RU98120256A - DERIVATIVES OF BENZAZEPINONE-N-ACETIC ACID, SUBSTITUTED BY PHOSPHIC ACID, METHOD FOR PRODUCING THEM AND MEDICINES CONTAINING THESE COMPOUNDS - Google Patents
DERIVATIVES OF BENZAZEPINONE-N-ACETIC ACID, SUBSTITUTED BY PHOSPHIC ACID, METHOD FOR PRODUCING THEM AND MEDICINES CONTAINING THESE COMPOUNDSInfo
- Publication number
- RU98120256A RU98120256A RU98120256/04A RU98120256A RU98120256A RU 98120256 A RU98120256 A RU 98120256A RU 98120256/04 A RU98120256/04 A RU 98120256/04A RU 98120256 A RU98120256 A RU 98120256A RU 98120256 A RU98120256 A RU 98120256A
- Authority
- RU
- Russia
- Prior art keywords
- biolabile
- phosphonic acid
- compounds
- formula
- general formula
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title claims 11
- 239000002253 acid Substances 0.000 title claims 6
- QTBSBXVTEAMEQO-UHFFFAOYSA-N acetic acid Substances CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 title claims 3
- 239000003814 drug Substances 0.000 title claims 2
- 238000004519 manufacturing process Methods 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 239000001257 hydrogen Substances 0.000 claims 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- ABLZXFCXXLZCGV-UHFFFAOYSA-N phosphonic acid group Chemical group P(O)(O)=O ABLZXFCXXLZCGV-UHFFFAOYSA-N 0.000 claims 6
- 150000003008 phosphonic acid esters Chemical class 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 4
- 239000011780 sodium chloride Substances 0.000 claims 4
- 150000007513 acids Chemical class 0.000 claims 2
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 2
- 150000001733 carboxylic acid esters Chemical class 0.000 claims 2
- 150000002148 esters Chemical class 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000006244 carboxylic acid protecting group Chemical group 0.000 claims 1
- 230000000875 corresponding Effects 0.000 claims 1
- 229940079593 drugs Drugs 0.000 claims 1
- 125000004185 ester group Chemical group 0.000 claims 1
- 238000005886 esterification reaction Methods 0.000 claims 1
- 125000001033 ether group Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- TUJKJAMUKRIRHC-UHFFFAOYSA-N hydroxyl radical Chemical compound [OH] TUJKJAMUKRIRHC-UHFFFAOYSA-N 0.000 claims 1
- 230000003993 interaction Effects 0.000 claims 1
- 230000000144 pharmacologic effect Effects 0.000 claims 1
- 230000001681 protective Effects 0.000 claims 1
Claims (4)
где R1 означает водород или группу, образующую биолабильный сложный эфир фосфоновой кислоты;
R2 означает водород иди группу, образующую биолабильный сложный эфир фосфоновой кислоты;
R3 означает водород или группу, образующую биолабильный сложный эфир карбоновой кислоты,
и физиологически приемлемые соли кислот формулы I.1. Derivatives of benzazepinone-N-acetic acid substituted with phosphonic acid of the general formula I:
where R 1 means hydrogen or a group forming a biolabile phosphonic acid ester;
R 2 means hydrogen or a group forming a biolabile phosphonic acid ester;
R 3 means hydrogen or a group forming a biolabile carboxylic acid ester,
and physiologically acceptable acid salts of formula I.
где R1 означает водород или группу, образующую биолабильный сложный эфир фосфоновой кислоты;
R2 означает водород иди группу, образующую биолабильный сложный эфир фосфоновой кислоты;
R3 означает водород или группу, образующую биолабильный сложный эфир карбоновой кислоты,
и физиологически приемлемых солей кислот формулы I, отличающийся там, что
а) для получения соединений общей формулы IV:
где R101 и R201, независимо друг от друга, означают водород или защитную группу фосфоновой кислоты, R302 означает защитную группу карбоновой кислоты,
соединения общей формулы II:
где R101 и R201 имеют приведенные выше значения,
вводят во взаимодействие с соединениями общей формулы III:
где R302 имеет указанное выше значение,
и в случае, если R101 и/или R201 означают водород, свободную функцию (свободные функции) фосфоновой кислоты, при необходимости, путем этерификации с соединением общей формулы Va и/или Vb,
R110-Y (Va), R210-Y (Vb),
где R110 и R201 обозначают соответственно группу, образующую биолабильный сложный эфир фосфоновой кислоты, Y означает гидроксильный радикал или отщепляемую летучую группу, переводят
в биолабильные эфирные группы фосфоновой кислоты,
б) если в соединениях формулы IV защитные группы R110, R201 и/или R302 не являются желаемыми группами, образующими биолабильный сложный эфир, то их отщепляют одновременно или в отдельности друг за другом в любой последовательности
и, при желании, переводят соответствующие высвободившиеся кислотные функции в биолабильные эфирные группы, этерифицируя при этом свободные функции фосфоновой кислоты с соединением формулы Va или Vb и/или свободные функции карбоновой кислоты с соединением общей формулы Vc:
R310-Y
где R310 означает группу, образующую биолабильный сложный эфир карбоновой кислоты, Y имеет указанное выше значение,
и, при необходимости, кислоты формулы I переводят в их физиологически приемлемые соли или соли кислот формулы I - в свободные соединения.4. A method of obtaining derivatives of benzazepinone-N-acetic acid substituted by phosphonic acid of the General formula:
where R 1 means hydrogen or a group forming a biolabile phosphonic acid ester;
R 2 means hydrogen or a group forming a biolabile phosphonic acid ester;
R 3 means hydrogen or a group forming a biolabile carboxylic acid ester,
and physiologically acceptable acid salts of the formula I, characterized therein that
a) to obtain compounds of General formula IV:
where R 101 and R 201 , independently of one another, are hydrogen or a phosphonic acid protecting group, R 302 is a carboxylic acid protecting group,
compounds of General formula II:
where R 101 and R 201 have the above meanings,
enter into interaction with compounds of General formula III:
where R 302 has the above meaning,
and if R 101 and / or R 201 mean hydrogen, the free function (free functions) of phosphonic acid, if necessary, by esterification with a compound of the general formula Va and / or Vb,
R 110 -Y (Va), R 210 -Y (Vb),
where R 110 and R 201 respectively denote a group forming a biolabile phosphonic acid ester, Y means a hydroxyl radical or a leaving volatile group,
into biolabile ester groups of phosphonic acid,
b) if in the compounds of formula IV the protective groups R 110 , R 201 and / or R 302 are not the desired groups forming a biolabile ester, then they are cleaved simultaneously or separately one after another in any sequence
and, if desired, translate the corresponding liberated acid functions into biolabile ether groups, esterifying the free functions of phosphonic acid with a compound of formula Va or Vb and / or the free functions of carboxylic acid with a compound of general formula Vc:
R 310 -Y
where R 310 means a group forming a biolabile ester of a carboxylic acid, Y has the above meaning,
and, if necessary, the acids of the formula I are converted into their physiologically acceptable salts or the salts of the acids of the formula I into free compounds.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19750002.1 | 1997-11-12 | ||
| DE19750002A DE19750002A1 (en) | 1997-11-12 | 1997-11-12 | Phosphonic acid-substituted benzazepinone-N-acetic acid derivatives and processes for their preparation and pharmaceuticals containing these compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU98120256A true RU98120256A (en) | 2000-09-10 |
| RU2211219C2 RU2211219C2 (en) | 2003-08-27 |
Family
ID=7848410
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU98120256/04A RU2211219C2 (en) | 1997-11-12 | 1998-11-11 | Derivatives of benzazepinon-n-acetic acid substituted with phosphonic acid, method for their preparing and medicinal agents containing these compounds |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US5952327A (en) |
| EP (1) | EP0916679B1 (en) |
| JP (1) | JP4162780B2 (en) |
| KR (1) | KR19990045100A (en) |
| CN (1) | CN1187361C (en) |
| AR (1) | AR009911A1 (en) |
| AT (1) | ATE228144T1 (en) |
| AU (1) | AU746907B2 (en) |
| BR (1) | BR9804582A (en) |
| CA (1) | CA2253997C (en) |
| CZ (1) | CZ296123B6 (en) |
| DE (2) | DE19750002A1 (en) |
| DK (1) | DK0916679T3 (en) |
| DZ (1) | DZ2652A1 (en) |
| ES (1) | ES2186961T3 (en) |
| HK (1) | HK1019338A1 (en) |
| HU (1) | HU221177B1 (en) |
| ID (1) | ID21393A (en) |
| IL (1) | IL126984A (en) |
| NO (1) | NO317640B1 (en) |
| NZ (1) | NZ332744A (en) |
| PL (1) | PL191436B1 (en) |
| PT (1) | PT916679E (en) |
| RU (1) | RU2211219C2 (en) |
| SK (1) | SK283233B6 (en) |
| TR (1) | TR199802289A3 (en) |
| UA (1) | UA60304C2 (en) |
| ZA (1) | ZA9810316B (en) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1520299A (en) * | 2001-05-18 | 2004-08-11 | ������ҩ������˾ | Use of compounds with combined NEP/MP-inbihitory activity in prepan. of medicaments |
| IL162645A0 (en) * | 2002-01-16 | 2005-11-20 | Solvay Pharm Bv | solid salts benzazepine compounds and their use inthe preparation of pharmaceuticals compounds |
| CL2004000544A1 (en) * | 2003-03-18 | 2005-01-28 | Pharmacia Corp Sa Organizada B | USE OF A PHARMACEUTICAL COMBINATION, OF AN ALGOSTERONE RECEIVER ANTAGONIST AND A NEUTRAL ENDOPEPTIDASE INHIBITOR, USEFUL FOR THE TREATMENT AND PREVENTION OF A PATHOLOGICAL CONDITION RELATED TO HYPERTENSION, RENAL DYSFUNCTION, INSULINOPATI |
| SA04250283B1 (en) * | 2003-09-26 | 2008-05-26 | سولفاي فارماسيتيكالز جي أم بي أتش | Derivatives of amidomethy1-substituted1-(carboxyalkyl)-cyclopentylcarbonylamino-benzazepine-N-acetic acid |
| US7262184B2 (en) * | 2003-09-26 | 2007-08-28 | Solvay Pharmaceuticals Gmbh | Amidomethyl-substituted 1-(carboxyalkyl) cyclopentyl-carbonylamino-benzazepine-N-acetic acid compounds, process and intermediate products for their preparation and pharmaceutical compositions containing them |
| US7427611B2 (en) * | 2003-09-26 | 2008-09-23 | Solvay Pharmaceuticals Gmbh | Amidomethyl-substituted 1-(carboxyalkyl)-cyclopentyl-carbonylamino-benzazepine-N-acetic acid compounds, process and intermediate products for their preparation and pharmaceutical compositions containing them |
| US7452875B2 (en) | 2003-09-26 | 2008-11-18 | Solvay Pharmaceuticals Gmbh | Amidomethyl-substituted 1-(carboxyalkyl) cyclopentyl-carbonylamino-benzazepine-N-acetic acid compounds, process and intermediate products for their preparation and pharmaceutical compositions containing them |
| US7232813B2 (en) * | 2004-01-12 | 2007-06-19 | Solvay Pharmaceuticals B.V. | Neutral endopeptidase (NEP) and human soluble endopeptidase (hSEP) inhibitors for prophylaxis and treatment of neuro-degenerative disorders |
| DE602005009487D1 (en) * | 2004-01-12 | 2008-10-16 | Solvay Pharm Bv | NEUTRAL ENDOPEPTIDASE (NEP) AND HUMAN SOLUBLE ENDOPEPTIDASE (HSEP) INHIBITORS FOR PROPHYLAXIS AND TREATMENT OF NEURODEEGENERATIVE ILLNESSES |
| US20050267072A1 (en) * | 2004-05-14 | 2005-12-01 | Solvay Pharmaceuticals Gmbh | Pharmaceutical compositions containing dually acting inhibitors of neutral endopeptidase for the treatment of sexual dysfunction |
| US20050267124A1 (en) * | 2004-05-14 | 2005-12-01 | Solvay Pharmaceuticals Gmbh | Pharmaceutical compositions comprising NEP-inhibitors, inhibitors of the endogenous producing system and PDEV inhibiitors |
| US20050288272A1 (en) * | 2004-06-23 | 2005-12-29 | Solvay Pharmaceuticals Gmbh | Pharmaceutical compositions comprising NEP-inhibitors, inhibitors of the endogenous endothelin producing system and AT1 receptor antagonists |
| BRPI0519919A2 (en) | 2004-12-15 | 2009-04-07 | Solvay Pharm Gmbh | pharmaceutical compositions comprising nep inhibitors, endogenous endothelin production system inhibitors and hmg coa reductase inhibitors |
| US20060205625A1 (en) * | 2005-02-18 | 2006-09-14 | Solvay Pharmaceuticals Gmbh | Pharmaceutical compositions comprising NEP-inhibitors, inhibitors of the endogenous endothelin producing system and diuretics |
| WO2007102171A2 (en) * | 2006-03-07 | 2007-09-13 | Panacea Biotec Ltd | Novel salts of 1h-1-benzazepine-1-acetic acid, their preparation and pharmaceutical composition |
| US8198341B2 (en) | 2008-12-18 | 2012-06-12 | Icl-Ip America Inc. | Method of making hydroxymethylphosphonate, polyurethane foam-forming compositions, polyurethane foam and articles made therefrom |
| US9441001B2 (en) | 2012-10-17 | 2016-09-13 | Icl-Ip America Inc. | Method of making hydroxymethylphosphonate, polyurethane foam-forming compositions, polyurethane foam and articles made therefrom |
| US9523195B2 (en) | 2014-06-09 | 2016-12-20 | Johns Manville | Wall insulation boards with non-halogenated fire retardant and insulated wall systems |
| US9815256B2 (en) | 2014-06-09 | 2017-11-14 | Johns Manville | Foam boards including non-halogenated fire retardants |
| US9528269B2 (en) | 2014-06-09 | 2016-12-27 | Johns Manville | Roofing systems and roofing boards with non-halogenated fire retardant |
| US9815966B2 (en) | 2014-07-18 | 2017-11-14 | Johns Manville | Spray foams containing non-halogenated fire retardants |
| CN107383084A (en) * | 2017-06-14 | 2017-11-24 | 浙江嘉华化工有限公司 | A kind of preparation method of 0 ethyl phosphonic acid sodium |
| PL424453A1 (en) * | 2018-01-31 | 2019-08-12 | Forty-Four Pharmaceuticals Spółka Z Ograniczoną Odpowiedzialnością | Methods for reducing harmful effect of the perenchymatous organs perfusion deficiency by the inhibitors of neutral endopeptidase (NEP) and human endopeptidase (hSEP) |
| PL424452A1 (en) * | 2018-01-31 | 2019-08-12 | Forty-Four Pharmaceuticals Spółka Z Ograniczoną Odpowiedzialnością | Inhibitors of inactive endopeptidase (NEP) and human soluble endopeptidase (hSEP) for prevention and treatment of eye diseases |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19510566A1 (en) * | 1995-03-23 | 1996-09-26 | Kali Chemie Pharma Gmbh | Benzazepine, benzoxazepine and benzothiazepine N-acetic acid derivatives and process for their preparation and medicaments containing these compounds |
| US5877313A (en) * | 1995-05-17 | 1999-03-02 | Bristol-Myers Squibb | Benzo-fused azepinone and piperidinone compounds useful in the inhibition of ACE and NEP |
| US5635504A (en) * | 1995-06-07 | 1997-06-03 | Bristol-Myers Squibb Co. | Diazepine containing dual action inhibitors |
-
1997
- 1997-11-12 DE DE19750002A patent/DE19750002A1/en not_active Withdrawn
-
1998
- 1998-10-21 AR ARP980105254A patent/AR009911A1/en unknown
- 1998-11-02 HU HU9802517A patent/HU221177B1/en not_active IP Right Cessation
- 1998-11-04 PT PT98120898T patent/PT916679E/en unknown
- 1998-11-04 DK DK98120898T patent/DK0916679T3/en active
- 1998-11-04 EP EP98120898A patent/EP0916679B1/en not_active Expired - Lifetime
- 1998-11-04 AT AT98120898T patent/ATE228144T1/en not_active IP Right Cessation
- 1998-11-04 DE DE59806345T patent/DE59806345D1/en not_active Expired - Lifetime
- 1998-11-04 CZ CZ0356298A patent/CZ296123B6/en not_active IP Right Cessation
- 1998-11-04 ES ES98120898T patent/ES2186961T3/en not_active Expired - Lifetime
- 1998-11-05 SK SK1516-98A patent/SK283233B6/en unknown
- 1998-11-07 KR KR1019980047652A patent/KR19990045100A/en not_active Application Discontinuation
- 1998-11-10 JP JP31913198A patent/JP4162780B2/en not_active Expired - Fee Related
- 1998-11-10 CN CNB981241433A patent/CN1187361C/en not_active Expired - Fee Related
- 1998-11-10 PL PL329635A patent/PL191436B1/en not_active IP Right Cessation
- 1998-11-10 IL IL12698498A patent/IL126984A/en not_active IP Right Cessation
- 1998-11-11 DZ DZ980262A patent/DZ2652A1/en active
- 1998-11-11 AU AU92344/98A patent/AU746907B2/en not_active Ceased
- 1998-11-11 ZA ZA9810316A patent/ZA9810316B/en unknown
- 1998-11-11 NO NO19985262A patent/NO317640B1/en not_active IP Right Cessation
- 1998-11-11 RU RU98120256/04A patent/RU2211219C2/en not_active IP Right Cessation
- 1998-11-11 BR BR9804582-2A patent/BR9804582A/en not_active IP Right Cessation
- 1998-11-11 TR TR1998/02289A patent/TR199802289A3/en unknown
- 1998-11-11 NZ NZ332744A patent/NZ332744A/en unknown
- 1998-11-12 CA CA002253997A patent/CA2253997C/en not_active Expired - Fee Related
- 1998-11-12 US US09/189,796 patent/US5952327A/en not_active Expired - Lifetime
- 1998-11-12 UA UA98116012A patent/UA60304C2/en unknown
- 1998-11-12 ID IDP981485A patent/ID21393A/en unknown
-
1999
- 1999-10-08 HK HK99104433A patent/HK1019338A1/en not_active IP Right Cessation
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