ES8206443A1 - Un procedimiento para preparar un derivado de amidina - Google Patents
Un procedimiento para preparar un derivado de amidinaInfo
- Publication number
- ES8206443A1 ES8206443A1 ES505460A ES505460A ES8206443A1 ES 8206443 A1 ES8206443 A1 ES 8206443A1 ES 505460 A ES505460 A ES 505460A ES 505460 A ES505460 A ES 505460A ES 8206443 A1 ES8206443 A1 ES 8206443A1
- Authority
- ES
- Spain
- Prior art keywords
- formula
- producing same
- reaction
- amidine compounds
- complement agent
- 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.)
- Expired
Links
- 238000000034 method Methods 0.000 title abstract 2
- -1 amidine compounds Chemical class 0.000 title 1
- 230000002391 anti-complement effect Effects 0.000 title 1
- 108010008730 anticomplement Proteins 0.000 title 1
- 239000002253 acid Substances 0.000 abstract 2
- 238000006243 chemical reaction Methods 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 150000001409 amidines Chemical class 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 238000009833 condensation Methods 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 230000032050 esterification Effects 0.000 abstract 1
- 238000005886 esterification reaction Methods 0.000 abstract 1
- 239000003960 organic solvent Substances 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000002753 trypsin inhibitor Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C257/00—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
- C07C257/10—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
- C07C257/18—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
- C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
- C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
- C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
- C07D317/62—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to atoms of the carbocyclic ring
- C07D317/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
- C07C279/18—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to carbon atoms of six-membered aromatic rings
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Superconductors And Manufacturing Methods Therefor (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pyridine Compounds (AREA)
- Diaphragms For Electromechanical Transducers (AREA)
- Heat Treatment Of Sheet Steel (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Breeding Of Plants And Reproduction By Means Of Culturing (AREA)
- Power Steering Mechanism (AREA)
- Medicinal Preparation (AREA)
Abstract
PROCEDIMIENTO PARA LA OBTENCION DE DERIVADOS DE AMIDINA Y DE SUS SALES DE ADICION DE ACIDO, FISIOLOGICAMENTE COMPATIBLES, DE FORMULA (I), EN LA QUE Z, R1 Y R2 PUEDEN SER VARIOS TIPOS RADICALES. CONSISTEN EN LA REACCION DE ESTERIFICACION DE UN COMPUESTO DE FORMULA (II), EN LA QUE Z, R1 Y R2 TIENEN EL MISMO SIGNIFICADO QUE EN LA FORMULA (I), O UN DERIVADO REACTIVO DEL MISMO, CON 6-AMIDIN-2-NAFTOL O UNA SAL DE ADICION DE ACIDO DE ESTE. LA REACCION SE LLEVA A CABO EN UN DISOLVENTE ORGANICO INERTE, EN PRESENCIA DE UN AGENTE DE DESHIDRATACION-CONDENSACION, A UNA TEMPERATURA ENTRE -30 Y 80 C. ESTOS COMPUESTOS TIENEN APLICACIONES FARMACOLOGICAS POR SUS ACTIVIDADES ANTITRIPSINA, ANTIPLASMINA, ANTICALICREINA Y ANTITROMBINA.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP12826980A JPS5753454A (en) | 1980-09-16 | 1980-09-16 | Guanidinobenzoate and anticomplementary agent |
JP6494281A JPS57179146A (en) | 1981-04-28 | 1981-04-28 | Amidine compound |
Publications (2)
Publication Number | Publication Date |
---|---|
ES505460A0 ES505460A0 (es) | 1982-08-16 |
ES8206443A1 true ES8206443A1 (es) | 1982-08-16 |
Family
ID=26406084
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ES505460A Expired ES8206443A1 (es) | 1980-09-16 | 1981-09-14 | Un procedimiento para preparar un derivado de amidina |
Country Status (17)
Country | Link |
---|---|
US (2) | US4454338A (es) |
EP (1) | EP0048433B1 (es) |
KR (1) | KR860000264B1 (es) |
AT (1) | ATE20051T1 (es) |
AU (1) | AU527371B2 (es) |
CA (1) | CA1177488A (es) |
CS (1) | CS228534B2 (es) |
DD (1) | DD201779A5 (es) |
DE (1) | DE3174717D1 (es) |
DK (1) | DK155003C (es) |
ES (1) | ES8206443A1 (es) |
FI (1) | FI73975C (es) |
GB (1) | GB2083818B (es) |
HU (1) | HU185956B (es) |
NO (1) | NO153568C (es) |
PH (1) | PH18109A (es) |
SU (1) | SU1176832A3 (es) |
Families Citing this family (60)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU527371B2 (en) * | 1980-09-16 | 1983-03-03 | Torii & Co., Ltd. | Amidine |
FR2500825B1 (fr) * | 1981-02-27 | 1985-08-23 | Torii & Co Ltd | Nouveau carboxylate de 4-amidino-phenyle substitue, son procede de preparation et agent anti-complement en comprenant |
JPS57179147A (en) * | 1981-04-28 | 1982-11-04 | Torii Yakuhin Kk | Amidine derivative |
JPS59139357A (ja) * | 1983-01-28 | 1984-08-10 | Torii Yakuhin Kk | アミジン誘導体 |
US4818273A (en) * | 1983-11-14 | 1989-04-04 | The Dow Chemical Company | Substituted 1,2,4-triazolo[1,5-a]pyrimidine-2-sulfonamides, compositions containing them, and their utility as herbicides |
US4563527A (en) * | 1984-07-19 | 1986-01-07 | Torii & Co., Ltd. | Amidine compounds |
JPS6133173A (ja) * | 1984-07-25 | 1986-02-17 | Torii Yakuhin Kk | アミジン化合物 |
FR2568253B1 (fr) * | 1984-07-26 | 1987-01-30 | Torii Co | Nouvelle amidine |
GB2162171B (en) * | 1984-07-26 | 1988-01-27 | Torii & Co Ltd | Amidine compounds |
DE3427865A1 (de) * | 1984-07-27 | 1986-02-06 | Torii & Co., Tokio/Tokyo | Amidinoverbindungen, verfahren zu deren herstellung und diese verbindungen enthaltende pharmazeutische mittel |
US4709082A (en) * | 1984-10-25 | 1987-11-24 | Nissan Chemical Industries, Ltd. | 2-phenylpropionic acid esters, method for optical resolution thereof and optically active substance thereof |
AU584502B2 (en) * | 1987-03-30 | 1989-05-25 | Shosuke Okamoto | Phenylalanine derivatives and proteinase inhibitor |
US4990537A (en) * | 1988-07-11 | 1991-02-05 | Banyu Pharmaceutical Co., Ltd. | Anti influenza agent |
US5116985A (en) * | 1989-12-28 | 1992-05-26 | Snow Brand Milk Products Co., Ltd. | Isoquinoline derivatives and salts thereof |
ATE119523T1 (de) * | 1989-12-28 | 1995-03-15 | Snow Brand Milk Products Co Ltd | Isochinolinderivate und ihre salze als proteasehemmer. |
US5238964A (en) * | 1990-04-05 | 1993-08-24 | Torii & Co., Ltd. | Agent for treatment of cerebrovascular contraction |
JPH078789B2 (ja) * | 1990-04-05 | 1995-02-01 | 鳥居薬品株式会社 | 脳血管攣縮治療剤 |
DE4102024A1 (de) * | 1991-01-24 | 1992-07-30 | Thomae Gmbh Dr K | Biphenylderivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung |
ZA928276B (en) * | 1991-10-31 | 1993-05-06 | Daiichi Seiyaku Co | Aromatic amidine derivates and salts thereof. |
EP0703216B1 (en) * | 1994-09-20 | 1999-04-07 | Ono Pharmaceutical Co., Ltd. | Amidinophenol derivatives as protease inhibitors |
AU688628B2 (en) * | 1994-12-02 | 1998-03-12 | Yamanouchi Pharmaceutical Co., Ltd. | Novel amidinonaphthyl derivative or salt thereof |
DE69527854T2 (de) * | 1995-01-05 | 2003-03-27 | Torii Pharmaceutical Co., Ltd. | Derivate substituierter amidinonaphthylester |
US6388122B1 (en) | 1996-04-10 | 2002-05-14 | Ono Pharmaceutical Co., Ltd. | Tryptase inhibitor and novel guanidino derivatives |
AU7808198A (en) | 1997-06-03 | 1998-12-21 | Biocryst Pharmaceuticals, Inc. | Novel compounds useful in the complement, coagulat and kallikrein pathways and method for their preparation |
WO1999024407A1 (en) * | 1997-11-10 | 1999-05-20 | Array Biopharma, Inc. | Compounds which inhibit tryptase activity |
US6066673A (en) | 1998-03-12 | 2000-05-23 | The Procter & Gamble Company | Enzyme inhibitors |
NZ506202A (en) | 1998-03-19 | 2003-10-31 | Bristol Myers Squibb Co | Biphasic controlled release delivery system for high solubility pharmaceuticals and method |
EP1066272A4 (en) * | 1998-03-27 | 2002-03-13 | Biocryst Pharm Inc | NEW CONNECTIONS USEFUL IN THE COMPLEMENT, COAGULATE AND KALLIKREIN REACTION WAY AND METHOD FOR THEIR PRODUCTION |
EP1073624A1 (en) * | 1998-04-24 | 2001-02-07 | Proteus Molecular Design Limited | Aminomethyl-benzoic ester derivatives as tryptase inhibitors |
US6362216B1 (en) | 1998-10-27 | 2002-03-26 | Array Biopharma Inc. | Compounds which inhibit tryptase activity |
AR037097A1 (es) | 2001-10-05 | 2004-10-20 | Novartis Ag | Compuestos acilsulfonamidas, composiciones farmaceuticas y el uso de dichos compuestos para la preparacion de un medicamento |
JP2006096668A (ja) * | 2002-11-08 | 2006-04-13 | Ono Pharmaceut Co Ltd | エラスターゼ阻害剤と血液凝固系および/または線溶系酵素阻害剤との組み合わせからなる医薬 |
NZ540767A (en) * | 2002-11-27 | 2009-03-31 | Dmi Biosciences Inc | Treatment of diseases and conditions mediated by increased phosphorylation |
EP1663196A2 (en) * | 2003-09-25 | 2006-06-07 | DMI Biosciences, Inc. | Methods and products which utilize n-acyl-l-aspartic acid |
EP2143431A1 (en) * | 2005-05-17 | 2010-01-13 | Santen Pharmaceutical Co., Ltd. | Protective agent for neurocyte comprising amidino derivative as active ingredient |
US20090253765A1 (en) * | 2005-05-17 | 2009-10-08 | Santen Pharmaceutical Co., Ltd. | Angiogenesis Inhibitor Containing Amine Derivative as Active Ingredient |
GB2445920A (en) * | 2007-01-25 | 2008-07-30 | Mucokinetica Ltd | Amidino compounds for treatment of respiratory disease |
WO2010005087A1 (ja) * | 2008-07-11 | 2010-01-14 | 味の素株式会社 | アミジン誘導体 |
JP5706825B2 (ja) | 2008-10-17 | 2015-04-22 | シグネーチャー セラピューティクス, インク.Signature Therapeutics, Inc. | フェノール性オピオイドの放出が減弱された医薬組成物 |
CA2773340C (en) | 2009-09-08 | 2019-07-23 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof |
US9238020B2 (en) | 2010-04-21 | 2016-01-19 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable phenol-modified tapentadol prodrug |
US20110262355A1 (en) | 2010-04-21 | 2011-10-27 | Jenkins Thomas E | Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof |
EP2560486B1 (en) | 2010-04-21 | 2018-11-21 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable amphetamine prodrugs and inhibitors thereof |
CN107080846A (zh) | 2010-07-09 | 2017-08-22 | 詹姆斯.特林卡.格林 | 用于包括瑞格列净的短半衰期药物的组合立即/延迟释放递送系统 |
RU2609412C2 (ru) | 2011-01-11 | 2017-02-01 | Сигничер Терапьютикс, Инк. | Композиции, содержащие расщепляемое ферментами пролекарство оксикодона |
WO2012096886A1 (en) | 2011-01-11 | 2012-07-19 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable oxycodone prodrug |
US8685916B2 (en) | 2011-03-09 | 2014-04-01 | Signature Therapeutics, Inc. | Opioid prodrugs with heterocyclic linkers |
CA2827662C (en) | 2011-03-09 | 2020-07-14 | Signature Therapeutics, Inc. | Active agent prodrugs with heterocyclic linkers |
AU2012309438A1 (en) | 2011-09-15 | 2014-03-27 | Astellas Pharma Inc. | Guanidinobenzoic acid compound |
CN103012214A (zh) * | 2011-09-28 | 2013-04-03 | 南京长澳医药科技有限公司 | 一种萘莫司他盐酸盐及萘莫司他甲磺酸盐的制备方法 |
CA2905606C (en) * | 2013-03-13 | 2021-03-09 | Astellas Pharma Inc. | Guanidino benzoic acid esters useful in treating renal disorders |
CN103641749B (zh) * | 2013-12-02 | 2016-02-10 | 山东永泰化工有限公司 | 一种甲磺酸萘莫司他的制备方法 |
US9428470B2 (en) | 2014-02-13 | 2016-08-30 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
US9346776B2 (en) | 2014-02-13 | 2016-05-24 | Takeda Pharmaceutical Company Limited | Fused heterocyclic compound |
CN110330447B (zh) * | 2019-07-16 | 2022-04-15 | 北京赛升药业股份有限公司 | 一种甲磺酸萘莫司他中间体的制备方法及其应用 |
CN111803483B (zh) * | 2020-01-21 | 2021-04-06 | 中国人民解放军军事科学院军事医学研究院 | 苯甲酸酯类化合物在治疗SARS-CoV-2感染方面的应用 |
WO2021209563A1 (en) | 2020-04-16 | 2021-10-21 | Som Innovation Biotech, S.A. | Compounds for use in the treatment of viral infections by respiratory syndrome-related coronavirus |
CN111574409A (zh) * | 2020-05-14 | 2020-08-25 | 河北省医疗器械与药品包装材料检验研究院(河北省医疗器械技术审评中心) | 一种甲磺酸萘莫司他的重结晶工艺方法 |
CN113999145B (zh) * | 2021-11-12 | 2023-02-03 | 开封明仁药业有限公司 | 一种甲磺酸萘莫司他的合成方法 |
WO2023118896A1 (en) | 2021-12-23 | 2023-06-29 | Subintro Limited | Novel antiviral compositions comprising oleic acid |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DD89611A (es) * | ||||
DE1905813A1 (de) * | 1968-07-04 | 1970-03-05 | Akad Wissenschaften Ddr | 3- oder 4-Guanidobenzoesaeurebenzyl- oder -phenylestern und deren Verwendung als Inhibitoren |
GB1472700A (en) * | 1974-11-01 | 1977-05-04 | Ono Pharmaceutical Co | Guanidinobehzoic acid derivatives and process for preparing the same |
AU527371B2 (en) * | 1980-09-16 | 1983-03-03 | Torii & Co., Ltd. | Amidine |
-
1981
- 1981-09-08 AU AU75062/81A patent/AU527371B2/en not_active Expired
- 1981-09-09 US US06/300,534 patent/US4454338A/en not_active Expired - Lifetime
- 1981-09-10 CA CA000385570A patent/CA1177488A/en not_active Expired
- 1981-09-14 ES ES505460A patent/ES8206443A1/es not_active Expired
- 1981-09-15 FI FI812876A patent/FI73975C/fi not_active IP Right Cessation
- 1981-09-15 GB GB8127837A patent/GB2083818B/en not_active Expired
- 1981-09-15 PH PH26206A patent/PH18109A/en unknown
- 1981-09-15 HU HU812665A patent/HU185956B/hu unknown
- 1981-09-15 CS CS816809A patent/CS228534B2/cs unknown
- 1981-09-15 EP EP81107274A patent/EP0048433B1/en not_active Expired
- 1981-09-15 DE DE8181107274T patent/DE3174717D1/de not_active Expired
- 1981-09-15 DK DK410681A patent/DK155003C/da not_active IP Right Cessation
- 1981-09-15 KR KR1019810003427A patent/KR860000264B1/ko not_active Expired
- 1981-09-15 NO NO813138A patent/NO153568C/no unknown
- 1981-09-15 SU SU813384251A patent/SU1176832A3/ru active
- 1981-09-15 AT AT81107274T patent/ATE20051T1/de not_active IP Right Cessation
- 1981-09-16 DD DD81233339A patent/DD201779A5/de not_active IP Right Cessation
-
1984
- 1984-01-20 US US06/572,269 patent/US4532255A/en not_active Expired - Lifetime
Also Published As
Publication number | Publication date |
---|---|
EP0048433A3 (en) | 1982-07-21 |
FI73975C (fi) | 1987-12-10 |
NO153568C (no) | 1986-05-21 |
NO153568B (no) | 1986-01-06 |
US4454338A (en) | 1984-06-12 |
NO813138L (no) | 1982-03-17 |
AU527371B2 (en) | 1983-03-03 |
ATE20051T1 (de) | 1986-06-15 |
DK410681A (da) | 1982-03-17 |
DD201779A5 (de) | 1983-08-10 |
EP0048433A2 (en) | 1982-03-31 |
DK155003B (da) | 1989-01-23 |
CS228534B2 (en) | 1984-05-14 |
FI812876L (fi) | 1982-03-17 |
AU7506281A (en) | 1982-03-25 |
SU1176832A3 (ru) | 1985-08-30 |
ES505460A0 (es) | 1982-08-16 |
FI73975B (fi) | 1987-08-31 |
CA1177488A (en) | 1984-11-06 |
GB2083818A (en) | 1982-03-31 |
PH18109A (en) | 1985-03-22 |
DE3174717D1 (en) | 1986-07-03 |
DK155003C (da) | 1989-05-29 |
EP0048433B1 (en) | 1986-05-28 |
GB2083818B (en) | 1984-05-10 |
US4532255A (en) | 1985-07-30 |
KR830007527A (ko) | 1983-10-21 |
KR860000264B1 (ko) | 1986-03-22 |
HU185956B (en) | 1985-04-28 |
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