JP2012524107A5 - - Google Patents
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- Publication number
- JP2012524107A5 JP2012524107A5 JP2012506216A JP2012506216A JP2012524107A5 JP 2012524107 A5 JP2012524107 A5 JP 2012524107A5 JP 2012506216 A JP2012506216 A JP 2012506216A JP 2012506216 A JP2012506216 A JP 2012506216A JP 2012524107 A5 JP2012524107 A5 JP 2012524107A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- group
- pyridyl
- optionally
- 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 43
- -1 pyridyl-N-oxide Chemical group 0.000 claims 32
- 150000001875 compounds Chemical class 0.000 claims 26
- 125000004432 carbon atom Chemical group C* 0.000 claims 20
- 229910052799 carbon Inorganic materials 0.000 claims 19
- 125000000335 thiazolyl group Chemical group 0.000 claims 16
- 125000004076 pyridyl group Chemical group 0.000 claims 15
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 15
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 11
- 125000001424 substituent group Chemical group 0.000 claims 11
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 10
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 10
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims 9
- 239000000651 prodrug Substances 0.000 claims 8
- 229940002612 prodrug Drugs 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 239000012453 solvate Substances 0.000 claims 8
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 7
- 208000035475 disorder Diseases 0.000 claims 6
- 208000006673 asthma Diseases 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 5
- 125000001041 indolyl group Chemical group 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000003373 pyrazinyl group Chemical group 0.000 claims 5
- 208000011580 syndromic disease Diseases 0.000 claims 5
- 102100021943 C-C motif chemokine 2 Human genes 0.000 claims 4
- 101710155857 C-C motif chemokine 2 Proteins 0.000 claims 4
- 208000008589 Obesity Diseases 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 235000020824 obesity Nutrition 0.000 claims 4
- 125000001544 thienyl group Chemical group 0.000 claims 4
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 4
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 125000002883 imidazolyl group Chemical group 0.000 claims 3
- 125000001786 isothiazolyl group Chemical group 0.000 claims 3
- 125000002971 oxazolyl group Chemical group 0.000 claims 3
- 239000000825 pharmaceutical preparation Substances 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000003226 pyrazolyl group Chemical group 0.000 claims 3
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 2
- 208000002249 Diabetes Complications Diseases 0.000 claims 2
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 2
- 206010012655 Diabetic complications Diseases 0.000 claims 2
- 206010054044 Diabetic microangiopathy Diseases 0.000 claims 2
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 2
- 206010038910 Retinitis Diseases 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 201000009961 allergic asthma Diseases 0.000 claims 2
- 125000004190 benzothiazol-2-yl group Chemical group [H]C1=C([H])C([H])=C2N=C(*)SC2=C1[H] 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 201000009101 diabetic angiopathy Diseases 0.000 claims 2
- 208000033679 diabetic kidney disease Diseases 0.000 claims 2
- 230000014509 gene expression Effects 0.000 claims 2
- 230000002018 overexpression Effects 0.000 claims 2
- LMDZBCPBFSXMTL-UHFFFAOYSA-N 1-Ethyl-3-(3-dimethylaminopropyl)carbodiimide Substances CCN=C=NCCCN(C)C LMDZBCPBFSXMTL-UHFFFAOYSA-N 0.000 claims 1
- FPQQSJJWHUJYPU-UHFFFAOYSA-N 3-(dimethylamino)propyliminomethylidene-ethylazanium;chloride Chemical compound Cl.CCN=C=NCCCN(C)C FPQQSJJWHUJYPU-UHFFFAOYSA-N 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 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
- 206010007558 Cardiac failure chronic Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010056370 Congestive cardiomyopathy Diseases 0.000 claims 1
- 206010010741 Conjunctivitis Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 201000010046 Dilated cardiomyopathy Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000009525 Myocarditis Diseases 0.000 claims 1
- 206010033307 Overweight Diseases 0.000 claims 1
- 206010036346 Posterior capsule opacification Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 1
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 1
- 208000001647 Renal Insufficiency Diseases 0.000 claims 1
- 206010063837 Reperfusion injury Diseases 0.000 claims 1
- 206010039085 Rhinitis allergic Diseases 0.000 claims 1
- 206010041925 Staphylococcal infections Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 206010052568 Urticaria chronic Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 206010046851 Uveitis Diseases 0.000 claims 1
- 206010057469 Vascular stenosis Diseases 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 201000010105 allergic rhinitis Diseases 0.000 claims 1
- 230000007815 allergy Effects 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 239000003638 chemical reducing agent Substances 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000024376 chronic urticaria Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 208000030533 eye disease Diseases 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 208000024693 gingival disease Diseases 0.000 claims 1
- 208000007565 gingivitis Diseases 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- NPZTUJOABDZTLV-UHFFFAOYSA-N hydroxybenzotriazole Substances O=C1C=CC=C2NNN=C12 NPZTUJOABDZTLV-UHFFFAOYSA-N 0.000 claims 1
- 230000004968 inflammatory condition Effects 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 201000006370 kidney failure Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 230000003211 malignant effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 201000000050 myeloid neoplasm Diseases 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 201000008383 nephritis Diseases 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 235000020825 overweight Nutrition 0.000 claims 1
- 208000028169 periodontal disease Diseases 0.000 claims 1
- 201000001245 periodontitis Diseases 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 201000000306 sarcoidosis Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 238000001356 surgical procedure Methods 0.000 claims 1
- 201000008827 tuberculosis Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US16987609P | 2009-04-16 | 2009-04-16 | |
| US61/169,876 | 2009-04-16 | ||
| PCT/US2010/031212 WO2010121011A1 (en) | 2009-04-16 | 2010-04-15 | 4-azetidinyl-1-heteroaryl-cyclohexane antagonists of ccr2 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012524107A JP2012524107A (ja) | 2012-10-11 |
| JP2012524107A5 true JP2012524107A5 (enExample) | 2013-05-30 |
| JP5685580B2 JP5685580B2 (ja) | 2015-03-18 |
Family
ID=42154522
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012506216A Expired - Fee Related JP5685580B2 (ja) | 2009-04-16 | 2010-04-15 | Ｃｃｒ２の４−アゼチジニル−１−ヘテロアリール−シクロヘキサンアンタゴニスト |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US8269015B2 (enExample) |
| EP (1) | EP2419417B1 (enExample) |
| JP (1) | JP5685580B2 (enExample) |
| KR (1) | KR20120061060A (enExample) |
| CN (1) | CN102459225B (enExample) |
| AR (1) | AR076310A1 (enExample) |
| AU (1) | AU2010236393B2 (enExample) |
| BR (1) | BRPI1016207A2 (enExample) |
| CA (1) | CA2758918A1 (enExample) |
| ES (1) | ES2539161T3 (enExample) |
| MX (1) | MX2011010919A (enExample) |
| NZ (1) | NZ595431A (enExample) |
| TW (1) | TW201105649A (enExample) |
| WO (1) | WO2010121011A1 (enExample) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2745969C (en) * | 2008-12-10 | 2017-04-25 | Janssen Pharmaceutica Nv | 4-azetidinyl-1-heteroaryl-cyclohexanol antagonists of ccr2 |
| ES2528625T3 (es) * | 2009-04-17 | 2015-02-11 | Janssen Pharmaceutica Nv | Antagonistas de 4-azetidinil-1-fenil-ciclohexano de CCR2 |
| CA2758929A1 (en) | 2009-04-17 | 2010-10-21 | Janssen Pharmaceutica Nv | 4-azetidinyl-1-heteroatom linked-cyclohexane antagonists of ccr2 |
| TW201211027A (en) * | 2010-06-09 | 2012-03-16 | Janssen Pharmaceutica Nv | Cyclohexyl-azetidinyl antagonists of CCR2 |
| WO2011159854A1 (en) | 2010-06-17 | 2011-12-22 | Janssen Pharmaceutica Nv | Cyclohexyl-azetidinyl antagonists of ccr2 |
| CA2852160A1 (en) | 2011-10-28 | 2013-05-02 | Galderma Research & Development | New leukocyte infiltrate markers for rosacea and uses thereof |
| RU2726206C2 (ru) | 2015-05-21 | 2020-07-09 | Кемосентрикс, Инк. | Модуляторы ccr2 |
| EP3687525B1 (en) | 2017-09-25 | 2025-10-29 | ChemoCentryx, Inc. | Combination therapy using a chemokine receptor 2 (ccr2) antagonist and a pd-1/pd-l1 inhibitor |
| CN112105353B (zh) | 2018-01-08 | 2024-04-19 | 凯莫森特里克斯股份有限公司 | Ccr2拮抗剂治疗实体瘤的方法 |
| US20190269664A1 (en) | 2018-01-08 | 2019-09-05 | Chemocentryx, Inc. | Methods of treating solid tumors with ccr2 antagonists |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6037354A (en) | 1997-06-18 | 2000-03-14 | Merck & Co., Inc. | Alpha 1a adrenergic receptor antagonists |
| CA2378499A1 (en) | 1999-08-04 | 2001-02-15 | Teijin Limited | Cyclic amine ccr3 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 |
| 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 |
| WO2004050024A2 (en) * | 2002-11-27 | 2004-06-17 | Incyte Corporation | 3-aminopyrrolidine derivatives as modulators of chemokine receptors |
| GB0417801D0 (en) * | 2004-08-10 | 2004-09-15 | Novartis Ag | Organic compounds |
| KR20070063562A (ko) | 2004-09-28 | 2007-06-19 | 얀센 파마슈티카 엔.브이. | 치환 디피페리딘 ｃｃｒ２ 길항제 |
| PA8653301A1 (es) | 2004-11-22 | 2006-11-09 | Incyte Corp Incyte Corp | Sales de la n-[2-({(3r)-1-[trans-4-hidroxi-4-(6-metoxipiridin-3-il) ciclohexil)pirrolidin |
| US8067457B2 (en) | 2005-11-01 | 2011-11-29 | Millennium Pharmaceuticals, Inc. | Compounds useful as antagonists of CCR2 |
| US20070197590A1 (en) | 2006-01-31 | 2007-08-23 | Demong Duane E | Substituted dipiperidine ccr2 antagonists |
| AU2008335135A1 (en) * | 2007-12-11 | 2009-06-18 | Cytopathfinder, Inc. | Carboxamide compounds and their use as chemokine receptor agonists |
| CA2745969C (en) * | 2008-12-10 | 2017-04-25 | Janssen Pharmaceutica Nv | 4-azetidinyl-1-heteroaryl-cyclohexanol antagonists of ccr2 |
| CA2758929A1 (en) | 2009-04-17 | 2010-10-21 | Janssen Pharmaceutica Nv | 4-azetidinyl-1-heteroatom linked-cyclohexane antagonists of ccr2 |
| ES2528625T3 (es) | 2009-04-17 | 2015-02-11 | Janssen Pharmaceutica Nv | Antagonistas de 4-azetidinil-1-fenil-ciclohexano de CCR2 |
-
2010
- 2010-04-15 NZ NZ595431A patent/NZ595431A/en not_active IP Right Cessation
- 2010-04-15 JP JP2012506216A patent/JP5685580B2/ja not_active Expired - Fee Related
- 2010-04-15 WO PCT/US2010/031212 patent/WO2010121011A1/en not_active Ceased
- 2010-04-15 EP EP10714148.3A patent/EP2419417B1/en active Active
- 2010-04-15 AU AU2010236393A patent/AU2010236393B2/en not_active Ceased
- 2010-04-15 KR KR1020117026815A patent/KR20120061060A/ko not_active Withdrawn
- 2010-04-15 TW TW099111730A patent/TW201105649A/zh unknown
- 2010-04-15 AR ARP100101263A patent/AR076310A1/es unknown
- 2010-04-15 CA CA2758918A patent/CA2758918A1/en not_active Abandoned
- 2010-04-15 MX MX2011010919A patent/MX2011010919A/es active IP Right Grant
- 2010-04-15 BR BRPI1016207A patent/BRPI1016207A2/pt not_active Application Discontinuation
- 2010-04-15 US US12/760,832 patent/US8269015B2/en not_active Expired - Fee Related
- 2010-04-15 CN CN201080027215.2A patent/CN102459225B/zh not_active Expired - Fee Related
- 2010-04-15 ES ES10714148.3T patent/ES2539161T3/es active Active
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