Patents Represented by Attorney, Agent or Law Firm Elsa Djuardi
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Patent number: 7462634Abstract: The present invention relates to novel compounds, to pharmaceutical compositions comprising the compounds described herein, their pharmaceutically acceptable salts, hydrates and solvates, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme (11?HSD1).Type: GrantFiled: June 15, 2006Date of Patent: December 9, 2008Assignees: Agouron Pharmaceuticals, Inc., Pfizer IncInventors: Sajiv Krishnan Nair, Michael Siu, Wendy Dianne Taylor
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Patent number: 7198796Abstract: Parenteral pharmaceutical formulations containing an echinocandin antifungal compound and an aqueous solvent are provided, wherein the formulation includes ethanol, for example about 20% w/v ethanol. The parenteral pharmaceutical formulation may further include one or more additives, such as a stabilizing agent, buffer or tonicity agent. The parenteral pharmaceutical formulations are useful in extending the shelf life and improving the solubility of the echinocandin antifungal compound.Type: GrantFiled: August 1, 2005Date of Patent: April 3, 2007Assignee: Vicuron Pharmaceuticals Inc.Inventor: Martin Stogniew
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Patent number: 7193083Abstract: The invention provides a process for the preparation of a compound of the formula: or an acid addition or base salt thereof, wherein R is phenyl optionally substituted by 1 to 3 substituents each independently selected from halo and trifluoromethyl; R1 is C1–C6 alkyl; and “Het” is pyrimidinyl optionally substituted by 1 to 3 substituents each independently selected from C1–C4 alkyl, C1–C4 alkoxy, halo, oxo, benzyl and benzyloxy, comprising reaction of a compound of the formula: wherein R is as previously defined for a compound of the formula (I), with a compound of the formula: wherein R1 and “Het” are as previously defined for a compound of the formula (I) and X is chloro, bromo or iodo, in the presence of zinc, iodine and/or a Lewis acid and an aprotic organic solvent: said process being optionally followed by conversion of the compound of the formula (I) to an acid addition or base salt thereof.Type: GrantFiled: May 2, 2005Date of Patent: March 20, 2007Assignee: Pfizer, Inc.Inventors: Michael Butters, Alan John Pettman
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Patent number: 6897306Abstract: Compounds of formula (I): and their salts, solvates, prodrugs, etc., wherein the substituents have the values mentioned herein, are Procollagen C-Proteinase (PCP) inhibitors and have utility in conditions mediated by PCP.Type: GrantFiled: July 16, 2002Date of Patent: May 24, 2005Assignee: Pfizer Products, Inc.Inventors: Simon Bailey, Stephane Billotte, Paul Vincent Fish, Kim James, Nicholas Murray Thomson, Andrew Michael Derrick
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Patent number: 6790957Abstract: The invention provides compounds of formula I, R1—OP(O)(OH)2 I wherein R1 represents the non-hydroxy portion of a triazole antifungal compound of the type comprising a tertiary hydroxy group; or a pharmaceutically acceptable salt thereof. The compounds of the invention are useful in the treatment of fungal infections, and have good aqueous solubility.Type: GrantFiled: January 9, 2003Date of Patent: September 14, 2004Assignee: Pfizer, Inc.Inventors: Stuart Green, Peter T. Stephenson, Charles W. Murtiashaw
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Patent number: 6696474Abstract: Compounds of formula I: wherein X, Y, B, E, J, K, L, Z, and R9-R12 have any of the meanings described herein, their pharmaceutically acceptable salts, lower blood glucose levels and are useful for treating diseases in mammals such as Non-Insulin Dependent Diabetes Mellitus. Also disclosed are pharmaceutical compositions, processes for preparing compounds of formula (I) and intermediates useful for preparing compounds of formula I.Type: GrantFiled: March 17, 2003Date of Patent: February 24, 2004Assignee: Warner Lambert Co. LLC.Inventors: Christopher F. Bigge, Robert P. Schaum
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Patent number: 6670167Abstract: The present invention relates to the identification, isolation and purification of the catalytic domain of the human effector checkpoint protein kinase (hChk1). A 1.7Å crystal structure of the hChk1 kinase domain in the active conformation is reported herein. The kinase domain of hChk1 and its associated crystal structure is described for use in the discovery, identification and characterization of inhibitors of hChk1. This structure provides a three-dimensional description of the binding site of the hChk1 for structure-based design of small molecule inhibitors thereof as therapeutic agents. Inhibitors of hChk1 find utility in the treatment of hyperproliferative disorders such as HIV and cancer.Type: GrantFiled: December 14, 1999Date of Patent: December 30, 2003Assignee: Agouron Pharmaceuticals, Inc.Inventors: Ping Chen, Mark Anderson, Ya-Li Deng, Smita Gaur, Chen Chen Kan, Chun Luo, Karen Lundgren, Stephen Margosiak, Binh Nguyen, Patrick O'Connor, James Register, Anna Tempczyk Russell, Jay Sarup
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Patent number: 6586594Abstract: A process for the preparation of a compound of the formula: or an acid addition or base salt thereof, wherein R is phenyl optionally substituted by 1 to 3 substituents each independently selected from halo and trifluoromethyl; R1 is C1-C6 alkyl; and “Het” is pyrimidinyl optionally substituted by 1 to 3 substituents each independently selected from C1-C4 alkyl, C1-C4 alkoxy, halo, oxo, benzyl and benzyloxy, comprising reacting a compound of the formula: with a compound of the formula wherein X is chloro, bromo or iodo, the reaction taking place in the presence of zinc; at least one of iodine or a Lewis acid; and an aprotic organic solvent: optionally further reacting the resulting compound with an acid or base to form the corresponding acid addition or base salt thereof.Type: GrantFiled: February 4, 1998Date of Patent: July 1, 2003Assignee: Pfizer, Inc.Inventors: Michael Butters, Alan John Pettman, Julie Ann Harrison
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Patent number: 6444677Abstract: This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof wherein A is independently halo; Y1 is —(CH2)m—, C(O) or S(O); Y2 is N or CH; R1 and R2 are independently C1-4 alkyl; R3 is selected from the following: (a) optionally substituted —(CH2)p—C3-7 cycloalkyl; (b) optionally substituted —C5-7 alkyl; and (c) substituted —C1-4 alkyl; and (d) optionally substituted C7-9 bicycloalkyl; R4 is optionally substituted thiazolyl, imidazolyl or oxazolyl; X is S, —NH, —N—C1-4 alkyl or O; R5 is hydrogen or C1-4 alkyl; R6 is C1-4 alkyl or halo; m is 0, 1 or 2; n is 0, 1, 2, 3, 4 or S; and p is 0, 1, 2, 3, 4, 5 or 6. These compounds are useful for the treatment of medical conditions caused by bradykinin such as inflammation, cardiovascular disease, pain, etc. This invention also provides a pharmaceutical composition comprising the above compound.Type: GrantFiled: December 7, 2000Date of Patent: September 3, 2002Assignee: Pfizer Inc.Inventors: Takafumi Ikeda, Mitsuhiro Kawamura, Noriaki Murase, Seiji Nukui, Yuji Shishido, Makato Kawai, Yoshiyuki Okumura
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Patent number: 6387901Abstract: The present invention relates to alkyne containing metalloproteinase inhibitors of the formula wherein n, X, and R1-R9 are as defined in the specification, and to pharmaceutical compositions and methods of treatment thereof.Type: GrantFiled: June 30, 2000Date of Patent: May 14, 2002Assignee: Pfizer INCInventor: Louis S. Chupak
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Patent number: 6387931Abstract: Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin diType: GrantFiled: October 12, 2001Date of Patent: May 14, 2002Assignee: Pfizer INCInventors: Kevin Neil Dack, Gavin Alistair Whitlock
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Patent number: 6350907Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, or solvates of either entity, wherein the substituents have the values described herein, are useful as matrix metalloprotease (MMP) inhibitorsType: GrantFiled: April 11, 2000Date of Patent: February 26, 2002Assignee: Pfizer IncInventors: Michael Jonathan Fray, Roger Peter Dickinson, Kevin Neil Dack
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Patent number: 6342521Abstract: A compound of the formula wherein R1, R2 and Q is as defined above, are useful in the treatment of a arthritis (including osteoarthritis and rheumatoid arthritis), cancer (such as solid tumor cancer including colon cancer, breast cancer, lung cancer and prostrate cancer and hematopoietic malignancies including leukemias and lymphomas), and other disorders. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S) and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.Type: GrantFiled: May 25, 2000Date of Patent: January 29, 2002Assignee: Pfizer Inc.Inventor: Lawrence A. Reiter
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Patent number: 6340681Abstract: A compound of the formula: or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are independently selected from hydrogen, halo, hydroxy, (C1-C4)alkyl, halo (C1-C4)alkyl and the like; R3 and R4 are independently selected from hydrogen, halo(C1-C10)alkyl, optionally substituted (C1-C6)alkyl and the like, or R3 and R4, together with the nitrogen atom to which they are attached, form an optionally substituted fully saturated, partially saturated or fully unsaturated heterocyclic ring; and R5 is (C4-C11)cycloalkyl and the like, has ORL1-receptor agonist activity, and are useful as analgesics or the like in mammalian subjects.Type: GrantFiled: June 29, 2000Date of Patent: January 22, 2002Assignee: Pfizer IncInventor: Fumitaka Ito
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Patent number: 6310079Abstract: This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof, wherein Ar is heteroaryl; X1 and X2 are independently selected from halo, C1-C4 alkyl, hydroxy, C1-C4 alkoxy, amino, C1-C4 alkanoyl, carboxy, carbamoyl, cyano, nitro, mercapto, (C1-C4 alkyl)thio, (C1-C4 alkyl)sulfinyl, (C1-C4 alkyl)sulfonyl, aminosulfonyl, or the like; R1 is selected from hydrogen, straight or branched C1-C4 alkyl, C3-C8 cycloalkyl, C4-C8 cycloalkenyl, phenyl , heteroaryl and the like; R2 and R3 are independently selected from hydrogen, halo, C1-C4 alkyl, phenyl and the like; or R1 and R2 can form, together with the carbon atom to which they are attached, a C5-C7 cycloalkyl ring; and m and n are independently 0, 1, 2 or 3. These compounds and pharmaceutical compositions containing such compounds are useful as analgesics and anti-inflammatory agents.Type: GrantFiled: February 5, 1999Date of Patent: October 30, 2001Assignee: Pfizer Inc.Inventors: Yoshiyuki Okumura, Yoshinori Murata, Takashi Mano
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Patent number: 6303628Abstract: This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof wherein A is C 1-6 alkylene or —NR1—; Z is C(═L)R2, or SO2R3; U is CH or N; W and Y are independently selected from —CH2—, O, S and —N—R1; m is 1, 2 or 3; q and r are independently 0, 1 or 2; X is independently selected from halogen, C1-4 alkyl, halo-substituted C1-4 alkyl, hydroxy, C1-4 alkoxy, halo-substituted C1-4 alkoxy or the like; n is 1 or 2; L is oxygen or sulfur; R1 is hydrogen or C1-4 alkyl; R2 is hydroxy, C1-6alkyl, halo-substituted C1-6 alkyl, C1-6 alkoxy, halo-substituted C1-6 alkoxy, C3-7 cycloalkoxy, C1-4 alkyl(C3-7 cycloalkoxy), —NR4R5 or the like; R3 is C1-6 alkyl or halo-substituted C1-6 alkyl; and R4 and R5 are independently selected from hydrogen, C1-6 alkyl and halo-substituted C1-6alkyl.Type: GrantFiled: June 28, 2000Date of Patent: October 16, 2001Assignee: Pfizer IncInventors: Kazunari Nakao, Shigeo Hayashi, Rodney W. Stevens
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Patent number: 6291520Abstract: Certain novel hydroxamic acid derivatives having the structure inhibit the enzyme lipoxygenase. These compounds, and the pharmaceutically acceptable salts thereof, are useful in the treatment or alleviation of inflammatory diseases, allergic conditions and cardiovascular diseases in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.Type: GrantFiled: June 28, 1993Date of Patent: September 18, 2001Assignee: PfizerInventors: Takafumi Ikeda, Akiyoshi Kawai, Takashi Mano, Yoshiyuki Okumura, Rodney William Stevens
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Patent number: 6277878Abstract: This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof wherein R1 is H or C1-4 alkyl; R2 is C(═L′)R3 or So2R4; Y is a direct bond or C1-4 alkylene; L and L′ are independently oxygen or sulfur; Q is selected from the following: C1-6 alkyl, halo-substituted C1-4 alkyl, optionally substituted C3-7 cycloalkyl, optionally substituted phenyl or naphthyl, optionally substituted 5 or 6-membered monocyclic aromatic group; R3 is —OR6, —NR7R8, N(OR1)R7 or a group of formula: Z is a direct bond, O, S or NR5; R4 is C1-6 alkyl, halo-substituted C1-4 alkyl, optionally substituted phenyl or naphthyl; R5 is C1-4 alkyl or halo-substituted C1-4 alkyl; R6 is C1-4 alkyl C3-7 cycloalkyl, C1-4 alkyl-C3-7 cycloalkyl, halo-substituted C1-4 alkyl, optionally substituted C1-4 alkyl-phenyl or phenyl; R7 and R8 are each selected from the following: H, optionally substituted C1-6 alkyl, optionally substituted C3-7 cycloType: GrantFiled: August 26, 1999Date of Patent: August 21, 2001Assignee: Pfizer IncInventors: Kazunari Nakao, Rodney W. Stevens, Kiyoshi Kawamura, Chikara Uchida
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Patent number: 6214870Abstract: The present invention relates to dioxocyclopentyl hydroxamide derivatives of the formula wherein X, Z and Q are as defined in the specification, and to pharmaceutical compositions and methods of treatment thereof.Type: GrantFiled: March 28, 2000Date of Patent: April 10, 2001Assignee: Pfizer IncInventors: Kim F. McClure, Ralph P. Robinson
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Patent number: 6172067Abstract: A compound of the formula: or a pharmaceutically acceptable salt thereof, wherein R is unsubstituted, mono-, di- or tri-substituted (C3-C11)cycloalkyl or (C3-C11)cycloalkenyl or the like, A is unsubstituted (C1-C7)alkyl or (C2-C5 )alkenyl, or unsubstituted, mono-, di- or tri-substituted aryl, or aromatic-heterocyclic or the like, Y is hydrogen, halo, amino or mercapto, or unsubstituted, mono-, di- or tri- substituted (C1-C10)alkyl-M—, (C3-C7)cycloalkyl-M—, (C2-C6)alkenyl-M—, (C1-C4)alkyl-NH-((C1-C4)alkyl)-M—, di(C1-C4)alkyl-N-((C1-C4)alkyl)-M—, aryl-M—, aromatic or non-aromatic heterocyclic-M—, aryl-(C1-C5)alkyl-M— or aromatic non-aromatic heterocyclic-(C1-C5)alkyl-M—, wherein M is a covalent bond O, S, NH or the like, or the like; Z1, Z2, Z3 and Z4 are hydrogen or the like, has ORL1-receptor agonist activity, and are useful as analgesics or the like in mammalian subjects.Type: GrantFiled: August 5, 1999Date of Patent: January 9, 2001Assignee: Pfizer Inc.Inventors: Fumitaka Ito, Hirohide Noguchi, Hiroshi Kondo