FI64376C - Foerfarande foer framstaellning av en farmakologiskt anvaendbar 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol - Google Patents

Foerfarande foer framstaellning av en farmakologiskt anvaendbar 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol Download PDF

Info

Publication number: FI64376C
Authority: FI; Finland
Prior art keywords: compound; acid; formula; gaba; tetrahydroisoxazolo
Prior art date: 1977-06-20

Application number

FI781954A

Other languages

English (en)

Finnish (fi)

Other versions

FI64376B (fi

FI781954A7 (fi

Inventor

Povl Krogsgaard-Larsen

Original Assignee

Lundbeck & Co As H

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.)

1977-06-20

Filing date

1978-06-19

Publication date

1983-11-10

1978-06-19 Application filed by Lundbeck & Co As H filed Critical Lundbeck & Co As H

1978-12-21 Publication of FI781954A7 publication Critical patent/FI781954A7/fi

1983-07-29 Publication of FI64376B publication Critical patent/FI64376B/fi

1983-11-10 Application granted granted Critical

1983-11-10 Publication of FI64376C publication Critical patent/FI64376C/fi

Links

ZXRVKCBLGJOCEE-UHFFFAOYSA-N Gaboxadol Chemical compound C1NCCC2=C1ONC2=O ZXRVKCBLGJOCEE-UHFFFAOYSA-N 0.000 title claims description 4
230000000144 pharmacologic effect Effects 0.000 title description 4
150000001875 compounds Chemical class 0.000 claims description 65
150000003839 salts Chemical class 0.000 claims description 22
239000002253 acid Substances 0.000 claims description 13
238000000034 method Methods 0.000 claims description 10
238000002360 preparation method Methods 0.000 claims description 10
230000007062 hydrolysis Effects 0.000 claims description 6
238000006460 hydrolysis reaction Methods 0.000 claims description 6
150000007522 mineralic acids Chemical class 0.000 claims description 4
230000008569 process Effects 0.000 claims description 4
150000007524 organic acids Chemical class 0.000 claims description 3
150000007513 acids Chemical class 0.000 claims description 2
125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 2
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
WWFHMEXCBGNTPW-UHFFFAOYSA-N 2,3,3a,4-tetrahydro-[1,2]oxazolo[5,4-c]pyridin-3-ol Chemical compound N1=CCC2C(O)NOC2=C1 WWFHMEXCBGNTPW-UHFFFAOYSA-N 0.000 claims 1
BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 description 44
ZJQHPWUVQPJPQT-UHFFFAOYSA-N muscimol Chemical compound NCC1=CC(=O)NO1 ZJQHPWUVQPJPQT-UHFFFAOYSA-N 0.000 description 40
CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 description 26
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BNMXDQXGFBXOQQ-UHFFFAOYSA-N ethyl acetate;formic acid;methanol Chemical compound OC.OC=O.CCOC(C)=O BNMXDQXGFBXOQQ-UHFFFAOYSA-N 0.000 description 1
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Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
- C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
- C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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, directly attached to ring carbon atoms
- C07D211/78—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Life Sciences & Earth Sciences (AREA)
General Health & Medical Sciences (AREA)
Veterinary Medicine (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Public Health (AREA)
Pharmacology & Pharmacy (AREA)
Animal Behavior & Ethology (AREA)
Biomedical Technology (AREA)
Neurosurgery (AREA)
Neurology (AREA)
Cardiology (AREA)
Pain & Pain Management (AREA)
Urology & Nephrology (AREA)
Vascular Medicine (AREA)
Heart & Thoracic Surgery (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Pyridine Compounds (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Hydrogenated Pyridines (AREA)

FI781954A 1977-06-20 1978-06-19 Foerfarande foer framstaellning av en farmakologiskt anvaendbar 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol FI64376C (fi)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
GB2574077		1977-06-20
GB2574077		1977-06-20

Publications (3)

Publication Number	Publication Date
FI781954A7 FI781954A7 (fi)	1978-12-21
FI64376B FI64376B (fi)	1983-07-29
FI64376C true FI64376C (fi)	1983-11-10

Family

ID=10232513

Family Applications (2)

Application Number	Title	Priority Date	Filing Date
FI781955A FI781955A7 (fi)	1977-06-20	1978-06-19	Foerfarande foer framstaellning av farmakologiskt anvaendbara 1,2,3,6-tetrahydroisonikotinsyraderivater
FI781954A FI64376C (fi)	1977-06-20	1978-06-19	Foerfarande foer framstaellning av en farmakologiskt anvaendbar 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol

Family Applications Before (1)

Application Number	Title	Priority Date	Filing Date
FI781955A FI781955A7 (fi)	1977-06-20	1978-06-19	Foerfarande foer framstaellning av farmakologiskt anvaendbara 1,2,3,6-tetrahydroisonikotinsyraderivater

Country Status (14)

Country	Link
US (2)	US4278676A (de)
EP (4)	EP0000338B1 (de)
JP (2)	JPS5436290A (de)
AT (1)	AT368505B (de)
AU (2)	AU3724478A (de)
CA (1)	CA1107736A (de)
DK (2)	DK270278A (de)
ES (2)	ES470913A1 (de)
FI (2)	FI781955A7 (de)
IE (1)	IE47200B1 (de)
IT (2)	IT7868449A0 (de)
NO (3)	NO782128L (de)
NZ (1)	NZ187615A (de)
ZA (2)	ZA783493B (de)

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* Cited by examiner, † Cited by third party
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DE3145474A1 (de) *	1980-11-27	1982-09-02	Kefalas A/S, Koebenhavn-Valby	3-substituierte 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridinverbindungen, verfahren zu ihrer herstellung und diese enthaltende arzneimittel
DE3145473A1 (de) *	1980-11-27	1982-08-26	Kefalas A/S, Koebenhavn-Valby	2-substituierte 4,5,6,7-tetrahydroisoxazolo (5,4-c) pyridin-3-on-verbindungen, verfahren zu ihrer herstellung und diese enthaltende arzneimittel
EP0083378A1 (de) *	1981-12-22	1983-07-13	Chugai Seiyaku Kabushiki Kaisha	Tetrahydronicotinsäureamide, Verfahren zu ihrer Herstellung und diese enthaltende pharmazeutische Zusammensetzungen
GB8314391D0 (en) *	1983-05-24	1983-06-29	Kefalas As	Heterocyclic compounds
IT1228426B (it) *	1987-07-20	1991-06-17	Ausimont Spa	Perossiacidi eterociclici
US4859666A (en) *	1988-07-06	1989-08-22	Bristol-Myers Company	THAZ derivatives for enhancement of cerebral function
CN1043051C (zh) *	1994-07-22	1999-04-21	国际壳牌研究有限公司	制备氢化石蜡的方法
DK1641456T3 (da)	2003-06-25	2010-06-21	Lundbeck & Co As H	Gaboxadol til behandling af depression og andre affektive lidelser
US20050234093A1 (en) *	2003-06-25	2005-10-20	H. Lundbeck A/S	Treatment of depression and other affective disorders
AR045540A1 (es)	2003-09-05	2005-11-02	Lundbeck & Co As H	Metodo de elaboracion de 4,5,6,7 tetrahidroisoxazol [5,4-c] piridin-3-ol (thip)
US20050176680A1 (en)	2003-12-11	2005-08-11	Sepracor, Inc.	Combination of sedative and a neurotransmitter modulator, and methods for improving sleep quality and treating depression
US20050137222A1 (en) *	2003-12-18	2005-06-23	H. Lundbeck A/S	Treatment of insomnia in human patients
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CA2551637A1 (en) *	2003-12-24	2005-07-14	Sepracor Inc.	Melatonin combination therapy for improving sleep quality
GB0402118D0 (en) *	2004-01-30	2004-03-03	Merck Sharp & Dohme	Polymorphic forms of a GABAA agonist
WO2005079851A2 (en) *	2004-02-18	2005-09-01	Sepracor, Inc.	Dopamine-agonist combination therapy with sedatives for improving sleep quality
GB0417558D0 (en) *	2004-08-06	2004-09-08	Merck Sharp & Dohme	Novel combination therapy
WO2006083682A2 (en)	2005-01-28	2006-08-10	H.Lundbeck A/S	Polymorphic forms of a gabaa agonist
US20080262029A1 (en) *	2005-04-29	2008-10-23	H. Lundbeck A/S	Acid and Base Salt Forms of Gaboxadol
EP2258358A3 (de)	2005-08-26	2011-09-07	Braincells, Inc.	Neurogenese mit Acetylcholinesterasehemmer
EP1928437A2 (de)	2005-08-26	2008-06-11	Braincells, Inc.	Neurogenese mittels muscarinrezeptormodulation
EP1940389A2 (de)	2005-10-21	2008-07-09	Braincells, Inc.	Modulation von neurogenese durch pde-hemmung
US20070112017A1 (en) *	2005-10-31	2007-05-17	Braincells, Inc.	Gaba receptor mediated modulation of neurogenesis
US20070203216A1 (en) *	2006-02-14	2007-08-30	Bjarke Ebert	Method of treating inflammatory diseases
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1978
- 1978-06-15 DK DK270278A patent/DK270278A/da unknown
- 1978-06-15 DK DK270378A patent/DK270378A/da unknown
- 1978-06-19 NZ NZ187615A patent/NZ187615A/xx unknown
- 1978-06-19 ZA ZA00783493A patent/ZA783493B/xx unknown
- 1978-06-19 NO NO782128A patent/NO782128L/no unknown
- 1978-06-19 EP EP78100191A patent/EP0000338B1/de not_active Expired
- 1978-06-19 EP EP78100190A patent/EP0000167A1/de not_active Withdrawn
- 1978-06-19 FI FI781955A patent/FI781955A7/fi not_active Application Discontinuation
- 1978-06-19 IE IE1234/78A patent/IE47200B1/en unknown
- 1978-06-19 ZA ZA00783492A patent/ZA783492B/xx unknown
- 1978-06-19 EP EP80106497A patent/EP0027279A1/de not_active Withdrawn
- 1978-06-19 ES ES470913A patent/ES470913A1/es not_active Expired
- 1978-06-19 US US05/917,118 patent/US4278676A/en not_active Expired - Lifetime
- 1978-06-19 ES ES470912A patent/ES470912A1/es not_active Expired
- 1978-06-19 AU AU37244/78A patent/AU3724478A/en active Pending
- 1978-06-19 NO NO782127A patent/NO152049C/no unknown
- 1978-06-19 FI FI781954A patent/FI64376C/fi not_active IP Right Cessation
- 1978-06-19 EP EP80106498A patent/EP0028017A1/de not_active Withdrawn
- 1978-06-20 AU AU37298/78A patent/AU521040B2/en not_active Expired
- 1978-06-20 CA CA305,798A patent/CA1107736A/en not_active Expired
- 1978-06-20 AT AT0448678A patent/AT368505B/de not_active IP Right Cessation
- 1978-06-20 IT IT7868449A patent/IT7868449A0/it unknown
- 1978-06-20 IT IT68450/78A patent/IT1159739B/it active
- 1978-06-20 JP JP7480078A patent/JPS5436290A/ja active Pending
- 1978-06-20 JP JP7479978A patent/JPS5436275A/ja active Pending
1979
- 1979-09-03 NO NO792839A patent/NO792839L/no unknown
- 1979-12-17 US US06/104,080 patent/US4301287A/en not_active Expired - Lifetime

Also Published As

Publication number	Publication date
AU521040B2 (en)	1982-03-11
NO782127L (no)	1978-12-21
EP0000338A2 (de)	1979-01-24
CA1107736A (en)	1981-08-25
ES470912A1 (es)	1979-02-01
IT1159739B (it)	1987-03-04
ES470913A1 (es)	1979-02-01
ATA448678A (de)	1982-02-15
EP0027279A1 (de)	1981-04-22
EP0000167A1 (de)	1979-01-10
JPS5436275A (en)	1979-03-16
AU3729878A (en)	1980-01-03
FI64376B (fi)	1983-07-29
ZA783492B (en)	1979-06-27
IE781234L (en)	1978-12-20
IT7868450A0 (it)	1978-06-20
FI781955A7 (fi)	1978-12-21
NO152049C (no)	1985-07-24
DK270378A (da)	1978-12-21
IE47200B1 (en)	1984-01-11
NO152049B (no)	1985-04-15
FI781954A7 (fi)	1978-12-21
US4301287A (en)	1981-11-17
EP0028017A1 (de)	1981-05-06
DK270278A (da)	1978-12-21
JPS5436290A (en)	1979-03-16
AT368505B (de)	1982-10-25
EP0000338B1 (de)	1981-11-25
NZ187615A (en)	1981-12-15
IT7868449A0 (it)	1978-06-20
US4278676A (en)	1981-07-14
AU3724478A (en)	1980-01-03
ZA783493B (en)	1979-06-27
NO782128L (no)	1978-12-21
NO792839L (no)	1978-12-21
EP0000338A3 (en)	1979-06-27

Legal Events

Date	Code	Title	Description
2004-08-31	MM	Patent lapsed	Owner name: H. LUNDBECK & CO A/S

Publication	Publication Date	Title
FI64376C (fi)	1983-11-10	Foerfarande foer framstaellning av en farmakologiskt anvaendbar 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol
JP2756742B2 (ja)	1998-05-25	Ｎ−アシル−２，３−ベンゾジアゼピン誘導体、その製造法、それを含有する医薬組成物、およびその製造法
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PL164244B1 (en)	1994-07-29	Method of obtaining novel heterocyclic compounds
AU2018235266B2 (en)	2021-09-30	Pharmacologically active alicyclic-substituted pyrazolo[1,5-a]pyrimidine derivatives
US4686213A (en)	1987-08-11	Substituted 1,3,4,9-tetrahydropyrano(3,4-b)indole-1-acetic acids
US5639751A (en)	1997-06-17	N-acyl-2,3-benzodiazepine derivatives for treating acute and chronic neurodegenerative disorders
US4193998A (en)	1980-03-18	1,2,3,4,6,7-Hexahydro-11BαH-benzo[a]quinolizine-derivatives
JPS6216952B2 (de)	1987-04-15
JP3266624B2 (ja)	2002-03-18	スピロ橋かけ型および非橋かけ型複素環式化合物
US5521174A (en)	1996-05-28	N-acyl-2,3-benzodiazepine derivatives and a method of treating spasms of the skeletal musculature therewith
JP2778832B2 (ja)	1998-07-23	Ｇａｂａ−ｂアンタゴニストとしての２−置換モルホリンおよびチオモルホリン誘導体
JPH11503126A (ja)	1999-03-23	新規な複素環式化合物
DE69822937T2 (de)	2004-08-12	Indolmorphinan-derivate und medikamente zur behandlung/mittel zur vorbeugung von cerebralen störungen
DD252376A5 (de)	1987-12-16	Verfahren zur herstellung von hexohydro-(1)-benzo-(pyrane und thiopyrano)-4,3-c)pyridinen
KR910002566B1 (ko)	1991-04-26	2,3,4,5,6,7-헥사하이드로-2,7-메타노-1,5-벤조옥사조닌 및 -1,4-벤조옥사조닌 화합물들, 이들의 제조방법 및 이들을 포함하는 약학적 조성물
US4287211A (en)	1981-09-01	Derivatives of phenylethylamines, processes for their preparation and related pharmaceutical compositions
US4609657A (en)	1986-09-02	Ergot peptide alkaloid derivatives, processes for their preparation and pharmaceutical compositions containing them
EP0240986B1 (de)	1991-01-23	D-Nor-7-ergolinderivate, Verfahren zu ihrer Herstellung, pharmazeutische Zubereitung und Verwendung
NO823824L (no)	1983-05-19	Fremgangsmaate for fremstilling av benzylidenderivater
FR2508457A1 (fr)	1982-12-31	Pyrrolo(2,1-b)quinazolines et pyrido(2,1-b)quinazolines substituees, leur preparation et leurs utilisations therapeutiques
US3825533A (en)	1974-07-23	N-carboxymethyl-n-substituted glycinate esters of 3-hydroxy-1,4-benzo-diazepin-2-ones
EP0001585B1 (de)	1981-07-22	Piperazino-pyrrolobenzodiazepine, Verfahren zu ihrer Herstellung sowie pharmazeutische Präparate enthaltend diese Verbindungen
KR920000763B1 (ko)	1992-01-21	신규 벤조디아제핀의 제조 방법
DE3124086A1 (de)	1982-03-04	Heterozyklische verbindungen, verfahren zu deren herstellung und pharmazeutische zusammensetzungen, welche diese verbindungen enthalten