DE3007498A1 - Neue piperidin-derivate mit antihistaminwirkung - Google Patents
Neue piperidin-derivate mit antihistaminwirkungInfo
- Publication number
- DE3007498A1 DE3007498A1 DE19803007498 DE3007498A DE3007498A1 DE 3007498 A1 DE3007498 A1 DE 3007498A1 DE 19803007498 DE19803007498 DE 19803007498 DE 3007498 A DE3007498 A DE 3007498A DE 3007498 A1 DE3007498 A1 DE 3007498A1
- Authority
- DE
- Germany
- Prior art keywords
- hydrogen
- acid
- pharmaceutically acceptable
- carbon atoms
- hydroxyl group
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/20—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
- C07D211/22—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Hydrogenated Pyridines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US06/028,813 US4254129A (en) | 1979-04-10 | 1979-04-10 | Piperidine derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE3007498A1 true DE3007498A1 (de) | 1980-10-23 |
| DE3007498C2 DE3007498C2 (https=) | 1989-09-07 |
Family
ID=21845568
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE19803007498 Granted DE3007498A1 (de) | 1979-04-10 | 1980-02-28 | Neue piperidin-derivate mit antihistaminwirkung |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US4254129A (https=) |
| JP (1) | JPS55141469A (https=) |
| AT (1) | AT376208B (https=) |
| AU (1) | AU531146B2 (https=) |
| BE (1) | BE882703A (https=) |
| CA (1) | CA1123438A (https=) |
| CH (1) | CH643245A5 (https=) |
| DE (1) | DE3007498A1 (https=) |
| DK (1) | DK153709C (https=) |
| ES (1) | ES8103735A1 (https=) |
| FR (1) | FR2453854A1 (https=) |
| IL (1) | IL59158A (https=) |
| IT (1) | IT1143960B (https=) |
| NL (2) | NL190580C (https=) |
| NO (2) | NO154521C (https=) |
| NZ (1) | NZ192653A (https=) |
| PH (1) | PH17023A (https=) |
| SE (1) | SE448726B (https=) |
| ZA (1) | ZA80332B (https=) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3917241A1 (de) * | 1989-05-26 | 1990-11-29 | Schaper & Bruemmer Gmbh | 4-(hydroxydiphenylmethyl)-1-piperidyl-phenylalkan-derivate |
| WO1993021156A1 (en) * | 1992-04-10 | 1993-10-28 | Merrell Dow Pharmaceuticals Inc. | 4-diphenylmethyl piperidine derivatives and process for their preparation |
Families Citing this family (115)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1053570C (zh) | 1987-10-07 | 2000-06-21 | 默尔多药物公司 | 哌啶子基链烷醇的药用组合物-减充血剂复方的制备方法 |
| AR240018A1 (es) * | 1987-10-07 | 1990-01-31 | Merrell Pharma Inc | Procedimiento para preparar una composicion que comprende derivados de piperidinoalcanol. |
| US4929605A (en) * | 1987-10-07 | 1990-05-29 | Merrell Dow Pharmaceuticals Inc. | Pharmaceutical composition for piperidinoalkanol derivatives |
| US4908372A (en) * | 1988-10-13 | 1990-03-13 | Merrell Dow Pharmaceuticals Inc. | Antihistaminic piperidinyl benzimidazoles |
| ZA90341B (en) * | 1989-01-23 | 1990-10-31 | Merrell Dow Pharma | Liquid pharmaceutical composition for piperidinoalkanol derivatives |
| US5190029A (en) * | 1991-02-14 | 1993-03-02 | Virginia Commonwealth University | Formulation for delivery of drugs by metered dose inhalers with reduced or no chlorofluorocarbon content |
| US5182097A (en) * | 1991-02-14 | 1993-01-26 | Virginia Commonwealth University | Formulations for delivery of drugs by metered dose inhalers with reduced or no chlorofluorocarbon content |
| TW198008B (https=) * | 1991-04-08 | 1993-01-11 | Green Cross Corp | |
| HU211019B (en) * | 1991-12-02 | 1995-09-28 | Richter Gedeon Vegyeszet | Process for producing new 1,2,3,6-tetrahydropyridine and piperidine derivatives substituted with n-(hydroxylalkyl) group and compositions comprising such compounds |
| WO1993016081A1 (en) * | 1992-02-13 | 1993-08-19 | Merrell Dow Pharmaceuticals Inc. | Piperidinyl thiacyclic derivatives |
| US5631375A (en) * | 1992-04-10 | 1997-05-20 | Merrell Pharmaceuticals, Inc. | Process for piperidine derivatives |
| HU223774B1 (hu) | 1992-05-11 | 2005-01-28 | Merrell Dow Pharmaceuticals Inc. | Terfenadinszármazékok alkalmazása antihisztamin hatású gyógyszerkészítmények előállítására |
| DE9320925U1 (de) * | 1992-08-03 | 1995-08-31 | Georgetown University, Washington, D.C. | Terfenadin-Metabolite und deren optisch reine Isomere für die Behandlung von allergischen Störungen |
| US5654433A (en) * | 1993-01-26 | 1997-08-05 | Merrell Pharmaceuticals Inc. | Process for piperidine derivatives |
| US20020007068A1 (en) * | 1999-07-16 | 2002-01-17 | D'ambra Thomas E. | Piperidine derivatives and process for their production |
| EP0703902B1 (en) * | 1993-06-24 | 1998-12-16 | Albany Molecular Research, Inc. | Process for the production of piperidine derivatives |
| JP3712208B2 (ja) * | 1993-06-25 | 2005-11-02 | メレルファーマスーティカルズ インコーポレイテッド | 抗ヒスタミン性の4−ジフェニルメチル/ジフェニルメトキシピペリジン誘導体類を製造する新規な中間体 |
| US6147216A (en) * | 1993-06-25 | 2000-11-14 | Merrell Pharmaceuticals Inc. | Intermediates useful for the preparation of antihistaminic piperidine derivatives |
| WO1995010278A1 (en) * | 1993-10-15 | 1995-04-20 | Hoechst Marion Roussel, Inc. | Treatment of allergic disorders with terfenadine carboxylate |
| CA2173467A1 (en) * | 1993-10-25 | 1995-05-04 | Keith D. Ertel | A stable pharmaceutical composition of terfenadine and ibuprofen |
| DE69517810T2 (de) * | 1994-05-16 | 2000-12-14 | Merrell Pharmaceuticals Inc., Cincinnati | Verfahren und diastereomere salze nützlich bei der racemattrennung von racemischer 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-alpha,alpha-dimethylphenyl essigsäure sowie entsprechende diastereomere salze |
| CN101497581B (zh) * | 1994-05-18 | 2012-07-11 | 安万特萨博Ⅱ有限公司 | 抗组胺哌啶衍生物,其多晶形物和假同晶物的无水和水合物形式的制备方法 |
| CN1148849A (zh) * | 1994-05-18 | 1997-04-30 | 赫彻斯特马里恩鲁斯公司 | 抗组胺哌啶衍生物,其多晶形物和假同晶物的无水和水合物形式的制备方法 |
| US20030045722A1 (en) * | 1994-05-18 | 2003-03-06 | Henton Daniel R. | Processes for preparing anhydrous and hydrate forms of antihistaminic piperidine derivatives, polymorphs and pseudomorphs thereof |
| MX9701305A (es) | 1994-08-25 | 1998-05-31 | Merrell Pharma Inc | Piperidinas sustituidas novedosas utiles para el tratamiento de enfermedades alergicas. |
| WO1996026726A1 (en) * | 1995-02-28 | 1996-09-06 | Hoechst Marion Roussel, Inc. | Pharmaceutical composition for piperidinoalkanol compounds |
| KR19990008406A (ko) * | 1995-05-08 | 1999-01-25 | 스티븐엘.네스비트 | 알파-(치환된 알킬페닐)-4-(히드록시디페닐메틸)-1-피페리딘 부탄올 유도체들, 그들의 제조 방법 및 항히스타민제, 항알러지제및 기관지 확장제로서 그들의 용도 |
| US5574045A (en) * | 1995-06-06 | 1996-11-12 | Hoechst Marion Roussel, Inc. | Oral pharmaceutical composition of piperidinoalkanol compounds in solution form |
| US5906747A (en) * | 1995-11-13 | 1999-05-25 | Biosepra Inc. | Separation of molecules from dilute solutions using composite chromatography media having high dynamic sorptive capacity at high flow rates |
| US6211199B1 (en) | 1995-11-17 | 2001-04-03 | Aventis Pharmaceuticals Inc. | Substituted 4-(1H-benzimidazol-2-yl-amino)piperidines useful for the treatment of allergic diseases |
| US6423704B2 (en) | 1995-12-20 | 2002-07-23 | Aventis Pharmaceuticals Inc. | Substituted 4-(1H-benzimidazol-2-yl)[1,4]diazepanes useful for the treatment of allergic diseases |
| US6194406B1 (en) | 1995-12-20 | 2001-02-27 | Aventis Pharmaceuticals Inc. | Substituted 4-(1H-benzimidazol-2-yl)[1,4]diazepanes useful for the treatment of allergic disease |
| US6153754A (en) * | 1995-12-21 | 2000-11-28 | Albany Molecular Research, Inc. | Process for production of piperidine derivatives |
| US6201124B1 (en) | 1995-12-21 | 2001-03-13 | Albany Molecular Research, Inc. | Process for production of piperidine derivatives |
| US5998439A (en) * | 1996-02-21 | 1999-12-07 | Hoescht Marion Roussel, Inc. | Substituted N-methyl-N-(4-(piperidin-1-yl)-2-(aryl)butyl)benzamides useful for the treatment of allergic diseases |
| US5932571A (en) * | 1996-02-21 | 1999-08-03 | Hoechst Marion Roussel, Inc. | Substituted N-methyl-N-(4-(4-(1H-benzimidazol-2-yl) {1,4}diazepan-1-yl)-2-(aryl) butyl) benzamides useful for the treatment of allergic diseases |
| US5922737A (en) * | 1996-02-21 | 1999-07-13 | Hoechst Marion Roussel, Inc. | Substituted N-methyl-N-(4-(4-(1H-Benzimidazol-2-YL-amino) piperidin-1-YL)-2-(arlyl) butyl) benzamides useful for the treatment of allergic diseases |
| US5925761A (en) * | 1997-02-04 | 1999-07-20 | Sepracor Inc. | Synthesis of terfenadine and derivatives |
| DE59810863D1 (de) * | 1997-03-11 | 2004-04-08 | Aventis Pharma Inc | Verfahren zur Herstellung von 4-(4-(4-(Hydroxydiphenyl)-1-piperidinyl)-1-hydroxybutyl)-alpha,alpha-dimenthylphenylessigsäure und phosphorylierter Derivate |
| DE69808303T2 (de) * | 1997-08-14 | 2003-05-22 | Aventis Pharmaceuticals Inc., Bridgewater | Verfahren zur verbesserung der bioverfügbarkeit des fexofenadins und seiner derivate |
| US6451815B1 (en) | 1997-08-14 | 2002-09-17 | Aventis Pharmaceuticals Inc. | Method of enhancing bioavailability of fexofenadine and its derivatives |
| CN1159012C (zh) * | 1997-08-26 | 2004-07-28 | 阿旺蒂斯制药公司 | 用于组合哌啶子基烷醇-减充血剂的药物组合物 |
| DK0924196T3 (da) * | 1997-12-17 | 2003-09-29 | Aventis Pharma Gmbh | Fremgangsmåde til alkylering af alkyl- eller benzylcyanderivater i nærværelse af trialkylaminer eller -phosphiner |
| PL193131B1 (pl) * | 1997-12-23 | 2007-01-31 | Schering Corp | Kompozycja farmaceutyczna zawierająca kombinację składników aktywnych i jej zastosowanie |
| US6194431B1 (en) | 1998-04-14 | 2001-02-27 | Paul D. Rubin | Methods and compositions using terfenadine metabolites in combination with leukotriene inhibitors |
| US6683094B2 (en) | 1998-07-02 | 2004-01-27 | Aventis Pharmaceuticals Inc. | Antihistaminic piperidine derivatives and intermediates for the preparation thereof |
| DK1091938T3 (da) * | 1998-07-02 | 2011-02-07 | Aventisub Ii Inc | Antihistamin piperidinderivativer og mellemprodukter til fremstilling af disse |
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| AU2007200674C1 (en) * | 1998-07-02 | 2011-02-24 | Aventisub Llc | Novel antihistaminic piperidine derivatives and intermediates for the preparation thereof |
| GB9822170D0 (en) * | 1998-10-13 | 1998-12-02 | Danbioyst Uk Ltd | Novel formulations of fexofenadine |
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| EP2578570A1 (en) | 2011-10-07 | 2013-04-10 | Almirall, S.A. | Novel process for preparing 5-(2-{[6-(2,2-difluoro-2-phenylethoxy)hexyl]amino}-1(r)-hydroxyethyl)-8-hydroxyquinolin-2(1h)-one via novel intermediates of synthesis. |
| EP2641900A1 (en) | 2012-03-20 | 2013-09-25 | Almirall, S.A. | Novel polymorphic Crystal forms of 5-(2-{[6-(2,2-difluoro-2-phenylethoxy) hexyl]amino}-1-(R)-hydroxyethyl)-8-hydroxyquinolin-2(1h)-one, heminapadisylate as agonist of the ß2 adrenergic receptor. |
| CN102659667B (zh) * | 2012-04-20 | 2013-08-14 | 浙江启明药业有限公司 | 一种非索非那定关键中间体的合成方法 |
| CN103333100B (zh) * | 2013-06-06 | 2016-04-06 | 池州东升药业有限公司 | 一种盐酸非索非那定的合成工艺 |
| ITMI20131652A1 (it) | 2013-10-07 | 2015-04-08 | Dipharma Francis Srl | Procedimento per la purificazione di derivati dell'acido 2-fenil-2-metil-propanoico |
| CN104557671B (zh) * | 2013-10-10 | 2018-04-13 | 池州东升药业有限公司 | 一种非索非那定及中间体的合成方法 |
| EP2949321A1 (en) | 2014-05-26 | 2015-12-02 | Sanovel Ilac Sanayi ve Ticaret A.S. | Multilayer formulations of fexofenadine and montelukast |
| RS58961B1 (sr) | 2015-01-22 | 2019-08-30 | Sanofi Aventis Deutschland | Proces proizvodnje 2-[4-(ciklopropankarbonil)fenil]-2-metil-propannitrila |
| ES2770341T3 (es) | 2015-10-22 | 2020-07-01 | Sanofi Aventis Deutschland | Proceso para la preparación de fexofenadina y de productos intermedios usados en ella |
| GB2629127A (en) | 2022-08-31 | 2024-10-23 | Novumgen Ltd | An orodispersible tablet of fexofenadine and its process of preparation |
| EP4651852A1 (en) | 2023-01-20 | 2025-11-26 | Opella Healthcare Group SAS | Paraben-free fexofenadine formulations |
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| DE2503362A1 (de) * | 1974-02-08 | 1975-08-21 | Richardson Merrell Inc | Alpha-aryl-4-substituierte piperidinoalkyl-derivate und verfahren zu deren herstellung |
| DE2506770A1 (de) * | 1974-03-04 | 1975-09-11 | Richardson Merrell Inc | Piperidinderivate |
| DE2303306B2 (de) * | 1972-01-28 | 1978-09-28 | Richardson-Merrell Inc., New York, N.Y. (V.St.A.) | Piperidinobutanol-Derivate, Verfahren zu deren Herstellung sowie diese enthaltende pharmazeutische Präparate |
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| GB1242169A (en) * | 1969-04-09 | 1971-08-11 | Ucb Sa | Piperidine derivatives |
| BE794596A (fr) * | 1972-01-28 | 1973-05-16 | Richardson Merrell Inc | Piperidinoalcanone-oximes substituees et leur procede de preparation |
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| BE794598A (fr) * | 1972-01-28 | 1973-05-16 | Richardson Merrell Inc | Nouveaux derives olefiniques de piperidines substituees en 4 et leur procede de preparation |
| US3931197A (en) * | 1974-02-08 | 1976-01-06 | Richardson-Merrell Inc. | Substituted piperidine derivatives |
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- 1980-01-18 NZ NZ192653A patent/NZ192653A/xx unknown
- 1980-01-18 IL IL59158A patent/IL59158A/xx unknown
- 1980-01-21 ZA ZA00800332A patent/ZA80332B/xx unknown
- 1980-01-29 AU AU55016/80A patent/AU531146B2/en not_active Expired
- 1980-02-07 NL NL8000754A patent/NL190580C/xx not_active IP Right Cessation
- 1980-02-28 DE DE19803007498 patent/DE3007498A1/de active Granted
- 1980-03-05 CH CH174180A patent/CH643245A5/de not_active IP Right Cessation
- 1980-03-17 AT AT0144880A patent/AT376208B/de not_active IP Right Cessation
- 1980-03-24 IT IT48245/80A patent/IT1143960B/it active Protection Beyond IP Right Term
- 1980-03-26 ES ES489934A patent/ES8103735A1/es not_active Expired
- 1980-03-27 DK DK132980A patent/DK153709C/da not_active IP Right Cessation
- 1980-03-28 PH PH23831A patent/PH17023A/en unknown
- 1980-04-08 SE SE8002634A patent/SE448726B/sv not_active IP Right Cessation
- 1980-04-09 NO NO801014A patent/NO154521C/no unknown
- 1980-04-09 BE BE0/200161A patent/BE882703A/fr not_active IP Right Cessation
- 1980-04-09 FR FR8007992A patent/FR2453854A1/fr active Granted
- 1980-04-09 JP JP4577180A patent/JPS55141469A/ja active Granted
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1998
- 1998-04-08 NL NL980013C patent/NL980013I2/nl unknown
- 1998-05-29 NO NO1998017C patent/NO1998017I1/no unknown
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| DE2303306B2 (de) * | 1972-01-28 | 1978-09-28 | Richardson-Merrell Inc., New York, N.Y. (V.St.A.) | Piperidinobutanol-Derivate, Verfahren zu deren Herstellung sowie diese enthaltende pharmazeutische Präparate |
| DE2503362A1 (de) * | 1974-02-08 | 1975-08-21 | Richardson Merrell Inc | Alpha-aryl-4-substituierte piperidinoalkyl-derivate und verfahren zu deren herstellung |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3917241A1 (de) * | 1989-05-26 | 1990-11-29 | Schaper & Bruemmer Gmbh | 4-(hydroxydiphenylmethyl)-1-piperidyl-phenylalkan-derivate |
| US5077301A (en) * | 1989-05-26 | 1991-12-31 | Schaper & Bruemmer Gmbh & Co. Kg | 4-(hydroxydiphenylmethyl)-1-piperidylphenylalkane derivatives as antihistamines and methods of treatment of an allergic response |
| WO1993021156A1 (en) * | 1992-04-10 | 1993-10-28 | Merrell Dow Pharmaceuticals Inc. | 4-diphenylmethyl piperidine derivatives and process for their preparation |
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