DD235637A5 - Verfahren zur herstellung von amidinverbindungen - Google Patents

Verfahren zur herstellung von amidinverbindungen Download PDF

Info

Publication number: DD235637A5
Authority: DD; German Democratic Republic
Prior art keywords: compounds; compound; acid; complement; carbon atoms
Prior art date: 1984-07-25

Application number

DD85278877A

Other languages

German (de)

English (en)

Inventor

Setsuro Fujii

Toshiyuki Okutome

Toyoo Nakayama

Shigeki Nunomura

Kimio Sudo

Shinichi Watanabe

Masateru Kurumi

Takuo Aoyama

Original Assignee

��@�K@�K@�Kk��

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.)

1984-07-25

Filing date

1985-07-23

Publication date

1986-05-14

1985-07-23 Application filed by ��@�K@�K@�Kk�� filed Critical ��@�K@�K@�Kk��

1986-05-14 Publication of DD235637A5 publication Critical patent/DD235637A5/de

Links

-1 AMIDINE COMPOUNDS Chemical class 0.000 title claims abstract description 11
238000004519 manufacturing process Methods 0.000 title abstract 2
150000001875 compounds Chemical class 0.000 claims abstract description 59
239000002253 acid Substances 0.000 claims abstract description 22
238000000034 method Methods 0.000 claims abstract description 14
150000003839 salts Chemical class 0.000 claims abstract description 14
ULKSSXOMKDEKPC-UHFFFAOYSA-N 6-hydroxynaphthalene-2-carboximidamide Chemical compound C1=C(O)C=CC2=CC(C(=N)N)=CC=C21 ULKSSXOMKDEKPC-UHFFFAOYSA-N 0.000 claims abstract description 6
239000012048 reactive intermediate Substances 0.000 claims abstract description 6
125000004432 carbon atom Chemical group C* 0.000 claims description 10
125000000217 alkyl group Chemical group 0.000 claims description 8
125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 4
239000012458 free base Substances 0.000 claims 1
125000000896 monocarboxylic acid group Chemical group 0.000 claims 1
239000003795 chemical substances by application Substances 0.000 abstract description 11
239000003814 drug Substances 0.000 abstract description 11
230000000694 effects Effects 0.000 abstract description 11
239000002753 trypsin inhibitor Substances 0.000 abstract description 9
101710081722 Antitrypsin Proteins 0.000 abstract description 8
230000001475 anti-trypsic effect Effects 0.000 abstract description 8
239000004019 antithrombin Substances 0.000 abstract description 7
230000002391 anti-complement effect Effects 0.000 abstract description 6
108010008730 anticomplement Proteins 0.000 abstract description 6
239000003112 inhibitor Substances 0.000 abstract description 3
230000000295 complement effect Effects 0.000 description 23
JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 20
CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 18
ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 description 18
239000002244 precipitate Substances 0.000 description 15
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AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 12
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UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 10
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MKRTXPORKIRPDG-UHFFFAOYSA-N diphenylphosphoryl azide Chemical compound C=1C=CC=CC=1P(=O)(N=[N+]=[N-])C1=CC=CC=C1 MKRTXPORKIRPDG-UHFFFAOYSA-N 0.000 description 4
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CQVKMVQRSNNAGO-UHFFFAOYSA-N 2-[4-formyl-3-methyl-n-(2-methylsulfonyloxyethyl)anilino]ethyl methanesulfonate Chemical compound CC1=CC(N(CCOS(C)(=O)=O)CCOS(C)(=O)=O)=CC=C1C=O CQVKMVQRSNNAGO-UHFFFAOYSA-N 0.000 description 2
SKAWDTAMLOJQNK-UHFFFAOYSA-N 2-acetamido-3-(4-hydroxyphenyl)propanoic acid ethyl ester Chemical compound CCOC(=O)C(NC(C)=O)CC1=CC=C(O)C=C1 SKAWDTAMLOJQNK-UHFFFAOYSA-N 0.000 description 2
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UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 2
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HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
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Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C277/00—Preparation of guanidine or its derivatives, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
- C07C277/08—Preparation of guanidine or its derivatives, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups of substituted guanidines
- 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
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings 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
- C07D233/44—Nitrogen atoms not forming part of a nitro radical
- C07D233/50—Nitrogen atoms not forming part of a nitro radical with carbocyclic radicals directly attached to said nitrogen atoms
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
- C07D233/88—Nitrogen atoms, e.g. allantoin
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
- C07D235/30—Nitrogen atoms not forming part of a nitro radical

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Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
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General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Bioinformatics & Cheminformatics (AREA)
Pharmacology & Pharmacy (AREA)
Engineering & Computer Science (AREA)
Animal Behavior & Ethology (AREA)
Chemical Kinetics & Catalysis (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Diabetes (AREA)
Hematology (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

DD85278877A 1984-07-25 1985-07-23 Verfahren zur herstellung von amidinverbindungen DD235637A5 (de)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
JP15504584A JPS6133173A (ja)	1984-07-25	1984-07-25	アミジン化合物

Publications (1)

Publication Number	Publication Date
DD235637A5 true DD235637A5 (de)	1986-05-14

Family

ID=15597463

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
DD85278877A DD235637A5 (de)	1984-07-25	1985-07-23	Verfahren zur herstellung von amidinverbindungen

Country Status (19)

Country	Link
US (2)	US4777182A (pt)
EP (1)	EP0190356B1 (pt)
JP (1)	JPS6133173A (pt)
KR (2)	KR870001087B1 (pt)
AU (1)	AU567039B2 (pt)
CA (1)	CA1254205A (pt)
CS (1)	CS255891B2 (pt)
DD (1)	DD235637A5 (pt)
DE (1)	DE3582057D1 (pt)
DK (1)	DK169069B1 (pt)
ES (1)	ES8607218A1 (pt)
FI (1)	FI78461C (pt)
HU (1)	HU195769B (pt)
MX (1)	MX160912A (pt)
NO (1)	NO163954C (pt)
PH (1)	PH20585A (pt)
SU (1)	SU1456008A3 (pt)
WO (1)	WO1986000893A1 (pt)
ZA (1)	ZA855552B (pt)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
DE3824236C1 (pt) *	1988-07-16	1989-12-28	Heidelberger Druckmaschinen Ag, 6900 Heidelberg, De
CA2032420A1 (en) *	1989-12-22	1991-06-23	Akira Okuyama	Guanidinobenzene derivatives
US5238964A (en) *	1990-04-05	1993-08-24	Torii & Co., Ltd.	Agent for treatment of cerebrovascular contraction
US5652237A (en) *	1994-09-09	1997-07-29	Warner-Lambert Company	2-substituted-4H-3, 1-benzoxazin-4-ones and benzthiazin-4-ones as inhibitors of complement C1r protease for the treatment of inflammatory processes
AU707215B2 (en) *	1995-01-05	1999-07-08	Torii Pharmaceutical Co., Ltd.	Thrombolytic agents
ATE222583T1 (de) *	1995-01-05	2002-09-15	Torii Pharmaceutical Co Ltd	Derivate substituierter amidinonaphthylester
EP1063973B1 (en)	1998-03-19	2016-11-16	Bristol-Myers Squibb Company	Biphasic controlled release delivery system for high solubility pharmaceuticals and method
WO2001077082A1 (en) *	1999-06-02	2001-10-18	Torii Pharmaceutical Co., Ltd.	Naphthalene derivatives
WO2001094299A1 (en) *	2000-06-08	2001-12-13	Shizuoka Coffein Co., Ltd.	Benzene derivatives
EP1884237B1 (en)	2005-05-17	2010-12-08	Santen Pharmaceutical Co., Ltd.	Amidino derivatives for use in the prevention or treatment of glaucoma
EP2119439A3 (en) *	2005-05-17	2010-01-27	Santen Pharmaceutical Co., Ltd.	Angiogenesis inhibitor for treating macular degeneration
WO2008058167A2 (en) *	2006-11-07	2008-05-15	Case Western Reserve University	Method for treating disorders associated with complement activation
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
JP6252991B2 (ja) *	2012-07-04	2017-12-27	味の素株式会社	ナファモスタットメシル酸塩の製造方法

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US4292429A (en) *	1978-03-08	1981-09-29	Ciba-Geigy Corporation	Imidazole urea and amido compounds
AU527371B2 (en) *	1980-09-16	1983-03-03	Torii & Co., Ltd.	Amidine
JPS57179146A (en) *	1981-04-28	1982-11-04	Torii Yakuhin Kk	Amidine compound
JPS60130561A (ja) *	1983-12-16	1985-07-12	Torii Yakuhin Kk	アミジン誘導体およびそれを含む強心剤

1984
- 1984-07-25 JP JP15504584A patent/JPS6133173A/ja active Granted
1985
- 1985-07-12 DE DE8585903394T patent/DE3582057D1/de not_active Expired - Fee Related
- 1985-07-12 HU HU853727A patent/HU195769B/hu not_active IP Right Cessation
- 1985-07-12 KR KR1019860700140A patent/KR870001087B1/ko not_active Expired
- 1985-07-12 WO PCT/JP1985/000392 patent/WO1986000893A1/ja not_active Ceased
- 1985-07-12 US US06/835,853 patent/US4777182A/en not_active Expired - Fee Related
- 1985-07-12 CA CA000486773A patent/CA1254205A/en not_active Expired
- 1985-07-12 EP EP85903394A patent/EP0190356B1/en not_active Expired - Lifetime
- 1985-07-12 AU AU45492/85A patent/AU567039B2/en not_active Ceased
- 1985-07-23 ZA ZA855552A patent/ZA855552B/xx unknown
- 1985-07-23 DD DD85278877A patent/DD235637A5/de not_active IP Right Cessation
- 1985-07-23 ES ES545482A patent/ES8607218A1/es not_active Expired
- 1985-07-23 PH PH32559A patent/PH20585A/en unknown
- 1985-07-24 MX MX206081A patent/MX160912A/es unknown
- 1985-07-24 CS CS855463A patent/CS255891B2/cs not_active IP Right Cessation
1986
- 1986-03-03 DK DK096286A patent/DK169069B1/da not_active IP Right Cessation
- 1986-03-04 FI FI860904A patent/FI78461C/fi not_active IP Right Cessation
- 1986-03-07 NO NO86860865A patent/NO163954C/no not_active IP Right Cessation
- 1986-03-10 KR KR1019860700140A patent/KR860700250A/ko active Granted
- 1986-03-24 SU SU864027333A patent/SU1456008A3/ru active
1988
- 1988-07-11 US US07/217,405 patent/US4820730A/en not_active Expired - Fee Related

Also Published As

Publication number	Publication date
KR860700250A (ko)	1986-08-01
AU567039B2 (en)	1987-11-05
WO1986000893A1 (fr)	1986-02-13
EP0190356A4 (en)	1987-12-09
ES545482A0 (es)	1986-05-16
JPS6133173A (ja)	1986-02-17
ZA855552B (en)	1986-03-26
DK169069B1 (da)	1994-08-08
CS546385A2 (en)	1987-07-16
US4777182A (en)	1988-10-11
KR870001087B1 (ko)	1987-06-04
AU4549285A (en)	1986-02-25
FI78461B (fi)	1989-04-28
HUT42433A (en)	1987-07-28
FI78461C (fi)	1989-08-10
EP0190356B1 (en)	1991-03-06
DE3582057D1 (en)	1991-04-11
SU1456008A3 (ru)	1989-01-30
HU195769B (en)	1988-07-28
NO860865L (no)	1986-04-10
CS255891B2 (en)	1988-03-15
US4820730A (en)	1989-04-11
FI860904A7 (fi)	1986-03-04
MX160912A (es)	1990-06-14
NO163954C (no)	1990-08-15
JPH0461868B2 (pt)	1992-10-02
ES8607218A1 (es)	1986-05-16
CA1254205A (en)	1989-05-16
PH20585A (en)	1987-02-20
FI860904A0 (fi)	1986-03-04
DK96286D0 (da)	1986-03-03
NO163954B (no)	1990-05-07
EP0190356A1 (en)	1986-08-13
DK96286A (da)	1986-03-03

Legal Events

Date	Code	Title	Description
1998-06-04	ENJ	Ceased due to non-payment of renewal fee

Publication	Publication Date	Title
DE3402628C2 (pt)	1987-08-20
DE69519921T2 (de)	2001-06-13	Imidazolidin-derivate und ihre verwendung
DE69628856T2 (de)	2004-05-06	Substituierte n-[(aminoiminomethyl oder aminomethyl)phenyl]propylamide
DE3207033C2 (de)	1984-09-13	Amidinverbindungen, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende pharmazeutische Mittel
DE60103390T2 (de)	2005-06-16	Diazepinderivate oder deren salze
DD141520A5 (de)	1980-05-07	Verfahren zur herstellung neuer derivate von 4-amino-5-alkylsulfonyl-ortho-anisamiden
DD201779A5 (de)	1983-08-10	Verfahren zur herstellung neuer amidinverbindungen
DE2548886C2 (de)	1986-03-13	p-(p'-Guanidinobenzoyloxy)-phenylcarbonsäureester, Verfahren zu deren Herstellung und diese enthaltende Arzneimittel
DE10041402A1 (de)	2002-03-14	Neue Verbindungen, die Faktor Xa-Aktivität inhibieren
DE69104615T2 (de)	1995-03-23	Diphenylpiperazinderivat.
DE3005580C2 (pt)	1988-12-22
DE2065636A1 (de)	1974-12-19	Neue tricyclische verbindungen
DE3031791C2 (pt)	1989-12-28
DE2652201A1 (de)	1977-06-02	Benzisothiazolone, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneipraeparate
DE2316920C3 (de)	1978-03-30	Benzo [d] [13] dioxolderivate, deren Herstellung und diese enthaltende Arzneimittel
DE69500673T2 (de)	1998-03-19	Arzneimittel zur therapeutischen und prophylaktischen Behandlung von Krankheiten, die durch Hyperplasie der glatten Muskelzellen bedingt sind
US4777182A (en)	1988-10-11	6-Amidino-2-naphthyl 4-guanidinobenzoate derivatives and pharmaceutical composition containing them
EP0303951A2 (de)	1989-02-22	2-Pyrimidinyl-1-piperazin-Derivate zur Behandlung von Alkoholismus
DE2718707A1 (de)	1977-11-10	Isothiazolopyridine, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneipraeparate
DE60206376T2 (de)	2006-06-22	Faktor xa inhibitor
DE2801478C2 (pt)	1991-01-31
CH645368A5 (de)	1984-09-28	2-hydroxy-5-(1-hydroxy-2-piperazinylethyl)benzoesaeure-derivate sowie verfahren zu deren herstellung.
DE3207023C2 (de)	1984-12-06	Amidinverbindungen, Verfahren zu ihrer Herstellung und pharmazeutische Mittel, die diese Verbindungen enthalten
DE3427865C2 (pt)	1987-08-20
EP1773855A1 (de)	2007-04-18	Neue verbindungen, die faktor xa-aktivität inhibieren