The Cyclisation Occurring Through The 4-amino Radical Of 2,4-diamino Butanoic Acid Patents (Class 530/318)
  • Publication number: 20150024997
    Abstract: The invention features echinocandin class compounds. The compounds can be useful for the treatment of fungal infections.
    Type: Application
    Filed: April 1, 2014
    Publication date: January 22, 2015
    Applicant: SEACHAID PHARMACEUTICALS, INC.
    Inventors: Kenneth Duke JAMES, JR., Christopher Patrick LAUDEMAN, Navdeep Balkrishna MALKAR, Balasingam RADHAKRISHNAN
  • Publication number: 20140256637
    Abstract: The present disclosure provides solid forms of a compound of formula I. In some embodiments, the present disclosure provides crystalline forms of Compound I. In some embodiments, the present disclosure provides solvate forms of Compound I. In some embodiments, the present disclosure provides amorphous Compound I.
    Type: Application
    Filed: May 19, 2014
    Publication date: September 11, 2014
    Applicant: Celgene Corporation
    Inventors: Jason HANKO, David Alan ENGERS, Eric HAGEN, Valelriya SMOLENSKAYA, Jeffrey Scott STULTS, Vijay Harishchandra NARINGREKAR, Victor PEYKOV, William Rodney FOSS, Neil Lawrence DARLING, Nicholas VROLIJK
  • Publication number: 20130196899
    Abstract: The invention provides a synthetic polypeptide of Formula I?: or an amide, an ester or a salt thereof, wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12 and X13 are defined herein. The polypeptides are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia.
    Type: Application
    Filed: January 23, 2013
    Publication date: August 1, 2013
    Applicant: NOVARTIS AG
    Inventors: Frédéric ZECRI, Andrei GOLOSOV, Philipp GROSCHE, Kayo YASOSHIMA, Hongjuan ZHAO, Qi-Ying HU, Hidetomo IMASE, David Thomas PARKER
  • Patent number: 8357662
    Abstract: A compound sensitive to and selective for ammonium ions over other ions. A sensor fabricated from a self assembled monolayer of said compound on gold, exhibiting sensitivity and selectivity for ammonium ions over other ions in aqueous solutions, including blood. A method of preparation of said compound and said sensor.
    Type: Grant
    Filed: September 10, 2007
    Date of Patent: January 22, 2013
    Assignee: Worcester Polytechnic Institute
    Inventors: W. Grant McGimpsey, Nantanit Wanichacheva, Christopher R. Lambert
  • Publication number: 20130005644
    Abstract: The present invention relates to novel cyclic or constrained acyclic compounds which modulate the activity of G protein-coupled receptors and are useful in the treatment of conditions mediated by G protein-coupled receptors, for example, inflammatory conditions.
    Type: Application
    Filed: January 12, 2012
    Publication date: January 3, 2013
    Applicant: PROMICS PTY LIMITED
    Inventors: David FAIRLIE, Stephen Maxwell Taylor, Angela Monique Finch, Allan Wong
  • Publication number: 20110224129
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain lipopeptide compounds comprising a cyclic peptide bearing a lipid side chain (for convenience, collectively referred to herein as “LP compounds”), which, inter alia, are antimicrobial, particularly antibacterial. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to provide an antimicrobial function, particularly an antibacterial function, and in the treatment of diseases and conditions that are mediated by microbes, particularly bacteria, that are ameliorated by the antimicrobial function, particularly an antibacterial function, including bacterial diseases, optionally in combination with another agent, for example, another antibacterial agent.
    Type: Application
    Filed: November 24, 2009
    Publication date: September 15, 2011
    Inventors: Rustum S. Boyce, Joseph Cherian, Cleofe Calanasan, Muhammad Sofian Asi Sihombing
  • Publication number: 20110183416
    Abstract: The present invention is directed to a method of decreasing the rate of proliferation of medullary thyroid carcinoma cells which comprises contacting medullary thyroid carcinoma cells with one or more SSTR2 agonist. A preferred selective somatostatin receptor type-2 (SSTR-2) agonist cyclo[Tic-Tyr-D-Trp-Lys-Abu-Phe] is also disclosed.
    Type: Application
    Filed: June 5, 2007
    Publication date: July 28, 2011
    Inventors: Ettore Ciro Degli Uberti, Maria Chiara Zatelli, Michael Dewitt Culler, David H. Coy
  • Patent number: 7214768
    Abstract: This invention relates to an improved process for the minimization of acid-catalyzed reactions of certain echinocandins of the kind disclosed in U.S. Pat. No. 5,378,804. The process involves the use of a boronic acid.
    Type: Grant
    Filed: April 8, 2002
    Date of Patent: May 8, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Kevin M. Belyk, William R. Leonard
  • Patent number: 7192920
    Abstract: A subject of the invention, in all possible isomer forms as well as their mixtures, is the compounds of formula (I): in which either R1: H or CH3 and R2: cyclohexyl substituted by an amine, a (CH2)b-C?N radical or R1 and R2 together with the nitrogen which carries them form a ring with 3, 4 or 5 carbons optionally substituted by an amine R3: hydrogen, methyl or hydroxyl R4: hydrogen or hydroxyl R: represents a linear, branched or cyclic chain T: hydrogen, methyl, CH2CONH2, CH2C?N, a (CH2)2NH2 or (CH2)2Nalk+X? radical, X halogen and alk alkyl Y: hydrogen, hydroxyl, halogen or OSO3H, W: H or OH, Z: H, CH3. The compounds of formula (I) have antifungal properties.
    Type: Grant
    Filed: September 13, 2005
    Date of Patent: March 20, 2007
    Assignee: Aventis Pharma SA
    Inventors: Patrick Fauveau, Stephen Hawser, Gilles Lebourg, Laurent Schio
  • Patent number: 7045591
    Abstract: Peptides cyclized via disulfide or lactam bridges are disclosed. The peptides exhibit melanocortin-4 receptor agonist activity and are useful for treating obesity.
    Type: Grant
    Filed: August 27, 2001
    Date of Patent: May 16, 2006
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Li Chen, Adrian Wai-Hing Cheung, Xin-Jie Chu, Waleed Danho, Joseph Swistok, Yao Wang, Keith Alan Yagaloff
  • Patent number: 7022669
    Abstract: A subject of the invention, in all possible isomer forms as well as their mixtures, is the compounds of formula (I): in which either R1: H or CH3 and R2: cyclohexyl substituted by an amine, a (CH2)b-C?N radical or R1 and R2 together with the nitrogen which carries them form a ring with 3, 4 or 5 carbons optionally substituted by an amine R3: hydrogen, methyl or hydroxyl R4: hydrogen or hydroxyl R: represents a linear, branched or cyclic chain T: hydrogen, methyl, CH2CONH2, CH2C?N, a (CH2)2NH2 or (CH2)2Nalk+X? radical, X halogen and alk alkyl Y: hydrogen, hydroxyl, halogen or OSO3H, W: H or OH, Z: H, CH3. The compounds of formula (I) have antifungal properties.
    Type: Grant
    Filed: June 8, 2000
    Date of Patent: April 4, 2006
    Assignee: Aventis Pharma S.A.
    Inventors: Patrick Fauveau, Stephen Hawser, Gilles Lebourg, Laurent Schio
  • Patent number: 6872713
    Abstract: Saponins of formula (I), a stereoisomeric form thereof or a pharmaceutically acceptable addition salt thereof, wherein R1 to R12 have the meaning given in the description, can be isolated from plants of the family Myrsinaceae and used, to decrease the infectiousness of and reduce the mortality associated with protozoan parasites of the genus Leishmania which are responsible for a group of conditions known as leishmaniases.
    Type: Grant
    Filed: December 15, 1999
    Date of Patent: March 29, 2005
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Louis Jules Roger Marie Maes, Nils Albert Gilbert Germonprez, Luc Emiel Mathilde Van Puyvelde, Norbert G. M. De Kimpe, Tran Ngoc Ninh
  • Patent number: 6809177
    Abstract: The invention relates to a process for the conversion of echinocandin class of peptides to their C4-homotyrosine monodeoxy analogues, particularly mulundocandin to deoxymulundocandin, which consists of a single step selective reduction of C4-htyr (homotyrosine) hydroxyl group of echinocandins to their monodeoxy analogues under neutral conditions without prior protection/deprotection of the equally facile C5-Orn (ornithine) hydroxyl group and purification of the monodeoxy compound from the crude reaction mixture.
    Type: Grant
    Filed: March 29, 2001
    Date of Patent: October 26, 2004
    Assignee: Aventis Pharma Deutschland GmbH.
    Inventors: Triptikumar Mukhopadhyay, Kenia Jayvanti, Erra Koteswara Satya Vijaya Kumar
  • Patent number: 6809077
    Abstract: The present invention relates to a cyclosporin analog of the following formula (I) or a pro-drug or pharmaceutically acceptable salt thereof: In particular, residue A maybe represented by either formula A1 or A2 as illustrated below: where X and Y are defined herein. In a second embodiment, the present invention relates to pharmaceutical compositions comprising pro-drugs or pharmaceutically acceptable salts of the compounds of the present invention and the use thereof for treating autoimmune diseases or for the prevention of organ transplantation rejection in a subject. In a third embodiment, the present invention relates to processes for the production of novel cyclosporin analogs of the present invention.
    Type: Grant
    Filed: October 12, 2001
    Date of Patent: October 26, 2004
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yat Sun Or, Tsvetelina Ivanova Lazarova, Blake Christopher Hamann, Jason Shih-Hao Chen
  • Patent number: 6617423
    Abstract: Calcitonins and calcitonin derivatives such as are employed for therapy for, for example, osteoporosis. Paget's disease or hypercalcemia. The calcitonins and calcitonin derivatives are distinguished by a bridging of the amino acids present in the positions 17 and 21. In this case, by means of a suitable choice of the amino acids present in these positions an 18- or 19-membered ring is produced. This ring leads to an increased conformational stability and to an increased activity of the modified calcitonin. A particularly suitable hCt (human Ct) analog is the cyclo17,21-[Asp17, Orn21]-hCt according to the invention having a 19-membered ring structure between the lactam-bridged Asp17 and Orn21.
    Type: Grant
    Filed: December 20, 2000
    Date of Patent: September 9, 2003
    Assignee: Fraunhofer-Gesellschaft zur Forderung der Angewandten Forschung E.V.
    Inventors: Afroditi Kapurniotu, Jurgen Bernhagen, Herwig Brunner
  • Publication number: 20030083238
    Abstract: This invention relates to new polypeptide compound represented by the general formula (I) wherein R1, R2, R3, R4, R5 and R6 are as defined in the description or a salt thereof which has antimicrobial activities (especially, antifungal activities), inhibitory activity on &bgr;-1,3-glucan synthase, to process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for prophylactic and/or therapeutic treatment of infectious diseases including Pneumocystic carinii infection (e.g. Pneumocystis carinii pneumonia) in a human being or an animal.
    Type: Application
    Filed: January 30, 2002
    Publication date: May 1, 2003
    Inventors: Ayako Toda, Takahiro Matsuya, Hiroaki Mizuno, Hiroshi Matsuda, Kenji Murano, David Barrett, Takashi Ogino, Keiji Matsuda
  • Patent number: 6521595
    Abstract: The present invention relates to methods for treating alopecia and stimulating hair growth and pharmaceutical compositions using nonimmunosuppressive [&ggr;-hydroxy-methylleucine4] cyclosporin A having superior hair growth-promoting effect, wherein the hydroxyl group is added to the carbon position of No. 4 methylleucine of cyclosporin A by the microorganism.
    Type: Grant
    Filed: May 30, 2000
    Date of Patent: February 18, 2003
    Assignee: LG Chemical, Ltd.
    Inventors: Sang-Nyun Kim, Ho-Jeong Ahn, Myung-Kee Kim, Jong-Il Kim, Jung-Hun Kim, Chang-Woo Lee, Min-Ho Lee, Chang-Deok Kim, Ho-Song Cho, Hyun-Sik Kim, Min-Hwan Jung, Seung-Jin Kim
  • Patent number: 6384026
    Abstract: The present invention describes an isolated macrocycle having the formula: where d is an integer from 0 to about 100; A, B, and each D are the same or different and are selected from the group consisting of each R1 is the same or different and is a bivalent alkylene moiety; each R2 is the same or different and is a bivalent alkylene moiety; and each R3 is the same or different and is selected from the group consisting of a hydrogen atom and an alkyl moiety. Methods for producing these macrocycles are also described. The macrocycles of the present invention can be used as arthropod repellents.
    Type: Grant
    Filed: April 2, 1999
    Date of Patent: May 7, 2002
    Assignee: Cornell Research Foundation, Inc.
    Inventors: Frank C. Schroeder, Jay J. Farmer, Thomas Eisner, Scott R. Smedley
  • Patent number: 6372474
    Abstract: The present invention provides a cyclic lipopeptide acrylase which may effectively deacylate the acyl side chain of a cyclic lipopeptide compound, specifically FR901379 Substance or its analog thereof shown by the following general formula [I], and a process for production of a cyclic peptide compound which comprises the use of said acylase.
    Type: Grant
    Filed: September 12, 2000
    Date of Patent: April 16, 2002
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Satoshi Ueda, Miho Tanaka, Masami Ezaki, Kazutoshi Sakamoto, Seiji Hashimoto, Nobutaka Oohata, Masaru Tsuboi, Michio Yamashita
  • Patent number: 6358921
    Abstract: The invention concerns antimicrobial cyclic peptides and peptide analogs having relatively low hemolytic activity. Peptides of the invention are effective in killing and/or inhibiting growth of a number of microorganisms, including gram-positive bacteria, gram-negative bacteria, fungi and mycoplasma. Also disclosed are methods for inhibiting or killing such microorganisms, and therapeutic preparations for such inhibiting or killing.
    Type: Grant
    Filed: October 10, 1997
    Date of Patent: March 19, 2002
    Assignee: Pence, Inc.
    Inventors: Leslie H. Kondejewski, Robert S. Hodges, David S. Wishart, Robert E. W. Hancock, Ronald N. McElhaney, Elmar J. Prenner, Ruthven N. A. H. Lewis
  • Patent number: 6265534
    Abstract: Superpotent calcitonin analogs have greatly increased hypocalcemic action in vivo. These calcitonins and calcitonin derivatives are employed for the therapy of, for example, osteoporosis, Paget's disease or hypercalcemia. The calcitonins and calcitonin derivatives are distinguished by a bridging of the amino acids present in the positions 17 and 21. By means of suitable choice of the amino acids present in these positions an 18-membered or 19-membered ring is produced. This ring leads to an increased conformational stability and to an increased activity of the modified calcitonin. A particularly suitable hCt (human calcitonin analog) is a cyclo17,21-[Asp17, Orn21]-hCt having a 19-membered ring structure between the lactam-bridged Asp17 and Orn21.
    Type: Grant
    Filed: August 20, 1998
    Date of Patent: July 24, 2001
    Assignee: Fraunhofer-Gesellschaft zur Forderung der Angewandten Forschung E.V.
    Inventors: Afroditi Kapurniotu, Jurgen Bernhagen, Herwig Brunner
  • Patent number: 6265375
    Abstract: Novel backbone cyclized peptide analogs are formed by means of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic linkages. Novel building units disclosed are N&agr;(&ohgr;-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these N&agr;(&ohgr;-functionalized) amino acids are incorporated into a peptide sequence, preferably during solid phase peptide synthesis. The reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect either backbone-to-backbone or backbone-to-side chain cyclizations. The invention is specifically exemplified by backbone cyclized bradykinin antagonists having biological activity. Further embodiments of the invention are somatostatin analogs having one or two ring structures involving backbone cyclization.
    Type: Grant
    Filed: July 22, 1998
    Date of Patent: July 24, 2001
    Assignees: Yissum Research Development Co. of the Hebrew University, Peptor Limited
    Inventors: Chaim Gilon, Doron Eren, Irina Zeltser, Alon Seri-Levy, Gal Gitan, Dan Muller
  • Patent number: 6194383
    Abstract: The invention relates to lipopeptides with very homologous amino-acid sequences but different fatty acid residues (lipid portion) which are synthesized by Actinoplanes sp. during fermentation and are released into the culture medium, to a process for isolating the lipopeptides from the culture medium and purifying them, to the use of the lipopeptides as pharmacologically active substances, in particular against Gram-positive bacteria, and to Actinoplanes sp. DSM 7358 for producing the abovementioned lipopeptides.
    Type: Grant
    Filed: March 5, 1997
    Date of Patent: February 27, 2001
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Peter Hammann, Johannes Meiwes, Gerhard Seibert, László Vertesy, Joachim Wink, Astrid Markus
  • Patent number: 6146872
    Abstract: The present invention provides a cyclic lipopeptide acylase which may effectively deacylate the acyl side chain of a cyclic lipopeptide compound, specifically FR901379 Substance or its analog thereof shown by the following general formula [I], and a process for production of a cyclic peptide compound which comprises the use of said acylase.
    Type: Grant
    Filed: December 31, 1998
    Date of Patent: November 14, 2000
    Assignee: Fukisawa Pharmaceutical Co., Ltd.
    Inventors: Satoshi Ueda, Miho Tanaka, Masami Ezaki, Kazutoshi Sakamoto, Seiji Hashimoto, Nobutaka Oohata, Masaru Tsuboi, Michio Yamashita
  • Patent number: 6127519
    Abstract: Peptides useful in the regulation of calcium metabolism are disclosed. Also disclosed are pharmaceutical compositions of matter containing such peptides as well as a method for the regulation of calcium metabolism in a patient in need of such treatment. The peptides contain modified or unmodified portions of an amino acid sequence at the 8- to 32-positions of native calcination.
    Type: Grant
    Filed: December 21, 1990
    Date of Patent: October 3, 2000
    Assignee: Tsumura & Co.
    Inventors: Ronald C. Orlowski, Satoshi Hanamura, Masahiko Marumoto, Kenji Sakamoto, Yoshihiro Waki
  • Patent number: 6030944
    Abstract: Certain bisamine compounds which have a cyclohexapeptidyl nucleus and which are found to have antibiotic activity with physical properties suitable for direct use in therapeutic compositions are described. A novel process for their preparation is also described.
    Type: Grant
    Filed: September 3, 1992
    Date of Patent: February 29, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Frances Aileen Bouffard, James F. Dropinski, Robert A. Zambias
  • Patent number: 6030942
    Abstract: The invention relates to compositions which are useful for inhibiting ribonucleotide reductase enzymes, including the mammalian ribonucleotide reductase enzyme. The compositions include, but are not limited to, linear peptides, cyclic peptides, peptide analogs, and peptidomimetics. Methods of using the compositions of the invention to treat cancer and viral and bacterial infections are disclosed.
    Type: Grant
    Filed: March 17, 1998
    Date of Patent: February 29, 2000
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Barry S. Cooperman, Ralph F. Hirschmann, Amos B. Smith, III, Paul Laub, Setsuya Sasho, Paul A. Sprengeler, Bari A. Barwis, Alison Fisher, Shrikumar Nair
  • Patent number: 5951964
    Abstract: This invention relates to radiolabeled reagents, including specific-binding peptide embodiments thereof, and methods for producing and using such reagents. Specifically, the invention relates to reagents for preparing scintigraphic imaging agents for imaging sites in a mammalian body. Reagents, methods and kits for making such reagents, and methods for using such reagents labeled with technetium-99m (Tc-99m) via Tc-99m binding moieties comprising said reagents, are provided. In particular, the specific-binding peptides and Tc-99m binding moieties comprising the reagents of the invention are covalently linked to a polyvalent linker moiety, so that the polyvalent linker moiety is covalently linked to a multiplicity of the specific-binding peptides, and the Tc-99m binding moieties are covalently linked to a plurality of the specific-binding peptides, the polyvalent linker moiety, or to both the specific-binding peptides and the polyvalent linker moiety.
    Type: Grant
    Filed: January 26, 1995
    Date of Patent: September 14, 1999
    Assignee: Diatide, Inc.
    Inventors: Richard T. Dean, John Lister-James
  • Patent number: 5948753
    Abstract: Certain propanolamine compounds are described which have a cyclohexapeptidyl nucleus and which possess antibiotic activity with physical properties suitable for direct use in therapeutic compositions. A process for their preparation is also described.
    Type: Grant
    Filed: May 4, 1993
    Date of Patent: September 7, 1999
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Milton L. Hammond, Robert A. Zambias
  • Patent number: 5939384
    Abstract: Certain propanolamine compounds which have a cyclohexapeptidyl nucleus and which are found to have extremely active antibiotic activity with physical properties suitable for direct use in therapeutic compositions are described. A novel process for their preparation is also described.
    Type: Grant
    Filed: September 3, 1992
    Date of Patent: August 17, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Milton L. Hammond, Robert A. Zambias
  • Patent number: 5922837
    Abstract: The present invention provides novel cyclic tetrapeptides useful in the treatment or prevention of protozoal diseases; in particular, the novel compounds are active against the causative pathogens in malaria, toxoplasmosis, and coccidiosis. The invention also relates to the use of known compounds which are histone deacetylase inhibitors as antiprotozoal agents.
    Type: Grant
    Filed: January 27, 1997
    Date of Patent: July 13, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Peter T. Meinke, Sandra J. Rattray, Dennis M. Schmatz
  • Patent number: 5914313
    Abstract: A compound having the formula ##STR1## in which R.sub.1 is an aminoalkyl group and ##STR2## is an acyl group and salts thereof having high antibiotic activity and being substantially free of lytic activity are described.
    Type: Grant
    Filed: January 15, 1993
    Date of Patent: June 22, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Frances Aileen Bouffard, James F. Dropinski
  • Patent number: 5874403
    Abstract: Novel amino acid conjugates of cyclohexa-peptidyl amines having the formula ##STR1## and having antifungal and antiparasital properties are described. The compounds exhibit less acute toxicity than the free amines.
    Type: Grant
    Filed: October 15, 1992
    Date of Patent: February 23, 1999
    Assignee: Merck & Co., Inc.
    Inventor: Robert A. Zambias
  • Patent number: 5872097
    Abstract: Straight or cyclic pentapeptides with receptor affinity to .mu. or .delta. opioid receptors having a primary sequence backbone of Tyr-X-Phe-Leu-Z, Seq. ID Nos. 1, 2, and 3. X and Z can be covalently coupled to provide a heterocyclic structure according to the following conditions:i) when the pentapeptide is straight X is selected from the group consisting of Ser, Gly, Pro, AMCA and D-Ala and Z is selected from the group consisting of Glu, Gln or amino derivatives of Glu or Gln, Seq. ID No. 1, with the proviso that if X is Ser, then Z is Glu or amino derivatives of Glu; andii) where the pentapeptide is cyclic X is selected from the group consisting of D- or L-2,4-diaminobutyric acid, D- or L-lysine, D- or L-ornithine and D or L-cysteine and Z is selected from the group consisting of Gln or Glu or amino derivatives of Gln or Glu, Seq. ID No. 2, and 3, with the proviso that if X is D-or L-Cys, then Z is Cys, Seq. ID No. 3.
    Type: Grant
    Filed: September 7, 1995
    Date of Patent: February 16, 1999
    Assignee: Pharmacia & Upjohn Aktiebolag
    Inventors: Karin Ingeborg Fholenhag, Linda Fryklund, Bo Christer Larsson, Fred Jarl Nyberg, Gertrud Elisabeth Westin-Sjodahl, Ronny Lundin
  • Patent number: 5871886
    Abstract: A method of patterning a layer of reflective material, such as a layer of conductor metal, using a layer of antireflection coating material sandwiched between two layers of photoresist. A first layer of photoresist is formed on an integrated circuit wafer and provides a planar surface for subsequent layers of material. A layer of antireflection coating material is formed on the layer of first photoresist and a layer of second photoresist is formed on the layer of antireflection coating material. The layer of second photoresist is selectively exposed and developed. The layer of antireflection coating material is patterned using dry etching and the patterned layer of second photoresist as a mask. The layer of first photoresist is then patterned using dry etching and the patterned layer of antireflection coating material as a mask. The layer of reflecting material is then patterned using dry etching and the patterned layer of first photoresist as a mask. The patterned layer of first photoresist is then removed.
    Type: Grant
    Filed: December 12, 1996
    Date of Patent: February 16, 1999
    Assignee: Taiwan Semiconductor Manufacturing Company, Ltd.
    Inventors: Chen-Hua Yu, Syun-Ming Jang
  • Patent number: 5861375
    Abstract: The present invention provides novel cyclic tetrapeptides useful in the treatment or prevention of protozoal diseases; in particular, the novel compounds are active against the causative pathogens in malaria, toxoplasmosis, and coccidiosis.
    Type: Grant
    Filed: January 28, 1997
    Date of Patent: January 19, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Christine Lange Cannova, Anne W. Dombrowski, Michael A. Goetz, Sandra J. Rattray, Sheo Bux Singh, Jon Polishook, Gerald F. Bills, Joyce A. Greene, Gary K. Darland
  • Patent number: 5821329
    Abstract: The present invention describes cyclic peptide compounds which modulate integrin mediated adhesion. These compounds can inhibit both .beta..sub.1 and .beta..sub.2 mediated adhesion. The invention further relates to therapeutic uses for these compounds in the treatment of adhesion related pathologies.
    Type: Grant
    Filed: October 28, 1996
    Date of Patent: October 13, 1998
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Thomas J. Lobl, Shiu-Lan Chiang, Wolfgang Scholz, Nancy Delaet, Pina Cardarelli
  • Patent number: 5750509
    Abstract: The present invention is directed to novel antibiotic A 40926 derivatives characterized by having a carboxy, (C.sub.1 -C.sub.4) alkoxy-carbonyl, aminocarbonyl, (C.sub.1 -C.sub.4) alkylaminocarbonyl, di (C.sub.4 -C.sub.4)alkylaminocarbonyl or hydroxymethyl substituent on the N-acylaminoglucuronyl moiety and a hydroxy or a polyamine substituent in position 63 of the molecule. The compounds of the invention show high in vitro activity against glycopeptide resistant Enterococci and Staphylococci.
    Type: Grant
    Filed: April 30, 1996
    Date of Patent: May 12, 1998
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Adriano Malabarba, Romeo Ciabatti, Gianbattista Panzone, Alessandra Maria Marazzi
  • Patent number: 5741775
    Abstract: There are disclosed compounds of the general formula ##STR1## wherein all substituents are defined herein. The compounds are useful as antibiotic and antifungal agents.
    Type: Grant
    Filed: June 13, 1995
    Date of Patent: April 21, 1998
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, James F. Dropinski, Frances Aileen Bouffard
  • Patent number: 5677419
    Abstract: Analogs of porcine Vasoactive Intestinal Peptide are disclosed. The analogs have been cyclized by the covalent attachment, via an amide bond, of the side-chain carboxy terminus of one amino acid in the peptide chain to the side-chain amino terminus of another amino acid in the peptide chain. The claimed compounds are useful for the treatment of asthma.
    Type: Grant
    Filed: September 19, 1994
    Date of Patent: October 14, 1997
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David Robert Bolin, Margaret O'Donnell
  • Patent number: 5629289
    Abstract: Provided are pharmaceutical formulations, and methods of inhibiting fungal and parasitic activity using a compound of formula I: ##STR1## wherein: R.sup.z1 is hydrogen, --CH.sub.2 OH, --CHOHCH.sub.3 or --CHOHCH.sub.2 C(O)NH.sub.2 ;R.sup.z2 is hydrogen, --CH.sub.2 OH or --CHOHCH.sub.3 ;R.sup.z3 is hydrogen or methyl;R.sup.x1 is hydrogen, hydroxy or O--R.sup.x1' ;R.sup.x1' is C.sub.1 -C.sub.6 alkyl, benzyl, --(CH.sub.2).sub.2 Si(CH.sub.3).sub.3, --CH.sub.2 CH.dbd.CH.sub.2, --CH.sub.2 CHOHCH.sub.2 OH, --(CH.sub.2).sub.a COOH, --(CH.sub.2).sub.b NR.sup.w1 R.sup.w2, --(CH.sub.2).sub.c POR.sup.w3 R.sup.w4 or --[(CH.sub.2).sub.2 O].sub.d --(C.sub.1 -C.sub.6)alkyl;a, b and c are independently 1, 2, 3, 4, 5 or 6;R.sup.w1 and R.sup.w2 are independently hydrogen, C.sub.1 -C.sub.6 alkyl, or R.sup.w1 and R.sup.w2 combine to form --CH.sub.2 (CH.sub.2).sub.e CH.sub.2 --;R.sup.w3 and R.sup.w4 are independently hydroxy, or C.sub.1 -C.sub.6 alkoxy;d is 1 or 2;e is 1, 2 or 3;R.sup.x2, R.sup.y1, R.sup.y2, R.sup.y3 and R.sup.
    Type: Grant
    Filed: July 25, 1995
    Date of Patent: May 13, 1997
    Assignee: Eli Lilly and Company
    Inventor: Michael J. Rodriguez
  • Patent number: 5569742
    Abstract: Centrally truncated NPY cyclic peptide analogs are described which have selective bioactivity for NPY Y1 receptors. Methods are provided for diagnosing physiological disorders manifested by abnormal levels of endogenous Y1 receptors, by means of measuring the amount of a NPY Y1 specific cyclic peptide analog which binds to a biological sample, and by means of administering a radiolabelled NPY Y1 specific cyclic peptide analog to a host subject followed by radiographic imaging. A method is further provided for therapeutic use of the cyclic peptide NPY analogs in clinical treatment of hypotension and anorexia.
    Type: Grant
    Filed: June 22, 1994
    Date of Patent: October 29, 1996
    Assignee: The Salk Institute for Biological Studies
    Inventors: Dean A. Kirby, Jean E. F. Rivier
  • Patent number: 5516756
    Abstract: The present invention is directed to novel aza cyclohexapeptide compounds of the formula ##STR1## where all substituents are defined herein, which are useful as antifungal agents and for the treatment of Pneumocystis carinii infections. Compositions containing the compounds of the invention are also disclosed.
    Type: Grant
    Filed: October 31, 1994
    Date of Patent: May 14, 1996
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Frances A. Bouffard, James F. Dropinski
  • Patent number: 5348940
    Abstract: Certain propionitrile compounds which have a cyclohexapeptidyl nucleus and which are found to have antibiotic activity with physical properties suitable for use in therapeutic compositions are described. A novel process for their preparation is also described.
    Type: Grant
    Filed: September 3, 1992
    Date of Patent: September 20, 1994
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Robert A. Zambias
  • Patent number: 5171835
    Abstract: Disclosed herein are analogues of the luteinizing hormone-releasing hormone (LH-RH), which are potent antagonists of LH-RH. These peptides inhibit the release of gonadotropins from the pituitary in mammals, including humans and possess antitumor activity.Formula I represents peptides which are within the scope of this invention:X--R.sup.1 --R.sup.2 --R.sup.3 --Ser--R.sup.5 --R.sup.6 (AY.sub.2)--Leu--Arg--Pro--D--Ala--NH.sub.2 Iand the pharmaceutically acceptable salts thereof, whereinR.sup.1 is D-Phe, D-Phe(4Cl), D-Nal(1) or D-Nal(2),R.sup.2 is D-Phe or D-Phe(4HI),R.sup.3 is D-Trp, D-Phe, D-Phe(4HI), D-Nal(1), D-Nal(2) or D-Pal(3),R.sup.5 is Tyr or Arg,R.sup.6 is D-Lys or D-Orn,HI is fluoro, chloro or bromoX is a lower alkanoyl group of 2-5 carbon atoms,A is a diaminoacyl residue having the formula ##STR1## where m is 0 or 1,n is 0 or 1,Y is Y.sup.1 or Y.sup.2, whereinY.sup.
    Type: Grant
    Filed: January 30, 1991
    Date of Patent: December 15, 1992
    Assignee: The Administrators of the Tulane Educational Fund
    Inventors: Tamas Janaky, Atilla Juhasz, Andrew V. Schally
  • Patent number: 5166135
    Abstract: A method for the treatment of Pneumocystis carinii, the causative agent of pneumonia of particular severity to immune compromised patients such as those with acquired immune deficiency syndrome (AIDS), by administering a lipophilic cyclohexapeptide compound of the general formula ##STR1## wherein the R groups are fully defined in the text, is described. Compositions suitable for the treatment of P. carinii are also disclosed.
    Type: Grant
    Filed: August 9, 1991
    Date of Patent: November 24, 1992
    Assignee: Merck & Company, Inc.
    Inventor: Dennis M. Schmatz
  • Patent number: 5114919
    Abstract: Various cyproheptadine derivatives sensitize multidrug resistant cells to certain chemotherapeutic agents. As such, these cyproheptadine derivatives are useful as adjuncts in the reversal of multidrug resistance in mammalian tumor cells either as compounds, pharmaceutically acceptable salts, or pharmaceutical composition ingredients in combination with anticancer chemotherapeutic agents or compounds.
    Type: Grant
    Filed: February 11, 1991
    Date of Patent: May 19, 1992
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, David C. Remy
  • Patent number: 5084442
    Abstract: Linear and cyclic Growth Hormone Releasing Factor Analogs and a method for stimulating the release of Growth Hormone in subjects by administering to the subject an effective amount of the compounds of the invention.
    Type: Grant
    Filed: September 6, 1988
    Date of Patent: January 28, 1992
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Arthur M. Felix, David C. Fry, Edgar P. Heimer, Vincent S. Madison
  • Patent number: 4758421
    Abstract: A bleomycin conjugate for use in targeting a compound to a body tumor. The conjugate includes an oxidized bleomycin/cobalt(III) complex and the compound to be targeted joined to the complex through a monodentate cobalt/sulfur coordinate bond. Also disclosed are methods for preparing the conjugate, and for targeting the compound to a body tumor, for purposes of tumor radioimaging or therapy.
    Type: Grant
    Filed: March 15, 1985
    Date of Patent: July 19, 1988
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: C. -H. Chang, Claude F. Meares, C.-H Chang
  • Patent number: 4703034
    Abstract: There is disclosed a series of novel cyclic tetrapeptides related to somatostatin. The compounds have surprisingly been found to have the activity of increasing blood glucose when administered. The compounds are prepared using the solid phase or mixed anhydride synthesis methods and compositions and methods utilizing the novel compounds are also disclosed.
    Type: Grant
    Filed: April 28, 1986
    Date of Patent: October 27, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Roger Freidinger, Ruth F. Nutt, Terry A. Lyle, Richard Saperstein