Polycyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/461)
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Patent number: 6489314Abstract: The present invention relates to 16-membered macrocyclic compounds. In one aspect of the present invention, compounds of the formula are provided wherein: R1, R2, R3, and R5 are each independently hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl or alkylaryl; R4 is hydrogen, halogen, C1-C10 alkyl, C1-C10 hydroxyalkyl, C1-C10 haloalkyl, aryl, —C(═O)R6, —C(═O)OR6, —NR6R7 where R6 and R7 are each independently hydrogen, C1-C10 aliphatic, aryl or alkylaryl; W is O, NR8 where R8 is hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl or alkylaryl; X is O, CH2 or a carbon-carbon double bond; Y is absent or a C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl; and Ar is aryl; provided that 10,11-dehydroepothilone C is excluded.Type: GrantFiled: April 3, 2001Date of Patent: December 3, 2002Assignee: Kosan Biosciences, Inc.Inventors: Gary Ashley, Brian Metcalf
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Patent number: 6482567Abstract: New photoacid generator compounds (“PAGs”) are provided and photoresist compositions that comprise such compounds. In particular, non-ionic PAGs are provided that contain an oxime sulfonate group, and/or an N-oxyimidosulfonate group. PAGs of the invention are particularly useful as photoactive components of photoresists imaged at short wavelengths such as 248 nm, 193 nm and 157 nm.Type: GrantFiled: August 25, 2000Date of Patent: November 19, 2002Assignee: Shipley Company, L.L.C.Inventors: James F. Cameron, Gerhard Pohlers
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Publication number: 20020143038Abstract: A process for formulating certain epothilone analogs for parenteral administration is disclosed wherein the analog is dissolved in a mixture of at least 50% by volume tertiary-butanol in water, the mixture is lyophilized, the resulting lyophilized product is packaged in one vial with a sufficient amount of solvent comprising anhydrous ethanol and a suitable nonionic surfactant in a second vial. All steps are carried out with protection from light. In use, the contents of the second or diluent vial are added to the lyophilized product and mixed to constitute the epothilone analog and the resulting solution is diluted with a suitable diluent to produce a solution for intravenous injection containing the epothilone analog in a concentration of from about 0.1 mg/mL to about 0.9 mg/mL. A preferred surfactant is polyethoxylated castor oil and a preferred diluent is Lactated Ringer's Injection.Type: ApplicationFiled: January 17, 2002Publication date: October 3, 2002Inventors: Rebanta Bandyopadhyay, Timothy M. Malloy, Andrea Panaggio, Krishnaswamy Srinivas Raghavan, Sailesh Amilal Varia
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Patent number: 6423840Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1&bgr; converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-&ggr;-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-&ggr;-mediated diseases and decreasing IGIF and IFN-&ggr; production using the compounds and compositions of this invention.Type: GrantFiled: January 31, 2001Date of Patent: July 23, 2002Assignee: Vertex Pharmaceuticals IncorporatedInventors: Mark James Batchelor, David Bebbington, Guy W. Bemis, Wolf Herman Fridman, Roger John Gillespie, Julian M. C. Golec, Yong Gu, David J. Lauffer, David J. Livingston, Saroop Singh Matharu, Michael D. Mullican, Mark A. Murcko, Robert Murdoch, Philip Nyce, Andrea L. C. Robidoux, Michael Su, M. Woods Wannamaker, Keith P. Wilson, Robert E. Zelle
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Patent number: 6410534Abstract: The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.Type: GrantFiled: June 29, 1999Date of Patent: June 25, 2002Assignee: Merck & Co., Inc.Inventors: Christopher J. Dinsmore, Ian M. Bell, Douglas C. Beshore, Theresa M. Williams
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Publication number: 20010044532Abstract: The invention relates to a process for the preparation of N,N′-carbonylbislactams by reaction of phosgene with at least one lactam which is characterized in that the tertiary amine is chosen from the group consisting of non-nucleophilic aliphatic tertiary amines.Type: ApplicationFiled: April 23, 2001Publication date: November 22, 2001Inventors: Hubert Bonnard, Laurence Ferruccio, Jean-Pierre Senet, Pierre-Yves Le Roy
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Patent number: 6303543Abstract: A compound represented by the formula (I) or its salt and herbicidal and desiccant use thereof: wherein X, Y are independently hydrogen, halogen, cyano, nito, or (C1-6)haloalkyl; Z is oxygen or sulfur; andType: GrantFiled: May 15, 2000Date of Patent: October 16, 2001Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: David A. Pulman, Bai-Ping Ying, Shao-Yong Wu, Sandeep Gupta, Masamitsu Tsukamoto, Takahiro Haga
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Patent number: 6277839Abstract: The present invention relates to biphenylene lactams of Formula II which are ligands at the prostaglandin receptors, as well as a method for treating prostaglandin mediated diseases comprising administration to a patient in need of such a treatment of a non-toxic therapeutically effective amount of compound of Formula II, and the like.Type: GrantFiled: October 1, 1999Date of Patent: August 21, 2001Assignee: Merck Frosst Canada & Co.Inventors: Joseph G. Atkinson, Marc Labelle, Patrick Lacombe, Rejean Ruel
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Patent number: 6268369Abstract: This invention is directed to dihydropyrimidine compounds of the following formula: which are selective antagonists for human &agr;1C receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotence, cardiac arrhythmia and for the treatment of any disease where antagonism of the &agr;1C receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: May 16, 1997Date of Patent: July 31, 2001Assignee: Synaptic Pharmaceutical CorporationInventors: Dhanapalan Nagarathnam, George Chiu, T. G. Murali Dhar, Wai C. Wong, Mohammad R. Marzabadi, Charles Gluchowski, Bharat Lagu, Shou Wu Miao
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Patent number: 6251885Abstract: An anti-tumor composition containing cytotrienin (I), (II), (III) or (IV) as the active ingredient, which compounds are produced by culturing a bacterium which produces cytotrienin (I), (II), (III) or (IV), in a medium and accumulating cytotrienin (I), (II), (III) or (IV) in the medium and harvesting the product.Type: GrantFiled: June 1, 1999Date of Patent: June 26, 2001Assignee: The Institute of Physical and Chemical ResearchInventors: Hiroyuki Osada, Hideaki Kakeya, Hui-ping Zhang, Kimie Kobinata
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Patent number: 6204261Abstract: The present invention relates to pyradazino[1,2-a][1,2]diazepine-1-carboxamide compounds of formula: which compounds are inhibitors of interleukin-1beta converting enzyme.Type: GrantFiled: December 6, 1996Date of Patent: March 20, 2001Assignee: Vertex Pharmaceuticals IncorporatedInventors: Mark James Batchelor, David Bebbington, Guy W. Bemis, Wolf Herman Fridman, Roger John Gillespie, Julian M. C. Golec, Yong Gu, David J. Lauffer, David J. Livingston, Saroop Singh Matharu, Michael D. Mullican, Mark A. Murcko, Robert Murdoch, Philip Nyce, Andrea L. C. Robidoux, Michael Su, M. Woods Wannamaker, Keith P. Wilson, Robert E. Zelle
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Patent number: 6180411Abstract: A new class of optical indicators which are capable of memorizing and preserving the spatial localization of intracellular analytes in a time resolved manner is described. The compounds comprise a chromophore carrying a photolabile group capable of undergoing an irreversible and detectable chemical transformation upon irradiation by light. The chromophore is linked to a binding site capable of binding an analyte, wherein binding of the analyte to the binding site alters an optical property of the chromophore, thus altering the ability of the photolabile group to undergo the chemical transformation. Methods and kits for memorizing the spatial localization of the analytes are also described.Type: GrantFiled: July 30, 1998Date of Patent: January 30, 2001Assignee: The Regents of the University of CaliforniaInventors: Roger Y. Tsien, Stephen R. Adams
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Patent number: 6177551Abstract: The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.Type: GrantFiled: May 12, 1999Date of Patent: January 23, 2001Assignee: NeoRx CorporationInventor: Sudhakar Kasina
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Patent number: 6127536Abstract: An improved synthesis for preparing a tetraamido-macrocyclic ligand, such as 5,6-Benzo-3,8,11,13-tetraoxo-2,2,9,9-tetramethyl-12,12-diethyl-1,4,7,10 -tetraazacyclotridecane, H.sub.4, in greatly improved yield and in a commercially viable manner, comprising the steps of dissolving a quantity of a 1,2-bis(2-aminoalkanamido)benzene in a solution comprised of ethyl acetate and methylene chloride to yield a first reaction solution; dissolving a quantity of a malonyl dihalide in an ethyl acetate solution to yield a second reaction solution; adding the first reaction solution and the second reaction solution to a reaction vessel containing a third reaction solution comprised of refluxing ethyl acetate solution and an acid scavenger to form a reaction mixture; and isolating a solid product comprised of the tetraamido-macrocycle directly from the reaction mixture by filtration.Type: GrantFiled: May 25, 1999Date of Patent: October 3, 2000Assignee: The Clorox CompanyInventors: James E. Deline, Michael M. Ott, Kevin A. Klotter
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Patent number: 6057311Abstract: Compounds of the formula whereinone of U and V is --CHR.sup.2 --, and the other of U and V is selected from --N(COR.sup.4)--, --CH(COR.sup.4)--, --N(SO.sub.2 R.sup.4)-- and --CH(SO.sub.2 R.sup.4)--,and pharmaceutically acceptable salts thereof are ligands at gastrin and/or cholecystokinin receptors.Type: GrantFiled: October 26, 1998Date of Patent: May 2, 2000Assignee: James Black Foundation LimitedInventors: Sarkis Barret Kalindjian, Iain Mair McDonald, Michael John Pether, Caroline Minli Rachel Low, Katherine Isobel Mary Steel, Ian Duncan Linney
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Patent number: 6040442Abstract: The presently claimed process provides a method for preparing compounds of the formula ##STR1## phosphorous (III) compound and a diester of azodicarboxylate.Type: GrantFiled: June 1, 1995Date of Patent: March 21, 2000Assignee: Eli Lilly and CompanyInventors: Leander Merritt, John S. Ward
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Patent number: 6015659Abstract: Thermotolerant phenotypes are developed in cells, tissues, organs and organisms by the administration of benzoquinonoid ansamycins such as herbimycin A and any of various analogs. The general stress tolerance resulting from this inducement offers benefits in a variety of ways, including rendering surgical patients more able to withstand the rigors of surgery, prolonging the shelf life of organs excised from organ donors, and prolonging the viability of tissue-cultured cells and organs.Type: GrantFiled: September 16, 1997Date of Patent: January 18, 2000Assignee: The Regents of the University of CaliforniaInventors: William J. Welch, Ramanujan Hegde
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Patent number: 5985869Abstract: Novel benzoheterocyclic compounds of the formula: ##STR1## wherein R.sup.1 is H, halogen, alkyl, optionally substituted amino, alkoxy; R.sup.2 is H, halogen, alkoxy, phenylalkoxy, OH, alkyl, optionally substituted amino, carbamoyl-alkoxy, optionally substituted amino-alkoxy, optionally substituted benzoyloxy; R.sup.3 is a group: --NR.sup.4 R.sup.5 or --CO--NR.sup.11 R.sup.12 ; R.sup.4 is H, optionally substitued benzoyl, alkyl; R.sup.5 is a group: ##STR2## [R.sup.16 is halogen, optionally substituted alkyl, OH, alkoxy, alkanoyloxy, alkylthio, alkanoyl, carboxy, alkoxycarbonyl, CN, NO.sub.2, optionally substituted amino, phenyl, cycloalkyl, etc., or a group: --O--A--NR.sup.6 R.sup.7 ; m is 0 to 3], phenyl-alkoxycarbonyl, alkanoyl, phenylalkanoyl, etc.; R.sup.11 is H or alkyl; R.sup.12 is cycloalkyl or optionally substituted phenyl; and W is a group: --(CH.sub.2).sub.p (p is 3 to 5) or --CH.dbd.CH--(CH.sub.2).sub.q (q is 1 to 3), the carbon atom of these groups beign optionally replaced by O, S, SO, SO.sub.Type: GrantFiled: July 15, 1997Date of Patent: November 16, 1999Assignee: Otsuka Pharmaceutical Company, LimitedInventors: Hidenori Ogawa, Hisashi Miyamoto, Kazumi Kondo, Hiroshi Yamashita, Kenji Nakaya, Hajime Komatsu, Michinori Tanaka, Shinya Kora, Michiaki Tominaga, Yoichi Yabuuchi
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Patent number: 5977129Abstract: The present invention relates to compounds of formula I: whereinone or both G is an azacyclic ring of formula II: ##STR1## and Z is oxygen or sulfur and the remaining variables are as defined in the specification. The compounds are useful as stimulants of the cognitive function of the forebrain and hippocampus of mammals and especially in the treatment of Alzheimer's disease, severe painful conditions and glaucoma.Type: GrantFiled: May 3, 1995Date of Patent: November 2, 1999Assignee: Novo Nordisk A/SInventors: Preben H. Olesen, Per Sauerberg
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Patent number: 5972926Abstract: The present invention relates to pyrazine fused to a cyclic peptide which is capable of regulating, in particular stimulating, haematopoiesis.Type: GrantFiled: June 5, 1998Date of Patent: October 26, 1999Assignee: Nycomed Imaging ASInventors: Jessie Sandosham, Johann Hiebl, Hermann Kollmann, Alan Cuthbertson, Peter Fischer, Michael Hartmann, Peter Kremminger, Franz Rovenszky, Mette Husbyn
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Patent number: 5952320Abstract: Macrocyclic compounds of formula ##STR1## are potent inhibitors of matrix metalloproteinase and are useful in the treatment of diseases in which matrix metalloproteinase play a role. Also disclosed are matrix metalloproteinase inhibiting compositions and a method of inhibiting matrix metalloproteinase in a mammal.Type: GrantFiled: December 17, 1997Date of Patent: September 14, 1999Assignee: Abbott LaboratoriesInventors: Steven K. Davidsen, Douglas H. Steinman, George S. Sheppard, Lianhong Xu, James H. Holms, Yan Guo, James B. Summers, Alan S. Florjancic, Michael R. Michaelides
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Patent number: 5932566Abstract: A compound of the formula ##STR1## and pharmaceutically acceptable salts and prodrugs thereof wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as defined below, methods and intermediates useful in the preparation thereof, pharmaceutical compositions thereof and methods of treatment therewith. The compounds of the above formula are useful in inhibiting oncogene products and as antitumor and anticancer agents.Type: GrantFiled: March 25, 1996Date of Patent: August 3, 1999Assignee: Pfizer Inc.Inventors: Rodney Caughren Schnur, Mikel Paul Moyer, Randall James Gallaschun
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Patent number: 5886019Abstract: Compositions of matter having protein kinase C-modulatory, anti-inflammatory, anti-viral and other activities are disclosed. The compounds are derived from tricyclic aromatic heterocyclic compounds incorporating indole, indene, benzofuran or benzothiophene structural elements.Type: GrantFiled: June 7, 1995Date of Patent: March 23, 1999Assignee: Procyon Pharmaceuticals, Inc.Inventors: Paul E. Driedger, James Quick
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Patent number: 5834454Abstract: A substituted guanidine derivative represented by the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently a hydrogen atom, an unsubstituted alkyl group, a substituted alkyl group, a halogen atom or the like; Y.sub.1, Y.sub.2, Y.sub.3, Y.sub.4, Y.sub.5, Y .sub.6 and Y.sub.7, which may be the same or different, are independently a single bond, --CH.sub.2 --, --O--, --CO--or the like, adjacent members of a group consisting of Y.sub.1 through Y.sub.7 being able to be taken together to represent --CH.dbd.CH--, and at least two of Y.sub.1 through Y.sub.7 being independently a group other than a single bond; Z may be absent, or one or more Zs may be present and are, the same or different, independently a substituent for a hydrogen atom bonded to any of the carbon atoms constituting the ring formed by Y.sub.1 through Y.sub.Type: GrantFiled: January 28, 1997Date of Patent: November 10, 1998Assignee: Sumitomo Pharmaceuticals Company, LimitedInventors: Masahumi Kitano, Naohito Ohashi
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Patent number: 5789587Abstract: There are disclosed certain novel compounds identified as heterocyclic-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such heterocyclic-fused lactams as the active ingredient thereof are also disclosed.Type: GrantFiled: November 6, 1996Date of Patent: August 4, 1998Assignee: Merck & Co., Inc.Inventors: Michael H. Fisher, Helmut Mrozik, William R. Schoen, Thomas L. Shih, Matthew J. Wyvratt
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Patent number: 5770590Abstract: Novel compounds of the following general formula or salts thereof. ##STR1## wherein Ring M is a heterocyclic ring having --N.dbd.C<, --CO--N< or --CS--N< as the partial structure --X . . . Y<; R.sup.a and R.sup.b are bonded to each other to form Ring A, or they are the same or different and represent, independently, a hydrogen atom or a substituent on the Ring M; Ring A and Ring B represent, independently, an optionally substituted homocyclic or heterocyclic ring, and at least one of them is optionally substituted heterocyclic ring; Rng C is optionally substituted homocyclic or heterocyclic ring; Rng Z is an optionally substituted ring; and n represents an integer of from 1 to 6, or a salt thereof, which has anexcellent tachykinin receptor antagonistic effect, and their production, and pharmaceutical compositions.Type: GrantFiled: September 23, 1996Date of Patent: June 23, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideaki Natsugari, Takenori Ishimaru, Takayuki Doi, Yoshinori Ikeura, Chiharu Kimura, Naoki Tarui
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Patent number: 5760220Abstract: A process is described for preparing a compound of the formula I: ##STR1## or a salt thereof; wherein X is a protecting group and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen, C.sub.1-6 alkyl or C.sub.1-6 perfluoroalkyl, R.sub.5 is hydrogen or when n is 1 R.sub.5 taken together with R.sub.3 comprises a double bond; m is 1, 2 or 3; n is 0 or 1, and p is 0, 1 or 2.Type: GrantFiled: June 4, 1996Date of Patent: June 2, 1998Assignee: American Home Products CorporationInventors: Pierre Giguere, Silvio Iera, Michel Bernatchez, Giuseppe Barreca, Graziano Castaldi, Vincenzo Cannata
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Patent number: 5750702Abstract: The present invention encompasses structures of the formula: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## wherein: W represents substituted or unsubstituted phenyl;X is hydrogen, hydroxy or lower alkyl;T is hydrogen, halogen, hydroxy, nitro, amino or alkyl;R.sub.3 is hydrogen or an organic group;R.sub.4 is hydrogen or substituted or unsubstituted organic substituent;R.sub.5 and R.sub.6 represent organic, and inorganic substituents; andn is 1, 2, 3, or 4,which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.Type: GrantFiled: July 16, 1996Date of Patent: May 12, 1998Assignee: Neurogen CorporationInventors: Pamela Albaugh, Alan Hutchison
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Patent number: 5747303Abstract: The invention is directed to a novel compound of formula ##STR1## in which R is a hydroxyl, alkyloxy, phenylalkyloxy or --NH--CH.sub.2 --COOH radical, R' and R" are identical and are each a hydroxy or methoxy radical and R'" represents a hydrogen, bromine, chlorine or iodine atom or a nitro radical. The invention is also directed to the salts of said compounds and their use.Type: GrantFiled: November 19, 1996Date of Patent: May 5, 1998Assignee: Rhone-Poulenc Rorer S.A.Inventors: Jean-Jacques Debernard, Catherine Dubertret, Gerard Helynck, Jean Leboul, Jean-Paul Martin
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Patent number: 5723457Abstract: Compounds of the formula ##STR1## wherein X.sub.1 is ##STR2## are disclosed. These compounds possess inhibitory activity against angiotensin converting enzyme and neutral endopeptidase and thus are useful as cardiovascular agents.Type: GrantFiled: July 8, 1996Date of Patent: March 3, 1998Assignee: E. R. Squibb & Sons, Inc.Inventors: Donald S. Karanewsky, Jeffrey A. Robl
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Patent number: 5686606Abstract: The present invention relates to UCF116 compounds represented by the formula (I) : ##STR1## wherein an example of Q.sup.1 representation is ##STR2## and an example of Q.sup.2 representation is ##STR3## which have antibacterial and antitumor activity and are useful as antibacterial and antitumor agents.Type: GrantFiled: July 12, 1996Date of Patent: November 11, 1997Assignee: Kyowa Hakko Kogyo, Co., Ltd.Inventors: Tamio Mizukami, Mikito Itoh, Mitsunobu Hara, Hirofumi Nakano, Yumiko Aotani, Keiko Ochiai, Shiro Akinaga, Akira Mihara
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Patent number: 5679673Abstract: Certain aralkyl diazabicycloalkyl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R, R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower-alkyl, benzyl, and haloloweralkyl; wherein each of R.sup.2, R.sup.3 and R.sup.10 through R.sup.13 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein each of R.sup.8 and R.sup.Type: GrantFiled: November 21, 1994Date of Patent: October 21, 1997Assignee: The United States of America, represented by the Department of Health and Human ServicesInventors: Wayne Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
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Patent number: 5674876Abstract: The present invention provides an antiproliferative p-heteroatom-substituted phenol compound having the structure formula ##STR1## wherein m is 0 to 3, n is 0 to 4 when Het is nitrogen, wherein R is selected from the group consisting of hydrogen, alkyl, arylmethyl and acyl; R.sup.1 is alkyl; R.sup.2 is selected from the group consisting of hydrogen and alkyl; R.sup.3 is selected from the group consisting of alkyl and acyl when Het is nitrogen, R.sup.4 is selected from the group consisting of hydrogen and alkyl; R.sup.5 is selected from the group consisting of hydrogen and alkyl; and R.sup.6 and R.sup.7 are selected from the group consisting of hydrogen, alkyl and R.sup.6 and R.sup.7 together may represent oxygen. Also provided are various methods for the treatment of a pathological cell proliferative disease comprising administering to an animal) a pharmacologically and therapeutically effective dose of a pharmaceutical composition comprising a p-heteroatom-substituted phenols or an analog thereof.Type: GrantFiled: January 20, 1995Date of Patent: October 7, 1997Assignee: Research Development FoundationInventors: John C. Gilbert, Kimberly Kline, Kathiresan Krishnan, Maria Simmons Menchaca, Marian Pinto, Robert G. Sanders
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Patent number: 5672596Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient therefore are also disclosed.Type: GrantFiled: April 18, 1995Date of Patent: September 30, 1997Assignee: Merck & Co., Inc.Inventors: Matthew Wyvratt, Robert DeVita, Richard Bochis, William Schoen
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Patent number: 5654298Abstract: This invention concerns novel aminopyridinium compounds of the formula I wherein R.sup.1, R.sup.2, R.sup.3, R.sup.5 and R.sup.6 are selected from the following combinations: ##STR1## (a) one of R.sup.2 and R.sup.6 is a basic group selected from amino, alkylamino, dialkylamino of up to eight carbon atoms, pyrrolidino, piperidino and morpholino, or is alkyl, alkenyl, alkoxyalkyl, alkoxy, alkylthio, phenyl, phenylalkyl, cycloalkyl or cycloalkylalkyl; and the other of R.sup.2 and R.sup.6 is hydrogen, alkyl or one of the above defined basic groups;R.sup.1 is alkyl, alkenyl, cycloalkyl, phenyl, phenylalkyl, cycloalkylalkyl; and R.sup.3 and R.sup.5 are independently hydrogen, alkyl or alkenyl;(b) R.sup.2 is a basic group as defined above, R.sup.5 and R.sup.6 together form alkylene or, together with the appendant carbon atoms of the pyridine ring, complete a benzene ring; has any of the meanings defined in(a) above; and R.sup.3 is hydrogen, alkyl or alkenyl; and(c) R2 has any of the meanings defined above and R.sup.Type: GrantFiled: April 16, 1991Date of Patent: August 5, 1997Assignee: Imperial Chemical IndustriesInventors: Stuart Dennett Mills, Rodney Brian Hargreaves, Bernard Joseph McLoughlin
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Patent number: 5639745Abstract: Disclosed are compounds, compositions and methods for inhibiting interleukin-1.beta. protease activity. The compounds, bicyclic derivatives of aldehydes and .alpha.-substituted methyl ketones, have the formula (A) set out herein.Type: GrantFiled: May 25, 1995Date of Patent: June 17, 1997Assignee: SanofiInventors: Roland E. Dolle, Prasad V. Chaturvedula, Tina Morgan Ross, Stanley J. Schmidt
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Patent number: 5621153Abstract: A process for the para-directed nuclear chlorination of an alkylbenzene, such as toluene, comprises reacting the alkylbenzene with chlorine in the presence of a Lewis acid catalyst and a novel co-catalyst of the formula: ##STR1## where Z is ##STR2## ; and R is Cl, Br, F, C.sub.1 to C.sub.8 alkyl to C.sub.1 to C.sub.8 alkoxy; x and y are each hydrogen, or taken together form a fused cyclopentyl or cyclohexyl ring; n is 0, 1 or 2, with the proviso that when Z is [3], n is 0 or 1.Type: GrantFiled: April 21, 1995Date of Patent: April 15, 1997Assignee: Occidental Chemical CorporationInventors: Ramesh Krishnamurti, Sandor Nagy, Thomas F. Smolka
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Patent number: 5606054Abstract: There are disclosed certain novel compounds identified as heterocyclic-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such heterocyclic-fused lactams as the active ingredient thereof are also disclosed.Type: GrantFiled: December 14, 1993Date of Patent: February 25, 1997Assignee: Merck & Co., Inc.Inventors: Michael H. Fisher, Helmut Mrozik, William R. Schoen, Thomas L. Shih, Matthew J. Wyvratt
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Patent number: 5599815Abstract: Compounds represented by the formula (I) and pharmacologically acceptable salts thereof: ##STR1## These compounds have little extrapyramidal effect and thus are effective as an anti-psychotic agent having few side effects.Type: GrantFiled: December 20, 1994Date of Patent: February 4, 1997Assignee: Meiji Seika Kabushiki KaishaInventors: Yoshimasa Fukuda, Toshiro Sasaki, Yuuko Nakatani, Yasuyuki Ichimaru, Taiichiro Imanishi
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Patent number: 5583130Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. The compounds are prepared by substitution of an amino-lactam with a substituted amide function. Growth promoting compositions containing such bezno-fused lactams as the active ingredient thereof are also disclosed.Type: GrantFiled: September 25, 1992Date of Patent: December 10, 1996Assignee: Merck & Co., Inc.Inventors: Richard J. Bochis, Michael H. Fisher, Robert J. Devita, William R. Schoen, Matthew J. Wyvratt
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Patent number: 5552400Abstract: Disclosed are compounds, compositions and methods for inhibiting interleukin-1.beta. protease activity. The compounds, bicyclic derivatives of aldehydes and .alpha.-substituted methyl ketones, have the formula (A) set out herein.Type: GrantFiled: June 8, 1994Date of Patent: September 3, 1996Assignee: Sterling Winthrop Inc.Inventors: Roland E. Dolle, Prasad V. Chaturvedula, Tina M. Ross, Stanley J. Schmidt
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Patent number: 5538961Abstract: Macrocylic lactam compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof, wherein A is selected from ##STR2## also disclosed are synthetic processes and intermediates useful in the preparation of the compounds of the invention, as well as compositions containing the same and methods for their use in stimulating contractile motion of the gastrointestinal tract.Type: GrantFiled: August 30, 1993Date of Patent: July 23, 1996Assignee: Abbott LaboratoriesInventors: Leslie A. Freiberg, Carla Edwards, Richard J. Pariza, Hugh N. Nellans
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Patent number: 5532240Abstract: A condensed thiophene compound represented by general formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein ring S represents a thiophene ring; R.sup.1 represents hydrogen, halogen, alkyl, etc.; R.sup.2 represents hydrogen, alkyl, acyl, etc.; G represents --CH.sub.2 --, --CH(OH)--, --CO--, etc.; Q represents alkylene; T represents --N(Rb)(Rc) (wherein Rb, Rc represents each alkyl etc.; or alternatively Rb and Rc are combined together to form cyclic amino); D represents --CH.sub.2 -- or --S--; A and B represent each carbonyl or thiocarbonyl, or are null; and m and n represent each 0, 1 to 4, provided that m+n represents an integer of 4 or less.This compound is useful as an antipsychotic drug having a reduced extrapyramidal side effect.Type: GrantFiled: July 8, 1994Date of Patent: July 2, 1996Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Tohru Nakao, Yuji Ono, Masahiro Bougauchi, Yasuto Morimoto
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Patent number: 5530125Abstract: A novel process for the preparation of .alpha.-substituted arylacetamides wherein the substituent is an aromatic group or a 1-alkenyl or 1-cycloalkenyl group and wherein the nitrogen atom carries no hydrogen atoms comprises the reaction of an arylacetamide having one or two hydrogen atoms on the .alpha.-carbon atom, wherein the nitrogen atom carries no hydrogen atoms, with a strong base in an inert aprotic organic solvent, followed by reaction with a zerovalent transition metal catalyst and then with a compound of the formula R.sup.4 --X, wherein R.sup.4 is selected from aromatic groups, 1-alkenyl groups and 1-cycloalkenyl groups and X is a particular leaving group, especially a triflate group. The .alpha.-substituted arylacetamides are useful as intermediates in the preparation (by reduction) of .alpha.-substituted arylethylamines, e.g., 1-substituted-2,3,4,5-tetrahydro-1H-3-benzazepines, having pharmacological activity. Certain benzazepines wherein the 1-substituent R.sup.4 is 1-(1-cycloalkenyl) are novel.Type: GrantFiled: August 19, 1994Date of Patent: June 25, 1996Assignee: Schering CorportionInventors: Joel G. Berger, Wei K. Chang, Joseph A. Kozlowski, Guowei Zhou
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Patent number: 5498776Abstract: This invention relates to pyrrolo-, pyrido-, azepino-, and azocinopyrimidines of the general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently H, lower alkyl containing 1 to 6 carbon atoms, or perfluoroalkyl containing 1 to 6 carbon atoms; R.sup.5 is H or, when n is 1, R.sup.5 taken together with R.sup.3 comprises a double bond, n is 0 or 1, p is 0 to 2, m is 0 to 3; Ar.sup.1 is ##STR2## wherein W is H, lower alkyl containing 1 to 6 carbon atoms, halogen, hydroxy, or lower alkoxy containing 1 to 6 carbon atoms; and Ar.sup.2 is ##STR3## wherein X is ##STR4## wherein R.sup.6 is H, tert-butyl, tri-n-butylstannyl, or triphenylmethyl; and the pharmaceutically acceptable salts thereof, which compounds are useful in the treatment of hypertension and congestive heart failure.Type: GrantFiled: August 8, 1994Date of Patent: March 12, 1996Assignee: American Home Products CorporationInventors: John W. Ellingboe, Madelene Nikaido, Jehan Bagli
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Patent number: 5492902Abstract: Shearinines A, B and C, and 21-Isopentenylpaxilline are ascostromatal metabolites of the fungus Eupenicillium shearii. These indole alkaloid compounds are effective for controlling Coleopteran and Lepidopteran insects and the fall armyworm, Spodoptera frugiperda.Type: GrantFiled: December 2, 1994Date of Patent: February 20, 1996Assignees: The United States of America as represented by the Secretary of Agriculture, University of Iowa Research Foundation, Biotechnology Research & Development CorporationInventors: Gilbert N. Belofsky, James B. Gloer, Donald T. Wicklow, Patrick F. Dowd
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Patent number: 5444056Abstract: An aminoalkoxyphenyl derivative of general formula:Cy--B--Ph--O--A--Am (1)as well as a pharmaceutically acceptable salt thereof in whichB represents a --S--, --SO-- or --SO.sub.2 -- group,Ph represents an optionally substituted phenyl radical,A denotes a straight or branched alkylene radical having from 2 to 5 carbon atoms or a 2-hydroxy propylene radical in which the hydroxy is optionally substituted by a C.sub.1 -C.sub.4 alkyl radical.Am represents a group: ##STR1## and Cy is a cyclic group, provided that when Cy represents either a benzo[b]furyl group substituted at position 4 by a halogen atom or a C.sub.1 -C.sub.4 alkyl group, or a benzo[b]thienyl group substituted at position 4 by a halogen atom or by a C.sub.1 -C.sub.4 alkyl group and when B represents a --SO.sub.2 -- group, R.sub.3 represents a --Alk--Ar radical.Type: GrantFiled: February 7, 1990Date of Patent: August 22, 1995Assignee: SanofiInventors: Jean Gubin, Pierre Chatelain, Henri Inion, Gilbert Rosseels
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Patent number: 5434261Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.Type: GrantFiled: July 26, 1993Date of Patent: July 18, 1995Assignee: Merck & Co., Inc.Inventors: William R. Schoen, Matthew J. Wyvratt, Jr.
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Patent number: 5430144Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.Type: GrantFiled: July 26, 1993Date of Patent: July 4, 1995Assignee: Merck & Co., Inc.Inventors: William R. Schoen, Matthew J. Wyvratt, Jr., Paul J. Hodges
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Patent number: 5414009Abstract: The present invention relates to compounds ##STR1## where G is ##STR2## and Z is oxygen or sulfur and the remaining variables are as defined in the Specification. The compounds are useful as stimulants of the cognitive function of the forebrain and hippocampus of mammals and especially in the treatment of Alzheimer's disease, severe painful conditions and glaucoma.Type: GrantFiled: January 4, 1993Date of Patent: May 9, 1995Assignee: Novo Nordisk A/SInventors: Preben H. Olesen, Per Sauerberg