Patents Represented by Attorney, Agent or Law Firm Paul R. Darkes
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Patent number: 7667054Abstract: The invention relates to novel cytotoxic agents comprising taxanes and their therapeutic use as a result of delivering the taxanes to a specific cell population in a targeted fashion by chemically linking the taxane to a cell binding agent.Type: GrantFiled: December 6, 2005Date of Patent: February 23, 2010Assignee: Aventis Pharma S.A.Inventors: Michael L. Miller, Ravi V. J. Chari, Erkan Baloglu, Alain Commercon
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Patent number: 7632952Abstract: The invention especially relates to novel chemical compounds, especially novel benzothiazole derivatives, to compositions containing said compounds, and to the use thereof as medicaments.Type: GrantFiled: September 29, 2006Date of Patent: December 15, 2009Assignee: Aventis Pharma S.A.Inventors: Stéphanie Deprets, Anke Steinmetz, Odile Angouillant-Boniface, Daniel Bezard, Jidong Zhang, Yannick Benedetti, François Clerc
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Patent number: 7504511Abstract: The invention relates to 2-acylamino-4-phenylthiazole derivatives of general formula (I): pharmaceutically acceptable acid-addition salts thereof, hydrates or solvates of such derivatives or such pharmaceutically acceptable acid addition salts, intermediates thereto, processes for the preparation thereof, and therapeutic application thereof.Type: GrantFiled: October 19, 2005Date of Patent: March 17, 2009Assignee: Sanofi-AventisInventors: Pierre Carayon, Pierre Casellas, Daniel Floutard, Pierre Fraisse, Samir Jegham, Bernard Labeeuw
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Patent number: 7462725Abstract: The process according to the invention relates to the preparation of 2-chloromethyl-thiophene of the formula (I). During this process thiophene is chloromethylated in the presence of one or more compounds containing keto group and optionally it is transformed into the compound of the formula (II). Compounds of formula (I) and (II) are intermediates of several pharmaceutically active ingredients.Type: GrantFiled: May 16, 2002Date of Patent: December 9, 2008Assignee: Sanofi-AventisInventors: Mátyás Aradi, Ferenc Bakos, Zsolt Dombrády, Antal Gajáry, István Gyöngyösi, Ferenc Kovács, Andrea Major, Erika Máténé Török, Zsolt Párkányi, László Schultz, Attila Supic, Sándor Szabó, Erzsébet Szalay, József Ugrics, József Zsiga
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Patent number: 7442708Abstract: Compounds of formula I or salts thereof: in which R1 represents —OH, (C1-C5)alkoxy, carboxyl, (C2-C6)alkoxycarbonyl, —NR5R6, —NH—SO2-Alk, —NH—SO2-Ph, —NH—CO-Ph, —N(Alk)-CO-Ph, —NH—CO—NH-Ph, —NH—CO-Alk, —NH—CO2-Alk, —O—(CH2)n-cAlk, —O-Alk-COOR7, —O-Alk-O—R8, —O-Alk-OH, —O-Alk-C(NH2):NOH, —O-Alk-NR5R6, —O-Alk-CN, —O—(CH2)n-Ph, —O-Alk-CO—NR5R6, —CO—NH—(CH2)m—COOR7, —CO—NH-Alk R2 represents H, (C1-C5)alkyl, (C1-C5)alkyl halide, (C3-C6)cycloalkyl or phenyl which is optionally substituted, A represents —CO—, —SO— or —SO2—, R3 and R4 which are identical or different, each represent H, (C1-C5)alkoxy, amino, carboxyl, (C2-C6)alkoxycarbonyl, —OH, nitro, hydroxyamino, -Alk-COOR7, —NR5R6, —NH-Alk-COOR7, —NH—COO-Alk, —N(R11)—SO2-Alk-NR9R10, —N(R11)—SO2-Alk, —N(R11)-Alk-NR5R6, —N(R11)—CO-Alk-NR9R10, —N(R11)—CO-Alk, —N(R11)—CO—CF3, —NH-Alk-HetN, —O-Alk-NR9R10, —O-Alk-CO—NR5R6, —O-Alk-HetN, or R3 and R4 form together a 5- to 6-membered unsaturated heterocycle, are inhibitors of basic fibroblast growth factors.Type: GrantFiled: April 2, 2003Date of Patent: October 28, 2008Assignee: Sanofi-AventisInventors: Alain Badorc, Francoise Bono, Marie-Francoise Bordes, Nathalie Guillo, Jean-Marc Herbert
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Patent number: 7381835Abstract: The subject of the present invention is the preparation of the (R)-(?)-2-hydroxy-2-(2-chlorophenyl)acetic acid of the formula (I) by the resolution of the corresponding racemic compound by using the compounds of the general formula (II).Type: GrantFiled: June 14, 2002Date of Patent: June 3, 2008Assignee: Sanofi-AventisInventors: József Bálint, Marianna Csatáriné Nagy, Zsolt Dombrády, Elemér Fogassy, Antal Gajáry, Charles Suba
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Patent number: 7322352Abstract: Provided herein are dry powder inhalers for the delivery of metered doses of medicament, counters associated with the inhalers for counting and displaying the number of doses administered or remaining within the inhaler, and methods of use thereof.Type: GrantFiled: September 18, 2003Date of Patent: January 29, 2008Assignee: Aventis Pharma LimitedInventors: Stephen John Minshull, Duncan Grant Young, Andrew J. Ledgeway, Simon Paul Wells, Graham Keith Lacy, Julian Francis R. Swan
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Patent number: 7214212Abstract: The present invention concerns a cap suitable for injection devices having an exchangeable needle assembly, which serves as a mounting/demounting tool of the said needle assembly.Type: GrantFiled: June 14, 2004Date of Patent: May 8, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Christian Pommereau, Carsten Larsen
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Patent number: 7025205Abstract: A method for maintaining the enclosed volume of a sealed package at about ambient pressure, wherein the package contains a pressurized container comprising a drug, and an HFA (hydrofluoroalkane) propellant selected from the group consisting of HFA 134a and HFA p227, or a mixture thereof; wherein the method comprises the steps of (1) positioning an effective amount of a HFA adsorbent material, and said pressurized container, within a sealable package; (2) sealing the package so that the pressurized container and adsorbent are in an enclosed volume within the package at a pressure equal to about ambient pressure; and (3) adsorbing any leakage of the HFA propellant into the HFA adsorbent material so as to maintain the enclosed volume at about ambient pressure.Type: GrantFiled: June 25, 2003Date of Patent: April 11, 2006Assignee: Aventis Pharma LimitedInventor: Frank C. Barker
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Patent number: 6716853Abstract: The invention is related to compounds of formula I to pharmaceutical compositions comprising such compounds, to processes for the preparation of such compounds, and to methods of prevention and treatment of disorders, the progression of which involve an enhanced activity of matrix metalloproteinase 13, by administering to a patient in need thereof, a pharmaceutically effective amount of such compounds.Type: GrantFiled: February 26, 2003Date of Patent: April 6, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Petra Stahl, Reinhard Kirsch, Sven Ruf, Volkmar Wehner, Klaus-Ulrich Weithmann
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Patent number: 6602877Abstract: Compounds of formula (I) are described in which R1 is optionally substituted heteroaryl; R2 is optionally substituted aryl or optionally substituted heteroaryl; R3 is a group —L1—R7 or —L2—R8 [where L1 is an optionally substituted alkylene linkage; R7 is hydrogen, aryl, cyano, cycloalkyl, heteroaryl, heterocycloalkyl, nitro, —S(O)nR9, —NHSO2R9, —C(═Z)OR10, —C(═Z)R10, —OR10, —N(R11)—C(═Z)R9, —NY1Y2, —SO2NY1Y2, —C(═Z)—NY1Y2, —N(R11)—C(═Z)—NY1Y2, —N(OR10)—C(═Z)—NY1Y2, —N(OR10)—C(═Z)R10, —C(═NOR10)R10, —C(═Z)NR10OR12, —N(R11)—C(═NR13)—NY1Y2 or —N(R11)—C(═Z)OR11; L2 is a direct bond or a straight- or branched-carbon chain comprising from 2 to about 6 carbon atoms and contains a double or triple carbon-carbon bond; and R8 is hydrogen, aryl, cycloalkenyl, cycloalkyl, heteroaryl orType: GrantFiled: December 8, 1999Date of Patent: August 5, 2003Assignee: Aventis Pharma LimitedInventors: Paul L. Bamborough, Alan J. Collis, Frank Halley, Richard A. Lewis, David J. Lythgoe, Jeffrey M. McKenna, Iain M. McLay, Barry Porter, Andrew J. Ratcliffe, Paul A. Wallace
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Patent number: 6559313Abstract: This invention is directed to intermediates of the formula wherein Z is 4-trifluoromethylpyridin-2-yl or 5-trifluoromethylpyridin-2-yl which are useful in the preparation of compounds useful as antihypertensive, anti-ischemic, cardioprotective, and antilipolytic agents.Type: GrantFiled: March 22, 2002Date of Patent: May 6, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Michael R. Myers, Martin P. Maguire, Alfred P. Spada, William R. Ewing, Henry W. Pauls, Yong Mi Choi-Sledeski
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Patent number: 6541482Abstract: The present invention relates to compounds of the formula wherein X is N3, NH2, NHR, N(R)2, CN, SH, SR, or OR1; R is C1-C4 alkyl or (CH2)n—&phgr;; n is an integer 0, 1, 2, 3 or 4; &phgr; is a phenyl group unsubstituted or substituted with from 1 to 3 substituents, each substituent is independently selected from the group consisting of C1-C4 alkyl, C1-C4 alkoxy, halogen, CF3, OCF3, OH, CN, NO2 or NH2; R1 is C1-C4 alkyl or (CH2)m—NR2R3; m is an integer 1, 2, 3 or 4; R2 and R3 are each independently C1-C4 fluorinated akyl or cycloalkyl; The X substituent on the cyclopentanyl ring is in the TRANS configuration relative to the bicyclic substituent; Y is nitrogen; Z1 and Z2 are each independently hydrogen, halogen or NH2; and ---- represents a singe or double bond; or pharmaceutically acceptable salts thereof, compositions comprising such compounds, and methods of treatment comprising administering of such compounds.Type: GrantFiled: February 3, 1995Date of Patent: April 1, 2003Inventors: Carl K. Edwards, III, David R Borcherding
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Patent number: 6472412Abstract: This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. The present invention is therefore directed to their pharmacological use for inhibiting TNF and/or cyclic AMP phosphodiesterase, pharmacological compositions comprising the compounds and methods for their preparation.Type: GrantFiled: January 26, 1996Date of Patent: October 29, 2002Assignee: Aventis Pharma LimitedInventors: Garry Fenton, Tahir Nadeem Majid, Malcolm Norman Palfreyman
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Patent number: 6436947Abstract: This invention relates to Trans cyclopentanyl purine analogs of the formula (1) wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent, Y3, Y5 Y7, Y9 are each nitrogen and Y8 is a CH group, R is a hydrogen, a C1-C7 alkyl acyl or aryl acyl, Q is NH2, halogen or hydrogen, Z is hydrogen, halogen, or NH2; or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.Type: GrantFiled: November 20, 1997Date of Patent: August 20, 2002Assignee: Aventis Pharmaceuticals Inc.Inventors: David R. Borcherding, Carl K. Edwards, III, Ronald E. Esser, Douglas L. Cole
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Patent number: 6433172Abstract: This invention is directed to methods for stereospecifically preparing [(1-optionally substituted aryl)- or (1-optionally substituted heteroaryl)]-2-substituted ethyl-2-amines, having chirality at the 2-position, and to intermediates to the substituted ethyl-2-amines.Type: GrantFiled: October 25, 1999Date of Patent: August 13, 2002Assignee: Aventis Pharmaceuticals Inc.Inventors: Luc Grondard, Jean-Paul Casimir, Patrick Leon, Michael K. O'Brien, Matthew R. Powers, Daniel Robin
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Patent number: 6429315Abstract: This invention is directed to a process for preparing N6-substituted adenosine derivatives, to intermediates useful therefor and to methods of preparing these intermediates.Type: GrantFiled: January 21, 2000Date of Patent: August 6, 2002Assignee: Aventis Pharmaceuticals Inc.Inventors: Adam W. Sledeski, Luc Grondard, Matthew R. Powers, Tory H. Powner, Michael K. O'Brien, Ching T. Tsuei, Patrick Leon, Gregory G. Kubiak, Laurence Pailleres-Hubert, Benoit Viguier
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Patent number: 6392049Abstract: The present invention is directed to a process for preparing 2,4-dihydroypyridine comprising heating a compound of the formula A wherein R is H, alkyl or aralkyl and phosphoric acid where the ratio of phosphoric acid to water is not less than about 27 to 1 weight %. The invention is also directed to a process for preparing 2,4-dihydroy-3-nitropyridine comprising reacting 2,4-dihydroypyridine with nitric acid. The processes of the present invention prepare intermediates which are useful in preparing compounds which are useful for treating cardiovascular disease marked by hypertension or myocardial ischeria, ameliorating ischemic injury or myocardial infarct size, or treating hyperlipidemia or hypercholesterolemia.Type: GrantFiled: May 18, 2001Date of Patent: May 21, 2002Assignee: Aventis Pharmaceuticals Inc.Inventors: Larry K. Truesdale, James P. Sherbine, Benoit J. Vanasse
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Patent number: 6376472Abstract: A compound of the formula wherein K is N; Q is CH2 or O; R6 is hydrogen, alkyl, allyl, 2-methylallyl, 2-butenyl, or cycloalkyl where the nitrogen of the ring of X is substituted by Y; E is O or S; Y is hydrogen, alkyl, aralkyl, substituted aralkyl, aryl, substituted aryl, heterocyclyl, substituted heterocyclyl, heterocyclylalkyl, or substituted heterocyclylalkyl; and n and p are independently 0, 1, 2, or 3, provided that n+p is at least 1; T is hydrogen, alkyl, alkylcarbonyl, alkylthiocarbonyl, halo, carboxyl, A and B are independently hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl, or OR′; or a pharmaceutically acceptable salt thereof, a pharmaceutic-ally acceptable prodrug thereof, an N-oxide thereof, a hydrate thereof or a solvate thereof.Type: GrantFiled: October 16, 1998Date of Patent: April 23, 2002Assignee: Aventis Pharmaceuticals, Inc.Inventors: Michael R. Myers, Martin P. Maguire, Alfred P. Spada, William R. Ewing, Henry W. Pauls, Yong Mi Choi-Sledeski
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Patent number: 6291446Abstract: A method for treating CMV infection and disease conditions associated therewith is disclosed, particularly using the isozyme selective PKC inhibitor, (S)-3,4-[N,N′-1,1′-((2″-ethoxy)-3′″(O)-4′″-(N,N-dimethylamino)-butane)-bis-(3,3′-indolyl)]-1(H)-pyrrole-2,5-dione hydrochloride salt.Type: GrantFiled: February 22, 1999Date of Patent: September 18, 2001Assignee: Eli Lilly and CompanyInventor: Douglas Kirk Ways