Phosphorus Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/337)
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Patent number: 5910600Abstract: A bisphosphite compound of the following formula (A): ##STR1## wherein --Ar--Ar-- is a bisarylene group represented by any one of the formulae (A-I) to (A-III) defined in the specification, and each of Z.sub.1 to Z.sub.4 is a C.sub.4-20 aromatic or heteroaromatic group which may have a substituent, wherein each of substituents on carbon atoms of an aromatic ring adjacent to the carbon atom bonded to the oxygen atom in each of Z.sub.1 to Z.sub.4, is a C.sub.0-2 group, and each pair of Z.sub.1 and Z.sub.2, and Z.sub.3 and Z.sub.4, are not bonded to each other.Type: GrantFiled: April 28, 1997Date of Patent: June 8, 1999Assignee: Mitsubishi Chemical CorporationInventors: Hisao Urata, Hiroaki Itagaki, Eitaro Takahashi, Yasuhiro Wada, Yoshiyuki Tanaka, Yasukazu Ogino
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Patent number: 5900410Abstract: The present invention is directed to compositions, methods and kits for treating areas of H. pylori infection in the GI tract. The active ingredient is an antibiotic-bisphosphonate adduct wherein the antibiotic is selected for its ability to eradicate H. pylori. Other components include a salt of a divalent cation that is insolubilized in vivo at alkaline pH, and optionally a substrate from which the enzyme urease liberates NH.sub.3.Type: GrantFiled: August 12, 1997Date of Patent: May 4, 1999Inventor: John F. Hartmann
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Patent number: 5854237Abstract: Tricyclic diazepines of the formula: ##STR1## wherein A, B, D, E, F, Y and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.Type: GrantFiled: June 17, 1997Date of Patent: December 29, 1998Assignee: American Cyanamid CompanyInventors: Jay Donald Albright, Marvin Fred Reich, Fuk-Wah Sum, Efren Guillermo Delos Santos
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Patent number: 5843944Abstract: Tricyclic diazepines of the formula: ##STR1## wherein A, B, D, E, F, Y and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.Type: GrantFiled: July 11, 1997Date of Patent: December 1, 1998Assignee: American Cyanamid CompanyInventors: Jay Donald Albright, Marvin Fred Reich, Fuk-Wah Sum, Efren Guillermo Delos Santos
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Patent number: 5840745Abstract: Novel hydrosoluble 3-arylidene-2-oxindole derivatives, having tyrosine kinase inhibitor activity, encompassed by general formula (I), wherein m is zero, 1 or 2; A is a bicyclic ring chosen from tetralin, naphthalene, quinoline and indole; R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl; one of R.sup.2 and R.sup.3 independently is hydrogen and the other is a substituent selected from: a C.sub.1 -C.sub.6 alkyl group substituted by 1, 2 or 3 hydroxy groups; --SO.sub.3 R.sup.4 in which R.sup.4 is hydrogen or C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by 1, 2 or 3 hydroxy groups; --SO.sub.2 NHR.sup.5 in which R.sup.5 is as R.sup.4 defined above or a --(CH.sub.2).sub.n --N(C.sub.1 -C.sub.6 alkyl).sub.2 group in which n is 2 or 3; --COOR.sup.6 in which R.sup.6 is C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl or by 1, 2 or 3 hydroxy groups or phenyl; --CONHR.sup.7 in which R.sup.7 is hydrogen, phenyl or C.sub.1 -C.sub.Type: GrantFiled: September 25, 1996Date of Patent: November 24, 1998Assignee: Pharmacia S. p. A.Inventors: Franco Buzzetti, Maria Gabriella Brasca, Antonio Longo, Dario Ballinari
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Patent number: 5827853Abstract: This invention relates to a cosmetic composition containing at least one NPY-antagonist component mixed with an excipient for cosmetic preparations.Type: GrantFiled: January 27, 1997Date of Patent: October 27, 1998Assignee: SanofiInventors: Elisabeth Blanc-Ferras, Francois Bomo Colombie, Bernard Breda, Jean Courregelogue, Catherine Ducasse, Remy Mounier, Paul Raymond, Michel Sabadie, Claudine Serradeil Le Gal, Vilain Pol, Jean Marie Pereillo
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Patent number: 5821241Abstract: Compounds of the invention have the formula ##STR1## The compounds have fibrinogen receptor antagonist activity.Type: GrantFiled: August 1, 1995Date of Patent: October 13, 1998Assignee: Merck & Co., Inc.Inventors: David Alan Claremon, John J. Baldwin, Nigel Liverton, Ben Askew
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Patent number: 5760028Abstract: This invention relates to novel heterocycles including 3-?1-?3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzylo xycarbonylamino)propionic acid, which are useful as antagonists of the .alpha..sub.v .beta..sub.3 integrin and related cell surface adhesive protein receptors, to 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 cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.Type: GrantFiled: December 20, 1996Date of Patent: June 2, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Prabhakar Kondaji Jadhav, Joseph James Petraitis, Douglas Guy Batt
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Patent number: 5750525Abstract: Compounds of formula I are described ##STR1## in which R.sup.1, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 have the meanings mentioned in the application as well as their production and use in pharmaceutical agents.Type: GrantFiled: March 8, 1996Date of Patent: May 12, 1998Assignee: Schering AktiengesellschaftInventors: Andreas Huth, Lechoslaw Turski
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Patent number: 5750526Abstract: Pyrido?1,2,3-de!quinoxaline derivatives of formula I ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 each mean hydrogen, --POXY, halogen or --COR,R.sup.4 means hydrogen or OH,R.sup.5, R.sup.6 and R.sup.7 are the same or different and mean hydrogen, halogen, nitro, NR.sup.12 R.sup.13, cyano, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-4 alkoxy, orR.sup.5 and R.sup.6 or R.sup.6 and R.sup.7 represent a fused benzene ring, and means a single or double bond,are described as well as their production and use in pharmaceutical agents.Type: GrantFiled: December 27, 1995Date of Patent: May 12, 1998Assignee: Schering AktiengesellschaftInventors: Martin Kruger, Werner Seelen, Lechoslaw Turski
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Patent number: 5741785Abstract: Imidazo?1,2-a!quinoxalinone derivatives of the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 are the same or independently are H, alkyl, alkoxy, halogen, NO.sub.2, NH.sub.2, CF.sub.3, CN, SO.sub.2 CH.sub.3, SO.sub.2 CF.sub.3, SO.sub.2 NR'R" or a 5- or 6-membered N-containing heterocyclic ring, optionally substituted, and R', R" are independently H or alkyl; and R.sup.4 is H or CH.sub.2 -R.sup.6 ; and R.sup.6 is H, halogen, POR'"R"", NR.sup.7 R.sup.8 or a 5- or 6-membered N-containing heterocyclic ring optionally substituted, and R'", R"" are independently hydroxy or alkoxy; and ##STR2## R.sup.7, R.sup.8 are the same or independently are H, or alkyl optionally substituted; and n is 1, 2 or 3;R.sup.5 is ##STR3## and R.sup.9 is OH, alkoxy, H or NR.sup.10 R.sup.11 ; and R.sup.10, R.sup.11 are the same or independently are H, NH.sub.2 or OH; and X is O or S; and Y is O, S or NH.sub.Type: GrantFiled: February 8, 1995Date of Patent: April 21, 1998Assignee: Novo Nordisk A/SInventor: Lone Jeppesen
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Patent number: 5716993Abstract: The present invention provides an anthranilic acid derivative having a cGMP-PDE inhibitory activity.An anthranilic acid derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof: ##STR1## ?wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent the same or different from each other, a hydrogen atom, a halogen atom, a hydroxy group, an optionally halogenated lower alkyl group, an optionally halogenated lower alkoxy group, a nitro group, a hydroxyalkyl group, a cyano group or the like; R.sup.5 and R.sup.6 represent the same or different from each other, a hydrogen atom, a halogen atom, a hydroxy group, a cyano group, an optionally halogenated lower alkyl group, an optionally halogenated lower alkoxy group or the like;W represents a group of the formula: --N.dbd. or --CH.dbd.; R.sup.7 and R.sup.Type: GrantFiled: September 14, 1995Date of Patent: February 10, 1998Assignee: Eisai Co., Ltd.Inventors: Fumihiro Ozaki, Keiji Ishibashi, Hironori Ikuta, Hiroki Ishihara, Shigeru Souda
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Patent number: 5716958Abstract: A compound represented by the formula (1): ##STR1## wherein, m is an integer of 1 to 3;n is an integer 0 or 1;A represents CH or N atom, and forms together with the N atom bonded to the carbonyl group a piperidine ring or a piperazine ring;R.sub.1 independently represents a straight or branched chain alkyl group having 1 to 4 carbon atoms; a cycloalkyl group having 3 to 8 carbon atoms; a phenyl group, unsubstituted or substituted with a halogen atom or with an alkoxy group having 1 to 4 carbon atoms; or a pyridyl group; or two R.sub.1, together with the group >CH-- to which they bind, form a dibenzo cycloheptenyl group or a fluorenyl group;R.sub.Type: GrantFiled: August 9, 1995Date of Patent: February 10, 1998Assignee: Tobishi Pharmaceutical Co., Ltd.Inventors: Masashi Ogawa, Tadashi Morita, Kiyoshi Matsuda, Norihiro Iibuchi, Shinpei Kidokoro
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Patent number: 5714479Abstract: A heteroaromatic ring-fused cyclopentene derivative of the formula: ##STR1## wherein the variables are as defined in the specification; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 20, 1996Date of Patent: February 3, 1998Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Kiyofumi Ishikawa, Toshio Nagase, Toshiaki Mase, Takashi Hayama, Masaki Ihara, Masaru Nishikibe, Mitsuo Yano
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Patent number: 5714490Abstract: A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R.sub.1 is a straight or branched chain (C.sub.3 to C.sub.8) alkyl group substituted by one or two amino acid ester groups (e.g., an amino acid ester group convertible in vivo into a hydroxy group) thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.Type: GrantFiled: June 2, 1995Date of Patent: February 3, 1998Assignee: Schering CorporationInventors: Anil K. Saksena, Viyyoor M. Girijavallabhan, Raymond G. Lovey, Russell E. Pike, Haiyan Wang, Yi-Tsung Liu, Ashit K. Ganguly, Frank Bennett
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Patent number: 5710288Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification, are capable of lowering intraocular pressure in the eye of a mammal.Type: GrantFiled: May 3, 1996Date of Patent: January 20, 1998Assignee: AllerganInventors: Robert M. Burk, David F. Woodward
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Patent number: 5710154Abstract: A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R.sub.1 is a straight or branched chain (C.sub.3 to C.sub.8) alkyl group substituted by one or two groups convertible in vivo into hydroxy moieties, (e.g., a polyether ester, amino acid ester or phosphate ester) thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.Type: GrantFiled: June 2, 1995Date of Patent: January 20, 1998Assignee: Schering CorporationInventors: Anil K. Saksena, Viyyoor M. Girijavallabhan, Raymond G. Lovey, Russell E. Pike, Haiyan Wang, Yi-Tsung Liu, Ashit K. Ganguly, Frank Bennett
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Patent number: 5710138Abstract: Compounds of formula I ##STR1## are described, in which substituents R.sup.1 -R.sup.4 have the meanings mentioned in the application as well as their production and use in pharmaceutical agents.Type: GrantFiled: January 22, 1996Date of Patent: January 20, 1998Assignee: Schering AktiengesellschaftInventors: Peter Holscher, Lechoslaw Turski
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Patent number: 5707977Abstract: A compound of formula (I), ##STR1## an acid or base addition salt thereof or a stereochemically isomeric form thereof, wherein A and B taken together form --N.dbd.CH--, --CH.dbd.N--, --CH.sub.2 --CH.sub.2, CH.dbd.CH--, --C(.dbd.O)--CH.sub.2 --, --CH.sub.2 --C(.dbd.O); D is a radical of formula ##STR2## L is a radical of formula ##STR3## Alk is a C.sub.1-4 alkanediyl radical; R.sup.1 is halo; R.sup.2 is hydrogen or halo; R.sup.3 is hydrogen, C.sub.1-6 alkyl, phenyl or halophenyl; R.sup.4 is hydrogen, C.sub.1-6 alkyl, phenyl or halophenyl; R.sup.5 is hydrogen or C.sub.1-6 alkyl; R.sup.6 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxycarbonyl, or R.sup.5 and R.sup.6 taken together with the nitrogen atom to which they are attached form a heterocyclic ring. Active intermediates, compositions and methods of preparing compounds, compositions are described.Type: GrantFiled: June 20, 1996Date of Patent: January 13, 1998Assignee: Janssen Pharmaceutica, N.V.Inventors: Jan Heeres, Leo Jacobus Jozef Backx, Luc Alfons Leo Van der Eycken, Frank Christopher Odds, Jean Louis Mesens
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Patent number: 5705645Abstract: Antibacterial activity is exhibited by novel compounds having the formula ##STR1## where R.sub.1, R.sub.2, and M are as defined herein and X is --(CH.sub.2).sub.n -- wherein n is 0, 1, 2, 3 or 4 or CR.sub.3 R.sub.4 wherein R.sub.3 and R.sub.4 are the same or different and each is hydrogen, --CH.sub.3 or --C.sub.2 H.sub.5 or R.sub.3 and R.sub.4 taken together with the carbon atom to which they are attached form a 3, 4, 5, 6 or 7-membered cycloalkyl ring.Type: GrantFiled: March 7, 1995Date of Patent: January 6, 1998Assignee: E. R. Squibb & Sons, Inc.Inventors: William H. Koster, Joseph E. Sundeen, Henner Straub, Peter Ermann, Uwe D. Treuner, Kent Amsberry, Michael Fakes, Sailesh A. Varia
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Patent number: 5693626Abstract: A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R.sub.1 is a straight or branched chain (C.sub.3 to C.sub.8) alkyl group substituted by one or two phosphate ester groups (e.g., a phosphate ester convertible in vivo into a hydroxy group) thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.Type: GrantFiled: June 2, 1995Date of Patent: December 2, 1997Assignee: Schering CorporationInventors: Anil K. Saksena, Viyyoor M. Girijavallabhan, Raymond G. Lovey, Russell E. Pike, Haiyan Wang, Yi-Tsung Liu, Ashit K. Ganguly, Frank Bennett
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Patent number: 5691323Abstract: Compounds, 1,3-dihydro-1-{1-?piperidin-4-yl!piperidin-4-yl}-2H-benzimidazol-2-ones and 1,3-dihydro-1-{4-amino-1-cyclohexyl}-2H-benzimidazol-2-ones and derivatives thereof, their preparation, method of use and pharmaceutical compositions are described. These compounds are endowed with antimuscarinic activity and are useful in the treatment and/or prevention of myopia (commonly known as nearsightedness).Type: GrantFiled: May 12, 1995Date of Patent: November 25, 1997Assignee: Merck & Co., Inc.Inventors: Wayne J. Thompson, Michael F. Sugrue, Richard W. Ransom, Pierre J. Mallorga, Ian M. Bell, Anthony M. Smith
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Patent number: 5686466Abstract: A novel compound of the formula: ##STR1## wherein Ar represents an optionally substituted tricyclic condensed benzene ring group which includes at least one heterocyclic ring as a component ring; n represents an integer from 2 to 10; R.sup.1 represents H or an optionally substituted hydrocarbon group, which may be different from one another in the repetition of n; and Y represents an optionally substituted 4-piperidinyl, 1-piperazinyl or 4-benzyl-1-piperidinyl group, or a salt thereof, inhibiting excellent cholinesterase inhibitory activity and monoamine reuptake inhibitory activity, thus being useful as therapeutic and/or prophylactic medicaments of senile dementia.Type: GrantFiled: March 20, 1996Date of Patent: November 11, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Giichi Goto, Yuji Ishihara, Keisuke Hirai
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Patent number: 5681830Abstract: Diarylmethyl piperazine compounds having utility as exogenous receptor combinant species for binding with receptors such as delta, mu, sigma, and/or kappa receptors are disclosed. Compounds of the invention may be employed as conjugates in agonist/antagonist pairs for transductional monitoring and assays of neurotransmitter function, and also variously exhibit therapeutic utility, including mediating analgesia, and possessing utility for the treatment of diarrhea, urinary incontinence, mental illness, drug and alcohol addiction/overdose, lung edema, depression, asthma, emphysema, cough, and apnea, respiratory depression, cognitive disorders, emesis and gastrointestinal disorders.Type: GrantFiled: August 3, 1994Date of Patent: October 28, 1997Assignee: Delta Pharmaceuticals, Inc.Inventors: Kwen-Jen Chang, Dulce G. Bubacz, Ann O. Davis, Robert W. McNutt, Jr., Mark A. Collins, Michael J. Bishop
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Patent number: 5679700Abstract: Novel phosphinic acid-containing peptidyl compounds of formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophobic epidermolysis bullosa, and coronary thrombosis associated with atherosclerotic plaque rupture. These inhibitors may also be useful in preventing the pathological sequelae following a traumatic injury that could lead to permanent disability. These compounds may also have utility as a means for birth control by preventing ovulation or implantation.Type: GrantFiled: November 9, 1995Date of Patent: October 21, 1997Assignee: Merck & Co., Inc.Inventors: Charles G. Caldwell, Philippe L. Durette, Joung L. Goulet, William K. Hagmann, Soumya P. Sahoo
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Patent number: 5661151Abstract: A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R.sub.1 is a straight or branched chain (C.sub.3 to C.sub.8) alkyl group substituted by one or two hydroxy moieties, an ether or ester thereof (e.g., a polyether ester amino acid ester or phosphate ester) thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.Type: GrantFiled: June 2, 1995Date of Patent: August 26, 1997Assignee: Schering CorporationInventors: Anil K. Saksena, Viyyoor M. Girijavallabhan, Raymond G. Lovey, Russell E. Pike, Haiyan Wang, Yi-Tsung Liu, Ashit K. Ganguly, Frank Bennett
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Patent number: 5654303Abstract: A novel series of substituted quinoxaline 2,3-diones useful as neuroprotective agents are taught. Novel intermediates, processes of preparation, and pharmaceutical compositions containing the compounds are also taught. The compounds are glutamate antagonists and are useful in the treatment of stroke, cerebral ischemia, or cerebral infarction resulting from thromboembolic or hemorrhagic stroke, cerebral vasospasms, hypoglycemia, cardiac arrest, status epilepticus, perinatal asphyxia, anoxia, Alzheimer's, Parkinson's, and Huntington's diseases.Type: GrantFiled: June 7, 1995Date of Patent: August 5, 1997Assignee: Warner-Lambert CompanyInventors: Brian Edward Kornberg, Sham Nikam, Michael Francis Rafferty
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Patent number: 5652238Abstract: A compound of structural Formula (I) or pharmaceutically acceptable salts thereof wherein: R is --C(O)--R.sup.1, --PO.sub.3 .dbd. or --P(O)(OH).sub.2 ; R.sup.1 is C.sub.1-6 alkyl, --N(R.sup.4).sub.2, C.sub.1-6 alkyl-N(R.sup.4).sub.2, --phenyl--N(R.sup.4).sub.2, --phenyl-NHC(O)CH.sub.2 NH.sub.2, --C.sub.2 H.sub.4 -morpholinyl, pyridinyl, C.sub.1-6 alkyl-OH, C.sub.1-6 alkyl-OCH.sub.3, C.sub.1-6 alkyl C(O)CH.sub.3, --O--C.sub.1-6 alkyl-OCH.sub.3, C.sub.0-3 alkyl-piperazinyl (optionally substituted with C.sub.1-3 alkyl), imidazolyl, C.sub.1-6 alkyl-COOH, --C(CH.sub.2 OH).sub.2 CH.sub.3 ; R.sup.2 and R.sup.3 are independently selected from hydrogen or F except at least one of R.sup.2 or R.sup.3 is F; R.sup.4 are independently selected from hydrogen or C.sub.1-6 alkyl.Type: GrantFiled: May 9, 1996Date of Patent: July 29, 1997Assignee: Pharmacia & Upjohn CompanyInventors: Steven J. Brickner, Michael R. Barbachyn, Douglas K. Hutchinson
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Patent number: 5646151Abstract: Compounds, compositions and method of treating hyperalgesia comprising a compound of formula I, II, III and IV as defined in the specification.Type: GrantFiled: March 8, 1996Date of Patent: July 8, 1997Assignee: Adolor CorporationInventors: Lawrence I. Kruse, Virendra Kumar, An-Chih Chang, Diane L. DeHaven-Hudkins, John J. Farrar, Alan L. Maycock
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Patent number: 5646146Abstract: The present invention relates to 9H-indeno[1,2-b]pyrazin-3(4H)-ones and 9H-indeno[1,2-b]pyrazine-2,3(1H,4H)-diones or tautomeric forms thereof which are useful in treating neurological and psychiatric diseases based on the antagonism of the glycine binding site on the NMDA receptor complex.Type: GrantFiled: May 25, 1995Date of Patent: July 8, 1997Assignee: Novo Nordisk A/SInventors: Peter Faarup, Palle Jakobsen, Anker Steen J.o slashed.rgensen, Henrik Klitgaard
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Patent number: 5631372Abstract: A process for producing 1-substituted-4-fluoro-1,4-diazoniabicyclo[2.2.2]octane salts having the formula ##STR1## wherein the Z substituent is OH, OR, OC(O)R, SO.sub.3, SO.sub.2 R, NO.sub.2, NO, or PO(OR).sub.2, wherein R is an aryl or C.sub.1 -C.sub.8 alkyl group; n is 0, 1 or 2; each of R.sub.1, R.sub.2, R.sub.3, P.sub.4 and R.sub.5 independently represent hydrogen, C.sub.1 to C.sub.8 alkyl, or aryl 1-substituted-1,4-diazoniabicyclo[2.2.2]octane or 1,4-diazoniabicyclo[2.2.2]octane mono-N-oxide is reacted to attach the Z group and then the result is reacted with molecular fluorine in the presence of a solvent that substantially does not react with fluorine and a fluoride scavenger that results in an X counter ion. These compounds are useful as fluorinating agents for the introduction of fluorine into organic compounds.Type: GrantFiled: May 6, 1996Date of Patent: May 20, 1997Assignee: AlliedSignal Inc.Inventors: Andrew J. Poss, George A. Shia, Dennis M. Lavery
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Patent number: 5620986Abstract: Novel substituted 4-azasteroid 5-.alpha.-reductase inhibitors of formula (I), wherein A is (a), (b) or (c), are claimed as well as pharmaceutically acceptable salts and formulations thereof. These compounds are effective inhibitors of testosterone 5.alpha.-reductase(s) and are thus useful in the treatment of a number of hyperandrogenic conditions including benign prostatic hypertrophy, acne, seborrhea, female hirsutism, and male and female pattern baldness (alopecia).Type: GrantFiled: March 1, 1995Date of Patent: April 15, 1997Assignee: Merck & Co., Inc.Inventors: Bruce E. Witzel, Richard L. Tolman
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Patent number: 5614508Abstract: A novel series of substituted quinoxaline 2,3-diones useful as neuroprotective agents are taught. Novel intermediates, processes of preparation, and pharmaceutical compositions containing the compounds are also taught. The compounds are glutamate antagonists and are useful in the treatment of stroke, cerebral ischemia, or cerebral infarction resulting from thromboembolic or hemorrhagic stroke, cerebral vasospasms, hypoglycemia, cardiac arrest, status epilepticus, perinatal asphyxia, anoxia, Alzheimer's, Parkinson's, and Huntington's diseases.Type: GrantFiled: June 7, 1995Date of Patent: March 25, 1997Assignee: Warner-Lambert CompanyInventor: Sham Nikam
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Patent number: 5563268Abstract: Heterobiaryl derivatives of the formulaR.sub.1 NH--X.sub.1 --X.sub.2 --X.sub.3 --Y.sub.1 --Y.sub.2 --Y.sub.3 --Y.sub.4 --E (I)whereinR.sub.1, X.sub.1 to X.sub.3 and Y.sub.1 to Y.sub.4 are as defined herein, the tautomers, stereoisomers and mixtures thereof, and the salts, particularly the physiologically acceptable salts, thereof with organic or inorganic acids or bases. The derivatives have valuable pharmacological properties, such as inhibiting cell-cell aggregation and cell-matrix interactions.Type: GrantFiled: January 19, 1995Date of Patent: October 8, 1996Assignee: Dr. Karl Thomae GmbHInventors: Guenter Linz, Helmut Pieper, Frank Himmelsbach, Volkhard Austel, Thomas Mueller, Johannes Weisenberger, Elke Seewaldt-Becker
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Patent number: 5559106Abstract: Quinoxaline compounds of the general formula ##STR1## wherein R.sup.1 is COX', POX'X" or alkyl substituted with COX' or POX'X", and X' and X" independently are hydroxy or alkoxy, and R.sup.6, R.sup.7, R.sup.8 and R.sup.9 independently are hydrogen, alkyl, halogen, NH.sub.2, NO.sub.2, CN, CF.sub.3, SO.sub.2 NY'Y" or COZ' wherein Z' is NY'Y" or alkyl and Y' and Y" independently are hydrogen or alkyl, triazolyl, imidazolyl, imidazolyl substituted with phenyl or alkyl, or R.sup.6 and R.sup.7, or R.sup.8 and R.sup.9, together form a further fused ring, are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters.Type: GrantFiled: December 7, 1994Date of Patent: September 24, 1996Assignee: Novo Nordisk A/SInventors: Poul Jacobsen, Flemming E. Nielsen, Lone Jeppesen
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Patent number: 5543517Abstract: This invention relates to substituted bicyclic phosphoramides and derivatives thereof, useful as retroviral protease inhibitors and as standards and reagents in determining the ability of a potential pharmaceutical to inhibit viral replication or HIV protease, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating viral infection.Type: GrantFiled: January 13, 1994Date of Patent: August 6, 1996Assignee: The DuPont Merck Pharmaceutical CompanyInventor: Joanne M. Smallheer
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Patent number: 5532226Abstract: Novel benzylphosphonate compounds of the general formula I: ##STR1## are disclosed as useful in treating bone wasting diseases including postmenopausal osteoporosis in increasing in mammals bone formation and bone mass.Type: GrantFiled: December 9, 1993Date of Patent: July 2, 1996Assignee: Ortho Pharmaceutical CorporationInventors: Keith Demarest, Charles Schwender, David Wustrow
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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: 5519013Abstract: The present invention relates to novel heterocycle-substituted diphosphonic acids, and the pharmaceutically-acceptable salts and esters thereof, in which the diphosphonate-substituted carbon atom moiety is attached to a carbon atom in a nitrogen-containing six membered ring heterocycle, preferably a piperidine ring. The heterocycle-substituted diphosphonic acid compounds have the general structure: ##STR1## wherein Z is a nitrogen-containing six membered ring heterocycle moiety selected from piperidinyl, diazinyl and triazinyl; m, n and m+n are from 0 to 10; Q is a covalent bond or a moiety selected from oxygen, sulfur or nitrogen; and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are substituent groups.The present invention further relates to pharmaceutical compositions containing these novel compounds. Finally this invention relates to methods for treating or preventing diseases characterized by abnormal calcium and phosphate metabolism by utilizing a compound or pharmaceutical composition of the present invention.Type: GrantFiled: April 7, 1994Date of Patent: May 21, 1996Assignee: The Procter & Gamble CompanyInventors: Frank H. Ebetino, James J. Benedict
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Patent number: 5516940Abstract: A compound and method of making a compound for use as a diagnostic or therapeutic pharmaceutical comprises either a phosphorous or germanium core and at least two hydrazine groups forming a ligand for bonding to a metal extending from the phosphorous or germanium core.Type: GrantFiled: April 29, 1994Date of Patent: May 14, 1996Assignee: Curators of the University of MissouriInventors: Kattesh V. Katti, Wynn A. Volkert, Alan R. Ketring, Prahlad R. Singh
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Patent number: 5510353Abstract: Compounds of formulaA--X--Y--NH--Bwherein A is derived from optionally substituted benzothiophene, indole, 4-aza-and 7-aza-benzothiophene or-indole, A bearing in position 5 hydrogen, halogen, optionally substituted alkyl, hydroxy, nitro, amino, alkylamino, acylamino, alkoxycarbonyl, sulfamoyl, cyano, trimethylsilyl, carboxy, carbamoyl, phosphate, oxycarbamoyl, heterocyclic radical or ether or ester group, X-Y is --CR.sub.8 .dbd.N-- or CH(R.sub.8)--NH-- wherein R.sub.8 is -H or alkyl and attached at position 3 of A, and B is a heterocyclic radical or a residue ##STR1## wherein R.sub.10 is H, optionally substituted alkyl, cycloalkyl, aryl, adamantyl, acyl or carbamoyl and X.sub.2 is alkylthio or NR.sub.3 R.sub.10 wherein R.sub.3 is H or alkyl or R.sub.3 and R.sub.10 together with the nitrogen atom to which they are attached form a heterocyclic radical, in free form or in salt form, have pharmacological activity, e.g. for treating gastrointestinal disorders.Type: GrantFiled: January 9, 1995Date of Patent: April 23, 1996Assignee: Sandoz Ltd.Inventors: Rudolf K. A. Giger, Henri Mattes
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Patent number: 5508403Abstract: An agent for enhancing the drug effects of an antitumor drug, which comprises a compound of the formula I: ##STR1## or a pharmaceutically acceptable salt of the compound.Type: GrantFiled: June 5, 1995Date of Patent: April 16, 1996Assignee: Nissan Chemical Industries Ltd.Inventors: Shin-ichi Akiyama, Ryozo Sakoda, Kiyotomo Seto, Norimasa Shudo
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Patent number: 5468748Abstract: The present invention relates to 9H-indeno[1,2-b]pyrazin-3(4H)-ones and 9H-indeno[1,2-b]pyrazine-2,3(1H,4H)-diones or tautomeric forms thereof which are useful in treating neurological and psychiatric diseases based on the antagonism of the glycine binding site on the NMDA receptor complex.Type: GrantFiled: January 31, 1994Date of Patent: November 21, 1995Inventors: Peter Faarup, Palle Jakobsen, Anker S. Jorgensen, Henrik Klitgaard
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Patent number: 5459267Abstract: SUBSTITUTED-4-FLUORO-1,4-DIAZONIABICYCLO[2.2.2]OCTANE SALTS AND THEIR APPLICATION AS FLUORINATING AGENTS The present invention relates to the preparation and uses of 1-substituted-4-fluoro-1,4-diazoniabicyclo[2.2.2]octane salts, specifically 1-hydroxyl-4-fluoro-1,4-diazoniabicyclo[2.2.2]octane salts as reagents for the introduction of fluorine in organic compounds.Type: GrantFiled: December 23, 1993Date of Patent: October 17, 1995Assignee: AlliedSignal Inc.Inventors: Andrew J. Poss, George Shia
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Patent number: 5457094Abstract: Compounds of formula I ##STR1## wherein R, R.sub.1, R.sub.2 and q are as defined in the description, have valuable pharmacological properties and are especially effective as calcium metabolism regulators. They are prepared in a manner known per se.Type: GrantFiled: February 7, 1995Date of Patent: October 10, 1995Assignee: Ciba-Geigy CorporationInventor: Knut A. Jaeggi
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Patent number: 5434150Abstract: The invention relates to cyclic imino derivatives of general formula ##STR1## wherein A to G, R.sub.1, Z.sub.1 to Z.sub.6, X and Y are defined as in claim 1, the tautomers, stereoisomers and mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, preferably aggregation-inhibiting properties, pharmaceutical compositions which contain these compounds and processes for preparing them.Type: GrantFiled: August 28, 1992Date of Patent: July 18, 1995Assignee: Dr. Karl Thomae GmbHInventors: Volhard Austel, Helmut Pieper, Frank Himmelsbach, Guenter Linz, Thomas Mueller, Johannes Weisenberger, Elke Seewaldt-Becker
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Patent number: 5420277Abstract: Antibacterial activity is exhibited by novel compounds having the formula ##STR1## where R.sub.1, R.sub.2, and M are as defined herein and X is --(CH.sub.2).sub.n -- wherein n is 0, 1, 2, 3 or 4 or CR.sub.3 R.sub.4 wherein R.sub.3 and R.sub.4 are the same or different and each is hydrogen, --CH.sub.3 or --C.sub.2 H.sub.5 or R.sub.3 and R.sub.4 taken together with the carbon atom to which they are attached form a 3, 4, 5, 6 or 7-membered cycloalkyl ring. Also described are various intermediates for the preparation of compounds of formula 1.Type: GrantFiled: November 29, 1993Date of Patent: May 30, 1995Assignee: E. R. Squibb & Sons, Inc.Inventors: William H. Koster, Joseph E. Sundeen, Henner Straub, Peter Ermann, Uwe D. Treuner, Kent Amsberry, Michael Fakes, Sailesh A. Varia
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Patent number: 5413994Abstract: Compounds of formula I ##STR1## wherein R, R.sub.1, R.sub.2 and q are as defined in the description, have valuable pharmacological properties and are especially effective as calcium metabolism regulators. They are prepared in a manner known per se.Type: GrantFiled: June 9, 1993Date of Patent: May 9, 1995Assignee: Ciba-Geigy CorporationInventor: Knut A. Jaeggi
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Patent number: 5405841Abstract: The invention relates to new phosphorylated aza compounds, to processes for their preparation and to their use as pesticides, in particular as soil-acting insecticides and nematicide.The new compounds have the general formula (I) ##STR1## in which R.sup.1 -R.sup.5, X and Y are defined as in the specification, with the exception of compound O-ethyl S-propyl 3-(6-chloro-3-pyridinylmethyl)-2-nitroimino-imidazolidine-1-thiophosphate.Type: GrantFiled: November 30, 1993Date of Patent: April 11, 1995Assignee: Bayer AktiengesellschaftInventors: Fritz Maurer, Jurgen Hartwig, Christoph Erdelen
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Patent number: 5399693Abstract: Compounds of the general formula ##STR1## wherein X is a C.sub.1 -C.sub.6, straight chain saturated or unsaturated hydrocarbyl group, the group R.sup.4 and the group Y are situated in any position in this chain and wherein at least one of the hydrogen atoms in X can be a heavy isotope of hydrogen;R.sup.4 is hydrogen or an alkyl, alkoxy, hydroxy, aryl, aryloxy, aralkyl, aralkoxy, aralkylamino, or morpholino group wherein the alkyl or aryl part of any one of said groups may be substituted by one or more halogeno groups; or R.sup.4, together with at least one carbon atom of the group X, forms a carbocyclic or heterocyclic ring of 5 to 6 ring atoms;Y is an acidic or related group giving rise to one or more electronegative sites in the group; or R.sup.4 --X--Y represents a carboxylic acyl group;R is hydrogen or an alkyl, haloalkyl, aryl, haloaryl, aralkyl or haloaralkyl;R.sup.1 is hydrogen or an alkyl, haloalkyl, aryl, haloaryl, aralkyl or haloaralkyl group;R.sup.2 R.sup.3 and R.sup.Type: GrantFiled: January 23, 1990Date of Patent: March 21, 1995Assignee: British Technology Group LimitedInventors: Jeffrey C. Watkins, Arwel W. Jones