JP2011510992A5 - - Google Patents
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- Publication number
- JP2011510992A5 JP2011510992A5 JP2010545098A JP2010545098A JP2011510992A5 JP 2011510992 A5 JP2011510992 A5 JP 2011510992A5 JP 2010545098 A JP2010545098 A JP 2010545098A JP 2010545098 A JP2010545098 A JP 2010545098A JP 2011510992 A5 JP2011510992 A5 JP 2011510992A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- compound
- ethyl
- methyl
- optionally substituted
- 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
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 12
- 208000035475 disorder Diseases 0.000 claims description 9
- 208000010877 cognitive disease Diseases 0.000 claims description 4
- 208000008589 Obesity Diseases 0.000 claims description 2
- 230000037007 arousal Effects 0.000 claims description 2
- 235000020824 obesity Nutrition 0.000 claims description 2
- 150000001875 compounds Chemical class 0.000 claims 36
- 229910052799 carbon Inorganic materials 0.000 claims 26
- 229910052739 hydrogen Inorganic materials 0.000 claims 19
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 18
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 18
- 229910052731 fluorine Inorganic materials 0.000 claims 17
- 229910052801 chlorine Inorganic materials 0.000 claims 13
- 125000004432 carbon atom Chemical group C* 0.000 claims 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 9
- 229910052794 bromium Inorganic materials 0.000 claims 8
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 8
- 125000005842 heteroatom Chemical group 0.000 claims 8
- 229910052760 oxygen Inorganic materials 0.000 claims 8
- 229910052717 sulfur Inorganic materials 0.000 claims 8
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 7
- 239000000203 mixture Substances 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 6
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 4
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 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 3
- 201000010099 disease Diseases 0.000 claims 3
- 125000002971 oxazolyl group Chemical group 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 125000000168 pyrrolyl group Chemical group 0.000 claims 3
- 125000001544 thienyl group Chemical group 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 2
- 206010062519 Poor quality sleep Diseases 0.000 claims 2
- 201000003631 narcolepsy Diseases 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- 206010000117 Abnormal behaviour Diseases 0.000 claims 1
- 208000036864 Attention deficit/hyperactivity disease Diseases 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
- 208000002193 Pain Diseases 0.000 claims 1
- 150000001413 amino acids Chemical class 0.000 claims 1
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 235000014632 disordered eating Nutrition 0.000 claims 1
- 230000020595 eating behavior Effects 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 230000004054 inflammatory process Effects 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
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 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
- 208000023504 respiratory system disease Diseases 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 1
- 102000005962 receptors Human genes 0.000 description 15
- 108020003175 receptors Proteins 0.000 description 15
- NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 description 10
- 210000004556 brain Anatomy 0.000 description 6
- 239000003814 drug Substances 0.000 description 6
- 229940079593 drug Drugs 0.000 description 6
- 229960001340 histamine Drugs 0.000 description 5
- 239000003395 histamine H3 receptor antagonist Substances 0.000 description 5
- 239000003446 ligand Substances 0.000 description 5
- 241000700159 Rattus Species 0.000 description 4
- 102000004384 Histamine H3 receptors Human genes 0.000 description 3
- 108090000981 Histamine H3 receptors Proteins 0.000 description 3
- 102000000543 Histamine Receptors Human genes 0.000 description 3
- 108010002059 Histamine Receptors Proteins 0.000 description 3
- 108010033040 Histones Proteins 0.000 description 3
- 210000003169 central nervous system Anatomy 0.000 description 3
- 230000001149 cognitive effect Effects 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 description 3
- 230000000144 pharmacologic effect Effects 0.000 description 3
- 230000001225 therapeutic effect Effects 0.000 description 3
- 229940115480 Histamine H3 receptor antagonist Drugs 0.000 description 2
- HNDVDQJCIGZPNO-UHFFFAOYSA-N Histidine Chemical compound OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 description 2
- 208000012902 Nervous system disease Diseases 0.000 description 2
- 208000025966 Neurological disease Diseases 0.000 description 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- 238000010367 cloning Methods 0.000 description 2
- 230000019771 cognition Effects 0.000 description 2
- 239000003596 drug target Substances 0.000 description 2
- 210000002569 neuron Anatomy 0.000 description 2
- 239000002464 receptor antagonist Substances 0.000 description 2
- 238000003786 synthesis reaction Methods 0.000 description 2
- 230000002618 waking effect Effects 0.000 description 2
- PLYSQHFCSVNUMZ-UHFFFAOYSA-N 4-(1h-imidazol-5-yl)butyl n'-[(4-chlorophenyl)methyl]carbamimidothioate Chemical compound C1=CC(Cl)=CC=C1CNC(=N)SCCCCC1=CNC=N1 PLYSQHFCSVNUMZ-UHFFFAOYSA-N 0.000 description 1
- -1 6-substituted phenyl-4,5-dihydro-3 (2H) -pyridazinones Chemical class 0.000 description 1
- 208000019901 Anxiety disease Diseases 0.000 description 1
- 241000282693 Cercopithecidae Species 0.000 description 1
- 241000282326 Felis catus Species 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- 241000699666 Mus <mouse, genus> Species 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 241000283973 Oryctolagus cuniculus Species 0.000 description 1
- 108010029485 Protein Isoforms Proteins 0.000 description 1
- 102000001708 Protein Isoforms Human genes 0.000 description 1
- 206010070834 Sensitisation Diseases 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 208000026935 allergic disease Diseases 0.000 description 1
- 230000007815 allergy Effects 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 230000036506 anxiety Effects 0.000 description 1
- 125000004104 aryloxy group Chemical group 0.000 description 1
- 208000006673 asthma Diseases 0.000 description 1
- 230000003542 behavioural effect Effects 0.000 description 1
- 230000007812 deficiency Effects 0.000 description 1
- 239000003623 enhancer Substances 0.000 description 1
- 238000012215 gene cloning Methods 0.000 description 1
- 230000002068 genetic effect Effects 0.000 description 1
- 229940124806 histamine H3 agonist Drugs 0.000 description 1
- 239000003382 histamine H3 receptor agonist Substances 0.000 description 1
- 230000000742 histaminergic effect Effects 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 230000001939 inductive effect Effects 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 238000011813 knockout mouse model Methods 0.000 description 1
- 230000003137 locomotive effect Effects 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 230000015654 memory Effects 0.000 description 1
- LYKMMUBOEFYJQG-UHFFFAOYSA-N piperoxan Chemical class C1OC2=CC=CC=C2OC1CN1CCCCC1 LYKMMUBOEFYJQG-UHFFFAOYSA-N 0.000 description 1
- 210000002970 posterior hypothalamus Anatomy 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 229940044551 receptor antagonist Drugs 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 230000008313 sensitization Effects 0.000 description 1
- 208000019116 sleep disease Diseases 0.000 description 1
- 230000006886 spatial memory Effects 0.000 description 1
- 125000003003 spiro group Chemical group 0.000 description 1
- 208000010110 spontaneous platelet aggregation Diseases 0.000 description 1
- 238000011699 spontaneously hypertensive rat Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US6290908P | 2008-01-30 | 2008-01-30 | |
| US61/062,909 | 2008-01-30 | ||
| PCT/US2009/032195 WO2009097309A1 (en) | 2008-01-30 | 2009-01-28 | Substituted spirocyclic piperidine derivatives as histamine-3 (h3) receptor ligands |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011510992A JP2011510992A (ja) | 2011-04-07 |
| JP2011510992A5 true JP2011510992A5 (https=) | 2013-04-04 |
| JP5524082B2 JP5524082B2 (ja) | 2014-06-18 |
Family
ID=40445314
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010545098A Expired - Fee Related JP5524082B2 (ja) | 2008-01-30 | 2009-01-28 | 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 (18)
| Country | Link |
|---|---|
| US (2) | US8524713B2 (https=) |
| EP (1) | EP2257553B1 (https=) |
| JP (1) | JP5524082B2 (https=) |
| KR (1) | KR20100105789A (https=) |
| CN (1) | CN101932585B (https=) |
| AT (1) | ATE522538T1 (https=) |
| AU (1) | AU2009209235B2 (https=) |
| BR (1) | BRPI0905849A2 (https=) |
| CA (1) | CA2712888A1 (https=) |
| EA (1) | EA018537B1 (https=) |
| ES (1) | ES2370378T3 (https=) |
| IL (1) | IL206914A (https=) |
| MX (1) | MX2010008382A (https=) |
| MY (1) | MY150062A (https=) |
| NZ (1) | NZ587034A (https=) |
| UA (1) | UA100877C2 (https=) |
| WO (1) | WO2009097309A1 (https=) |
| ZA (1) | ZA201005136B (https=) |
Families Citing this family (14)
| 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 |
| WO2009142732A2 (en) * | 2008-05-20 | 2009-11-26 | Cephalon, Inc. | Substituted pyridazinone derivatives as histamine-3 (h3) receptor ligands |
| CA2726588C (en) | 2008-06-03 | 2019-04-16 | Karl Kossen | Compounds and methods for treating inflammatory and fibrotic disorders |
| 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 |
| TW201206893A (en) | 2010-07-09 | 2012-02-16 | Abbott Healthcare Products Bv | Bisaryl (thio) morpholine derivatives as S1P modulators |
| 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 |
| WO2012077655A1 (ja) * | 2010-12-07 | 2012-06-14 | 塩野義製薬株式会社 | Ｇｐｒ１１９アゴニスト活性を有するスピロ誘導体 |
| CA2827673C (en) | 2011-02-18 | 2020-10-27 | Novartis Pharma Ag | Mtor/jak inhibitor combination therapy |
| AR092742A1 (es) | 2012-10-02 | 2015-04-29 | Intermune Inc | Piridinonas antifibroticas |
| MX382781B (es) | 2014-04-02 | 2025-03-13 | Intermune Inc | Piridinonas anti-fibroticas. |
| JP6643764B2 (ja) * | 2016-02-05 | 2020-02-12 | 国立大学法人岐阜大学 | 抗がん剤 |
| US12435078B2 (en) | 2017-09-18 | 2025-10-07 | Gfb (Abc), Llc | Pyridazinones and methods of use thereof |
| 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 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0313762D0 (en) * | 2003-06-13 | 2003-07-23 | Biofocus Plc | Compound libraries |
| 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 |
| US8158791B2 (en) * | 2005-11-10 | 2012-04-17 | Msd K.K. | Aza-substituted spiro derivatives |
| 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 |
-
2009
- 2009-01-28 MX MX2010008382A patent/MX2010008382A/es active IP Right Grant
- 2009-01-28 CA CA2712888A patent/CA2712888A1/en not_active Abandoned
- 2009-01-28 MY MYPI2010003298A patent/MY150062A/en unknown
- 2009-01-28 ES ES09706445T patent/ES2370378T3/es active Active
- 2009-01-28 AU AU2009209235A patent/AU2009209235B2/en not_active Ceased
- 2009-01-28 EA EA201070903A patent/EA018537B1/ru not_active IP Right Cessation
- 2009-01-28 NZ NZ587034A patent/NZ587034A/en not_active IP Right Cessation
- 2009-01-28 BR BRPI0905849-4A patent/BRPI0905849A2/pt not_active IP Right Cessation
- 2009-01-28 JP JP2010545098A patent/JP5524082B2/ja not_active Expired - Fee Related
- 2009-01-28 EP EP09706445A patent/EP2257553B1/en not_active Not-in-force
- 2009-01-28 AT AT09706445T patent/ATE522538T1/de not_active IP Right Cessation
- 2009-01-28 CN CN2009801037142A patent/CN101932585B/zh not_active Expired - Fee Related
- 2009-01-28 UA UAA201010456A patent/UA100877C2/ru unknown
- 2009-01-28 WO PCT/US2009/032195 patent/WO2009097309A1/en not_active Ceased
- 2009-01-28 KR KR1020107019040A patent/KR20100105789A/ko not_active Ceased
-
2010
- 2010-07-08 IL IL206914A patent/IL206914A/en not_active IP Right Cessation
- 2010-07-19 ZA ZA2010/05136A patent/ZA201005136B/en unknown
- 2010-07-29 US US12/846,108 patent/US8524713B2/en active Active
-
2013
- 2013-07-24 US US13/949,323 patent/US20130310389A1/en not_active Abandoned
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