DK186082A - Fremgangsmaade til fremstilling af eventuelt substitueret aminophosphinylalkanoylforbindelser - Google Patents

Fremgangsmaade til fremstilling af eventuelt substitueret aminophosphinylalkanoylforbindelser Download PDF

Info

Publication number: DK186082A
Authority: DK; Denmark
Prior art keywords: substituted; aminophosphinyl; procedure; preparation; alkyl
Prior art date: 1981-04-27

Application number

DK186082A

Other languages

English (en)

Inventor

E W Petrillo

Original Assignee

Squibb & Sons Inc

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.)

1981-04-27

Filing date

1982-04-26

Publication date

1982-10-28

1982-04-26 Application filed by Squibb & Sons Inc filed Critical Squibb & Sons Inc

1982-10-28 Publication of DK186082A publication Critical patent/DK186082A/da

Links

150000001875 compounds Chemical class 0.000 title abstract description 6
-1 AMINOPHOSPHINYL Chemical class 0.000 title description 6
229910052739 hydrogen Inorganic materials 0.000 abstract description 7
239000001257 hydrogen Substances 0.000 abstract description 7
UUUHXMGGBIUAPW-UHFFFAOYSA-N 1-[1-[2-[[5-amino-2-[[1-[5-(diaminomethylideneamino)-2-[[1-[3-(1h-indol-3-yl)-2-[(5-oxopyrrolidine-2-carbonyl)amino]propanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbon Chemical compound C1CCC(C(=O)N2C(CCC2)C(O)=O)N1C(=O)C(C(C)CC)NC(=O)C(CCC(N)=O)NC(=O)C1CCCN1C(=O)C(CCCN=C(N)N)NC(=O)C1CCCN1C(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C1CCC(=O)N1 UUUHXMGGBIUAPW-UHFFFAOYSA-N 0.000 abstract description 2
102000004270 Peptidyl-Dipeptidase A Human genes 0.000 abstract description 2
108090000882 Peptidyl-Dipeptidase A Proteins 0.000 abstract description 2
239000002253 acid Substances 0.000 abstract description 2
239000002220 antihypertensive agent Substances 0.000 abstract description 2
230000005764 inhibitory process Effects 0.000 abstract description 2
230000000694 effects Effects 0.000 abstract 1
150000002148 esters Chemical class 0.000 abstract 1
125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
125000001841 imino group Chemical group [H]N=* 0.000 abstract 1
125000000217 alkyl group Chemical group 0.000 description 9
125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 6
150000002431 hydrogen Chemical class 0.000 description 6
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 5
229910052736 halogen Inorganic materials 0.000 description 3
150000002367 halogens Chemical class 0.000 description 3
125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 description 2
YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 description 2
125000004414 alkyl thio group Chemical group 0.000 description 2
ZZVUWRFHKOJYTH-UHFFFAOYSA-N diphenhydramine Chemical group C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 ZZVUWRFHKOJYTH-UHFFFAOYSA-N 0.000 description 2
125000002541 furyl group Chemical group 0.000 description 2
125000003356 phenylsulfanyl group Chemical group [*]SC1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 2
125000004076 pyridyl group Chemical group 0.000 description 2
125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 2
125000003342 alkenyl group Chemical group 0.000 description 1
125000003545 alkoxy group Chemical group 0.000 description 1
125000003277 amino group Chemical group 0.000 description 1
125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 1
239000007822 coupling agent Substances 0.000 description 1
125000001188 haloalkyl group Chemical group 0.000 description 1
KHUXNRRPPZOJPT-UHFFFAOYSA-N phenoxy radical Chemical group O=C1C=C[CH]C=C1 KHUXNRRPPZOJPT-UHFFFAOYSA-N 0.000 description 1
125000006239 protecting group Chemical group 0.000 description 1
229930192474 thiophene Natural products 0.000 description 1

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
- C07F9/553—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
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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 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 ring carbon atoms
- C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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 ring carbon atoms
- 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)]
- C07F9/306—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
- C07F9/3211—Esters of 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)]
- C07F9/32—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
- C07F9/50—Organo-phosphines
- C07F9/52—Halophosphines

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Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
General Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Biochemistry (AREA)
Molecular Biology (AREA)
Engineering & Computer Science (AREA)
Animal Behavior & Ethology (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Chemical Kinetics & Catalysis (AREA)
Bioinformatics & Cheminformatics (AREA)
Heart & Thoracic Surgery (AREA)
Medicinal Chemistry (AREA)
Public Health (AREA)
Pharmacology & Pharmacy (AREA)
Veterinary Medicine (AREA)
Cardiology (AREA)
General Chemical & Material Sciences (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Peptides Or Proteins (AREA)
Saccharide Compounds (AREA)

Description

hvor R·^ er hydrogen, eventuelt med alkyl eller halogen eller amino substitueret alkyl, phenyl eller alkylenphenyl, der i kernen eventuelt er substitueret med en eller flere alkyl-, alkylthio-, halogen-, trifluormethyl-, hydroxy-, phenyl-, phenoxy-, phenylthio- eller phenylmethylgrupper, eller R^g er en eventuelt via en alkylenbro tilknyttet fura-nyl-, thiofen- eller pyridylgruppe eller en pyrrolidinoxy-eller piperidinoxygruppe, Rjq er alkyl, phenyl, benzyl eller phenethyl, R2 er hydrogen, alkyl, alkenyl, halogenalkyl, eller en eventuelt via en alkylenbro tilknyttet phenylgruppe, der eventuelt er substitueret med op til 3 alkyl-, alkylthio-, halogen-, trifluormethyl-, hydroxy-, phenyl-, phenoxyl-, phenylthio- og/eller phenylmethylgrupper, eller R2 er en eventuelt via en alkylenbro tilknyttet furanyl-, thiofenelier pyridylgruppe, R^ er hydrogen, alkyl, benzyl, benzhy-dryl eller har delformlen

hvor R^ er hydrogen, alkyl eller phenyl, og R^g er hydrogen, alkyl, alkoxy, phenyl, eller R^ og R^g er tilsammen -(CH2)2-, -(CH2)3-, -CH=CH- eller ortophenylen, Rs er hydrogen, alkyl, der eventuelt er halogensubstitueret, benzyl eller phenethyl, og n er 0 eller 1, fremstilles ved omsætning af en forbindelse med formlen

II eller en aktiveret form deraf, hvori R,1 er R^CO eller R20OCO, og R'3 er hydrogen, lavere alkyl, benzyl eller benz-hydryl, med en forbindelse med formlen

HX III i nærværelse af et koblingsmiddel eller ved «nsætning af en syre med formlen II, hvori er

med en forbindelse med formlen III, hvori carboxy-

gruppen ser forestret, hvorpå eventuelle beskyttelsesgrupper i det fremkomne produkt eventuelt fjernes.

Forbindelser med formlen I er anvendelige som hypo-tensive midler på grund af deres inhibering af det angiotensin-omdannende enzym.

DK186082A 1981-04-27 1982-04-26 Fremgangsmaade til fremstilling af eventuelt substitueret aminophosphinylalkanoylforbindelser DK186082A (da)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US06/258,194 US4374131A (en)	1981-04-27	1981-04-27	Amino and substituted amino phosphinyl-alkanoyl compounds

Publications (1)

Publication Number	Publication Date
DK186082A true DK186082A (da)	1982-10-28

Family

ID=22979499

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
DK186082A DK186082A (da)	1981-04-27	1982-04-26	Fremgangsmaade til fremstilling af eventuelt substitueret aminophosphinylalkanoylforbindelser

Country Status (11)

Country	Link
US (1)	US4374131A (da)
EP (1)	EP0063896B1 (da)
JP (1)	JPS57197290A (da)
AT (1)	ATE14882T1 (da)
AU (2)	AU556756B2 (da)
CA (1)	CA1192196A (da)
DE (1)	DE3265360D1 (da)
DK (1)	DK186082A (da)
HU (1)	HU186011B (da)
IE (1)	IE53030B1 (da)
ZA (1)	ZA822577B (da)

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WO2010054722A1 (de)	2008-11-11	2010-05-20	Clariant International Ltd	Verfahren zur herstellung von mono-allylfunktionalisierten dialkylphosphinsäuren, deren salze und ester mit allylischen verbindungen und ihre verwendung
DE102008060036A1 (de) *	2008-12-02	2010-06-10	Clariant International Limited	Verfahren zur Herstellung von mono-carboxyfunktionalisierten Dialkylphosphinsäuren, -estern und -salzen mittels Vinylester einer Carbonsäure und ihre Verwendung
DE102008060035A1 (de) *	2008-12-02	2010-06-10	Clariant International Limited	Verfahren zur Herstellung von mono-hydroxyfunktionalisierten Dialkylphosphinsäuren, -estern und -salzen mittels Vinylester einer Carbonsäure und ihre Verwendung
DE102008060535A1 (de) *	2008-12-04	2010-06-10	Clariant International Limited	Verfahren zur Herstellung von mono-carboxyfunktionalisierten Dialkylphosphinsäuren, -estern und -salzen mittels Vinylether und ihre Verwendung
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DE102008063627A1 (de)	2008-12-18	2010-06-24	Clariant International Limited	Verfahren zur Herstellung von monohydroxyfunktionalisierten Dialkylphosphinsäuren,-estern und -salzen mittels Ethylenoxid und ihre Verwendung
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JP5619769B2 (ja)	2008-12-18	2014-11-05	クラリアント・ファイナンス・（ビーブイアイ）・リミテッド	アセチレンを利用したエチレンジアルキルホスフィン酸、エチレンジアルキルホスフィン酸エステル、およびエチレンジアルキルホスフィン酸塩の製造方法、およびそれらの使用
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1981
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1982
- 1982-04-06 AU AU82379/82A patent/AU556756B2/en not_active Ceased
- 1982-04-08 CA CA000400780A patent/CA1192196A/en not_active Expired
- 1982-04-14 DE DE8282301923T patent/DE3265360D1/de not_active Expired
- 1982-04-14 EP EP82301923A patent/EP0063896B1/en not_active Expired
- 1982-04-14 IE IE862/82A patent/IE53030B1/en not_active IP Right Cessation
- 1982-04-14 AT AT82301923T patent/ATE14882T1/de not_active IP Right Cessation
- 1982-04-15 ZA ZA822577A patent/ZA822577B/xx unknown
- 1982-04-26 DK DK186082A patent/DK186082A/da not_active Application Discontinuation
- 1982-04-26 HU HU821315A patent/HU186011B/hu not_active IP Right Cessation
- 1982-04-27 JP JP57072541A patent/JPS57197290A/ja active Granted
1986
- 1986-09-29 AU AU63282/86A patent/AU589686B2/en not_active Ceased

Also Published As

Publication number	Publication date
HU186011B (en)	1985-05-28
AU589686B2 (en)	1989-10-19
JPH0354115B2 (da)	1991-08-19
AU556756B2 (en)	1986-11-20
ZA822577B (en)	1983-03-30
IE53030B1 (en)	1988-05-11
US4374131A (en)	1983-02-15
ATE14882T1 (de)	1985-08-15
JPS57197290A (en)	1982-12-03
AU6328286A (en)	1987-01-08
EP0063896B1 (en)	1985-08-14
AU8237982A (en)	1982-11-04
IE820862L (en)	1982-10-27
DE3265360D1 (en)	1985-09-19
CA1192196A (en)	1985-08-20
EP0063896A1 (en)	1982-11-03

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DK186082A (da)	1982-10-28	Fremgangsmaade til fremstilling af eventuelt substitueret aminophosphinylalkanoylforbindelser
ATE343383T1 (de)	2006-11-15	Hemmer der zelladhäsion
SE423812B (sv)	1982-06-07	Forfarande for framstellning av terapeutiskt aktiva derivat av azetidin-2-karboxylsyra, prolin och pipekolinsyra
EA199800650A1 (ru)	1999-02-25	Новые соединения
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DK1392306T3 (da)	2008-05-19	Substituerede tetrahydroisoquinoliner til anvendelse i behandlingen af inflammatoriske sygdomme
NO943055L (no)	1994-10-11	Bicyklo[2.2.2.Åoktanderivater som cholestocystokininhemmere
DK221882A (da)	1982-11-19	Fremgangsmaade til fremstilling af oxobenzoxaziner
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DK161385C (da)	1991-12-16	Analogifremgangsmaade til fremstilling af theophyllinylalkyloxadiazoler eller fysiologisk acceptable additionssalte deraf
NO20023251L (no)	2002-09-06	Nye tetrahydropyridiner, fremgangsmåte for deres fremstilling og farmasöytiske preparater inneholdende de samme
AR018632A1 (es)	2001-11-28	Compuestos derivados de acido 1,2,3,4-tetrahidroquinolin-2-carboxilico, su uso en la fabricacion de medicamentos, composicion farmaceutica que los contiene, proceso para su preparacion.
ID25477A (id)	2000-10-05	Turunan-turunan spiropiperidin
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PE20050579A1 (es)	2005-09-08	Derivados de quinolina-4-carboxilico como antagonistas de la selectina
YU136390A (sh)	1993-10-20	Postupak za dobijanje supstituisanih 2-imidazolina
NO985186L (no)	1998-11-06	Forbindelser med camptothecin-grunnstruktur, isolert fra Mappia foetida, og anvendelse derav som syntoner for nye legemidler samt som terapeutiske midler
DE69906243D1 (de)	2003-04-30	2-Indanmethanolderivate und ihre Verwendung als Riechstoffe
EA200200352A1 (ru)	2002-10-31	Фенил- и пиридил-тетрагидропиридины, обладающие ингибирующей активностью в отношении фактора некроза опухоли (фно)
FI95703C (fi)	1996-03-11	Fungisidiset 3-imino-1,4-oksatiinit
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ES2034537T3 (es)	1993-04-01	Procedimiento para la obtencion de derivados del acido 5-(n-3,4,5,6-tetrahidroftalimido)-canimico.
NO864760D0 (no)	1986-11-26	Nye fluorholdige 1,4-dihydropyridiner, fremgangsmaate til deres fremstilling, samt deres anvendelse som legemiddel.
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Date	Code	Title	Description
1985-08-19	AHS	Application shelved for other reasons than non-payment