The Tetracyclo Ring System Consists Of Four Six-membered Cyclos Patents (Class 549/384)
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Patent number: 5789438Abstract: The present invention is directed to steroidal or terpenoidal compounds which inhibit farnesyl-protein transferase (FPTase). The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer.Type: GrantFiled: September 5, 1997Date of Patent: August 4, 1998Assignee: Merck & Co., Inc.Inventors: Sheo B. Singh, Russell B. Lingham, Keith C. Silverman, Deborah L. Zink, Isabel Martin, Fernando Pelaez, Manuel Sanchez
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Patent number: 5783116Abstract: Described are novel pentahydrophenanthro?9,10-b!pyrans and tetrahydrocyclopenta?c!-naphtho?1,2-b!pyrans. Also described are polymeric organic host materials that contain or that are coated with such compounds.Type: GrantFiled: October 16, 1997Date of Patent: July 21, 1998Assignee: PPG Industries, Inc.Inventor: Jibing Lin
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Patent number: 5726186Abstract: The present invention provides compounds of formula I: ##STR1## wherein X is --O-- or --S--,Y is --O--, --S--, --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, or --NR.sup.5 --;R.sup.1, R.sup.2, and R.sup.3 are each independently --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl), --OSO.sub.2 CF.sub.3, Cl, or F;n is 1 or 2;W is CH.sub.2 or C.dbd.O;R.sup.4 is 1-piperidinyl, 2-oxo-1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 2-oxo-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino;R.sup.5 is C.sub.1 -C.sub.3 alkyl, --COC.sub.6 H.sub.5, --CO(C.sub.1 -C.sub.6 alkyl), --C(O)OC.sub.6 H.sub.5, --C(O)O(C.sub.1 -C.sub.6 alkyl), --SO.sub.2 (C.sub.1 -C.sub.6 alkyl), --SO.sub.2 C.sub.6 H.sub.5, or --SO.sub.2 CF.sub.3 ;or a pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: August 13, 1996Date of Patent: March 10, 1998Assignee: Eli Lilly and CompanyInventor: Timothy Alan Grese
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Patent number: 5723631Abstract: The present invention relates to a process for the preparation of a compound of the following structure: ##STR1## wherein, substituents are as defined in the specification.Type: GrantFiled: June 22, 1995Date of Patent: March 3, 1998Assignee: SmithKline Beecham CorporationInventors: Ashok Dharmaji Patil, Robert Philip Hertzberg, Geoffrey B. Dreyer, Alan James Freyer, John W. Westley, Balan Chenera, Michael Leo West
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Patent number: 5674432Abstract: Described are novel reversible photochromic diaryl-3H-naphtho?2,1-b!pyran compounds having a substituted or unsubstituted, five or six member heterocyclic ring fused to the g, i, or l side of the naphthopyran. The heterocyclic ring contains an oxygen or nitrogen atom and is attached to the number 5, 6, 7, 8, 9, or 10 carbon atom of the naphtho portion of the naphthopyran. Also described are organic host materials containing such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline)oxazine-type compounds, are also described.Type: GrantFiled: June 2, 1995Date of Patent: October 7, 1997Assignee: Transitions Optical, Inc.Inventors: David B. Knowles, Barry Van Gemert
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Patent number: 5565147Abstract: Described are novel reversible photochromic diaryl-3H-naphtho[2,1-b]pyran compounds having a substituted or unsubstituted, five or six member heterocyclic ring fused to the g, i, or l side of the naphthopyran. The heterocyclic ring contains an oxygen or nitrogen atom and is attached to the number 5, 6, 7, 8, 9, or 10 carbon atom of the naphtho portion of the naphthopyran. Also described are organic host materials containing such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline)oxazine-type compounds, are also described.Type: GrantFiled: June 2, 1995Date of Patent: October 15, 1996Assignee: Transitions Optical, Inc.Inventors: David B. Knowles, Barry Van Gemert
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Patent number: 5539127Abstract: A steroid compound represented by the formula ##STR1## which has an excellent aromatase-inhibiting effect and is useful for preventing or treating diseases caused by estrogens, such as breast cancer, uterine cancer and prostatomegaly. This compound has an oxygen or nitrogen atom as the heteroatom at the position A of the ring D and the 7-position (substituent R.sup.1) of the skeleton is substituted by --S--R.sup.2 (wherein R.sup.2 represents hydrogen, lower alkyl which may be substituted by hydroxy, amino or lower alkoxycarbonyl, lower alkenyl, aralkyl, aryl which may be substituted by halogen, amino, di(lower alkyl)amino, lower alkoxy or lower alkyl, acyl, or lower alkoxycarbonyl), --S(O)m--R.sub.3 (wherein R.sup.3 represents lower alkyl; and m represents 1 or 2), or aralkyl.Type: GrantFiled: March 24, 1995Date of Patent: July 23, 1996Assignee: Teikoku Hormone Mfg. Co., Ltd.Inventors: Naoyuki Koizumi, shigehiro Takegawa, Shigeki Iwashita, Tomoko Kawachi, Fumiko Inoue, Seijiro Honma, Hiroo Takahashi, Mamoru Mieda, Kaoru Ueda, Kenyu Shibata
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Patent number: 5519051Abstract: Compounds are described having the formula ##STR1## wherein A denotes C.dbd.O, CH.sub.2, C.dbd.CH.sub.2 or C.dbd.CH-lower alkyl;B denotes O, NH or N-lower alkyl;X does not exist, or denotes C.dbd.O or CH.sub.2 ;n denotes 2 or 3 when X does not exist, or denotes 1 or 2 when X denotes C.dbd.O or CH.sub.2 ; andthe broken line between the 1- and 2-positions of the steroid skeleton means that a double bond may optionally exist there. These compounds have an aromatase inhibition action and are useful for prophylaxis or treatment of diseases caused by excess of estrogens, for example, breast cancer, uterine cancer, prostatic hypertrophy, etc.Type: GrantFiled: September 28, 1993Date of Patent: May 21, 1996Assignee: Teikoku Hormone Mfg. Co., Ltd.Inventors: Naoyuki Koizumi, Shigehiro Takegawa, Shigeki Iwashita, Tomoko Kawachi, Teruaki Matsui, Seijiro Honma, Hiroo Takahashi, Mamoru Mieda, Koichi Minato, Kenyu Shibata, Mitsuteru Numazawa
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Patent number: 5514817Abstract: Described are novel reversible photochromic phenanthropyran compounds, examples of which are substituted 2H-phenanthro 4,3-b!pyran and 3H-phenanthro 1,2-b!pyran compounds. The 2H-phenanthropyran compounds have certain substituents at the number 5 and 6 carbon atoms of the phenanthro portion of the phenanthropyran and at the 2 position of the pyran ring. Certain substituents may also be present at the number 7, 8, 9, 10, 11, or 12 carbon atoms of the phenanthro portion of the phenanthropyran. The 3H-phenanthropyran compounds have certain substituents at the number 11 and 12 carbon atoms of the phenanthro portion of the phenanthropyran and at the 3 position of the pyran ring. Certain substituents may also be present at the number 5, 6, 7, 8, 9, or 10 carbon atoms of the phenanthro portion of the phenanthropyran. Also described are polymeric organic host materials that contain or that are coated with such compounds.Type: GrantFiled: August 4, 1994Date of Patent: May 7, 1996Assignee: PPG Industries, Inc.Inventor: David B. Knowles
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Patent number: 5504103Abstract: 17.beta.-hydroxywortmannin and certain of its analogs are inhibitors of phosphatidylinositol 3-kinase. The compounds are particularly useful for inhibiting phosphatidylinositol 3-kinase in mammals and for treating phosphatidylinositol 3-kinase-dependent conditions, especially neoplasms, in mammals.Type: GrantFiled: August 25, 1993Date of Patent: April 2, 1996Assignee: Eli Lilly and CompanyInventors: Rosanne Bonjouklian, Jeffrey A. Dodge, Chris J. Vlahos
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Patent number: 5464567Abstract: Described are novel reversible photochromic naphthopyran compounds which have two phenyl moieties adjacent to each oxygen of each pyran ring. The substituents on each pair of phenyl moieties mirror one another when the phenyl groups are substituted. The naphthodipyrans are prepared from .beta.,.beta.-dihydroxynaphthalene compounds.Type: GrantFiled: April 8, 1994Date of Patent: November 7, 1995Assignee: Transitions Optical, Inc.Inventors: David B. Knowles, Barry V. Gemert
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Patent number: 5416089Abstract: Anticancer compounds of formula I: ##STR1## and pharmaceutically acceptable salts thereof, wherein: R.sup.1, R.sup.2 and R.sup.3 are independently selected H, CH.sub.3, NH.sub.2, NO.sub.2, and CN;R.sup.9 and R.sup.10 are H or alkyl or halo, X.sup.1 and Y.sup.1 or X.sup.2 and Y.sup.2, when present, join together to form, independently, a six membered 1N heterocycle substituted with 1-2 R.sup.3 ; or the group: ##STR2## wherein one of W or Z is C.dbd.O and the other is C.dbd.O, NH, S or O; or when X.sup.2 and Y.sup.2 are not joined together and when R.sup.2 is in the 4-position, then X.sup.2 and R.sup.2 may join together to form an ethylene bridge; are disclosed.Type: GrantFiled: June 24, 1993Date of Patent: May 16, 1995Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Arthur D. Patten, Gregory Pacofsky, Steven P. Seitz, Emeka A. Akamike, Robert J. Cherney, Robert F. Kaltenbach, III, Michael J. Orwat
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Patent number: 5168100Abstract: Disclosed are novel HP530 compounds, their derivatives or their pharmaceutically permissible salts, a process for preparing them and an antitumor substances containing them as active ingredient. The HP530 compounds and their derivatives expressed by the general formula below can be prepared by cultivating Streptomyces sp. HP530 (FERM BP-2786) or and chemically derivation. ##STR1## where X is a C.sub.2 -C.sub.4 acyl group or a hydrogen atom, Y is a C.sub.2 -C.sub.4 acyl group or a hydrogen atom and Z is a group expressed by the formula (II), (III) or (IV).Type: GrantFiled: March 12, 1991Date of Patent: December 1, 1992Assignee: Sapporo Breweries LimitedInventors: Naoki Abe, Nobuyasu Enoki, Yasukazu Nakakita, Hideaki Uchida, Ryoichi Sato, Suguru Takeo, Nobuhiro Watanabe
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Patent number: 5104985Abstract: Novel labdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: May 28, 1991Date of Patent: April 14, 1992Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Raymond W. Kosley, Jr., Robert J. Cherill
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Patent number: 5066817Abstract: Disclosed are DC115A compounds represented by the following general formula: ##STR1## wherein R represents ethyl, propyl or 1-propenyl, and which have antibacterial and anti-tumor activity. DC115A compounds are produced by culturing a microorganism belonging to the genus Streptomyces.Type: GrantFiled: April 30, 1990Date of Patent: November 19, 1991Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Hirofumi Nakano, Mitsunobu Hara, Tsuyoshi Mokudai, Isao Kawamoto, Mayumi Yoshida, Eiji Kobayashi
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Patent number: 5061695Abstract: An antitumor substance BE-12406 or a pharmaceutically acceptable salt thereof, which is represented by the general formula ##STR1## and a method of producing the novel substance.Type: GrantFiled: January 30, 1990Date of Patent: October 29, 1991Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Hiroyuki Suda, Katuhisa Kojiri, Akira Okura, Koutaro Funaishi, Kenji Kawamura, Masanori Okanishi
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Patent number: 5051519Abstract: Novel terpene hydroquinones have been isolated from the marine sponge Strongylophora hartmanii. These compounds have been found to have antiviral and antitumor activity. Thus, these compounds, and derivatives thereof, can be used to treat human and animal tumors as well as viral infections. Additionally, the subject invention concerns the discovery that the terpene hydroquinone known as aureol has strong antiviral activity.Type: GrantFiled: February 16, 1990Date of Patent: September 24, 1991Assignee: Harbor Branch Oceanographic Institution, Inc.Inventors: Amy E. Wright, Sue S. Cross, Neal Burres, Frank Koehn
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Patent number: 5041558Abstract: An accelerator of the activity of hydrolase consisting of a coordination compound or a metal complex containing, as a ligand, an organic cyclic compound with carbonyl groups adjacent to each other in the structure shown in the following general formula I that are substantially in the same plane as each other; ##STR1## (wherein A is the cyclic compound moiety.Type: GrantFiled: April 10, 1987Date of Patent: August 20, 1991Assignee: Sekisui Kagaku Kogyo Kabushiki KaishaInventor: Hideo Anraku
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Patent number: 5034531Abstract: Novel polycyclic pyranyl compounds, pharmaceutical compositions, and their use as anti-viral agents are disclosed.Type: GrantFiled: December 23, 1988Date of Patent: July 23, 1991Assignee: Schering CorporationInventors: Richard J. Friary, John H. Schwerdt, Ashit K. Ganguly
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Patent number: 4954641Abstract: An antibiotic substance represented by formula (I) ##STR1## or a pharmaceutically acceptable salt thereof, which is produced by cultivating a microorganism belonging to the genus Streptomyces and isolating the substance from the cultured cells.Type: GrantFiled: January 30, 1989Date of Patent: September 4, 1990Assignee: Meiji Seika Kaisha, Ltd.Inventors: Yoshikazu Sato, Hiroomi Watabe, Shigetaka Ishii, Tadashi Nakazawa, Takashi Shomura, Masaji Sezaki, Shinichi Kondo
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Patent number: 4927848Abstract: A new antibiotic having the chromophore structure of the pluramycin family of antibiotics is produced by fermentation of Streptomyces ciolaceus ATCC 53807. The new antibiotic designated BU-3839T, exhibits potent antibacterial activity and also inhibits the growth of tumors in experimental animal systems.Type: GrantFiled: September 19, 1988Date of Patent: May 22, 1990Assignee: Bristol-Myers CompanyInventors: Masataka Konishi, Keiko Shimizu, Masaru Ohbayashi, Koji Tomita, Takeo Miyaki, Toshikazu Oki
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Patent number: 4853410Abstract: Racemic and chiral (2R,4R)-4-c-hydroxy-2-4-(substituted)chroman(and thiochroman)-4-acetic acids and their pharmaceutically acceptable salts, their use in the treatment of diabetic complications and intermediates therefor.Type: GrantFiled: October 9, 1987Date of Patent: August 1, 1989Assignee: Pfizer Inc.Inventor: Christopher A. Lipinski
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Patent number: 4847387Abstract: The present invention relates to novel compounds DC-92B and DC-92D having anthraquinone moiety and represented by the following planar structural formula (I) and to a process for producing the same. These compounds can be produced by culture of a microorganism belonging to the genus Actinomadura, and are useful as medicaments because of their antibacterial and anti-tumor activities.Type: GrantFiled: March 17, 1988Date of Patent: July 11, 1989Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Hirofumi Nakano, Isami Takahashi, Fusao Tomita, Kozo Asano, Toru Yasuzawa, Tadashi Ashizawa, Keiichi Takahashi
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Patent number: 4452991Abstract: A method of treating or preventing viral infections, in particular rhinovirus infections comprising the administration of an effective amount of a flavan derivative of formula (I). ##STR1## Pharmaceutical compositions containing these compounds, and some novel compounds are also disclosed.Type: GrantFiled: April 9, 1981Date of Patent: June 5, 1984Inventors: John F. Batchelor, Jeremy G. Vinter, Harold F. Hodson