Additional Ring Containing Patents (Class 546/337)
  • Patent number: 5767085
    Abstract: Compounds of the formula A--B--C--D(--E).sub.p are used to stimulate the release of growth hormone from the pituitary.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: June 16, 1998
    Assignee: Novo Nordisk A/S
    Inventors: Nils Langeland Johansen, Jesper Lau, Kjeld Madsen, Behrend Friedrich Lundt, Henning Th.o slashed.gersen, Birgit Sehested Hansen, Bernd Peschke
  • Patent number: 5763460
    Abstract: Compounds of formula (I) and the pharmaceutically acceptable acid addition salts thereof are 5-HT.sub.1A binding agents and may be used, for example, as anxiolytics. In the formula a and b each represents 0, 1, 2 or 3 such that the sum of a+b is 0, 1, 2 or 3, the dotted line represents an optional double bond which may be present in the ring, provided that a is at least 1, 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 with the proviso that R is not an unsubstituted phenyl group, R.sup.1 is a mono or bicyclic heteroaryl radical, and R.sup.2 is cycloalkyl or cycloalkenyl.
    Type: Grant
    Filed: January 16, 1996
    Date of Patent: June 9, 1998
    Assignees: John Wyeth & Brother Limited, American Home Products Corporation
    Inventors: Ian Anthony Cliffe, Terence James Ward, Chapman White Alan, Antony Ashwell Mark, Bernhard Baudy Reinhardt
  • Patent number: 5760246
    Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure ##STR1## including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2;R.sup.x is H, alkyl, aryl or halogen;A is(1) a bond;(2) --O--; or(3) ##STR2## B is: ##STR3## and wherein L.sup.2, L.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.3', R.sup.3a, R.sup.3b, R.sup.4, R.sup.4', R.sup.5, X, ##STR4## are as defined herein.
    Type: Grant
    Filed: December 17, 1996
    Date of Patent: June 2, 1998
    Inventors: Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Jeffrey A. Robl, William A. Slusarchyk, Richard B. Sulsky, Joseph A. Tino
  • Patent number: 5728838
    Abstract: A process for the preparation of a compound of structural formula I ##STR1## wherein R.sup.1 is alkyl, alkenyl, phenyl or substituted phenyl, which comprises the addition of R.sup.1 to an intermediate 2: ##STR2## by treatment of 2 with (R.sup.1).sub.3 M followed by reductive removal of the sulfinyl group.
    Type: Grant
    Filed: April 2, 1997
    Date of Patent: March 17, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Ioannis Houpis, Audrey Molina, Ralph P. Volante
  • Patent number: 5723475
    Abstract: The compound of the formula (I) or its salt or a medicament containing the same ##STR1## wherein, A and B represent a carbonyl group or sulfonyl group, m and p are different and represent 0 or 1,R.sup.1 and R.sup.2 may be the same or different from each other and represent a hydrogen atom, an unsubstituted or substituted alkyl group, an unsubstituted or substituted aryl group, an unsubstituted or substituted aralkyl group, an unsubstituted or substituted heterocyclic group containing nitrogen or an unsubstituted or substituted heterocyclic group containing oxygen, or R.sup.1 and R.sup.2, taken together with the nitrogen atom to which they are linked, may form an unsubstituted or substituted heterocyclic group, provided that when B is a sulfonyl group, R.sup.
    Type: Grant
    Filed: October 28, 1996
    Date of Patent: March 3, 1998
    Assignee: Suntory Limited
    Inventors: Hirokazu Annoura, Mayumi Uesugi, Atsuko Fukunaga, Shigeki Tamura
  • Patent number: 5714518
    Abstract: HIV protease inhibitors, obtainable by chemical synthesis, block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and possibly other anti-vital agents as ingredients, are thus suitable for the treatment of the HIV virus known to cause AIDS.
    Type: Grant
    Filed: October 27, 1994
    Date of Patent: February 3, 1998
    Assignee: Agouron Pharmaceuticals
    Inventors: Siegfried H. Reich, Mark J. Pino, Dzuy T. Nguyen, Anthony J. Trippe
  • Patent number: 5672615
    Abstract: Disclosed are the compounds of formula I ##STR1## wherein R and R.sub.1 together with the chain to which they are attached or R.sub.1 and R.sub.2 together with the carbon atom to which they are attached form a ring; pharmaceutically acceptable prodrug derivatives and pharmaceutically salts thereof; methods of preparation thereof; pharmaceutical compositions comprising said compounds; and a method of inhibiting matrix-degrading metalloproteinase and of treating matrix-degrading metalloproteinase dependent conditions in mammals using such compounds.
    Type: Grant
    Filed: March 11, 1996
    Date of Patent: September 30, 1997
    Assignee: Novartis Corporation
    Inventors: Lawrence J. MacPherson, David Thomas Parker
  • Patent number: 5665886
    Abstract: The invention concerns compounds of formula: ##STR1## in which Am.sup.+ represents a substituted 1-pyridylium radical, a substituted 3-thiazolylium radical, a substituted 1-pyridazinylium radical or a substituted 3-imidazolylium radical, and their salts with mineral or organic acids, whether in their optically pure or racemic form. The invention also concerns a process for the preparation of these compounds and pharmaceutical compositions containing them. Activity: antagonists of neurokinin receptors.
    Type: Grant
    Filed: November 24, 1995
    Date of Patent: September 9, 1997
    Assignee: Sanofi
    Inventors: Nathalie Chabert, Xavier Emonds-Alt, Vincenzo Proietto, Didier Van Broeck
  • Patent number: 5646167
    Abstract: Disclosed are compounds of formula I ##STR1## wherein R, R.sub.1, R.sub.2 and Ar have meanings as defined; pharmaceutically acceptable prodrug derivatives and pharmaceutically acceptable salts thereof; methods for preparation thereof; pharmaceutical compositions comprising said compounds; and methods of inhibiting matrix-degrading metalloproteinase and of treating matrix-degrading metalloproteinase dependent conditions in mammals using such compounds.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 8, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: Lawrence J. MacPherson, David T. Parker
  • Patent number: 5643914
    Abstract: This invention relates to a compound of formula 1 ##STR1## or an N-oxide, or a pharmaceutically acceptable salt, where A is CH.sub.2 and Z is S(O).sub.q where q is 0, 1 or 2, CH.sub.2, CHOH, CO, NR.sub.x, or O, orA is C.dbd.O and Z is NR.sub.x ;m is 0-5;R.sub.x is hydrogen or lower alkyl;R is C.sub.1 to C.sub.20 -aliphatic, unsubstituted or substituted five-membered heteroaryl-C.sub.1 to C.sub.10 -aliphatic-O--, unsubstituted or substituted phenyl-C.sub.1 to C.sub.10 -aliphatic where substituted p from the group consisting of lower alkoxy, lower alkyl, trihalomethyl, and halo, or R is C.sub.1 to C.sub.20 -aliphatic-O--, or R is unsubstituted or substituted phenyl-C.sub.1 to C.sub.10 -aliphatic-O-- where substituted phenyl has one or more radicals selected from the group consisting of lower alkoxy, lower alkyl, trihalomethyl, and halo;R.sub.1 is R.sub.4, --(C.sub.1 to C.sub.5 aliphatic)R.sub.4, --(C.sub.1 to C.sub.5 aliphatic)CHO, --(C.sub.1 to C.sub.5 aliphatic)CH.sub.2 OR.sub.5;R.sub.2 and R.sub.
    Type: Grant
    Filed: December 19, 1994
    Date of Patent: July 1, 1997
    Assignee: SmithKline Beecham Corporation
    Inventor: Robert A. Daines
  • Patent number: 5631262
    Type: Grant
    Filed: May 11, 1995
    Date of Patent: May 20, 1997
    Assignee: SmithKline Beecham Corporation
    Inventors: Pamela A. Chambers, Robert A. Daines, Dalia R. Jakas, William D. Kingsbury, Israil Pendrak
  • Patent number: 5623076
    Abstract: The invention relates to a new process for the preparation of chloromethylpyridines of the general formula (I) ##STR1## in which X.sup.1 represents hydrogen, halogen or alkyl,characterized in that pyridine derivatives of the general formula (II) ##STR2## in which R.sup.1 and X.sup.1 have the meaning given in the description,are reacted by means of a formamide derivative of the general formula (III) ##STR3## in which R.sup.2 and R.sup.3 are identical or different and represent alkyl or cycloalkyl or together represent alkanediyl,and with a chlorinating agent, if appropriate in the presence of a diluent, at temperatures between 20.degree. and 120.degree. C. The invention furthermore relates to new pyridine derivatives of the formula (II) and their preparation.
    Type: Grant
    Filed: December 18, 1995
    Date of Patent: April 22, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventor: Reinhard Lantzsch
  • Patent number: 5618931
    Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning described in the specification have retinoid-like biological activity.
    Type: Grant
    Filed: December 29, 1994
    Date of Patent: April 8, 1997
    Assignee: Allergan
    Inventors: Richard L. Beard, Min Teng, Alan T. Johnson, Vidyasagar Vuligonda, Roshantha A. Chandraratna
  • Patent number: 5618849
    Abstract: A compound represented by formula IAr.sub.1 --O--M--O--Ar.sub.2 Iwherein Ar.sub.1 and Ar.sub.2 are independently substituted phenyl or substituted pyridinyl, the substituents on said phenyl or pyridinyl being independently selected from one, two or three of (C.sub.1 -C.sub.10) alkyl, (C.sub.1 -C.sub.10) alkoxy, halogen, carbamyl, (C.sub.1 -C.sub.10) alkoxycarbonyl, oxazoyl, and (C.sub.1 -C.sub.10) alkyl substituted by halogen, (C.sub.1 -C.sub.10) alkoxy, hydroxy, or (C.sub.1 -C.sub.10) alkoxycarbonyl; ##STR1## (C.sub.4 -C.sub.8) alkylene, (C.sub.4 -C.sub.8) alkenylene or (C.sub.4 -C.sub.8)-alkynylene;O is oxygen;or pharmaceutically acceptable salts thereof.as well as pharmaceutical compositions containing the compounds and methods of treating or preventing viral infections, especially picornaviral infections, are disclosed.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: April 8, 1997
    Assignee: Schering Corporation
    Inventors: Viyyoor M. Girijavallabhan, Ashit K. Ganguly, Richard W. Versace
  • Patent number: 5612336
    Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q.sup.1 is phenyl substituted by one or more halo; optionally substituted naphthyl, indolyl, benzothiophenyl, benzofuranyl, benzyl or fluorenyl; the dotted line represents an optional covalent bond; one of X and Y is H and the other is hydroxy or C.sub.1-6 alkoxy, or X and Y together form a group .dbd.O or .dbd.NOR.sup.5 where R.sup.5 is H or C.sub.1-6 alkyl; R.sup.1 is H or C.sub.1-6 alkyl. R.sup.2 is CO--W--R.sup.6 where W represents a bond or a hydrocarbon chain of 1-6 carbon atoms and R.sup.6 is an azacyclic or azabicyclic group; R.sup.3 is H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; and R.sup.4 is phenyl optionally substituted by 1-3 of C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, OR.sup.a, SR.sup.a, SOR.sup.a, NR.sup.a R.sup.b, NR.sup.a COR.sup.b, NR.sup.a CO.sub.2 R.sup.b, CO.sub.2 R.sup.a or CONR.sup.a R.sup.b, where R.sup.a and R.sup.b are H, C.sub.
    Type: Grant
    Filed: January 13, 1995
    Date of Patent: March 18, 1997
    Assignee: Merck, Sharp & Dohme Ltd.
    Inventors: Richard J. Lewis, Angus M. MacLeod, Kevin J. Merchant
  • Patent number: 5607953
    Abstract: A butenoic or propenoic acid derivative having the following formula in which G is an aryl or a heterocyclic ring, R11 and R12 are hydroben or an alkyl, X is sulfur or oxygen, R2 and R3 are hydrogen, an substituent such as an alkyl and J is pyridyl or phenyl having substituents and a heterocyclic ring may be formed between R2, R3 and J is provided here and is useful in the pharmacological field.
    Type: Grant
    Filed: November 23, 1994
    Date of Patent: March 4, 1997
    Assignee: Eisai Co., Ltd.
    Inventors: Norio Minami, Fumihiro Ozaki, Keiji Ishibashi, Yasuhiro Kabasawa, Megumi Ikemori, Toshiaki Ogawa, Takanori Kawamura
  • Patent number: 5605915
    Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning defined in the specification.
    Type: Grant
    Filed: May 31, 1996
    Date of Patent: February 25, 1997
    Assignee: Allergan
    Inventors: Vidyasagar Vuligonda, Richard L. Beard, Alan T. Johnson, Min Teng, Tae K. Song, Roshantha A. Chandraratna
  • Patent number: 5602119
    Abstract: Succinoylamino hydroxyethylamino sulfamic acid derivative compounds which are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: January 31, 1995
    Date of Patent: February 11, 1997
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Patent number: 5597839
    Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## X represents a divalent radical, Z represents O, S or a divalent radical,and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.
    Type: Grant
    Filed: April 28, 1995
    Date of Patent: January 28, 1997
    Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)
    Inventors: Jean-Michel Bernardon, William R. Pilgrim
  • Patent number: 5587391
    Abstract: The invention relates to 7-[5-hydroxy-2-(hydroxyhydrocarbyl or heteroatom-substituted hydroxy hydrocarbyl)-3-hydroxycyclopentyl(enyl)] heptanoic or heptenoic acids and derivatives of said acids, wherein one or more of said hydroxy groups are replaced by an ether group. The compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma.
    Type: Grant
    Filed: July 11, 1995
    Date of Patent: December 24, 1996
    Assignee: Allergan
    Inventor: Robert M. Burk
  • Patent number: 5585374
    Abstract: Amide derivatives of formula (I) and their pharmaceutically acceptable salts (where a and b each represent 0, 1, 2 or 3 such that a+b=0, 1, 2 or 3, the dotted line represents an optional double bond, A is an optionally substituted C.sub.1-2 -alkylene chain, R is mono or bicyclic aryl or heteroaryl radical, R.sup.1 is hydrogen or lower alkyl, R.sup.2 is an aryl, aralkyl, heteroaryl or heteroarylalkyl and --CONR.sup.3 R.sup.4 represents a specified amide group) are 5-HT.sub.1A binding agents and may be used, for example, as anxiolytics.
    Type: Grant
    Filed: February 1, 1995
    Date of Patent: December 17, 1996
    Assignee: John Wyeth Brother, Limited
    Inventors: Ian A. Cliffe, Alan C. White
  • Patent number: 5583132
    Abstract: Sulfonylalkanoylamino hydroxyethylamino sulfamic acid compounds which are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: February 2, 1995
    Date of Patent: December 10, 1996
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Patent number: 5580983
    Abstract: 2-Chloro-5-(N-acyl-aminomethyl)pyridines can be prepared by hydrogenation of 2-chloro-5-cyanopyridine with hydrogen in an acylating agent using a hydrogenation catalyst.
    Type: Grant
    Filed: June 27, 1995
    Date of Patent: December 3, 1996
    Assignee: Bayer Aktiengesellschaft
    Inventor: Helmut Kraus
  • Patent number: 5563168
    Abstract: O-Benzyloxime ethers of the formula I ##STR1## where 5 X is substituted or unsubstituted CH.sub.2, NOalkylY isO, S, NR.sup.5R.sup.1, R.sup.2, R.sup.5 are H, alkylZ.sup.1, Z.sup.2 are H, halogen, methyl, methoxy, cyanoR.sup.3, R.sup.4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl,N(R.sup.6).sub.2, where R.sup.6 is H, alkyl, substituted or unsubstituted phenyl,--CO--N(R.sup.7).sub.2, where R.sup.
    Type: Grant
    Filed: June 16, 1995
    Date of Patent: October 8, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
  • Patent number: 5559140
    Abstract: This invention relates to novel difluoro statone analogs, to the processes and intermediates useful for their preparation and to their use as anti-viral agents.
    Type: Grant
    Filed: June 30, 1993
    Date of Patent: September 24, 1996
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Daniel Schirlin, Viviane Van Dorsselaer, Celine Tarnus
  • Patent number: 5557006
    Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth fire disclosed.
    Type: Grant
    Filed: April 20, 1995
    Date of Patent: September 17, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: John J. Tegeler, Barbara S. Rauckman, Russell R. L. Hamer, Brian S. Freed, Gregory H. Merriman
  • Patent number: 5552419
    Abstract: The invention relates to the compounds of formula I ##STR1## pharmaceutically acceptable prodrug derivatives and pharmaceutically acceptable salts thereof; methods for preparation thereof; pharmaceutical compositions comprising said compounds; and a method of inhibiting matrix-degrading metalloproteinase and of treating matrix-degrading metalloproteinase dependent conditions in mammals using such compounds.
    Type: Grant
    Filed: November 3, 1994
    Date of Patent: September 3, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Lawrence J. MacPherson, David T. Parker
  • Patent number: 5550137
    Type: Grant
    Filed: June 14, 1993
    Date of Patent: August 27, 1996
    Assignee: Celltech Therapeutics Limited
    Inventors: Nigel R. A. Beeley, Thomas A. Millican
  • Patent number: 5545741
    Abstract: The invention relates to a process for the preparation of racemic or optically active epibatidine of the Formula XIV ##STR1## which comprises subjecting racemic or optically active epi-epibatidine-of the Formula XIII ##STR2## to epimerization in the presence base. The advantage of the process is that readily available starting materials are used and the procedure is suitable for industrial scale productions too.Epibatidine is a known highly affective analgesic active ingredient.
    Type: Grant
    Filed: December 5, 1994
    Date of Patent: August 13, 1996
    Assignee: Egis Gyogyszergyar Rt.
    Inventors: Csaba Sz antay, Zsuzsanna B. Kardos, Istv an Moldvai, Eszter T. Major, Csaba Sz antay, Jr., Attila M andi, G abor Blask o, Gyula Simig, Gy orgyi Lax, S andor Drabant, Tamas Sz all asi, M arton Fekete, G abor Gigler
  • Patent number: 5545647
    Abstract: 3-Phenylpyrrolidine compounds of the formula ##STR1## effectively inhibit phosphodiesterase (PDE) IV activities and can be used as medicaments for conditions such as asthma.
    Type: Grant
    Filed: March 6, 1995
    Date of Patent: August 13, 1996
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Toshihiko Tanaka, Akihiro Yamamoto, Akira Amenomori
  • Patent number: 5543423
    Abstract: The present invention relates to compounds that can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for treatment of multi-drug resistant cells, for prevention of the development of multi-drug resistance, and for use in multi-drug resistant cancer therapy.
    Type: Grant
    Filed: January 23, 1995
    Date of Patent: August 6, 1996
    Assignee: Vertex Pharmaceuticals, Incorporated
    Inventors: Robert E. Zelle, Matthew W. Harding
  • Patent number: 5523315
    Abstract: Disclosed herein are compounds of the formula:A--N(R.sup.1)C(O)CH.sub.2 CHR.sup.2 C(O)--Bwherein A is various oxygen-bearing radicals; for example, HO--CH(R.sup.3)CH.sub.2 wherein R.sup.3 is, inter alia, hydrogen, lower alkyl, lower cycloalkyl or phenyl; or HO--CR.sup.5 (R.sup.6)CH.sub.2 wherein each of R.sup.5 and R.sup.6 is lower alkyl, or R.sup.5 and R.sup.6 together with the carbon atom to which they are attached form a 1,1-(lower cycloalkanediyl); R.sup.1 is, for example, benzyl, alkyl or a substituted alkyl such as cyclohexylmethyl; R.sup.2 is, for example, cyclo-alkylmethyl, 1H-imidazol-4-ylmethyl, 4-thiazolylmethyl or (2-amino-4-thiazolyl)methyl; and B is a renin substrate transition state mimic, for example, [1(S)-(cyclohexylmethyl)-2(R),3(S)-dihydroxy-5-methylhexyl]amino. The compounds inhibit renin activity and are indicated for the treatment of hypertension and congestive heart failure.
    Type: Grant
    Filed: September 20, 1993
    Date of Patent: June 4, 1996
    Assignee: Bio-Mega/Boehringer Ingelheim Research Inc.
    Inventors: Paul C. Anderson, Teddy Halmos, Grace L. Jung, Marc-Andre Poupart, Bruno Simoneau
  • Patent number: 5514694
    Abstract: A novel class of peptide .alpha.-ketoamides useful for selectively inhibiting serine proteases, selectively inhibiting cysteine proteases, generally inhibiting all serine proteases, and generally inhibiting all cysteine proteases, having the formula Y--CO--AA.sup.2 --AA.sup.1 --CO--NH--X. Processes for the synthesis of peptidyl .alpha.-ketoamide derivatives.
    Type: Grant
    Filed: June 24, 1993
    Date of Patent: May 7, 1996
    Assignee: Georgia Tech Research Corp
    Inventors: James C. Powers, Zhaozhao Li, Girish S. Patil, Der-Lun Chu
  • Patent number: 5514677
    Abstract: Compounds of general formula I: ##STR1## wherein: A represents the group --NH.sub.2, a substituted acyclic amine or a heterocyclic base;have collagenase inhibition activity and are useful in the management of disease involving tissue degradation and/or the promotion of wound healing. Diseases involving tissue degradation include arthropathy (particularly rheumatoid arthritis), inflammation, dermatological diseases, bone resorption diseases and tumour invasion.
    Type: Grant
    Filed: April 18, 1994
    Date of Patent: May 7, 1996
    Assignee: British Biotech Pharmaceuticals Limited
    Inventors: Alan H. Davidson, Jonathan P. Dickens, Michael J. Crimmin
  • Patent number: 5506242
    Abstract: The invention relates to a method of inhibiting metalloellastase activity, of inhibiting the degradation of elastin, or of treating macrophage metalloelastase dependent conditions in mammals which comprises administering to a mammal in need thereof an effective macrophage metalloelastase inhibiting amount of a compound of formula I ##STR1## wherein Ar, R, R.sub.1 and R.sub.2 have meanings as defined, or of a pharmaceutically acceptable prodrug derivative thereof, or of a pharmaceutically acceptable salt thereof, or of pharmaceutical compositions comprising a said compound.
    Type: Grant
    Filed: June 24, 1994
    Date of Patent: April 9, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Lawrence J. MacPherson, David T. Parker, Arco Y. Jeng
  • Patent number: 5476944
    Abstract: The present invention relates to derivatives of cyclic phenolic thioethers of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, which are inhibitors or stimulators of superoxide generation, and which may also inhibit cyclooxygenase and/or 5-lipoxygenase, to pharmaceutical compositions containing one or more of these compounds in combination with a pharmaceutically-acceptable carrier, and to medical methods of treatment employing these compounds.
    Type: Grant
    Filed: May 19, 1994
    Date of Patent: December 19, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Partis, Richard A. Mueller, Francis J. Koszyk, Richard M. Weier
  • Patent number: 5463067
    Abstract: Intermediates of structural formula ##STR1## can be made by reacting glycidol or an activated derivative thereof with an amide. The process and intermediates are useful for synthesizing HIV protease inhibitor compounds.
    Type: Grant
    Filed: January 26, 1994
    Date of Patent: October 31, 1995
    Assignee: Merck & Co., Inc.
    Inventors: David Askin, Kan K. Eng, Ralph P. Volante
  • Patent number: 5455258
    Abstract: Particularly the invention relates to the compounds of formula I ##STR1## (a) wherein Ar is carbocyclic or heterocyclic aryl;R is hydrogen, lower alkyl, carbocyclic aryl-lower alkyl, carbocyclic aryl, heterocyclic aryl, biaryl, biaryl-lower alkyl, heterocyclic aryl-lower alkyl, mono- or poly-halo-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, hydroxy-lower alkyl, acyloxy-lower alkyl, lower alkoxy-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, amino, mono- or di-lower alkylamino)-lower alkyl, acylamino-lower alkyl, (N-lower alkyl-piperazino or N-aryl-lower alkylpiperazino)-lower alkyl, or (morpholino, thiomorpholino, piperidino, pyrrolidino, piperidyl or N-lower alkylpiperidyl)-lower alkyl;R.sub.1 is hydrogen, lower alkyl, carbocyclic aryl-lower alkyl, carbocyclic aryl, heterocyclic aryl, biaryl, biaryl-lower alkyl, heterocyclic aryl-lower alkyl, mono- or poly-halo-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.3 -C.sub.
    Type: Grant
    Filed: January 6, 1993
    Date of Patent: October 3, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Lawrence J. MacPherson, David T. Parker
  • Patent number: 5449782
    Abstract: A compound represented by formula IAr.sub.1 --O--M--O--AR.sub.2 Iwherein Ar.sub.1 and Ar.sub.2 are independently substituted phenyl or substituted pyridinyl, the substituents on said phenyl or pyridinyl being independently selected from one, two or three of (C.sub.1 -C.sub.10)alkyl, (C.sub.1 -C.sub.10) alkoxy, halogen, carbamyl, (C.sub.1 -C.sub.10) alkoxycarbonyl, oxazoyl, and (C.sub.1 -C.sub.10) alkyl substituted by halogen, (C.sub.1 -C.sub.10) alkoxy, hydroxy, or (C.sub.1 -C.sub.10) alkoxycarbonyl; ##STR1## M is (C.sub.4 -C.sub.8) alkylene, (C.sub.4 -C.sub.8) alkenylene or(C.sub.4 -C.sub.8)-alkynylene;O is oxygen;or pharmaceutically acceptable salts thereof.as well as pharmaceutical compositions containing the compounds and methods of treating or preventing viral infections, especially picornaviral infections, are disclosed.
    Type: Grant
    Filed: August 8, 1994
    Date of Patent: September 12, 1995
    Assignee: Schering Corporation
    Inventors: Viyyoor M. Girijavallabhan, Ashit K. Ganguly, Richard W. Versace
  • Patent number: 5424325
    Abstract: Aminoketone derivatives according to the present invention strongly inhibit thiol protease such as calpain, papain, cathepsin B, cathepsin H, cathepsin L or the like and have excellent properties concerning absorbance on oral administration, tissue distribution and cell membrane permeability. The aminoketone derivatives cart thus be used as therapeutic agents for treating muscular dystrophy, cataract, cardiac infarction, stroke, Alzheimer's disease, amyotrophy, osteoporosis and hypercalcemia and so on. It may also be used as therapeutic agents for preventing metastasis of cancer. In addition, the present derivatives are also applicable as intermediates for the preparation of ketone derivatives, which have inhibitory activity against thiol protease.
    Type: Grant
    Filed: December 22, 1993
    Date of Patent: June 13, 1995
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Ryoichi Ando, Naoko Ando, Hirokazu Masuda, Toshiro Sasaki, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
  • Patent number: 5420145
    Abstract: Carboxylic acid derivatives having potent retinoid-type pharmacological activities are disclosed. The compounds disclosed are represented by the following formula: ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 independently represent a hydrogen atom or an alkyl group with the exception that all of R.sup.1, R.sup.2, and R.sup.3 do not simultaneously represent hydrogen atoms and R.sup.1 together with R.sup.2 optionally represent a cyclic structure formed by the combination thereof; R.sup.4 represents a hydrogen atom or an alkyl group; X represents a nitrogen atom or C--OH; and A represents --CO--NH-- or --NH--CO--.
    Type: Grant
    Filed: March 23, 1993
    Date of Patent: May 30, 1995
    Assignees: Koichi Shudo, Shionogi Pharmaceutical Co., Ltd.
    Inventor: Koichi Shudo
  • Patent number: 5416118
    Abstract: Novel bicyclic amides of the formula ##STR1## wherein Ar.sup.1 and Ar.sup.2 are phenyl, R.sup.2 -substituted phenyl, heteroaryl or R.sup.2 -substituted heteroaryl, wherein R.sup.2 is 1 to 3 substituents independently selected from the group consisting of halogeno, hydroxy, lower alkyl, lower alkoxy, nitro, amino, lower alkylamino and lower dialkylamino;X, Y and Z are --CH.sub.2 --, --CH(alkyl)--, --C(alkyl).sub.2 --, --NH--, --N(alkyl)--, --O-- or --SO.sub.r, wherein r is 0, 1 or 2, and m, n and p are 0 or 1;R.sup.1 is an alkyl chain of 1 to 25 carbon atoms; an alkyl chain substituted by one or more optionally substituted phenyl or heteroaryl groups; an alkyl chain --O--, --SO.sub.r, phenylene, R.sup.2 -substituted phenylene, heteroarylene or R.sup.
    Type: Grant
    Filed: September 28, 1993
    Date of Patent: May 16, 1995
    Assignee: Schering Corporation
    Inventors: John W. Clader, Thomas Fevig, Wayne Vaccaro, Joel G. Berger
  • Patent number: 5407902
    Abstract: A methoxyiminoacetic acid derivative represented by the following formula (I): ##STR1## wherein X represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 4 carbon atoms or an alkoxy group having 1 to 4 carbon atoms; A represents a methoxy group or a methylamino group; when A is a methoxy group, B represents --O--CO-- or --N=C(R.sup.1)-- and when A is a methylamino group, B represents --O--CR.sup.1 R.sup.2 --, wherein R.sup.1 and R.sup.2 independently represent a hydrogen atom, an alkyl group having 1 to 4 carbon atoms or a trifluoromethyl group; and Ar represents an optionally substituted aryl group or an optionally substituted heteroaryl group, and an agricultural/horticultural fungicide containing the same as an active ingredient.
    Type: Grant
    Filed: October 1, 1993
    Date of Patent: April 18, 1995
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Masatsugu Oda, Manabu Katsurada, Hirofumi Tomita
  • Patent number: 5387595
    Abstract: Substituted alicyclic compounds of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma.
    Type: Grant
    Filed: August 26, 1992
    Date of Patent: February 7, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Sander G. Mills, Paul E. Finke, Malcolm MacCoss, Daniel J. Miller, Dennis J. Underwood
  • Patent number: 5356914
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sub.1 represents a 1,2,5,6-tetrahydropyridin-3-yl group N-substituted by R.sub.10 wherein R.sub.10 represents OH; a group hydrolysable in vivo to OH or hydrogen; C.sub.1-8 alkoxy; C.sub.2-8 alkenyloxy; C.sub.2-8 alkynyloxy; C.sub.3-8 cycloalkyloxy; or COR.sub.13 wherein R.sub.13 represents hydrogen, C.sub.1-8 alkyl, phenyl or phenyl C.sub.1-4 alkyl; in which any phenyl moiety is optionally substituted by up to 3 substituents independently selected from C.sub.1-6 alkoxy, C.sub.1-6 alkyl, halo, C.sub.1-6 alkoxycarbonyl, cyano, C.sub.1-6 alkylthio or C.sub.1-6 alkylsulphonyl; enhance acetylcholine function via an action at muscarinic receptors within the central nervous system and are therefore of potential use in the treatment and/or prophylaxis of dementia in mammals.
    Type: Grant
    Filed: April 5, 1993
    Date of Patent: October 18, 1994
    Assignee: Beecham Group p.l.c.
    Inventors: Steven M. Bromidge, Barry S. Orlek, Steven Dabbs
  • Patent number: 5330737
    Abstract: The present invention relates particularly to novel aminothiol ligands that are suitable for complexing with a radionuclide, such as Tc, Re, or Ga, and are useful as general imaging agents for diagnostic purposes. The ligands have the general formulae (I) and (II): ##STR1## wherein for formula I, R.sup.1 -R.sup.4, R.sup.6, R.sup.7 and R.sup.9 -R.sup.14 can each be one of H, alkyl, aryl, hydroxyalkyl, alkoxycarbonyl, etc.; R.sup.5 and R.sup.8 are suitable sulfur protecting groups; m and n are 1-3; B can be one of C(O)CHR.sup.6 CHR.sup.7 SR.sup.8, CHR.sup.9 CHR.sup.10 C(O)NHR.sup.11, or C(O)CHR.sup.12 CHR.sup.13 NHR.sup.14 ;and wherein for formula II, R.sup.15 -R.sup.18, R.sup.20 and R.sup.21 are defined in the same manner as R.sup.1 above; D and E are either C(O) or CHR.sup.17 ; F is either (CH.sub.2).sub.d NR.sup.18 (CH.sub.2).sub.e SR.sup.19 or CHNR.sup.20 R.sup.21 (CH.sub.2).sub.f SR.sup.22 ; R.sup.19 and R.sup.22 are defined in the same manner as R.sup.5 above; d, e and f are 1-3.
    Type: Grant
    Filed: December 6, 1991
    Date of Patent: July 19, 1994
    Assignee: Mallinckrodt Medical, Inc.
    Inventor: Raghavan Rajagopalan
  • Patent number: 5326762
    Abstract: Amides of the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently heteroaryl, X-substituted heteroaryl, X-substituted phenyl, N-substituted triazinyl or N-substituted imidazolyl;and in addition, one of R.sub.1 and R.sub.2 can be as defined above and the other can be phenyl;R.sub.3 is an alkyl chain of 2 to 25 carbon atoms, saturated or unsaturated; an alkyl chain as defined substituted by one or more substituents selected from the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl; an alkyl chain as defined interrupted by one or more groups independently selected from the group consisting of --O--, --S--, --SO--, --SO.sub.2 --, --NH--, --N(lower alkyl)--, --C(O)--, phenylene, X-substituted phenylene, heteroarylene and X-substituted heteroarylene; or an interrupted alkyl chain as defined substituted by one or more substituents selected form the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl;R.sub.
    Type: Grant
    Filed: May 19, 1992
    Date of Patent: July 5, 1994
    Assignee: Schering Corporation
    Inventors: John Clader, Sundeep Dugar, Timothy Kogan, Bradley Tait, Wayne Vaccaro
  • Patent number: 5314918
    Abstract: This invention relates to alkanoic acid compounds having phenyl and heteroarylthio substituents which are useful as leukotriene antagonists, processes for the preparation thereof, and pharmaceutical compositions containing such compounds.This invention also relates to methods of treating diseases in which leukotrienes are a factor by administration of an effective amount of the above compounds or compositions.
    Type: Grant
    Filed: April 2, 1992
    Date of Patent: May 24, 1994
    Assignee: SmithKline Beecham Corporation
    Inventors: James S. Frazee, John G. Gleason, Ralph F. Hall
  • Patent number: 5300501
    Abstract: A compound of formula (I): ##STR1## wherein R represents a --CONHOH, carboxyl (--CO.sub.2 H) or esterified carboxyl group;X represents an amino (--NH.sub.2), or substituted amino, hydroxyl or substituted hydroxyl group; and their use as metalloproteinase inhibitors.
    Type: Grant
    Filed: July 29, 1992
    Date of Patent: April 5, 1994
    Assignee: Celltech Limited
    Inventors: John R. Porter, Thomas A. Millican, John R. Morphy, Nigel R. A. Beeley
  • Patent number: 5298514
    Abstract: The present invention relates to phenolic thioetheramides of the formula ##STR1## wherein R.sup.1 and R.sup.2 are tert-alkyl or phenyl, Alk.sup.1 and Alk.sup.2 are alkylene; X is sulfur or oxygen, m is 0, 1, or 2; and R is ##STR2## wherein R.sup.3 and R.sup.4 are hydrogen or alkyl and Alk.sup.3 is alkylene.
    Type: Grant
    Filed: September 10, 1992
    Date of Patent: March 29, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis