The Additional Unsaturated Hetero Ring And The Triazole Ring Are Attached To The Same Acyclic Atom Or To The Same Acyclic Chain Patents (Class 548/266.6)
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Patent number: 7102012Abstract: A process is provided for preparing N,N?-carbonyldiazoles by reacting azoles with phosgene in halogenated aliphatic hydrocarbon solvents, the entirety of the azole for reaction being introduced in the solvent, followed by the addition of phosgene.Type: GrantFiled: May 11, 2005Date of Patent: September 5, 2006Assignee: LANXESS Deutschland GmbHInventors: Andreas Job, Bernd Griehsel
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Patent number: 7094904Abstract: A new process is disclosed for the synthesis of fluconazole monohydrate and for crystal modifications of fluconazole which comprises the step of hydrolyzing a silyl ether of the formula (II) ?wherein R2 is hydrogen, or a C1 to C10 alkyl or phenyl group, R3 and R4 independently of each other are a C1 to C10 alkyl or phenyl group in an aqueous solution, preferably at a pH below 3 or above 8.Type: GrantFiled: September 22, 2003Date of Patent: August 22, 2006Assignee: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: Jánosné´ Kreidl née Regina Hegedus, legal representative, Laszlo Czibula, Csaba Szantay, Jenone Farkas, Ida Deutschne Juhasz, Istvan Hegedus, Eva Werkne Papp, Judit Nagyne Bagdy, Agnes Piller, Janos Kreidl, deceased
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Patent number: 6969727Abstract: Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength. The heterocyclic aromatic compounds have the structure including pharmaceutically acceptable salts thereof and all stereoisomers thereof, wherein Xa is heteroaryl, preferably, and R1, R1a, R6, Y, Xb, A, B, Z, R3, R4, R4a, R5 and R5a are as defined herein.Type: GrantFiled: October 28, 2002Date of Patent: November 29, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Jeffrey A. Robl, Joseph A. Tino, Andres S. Hernandez, Jun Li
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Patent number: 6831177Abstract: Industrial and commercial processes for the preparation of 2-acyl-5-benzylfuran derivatives, 1,2,4-triazole-3-carboxylic acid ester derivatives or propenone derivatives having an anti-HIV activity; and useful crystals of the derivatives. A deblocking: (III-2), (IV-10), (VI-1), wherein R1, R2 and R4 are each independently hydrogen or the like; A is CR6 or N; R6 is hydrogen or the like; Q is a protecting group; and L is a leaving group.Type: GrantFiled: December 3, 2001Date of Patent: December 14, 2004Assignee: Shionogi & Co., Ltd.Inventors: Masaaki Uenaka, Kyozo Kawata, Masahiko Nagai, Takeshi Endoh
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Patent number: 6759387Abstract: This invention provides compositions and methods for enhancing delivery of drugs and other agents across epithelial tissues, including the skin, gastrointestinal tract, pulmonary epithelium, and the like. The compositions and methods are also useful for delivery across endothelial tissues, including the blood brain barrier. The compositions and methods employ a delivery enhancing transporter that has sufficient guanidino or amidino sidechain moieties to enhance delivery of a compound conjugated to the reagent across one or more layers of the tissue, compared to the non-conjugated compound. The delivery-enhancing polymers include, for example, poly-arginine molecules that are preferably between about 6 and 25 residues in length (SEQ ID NO:50).Type: GrantFiled: July 30, 2002Date of Patent: July 6, 2004Assignee: Cellgate, Inc.Inventors: Jonathan B. Rothbard, Paul A. Wender, P. Leo McGrane, Lalitha V. S. Sista, Thorsten A. Kirschberg
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Publication number: 20040097564Abstract: Provided, among things, is a method of decreasing intraocular pressure in an animal, including a human, comprising administering an intraocular pressure decreasing amount of a compound of the formula I: 1Type: ApplicationFiled: September 25, 2003Publication date: May 20, 2004Inventor: Martin Gall
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Patent number: 6630468Abstract: The present application describes disubstituted pyrazolines and triazolines of formulae I and II: or pharmaceutically acceptable salt forms thereof, wherein one of M1 and M2 maybe N and D may be a variety of N-containing groups, which are useful as inhibitors of factor Xa.Type: GrantFiled: June 26, 2002Date of Patent: October 7, 2003Inventor: Donald J. P. Pinto
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Patent number: 6486159Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided having the general formula wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and n, R1 and R2 are as defined in the specification.Type: GrantFiled: February 21, 2001Date of Patent: November 26, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Thomas W. Hudyma, Oak K. Kim, Xiaofan Zheng
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Patent number: 6451833Abstract: A class of N-substituted (&agr;-imidazolyl-toluyl)pyrrole compounds described for use in treatment of circulatory disorders.Type: GrantFiled: November 1, 2000Date of Patent: September 17, 2002Assignee: Pharmacia CorporationInventors: Philippe R. Bovy, Joe T. Collins, Robert E. Manning
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Patent number: 6410582Abstract: The thienylazolylalkoxyethanamines (I) where R1 is a hydrogen atom, a halogen atom or a lower alkyl radical; R2, R3 and R4 represent, independently, a hydrogen atom or a lower alkyl radical; and Az represents a five-member nitrogenated hetercyclic aromatic group, N-methyl-substituted, that contains from one to three nitrogen atoms. They have analgesic activity in mammals, including humans. The compounds (I) can be obtained, for example, by reaction of a derivative of hydroxy-thienylazol (IV) with a derivative of a suitable N-(ethyl)amine. The compounds (IV) are useful intermediates in the synthesis of the compounds (I). The compounds (I) have an application in human and/or veterinary medicine.Type: GrantFiled: October 12, 2000Date of Patent: June 25, 2002Assignee: Laboratorios Del Dr. Esteve, S.A.Inventors: Ramon Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
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Patent number: 6376526Abstract: An antifungal compound of formula (I): or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of either entity, wherein X is CH or N; R1 is phenyl subsituted with 1 to 3 substituents each independently selected from halo and CF3; R2 is (hydroxy)C1-C4 alkyl, CONH2, S(O)m(C1-C4 alkyl), Ar or Het; m is 1 or 2; Ar is phenyl optionally monosubstituted with halo or CF3; and Het is a C-linked 6-membered nitrogen-containing aromatic heterocyclic group containing 1 or 2 nitrogen atoms, or a C- or N-linked 5-membered nitrogen-containing aromatic heterocyclic group containing from 2 to 4 nitrogen atoms, wherein either of said heterocyclic groups is optionally substituted with C1-C4 alkyl or (C1-C4 alkoxy)methyl.Type: GrantFiled: December 1, 1999Date of Patent: April 23, 2002Assignee: Pfizer Inc.Inventors: Andrew Simon Bell, Peter Thomas Stephenson
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Patent number: 6362206Abstract: The present invention provides an azole compound represented by the formula (I): wherein Ar is an optionally substituted phenyl group; R1 and R2, the same or different, are a hydrogen atom or a lower alkyl group, or R1 and R2 may combine together to form a lower alkylene group; R is a hydrogen atom or an acyl group; X is a nitrogen atom or a methine group; A is Y═Z (Y and Z, the same or different, are a nitrogen atom or a methine group optionally substituted with a lower alkyl group) or an ethylene group optionally substituted with a lower alkyl group; n is an integer from 0 to 2; and Az is an optionally substituted azolyl group, or its salt, which is useful for a prevention and therapy of a fungal infection of a mammal as a antifungal agent.Type: GrantFiled: October 7, 1999Date of Patent: March 26, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Katsumi Itoh, Kenji Okonogi, Akihiro Tasaka
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Patent number: 6359141Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided having the general formula wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and n, R1 and R2 are as defined in the specification.Type: GrantFiled: February 21, 2001Date of Patent: March 19, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Thomas W. Hudyma, Oak K. Kim, Xiaofan Zheng
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Patent number: 6358984Abstract: Compounds including 1-(biphenyl-4-yl)methyl-1H-1,2,4-triazoles and 1-(biphenyl-4-yl)methyl-4H-1,2,4-triazoles each having a (2,4-dioxopyrrolidine-5-ylidene) methyl or (2,4-dioxo-tetrahydrofuran-5-ylidene)methyl group as the substituent at the 2′-position and salts thereof are lowly toxic and highly safe and are useful as an angiotensin II antagonist. Thus, these compounds can be used in medicines, which contain these compounds as an active ingredient.Type: GrantFiled: August 11, 2000Date of Patent: March 19, 2002Assignee: Lead Chemical Co., Ltd.Inventors: Eiichi Yoshii, Masao Mori
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Patent number: 6333323Abstract: A compound of the formula: wherein R1 is hydrogen, lower alkyl, or optionally substituted arylsulfonyl, or the like, R2 is hydrogen, lower alkyl, or optionally substituted aralklyl, or the like, R3, R4, R5, and R6 each is independently hydrogen, halogen, trihalogenated lower alkyl, or the like, X is hydroxy or optionally substituted amino, Y is COOR R is hydrogen or an ester residue), optionally substituted aryl, or optionally substituted heteroaryl, has integrase inhibition activity, and is useful as an anti-HIV drug.Type: GrantFiled: August 18, 2000Date of Patent: December 25, 2001Assignee: Shionogi & Co., Ltd.Inventors: Toshio Fujishita, Tomokazu Yoshinaga
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Patent number: 6316505Abstract: Block copolymers containing a fluorinated hydrocarbon unit, a hydrocarbon unit, and a poly(oxyethylene) unit are useful in fluid formulations of pharmaceutical agents. A typical embodiment is: C11H23—CONHC2H4NHCO—C8F16—CONHC2H4NHCOO—(C2H4O)34—H.Type: GrantFiled: August 5, 1999Date of Patent: November 13, 2001Assignee: Supratek Pharma, Inc.Inventors: Alexander V. Kabanov, Serguei V. Vinogradov
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Patent number: 6300357Abstract: A triazole compound having the formula: wherein Ar1 represents a phenyl group which may be substituted, Ar2 represents a heterocyclic group which may be substituted, R0 represents a hydrogen atom or a lower alkyl; R1 represents a lower alkyl; R2 to R5 each represent a hydrogen atom or an unsubstituted or halo substituted alkyl; n represents 0 to 2; p represents 0 or 1; q, r and s each represent 0 to 2; A represents a 4- to 7-membered carbon ring or a 4- to 7-membered heterocyclic group. The compound of the present invention exhibits an excellent antifungal activity.Type: GrantFiled: February 1, 1999Date of Patent: October 9, 2001Assignee: Sankyo Company, LimitedInventors: Sadao Oida, Teruo Tanaka, Yawara Tajima, Toshiyuki Konosu, Atsushi Somada, Takeo Miyaoka, Hiroshi Yasuda
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Patent number: 6265584Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided having the general formula wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and n, R1 and R2 are as defined in the specification.Type: GrantFiled: May 20, 1999Date of Patent: July 24, 2001Assignee: Bristol-Myers Squibb CompanyInventors: Thomas W. Hudyma, Oak K. Kim, Xiaofan Zheng
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Patent number: 6265352Abstract: Substituted carbamoyltriazoles of the formula I as defined in the specification and the agriculturally useful salts thereof, processes for their preparation and their use as herbicides.Type: GrantFiled: March 17, 1999Date of Patent: July 24, 2001Assignee: BASF AktiengesellschaftInventors: Ernst Baumann, Cyrill Zagar, Uwe Kardorff, Ulf Misslitz, Karl-Otto Westphalen, Helmut Walter, Gerhard Hamprecht
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Patent number: 6245804Abstract: This invention describes the new, nonsteroidal gestagens of general formula I in which A, B, Ar, R1, R2 and R3 have the meanings that are indicated in more detail in the description. The new compounds show a very great affinity to the gestagen receptor. They can be used alone or in combination with estrogens in contraceptive preparations. In addition, they can be used for treating endometriosis. Together with estrogens, they can also be used in preparations for treating gynecological disorders, for treating premenstrual symptoms and for substitution therapy. Based on the androgenic action, they can also be used for male birth control, male HRT and hormone therapy and for treating andrological disease agents.Type: GrantFiled: May 29, 1998Date of Patent: June 12, 2001Assignee: Schering AktiengesellschaftInventors: Manfred Lehmann, Klaus Schoellkopf, Peter Strehlke, Nikolaus Heinrich, Karl-Heinrich Fritzemeier, Rolf Krattenmacher, Hans-Peter Muhn