JP2008540443A5 - - Google Patents
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- JP2008540443A5 JP2008540443A5 JP2008510216A JP2008510216A JP2008540443A5 JP 2008540443 A5 JP2008540443 A5 JP 2008540443A5 JP 2008510216 A JP2008510216 A JP 2008510216A JP 2008510216 A JP2008510216 A JP 2008510216A JP 2008540443 A5 JP2008540443 A5 JP 2008540443A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- compound according
- pain
- optionally
- hydrogen
- 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- Withdrawn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
- 150000001875 compounds Chemical class 0.000 claims 173
- 229910052739 hydrogen Inorganic materials 0.000 claims 50
- 239000001257 hydrogen Substances 0.000 claims 50
- -1 2 -Methyl-piperidin-1-yl Chemical group 0.000 claims 34
- 229910052757 nitrogen Inorganic materials 0.000 claims 34
- 125000005842 heteroatom Chemical group 0.000 claims 32
- 229910052760 oxygen Chemical group 0.000 claims 32
- 229910052717 sulfur Inorganic materials 0.000 claims 32
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 31
- 208000002193 Pain Diseases 0.000 claims 26
- 150000002431 hydrogen Chemical class 0.000 claims 25
- 229920006395 saturated elastomer Polymers 0.000 claims 24
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 22
- 239000001301 oxygen Chemical group 0.000 claims 22
- 239000011593 sulfur Chemical group 0.000 claims 22
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 21
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 18
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 17
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 15
- 239000000126 substance Substances 0.000 claims 15
- 125000001931 aliphatic group Chemical group 0.000 claims 12
- 125000002950 monocyclic group Chemical group 0.000 claims 12
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical group C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 10
- 125000002619 bicyclic group Chemical group 0.000 claims 8
- 229910052736 halogen Inorganic materials 0.000 claims 8
- 150000002367 halogens Chemical class 0.000 claims 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 8
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 8
- 125000001424 substituent group Chemical group 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- 208000004296 neuralgia Diseases 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 125000004429 atom Chemical group 0.000 claims 6
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims 6
- 125000005322 morpholin-1-yl group Chemical group 0.000 claims 6
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 6
- 208000005615 Interstitial Cystitis Diseases 0.000 claims 5
- 230000001154 acute effect Effects 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 208000035475 disorder Diseases 0.000 claims 5
- 229910052731 fluorine Inorganic materials 0.000 claims 5
- 208000021722 neuropathic pain Diseases 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 125000003386 piperidinyl group Chemical group 0.000 claims 5
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical group C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 125000004566 azetidin-1-yl group Chemical group N1(CCC1)* 0.000 claims 4
- 229910052794 bromium Inorganic materials 0.000 claims 4
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 4
- 229910052801 chlorine Inorganic materials 0.000 claims 4
- 230000001684 chronic effect Effects 0.000 claims 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 3
- 208000008035 Back Pain Diseases 0.000 claims 3
- 206010019233 Headaches Diseases 0.000 claims 3
- 208000004404 Intractable Pain Diseases 0.000 claims 3
- 206010028836 Neck pain Diseases 0.000 claims 3
- 208000005298 acute pain Diseases 0.000 claims 3
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 3
- 201000006417 multiple sclerosis Diseases 0.000 claims 3
- 230000002981 neuropathic effect Effects 0.000 claims 3
- 208000011580 syndromic disease Diseases 0.000 claims 3
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 3
- 208000000003 Breakthrough pain Diseases 0.000 claims 2
- 206010058019 Cancer Pain Diseases 0.000 claims 2
- 208000000094 Chronic Pain Diseases 0.000 claims 2
- 208000006561 Cluster Headache Diseases 0.000 claims 2
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 2
- 206010065390 Inflammatory pain Diseases 0.000 claims 2
- 208000019695 Migraine disease Diseases 0.000 claims 2
- 206010036376 Postherpetic Neuralgia Diseases 0.000 claims 2
- 208000004550 Postoperative Pain Diseases 0.000 claims 2
- 206010059604 Radicular pain Diseases 0.000 claims 2
- 208000008765 Sciatica Diseases 0.000 claims 2
- QXNDZONIWRINJR-UHFFFAOYSA-N azocane Chemical group C1CCCNCCC1 QXNDZONIWRINJR-UHFFFAOYSA-N 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 150000001721 carbon Chemical class 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 208000018912 cluster headache syndrome Diseases 0.000 claims 2
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 206010027599 migraine Diseases 0.000 claims 2
- 201000001119 neuropathy Diseases 0.000 claims 2
- 230000007823 neuropathy Effects 0.000 claims 2
- 208000033808 peripheral neuropathy Diseases 0.000 claims 2
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 206010044652 trigeminal neuralgia Diseases 0.000 claims 2
- 208000009935 visceral pain Diseases 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000004195 4-methylpiperazin-1-yl group Chemical group [H]C([H])([H])N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 208000004998 Abdominal Pain Diseases 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 206010003011 Appendicitis Diseases 0.000 claims 1
- 208000006820 Arthralgia Diseases 0.000 claims 1
- 206010003591 Ataxia Diseases 0.000 claims 1
- 208000009137 Behcet syndrome Diseases 0.000 claims 1
- 206010006002 Bone pain Diseases 0.000 claims 1
- 206010064012 Central pain syndrome Diseases 0.000 claims 1
- 206010008479 Chest Pain Diseases 0.000 claims 1
- 201000009273 Endometriosis Diseases 0.000 claims 1
- 206010015150 Erythema Diseases 0.000 claims 1
- 208000024720 Fabry Disease Diseases 0.000 claims 1
- 208000001640 Fibromyalgia Diseases 0.000 claims 1
- 206010019909 Hernia Diseases 0.000 claims 1
- 208000007514 Herpes zoster Diseases 0.000 claims 1
- 206010020853 Hypertonic bladder Diseases 0.000 claims 1
- 206010021639 Incontinence Diseases 0.000 claims 1
- 208000007914 Labor Pain Diseases 0.000 claims 1
- 208000035945 Labour pain Diseases 0.000 claims 1
- 206010024229 Leprosy Diseases 0.000 claims 1
- 208000008930 Low Back Pain Diseases 0.000 claims 1
- 206010026749 Mania Diseases 0.000 claims 1
- 208000016285 Movement disease Diseases 0.000 claims 1
- 208000000112 Myalgia Diseases 0.000 claims 1
- 208000005890 Neuroma Diseases 0.000 claims 1
- 208000001294 Nociceptive Pain Diseases 0.000 claims 1
- 208000009722 Overactive Urinary Bladder Diseases 0.000 claims 1
- 206010033425 Pain in extremity Diseases 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 206010033647 Pancreatitis acute Diseases 0.000 claims 1
- 208000000450 Pelvic Pain Diseases 0.000 claims 1
- 208000010886 Peripheral nerve injury Diseases 0.000 claims 1
- 208000004983 Phantom Limb Diseases 0.000 claims 1
- 206010056238 Phantom pain Diseases 0.000 claims 1
- 206010037211 Psychomotor hyperactivity Diseases 0.000 claims 1
- 206010037596 Pyelonephritis Diseases 0.000 claims 1
- 206010037779 Radiculopathy Diseases 0.000 claims 1
- 206010051496 Rhinalgia Diseases 0.000 claims 1
- 206010040037 Sensory neuropathy hereditary Diseases 0.000 claims 1
- 208000000491 Tendinopathy Diseases 0.000 claims 1
- 206010043255 Tendonitis Diseases 0.000 claims 1
- 206010043269 Tension headache Diseases 0.000 claims 1
- 208000008548 Tension-Type Headache Diseases 0.000 claims 1
- 206010046543 Urinary incontinence Diseases 0.000 claims 1
- 102000016913 Voltage-Gated Sodium Channels Human genes 0.000 claims 1
- 108010053752 Voltage-Gated Sodium Channels Proteins 0.000 claims 1
- 208000027418 Wounds and injury Diseases 0.000 claims 1
- 210000001015 abdomen Anatomy 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 208000038016 acute inflammation Diseases 0.000 claims 1
- 230000006022 acute inflammation Effects 0.000 claims 1
- 201000003229 acute pancreatitis Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 206010003119 arrhythmia Diseases 0.000 claims 1
- 230000006793 arrhythmia Effects 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- ZSIQJIWKELUFRJ-UHFFFAOYSA-N azepane Chemical group C1CCCNCC1 ZSIQJIWKELUFRJ-UHFFFAOYSA-N 0.000 claims 1
- 125000003725 azepanyl group Chemical group 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 238000002512 chemotherapy Methods 0.000 claims 1
- 201000001352 cholecystitis Diseases 0.000 claims 1
- 125000004122 cyclic group Chemical group 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
- 230000006378 damage Effects 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 231100000321 erythema Toxicity 0.000 claims 1
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 claims 1
- 210000001097 facial muscle Anatomy 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 208000037584 hereditary sensory and autonomic neuropathy Diseases 0.000 claims 1
- 201000006847 hereditary sensory neuropathy Diseases 0.000 claims 1
- 208000014674 injury Diseases 0.000 claims 1
- 208000003243 intestinal obstruction Diseases 0.000 claims 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 208000013465 muscle pain Diseases 0.000 claims 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 208000015706 neuroendocrine disease Diseases 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 208000020629 overactive bladder Diseases 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 1
- 208000001297 phlebitis Diseases 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 201000007094 prostatitis Diseases 0.000 claims 1
- 208000020016 psychiatric disease Diseases 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 238000001959 radiotherapy Methods 0.000 claims 1
- 238000002271 resection Methods 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 208000007056 sickle cell anemia Diseases 0.000 claims 1
- 208000020431 spinal cord injury Diseases 0.000 claims 1
- 208000005198 spinal stenosis Diseases 0.000 claims 1
- 230000007863 steatosis Effects 0.000 claims 1
- 231100000240 steatosis hepatitis Toxicity 0.000 claims 1
- 125000004434 sulfur atom Chemical class 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 230000002123 temporal effect Effects 0.000 claims 1
- 201000004415 tendinitis Diseases 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 1
- 208000004371 toothache Diseases 0.000 claims 1
- 230000000472 traumatic effect Effects 0.000 claims 1
- 208000026533 urinary bladder disease Diseases 0.000 claims 1
- 208000014001 urinary system disease Diseases 0.000 claims 1
- 0 CC(*)N1CC(C)(*)CNCC1 Chemical compound CC(*)N1CC(C)(*)CNCC1 0.000 description 2
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US67810405P | 2005-05-04 | 2005-05-04 | |
| PCT/US2006/017214 WO2006119451A1 (en) | 2005-05-04 | 2006-05-04 | Pyrimidines and pyrazines useful as modulators of ion channels |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008540443A JP2008540443A (ja) | 2008-11-20 |
| JP2008540443A5 true JP2008540443A5 (https=) | 2009-07-16 |
Family
ID=36874162
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008510216A Withdrawn JP2008540443A (ja) | 2005-05-04 | 2006-05-04 | イオンチャネルのモジュレーターとして有用なピリミジンおよびピラジン |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US7858786B2 (https=) |
| EP (1) | EP1877385A1 (https=) |
| JP (1) | JP2008540443A (https=) |
| WO (1) | WO2006119451A1 (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200519094A (en) * | 2003-07-02 | 2005-06-16 | Vertex Pharma | Pyrimidines useful as modulators of voltage-gated ion channels |
| JP5388574B2 (ja) * | 2005-05-31 | 2014-01-15 | バーテックス ファーマシューティカルズ インコーポレイテッド | イオンチャネルのモジュレーターとして有用なヘテロ環式類 |
| TW200728258A (en) | 2005-10-10 | 2007-08-01 | Glaxo Group Ltd | Novel compounds |
| TW200730494A (en) | 2005-10-10 | 2007-08-16 | Glaxo Group Ltd | Novel compounds |
| EP1943216B1 (en) | 2005-10-10 | 2010-06-30 | Glaxo Group Limited | Prolinamide derivatives as sodium channel modulators |
| SA08290245B1 (ar) * | 2007-04-23 | 2012-02-12 | استرازينيكا ايه بي | مشتقات كربو كساميد جديدة من -n (8-اريل رباعي هيدرو نفثالين غير متجانس- 2- يل) أو -n (5-اريل كرومان غير متجانس -3-يل) لعلاج الألم |
| EP2203436A1 (en) * | 2007-09-17 | 2010-07-07 | Neurosearch A/S | Pyrazine derivatives and their use as potassium channel modulators |
| WO2012020567A1 (en) * | 2010-08-09 | 2012-02-16 | Raqualia Pharma Inc. | Acyl piperazine derivatives as ttx-s blockers |
| AU2012318874A1 (en) * | 2011-10-06 | 2014-05-15 | Merck Sharp & Dohme Corp. | 1,3-substituted azetidine PDE10 inhibitors |
| ES2798138T3 (es) | 2012-10-15 | 2020-12-09 | Dae Woong Pharma | Bloqueadores de los canales de sodio, método de preparación de los mismos y uso de los mismos |
| ES2912881T3 (es) | 2014-12-23 | 2022-05-30 | Convergence Pharmaceuticals | Procedimiento para preparar derivados de alfa-carboxamida pirrolidina |
| US11192856B2 (en) | 2017-10-05 | 2021-12-07 | Biogen Inc. | Process for preparing alpha-carboxamide pyrrolidine derivatives |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19836697A1 (de) * | 1998-08-13 | 2000-02-17 | Hoechst Marion Roussel De Gmbh | Substituierte 4-Amino-2-aryl-pyrimidine, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate |
| PL350884A1 (en) * | 1999-04-01 | 2003-02-10 | Pfizer Prod Inc | Aminopyrimidines as sorbitol dehydrogenase inhibitors |
| GB0127929D0 (en) * | 2001-11-21 | 2002-01-16 | Celltech R&D Ltd | Chemical compounds |
| ATE466581T1 (de) * | 2001-12-07 | 2010-05-15 | Vertex Pharma | Verbindungen auf pyrimidin-basis als gsk-3-hemmer |
| US7111952B2 (en) * | 2003-03-24 | 2006-09-26 | Lutron Electronics Co., Inc. | System to control daylight and artificial illumination and sun glare in a space |
| WO2004092123A2 (en) * | 2003-04-10 | 2004-10-28 | Microbia, Inc. | Inhibitors of fungal invasion |
| TW200519094A (en) * | 2003-07-02 | 2005-06-16 | Vertex Pharma | Pyrimidines useful as modulators of voltage-gated ion channels |
| US20070099938A1 (en) | 2003-10-24 | 2007-05-03 | Ono Pharmaceutical Co., Ltd. | Antistress drug and medical use thereof |
| US20080194574A1 (en) * | 2003-12-16 | 2008-08-14 | Axxima Pharmaceuticals Ag | Pyrazine Derivatives As Effective Compounds Against Infectious Diseases |
| JP4906715B2 (ja) | 2004-05-08 | 2012-03-28 | ニューロジェン・コーポレーション | ４，５−ジ置換−２−アリールピリミジン類 |
| JP4797021B2 (ja) * | 2004-10-01 | 2011-10-19 | メルク・シャープ・エンド・ドーム・コーポレイション | 糖尿病の治療または予防用のジペプチジルペプチダ−ゼ−ｉｖ阻害剤としてのアミノピペリジン |
| US7589088B2 (en) | 2004-12-29 | 2009-09-15 | Bristol-Myers Squibb Company | Pyrimidine-based inhibitors of dipeptidyl peptidase IV and methods |
-
2006
- 2006-05-04 JP JP2008510216A patent/JP2008540443A/ja not_active Withdrawn
- 2006-05-04 WO PCT/US2006/017214 patent/WO2006119451A1/en not_active Ceased
- 2006-05-04 EP EP06770014A patent/EP1877385A1/en not_active Withdrawn
- 2006-05-04 US US11/418,163 patent/US7858786B2/en active Active
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