At 2-,6-, And 8-positions Patents (Class 544/266)
  • Publication number: 20150132280
    Abstract: A human dietary supplement comprises theacrine and optionally other compounds that modulate the effects of theacrine. Uses for the theacrine-containing supplement include improvement of at least one of mood, energy, focus, concentration or sexual desire or a reduction of at least one of anxiety or fatigue.
    Type: Application
    Filed: November 12, 2014
    Publication date: May 14, 2015
    Applicant: ORTHO-NUTRA, LLC
    Inventors: Hector L Lopez, Shawn Wells, Tim N. Ziegenfuss
  • Patent number: 8952167
    Abstract: A pseudorotaxane, a rotaxane and a catenane are provided. The pseudorotaxane includes at least a macrocyclic host molecule, a guest molecule, and a metal ion. The host molecule contains at least a binding unit and an aromatic linking spacer. The guest molecule has at least a recognition unit. The metal ion is used to template the threading of the guest molecule through the macrocycle host molecule by coordinating to a binding pocket formed from the binding unit of the macrocycle and the recognition moiety of the guest molecule. Rotaxanes or catenanes can be synthesized from the pseudorotaxane complexes, with or without the metal template ion in their molecular structures.
    Type: Grant
    Filed: May 24, 2013
    Date of Patent: February 10, 2015
    Assignee: National Taiwan University
    Inventors: Sheng-Hsien Chiu, You-Han Lin
  • Patent number: 8901136
    Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
    Type: Grant
    Filed: June 6, 2013
    Date of Patent: December 2, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Stephen Critchley, Courtney A. Cullis, Steven P. Langston, Hirotake Mitzutani, Edward J. Olhava, Stephane Peluso, Irache Visiers, Stepan Vyskocil, Gabriel S. Weatherhead
  • Publication number: 20120201754
    Abstract: Tracers targeting phosphodiesterase 1 for use in gamma radiation detection-based diagnostic techniques, particulaly gamma-emitter labeled tracers for SPECT and positron emitter-labeled compositions for PET are disclosed. Radio-labeled multiple novel scaffolds as PDE1 inhibitors such as substituted pyrazolo-pyrimidin-4-one derivatives, biomarkers for phosphodiesterase 1 [PDE1) in vivo, methods for developing novel therapies for PDE1-implicated conditions such as pulmonary arterial hypertension (PAH), Central Nervous System (CNS) and Cardiovascular (CV) disorders, and methods of detection and treatment are also disclosed.
    Type: Application
    Filed: October 7, 2010
    Publication date: August 9, 2012
    Inventors: Peng Li, Lawrence P. Wennogle, Jun Zhao, Hailin Zheng
  • Publication number: 20110212467
    Abstract: Evidence demonstrating that elevated expression of dUTPase protects breast cancer cells from the expansion of the intracellular uracil pool, translating to reduced growth inhibition following treatment with 5-FU is provided. The implementation of in silica drug development techniques to identify and develop small molecule inhibitors of dUTPase are reported. As 5-FU and the oral 5-FU pro-drug capecitabine remain central agents in the treatment of a variety of malignancies, the clinical utility of a small molecule inhibitor to dUTPase represents a viable strategy to improve the clinical efficacy of these mainstay chemotherapeutic agents.
    Type: Application
    Filed: August 27, 2009
    Publication date: September 1, 2011
    Applicant: UNIVERSITY OF SOUTHERN CALIFORNIA
    Inventors: Robert D. Ladner, Nouri Neamati
  • Patent number: 7875620
    Abstract: The present invention provides methods of treating microbacterial infections comprising administering to a subject in need thereof, a composition comprising a compound of formula I: wherein: X1, X2 and X3 are selected from the group consisting of oxygen, sulfur, aminoalkyl, alkoxy, aryl, and heteroaryl, unsubstituted or substituted; and R1, R2, R3 and R4 are selected from the group consisting of hydrogen, actinium, silicon, germanium, cyano, alkyl, alkoxy, allyl, alkenyl, alkynyl, alkylaryl, arylalkyl, aminoalkyl, alkylamino, alkene, alkyne, aryl, halide, alkylhalide, alkyloxyalkyl, thioalkyl, alkylthioalkyl, alkylamino, cycloalkyl, heterocyclyl, unsubstituted or substituted; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 30, 2006
    Date of Patent: January 25, 2011
    Assignee: Piper Medical, Inc.
    Inventor: Mark J. Warburton
  • Patent number: 7772226
    Abstract: The present invention is related to compounds represented by the following formula, or salts or hydrates thereof wherein, T1 represents a 4- to 12-membered heterocyclic group containing one or two nitrogen atoms in the ring, which is a monocyclic or bicyclic structure that may have one or more substituents; X represents a C1-6 alkyl group which may have one or more substituents, or such; Z1 and Z2 each independently represent a nitrogen atom or a group represented by the formula —CR2—; R1 and R2 independently represent a hydrogen atom, a C1-6 alkyl group which may have one or more substituents, or a C1-6 alkoxy group which may have one or more substituents, or such. These are novel compounds that exhibit an excellent DPPIV-inhibiting activity.
    Type: Grant
    Filed: August 28, 2008
    Date of Patent: August 10, 2010
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Seiji Yoshikawa, Eita Emori, Fumiyoshi Matsuura, Richard Clark, Hironori Ikuta, Kazunobu Kira, Nobuyuki Yasuda, Tadashi Nagakura, Kazuto Yamazaki
  • Publication number: 20100112090
    Abstract: [Purpose] The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. [Solution] The present invention provides nitrogen-containing fused ring derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, prodrugs, salts, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A and B are independently aryl or heteroaryl; RA and RB are independently halogen, cyano, alkyl, alkylsulfonyl, —OW1, —SW1, —COW2, —NW3W4, —SO2NW3W4, aryl, etc.; RC is H or alkyl; E is oxygen atom, etc.; U is single bond or alkylene; and X is Y, —CO—Y, —SO2—Y, —S-(alkylene)-Y, —O-(alkylene)-Y, —SO2-(alkylene)-Y, etc.; Y is Z or amino, etc.; and Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.
    Type: Application
    Filed: April 16, 2008
    Publication date: May 6, 2010
    Applicant: KISSEI PHARMACEUTICAL CO., LTD
    Inventors: Shigeru Yonekubo, Takashi Miyagi, Kohsuke Ohno, Mikie Kambara, Nobuhiko Fushimi
  • Publication number: 20090018148
    Abstract: The present invention concerns xanthine derivatives, having formula (I), processes for preparing them, pharmaccutical compositions containing them and their use as pharmaceuticals.
    Type: Application
    Filed: November 30, 2006
    Publication date: January 15, 2009
    Applicant: UCB PHARMA, S.A.
    Inventors: Florence Moureau, Benoit Kenda, Frank Driessens, Luc Quere
  • Patent number: 7427616
    Abstract: A compound of the Formula (I), wherein A together with the carbon atoms to which it is attached forms a fused 5-membered heteroaryl ring, wherein said heteroaryl ring contains 1 or 2 heteroatoms selected from O, N and S, and wherein the 5-membered ring containing G is linked to the ring formed by A in the meta position to the bridgehead carbon marked # in Formula (I): G is selected from O, S and NR5; Z is selected from N and CR6; Q1 is selected from optionally substituted aryl and heteroaryl, and the substituents R1 to R6 are as defined in the text for use in the production of an anti-angiogenic effect in a warm blooded animal such as man.
    Type: Grant
    Filed: August 1, 2003
    Date of Patent: September 23, 2008
    Assignee: AstraZeneca AB
    Inventors: Richard William Arthur Luke, Clifford David Jones, William McCoull, Barry Raymond Hayter
  • Patent number: 7307166
    Abstract: The invention relates to certain oxypurine nucleosides, congeners of such oxypurine nucleosides, and acyl derivatives thereof, and compositions which contain at least one of these compounds. The invention also relates to methods of treating or preventing hematopoietic disorders and modifying hematopoiesis, and treating or preventing inflammatory diseases and bacterial infections by administering a compound or composition of the present invention to an animal.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: December 11, 2007
    Assignee: Wellstat Therapeutics Corporation
    Inventors: Reid W. von Borstel, Michael K. Bamat, Bradley M. Hiltbrand, James C. Butler, Shyam Shirali
  • Patent number: 6723727
    Abstract: The present invention relates to compounds of the formulae I and Ia in which X, Y, W, Wa, G and Ga have the meanings given in the patent claims, and their physiologically tolerable salts and their prodrugs, their preparation, their use, in particular as pharmaceutical active compounds, and pharmaceutical preparations comprising them. The compounds of the formula I are vitronectin receptor antagonists and can be employed, for example, as inhibitors of bone resorption and for the treatment of osteoporosis.
    Type: Grant
    Filed: June 15, 2000
    Date of Patent: April 20, 2004
    Assignees: Hoechst Aktiengesellschaft, Genentech
    Inventors: Anuschirwan Peyman, Jochen Knolle, Volkmar Wehner, Gerhard Breipohl, Jean-Francois Gourvest, Denis Carniato, Thomas Richard Gadek
  • Publication number: 20030162699
    Abstract: Chiral peptide nucleic acids are provided which hybridise strongly with complementary nucleic acids and have potential as antigene and antisense agents and as tools in molecular biology.
    Type: Application
    Filed: October 30, 2001
    Publication date: August 28, 2003
    Inventor: Gordon Lowe
  • Publication number: 20030149059
    Abstract: Compounds provided herein are novel substituted tetrahydropurinones of Formula (I): 1
    Type: Application
    Filed: July 10, 2002
    Publication date: August 7, 2003
    Inventor: Richard A. Hartz
  • Patent number: 6600044
    Abstract: A process for the preparation of 1,3-oxathiolane nucleoside analogues in predominantly the cis-form, from mixture of cis-/trans-1,3-oxathiolane nucleosides or their protected derivatives thereof, comprising: (i) treatment of the cis-/trans-1,3-oxathiolane nucleosides (or protected derivatives thereof) with a pyrimidine base (or it derivatives thereof) and an acid, (ii) adding a suitable acid to the obtained cis-/trans-mixture of isomers, (iii) selective crystallization of the desired cis-isomer salt from a solvent or combination of solvents, and (iv) treatment of the predominantly cis-isomer salt with a suitable base to offer the free 1,3-oxathiolane nucleosides, and thereafter optionally repeating steps (i) to (iv) inclusive.
    Type: Grant
    Filed: June 18, 2001
    Date of Patent: July 29, 2003
    Assignee: Brantford Chemicals Inc.
    Inventors: K. S. Keshava Murthy, Gurijala V. Reddy, Zhi-xian Wang, Chandrawansha B. W. Senanayake
  • Patent number: 6518425
    Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.
    Type: Grant
    Filed: May 15, 2000
    Date of Patent: February 11, 2003
    Assignees: Emory University, Triangle Pharmaceuticals, Inc.
    Inventors: George R. Painter, Dennis C. Liotta, Merrick R. Almond, Darryl G. Cleary, Josè D. Soria, Marcos Sznaidman
  • Patent number: 6489344
    Abstract: New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.
    Type: Grant
    Filed: June 18, 1999
    Date of Patent: December 3, 2002
    Assignee: Chiron Corporation
    Inventors: John M. Nuss, Stephen D. Harrison, David B. Ring, Rustum S. Boyce, Sean P. Brown, Dane A. Goff, Kirk W. Johnson, Keith B. Pfister, Savithri Ramurthy, Paul A. Renhowe, Lynn Seely, Sharadha Subramanian, Allan S. Wagman, Xiaohui A. Zhou
  • Patent number: 6465650
    Abstract: The invention provides a processes for the preparation of a compound of Formula I, or a salt thereof wherein PG is a urethane- or trityl-type protective group; X is NH, O, or S; Y is CH2, O, or NH; and B′ is a base customary in nucleotide chemistry. The processes include reacting a compound of Formula (II) with a compound of Formula (III) a compound of Formula (V) B′—CH2—CO—R2  (V), a monohaloacetic acid derivative in a suitable solvent with an auxiliary base, or a compound of Formula (VII) B′—CH2—CO—R3  (VII), and converting the resulting compounds to that of Formula I.
    Type: Grant
    Filed: February 18, 2000
    Date of Patent: October 15, 2002
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Gerhard Breipohl, Eugen Uhlmann, Jochen Knolle
  • Patent number: 6333331
    Abstract: The present invention provides AGT inactivating compounds such as substituted O6-benzylguanines of the formula 7- or 9-substituted 8-aza-O6-benzylguanines, 7,8-disubstituted O6-benzylguanines, 7,9-disubstituted O6-benzylguanines, 4(6)-substituted 2-amino-5-nitro-6(4)-benzyloxypyrimidines, and 4(6)-substituted 2-amino-5-nitroso-6(4)-benzyloxypyrimidines, as well as pharmaceutical compositions comprising such compounds along with a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: June 15, 1999
    Date of Patent: December 25, 2001
    Assignees: The United States of America as represented by the Department of Health and Human Services, The Penn State Research Foundation, ARCH Development Corporation
    Inventors: Robert C. Moschel, Anthony E. Pegg, M. Eileen Dolan, Mi-Young Chae
  • Patent number: 6258809
    Abstract: Novel compounds and pharmaceutical compositions thereof, and methods of using same in treating anxiety, depression, and other psychiatric and neurological disorders. The novel compounds provided by this invention are those of the following formulae: wherein R1, R13, X, Y, Z, G and Q are as defined herein.
    Type: Grant
    Filed: March 3, 2000
    Date of Patent: July 10, 2001
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Parthasarathi Rajagopalan, Robert John Chorvat, Rajagopal Bakthavatchalam, James Peter Beck, Paul Joseph Gilligan, Richard Eric Olson
  • Patent number: 6175008
    Abstract: Disclosed are processes for preparing compounds of the formula (I) and pharmaceutically acceptable salts or esters thereof: wherein R2 is a purine or pyrimidine base or an analogue or derivative thereof; and Z is S, S═O or SO2. The invention also relates to intermediates of use in the preparation of these compounds.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: January 16, 2001
    Assignee: BioChem Pharma Inc.
    Inventors: Bernard Belleau, Tarek Mansour, Allan Tse, Colleen A. Evans, Haolun Jin, Boulos Zacharie, Nghe Nguyen-Ba
  • Patent number: 6166019
    Abstract: Compounds of Formula I and II and their pharmaceutically acceptable, salts, esters and prodrugs thereof are selective alpha-1D adrenoceptor anatagonists and may be useful for treating disease states.
    Type: Grant
    Filed: July 9, 1999
    Date of Patent: December 26, 2000
    Assignee: Abbott Laboratories
    Inventors: Michael D. Meyer, William A. Caroll
  • Patent number: 6143743
    Abstract: Corticotropin releasing factor (CRF) antagonists of formula (I): ##STR1## and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.
    Type: Grant
    Filed: July 2, 1998
    Date of Patent: November 7, 2000
    Assignee: Dupont Pharmaceuticals Company
    Inventors: Richard Gerald Wilde, Rajagopal Bakthavatchalam, James Peter Beck, Argyrios Georgious Arvanitis
  • Patent number: 6103707
    Abstract: The present invention relates to 9-(2-deoxy-2-fluoro-4-thio-beta-D-arabinofuranosyl)purine derivatives having antiviral activity, represented by formula [I]: ##STR1## wherein B represents a base selected from the group consisting of purine, azapurine and deazapurine, which may be substituted with halogen, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, alkylamino, hydroxyl, hydroxyamino, aminoxy, alkoxy, mercapto, alkylmercapto, aryl, aryloxy or cyano; and R represents a hydrogen atom or a phosphoric acid residue, and to a process for the production and use thereof.
    Type: Grant
    Filed: June 29, 1998
    Date of Patent: August 15, 2000
    Assignee: Yamasa Corporation
    Inventors: Kohei Yamada, Yuichi Yoshimura, Haruhiko Machida, Mikari Watanabe
  • Patent number: 6075143
    Abstract: There are described N-ethylglycine derivatives of the formula I ##STR1## in which PG is a urethane-type or trityl-type amino protective group which is labile to weak acids, X is NH, O or S, Y is CH.sub.2, NH or O, and B' are bases customary in nucleotide chemistry, the exocyclic amino or hydroxyl groups of which being protected by suitable, known protective groups, or are base substitute compounds, and their salts with tert-organic bases, as well as a process for their preparation. The N-ethylglycine derivatives of the formula I are used in the preparation of PNA and PNA/DNA hybrids.
    Type: Grant
    Filed: March 13, 1995
    Date of Patent: June 13, 2000
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerhard Breipohl, Eugen Uhlmann, Jochen Knolle
  • Patent number: 6046207
    Abstract: The present invention relates to a compound of the formula and the pharmaceutically acceptable salts thereof wherein W is a bicyclic heterocyclic ring system. The compounds are .alpha.-1 adrenergic antagonists and are useful in the treatment of BPH; also disclosed are .alpha.-1 antagonist compositions and a method for antagonizing .alpha.-1 adrenoreceptors and treating BPH.
    Type: Grant
    Filed: November 26, 1997
    Date of Patent: April 4, 2000
    Inventors: Michael D. Meyer, Robert J. Altenbach, Fatima Z. Basha, William A. Carroll, Irene Drizin, James F. Kerwin, Jr., Michael D. Wendt, Anthony R. Haight, Weijiang Zhang
  • Patent number: 6004966
    Abstract: The use of a compound of formula I ##STR1## in which R.sub.1 and R.sub.2 are N, X.sub.1 and X.sub.2 which may be the same or different are hydrogen, hydroxy, or an optionally substituted alkyl, and Z.sub.1 and Z.sub.2 which may be the same or different are hydrogen, hydroxy, keto (.dbd.O), or one of Z.sub.1 and X.sub.1 and Z.sub.2 and X.sub.2 form a second bond of a double bond at the 1,6 or 2,3 positions with the proviso that at least one of the groupings R.sub.1 Z.sub.1 X.sub.1 R.sub.2 Z.sub.2 X.sub.2 and R.sub.1 X.sub.1 Z.sub.2 form a hydroxamate moiety (--N(OH)C(.dbd.O)-- in which R.sub.1 and R.sub.2 is N, Z.sub.1 and/or Z.sub.2 is .dbd.O and X.sub.1 and/or X.sub.2 is OH or R.sub.1 is N, Z.sub.2 is .dbd.O and X.sub.1 is OH and B is a 5 or 6 membered ring of formula II or III ##STR2## in which R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, and R.sub.
    Type: Grant
    Filed: June 9, 1997
    Date of Patent: December 21, 1999
    Assignee: BTG International Limited
    Inventors: Surinder Singh, Anthony Edward Lewis
  • Patent number: 6001844
    Abstract: Compounds of structural Formula (I) ##STR1## and pharmacologically acceptable salts and esters thereof possess 5.alpha.-reductase inhibitory activity. These compounds inhibit 5.alpha.-reductase type 1 and type 2. The compounds of structural Formula I are useful in the systemic, including oral, and parenteral, including topical, treatment and prevention of hyperandrogenic conditions including prostatic carcinoma, benign prostatic hyperplasia, acne vulgaris, seborrhea, androgenic alopecia (also called androgenetic alopecia) which includes male- and female-pattern baldness, female hirsutism, and prostatitis. A class of compounds of the present invention are also potent antiandrogens. The present invention also relates to novel compositions containing such compounds, methods of their use and methods of their manufacture.
    Type: Grant
    Filed: March 11, 1998
    Date of Patent: December 14, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Raman K. Bakshi, Soumya P Sahoo, Richard L. Tolman
  • Patent number: 5998456
    Abstract: Benzimidazole compounds represented by the formula set out below and analogs thereof, wherein Y represents a single bond or sulfur atom; Z represents oxygen atom, sulfur atom, or N--R.sup.4 ; R.sup.1 and R.sup.2 independently represent hydrogen, a halogen atom, alkyl group or other; R.sup.1 and R.sup.4 independently represent hydrogen, alkyl group, acyl group or other; n and m independently represent an integer of 1, 2, or 3; and L represents a linking group such as C.sub.2-12 alkylene group or an alkylene group containing one or more phenylene groups or ether groups. The compounds are useful as an active ingredient of a medicament such as a preventive and therapeutic medicament for hyperlipemia or arterial sclerosis.
    Type: Grant
    Filed: January 16, 1998
    Date of Patent: December 7, 1999
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Kozo Aoki, Kazuhiro Aikawa
  • Patent number: 5994361
    Abstract: The present invention comprises a compound of formula I: ##STR1## R.sub.1 of Formula I is substituted amino represented by formula NR.sup.5 R.sup.6 wherein R.sup.5 and R.sup.6 are independently selected from the group consisting of hydrogen, C.sub.1-4 alkyl, and unsubstituted amino with the proviso that R.sup.5 and R.sup.6 are not both hydrogen, and further that R.sup.5 and R.sup.6 are not both amino. R.sub.2 and R.sub.3 of Formula I are independently selected from the group consisting of hydrogen; C.sub.1-4 alkyl; amino; substituted or unsubstituted thiol; and halogen. Moreover, R.sub.4 of Formula I is represented by the formula R.sup.12 -X.sup.12 wherein R.sup.12 is a saturated or unsaturated linear hydrocarbon chain of 5-20 carbons optionally containing one or more interruptions within the chain by a heteroatom, and optionally substituted with one or more .dbd.O, or .dbd.S. Finally, X.sup.12 is selected from the group consisting of hydroxy, an aminoalkyl group, and a known amino acid bound by its .alpha.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: November 30, 1999
    Assignee: Biochem Pharma
    Inventors: Christopher Penney, Boulos Zacharie, Lyne Gagnon, Giorgio Attardo, Timothy P. Connolly, Yves St-Denis, Salam Kadhim
  • Patent number: 5958932
    Abstract: The present invention provides AGT inactivating compounds such as substituted O.sup.6 -benzylguanines of the formula ##STR1## wherein, for example, R.sub.1 is amino, hydroxy, or alkylamino, R.sub.2 is aminoalkyl, hydroxyalkyl, or alkylaminoalkyl, and R.sub.3 is halo, hydroxyalkyl, thiol or alkylthio, as well as pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The present invention further provides a method of enhancing the chemotherapeutic treatment of tumor cells in a mammal with an antineoplastic alkylating agent which causes cytotoxic lesions at the O.sup.6 -position of guanine comprising administering to a mammal an effective amount of one of the aforesaid compounds and administering to the mammal an effective amount of an antineoplastic alkylating agent which causes cytotoxic lesions at the O.sup.6 -position of guanine.
    Type: Grant
    Filed: April 28, 1997
    Date of Patent: September 28, 1999
    Assignees: The United States of America as represented by the Secretary of the Department of Health and Human Services, Arch Development Corporation, Penn State Research Foundation
    Inventors: Robert C. Moschel, Anthony E. Pegg, M. Eileen Dolan, Mi-Young Chae
  • Patent number: 5916894
    Abstract: The present invention provides 8-substituted O.sup.6 -benzylguanine derivatives which have been found to be effective AGT inactivators, as well as pharmaceutical compositions comprising such derivatives along with a pharmaceutically acceptable carrier. Thus, for example, the present invention provides a compound of the formula ##STR1## wherein R.sub.1 is a substituent selected from the group consisting of amino, hydroxy, C.sub.1 -C.sub.4 alkylamino, C.sub.1 -C.sub.4 dialkylamino, and C.sub.1 -C.sub.4 acylamino, R.sub.2 is a substituent selected from the group consisting of C.sub.1 -C.sub.4 aminoalkyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 dialkylamino alkyl, and C.sub.1 -C.sub.4 pivaloylalkyl, and R.sub.3 is a C.sub.1 -C.sub.4 alkyl. The present invention further provides a method of enhancing the chemotherapeutic treatment of tumor cells in a mammal with an antineoplastic alkylating agent which causes cytotoxic lessons at the O.sup.
    Type: Grant
    Filed: September 11, 1997
    Date of Patent: June 29, 1999
    Assignees: The United States of America as represented by the Department of Health and Human Services, The Penn State Research Foundation, Arch Development Corporation
    Inventors: Robert C. Moschel, Anthony E. Pegg, M. Eileen Dolan, Mi-Young Chae
  • Patent number: 5840729
    Abstract: A method of attenuating a cognitive deficit in a patient in need thereof comprising administering to the patient a xanthine derivative.
    Type: Grant
    Filed: December 18, 1995
    Date of Patent: November 24, 1998
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Janice M. Hitchcock, Stephen M. Sorensen, Mark W. Dudley, Norton P. Peet
  • Patent number: 5807854
    Abstract: Compounds of general formula I and their salts and solvates are antifungal agents and as such are useful in the treatment of various fungal infections. Pharmaceutical compositions including these compounds and processes for their preparation are also provided.
    Type: Grant
    Filed: March 31, 1997
    Date of Patent: September 15, 1998
    Assignee: J. Uriah & Cia. S.A.
    Inventors: Javier Bartroli, Enric Turmo, Manuel Anguita
  • Patent number: 5674998
    Abstract: This invention relates to adenosine kinase inhibitors and to nucleoside analogs, C-4' modified pyrrolo?2,3-d!pyrimidine and pyrazolo?3,4-d!pyrimidine nucleoside analogs having activity as adenosine kinase inhibitors. The invention relates to nucleoside analogs of this kind, having zero substitutions or two substitutions at the C-4' position of the furanose (sugar) moiety. The invention also relates to the preparation and use of these adenosine kinase inhibitors in the treatment of cardiovascular, and cerebrovascular diseases, inflammation and other diseases which can be regulated by increasing the local concentration of adenosine.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 7, 1997
    Assignee: Gensia Inc.
    Inventors: Serge H. Boyer, Mark D. Erion, Bheemarao G. Ugarkar
  • Patent number: 5538978
    Abstract: This invention relates to novel purine nucleoside phosphorylase inhibitors, to the methods and intermediates for their preparation and to their use as immuno-suppressants, antilymphoma, antileukemic, antiviral and antiprotozoal agents.
    Type: Grant
    Filed: November 8, 1994
    Date of Patent: July 23, 1996
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Serge Halazy, Charles Danzin
  • Patent number: 5527803
    Abstract: This invention relates to novel purine nucleoside phosphorylase inhibitors, to the methods and intermediates for their preparation and to their use as immuno-suppressants, antilymphoma, antileukemic, antiviral and antiprotozoal agents.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: June 18, 1996
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Serge Halazy, Charles Danzin
  • Patent number: 5525606
    Abstract: The present invention provides 8-substituted O.sup.6 -benzylguanines of the formula ##STR1## wherein R.sub.1, R.sub.2, and R.sub.3 are as defined in the specification, and 4(6)-substituted 2-amino-5-nitro-6(4)-benzyloxypyrimidine, and 4(6)-substituted 2-amino-5-nitroso-6(4)-benzyloxypyrimidine derivatives which have been found to be effective AGT inactivators, as well as pharmaceutical compositions comprising such derivatives along with a pharmaceutically acceptable carrier. The present invention further provides a method of enhancing the chemotherapeutic treatment of tumor cells in a mammal with an antineoplastic alkylating agent which causes cytotoxic lesions at the O.sup.6 -position of guanine, by administering to a mammal an effective amount of one of the aforesaid derivatives, 2,4-diamino-6-benzyloxy-s-triazine, 5-substituted 2,4-diamino-6-benzyloxypyrimidines, or 8-aza-O.sup.
    Type: Grant
    Filed: August 1, 1994
    Date of Patent: June 11, 1996
    Assignees: The United States of America as represented by the Department of Health and Human Services, ARCH Development Corporation, Penn State Research Foundation, Inc.
    Inventors: Robert C. Moschel, Anthony E. Pegg, M. Eileen Dolan, Mi-Young Chae
  • Patent number: 5516903
    Abstract: The protected cyclobutanone of the formula ##STR1## is treated with a dialkylaluminum chloride, an alkylaluminum dichloride, a trialkylaluminum compound, hydrogen in the presence of the catalysts ruthenium black or ruthenium on alumina, diphenyl-silane in the presence of tris(triphenylphosphine) rhodium (I) chloride, or iridium tetrachloride to yield the corresponding diprotected cyclobutanol. This compound is useful as an intermediate in the preparation of antiviral agents.
    Type: Grant
    Filed: November 4, 1994
    Date of Patent: May 14, 1996
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Janak Singh, Gregory S. Bisacchi, Richard H. Mueller
  • Patent number: 5506347
    Abstract: Novel lyxose derivatives which selectively inhibit adenosine kinase and methods of preparing these compounds are provided. These compounds are useful in treating certain conditions in vivo which may be ameliorated by increased local concentrations of adenosine.
    Type: Grant
    Filed: February 3, 1994
    Date of Patent: April 9, 1996
    Assignee: Gensia, Inc.
    Inventors: Mark D. Erion, Bheemarao G. Ugarkar, Angelo J. Castellino
  • Patent number: 5393883
    Abstract: The present invention relates to novel ribonucleotide reductase inhibitors and new combinations comprising an antiviral compound, such as acyclovir, and a thiocarbonohydrazone ribonucleotide reductase inhibitor for the chemotherapeutic treatment of virus infections, especially viruses of the herpes group.
    Type: Grant
    Filed: February 7, 1992
    Date of Patent: February 28, 1995
    Assignee: Burroughs Wellcome Co.
    Inventors: Todd A. Blumenhopf, Thomas Spector, Devron R. Averett, Robert W. Morrison, Jr., Eric C. Bigham, Virgil L. Styles
  • Patent number: 5332814
    Abstract: Process for the preparation of racemic compounds of the formula I ##STR1## or enantiomers thereof, in which B is the radical of a nucleic base from the series comprising purine, a purine analogue or a pyridine analogue, and R is H or a protective group R.sub.1, by reactinga) a compound of the formula II or enantiomer thereof ##STR2## with a compound of the formulae X--CO--X, X--CS--X, X--SO--X, X--SO.sub.2 --X, R.sub.2 --NCO, R.sub.3 R.sub.4 N--C(O)--R.sub.5, X.sub.2 P--R.sub.6 or X.sub.2 P(O)--R.sub.6, in which X is a leaving group, R.sub.2 is, for example, C.sub.1 -C.sub.18 alkyl, R.sub.3 and R.sub.4 are, for example, H or C.sub.1 -C.sub.18 alkyl, R.sub.5 is, for example, H or C.sub.1 -C.sub.12 alkyl, and R.sub.6 is, for example, C.sub.1 -C.sub.12 alkyl or C.sub.1 -C.sub.12 alkoxy, to give a compound of the formula III or enantiomers thereof ##STR3## in which Y is the groups --C(O)--, --C(S)--, --SO--, --SO.sub.2 --, R.sub.2 NH--CH.dbd., R.sub.3 R.sub.4 N--CR.sub.5 .dbd., R.sub.6 P.dbd. and R.sub.6 (O)P.
    Type: Grant
    Filed: October 30, 1992
    Date of Patent: July 26, 1994
    Assignee: Ciba-Geigy Corporation
    Inventor: Heinz Moser
  • Patent number: 5332744
    Abstract: Substituted Imidazo-fused 6-membered heterocycles of structural formula: ##STR1## wherein A, B, C, and D are independently carbon atoms or nitrogen atoms are angiotensin II antagonists useful in the treatment of hypertension and congestive heart failure.
    Type: Grant
    Filed: May 4, 1990
    Date of Patent: July 26, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Prasun K. Chakravarty, William J. Greenlee, Nathan B. Mantlo, Arthur A. Patchett, Thomas F. Walsh
  • Patent number: 5208240
    Abstract: The present invention relates to certain novel 8-substituted purines as selective A.sub.1 -adenosine receptor antagonists which are useful in the treatment of patients suffering from Alzheimer's disease, congestive heart failure or pulmonary bronchoconstriction.
    Type: Grant
    Filed: March 12, 1991
    Date of Patent: May 4, 1993
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Norton P. Peet, Nelsen L. Lentz, Mark W. Dudley
  • Patent number: 5177074
    Abstract: There are disclosed substituted thiophene and furan derivatives of Formula I which are useful as angiotensin II antagonists.
    Type: Grant
    Filed: March 11, 1992
    Date of Patent: January 5, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Eric E. Allen, Ralph A. Rivero, Nancy Kevin
  • Patent number: 5171353
    Abstract: Sulfonamides of the general formula I ##STR1## where R.sup.1 is hydrogen of C.sub.1 -C.sub.4 -alkyl,R.sup.2 is hydrogen or substituted or unsubstituted C.sub.1 -C.sub.6 -alkyl; C.sub.3 -C.sub.4 -alkenyl; C.sub.3 -C.sub.4 -alkynyl or substituted or unsubstituted saturated or singly unsaturated 5- to 7- membered heteroaryl;R.sup.3 and R.sup.4 are halogen; substituted or unsubstituted C.sub.1 -C.sub.4 -alkoxy C.sub.1 -C.sub.4 -alkylthio, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkenyloxy, C.sub.2 -C.sub.6 -alkenylthio, C.sub.2 -C.sub.6 -alkynyl, C.sub.2 -C.sub.6 -alkynyloxy, C.sub.2 -C.sub.6 -alkynylthio, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -cycloalkylthio, C.sub.5 -C.sub.6 -cycloalkenyl, C.sub.3 -C.sub.6 -cycloalkoxy, C.sub.5 -C.sub.6 -cycloalkenyloxy, C.sub.5 -C.sub.6 -cycloalkenylthio, phenyl, phenoxy, phenylthio, benzyl, benzyloxy or benzylthio;the group given for R.sup.2, or NR.sup.7 R.sup.8, where R.sup.7 and R.sup.8 are hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.
    Type: Grant
    Filed: May 9, 1990
    Date of Patent: December 15, 1992
    Assignee: BASF Akteingesellschaft
    Inventors: Klaus Fischer, Horst Mayer, Klaus Ditrich, Gerhard Hamprecht, Bruno Wuerzer, Karl-Otto Westphalen
  • Patent number: 5158954
    Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein K is oxygen or sulphur; Z is optionally substituted aryl or optionally substituted heteroaryl; X is O, S(O).sub.n, NR.sup.4, CR.sup.1 R.sup.2, CHR.sup.5, CO, CR.sup.1 (OR.sup.2), C.dbd.CR.sup.1 R.sup.2, CHR.sup.1 CHR.sup.2, CR.sup.1 .dbd.CR.sup.2, CHR.sup.1 CR.sup.2 .dbd.CH, C.dbd.C, OCHR.sup.1, CHR.sup.1 O, OCHR.sup.1 O, S(O).sub.n CHR.sup.1, S(O).sub.n CHR.sup.1 O, CHR.sup.1 S(O).sub.n, CHR.sup.1 OSO.sub.2, NR.sup.4 CHR.sup.1, CHR.sup.1 NR.sup.4, CO.sub.2, O.sub.2 C, SO.sub.2 O, OSO.sub.2, CO.CO, COCHR.sup.1, COCHR.sup.1 O, CHR.sup.1 CO, CHOH.CHR.sup.1, CHR.sup.1.CHOH, ##STR2## CONR.sup.4, OCONR.sup.4, NR.sup.4 CO, CSNR.sup.4, OCS.NR.sup.4, SCO.NR.sup.4, NR.sup.4 CO.sub.2, NR.sup.4 CS, NR.sup.4 CSO, NR.sup.4 COS, NR.sup.4 CONR.sup.4, S(O).sub.n NR.sup.4, NR.sup.4 S(O).sub.n, CS.sub.2, S.sub.2 C, CO.S, SCO, N.dbd.N, N.dbd.CR.sup.1, CR.sup.1 .dbd.N, CHR.sup.1 CHR.sup.2 CH(OH), CHR.sup.1 OCO, CHR.sup.1 SCO, CHR.sup.1 NR.sup.
    Type: Grant
    Filed: October 15, 1990
    Date of Patent: October 27, 1992
    Assignee: Imperial Chemical Industries PLC
    Inventors: John M. Clough, Christopher R. A. Godfrey, Stephen P. Heaney, Kenneth Anderton
  • Patent number: 5157026
    Abstract: Substituted Imidazo-fused 6-membered heterocycles of structural formula: ##STR1## wherein A, B, C, and D are independently carbon atoms or nitrogen atoms are angiotensin II antagonists useful in the treatment of hypertension and congestive heart failure.
    Type: Grant
    Filed: February 24, 1992
    Date of Patent: October 20, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Prasun K. Chakravarty, William J. Greenlee, Nathan B. Mantlo, Arthur A. Patchett, Thomas F. Walsh
  • Patent number: RE39056
    Abstract: Compounds of structural Formula (I) and pharmacologically acceptable salts and esters thereof possess 5?-reductase inhibitory activity. These compounds inhibit 5?-reductase type 1 and type 2. The compounds of structural Formula I are useful in the systemic, including oral, and parenteral, including topical, treatment and prevention of hyperandrogenic conditions including prostatic carcinoma, benign prostatic hyperplasia, acne vulgaris, seborrhea, androgenic alopecia (also called androgenetic alopecia) which includes male- and female-pattern baldness, female hirsutism, and prostatitis. A class of compounds of the present invention are also potent antiandrogens. The present invention also relates to novel compositions containing such compounds, methods of their use and methods of their manufacture.
    Type: Grant
    Filed: September 11, 1996
    Date of Patent: April 4, 2006
    Assignee: Merck & Co, Inc.
    Inventors: Raman K. Bakshi, Soumya P. Sahoo, Richard L. Tolman
  • Patent number: RE34201
    Abstract: This invention pertains to novel substituted N/aryl-N-[4-(1-heterocyclicalkyl)piperidinyl]amides useful as analgesics, and methods of administering analgesia, which comprises the systemic administration to mammals of such compounds, and pharmaceutical compositions containing such compounds, wherein the novel compounds have the general formula: ##STR1## including optically active isomeric forms, and the pharmaceutically acceptable acid addition salts thereof, wherein R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are defined in the disclosure.
    Type: Grant
    Filed: April 14, 1992
    Date of Patent: March 23, 1993
    Assignee: Anaquest, Inc.
    Inventors: Jerome R. Bagley, Nhora L. Lalinde, Bao-Shan Huang, H. Kenneth Spencer