DE2942781A1 - Phosphinylalkanoylproline, verfahren zu ihrer herstellung und ihre verwendung als hypotensive wirkstoffe - Google Patents

Phosphinylalkanoylproline, verfahren zu ihrer herstellung und ihre verwendung als hypotensive wirkstoffe

Info

Publication number
DE2942781A1
DE2942781A1 DE19792942781 DE2942781A DE2942781A1 DE 2942781 A1 DE2942781 A1 DE 2942781A1 DE 19792942781 DE19792942781 DE 19792942781 DE 2942781 A DE2942781 A DE 2942781A DE 2942781 A1 DE2942781 A1 DE 2942781A1
Authority
DE
Germany
Prior art keywords
hydrogen atom
group
compound according
represent
general formula
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.)
Ceased
Application number
DE19792942781
Other languages
German (de)
English (en)
Inventor
Jun Edward W Petrillo
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
ER Squibb and Sons LLC
Original Assignee
ER Squibb and Sons LLC
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 ER Squibb and Sons LLC filed Critical ER Squibb and Sons LLC
Publication of DE2942781A1 publication Critical patent/DE2942781A1/de
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6571—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
    • C07F9/657163—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms the ring phosphorus atom being bound to at least one carbon atom
    • C07F9/657172—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms the ring phosphorus atom being bound to at least one carbon atom the ring phosphorus atom and one oxygen atom being part of a (thio)phosphinic acid ester: (X = O, S)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/30—Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
    • C07F9/301—Acyclic saturated acids which can have further substituents on alkyl
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/30—Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
    • C07F9/304—Aromatic acids (P-C aromatic linkage)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/30—Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
    • C07F9/306—Arylalkanephosphinic acids, e.g. Ar-(CH2)n-P(=X)(R)(XH), (X = O,S, Se; n>=1)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/30—Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
    • C07F9/32—Esters thereof
    • C07F9/3205—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/3229—Esters of aromatic acids (P-C aromatic linkage)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/30—Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
    • C07F9/32—Esters thereof
    • C07F9/3205—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/3241—Esters of arylalkanephosphinic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/30—Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
    • C07F9/32—Esters thereof
    • C07F9/3258—Esters thereof the ester moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/3288—Esters with arylalkanols
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/30—Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
    • C07F9/34—Halides thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/48—Phosphonous acids [RP(OH)2] including [RHP(=O)(OH)]; Thiophosphonous acids including [RP(SH)2], [RHP(=S)(SH)]; Derivatives thereof
    • C07F9/4808—Phosphonous acids [RP(OH)2] including [RHP(=O)(OH)]; Thiophosphonous acids including [RP(SH)2], [RHP(=S)(SH)]; Derivatives thereof the acid moiety containing a substituent or structure which is considered as characteristic
    • C07F9/4816—Acyclic saturated acids or derivatices which can have further substituents on alkyl
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/48—Phosphonous acids [RP(OH)2] including [RHP(=O)(OH)]; Thiophosphonous acids including [RP(SH)2], [RHP(=S)(SH)]; Derivatives thereof
    • C07F9/4891—Monohalide derivatives RP (XR') (Hal) (X = O, S, N)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/572—Five-membered rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cardiology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
DE19792942781 1978-10-23 1979-10-23 Phosphinylalkanoylproline, verfahren zu ihrer herstellung und ihre verwendung als hypotensive wirkstoffe Ceased DE2942781A1 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US05/953,711 US4168267A (en) 1978-10-23 1978-10-23 Phosphinylalkanoyl prolines

Publications (1)

Publication Number Publication Date
DE2942781A1 true DE2942781A1 (de) 1980-04-30

Family

ID=25494430

Family Applications (1)

Application Number Title Priority Date Filing Date
DE19792942781 Ceased DE2942781A1 (de) 1978-10-23 1979-10-23 Phosphinylalkanoylproline, verfahren zu ihrer herstellung und ihre verwendung als hypotensive wirkstoffe

Country Status (18)

Country Link
US (1) US4168267A (US06650917-20031118-M00005.png)
JP (1) JPS5557597A (US06650917-20031118-M00005.png)
AU (1) AU529134B2 (US06650917-20031118-M00005.png)
BE (1) BE879586A (US06650917-20031118-M00005.png)
CA (1) CA1133496A (US06650917-20031118-M00005.png)
CH (1) CH645382A5 (US06650917-20031118-M00005.png)
DE (1) DE2942781A1 (US06650917-20031118-M00005.png)
DK (1) DK148141C (US06650917-20031118-M00005.png)
FR (1) FR2439790A1 (US06650917-20031118-M00005.png)
GB (1) GB2031897B (US06650917-20031118-M00005.png)
IE (1) IE49020B1 (US06650917-20031118-M00005.png)
IT (1) IT1125558B (US06650917-20031118-M00005.png)
LU (1) LU81809A1 (US06650917-20031118-M00005.png)
NL (1) NL7907568A (US06650917-20031118-M00005.png)
PH (1) PH13931A (US06650917-20031118-M00005.png)
SE (1) SE7908727L (US06650917-20031118-M00005.png)
SU (1) SU988194A3 (US06650917-20031118-M00005.png)
ZA (1) ZA795048B (US06650917-20031118-M00005.png)

Cited By (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2525607A1 (fr) * 1982-04-22 1983-10-28 Squibb & Sons Inc Phosphinylmethylaminocarbonyl imino acides a action anti-hypertensive
WO2010063342A1 (de) * 2008-12-02 2010-06-10 Clariant International Ltd Verfahren zur herstellung von mono-carboxyfunktionalisierten dialkylphosphinsäuren, -estern und -salzen mittels vinylester einer carbonsäure und ihre verwendung
WO2010063344A1 (de) * 2008-12-04 2010-06-10 Clariant International Ltd Verfahren zur herstellung von mono-carboxyfunktionalisierten dialkylphosphinsäuren, -estern und -salzen mittels vinylether und ihre verwendung
WO2010069416A1 (de) * 2008-12-18 2010-06-24 Clariant International Ltd Verfahren zur herstellung von mono-carboxyfunktionalisierten dialkylphosphinsäuren, -estern und -salzen mittels alkylenoxiden und ihre verwendung
US8592505B2 (en) 2008-12-19 2013-11-26 Clariant Finance (Bvi) Limited Hydrophosphorylation of phosphonous acid derivatives for flame retardants
US8604232B2 (en) 2008-11-07 2013-12-10 Clariant Finance (Bvi) Limited Method for producing monoamino-functionalised dialkylphosphinite acids esters and salts and use thereof
US8604108B2 (en) 2008-11-05 2013-12-10 Clariant Finance (Bvi) Limited Method for producing mono-hydroxyfunctionalized dialkylphosphinic acids and esters and salts thereof by means of acroleins and use thereof
US8614267B2 (en) 2008-11-05 2013-12-24 Clariant Finance (Bvi) Limited Method for producing mono-hydroxyfunctionalized dialkylphosphinic acids and esters and salts thereof by means of allyl alcohols and use thereof
US8664418B2 (en) 2008-11-07 2014-03-04 Clariant Finance (Bvi) Limited Method for producing dialkylphosphinic acids and esters and salts thereof by means of acrylic acid derivatives and use thereof
US8735477B2 (en) 2008-11-07 2014-05-27 Clariant Finance (Bvi) Limited Method for producing dialkylphosphinic acids and esters and salts thereof by means of acrylnitriles and use thereof
US8772519B2 (en) 2008-11-11 2014-07-08 Clariant Finance (Bvi) Limited Process for preparing mono-allyl-functionalized dialkylphosphinic acids, salts and esters thereof with allylic compounds, and the use thereof
US8987490B2 (en) 2008-12-18 2015-03-24 Clariant Finance (Bvi) Limited Method for the production of monohydroxy-functionalized dialkylphosphinic acids, esters, and salts using ethylene oxide, and use thereof
US9018413B2 (en) 2008-12-18 2015-04-28 Clariant Finance (Bvi) Limited Method for the production of alkylphosphonic acids, esters, and salts by oxidizing alkylphosphonous acids, and use thereof
US9035088B2 (en) 2008-11-07 2015-05-19 Clariant Finance (Bvi) Limited Method for producing mono-aminofunctionalized dialkylphosphinic acids and esters and salts thereof by means of acrylnitriles and use thereof
US9068119B2 (en) 2008-12-02 2015-06-30 Clariant Finance (Bvi) Limited Method for producing mono-hydroxy-functionalized dialkylphosphinic acids, esters and salts using a vinyl ester of a carobxylic acid and the use thereof
US9139714B2 (en) 2008-11-05 2015-09-22 Clariant Finance (Bvi) Limited Method for producing dialkylphosphinic acids and esters and salts thereof by means of allyl alcohols-acroleins and use thereof
US9181487B2 (en) 2008-12-18 2015-11-10 Clariant Finance (Bvi) Limited Process for preparing ethylenedialkylphosphinic acids, esters and salts by means of acetylene and use thereof
US9279085B2 (en) 2008-12-19 2016-03-08 Clariant Finance (Bvi) Limited Method for the production of monofunctionalized dialkylphosphinic acids, esters and salts, and use thereof

Families Citing this family (101)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6458772B1 (en) 1909-10-07 2002-10-01 Medivir Ab Prodrugs
US4690940A (en) * 1979-08-14 1987-09-01 University Of Miami Anti-hypertensive agents
US4698355A (en) * 1979-08-14 1987-10-06 University Of Miami Anti-hypertensive agents
ZA794723B (en) * 1978-09-11 1980-08-27 Univ Miami Anti-hypertensive agents
US4690939A (en) * 1979-08-14 1987-09-01 University Of Miami Anti-hypertensive agents
US4690938A (en) * 1979-08-14 1987-09-01 University Of Miami Anti-hypertensive agents
US4698356A (en) * 1979-08-14 1987-10-06 University Of Miami Anti-hypertensive agents
US4690937A (en) * 1979-08-14 1987-09-01 University Of Miami Anti-hypertensive agents
US4695577A (en) * 1979-08-14 1987-09-22 University Of Miami Anti-hypertensive agents
US4168267A (en) * 1978-10-23 1979-09-18 E. R. Squibb & Sons, Inc. Phosphinylalkanoyl prolines
US4734420A (en) * 1980-03-05 1988-03-29 University Of Miami Anti-hypertensive agents
US4690936A (en) * 1980-03-05 1987-09-01 University Of Miami Anti-hypertensive agents
US4312809A (en) * 1980-10-31 1982-01-26 E. R. Squibb & Sons, Inc. Lactam derivatives of mercaptoacylamino acids
US4337201A (en) * 1980-12-04 1982-06-29 E. R. Squibb & Sons, Inc. Phosphinylalkanoyl substituted prolines
US4384123A (en) * 1980-12-04 1983-05-17 E. R. Squibb & Sons, Inc. Phosphinylalkanoyl substituted prolines
US4379146A (en) * 1981-02-17 1983-04-05 Merck & Co., Inc. Substituted phosphonamides as antihypertensives
US4416831A (en) * 1981-04-27 1983-11-22 E. R. Squibb & Sons, Inc. Amino and substituted amino phosphinylalkanoyl compounds
US4374131A (en) * 1981-04-27 1983-02-15 E. R. Squibb & Sons, Inc. Amino and substituted amino phosphinyl-alkanoyl compounds
US4381297A (en) * 1981-05-04 1983-04-26 E. R. Squibb & Sons, Inc. Substituted carbonyl phosphinyl-alkanoyl compounds
US4416833A (en) * 1981-05-04 1983-11-22 E. R. Squibb & Sons, Inc. Substituted carbonyl phosphinyl-alkanoyl compounds
EP0070131A1 (en) * 1981-07-09 1983-01-19 Analytical Research Pharmaceuticals Pty. Ltd. Phosphonoalkanoylamino acids
US4432972A (en) * 1981-08-03 1984-02-21 E. R. Squibb & Sons, Inc. Phosphonamidate compounds
US4432971A (en) * 1981-08-03 1984-02-21 E. R. Squibb & Sons, Inc. Phosphonamidate compounds
US4371526A (en) * 1981-08-21 1983-02-01 E. R. Squibb & Sons, Inc. Phosphinylalkanoyl substituted 4,5-dihydropyrazole-5-carboxylic acid derivatives and hypotensive method and composition
GB2106115B (en) * 1981-09-25 1985-06-26 Wellcome Found Pharmaceutical amides, and preparation, formulations and use thereof
US4396772A (en) * 1981-11-23 1983-08-02 F. R. Squibb & Sons, Inc. Phosphinylalkanoyl amino acids
US4555506A (en) * 1981-12-24 1985-11-26 E. R. Squibb & Sons, Inc. Phosphorus containing compounds and use as hypotensives
US4716155A (en) * 1981-12-24 1987-12-29 E. R. Squibb & Sons, Inc. Phosphorus containing compounds and hypotensive use thereof
US4452791A (en) * 1982-03-15 1984-06-05 E. R. Squibb & Sons, Inc. Aminoalkyl and related substituted phosphinic acid angiotensin converting enzyme inhibitors
US4560680A (en) * 1982-03-15 1985-12-24 E. R. Squibb & Sons, Inc. Aminoalkyl and related substituted phosphinic acid angiotensin converting enzyme inhibitors
EP0091525A3 (en) * 1982-04-08 1984-02-29 Analytical Research Pharmaceuticals Pty. Ltd. Phosphonoalkanoylamino acids
US4560681A (en) * 1982-04-22 1985-12-24 E. R. Squibb & Sons, Inc. Phosphinylmethylaminocarbonyl imino acid compounds useful for treating hypertension
ZA832762B (en) * 1982-04-30 1983-12-28 Squibb & Sons Inc Substituted 4-phenoxy prolines
US4681886A (en) * 1982-04-30 1987-07-21 E. R. Squibb & Sons, Inc. Substituted 4-phenoxy or 4-phenylthio prolines
US4427665A (en) 1982-05-19 1984-01-24 E. R. Squibb & Sons, Inc. Phosphinylalkanoyl substituted imino acids and their use in hypotensive compositions
US4468519A (en) * 1982-06-14 1984-08-28 E. R. Squibb & Sons, Inc. Esters of phosphinylalkanoyl substituted prolines
US4616005A (en) * 1982-06-23 1986-10-07 E. R. Squibb & Sons, Inc. Phosphonyl hydroxyacyl amino acid derivatives as antihypertensives
US4703043A (en) * 1982-06-23 1987-10-27 E. R. Squibb & Sons, Inc. Phosphonyl hydroxyacyl amino acid derivatives as antihypertensive
US4452790A (en) * 1982-06-23 1984-06-05 E. R. Squibb & Sons, Inc. Phosphonyl hydroxyacyl amino acid derivatives as antihypertensives
US4442089A (en) * 1982-07-06 1984-04-10 E. R. Squibb & Sons, Inc. Method for treating glaucoma with topical or systemic ACE inhibitor compositions
US4567166A (en) * 1982-07-14 1986-01-28 E. R. Squibb & Sons, Inc. Amino and substituted amino phosphinylalkanoyl compounds useful for treating hypertension
US4826812A (en) * 1982-12-27 1989-05-02 Schering Corporation Antiglaucoma agent
US4555579A (en) * 1983-03-24 1985-11-26 E. R. Squibb & Sons, Inc. Dioxolenylmethyl ester prodrugs of phosphinic acid ace inhibitors
US4594199A (en) * 1983-09-19 1986-06-10 E. R. Squibb & Sons, Inc. Method for making phosphinic acid intermediates
US4602092A (en) * 1983-09-19 1986-07-22 E. R. Squibb & Sons, Inc. Method for making phosphinic acid intermediates
JPS6087293A (ja) * 1983-09-19 1985-05-16 イーアール・スクイブ・アンド・サンズ・インコーポレイテツド ホスフィン酸中間体の製造法
IE58127B1 (en) * 1983-09-19 1993-07-14 Squibb & Sons Inc Process for preparing phosphinic acid intermediates
US4536501A (en) * 1984-03-30 1985-08-20 E. R. Squibb & Sons, Inc. Substituted 4-phenoxy or 4-phenylthio prolines
US4588819A (en) * 1984-11-19 1986-05-13 E. R. Squibb & Sons, Inc. Process and intermediates for preparing trans-4-substituted-s-prolines
US4625038A (en) * 1984-11-19 1986-11-25 E. R. Squibb & Sons, Inc. (25-trans)-4-substituted-2-pyrrolidines-methanols
US4900860A (en) * 1986-03-13 1990-02-13 E. R. Squibb & Sons, Inc. Process for preparing phosphonyloxyacyl amino acids
US4885380A (en) * 1986-03-13 1989-12-05 Thottathil John K Process for preparing phosphonyloxyacyl amino acids and derivatives thereof
US4670193A (en) * 1986-05-12 1987-06-02 E. R. Squibb & Sons, Inc. Process for preparing phosphonic acids
US4738850A (en) * 1986-05-27 1988-04-19 E. R. Squibb & Sons, Inc. Controlled release formulation and method
JPS6435273U (US06650917-20031118-M00005.png) * 1987-08-26 1989-03-03
US6187752B1 (en) * 1988-03-07 2001-02-13 E.R. Squibb & Sons, Inc. Method for treating schizophrenia employing an ace inhibitor
IL90189A0 (en) * 1988-06-01 1989-12-15 Squibb & Sons Inc Pharmaceutical compositions containing a benzazepine-type calcium channel blocker
CA2021409A1 (en) * 1989-08-21 1991-02-22 Donald S. Karanewsky Phosphonate substituted amino or imino acids useful as antihypertensives
US5189023A (en) * 1990-09-04 1993-02-23 American Cyanamid Company Renin inhibitors
US6011021A (en) * 1996-06-17 2000-01-04 Guilford Pharmaceuticals Inc. Methods of cancer treatment using naaladase inhibitors
US5795877A (en) * 1996-12-31 1998-08-18 Guilford Pharmaceuticals Inc. Inhibitors of NAALADase enzyme activity
US6025344A (en) 1996-06-17 2000-02-15 Guilford Pharmaceuticals Inc. Certain dioic acid derivatives useful as NAALADase inhibitors
RU2218179C2 (ru) 1996-06-17 2003-12-10 Гилфорд Фармасьютикалз Инк. СПОСОБЫ ЛЕЧЕНИЯ РАКА С ПРИМЕНЕНИЕМ ИНГИБИТОРОВ NAALADазы
US6071965A (en) * 1996-06-17 2000-06-06 Guilford Pharmaceuticals Inc. Phosphinic alkanoic acid derivatives
US6054444A (en) 1997-04-24 2000-04-25 Guilford Pharmaceuticals Inc. Phosphonic acid derivatives
US5977090A (en) * 1996-09-27 1999-11-02 Guilford Pharmaceuticals Inc. Pharmaceutical compositions and methods of treating compulsive disorders using NAALADase inhibitors
US6046180A (en) * 1996-06-17 2000-04-04 Guilford Pharmaceuticals Inc. NAALADase inhibitors
US6384022B1 (en) 1996-06-17 2002-05-07 Guilford Pharmaceuticals Inc. Prodrugs of NAALAdase inhibitors
US5672592A (en) * 1996-06-17 1997-09-30 Guilford Pharmaceuticals Inc. Certain phosphonomethyl-pentanedioic acid derivatives thereof
US6025345A (en) * 1996-06-17 2000-02-15 Guilford Pharmaceuticals Inc. Inhibitors of NAALADase enzyme activity
US5902817A (en) * 1997-04-09 1999-05-11 Guilford Pharmaceuticals Inc. Certain sulfoxide and sulfone derivatives
US5863536A (en) * 1996-12-31 1999-01-26 Guilford Pharmaceuticals Inc. Phosphoramidate derivatives
US5962521A (en) * 1997-04-04 1999-10-05 Guilford Pharmaceuticals Inc. Hydroxamic acid derivatives
US5981209A (en) * 1997-12-04 1999-11-09 Guilford Pharmaceuticals Inc. Use of NAALADase activity to identify prostate cancer and benign prostatic hyperplasia
US6028216A (en) * 1997-12-31 2000-02-22 Guilford Pharmaceuticals Inc. Asymmetric syntheses and intermediates for preparing enantiomer-enriched hydroxyphosphinyl derivatives
US20020128301A1 (en) * 1998-02-13 2002-09-12 Medivir AB Non-nucleoside reverse transcriptase inhibitors
US6121252A (en) * 1998-03-30 2000-09-19 Guilford Pharmaceuticals Inc. Phosphinic acid derivatives
US6395718B1 (en) * 1998-07-06 2002-05-28 Guilford Pharmaceuticals Inc. Pharmaceutical compositions and methods of inhibiting angiogenesis using naaladase inhibitors
US6265609B1 (en) 1998-07-06 2001-07-24 Guilford Pharmaceuticals Inc. Thio-substituted pentanedioic acid derivatives
EP1571141A2 (en) 1998-07-06 2005-09-07 Guilford Pharmaceuticals Inc. Naaladase inhibitors useful as pharmaceutical compounds and compositions
US6313159B1 (en) 1999-08-20 2001-11-06 Guilford Pharmaceuticals Inc. Metabotropic glutamate receptor ligand derivatives as naaladase inhibitors
US20060135480A1 (en) * 2002-12-03 2006-06-22 Enobia Pharma Derivatives of succinic and glutaric acids and analogs thereof useful as inhibitors of phex
US7459474B2 (en) * 2003-06-11 2008-12-02 Bristol-Myers Squibb Company Modulators of the glucocorticoid receptor and method
US7371759B2 (en) * 2003-09-25 2008-05-13 Bristol-Myers Squibb Company HMG-CoA reductase inhibitors and method
US7420059B2 (en) * 2003-11-20 2008-09-02 Bristol-Myers Squibb Company HMG-CoA reductase inhibitors and method
US7592461B2 (en) 2005-12-21 2009-09-22 Bristol-Myers Squibb Company Indane modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
CN101432025B (zh) * 2006-03-21 2012-04-04 安米林药品公司 肽-肽酶抑制剂结合物及其使用方法
US20070238770A1 (en) * 2006-04-05 2007-10-11 Bristol-Myers Squibb Company Process for preparing novel crystalline forms of peliglitazar, novel stable forms produced therein and formulations
WO2008057857A1 (en) 2006-11-01 2008-05-15 Bristol-Myers Squibb Company MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-ϰB ACTIVITY AND USE THEREOF
EP2089355A2 (en) 2006-11-01 2009-08-19 Brystol-Myers Squibb Company Modulators of glucocorticoid receptor, ap-1, and/or nf- kappa b activity and use thereof
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
ES2393885T7 (es) 2007-06-04 2014-01-30 Synergy Pharmaceuticals Inc. Agonistas de la guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros trastornos
EP2195034A2 (en) * 2007-09-27 2010-06-16 Amylin Pharmaceuticals, Inc. Peptide-peptidase inhibitor conjugates and methods of making and using same
US7828840B2 (en) * 2007-11-15 2010-11-09 Med Institute, Inc. Medical devices and methods for local delivery of angiotensin II type 2 receptor antagonists
ES2627848T3 (es) 2008-06-04 2017-07-31 Synergy Pharmaceuticals Inc. Agonistas de la guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros trastornos
AU2009270833B2 (en) 2008-07-16 2015-02-19 Bausch Health Ireland Limited Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
US9708367B2 (en) 2013-03-15 2017-07-18 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase and their uses
CA2905435A1 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Compositions useful for the treatment of gastrointestinal disorders
WO2014197720A2 (en) 2013-06-05 2014-12-11 Synergy Pharmaceuticals, Inc. Ultra-pure agonists of guanylate cyclase c, method of making and using same
US9593113B2 (en) 2013-08-22 2017-03-14 Bristol-Myers Squibb Company Imide and acylurea derivatives as modulators of the glucocorticoid receptor

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4046889A (en) * 1976-02-13 1977-09-06 E. R. Squibb & Sons, Inc. Azetidine-2-carboxylic acid derivatives

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2288100A1 (fr) * 1974-10-17 1976-05-14 Poudres & Explosifs Ste Nale Carbamates phosphonates, leur procede de preparation et leurs applications en tant qu'agents d'ignifugation
US4151172A (en) * 1977-08-11 1979-04-24 E. R. Squibb & Sons, Inc. Phosphonoacyl prolines and related compounds
US4168267A (en) * 1978-10-23 1979-09-18 E. R. Squibb & Sons, Inc. Phosphinylalkanoyl prolines

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4046889A (en) * 1976-02-13 1977-09-06 E. R. Squibb & Sons, Inc. Azetidine-2-carboxylic acid derivatives

Cited By (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2525607A1 (fr) * 1982-04-22 1983-10-28 Squibb & Sons Inc Phosphinylmethylaminocarbonyl imino acides a action anti-hypertensive
US8604108B2 (en) 2008-11-05 2013-12-10 Clariant Finance (Bvi) Limited Method for producing mono-hydroxyfunctionalized dialkylphosphinic acids and esters and salts thereof by means of acroleins and use thereof
US9139714B2 (en) 2008-11-05 2015-09-22 Clariant Finance (Bvi) Limited Method for producing dialkylphosphinic acids and esters and salts thereof by means of allyl alcohols-acroleins and use thereof
US8614267B2 (en) 2008-11-05 2013-12-24 Clariant Finance (Bvi) Limited Method for producing mono-hydroxyfunctionalized dialkylphosphinic acids and esters and salts thereof by means of allyl alcohols and use thereof
US9035088B2 (en) 2008-11-07 2015-05-19 Clariant Finance (Bvi) Limited Method for producing mono-aminofunctionalized dialkylphosphinic acids and esters and salts thereof by means of acrylnitriles and use thereof
US8604232B2 (en) 2008-11-07 2013-12-10 Clariant Finance (Bvi) Limited Method for producing monoamino-functionalised dialkylphosphinite acids esters and salts and use thereof
US8664418B2 (en) 2008-11-07 2014-03-04 Clariant Finance (Bvi) Limited Method for producing dialkylphosphinic acids and esters and salts thereof by means of acrylic acid derivatives and use thereof
US8735477B2 (en) 2008-11-07 2014-05-27 Clariant Finance (Bvi) Limited Method for producing dialkylphosphinic acids and esters and salts thereof by means of acrylnitriles and use thereof
US8772519B2 (en) 2008-11-11 2014-07-08 Clariant Finance (Bvi) Limited Process for preparing mono-allyl-functionalized dialkylphosphinic acids, salts and esters thereof with allylic compounds, and the use thereof
WO2010063342A1 (de) * 2008-12-02 2010-06-10 Clariant International Ltd Verfahren zur herstellung von mono-carboxyfunktionalisierten dialkylphosphinsäuren, -estern und -salzen mittels vinylester einer carbonsäure und ihre verwendung
US9068119B2 (en) 2008-12-02 2015-06-30 Clariant Finance (Bvi) Limited Method for producing mono-hydroxy-functionalized dialkylphosphinic acids, esters and salts using a vinyl ester of a carobxylic acid and the use thereof
US8735476B2 (en) 2008-12-02 2014-05-27 Clariant Finance (Bvi) Limited Method for producing mono-carboxy-functionalized dialkylphosphinic acids, esters and salts using a vinyl ester of a carboxylic acid and the use thereof
US8987489B2 (en) 2008-12-04 2015-03-24 Clariant Finance (Bvi) Limited Method for producing mono-carboxy-functionalized dialkylphosphinic acids, esters and salts using a vinyl ether and the use thereof
WO2010063344A1 (de) * 2008-12-04 2010-06-10 Clariant International Ltd Verfahren zur herstellung von mono-carboxyfunktionalisierten dialkylphosphinsäuren, -estern und -salzen mittels vinylether und ihre verwendung
US8987490B2 (en) 2008-12-18 2015-03-24 Clariant Finance (Bvi) Limited Method for the production of monohydroxy-functionalized dialkylphosphinic acids, esters, and salts using ethylene oxide, and use thereof
US9018413B2 (en) 2008-12-18 2015-04-28 Clariant Finance (Bvi) Limited Method for the production of alkylphosphonic acids, esters, and salts by oxidizing alkylphosphonous acids, and use thereof
WO2010069416A1 (de) * 2008-12-18 2010-06-24 Clariant International Ltd Verfahren zur herstellung von mono-carboxyfunktionalisierten dialkylphosphinsäuren, -estern und -salzen mittels alkylenoxiden und ihre verwendung
US9085734B2 (en) 2008-12-18 2015-07-21 Clariant Finance (Bvi) Limited Process for preparing mono-carboxy-functionalized dialkylphosphinic acids, esters and salts by means of alkylene oxides and use thereof
US9181487B2 (en) 2008-12-18 2015-11-10 Clariant Finance (Bvi) Limited Process for preparing ethylenedialkylphosphinic acids, esters and salts by means of acetylene and use thereof
US8592505B2 (en) 2008-12-19 2013-11-26 Clariant Finance (Bvi) Limited Hydrophosphorylation of phosphonous acid derivatives for flame retardants
US9279085B2 (en) 2008-12-19 2016-03-08 Clariant Finance (Bvi) Limited Method for the production of monofunctionalized dialkylphosphinic acids, esters and salts, and use thereof

Also Published As

Publication number Publication date
AU5130079A (en) 1980-05-01
PH13931A (en) 1980-11-04
SU988194A3 (ru) 1983-01-07
NL7907568A (nl) 1980-04-25
IT1125558B (it) 1986-05-14
IE49020B1 (en) 1985-07-10
JPS6256880B2 (US06650917-20031118-M00005.png) 1987-11-27
JPS5557597A (en) 1980-04-28
AU529134B2 (en) 1983-05-26
SE7908727L (sv) 1980-06-12
GB2031897B (en) 1983-03-02
GB2031897A (en) 1980-04-30
FR2439790A1 (fr) 1980-05-23
IE791895L (en) 1980-04-23
LU81809A1 (fr) 1980-01-25
ZA795048B (en) 1980-09-24
CA1133496A (en) 1982-10-12
US4168267A (en) 1979-09-18
BE879586A (fr) 1980-04-23
DK148141C (da) 1985-09-02
IT7926704A0 (it) 1979-10-22
DK148141B (da) 1985-03-18
DK445579A (da) 1980-04-24
FR2439790B1 (US06650917-20031118-M00005.png) 1984-01-13
CH645382A5 (de) 1984-09-28

Similar Documents

Publication Publication Date Title
DE2942781A1 (de) Phosphinylalkanoylproline, verfahren zu ihrer herstellung und ihre verwendung als hypotensive wirkstoffe
US4151172A (en) Phosphonoacyl prolines and related compounds
US4337201A (en) Phosphinylalkanoyl substituted prolines
EP0085321B1 (de) Diphosphonsäure-Derivate und diese enthaltende pharmazeutische Präparate
DE2904823A1 (de) Aminosaeurederivate und ihre salze sowie verfahren zu ihrer herstellung
JPH0354115B2 (US06650917-20031118-M00005.png)
DD255163A5 (de) Verfahren zur herstellung von diphesphenaten
JPH10501546A (ja) メタロペプチダーゼ阻害作用を有するホスフィン酸誘導体
NL8702485A (nl) Gesubstitueerde alfa-aminozuren, werkwijzen voor hun bereiding en farmaceutische preparaten die ze bevatten.
EP0233154B1 (de) Ungesättigte Aminosäuren
CA1328113C (en) Process for the manufacture of novel unsaturated amino acid compounds
US4384123A (en) Phosphinylalkanoyl substituted prolines
DD273837A5 (de) Verfahren zur herstellunng von ungesaettigten phosphonsaeuren und derivaten hiervon
DE69017183T2 (de) Diastereoselektive Herstellung von Phosphinsäureestern.
DE60005788T2 (de) Phosphinic pseudopeptide als matrix metalloprotease-inhibitoren
DE3833082A1 (de) Verfahren zur herstellung von phosphinsaeuren, die bei der herstellung von ace-inhibitoren verwendet werden, und dabei gebildete zwischenprodukte
KR100297180B1 (ko) 인지질유도체및이의제조방법
DE2914793A1 (de) Pyrrolidincarboxaldehyd- und piperidincarboxaldehyd-derivate, verfahren zu ihrer herstellung und ihre verwendung als blutdrucksenkende wirkstoffe
DE4100856C2 (de) Verfahren zur Herstellung von N-alkylsubstituierten Aminomethylphosphonsäurederivaten
DE3203307A1 (de) Phosphonate, und diese enthaltende pharmazeutische verbindungen
DE3203309A1 (de) Diphosphonsaeure-derivate und diese enthaltende pharmazeutische praeparate
DD258415A5 (de) Verfahren zur herstellung von phoshonylhydroxyacylprolinen
EP0703919B1 (de) Phosphonobernsteinsäurederivate und ihre verwendung als arzneimittel
EP0061106A2 (de) Verfahren zur Herstellung von Oligophosphonsäuren bzw. Oligophosphinsäuren, ihren Salzen und/oder Estern sowie neue Phosphonsäurederivate
DE2918160B2 (de) Verfahren zur Herstellung von 1.2-Diphosphonobernsteinsäureestern

Legal Events

Date Code Title Description
8110 Request for examination paragraph 44
8131 Rejection