The Five-membered Hetero Ring Contains One Double Bond Only (i.e., Indolines) Patents (Class 548/490)
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Patent number: 6562989Abstract: The present invention is directed to a transition metal catalyst, comprising a Group 8 metal and a ligand having the structure wherein R, R′ and R″ are organic groups having 1-15 carbon atoms, n=1-5, and m=0-4. The present invention is also directed to a method of forming a compound having an aromatic or vinylic carbon-oxygen, carbon-nitrogen, or carbon-carbon bond using the above catalyst. The catalyst and the method of using the catalyst are advantageous in preparation of compounds under mild conditions of approximately room temperature and pressure.Type: GrantFiled: August 3, 2001Date of Patent: May 13, 2003Assignee: Yale UniversityInventors: John F. Hartwig, Quinetta Shelby, Noriyasu Kataoka
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Patent number: 6541669Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.Type: GrantFiled: June 2, 1999Date of Patent: April 1, 2003Assignee: Theravance, Inc.Inventors: Edmund J. Moran, Seok-Ki Choi
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Patent number: 6528650Abstract: The invention relates to novel 4-hydroxyindole derivatives comprising at least one cationic group Z, Z being selected from quaternized aliphatic chains, aliphatic chains containing at least one quaternized saturated ring, and aliphatic chains containing at least one quaternized unsaturated ring, to their use as a coupler for the oxidation dyeing of keratinous fibers, to the dyeing compositions comprising them, and to the methods of oxidation dyeing which employ them.Type: GrantFiled: August 9, 2001Date of Patent: March 4, 2003Assignee: L'Oreal S.A.Inventors: Eric Terranova, Aziz Fadli, Alain LaGrange
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Patent number: 6509467Abstract: A catalytic transfer hydrogenation process is provided. The catalyst employed in the process is a metal neutral hydrocarbyl complex which is coordinated to defined bidentate ligands. Preferred metals include rhodium, ruthenium and iridium. Preferred bidentate ligands are diamines and aminoalcohols, particularly those comprising chiral centers. The hydrogen donor is advantageously a mixture of triethylamine and formic acid. The process can be employed to transfer hydrogenate iminium salts, which are preferably prochiral.Type: GrantFiled: March 21, 2001Date of Patent: January 21, 2003Assignee: Avecia LimitedInventors: Andrew John Blacker, Lynne Alison Campbell
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Patent number: 6503907Abstract: The present invention relates to indole derivatives, dihydroindole derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.Type: GrantFiled: November 20, 2001Date of Patent: January 7, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, Johannes Aebi, Henrietta Dehmlow, Olivier Morand, Narendra Panday, Thomas Weller
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Patent number: 6492366Abstract: A compound selected from those of formula (I): wherein: R1 and R2 each independently represent hydrogen or, alkyl, T1 and T2 each independently represent alkylene, G represents a heterocyclic group selected of formula (&agr;): wherein: W1 to W5 and X1 to X4 are so defined in the description. Medicinal products containing the same are useful as serotonin-reuptake inhibitors.Type: GrantFiled: October 11, 2000Date of Patent: December 10, 2002Assignee: Les Laboratoires ServierInventors: Gilbert Lavielle, Olivier Muller, Mark Millan, Didier Cussac, Anne Dekeyne
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Patent number: 6489480Abstract: This description addresses fluorinated amine compounds meeting the general formula R′iArF—ER2, where ArF is a fluoroaryl group, E is nitrogen or phosphorous, each R is independently a C1-C20 hydrocarbyl group; or the two Rs may connect to form an unsubstituted or substituted C2-C20 cycloaliphatic group, R′ is a C1-C20 hydrocarbyl or halogenated hydrocarbyl, and i is 0, 1 or 2. These compounds may be protonated with strong Bronsted acids to form protonated amine compounds that are useful for the preparation of organometallic catalyst-cocatalyst compounds comprising noncoordinating or weakly coordinating anions. The resulting organometallic catalyst-cocatalyst complexes can be effectively used as olefin polymerization catalysts.Type: GrantFiled: December 11, 2000Date of Patent: December 3, 2002Assignee: ExxonMobil Chemical Patents Inc.Inventor: George Rodriguez
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Patent number: 6472418Abstract: Non-peptide acetamide derivatives of Formula I are specific NK1 antagonist, where R is aryl, R1 and R2 are H or alkyl, m, n and q are integers from 0 to 4, X is NR8 or NHCONH, R3 and R9 are H or alkyl, R4 is naphthyl or indolyl, R5 and R2 are H or alkyl, and R6 is aryl. The compounds are useful agents for treating inflammatory and allergic disorders, pain, anxiety, depression, schizophrenia and emesis.Type: GrantFiled: June 18, 2001Date of Patent: October 29, 2002Assignee: Warner-Lambert CompanyInventors: Mark Wallace Creswell, Michael Higginbottom, David Christopher Horwell, Russel Andrew Lewthwaite, Martyn Clive Pritchard, Jennifer Raphy
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Patent number: 6469043Abstract: The present invention creates a novel antiangiogenic agent and provides an antitumor agent which shows high safety as compared with conventional antitumor agents, has a sure effect and is able to be administered for a long period. That is, it provides an indole compound represented by the following formula (I), its pharmacologically acceptable salt or hydrates thereof. In the formula, R1 represents hydrogen atom, a halogen atom or cyano group; R2 and R3 are the same as or different from and each represents hydrogen atom, a C1˜C4 lower alkyl group or a halogen atom; R4 represents hydrogen atom or a C1˜C4 lower alkyl group; and the ring A represents cyanophenyl group, aminosulfonylphenyl group, aminopyridyl group, aminopyrimidyl group, a halopyridyl group or cyanothiophenyl group, provided that the case where all of R1, R2 and R3 are hydrogen atoms, where both R2 and R3 are hydrogen atoms or where the ring A is aminosulfonyl group and both R1 and R2 are halogen atoms is excluded.Type: GrantFiled: September 28, 2000Date of Patent: October 22, 2002Assignee: Eisai Co., Ltd.Inventors: Toru Haneda, Akihiko Tsuruoka, Junichi Kamata, Tadashi Okabe, Keiko Takahashi, Kazumasa Nara, Shinichi Hamaoka, Norihiro Ueda, Takashi Owa, Toshiaki Wakabayashi, Yasuhiro Funahashi, Taro Semba, Naoko Hata, Yuji Yamamoto, Yoichi Ozawa, Noako Tsukahara
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Patent number: 6441004Abstract: The invention concerns the use of a compound of the formula (I) in which Z, X, T, A, R1, R2, p and q have any of the meanings defined herein, and their pharmaceutically acceptable salts or in vivo hydrolysable esters, in the treatment of a disease or condition mediated by monocyte chemoattractant protein-1 (MCP-1). Certain of the components of formula (I) are novel and are provided, together with pharmaceutical compositions thereof, as further features of the invention.Type: GrantFiled: February 3, 2000Date of Patent: August 27, 2002Assignee: Zeneca LimitedInventors: Alan Wellington Faull, Andrew John Barker, Jason Grant Kettle
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Publication number: 20020103210Abstract: A compound of the formula: 1Type: ApplicationFiled: January 11, 2002Publication date: August 1, 2002Applicant: TAKEDA CHEMICAL INDUSTRIES, LTD.Inventors: Shuichi Furuya, Toshihiro Imaeda, Satoshi Sasaki
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Patent number: 6403808Abstract: Compounds which have enhanced affinity and selectivity for 5-HT6 receptors have been identified. These compounds can be used therapeutically in the treatment of mental disorders via administration in a pharmacologically acceptable delivery route to a patient in need thereof, or can be used to identify antagonists of 5-HT6 receptors by well known screening methodologies which could themselves be used in the treatment of mental disorders.Type: GrantFiled: August 20, 2001Date of Patent: June 11, 2002Assignee: Virginia Commonwealth UniversityInventors: Richard A. Glennon, Bryan Roth
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Patent number: 6391916Abstract: Novel C3-substituted cyclodeca-1,5-diynes can be prepared through novel synthetic procedures using starting (E)-C3-substituted-4-(aryl- or heteroarylmethylidene)cyclodeca-1,5-diynes reagents. Both the C3-substituted cyclodeca-1,5-diyn-3-enes and the starting reagents have improved thermal stability compared to unsubstituted counterparts.Type: GrantFiled: July 21, 2000Date of Patent: May 21, 2002Assignee: The Hong Kong University of Science and TechnologyInventors: Wei-Min Dai, Anxin Wu, Yuk Ha Lee, Wataru Hamaguchi, Sei-ichi Nishimoto, Ling Zhou, Atsushi Ishii
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Patent number: 6388095Abstract: Compounds and pharmaceutical compositions containing such compounds and possessing anti-tussive activity, and a method of administering the same to warm-blooded animals, including humans.Type: GrantFiled: June 9, 1999Date of Patent: May 14, 2002Assignee: Cardiome Pharma Corp.Inventors: Gregory N. Beatch, Lewis S. L. Choi, Clive P. Page, Bertrand M. C. Plouvier, Yuzhong Liu
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Patent number: 6384281Abstract: A pharmaceutical compound of formula (I) in which R1 and R2 are each hydrogen or C1-4 alkyl, or R1 and R2 together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, or morpholino group, said group being optionally substituted with 1 to 3 C1-4alkyl substituents, R3 is a naphythyl, indolyl, benzothienyl, benzofuranyl, benzothiazolyl, quinolinyl or isoquinolinyl group, said group being optionally substituted, and n is 1 or 2; or a salt or ester thereof.Type: GrantFiled: October 3, 2001Date of Patent: May 7, 2002Assignee: Eli Lilly and CompanyInventors: Martine Keenan, Sandra Ginette Milutinovic, David Edward Tupper
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Publication number: 20020052512Abstract: A compound of formula 1a 1Type: ApplicationFiled: June 12, 2001Publication date: May 2, 2002Inventors: Nader Fotouhi, Paul Gillespie, Robert W. Guthrie, Sherrie L. Pietranico-Cole, Weiya Yun
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Patent number: 6323315Abstract: The present invention provides compounds of the formula where R1-R5 are each, independently, a hydrogen atom or a normal or branched C1-C6-alkyl group; A is a methionyl, phenylalanyl or phenylglycyl residue; n is 0 or 1; R6 is a hydrogen atom; and R7 is a carbocylic group, an aromatic group, a C1-C4-alkyl group, a pyridylalkyl group or a heterocyclic group. In another embodiment, R6 is benzyl or —C(O)OR8, where R8 is a C1-C6-alkyl group, and R7 is a heteroaromatic group, such as a 2-thiazolyl group.Type: GrantFiled: March 31, 2000Date of Patent: November 27, 2001Assignees: BASF Aktiengesellschaft, Arizona Board of RegentsInventors: George R. Pettit, Jayaram K. Srirangam, Michael D. Williams, Kieran P. M. Durkin, Teresa Barlozzari, Andreas Kling, Bernd Janssen, Andreas Haupt
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Patent number: 6297270Abstract: A process for the preparation of 2,3-dihydroindoles of the formula (I) by reaction of halostyrenes of the formula (IIa) or (IIb) with amines of the formula (III) R1—NH2 (III) in at least one inert solvent or in water, and in the presence of at least one base.Type: GrantFiled: November 18, 1999Date of Patent: October 2, 2001Assignee: Aventis Research & Technologies GmbH & Co. KGInventors: Matthias Beller, Thomas Riermeier, Harald Trauthwein, Claudia Breindl
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Patent number: 6274584Abstract: Novel peptide derivatives, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone are disclosed. The peptides have the formula (1): wherein a, b, A, R1, L1, D, R3, R4, R2, L2, E and G are as defined in the specification. These peptides exhibit improved resistance to proteolytic degradation, and hence, improved bioavailability.Type: GrantFiled: July 19, 2000Date of Patent: August 14, 2001Assignee: Novo Nordisk A/SInventors: Bernd Peschke, Michael Ankersen, Thomas Kruse Hansen, Henning Thøgersen
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Patent number: 6258815Abstract: The novel specific immunophilin ligands of the general formula I have an antiasthmatic and immunosuppressive action and are suitable for the preparation of drugs.Type: GrantFiled: April 25, 1997Date of Patent: July 10, 2001Assignee: ASTA Medica AktiengesellschaftInventors: Dietmar Reichert, Bernhard Kutscher, Holger Bang, Kay Brune, Gerhard Quinkert, Hans-Günter Schaible
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Patent number: 6221902Abstract: This invention provides compounds of Formula I having the structure wherein A, Q, R3, and R4 are as defined hereinbefore in the specification, or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.Type: GrantFiled: May 10, 1999Date of Patent: April 24, 2001Assignee: American Home Products CorporationInventors: Michael S. Malamas, Folake O. Adebayo, Paul J. Dollings
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Patent number: 6214856Abstract: Pharmaceutical compositions and methods of inhibiting calpain using novel indolecarboxamides are disclosed.Type: GrantFiled: August 30, 1999Date of Patent: April 10, 2001Assignee: SmithKline Beecham CorporationInventors: Robert A Daines, Kelvin Kin-Cheong Sham
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Patent number: 6204392Abstract: Heterocyclic derivatives of the formula (I) wherein each symbol is as defined in the specification, pharmaceutically acceptable salts thereof and method of producing them. Pharmaceutical compositions containing the heterocyclic derivative or a pharmaceutically acceptable salt thereof, particularly, ACAT inhibitors and lipoperoxidation inhibitors. The heterocyclic derivatives and pharmaceutically acceptable salts thereof of the present invention show superior ACAT inhibitory activity and lipoperoxidation inhibitory activity, and are useful as ACAT inhibitors and hyperlipemia inhibitors. To be specific, they are useful for the prevention and treatment of arteriosclerotic lesions of arteriosclerosis, hyperlipemia and diabetes, as well as ischemic diseases of brain, heart and the like.Type: GrantFiled: April 1, 1999Date of Patent: March 20, 2001Assignee: Sankyo Company, LimitedInventors: Hiroshi Matsui, Shoji Kamiya, Hiroaki Shirahase, Shohei Nakamura
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Patent number: 6162818Abstract: This invention involves compounds having the following structure: ##STR1## wherein: a) R.sub.1 is hydrogen; or alkyl; bond (a) is a single or a double bond;b) R.sub.2 and R.sub.3 are each independently selected from hydrogen; unsubstituted C.sub.1 -C.sub.3 alkanyl, alkenyl or alkynyl; cycloalkanyl, cycloalkenyl; unsubstituted C.sub.1 -C.sub.3 alkylthio or alkoxy; hydroxy; thio; nitro; cyano; amino; C.sub.1 -C.sub.3 alkylamino or C.sub.1 -C.sub.3 dialkylamino and halo;c) R.sub.4, R.sub.5 and R.sub.6 are each independently selected from hydrogen; unsubstituted C.sub.1 -C.sub.3 alkanyl, alkenyl or alkynyl; cycloalkanyl, cycloalkenyl; unsubstituted C.sub.1 -C.sub.3 alkylthio or alkoxy; hydroxy; thio; nitro; cyano; amino; C.sub.1 -C.sub.3 alkylamino or C.sub.1 -C.sub.3 dialkylamino; halo; and 2-imidazolinylamino; and wherein one and only one of R.sub.4, R.sub.5 and R.sub.6 is 2-imidazolinylamino;d) R.sub.7 is selected from hydrogen; unsubstituted C.sub.1 -C.sub.Type: GrantFiled: April 13, 1999Date of Patent: December 19, 2000Assignee: The Procter & Gamble CompanyInventors: Raymond Todd Henry, Russell James Sheldon, William Lee Seibel
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Patent number: 6160127Abstract: A process for the preparation of 5,6-disubstituted indoles in which a 4-5-disubstituted-2,.beta.-nitrostyrene is subjected to a reductive cyclization in the presence of a water soluble dithionite salt.Type: GrantFiled: July 15, 1998Date of Patent: December 12, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Giuseppe Prota, Gottfried Wenke
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Patent number: 6110956Abstract: Compounds effective in treating disorders of the serotonin-affected neurological systems are provided, such compounds having the following formula: ##STR1## wherein: R.sub.1 and R.sub.2 are each, independently, hydrogen, halogen, CF.sub.3, lower alkyl, lower alkoxy, MeSO.sub.2, or together can form a 5-7 membered carbocyclic or heterocyclic ring;R.sub.3 is alkoxy, halogen, hydrogen or carbamoyl;R.sub.4 is hydrogen, hydroxy, lower alkyl, or lower alkoxy;R.sub.5 is hydrogen, lower alkyl, or halogen;R.sub.6 is hydrogen, lower alkyl, or phenyl;R.sub.7 is hydrogen, lower alkyl, lower alkoxy, halogen, CN, CF.sub.3, or hydroxy; andX is (CH.sub.2).sub.n,wherein n is 0 to 3; or pharmaceutically acceptable salts thereof.Type: GrantFiled: April 7, 1999Date of Patent: August 29, 2000Assignee: American Home Products Corp.Inventors: Richard E. Mewshaw, Dahui Zhou, Ping Zhou
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Patent number: 6103752Abstract: Compounds of formula (I) ##STR1## wherein R and R.sup.1 are hydrogen, C.sub.1-4 alkyl or are linked to form a ring,A is a cycloalkyl or alkyl-cycloalkyl group,n is an integer from 0 to 3,W is an optionally substituted 5- or 6-membered heterocyclic ring; or W is an optionally substituted aryl, heteroaryl, aryloxy or thiophenoxy group; orW is a group --SO.sub.2 NR.sup.6 R.sup.7 --NHC(O)R.sup.6 R.sup.7 or --C(O)NHR.sup.6 R.sup.7 ;are useful in treating clinical conditions for which a "5-HT.sub.1 -like" receptor agonist is indicated.Type: GrantFiled: February 23, 1999Date of Patent: August 15, 2000Assignee: Glaxo Wellcome Inc.Inventors: Robert Charles Glen, David Lawrence Selwood, Graeme Richard Martin, Christopher James Foster
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Patent number: 6090839Abstract: The instant invention is concerned with aryl and heteroaryl oxyacetic acid type compounds which are useful antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and related diseases and for lowering triglyceride levels are also disclosed.Type: GrantFiled: December 19, 1997Date of Patent: July 18, 2000Assignee: Merck & Co., Inc.Inventors: Alan D. Adams, Derek Von Langen, Richard L. Tolman, Hiroo Koyama
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Patent number: 6071947Abstract: The present invention relates to substituted (1H-indol-2-yl)-5[(2H-pyrrol-2-ylidene) methyl]-1H-pyrrole compounds and their use as immunomodulating agents, to the preparation of the compounds and to pharmaceutical compositions comprising them.Type: GrantFiled: November 12, 1998Date of Patent: June 6, 2000Assignee: Pharmacia & Upjohn S.p.A.Inventors: Roberto D'Alessio, Marcellino Tibolla, Alberto Bargiotti, Anna Maria Isetta, Mario Ferrari, Francesco Colotta
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Patent number: 6066744Abstract: Presentation of a method for producing a 5-methylindoline represented by the formula: ##STR1## (wherein R is a hydrogen atom or a lower alkyl group), which comprises catalytically hydrogenating a 1-(substituted)benzyl-5-formylindoline represented by the formula: ##STR2## (wherein R.sup.1 is a hydrogen atom or a lower alkyl group, and R.sup.2 is a hydrogen atom, a lower alkyl group or a lower alkoxy group) in the presence of an inert solvent and a palladium catalyst.Type: GrantFiled: October 7, 1999Date of Patent: May 23, 2000Assignee: Ihara Chemical Industry Co., Ltd.Inventors: Hideo Ooi, Toshihisa Watanabe, Chikara Hijikata
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Patent number: 6063806Abstract: A heterocyclic derivative of the formula (I) ##STR1## wherein each symbol is as defined in the specification, and pharmaceutically acceptable salts thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof exhibit superior ACAT inhibitory activity and lipoperoxidation inhibitory activity in mammals, and are useful as ACAT inhibitors and lipoperoxidation inhibitors. Specifically, they are useful for the prophylaxis and treatment of arteriosclerosis, hyperlipemia, arteriosclerosis in diabetes, and cerebrovascular and cardiovascular ischemic diseases.Type: GrantFiled: April 3, 1998Date of Patent: May 16, 2000Assignee: Kyoto Pharmaceutical Industries, Ltd.Inventors: Shoji Kamiya, Hiroaki Shirahase, Hiroshi Matsui, Shohei Nakamura, Katsuo Wada
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Patent number: 6060498Abstract: The present invention provides a preparation for injection comprising an antitumor agent which is sparingly soluble in water.Specifically, it provides a composition containing N-(3-chloro-1H-indol-7-yl)-4-sulfamoylbenzenesulfonamide, which contains N-(3-chloro-1H-indol-7-yl)-4-sulfamoylbenzenesulfonamide and a basic substance and will provide an aqueous solution having a pH of 7 or higher when dissolved in water.Type: GrantFiled: August 26, 1998Date of Patent: May 9, 2000Assignee: Eisai Co., Ltd.Inventors: Kazuhide Ashizawa, Hidenobu Ando
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Patent number: 6046190Abstract: The invention relates to sulfonamide-containing hydroxyethylamine protease inhibitor compounds, their process of making, composition and method of use for inhibiting retroviral proteases such as human immunodeficiency virus.Type: GrantFiled: January 24, 1996Date of Patent: April 4, 2000Assignee: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Deborah E. Bertenshaw, Robert M. Heintz
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Patent number: 5994546Abstract: Disclosed are 4-(N,N-dialkylamino)aniline compounds having a 4-N substituent which is a polyethyleneoxy group and which forms a condensed ring with benzene ring, such as aniline compounds having the following structure, a processing composition containing such a compound and a method for forming a color image with the processing solution. The aniline compound is useful as a color developing agent capable of having a low fog density and sufficient yellow and cyan image densities and suitable for the rapid process.Type: GrantFiled: February 11, 1998Date of Patent: November 30, 1999Assignee: Fuji Photo Film Co., Ltd.Inventors: Keizo Kimura, Shigeo Hirano, Hiroshi Kawamoto
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Patent number: 5990150Abstract: Heterocyclic derivatives of the formula (I) ##STR1## wherein each symbol is as defined in the specification, pharmaceutically acceptable salts thereof and method of producing them. Pharmaceutical compositions containing the heterocyclic derivative or a pharmaceutically acceptable salt thereof, particularly, ACAT inhibitors and lipoperoxidation inhibitors. The heterocyclic derivatives and pharmaceutically acceptable salts thereof of the present invention show superior ACAT inhibitory activity and lipoperoxidation inhibitory activity, and are useful as ACAT inhibitors and hyperlipemia inhibitors. To be specific, they are useful for the prevention and treatment of arteriosclerotic lesions of arteriosclerosis, hyperlipemia and diabetes, as well as ischemic diseases of brain, heart and the like.Type: GrantFiled: March 19, 1997Date of Patent: November 23, 1999Assignee: Sankyo Company, Ltd.Inventors: Hiroshi Matsui, Shoji Kamiya, Hiroaki Shirahase, Shohei Nakamura, Katsuo Wada
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Patent number: 5985910Abstract: The present invention relates to new 3-[4-(2-Phenyl-Indole-1-ylmethyl)-Phenyl]-Acrylamide compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, the compounds having the following general structure.Type: GrantFiled: April 14, 1997Date of Patent: November 16, 1999Assignee: American Home Products CorporationInventors: Chris P. Miller, Bach D. Tran
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Patent number: 5958965Abstract: Compounds of the formula: ##STR1## in which R.sub.1 is hydrogen, alkyl, cycloalkylalkyl, arylalkyl, (haloaryl)alkyl, (alkoxyaryl)alkyl, thienylmethyl, furanylmethyl, pyridinylmethyl, alkylphenyl, 4-fluorobutyrophenone or 6-fluoro-1,2-benzisoxazol-yl-propyl; X is hydrogen, halogen, cyano, alkyl, acetyl, trifluoroacetyl, trifluoromethyl or formyl; Y is hydrogen, halogen, alkoxy or alkyl; or a pharmaceutically acceptable salt thereof are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analagous drugs and they also have affinity for the 5-HT.sub.1A receptors which characterizes them as useful in the treatment of diseases attending disturbances in the serotinergic systems, such as anxiety, stress, depression, sexual dysfunctions and sleep disturbances.Type: GrantFiled: August 12, 1997Date of Patent: September 28, 1999Assignee: American Home Products CorporationInventors: Richard Eric Mewshaw, Michael Byron Webb
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Patent number: 5955492Abstract: This invention relates to novel carboxylic acid indole compounds and compositions for use in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: GrantFiled: September 24, 1998Date of Patent: September 21, 1999Assignee: SmithKline Beecham CorporationInventors: Scott K. Thompson, Stacie M. Halbert, Katherine L. Widdowson
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Patent number: 5936098Abstract: This invention concerns a method for the production of a 3-arylindoline compound represented by the general formula ##STR1##Type: GrantFiled: August 14, 1997Date of Patent: August 10, 1999Assignee: Tokyo Tanabe Company LimitedInventors: Nobuyuki Yasuda, Shin-ichi Kunii, Kouichi Kazama
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Patent number: 5932743Abstract: The present invention relates to novel substituted indole compounds of formula (I) ##STR1## having pharmacological activity, to processes for their preparation, to solid phase methods for preparing libraries of the compounds, to utilizing libraries of the compounds for drug discovery, and to pharmaceutical compositions thereof.Type: GrantFiled: July 29, 1998Date of Patent: August 3, 1999Assignee: American Home Products CorporationInventors: Michael D. Collini, John W. Ellingboe
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Patent number: 5929265Abstract: Binuclear iridium (I) phosphine complexes of the general formula: ##STR1## in which X is fluorine, chlorine, bromine or iodine, and ##STR2## is in each case a chiral bidentate diphosphine ligand. The complexes are particularly suitable as catalysts for the inter- or intramolecular asymmetric hydroamination of prochiral olefins.Type: GrantFiled: October 13, 1998Date of Patent: July 27, 1999Assignee: Lonza AGInventors: Romano Dorta, Patrick Egli, Nikolaus H Bieler, Antonio Togni, Martin Eyer
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Patent number: 5919469Abstract: Products derived from 2-imino-2,3-dihydro-1H-indoles resulting from the oxidative polymerization of at least one compound of formula (I) or (II) below: ##STR1## in which: R.sub.1, R.sub.2 and R.sub.3 denote hydrogen, alkyl, carboxyl, alkoxycarbonyl, monohydroxyalkyl, polyhydroxyalkyl, alkoxyalkyl, monoalkylaminoalkyl or dialkylaminoalkyl; R'.sub.3 and R.sub.4 denote alkyl, carboxyl, alkoxycarbonyl, monohydroxyalkyl, polyhydroxyalkyl, alkoxyalkyl, monoalkylaminoalkyl or dialkylaminoalkyl;R.sub.5 denotes hydrogen, alkyl, monohydroxyalkyl, polyhydroxyalkyl, alkoxyalkyl, monoalkylaminoalkyl or dialkylaminoalkyl;and to the addition salts thereof with an acid, as well as to their uses in cosmetics for making up the exoskeleton and/or the skin.Type: GrantFiled: August 22, 1997Date of Patent: July 6, 1999Assignee: L'OrealInventor: Alain Lagrange
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Patent number: 5891902Abstract: The present invention relates to indole derivatives represented by formula (I): ##STR1## wherein R.sup.1 and R.sup.2 independently represent hydrogen, lower alkyl, hydroxy, lower alkoxy, halogen, --O--(CH.sub.2).sub.n --OR.sup.5, or ##STR2## R.sup.3 represents hydrogen, lower alkyl, or ##STR3## R.sup.4 represents hydroxy, lower alkoxy, substituted or unsubstituted aryloxy, or --NR.sup.10 R.sup.11, and X represents CO or SO.sub.2, with the proviso that when R.sup.3 is hydrogen or lower alkyl, and X is CO, R.sup.4 is --NR.sup.10 R.sup.11, or pharmaceutically acceptable salts thereof.Type: GrantFiled: July 15, 1996Date of Patent: April 6, 1999Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Daisuke Machii, Haruki Takai, Nobuo Kosaka, Hisakatsu Seo, Tomomi Sugiyama, Joji Nakamura, Hiroyuki Ishida, Katsushige Gomi, Soichiro Sato, Masako Uchii, Koji Suzuki
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Patent number: 5886191Abstract: The present application describes amidinoindoles, amidinoazoles, and analogs thereof of formula I: ##STR1## wherein W, W.sup.1, W.sup.2, and W.sup.3 are selected from CH and N, provided that one of W.sup.1 and W.sup.2 is C(C(.dbd.NH)NH.sub.2) and at most two of W, W.sup.1, W.sup.2, and W.sup.3 are N and one of J.sup.a and J.sup.b is substituted by --(CH.sub.2).sub.n --Z--A--B, which are useful as inhibitors of factor Xa or thrombin.Type: GrantFiled: August 18, 1997Date of Patent: March 23, 1999Assignee: DuPont Pharmaceuticals CompanyInventors: Celia Dominguez, Qi Han, Daniel Emmett Duffy, Jeongsook Maria Park, Mimi Lifen Quan, Karen Anita Rossi, Ruth Richmond Wexler
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Patent number: 5874588Abstract: Diketopyrrolopyrroles of formula I ##STR1## are prepared by reacting a diketopyrrolopyrrole of formula II ##STR2## with a) formic acid or b) a compound of formula IIIX'--H (III)or with an alkali metal formate or alkaline earth metal formate together with carbon monoxide in the presence of a catalyst, wherein, in formulae I, II and III, A is a direct bond or a group ##STR3## wherein phenylene is bound to the pyrrolopyrrole, R.sub.1, R.sub.2 and R.sub.3 are each independently of one another hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.6 cycloalkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylamino, C.sub.1 -C.sub.6 alkylmercapto, --CF.sub.3, --CN or --NO.sub.2, X is X' or OH, X' is --OR.sub.4 or --N(R.sub.5)(R.sub.6), wherein R.sub.4 is C.sub.1 -C.sub.18 alkyl, C.sub.5 -C.sub.6 cycloalkyl; phenyl or naphthyl which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylamino, --CN or --NO.sub.2, R.sub.5 and R.sub.Type: GrantFiled: September 19, 1997Date of Patent: February 23, 1999Assignee: Ciba Specialty Chemicals CorporationInventors: Bernd Lamatsch, Olof Wallquist
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Patent number: 5864045Abstract: The present invention relates to substituted piperazinone derivatives of formula (1) or stereoisomers, or pharmaceutically acceptable salts thereof and their use as tachykinin receptor antagonists. Such antagonists are useful in the treatment of tachykinin-mediated diseases and conditions disclosed herein including: asthma, cough, and bronchitis. The present invention also relates to intermediates useful in the preparation of compounds of formula (1).Type: GrantFiled: April 27, 1998Date of Patent: January 26, 1999Assignee: Hoechst Marion Roussel, Inc.Inventors: Timothy P. Burkholder, Elizabeth M. Kudlacz, Tieu-Binh Le
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Patent number: 5856529Abstract: Novel derivatives of benzofuran and dihydrobenzofuran are provided which are useful as melatonergic agents.Type: GrantFiled: December 9, 1997Date of Patent: January 5, 1999Assignee: Bristol-Myers Squibb CompanyInventors: John D. Catt, Graham Johnson, Daniel J. Keavy, Ronald J. Mattson, Michael F. Parker, Katherine S. Takaki, Joseph P. Yevich
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Patent number: 5849710Abstract: The present invention relates to indol-3-ylmethylene-2-oxindole derivatives which are useful as tyrosine kinase inhibitors. The compounds are suitable for use as anti-proliferative agents, anti-metastatic agents, anti-cancer agents, and in the control of angiogenesis and in inhibiting the development of atheromatous and an immunomogulating agents.Type: GrantFiled: December 4, 1996Date of Patent: December 15, 1998Assignee: Pharmacia & Upjohn S.p.A.Inventors: Carlo Battistini, Dario Ballinari, Antonella Ermoli, Sergio Penco, Sergio Vioglio
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Patent number: 5776497Abstract: A mineral or organic particle-based product comprising an indoline product, a method for preparing same, and the use thereof in cosmetics. The product is a powder consisting of mineral or organic particles smaller than 200 microns, and comprises, in and/or on the particles, an indoline product obtained by oxidative polymerization using at least one indoline.Type: GrantFiled: June 7, 1995Date of Patent: July 7, 1998Assignee: L'OrealInventors: Alain Lagrange, Herve Andrean, Alex Junino
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Patent number: 5721276Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which A, B, X and R.sub.1 are as defined in the description, and medicinal product containing the same useful for treating a disorder of the melatoninergic system.Type: GrantFiled: May 30, 1996Date of Patent: February 24, 1998Assignee: Adir et CompagnieInventors: Isabelle Lesieur, Patrick Depreux, Veronique Leclerc, Philippe Delagrange, Pierre Renard, Beatrice Guardiola Lemaitre