The Spiro Includes The Lactone Ring Patents (Class 549/265)
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Patent number: 7417140Abstract: The present invention involves intermediates, including a 7?-substituted steroid (II), and processes which are used to prepare eplerenone, a useful pharmaceutical agent.Type: GrantFiled: December 21, 2006Date of Patent: August 26, 2008
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Patent number: 7414127Abstract: The present invention involves intermediates, including a 7?-substituted steroid (II), and processes which are used to prepare eplerenone, a useful pharmaceutical agent.Type: GrantFiled: December 21, 2006Date of Patent: August 19, 2008
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Patent number: 7411062Abstract: The present invention involves intermediates, including a 7?-substituted steroid (II), and processes which are used to prepare eplerenone, a useful pharmaceutical agent.Type: GrantFiled: December 21, 2006Date of Patent: August 12, 2008
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Publication number: 20080171888Abstract: This invention relates to a process for making spirolactone compounds analogous to formula I.Type: ApplicationFiled: March 19, 2008Publication date: July 17, 2008Inventors: Ralph P. Volante, David M. Tschaen, Steven A. Weissman, Matthew Heileman, Toshiaki Mase, Takehiko Iida, Kenji Maeda, Toshihiro Wada, Hiroki Sato, Kenichi Asakawa
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Publication number: 20080132565Abstract: The invention provides novel polycyclic macrolactones which can be produced, in particular, by a representative of the bacterial genus Verrucosispora. These substances are preferentially distinguished by their pharmacological effect. In particular, they exhibit an antibiotic effect. This antibiotic effect is preferably directed against Gram-positive bacteria.Type: ApplicationFiled: September 23, 2004Publication date: June 5, 2008Inventors: Hans-Peter Fiedler, Roderich Suebmuth, Hana Zaehner, Alan Bull
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Publication number: 20080108141Abstract: A compound represented by the following formula (I) or (II): wherein, in the formula (I), R1, R2, R3, and R4 independently represent methyl group or ethyl group; and in the formula (II), R5, R6, R7, and R8 independently represent methyl group or ethyl group and X— represents an anion, and a reagent for measurement of nitric oxide which comprises said compound.Type: ApplicationFiled: June 4, 2007Publication date: May 8, 2008Applicants: DAIICHI PURE CHEMICALS CO., LTD.Inventors: Tetsuo NAGANO, Hirotatsu KOJIMA, Kazuya KIKUCHI
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Patent number: 7368569Abstract: This invention relates to a process for making spirolactone compounds analogous to formula IType: GrantFiled: October 14, 2003Date of Patent: May 6, 2008Assignees: Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd.Inventors: Ralph P. Volante, David M. Tschaen, Steven A. Weissman, Matthew Heileman, Toshiaki Mase, Takehiko Iida, Kenji Maeda, Toshihiro Wada, Hiroki Sato, Kenichi Asakawa
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Patent number: 7319154Abstract: This invention relates to processes for the production of 3-oxo-pregnane-21,17-carbolactones of formula II as well as 3-oxo-pregn-4-ene-21,17-carbolactones of formula III by the metal-free oxidation of 17-(3-hydroxypropyl)-3,17-dihydroxyandrostanes of formula I In addition, the invention relates to the dichloromethane hemisolvate of 6B,7B;15?,16?-diethylene-3-oxo-17?-pregnan-5?-ol-21,17-carbolactone (IV) as such.Type: GrantFiled: July 21, 2005Date of Patent: January 15, 2008Assignee: Bayer Schering Pharma AGInventors: Carsten Seilz, Hartmut Seba
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Patent number: 7304072Abstract: Compounds represented by the general formula (I) wherein Ar1 represents an aryl or heteroaryl which may be substituted; n represents 0 or 1; T, U, V and W each independently represent a nitrogen atom or a methine group which may have a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, wherein at least two of which represent said methine group; X represents methine, hydroxy substituted methine or nitrogen atom; Y represents an imino which may be substituted with lower alkyl, or oxygen; and a salt, ester or N-oxide derivative thereof. The compounds exhibit NPY antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders, central nervous system disorders, metabolic diseases, sexual and reproductive dysfunctions, gastro-intestinal disorders, respiratory disorders, inflammation or glaucoma, and the like.Type: GrantFiled: August 23, 2004Date of Patent: December 4, 2007Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takehiro Fukami, Akio Kanatani, Akane Ishihara, Yasuyuki Ishii, Toshiyuki Takahashi, Yuji Haga, Toshihiro Sakamoto, Takahiro Itoh, Masato Chiba
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Patent number: 7294724Abstract: The invention teaches an improved process for the manufacture of useful fluoran dyes of the structure according to formula 1 comprising condensing in an alkanesulfonic acid or an arenesulfonic acid to acid according to formula 2 with an aminodiphenylamine of formula 3 wherein R, R1-R6 are as defined in the specification.Type: GrantFiled: August 11, 2005Date of Patent: November 13, 2007Assignee: Appleton Papers Inc.Inventor: Ponnampalam Mathiaparanam
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Patent number: 7235672Abstract: A probe, kit comprising the probe, and methods for using the probe are provided where the probe comprises: wherein DM is a detectable marker; and L is a straight or branched chain moiety providing between 1 and 20 atom separation between DM and the ring atom to which DM is attached.Type: GrantFiled: March 11, 2004Date of Patent: June 26, 2007Assignee: Takeda San Diego, Inc.Inventors: Christopher L. Caster, Andrew J. Jennings, Marc E. Navre, Michael B. Wallace, Yiqin Wu
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Patent number: 7196208Abstract: This invention relates to processes for the preparation of 7-carboxy substituted steroid compounds of Formula I, wherein R1 is selected from H or COR4; R4 is C1–C6 alkyl or C1–C6 alkoxy; R3 is C1–C6 alkyl; Z1 is —CH2— or ?wherein O—COR4 is in the ? configuration; Z2 is —CH—; or Z1 and Z2 may be taken together to form a carbon-carbon double bond; Q is These intermediates are useful in the preparation of 7-carboxy substituted steroid compounds, and particularly, the invention is directed to novel and advantageous methods for the preparation of 9,11-?-epoxy-17-?-hydroxy-3-oxopregn-4-ene-?-7-21-dicarboxylic acid, ?-lactone, methyl ester (eplerenone; epoxymexrenone).Type: GrantFiled: March 21, 2003Date of Patent: March 27, 2007Inventor: Peter Guillaume Marie Wuts
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Patent number: 7160732Abstract: The present invention is directed, in part, to fluorescein-based ligands for detection of metal ions, and methods of making and using the same.Type: GrantFiled: July 9, 2001Date of Patent: January 9, 2007Assignee: Massachusetts Institute of TechnologyInventors: Stephen J. Lippard, Shawn Burdette, Scott Hilderbrand, Roger Y. Tsien, Grant K. Walkup
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Patent number: 7026352Abstract: The present invention provides a novel bioactive substance having an antitumor activity and a process for producing it, and a medical use thereof. Namely, it provides a 12-membered ring macrolide compound represented by the following formula obtained from the incubation solution of Streptomyces sp. Mer.Type: GrantFiled: February 1, 2002Date of Patent: April 11, 2006Assignees: Mercian Corporation, Eisai Co., Ltd.Inventors: Yoshiharu Mizui, Takashi Sakai, Satoshi Yamamoto, Keisuke Komeda, Masanori Fujita, Akifumi Okuda, Kumiko Kishi, Jun Niijima, Mitsuo Nagai, Kiyoshi Okamoto, Masao Iwata, Yoshihiko Kotake, Toshimitsu Uenaka, Naoki Asai, Motoko Matsufuji, Tomohiro Sameshima, Naoto Kawamura, Kazuyuki Dobashi, Takashi Nakashima, Masashi Yoshida, Toshio Tsuchida, Susumu Takeda, Tomonari Yamada, Koji Norihisa, Takao Yamori
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Patent number: 6974806Abstract: The present invention provides a lipid-rich plaque regressing agent comprising a compound represented by Formula: in which ring A is a cyclic hydrocarbon or the like; ring B is a heterocyclic ring or the like; each of X and Y is —NR1— (in which R1 is a hydrocarbon or the like); D is a C1-3 alkylene group or the like; E is —NH— or the like; G is a bond or the like; and Ar is an aryl or the like; D may be taken together with a constituent atom of the ring B to form a ring, and R4 may be taken together with a constituent atom of the ring B to form a ring.Type: GrantFiled: July 13, 2001Date of Patent: December 13, 2005Assignee: Takeda Pharmaceutical Company LimitedInventors: Zen-ichi Terashita, Masahira Nakamura, Shogo Marui, Masaki Ogino
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Patent number: 6962894Abstract: A selectively herbicidal composition for controlling grasses and weeds in crops of useful plants, comprising a) a herbicidally effective amount of a compound of formula I or a salt or diastereoisomer of a compound of formula I, and b) an amount, which is effective for antagonism of the herbicide, of a compound of formula IIaType: GrantFiled: September 5, 2000Date of Patent: November 8, 2005Assignee: Syngenta Crop Protection, Inc.Inventor: Jutta Glock
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Patent number: 6951952Abstract: There are described novel rhodol dye compounds The dye compounds exhibit a first color when in the crystalline form and a second color, different from the first color, when in the liquid, amorphous form.Type: GrantFiled: February 27, 2004Date of Patent: October 4, 2005Assignee: Polaroid CorporationInventors: Kap-Soo Cheon, Michael P. Filosa, Stephen J. Telfer
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Patent number: 6933395Abstract: Process for the production of drospirenone (6?,7?; 15?,16?-dimethylene-3-oxo-17?-pregn-4-ene-21,17-carbolactone, DRSP) (1) and 7?-(3-hydroxy-1-propyl)-6?,7?; 15?,16?-dimethylene-5?-androstane-3?,5,17?-triol (ZK 92836) and 6?,7?; 15?,16?-dimethylene-5?-hydroxy-3-oxo-17?-androstane-21,17-carbolactone (ZK 90965) as intermediate products of the process.Type: GrantFiled: August 18, 2000Date of Patent: August 23, 2005Assignee: Schering AGInventors: Jörg-Thorsten Mohr, Klaus Nickisch
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Patent number: 6933261Abstract: The invention relates to new phenyl-substituted cyclic ketoenols of the formula (I) in which Het represents one of the groups wherein A, B, D, G, X, Y and Z have the meaning given in the description, several processes and intermediate products for their preparation and their use as pest control agents and herbicides.Type: GrantFiled: September 19, 2002Date of Patent: August 23, 2005Assignee: Bayer AktiengesellschaftInventors: Folker Lieb, Hermann Hagemann, Arno Widdig, Michael Ruther, Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger, Alan Graff, Norbert Mencke, Andreas Turberg, Peter Dahmen
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Patent number: 6861391Abstract: Trifluoromethyl-substituted spirocyclic ketoenols of the formula (I) are provided wherein Het represents one of the groups and G, V, W, X, Y, and Z are as defined in the specification. Also provides are processes for the preparation of the compounds. The compounds of formula (I) find use as pesticides.Type: GrantFiled: September 19, 2000Date of Patent: March 1, 2005Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Alan Graff, Thomas Bretschneider, Christoph Erdelen, Mark Wilhelm Drewes, Dieter Feucht
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Publication number: 20040242904Abstract: A novel sordarin derivative was isolated from fungal cultures. The compound is useful in the treatment and/or prevention of human and animal fungal infections, as well as in the control of phytopathogenic fungi in crops. Two novel cultures of fungi, ATCC No. PTA-3862 and ATCC No. PTA-3861 can be used to ferment and produce the present compound.Type: ApplicationFiled: June 3, 2004Publication date: December 2, 2004Inventors: Angelo Basilio, Javier Collado, Maria Teresa Diez, Ziqiang Guan, Guy H Harris, Michael C Justice, Jennifer Nielsen-Kahn, Mythili S Shastry
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Patent number: 6803372Abstract: Compounds of the general formula (I): wherein Ar1 represents optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V, and W each independently represent nitrogen atom or optionally substituted methine group, where at least two of them represent the said methine group; X represents methine or hydroxy substituted methine; Y represents an optionally substituted imino or oxygen atom are described and claimed. These novel spiro compounds are useful as neuropeptide Y receptor antagonists and as agents for the treatment of various kinds of cardiovascular disorders, central nervous system disorders, metabolic diseases and the like.Type: GrantFiled: March 8, 2002Date of Patent: October 12, 2004Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takehiro Fukami, Akio Kanatani, Akane Ishihara, Yasuyuki Ishii, Toshiyuki Takahashi, Yuji Haga, Toshihiro Sakamoto, Takahiro Itoh
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Patent number: 6790965Abstract: Combinatorial libraries are disclosed which are represented by Formula I: (T′—L)q—Ŝ—C(O)—L′—II′ I wherein: Ŝ is a solid support; T′—L— is an identifier residue; and —L′—II′ is a ligand/linker residue. These libraries contain dihydrobenzopyrans of the formula: which interact (i.e., as agonists or antagonists) with &agr; adrenergic receptors, dopamine receptors, &dgr;-opiate receptors, and K+ channels and are inhibitors of carbonic anhydrase isozymes. They are useful in the treatement of ocular diseases such as glaucoma.Type: GrantFiled: September 8, 1999Date of Patent: September 14, 2004Assignee: Pharmacopeia Drug Discovery, Inc.Inventors: John J. Baldwin, John C. Reader, Lawrence W. Dillard, Ge Li, Wenguang Zeng
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Publication number: 20040127432Abstract: Epothilone A, epothilone B, analogs of epothilone and libraries of epothilone analogs are synthesized. Epothilone A and B are known anticancers agents that derive their anticancer activity by the prevention of mitosis through the induction and stabilization of microtubulin assembly. The analogs of epothilone are novel. Several of the analogs are demonstrated to have a superior cytotoxic activity as compared to epothilone A or epothilone B as demonstrated by their enhanced ability to induce the polymerization and stabilization of microtubules.Type: ApplicationFiled: December 9, 2003Publication date: July 1, 2004Applicant: The Scripps Research InstituteInventors: Kyriacos C. Nicolaou, Yun He, Sacha Ninkovic, Joaquin Pastor, Frank Roschangar, Francisco Sarabia, Hans Vallberg, Dionisios Vourloumis, Nicolas Winssinger, Zhen Yang, Nigel Paul King, M. Ray Finlay
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Patent number: 6756231Abstract: A compound represented by the following formula (I) or (II): wherein, in the formula (I), R1, R2, R3, and R4 independently represent methyl group or ethyl group; and in the formula (II), R5, R6, R7, and R8 independently represent methyl group or ethyl group and X− represents an anion, and a reagent for measurement of nitric oxide which comprises said compound.Type: GrantFiled: August 18, 2000Date of Patent: June 29, 2004Assignees: Daiichi Pure Chemicals Co., Ltd.Inventors: Tetsuo Nagano, Hirotatsu Kojima, Kazuya Kikuchi
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Patent number: 6746818Abstract: (Meth)acrylate compounds having a norbornane, bicyclo[2.2.2]octane, 7-oxanorbornane or cyclohexane ring structure and a &ggr;-butyrolactone ring structure connected together by a suitable linker are novel and useful in forming polymers having high transparency, especially at the exposure wavelength of an excimer laser.Type: GrantFiled: June 13, 2002Date of Patent: June 8, 2004Assignee: Shin-Etsu Chemical Co., Ltd.Inventors: Takeshi Kinsho, Koji Hasegawa, Takeru Watanabe
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Patent number: 6746990Abstract: The present invention relates to new compounds of the formula (I): in which X, Y and Z have the meanings given in the description and Het represents one of the groups: in which A, B, D and G have the meanings given in the description, a plurality of processes for their preparation, and to their use as pesticides and herbicides.Type: GrantFiled: December 11, 2001Date of Patent: June 8, 2004Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Hermann Hagemann, Folker Lieb, Norbert Lui, Michael Ruther, Arno Widdig, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger, Peter Dahmen, Norbert Mencke, Andreas Turberg
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Patent number: 6713435Abstract: A method for producing an optically active lactone compound by Baeyer-Villiger oxidation of a cyclic ketone compound with at least one kind of oxidants selected from the group consisting of hydrogen peroxide and urine-hydrogen peroxide adduct (UHP) using a cobalt(salen) complex having a cis-&bgr; structure expressed by the following formula (I) or (II) as a catalyst. in which X and Y independently denote H, a t-butyl group or an electron-withdrawing substituting group and W is a halogen element. in which X and Y independently denote H, a t-butyl group or an electron-withdrawing substituting group and Z− is a monovalent anion. The optically active lactone compounds can be used for the synthesis of medicines and argochemicals.Type: GrantFiled: September 3, 2002Date of Patent: March 30, 2004Assignee: Kyushu UniversityInventors: Tsutomu Katsuki, Tatsuya Uchida, Katsuji Ito
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Patent number: 6696217Abstract: A photosensitive monomer including a methylene butyrolactone derivative represented by the following formula: wherein R1 is a hydrogen atom or alkyl group, R2 is an acid-labile group, X is a hydrogen atom, or substituted or unsubstituted alkyl group having 1 to 10 carbon atoms, and Y is a substituted or unsubstitued alkyl group or alicyclic hydrocarbon group having 1 to 20 carbon atoms.Type: GrantFiled: February 20, 2002Date of Patent: February 24, 2004Assignee: Samsung Electronics Co., Ltd.Inventors: Kwang-sub Yoon, Sang-gyun Woo
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Patent number: 6639095Abstract: The present invention provides a process for preparing optically active &agr;-hydroxy acids and derivatives thereof by subjecting the alkylated 1,3-dioxolanones of formula (IV) wherein R1 and R2 are the same or different and are each independently H or C1-6 alkyl; R5 is H, C1-16 alkyl, or unsubstituted or substituted phenyl; and R6 is C1-8 alkyl, C2-7 alkenyl or unsubstituted or substituted benzyl, to either alcoholysis or hydrolysis, in which the alkylated 1,3-dioxolanones are obtained by using 10-camphorsulfonamide as a chiral auxiliary.Type: GrantFiled: October 8, 2002Date of Patent: October 28, 2003Inventors: Biing-Jiun Uang, Jia-Wen Chang, Der-Pin Jang
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Patent number: 6630594Abstract: The present invention provides methods of making substituted phenylketoenols of the general formula I, wherein V, W, X, Y, Z and Het are as defined herein. The compounds have pesticidal and herbicidal activity.Type: GrantFiled: January 28, 2002Date of Patent: October 7, 2003Assignee: Bayer AktiengesellschaftInventors: Hermann Hagemann, Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Peter Dahmen, Markus Dollinger, Alan Graff, Wolfram Andersch
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Publication number: 20030064985Abstract: A compound of formula (I) or its enantiomers or diastereoisomers thereof: 1Type: ApplicationFiled: December 17, 2001Publication date: April 3, 2003Inventors: Christiane Yoakim, Bruno Hache, William W. Ogilvie, Jeffrey O'Meara, Peter White, Nathalie Goudreau
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Patent number: 6525088Abstract: Compounds represented by the following general formula (I): wherein R1, R2, R3, R4, R5, and R6 independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, or a C1-6 alkoxyl group, R7 and R8 independently represent a C1-6 alkyl group or an aryl group which may be substituted, R9 and R10 independently represent a hydrogen atom, a C1-6 alkyl group, or a C1-6 alkoxyl group, and R11 represents a hydrogen atom or a C1-6 alkanoyl group, or salts thereof. The aforementioned compounds are substantially non-fluorescent and react with singlet oxygen under a physiological condition to give a fluorescent substance, and therefore they are useful as agents for measurement of singlet oxygen.Type: GrantFiled: January 3, 2001Date of Patent: February 25, 2003Inventors: Tetsuo Nagano, Naoki Umezawa
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Patent number: 6521622Abstract: Heterocyclic aromatic amides having a hydroxy group adjacent to the amide functionality are useful as antifungal agents, particularly for plants.Type: GrantFiled: July 20, 2000Date of Patent: February 18, 2003Assignee: Dow AgroSciences LLCInventors: Michael J. Ricks, William H. Dent, III, Richard B. Rogers, Chenglin Yao, Bassam S. Nader, John L. Miesel, Gina M. Fitzpatrick, Kevin G. Meyer, Noormohamed M. Niyaz, Irene M. Morrison, Robert P. Gajewski
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Publication number: 20030008232Abstract: (Meth)acrylate compounds having a norbornane, bicyclo[2.2.2]octane, 7-oxanorbornane or cyclohexane ring structure and a &ggr;-butyrolactone ring structure connected together by a suitable linker are novel and useful in forming polymers having high transparency, especially at the exposure wavelength of an excimer laser.Type: ApplicationFiled: June 13, 2002Publication date: January 9, 2003Applicant: Shin-Etsu Chemical Co., Ltd.Inventors: Takeshi Kinsho, Koji Hasegawa, Takeru Watanabe
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Patent number: 6504036Abstract: The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) in which Het represents one of the groups in which A, B, D, G, X and Z are each as defined in the description, to a plurality of processes and intermediates for their preparation, and to their use as pesticides.Type: GrantFiled: December 10, 2001Date of Patent: January 7, 2003Assignee: Bayer AktiengesellschaftInventors: Folker Lieb, Reiner Fischer, Thomas Bretschneider, Michael Ruther, Alan Graff, Udo Schneider, Christoph Erdelen, Ulrike Wachendorff-Neuman, Wolfram Andersch, Andreas Turberg
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Publication number: 20020183528Abstract: The rate of aminolysis of butyrolactones is predictably adjusted by attaching a substituent having a known field effect value (F) to the alpha position before reacting the substituted buytrolactone with an amine. The aminolysis product is a gamma-hydroxy amide. The resulting materials are useful as the cross-linking agents in a variety of coatings and coatings processes.Type: ApplicationFiled: November 28, 2001Publication date: December 5, 2002Inventor: Albert Gordon Anderson
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Patent number: 6469051Abstract: A compound represented by the following general formula: wherein R1 and R2 represent amino groups present at adjacent positions each other on the phenyl ring; R3, R4, R5 and R6 independently represent a C1-6 alkyl group; R7, R8, R9 and R10 independently represent a hydrogen atom, a C1-6 alkyl group, an allyl group, or a halogen atom; R11 represents a hydrogen atom or a C1-18 alkyl group; and X− represents an anion, and an agent for nitric oxide measurement comprising said compound. The compound efficiently reacts with nitric oxide to give a fluorescent compound that emits strong fluorescence by irradiation with excitation light of a long wavelength. This fluorescent compound is characterized in that said compound is detectable in a fluorescence wavelength range hardly influenced by autofluorescence of cells, and its fluorescence intensity is not attenuated under an acidic condition.Type: GrantFiled: December 29, 2000Date of Patent: October 22, 2002Inventors: Tetsuo Nagano, Hirotatsu Kojima
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Patent number: 6395681Abstract: Chromogenic compounds of colorless or lightly colored form are disclosed having the following structural formula: wherein E represents a six-membered aromatic or heterocyclic ring which may have an aromatic condensed ring and both the E ring and the condensed ring may be substituted. Each of R1, R2, R3 and R4 independently represents hydrogen, alkyl of not more than 12 carbon atoms which is unsubstituted or substituted by halogen, hydroxyl, cyano or lower alkoxy or represents cycloalkyl, phenyl, benzyl, or phenyl or benzyl which is substituted by halogen, lower alkyl or lower alkoxy or R1 and R2 or R3 and R4 together with the nitrogen atom to which they are attached represent a 5- or 6-membered heterocyclic radical. Each of R7 and R8 independently represents hydrogen, lower alkyl, lower alkoxy or halo. The compounds of this invention are eligible for use in pressure-sensitive and heat-sensitive record materials and manifold marking systems.Type: GrantFiled: September 22, 1986Date of Patent: May 28, 2002Assignee: Appleton Papers Inc.Inventors: Seishi Ikegami, Takamichi Amako
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Patent number: 6391912Abstract: The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) in which Het represents one of the groups and G, V, W, X, Y and Z are each as defined in the description, to processes and intermediates for their preparation and to their use as pesticides and herbicides.Type: GrantFiled: June 29, 2001Date of Patent: May 21, 2002Assignee: Bayer AktiengesellschaftInventors: Hermann Hagemann, Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Peter Dahmen, Markus Dollinger, Alan Graff, Wolfram Andersch
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Patent number: 6388077Abstract: Compounds of the general formula VI-1 and processes for their preparation: wherein t, u, v and w each independently represent a nitrogen atom or a methine group which may have a substituent selected from the group consisting of halogen, lower alkyl, lower alkoxy and optionally protected hydroxy; and wherein at least two of which represent the methine group. These compounds serve as intermediates for novel spiro compounds which exhibit neuropeptide Y receptor (NPY) antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders, central nervous system disorders, metabolic diseases and the like.Type: GrantFiled: October 25, 2001Date of Patent: May 14, 2002Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takehiro Fukami, Akio Kanatani, Akane Ishihara, Yasuyuki Ishii, Toshiyuki Takahashi, Yuji Haga, Toshihiro Sakamoto, Takahiro Itoh
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Patent number: 6387948Abstract: 8-Acetylarteminolide of the formula (I) having inhibitory activities against farnesyl-protein transferase(FPTase), a progression of the cell cycle and angiogenesis may be useful for the prevention and treatment of various cancers and angiogenesis-related diseases:Type: GrantFiled: June 17, 2000Date of Patent: May 14, 2002Assignee: Korea Research Institute of Bioscience and BiotechnologyInventors: Byoung-Mog Kwon, Kwang-Hee Son, Ha-Won Jeong, Seung-Ho Lee, Mi-Young Han, Hyun-Mi Kang, Hyae-Kyeong Kim, Soo-Ik Chang
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Patent number: 6362230Abstract: The present invention provides novel sulphonamide derivatives which are useful for potentiating glutamate receptor function in a mammal requiring treatment, processes for their preparation, and pharmaceutical compositions containing them.Type: GrantFiled: November 21, 2000Date of Patent: March 26, 2002Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, Paul Leslie Ornstein, Dennis Michael Zimmerman, Ana Maria Escribano
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Patent number: 6359151Abstract: The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) in which Het represents one of the groups in which A, B, D, G, X and Z are each as defined in the description, to a plurality of processes and intermediates for their preparation, and to their use as pesticides.Type: GrantFiled: March 15, 2001Date of Patent: March 19, 2002Assignee: Bayer AktiengesellschaftInventors: Folker Lieb, Reiner Fischer, Thomas Bretschneider, Michael Ruther, Alan Graff, Udo Schneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Wolfram Andersch, Andreas Turberg
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Patent number: 6335345Abstract: Spiro compounds of the general formula (I): wherein Ar1 represents an optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V and W each represent a nitrogen atom or an optionally substituted methine group, wherein at least two of which represent said methine group; X represents methine; Y represents an optionally substituted imino or oxygen atom. These novel spiro compounds exhibit neuropeptide Y receptor (NPY) antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders, central nervous system disorders, metobolic diseases and the like.Type: GrantFiled: August 14, 2001Date of Patent: January 1, 2002Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takehiro Fukami, Akio Kanatani, Akane Ishihara, Yasuyuki Ishii, Toshiyuki Takahashi, Yuji Haga, Toshihiro Sakamoto, Takahiro Itoh
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Patent number: 6320045Abstract: The invention as claimed is directed to a process for making an epothilone having the following structures from ones having an oxiranyl moiety, by reacting a compound having the latter structure with a metal or metal-assisted reagent. Said metal or metal-assisted reagent is selected from the group consisting of a) reactive metallocenes; b) [N2C(CO2Me)2, cat Rh2,(OAC)4]; c) [N2C(CO2Me)2, cat[(n-C7H15CO2)2 Rh]2]; d) [Zn—Cu, EtOH]; e) [Mg(Hg), MgBr]; f) Cr; g) [FeCl3, n-BuLi]; h) [TiCl3, LiAlH4]; i) [TiCl4, Zn]; j) [WCl6, LiAlH4,]; k) [NbCl5, NaAlH4]; l) [VCl3,Zn] and m) [WCl6, n-BuLi].Type: GrantFiled: May 21, 1999Date of Patent: November 20, 2001Assignee: Bristol-Myers Squibb CompanyInventors: Soong-Hoon Kim, James A. Johnson
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Patent number: 6252075Abstract: A process for preparing 7-benzylpurine derivatives is provided. An acetylpurine nucleoside is reacted with a benzyl halide to benzylate the 7-position of the purine base, and an acid is then added to the reaction mixture to hydrolyze the glycoside bond. The 7-benzylpurines may be used to prepare 9-substituted purine derivatives.Type: GrantFiled: May 26, 1999Date of Patent: June 26, 2001Assignee: Ajinomoto Co., Inc.Inventors: Hiroshi Shiragami, Kunisuke Izawa, Keizo Yamashita, Satoshi Katayama
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Patent number: 6251830Abstract: The present invention relates to new compounds of the formula (I) in which X represents alkyl, Y represents halogen or alkyl and Z represents halogen or alkyl, with the proviso that one of the radicals Y and Z always represents halogen and the other alkyl, Het represents one of the groups in which A, B, D and G have the meanings given in the description, a plurality of processes for their preparation and their use as pesticides and herbicides.Type: GrantFiled: July 26, 1999Date of Patent: June 26, 2001Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Hermann Hagemann, Folker Lieb, Michael Ruther, Arno Widdig, Peter Dahmen, Markus Dollinger, Christoph Erdelen, Hans-Joachim Santel, Ulrike Wachendorff-Neumann, Alan Graff, Wolfram Andersch
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Patent number: 6174922Abstract: The present invention provides novel sulphonamide derivatives which are useful for potentiating glutamate receptor function in a mammal requiring treatment, processes for their preparation, and pharmaceutical compositions containing them.Type: GrantFiled: February 23, 1999Date of Patent: January 16, 2001Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, Paul Leslie Ornstein, Dennis Michael Zimmerman, Ana Maria Escribano
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Patent number: 6121465Abstract: Process for the production of drospirenone (6.beta., 7.beta.; 15.beta., 16.beta.-dimethylene-3-oxo-17.alpha.-pregn-4-ene-21, 17-carbolactone, DRSP) (1) and 7.alpha.-(3-hydroxy-1-propyl)-6.beta., 7.beta.; 15.beta., 16.beta.-dimethylene-5.beta.-androstane-3.beta., 5, 17.beta.-triol (ZK 92836) and 6.beta., 7.beta.; 15.beta., 16.beta.-dimethylene-5.beta.-hydroxy-3-oxo-17.alpha.-androstane-21, 17-carbolactone (ZK 90965) as intermediate products of the process.Type: GrantFiled: February 11, 1999Date of Patent: September 19, 2000Assignee: Schering AktiengesellschaftInventors: Jorg-Thorsten Mohr, Klaus Nickisch