Three Or More Hetero Atoms In The Hetero Ring Patents (Class 514/435)
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Publication number: 20150126437Abstract: The disclosure provides compounds useful as insect repellents, compositions comprising such repellents, and methods of repelling an arthropod using such compounds and compositions. The disclosure further provides insect traps and method for identifying ligands and cognates for biological molecules.Type: ApplicationFiled: October 17, 2012Publication date: May 7, 2015Applicant: The Regents of the University of CaliforniaInventors: Anandasankar Ray, Sean Michael Boyle
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Patent number: 8951992Abstract: The present invention is directed to methods and compounds for inhibiting bacterial growth and treating a bacterial infection in a subject. These methods involve providing an inhibitor of intrabacterial pH homeostasis, including inhibitors of the Mycobacterium tuberculosis Rv3671c gene encoded membrane protease. Methods for identifying novel compounds that disrupt intrabacterial pH homeostasis and their use for inhibiting bacterial growth and treating a bacterial infection in a subject are also disclosed.Type: GrantFiled: July 20, 2009Date of Patent: February 10, 2015Assignee: Cornell UniversityInventors: Carl Nathan, Sabine Ehrt, Omar Vandal, Crystal Darby
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Patent number: 8901170Abstract: Compounds of formula (I) wherein the symbols have the meaning given in the specification, as well as processes for preparing the compounds (I), pesticidal compositions and synergistic mixtures comprising compounds (I), methods for the control of insects, acarids or nematodes by contacting the pests or their food supply, habitat or breeding grounds with a pesticidally effective amount of compounds formula (I), and a method for treating, controlling, preventing or protecting animals against infestation or infection by parasites which comprises orally, topically or parenterally administering or applying to the animals a parasiticidally effective amount of compounds of formula (I).Type: GrantFiled: June 22, 2007Date of Patent: December 2, 2014Assignee: BASF SEInventors: Matthias Pohlman, Michael Hofmann, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Hassan Oloumi-Sadeghi, Takeo Hokama, Christopher Palmer
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Patent number: 8815936Abstract: Described is a composition for preventing or treating an oxidative stress related disease or condition in a subject. The disease or condition is characterized by the presence of excess oxidative compounds in the subject, and the composition includes a synergistic combination of therapeutically effective amounts of resveratrol to promote NAD+ synthesis in the subject; a chelating agent to reduce production of additional oxidative compounds in the subject; and an antioxidant to minimize the oxidative activity in the subject.Type: GrantFiled: March 3, 2009Date of Patent: August 26, 2014Assignee: Nad Life Pty LtdInventors: Ross Stewart Grant, Nady Braidy, Gilles Guillemin, George Smythe
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Patent number: 8476233Abstract: The subject invention pertains to materials and methods for the prevention and treatment of disease conditions associated with oxidative stress or a compromised reducing environment, including inflammatory bowel diseases such as ulcerative colitis. Another aspect of the subject invention concerns compositions formulated for administration as an enema. The subject invention also concerns compositions formulated for oral administration. Methods of the invention include administration of compounds or compositions of the invention. In one embodiment, compounds or compositions of the invention are rectally instilled in a patient. In another embodiment, compounds or compositions are orally administered.Type: GrantFiled: June 13, 2008Date of Patent: July 2, 2013Assignee: Therapeutic Research, LLCInventor: Jay Pravda
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Publication number: 20120208850Abstract: The invention relates to methods, compounds, and compositions for delivering 1,3-propanedisulfonic acid (1,3PDS) in a subject, preferably a human subject. The invention encompasses compounds that will yield or generate 1,3PDS, either in vitro or in vivo. The invention also relates to sulfonate ester prodrugs of 1,3PDS as well as Gemini dimmers and oligomers of 1,3PDS for the prevention or treatment of associated diseases and conditions.Type: ApplicationFiled: August 6, 2010Publication date: August 16, 2012Applicant: BELLUS HEALTH INC.Inventors: Xianqi Kong, Nigel Levens, Abderrahim Bouzide, Stephane Ciblat, Richard Frenette, Johanne Renaud
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Patent number: 8026274Abstract: The subject invention provides a method of treating burn-induced weight loss in a burn patient which comprises administering a therapeutically effective amount of an oxandrolone to the patient. The invention also provides a method of treating a wound in a patient suffering from a wound which comprises administering a therapeutically effective amount of an oxandrolone to the patient. The subject invention further provides a method of treating burn-induced weight loss in a burn patient which comprises administering a therapeutically effective amount of an oxandrolone in conjunction with a protein supplement to the patient.Type: GrantFiled: March 12, 2004Date of Patent: September 27, 2011Assignee: Savient Pharmaceuticals, Inc.Inventor: Don Fishbein
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Publication number: 20100215777Abstract: Compounds of formula (I) wherein the symbols have the meaning given in the specification, as well as processes for preparing the compounds (I), pesticidal compositions and synergistic mixtures comprising compounds (I), methods for the control of insects, acarids or nematodes by contacting the pests or their food supply, habitat or breeding grounds with a pesticidally effective amount of compounds formula (I), and a method for treating, controlling, preventing or protecting animals against infestation or infection by parasites which comprises orally, topically or parenterally administering or applying to the animals a parasiticidally effective amount of compounds of formula (I).Type: ApplicationFiled: June 22, 2007Publication date: August 26, 2010Applicant: BASF SEInventors: Matthias Pohlman, Michael Hofmann, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Hassan Oloumi-Sadeghi, Takeo Hokama, Christopher Palmer
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Patent number: 7144985Abstract: The invention relates to methods of determining islet cell activity by detecting the level of Archipelin or a fragment thereof and comparing the level to a baseline level or range associated with a known islet cell activity. Such methods are useful in diagnosing and studying the development of diabetes.Type: GrantFiled: December 2, 2002Date of Patent: December 5, 2006Assignee: Metabolex, Inc.Inventors: Jeffrey D. Johnson, John E. Blume, John F. Palma, Yun-Ping Zhou
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Patent number: 6825226Abstract: The invention relates to the discovery that specific adamantyl or adamantyl group derivatives containing retinoid-related compounds induce apoptosis of cancer cells and therefore may be used for the treatment of cancer, including advanced cancer. Also, the present invention relates to novel adamantyl or adamantyl group derivatives containing retinoid compounds and their usage for treatment and/or prevention of cancer, keratinization disorders, dermatological conditions, and other therapies More specifically, it has been shown that such adamantyl compounds, e.g., 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoicacid, 2-[3-(1-adamantyl)-4-methoxyphenyl]-5-benzimidazole carboxylic acid, and 6-[3-(1-adamantyl)-4,5-methylenedioxyphenyl]-2-naphthoic acid, can be used to treat or prevent cervical cancers and precancers such as cervical dysplasias, including high grade and low grade dysplasias.Type: GrantFiled: June 24, 2002Date of Patent: November 30, 2004Assignee: Galderma Research & Development, S.N.C.Inventors: Magnus Pfahl, Xian-Ping Lu, Darryl Rideout, Hongyue Zhang
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Patent number: 6727258Abstract: The present invention relates to compounds of formula (IA): the preparation thereof, pharmaceutical formulations thereof, and their use in medicine as allosteric adenosine receptor modulators for uses including protection against hypoxia and ischemia induced injury and treatment of adenosine-sensitive cardiac arrhythmias.Type: GrantFiled: March 19, 2001Date of Patent: April 27, 2004Assignee: King Pharmaceutical Research & Development, Inc.Inventor: Pier Giovanni Baraldi
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Patent number: 6620782Abstract: The present invention is directed to novel 2-aminobenzamide thereof, represented by the general Formula I: where R1-R3, X, and A—D are defined herein. The present invention also relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.Type: GrantFiled: March 16, 2000Date of Patent: September 16, 2003Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Yan Wang
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Patent number: 6548534Abstract: This invention describes the new, nonsteroidal gestagens of general formula I in which A, B, Ar1, R1, R2 and R3 have the meanings that are indicated in more detail in the description. The new compounds show a very great affinity to the gestagen receptor. They can be used alone or in combination with estrogens in contraceptive preparations. In addition, they can be used for treating endometriosis. Together with estrogens, they can also be used in preparations for treating gynecological disorders, for treating premenstrual symptoms and for substitution therapy. Based on the androgenic action, they can also be used for male birth control, male HRT and hormone therapy and for treating andrological disease agents.Type: GrantFiled: July 27, 2001Date of Patent: April 15, 2003Assignee: Schering AktiengesellschaftInventors: Manfred Lehmann, Klaus Schoellkopf, Peter Strehlke, Nikolaus Heinrich, Karl-Heinrich Fritzemeier, Rolf Krattenmacher, Hans-Peter Muhn
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Patent number: 6541506Abstract: The invention features enediynes and methods for their production and use. The enediynes of the invention have the formula: wherein R1 is a hydroxyl group or a moiety that can be replaced by a hydroxyl group in a hydrolysis reaction; each R2 is, independently, H or a monovalent hydrocarbon moiety containing between 1 and 4 carbon atoms, inclusive; R3 is a pyrrole, furan, or thiophene ring; and X is an integer between 4 and 10, inclusive.Type: GrantFiled: October 5, 2000Date of Patent: April 1, 2003Assignee: Phytera IncorporatedInventors: Baoliang Cui, James Bruce McAlpine, Maureen Kelly Talbot, Shu-Wei Yang, Catherine Heintz, Angela Stafford
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Patent number: 6462064Abstract: The invention relates to the discovery that specific adamantyl or adamantyl group derivatives containing retinoid-related compounds induce apoptosis of cancer cells and therefore may be used for the treatment of cancer, including advanced cancer. Also, the present invention relates to novel adamantyl or adamantyl group derivatives containing retinoid compounds and their usage for treatment and/or prevention of cancer, keratinization disorders, dermatological conditions, and other therapies More specifically, it has been shown that such adamantyl compounds, e.g., 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid, 2-[3-(1-adamantyl)-4-methoxyphenyl]-5-benzimidazole carboxylic acid, and 6-[3-(1-adamantyl)-4,5-methylenedioxyphenyl]-2-naphthoic acid, can be used to treat or prevent cervical cancers and precancers such as cervical dysplasias, including high grade and low grade dysplasias.Type: GrantFiled: February 4, 2000Date of Patent: October 8, 2002Assignee: Galderma Research & Development S.N.C.Inventors: Magnus Pfahl, Xian-Ping Lu, Darryl Rideout, Hongyue Zhang
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Patent number: 6221896Abstract: This invention relates to an insecticidal and miticidal composition which contains as active ingredients chlorfenapyr in combination with one or more compounds selected from the group consisting of benzoepin, nereistoxin-type insecticidal agents and diafenthiuron.Type: GrantFiled: May 24, 1999Date of Patent: April 24, 2001Assignee: American Cyanamid Co.Inventor: Toshiki Fukuchi
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Patent number: 6127415Abstract: The present invention relates to specific adamantyl or adamantyl group derivative containing retinoid compounds induce apoptosis of cancer cells. These adamantyl retinoid derivatives are useful for the treatment of many cancers and solid tumors, especially androgen-independent prostate cancer, skin cancer, pancreatic carcinomas, colon cancer, melanoma, ovarian cancer, liver cancer, small cell lung carcinoma, non-small cell lung carcinoma, cervical carcinoma, brain cancer, bladder cancer, breast cancer, neuroblastoma/glioblastoma, and leukemia. Also, the invention relates to novel adamantyl or adamantyl group derivative compounds which are useful as active agents for the treatment or prevention of keratinization disorders and other dermatological conditions, and other diseases.Type: GrantFiled: April 14, 1999Date of Patent: October 3, 2000Assignee: Galderma Research & Development, S.N.C.Inventors: Magnus Pfahl, Xian-Ping Lu, Darryl Rideout, Hongyue Zhang
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Patent number: 5869520Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.Type: GrantFiled: January 8, 1997Date of Patent: February 9, 1999Assignee: Hoechst Marion Roussel, Inc.Inventors: Raymond W. Kosley, Jr., Robert Joseph Cherill, Gerard O'Malley
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Patent number: 5856323Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.Type: GrantFiled: June 7, 1995Date of Patent: January 5, 1999Assignee: CytoMed, Inc.Inventors: Xiong Cai, Sajjat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
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Patent number: 5827876Abstract: This invention relates to 3-(4-acrylamidobenzoyl)benzo?b! thiophenes, to the process for their preparation, to pharmaceutical compositions and to their use for modifying the balance between bone resorption and bone production in a mammal. The compounds useful in this invention are represented by the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl containing 1-8 carbon atoms, or R.sup.1 and R.sup.2 together with the interposed nitrogen forms a 5-7 membered ring optionally containing an additional heteroatom selected from nitrogen, sulfur or oxygen.Type: GrantFiled: April 8, 1997Date of Patent: October 27, 1998Assignee: American Home Products CorporationInventor: Joseph Peter Sabatucci
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Patent number: 5646175Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.Type: GrantFiled: June 1, 1995Date of Patent: July 8, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Raymond W. Kosley, Jr., Robert Joseph Cherill, Gerard O'Malley
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Patent number: 5543427Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.Type: GrantFiled: August 24, 1994Date of Patent: August 6, 1996Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Raymond W. Kosley, Jr., Robert J. Cherill, Gerard O'Malley
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Patent number: 5374650Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.Type: GrantFiled: March 25, 1993Date of Patent: December 20, 1994Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Raymond W. Kosley, Jr., Robert J. Cherill, Gerard O'Malley
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Patent number: 5356925Abstract: Novel N-(mercaptoalkyl)urea or carbamates of the formulae I and II ##STR1## wherein A is a monocyclic or bicyclic arylene or heteroarylene;Q is hydrogen or R.sub.9 CO--;Y is --O--,--S-- or --NR.sub.8 --;R.sub.1 is lower alkyl, cyclolower alkyl, aryl or heteroaryl;R.sub.2 and R.sub.8 are independently hydrogen; lower alkyl; cyclolower alkyl; substituted lower alkyl; aryl; or heteroaryl;R.sup.3 is --OR.sub.5 or --NR.sub.5 R.sub.6 ;R.sub.4 is --(CH.sub.2).sub.q R.sub.7 ; or R.sub.2 and R.sub.4 and the carbons to which they are attached complete a ring;R.sub.5 and R.sub.6 are hydrogen, lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl or aryl lower alkyl, or R.sub.5 and R.sub.Type: GrantFiled: February 11, 1993Date of Patent: October 18, 1994Assignee: Schering CorporationInventors: Bernard R. Neustadt, Alan Bronnenkant
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Patent number: 5140039Abstract: The present invention includes compounds represented by the formula: ##STR1## wherein X is O or S; R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, hydroxy, halo, loweralkoxy, thioalkoxy and loweralkyl; or R.sub.1 and R.sub.2 taken together can form a methylenedioxy or ethylenedioxy bridge;R.sub.3 is loweralkyl;R.sub.4 is selected from ##STR2## wherein Y is O or S, R.sub.6 is hydrogen, methoxy or halo and m is 0 or 1; R.sub.5 is hydrogen, loweralkyl, phenyl or substituted phenyl wherein the phenyl ring is substituted with one, two or three substituents independently selected from loweralkyl, halo, hydroxy, loweralkoxy, amino and thioalkoxy; andR.sub.8 hydrogen or R.sub.3 and R.sub.8 taken together form a pyrrolidine ring; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 31, 1991Date of Patent: August 18, 1992Assignee: Abbott LaboratoriesInventors: John F. DeBernardis, David L. Arendsen, Robert E. Zelle
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Patent number: 5045562Abstract: 1,3,5-trithiane derivatives represented by the formula (I) ##STR1## wherein the substituents are defined herein, are disclosed. The trithiane derivatives and their compositions are useful as anti-arteriosclerotic or anti-hyperlipemic agents.Type: GrantFiled: October 17, 1988Date of Patent: September 3, 1991Assignee: Nihon Nohyaku Co., Ltd.Inventors: Masashi Nagamine, Kunikazu Hiraga, Atsushi Sakai, Matazaemon Uchida
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Patent number: 4942161Abstract: The invention relates to the use of beta blockers for the treatment of the progression of infantile axial myopia.Type: GrantFiled: February 24, 1989Date of Patent: July 17, 1990Inventor: Heinfried Tiburtius
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Patent number: 4816475Abstract: An anti-arteriosclerotic or anti-hyperlipemic 1,3,5-trithiane derivative according to the formula (I): ##STR1## a pharmaceutical composition containing the same, and a process for producing the same.Type: GrantFiled: July 14, 1987Date of Patent: March 28, 1989Assignee: Nihon Nohyaku Co. Ltd.Inventors: Masashi Nagamine, Kunikazu Hiraga, Atsushi Sakai, Matazaemon Uchida
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Patent number: 4804677Abstract: Novel compounds of the general formula ##STR1## wherein R.sub.1 is lower alkyl, lower cycloalkyl, lower alkenyl, lower alkynyl, lower alkyl carboxymethyl, aryl carboxymethyl, aryl, or aralkyl; A is a direct bond, lower alkylene, or lower alkenylene; x is 1 or 2, provided that when x is greater than 1, different occurrences of the ##STR2## group may be the same or different; Ar is heterocyclic unsubstituted aromatic or aromatic substituted with lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy, halogen, acetamido, amino, nitro, lower alkylamino, hydroxy, lower hydroxyalkyl or cyano; W is alkylene containing from 1 to about 10 carbon atoms; and B is --NR.sub.2 COR.sub.3, --NR.sub.2 CONR.sub.3 R.sub.4, --NR.sub.2 SO.sub.2 R.sub.3, --NR.sub.2 SO.sub.2 NR.sub.3 R.sub.4, or --NR.sub.2 COOR.sub.5, wherein R.sub.2, R.sub.3, R.sub.4 and R.sub.5 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, alkoxyaryl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.3 and R.Type: GrantFiled: September 8, 1987Date of Patent: February 14, 1989Assignee: E. I. du Pont de Nemours and CompanyInventors: Paul W. Erhardt, William L. Matier
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Patent number: 4725591Abstract: Compounds having one or two substituents at the 3-position, represented by the general formula ##STR1## wherein R.sub.1 is an optionally acylated or protected amino group and X is hydrogen atom or methoxy group, or a pharmaceutically acceptable salt thereof; when used either alone or in combination with a .beta.-lactam antibiotic, show excellent .beta.-lactamase inhibitory activity and can be used as drugs for use in humans and domestic animals.Type: GrantFiled: February 3, 1984Date of Patent: February 16, 1988Assignee: Takeda Chemical Industries, Ltd.Inventors: Taisuke Matsuo, Mitsuzo Kuno, Kenji Okonogi
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Patent number: 4551472Abstract: Unsymmetrical N-substituted bis-carbamoyl sulfide compounds exhibit exceptional broad spectrum pesticidal activity coupled with extremely low mammalian toxicity and phytotoxicity.Type: GrantFiled: January 9, 1984Date of Patent: November 5, 1985Assignee: Union Carbide CorporationInventor: Themistocles D. J. D'Silva