Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Ring Nitrogen Of The Bicyclo Ring System Patents (Class 540/583)
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Patent number: 10604480Abstract: The invention provides compounds of formula I and II and salts thereof, wherein R1, R2, Y, R3, and R4 have any of the meanings described in the specification, as well as compositions comprising such compounds and salts, and methods for treating cancer using such compounds and salts.Type: GrantFiled: January 27, 2016Date of Patent: March 31, 2020Assignees: Rutgers, The State University of New Jersey, The Research Foundation for the State University of New YorkInventors: David J. Augeri, Anthony F. Bencivenga, Adam Blanden, Darren R. Carpizo, John A. Gilleran, Spencer David Kimball, Stewart N. Loh, Xin Yu
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Patent number: 8877745Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (I) wherein HET is a group selected from among formulas (IIa) (IIb) (IIc) (IId) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD and pain diseases.Type: GrantFiled: May 10, 2011Date of Patent: November 4, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Rocco Mazzaferro, Stefan Scheuerer
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Patent number: 8614209Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.Type: GrantFiled: September 13, 2012Date of Patent: December 24, 2013Assignee: The University of EdinburghInventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
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Publication number: 20130165426Abstract: Disclosed is a compound of Formula I or a salt thereof, in which X, X1, X2, R1, R2, and R3 are described herein. Also disclosed are pharmaceutical compositions and methods of using the compounds of Formula I to treat disorders mediated by melanocortin-4 receptors.Type: ApplicationFiled: July 5, 2011Publication date: June 27, 2013Applicant: UNIVERSITÉ DE MONTRÉALInventors: Réjean Ruel, Yves Chantigny, Anne Marinier, Patricia Rene, Michel Bouvier
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Publication number: 20130150342Abstract: The invention is directed to novel pyrrolopyrimidine compounds of formula (I) wherein R1, R2Y, R4, R8-R11, A and L are defined herein and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: February 17, 2011Publication date: June 13, 2013Applicant: NOVARTIS AGInventors: Christopher Thomas Brain, Young Shin Cho, John William Giraldes, Bharat Lagu, Julian Roy Levell, Michael J. Luzzio, Lawrence Blas Perez, Yaping Wang, Fan Yang
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Publication number: 20130017273Abstract: The present invention relates to pyrrolopyrazines compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.Type: ApplicationFiled: June 22, 2012Publication date: January 17, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Simon Everitt, Michael Paul Mortimore, Jean-Damien Charrier, Somhairle MacCormick, Pierre-Henri Storck, Ronald Knegtel, Joanne Pinder, Steven John Durrant
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Publication number: 20100292215Abstract: A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11?-hydroxy-steroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.Type: ApplicationFiled: March 27, 2007Publication date: November 18, 2010Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Soren Ebdrup, Henrik Sune Andersen
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Publication number: 20100197662Abstract: Disclosed is a compound useful as a type I 11?hydroxysteroid dehydrogenase inhibitor. A compound represented by the formula: a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkenyl or the like, One of R2 and R3 is a group of the formula: —C(?O)—Y—R4, wherein Y is —NR9— or the like, R4 is optionally substituted cycloalkyl or the like, R9 is hydrogen or optionally substituted alkyl, W is optionally substituted alkylene, The other is a group of the formula: —V—R5, wherein V is a bond, —O— or the like, R6 is hydrogen or optionally substituted alkyl, R5 is hydrogen, optionally substituted alkyl or the like, X is a bond, —S—, —SO— or the like, U is a bond or optionally substituted alkylene, R7 is hydrogen or optionally substituted alkyl, Z is —S—, —O— or —NR8—, R8 is hydrogen, optionally substituted alkyl or the like.Type: ApplicationFiled: June 6, 2006Publication date: August 5, 2010Applicant: Shionogi & Co., Ltd.Inventors: Tomoyuki Ogawa, Noriyuki Kurose, Satoru Tanaka, Koichi Nishi
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Publication number: 20100009968Abstract: The use of substituted amides for modulating the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, of the general formula I. Their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11?HSDI and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.Type: ApplicationFiled: June 28, 2007Publication date: January 14, 2010Applicant: High Point Pharmaceuticals, LLCInventors: Soren Ebdrup, Henrik Sune Andersen
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Publication number: 20090325932Abstract: A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11?-hydroxy-steroid dehydrogenase type 1 (11 ?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g the metabolic syndrome.Type: ApplicationFiled: June 28, 2007Publication date: December 31, 2009Inventors: Soren Ebdrup, Henrik Sune Andersen
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Publication number: 20090124598Abstract: The use of substituted amides for modulating the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11?HSD1 and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.Type: ApplicationFiled: November 1, 2006Publication date: May 14, 2009Inventors: Henrik Sune Andersen, Anker Steen Jorgensen, John Paul Kilburn, Gita Camilla Tejlgaard Kampen, Soren Ebdrup
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Publication number: 20080226591Abstract: The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.Type: ApplicationFiled: March 11, 2008Publication date: September 18, 2008Inventors: Robert G. Gentles, Xiaofan Zheng, Min Ding, Yong Tu, Ying Han, Piyasena Hewawasam, John F. Kadow, John A. Bender, Kap-Sun Yeung, Katharine A. Grant-Young, Thomas W. Hudyma
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Patent number: 6812234Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.Type: GrantFiled: April 29, 2003Date of Patent: November 2, 2004Assignees: Merck & Co., Inc., Merck Sharp & Dohme Ltd.Inventors: Richard Jiao, Gregori Morriello, Lihu Yang, Stephen D. Goble, Sander G. Mills, Alexander Pasternak, Changyou Zhou, Gabor Butora, Shankaran Kothandaraman, Deodialsingh Guiadeen, Christopher Moyes, Cheng Tang
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Patent number: 6670371Abstract: Disclosed are compounds of the formula: wherein Ar is optionally substituted aryl or heteroaryl R1 is hydrogen or alkyl; R7 is hydrogen or alkyl; R2 is hydrogen, halogen, alkyl or alkoxy; or R1 and R2 taken together with the ring to which they are attached form a 5-9 membered saturated or aromatic ring optionally having a hetero atom selected from oxygen, sulfur or nitrogen; R3 and R4 are independently hydrogen, alkyl, cycloalkyl, aryl or heteroaryl groups; or R3 and R4 together with the nitrogen atom to which they are attached form a 5-8 membered ring; and R5 is hydrogen, halogen, straight or branched chain lower alkyl having 1-6 carbon atoms, or straight or branched chain lower alkoxy or thioalkoxy having 1-6 carbon atoms, which compounds are highly selective partial agonists or antagonists at human Corticotropin-Releasing Factor 1 (CRF1) receptors and are useful in the diagnosis and treatment of treating stress related disorders such as post trumatic stress disorder (PTSD) as welType: GrantFiled: March 12, 2002Date of Patent: December 30, 2003Assignee: Neurogen CorporationInventors: Raymond F. Horvath, Alan Hutchison
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Patent number: 6552015Abstract: The present invention is directed to a compound of the formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, Y, U, W, k, A, E, V, R4 and R5 are as defined herein, pharmaceutical compositions thereof, and methods of use thereof in the inhibition of serotonin reuptake, the inhibition of the binding of 5-HT2A serotonin receptors and the treatment of diseases, conditions or disorders of the central nervous system. Further, the present invention is also directed to methods for the preparation of compounds of formula (I) and intermediates useful therefor.Type: GrantFiled: August 1, 2001Date of Patent: April 22, 2003Assignee: Pfizer Inc.Inventors: Anton Franz Joseph Fliri, Todd William Butler, Randall James Gallaschun
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Patent number: 6531468Abstract: The present invention provides diazabicyclooctane derivatives of formula (I): and pharmaceutically acceptable salts thereof, wherein the group represents R1 and R2 are selected independently from H, (C1-C6)alkyl, (C1-C6)fluoroalkyl, halogen (e.g., F.Type: GrantFiled: August 1, 2001Date of Patent: March 11, 2003Assignee: Pfizer IncInventors: Anton Franz Joseph Fliri, Randall James Gallaschun
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Patent number: 6355651Abstract: Disclosed are compounds of the formula: wherein Ar is optionally substituted aryl or heteroaryl R1 is hydrogen or alkyl; R7 is hydrogen or alkyl; R2 is hydrogen, halogen, alkyl or alkoxy; or R1 and R2 taken together with the ring to which they are attached form a 5-9 membered saturated or aromatic ring optionally having a hetero atom selected from oxygen, sulfur or nitrogen; R3 and R4 are independently hydrogen, alkyl, cycloalkyl, aryl or heteroaryl groups; or R3 and R4 together with the nitrogen atom to which they are attached form a 5-8 membered ring; and R5 is hydrogen, halogen, straight or branched chain lower alkyl having 1-6 carbon atoms, or straight or branched chain lower alkoxy or thioalkoxy having 1-6 carbon atoms, which compounds are highly selective partial agonists or antagonists at human Corticotropin-Releasing Factor 1 (CRF1) receptors and are useful in the diagnosis and treatment of treating stress related disorders such as post trumatic stress disorder (PTSD) as welType: GrantFiled: September 6, 2000Date of Patent: March 12, 2002Assignee: Neurogen CorporationInventors: Raymond F. Horvath, Alan Hutchison
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Patent number: 6133282Abstract: Disclosed are compounds of the formula: ##STR1## wherein Ar is optionally substituted aryl or heteroarylR.sub.1 is hydrogen or alkyl;R.sub.7 is hydrogen or alkyl;R.sub.2 is hydrogen, halogen, alkyl or alkoxy; orR.sub.1 and R.sub.2 taken together with the ring to which they are attached form a 5-9 membered saturated or aromatic ring optionally having a hetero atom selected from oxygen, sulfur or nitrogen;R.sub.3 and R.sub.4 are independently hydrogen, alkyl, cycloalkyl, aryl or heteroaryl groups; orR.sub.3 and R.sub.4 together with the nitrogen atom to which they are attached form a 5-8 membered ring; andR.sub.Type: GrantFiled: August 5, 1999Date of Patent: October 17, 2000Assignee: Neurogen CorporationInventors: Raymond F. Horvath, Alan Hutchison
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Patent number: 5889022Abstract: Novel indole, indoline and quinoline derivatives of formula (I) processes for their preparation, pharmaceutical compositions containing them, and their use in medicine is disclosed. A structurally distinct class of compounds have now been discovered and have been found to exhibit 5HT.sub.1-D antagonist activity. In a first aspect, the present invention therefore provides a compound of formula (I) or a salt thereof, in which P is a 5-7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen or sulphur, A, B, m, R.sup.1 -R.sup.8 are defined in the application.Type: GrantFiled: June 20, 1996Date of Patent: March 30, 1999Assignee: SmithKline Beecham, p.l.c.Inventors: Laramie Mary Gaster, Paul Adrian Wyman
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Patent number: 5698690Abstract: The invention provides hydroxamic acid derivatives of the general formula ##STR1## wherein Bz represents benzyl; R.sup.1 represents cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; R.sup.2 represents a saturated 5- to 8-membered monocyclic or bridged N-heterocyclic ring, which N-heterocyclic ring is attached via the N atom and when it is monocyclic, optionally contains NR.sup.4, O, S, SO or SO.sub.2 as a ring member and/or is optionally substituted on one or more C atoms by hydroxy, lower alkyl, lower alkoxy, oxo, ketalized oxo, amino, mono(lower alkyl)amino, di(lower alkyl)amino,carboxy, lower alkoxycarbonyl, hydroxy-methyl, lower alkoxymethyl, carbamoyl, mono(lower alkyl)-carbamoyl, di(lower alkyl)carbamoyl or hydroxy-imino; R.sup.3 represents a 5- or 6-membered N-heterocyclic ring which (a) is attached via the N atom, (b) optionally contains N, O and/or S, SO or SO.sub.Type: GrantFiled: October 29, 1996Date of Patent: December 16, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Michael John Broadhurst, Paul Anthony Brown, William Henry Johnson
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Patent number: 5614625Abstract: The invention provides hydroxamic acid derivatives of the general formula ##STR1## wherein R.sup.1 represents cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; R.sup.2 represents a saturated 5- to 8-membered monocyclic or bridged N-heterocyclic ring, which N-heterocyclic ring is attached via the N atom and when it is monocyclic, optionally contains NR.sup.4, O, S, SO or SO.sub.2 as a ring member and/or is optionally substituted on one or more C atoms by hydroxy, lower alkyl, lower alkoxy, oxo, ketalized oxo, amino, mono(lower alkyl)amino, di(lower alkyl)amino, carboxy, lower alkoxycarbonyl, hydroxy-methyl, lower alkoxymethyl, carbamoyl, mono(lower alkyl)-carbamoyl, di(lower alkyl)carbamoyl or hydroxyimino; R.sup.3 represents a 5- or 6-membered N-heterocyclic ring which (a) is attached via the N atom, (b) optionally contains N, O and/or S, SO or SO.sub.Type: GrantFiled: April 5, 1995Date of Patent: March 25, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Michael J. Broadhurst, Paul A. Brown, William H. Johnson
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Patent number: 5610154Abstract: Bicyclic carboxamides of formula I ##STR1## and the pharmaceutically acceptable acid addition salts are 5-HT.sub.1A binding agents, particularly 5-HT.sub.1A antagonists and may be used, for example, as anxiolytics. In the formulaX represents --CR.sup.2 .dbd.CR.sup.2 -- or --(CR.sup.2)q--;m represents 0,1 or 2; n represents 0,1 or 2; p represents 0,1,2 or 3 and q represents 0,1,2 or 3;A is an alkylene chain of 1 or 2 carbon atoms optionally substituted by one or more lower alkyl groups,R is a mono or bicyclic aryl or heteroaryl radical,R.sup.1 is an aryl or aryl(lower)alkyl radicaland each R.sup.2 is independently hydrogen or lower alkyl.Type: GrantFiled: May 24, 1995Date of Patent: March 11, 1997Assignees: John Wyeth & Brother, Ltd., American Home Products Corp.Inventors: Ian A. Cliffe, Howard L. Mansell, Terence J. Ward, James A. Nelson, Uresh S. Shah, Mira A. Kanzelberger
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Patent number: 5569659Abstract: Compounds of the general formula I: ##STR1## are disclosed as novel antipsychotic agents.Type: GrantFiled: May 17, 1995Date of Patent: October 29, 1996Assignee: McNeilab, Inc.Inventor: Allen B. Reitz
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Patent number: 5538950Abstract: A compound of the formula: ##STR1## in which R.sup.3 is hydrogen or lower alkyl, R.sup.4 is pyridyl (lower) alkyl; andR.sup.1, R.sup.2, R.sup.5 and A are defined in the description;or a pharmaceutically acceptable salt thereof, which have endothelin antagonistic activity.Type: GrantFiled: May 12, 1994Date of Patent: July 23, 1996Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Keiji Hemmi, Masahiro Neya, Naoki Fukami, Masashi Hashimoto, Hirokazu Tanaka, Natsuko Kayakiri
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Patent number: 5413997Abstract: A triphenylmethane derivative represented by the following general formula: ##STR1## exhibits bone absorption inhibiting effects and is useful as a medicament for treating osteoporosis.Type: GrantFiled: January 21, 1993Date of Patent: May 9, 1995Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Iwao Kinoshita, Daisuke Machii, Yasuo Onoda, Haruki Takai, Nobuo Kosaka, Katsuichi Shuto, Katsushige Gomi, Makoto Morimoto, Akio Ishii
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Patent number: 5411957Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having a 3-azabicyclo[3.2.2]-nonanyl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.Type: GrantFiled: January 25, 1994Date of Patent: May 2, 1995Assignee: G.D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5399553Abstract: A tricyclic compound represented by the general formula (1) and salts thereof are disclosed. ##STR1## A method for producing the tricyclic compound and salts thereof, and an antimicrobial agent containing the tricyclic compound and salts thereof as an active ingredient are also disclosed.Type: GrantFiled: June 16, 1993Date of Patent: March 21, 1995Assignees: Wakunaga Seiyaku Kabushiki Kaisha, Fujisawa Pharmaceutical Company, Ltd.Inventors: Masaharu Yokomoto, Akira Yazaki, Norihiro Hayashi, Shunso Hatono, Satoshi Inoue, Yasuhiro Kuramoto
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Patent number: 5244899Abstract: The compounds of this invention are azabicyclic and azatricyclic amides represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided that n+m+p is equal to or less than 10; X is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene; R.sub.3 is selected from the group consisting of a azabicycloalkylamino, azatricycloalkylamino or dicycloalkylamino. The compounds are useful as anti-inflammatory and anti-allergy agents.Type: GrantFiled: July 29, 1992Date of Patent: September 14, 1993Assignee: G. D. Searle and Co.Inventors: Richard A. Mueller, Richard A. Partis, James R. Deason
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Patent number: 5198435Abstract: The compounds of this invention are bicyclic, tricyclic, azabicyclic and azatricyclic amides represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided than n+m+p is equal to or less than 10; x is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene; R.sub.3 is selected from the group consisting of a bicycloalkylamino, tricycloalkylamino, azabicycloalkyl, azatricycloalkyl, azabicycloalkylamino, azatricycloalkylamino or dicycloalkylamino. The compounds are useful as anti-inflammatory and anti-allergy agents.Type: GrantFiled: March 14, 1991Date of Patent: March 30, 1993Assignee: G. D. Searle & Co.Inventors: Richard A. Mueller, Richard A. Partis, James R. Deason
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Patent number: 5081117Abstract: This invention relates to 4- and 6-carbamates related to physostigmine of the formula ##STR1## where R.sub.1 is alkyl, cycloalkyl, bicycloalkyl, aryl or arylloweralkyl; R.sub.2 is hydrogen or alkyl or the group --NR.sub.1 R.sub.2 taken together forms a monocyclic or bicyclic ring of 5 to 12 carbons; m is 0,1, or 2; each X is independently hydrogen, halogen, loweralkyl, nitro or amino; and the pharmaceutically acceptable acid addition salts thereof, and where applicable, the geometric and optical isomers and racemic mixtures thereof. This invention also relates to novel intermediates useful in the preparation of the 4- and 6-carbamates. The compounds of this invention display utility for alleviating various memory dysfunctions characterized by a decreased cholinergic function, such as Alzheimer's disease.Type: GrantFiled: November 3, 1989Date of Patent: January 14, 1992Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Edward J. Glamkowski, Barbara E. Kurys
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Patent number: 4968341Abstract: Novel substituted aryloxyureas, processes for their production, and herbicides comprising them as active ingredients are provided.The substituted aryloxyureas exhibit an excellent herbicidal efficacy against weeds when applied, for example, to the weeds in a wide range of period from a preemergence stage to a growth stage.The substituted aryloxyureas of the invention have the excellent advantage of maintaining high safety on crops or crop plants in spite of their herbicidal efficacy.Type: GrantFiled: August 16, 1988Date of Patent: November 6, 1990Assignees: Kumiai Chemical Industry Co., Mitsui Petrochemical Industries, Ltd.Inventors: Isao Hashimoto, Tatsuyodihi Ishida, Kazutaka Tsuru, Yuji Yamada, Takeshige Miyazawa, Yasuo Nakamura, Susumu Katou, Katsuya Takahashi
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Patent number: 4925849Abstract: The disclosure deals with a pyrazolopyridine compound of the formula ##STR1## wherein the variables are defined in the specification. The compounds are useful as a diuretic, antihypertensive agent, etc.Type: GrantFiled: June 6, 1988Date of Patent: May 15, 1990Assignee: Fujisawa Pharmaceutical Company, Ltd.Inventors: Youichi Shiokawa, Atsushi Akahane, Hirohito Katayama, Takafumi Mitsunaga
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Patent number: 4775668Abstract: Antibacterial compounds have the formula ##STR1## wherein R.sup.1 is hydrogen, a pharmaceutically aceptable cation, or alkyl; A is CH, CF, CCl or N; Y is alkyl, haloalkyl, cyclopropyl, vinyl, methoxy, N-methylamino, p-fluorophenyl, p-hydroxyphenyl or p-aminophenyl; or A is carbon and is taken together with Y and the carbon and nitrogen to which A and Y are attached to form a five to seven membered ring which is optionally substituted; and R.sup.2 is a bridged-diazabicycloalkyl group.Type: GrantFiled: August 19, 1986Date of Patent: October 4, 1988Assignee: Pfizer Inc.Inventors: Martin R. Jefson, Paul R. McGuirk
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Patent number: 4665173Abstract: This invention relates to novel 2-acetyl- and 2-propionylpyridine selenosemicarbazones. These compounds are useful as antimalarial and antileukemic agents. Also disclosed are several synthetic procedures used to prepare the selenosemicarbazones.Type: GrantFiled: March 31, 1982Date of Patent: May 12, 1987Inventors: Daniel L. Klayman, John P. Scovill