WO2002020529A8 - PROCEDIMIENTO PARA LA OBTENCIÓN DE 4-(N-ALQUILAMINO)-5,6-DIHIDRO-4H-TIENO-(2,3-b)-TIOPIRAN-2-SULFONAMIDA-7,7-DIÓXIDOS, E INTERMEDIOS - Google Patents

PROCEDIMIENTO PARA LA OBTENCIÓN DE 4-(N-ALQUILAMINO)-5,6-DIHIDRO-4H-TIENO-(2,3-b)-TIOPIRAN-2-SULFONAMIDA-7,7-DIÓXIDOS, E INTERMEDIOS

Info

Publication number
WO2002020529A8
WO2002020529A8 PCT/ES2001/000335 ES0100335W WO0220529A8 WO 2002020529 A8 WO2002020529 A8 WO 2002020529A8 ES 0100335 W ES0100335 W ES 0100335W WO 0220529 A8 WO0220529 A8 WO 0220529A8
Authority
WO
WIPO (PCT)
Prior art keywords
alkylamine
thiopyran
dioxides
thieno
dihydro
Prior art date
Application number
PCT/ES2001/000335
Other languages
English (en)
French (fr)
Other versions
WO2002020529A1 (es
Inventor
Losada Pablo Garcia
Guisasola Luis Octavio Silva
Bonde-Larsen Antonio Lorente
Juarez Jorge Martin
Original Assignee
Raga Consultores S L
Losada Pablo Garcia
Guisasola Luis Octavio Silva
Bonde-Larsen Antonio Lorente
Juarez Jorge Martin
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Raga Consultores S L, Losada Pablo Garcia, Guisasola Luis Octavio Silva, Bonde-Larsen Antonio Lorente, Juarez Jorge Martin filed Critical Raga Consultores S L
Priority to CA002436185A priority Critical patent/CA2436185C/en
Priority to EP01965290A priority patent/EP1329453B1/en
Priority to DE60103921T priority patent/DE60103921T2/de
Priority to AU2001285958A priority patent/AU2001285958A1/en
Priority to AT01965290T priority patent/ATE269338T1/de
Priority to JP2002525150A priority patent/JP5137284B2/ja
Publication of WO2002020529A1 publication Critical patent/WO2002020529A1/es
Publication of WO2002020529A8 publication Critical patent/WO2002020529A8/es
Priority to US10/379,096 priority patent/US7030250B2/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

El procedimiento para la obtención de 4-(N-alquilamino)-5,6-dihidro-4H-tieno-(2,3-b)-tiopiran-2-sulfonamida-7,7-dióxidos (I) donde R1 es H o alquilo C1-5 y R2 es alquilo C1-5, parte de los correspondientes 4-(N-alquilamino)-5,6-dihidro-4H-tieno-(2,3-b)-tiopiran-7,7-dióxidos y comprende la protección del grupo alquilamino, la introducción del grupo sulfonamida y la liberación del grupo protector. Algunos compuestos (I) son inhibidores de la anhidrasa carbónica y pueden ser utilizados en el tratamiento de la presión intraocular elevada.
PCT/ES2001/000335 2000-09-04 2001-09-04 PROCEDIMIENTO PARA LA OBTENCIÓN DE 4-(N-ALQUILAMINO)-5,6-DIHIDRO-4H-TIENO-(2,3-b)-TIOPIRAN-2-SULFONAMIDA-7,7-DIÓXIDOS, E INTERMEDIOS WO2002020529A1 (es)

Priority Applications (7)

Application Number Priority Date Filing Date Title
CA002436185A CA2436185C (en) 2000-09-04 2001-09-04 Method for obtaining 4-(n-alkylamine)-5, 6-dihydro-4h-thieno-(2,3-b)-thiopyran-2-sulfamide-7, 7-dioxides and intermediate products
EP01965290A EP1329453B1 (en) 2000-09-04 2001-09-04 Method for obtaining 4-(n-alkylamine)-5, 6-dihydro-4h-thieno-(2,3-b)-thiopyran-2-sulfonamide-7, 7-dioxides and intermediate products
DE60103921T DE60103921T2 (de) 2000-09-04 2001-09-04 Verfahren zur herstellung von 4-(n-alkylamin)-5,6-dihydro-4h-thieno-(2,3-b)-thiopyran-2-sulfonamid-7,7-dioxiden und zwischenprodukte
AU2001285958A AU2001285958A1 (en) 2000-09-04 2001-09-04 Method for obtaining 4-(n-alkylamine)-5, 6-dihydro-4h-thieno-(2,3-b)-thiopyran-2-sulfamide-7, 7-dioxides and intermediate products
AT01965290T ATE269338T1 (de) 2000-09-04 2001-09-04 Verfahren zur herstellung von 4-(n-alkylamin)-5,6-dihydro-4h-thieno-(2,3-b)-t iopyran-2-sulfonamid- 7,7-dioxiden und zwischenprodukte
JP2002525150A JP5137284B2 (ja) 2000-09-04 2001-09-04 ４−（Ｎ−アルキルアミノ）−５，６−ジヒドロ−４Ｈ−チエン−（２，３−ｂ）−チオピラン−２−スルホンアミド−７，７−ジオキシドおよび中間体を得る方法
US10/379,096 US7030250B2 (en) 2000-09-04 2003-03-03 Process for obtaining 4-(N-alkylamino)-5,6-dihydro-4H-thien-(2,3-b)-thiopyran-2-sulfonamide-7,7-dioxides and intermediates

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ESP200002171 2000-09-04
ES200002171A ES2177415B1 (es) 2000-09-04 2000-09-04 Procedimiento para la obtencion de 4-alquilamino-5, 6-dihidro-4h-tieno-(2,3b)-tiopiran-2-sulfonamida-7-dioxidos, e intermedios.

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US10/379,096 Continuation US7030250B2 (en) 2000-09-04 2003-03-03 Process for obtaining 4-(N-alkylamino)-5,6-dihydro-4H-thien-(2,3-b)-thiopyran-2-sulfonamide-7,7-dioxides and intermediates

Publications (2)

Publication Number Publication Date
WO2002020529A1 WO2002020529A1 (es) 2002-03-14
WO2002020529A8 true WO2002020529A8 (es) 2002-07-25

Family

ID=8494840

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/ES2001/000335 WO2002020529A1 (es) 2000-09-04 2001-09-04 PROCEDIMIENTO PARA LA OBTENCIÓN DE 4-(N-ALQUILAMINO)-5,6-DIHIDRO-4H-TIENO-(2,3-b)-TIOPIRAN-2-SULFONAMIDA-7,7-DIÓXIDOS, E INTERMEDIOS

Country Status (9)

Country Link
US (1) US7030250B2 (es)
EP (1) EP1329453B1 (es)
JP (1) JP5137284B2 (es)
AT (1) ATE269338T1 (es)
AU (1) AU2001285958A1 (es)
CA (1) CA2436185C (es)
DE (1) DE60103921T2 (es)
ES (2) ES2177415B1 (es)
WO (1) WO2002020529A1 (es)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1765828B1 (en) * 2004-07-09 2007-12-05 FDC Limited AN IMPROVED PROCESS FOR THE PREPARATION OF 5,6 -DIHYDRO -4H-4(S)-ETHYLAMINO-6(S)-METHYLTHIENO[2,3-b] THIOPYRAN-2-SULFONAMIDE- 7,7 -DIOXIDE AND ITS SALT
ES2253112B1 (es) * 2004-11-05 2007-03-16 Ragactives, S.L. Procedimiento para la obtencion de derivados de 4-(n-alquilamino)-5, 6-dihidro-4h-tieno-(2,3-b)-tiopirano.
US7109353B2 (en) * 2004-12-28 2006-09-19 Council Of Scientific And Industrial Research Process for preparing 5,6-dihydro-4-(S)-(ethylamino)-6-(S) methyl-4H-thieno[2,3b]thiopyran-2-sulphonamide-7,7-dioxide HCl
US20060155132A1 (en) * 2005-01-06 2006-07-13 Kovacs Laszlo Z Method of making dorzolamide hydrochloride
US20060173068A1 (en) * 2005-01-18 2006-08-03 Judith Aronhime Amorphous and crystalline forms of dorzolamide hydrochloride and processes of making same
CN1939923B (zh) * 2005-09-30 2010-05-05 北京德众万全医药科技有限公司 一种多佐胺中间体的制备方法
LT5504B (lt) 2006-08-02 2008-06-25 Biotechnologijos Institutas Benzimidazo[1,2-c][1,2,3]tiadiazolo sulfonamidai - karboanhidrazių slopikliai ir tarpiniai junginiai jiems gauti
WO2010013240A1 (en) 2008-07-31 2010-02-04 Dekel Pharmaceuticals Ltd. Compositions and methods for treating inflammatory disorders
KR20180058758A (ko) 2015-09-22 2018-06-01 그레이버그 비젼, 인크. 안구 장애의 치료를 위한 화합물 및 조성물
CN110662543A (zh) 2017-03-23 2020-01-07 灰色视觉公司 用于治疗眼部疾病的药物和组合物
MX2019013363A (es) 2017-05-10 2020-01-13 Graybug Vision Inc Microparticulas de liberacion extendida y suspensiones de las mismas para terapia medica.
WO2020069353A1 (en) * 2018-09-27 2020-04-02 Graybug Vision, Inc. Compounds and compositions for ocular delivery
EP3908268A1 (en) * 2019-01-09 2021-11-17 Yeda Research and Development Co. Ltd Modulators of pin1 activity and uses thereof
CN113336770B (zh) * 2021-06-24 2022-05-20 中南林业科技大学 一种盐酸多佐胺的手性合成方法

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4797413A (en) * 1986-05-14 1989-01-10 Merck & Co., Inc. Thieno thiopyran sulfonamide derivatives, pharmaceutical compositions and use
US4863922A (en) * 1984-12-12 1989-09-05 Merck & Co., Inc. Substituted aromatic sulfonamides as antiglaucoma agents, compositions and use
US4820848A (en) * 1984-12-12 1989-04-11 Merck & Co., Inc. Substituted aromatic sulfonamides as antiglaucoma agents
US4677115A (en) * 1984-12-12 1987-06-30 Merck & Co., Inc. Antiglaucoma thieno-thiopyran and thieno-thiepin sulfonamide derivatives, compositions, and method of use thereof
US4824968A (en) * 1984-12-12 1989-04-25 Merck & Co., Inc. Substituted aromatic sulfonamides as antiglaucoma agents
US5120757A (en) * 1989-07-31 1992-06-09 Merck & Co., Inc. Substituted aromatic sulfonamides as antiglaucoma agents
US5011942A (en) * 1990-02-05 1991-04-30 Merck & Co., Inc. Process for racemizing an enantiomer of 5,6-dihydro-4-alkylamino-4H-thieno(or furo) [2,3-B]-thiopyran-2-sulfonamide-7,7-dioxide
IE911192A1 (en) * 1990-04-12 1991-10-23 Merck & Co Inc Substituted aromatic sulfonamides as antiglaucoma agents
US5091409A (en) * 1990-05-17 1992-02-25 Merck & Co., Inc. 4-alkylamino-6-(C3-5 -hydrocarbyl)thieno[2,3-B]thiopyran-2-sulfonamide-7,7-dioxides
KR100319837B1 (ko) 1992-08-28 2002-04-22 커스티 마가렛 핀더 4h-티에노(2,3-6)티오피란유도체를제조하기위한효소적비대칭환원방법
JP3279671B2 (ja) 1992-09-28 2002-04-30 鐘淵化学工業株式会社 チエノチオピラン誘導体の製造方法
TW265343B (es) * 1993-03-22 1995-12-11 Merck & Co Inc
US5391772A (en) * 1993-07-08 1995-02-21 Merck & Co., Inc. Converting an alcohol to an azide with SN 2 inversion using a phosphoryl azide
US5441722A (en) * 1994-02-18 1995-08-15 Merck & Co., Inc. Short synthesis of 5,6-dihydro-(S)-4-(ethylamino)-(S)-6-[C3 H3 ]-4[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide and related non radioactive compounds
US5474919A (en) * 1994-09-13 1995-12-12 Merck & Co., Inc. Bioconversion process for the synthesis of transhydroxy sulfone by Rhodotorula rubra or Rhodotorula piliminae
US5760249A (en) * 1995-08-29 1998-06-02 Merck & Co., Inc. Synthesis of hydroxysulfone and related compounds

Also Published As

Publication number Publication date
US20030220509A1 (en) 2003-11-27
AU2001285958A1 (en) 2002-03-22
DE60103921D1 (de) 2004-07-22
CA2436185C (en) 2009-06-02
WO2002020529A1 (es) 2002-03-14
US7030250B2 (en) 2006-04-18
ES2223907T3 (es) 2005-03-01
JP2004508375A (ja) 2004-03-18
ATE269338T1 (de) 2004-07-15
EP1329453B1 (en) 2004-06-16
EP1329453A1 (en) 2003-07-23
DE60103921T2 (de) 2005-06-30
JP5137284B2 (ja) 2013-02-06
CA2436185A1 (en) 2002-03-14
ES2177415B1 (es) 2004-10-16
ES2177415A1 (es) 2002-12-01

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