DK175235B1 - Ny anvendelse af azatricycloderivater og farmaceutiske præparater med indhold deraf - Google Patents

Ny anvendelse af azatricycloderivater og farmaceutiske præparater med indhold deraf Download PDF

Info

Publication number: DK175235B1
Authority: DK; Denmark
Prior art keywords: dermatitis; topical; medicament; treatment; use according
Prior art date: 1987-11-09

Application number

DK198806203A

Other languages

Danish (da)

English (en)

Other versions

DK620388A (da

DK620388D0 (da

Inventor

Anton Stuetz

Peter Stuetz

Maximilian Grassberger

Josef Gottfried Meingassner

Original Assignee

Novartis Ag

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.)

1987-11-09

Filing date

1988-11-07

Publication date

2004-07-19

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=25599336&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=DK175235(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

1987-11-09 Priority claimed from AT0295287A external-priority patent/AT400808B/de

1988-11-07 Application filed by Novartis Ag filed Critical Novartis Ag

1988-11-07 Publication of DK620388D0 publication Critical patent/DK620388D0/da

1989-05-10 Publication of DK620388A publication Critical patent/DK620388A/da

2004-07-19 Application granted granted Critical

2004-07-19 Publication of DK175235B1 publication Critical patent/DK175235B1/da

Links

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Classifications

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- A61K31/436—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
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- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents

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Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Animal Behavior & Ethology (AREA)
Medicinal Chemistry (AREA)
Epidemiology (AREA)
Chemical Kinetics & Catalysis (AREA)
Organic Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Molecular Biology (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Pain & Pain Management (AREA)
Rheumatology (AREA)
Dermatology (AREA)
Pulmonology (AREA)
Immunology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

DK198806203A 1987-11-09 1988-11-07 Ny anvendelse af azatricycloderivater og farmaceutiske præparater med indhold deraf DK175235B1 (da)

Applications Claiming Priority (4)

Application Number	Priority Date	Filing Date	Title
AT0295287A AT400808B (de)	1987-11-09	1987-11-09	Verwendung von tricyclischen verbindungen zur herstellung von topischen arzneimitteln
AT295287		1987-11-09
DE3742805		1987-12-17
DE3742805		1987-12-17

Publications (3)

Publication Number	Publication Date
DK620388D0 DK620388D0 (da)	1988-11-07
DK620388A DK620388A (da)	1989-05-10
DK175235B1 true DK175235B1 (da)	2004-07-19

Family

ID=25599336

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
DK198806203A DK175235B1 (da)	1987-11-09	1988-11-07	Ny anvendelse af azatricycloderivater og farmaceutiske præparater med indhold deraf

Country Status (13)

Country	Link
US (1)	US20050059694A1 (2)
EP (2)	EP0315978B1 (2)
JP (1)	JP2604834B2 (2)
KR (1)	KR0133916B1 (2)
AU (1)	AU619772B2 (2)
CH (1)	CH677448A5 (2)
CY (1)	CY1730A (2)
DK (1)	DK175235B1 (2)
GB (1)	GB2212061B (2)
HK (1)	HK8694A (2)
NL (1)	NL195077C (2)
PH (1)	PH26083A (2)
SE (2)	SE503236C2 (2)

Families Citing this family (41)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US4894366A (en) *	1984-12-03	1990-01-16	Fujisawa Pharmaceutical Company, Ltd.	Tricyclo compounds, a process for their production and a pharmaceutical composition containing the same
IE64214B1 (en) *	1989-06-06	1995-07-26	Fujisawa Pharmaceutical Co	Macrolides for the treatment of reversible obstructive airways diseases
US5519049A (en) *	1989-06-06	1996-05-21	Fisons Plc	Macrolides for the treatment of reversible obstructive airways diseases
DK0406791T3 (da) *	1989-07-05	1995-03-27	Fujisawa Pharmaceutical Co	Vandigt flydende præparat til ekstern anvendelse
US5215995A (en) *	1989-10-16	1993-06-01	Fujisawa Pharmaceutical Co., Ltd.	Hair revitalizing agent
KR0159766B1 (ko) *	1989-10-16	1998-12-01	후지사와 토모키치로	양모제 조성물
US5208228A (en) *	1989-11-13	1993-05-04	Merck & Co., Inc.	Aminomacrolides and derivatives having immunosuppressive activity
GB8925797D0 (en) *	1989-11-15	1990-01-04	Fisons Plc	Compositions
US5064835A (en) *	1990-03-01	1991-11-12	Merck & Co., Inc.	Hydroxymacrolide derivatives having immunosuppressive activity
KR0177158B1 (ko) *	1990-03-01	1999-03-20	후지사와 도모기찌로	면역억제 활성을 갖는 트리사이클릭 화합물 함유 용액 제제
WO1991013899A1 (en) *	1990-03-12	1991-09-19	Fujisawa Pharmaceutical Co., Ltd.	Tricyclo compounds
EP0455427A1 (en) *	1990-04-30	1991-11-06	Merck & Co. Inc.	Deoxymacrolide derivatives having immunosuppressive activity
US5342935A (en) *	1990-06-25	1994-08-30	Merck & Co., Inc.	Antagonists of immunosuppressive macrolides
US5190950A (en) *	1990-06-25	1993-03-02	Merck & Co., Inc.	Antagonists of immunosuppressive macrolides
ES2099112T3 (es) *	1990-09-04	1997-05-16	Fujisawa Pharmaceutical Co	Pomadas que contienen un compuesto triciclico.
GB2248184A (en) *	1990-09-28	1992-04-01	Fujisawa Pharmaceutical Co	New use of macrolide compounds for active oxygen-mediated diseases
US5143918A (en) *	1990-10-11	1992-09-01	Merck & Co., Inc.	Halomacrolides and derivatives having immunosuppressive activity
US5348966A (en) *	1990-10-24	1994-09-20	Fujisawa Pharmaceutical Co., Ltd.	Method for treating pyoderma and Sezary's syndrome using FK 506 and related compounds
PH31204A (en) *	1990-11-02	1998-05-05	Fujisawa Pharmaceutical Co	Pharmaceutical composition.
US5147877A (en) *	1991-04-18	1992-09-15	Merck & Co. Inc.	Semi-synthetic immunosuppressive macrolides
US5565560A (en) *	1991-05-13	1996-10-15	Merck & Co., Inc.	O-Aryl,O-alkyl,O-alkenyl and O-alkynylmacrolides having immunosuppressive activity
US5162334A (en) *	1991-05-13	1992-11-10	Merck & Co., Inc.	Amino O-alkyl, O-alkenyl and O-alkynlmacrolides having immunosuppressive activity
US5250678A (en)	1991-05-13	1993-10-05	Merck & Co., Inc.	O-aryl, O-alkyl, O-alkenyl and O-alkynylmacrolides having immunosuppressive activity
US5189042A (en) *	1991-08-22	1993-02-23	Merck & Co. Inc.	Fluoromacrolides having immunosuppressive activity
ZA926812B (en)	1991-09-09	1993-04-28	Merck & Co Inc	O-heteroaryl,o-alkylheteroaryl,o-alkenylheteroaryl and o-alkynylheteroaryl macrolides having immunosupressive activity
US5247076A (en) *	1991-09-09	1993-09-21	Merck & Co., Inc.	Imidazolidyl macrolides having immunosuppressive activity
US5208241A (en) *	1991-09-09	1993-05-04	Merck & Co., Inc.	N-heteroaryl, n-alkylheteroaryl, n-alkenylheteroaryl and n-alkynylheteroarylmacrolides having immunosuppressive activity
US5286731A (en) *	1991-09-17	1994-02-15	American Home Products Corporation	Method of treating immunoinflammatory bowel disease
US5286730A (en) *	1991-09-17	1994-02-15	American Home Products Corporation	Method of treating immunoinflammatory disease
GB9218597D0 (en) *	1992-08-25	1992-10-14	Fisons Plc	Novel method of treatment
MY110603A (en) *	1993-05-27	1998-08-29	Novartis Ag	Tetrahydropyran derivatives
JPH06345646A (ja) *	1993-06-08	1994-12-20	Fujisawa Pharmaceut Co Ltd	ローション剤
US5693648A (en) *	1994-09-30	1997-12-02	Merck & Co., Inc.	O-aryl, O-alkyl, O-alkenyl and O-alkynyl-macrolides having immunosuppressive activity
CN100335063C (zh)	1994-10-26	2007-09-05	诺瓦蒂斯有限公司	药物组合物
CA2326222C (en) *	1998-04-27	2008-09-23	Fujisawa Pharmaceutical Co., Ltd.	Medicinal compositions
GB9826656D0 (en)	1998-12-03	1999-01-27	Novartis Ag	Organic compounds
EP1603560A1 (en) *	2003-02-06	2005-12-14	Cipla Ltd.	Topical immunotherapy and compositions for use therein
US7186518B2 (en) *	2003-11-21	2007-03-06	Dade Behring Inc.	Method and composition useful for determining FK 506
WO2010041684A1 (ja)	2008-10-08	2010-04-15	高田製薬株式会社	タクロリムス外用剤
EP2308468A1 (en) *	2009-10-08	2011-04-13	Novaliq GmbH	Novel pharmaceutical composition comprising a macrolide immunosuppressant drug
CN106074367A (zh) *	2016-07-20	2016-11-09	中山大学中山眼科中心	含fk506类化合物/fkbp蛋白二聚体的药物组合物及其制备方法

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US4139563A (en) *	1977-07-01	1979-02-13	Merrell Toraude Et Compagnie	α-ACETYLENIC DERIVATIVES OF AMINES
EP0012866B1 (en) *	1978-12-21	1983-01-19	Gruppo Lepetit S.P.A.	New 3h-naphtho(1,2-d)imidazoles, processes for preparing them, compounds for use as antiinflammatory and antimicrobial agents and compositions for that use containing them
US4411893A (en) *	1981-08-14	1983-10-25	Minnesota Mining And Manufacturing Company	Topical medicament preparations
US4556654A (en) *	1983-06-28	1985-12-03	Warner-Lambert Company	Antimicrobial substituted anthra[1,9-cd]pyrazol-6(2H)-ones
US4894366A (en) *	1984-12-03	1990-01-16	Fujisawa Pharmaceutical Company, Ltd.	Tricyclo compounds, a process for their production and a pharmaceutical composition containing the same
CA1272953A (en) *	1984-10-08	1990-08-21	Yuji Makino	Pharmaceutical composition for external use containing active-type vitamin d.sub.3

1988
- 1988-11-07 DK DK198806203A patent/DK175235B1/da not_active IP Right Cessation
- 1988-11-07 GB GB8826066A patent/GB2212061B/en not_active Expired - Lifetime
- 1988-11-07 PH PH37779A patent/PH26083A/en unknown
- 1988-11-07 CH CH4131/88A patent/CH677448A5/de not_active IP Right Cessation
- 1988-11-08 JP JP63283524A patent/JP2604834B2/ja not_active Expired - Lifetime
- 1988-11-08 NL NL8802734A patent/NL195077C/nl not_active IP Right Cessation
- 1988-11-08 AU AU24902/88A patent/AU619772B2/en not_active Expired
- 1988-11-08 KR KR1019880014649A patent/KR0133916B1/ko not_active Expired - Lifetime
- 1988-11-08 SE SE8804036A patent/SE503236C2/sv unknown
- 1988-11-09 EP EP88118669A patent/EP0315978B1/en not_active Expired - Lifetime
- 1988-11-09 EP EP93120261A patent/EP0596541B1/en not_active Expired - Lifetime
1994
- 1994-01-21 HK HK86/94A patent/HK8694A/xx not_active IP Right Cessation
- 1994-05-06 CY CY173094A patent/CY1730A/en unknown
- 1994-07-22 SE SE9402558A patent/SE519137C2/sv unknown
2004
- 2004-09-24 US US10/948,188 patent/US20050059694A1/en not_active Abandoned

Also Published As

Publication number	Publication date
JPH01157913A (ja)	1989-06-21
EP0596541A1 (en)	1994-05-11
EP0315978A3 (en)	1990-06-13
EP0315978A2 (en)	1989-05-17
NL8802734A (nl)	1989-06-01
SE8804036L (sv)	1989-05-10
DK620388A (da)	1989-05-10
US20050059694A1 (en)	2005-03-17
KR890007736A (ko)	1989-07-05
PH26083A (en)	1992-02-06
AU619772B2 (en)	1992-02-06
CY1730A (en)	1994-05-06
JP2604834B2 (ja)	1997-04-30
GB2212061A (en)	1989-07-19
NL195077C (nl)	2003-07-23
GB2212061B (en)	1991-08-28
KR0133916B1 (ko)	1998-04-22
EP0596541B1 (en)	2000-03-15
SE503236C2 (sv)	1996-04-22
SE8804036D0 (sv)	1988-11-08
GB8826066D0 (en)	1988-12-14
CH677448A5 (2)	1991-05-31
DK620388D0 (da)	1988-11-07
SE519137C2 (sv)	2003-01-21
EP0315978B1 (en)	1994-10-26
AU2490288A (en)	1989-05-11
SE9402558D0 (sv)	1994-07-22
HK8694A (en)	1994-02-04

Legal Events

Date	Code	Title	Description
1993-02-22	AHB	Application shelved due to non-payment
2008-11-24	PUP	Patent expired

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DK175235B1 (da)	2004-07-19	Ny anvendelse af azatricycloderivater og farmaceutiske præparater med indhold deraf
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DE3844904C2 (de)	1997-01-30	Neue Verwendung von 11,28-Dioxa-4-azatricyclo-[22.3.1.0·4·,·9·]octacos-18-en-Derivaten
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Bortel-Badura et al.	1992	The catalepsy in rats during chronic treatment with atypical neuroleptics; The different testing procedures