Naphtho-pyrans (including Hydrogenated) Patents (Class 549/389)
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Patent number: 5384414Abstract: Benzopyran derivatives of the formula: ##STR1## wherein R.sup.1a is hydrogen, C1-4 alkyl or C1-4 alkoxy; or two R.sup.1a taken together with 7th- and 8th-carbon to which they are attached form a C6 carbocyclic ring;R.sup.2a is hydrogen, C1-4 alkyl or C1-4 alkoxy;R.sup.3a is hydrogen, C2-4 acyl or benzoyl;na is 1-3;Ya is C1-7 alkylene, C2-7 alkenylene or C2-7 alkynylene;Ma isi) bond orii) a group of the formula: --Da--Ba--;Da isi) --O-- orii) --S--;Ba isi) C1-4 alkylene orii) a group of the formula: ##STR2## Za is i) bond,ii) --OCO--,iii) CONR.sup.9a --,iv) --COO--,v) --NR.sup.9a CO--,vi) --O-- orvii) --NH--CO--NH--;Wa is a group of the formula: --W1a--Aa--W2 a--;Aa isi) bond orii) a group of the formula: --Ea-- .circle.Ga --;Ea isi) bond,ii) --O-- oriii) --S--;.circle.Ga is C4-10 carbocyclic or heterocyclic ring; or C4-10 carbocyclic or heterocyclic ring substituted by one to three C1-4 alkyl, C1-4 alkoxy, halogen, a group of the formula: --COOR.sup.Type: GrantFiled: August 18, 1993Date of Patent: January 24, 1995Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Shuichi Ohuchida, Masaaki Toda, Tsumoru Miyamoto
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Patent number: 5378699Abstract: Methods of treating an immune disease, cell proliferation, restenosis and vascular smooth muscle cells using the pharmaceutical compounds of the formula ##STR1## in which R.sup.2 is phenyl, naphthyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted, or R.sup.2 is furanyl optionally substituted with C.sub.1-4 alkyl; and salts thereof.Type: GrantFiled: February 5, 1993Date of Patent: January 3, 1995Assignees: Lilly Industries Limited, Eli Lilly and CompanyInventors: Michael Brunavs, Colin P. Dell, Peter T. Gallagher, William M. Owton, Jai P. Singh, Colin W. Smith
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Patent number: 5369158Abstract: Described are novel reversible photochromic naphthopyran compounds substituted at the number eight carbon atom on the naphtho portion of the naphthopyran ring with, for example, a methoxy group. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds are also described.Type: GrantFiled: June 2, 1993Date of Patent: November 29, 1994Assignee: Transitions Optical, Inc.Inventor: David B. Knowles
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Patent number: 5356933Abstract: Novel compounds having the structural formula ##STR1## and pharmaceutically acceptable salts and prodrugs thereof, wherein one of R.sup.1 and R.sup.2 is hydrogen and the other is --CH.dbd.CHCOOH, X is >CH--, and Y is --0--; or, alternatively, the bond between X and Y is not present, X is --CH.sub.2 --, and Y is --OH, as well as methods for their use, pharmaceutical compositions containing the same, and a process for their preparation via fermentation.Type: GrantFiled: June 28, 1993Date of Patent: October 18, 1994Assignee: Abbott LaboratoriesInventors: Gregory M. Brill, James B. McAlpine, Ronald R. Rasmussen
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Patent number: 5350864Abstract: The subject matter of the present invention relates to aminoalkylcarbamates of forskolin and the methods of using these compounds. Specifically, the aminoalkylcarbamates may be utilized in the synthesis of forskolin derivatives. The final derivatives may, in turn, be used in the development of in vivo and in vitro assays designed to study different proteins.Type: GrantFiled: May 3, 1990Date of Patent: September 27, 1994Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Kenneth B. Seamon, Joan Robbins, Antonio Laurenza
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Patent number: 5302730Abstract: This invention relates to a process for the preparation of a 6,7-diacyl-7-deacetylforskolin derivative represented by the general formula: ##STR1## wherein R.sup.1 and R.sup.2 each stands for an acyl group and R.sup.3 stands for an aliphatic group having 2 to 3 carbon atoms, which comprises eliminating the acyl group at position 1 in a 1,6,7-triacyl-7-deacetylforskolin derivative represented by the general formula: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, by solvolysis. The compound of the formula (I) is expected as medicine.Type: GrantFiled: June 4, 1993Date of Patent: April 12, 1994Inventors: Tochiro Tatee, Akira Shiozawa, Hirotaka Yamamoto, Yuh-ichiro Ichikawa, Aya Narita, Chikara Komuro, Kazuhisa Narita
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Patent number: 5284868Abstract: A pharmaceutical compound of the formula ##STR1## in which n is 0, 1 or 2 and R.sup.1 is attached at any of the positions 5, 6, 7, 8, 9 or 10, and each R.sup.1 is halo, trifluoromethyl, C.sub.1-4 alkoxy, hydroxy, nitro, C.sub.1-4 alkyl, C.sub.1-4 alkylthio, hydroxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkoxy, trifluoromethoxy, carboxy, --COOR.sup.5 where R.sup.5 is an ester group, --CONR.sup.6 R.sup.7 or --NR.sup.6 R.sup.7 where R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl; R.sup.2 is phenyl, naphthyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted, or R.sup.2 is furanyl optionally substituted with C.sub.1-4 alkyl; R.sup.3 is nitrile, carboxy, --COOR.sup.8 where R.sup.8 is an ester group, --CONR.sup.9 R.sup.10 where R.sup.9 and R.sup.10 are each hydrogen or C.sub.1-4 alkyl, or R.sup.11 SO.sub.2 -- where R.sup.11 is C.sub.1-4 alkyl or optionally substituted phenyl; and R.Type: GrantFiled: September 25, 1992Date of Patent: February 8, 1994Assignees: Eli Lilly and Company, Lilly Industries LimitedInventors: Colin P. Dell, Jai P. Singh, Colin W. Smith
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Patent number: 5274132Abstract: Described are novel reversible photochromic naphthopyran compounds, examples of which are 3-aryl-3-arylalkenyl naphthopyrans. Also described are organic host materials that contain or that are coated with 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) type compounds, are also described.Type: GrantFiled: September 30, 1992Date of Patent: December 28, 1993Assignee: Transitions Optical, Inc.Inventor: Barry VanGemert
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Patent number: 5268471Abstract: Process for the preparation of 6-acyl-, 7-acyl- or 6,7-diacyl analogues of forskolin of the general formula ##STR1##Type: GrantFiled: January 15, 1993Date of Patent: December 7, 1993Assignee: Hoechst AktiengesellschaftInventors: Noel J. de Souza, Premanand D. Desai, Shrikant V. Savanur, Jurgen Blumbach
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Patent number: 5266709Abstract: Benzopyran derivatives of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof possess the inhibitory activity on Maillard reaction and an antioxidizing effect, and therefore, are useful for the prevention and treatment of several diabetic complications, diseases induced by aging and several diseases caused by formation of peroxidized fat.Type: GrantFiled: August 28, 1992Date of Patent: November 30, 1993Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Shuichi Ohuchida, Masaaki Toda, Tsumoru Miyamoto
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Patent number: 5252598Abstract: The present invention relates to labdane-derivatives of the formula ##STR1## a process for their preparation and the use of these substances as medicaments, preferably as medicaments having a positive ionotropic effect, an effect of lowering intraocular pressure and lowing blood pressure.Type: GrantFiled: May 4, 1992Date of Patent: October 12, 1993Assignee: Hoechst AktiengesellschaftInventors: Yatendra Khandelwal, Greta Moraes, Bansi Lal, Vijay A. Aroskar, Alihussein N. Dohadwalla, Richard H. Rupp
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Patent number: 5250682Abstract: Process for the manufacture of 6.beta.Type: GrantFiled: July 22, 1991Date of Patent: October 5, 1993Assignee: Hoechst AktiengesellschaftInventors: Yatendra Khandelwal, Bansi Lal, Jurgen Blumbach
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Patent number: 5247097Abstract: Novel oxolabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: May 28, 1992Date of Patent: September 21, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventor: Nicholas J. Hrib
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Patent number: 5247100Abstract: A process for the production of sclareolide from sclareol comprising the steps ofA) oxidatively degrading sclareol to a reaction product which is one or both of the following compounds: ##STR1## using either a hypochlorite salt in the presence of a ruthenium salt or potassium permanganate, andB) oxidizing the above reaction product with a peracid or salt thereof to form sclareolide.The above process results in good yields and much shorter reaction times than prior art processes.Type: GrantFiled: June 22, 1992Date of Patent: September 21, 1993Assignee: Henkel Kommanditgesellschaft auf AktienInventors: Thomas Gerke, Klaus Bruns
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Patent number: 5245052Abstract: A process for the manufacture of a 6-acyl-7-deacetylforskolin derivative represented by formula (I) ##STR1## by reacting a 7-acyl-7-deacetylforskolin derivative represented by formula (II) ##STR2## with a strong base in an aprotic solvent.Type: GrantFiled: July 19, 1991Date of Patent: September 14, 1993Assignees: Nippon Kayaku Co. Ltd., Hoechst Japan LimitedInventors: Tochiro Tatee, Tatsuo Sugioka
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Patent number: 5244602Abstract: Described are novel reversible photochromic naphthopyran compounds substituted on the naphthyl portion at the carbon atom juxtaposed to the oxygen of the pyran ring with, for example, an acetoxy group. Also described are organic host materials that contain or that are coated with 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(indolino)-oxazine type compounds, are also described.Type: GrantFiled: December 3, 1990Date of Patent: September 14, 1993Assignee: PPG Industries, Inc.Inventor: Barry Van Gemert
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Patent number: 5238981Abstract: Described are novel reversible photochromic naphthopyran compounds substituted at the number eight carbon atom on the naphtho portion of the naphthopyran ring with, for example, a methoxy group. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds are also described.Type: GrantFiled: February 24, 1992Date of Patent: August 24, 1993Assignee: Transitions Optical, Inc.Inventor: David B. Knowles
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Patent number: 5232943Abstract: Antibiotic Mer-AF1032A represented by the following formula (I) and its isomer antibiotic Mer-AF1032B are disclosed. Also disclosed are a method for preparing the antibiotics comprising the cultivation of a strain belonging to genus Penicillium and a pharmaceutical composition comprising one of these antibiotics and useful as an antifungal agent.Type: GrantFiled: May 20, 1992Date of Patent: August 3, 1993Assignee: Mercian CorporationInventors: Hitosi Agematu, Yoshio Watanabe, Hiroyuki Chiba, Rei Kaneto, Norio Shibamoto, Takeo Yoshioka, Toshihiko Kumamoto, Hiroshi Nishida, Rokuro Okamoto
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Patent number: 5212323Abstract: Disclosed in a process for producing 6-(3-dimethylaminopropionyl)forskolin, comprising the sequential steps of:(1) acetylating hydroxy groups in the 1-position and 7-position of a compound represented by the formula (III): ##STR1## to prepare 1-acetyl-6-(3-dimethylaminopropionyl)-forskolin represented by the formula (II): ##STR2##(wherein Ac represents acetyl group), and (2) selectively removing the acetyl group in the 1-position of the compound represented by the formula (II) in the presence of an amine represented by the formula (IV): ##STR3##(wherein R.sub.1 represents hydrogen atom or lower alkyl group having 1-6 carbon atoms, and R.sub.2 represents lower alkyl group having 1-6 carbon atoms, alkoxyalkyl group, aminoalkyl group or benzyl group) in a solvent to prepare 6-(3-dimethylaminopropionyl)forskolin represented by the formula (I): ##STR4##(wherein Ac represents the same as defined in the formula (II)).The compound (I) is promising as a therapeutic agent for cardiac failure.Type: GrantFiled: October 24, 1991Date of Patent: May 18, 1993Assignee: Nippon Kayaku Kabushiki KaishaInventors: Akihiro Mashiba, Yutaka Ogawa
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Patent number: 5206241Abstract: Labdanes of the formula ##STR1## a process for their manufacture, pharmaceutical preparations containing an effective amount of these compounds and their use for the manufacture of a pharmaceutical preparation for treatment of cardiovascular diseases and high intraocular pressure.Type: GrantFiled: March 14, 1991Date of Patent: April 27, 1993Assignee: Hoechst AktiengesellschaftInventors: Yatendra Khandelwal, Rajeshwari Kannan, Bansi Lal, Ramanujam Rajagopalan, Vijay A. Aroskar, deceased AliHussein N. Dohadwalla, Rashida A. Dohadwalla, Anis S. Dohadwalla, Samina A. Dohadwalla, Richard H. Rupp
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Patent number: 5200116Abstract: Described are a series of novel photochromic benzopyran and naphthopyran compounds substituted with (1) a cyclopropyl group and (2) a phenyl, substituted phenyl, or 5-member aromatic heterocyclic group at the 2-position of the benzopyran or naphthopyran ring. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic or plano lenses that incorporate the novel pyran compounds or combinations of the novel pyran compounds with other complementary photochromic compounds are described.Type: GrantFiled: July 23, 1990Date of Patent: April 6, 1993Assignee: PPG Industries, Inc.Inventor: Harry G. Heller
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Patent number: 5191092Abstract: Iso- and heterocyclic phenylsulphonamides can be prepared by reaction of corresponding iso- and heterocyclic amines with phenylsulphonic acid derivatives. The iso- and heterocyclic phenylsulphonamides have thrombocyte aggregation-inhibiting and thromboxane A.sub.2 antagonist action and can be used in medicaments.Type: GrantFiled: September 26, 1990Date of Patent: March 2, 1993Assignee: Bayer AktiengesellschaftInventors: Ulrich Niewohner, Franz-Peter Hoever, Elisabeth Perzborn, Volker-Bernd Fiedler, Peter Norma, Hilary P. Francis, Marie G. McKenniff
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Patent number: 5182298Abstract: This invention relates to compounds of structural formula (I) ##STR1## which are useful as Cholestrol lowering agents.Type: GrantFiled: March 18, 1991Date of Patent: January 26, 1993Assignee: Merck & Co., Inc.Inventors: Gregory L. Helms, Wendy S. Horn, E. Tracy T. Jones, David L. Linemeyer
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Patent number: 5169957Abstract: Benzopyran derivatives of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof possess the inhibitory activity on Maillard reaction and an antioxidizing effect, and therefore, are useful for the prevention and treatment of several diabetic complications, diseases induced by aging and several diseases caused by formation of peroxidized fat.Type: GrantFiled: July 26, 1991Date of Patent: December 8, 1992Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Shuichi Ohuchida, Masaaki Toda, Tsumoru Miyamoto
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Patent number: 5166217Abstract: This invention relates to methods for inhibiting fungal growth employing compounds of formula (I) ##STR1##Type: GrantFiled: November 26, 1991Date of Patent: November 24, 1992Assignee: Merck & Co., Inc.Inventors: Kenneth F. Bartizal, Walter Rozdilsky, Wendy S. Horn
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Patent number: 5155029Abstract: Described is a microbiological method for producing the cyclic ether having the chemical structure: ##STR1## using a sclareol derivative having one of the structures: ##STR2## and using the microorganism: Cryptococcus laurentii, ATCC 20920.Type: GrantFiled: July 20, 1990Date of Patent: October 13, 1992Assignee: International Flavors & Fragrances Inc.Inventors: Mohamad I. Farbood, James A. Morris, Arthur E. Downey
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Patent number: 5151529Abstract: A series of new compounds, called "the phomactins" is provided and may be isolated from the culture broth of fungi of the genus Phoma, especially Phoma sp. SANK 11486 (No. FERM BP-2598). These compounds are platelet activating factor antagonists and may be used for the treatment of disorders for which known such agents may also be used.Type: GrantFiled: October 10, 1990Date of Patent: September 29, 1992Assignee: Sankyo Company, LimitedInventors: Aiya Sato, Michihiro Sugano, Kouhei Furuya, Takeshi Oshima, Harumitsu Kuwano, Tadashi Hata, Hideyuki Haruyama
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Patent number: 5145855Abstract: Novel forskolin derivatives, intermediates and processes for the preparation thereof, and methods for treating cardiac failure and memory deficit utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: November 15, 1991Date of Patent: September 8, 1992Assignee: Hoechst Roussel Pharmaceuticals, Inc.Inventors: Raymond W. Kosley, Jr., Bettina Spahl
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Patent number: 5130332Abstract: Novel oxolabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: February 11, 1991Date of Patent: July 14, 1992Assignee: Hoechst Roussel Pharmaceuticals Inc.Inventor: Nicholas J. Hrib
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Patent number: 5116954Abstract: Substituted six-membered benzo-fused heterocycles of the formula (I) ##STR1## in which: X=0, NH, S.fwdarw.(O).sub.n (n=0 or 2);R.sub.1 is phenyl, phenyl substituted by methoxy, hydroxy, chlorine, fluorine, diethylaminoethoxy, phenoxy, 2-methyl-4-thiazolyl, 2-amino-4-thiazolyl, phenyl, amino, nitro, terbutyl, carboxymethyl, acetamido, dimethyltriazenyl, benzoyl, hexyl, undecyl, trifluoromethyl, carbamoyl; or R.sub.1 is trifluoromethyl, pyridyl-2,pyridyl-4;R.sub.2 is H, methoxy, hydroxy; orR.sub.1 and R.sub.2 are --CH.dbd.CH--CH.dbd.CH--;R.sub.3 and R.sub.4 are methoxy, hydroxy, fluorine or form a fused benzene ring;CR.sub.5 R.sub.6 R.sub.7 is carboxymethyl, --CH.sub.2 --PO.sub.3 H,--CH.sub.2 --PO(oET).sub.2, 4-methylpiperazinyl, aminomethyl,3-4-5-trimethoxyphenylaminomethyl, acetyl, bromoacetyl, hydroxyethyl, acetoxyethyl, mercaptomethyl, acetylthiomethyl, methoxy-carbopnylthiomethyl, --CH--CONH.sub.2, ##STR2## substituted thiazolyl, subsituted furanone, imidazo(1,2-a)pyridinyl, indolizinyl, or R.sub.4 and R.Type: GrantFiled: August 2, 1989Date of Patent: May 26, 1992Assignee: Lipha, Lyonnaise Industrielle PharmaceutiqueInventors: Philippe Briet, Jean-Jacques Berthelon, Francois Collonges
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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: 5093336Abstract: Novel forskolin derivatives, intermediates and processes for the preparation thereof, and methods for treating cardiac failure and memory deficit utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: July 6, 1989Date of Patent: March 3, 1992Assignee: Hoechat-Roussel Pharmaceuticals, Inc.Inventors: Raymond W. Kosley, Jr., Bettina Spahl
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Patent number: 5093331Abstract: The present invention relates to polyoxygenated labdane-derivatives of the formula ##STR1## a process for their preparation and the use of these substances as medicaments, preferably as medicaments having a positive inotropic effect, an effect of lowering intraocular pressure and lowering blood pressure.Type: GrantFiled: October 9, 1990Date of Patent: March 3, 1992Assignee: Hoechst AktiengesellschaftInventors: Bansi Lal, Ashok K. Gangopadbya, Alihussein N. Dohadwalla, Ramanujam Rajgopalan, Richard H. Rupp
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Patent number: 5081264Abstract: A compound of formula (I): ##STR1## wherein R.sub.1 represents hydrogen, hydroxy or acetoxy and R.sub.2 represents hydroxy or acetoxy.The compounds are capable of protecting the nerve cells and also antagonistic activity against N-methyl-D-aspartic acid receptors.They may be prepared by fermentation of a microorganism of the genus Verticillium or a mutant thereof.Type: GrantFiled: September 18, 1990Date of Patent: January 14, 1992Assignee: Kyowa Hakko Kabushiki KaishaInventors: Shinichiro Toki, Mika Nozawa, Mayumi Yoshida, Hiroshi Sano, Katsuhiko Ando, Isao Kawamoto, Yuzuru Matsuda, Junichi Ikeda, Kazuhiro Kubo
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Patent number: 5077417Abstract: Process for the preparation of polycyclic ethers of formula ##STR1## wherein X represents --(CH.sub.2).sub.n --, index n stands for integer 0 or 1, symbol R.sup.4 designates a hydrogen atom or a methyl radical, symbols R.sup.1 and R.sup.2, identical or different, represent each a hydrogen atom or a lower alkyl radical from C.sub.1 to C.sub.3 and R designates either a C.sub.1 to C.sub.6 linear or branched alkyl radical, or a substituted or unsubstituted alkylene radical having 2 or 3 carbon atoms in the main chain, said alkylene radical forming a ring such as indicated by the dotted line, which process comprises the cyclization by means of an acidic agent of an unsaturated compound:a) of formula ##STR2## having a double bond in one of the positions indicated by the dotted lines, and wherein index m defines an integer number equal to 1 or 2, symbol R.sup.Type: GrantFiled: June 15, 1990Date of Patent: December 31, 1991Assignee: Firmenich SAInventors: Karl-Heinrich Schulte-Elte, Roger L. Snowden, Claudio Tarchini, Beatrice Baer, Christian Vial
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Patent number: 5066818Abstract: Described are novel reversible photochromic naphthopyran compounds having at least one ortho substituted phenyl group at the 3-position of the pyran ring. Also described are organic host materials that contain or that are coated with 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(indolino)-oxazine type compounds, are also described.Type: GrantFiled: March 7, 1990Date of Patent: November 19, 1991Assignee: PPG Industries, Inc.Inventors: Barry V. Gemert, Maria P. Bergomi
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Patent number: 5055598Abstract: Benzopyran derivatives of the formula: ##STR1## wherein the variables are defined in the specification and the pharmaceutically acceptable acid addition salts thereof possess the inhibitory activity on Maillard reaction and an antioxidizing effect, and therefore, are useful for the prevention and treatment of several diabetic complications, diseases induced by aging and several diseases caused by formation of peroxidized fat.Type: GrantFiled: March 12, 1990Date of Patent: October 8, 1991Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Shuichi Ohuchida, Masaaki Toda, Tsumoru Miyamoto
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Patent number: 5043350Abstract: Benzo-fused cycloalkane and oxa- and thia- cycloalkane trans-1,2-diamine compounds of the formula: ##STR1## wherein A, B, C, D, n, X, Y, R, R.sup.1, R.sup.2 and R.sup.3 are as defined in the specification, e.g., trans-3,4-dichloro-N-methyl-N-[2-(pyrrolidin-1-yl)-5-methoxy-1,2,3,4-tetra hydronaphth-1-yl]benzeneacetamide, and the pharmaceutically acceptable salts or N-oxides thereof, are useful as analgesics and/or diuretics.Type: GrantFiled: December 21, 1989Date of Patent: August 27, 1991Assignee: Du Pont Merck Pharmaceutical CompanyInventors: Penio Pennev, Parthasarathi Rajagopalan, Richard M. Scribner
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Patent number: 5041565Abstract: Novel hydrazinocarbonyloxylabdanes, intermediates and processes for the preparation thereof, and a method for treating cardiac failure utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: August 30, 1989Date of Patent: August 20, 1991Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Raymond W. Kosley, Jr., Gerard J. O'Malley
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Patent number: 5008407Abstract: A method of regioselectively and stereoselectively synthesizing forskolin (8,13-epoxy-1.alpha.,6.beta.,7.beta.,9.alpha.-tetrahydroxylabd-14-en-11-on e) from 9-deoxyforskolin (8,13-epoxy-1.alpha.,6.beta.,7.beta.-trihydroxylabd-14-en-11-one) with a good yield is described. In a preferred embodiment, it comprises an enol ether formation from 8,13-epoxy-1.alpha.,6.beta.,7.beta.-trihydroxylabd-14-en-11-one-6,7-carbon ate, oxidation of the enol ether with a suitable peroxy acid to obtain 11,12-dehydro-8,13-epoxy-11-methoxy-1.alpha.,6.beta.,7.beta.,9.alpha.-tetr ahydrolabd-14-ene-6,7-carbonate and hydrolysis of the latter under an acidic condition to obtain 8,13-epoxy-1.alpha.,6.beta.,7.beta.,9.alpha.-tetrahydroxylabd-14-en-11-one -6,7-carbonate. As an alternative way of protecting the two hydroxy groups at carbon-6 and carbon-7, they may also be converted to dimethyl acetal during the synthetic sequence. Four compounds produced in the synthetic scheme as intermediates, namely, 9,11-dehydro-8,13-epoxy-11-methoxy-1.Type: GrantFiled: November 24, 1989Date of Patent: April 16, 1991Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventor: Nicholas J. Hrib
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Patent number: 4999351Abstract: Novel forskolin derivatives, intermediates and processes for the preparation thereof, and methods for treating cardiac failure and memory deficit utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: January 11, 1989Date of Patent: March 12, 1991Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Raymond W. Kosley, Jr., Gerard O'Malley, Bettina Spahl
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Patent number: 4978678Abstract: Novel 12-halogenated forskolin derivatives, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: August 7, 1989Date of Patent: December 18, 1990Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventor: Gregory M. Shutske
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Patent number: 4975451Abstract: Compounds of the formula ##STR1## in which Ar is substituted or unsubstituted phenyl, naphthyl, or thienyl; and Ar.sup.1 is 3-phenoxyphenyl, 4-fluoro-3-phenoxyphenyl, 2-methyl[1-1'-biphenyl]-3-yl, or 6-phenoxy-2-pyridyl, exhibit pyrethroid-like insecticidal and acaricidal activity and are relatively nontoxic to fish.Type: GrantFiled: March 2, 1989Date of Patent: December 4, 1990Assignee: FMC CorporationInventors: Thomas G. Cullen, Scott McN. Sieburth, Gary A. Meier, John F. Engel, Leslie W. Stratton, Alan W. Fritz
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Patent number: 4966983Abstract: Benzopyrans of the formula ##STR1## where X is a radical ##STR2## and R.sup.1, R.sup.2, R.sup.3, R.sup.4 and the ring A have the meanings stated in the description, a process for their preparation, and their use in pressure-sensitive or heat-sensitive layers.Type: GrantFiled: March 16, 1989Date of Patent: October 30, 1990Assignee: BASF AktiengesellschaftInventors: Andreas Guentner, Udo Mayer, Andreas Oberlinner
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Patent number: 4963537Abstract: Novel labdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: April 26, 1989Date of Patent: October 16, 1990Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Raymond W. Kosley, Jr., Robert J. Cherill
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Patent number: 4954642Abstract: This invention relates to forskolin derivatives, their physiologically acceptable salts, and a process for producing these compounds. The forskolin derivative is represented by the general formula ##STR1## wherein; I. when R.sup.1 is hydrogen and R.sup.4 is vinyl, ethyl, or cyclopropyl,(1) either of R.sup.2 and R.sup.3 denotes a residue represented by the formula ##STR2## wherein each of R.sup.5 and R.sup.6 denotes hydrogen or lower alkyl or R.sup.5 and R.sup.6 combine with each other to form a lower alkylene chain which may or may not contain an oxygen or nitrogen atom and m is an integer of 1 to 5, and the other one of R.sup.2 and R.sup.3 denotes hydrogen or a residue represented by the formula CO(CH.sub.2).sub.n X, X being hydrogen or ##STR3## wherein, each of R.sup.7 and R.sup.8 denotes hydrogen or lower alkyl or R.sup.7 and R.sup.8 combine with each other to form a lower alkylene chain which may or may not contain an oxygen or nitrogen atom, and n being an integer of 1 to 5, or(2) R.sup.Type: GrantFiled: May 30, 1989Date of Patent: September 4, 1990Assignee: Nippon Kayaku Kabushiki KaishaInventors: Tochiro Tatee, Takashi Takahira, Kouwa Yamashita, Masao Sakurai, Akira Shiozawa, Kazuhisa Narita
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Patent number: 4933476Abstract: Novel oxolabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: July 19, 1989Date of Patent: June 12, 1990Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventor: Nicholas J. Hrib
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Patent number: 4931221Abstract: Described are a series of novel photochromic benzopyran and naphthopyran compounds in which two cyclopropyl groups are appended at the 2-position of the benzopyran or naphthopyran ring. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic or plano lenses that incorporate the noval pyran compounds or combinations of the novel pyran compounds with other complementary photochromic compounds are described.Type: GrantFiled: December 30, 1988Date of Patent: June 5, 1990Assignee: PPG Industries, Inc.Inventor: Harry G. Heller
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Patent number: 4904590Abstract: New antibiotic A80915 and its dehydrochlorination derivatives are useful antibacterial agents. Methods of making antibiotic A80915 by culture of Streptomyces aculeolatus, NRRL 18422, and compositions containing an A80915 antibiotic also are provided.Type: GrantFiled: December 27, 1988Date of Patent: February 27, 1990Assignee: Eli Lilly and CompanyInventors: David S. Fukuda, Jon S. Mynderse, Raymond C. Yao
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Patent number: 4883885Abstract: Novel oxolabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: February 8, 1988Date of Patent: November 28, 1989Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventor: Nicholas J. Hrib