JP2006503062A5 - - Google Patents
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- Publication number
- JP2006503062A5 JP2006503062A5 JP2004538781A JP2004538781A JP2006503062A5 JP 2006503062 A5 JP2006503062 A5 JP 2006503062A5 JP 2004538781 A JP2004538781 A JP 2004538781A JP 2004538781 A JP2004538781 A JP 2004538781A JP 2006503062 A5 JP2006503062 A5 JP 2006503062A5
- Authority
- JP
- Japan
- Prior art keywords
- oxadiazol
- nonane
- diazabicyclo
- phenyl
- alkoxy
- 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
- 208000024827 Alzheimer disease Diseases 0.000 claims description 6
- 230000006735 deficit Effects 0.000 claims description 5
- 208000028698 Cognitive impairment Diseases 0.000 claims description 3
- 206010039966 Senile dementia Diseases 0.000 claims description 3
- 208000010877 cognitive disease Diseases 0.000 claims description 3
- 206010027175 memory impairment Diseases 0.000 claims description 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- -1 carboxy, carbamoyl Chemical group 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 2
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 2
- 125000003118 aryl group Chemical group 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
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 2
- FIFMTMSMJXYGQN-UHFFFAOYSA-N 2-(1,4-diazabicyclo[3.2.2]nonan-4-yl)-5-(3-methoxyphenyl)-1,3,4-oxadiazole Chemical compound COC1=CC=CC(C=2OC(=NN=2)N2C3CCN(CC3)CC2)=C1 FIFMTMSMJXYGQN-UHFFFAOYSA-N 0.000 claims 1
- HEOSAVOMNPCPTH-UHFFFAOYSA-N 2-(1,4-diazabicyclo[3.2.2]nonan-4-yl)-5-(4-methoxyphenyl)-1,3,4-oxadiazole Chemical compound C1=CC(OC)=CC=C1C1=NN=C(N2C3CCN(CC3)CC2)O1 HEOSAVOMNPCPTH-UHFFFAOYSA-N 0.000 claims 1
- PBRDJMBPMCWKLP-UHFFFAOYSA-N 2-(1,4-diazabicyclo[3.2.2]nonan-4-yl)-5-(4-phenylphenyl)-1,3,4-oxadiazole Chemical compound C1CN(CC2)CCC1N2C(O1)=NN=C1C(C=C1)=CC=C1C1=CC=CC=C1 PBRDJMBPMCWKLP-UHFFFAOYSA-N 0.000 claims 1
- GYNXMRDDGAXVNF-UHFFFAOYSA-N 2-(1,4-diazabicyclo[3.2.2]nonan-4-yl)-5-(furan-2-yl)-1,3,4-oxadiazole Chemical compound C1CN(CC2)CCC1N2C(O1)=NN=C1C1=CC=CO1 GYNXMRDDGAXVNF-UHFFFAOYSA-N 0.000 claims 1
- IFEAJBAVNOCULL-UHFFFAOYSA-N 2-(1,4-diazabicyclo[3.2.2]nonan-4-yl)-5-naphthalen-2-yl-1,3,4-oxadiazole Chemical compound C1CC2CCN1CCN2C1=NN=C(C=2C=C3C=CC=CC3=CC=2)O1 IFEAJBAVNOCULL-UHFFFAOYSA-N 0.000 claims 1
- NFQNAHNFWFCCMJ-UHFFFAOYSA-N 2-(1,4-diazabicyclo[3.2.2]nonan-4-yl)-5-phenyl-1,3,4-oxadiazole Chemical compound C1CN(CC2)CCC1N2C(O1)=NN=C1C1=CC=CC=C1 NFQNAHNFWFCCMJ-UHFFFAOYSA-N 0.000 claims 1
- MEWUVJHFNOWLJM-UHFFFAOYSA-N 2-(1,4-diazabicyclo[3.2.2]nonan-4-yl)-5-pyridin-3-yl-1,3,4-oxadiazole Chemical compound C1CN(CC2)CCC1N2C(O1)=NN=C1C1=CC=CN=C1 MEWUVJHFNOWLJM-UHFFFAOYSA-N 0.000 claims 1
- CORKMSCCLJZCIM-UHFFFAOYSA-N 2-(1,4-diazabicyclo[3.2.2]nonan-4-yl)-5-pyridin-4-yl-1,3,4-oxadiazole Chemical compound C1CN(CC2)CCC1N2C(O1)=NN=C1C1=CC=NC=C1 CORKMSCCLJZCIM-UHFFFAOYSA-N 0.000 claims 1
- DZQAGBGRTLEXOZ-UHFFFAOYSA-N 2-(1,4-diazabicyclo[3.2.2]nonan-4-yl)-5-thiophen-2-yl-1,3,4-oxadiazole Chemical compound C1CN(CC2)CCC1N2C(O1)=NN=C1C1=CC=CS1 DZQAGBGRTLEXOZ-UHFFFAOYSA-N 0.000 claims 1
- FSQJLWBCAJDHEK-UHFFFAOYSA-N 2-(4-chlorophenyl)-5-(1,4-diazabicyclo[3.2.2]nonan-4-yl)-1,3,4-oxadiazole Chemical compound C1=CC(Cl)=CC=C1C1=NN=C(N2C3CCN(CC3)CC2)O1 FSQJLWBCAJDHEK-UHFFFAOYSA-N 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000005083 alkoxyalkoxy group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000003368 amide group Chemical group 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 125000004858 cycloalkoxyalkyl group Chemical group 0.000 claims 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000009760 functional impairment Effects 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 46
- 201000010099 disease Diseases 0.000 description 23
- 208000035475 disorder Diseases 0.000 description 23
- 208000002193 Pain Diseases 0.000 description 8
- 210000003169 central nervous system Anatomy 0.000 description 8
- 210000001428 peripheral nervous system Anatomy 0.000 description 6
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 description 4
- 208000011580 syndromic disease Diseases 0.000 description 4
- 208000032841 Bulimia Diseases 0.000 description 3
- 206010006550 Bulimia nervosa Diseases 0.000 description 3
- 206010061218 Inflammation Diseases 0.000 description 3
- 208000007271 Substance Withdrawal Syndrome Diseases 0.000 description 3
- 230000001713 cholinergic effect Effects 0.000 description 3
- 230000004054 inflammatory process Effects 0.000 description 3
- 230000004770 neurodegeneration Effects 0.000 description 3
- 230000000144 pharmacologic effect Effects 0.000 description 3
- 230000016160 smooth muscle contraction Effects 0.000 description 3
- 239000000126 substance Substances 0.000 description 3
- 208000030507 AIDS Diseases 0.000 description 2
- 208000000103 Anorexia Nervosa Diseases 0.000 description 2
- 208000019901 Anxiety disease Diseases 0.000 description 2
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 description 2
- 206010003805 Autism Diseases 0.000 description 2
- 208000020706 Autistic disease Diseases 0.000 description 2
- 208000020925 Bipolar disease Diseases 0.000 description 2
- 206010008874 Chronic Fatigue Syndrome Diseases 0.000 description 2
- 208000019888 Circadian rhythm sleep disease Diseases 0.000 description 2
- 206010010904 Convulsion Diseases 0.000 description 2
- 206010012289 Dementia Diseases 0.000 description 2
- 208000012661 Dyskinesia Diseases 0.000 description 2
- 208000030814 Eating disease Diseases 0.000 description 2
- 208000026097 Factitious disease Diseases 0.000 description 2
- 208000019454 Feeding and Eating disease Diseases 0.000 description 2
- 201000004311 Gilles de la Tourette syndrome Diseases 0.000 description 2
- 208000023105 Huntington disease Diseases 0.000 description 2
- 208000001456 Jet Lag Syndrome Diseases 0.000 description 2
- 206010026749 Mania Diseases 0.000 description 2
- 208000019695 Migraine disease Diseases 0.000 description 2
- 102000019315 Nicotinic acetylcholine receptors Human genes 0.000 description 2
- 108050006807 Nicotinic acetylcholine receptors Proteins 0.000 description 2
- 208000008589 Obesity Diseases 0.000 description 2
- 208000018737 Parkinson disease Diseases 0.000 description 2
- 208000008348 Post-Concussion Syndrome Diseases 0.000 description 2
- 208000004550 Postoperative Pain Diseases 0.000 description 2
- 206010036618 Premenstrual syndrome Diseases 0.000 description 2
- 206010052276 Pseudodementia Diseases 0.000 description 2
- 208000022372 Reading disease Diseases 0.000 description 2
- 208000000323 Tourette Syndrome Diseases 0.000 description 2
- 208000016620 Tourette disease Diseases 0.000 description 2
- 230000001154 acute effect Effects 0.000 description 2
- 239000000556 agonist Substances 0.000 description 2
- 230000036506 anxiety Effects 0.000 description 2
- 208000028683 bipolar I disease Diseases 0.000 description 2
- 230000001684 chronic effect Effects 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 235000014632 disordered eating Nutrition 0.000 description 2
- 230000004064 dysfunction Effects 0.000 description 2
- 206010013932 dyslexia Diseases 0.000 description 2
- 230000002124 endocrine Effects 0.000 description 2
- 206010015037 epilepsy Diseases 0.000 description 2
- 230000002650 habitual effect Effects 0.000 description 2
- 208000033915 jet lag type circadian rhythm sleep disease Diseases 0.000 description 2
- 206010027599 migraine Diseases 0.000 description 2
- 208000029766 myalgic encephalomeyelitis/chronic fatigue syndrome Diseases 0.000 description 2
- 201000001119 neuropathy Diseases 0.000 description 2
- 230000007823 neuropathy Effects 0.000 description 2
- 235000020824 obesity Nutrition 0.000 description 2
- 208000019906 panic disease Diseases 0.000 description 2
- 208000033808 peripheral neuropathy Diseases 0.000 description 2
- 102000005962 receptors Human genes 0.000 description 2
- 108020003175 receptors Proteins 0.000 description 2
- 201000000980 schizophrenia Diseases 0.000 description 2
- 230000020341 sensory perception of pain Effects 0.000 description 2
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 description 2
- 208000019116 sleep disease Diseases 0.000 description 2
- 208000020685 sleep-wake disease Diseases 0.000 description 2
- 102000040125 5-hydroxytryptamine receptor family Human genes 0.000 description 1
- 108091032151 5-hydroxytryptamine receptor family Proteins 0.000 description 1
- 108010078791 Carrier Proteins Proteins 0.000 description 1
- 108010009685 Cholinergic Receptors Proteins 0.000 description 1
- 208000017701 Endocrine disease Diseases 0.000 description 1
- 206010020710 Hyperphagia Diseases 0.000 description 1
- 206010028289 Muscle atrophy Diseases 0.000 description 1
- 208000004983 Phantom Limb Diseases 0.000 description 1
- 206010056238 Phantom pain Diseases 0.000 description 1
- 102000034337 acetylcholine receptors Human genes 0.000 description 1
- 230000003281 allosteric effect Effects 0.000 description 1
- 150000001412 amines Chemical class 0.000 description 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 description 1
- 230000000035 biogenic effect Effects 0.000 description 1
- 208000030172 endocrine system disease Diseases 0.000 description 1
- 208000013403 hyperactivity Diseases 0.000 description 1
- 208000035231 inattentive type attention deficit hyperactivity disease Diseases 0.000 description 1
- 201000010901 lateral sclerosis Diseases 0.000 description 1
- 230000000938 luteal effect Effects 0.000 description 1
- 230000029849 luteinization Effects 0.000 description 1
- 208000005264 motor neuron disease Diseases 0.000 description 1
- 210000003205 muscle Anatomy 0.000 description 1
- 230000020763 muscle atrophy Effects 0.000 description 1
- 201000000585 muscular atrophy Diseases 0.000 description 1
- 235000020830 overeating Nutrition 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DKPA200201456 | 2002-09-30 | ||
| DKPA200201456 | 2002-09-30 | ||
| DKPA200201738 | 2002-11-11 | ||
| DKPA200201738 | 2002-11-11 | ||
| US42636802P | 2002-11-15 | 2002-11-15 | |
| US60/426,368 | 2002-11-15 | ||
| PCT/DK2003/000639 WO2004029053A1 (en) | 2002-09-30 | 2003-09-29 | Novel 1,4-diazabicycloalkane derivatives, their preparation and use |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2006503062A JP2006503062A (ja) | 2006-01-26 |
| JP2006503062A5 true JP2006503062A5 (https=) | 2010-07-15 |
| JP4711391B2 JP4711391B2 (ja) | 2011-06-29 |
Family
ID=34828377
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004538781A Expired - Fee Related JP4711391B2 (ja) | 2002-09-30 | 2003-09-29 | 新規１，４−ジアザビシクロアルカン誘導体及びその製造方法 |
Country Status (11)
| Country | Link |
|---|---|
| JP (1) | JP4711391B2 (https=) |
| KR (1) | KR20050062575A (https=) |
| CN (1) | CN1326857C (https=) |
| BR (1) | BR0314183A (https=) |
| IL (1) | IL166821A (https=) |
| IS (1) | IS7829A (https=) |
| MX (1) | MXPA05003344A (https=) |
| NO (1) | NO20052124L (https=) |
| PT (1) | PT1551835E (https=) |
| RU (1) | RU2323218C2 (https=) |
| SI (1) | SI1551835T1 (https=) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2368614C2 (ru) * | 2004-02-04 | 2009-09-27 | НьюроСёрч А/С | Диазабициклические арильные производные в качестве модуляторов холинергических рецепторов |
| JO3019B1 (ar) * | 2006-04-19 | 2016-09-05 | Janssen Pharmaceutica Nv | ثلاثي مستبدل 4،2،1-ثلاثي زولات |
| WO2007138038A1 (en) * | 2006-05-30 | 2007-12-06 | Neurosearch A/S | Novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their medical use |
| US8492378B2 (en) | 2006-08-03 | 2013-07-23 | Takeda Pharmaceutical Company Limited | GSK-3β inhibitor |
| EP2121688A1 (en) * | 2007-02-15 | 2009-11-25 | Argenta Discovery Ltd | Heterocyclic derivatives as m3 muscarinic receptors |
| EP2780015B1 (en) | 2011-11-18 | 2017-01-04 | Heptares Therapeutics Limited | Muscarinic m1 receptor agonists |
| GB201404922D0 (en) | 2014-03-19 | 2014-04-30 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| GB201513743D0 (en) | 2015-08-03 | 2015-09-16 | Heptares Therapeutics Ltd | Muscarinic agonists |
| GB201519352D0 (en) | 2015-11-02 | 2015-12-16 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| IL294124B2 (en) * | 2015-12-10 | 2024-02-01 | Ptc Therapeutics Inc | Methods for treating huntington's disease |
| CN108623530B (zh) * | 2016-09-18 | 2021-05-11 | 广西师范大学 | 1，2，8-氧代二氮杂环壬-9-硫酮衍生物及其合成方法和应用 |
| GB201617454D0 (en) | 2016-10-14 | 2016-11-30 | Heptares Therapeutics Limited | Pharmaceutical compounds |
| GB201810239D0 (en) | 2018-06-22 | 2018-08-08 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| GB201819960D0 (en) | 2018-12-07 | 2019-01-23 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| GB201819961D0 (en) | 2018-12-07 | 2019-01-23 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| GB202020191D0 (en) | 2020-12-18 | 2021-02-03 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ226000A (en) * | 1987-09-10 | 1991-06-25 | Merck Sharp & Dohme | Oxadiazolyl-azabicycloheptanes and pharmaceutical compositions |
| HUT74682A (en) * | 1993-12-29 | 1997-01-28 | Pfizer | Diazabicyclic neurokinin antagonists and pharmaceutical compositions containing them |
| US5478939A (en) * | 1994-07-20 | 1995-12-26 | American Cyanamid Company | (R,R) and (S,S) 2,5-diazabicyclo [2,2,1]heptane derivatives |
| FR2786770B1 (fr) * | 1998-12-04 | 2001-01-19 | Synthelabo | Derives de 1,4-diazabicyclo[3.2.2.]nonane, leur preparation et leur application en therapeutique |
| BR0012327A (pt) * | 1999-07-09 | 2002-07-02 | Ortho Mcneil Pharm Inc | Pirrolidinas e piperidinas neurotróficas, e composições e métodos relacionados |
| FR2804430B1 (fr) * | 2000-01-28 | 2002-03-22 | Sanofi Synthelabo | Derives de 4-heteroaryl-1,4-diazabicyclo[3.2.2] nonane, leur preparation et leur application en therapeutique |
| FR2809731B1 (fr) * | 2000-05-31 | 2002-07-19 | Sanofi Synthelabo | Derives de 1,4-diazabicyclo-[3.2.2] nonane-pheylisoxazole, leur preparation et leur application en therapeutique |
| FR2809732B1 (fr) * | 2000-05-31 | 2002-07-19 | Sanofi Synthelabo | DERIVES DE 4(-2-PHENYLTHIAZOL-5-yl)-1,4-DIAZABICYCLO-[3.2.2] NONANE, LEUR PREPARATION ET LEUR APPLICATION ENTHERAPEUTIQUE |
| US20020086871A1 (en) * | 2000-12-29 | 2002-07-04 | O'neill Brian Thomas | Pharmaceutical composition for the treatment of CNS and other disorders |
| FR2832713B1 (fr) * | 2001-11-23 | 2004-02-13 | Sanofi Synthelabo | Derives de 4-(1,3,4-thiadiazol-2-yl)-1,4-diazabicyclo[3.2.2] nonane, leur preparation et leur application en therapeutique |
-
2003
- 2003-09-29 JP JP2004538781A patent/JP4711391B2/ja not_active Expired - Fee Related
- 2003-09-29 BR BR0314183-7A patent/BR0314183A/pt not_active Application Discontinuation
- 2003-09-29 MX MXPA05003344A patent/MXPA05003344A/es active IP Right Grant
- 2003-09-29 KR KR1020057005508A patent/KR20050062575A/ko not_active Ceased
- 2003-09-29 RU RU2005105048/04A patent/RU2323218C2/ru not_active IP Right Cessation
- 2003-09-29 PT PT03798094T patent/PT1551835E/pt unknown
- 2003-09-29 SI SI200330715T patent/SI1551835T1/sl unknown
- 2003-09-29 CN CNB038232626A patent/CN1326857C/zh not_active Expired - Fee Related
-
2005
- 2005-02-10 IL IL166821A patent/IL166821A/en not_active IP Right Cessation
- 2005-04-28 IS IS7829A patent/IS7829A/is unknown
- 2005-04-29 NO NO20052124A patent/NO20052124L/no unknown
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