JP2013514302A5 - - Google Patents
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- JP2013514302A5 JP2013514302A5 JP2012543668A JP2012543668A JP2013514302A5 JP 2013514302 A5 JP2013514302 A5 JP 2013514302A5 JP 2012543668 A JP2012543668 A JP 2012543668A JP 2012543668 A JP2012543668 A JP 2012543668A JP 2013514302 A5 JP2013514302 A5 JP 2013514302A5
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- JP
- Japan
- Prior art keywords
- alkyl
- alkylene
- ring
- cycloalkyl
- groups selected
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims description 47
- 239000003814 drug Substances 0.000 claims description 25
- 208000027866 inflammatory disease Diseases 0.000 claims description 19
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 14
- 201000010099 disease Diseases 0.000 claims description 8
- 208000012902 Nervous system disease Diseases 0.000 claims description 6
- 208000025966 Neurological disease Diseases 0.000 claims description 6
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 4
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims description 4
- 208000033679 diabetic kidney disease Diseases 0.000 claims description 4
- 229910052736 halogen Inorganic materials 0.000 claims 19
- 150000002367 halogens Chemical class 0.000 claims 9
- 125000006413 ring segment Chemical group 0.000 claims 8
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 6
- 125000005842 heteroatom Chemical group 0.000 claims 5
- 238000004519 manufacturing process Methods 0.000 claims 5
- 125000003003 spiro group Chemical group 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 125000002541 furyl group Chemical group 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 239000002253 acid Substances 0.000 claims 2
- 125000004419 alkynylene group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- -1 methenylene Chemical group 0.000 claims 2
- 238000007117 Nylen reaction Methods 0.000 claims 1
- 150000007513 acids Chemical class 0.000 claims 1
- 125000004450 alkenylene group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- IYABWNGZIDDRAK-UHFFFAOYSA-N allene Chemical group C=C=C IYABWNGZIDDRAK-UHFFFAOYSA-N 0.000 claims 1
- 125000003725 azepanyl group Chemical group 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 125000005678 ethenylene group Chemical group [H]C([*:1])=C([H])[*:2] 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000005647 linker group Chemical group 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000003551 oxepanyl group Chemical group 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- RWRDLPDLKQPQOW-UHFFFAOYSA-N tetrahydropyrrole Substances C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 1
- 229940079593 drug Drugs 0.000 description 16
- 208000002193 Pain Diseases 0.000 description 10
- 208000004296 neuralgia Diseases 0.000 description 6
- 208000000094 Chronic Pain Diseases 0.000 description 4
- 208000035475 disorder Diseases 0.000 description 4
- 201000006417 multiple sclerosis Diseases 0.000 description 4
- 208000011580 syndromic disease Diseases 0.000 description 4
- 208000030507 AIDS Diseases 0.000 description 3
- 201000001320 Atherosclerosis Diseases 0.000 description 3
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 description 3
- 201000003883 Cystic fibrosis Diseases 0.000 description 3
- 206010065390 Inflammatory pain Diseases 0.000 description 3
- 208000006673 asthma Diseases 0.000 description 3
- 206010012601 diabetes mellitus Diseases 0.000 description 3
- 230000002757 inflammatory effect Effects 0.000 description 3
- 208000021722 neuropathic pain Diseases 0.000 description 3
- 208000027753 pain disease Diseases 0.000 description 3
- 230000002093 peripheral effect Effects 0.000 description 3
- 208000007848 Alcoholism Diseases 0.000 description 2
- 206010003591 Ataxia Diseases 0.000 description 2
- 208000015879 Cerebellar disease Diseases 0.000 description 2
- 206010012289 Dementia Diseases 0.000 description 2
- 208000004454 Hyperalgesia Diseases 0.000 description 2
- 208000016285 Movement disease Diseases 0.000 description 2
- 208000003954 Spinal Muscular Atrophies of Childhood Diseases 0.000 description 2
- 208000027418 Wounds and injury Diseases 0.000 description 2
- 208000018254 acute transverse myelitis Diseases 0.000 description 2
- 208000018300 basal ganglia disease Diseases 0.000 description 2
- 210000003169 central nervous system Anatomy 0.000 description 2
- 208000025434 cerebellar degeneration Diseases 0.000 description 2
- 230000006378 damage Effects 0.000 description 2
- 230000007850 degeneration Effects 0.000 description 2
- 208000014674 injury Diseases 0.000 description 2
- 230000003902 lesion Effects 0.000 description 2
- 230000001537 neural effect Effects 0.000 description 2
- 210000002345 respiratory system Anatomy 0.000 description 2
- 208000009174 transverse myelitis Diseases 0.000 description 2
- 208000024827 Alzheimer disease Diseases 0.000 description 1
- 206010003694 Atrophy Diseases 0.000 description 1
- 208000008035 Back Pain Diseases 0.000 description 1
- YNQLUTRBYVCPMQ-UHFFFAOYSA-N CCc1ccccc1 Chemical compound CCc1ccccc1 YNQLUTRBYVCPMQ-UHFFFAOYSA-N 0.000 description 1
- 206010064012 Central pain syndrome Diseases 0.000 description 1
- 206010008748 Chorea Diseases 0.000 description 1
- 208000020406 Creutzfeldt Jacob disease Diseases 0.000 description 1
- 208000003407 Creutzfeldt-Jakob Syndrome Diseases 0.000 description 1
- 208000010859 Creutzfeldt-Jakob disease Diseases 0.000 description 1
- 206010067889 Dementia with Lewy bodies Diseases 0.000 description 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 description 1
- 102000015554 Dopamine receptor Human genes 0.000 description 1
- 108050004812 Dopamine receptor Proteins 0.000 description 1
- 201000010374 Down Syndrome Diseases 0.000 description 1
- 208000024412 Friedreich ataxia Diseases 0.000 description 1
- 206010019196 Head injury Diseases 0.000 description 1
- 208000023105 Huntington disease Diseases 0.000 description 1
- 208000035154 Hyperesthesia Diseases 0.000 description 1
- 208000006264 Korsakoff syndrome Diseases 0.000 description 1
- 102000007330 LDL Lipoproteins Human genes 0.000 description 1
- 108010007622 LDL Lipoproteins Proteins 0.000 description 1
- 208000009829 Lewy Body Disease Diseases 0.000 description 1
- 206010024626 Lipoprotein deficiency Diseases 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 208000019695 Migraine disease Diseases 0.000 description 1
- 208000001738 Nervous System Trauma Diseases 0.000 description 1
- 206010033425 Pain in extremity Diseases 0.000 description 1
- 208000018737 Parkinson disease Diseases 0.000 description 1
- 206010036105 Polyneuropathy Diseases 0.000 description 1
- 206010036376 Postherpetic Neuralgia Diseases 0.000 description 1
- 208000004550 Postoperative Pain Diseases 0.000 description 1
- 208000012287 Prolapse Diseases 0.000 description 1
- 208000032225 Proximal spinal muscular atrophy type 1 Diseases 0.000 description 1
- 208000033526 Proximal spinal muscular atrophy type 3 Diseases 0.000 description 1
- 208000037065 Subacute sclerosing leukoencephalitis Diseases 0.000 description 1
- 206010042297 Subacute sclerosing panencephalitis Diseases 0.000 description 1
- 206010043189 Telangiectasia Diseases 0.000 description 1
- 201000008485 Wernicke-Korsakoff syndrome Diseases 0.000 description 1
- 201000007930 alcohol dependence Diseases 0.000 description 1
- 206010053552 allodynia Diseases 0.000 description 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 description 1
- 210000002226 anterior horn cell Anatomy 0.000 description 1
- 230000037444 atrophy Effects 0.000 description 1
- 210000004227 basal ganglia Anatomy 0.000 description 1
- 208000003295 carpal tunnel syndrome Diseases 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 230000002490 cerebral effect Effects 0.000 description 1
- 238000002512 chemotherapy Methods 0.000 description 1
- 230000001054 cortical effect Effects 0.000 description 1
- 230000002594 corticospinal effect Effects 0.000 description 1
- 230000006735 deficit Effects 0.000 description 1
- 230000003210 demyelinating effect Effects 0.000 description 1
- 208000012285 hip pain Diseases 0.000 description 1
- 201000004815 juvenile spinal muscular atrophy Diseases 0.000 description 1
- 238000011542 limb amputation Methods 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 206010027599 migraine Diseases 0.000 description 1
- 230000002438 mitochondrial effect Effects 0.000 description 1
- 201000005518 mononeuropathy Diseases 0.000 description 1
- 230000007659 motor function Effects 0.000 description 1
- 208000028412 nervous system injury Diseases 0.000 description 1
- 230000004770 neurodegeneration Effects 0.000 description 1
- 208000015122 neurodegenerative disease Diseases 0.000 description 1
- 208000036339 neurological pain disease Diseases 0.000 description 1
- 230000002232 neuromuscular Effects 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 210000000496 pancreas Anatomy 0.000 description 1
- 230000007824 polyneuropathy Effects 0.000 description 1
- 201000002212 progressive supranuclear palsy Diseases 0.000 description 1
- 230000003252 repetitive effect Effects 0.000 description 1
- 230000000241 respiratory effect Effects 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 208000009056 telangiectasis Diseases 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 239000003053 toxin Substances 0.000 description 1
- 231100000765 toxin Toxicity 0.000 description 1
- 230000000472 traumatic effect Effects 0.000 description 1
- 206010044652 trigeminal neuralgia Diseases 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09179567 | 2009-12-17 | ||
| EP09179567.4 | 2009-12-17 | ||
| EP10162624 | 2010-05-12 | ||
| EP10162624.0 | 2010-05-12 | ||
| PCT/EP2010/069550 WO2011073155A1 (en) | 2009-12-17 | 2010-12-13 | Novel antagonists for ccr2 and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013514302A JP2013514302A (ja) | 2013-04-25 |
| JP2013514302A5 true JP2013514302A5 (https=) | 2014-11-06 |
| JP5658272B2 JP5658272B2 (ja) | 2015-01-21 |
Family
ID=43532680
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012543668A Active JP5658272B2 (ja) | 2009-12-17 | 2010-12-13 | Ｃｃｒ２の新規アンタゴニスト及びこれらの使用 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US20130143905A1 (https=) |
| EP (1) | EP2513086B1 (https=) |
| JP (1) | JP5658272B2 (https=) |
| WO (1) | WO2011073155A1 (https=) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2687931C (en) | 2007-05-31 | 2016-05-24 | Boehringer Ingelheim International Gmbh | Ccr2 receptor antagonists and uses thereof |
| HUE025547T2 (en) * | 2008-12-19 | 2016-02-29 | Boehringer Ingelheim Int | Cyclic pyrimidine-4-carboxamides as CCR2 receptor antagonists for the treatment of inflammation, asthma and COPD |
| ES2674275T3 (es) | 2009-12-17 | 2018-06-28 | Centrexion Therapeutics Corporation | Antagonistas del receptor CCR2 y usos de los mismos |
| WO2011141477A1 (en) | 2010-05-12 | 2011-11-17 | Boehringer Ingelheim International Gmbh | New ccr2 receptor antagonists, method for producing the same, and use thereof as medicaments |
| EP2569298B1 (en) | 2010-05-12 | 2015-11-25 | Boehringer Ingelheim International GmbH | Novel ccr2 receptor antagonists, method for producing the same, and use thereof as medicaments |
| WO2011144501A1 (en) | 2010-05-17 | 2011-11-24 | Boehringer Ingelheim International Gmbh | Ccr2 antagonists and uses thereof |
| EP2576542B1 (en) | 2010-05-25 | 2015-04-22 | Boehringer Ingelheim International GmbH | Cyclic amide derivatives of pyridazine-3-carboxylic acids and their use in the treatment of pulmonary, pain, immune related and cardiovascular diseases |
| EP2576538B1 (en) | 2010-06-01 | 2015-10-28 | Boehringer Ingelheim International GmbH | New CCR2 antagonists |
| EP2731941B1 (en) | 2011-07-15 | 2019-05-08 | Boehringer Ingelheim International GmbH | Novel and selective ccr2 antagonists |
| CA2852160A1 (en) | 2011-10-28 | 2013-05-02 | Galderma Research & Development | New leukocyte infiltrate markers for rosacea and uses thereof |
| CN104086539A (zh) * | 2014-07-17 | 2014-10-08 | 天津炜捷制药有限公司 | 一种利伐沙班的制备方法 |
| MX383744B (es) | 2015-07-02 | 2025-03-14 | Centrexion Therapeutics Corp | Citrato de (4-((3r,4r)-3-metoxitetrahidro-piran-4-ilamino)piperidin-1-il) (5-metil-6-(((2r, 6s)-6-(p-tolil)tetrahidro-2h-piran-2-il) metilamino) pirimidin-4-il) metanona. |
| CN114349728A (zh) * | 2020-10-12 | 2022-04-15 | 南京药石科技股份有限公司 | （3r，4r）-4-氨基四氢吡喃-3-醇及其盐的制备方法 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2371583C (en) * | 1999-05-04 | 2005-09-13 | Schering Corporation | Piperazine derivatives useful as ccr5 antagonists |
| GB0004153D0 (en) | 2000-02-23 | 2000-04-12 | Astrazeneca Uk Ltd | Novel use |
| CN100519558C (zh) | 2000-10-12 | 2009-07-29 | 贝林格尔英格海姆法玛两合公司 | 结晶单水合物、其制备方法及其在制备药物组合中的用途 |
| AR035700A1 (es) | 2001-05-08 | 2004-06-23 | Astrazeneca Ab | Derivados de arilheteroalquilamina, composicion farmaceutica, usos de estos derivados para la fabricacion de medicamentos, metodos de tratamiento, y proceso para la preparacion de estos derivados |
| CZ302786B6 (cs) | 2001-06-22 | 2011-11-09 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Krystalický bezvodý tiotropiumbromid, zpusob jeho výroby a jeho použití pro výrobu léciva pro lécbu asthmatu |
| AU2002363236A1 (en) * | 2001-10-30 | 2003-05-12 | Millennium Pharmaceuticals, Inc. | Compounds, pharmaceutical compositions and methods of use therefor |
| SE0203304D0 (sv) | 2002-11-07 | 2002-11-07 | Astrazeneca Ab | Novel Coumpounds |
| WO2004074438A2 (en) * | 2003-02-14 | 2004-09-02 | Smithkline Beecham Corporation | Ccr8 antagonists |
| WO2006004741A2 (en) * | 2004-06-28 | 2006-01-12 | Incyte Corporation | 3-aminocyclopentanecarboxamides as modulators of chemokine receptors |
| CN101801952A (zh) * | 2007-10-01 | 2010-08-11 | 弗·哈夫曼-拉罗切有限公司 | 用作ccr受体拮抗剂的n-杂环联芳基甲酰胺类化合物 |
| MX2010003868A (es) | 2007-10-09 | 2010-04-27 | Hoffmann La Roche | Cis-imidazolinas quirales. |
| HUE025547T2 (en) * | 2008-12-19 | 2016-02-29 | Boehringer Ingelheim Int | Cyclic pyrimidine-4-carboxamides as CCR2 receptor antagonists for the treatment of inflammation, asthma and COPD |
-
2010
- 2010-12-13 US US13/515,852 patent/US20130143905A1/en not_active Abandoned
- 2010-12-13 WO PCT/EP2010/069550 patent/WO2011073155A1/en not_active Ceased
- 2010-12-13 EP EP20100796008 patent/EP2513086B1/en active Active
- 2010-12-13 JP JP2012543668A patent/JP5658272B2/ja active Active
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