JP2012524110A5 - - Google Patents
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- Publication number
- JP2012524110A5 JP2012524110A5 JP2012506227A JP2012506227A JP2012524110A5 JP 2012524110 A5 JP2012524110 A5 JP 2012524110A5 JP 2012506227 A JP2012506227 A JP 2012506227A JP 2012506227 A JP2012506227 A JP 2012506227A JP 2012524110 A5 JP2012524110 A5 JP 2012524110A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- optionally
- group
- ocf
- 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.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims 37
- -1 -O-pyridyl Chemical group 0.000 claims 13
- 150000001875 compounds Chemical class 0.000 claims 10
- 125000002962 imidazol-1-yl group Chemical group [*]N1C([H])=NC([H])=C1[H] 0.000 claims 8
- 125000004353 pyrazol-1-yl group Chemical group [H]C1=NN(*)C([H])=C1[H] 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 239000012453 solvate Substances 0.000 claims 7
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 125000004432 carbon atom Chemical group C* 0.000 claims 5
- 125000004536 indazol-1-yl group Chemical group N1(N=CC2=CC=CC=C12)* 0.000 claims 5
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 4
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 208000011580 syndromic disease Diseases 0.000 claims 3
- 125000001462 1-pyrrolyl group Chemical group [*]N1C([H])=C([H])C([H])=C1[H] 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 125000005605 benzo group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000000593 indol-1-yl group Chemical group [H]C1=C([H])C([H])=C2N([*])C([H])=C([H])C2=C1[H] 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 102100031151 C-C chemokine receptor type 2 Human genes 0.000 claims 1
- 101710149815 C-C chemokine receptor type 2 Proteins 0.000 claims 1
- 208000002249 Diabetes Complications Diseases 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 206010012655 Diabetic complications Diseases 0.000 claims 1
- 206010054044 Diabetic microangiopathy Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010038910 Retinitis Diseases 0.000 claims 1
- 201000009961 allergic asthma Diseases 0.000 claims 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 201000009101 diabetic angiopathy Diseases 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 0 CC(*)(CC1)CCC1N(C1)CC1NC(CNC(c1ccccc1)=O)=O Chemical compound CC(*)(CC1)CCC1N(C1)CC1NC(CNC(c1ccccc1)=O)=O 0.000 description 3
- KJORPCUDZBGQEI-UHFFFAOYSA-N NC(CCNN)(c(cccc1)c1N1)OC1=O Chemical compound NC(CCNN)(c(cccc1)c1N1)OC1=O KJORPCUDZBGQEI-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US17022509P | 2009-04-17 | 2009-04-17 | |
| US61/170,225 | 2009-04-17 | ||
| PCT/US2010/031255 WO2010121036A1 (en) | 2009-04-17 | 2010-04-15 | 4-azetidinyl-1-heteroatom linked-cyclohexane antagonists of ccr2 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012524110A JP2012524110A (ja) | 2012-10-11 |
| JP2012524110A5 true JP2012524110A5 (enExample) | 2013-05-09 |
| JP5685581B2 JP5685581B2 (ja) | 2015-03-18 |
Family
ID=42169493
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012506227A Expired - Fee Related JP5685581B2 (ja) | 2009-04-17 | 2010-04-15 | Ｃｃｒ２の４−アゼチジニル−１−ヘテロ原子結合シクロヘキサンアンタゴニスト |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US8324186B2 (enExample) |
| EP (1) | EP2419418B1 (enExample) |
| JP (1) | JP5685581B2 (enExample) |
| KR (1) | KR20120006051A (enExample) |
| CN (1) | CN102459226B (enExample) |
| AR (1) | AR076329A1 (enExample) |
| AU (1) | AU2010236336B2 (enExample) |
| BR (1) | BRPI1016205A2 (enExample) |
| CA (1) | CA2758929A1 (enExample) |
| ES (1) | ES2541607T3 (enExample) |
| MX (1) | MX2011010963A (enExample) |
| NZ (1) | NZ595433A (enExample) |
| TW (1) | TW201102379A (enExample) |
| WO (1) | WO2010121036A1 (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2376475B1 (en) | 2008-12-10 | 2015-09-02 | Janssen Pharmaceutica NV | 4-azetidinyl-1-heteroaryl-cyclohexanol antagonists of ccr2 |
| EP2419417B1 (en) * | 2009-04-16 | 2015-03-25 | Janssen Pharmaceutica NV | 4-azetidinyl-1-heteroaryl-cyclohexane antagonists of ccr2 |
| WO2010121036A1 (en) | 2009-04-17 | 2010-10-21 | Janssen Pharmaceutica Nv | 4-azetidinyl-1-heteroatom linked-cyclohexane antagonists of ccr2 |
| NZ595432A (en) * | 2009-04-17 | 2013-12-20 | Janssen Pharmaceutica Nv | 4-azetidinyl-1-phenyl-cyclohexane antagonists of ccr2 |
| TW201211027A (en) * | 2010-06-09 | 2012-03-16 | Janssen Pharmaceutica Nv | Cyclohexyl-azetidinyl antagonists of CCR2 |
| KR101743280B1 (ko) | 2010-06-17 | 2017-06-02 | 얀센 파마슈티카 엔.브이. | Ccr2의 사이클로헥실-아제티디닐 길항제 |
| US20140329809A1 (en) | 2011-10-28 | 2014-11-06 | Galderma Research & Development | New leukocyte infiltrate markers for rosacea and uses thereof |
| WO2015056782A1 (ja) * | 2013-10-17 | 2015-04-23 | 塩野義製薬株式会社 | 新規アルキレン誘導体 |
| US20230174633A1 (en) * | 2020-03-30 | 2023-06-08 | Memorial Sloan Kettering Cancer Center | Methods and compositions for modulating lipid storage in adipose tissue |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1998057641A1 (en) | 1997-06-18 | 1998-12-23 | Merck & Co., Inc. | ALPHA 1a ADRENERGIC RECEPTOR ANTAGONISTS |
| US6037354A (en) | 1997-06-18 | 2000-03-14 | Merck & Co., Inc. | Alpha 1a adrenergic receptor antagonists |
| EP1201239A4 (en) | 1999-08-04 | 2004-12-08 | Teijin Ltd | CCR3 CYCLIC AMINE ANTAGONISTS |
| US6245799B1 (en) | 1999-11-08 | 2001-06-12 | American Home Products Corp | [(Indol-3-yl)-cycloalkyl]-3-substituted azetidines for the treatment of central nervous system disorders |
| AU1446601A (en) | 1999-11-08 | 2001-06-06 | American Home Products Corporation | ((indol-3-yl)-cycloalkyl)-3-substituted azetidines for the treatment of central nervous system disorders |
| AR035773A1 (es) | 2000-12-20 | 2004-07-14 | Bristol Myers Squibb Pharma Co | Compuestos diamino ciclico, composicion farmaceutica y su uso en la fabricacion de un medicamento util para modular la actividad de una quimioquina |
| UA87449C2 (ru) * | 2002-11-27 | 2009-07-27 | Инсайт Корпорейшн | Производные 3-аминопиролидина как модуляторы рецепторов хемокина |
| ATE555087T1 (de) | 2002-11-27 | 2012-05-15 | Incyte Corp | 3-aminopyrrolidinderivate als modulatoren von chemokinrezeptoren |
| GB0417801D0 (en) * | 2004-08-10 | 2004-09-15 | Novartis Ag | Organic compounds |
| JP2008514700A (ja) | 2004-09-28 | 2008-05-08 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | 置換されたジピペリジンｃｃｒ２アンタゴニスト |
| UY29219A1 (es) * | 2004-11-22 | 2006-04-28 | Incyte Corp | Sales de la n-(2- (((3r)-1-(trans-4-hidroxi-4-(6-metoxipiridin-3-il)-cilohexil) pirrolidin-3-il)amino)-2-oxoetil)-3- (trifluorometil) benzamida |
| GB0513747D0 (en) | 2005-07-06 | 2005-08-10 | Merck Sharp & Dohme | Therapeutic compounds |
| WO2007053498A1 (en) | 2005-11-01 | 2007-05-10 | Millennium Pharmaceuticals, Inc. | Compounds useful as antagonists of ccr2 |
| US20070197590A1 (en) | 2006-01-31 | 2007-08-23 | Demong Duane E | Substituted dipiperidine ccr2 antagonists |
| CA2708364A1 (en) * | 2007-12-11 | 2009-06-18 | Efrat Ben-Zeev | Carboxamide compounds and their use as chemokine receptor agonists |
| EP2376475B1 (en) * | 2008-12-10 | 2015-09-02 | Janssen Pharmaceutica NV | 4-azetidinyl-1-heteroaryl-cyclohexanol antagonists of ccr2 |
| EP2419417B1 (en) | 2009-04-16 | 2015-03-25 | Janssen Pharmaceutica NV | 4-azetidinyl-1-heteroaryl-cyclohexane antagonists of ccr2 |
| WO2010121036A1 (en) | 2009-04-17 | 2010-10-21 | Janssen Pharmaceutica Nv | 4-azetidinyl-1-heteroatom linked-cyclohexane antagonists of ccr2 |
| NZ595432A (en) | 2009-04-17 | 2013-12-20 | Janssen Pharmaceutica Nv | 4-azetidinyl-1-phenyl-cyclohexane antagonists of ccr2 |
-
2010
- 2010-04-15 WO PCT/US2010/031255 patent/WO2010121036A1/en not_active Ceased
- 2010-04-15 ES ES10714151.7T patent/ES2541607T3/es active Active
- 2010-04-15 AU AU2010236336A patent/AU2010236336B2/en not_active Ceased
- 2010-04-15 US US12/760,855 patent/US8324186B2/en not_active Expired - Fee Related
- 2010-04-15 EP EP10714151.7A patent/EP2419418B1/en active Active
- 2010-04-15 KR KR1020117026820A patent/KR20120006051A/ko not_active Withdrawn
- 2010-04-15 JP JP2012506227A patent/JP5685581B2/ja not_active Expired - Fee Related
- 2010-04-15 CA CA2758929A patent/CA2758929A1/en not_active Abandoned
- 2010-04-15 BR BRPI1016205A patent/BRPI1016205A2/pt not_active Application Discontinuation
- 2010-04-15 NZ NZ595433A patent/NZ595433A/en not_active IP Right Cessation
- 2010-04-15 MX MX2011010963A patent/MX2011010963A/es active IP Right Grant
- 2010-04-15 CN CN201080027621.9A patent/CN102459226B/zh not_active Expired - Fee Related
- 2010-04-16 TW TW099111900A patent/TW201102379A/zh unknown
- 2010-04-19 AR ARP100101288A patent/AR076329A1/es unknown