ATE389642T1 - Makrozyklische verbindungen mit asparaginproteasehemmender wirkung und deren pharmazeutische verwendung - Google Patents

Makrozyklische verbindungen mit asparaginproteasehemmender wirkung und deren pharmazeutische verwendung

Info

Publication number: ATE389642T1
Authority: AT; Austria
Prior art keywords: sub; alkyl; cycloalkyl; alkylen; hydrogen
Prior art date: 2003-07-03

Application number

AT04740596T

Other languages

English (en)

Inventor

Claudia Betschart

Marina Tintelnot-Blomley

Original Assignee

Novartis Pharma Gmbh

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.)

2003-07-03

Filing date

2004-07-02

Publication date

2008-04-15

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=27741562&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ATE389642(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

2004-07-02 Application filed by Novartis Pharma Gmbh filed Critical Novartis Pharma Gmbh

2008-04-15 Application granted granted Critical

2008-04-15 Publication of ATE389642T1 publication Critical patent/ATE389642T1/de

Links

150000002678 macrocyclic compounds Chemical class 0.000 title abstract 2
DCXYFEDJOCDNAF-UHFFFAOYSA-N Asparagine Natural products OC(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-N 0.000 title 1
DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 title 1
108091005804 Peptidases Proteins 0.000 title 1
239000004365 Protease Substances 0.000 title 1
102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 title 1
229960001230 asparagine Drugs 0.000 title 1
235000009582 asparagine Nutrition 0.000 title 1
230000002401 inhibitory effect Effects 0.000 title 1
125000000217 alkyl group Chemical group 0.000 abstract 11
125000000753 cycloalkyl group Chemical group 0.000 abstract 4
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 3
229910052739 hydrogen Inorganic materials 0.000 abstract 3
239000001257 hydrogen Substances 0.000 abstract 3
IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 3
150000001370 alpha-amino acid derivatives Chemical class 0.000 abstract 2
235000008206 alpha-amino acids Nutrition 0.000 abstract 2
125000003118 aryl group Chemical group 0.000 abstract 2
125000001072 heteroaryl group Chemical group 0.000 abstract 2
125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
229910052757 nitrogen Inorganic materials 0.000 abstract 2
-1 piperidino, pyrrolidinyl Chemical group 0.000 abstract 2
102000013455 Amyloid beta-Peptides Human genes 0.000 abstract 1
108010090849 Amyloid beta-Peptides Proteins 0.000 abstract 1
208000012902 Nervous system disease Diseases 0.000 abstract 1
208000025966 Neurological disease Diseases 0.000 abstract 1
238000004220 aggregation Methods 0.000 abstract 1
230000002776 aggregation Effects 0.000 abstract 1
125000003342 alkenyl group Chemical group 0.000 abstract 1
125000003545 alkoxy group Chemical group 0.000 abstract 1
125000004414 alkyl thio group Chemical group 0.000 abstract 1
125000005529 alkyleneoxy group Chemical group 0.000 abstract 1
125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 abstract 1
229910002091 carbon monoxide Inorganic materials 0.000 abstract 1
125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 abstract 1
150000001875 compounds Chemical class 0.000 abstract 1
229910052736 halogen Inorganic materials 0.000 abstract 1
150000002367 halogens Chemical class 0.000 abstract 1
238000000034 method Methods 0.000 abstract 1
125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 abstract 1
125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 abstract 1
230000000926 neurological effect Effects 0.000 abstract 1
QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
229910052760 oxygen Inorganic materials 0.000 abstract 1
239000008194 pharmaceutical composition Substances 0.000 abstract 1
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
125000004193 piperazinyl group Chemical group 0.000 abstract 1
125000003386 piperidinyl group Chemical group 0.000 abstract 1
125000000719 pyrrolidinyl group Chemical group 0.000 abstract 1
229910052717 sulfur Inorganic materials 0.000 abstract 1
208000019553 vascular disease Diseases 0.000 abstract 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- 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
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
- 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
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D273/00—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
- C07D273/02—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00 having two nitrogen atoms and only one oxygen atom
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D291/00—Heterocyclic compounds containing rings having nitrogen, oxygen and sulfur atoms as the only ring hetero atoms
- C07D291/08—Heterocyclic compounds containing rings having nitrogen, oxygen and sulfur atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
Animal Behavior & Ethology (AREA)
Pharmacology & Pharmacy (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Neurosurgery (AREA)
Biomedical Technology (AREA)
Neurology (AREA)
Heart & Thoracic Surgery (AREA)
Cardiology (AREA)
Epidemiology (AREA)
Vascular Medicine (AREA)
Psychiatry (AREA)
Hospice & Palliative Care (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

AT04740596T 2003-07-03 2004-07-02 Makrozyklische verbindungen mit asparaginproteasehemmender wirkung und deren pharmazeutische verwendung ATE389642T1 (de)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
GBGB0315654.4A GB0315654D0 (en)	2003-07-03	2003-07-03	Organic compounds

Publications (1)

Publication Number	Publication Date
ATE389642T1 true ATE389642T1 (de)	2008-04-15

Family

ID=27741562

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
AT04740596T ATE389642T1 (de)	2003-07-03	2004-07-02	Makrozyklische verbindungen mit asparaginproteasehemmender wirkung und deren pharmazeutische verwendung

Country Status (15)

Country	Link
US (2)	US20060223745A1 (de)
EP (1)	EP1654241B1 (de)
JP (1)	JP2009513510A (de)
CN (1)	CN1809542A (de)
AT (1)	ATE389642T1 (de)
AU (1)	AU2004253667B2 (de)
BR (1)	BRPI0412286A (de)
CA (1)	CA2529571A1 (de)
DE (1)	DE602004012572T2 (de)
ES (1)	ES2300790T3 (de)
GB (1)	GB0315654D0 (de)
MX (1)	MXPA05014011A (de)
PL (1)	PL1654241T3 (de)
PT (1)	PT1654241E (de)
WO (1)	WO2005003106A1 (de)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
BRPI0606636A2 (pt) *	2005-01-13	2009-07-07	Novartis Ag	compostos macrocìclicos úteis como inibidores de bace
GB0500683D0 (en) *	2005-01-13	2005-02-23	Novartis Ag	Organic compounds
CA2609562A1 (en)	2005-06-14	2006-12-28	Schering Corporation	Macrocyclic heterocyclic aspartyl protease inhibitors
GB0526614D0 (en)	2005-12-30	2006-02-08	Novartis Ag	Organic compounds
CN107849026B (zh)	2015-07-29	2021-01-01	百时美施贵宝公司	携带烷基或环烷基p2′部分的因子xia大环抑制剂

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US6184241B1 (en) *	1998-08-24	2001-02-06	Kansas State University Research Foundation	Aspartic protease inhibitors

2003
- 2003-07-03 GB GBGB0315654.4A patent/GB0315654D0/en not_active Ceased
2004
- 2004-07-02 JP JP2006518098A patent/JP2009513510A/ja active Pending
- 2004-07-02 CA CA002529571A patent/CA2529571A1/en not_active Abandoned
- 2004-07-02 PT PT04740596T patent/PT1654241E/pt unknown
- 2004-07-02 ES ES04740596T patent/ES2300790T3/es not_active Expired - Lifetime
- 2004-07-02 EP EP04740596A patent/EP1654241B1/de not_active Expired - Lifetime
- 2004-07-02 CN CNA2004800174050A patent/CN1809542A/zh active Pending
- 2004-07-02 AU AU2004253667A patent/AU2004253667B2/en not_active Ceased
- 2004-07-02 BR BRPI0412286-0A patent/BRPI0412286A/pt not_active IP Right Cessation
- 2004-07-02 US US10/561,949 patent/US20060223745A1/en not_active Abandoned
- 2004-07-02 DE DE602004012572T patent/DE602004012572T2/de not_active Expired - Lifetime
- 2004-07-02 MX MXPA05014011A patent/MXPA05014011A/es active IP Right Grant
- 2004-07-02 AT AT04740596T patent/ATE389642T1/de not_active IP Right Cessation
- 2004-07-02 PL PL04740596T patent/PL1654241T3/pl unknown
- 2004-07-02 WO PCT/EP2004/007247 patent/WO2005003106A1/en not_active Ceased
2007
- 2007-11-14 US US11/939,936 patent/US20080070885A1/en not_active Abandoned

Also Published As

Publication number	Publication date
AU2004253667B2 (en)	2008-12-18
WO2005003106A1 (en)	2005-01-13
AU2004253667A1 (en)	2005-01-13
US20060223745A1 (en)	2006-10-05
GB0315654D0 (en)	2003-08-13
HK1090366A1 (en)	2006-12-22
CN1809542A (zh)	2006-07-26
EP1654241B1 (de)	2008-03-19
EP1654241A1 (de)	2006-05-10
JP2009513510A (ja)	2009-04-02
BRPI0412286A (pt)	2006-09-19
ES2300790T3 (es)	2008-06-16
MXPA05014011A (es)	2006-03-02
US20080070885A1 (en)	2008-03-20
DE602004012572T2 (de)	2009-04-16
PL1654241T3 (pl)	2008-09-30
CA2529571A1 (en)	2005-01-13
PT1654241E (pt)	2008-06-03
DE602004012572D1 (de)	2008-04-30

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2008-10-15

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