Plural Carbocyclic Rings Containing Patents (Class 546/239)
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Publication number: 20090048257Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPAR? and should be useful for treating conditions mediated by the same.Type: ApplicationFiled: March 7, 2007Publication date: February 19, 2009Inventor: Per Sauerberg
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Publication number: 20090012301Abstract: Provided is a crystalline form of fexofenadine free base and processes for its preparation.Type: ApplicationFiled: September 12, 2008Publication date: January 8, 2009Inventors: Shlomit Wizel, Ilan Kor-Sade
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Publication number: 20090012121Abstract: The present invention provides novel crystal forms of fexofenadine hydrochloride Forms V, VI and VIII through XV and processes for their preparation and preparation of amorphous form and other crystalline forms of fexofenadine hydrochloride. Forms XIV and XV are solvates of ethyl acetate, while Form IX is a solvate of MTBE or cyclohexane. The forms are useful for administration to humans and animals to alleviate symptoms caused by histamine. The present invention further provides pharmaceutical compositions of the new crystalline forms.Type: ApplicationFiled: September 9, 2008Publication date: January 8, 2009Inventors: Ben-Zion DOLITZKY, Shlomit Wizel, Barnaba Krochmal, Dov Diller, Irwin Gross
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Patent number: 7470789Abstract: Anhydrous crystalline fexofenadine hydrochloride Form C, crystalline fexofenadine acetate monohydrate Form D, crystalline fexofenadine acetate dihydrate Form E and crystalline fexofenadine free base monohydrate Form F, processes of preparing the same, pharmaceutical compositions thereof, therapeutic uses thereof and methods of treatment therewith.Type: GrantFiled: August 25, 2004Date of Patent: December 30, 2008Assignee: Cipla LimitedInventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Manish Gopaldas Gangrade, Dilip Ramdas Birari
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Publication number: 20080306071Abstract: Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.Type: ApplicationFiled: April 28, 2008Publication date: December 11, 2008Applicant: Adolor CorporationInventors: Roland Ellwood Dolle, Bertrand Le Bourdonnec
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Publication number: 20080167471Abstract: The present invention is related to novel processes for preparing anhydrous and hydrated forms of piperidine derivatives, polymorphs and pseudomorphs thereof of the formulas which are useful as antihistamines, antiallergic agents and bronchodilators.Type: ApplicationFiled: October 30, 2007Publication date: July 10, 2008Inventors: Daniel R. Henton, Frederick J. McCarty, Susan I. Tripp, Jill E. DeWitt
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Patent number: 7396844Abstract: Benzamidine derivatives of the following formulae or analogs thereof, i.e., pharmaceutically acceptable salts thereof, are provided.Type: GrantFiled: July 19, 1999Date of Patent: July 8, 2008Assignee: Ajinomoto Co., Inc.Inventors: Masaru Takayanagi, Kazuyuki Sagi, Tadakiyo Nakagawa, Masahiro Yamanashi, Takashi Kayahara, Shunji Takehana, Yumiko Fukuda, Mitsuo Takahashi, Masataka Shoji
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Patent number: 7381721Abstract: 3,4-Disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.Type: GrantFiled: March 17, 2003Date of Patent: June 3, 2008Assignee: Adolor CorporationInventors: Roland Ellwood Dolle, Bertrand Le Bourdonnec
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Patent number: 7238834Abstract: The present invention relates to substantially pure piperidine derivative compounds of the formulae: wherein R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; R3 is —COOH or —COOR4; R4 has 1 to 6 carbon atoms; A, B, and D are the substituents of their respective rings each of which may be different or the same and are hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents. A process of preparing such piperidine derivative compounds in substantially pure form is also disclosed.Type: GrantFiled: October 14, 2005Date of Patent: July 3, 2007Assignee: AMR Technology, Inc.Inventor: Thomas E. D'Ambra
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Patent number: 7235665Abstract: The present invention relates to processes for preparing certain piperidine derivatives, including fexofenadine (F), the active ingredient in the non-sedating antihistamine sold in the U.S. under the designation “Allegra®”. This invention also relates to novel synthetic intermediates useful in the processes of the present invention.Type: GrantFiled: April 22, 2004Date of Patent: June 26, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Collin H. Schroeder, Ryan R. Huddleston, Richard H. Charles
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Patent number: 7232908Abstract: The present invention relates to a process for the production of piperidine derivatives with microorganisms. This is carried out by incubating starting compounds in the presence of a microorganism under conditions effective to produce piperidine derivative products. Suitable microorganisms can be from any one of the genus of Stemphylium, Gliocladium, Bacillus, Botrytis, Cyathus, Rhizopus, Pycniodosphora, Pseudomonas, Helicostylum, Mucor, Gelasinospora, Rhodotorula, Candida, Mycobacterium, and Penicillium. In another aspect of the invention, starting compounds are incubated in the presence of Cunninghamella bainieria under conditions effective to produce piperidine derivative products.Type: GrantFiled: August 11, 2003Date of Patent: June 19, 2007Assignee: AMR Technology, Inc.Inventors: Peter C. Michels, Eric L. Zirbes
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Patent number: 7220752Abstract: This invention relates to novel compounds that are liver selective glucocorticoid receptor antagonists, to methods of preparing such compounds, and to methods for using such compounds in therapy and in the regulation of metabolism, especially lowering blood glucose levels. The compounds referred to are compounds according to the formula 1: wherein the variables are as defined herein.Type: GrantFiled: November 28, 2001Date of Patent: May 22, 2007Assignees: Karo Bio AB, Abbott LaboratoriesInventors: Benjamin Pelcman, Annika Gustafsson, Philip R. Kym
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Patent number: 7176318Abstract: An improved process for the manufacture of fexofenadine is described in which a compound of formula (F): wherein R2 represents COOH, COO—C1-6 alkyl or CN; and R3 represents hydrogen, mesylate, triflate, tosylate or carboxy-C1-6-alkyl, or a salt thereof is prepared by: (I) reacting a compound of formula (B): wherein R1 represents hydrogen or carboxy-C1-6-alkyl; and R2 is a hereinbefore defined, with a copper and/or silver compound in the presence of palladium or a compound thereof to yield a compound of formula (C): wherein R1, and R2 are as hereinbefore defined; (II) converting said compound of formula (C) into a compound of formula (E): wherein R2 and R3 are as hereinbefore defined and R4 represents a halogen atom, and (III) reacting said compound of formula (E) with azacyclonol.Type: GrantFiled: July 19, 2001Date of Patent: February 13, 2007Assignee: Texcontor EstablissementInventors: Federico Junquera Milla, William Paul Jackson
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Patent number: 7141573Abstract: One aspect of the present invention relates to polypharmacophoric compounds. In certain embodiments, the polyphamacophore compounds comprise individual pharmacophore units selected from the group consisting of D-1 agonists, D-2 agonists, D-3 agonists, D-4 agonists, irreversible monoamine inhibitors, reversible monoamine inhibitors, monoamine transporter inhibitors, COMT inhibitors, MAO inhibitors, and dopamine transporter inhibitors. Moreover, the present invention also relates to combinatorial libraries of polypharmacophoric compounds. Another aspect of the present invention relates to the use of a polypharmacophoric compound in a method of treating a mammal in need thereof. For example, a polypharmacophoric compound of the present invention may be used in a method of treating a mammal afflicted with Alzheimer's Disease, Huntington's Disease, depression, attention deficit disorder, autism, obesity, or inflammation.Type: GrantFiled: January 11, 2001Date of Patent: November 28, 2006Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: Robert N. Hanson, John W. Babich
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Patent number: 7138524Abstract: The present invention is related to novel processes for preparing anhydrous and hydrated forms of piperidine derivatives, polymorphs and pseudomorphs thereof of the formulas which are useful as antihistamines, antiallergic agents and bronchodilators.Type: GrantFiled: June 3, 2002Date of Patent: November 21, 2006Assignee: Aventis Pharmaceuticals, Inc.Inventors: Frederick J. McCarty, Albert A. Carr
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Patent number: 7135571Abstract: The present invention is related to novel processes for preparing anhydrous and hydrated forms of piperidine derivatives, polymorphs and pseudomorphs thereof of the formulas which are useful as antihistamines, antiallergic agents and bronchodilators.Type: GrantFiled: June 3, 2002Date of Patent: November 14, 2006Assignee: Aventis Pharmaceuticals, Inc.Inventors: Daniel R Henton, Frederick J McCarty, Susan I Tripp, Jill E DeWitt
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Patent number: 7078402Abstract: The invention relates to novel aminothiol ester compounds having the general formula (I): and to a method for preparing them and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (cancers and precancers, dermatological, rheumatic and ophthalmological complaints in particular) or in cosmetic compositions. The invention also relates to a pharmaceutical or cosmetic composition, characterized in that it comprises, as active agent, a compound of general formula (I) in combination with a pharmaceutically or cosmetically acceptable support.Type: GrantFiled: May 31, 2001Date of Patent: July 18, 2006Assignee: Centre National de la Recherche Scientifique (CNRS)Inventors: Guy Fournet, Gerard Anthony Quash, Jacques Gore
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Patent number: 6992090Abstract: Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.Type: GrantFiled: June 16, 2003Date of Patent: January 31, 2006Assignee: Adolor CorporationInventors: Bertrand Le Bourdonnec, Roland E. Dolle
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Patent number: 6974872Abstract: The present invention discloses processes for preparing piperidine derivative compounds of the formulae: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.Type: GrantFiled: August 5, 2002Date of Patent: December 13, 2005Assignee: AMR Technology, Inc.Inventors: Thomas E. D'Ambra, Garry M. Pilling
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Patent number: 6930197Abstract: This invention relates to a process for the preparation of compounds of the formula: wherein R1 is C1-C6alkyl and the C1-C6alkyl moiety is straight or branched.Type: GrantFiled: March 22, 2002Date of Patent: August 16, 2005Assignee: Aventis Pharmaceuticals Inc.Inventor: Timothy A. Ayers
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Patent number: 6919458Abstract: The present invention relates to a process for preparing piperidine derivative compounds of the formulae: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents, The process comprises providing a regiosomer of the following formula: wherein Z is —CG1G2G3, m is an integer from 1 to 6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; G1, G2, and G3 are the same or different and are selected from the group consisting of OR8, SR8, and NR8R9; R6 and R7 are the same or different and are selected from the group consisting of hydrType: GrantFiled: August 5, 2002Date of Patent: July 19, 2005Assignee: AMR Technology, Inc.Inventors: Thomas E. D'Ambra, Garry M. Pilling
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Patent number: 6881845Abstract: The present invention relates to a process for preparing (±)-trans-4-p-fluorophenyl-3-hyroxymethyl-1-methylpiperdine of formula (I). The present invention also relates to novel intermediates of the formula (IX) and (IX?) methods for preparing said intermediates and the use of said compounds for preparing Paroxetine and Omiloxetine.Type: GrantFiled: January 4, 2001Date of Patent: April 19, 2005Assignee: Ferrer Internacional, S.A.Inventors: Rafael Foguet, Jorge Ramentol, Diego Fernandez-Cano, Miguel P. Armengol, Inés Petschen, Juan Sallares, Francesc X. Camps, Manuel M. Raga, Josep M. Castello
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Patent number: 6875775Abstract: The invention provides novel selective estrogen receptor modulator compounds of the general formula: wherein R1 and R2, which are the same or different are a) H, halogen, OCH3, OH; or where X is O, NH or S; and n is an integer from 1 to 4; and R4 and R5, which are the same or different, are a 1 to 4 carbon alkyl, H, —CH2C?CH or —CH2CH2OH; or R4 and R5 form an N-containing five- or six-membered ring or heteroaromatic ring; or c) —Y—(CH2)nCH2—O—R6 where Y is O, NH or S and n is an integer from 1 to 4; and R6 is H, —CH2CH2OH, or —CH2CH2Cl; or d) 2,3-dihydroxypropoxy, 2-methylsulfamylethoxy, 2-chloroethoxy, 1-ethyl-2-hydroxyethoxy, 2,2-diethyl-2-hydroxyethoxy or carboxymethoxy; and ?R3 is H, halogen, OH or —OCH3; stereoisomers thereof and their non-toxic pharmaceutically acceptable salts and esters and mixtures thereof, which compounds exhibit valuable pharmacological properties.Type: GrantFiled: April 8, 2003Date of Patent: April 5, 2005Assignee: Hormos Medical Oy LTDInventors: Marja-Liisa Södervall, Arja Kalapudas, Lauri Kangas, Risto Lammintausta, Pirkko Härkönen, Kalervo Väänänen, Arto Karjalainen
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Publication number: 20040254377Abstract: Novel processes for the preparation of peripheral opioid antagonist compounds and intermediates thereto. The compounds prepared by the present processes may be useful, for example, as antagonists to the mu, kappa and delta opioid receptors, and thereby may be useful in the treatment of gastrointestinal motility disorders, and in preventing peripheral opiate induced side effects. The present processes may offer improved yields, purity, ease of preparation and/or isolation of intermediates and final product, and more industrially useful reaction conditions and workability.Type: ApplicationFiled: July 9, 2004Publication date: December 16, 2004Applicant: Adolor CorporationInventors: Bertrand Le Bourdonnec, Roland Ellwood Dolle
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Patent number: 6815549Abstract: A process for the preparation of 4-[1-hydroxy-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-butyl]-&agr;,&agr;-dimethylbenzeneacetic acid (Fexofenadine) of formulaType: GrantFiled: May 16, 2002Date of Patent: November 9, 2004Assignee: Dinamite Dipharma S.p.A.Inventors: Graziano Castaldi, Giuseppe Barreca, Domenico Magrone
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Publication number: 20040186137Abstract: A process and diastereomeric salts useful for the optical resolution of racemic &agr;-[4-(1,1-dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol, 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-&agr;,&agr;-dimethylbenzeneacetic acid and lower alkyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-&agr;,&agr;-dimethylbenzeneacetates. The process comprises placing into solution a chiral resolving agent, either (+)/(−)-di-paratoluoyltartaric acid or (−)/(+)-mandelic acid, in an amount equimolar to a compound corresponding to the desired enantiomer of the above compound, precipitating the resulting diastereomeric salt between the chiral resolving agent and the target enantiomer and separating the enantiomer.Type: ApplicationFiled: January 29, 2004Publication date: September 23, 2004Applicant: Merrell Pharmaceuticals Inc.Inventors: Mitsuo Nakamura, Masatoshi Shiga
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Patent number: 6777555Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, n is an integer 0.Type: GrantFiled: February 12, 2003Date of Patent: August 17, 2004Assignee: Merrell Pharmaceuticals, Inc.Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
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Patent number: 6730791Abstract: This invention relates to novel compounds of the following formula and a process for the preparation thereof. wherein X is Cl, Br or I.Type: GrantFiled: March 22, 2002Date of Patent: May 4, 2004Assignee: Aventis Pharmaceuticals Inc.Inventor: Timothy A. Ayers
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Publication number: 20040077683Abstract: The present invention is related to novel polymorph of Fexofenadine and Fexofenadine hydrochloride of formula 1 and process of preparation thereof. The present invention is also directed to provide pure novel polymorphs of Fexofenadine and its hydrochloride by a simple process which is cost effective, commercially viable and environment friendly.Type: ApplicationFiled: November 12, 2003Publication date: April 22, 2004Inventors: M. Satyanarayana Reddy, S. Thirumalai Rajan, U.V. Bhaskara Rao
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Patent number: 6723738Abstract: The invention provides novel selective estrogen receptor modulator compounds of the general formula: wherein R1 and R2 , which are the same or different are a) H, halogen, OCH3, OH; or where X is O, NH or S; and n is an integer from 1 to 4; and R4 and R5, which are the same or different, are a 1 to 4 carbon alkyl, H, —CH2C≡CH or —CH2CH2OH; or R4 and R5 form an N-containing five- or six-membered ring or heteroaromatic ring; or c) —Y—(CH2)nCH2—O—R6 where Y is O, NH or S and n is an integer from 1 to 4; and R6 is H, —CH2CH2OH, or —CH2CH2Cl; or d) 2,3-dihydroxypropoxy, 2-methylsulfamylethoxy, 2-chloroethoxy, 1-ethyl-2-hydroxyethoxy, 2,2-diethyl-2-hydroxyethoxy or carboxymethoxy; and R3 is H, halogen, OH or —OCH3; stereoisomers thereof and their non-toxic pharmaceutically acceptable salts and esters and mixtures thereof, which compounds exhibit valuable pharmacological properties.Type: GrantFiled: April 8, 2003Date of Patent: April 20, 2004Assignee: Hormos Medical Oy LtdInventors: Marja-Liisa Södervall, Arja Kalapudas, Lauri Kangas, Risto Lammintausta, Pirkko Härkönen, Kalervo Väänänen
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Patent number: 6716986Abstract: The present invention is directed to sulfuric acid mono-[3-({1-[2-(4-fluoro-phenyl)-ethyl]-piperidin-4-yl}-hydroxy-methyl)-2-methoxy-phenyl]ester, a metabolite of the 5HT2A antagonist (+)-&agr;-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol and a processes for its preparation and its use in the treatment for a number of disease states.Type: GrantFiled: July 22, 2002Date of Patent: April 6, 2004Assignee: Aventis Pharmaceuticals Inc.Inventors: Ronald Charles Bernotas, Paul Wayne Brown, Gary Thomas Emmons, Chi-Hsin Richard King
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Publication number: 20040044038Abstract: Provided is a crystalline (polymorphic) form of fexofenadine hydrochloride, denominated fexofenadine hydrochloride Form XVI.Type: ApplicationFiled: June 10, 2003Publication date: March 4, 2004Inventors: Barnaba Krochmal, Dov Diller, Ben-Zion Dolitzky, Judith Aronhime, Shlomit Wizel, Boaz Gome, Igor Lifshitz
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Patent number: 6683094Abstract: This invention relates to novel piperidine derivatives of formula (I) and a process for the preparation thereof. wherein R1 is H or C1-C6alkyl wherein the C1-C6alkyl moiety is straight or branched; R2 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; or stereoisomers or pharmaceutically acceptable acid addition salt thereof.Type: GrantFiled: June 12, 2002Date of Patent: January 27, 2004Assignee: Aventis Pharmaceuticals Inc.Inventors: Timothy A. Ayers, Paul W. Brown
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Patent number: 6673933Abstract: This invention relates to novel compounds of formula: wherein R1 is H or C1-C6alkyl and the C1-C6alkyl moiety is straight or branched; R2 and R3 are each independently C1-C6alkyl and the C1-C6alkyl moiety is straight or branched; or stereoisomers or pharmaceutically acceptable acid addition salt thereof.Type: GrantFiled: March 22, 2002Date of Patent: January 6, 2004Assignee: Aventis Pharmaceutical Inc.Inventor: Timothy A. Ayers
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Patent number: 6613907Abstract: The present invention relates to the production of a product compound having a structure according to Formulae IA and/or IB: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, and alkoxy. This process involves incubating a starting compound having a structure according to Formulae IIA and/or IIB: wherein R3 is —CH3 and R1, R2, A, B, and D are defined above In the presence of a microorganism under conditions effective to produce the product compound.Type: GrantFiled: January 4, 2001Date of Patent: September 2, 2003Assignee: AMR Technology, Inc.Inventors: Peter C. Michels, Eric L. Zirbes
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Patent number: 6613906Abstract: A novel crystal form of ,&agr;-dimethyl-4-{1-hydroxy-4-{4-(hydroxydiphenylmethyl)-1-piperidinyl}butyl}benzeneacetic acid hydrochloride, processes for its preparation and its pharmaceutical use are disclosed.Type: GrantFiled: June 6, 2000Date of Patent: September 2, 2003Assignee: Geneva Pharmaceuticals, Inc.Inventors: Julian Anthony Davies, James E. Gano
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Patent number: 6576645Abstract: The invention provides novel selective estrogen receptor modulator compounds of the general formula: wherein R1 and R2, which are the same or different are a) H, halogen, OCH3, OH; or where X is O, NH or S; and n is an integer from 1 to 4; and R4 and R5, which are the same or different, are a 1 to 4 carbon alkyl, H, —CH2C≡CH or —CH2CH2OH; or R4 and R5 form an N-containing five- or six-membered ring or heteroaromatic ring; or c) —Y—(CH2)nCH2—O—R6 where Y is O, NH or S and n is an integer from 1 to 4; and R6 is H, —CH2CH2OH, or —CH2CH2Cl; or d) 2,3-dihydroxypropoxy, 2-methylsulfamylethoxy, 2-chloroethoxy, 1-ethyl-2-hydroxyethoxy, 2,2-diethyl-2-hydroxyethoxy or carboxymethoxy; and R3 is H, halogen, OH or —OCH3; stereoisomers thereof and their non-toxic pharmaceutically acceptable salts and esters and mixtures thereof, which compounds exhibit valuable pharmacological properties.Type: GrantFiled: November 15, 2000Date of Patent: June 10, 2003Assignee: Hormos Medical Oy LtdInventors: Marja-Liisa Södervall, Arja Kalapudas, Lauri Kangas, Risto Lammintausta, Pirkko Härkönen, Kalervo V{umlaut over (aa)}nänen
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Patent number: 6566526Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 to 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, m is an integer 0.Type: GrantFiled: November 29, 2000Date of Patent: May 20, 2003Assignee: Merrell Pharmaceuticals Inc.Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
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Patent number: 6559312Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer of 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, m is an integer 0.Type: GrantFiled: December 8, 2000Date of Patent: May 6, 2003Assignee: Merrell Pharmaceuticals Inc.Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
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Patent number: 6555689Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, m is an integer 0.Type: GrantFiled: December 1, 2000Date of Patent: April 29, 2003Assignee: Merrell Pharmaceuticals Inc.Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
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Patent number: 6552200Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1represented hydroxy, n is an integer 0.Type: GrantFiled: November 29, 2000Date of Patent: April 22, 2003Assignee: Merrell Pharmaceuticals Inc.Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
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Patent number: 6548675Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken to form a second bond between the carbon atoms R1 and R2 or where R1 represented hydroxy integer 0.Type: GrantFiled: December 5, 2000Date of Patent: April 15, 2003Assignee: Merrell Pharmaceuticals Inc.Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
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Patent number: 6538002Abstract: The present in to s directed to compounds of the formula I: (wherein R1, R2, R3, R7, R8, X, Y, Z, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.Type: GrantFiled: June 8, 2000Date of Patent: March 25, 2003Assignee: Merck & Co., Inc.Inventors: Paul E. Finke, Malcolm Maccoss, Sander G. Mills, Bryan Oates
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Publication number: 20030045721Abstract: The present invention is related to novel processes for preparing anhydrous and hydrated forms of piperidine derivatives, polymorphs and pseudomorphs thereof of the formulas 1Type: ApplicationFiled: August 7, 2002Publication date: March 6, 2003Inventors: Daniel R. Henton, Jill E. Dewitt, Frederick J. McCarty, Susan I. Tripp
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Publication number: 20020198233Abstract: A process for the preparation of 4-[1-hydroxy-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-butyl]-&agr;,&agr;-dimethylbenzeneacetic acid (Fexofenadine) of formula 1Type: ApplicationFiled: May 16, 2002Publication date: December 26, 2002Inventors: Graziano Castaldi, Giuseppe Barreca, Domenico Magrone
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Publication number: 20020193603Abstract: The present invention is related to novel processes for preparing anhydrous and hydrated forms of piperidine derivatives, polymorphs and pseudomorphs thereof of the formulas 1Type: ApplicationFiled: June 3, 2002Publication date: December 19, 2002Inventors: Daniel R. Henton, Susan I. Tripp, Frederick J. McCarty, Jill E. DeWitt
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Patent number: 6479518Abstract: The present invention is directed to certain novel compounds represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein R3, R5, R6, R7, R8, R11, R12, R13, Q, W, X, Y and Z are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of psychiatric disorders including depression and anxiety.Type: GrantFiled: September 21, 2001Date of Patent: November 12, 2002Assignee: Merck & Co., Inc.Inventors: Paul E. Finke, Laura C. Meurer, Sander G. Mills, Malcolm MacCoss, Hongbo Qi
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Patent number: 6479663Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy m is an integer 0.Type: GrantFiled: December 1, 2000Date of Patent: November 12, 2002Assignee: Merrell Pharmaceuticals Inc.Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
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Patent number: 6458958Abstract: The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula: where Z is —CG1G2G3; G1, G2, and G3 are the same or different and are selected from the group consisting of OR8, SR8, and NR8R9; and R8, and R9 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety.Type: GrantFiled: August 9, 2000Date of Patent: October 1, 2002Assignee: Albany Molecular Research, Inc.Inventors: Thomas E. D'Ambra, Garry M. Pilling
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Patent number: RE39128Abstract: The present invention relates to pleuromutilin derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medical therapy, particularly antibacterial therapy.Type: GrantFiled: October 27, 1998Date of Patent: June 13, 2006Assignee: SmithKline Beecham p.l.c.Inventors: Valerie Joan Berry, Steven Dabbs, Colin Henry Frydrych, Eric Hunt, Francis Dominic Sanderson, Gary Woodnutt