Plural Nitrogens In The Heterocyclic Ring Patents (Class 540/545)
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Patent number: 6852714Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein Alk1 is C1-6alkanediyl optionally substituted with hydroxy, C1-4alkyloxy or C1-4alkylcarbonyloxy; -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical; R4 is hydrogen or C1-6alkyl; A is a bivalent radical of formula —NR6-Alk2-(b-1), or -Npiperidinyl-(CH2)m (b-2) wherein m is 0 or 1; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hType: GrantFiled: September 5, 2002Date of Patent: February 8, 2005Assignee: Janssen Pharmaceutica N.V.Inventors: Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren, Marc Francis Josephine Schroven, Marcel Frans Leopold De Bruyn
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Patent number: 6844347Abstract: The invention relates to compounds of formula I, in which R1, R2, R3 and R4 have the meanings given in the claims. Said compounds are valuable active ingredients for the treatment and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, heart failure, thrombosis or atherosclerosis. The compounds of the formula I are able to modulate the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the treatment and prophylaxis of disorders associated with impaired cGMP balance. The invention furthermore relates to methods for producing compounds of the formula I, their use in the treatment and prophylaxis of the above diseases and in the preparation of medicaments for such diseases, and pharmaceutical preparations containing the compounds of formula I.Type: GrantFiled: August 4, 1999Date of Patent: January 18, 2005Assignee: Aventis Pharma Deutschland GmbHInventors: Ursula Schnidler, Karl Schoenafinger, Hartmut Strobel
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Publication number: 20040254161Abstract: Compounds of formula (I): 1Type: ApplicationFiled: June 10, 2004Publication date: December 16, 2004Inventors: Patrice Desos, Alex Cordi, Pierre Lestage
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Publication number: 20040248877Abstract: Compounds of Formula 8 are provided: 1Type: ApplicationFiled: April 30, 2004Publication date: December 9, 2004Inventors: Sandeep Gupta, David Michael Carrig, Raghavan Rajagopalan, Prabhavathi Fernandes
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Patent number: 6806266Abstract: The present invention provides an antitumor agent comprising a staurosporin derivative or a pharmaceutically acceptable salt thereof, as an active ingredient, which is represented by the general formula (I): wherein R1 represents hydrogen, hydroxy or lower alkoxy, R2 and R3 are the same or different and represent hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted lower alkenyl, substituted or unsubstituted lower alkynyl, substituted or unsubstituted aryl, a substituted or unsubstituted heterocyclic group, halogen, nitro, formyl, etc., R4 represents hydrogen, etc., R5 represents NR11AR12A (wherein R11A and R12A represent hydrogen, substituted or unsubstituted lower alkyl, etc.), provided that R2 and R3 are not simultaneously hydrogen.Type: GrantFiled: January 11, 2002Date of Patent: October 19, 2004Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Fumihiko Kanai, Nobuyoshi Amishiro, Yushi Kitamura, Chikara Murakata, Tadakazu Akiyama, Shiro Akinaga, Eiichi Fuse, Takashi Kuwabara, Kenichi Yasoshima
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Patent number: 6723844Abstract: The present invention provides a process for the synthesis of K-252a and intermediates useful in the process.Type: GrantFiled: February 27, 2003Date of Patent: April 20, 2004Assignee: Abbott LaboratoriesInventors: Navayath Shobana, John C. Strong, Mark W. Tubergen, Russell A. Brierley
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Patent number: 6677450Abstract: The present invention relates to novel N12, N13-bridged sugar derivatives of indolylopyrrolocarbazoles and pharmaceutical formulations thereof which exhibit topoisomerase-I activity and are useful in inhibiting the proliferation of tumor cells.Type: GrantFiled: September 27, 2001Date of Patent: January 13, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Mark G. Saulnier, Edward H. Ruediger, Neelakantan Balasubramanian, Mikael Mahler, Francis Beaulieu, Carol Bachand, David B. Frennesson
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Patent number: 6660729Abstract: A non-aqueous, particle-forming, fused pyrrolocarbazole-containing composition is disclosed. Upon contact with an aqueous medium, the particle-forming composition spontaneously disperses into suspended particles, thereby forming a stable suspension that provides greatly improved bioavailability of orally administered fused pyrrolocarbazole compounds.Type: GrantFiled: October 27, 2000Date of Patent: December 9, 2003Assignee: Cephalon, Inc.Inventors: David A. Dickason, Piyush R. Patel, Vincent Corvari, Efraim Shek, Joseph L. Herman, Jeffry M. Skell
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Publication number: 20030212057Abstract: The present invention relates to substituted piperidines of general formula 1Type: ApplicationFiled: November 7, 2002Publication date: November 13, 2003Inventors: Klaus Rudolf, Henri Doods, Eckhart Bauer, Rudolf Hurnaus, Wolfgang Eberlein, Alexander Dreyer, Stephan Georg Mueller
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Publication number: 20030203891Abstract: Novel pesticides of formula (I) 1Type: ApplicationFiled: January 21, 2003Publication date: October 30, 2003Inventors: Thomas Goebel, Eliane Humbert-Droz, Maurizio Schwarzenbach
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Patent number: 6635637Abstract: Cyclic oxyguanidine compounds, including compounds of Formulae I and II: wherein R1, R3-R6, R21-R26, L, Y, Z, and A are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formulae I and II. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: August 2, 2001Date of Patent: October 21, 2003Assignee: Dimensional Pharmaceuticals, Inc.Inventors: Aihua Wang, Tianbao Lu, Bruce Edward Tomczuk, Richard M. Soll, John Curtis Spurlino, Roger Francis Bone
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Patent number: 6624157Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formulas and their enantiomers, diastereomers, and their pharmaceutically acceptable salts, including prodrugs and solvates thereof wherein: r, s and t are 0 or 1; m=0, 1, 2; p is 0, 1 or 2; X is selected from the group consisting of oxygen, hydrogen or R1, R2, R3; Y is selected from the group consisting of CHR9, SO2, CO, CO2, O, NR10, SO2NR11 and CONR12; R6, R7, R9, R10, R11, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, R25, R26, R27, and R28 are selected from the group consisting of hydrogen, lower alkyl or substituted alkyl; R4, R5 are selected from the group consisting of hydrogen, halo, nitro, cyano and U-R13; R12 is selected from the group consisting of hydrogen, lower alkyl, aryl, substituted alkyl or aryl; U is selected from the group consisting of sulfur, oxygen, NR14, CO, SO, SO2, CO2, NR15CO2, NR16CONR17, NR19SO2, NR19SO2NR20, SO2NR2Type: GrantFiled: January 26, 2001Date of Patent: September 23, 2003Assignee: Bristol-Myers Squibb CompanyInventor: Charles Z. Ding
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Publication number: 20030087892Abstract: This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V1 and V2 are both H, OMe or F, or one of V1 and V2 is Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N3, NH2, NHBn or NH-acyl and the other is H, or V1 and V2 together are ═O, —O(CH2)pO— or —S(CH2)pS—; W1 is either O or S; X1 and X2 are both H, or together are ═O or ═S; Y is OR5 or NR6R7; R1, R2, R3 and R4 are independently selected from H, lower alkyl, lower alkyloxy, F, Cl and Br; R5 is selected from H and lower alkyl; R6 and R7 are independently selected from H and lower alkyl, or together are —(CH2)n; n=3, 4, 5, 6; and p is 2 or 3. The compounds are agonists at the vasopressin V2 receptor and are useful as antidiuretics and procoagulants.Type: ApplicationFiled: May 23, 2002Publication date: May 8, 2003Inventors: Doreen Mary Ashworth, Gary Robert William Pitt, Peter Hudson, Chritpoher Martyn Yea, Richard Jeremy Franklin
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Patent number: 6552187Abstract: A process for the preparation of compounds of formula (I), which process comprises reacting a compound of formula (II), in an inert organic solvent, optionally in the presence of a base, with a compound of formula (IV), (IVa) or (IVb), and optionally converting the resulting compound of formula (I) wherein G is a metal ion equivalent or an ammonium cation, by salt conversion into the corresponding salt of formula (I) wherein G is a sulfonium or phosphonium cation, or by treatment with a Brönsted acid into the corresponding compound of formula (I) wherein G is hydrogen, and ‘in situ’ conversion of compounds of formula (I) with an electrophile of formula (XII) or (XIId) G0—L (XII) or R32—N═C═X3 (XIId), optionally in the presence of an acid-binding agent or a catalyst, to the compounds of formula (Ia).Type: GrantFiled: November 29, 2001Date of Patent: April 22, 2003Assignee: Syngenta Crop Protection, Inc.Inventors: Thomas Maetzke, René Mutti, Henry Szczepanski
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Patent number: 6509334Abstract: This invention provides compounds of Formula (I): wherein R1 and R2 may be single substituents or fused to form spirocyclic or hetero-spirocyclic rings; R3 is H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, or substituted alkynyl, CORC; RC is H, C1 to C3 alkyl, substituted C1 to C3 alkyl, aryl, substituted aryl, C1 to C3 alkoxy, substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; R4 is H, halogen, CN, NO2, C1 to C6 alkyl, substituted C1 to C6 alkyl, alkynyl, or substituted alkynyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, amino, C1 to C6 aminoalkyl, or substituted C1 to C6 aminoalkyl; and R5 is selected from a trisubstituted benzene ring of a five or six membered ring with 1, 2, or 3 heteroatoms from the group including O, S, SO, SO2 or NR6 and containing one or two independent substituents from the group including H, halogen, CN, N02, amino, and C1 to C3 alkyl, C1 to C3 alkoxy, C1 to C3 aType: GrantFiled: April 19, 2000Date of Patent: January 21, 2003Assignees: American Home Products Corporation, Ligand Pharmaceuticals, Inc.Inventors: Puwen Zhang, Eugene A. Terefenko, Andrew Fensome, Jay E. Wrobel, Horace Fletcher, III, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Publication number: 20030013874Abstract: A compound of the having the general formula (I) or general formula (II): 1Type: ApplicationFiled: April 18, 2002Publication date: January 16, 2003Inventors: R. Richard Goehring, Zhengming Chen, John Whitehead, Parviz Gharagozloo, Sam Victory, Donald Kyle
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Patent number: 6503898Abstract: This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating viral infection. A representative compound of the invention is the compound of formula: wherein R22 and R23 are allyl.Type: GrantFiled: July 10, 1998Date of Patent: January 7, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Patrick Yuk-Sun Lam, Prabhakar Kondaji Jadhav, Charles Joseph Eyermann, Carl Nicholas Hodge, George Vincent De Lucca, James David Rodgers
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Patent number: 6500818Abstract: Compounds having the following formula wherein L, M, R2, R3, R4, R5, R6, R7, X1 and X2 are as defined in the specification, pharmaceutically-acceptable salt thereof, useful for treating depression, anxiety, asthma, rheumatoid arthritis, Alzheimer's disease, cancer, schizophrenia, oedema, allergic rhinitis, inflammation, pain, gastrointestinal-hypermotility, emesis, Huntington's disease, psychoses, hypertension, migraine, bladder hypermotility, or urticaria, compositions including such compounds and processes for making such compounds.Type: GrantFiled: March 30, 2001Date of Patent: December 31, 2002Assignee: Astrazeneca ABInventors: Peter Robert Bernstein, Robert Frank Dedinas, Cyrus John Ohnmacht, Keith Russell
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Patent number: 6476016Abstract: Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described.Type: GrantFiled: July 17, 2001Date of Patent: November 5, 2002Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Aihua Wang, Bruce Edward Tomczuk, Tianbao Lu, Richard M. Soll, John Curtis Spurlino, Roger Francis Bone
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Patent number: 6472385Abstract: Compositions which abrogate DNA damage induced cell cycle arrest thereby enhancing the cell killing activity of DNA damaging anticancer agents for use in the treatment of cancer, and in particular, p53 defective cancers are provided.Type: GrantFiled: August 8, 2000Date of Patent: October 29, 2002Assignee: Trustees of Darmouth CollegeInventors: Alan Eastman, Gordon W. Gribble
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Patent number: 6451787Abstract: Use of the compound represented by general formula (I) for remedies of and protection against eye diseases is disclosed. General formula (I): (wherein, R1 and R2 independently represent a lower alkyl group, R3 and R4 independently represent a hydrogen atom or a lower alkyl group).Type: GrantFiled: June 11, 2001Date of Patent: September 17, 2002Assignees: Cephalon, Inc., Kyowa Hakko Kogyo Co., Ltd.Inventors: Katsuhiko Nakata, Masaaki Kageyama
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Publication number: 20020107237Abstract: The present invention relates to novel N12, N13-bridged sugar derivatives of indolylopyrrolocarbazoles and pharmaceutical formulations thereof which exhibit topoisomerase-I activity and are useful in inhibiting the proliferation of tumor cells.Type: ApplicationFiled: September 27, 2001Publication date: August 8, 2002Inventors: Mark G. Saulnier, Edward H. Ruediger, Neelakantan Balasubramanian, Mikael Mahler, Francis Beaulieu, Carol Bachand, David B. Frennesson
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Publication number: 20020058645Abstract: The invention relates to compounds of formula I 1Type: ApplicationFiled: June 22, 2001Publication date: May 16, 2002Inventors: Laszlo Vertesy, Klaus Ehrlich, Michael Kurz, Joachim Wink
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Publication number: 20020052357Abstract: Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: 1Type: ApplicationFiled: July 17, 2001Publication date: May 2, 2002Applicant: 3-Dimensional Pharmaceuticals, Inc.Inventors: Aihua Wang, Bruce Edward Tomczuk, Tianbao Lu, Richard M. Soll, John Curtis Spurlino, Roger Francis Bone
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Publication number: 20020037888Abstract: The present invention is directed to compounds which inhibit prenyl-protein transferase (FTase) and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.Type: ApplicationFiled: March 28, 2001Publication date: March 28, 2002Applicant: Merck & Co., Inc.Inventors: S. Jane deSolms, Samuel L. Graham, Anthony W. Shaw, Terrence M. Ciccarone, Gerald E. Stokker
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Patent number: 6359129Abstract: New sulfamide compounds and methods of forming those compounds are provided. The inventive methods comprise subjecting a template opened-ring sulfamide compound to a ring-closing metathesis reaction in the presence of a Grubbs catalyst to yield a heterocyclic sulfamide. Advantageously, the template structures can be provided with a wide array of functional groups (e.g., substituted and unsubstituted amino acid side chains, peptides) chosen to provide particular properties to the compound.Type: GrantFiled: August 15, 2000Date of Patent: March 19, 2002Assignee: University of KansasInventors: Paul R. Hanson, Joseph M. Dougherty, Donald A. Probst
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Publication number: 20020032325Abstract: Synthesis, nitric oxide synthase inhibition, and antiproliferative activity of eight structural variants of functionalized 4-amino-3-mercapto-1,2,4-triazoles, specificallyType: ApplicationFiled: February 21, 2001Publication date: March 14, 2002Inventors: Ned D. Heindel, Jeffrey D. Laskin, Diane E. Heck, Robert D. Rapp, Christophe Guillon, Angela M. Mendel
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Publication number: 20020010170Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: ApplicationFiled: March 16, 2001Publication date: January 24, 2002Inventors: Francesco Salituro, Guy Bemis, Huai Gao, Ghotas Evindar
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Publication number: 20010039273Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formulas 1Type: ApplicationFiled: January 26, 2001Publication date: November 8, 2001Inventor: Charles Z. Ding
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Publication number: 20010001791Abstract: A method for treating neoplasms is disclosed, particularly using the &bgr;-isozyme selective PKC inhibitor, (S)-3,4-[N, N′-1,1′-((2″-ethoxy)-3′″(O)-4′″-(N,N-dimethylamino)-butane)-bis-(3,3′-indolyl)]-1(H)-pyrrole-2,5-dione or one of its salts, such PKC inhibitors enhance the clinical efficacy of oncolytic agents and radiation therapy.Type: ApplicationFiled: January 10, 2001Publication date: May 24, 2001Inventors: Michael R. Jirousek, Lawrence E. Stramm, Douglas Kirk Ways
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Patent number: 6225306Abstract: A biphenyl derivative represented by the following general formula (1) and a pharmaceutically acceptable salt thereof: [In the formula (1), A represents a single bond, —CH2—, —CO—, —CS— or —SO2—; B represents a single bond or —CH2—; R1 represents a hydrogen atom, —OH, —NR11R12 (wherein R11 and R12 each independently represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms), —OCOCH3, or a halogen atom; R2 represents a hydrogen atom or R1 and R2 form a group ═O together; R3 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms; provided that in the formula, the absolute configuration of the position a may be either R or S]. The compound of the present invention has considerably high safety and efficacy and is useful as, in particular, a vasopressin receptor antagonist.Type: GrantFiled: September 30, 1999Date of Patent: May 1, 2001Assignee: Wakamoto Pharmaceutical Co., Ltd.Inventors: Yasuhiro Ohtake, Akira Naito, Kenji Naito, Hidehiko Matsukawa, Yoshiaki Saito, Hatsunori Toyofuku
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Patent number: 6200968Abstract: A non-aqueous, particle-forming, fused pyrrolocarbazole-containing composition is disclosed. Upon contact with an aqueous medium, the particle-forming composition spontaneously disperses into suspended particles, thereby forming a stable suspension that provides greatly improved bioavailability of orally administered fused pyrrolocarbazole compounds.Type: GrantFiled: August 5, 1999Date of Patent: March 13, 2001Assignee: Cephalon, Inc.Inventors: David A. Dickason, Piyush R. Patel, Vincent Corvari, Efraim Shek, Joseph L. Herman, Jeffry M. Skell
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Patent number: 6197955Abstract: A staurosporine derivative with anti-cancer activity and anti-bacterial activity is produced by acidifying a solution containing staurosporine to isomerize staurosporine to its desired derivative, whereby the derivative is recovered from the acidified solution.Type: GrantFiled: December 20, 1999Date of Patent: March 6, 2001Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Satoru Nagamura, Hidenori Aoki, Mitsutaka Kino, Toshimitsu Takiguchi
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Patent number: 6156746Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formula ##STR1## and their enantiomers, diastereomers, and their pharmaceutically acceptable salts, including prodrugs and solvates thereof.The compounds of formula I are useful in the treatment of a variety of cancers. In addition, the formula I compounds may also be useful in the treatment of diseases other than cancer.Type: GrantFiled: July 15, 1999Date of Patent: December 5, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Katerina Leftheris, John T. Hunt, Charles Z. Ding
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Patent number: 6127359Abstract: Compounds of the formula: ##STR1## wherein A.sup.1 to A.sup.5 form a seven-membered ring containing one optionally substituted nitrogen atom and one heteroatom selected from oxygen and nitrogen;D.sup.1 to D.sup.4 form a substituted six membered ring, optionally containing up to two nitrogen atoms;R is preferably at least one acid containing substituent;R* is is one or more groups chosen from H, Q-C.sub.1-6 alkyl, Q-C.sub.1-6 oxoalkyl, Q-C.sub.2-6 alkenyl, Q-C.sub.3-4 oxoalkenyl, Q-C.sub.3-4 oxoalkynyl, Q-C.sub.2-4 alkynyl, C.sub.3-6 cycloalkyl, Ar or Het;Q is H, C.sub.3-6 cycloalkyl, Het or Ar;R.sup.6 is preferably a basic nitrogen containing substituent;are inhibitors of platelet aggregation.Type: GrantFiled: May 14, 1999Date of Patent: October 3, 2000Assignee: SmithKline Beecham CorporationInventors: William Edward Bondinell, James Francis Callahan, William Francis Huffman, Richard McCulloch Keenan, Thomas Wen-Fu Ku, Kenneth Allen Newlander
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Patent number: 6127401Abstract: The present invention is directed to novel fused aryl and heteroaryl bridged indenopyrrolocarbazoles which are useful, inter alia, as therapeutic agents. The invention is also directed to methods for making and using the bridged indenopyrrolocarbazoles.Type: GrantFiled: June 3, 1999Date of Patent: October 3, 2000Assignee: Cephalon, Inc.Inventors: Jasbir Singh, Robert L. Hudkins, John P. Mallamo, Theodore L. Underiner, Rabindranath Tripathy
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Patent number: 6080758Abstract: The present invention relates to compounds selected from the group consisting of the compounds of formula (I): ##STR1## X is a halogen atom, A is --CH.sub.2 --, --CH(OH)--, --CH(NH--COCH.sub.3)-- or S, R is H, CO.sub.2 H, CO.sub.2 --B--R.sub.1 or CO--N(R.sub.2)--B--R.sub.1, B is linear, branched or cyclic C.sub.1 -C.sub.10 -alkylene, R.sub.1 is H, CH.sub.2 OH, CH.sub.2 --O--CH.sub.3, CH.sub.2 --NR.sub.3 R.sub.4 or phenyl, R.sub.2 is H or C.sub.1 -C.sub.4 -alkyl, R.sub.3 is H or linear, branched or cyclic C.sub.1 -C.sub.10 -alkyl, R.sub.4 is H or linear or branched C.sub.1 -C.sub.10 -alkyl, it being possible for NR.sub.3 R.sub.4 to be a saturated heterocyclic radical having from 5 to 8 ring members and containing at least one nitrogen atom, and the carbon carrying the substituent R, when Q is saturated, can be of indeterminate (R,S) configuration or of determinate (R) or (S) configuration; and their addition salts.Type: GrantFiled: April 7, 1997Date of Patent: June 27, 2000Assignee: Fournier Industrie et SanteInventors: Pierre Dodey, Michel Bondoux, Patrick Houziaux, Martine Barth, Khan Ou
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Patent number: 6037468Abstract: Tertiary alcohols containing the structural features illustrated in 3 or 4 below (Scheme I) are prepared by reacting at least one diazo carbonyl compound, e.g., 1 in Scheme I) and at least one allylic alcohol (e.g., 2 in Scheme I) in a coupling reaction run under conditions that produce carbene or carbenoid intemediates from the diazo containing substrate such as transition metal catalysis or either thermal or photochemical decomposition. In some preferred embodiments, Rh.sub.2 (OAc).sub.4 is employed to catalyze the coupling reaction. ##STR1## Indolocarbazoles (e.g., 7 below) are prepared by coupling of diazo carbonyl compounds (e.g., 5) and biindoles (e.g., 6). Indolocarbazoles are furanosylated (e.g., 7) with acetals (e.g., 8) or their open chain congeners (e.g., 9) under conditions known to promote acetal exchange or formation, such as protic or Lewis acids. Furanosylated indolocarbazoles (e.g., 10) are also prepared via ring contraction of pyranosylated indolocarbazoles (e.g.Type: GrantFiled: December 4, 1998Date of Patent: March 14, 2000Assignee: Yale UniversityInventors: John L. Wood, Brian M. Stoltz
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Patent number: 6005102Abstract: The present invention provides compounds useful in the synthesis of biologically active compounds, and processes for their production, the compounds having the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are, independently, selected from H; C.sub.1 -C.sub.12 alkyl or C.sub.1 -C.sub.6 perfluorinated alkyl; X represents a leaving group; A is O or S; m is an integer from 1 to 3, preferably 2; R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are independently selected from H, halogen, --NO.sub.2, alkyl, alkoxy, C.sub.1 -C.sub.6 perfluorinated alkyl, OH or the C.sub.1 -C.sub.4 esters or alkyl ethers thereof, --CN, --O--R.sup.1, --O--Ar, --S--R.sup.1, --S--Ar, --SO--R.sup.1, --SO--Ar, --SO.sub.2 --R.sup.1, --SO.sub.2 --Ar, --CO--R.sup.1, --CO--Ar, --CO.sub.2 --R.sup.1, or --CO.sub.2 --Ar; and Y is selected from a) the moiety: ##STR2## wherein R.sub.7 and R.sub.8 are independently selected from the group of H, C.sub.1 -C.sub.Type: GrantFiled: September 28, 1998Date of Patent: December 21, 1999Assignee: American Home Products CorporationInventors: Panolil Raveendranath, Joseph Zeldis, Galina Vid, John R. Potoski, Jianxin Ren, Silvio Iera
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Patent number: 5882544Abstract: The present invention relates to polycyclic iminooxadiazinediones A corresponding to formula I ##STR1## The present invention also relates to mixtures of these polycyclic iminooxadiazinediones with other isocyanate derivatives and to their use for the production of optionally foamed polyurethane plastics, for the production of paints and coatings and for the production or formulation of active ingredients, pharmaceutical products, etc.Type: GrantFiled: December 11, 1997Date of Patent: March 16, 1999Assignee: Bayer AktiengesellschaftInventors: Frank Richter, Dieter Mager, Josef Pedain
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Patent number: 5827846Abstract: The utility of known and novel staurosporin derivatives of formula I ##STR1## wherein R.sub.1 is formyl, an aliphatic hydrocarbon radical having up to 29 carbon atoms that is unsubstituted or substituted by aryl, or is an aryl radical,R.sub.2 is hydrogen, C.sub.1 -C.sub.5 alkyl, benzoyl, lower alkanoyl or .alpha.-aminoacyl having a free or protected amino group, andR.sub.3 is hydrogen, hydroxy, lower alkoxy or oxo,or whereinR.sub.1 is methoxycarbonylmethyl,R.sub.2 is benzoyl, andR.sub.3 is hydrogen,for avoiding or removing multi-drug resistance to anti-tumour agents, such as vinblastine or adriamycin, is described.Type: GrantFiled: November 27, 1996Date of Patent: October 27, 1998Assignee: Novartis Corp.Inventors: Urs Regenass, Giorgio Caravatti, Oskar Wacker
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Patent number: 5786352Abstract: Novel compounds of the following general formula or salts thereof. ##STR1## wherein Ring M is a heterocyclic ring having --N.dbd.C<, --CO--N< or --CS--N< as the partial structure --X . . . Y<; R.sup.a and R.sup.b are bonded to each other to form Ring A, or they are the same or different and represent, independently, a hydrogen atom or a substituent on the Ring M; Ring A and Ring B represent, independently, an optionally substituted homocyclic or heterocyclic ring, and at least one of them is optionally substituted heterocyclic ring; Ring C is optionally substituted homocyclic or heterocyclic ring; Ring Z is an optionally substituted ring; and n represents an integer of from 1 to 6, or a salt thereof, which has an excellent tachykinin receptor antagonistic effect, and their production, and pharmaceutical compositions.Type: GrantFiled: March 25, 1996Date of Patent: July 28, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideaki Natsugari, Takenori Ishimaru, Takayuki Doi, Yoshinori Ikeura, Chiharu Kimura
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Patent number: 5780461Abstract: This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals. The compounds of the present invention can be used to treat cancer and inhibiting tumor growth in mammals.Type: GrantFiled: May 6, 1996Date of Patent: July 14, 1998Assignee: Eli Lilly and CompanyInventors: William F. Heath, Jr., Michael R. Jirousek, John H. McDonald, III, Christopher J. Rito
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Patent number: 5760222Abstract: Bleaches, a method for bleaching substrates using these materials and detergent compositions containing same are reported. The bleaches are thiadiazole dioxide derived mono- and di- oxaziridines. Substrates such as fabrics may be bleached in an aqueous solution containing the oxaziridine.Type: GrantFiled: December 3, 1996Date of Patent: June 2, 1998Assignee: Lever Brothers Company, Division of Conopco, Inc.Inventor: Janet Lynn Coope
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Patent number: 5760028Abstract: This invention relates to novel heterocycles including 3-?1-?3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzylo xycarbonylamino)propionic acid, which are useful as antagonists of the .alpha..sub.v .beta..sub.3 integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.Type: GrantFiled: December 20, 1996Date of Patent: June 2, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Prabhakar Kondaji Jadhav, Joseph James Petraitis, Douglas Guy Batt
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Patent number: 5756494Abstract: The invention features novel derivatives of K-252a, as well as novel bis-N-substituted derivatives of staurosporine. The invention also features a method for treating diseased neuronal cells involving the administration of either the novel staurosporine derivatives or specified functional derivatives of K-252a.Type: GrantFiled: June 2, 1995Date of Patent: May 26, 1998Assignees: Cephalon, Inc., Kyowa Hakko Kogyo Co., Ltd.Inventors: Michael E. Lewis, James C. Kauer, Nicola Neff, Jill Roberts-Lewis, Chikara Murakata, Hiromitsu Saito, Yuzuru Matsuda, Marcie A. Glicksman, Fumihiko Kanai, Masami Kaneko
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Patent number: 5753643Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: May 22, 1997Date of Patent: May 19, 1998Assignee: Novo Nordisk A/SInventors: Henrik Sune Andersen, Knud Erik Andersen, Rolf Hohlweg, Peter Madsen, Tine Krogh J.o slashed.rgensen, Uffe Bang Olsen
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Patent number: 5698691Abstract: Disclosed is a squalene synthetase inhibitor which comprises the compound represented by the formula ##STR1## wherein R.sub.1 is hydrogen or an optionally substituted hydrocarbon group; R.sub.2 is hydrogen, an optionally substituted alkyl group, an optionally substituted phenyl group or an optionally substituted aromatic heterocyclic ring group; X' is a substituent comprising an optionally esterified carboxyl group, an optionally substituted carbamoyl group, an optionally substituted hydroxyl group, an optionally substituted amino group or an optionally substituted heterocyclic radical having a protonizable hydrogen; Ring A is an optionally substituted benzene ring or an optionally substituted aromatic heterocyclic ring; Ring J' is a 7- to 8-membered heterocyclic ring containing at most three ring constituting hetero atoms; D is C or N; the Ring J' optionally having, besides R.sub.1, R.sub.Type: GrantFiled: September 26, 1994Date of Patent: December 16, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Hidefumi Yukimasa, Ryuichi Tozawa, Yasuo Sugiyama, Masakuni Kori
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Patent number: 5698578Abstract: This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.Type: GrantFiled: October 21, 1996Date of Patent: December 16, 1997Assignee: Eli Lilly and CompanyInventors: William F. Heath, Jr., Michael R. Jirousek, John H. McDonald, III, Christopher J. Rito
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Patent number: RE37781Abstract: This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating viral infection. A representative compound of the invention is the compound of formula: wherein R22 and R23 are allyl.Type: GrantFiled: March 10, 1999Date of Patent: July 2, 2002Assignee: DuPont Pharmaceuticals CompanyInventors: Patrick Y. Lam, Prabhakar K. Jadhav, Charles J. Eyermann, Carl N. Hodge, George V. De Lucca, James D. Rodgers