The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 544/125)
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Patent number: 6956035Abstract: The invention provides novel classes of Isoquinoline Derivatives. Pharmaceutical compositions and methods of making and using the compounds, are also described.Type: GrantFiled: February 28, 2003Date of Patent: October 18, 2005Assignee: Inotek Pharmaceuticals CorporationInventors: Prakash Jagtap, Erkan Baloglu, John H. van Duzer, Csaba Szabo, Andrew L. Salzman
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Patent number: 6933302Abstract: (20) esters of camptothecin analogs are provided. The compounds are (20) esters of an aminoalkanoic acid or an imidoalkanoic acid and homocamptothecin, which is optionally substituted at the 7, 9, 10, 11, and 12 positions of the homocamptothecin ring. The compounds are useful for treating cancer.Type: GrantFiled: June 3, 2003Date of Patent: August 23, 2005Assignees: California Pacific Medical Center, Catholic Healthcare WestInventor: Li-Xi Yang
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Patent number: 6927292Abstract: The invention relates to compounds of Formula (1), in which the substituents and symbols have the meanings indicated in the description. The compounds are valuable intermediates for the preparation of pharmaceutical active compounds.Type: GrantFiled: July 31, 2002Date of Patent: August 9, 2005Assignee: Altana Pharma AGInventors: Jörg Senn-Bilfinger, Peter Jan Zimmermann
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Patent number: 6906063Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 2, 2001Date of Patent: June 14, 2005Assignee: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Wolin Huang, Charles K. Marlowe, Kim A. Kane-MaGuire
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Patent number: 6894041Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; —G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems recitType: GrantFiled: November 20, 2002Date of Patent: May 17, 2005Assignee: Pfizer IncInventors: Anthony Marfat, Michael William McKechney
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Patent number: 6869945Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N?(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; -G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems reType: GrantFiled: November 20, 2002Date of Patent: March 22, 2005Assignee: Pfizer IncInventors: Anthony Marfat, Michael William McKechney
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Patent number: 6838456Abstract: Compounds of the general structural formula and use of the compounds and salts and solvates thereof, as therapeutic agents.Type: GrantFiled: September 17, 2001Date of Patent: January 4, 2005Assignee: Lilly ICOS LLCInventors: Mark W. Orme, Jason Scott Sawyer, Alain Claude-Marie Daugan, Françoise Gellibert, Romain Luc Marie Gosmini
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Publication number: 20040254163Abstract: Compositions for treating cancer comprising an amount of a camptothecin with a 7-ring &bgr;-hydroxy lactone ring of the formula 1Type: ApplicationFiled: June 7, 2004Publication date: December 16, 2004Applicant: SOCIETE DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES (S.C.R.A.S.)Inventors: Dennis Bigg, Olivier Lavergne, Francesc Pla Rodas, Jacques Pommier, Gerard Ulibarri, Jerry Harnett, Alain Rolland, Anne-Marie Liberatore, Christophe Lanco, Jean-Bernard Cazaux, Christine Le Breton, Eric Manginot
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Publication number: 20040248889Abstract: Substituted 5,6,6a, 11b-tetrahydro-7-oxa-5-aza-benzo[c]fluorene-6-carboxylic acid compounds, and processes for the production thereof, pharmaceutical compositions containing these compounds and the use thereof in treatment methods and for the production of pharmaceutical preparations for specific indications, in particular for the treatment of pain.Type: ApplicationFiled: February 3, 2004Publication date: December 9, 2004Applicant: Gruenenthal GmbHInventors: Matthias Gerlach, Michael Przewosny, Werner Guenter Englberger, Elke Reissmueller, Petra Bloms-Funke, Corinna Maul, Utz-Peter Jagusch
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Patent number: 6828319Abstract: The invention provides novel classes of substituted Indeno[1,2-c]isoquinoline Compounds. Pharmaceutical compositions and methods of making and using the compounds, are also described.Type: GrantFiled: August 30, 2002Date of Patent: December 7, 2004Assignee: Inotek Pharmaceuticals CorporationInventors: Prakash Jagtap, Erkan Baloglu, John H. van Duzer, Csaba Szabo, Andrew L. Salzman
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Patent number: 6825208Abstract: This invention relates generally to tetracyclic tetrahydroquinoline compounds, and analogues thereof, and pharmaceutically acceptable salt forms thereof, which are selective inhibitors of serine protease enzymes, especially factor VIIa; pharmaceutical compositions containing the same; and methods of using the same as anticoagulant agents for modulation of the coagulation cascade.Type: GrantFiled: August 20, 2002Date of Patent: November 30, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Jinglan Zhou, Leslie Robinson, Nikolaus M. Gubernator, Eddine Saiah, Xu Bai, Xin Gu
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Patent number: 6809096Abstract: A pharmaceutical composition including an efficient amount of a compound selected among the compounds of formulae (I) and (Ia). The compounds have interesting cytotoxic properties leading to a therapeutic use as antitumoral medicines.Type: GrantFiled: February 13, 2002Date of Patent: October 26, 2004Assignee: Laboratoire L. LafonInventors: Evelyne Delfourne, Francis Darro, Jean Bastide, Robert Kiss, Armand Frydman
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Publication number: 20040029879Abstract: The present invention provides a compound of formula I 1Type: ApplicationFiled: July 31, 2003Publication date: February 12, 2004Inventors: David John Anderson, Thomas J. Beauchamp, Gordon L. Bundy, Fred L. Ciske, John R. Farrell, David R. Graber, Michael J. Genin, Thomas M. Judge, Malcolm Wilson Moon, Mark E. Schnute, Joseph Walter Strohbach, Suvit Thaisrivongs, Atli Thorarensen, Steven Ronald Turner, Valerie A. Vaillancourt, Allison J. Wolf
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Publication number: 20040009977Abstract: The present invention relates to substituted 1,4-dihydro-4-oxoquinolines having antiviral activity. The substituents are present at positions 1, 2 and at least one of 5-8 positions of the quinoline ring.Type: ApplicationFiled: February 21, 2003Publication date: January 15, 2004Applicant: Maruishi Pharmaceutical Co., Ltd.Inventors: Takashi Tamura, Haruo Kuriyama, Masanobu Agoh, Yumi Agoh, Manabu Soga, Teruyo Mori
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Publication number: 20030216386Abstract: The invention relates to isoxazole and oxadiazole compounds of Formulae I and II, 1Type: ApplicationFiled: April 10, 2003Publication date: November 20, 2003Inventors: Michele A. Weidner-Wells, Todd C. Henninger, Dennis J. Hlasta
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Patent number: 6642248Abstract: A compound selected from those of formula (I): wherein: X and Y represent group selected from hydrogen, halogen, mercapto, cyano, nitro, alkyl, trihaloalkyl, trihaloalkylcarbonylamino, —ORa, —NRaRb, —NRa—C(O)—T1, —O—C(O)—T1, —O—T2-NRaRb, —O—T2-ORa, —NRa—T2-NRaRb, —NRa—T2-ORa and —NRa—T2-CO2Ra wherein Ra, Rb, T1, T2 are as defined in the description, R1 represents hydrogen or alkyl, R2 represents a group selected from hydrogen, —ORa, —NRaRb, —NRa—C(O)—T1, —O—C(O)—T1, —O—T2-NRaRb, —O—T2-ORa, —NRa—T2-NRaRb, —NRa—T2-ORa and —NRa—T2-CO2Ra wherein Ra, Rb, T1 and T2 are as defined hereinbefore, R3 and R4 represent hydrogen or alkyl, W represents a group of formula —CH(R5)—CH(R6)—, —CH═C(R7)—, —C(R7)═CH— or —C(O)—CH(R8)Type: GrantFiled: July 25, 2002Date of Patent: November 4, 2003Assignee: Les Laboratories ServierInventors: Michel Koch, François Tillequin, Sylvie Michel, Elisabeth Seguin, Abdelhakim El Omri, John Hickman, Alain Pierre, Bruno Pfeiffer, Pierre Renard
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Publication number: 20030176694Abstract: Compounds, compositions and methods are provided that are useful in the treatment and/or prevention of a condition or disorder mediated by a G-protein coupled receptor. In particular, the compounds of the invention are useful in the treatment and/or prevention of eating disorders, obesity, anxiety disorders and mood disorders.Type: ApplicationFiled: November 6, 2002Publication date: September 18, 2003Inventors: Xiaoqi Chen, Pingchen Fan, Juan Jaen, Leping Li, Mike Lizarzaburu, Jeffrey Thomas Mihalic, Stephen Joseph Shuttleworth
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Patent number: 6605610Abstract: Compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of neurological and psychological disorders.Type: GrantFiled: February 25, 2000Date of Patent: August 12, 2003Assignee: Pfizer IncInventors: Jotham Wadsworth Coe, Paige Roanne Palmer Brooks
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Patent number: 6602867Abstract: Triazole compounds of the following formula where R1, R2, A and B have the meanings given in the description are described. The compounds according to the invention possess a high affinity for the dopamine D3 receptor and can therefore be used for treating diseases which respond to the influence of dopamine D3 ligands.Type: GrantFiled: July 11, 2001Date of Patent: August 5, 2003Assignee: Abbott LaboratoriesInventors: Dorothea Starck, Hans-Jörg Treiber, Liliane Unger, Barbara Neumann-Schultz, Kai Blumbach, Dietmar Schöbel
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Patent number: 6545011Abstract: This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.Type: GrantFiled: July 2, 2001Date of Patent: April 8, 2003Assignee: Guilford Pharmaceuticals Inc.Inventors: Jia-He Li, Jie Zhang, Vincent J. Kalish
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Publication number: 20030004150Abstract: A compound of the formula 1Type: ApplicationFiled: February 6, 2002Publication date: January 2, 2003Inventors: Dennis Bigg, Olivier Lavergne, Francesc Pla Rodas, Jacques Pommier, Gerard Ulibarri, Jerry Harnett, Alain Rolland, Anne-Marie Liberatore, Christophe Lanco, Jean-Bernard Cazaux, Christine Le Breton, Eric Manginot
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Patent number: 6500824Abstract: The invention provides kappa receptor antagonists of formula (I), wherein R1-R6 X and Y have any of the meanings given in the specification, as well as compositions comprising them, and methods for their use.Type: GrantFiled: February 6, 2001Date of Patent: December 31, 2002Assignee: Regents of the University of MinnesotaInventors: Philip S. Portoghese, Robert M. Jones
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Publication number: 20020160994Abstract: A process for the preparation of a compound of the formula 1Type: ApplicationFiled: January 30, 2002Publication date: October 31, 2002Applicant: SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES (S.C.R.A.S.)Inventors: Dennis Bigg, Olivier Lavergne, Francesc Pla Rodas, Jacques Pommier, Gerard Ulibarri, Jerry Harnett, Alain Rolland, Anne-Marie Liberatore, Christophe Lanco, Jean-Bernard Cazaux, Christine Le Breton, Eric Manginot
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Publication number: 20020132824Abstract: Compounds of the formula 1Type: ApplicationFiled: April 23, 2002Publication date: September 19, 2002Inventors: Jotham Wadsworth Coe, Paige Roanne Palmer Brooks
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Publication number: 20020111350Abstract: Compounds of the formula 1Type: ApplicationFiled: April 22, 2002Publication date: August 15, 2002Inventors: Jotham Wadsworth Coe, Paige Roanne Palmer Brooks
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Patent number: 6410550Abstract: Compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are defined as in the specification, intermediates in the synthesis of such compounds. pharmaceutical compositions containing such compounds and methods of using such compounds, in the treatment of neurological and psychological disorders.Type: GrantFiled: September 28, 1999Date of Patent: June 25, 2002Assignee: Pfizer INCInventors: Jotham Wadsworth Coe, Paige Roanne Palmer Brooks
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Patent number: 6406533Abstract: A 6,13-dihydroquinacridone derivative of formula I: (MO3S)m—Q—[CH2—(X)—(Y)n]o (I) wherein: Q represents a 6,13-dihydroquinacridone moiety of formula II; A and B each independently represent a substituent selected from H, F, Cl, C1-C3alkyl and C1-C3alkoxy M represents a metal cation, quaternary N cation or H; X is an aromatic group, a cyclo-hetero aliphatic group with at least one 5 or 6 atom ring or a hetero aromatic group with at least one 5 or 6 atom ring and which is not a phthalimido group; Y is a sulfonic or carboxylic acid or salt thereof; m and n independently from each other are numbers from zero to 2.5; and o is a number from zero to 4, wherein m and o are not zero simultaneously.Type: GrantFiled: March 7, 2001Date of Patent: June 18, 2002Assignee: Ciba Specialty Chemicals CorporationInventor: Fridolin Bäbler
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Patent number: 6407115Abstract: Accordingly, an object of this invention is to provide a hexa-cyclic compound represented by the following general formula: wherein R1 and R2 individually represent a hydrogen atom, a hydroxyl group, a C1-6 alkyl group (“C1-6 alkyl group means an alkyl group having 1 to 6 carbon atoms. Hereinafter defined in the same manner.) The present inventors have conducted extensive studies for the purpose of obtaining camptothecin derivatives with more excellent activity and higher safety, as well as excellent characteristics required for a drug to be administered, and found that hexa-cyclic compounds obtained by the addition of a water-soluble ring to camptothecin had characteristics superior to camptothecin. This finding has led to the completion of this invention.Type: GrantFiled: May 26, 1995Date of Patent: June 18, 2002Assignees: Daiichi Pharmaceutical Co., Ltd., Kabushiki Kaisha Yakult HonshaInventors: Hirofumi Terasawa, Akio Ejima, Satoru Ohsuki, Kouichi Uoto
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Patent number: 6376491Abstract: The present invention is directed to new bicyclic compounds of the formula [I], and pharmaceutically acceptable salts thereof wherein R1, R2, R3, R4, R5, R6, R7, Q1 Q2 and Q3 are as defined in the claims. The compounds have N-myristoyltransferase inhibitory and antifungal activity.Type: GrantFiled: December 15, 1999Date of Patent: April 23, 2002Assignee: Basilea Pharmaceutica AGInventors: Yuhko Aoki, Hirosato Ebiike, Toshihiko Fujii, Kenichi Kawasaki, Pingli Liu, Miyako Masubuchi, Tatsuo Ohtsuka, Shinji Tsujii
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Publication number: 20020022624Abstract: The present invention relates to compounds of the formula (I): 1Type: ApplicationFiled: July 11, 2001Publication date: February 21, 2002Inventors: Kevin Dinnell, Jason Matthew Elliott, Gregory John Hollingworth, Duncan Edward Shaw
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Patent number: 6288073Abstract: A compound selected from those of formula (I): in which: X and Y represent hydrogen, halogen, hydroxy, mercapto, cyano, nitro, alkyl, alkoxy, trihaloalkyl, optionally substituted amino, methylenedioxy, or ethylenedioxy, R1 represents hydrogen, or alkyl, R2 represents hydrogen, hydroxy, alkyl, alkoxy, alkylcarbonyloxy, or optionally substituted ammo, R3 and R4 represent hydrogen, or alkyl, A represents —CH═CH—, or —CH(R5)—CH(R6)— wherein R5 and R6 are as defined in the description, their isomers, N-oxides, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful in the treatment of cancer.Type: GrantFiled: June 19, 2000Date of Patent: September 11, 2001Assignee: Adir et CompagnieInventors: Michel Koch, François Tillequin, Sylvie Michel, Ghanem Atassi, Alain Pierre, Bruno Pfeiffer, Pierre Renard
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Patent number: 6274728Abstract: Compounds of formula A(B)x (I), wherein x is an integer from 1 to 8, A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, indanthrone, isoindolinone, isoindoline, dioxazine, azo, phthalocyanine or diketopyrrolopyrrole series that is bonded to x groups B via one or more hetero atoms, those hetero atoms being selected from the group consisting of N, O and S and forming part of the radical A, each group B independently of any other(s) is hydrogen or a group of the formula at least one group B being a group of the formula The compounds according to the invention are used in high-molecular-weight organic materials, thermo-, photo- or chemo-sensitive recording materials, light-sensitive negative or positive resist compositions, ink compositions for ink-jet printing and color tapes for thermal transfer printing.Type: GrantFiled: December 16, 1999Date of Patent: August 14, 2001Assignee: Ciba Specialty Chemicals Corp.Inventors: Véronique Hall-Goulle, Aline Bize
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Patent number: 6264733Abstract: Pigment particle growth and/or crystal phase directors of the following formula: (MO3S)m—Q—(CH2—(X)—(Y)n)o wherein: Q represents a pigment moiety; M represents a metal cation, quaternary N cation or H; X is an aromatic group, a cyclo-hetero aliphatic group with at least one 5 atom or 6 atom ring or a hetero aromatic group with at least one 6 atom ring and which is not a phthalimido group; Y is a sulfonic or carboxylic acid or salt thereof; m and n independently from each other represent an integer from 0 to 2.5; and o is an integer from 0.05 to 4.Type: GrantFiled: February 2, 2000Date of Patent: July 24, 2001Assignee: Ciba Specialty Chemicals CorporationInventor: Fridolin Bäbler
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Patent number: 6133288Abstract: The present invention provides compounds of formula I and II: ##STR1## wherein X is --O--, --S--, or --NR.sup.5 --;Y is --O--, --S--, --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, or --NR.sup.5 --;B is --CH.sup.2 -- or --CO--;R.sup.1, R.sup.2, and R.sup.3 are each independently --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl), --OSO.sub.2 CF.sub.3, Cl, or F;n is 1 or 2;W is CH.sub.2 or C.dbd.O;R.sup.4 is 1-piperidinyl, 2-oxo-1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 2-oxo-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino;R.sup.5 is C.sub.1 -C.sub.3 alkyl, --COC.sub.6 H.sub.5, --CO(C.sub.1 -C.sub.6 alkyl), --C(O)OC.sub.6 H.sub.5, --C(O)O(C.sub.1 -C.sub.6 alkyl), --SO.sub.2 (C.sub.1 -C.sub.6 alkyl), --SO.sub.2 C.sub.6 H.sub.5, or --SO.sub.2 CF.sub.3 ;or a pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: November 9, 1999Date of Patent: October 17, 2000Assignee: Eli Lilly and CompanyInventor: Timothy Alan Grese
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Patent number: 6030967Abstract: A compound of the formula: whereinQ is an optionally substituted carbon atom or N(O)p wherein p is 0 or 1;Y is an optionally substituted methylene group, S(O)q wherein q is an integer of 0 to 2, or an optionally substituted imino group;Z.sup.1 is a C.sub.1-3 alkylene group which may have an oxo group or a thioxo group and may contain etherified oxygen or sulfur within the carbon chain;Z.sup.2 is an optionally substituted C.sub.1-3 alkylene group;Ar is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group;one of R.sup.1 and R.sup.2 is a hydrogen atom, a halogen atom, a hydroxyl group, an optionally substituted lower alkyl group, or an optionally substituted lower alkoxy group;the other is a halogen atom, a hydroxyl group, an optionally substituted lower alkyl group, or an optionally substituted lower alkoxy group; orR.sup.1 and R.sup.2 taken together with adjacent --c.dbd.c-- form a ring; andring A is a benzene ring which may be substituted in addition to R.sup.1 and R.Type: GrantFiled: October 30, 1997Date of Patent: February 29, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Shogo Marui, Masatoshi Hazama, Kohei Notoya, Masaki Ogino
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Patent number: 6013796Abstract: For the synthesis of 3-methylnaltrexone from codeine in this invention, codeine is converted to 6-acetylcodeine, which is N-demethylated to 6-acetylcodeine hydrochloride, followed by alkylating the nitrogen to form 17-cyclopropylmethylnorcodeine. The latter is oxidized to 17-cyclopropylmethylnorcodeinone. For the synthesis of naltrexone from morphine in this invention, morphine is converted to 3-benzylnormorphine as described above in the synthesis of noroxymorphone. 3-Benzylnormorphine is reacted with cyclopropylmethyl halide to produce 3-benzyl-17cyclopropylmethylnormorphine, a novel compound, which is oxidized to 3-benzyl-17-cyclopropylmethyl-normorphinone, a novel compound, by Swern oxidation.Type: GrantFiled: July 16, 1998Date of Patent: January 11, 2000Assignee: Penick CorporationInventors: Bao-Shan Huang, Yansong Lu, Ben-Yi Ji, Aris P Christodoulou
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Patent number: 6004971Abstract: The present invention provides compounds of formula I and II: ##STR1## wherein X is --O--, --S--, or --NR.sup.5 --;Y is --O--, --S--, --CH.sub.2 --, --Ch.sub.2 CH.sub.2 --, --CH.dbd.CH--, or --NR.sup.5 --;B is --CH.sup.2 -- or --CO--;R.sup.1, R.sup.2, and R.sup.3 are each independently --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl), --OSO.sub.2 CF.sub.3, Cl, or F;n is 1 or 2;W is CH.sub.2 or C.dbd.O;R.sup.4 is 1-piperidinyl, 2-oxo-1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 2-oxo-1-pyrrolidinyl, 4-morpholino, dimechylamino, diethylamino, or 1-hexamethyieneimino;R.sup.5 is C.sub.1 -C.sub.3 alkyl, --COC.sub.6 H.sub.5, --CO(C.sub.1 -C.sub.6 alkyl), --C(O)OC.sub.6 H.sub.5, --C(O)O(C.sub.1 -C.sub.6 alkyl), --SO.sub.2 (C.sub.1 -C.sub.6 alkyl), --SO.sub.2 C.sub.6 H.sub.5,or --SO.sub.2 CF.sub.3 ; or a pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: June 19, 1997Date of Patent: December 21, 1999Assignee: Eli Lilly and CompanyInventor: Timothy Alan Grese
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Patent number: 5981540Abstract: Compounds of formula (I), are selective delta opioid agonsist and antagonists, and are useful as analgesics and in treating general neurologic disorders.Type: GrantFiled: April 24, 1997Date of Patent: November 9, 1999Assignee: SmithKline Beecham Farmaceutici S.P.A.Inventors: Giulio Dondio, Silvano Ronzoni
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Patent number: 5965565Abstract: The present invention is directed to certain piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein B is selected from: ##STR2## and R.sup.1, R.sup.1a, R.sup.2a, R.sup.3a, R.sup.3b, R.sup.4, R.sup.4a, R.sup.4b, R.sup.4c, R.sup.5, D, X, Y, n, x and y are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.Type: GrantFiled: December 11, 1997Date of Patent: October 12, 1999Assignee: Merck & Co., Inc.Inventors: Meng H. Chen, Zhijian Lu, Ravi Nargund, Arthur A. Patchett, James R. Tata, Lihu Yang, Mu Tsu Wu
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Patent number: 5952495Abstract: A process is provided for preparing 14-hydroxynormorphinones having the formula: ##STR1## which comprises reacting normorphinones having the formula: ##STR2## wherein R is selected from the group consisting of lower alkyl of 1 to 7 carbon atoms, cycloalkyl-lower alkyl with 3-6 ring carbon atoms, benzyl and a substituted-benzyl having the formula: ##STR3## wherein Q and Q.sup.1 are individually selected from the group consisting of hydrogen, lower alkyl, trifluoromethyl, nitro, dialkylamino and cyano;R' is selected from the group consisting of R, 2-(4-morpholinyl)ethyl, benzyloxy carbonyl and R"C(O)-- wherein R" is lower alkyl of 1-4 carbon atoms;with hydrogen peroxide at a temperature of from about 15.degree. C. to about 70.degree. C. in the presence of an acid and an aqueous solvent system to solubilize the reactant for a period of time so as to form the 14-hydroxynormorphinones.Type: GrantFiled: July 16, 1998Date of Patent: September 14, 1999Assignee: Penick CorporationInventors: Bao-Shan Huang, Yansong Lu, Ben-Yi Ji, Aris P Christodoulou
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Patent number: 5874580Abstract: Compounds of formulaA(B).sub.x, (I),wherein x is an integer from 1 to 4, A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, isoindolinone, isoindoline, dioxazine, phthalocyanine or azo series, which radical contains x N-atoms attached to B, preferably with at least one directly adjacent or conjugated carbonyl group,B is a group of formula ##STR1## and, if x is 2,3 or 4, may also be one, two or three hydrogen atoms. The symbols Q, R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, Y, Z, m und n, are as defined in claim 1.These carbamate group-containing soluble chromophores are distinguished by outstanding solid state fluorescence in the UV range as well as the by ease with which they can be converted to the corresponding pigments in the substrate in which they are incorporated.Type: GrantFiled: June 2, 1998Date of Patent: February 23, 1999Assignee: Ciba Specialty Chemicals CorporationInventors: Zhimin Hao, John S. Zambounis, Abul Iqbal
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Patent number: 5843952Abstract: Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.Type: GrantFiled: July 8, 1997Date of Patent: December 1, 1998Assignee: American Cyanamid CompanyInventors: Jay Donald Albright, Fuk-Wah Sum
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Patent number: 5814642Abstract: A novel compound of the formula ##STR1## wherein Ar represents a tetracyclic fused heterocyclic group which may be substituted; R.sup.1 represents H or a hydrocarbon group which may be substituted; Y represents an amino acid or nitrogen-containing saturated heterocyclic group which may be substituted, its salt, inhibiting excellent cholinesterase inhibitory activity and monoamine uptake inhibitory activity, thus being useful as therapeutic and/or prophylactic medicaments of senile dementia.Type: GrantFiled: July 30, 1996Date of Patent: September 29, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Giichi Goto, Yuji Ishihara, Masaomi Miyamoto
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Patent number: 5801167Abstract: The present invention relates to new camptothecin derivatives which display antitumor activity. The present invention also provides processes for their preparation as well as pharmaceutical compositions containing the same.Type: GrantFiled: August 20, 1996Date of Patent: September 1, 1998Assignee: Pharmacia S.p.A.Inventors: Angelo Bedeschi, Franco Zarini, Walter Cabri, Ilaria Candiani, Sergio Penco, Laura Capolongo
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Patent number: 5785750Abstract: Pyrrolopyrrole derivatives of the formula (I) ##STR1## wherein QA is a quinacridone radical are disclosed. The inventive pyrrolopyrrole derivatives show excellent rheology enhancing properties for pigment dispersions, especially those containing quinacridones, DPPs and their solid solution pigments.Type: GrantFiled: September 26, 1997Date of Patent: July 28, 1998Assignee: Ciba Specialty Chemicals CorporationInventor: Shivakumar B. Hendi
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Patent number: 5780633Abstract: A new process for preparing a compound of the formula: ##STR1##Type: GrantFiled: May 6, 1996Date of Patent: July 14, 1998Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Satoshi Okada, Kozo Sawada, Akio Kuroda, Shinya Watanabe, Hirokazu Tanaka
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Patent number: 5734056Abstract: A process for the preparation of water soluble camptothecin analogs, including methods for the preparation of intermediates thereof, and the compounds prepared by said process. Water soluble camptothecin analogs are prepared which may be used for inhibiting the growth of tumor cells sensitive to such analogs.Type: GrantFiled: May 25, 1995Date of Patent: March 31, 1998Assignee: SmithKline Beecham CorporationInventors: Patrick Lee Burk, Joseph Marian Fortunak, Antonietta Rose Mastrocola, Mark Mellinger, Jeffrey Lee Wood
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Patent number: 5728696Abstract: Acaricidal, insecticidal and nematicidal substituted (hetero)arylalkyl ketone oxime O-ethers, processes for their preparation, agents containing them, and their use as pesticides.The invention relates to compounds of the formula ##STR1## in which Ar.sup.1 and Ar.sup.2 are aryl or heteroaryl, each of which is optionally substituted, and R is an optionally substituted aliphatic or alicyclic radical, to processes for their preparation, and to agents containing these compounds, and to their use for controlling animal pests.Type: GrantFiled: June 5, 1995Date of Patent: March 17, 1998Assignee: Hoechst AktiengesellschaftInventors: Birgit Kuhn, Gerhard Salbeck, deceased, Uwe Doller, Stefan Schnatterer, Hans-Herbert Schubert, Werner Knauf, Anna Waltersdorfer, Manfred Kern
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Patent number: 5726186Abstract: The present invention provides compounds of formula I: ##STR1## wherein X is --O-- or --S--,Y is --O--, --S--, --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, or --NR.sup.5 --;R.sup.1, R.sup.2, and R.sup.3 are each independently --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl), --OSO.sub.2 CF.sub.3, Cl, or F;n is 1 or 2;W is CH.sub.2 or C.dbd.O;R.sup.4 is 1-piperidinyl, 2-oxo-1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 2-oxo-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino;R.sup.5 is C.sub.1 -C.sub.3 alkyl, --COC.sub.6 H.sub.5, --CO(C.sub.1 -C.sub.6 alkyl), --C(O)OC.sub.6 H.sub.5, --C(O)O(C.sub.1 -C.sub.6 alkyl), --SO.sub.2 (C.sub.1 -C.sub.6 alkyl), --SO.sub.2 C.sub.6 H.sub.5, or --SO.sub.2 CF.sub.3 ;or a pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: August 13, 1996Date of Patent: March 10, 1998Assignee: Eli Lilly and CompanyInventor: Timothy Alan Grese
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Patent number: 5670500Abstract: The present invention provides water soluble camptothecin analogs of Formula I: ##STR1## which are particularly useful as antineoplastic agents; pharmaceutical compositions thereof; and a method of treating cancer in an animal in need thereof, including human beings, comprising inhibition of the growth of tumor cells in said animal by administration of an effective amount of a compound of Formula I.Type: GrantFiled: May 31, 1995Date of Patent: September 23, 1997Assignee: SmithKline Beecham CorporationInventors: David A. Berges, John J. Taggart