R.sub.3 is hydrogen, alkyl having about 1 to about 100 carbon atoms, phenyl, aralkyl having about 7 to about 100 carbon atoms or alkaryl having about 7 to about 100 carbon atoms; x is an integer from about 1 to about 10, y is an integer from 0 to about 10; and z is an integer from about 1 to about 100.Type: GrantFiled: December 30, 1996Date of Patent: January 20, 1998Assignee: Chevron Chemical CompanyInventor: Richard E. Cherpeck
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Patent number: 5693669Abstract: The instant invention is a tilidine salt, tilidine dihydrogen orthophosphate, which owing to its surprising stability, is particularly suitable for use in the preparation of solid, in particular delayed-action, drugs in tablet, pill or capsule form.Type: GrantFiled: April 25, 1995Date of Patent: December 2, 1997Assignee: Godecke AktiengesellschaftInventors: Wolfgang Herrmann, Armin Knapp, Hans Klausmann
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Patent number: 5659036Abstract: A process for producing 2,5-di(arylamino)-3,6-dihydroterephthalic acid dialkyl ester having a high purity from 1,4-cyclohexanedione-2,5-di(carboxylic acid alkyl ester) at high yields for a short period of time; a process for producing quinacridone of which the byproduct content is small, from the above 2,5-di(arylamino)-3,6-dihydroterephthalic acid dialkyl ester; and a process for producing quinacridone of which the particle diameter is adjusted as desired, from the above 2,5-di(arylamino)-3,6-dihydroterephthalic acid dialkyl ester without adding a step of forming a pigment.Type: GrantFiled: March 23, 1995Date of Patent: August 19, 1997Assignee: Toyo Ink Manufacturing Co., Ltd.Inventors: Hitoshi Maki, Shigeki Kato, Yoshimi Kikuchi
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Patent number: 5656619Abstract: Abstract of the Disclosure: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: June 6, 1995Date of Patent: August 12, 1997Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5637256Abstract: This invention provides chiral nonracemic compound of formula: ##STR1## wherein n and m are 0 or 1, but one of n or m must be 1; k=0 or 1; B=COO or OOC; X.sub.1, X.sub.2, X.sub.3 and X.sub.4 are either H, an electron donor or an electron acceptor where at least one of the groups X.sub.1, X.sub.2, X.sub.3 or X.sub.4 is an electron acceptor and at least one of these groups is an electron donor and when one of X.sub.1 or X.sub.3 is an electron donor, the other is an electro a acceptor and when one of X.sub.2 or X.sub.4 is an electron donor, the other is an electron acceptor; and R.sub.1 and R.sub.2 can be various substituted and unsubstituted alkanes and monoalkenes. Compounds provided include those where one of R.sub.1 or R.sub.2 is a chiral non-racemic tail group, particularly a group selected from --O--C.sup.* H(CH.sub.3)R.sub.c, --O--C.sup.* H(CH.sub.3)COOR.sub.d, and --O--CH.sub.2 C.sup.* HF--C.sup.* HF--R.sub.2 in which the .sup.* indicates an asymmetric carbon enriched in one stereoconfiguration where R.Type: GrantFiled: May 26, 1995Date of Patent: June 10, 1997Assignee: University Research CorporationInventors: David M. Walba, Maria B. Ros, James A. Rego, Teresa Sierra
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Patent number: 5622916Abstract: A method of combating pests which comprises applying to such pests or to a pest habitat a pesticidally effective amount of a substituted 2-cyclohexen-1-yl-amine derivative of the formula ##STR1## and addition products thereof with acids and metal salts. Most of the compounds are new.Type: GrantFiled: September 15, 1993Date of Patent: April 22, 1997Assignee: Bayer AktiengesellschaftInventors: Franz Kunisch, Peter Babczinski, Dieter Arlt, Hans-Joachim Santel, Robert R. Schmidt, Wilhelm Brandes, Harry Strang
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Patent number: 5618839Abstract: The present invention relates to a compound of formula I ##STR1## or a nontoxic pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof, in whichX is --O--CO--, --NH--CO--, --CS--NH--, --CO--O--, --CO--NH--, --COS--, --SCO--, --SCH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --C.tbd.C--, --CH.sub.2 --NH--, --COCH.sub.2 --, --NHCS--, --CH.sub.2 S--, --CH.sub.2 O--, --OCH.sub.2 --, --NHCH.sub.2 -- or --CR.sup.5 .dbd.CR.sup.6 --;R.sup.m and R.sup.k are independently hydrogen, halogen, C.sub.1-6 alkyl, hydroxy, C.sub.1-6 alkyloxy or nitro;n is zero or one;R.sup.4 is --(CH.sub.2).sub.t --Y, C.sub.1-6 alkyl, or C.sub.3-6 cycloalkyl;R.sup.1 is --CO.sub.2 Z, C.sub.1-6 alkyl, CH.sub.2 OH, --CONHR.sup.y, or CHO;R.sup.2 and R.sup.3 are independently hydrogen or C.sub.1-6 alkyl;R.sup.a and R.sup.b are independently hydrogen or C.sub.1-6 alkyl; but when n is one, R.sup.a and R.sup.Type: GrantFiled: May 2, 1996Date of Patent: April 8, 1997Assignee: Bristol-Myers Squibb CompanyInventors: John E. Starrett, Jr., Kuo-Long Yu, Muzammil M. Mansuri, David R. Tortolani, Peter R. Reczek
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Patent number: 5616779Abstract: The present invention relates to a process for the preparation of 2,5-di-phenylamino-terephthalic acid and its dialkyl esters of the formula ##STR1## in which R is a hydrogen atom or a methyl or an ethyl group, by reaction of a succinic acid dialkyl ester with a sodium alcoholate in xylene, treatment of the resulting 2,5-dihydroxy-cyclohexadiene-1,4-di-carboxylic acid dialkyl ester with acid and aniline, dehydrogenation of the resulting 2,5-di-phenylamino-dihydro-(3,6)-terephthalic acid dialkyl ester by means of oxygen, if appropriate hydrolysis of the 2,5-di-phenylamino-terephthalic acid dialkyl ester formed and liberation of the 2,5-di-phenylamino-terephthalic acid from the di-sodium salt formed. The 2,5-di-phenylamino-dihydro-(3,6)-terephthalic acid dialkyl ester is reacted with pure oxygen in the presence of an alkali metal ion and/or an alkaline earth metal ion. This significantly decreases undesirable impurities.Type: GrantFiled: March 2, 1995Date of Patent: April 1, 1997Assignee: Hoechst AGInventor: Otto Arndt
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Patent number: 5616805Abstract: A pyrenylamine derivative having an unsaturated bond formula (I), which can be employed as an organic photoconductive material for use in electrophotography: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, W, l, m, n, j and k are specifically defined in the specification, an aldehyde compound of formula (II), which is an intermediate for preparing the pyrenylamine derivative: ##STR2## and methods of producing the pyrenylamine derivative and the aldehyde compound are disclosed.Type: GrantFiled: May 11, 1995Date of Patent: April 1, 1997Assignee: Ricoh Company, Ltd.Inventors: Chiaki Tanaka, Masaomi Sasaki, Tamotsu Aruga, Tomoyuki Shimada, Hiroshi Adachi
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Patent number: 5616615Abstract: The present invention concerns enaminones having the formula: ##STR1## wherein R is COOCH.sub.3 ; R.sup.1 is CH.sub.3 ; R.sup.2 is H; and R.sup.3 is selected from the group consisting of C.sub.6 H.sub.4 (p-Cl) and CH.sub.2 C.sub.6 H.sub.5.Type: GrantFiled: June 7, 1995Date of Patent: April 1, 1997Assignee: Howard UniversityInventors: Kenneth R. Scott, Jesse M. Nicholson, Ivan O. Edafiogho
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Patent number: 5599813Abstract: Thiazolopyrimidine derivatives represented by the formula ##STR1## and salts thereof are provided, which are characterized by a carboxamide residue substituted with R.sup.4 and R.sup.5. The derivatives and salts thereof exhibit antiangiogenic activity and are useful for treatment and cure of diseases, the development of which may be related to angiogenesis, including diabetic retinopathy, various chronic inflammation conditions, growth or metastasis of malignant solid tumors, rheumatism and psoriasis.Type: GrantFiled: April 1, 1994Date of Patent: February 4, 1997Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Hiroo Matsumoto, Noriko Tanaka, Kiyoshi Nakayama, Haruko Chatani, Michio Iwahana
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Patent number: 5599967Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning defined in the specification have retinoid-like biological activity.Type: GrantFiled: December 29, 1994Date of Patent: February 4, 1997Assignee: AllerganInventors: Vidyasagar Vuligonda, Richard L. Beard, Alan T. Johnson, Min Teng, Tae K. Song, Roshantha A. Chandraratna
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Patent number: 5576460Abstract: A method of preparing an arylamine compound includes reacting a metal amide comprising a metal selected from the group consisting of tin, boron, zinc, magnesium, indium and silicon, with an aromatic compound comprising an activated substituent in the presence of a transition metal catalyst to form an arylamine. The method is useful in preparing mixtures of arylamines for use in screening for pharmaceutical and biological activity and in preparing poly(anilines).Type: GrantFiled: July 27, 1994Date of Patent: November 19, 1996Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, Anil Guram
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Patent number: 5571942Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes and 3-aminochromanes which exhibit binding activity at the serotonin 1A receptor.Type: GrantFiled: August 22, 1995Date of Patent: November 5, 1996Assignee: Eli Lilly and CompanyInventors: Craig S. Hoechstetter, Diane L. Huser, John M. Schaus, Robert D. Titus
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Patent number: 5543078Abstract: The present invention provides ferroelectric liquid crystal and liquid crystal compounds, among which are compounds which possess large X.sup.(2), i.e. second order nonlinear susceptibility and thus make them useful in optical and nonlinear optical applications. The invention includes chiral nonracemic compounds of formula ##STR1## where one of n or m is 1; k is 1 and B is COO or OOC; R' is a straight-chain or branched alkyl or monoalkene group having from 1 to 20 carbon atoms where one or more of the non-neighboring carbon atoms in R', except any unsaturated carbon atoms, can be replaced with O, S or a Si(CH.sub.3).sub.2 group; and R' is a chiral nonracemic tail group selected from the group consisting of --O--C*H(CH.sub.3)R.sub.c, --O--C*H(CH.sub.3)COOR.sub.d and --O--CH.sub.2 C*HF--C*HF--R.sub.6 in which the * indicates an asymmetric carbon enriched in one stereoconfiguration which for --O--CH.sub.2 C*HF--C*HF--R.sub.e is either the (S,S) or (R,R) stereoconfiguration wherein: R.sub.Type: GrantFiled: November 19, 1993Date of Patent: August 6, 1996Assignee: University Research CorporationInventors: David M. Walba, Maria B. Ros, James A. Rego, Teresa Sierra
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Patent number: 5536874Abstract: There is provided a process for preparing an arylacetic acid or arylpropionic acid divative from an arylcarbinol which comprises the step of subjecting said arylcarbinol to suitable carbonylation conditions for a sufficient period of time and under suitable pressure and temperature to form said acid derivative, with the proviso that said carbonylation conditions include conducting the reaction in a two-phase system wherein one phase is an aqueous medium which contains (1) a catalyst which is a water-soluble metal complex consisting essentially of a Group VIII metal and a hydrophilic ligand such as palladium complexed with trisulfonated triphenylphosphine, and (2) optionally an acid, and wherein the second phase comprises said arylcarbinol.Type: GrantFiled: November 30, 1994Date of Patent: July 16, 1996Assignee: Hoechst Celanese CorporationInventors: Roger A. Sheldon, Leendert Maat, Georgios Papadogianakis
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Patent number: 5530014Abstract: The cyclohexadiene derivatives are prepared by reaction of cyclohexanones with amines and subsequent dehydration. The compounds are suitable as active compounds in medicaments on account of their property of being selective modulators of calcium channel-dependent potassium channels.Type: GrantFiled: August 18, 1995Date of Patent: June 25, 1996Assignee: Bayer AktiengesellschaftInventors: Klaus Urbahns, Hans-Georg Heine, Bodo Junge, Rudolf Schohe-Loop, Hartmund Wollweber, Henning Sommermeyer, Thomas Glaser, Reilinde Wittka, Jean-Marie-Viktor De Vry
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Patent number: 5523457Abstract: This invention relates to a retinoid mpound of formula I ##STR1## in which Y is --CO--NH--, --CR.sup.2 .dbd.CR.sup.3 --, --CO--O--, --O--CO--, --C(.dbd.S)--NH--, --C.tbd.C--, --O--CH.sub.2 --, --CH.sub.2 --O--, or --CH.sub.2 --CH.sub.2 --;A is --(CH.sub.2).sub.t -- or a bond;Q is phenyl optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen, or --CO.sub.2 R.sup.4 ;R.sup.1 is --CO.sub.2 Z, --CONHR.sup.5, C.sub.1-6 alkyl, --CH.sub.2 OH, or --CHO;R.sup.2, R.sup.3, R.sup.4, R.sup.5, and Z are independently hydrogen or C.sub.1-6 alkyl;t is one to six.Type: GrantFiled: June 2, 1995Date of Patent: June 4, 1996Assignee: Bristol-Myers Squibb CompanyInventors: John E. Starrett, Jr., Muzammil M. Mansuri, David R. Tortolani
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Patent number: 5495021Abstract: This invention relates to hexa- and octahydrobenzo[f]quinolin-3-ones, pharmaceutical formulations containing those compounds and methods of their use as steroid 5.alpha.-reductase inhibitors.Type: GrantFiled: April 6, 1994Date of Patent: February 27, 1996Assignee: Eli Lilly and CompanyInventors: James E. Audia, David E. Lawhorn, Leland O. Weigel
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Patent number: 5482942Abstract: This invention relates to novel 4-(3,4-dioxocyclobuten-1-yl)chromenes and dihydronaphthalenones and 3-(3,4-dioxocyclobuten-1-yl)indenes and salts thereof having smooth muscle relaxing activity, to their use in the treatment of hypertension as well as for treatment of peripheral vascular disease, congestive heart failure, disorders involving excessive smooth muscle contraction of the urinary tract such as incontinence or of the gastrointestinal tract such as irritable bowel syndrome, asthma, and hair loss and to pharmaceutical compositions containing an invention compound. The present invention discloses compounds represented by the formula (I): ##STR1## wherein: R.sub.1 and R.sub.2, independent from each other, are selected from the following: C.sub.1-6 perfluoroalkoxy, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxyl, C.sub.1-6 alkoxycarbonyl, nitro, cyano, halogen, C.sub.1-6 alkylsulfonamido, C.sub.1-6 perfluoroalkylsulfonamido, amino, C.sub.1-6 acylamino, C.sub.Type: GrantFiled: June 28, 1994Date of Patent: January 9, 1996Assignee: American Home Products CorporationInventors: Richard M. Soll, Paul J. Dollings
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Patent number: 5475132Abstract: R.sub.3, R.sub.4 and R.sub.5, each represents a hydrogen or halogen atom (at least one of R.sub.3, R.sub.4 and R.sub.5 being other than hydrogen or halogen); optionally substituted amino; optionally halogenated or hydroxylated alkyl, alkoxy, alkylalkoxy or alkylthio; or R.sub.3 and R.sub.4 (in the 3- and 4-positions) can together form a single divalent radical with 3 or 4 members containing 1 or 2 non-adjacent oxygen atoms; are useful as agricultural fungicides.Type: GrantFiled: May 27, 1994Date of Patent: December 12, 1995Assignee: Rhone-Poulenc AgrochimieInventors: Regis Pepin, Christian Schmitz, Guy-Bernard Lacroix, Philippe Dellis, Christine Veyrat
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Patent number: 5468775Abstract: The present invention concerns enaminones having the formula: ##STR1## wherein R is from the group consisting of COOCH.sub.3 and COOC.sub.2 H.sub.5 ; R.sup.1 is from the group consisting of H and CH.sub.3 ; R.sup.2 is from the group consisting of H when R.sup.1 is CH.sub.3 and CH.sub.3 when R.sup.1 is H; and R.sup.3 is from the group of first radicals consisting of benzyl, phenethyl, disubstituted phenyl and trisubstituted phenyl. The substituted species are second radicals having positive lipophilicity selected from the group consisting of F, Cl, Br, and I.Type: GrantFiled: March 2, 1993Date of Patent: November 21, 1995Assignee: Howard UniversityInventors: Kenneth R. Scott, Jesse M. Nicholson, Ivan O. Edafiogho
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Patent number: 5461045Abstract: A fused benzeneoxyacetic acid derivative of the formula: ##STR1## wherein ##STR2## is (i) ##STR3## (ii) ##STR4## (iii) ##STR5## or (iv) ##STR6## A is (i) ##STR7## or (ii) ##STR8## R.sup.1 is hydrogen or C.sub.1-4 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl or phenyl;R.sup.3 is(i) C.sub.1-15 alkyl,(ii) C.sub.1-8 alkyl substituted by one or two of benzene, C.sub.4-7 cycloalkane or 4-7 ring-membered monocyclic ring which contains one nitrogen atom or(iii) C.sub.10-15 condensed tricyclic ring;e is 3-5;f is 1-3;p is 0-4;q is 0-2;s is 0-3With the proviso that, ring(s) in R.sup.3 may be substituted by one to three of C.sub.1-4 alkyl, .sub.1-4 alkoxy, halogen atom, nitro or trihalomethyl. And, when D--B is the formula (iii) or (iv), --(CH2)p- or .dbd.CH--(CH2)s- is attached at the position of a or b on the ring.Type: GrantFiled: July 14, 1992Date of Patent: October 24, 1995Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Nobuyuki Hamanaka, Kanji Takahashi, Hidekado Tokumoto
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Patent number: 5459275Abstract: An electrophotographic photoconductor comprises an electroconductive substrate and a photoconductive layer formed thereon comprising as an effective component at least one pyrenylamine derivative of formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, W, j, k, l, m and n are specifically defined in the specification. Furthermore, a novel pyrenylamine derivative for use in the above electrophotographic photoconductor, an aldehyde compound, which is an intermediate for producing the pyrenylamine derivative, and methods of preparing the pyrenylamine derivative and the aldehyde compound are disclosed.Type: GrantFiled: June 15, 1994Date of Patent: October 17, 1995Assignee: Ricoh Company, Ltd.Inventors: Chiaki Tanaka, Masaomi Sasaki, Tamotsu Aruga, Tomoyuki Shimida, Hiroshi Adachi
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Patent number: 5457232Abstract: A pyrenylamine derivative having an unsaturated bond of formula (I), which can be employed as an organic photoconductive material for use in electrophotography: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, W, l, m, n, j and k are specifically defined in the specification, an aldehyde compound of formula (II), which is an intermediate for preparing the pyrenylamine derivative: ##STR2## and methods of producing the pyrenylamine derivative and the aldehyde compound are disclosed.Type: GrantFiled: September 9, 1994Date of Patent: October 10, 1995Assignee: Ricoh Company, Ltd.Inventors: Chiaki Tanaka, Masaomi Sasaki, Tamotsu Aruga, Tomoyuki Shimada, Hiroshi Adachi
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Patent number: 5401879Abstract: Phenylethanolamino- and phenylethanolaminomethyltetralines of formula (I) ##STR1## wherein X represents a hydrogen atom, a halogen atom, a (C.sub.1 -C.sub.4)alkyl group or a trifluoromethyl group,A represents a bond between the --COOR group and the tetraline ring, a (C.sub.1 -C.sub.4)alkylene or a (C.sub.2 -C.sub.4)alkenylene group,R is hydrogen or a (C.sub.1 -C.sub.4)alkyl group, andn is 0 or 1and their salts, are typically prepared by reaction of an epoxide of formula (IIa) ##STR2## with a tetraline derivative of formula (III) ##STR3## wherein A and n are as defined above and R' is a (C.sub.1 -C.sub.4)alkyl group, optionally followed by basic hydrolysis to obtain the compounds (I) wherein R is hydrogen. The new compounds show very interesting properties as antidepressant and intestinal spasmolytic agents.The new intermediates of formula (III) are also claimed.Type: GrantFiled: February 2, 1993Date of Patent: March 28, 1995Assignee: SanofiInventors: Domenico Badone, Umberto Guzzi, Roberto Cecchi
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Patent number: 5387594Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical,and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.Type: GrantFiled: August 4, 1992Date of Patent: February 7, 1995Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)Inventors: Jean-Michel Bernardon, William R. Pilgrim
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Patent number: 5385917Abstract: Carboxylic acid derivatives of the formula: ##STR1## are provided, which are useful for treatment of androgen dependent diseases.Type: GrantFiled: July 16, 1993Date of Patent: January 31, 1995Assignee: Mitsubishi Kasei CorporationInventors: Hiroaki Ueno, Masahiko Morioka, Fumiko Hatanaka
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Patent number: 5367096Abstract: Process for the preparation of 2,5-di(phenylamino)terephthalic acid and dialkyl esters thereof in high purity.The invention relates to a process for the preparation of dialkyl 2,5-di(phenylamino)terephthalates of the formula (I) ##STR1## in which R is a hydrogen atom or a methyl group and R' is a methyl group or ethyl group, by dehydrogenation (oxidation) of the corresponding dialkyl 2,5-di(phenylamino)-3,6-dihydroterephthalate with oxygen, which comprises blanketing with oxygen a solution or suspension of the dialkyl 2,5-di(phenylamino)-3,6-dihydroterephthalate in aromatic hydrocarbons in a stirred vessel, circulating this reaction mixture via a spraying device, so that the sprayed reaction mixture is distributed over the reaction mixture present in the stirred vessel, the sprayed reaction mixture being mixed with the circulating gas.The process has the advantage of a short reaction time, combined with favorable space-time yields and simplicity in terms of apparatus.Type: GrantFiled: August 20, 1992Date of Patent: November 22, 1994Assignee: Hoechst AktiengesellschaftInventors: Eberhard Ritter, Hans Schafer, Thomas Vollheim, Martin Schottler
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Patent number: 5357032Abstract: A diamine compound of the general formula ##STR1## wherein the arrows denote isomerism, R.sub.1 is a divalent aromatic group selected from the group consisting of ##STR2## R.sub.2 is a tetravalent aromatic group selected from the group consisting of ##STR3## and R.sub.4 is a monovalent aliphatic group selected from the group consisting of ethyl and isopropyl; and, a process for preparing same.Type: GrantFiled: August 17, 1992Date of Patent: October 18, 1994Assignee: Korea Research Institute of Chemical TechnologyInventors: Suh Bong Rhee, Ji Y. Chang, Bong S. Moon, Ji-Woong Park
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Patent number: 5347038Abstract: An ecologically and economically improved process for the preparation of 2,5-di-phenylamino-terephthalic acid and its di-alkyl esters of the formula (1) ##STR1## in which R is a hydrogen atom or a methyl group and R' is a hydrogen atom or a methyl or ethyl group.Type: GrantFiled: May 20, 1993Date of Patent: September 13, 1994Assignee: Hoechst AktiengesellschaftInventors: Otto Arndt, Hermann Fuchs, Walter Gilb
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Patent number: 5338773Abstract: The invention provides dental cement compositions and methods of using them for binding hard tooth material, metal and ceramic. The cement compositions include polymerizable acid reactive ethylenically unsaturated monomers, and a source of cations reactive therewith, to further crosslink the resulting polymer. The cements have superior adhesion to tooth without separately acid etching dentin or enamel. Compositions of are useful as dental luting cements, liners, bases and restoratives.Type: GrantFiled: April 19, 1993Date of Patent: August 16, 1994Assignee: Dentsply Research & Development Corp.Inventors: Kewang Lu, Chin-Teh Huang, Paul Hammesfahr
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Patent number: 5310682Abstract: Compounds containing .alpha.-discarbonyl groups are rendered capable of fluorescent emission by conjugation with carboxylic acid-terminated ortho-diaminoaryl reagents. The carboxylic acid groups serve as ionizable moieties which facilitate the conjugation reaction, and are retained in the conjugation product to enable, or enhance the ability of, the conjugated compounds to be separated in chromatographic and electromigration separation processes, notably electrophoresis. Ortho-dinitro derivatives of the reagents are also disclosed, these derivatives offering the advantage of stability as well as the ability to be used directly in the reaction in the presence of a reducing agent.Type: GrantFiled: June 17, 1992Date of Patent: May 10, 1994Assignee: Indiana University FoundationInventors: Milos V. Novotny, Osamu Shirota, Donald Wiesler
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Patent number: 5298647Abstract: Aromatic compounds absorbing UVB and/or UVA, substituted with an amide function, selected from the group consisting of ##STR1## whose variable substituents are as defined in the specification, e.g. ##STR2## are useful as photoprotective agents or tanning accelerators.Type: GrantFiled: December 14, 1987Date of Patent: March 29, 1994Inventors: Dominique Robert, Louis Jung
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Patent number: 5292896Abstract: Styrene derivatives of the formula ##STR1## and an electrophotographic photoconductor comprising an electroconductive support material and a photosensitive layer comprising at least one styrene derivatives of the same formula are disclosed, in which Ar represents an unsubstituted of substituted phenyl group or an unsubstituted or substituted styryl group, R represents hydrogen, a lower alkyl group or an unsubstituted or substituted phenyl group, and A is selected from the group consisting of ##STR2## wherein R.sup.1 represents a lower alkyl group or a lower alkoxy group, R.sup.2 and R.sup.3 each represent a lower alkyl group, an aralkyl group, or an unsubstituted or substituted phenyl group.Type: GrantFiled: September 4, 1991Date of Patent: March 8, 1994Assignee: Ricoh Company, Ltd.Inventors: Masayuki Shoshi, Masaomi Sasaki
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Patent number: 5292922Abstract: The invention provides N-acyl-N-phenyltetrahydrophthalamic acid derivatives represented by the general formula [I], methods of producing the same, and herbicides containing the same as the effective components, ##STR1## wherein X and Y each individually represent hydrogen atoms or halogen atoms, R.sup.1 represents a hydrogen atom, a halogen atom, a lower alkoxy group, a lower alkenyloxy group, a lower alkynyloxy group, a lower alkoxyalkoxy group or a lower alkoxycarbonylalkoxy group, R.sup.2 represents a lower alkyl group, a halogenated lower alkyl group, or a substituted or unsubstituted phenyl group, and R.sup.3 represents a lower alkoxy group, a lower alkenyloxy group, a lower alkynyloxy group, a lower alkoxyalkoxy group, a benzyloxy group or a lower alkoxycarbonylalkoxy group. The herbicides which are very useful can be widely applied to upland, paddy field, orchard, turf, forest, non-crop land, etc, and are not harmful to crops.Type: GrantFiled: April 22, 1992Date of Patent: March 8, 1994Assignee: Central Glass Company, LimitedInventors: Tetsuo Takematsu, Takashi Kume, Takeo Komata, Kiyoshi Suzuki, Matsue Minezaki, Yumiko Shirakawa, Kaoru Mori
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Patent number: 5258407Abstract: Certain 3,4-disubstituted phenols and pharmaceutically acceptable salts thereof are provided which mimic IL-1 activity by inducing IL-2 synthesis and subsequent IL-2 receptor expression. Specifically, the invention provides compounds of Formula I and acid addition salts thereof: ##STR1## wherein Y is ##STR2## NHSO.sub.2 or SO.sub.2 NH where R.sup.4 is H; Z is --O--, --NH--, --NR--, --S--, or other heteroatoms capable of hydrogen bonding with R.sup.4 to give a preferred conformation;R is alkyl;R.sup.1 is --OH;R.sup.2 is H, alkyl, cycloalkyl, aralkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted nitrogen heterocyclic group having 4 to 5 nuclear carbon atoms; andR.sup.3 is a lipophilic moiety.Type: GrantFiled: December 31, 1991Date of Patent: November 2, 1993Assignee: Sterling Winthrop Inc.Inventors: William N. Washburn, Barbara B. Lussier, Carl B. Illig, Lee H. Latimer
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Patent number: 5247091Abstract: The synthesis of enamines in aqueous media and a process for the preparation of memory enhancing 9-amino-1,2,3,4-tetrahydracridines are described.Type: GrantFiled: July 30, 1992Date of Patent: September 21, 1993Assignee: Hoechst Celanese CorporationInventor: Juergen Mueller-Lehar
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Patent number: 5241119Abstract: Process for the preparation of 4,4'-diaminodiphenylmethane and its derivatives.4,4'-diaminodiphenylmethane and its derivatives are prepared by the condensation of aniline, or its derivative, and aldehyde, or its precursor and/or isomerization of appropriate intermediate products. The reaction proceeds with zeolites acting as catalysts; these catalysts, which are selected in accordance with the reaction to be effected, are preferably zeolites based on Si, Al and B; Si, Al and Ti; Ti and Fe; ZSM-5; or Y zeolites.Type: GrantFiled: October 11, 1990Date of Patent: August 31, 1993Assignees: Eniricerche S.p.A., Enichem Synthesis S.p.A.Inventors: Mario G. Clerici, Giuseppe Bellussi, Ugo Romano
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Patent number: 5223529Abstract: Compounds of formula: ##STR1## in which R.sub.1 is (a) a phenyl radical or a substituted phenyl radical, (b) a chain --CH(R.sub.8)--COOR.sub.4, (c) a chain --CH.sub.2 --CO--NR.sub.5 R.sub.6 or (d) a phenylalkyl radical, R.sub.2 is a methylene or ethylene radical or a radical --CH(R.sub.7)--, R.sub.3 is a 1- or 2-naphthyl radical, 2- or 3-indolyl or phenylamino radical in which the phenyl ring is optionally substituted on the understanding that, when R.sub.3 is 1- or 2-naphthyl or 2- or 3-indolyl radical, R.sub.7 cannot represent a benzyl, alkylthioalkyl or phenyl radical, as well as, when R.sub.2 is a radical --CH(R.sub.7)--, their racemates and their stereoisomers, and medicinal products containing them.Type: GrantFiled: May 11, 1990Date of Patent: June 29, 1993Assignee: Rhone-Poulenc SanteInventors: Jean-Dominique Bourzat, Marc Capet, Claude Cotrel, Claude Guyon, Gerard Roussel, Franco Manfre
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Patent number: 5208365Abstract: A process for the preparation of 2,5-di(phenylamino)terephthalic acid and its dialkyl esters of formula (I): ##STR1## in which R is a hydrogen atom or a methyl group and R' is a hydrogen atom or a methyl or ethyl group.Type: GrantFiled: June 11, 1992Date of Patent: May 4, 1993Assignee: Hoechst AktiengesellschaftInventors: Hermann Fuchs, Walter Gilb, Otto Arndt
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Patent number: 5206418Abstract: The invention relates to aminotetrahydronaphthalene derivatives which are intermediates for the preparation of sulfonylaminotetrahydronaphthalenes.Type: GrantFiled: March 13, 1992Date of Patent: April 27, 1993Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Hideo Nakai, Toyoharu Yamashita, Harumichi Kohno, Yasuhiko Sasaki, Akio Odawara
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Patent number: RE34137Abstract: The present invention relates to a method of manufacturing aromatic urethane, an aromatic mononitro-compound, an aromatic primary amine, and carbon monoxide being reacted using a catalyst containing a platinum group metal-containing compound as a major constituent to prepare N,N'-di-substituted urea. The resultant N,N'-di-substituted urea is reacted with a hydroxyl group-containing organic compound to prepare an aromatic primary amine and aromatic urethane, and the aromatic primary amine is separated to obtain aromatic urethane.Type: GrantFiled: October 12, 1989Date of Patent: December 1, 1992Assignee: NKK CorporationInventors: Takao Ikariya, Masanori Itagaki, Masatsugu Mizuguchi, Itaru Sakai, Osamu Tajima