JP2008543795A - Ｃｃｒ１アンタゴニストとしての８−アザビシクロ［３．２．１］オクト−３−イルのｎ−アミド誘導体 - Google Patents
Ｃｃｒ１アンタゴニストとしての８−アザビシクロ［３．２．１］オクト−３−イルのｎ−アミド誘導体 Download PDFInfo
- Publication number
- JP2008543795A JP2008543795A JP2008516161A JP2008516161A JP2008543795A JP 2008543795 A JP2008543795 A JP 2008543795A JP 2008516161 A JP2008516161 A JP 2008516161A JP 2008516161 A JP2008516161 A JP 2008516161A JP 2008543795 A JP2008543795 A JP 2008543795A
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- JP
- Japan
- Prior art keywords
- azabicyclo
- octane
- endo
- chlorobenzyl
- ylamino
- Prior art date
- Legal status (The legal status 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 status listed.)
- Withdrawn
Links
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- 239000003446 ligand Substances 0.000 claims abstract description 5
- 150000001875 compounds Chemical class 0.000 claims description 421
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- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims description 126
- 238000000034 method Methods 0.000 claims description 107
- 125000006283 4-chlorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1Cl)C([H])([H])* 0.000 claims description 71
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 66
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 45
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 42
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- 125000005843 halogen group Chemical group 0.000 claims description 38
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- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims description 10
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- 125000005037 alkyl phenyl group Chemical group 0.000 claims description 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 3
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- FBOZXECLQNJBKD-ZDUSSCGKSA-N L-methotrexate Chemical compound C=1N=C2N=C(N)N=C(N)C2=NC=1CN(C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 FBOZXECLQNJBKD-ZDUSSCGKSA-N 0.000 claims description 2
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- FHEAIOHRHQGZPC-KIWGSFCNSA-N acetic acid;(2s)-2-amino-3-(4-hydroxyphenyl)propanoic acid;(2s)-2-aminopentanedioic acid;(2s)-2-aminopropanoic acid;(2s)-2,6-diaminohexanoic acid Chemical compound CC(O)=O.C[C@H](N)C(O)=O.NCCCC[C@H](N)C(O)=O.OC(=O)[C@@H](N)CCC(O)=O.OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 FHEAIOHRHQGZPC-KIWGSFCNSA-N 0.000 claims description 2
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- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 claims description 2
- XXSMGPRMXLTPCZ-UHFFFAOYSA-N hydroxychloroquine Chemical compound ClC1=CC=C2C(NC(C)CCCN(CCO)CC)=CC=NC2=C1 XXSMGPRMXLTPCZ-UHFFFAOYSA-N 0.000 claims description 2
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- VHOGYURTWQBHIL-UHFFFAOYSA-N leflunomide Chemical compound O1N=CC(C(=O)NC=2C=CC(=CC=2)C(F)(F)F)=C1C VHOGYURTWQBHIL-UHFFFAOYSA-N 0.000 claims description 2
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- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- LZRDHSFPLUWYAX-UHFFFAOYSA-N tert-butyl 4-aminopiperidine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCC(N)CC1 LZRDHSFPLUWYAX-UHFFFAOYSA-N 0.000 description 1
- CKXZPVPIDOJLLM-UHFFFAOYSA-N tert-butyl n-piperidin-4-ylcarbamate Chemical compound CC(C)(C)OC(=O)NC1CCNCC1 CKXZPVPIDOJLLM-UHFFFAOYSA-N 0.000 description 1
- YJBKVPRVZAQTPY-UHFFFAOYSA-J tetrachlorostannane;dihydrate Chemical compound O.O.Cl[Sn](Cl)(Cl)Cl YJBKVPRVZAQTPY-UHFFFAOYSA-J 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 238000002054 transplantation Methods 0.000 description 1
- 230000032258 transport Effects 0.000 description 1
- 230000003827 upregulation Effects 0.000 description 1
- 239000003643 water by type Substances 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
- C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
-
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- 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
- A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
-
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- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P25/22—Anxiolytics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- 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]
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
- A61P33/06—Antimalarials
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
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- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Pulmonology (AREA)
- Oncology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Communicable Diseases (AREA)
- Virology (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Psychiatry (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- AIDS & HIV (AREA)
- Gastroenterology & Hepatology (AREA)
- Molecular Biology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Transplantation (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ES200501431A ES2277745B1 (es) | 2005-06-14 | 2005-06-14 | Derivados n-amida de 8-azabiciclo /3.2.1/oct-3-ilo como antagonistas de ccr1. |
| PCT/EP2006/005129 WO2006133802A1 (en) | 2005-06-14 | 2006-05-30 | N-amide derivatives of 8-azabicyclo[3.2.1]oct-3-yl as ccr1 antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008543795A true JP2008543795A (ja) | 2008-12-04 |
| JP2008543795A5 JP2008543795A5 (enExample) | 2009-06-04 |
Family
ID=35740673
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008516161A Withdrawn JP2008543795A (ja) | 2005-06-14 | 2006-05-30 | Ｃｃｒ１アンタゴニストとしての８−アザビシクロ［３．２．１］オクト−３−イルのｎ−アミド誘導体 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US20090130090A1 (enExample) |
| EP (1) | EP1891064B1 (enExample) |
| JP (1) | JP2008543795A (enExample) |
| CN (1) | CN101228158A (enExample) |
| AR (1) | AR057651A1 (enExample) |
| AT (1) | ATE441647T1 (enExample) |
| DE (1) | DE602006008937D1 (enExample) |
| ES (2) | ES2277745B1 (enExample) |
| PE (1) | PE20070017A1 (enExample) |
| TW (1) | TW200716626A (enExample) |
| UY (1) | UY29572A1 (enExample) |
| WO (1) | WO2006133802A1 (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1994003A4 (en) * | 2006-03-07 | 2009-12-02 | Astrazeneca Ab | PIPERIDINE DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF, THEIR USE AS THERAPEUTIC AGENTS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEY |
| MX2010011154A (es) | 2008-04-11 | 2010-12-21 | Janssen Pharmaceutica Nv | Tiazolopiridin-2-iloxi-fenilo y tiazolopirazin-2-iloxifenilaminas como moduladores de la leucotrieno a4 hidrolasa. |
| WO2010091104A1 (en) * | 2009-02-06 | 2010-08-12 | Exelixis, Inc. | Glucosylceramide synthase inhibitors |
| AU2010249041B2 (en) | 2009-05-14 | 2014-11-13 | Janssen Pharmaceutica Nv | Compounds with two fused bicyclic heteroaryl moieties as modulators of leukotriene A4 hydrolase |
| WO2011087812A1 (en) * | 2009-12-21 | 2011-07-21 | Vanderbilt University | Alkyl 3-((2-amidoethyl)amino)-8-azabicyclo[3.2.1]octane-8-carboxylate analogs as selective m1 agonists and methods of making and using same |
| EP2771484A1 (en) | 2011-10-28 | 2014-09-03 | Galderma Research & Development | New leukocyte infiltrate markers for rosacea and uses thereof |
| JP6204983B2 (ja) * | 2012-07-19 | 2017-09-27 | ヤンセン ファーマシューティカ エヌ．ベー． | Ｃｃｒ２のオクタヒドロ−シクロペンタピロリル拮抗薬 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU3633997A (en) * | 1996-07-29 | 1998-02-20 | Banyu Pharmaceutical Co., Ltd. | Chemokine receptor antagonists |
| PE20001420A1 (es) * | 1998-12-23 | 2000-12-18 | Pfizer | Moduladores de ccr5 |
| SE0200919D0 (sv) * | 2002-03-25 | 2002-03-25 | Astrazeneca Ab | Chemical compounds |
| AP2005003196A0 (en) * | 2002-07-18 | 2005-03-31 | Pfizer Prod Inc | Bicyclic piperidine derivatives as antagonists of the CCR1 chemokine receptor. |
| SE0301369D0 (sv) * | 2003-05-09 | 2003-05-09 | Astrazeneca Ab | Chemical compounds |
-
2005
- 2005-06-14 ES ES200501431A patent/ES2277745B1/es not_active Expired - Fee Related
-
2006
- 2006-05-30 US US11/921,961 patent/US20090130090A1/en not_active Abandoned
- 2006-05-30 EP EP06753965A patent/EP1891064B1/en active Active
- 2006-05-30 ES ES06753965T patent/ES2332819T3/es active Active
- 2006-05-30 JP JP2008516161A patent/JP2008543795A/ja not_active Withdrawn
- 2006-05-30 CN CNA2006800266367A patent/CN101228158A/zh active Pending
- 2006-05-30 AT AT06753965T patent/ATE441647T1/de not_active IP Right Cessation
- 2006-05-30 WO PCT/EP2006/005129 patent/WO2006133802A1/en not_active Ceased
- 2006-05-30 UY UY29572A patent/UY29572A1/es unknown
- 2006-05-30 DE DE602006008937T patent/DE602006008937D1/de active Active
- 2006-06-12 AR ARP060102442A patent/AR057651A1/es not_active Application Discontinuation
- 2006-06-12 PE PE2006000656A patent/PE20070017A1/es not_active Application Discontinuation
- 2006-06-13 TW TW095121003A patent/TW200716626A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| PE20070017A1 (es) | 2007-02-05 |
| AR057651A1 (es) | 2007-12-12 |
| ES2277745A1 (es) | 2007-07-16 |
| ATE441647T1 (de) | 2009-09-15 |
| UY29572A1 (es) | 2006-12-29 |
| EP1891064B1 (en) | 2009-09-02 |
| ES2332819T3 (es) | 2010-02-12 |
| EP1891064A1 (en) | 2008-02-27 |
| DE602006008937D1 (de) | 2009-10-15 |
| ES2277745B1 (es) | 2008-06-01 |
| TW200716626A (en) | 2007-05-01 |
| CN101228158A (zh) | 2008-07-23 |
| WO2006133802A1 (en) | 2006-12-21 |
| US20090130090A1 (en) | 2009-05-21 |
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