Polycyclo Ring System Which Includes Ring Chalcogen Patents (Class 548/525)
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Patent number: 5650098Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b]pyran compounds, examples of which are compounds having certain substituents at the 5 and 6-positions of the naphtho portion of the naphthopyran and at the 2-position of the pyran ring, e.g., 2,2-bis(4-methoxy phenyl)-5-methoxycarbonyl-6-morpholino-2H-naphtho[1,2-b]pyran. Certain substituents may also be present at the number 7, 8, 9 or 10 carbon atoms of the naphtho portion of the naphthopyran. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.Type: GrantFiled: October 13, 1995Date of Patent: July 22, 1997Assignee: Transitions Optical, Inc.Inventors: Anil Kumar, David B. Knowles, Barry Van Gemert
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Patent number: 5645767Abstract: Described are novel photochromic indeno-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted indeno group, the 2,1 positions of which are fused to the f side of the naphtho portion of the naphthopyran, and certain substituents at the 3-position of the pyran ring. Certain substituents may also be present at the number 5, 6, 7, 8, 9, 10, 11, 12, or 13 carbon atoms of the compounds. These compounds may be represented by the following graphic formula: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds. Optically clear articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans, and spiro(indoline)type compounds, are also described.Type: GrantFiled: October 13, 1995Date of Patent: July 8, 1997Assignee: Transitions Optical, Inc.Inventor: Barry Van Gemert
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Patent number: 5646175Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.Type: GrantFiled: June 1, 1995Date of Patent: July 8, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Raymond W. Kosley, Jr., Robert Joseph Cherill, Gerard O'Malley
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Patent number: 5646309Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are employed as intermediates in the synthesis of aminochroman compounds useful in the treatment of CNS disorders.Type: GrantFiled: May 30, 1995Date of Patent: July 8, 1997Assignee: Astra AktiebolagInventors: Eva Maria Hammarberg, Lars George Johansson, Lars-Gunnar Larsson, Rolf Noreen, Lucy Anna Renyi, Svante Bertil Ross, Daniel Dungan Sohn, Bjorn Eric Svensson, Seth-Olov Thorberg
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Patent number: 5643896Abstract: The present invention provides a compound of formula I ##STR1## wherein R.sub.1 is hydrogen, a hydroxy protecting group, or methyl;R.sub.2 and R.sub.3 are independently C.sub.1 -C.sub.6 alkyl, or R.sub.2 and R.sub.3, together with the nitrogen to which they are attached, form a heterocycle selected from the group consisting of pyrrolidino, hexamethyleneimino, morpholino, and piperidino;Z is bromo, chloro, fluoro, hydroxy, a protected hydroxy, or hydrogen; and pharmaceutically acceptable salts and solvates thereof.The present invention further provides pharmaceutical compositions containing compounds of formula I, optionally containing estrogen or progestin, and the use of such compounds alone, or in combination with estrogen or progestin, for alleviating the symptoms of post-menopausal syndrome, particularly osteoporosis, cardiovascular related pathological conditions, and estrogen-dependent cancer.Type: GrantFiled: September 22, 1995Date of Patent: July 1, 1997Assignee: Eli Lilly and CompanyInventors: George J. Cullinan, James J. Sales
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Patent number: 5639772Abstract: 3-amino-5-aryl- and 5-heteroarylchromans, as well as enantiomers and salts thereof are disclosed. Pharmaceutical compositions containing the compounds as active ingredients are also disclosed. The compounds are useful in the treatment of 5-hydroxytryptamine-mediated disorders of the central nervous system.Type: GrantFiled: May 30, 1995Date of Patent: June 17, 1997Assignee: Astra AktiebolagInventors: Eva Maria Hammarberg, Lars George Johansson, Lars-Gunnar Larsson, Rolf Noreen, Lucy Anna Renyi, Svante Bertil Ross, Daniel Dungan Sohn, Bjorn Eric Svensson, Seth-Olov Thorberg
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Patent number: 5637262Abstract: Described are novel reversible photochromic 3H-naphtho[2,1-b]pyran compounds, of the following graphic formula: ##STR1## wherein R.sub.1 is hydrogen or alkyl, R.sub.2 is hydrogen or preferably a carboalkoxy group and R.sub.3 is hydrogen or preferably an alkyl group, provided that either R.sub.1 or R.sub.2 is hydrogen, and B and B' are the aryl groups phenyl or naphthyl, a heterocyclic aromatic group or together form a spiro adamantylene group. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(oxazine) type compounds, are also described.Type: GrantFiled: May 31, 1995Date of Patent: June 10, 1997Assignee: Transitions Optical, Inc.Inventors: Barry Van Gemert, Anil Kumar
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Patent number: 5637583Abstract: Aminocyclohexylester compounds, including thioesters, are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the blockade of ion channels and the treatment of arrhythmias.Type: GrantFiled: September 27, 1994Date of Patent: June 10, 1997Assignee: University of British ColumbiaInventors: Bernard A. MacLeod, Michael J. A. Walker, Richard A. Wall
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Patent number: 5637609Abstract: A compound of formula (I): ##STR1## which have high affinity for dopamine D.sub.3 receptors and thus have potential as antipsychotic agents.Type: GrantFiled: January 29, 1996Date of Patent: June 10, 1997Assignee: SmithKline Beecham plcInventors: Geoffrey Stemp, Christopher N. Johnson
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Patent number: 5635537Abstract: A compound of the formula ##STR1## Z is hydrogen or halogen, Q is COR.sup.1 or 5-or 6-membered aryl which may contain 1 or 2 heteroatoms selected from N, 0 or S and may be substituted or fused wherein R is hydrogen or C.sub.1 -methyl (cis-configuration), R.sup.1 is C.sub.1 -C.sub.6 alkyl or an aromatic ring which may contain heteroatoms selected from O and S and may be substituted or fused to an optionally substituted benzene ring, R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sup.3 may be different groups defined in claim 1, and enantiomers/salts thereof, processes for preparation of said compounds, pharmaceutical preparations containing said compounds, use of and method of treatment of disorders in CNS by using said compounds.Type: GrantFiled: March 18, 1993Date of Patent: June 3, 1997Assignee: Astra AktiebolagInventors: Nils-Erik Anden, Berit C. E. Backlund Hook, Anna L. Bjork, Uli A. Hacksell, Sven-Erik Hillver, Ye Liu, Eva C. Mellin, Eva M. Persson, Karl J. Vallg.ang.rda, Hong Yu
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Patent number: 5635527Abstract: A novel carboxylic acid compound having a condensed ring, which is represented by the formula (I) ##STR1## wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition thereof and pharmaceutical use thereof. The novel carboxylic acid compound having a condensed ring and pharmacologically acceptable salt thereof of the present invention have superior GPIIb/IIIa antagonism in mammals inclusive of human; can be administered orally; have long life in blood and low toxicity; and show less side-effects. Accordingly, they are extremely useful for the prophylaxis and treatment of thrombotic diseases and other diseases.Type: GrantFiled: February 6, 1996Date of Patent: June 3, 1997Assignee: The Green Cross CorporationInventors: Shinichiro Ono, Tomohiro Yoshida, Atsuyuki Ashimori, Keigo Kosaka, Takehiro Okada, Kazuhiro Maeda, Masahiro Eda, Fumio Mori, Yoshihisa Inoue, Hajime Ebisu, Teruaki Imada, Ruriko Ikegawa, Feng Wang, Norifumi Nakamura
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Patent number: 5624952Abstract: The present invention is concerned with vasoconstricive [(benzodioxan, benzofuran or benzopyran)alkylamino]alkyl substituted guanidines having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein X is O, CH.sub.2 or a direct bond; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; or R.sup.2 and R.sup.3 may be taken together to form a bivalent radical of formula --(CH.sub.2).sub.m --, wherein m is 4 or 5; or R.sup.1 and R.sup.2 taken together may form a bivalent radical of formula --CH.dbd.CH-- or of formula --(CH.sub.2).sub.n --, wherein n is 2, 3 or 4; or R.sup.3 may represent a bond when R.sub.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd., --CH.dbd.CH--N.dbd., or --CH.dbd.N--CH.dbd.; R.sup.4 is hydrogen or C.sub.1-6 alkyl; Alk.sup.1 is a bivalent C.sub.Type: GrantFiled: April 15, 1996Date of Patent: April 29, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Guy R. E. Van Lommen, Marcel F. L. De Bruyn, Walter J. J. Janssens
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Patent number: 5624951Abstract: A compound of formula V: ##STR1## wherein all the R's groups are as defined in the specification, is useful in the treatment of bacterial infections.Type: GrantFiled: March 1, 1995Date of Patent: April 29, 1997Assignee: Pfizer Inc.Inventors: Bingwei Yang, Joyce Sutcliffe, Chris J. Dutton
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Patent number: 5624953Abstract: This invention provides novel compounds and pharmaceutical methods comprising the administration of a compound of the Formula I: ##STR1## wherein n, m, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are variables.Type: GrantFiled: February 2, 1996Date of Patent: April 29, 1997Assignee: Eli Lilly and CompanyInventors: Samantha J. Ambler, William F. Heath, Jr., Jai Pal Singh, Colin W. Smith, Lawrence E. Stramm
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Patent number: 5622974Abstract: This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 3-benzyl-benzofurans which are .alpha.-substituted with ether, thioether amino, cyano or halo that are useful for the treatment of the various medical indications associated with post-menopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus and cervix. The present invention further relates to intermediate compounds and processes useful for preparing the pharmaceutically active compounds of the present invention, and pharmaceutical compositions.Type: GrantFiled: March 10, 1995Date of Patent: April 22, 1997Assignee: Eli Lilly and CompanyInventor: Brian S. Muehl
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Patent number: 5623005Abstract: A naphthopyran compound of general formula (I) ##STR1## wherein R.sub.1 represents a group of the formula --NR.sub.2 R.sub.3 wherein each of R.sub.2 and R.sub.3, which may be the same or different, independently represents an alkyl group, or a carbocyclic or heterocyclic group, or R.sub.2 and R.sub.3 taken together with the nitrogen atom to which they are attached represent a heterocyclic ring having one or more hetero atoms and which may optionally carry at least one substituent selected from alkyl, aryl, or heteroaryl groups; each of R.sub.4 and R.sub.5, which may be the same or different, independently represents an alkyl, alkenyl, carbocyclic or heterocyclic group, or R.sub.4 and R.sub.5 taken together with the carbon atom to which they are attached form a carboxylcyclic ring or a heterocyclic ring; and R.sub.6 represents a hydrogen atom or a substituent selected from alkyl, alkoxy, aryl, aryloxy, heteroaryl, halogen, a group of formula R.sub.Type: GrantFiled: November 2, 1995Date of Patent: April 22, 1997Assignee: Pilkington PLCInventors: Martin Rickwood, Katharine E. Smith, Christopher D. Gabbutt, John D. Hepworth
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Patent number: 5618835Abstract: A compound having the structure: ##STR1## pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.Type: GrantFiled: February 1, 1996Date of Patent: April 8, 1997Assignee: The Procter & Gamble CompanyInventors: Laurence I. Wu, John M. Janusz
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Patent number: 5612370Abstract: Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein a, b and d are all carbon atoms or one of a, b and d is a nitrogen atom or --N(O)-- and the others are carbon atoms; Y is a single bond, --CH.sub.2 --, --C(O)--, --O--, --S-- or --N(R.sup.8)--; and R.sup.1 to R.sup.7 are as defined herein. These compounds have potassium channel activating activity and are useful, therefore for example, as cardiovascular agents.Type: GrantFiled: June 7, 1995Date of Patent: March 18, 1997Assignee: Bristol-Myers Squibb CompanyInventor: Karnail S. Atwal
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Patent number: 5607624Abstract: A process for the preparation of compounds of formula I ##STR1## wherein the general symbols are as defined in claim 1, which comprises reacting a compound of formula III ##STR2## wherein the general symbols are as defined in claim 1, with a compound of formula IV[H].sub.n --R.sub.1 (IV).Type: GrantFiled: September 12, 1994Date of Patent: March 4, 1997Assignee: Ciba-Geigy CorporationInventors: Peter Nesvadba, Samuel Evans, Ralf Schmitt
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Patent number: 5605924Abstract: The present invention relates to compounds of the formula ##STR1## where X is a bond or --CH2--;R.sup.2 is pyrrolidino;R is OH, --OSO.sub.2 --(CH.sub.2).sub.n --CH.sub.3 or ##STR2## R.sup.1 is hydrogen, OH, fluoro, chloro, --OSO.sub.2 --(CH.sub.2).sub.n --CH.sub.3 or ##STR3## each R.sup.3 is independently C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, unsubstituted or substituted phenyl where the substituent is fluoro, chloro, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy;each n is independently 3, 4 or 5; and pharmaceutically acceptable salts and solvates thereof; provided that at least one of R and R.sup.1 is ##STR4## The invention also relates to methods of use of the compounds of formula I and pharmaceutical compositions which comprise compounds of formula I.Type: GrantFiled: January 17, 1996Date of Patent: February 25, 1997Assignee: Eli Lilly and CompanyInventors: Larry J. Black, Henry U. Bryant, George J. Cullinan
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Patent number: 5606080Abstract: Tocopherol derivatives of the following formula (I) or a pharmacologically acceptable salt thereof ##STR1## wherein R.sub.l and R.sub.2 are the same or different and each represents hydrogen or methyl; R.sub.3 represents an .alpha.-amino acid, .omega.-amino acid, or peptide bonding via the N terminus thereof, except that in the case of cysteine or glutathione which has a thiol group, bonding via the thiol group, are water-soluble and can be expected to be of use as a cerebral function-improving drug and an anticataract drug. Moreover, these compounds are of value as an UV-absorber, a skin care ingredient, or a stabilizer for other cosmetic ingredients.Type: GrantFiled: May 11, 1995Date of Patent: February 25, 1997Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Kazumi Ogata, Hidetoshi Nakao
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Patent number: 5604182Abstract: Compounds of formula (I): ##STR1## and salts and esters thereof have valuable anthelmintic, acaricidal and insecticidal activities. Methods of preparing the compounds are also provided.Type: GrantFiled: July 11, 1994Date of Patent: February 18, 1997Assignee: Sankyo Company LimitedInventors: Yasuhiro Morisawa, Akio Saito, Toshimitsu Toyama, Susumu Kaneko
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Anti-tumor compounds, pharmaceutical compositions, methods for preparation thereof and for treatment
Patent number: 5599820Abstract: The present invention is directed to novel taxanes useful as chemotherapeutic agents or their precursors. Processes for preparing the novel taxanes include coupling reactions, in the presence of a base, of baccatin of formula (III) or (IV) ##STR1## with .beta.-lactams of formula (V). ##STR2## The invention also provides pharmaceutical compositions including the novel taxanes and methods for treatment of certain cancers with these new compounds.Type: GrantFiled: June 5, 1995Date of Patent: February 4, 1997Assignees: The Research Foundation of State University of New York, Indena SpA Gruppo Inverni Della BeffaInventors: Iwao Ojima, Ezio Bombardelli -
Patent number: 5599833Abstract: The present invention relates to sulfonate and carbamate derivatives of 3-aroylbenzo[b]thiophenes, pharmaceutical formulations containing these compounds and methods of using such compounds for inhibiting the loss of bone, lowering serum cholesterol levels and therapeutically treating hormone dependent mammalian breast and uterine carcinoma.Type: GrantFiled: January 17, 1996Date of Patent: February 4, 1997Assignee: Eli Lilly and CompanyInventors: Larry J. Black, Henry U. Bryant, George J. Cullinan
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Patent number: 5578619Abstract: This invention relates to compounds of Formula I and the stereoisomers and pharmaceutically acceptable salts thereof ##STR1## wherein R is alkyl, alkenyl, alkynyl, or (CH.sub.2).sub.m R.sup.3 where R.sup.3 is cycloalkyl and m is 1 or 2;R.sup.1 is alkyl;R.sup.2 is alkyl, aryl or aryl substituted with halogen or alkyl;R.sup.4 is alkyl;n is an integer from 1 to 5;p is an integer from 0 to 6;Y is NH, oxygen or sulfur; andZ is hydrogen, alkyl, alkoxy, NR.sup.6 R.sup.5 wherein R.sup.6 and R.sup.5 are independently hydrogen or alkyl, or SR.sup.7 wherein R.sup.7 is hydrogen, benzyl or alkyl.The compounds of Formula I are leukotriene B.sub.4 antagonists and are useful as anti-inflammatory agents and in the treatment of leukotriene B.sub.4 mediated conditions.Type: GrantFiled: December 8, 1995Date of Patent: November 26, 1996Inventors: Stevan W. Djuric, Thomas D. Penning
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Patent number: 5576343Abstract: An anticoagulant agent which comprises, as an active ingredient, an aromatic amidine derivative represented by the following general formula (1) or a salt thereof: ##STR1## wherein the group represented by ##STR2## is a group selected from indolyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, naphthyl, tetrahydronaphthyl and indanyl; X is a single bond, an oxygen atom, a sulfur atom or a carbonyl group; and Y is a saturated or unsaturated 5- or 6-membered heterocyclic moiety or cyclic hydrocarbon moiety optionally having a substituent group, an amino group optionally having a substituent group or an aminoalkyl group optionally having a substituent group.The inventive compound has a high anticoagulant capacity based on its excellent FXa inhibition activity.Type: GrantFiled: June 6, 1995Date of Patent: November 19, 1996Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Takayasu Nagahara, Naoaki Kanaya, Kazue Inamura, Yukio Yokoyama
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Patent number: 5574175Abstract: The present invention provides a process for the manufacture of 2-aryl-5-(perfluoroalkyl)pyrrole-3-carbonitrile comprising the cycloaddition of 5-amino-4-aryl-2-perfluoroalkyl-1,3-oxazole and the appropriate 1,3-dipolarifile. The arylpyrrole-3-carbonitrile product and its derivatives are highly effective insecticidal, acaricidal and nematocidal agents.Type: GrantFiled: May 16, 1995Date of Patent: November 12, 1996Assignee: American Cyanamid Co.Inventor: Venkataraman Kameswaran
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Patent number: 5574034Abstract: The invention provides pharmaceutical compounds of the formula: ##STR1## in which A - - - B is CH.sub.2 --CH.sub.2 or CH.dbd.CH;X is a pyridine or benzene ring;when X is pyridine n is 0;when x is benzene n is 0, 1 or 2 and when A - - - B is CH.sub.2 --CH.sub.2. R.sup.1 is attached at any of the positions 7 to 10, and when A - - - B is CH.dbd.CH, R.sup.1 is attached at any of the positions 5 to 10;each R.sup.1 is halo, carboxy, trifluoromethyl, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, hydroxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkoxy, nitrogen-containing heterocyclyl, nitro, trifluoromethoxy, --COOR.sup.5 where --R.sup.5 is an ester group, --COR.sup.6, --CONR.sup.6 R.sup.7 or --NR.sup.6 R.sup.7 where R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl;R.sup.2 is phenyl, naphthyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted, or R.sup.Type: GrantFiled: June 5, 1995Date of Patent: November 12, 1996Assignee: Eli Lilly and CompanyInventor: Andrew C. Williams
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Patent number: 5554612Abstract: The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.Type: GrantFiled: May 26, 1995Date of Patent: September 10, 1996Inventors: John W. Patterson, David Morgans, Jr., Eric B. Sjogren, David B Smith, Francisco X. Talam as, Dean R. Artis, Alicia Cervantes, Todd R. Elworthy, Mario Fern andez, Fidencio Franco, Ronald C. Hawley, Teresa Lara, David G. Loughhead, Peter H. Nelson, Alejandra Trejo, Ann M. Waltos, Robert J. Weikert
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Patent number: 5552090Abstract: Described are novel reversible photochromic naphthopyran compounds, examples of which are compounds substituted at the 3 position of the pyran ring with (i) an aryl substituent and (ii) a phenyl substituent having a 5- or 6-member heterocyclic ring fused at the number 3 and 4 carbon atoms of the phenyl substituent, and at the 6 position of the naphthyl portion of the naphthopyran compound with a nitrogen-containing heterocyclic ring. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.Type: GrantFiled: December 20, 1994Date of Patent: September 3, 1996Assignee: PPG Industries, Inc.Inventors: Barry Van Gemert, David B. Knowles
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Patent number: 5552401Abstract: The present invention provides a compound of formula I ##STR1## wherein R.sub.1 is hydrogen, a hydroxy protecting group, or methyl;R.sub.2 and R.sub.3 are independently C.sub.1 -C.sub.6 alkyl, or R.sub.2 and R.sub.3, together with the nitrogen to which they are attached, form a heterocycle selected from the group consisting of pyrrolidino, hexamethyleneimino, morpholino, and piperidino;Z is bromo, chloro, fluoro, hydroxy, a protected hydroxy, or hydrogen; and pharmaceutically acceptable salts and solvates thereof.The present invention further provides pharmaceutical compositions containing compounds of formula I, optionally containing estrogen or progestin, and the use of such compounds alone, or in combination with estrogen or progestin, for alleviating the symptoms of post-menopausal syndrome, particularly osteoporosis, cardiovascular related pathological conditions, and estrogen-dependent cancer.Type: GrantFiled: February 28, 1995Date of Patent: September 3, 1996Assignee: Eli Lilly and CompanyInventors: George J. Cullinan, James J. Sales
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Patent number: 5543533Abstract: Photochromic products belonging to the group of chromenes having general formula (I): ##STR1##Type: GrantFiled: June 2, 1994Date of Patent: August 6, 1996Assignee: Great Lakes Chemical Italia S.r.l.Inventors: Pietro Allegrini, Nereo Nodari, Luciana Crisci, Vincenzo Malatesta
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Patent number: 5543422Abstract: Heterocyclic amines of the formulaAr-X-A-NR.sup.1 R.sup.2wherein Ar is a bicyclic or tricyclic aromatic group which is unsubstituted or which bears one or more substituents selected from halo, nitro and cyano groups and alkyl and alkoxy groups each of up to 4 carbon atoms;wherein X is a direct link or is --O--, --S--, --SO-- or --SO.sub.2 -- or has the formula --C(R.sup.3).dbd.CH-- wherein R.sup.3 is hydrogen or alkyl of up to 4 carbon atoms;wherein A is straight or branched alkylene or alkenylene of 3 to 8 carbon atoms which may be interrupted by --O--, --S-- or --NH--;and wherein NR.sup.1 R.sup.2 is a cyclic amino group;or a pharmaceutically acceptable acid addition salt thereof, are of value for therapeutic use, particularly in the treatment of myocardial ischaemia and hypertension and in the treatment of fungal infections.Type: GrantFiled: March 23, 1995Date of Patent: August 6, 1996Assignee: British Technology Group LimitedInventors: Ian G. C. Coutts, Pamela J. Cummins
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Patent number: 5543427Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.Type: GrantFiled: August 24, 1994Date of Patent: August 6, 1996Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Raymond W. Kosley, Jr., Robert J. Cherill, Gerard O'Malley
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Patent number: 5541199Abstract: Compounds of the formula: ##STR1## in which n is one of the integers 1, 2, 3,or 4; m is one of the integers 0 or 1; R is ##STR2## or a pharmaceutically acceptable salt thereof, are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analagous drugs.Type: GrantFiled: June 2, 1995Date of Patent: July 30, 1996Assignee: American Home Products CorporationInventor: Richard E. Mewshaw
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Patent number: 5538969Abstract: The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.Type: GrantFiled: May 26, 1995Date of Patent: July 23, 1996Assignee: Syntex (U.S.A.) Inc.Inventors: David Morgans, Jr., Eric B. Sjogren, David B. Smith, Francisco X. Talam as, Dean R. Artis, Alicia Cervantes, Todd R. Elworthy, Mario Fern andez, Fidencio Franco, Ronald C. Hawley, Teresa Lara, David G. Loughhead, Peter H. Nelson, John W. Patterson, Alejandra Trejo, Ann M. Waltos, Robert J. Weikert
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Patent number: 5539112Abstract: 5-Aminoflavone derivatives represented by the formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and represent hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, halogen-substituted or unsubstituted lower alkanoyl or lower alkoxycarbonyl, X.sup.1, X.sup.2, Y.sup.1 and Y.sup.2 are the same or different and represent hydrogen, halogen or lower alkyl, at least one of X.sup.1 and X.sup.2 represents halogen or lower alkyl, X.sup.3 represents hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, lower alkynyl, halogen, hydroxy, substituted or unsubstituted lower alkoxy, NR.sup.5 R.sup.6 (wherein R.sup.5 and R.sup.6 are the same or different and represent hydrogen, or substituted or unsubstituted lower alkyl, or R.sup.5 and R.sup.Type: GrantFiled: June 5, 1995Date of Patent: July 23, 1996Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Tsutomu Akama, Shun-ichi Ikeda, Yasushi Shida, Masaji Kasai, Hiroyuki Ishida, Uichiro Kimura, Katsushige Gomi, Hiromitsu Saito, Kimihisa Ueno
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Patent number: 5536833Abstract: A process for preparing compounds of the formula ##STR1## where a, b, c, R.sub.1, R.sub.2, and R.sub.3 are as defined herein including the step of alkylating a phenol of formula ##STR2## with an acetylene of formula ##STR3## where X is chlorine; bromine; --OC(O)--R.sub.5, where R.sub.5 is alkyl, aryl or substituted aryl; or --OCO.sub.2 R.sub.6, where R.sub.6 is alkyl or ##STR4## in the presence of a catalytic amount of a cuprous or cupric salt. The compounds of formula I are intermediates useful in the preparation of pyranyl cyanoguanidine derivatives.Type: GrantFiled: May 26, 1995Date of Patent: July 16, 1996Assignee: E. R. Squibb & Sons, Inc.Inventors: Jollie D. Godfrey, Jr., Richard H. Mueller, Thomas C. Sedergran, Nachimuthu Soundararajan
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Patent number: 5532254Abstract: A method for modulating calcium channels, increasing the density of calcium channels in vascular and cardiac tissue with no changes in inotropic or pressor response, comprising administering to a warm-blooded animal in need thereof a pharmaceutically-effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.4 alkyl, --CO--(C.sub.1 -C.sub.6 alkyl), or --CH.sub.2 Ar, --CO--Ar, wherein Ar is phenyl or substituted phenyl;R.sup.2 is selected from the group consisting of pyrrolidine, hexamethylenemino, and piperidino; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: June 7, 1995Date of Patent: July 2, 1996Assignee: Eli Lilly and CompanyInventor: Nancy L. Bowling
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Patent number: 5523309Abstract: The present invention provides a compound of formula I ##STR1## wherein R.sub.1 is H, OH, halo, OCO(C.sub.1 -C.sub.6 alkyl), OCO(aryl), OSO.sub.2 (C.sub.4 -C.sub.6 alkyl), OCOO(C.sub.1 -C.sub.6 alkyl), OCOO(aryl), OCONH(C.sub.1 -C.sub.6 alkyl), or OCON(C.sub.1 -C.sub.6 alkyl).sub.2 ;R.sub.2 is aryl, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, or 4-cyclohexanol;R.sub.3 is O(CH.sub.2).sub.2 or O(CH.sub.2).sub.3 ;R.sub.4 and R.sub.5 are optionally CO(CH.sub.2).sub.2 CH.sub.3, CO(CH.sub.2).sub.3 CH.sub.3 C.sub.1 -C.sub.6 alkyl, or R.sub.4 and R.sub.5 combine to form, with the nitrogen to which they are attached, piperidine, morpholine, pyrrolidine, 3-methylpyrrolidine, 3,3-dimethylpyrrolidine, 3,4-dimethylpyrrolidine, azepine, or pipecoline;R.sub.6 is >CH(C.sub.1 -C.sub.5 alkyl), >CH(C.sub.2 -C.sub.5 alkenyl), >C.dbd.CH(C.sub.1 -C.sub.5 alkyl) >CH(aryl), >C(OH)(C.sub.1 -C.sub.5 alkyl), >C(OH)(C.sub.2 -C.sub.5 alkenyl), >C(OH)aryl;and pharmaceutically acceptable salts thereof.Type: GrantFiled: March 10, 1995Date of Patent: June 4, 1996Assignee: Eli Lilly and CompanyInventors: Henry U. Bryant, Jeffrey A. Dodge
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Patent number: 5519052Abstract: Carbonarins A, B, C, D, E, F, G, and H have been isolated from the sclerotia of the fungus Aspergillus carbonarius. The carbonarins are effective for controlling Coleopteran and Lepidopteran insects. The carbonarins have the structure: ##STR1## wherein: R.sub.1 is a hydrogen atom or a hydroxy group; R.sub.2 is a hydrogen atom or a methoxy group; R.sub.3 is a hydrogen atom or a naphthopyrone group; and X is an oxygen atom or an NH group.Type: GrantFiled: July 29, 1994Date of Patent: May 21, 1996Assignees: The United States of America as represented by the Secretary of Agriculture, University of Iowa Research Foundation and Biotechnology Research and Development Corp.Inventors: Ali A. Alfatafta, Patrick F. Dowd, James B. Gloer, Donald T. Wicklow
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Patent number: 5519023Abstract: The invention relates to compounds of the general formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and Z are as defined in the description, their optical isomers and their addition salts with a pharmaceutically-acceptable acid or base and medicaments containing the same, useful in the treatment and prevention of stress, anxiety, and related ailments.Type: GrantFiled: July 2, 1993Date of Patent: May 21, 1996Assignee: Adir et CompagnieInventors: Marc Payard, Genevieve Baziard-Mouysset, Gilbert De Saqui-Sannes, Beatrice Guardiola, Daniel-Henri Caignard, Pierre Renard, Gerard Adam
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Patent number: 5516917Abstract: This invention relates to compounds of Formula I and the stereoisomers and pharmaceutically acceptable salts thereof ##STR1## wherein R is alkyl, alkenyl, alkynyl, or cycloalkylalkyl;R.sup.1 is alkyl;R.sup.2 represents alkyl from 1 to 5 carbon atoms, aryl or aryl substituted with halogen or alkyl from 1 to 5 carbon atoms;R.sup.6 is alkyl;n is 1 to 5;p is 0 to 6;x is 0 or 2; andR.sup.4 and R.sup.5 are independently hydrogen or alkyl or together with N form a cycloalkylamine.The compounds of Formula I are leukotriene B.sub.4 antagonists and are useful as anti-inflammatory agents and in treating disease conditions mediated by LTB.sub.4.Type: GrantFiled: June 8, 1994Date of Patent: May 14, 1996Assignee: G. D. Searle & Co.Inventors: Steven W. Djuric, Stella S. Yu
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Patent number: 5514699Abstract: The invention provides pharmaceutical compounds of the formula: ##STR1## in which A - - - B is CH.sub.2 --CH.sub.2 or CH.dbd.CH;X is a pyridine or benzene ring;when X is pyridine n is 0;when X is benzene n is 0, 1 or 2 and when A - - - B is CH.sub.2 --CH.sub.2, R.sup.1 is attached at any of the positions 7 to 10, and when A - - - B is CH.dbd.CH, R.sup.1 is attached at any of the positions 5 to 10;and salts thereof.Type: GrantFiled: March 21, 1994Date of Patent: May 7, 1996Assignee: Lilly Industries LimitedInventor: Andrew C. Williams
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Patent number: 5514706Abstract: This invention provides novel compounds and pharmaceutical methods comprising the administration of a compound of the Formula I: ##STR1## wherein n, m, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are variables.Type: GrantFiled: November 21, 1994Date of Patent: May 7, 1996Assignee: Eli Lilly and CompanyInventors: Samantha J. Ambler, William F. Heath, Jr., Jai P. Singh, Colin W. Smith, Lawrence E. Stramm
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Patent number: 5514817Abstract: Described are novel reversible photochromic phenanthropyran compounds, examples of which are substituted 2H-phenanthro 4,3-b!pyran and 3H-phenanthro 1,2-b!pyran compounds. The 2H-phenanthropyran compounds have certain substituents at the number 5 and 6 carbon atoms of the phenanthro portion of the phenanthropyran and at the 2 position of the pyran ring. Certain substituents may also be present at the number 7, 8, 9, 10, 11, or 12 carbon atoms of the phenanthro portion of the phenanthropyran. The 3H-phenanthropyran compounds have certain substituents at the number 11 and 12 carbon atoms of the phenanthro portion of the phenanthropyran and at the 3 position of the pyran ring. Certain substituents may also be present at the number 5, 6, 7, 8, 9, or 10 carbon atoms of the phenanthro portion of the phenanthropyran. Also described are polymeric organic host materials that contain or that are coated with such compounds.Type: GrantFiled: August 4, 1994Date of Patent: May 7, 1996Assignee: PPG Industries, Inc.Inventor: David B. Knowles
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Patent number: 5512560Abstract: HIV protease inhibitors containing hydroxypyrrolidine or hydroxypiperidine with one or more basic amines are disclosed.Type: GrantFiled: March 29, 1994Date of Patent: April 30, 1996Assignee: Merck & Co., Inc.Inventors: Byeong M. Kim, Joseph P. Vacca
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Patent number: 5510357Abstract: The present invention provides pharmaceutically active compounds of formula I ##STR1## wherein R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO (C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl);R.sup.2 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl), or halo, providing when Z is --S--, R.sup.2 is not halo;R.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino;n is 2 or 3; andz is --O-- or --S--;or a pharmaceutically acceptable salt thereof for, inter alia, alleviating the symptoms of post menopausal syndrome and hormonally-dependent cancer, particularly breast cancer.Type: GrantFiled: February 28, 1995Date of Patent: April 23, 1996Assignee: Eli Lilly and CompanyInventor: Alan D. Palkowitz
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Patent number: 5510358Abstract: The present invention provides pharmaceutically active compounds of formula I ##STR1## wherein R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl);R.sup.2 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl), or halo, providing when Z is --S--, R.sup.2 is not halo;R.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino;n is 2 or 3; andz is --O-- or --S--;or a pharmaceutically acceptable salt thereof, for treating endometriosis.Type: GrantFiled: June 6, 1995Date of Patent: April 23, 1996Assignee: Eli Lilly and CompanyInventor: Alan D. Palkowitz
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Patent number: 5508450Abstract: Benzopyran derivatives which have an inhibitory effect on the Maillard reaction as well as an antioxidizing effect are described herein. These derivatives may be utilized in the treatment and/or prevention of diabetic complications such as, for example, coronary heart disease, peripheral circulatory insufficiency or failure, cerebrovascular hindrance, neurogenous diabetes, nephropathy, arteriosclerosis, arthrosclerosis, cataracts and retinopathy. Further, the derivatives may also be used in the treatment and/or prevention of diseases induced by aging and in the treatment and/or prevention of diseases caused by the formation of peroxidized fat.Type: GrantFiled: September 30, 1994Date of Patent: April 16, 1996Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Shuichi Ohuchida, Masaaki Toda, Tsumoru Miyamoto