JP2011511001A5 - - Google Patents
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- Publication number
- JP2011511001A5 JP2011511001A5 JP2010545227A JP2010545227A JP2011511001A5 JP 2011511001 A5 JP2011511001 A5 JP 2011511001A5 JP 2010545227 A JP2010545227 A JP 2010545227A JP 2010545227 A JP2010545227 A JP 2010545227A JP 2011511001 A5 JP2011511001 A5 JP 2011511001A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- independently
- occurrence
- stereoisomer
- pharmaceutically acceptable
- 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
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- -1 methylenedioxy, ethylenedioxy, propylenedioxy Chemical group 0.000 claims description 31
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 10
- 208000035475 disorder Diseases 0.000 claims description 7
- 150000001875 compounds Chemical class 0.000 claims 35
- SVSARCCKBMZNMR-UHFFFAOYSA-N [1-[2-[methyl-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethyl]amino]ethyl]pyridin-4-ylidene]methyl-oxoazanium;dichloride Chemical compound [Cl-].[Cl-].C1=CC(=C[NH+]=O)C=CN1CCN(C)CCN1C=CC(=C[NH+]=O)C=C1 SVSARCCKBMZNMR-UHFFFAOYSA-N 0.000 claims 27
- 239000000203 mixture Substances 0.000 claims 26
- 150000003839 salts Chemical class 0.000 claims 26
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 25
- 229910052760 oxygen Inorganic materials 0.000 claims 25
- 125000005842 heteroatom Chemical group 0.000 claims 24
- 229910052717 sulfur Inorganic materials 0.000 claims 23
- 150000001204 N-oxides Chemical class 0.000 claims 20
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 17
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 15
- 229910052757 nitrogen Inorganic materials 0.000 claims 14
- 125000003118 aryl group Chemical group 0.000 claims 13
- 229910052799 carbon Inorganic materials 0.000 claims 11
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 11
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims 10
- 125000002757 morpholinyl group Chemical group 0.000 claims 10
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 10
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 125000004193 piperazinyl group Chemical group 0.000 claims 8
- 125000003386 piperidinyl group Chemical group 0.000 claims 8
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 6
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 5
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 4
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 4
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical group C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 4
- 125000002393 azetidinyl group Chemical group 0.000 claims 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 4
- 125000002541 furyl group Chemical group 0.000 claims 4
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 4
- 239000001301 oxygen Substances 0.000 claims 4
- 125000003373 pyrazinyl group Chemical group 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 239000011593 sulfur Substances 0.000 claims 4
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 4
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 4
- 125000000335 thiazolyl group Chemical group 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 125000005988 1,1-dioxo-thiomorpholinyl group Chemical group 0.000 claims 2
- 125000005955 1H-indazolyl group Chemical group 0.000 claims 2
- AAILEWXSEQLMNI-UHFFFAOYSA-N 1h-pyridazin-6-one Chemical compound OC1=CC=CN=N1 AAILEWXSEQLMNI-UHFFFAOYSA-N 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 2
- GAWIXWVDTYZWAW-UHFFFAOYSA-N C[CH]O Chemical group C[CH]O GAWIXWVDTYZWAW-UHFFFAOYSA-N 0.000 claims 2
- 206010062519 Poor quality sleep Diseases 0.000 claims 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 2
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 2
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 2
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 2
- 125000000259 cinnolinyl group Chemical group N1=NC(=CC2=CC=CC=C12)* 0.000 claims 2
- 208000010877 cognitive disease Diseases 0.000 claims 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 2
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 2
- 125000005050 dihydrooxazolyl group Chemical group O1C(NC=C1)* 0.000 claims 2
- 125000005448 ethoxyethyl group Chemical group [H]C([H])([H])C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims 2
- 125000002632 imidazolidinyl group Chemical group 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 125000004857 imidazopyridinyl group Chemical group N1C(=NC2=C1C=CC=N2)* 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- 125000001786 isothiazolyl group Chemical group 0.000 claims 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims 2
- 201000003631 narcolepsy Diseases 0.000 claims 2
- 125000000160 oxazolidinyl group Chemical group 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims 2
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 206010000117 Abnormal behaviour Diseases 0.000 claims 1
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 1
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 208000030814 Eating disease Diseases 0.000 claims 1
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 1
- 208000018522 Gastrointestinal disease Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000026139 Memory disease Diseases 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 208000019022 Mood disease Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 230000037007 arousal Effects 0.000 claims 1
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims 1
- 235000014632 disordered eating Nutrition 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000020595 eating behavior Effects 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 230000036651 mood Effects 0.000 claims 1
- 201000003152 motion sickness Diseases 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 208000020016 psychiatric disease Diseases 0.000 claims 1
- PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical group C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 claims 1
- 150000004892 pyridazines Chemical class 0.000 claims 1
- 208000023504 respiratory system disease Diseases 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 description 3
- 102000005962 receptors Human genes 0.000 description 3
- 108020003175 receptors Proteins 0.000 description 3
- 230000015572 biosynthetic process Effects 0.000 description 2
- 238000003786 synthesis reaction Methods 0.000 description 2
- 0 ***(CC1)CCC1(OC(C1=CN*C=**)=C)S1(=C)=C Chemical compound ***(CC1)CCC1(OC(C1=CN*C=**)=C)S1(=C)=C 0.000 description 1
- 102000004384 Histamine H3 receptors Human genes 0.000 description 1
- 108090000981 Histamine H3 receptors Proteins 0.000 description 1
- 102000000543 Histamine Receptors Human genes 0.000 description 1
- 108010002059 Histamine Receptors Proteins 0.000 description 1
- 241000283973 Oryctolagus cuniculus Species 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 239000003446 ligand Substances 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- LYKMMUBOEFYJQG-UHFFFAOYSA-N piperoxan Chemical class C1OC2=CC=CC=C2OC1CN1CCCCC1 LYKMMUBOEFYJQG-UHFFFAOYSA-N 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 239000002464 receptor antagonist Substances 0.000 description 1
- 229940044551 receptor antagonist Drugs 0.000 description 1
- 125000003003 spiro group Chemical group 0.000 description 1
- 208000010110 spontaneous platelet aggregation Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US6290708P | 2008-01-30 | 2008-01-30 | |
| US61/062,907 | 2008-01-30 | ||
| PCT/US2009/032709 WO2009097567A1 (en) | 2008-01-30 | 2009-01-30 | Substituted spirocyclic piperidine derivatives as histamine-3 (h3) receptor ligands |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011511001A JP2011511001A (ja) | 2011-04-07 |
| JP2011511001A5 true JP2011511001A5 (https=) | 2012-03-15 |
| JP5524083B2 JP5524083B2 (ja) | 2014-06-18 |
Family
ID=40626933
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010545227A Expired - Fee Related JP5524083B2 (ja) | 2008-01-30 | 2009-01-30 | ヒスタミン−３（ｈ３）受容体リガンドとしての置換スピロ環状ピペリジン誘導体 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US8513232B2 (https=) |
| EP (1) | EP2250176B1 (https=) |
| JP (1) | JP5524083B2 (https=) |
| CA (1) | CA2712897A1 (https=) |
| ES (1) | ES2390004T3 (https=) |
| MX (1) | MX2010008375A (https=) |
| WO (1) | WO2009097567A1 (https=) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA95644C2 (ru) * | 2006-07-25 | 2011-08-25 | Сефалон, Инк. | Пиридазиноновые производные, фармацевтическая композиция и способ лечения заболеваний |
| CA2712885A1 (en) | 2008-01-30 | 2009-08-06 | Cephalon, Inc. | Substituted pyridazine derivatives which have histamine h3 antagonist activity |
| MX2010008375A (es) | 2008-01-30 | 2011-03-04 | Cephalon Inc Star | Derivados de piperidina espirocíclicos substituidos como ligandos de receptores de histamina-3 (h3). |
| WO2009142732A2 (en) * | 2008-05-20 | 2009-11-26 | Cephalon, Inc. | Substituted pyridazinone derivatives as histamine-3 (h3) receptor ligands |
| UY32730A (es) * | 2009-06-26 | 2011-01-31 | Novartis Ag | Inhibidores de cyp17 |
| WO2011020193A1 (en) * | 2009-08-18 | 2011-02-24 | Merck Frosst Canada Ltd. | Renin inhibitors |
| EP2488530A4 (en) * | 2009-10-13 | 2014-03-19 | Merck Canada Inc | SPIROCYCLIC PIPERIDINE DERIVATIVES AS RENIN INHIBITORS |
| TWI522361B (zh) | 2010-07-09 | 2016-02-21 | 艾伯維公司 | 作為s1p調節劑的稠合雜環衍生物 |
| TW201643169A (zh) | 2010-07-09 | 2016-12-16 | 艾伯維股份有限公司 | 作為s1p調節劑的螺-哌啶衍生物 |
| TW201206893A (en) | 2010-07-09 | 2012-02-16 | Abbott Healthcare Products Bv | Bisaryl (thio) morpholine derivatives as S1P modulators |
| AU2012249421B9 (en) | 2011-04-28 | 2015-10-22 | Novartis Ag | 17alpha-hydroxylase/C17,20-lyase inhibitors |
| WO2013151982A1 (en) | 2012-04-03 | 2013-10-10 | Arena Pharmaceuticals, Inc. | Methods and compounds useful in treating pruritus, and methods for identifying such compounds |
| EP3290407B1 (en) | 2013-10-18 | 2020-01-01 | Celgene Quanticel Research, Inc | Bromodomain inhibitors |
| AR104259A1 (es) | 2015-04-15 | 2017-07-05 | Celgene Quanticel Res Inc | Inhibidores de bromodominio |
| AU2017252276A1 (en) | 2016-04-18 | 2018-11-15 | Celgene Quanticel Research, Inc. | Therapeutic compounds |
| US10150754B2 (en) | 2016-04-19 | 2018-12-11 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| WO2018083171A1 (en) * | 2016-11-02 | 2018-05-11 | AbbVie Deutschland GmbH & Co. KG | Spiro-compounds as s1p modulators |
| WO2018112204A1 (en) * | 2016-12-14 | 2018-06-21 | Cephalon, Inc. | Spiropiperidine derivatives |
| CN114728982A (zh) | 2019-10-31 | 2022-07-08 | 逃逸生物有限公司 | 固体形式的s1p-受体调节剂 |
| GB201917101D0 (en) * | 2019-11-25 | 2020-01-08 | Uea Enterprises Ltd | Method for digesting nucleic acid in a sample |
| EP4725946A1 (en) * | 2023-06-09 | 2026-04-15 | Guangzhou Unirise Pharmaceutical Co., Ltd. | Irak4 degradation agent and use thereof |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4166120A (en) * | 1978-04-14 | 1979-08-28 | American Hoechst Corporation | Analgesic and tranquilizing benzoylpropyl-spiro[dihydrobenzofuran]piperidines and pyrrolidines |
| CZ2003686A3 (cs) | 2000-08-08 | 2003-08-13 | Ortho Mcneil Pharmaceutical, Inc. | Neimidazolové aryloxypiperidiny |
| KR101011657B1 (ko) * | 2002-03-01 | 2011-01-28 | 다케다 야쿠힌 고교 가부시키가이샤 | 항우울제 |
| SE0202133D0 (sv) * | 2002-07-08 | 2002-07-08 | Astrazeneca Ab | Novel compounds |
| EP1642898B1 (en) | 2003-06-27 | 2013-03-27 | Msd K.K. | Heteroaryloxy nitrogenous saturated heterocyclic derivative |
| CN100418948C (zh) | 2003-07-15 | 2008-09-17 | 麦克公司 | 羟基吡啶cgrp受体抗拮抗剂 |
| CN101921279A (zh) * | 2003-10-01 | 2010-12-22 | 阿得罗公司 | 螺环杂环衍生物及其应用方法 |
| SE0403160D0 (sv) | 2004-12-23 | 2004-12-23 | Biovitrum Ab | New compounds |
| CA2602336A1 (en) | 2005-03-31 | 2006-10-05 | Ucb Pharma S.A. | Compounds comprising an oxazole or thiazole moiety, processes for making them, and their uses |
| EP1707203A1 (en) | 2005-04-01 | 2006-10-04 | Bioprojet | Treatment of parkinson's disease obstructive sleep apnea, dementia with lewy bodies, vascular dementia with non-imidazole alkylamines histamine H3- receptor ligands |
| EP1717235A3 (en) | 2005-04-29 | 2007-02-28 | Bioprojet | Phenoxypropylpiperidines and -pyrrolidines and their use as histamine H3-receptor ligands |
| WO2007063385A2 (en) * | 2005-12-01 | 2007-06-07 | Pfizer Products Inc. | Spirocyclic amine histamine-3 receptor antagonists |
| WO2007088462A1 (en) * | 2006-02-01 | 2007-08-09 | Pfizer Products Inc. | Spirochromane antagonists of the h-3 receptor |
| US20100317679A1 (en) * | 2007-09-21 | 2010-12-16 | Ligand Pharmaceuticals, Inc. | Substituted aryl-fused spirocyclic amines |
| MX2010008375A (es) | 2008-01-30 | 2011-03-04 | Cephalon Inc Star | Derivados de piperidina espirocíclicos substituidos como ligandos de receptores de histamina-3 (h3). |
-
2009
- 2009-01-30 MX MX2010008375A patent/MX2010008375A/es active IP Right Grant
- 2009-01-30 EP EP09707104A patent/EP2250176B1/en not_active Not-in-force
- 2009-01-30 JP JP2010545227A patent/JP5524083B2/ja not_active Expired - Fee Related
- 2009-01-30 WO PCT/US2009/032709 patent/WO2009097567A1/en not_active Ceased
- 2009-01-30 CA CA2712897A patent/CA2712897A1/en not_active Abandoned
- 2009-01-30 ES ES09707104T patent/ES2390004T3/es active Active
-
2010
- 2010-07-29 US US12/846,100 patent/US8513232B2/en not_active Expired - Fee Related
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