JP2014504642A5 - - Google Patents
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- JP2014504642A5 JP2014504642A5 JP2013552619A JP2013552619A JP2014504642A5 JP 2014504642 A5 JP2014504642 A5 JP 2014504642A5 JP 2013552619 A JP2013552619 A JP 2013552619A JP 2013552619 A JP2013552619 A JP 2013552619A JP 2014504642 A5 JP2014504642 A5 JP 2014504642A5
- Authority
- JP
- Japan
- Prior art keywords
- pain
- alkyl
- replaced
- cycloalkyl
- compound according
- 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 75
- 208000002193 Pain Diseases 0.000 claims description 65
- 125000004122 cyclic group Chemical group 0.000 claims description 53
- 229910052760 oxygen Inorganic materials 0.000 claims description 48
- 229910002091 carbon monoxide Inorganic materials 0.000 claims description 44
- 229910052717 sulfur Inorganic materials 0.000 claims description 42
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 34
- 125000005843 halogen group Chemical group 0.000 claims description 32
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims description 30
- 125000001072 heteroaryl group Chemical group 0.000 claims description 26
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 22
- -1 CF 3 Chemical group 0.000 claims description 20
- 125000003118 aryl group Chemical group 0.000 claims description 20
- 230000001154 acute effect Effects 0.000 claims description 19
- 208000004296 neuralgia Diseases 0.000 claims description 13
- 230000001684 chronic effect Effects 0.000 claims description 11
- 229910052799 carbon Inorganic materials 0.000 claims description 10
- 239000000203 mixture Substances 0.000 claims description 10
- 208000008035 Back Pain Diseases 0.000 claims description 9
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 8
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims description 8
- 125000002347 octyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 8
- 208000019695 Migraine disease Diseases 0.000 claims description 7
- 206010027599 migraine Diseases 0.000 claims description 7
- 201000006417 multiple sclerosis Diseases 0.000 claims description 7
- 230000002981 neuropathic effect Effects 0.000 claims description 7
- 208000021722 neuropathic pain Diseases 0.000 claims description 7
- 208000009935 visceral pain Diseases 0.000 claims description 7
- 125000004429 atom Chemical group 0.000 claims description 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 6
- 125000005842 heteroatom Chemical group 0.000 claims description 6
- 125000000623 heterocyclic group Chemical group 0.000 claims description 6
- 208000014674 injury Diseases 0.000 claims description 6
- 208000011580 syndromic disease Diseases 0.000 claims description 6
- 208000000003 Breakthrough pain Diseases 0.000 claims description 5
- 208000006561 Cluster Headache Diseases 0.000 claims description 5
- 206010019233 Headaches Diseases 0.000 claims description 5
- 206010028836 Neck pain Diseases 0.000 claims description 5
- 206010036376 Postherpetic Neuralgia Diseases 0.000 claims description 5
- 208000018912 cluster headache syndrome Diseases 0.000 claims description 5
- 231100000869 headache Toxicity 0.000 claims description 5
- 208000002551 irritable bowel syndrome Diseases 0.000 claims description 5
- 201000008482 osteoarthritis Diseases 0.000 claims description 5
- 206010044652 trigeminal neuralgia Diseases 0.000 claims description 5
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 4
- 208000004998 Abdominal Pain Diseases 0.000 claims description 4
- 206010002383 Angina Pectoris Diseases 0.000 claims description 4
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims description 4
- 208000007914 Labor Pain Diseases 0.000 claims description 4
- 208000004550 Postoperative Pain Diseases 0.000 claims description 4
- 108010052164 Sodium Channels Proteins 0.000 claims description 4
- 102000018674 Sodium Channels Human genes 0.000 claims description 4
- 208000027418 Wounds and injury Diseases 0.000 claims description 4
- 208000005298 acute pain Diseases 0.000 claims description 4
- 125000000217 alkyl group Chemical group 0.000 claims description 4
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 4
- 239000012472 biological sample Substances 0.000 claims description 4
- 125000000000 cycloalkoxy group Chemical group 0.000 claims description 4
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 4
- 230000006378 damage Effects 0.000 claims description 4
- 125000004043 oxo group Chemical group O=* 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- 125000003107 substituted aryl group Chemical group 0.000 claims description 4
- 208000019901 Anxiety disease Diseases 0.000 claims description 3
- 206010003591 Ataxia Diseases 0.000 claims description 3
- 206010058019 Cancer Pain Diseases 0.000 claims description 3
- 208000000094 Chronic Pain Diseases 0.000 claims description 3
- 206010021639 Incontinence Diseases 0.000 claims description 3
- 206010065390 Inflammatory pain Diseases 0.000 claims description 3
- 208000005615 Interstitial Cystitis Diseases 0.000 claims description 3
- 208000004404 Intractable Pain Diseases 0.000 claims description 3
- 206010026749 Mania Diseases 0.000 claims description 3
- 208000016285 Movement disease Diseases 0.000 claims description 3
- 206010061533 Myotonia Diseases 0.000 claims description 3
- 208000001294 Nociceptive Pain Diseases 0.000 claims description 3
- 208000008765 Sciatica Diseases 0.000 claims description 3
- 208000006011 Stroke Diseases 0.000 claims description 3
- 230000036506 anxiety Effects 0.000 claims description 3
- 206010003119 arrhythmia Diseases 0.000 claims description 3
- 230000006793 arrhythmia Effects 0.000 claims description 3
- 206010003246 arthritis Diseases 0.000 claims description 3
- 206010015037 epilepsy Diseases 0.000 claims description 3
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 3
- 208000015706 neuroendocrine disease Diseases 0.000 claims description 3
- 208000020016 psychiatric disease Diseases 0.000 claims description 3
- 230000009885 systemic effect Effects 0.000 claims description 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 2
- 206010000087 Abdominal pain upper Diseases 0.000 claims description 2
- 208000006820 Arthralgia Diseases 0.000 claims description 2
- 208000009137 Behcet syndrome Diseases 0.000 claims description 2
- 208000020925 Bipolar disease Diseases 0.000 claims description 2
- 206010006002 Bone pain Diseases 0.000 claims description 2
- 201000006474 Brain Ischemia Diseases 0.000 claims description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 2
- 206010064012 Central pain syndrome Diseases 0.000 claims description 2
- 206010008120 Cerebral ischaemia Diseases 0.000 claims description 2
- 201000009273 Endometriosis Diseases 0.000 claims description 2
- 208000024720 Fabry Disease Diseases 0.000 claims description 2
- 206010016059 Facial pain Diseases 0.000 claims description 2
- 208000001640 Fibromyalgia Diseases 0.000 claims description 2
- 208000007514 Herpes zoster Diseases 0.000 claims description 2
- 206010020772 Hypertension Diseases 0.000 claims description 2
- 208000035945 Labour pain Diseases 0.000 claims description 2
- 206010024229 Leprosy Diseases 0.000 claims description 2
- 206010028391 Musculoskeletal Pain Diseases 0.000 claims description 2
- 208000030858 Myofascial Pain Syndromes Diseases 0.000 claims description 2
- 208000005890 Neuroma Diseases 0.000 claims description 2
- 206010033557 Palpitations Diseases 0.000 claims description 2
- 206010033645 Pancreatitis Diseases 0.000 claims description 2
- 206010033647 Pancreatitis acute Diseases 0.000 claims description 2
- 208000000450 Pelvic Pain Diseases 0.000 claims description 2
- 208000010886 Peripheral nerve injury Diseases 0.000 claims description 2
- 208000004983 Phantom Limb Diseases 0.000 claims description 2
- 206010056238 Phantom pain Diseases 0.000 claims description 2
- 208000003251 Pruritus Diseases 0.000 claims description 2
- 206010037596 Pyelonephritis Diseases 0.000 claims description 2
- 206010037779 Radiculopathy Diseases 0.000 claims description 2
- 208000000491 Tendinopathy Diseases 0.000 claims description 2
- 206010043255 Tendonitis Diseases 0.000 claims description 2
- 206010043269 Tension headache Diseases 0.000 claims description 2
- 208000008548 Tension-Type Headache Diseases 0.000 claims description 2
- 208000009205 Tinnitus Diseases 0.000 claims description 2
- 206010046543 Urinary incontinence Diseases 0.000 claims description 2
- 208000025609 Urogenital disease Diseases 0.000 claims description 2
- 230000002159 abnormal effect Effects 0.000 claims description 2
- 201000003229 acute pancreatitis Diseases 0.000 claims description 2
- 125000003545 alkoxy group Chemical group 0.000 claims description 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 2
- 208000034757 axonal type 2FF Charcot-Marie-Tooth disease Diseases 0.000 claims description 2
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims description 2
- 210000004556 brain Anatomy 0.000 claims description 2
- 206010008118 cerebral infarction Diseases 0.000 claims description 2
- 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 description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000003709 fluoroalkyl group Chemical group 0.000 claims description 2
- 230000005176 gastrointestinal motility Effects 0.000 claims description 2
- 125000001188 haloalkyl group Chemical group 0.000 claims description 2
- 208000037584 hereditary sensory and autonomic neuropathy Diseases 0.000 claims description 2
- 230000002757 inflammatory effect Effects 0.000 claims description 2
- 201000001119 neuropathy Diseases 0.000 claims description 2
- 230000007823 neuropathy Effects 0.000 claims description 2
- 230000001314 paroxysmal effect Effects 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 201000007094 prostatitis Diseases 0.000 claims description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 2
- 201000009890 sinusitis Diseases 0.000 claims description 2
- 208000020431 spinal cord injury Diseases 0.000 claims description 2
- 208000005198 spinal stenosis Diseases 0.000 claims description 2
- 201000004415 tendinitis Diseases 0.000 claims description 2
- 231100000886 tinnitus Toxicity 0.000 claims description 2
- 208000004371 toothache Diseases 0.000 claims description 2
- 230000008733 trauma Effects 0.000 claims description 2
- 230000000472 traumatic effect Effects 0.000 claims description 2
- 208000026533 urinary bladder disease Diseases 0.000 claims description 2
- 208000008930 Low Back Pain Diseases 0.000 claims 2
- 206010005949 Bone cancer Diseases 0.000 claims 1
- 208000018084 Bone neoplasm Diseases 0.000 claims 1
- 208000023890 Complex Regional Pain Syndromes Diseases 0.000 claims 1
- 206010063057 Cystitis noninfective Diseases 0.000 claims 1
- 208000004454 Hyperalgesia Diseases 0.000 claims 1
- 206010038419 Renal colic Diseases 0.000 claims 1
- 206010053552 allodynia Diseases 0.000 claims 1
- 201000001352 cholecystitis Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000007803 itching Effects 0.000 claims 1
- 210000002414 leg Anatomy 0.000 claims 1
- 230000003211 malignant effect Effects 0.000 claims 1
- 208000007056 sickle cell anemia Diseases 0.000 claims 1
- 230000007863 steatosis Effects 0.000 claims 1
- 231100000240 steatosis hepatitis Toxicity 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 210000001694 thigh bone Anatomy 0.000 claims 1
- 238000000034 method Methods 0.000 description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 206010020853 Hypertonic bladder Diseases 0.000 description 1
- 206010040037 Sensory neuropathy hereditary Diseases 0.000 description 1
- 208000007502 anemia Diseases 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 210000003743 erythrocyte Anatomy 0.000 description 1
- 230000005284 excitation Effects 0.000 description 1
- 201000006847 hereditary sensory neuropathy Diseases 0.000 description 1
- 208000033808 peripheral neuropathy Diseases 0.000 description 1
- 238000001959 radiotherapy Methods 0.000 description 1
- 230000002123 temporal effect Effects 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161438685P | 2011-02-02 | 2011-02-02 | |
| US61/438,685 | 2011-02-02 | ||
| US201161440987P | 2011-02-09 | 2011-02-09 | |
| US61/440,987 | 2011-02-09 | ||
| US201161495538P | 2011-06-10 | 2011-06-10 | |
| US61/495,538 | 2011-06-10 | ||
| PCT/US2012/023593 WO2012106499A1 (en) | 2011-02-02 | 2012-02-02 | Pyrrolopyrazine-spirocyclic piperidine amides as modulators of ion channels |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015251126A Division JP6261558B2 (ja) | 2011-02-02 | 2015-12-24 | イオンチャネルのモジュレーターとしてのピロロピラジン−スピロ環式ピペリジンアミド |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014504642A JP2014504642A (ja) | 2014-02-24 |
| JP2014504642A5 true JP2014504642A5 (enExample) | 2015-03-19 |
| JP6021824B2 JP6021824B2 (ja) | 2016-11-09 |
Family
ID=45689011
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013552619A Active JP6021824B2 (ja) | 2011-02-02 | 2012-02-02 | イオンチャネルのモジュレーターとしてのピロロピラジン−スピロ環式ピペリジンアミド |
| JP2015251126A Active JP6261558B2 (ja) | 2011-02-02 | 2015-12-24 | イオンチャネルのモジュレーターとしてのピロロピラジン−スピロ環式ピペリジンアミド |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015251126A Active JP6261558B2 (ja) | 2011-02-02 | 2015-12-24 | イオンチャネルのモジュレーターとしてのピロロピラジン−スピロ環式ピペリジンアミド |
Country Status (27)
| Country | Link |
|---|---|
| US (3) | US8916565B2 (enExample) |
| EP (2) | EP2670752B1 (enExample) |
| JP (2) | JP6021824B2 (enExample) |
| KR (1) | KR101923367B1 (enExample) |
| CN (2) | CN103403004B (enExample) |
| AR (1) | AR085893A1 (enExample) |
| AU (1) | AU2012212196B2 (enExample) |
| BR (1) | BR112013019211A2 (enExample) |
| CA (1) | CA2825204C (enExample) |
| CY (1) | CY1117471T1 (enExample) |
| DK (1) | DK2670752T3 (enExample) |
| ES (1) | ES2573497T3 (enExample) |
| HR (1) | HRP20160382T8 (enExample) |
| HU (1) | HUE028789T2 (enExample) |
| IL (1) | IL227815B (enExample) |
| MX (1) | MX355907B (enExample) |
| NZ (1) | NZ613028A (enExample) |
| PL (1) | PL2670752T3 (enExample) |
| PT (1) | PT2670752E (enExample) |
| RS (1) | RS54785B1 (enExample) |
| RU (1) | RU2634900C2 (enExample) |
| SG (1) | SG192248A1 (enExample) |
| SI (1) | SI2670752T1 (enExample) |
| SM (1) | SMT201600162B (enExample) |
| TW (2) | TWI520964B (enExample) |
| WO (1) | WO2012106499A1 (enExample) |
| ZA (1) | ZA201305152B (enExample) |
Families Citing this family (70)
| Publication number | Priority date | Publication date | Assignee | Title |
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| JP5389030B2 (ja) | 2007-08-24 | 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 | （特に）嚢胞性線維症の処置に有用なイソチアゾロピリジノン |
| WO2011140425A1 (en) | 2010-05-06 | 2011-11-10 | Vertex Pharmaceuticals Incorporated | Heterocyclic chromene-spirocyclic piperidine amides as modulators of ion channels |
| ES2573497T3 (es) | 2011-02-02 | 2016-06-08 | Vertex Pharmaceuticals Incorporated | Pirrolopirazin-amidas de piperidina espirocíclicas como moduladores de canales iónicos |
| CA2827311A1 (en) | 2011-02-18 | 2012-08-23 | Vertex Pharmaceuticals Incorporated | Chroman-spirocyclic piperidine amides as modulators of ion channels |
| CA2829803A1 (en) | 2011-03-14 | 2012-09-20 | Vertex Pharmaceuticals Incorporated | Morpholine-spirocyclic piperidine amides as modulators of ion channels |
| EP2773641B1 (en) | 2011-10-31 | 2017-09-27 | Xenon Pharmaceuticals Inc. | Biaryl ether sulfonamides and their use as therapeutic agents |
| ES2586213T3 (es) | 2011-10-31 | 2016-10-13 | Xenon Pharmaceuticals Inc. | Compuestos de bencenosulfonamida y su uso como agentes terapéuticos |
| PE20150400A1 (es) | 2012-05-22 | 2015-03-27 | Genentech Inc | Benzamidas n-sustituidas y su uso en el tratamiento del dolor |
| US10071957B2 (en) | 2012-07-06 | 2018-09-11 | Genentech, Inc. | N-substituted benzamides and methods of use thereof |
| WO2014022639A1 (en) | 2012-08-01 | 2014-02-06 | Vertex Pharmaceuticals Incorporated | Solid forms of (4-isopropoxy-3-methoxyphenyl)(2'-methyl-6'-(trifluoromethyl)-3',4'-dihydro-2'h-spiro[piperidine-4,1'-pyrrolo[1,2-a]pyrazine]-1-yl)methanone |
| EP3239134B1 (en) | 2013-01-31 | 2020-12-23 | Vertex Pharmaceuticals Incorporated | Pyridone amides as modulators of sodium channels |
| AR095192A1 (es) | 2013-01-31 | 2015-09-30 | Vertex Pharma | Quinolina y quinazolinamidas como modulares de canales de sodio |
| TW201444798A (zh) | 2013-02-28 | 2014-12-01 | 必治妥美雅史谷比公司 | 作爲強效ｒｏｃｋ１及ｒｏｃｋ２抑制劑之苯基吡唑衍生物 |
| WO2014134391A1 (en) | 2013-02-28 | 2014-09-04 | Bristol-Myers Squibb Company | Phenylpyrazole derivatives as potent rock1 and rock2 inhibitors |
| RU2015143906A (ru) | 2013-03-14 | 2017-04-18 | Дженентек, Инк. | Замещенные триазолопиридины и способы их применения |
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| AU2014287471C1 (en) * | 2013-07-10 | 2019-11-28 | Vertex Pharmaceuticals Incorporated | Fused piperidine amides as modulators of ion channels |
| EP3022175B1 (en) | 2013-07-19 | 2017-11-08 | Vertex Pharmaceuticals Incorporated | Sulfonamides as modulators of sodium channels |
| CA2931732A1 (en) | 2013-11-27 | 2015-06-04 | Genentech, Inc. | Substituted benzamides and methods of use thereof |
| KR102435145B1 (ko) | 2013-12-13 | 2022-08-24 | 버텍스 파마슈티칼스 인코포레이티드 | 나트륨 채널의 조절제로서의 피리돈 아미드의 프로드럭 |
| JP2017525677A (ja) | 2014-07-07 | 2017-09-07 | ジェネンテック， インコーポレイテッド | 治療用化合物及びその使用方法 |
| MA42118A (fr) | 2015-05-22 | 2018-03-28 | Genentech Inc | Benzamides substitués et leurs méthodes d'utilisation |
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