JP2010540562A5 - - Google Patents
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- Publication number
- JP2010540562A5 JP2010540562A5 JP2010527249A JP2010527249A JP2010540562A5 JP 2010540562 A5 JP2010540562 A5 JP 2010540562A5 JP 2010527249 A JP2010527249 A JP 2010527249A JP 2010527249 A JP2010527249 A JP 2010527249A JP 2010540562 A5 JP2010540562 A5 JP 2010540562A5
- Authority
- JP
- Japan
- Prior art keywords
- ylmethyl
- indole
- carboxylate
- quinuclidin
- heptan
- 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
- 150000001875 compounds Chemical class 0.000 claims 35
- 150000003839 salts Chemical class 0.000 claims 25
- 239000012453 solvate Substances 0.000 claims 25
- 125000001475 halogen functional group Chemical group 0.000 claims 19
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 19
- 208000024827 Alzheimer disease Diseases 0.000 claims 16
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims 12
- 206010012289 Dementia Diseases 0.000 claims 12
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims 12
- 208000010877 cognitive disease Diseases 0.000 claims 12
- 208000028698 Cognitive impairment Diseases 0.000 claims 8
- 208000028017 Psychotic disease Diseases 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 201000000980 schizophrenia Diseases 0.000 claims 8
- -1 Quinuclidin-4-ylmethyl 1H-indole-3-carboxylate Chemical compound 0.000 claims 6
- 208000007271 Substance Withdrawal Syndrome Diseases 0.000 claims 6
- 230000004770 neurodegeneration Effects 0.000 claims 6
- 208000024891 symptom Diseases 0.000 claims 6
- IHPXOQDYLTYWAR-UHFFFAOYSA-N (3-oxo-1-azabicyclo[2.2.2]octan-4-yl)methyl 1h-indole-3-carboxylate Chemical compound C1=CC=C2C(C(OCC34CCN(CC3)CC4=O)=O)=CNC2=C1 IHPXOQDYLTYWAR-UHFFFAOYSA-N 0.000 claims 5
- SEDHPUZKCQBANK-UHFFFAOYSA-N 1-azabicyclo[2.2.1]heptan-4-ylmethyl 1h-indole-3-carboxylate Chemical compound C1=CC=C2C(C(OCC34CCN(CC3)C4)=O)=CNC2=C1 SEDHPUZKCQBANK-UHFFFAOYSA-N 0.000 claims 5
- AMLBBMMFMLVCAJ-UHFFFAOYSA-N 1-azabicyclo[2.2.1]heptan-4-ylmethyl 5-(difluoromethoxy)-1h-indole-3-carboxylate Chemical compound C12=CC(OC(F)F)=CC=C2NC=C1C(=O)OCC1(C2)CCN2CC1 AMLBBMMFMLVCAJ-UHFFFAOYSA-N 0.000 claims 5
- YNUMJLHUOOGLJA-UHFFFAOYSA-N 1-azabicyclo[2.2.1]heptan-4-ylmethyl 5-chloro-1h-indole-3-carboxylate Chemical compound C12=CC(Cl)=CC=C2NC=C1C(=O)OCC1(C2)CCN2CC1 YNUMJLHUOOGLJA-UHFFFAOYSA-N 0.000 claims 5
- QZAHPOTXRJLXFT-UHFFFAOYSA-N 1-azabicyclo[2.2.1]heptan-4-ylmethyl 5-fluoro-1h-indole-3-carboxylate Chemical compound C12=CC(F)=CC=C2NC=C1C(=O)OCC1(C2)CCN2CC1 QZAHPOTXRJLXFT-UHFFFAOYSA-N 0.000 claims 5
- BYCMSLAAWXLXLI-UHFFFAOYSA-N 1-azabicyclo[2.2.1]heptan-4-ylmethyl 5-methoxy-1h-indole-3-carboxylate Chemical compound C12=CC(OC)=CC=C2NC=C1C(=O)OCC1(C2)CCN2CC1 BYCMSLAAWXLXLI-UHFFFAOYSA-N 0.000 claims 5
- OUCGTTDCRABIMA-UHFFFAOYSA-N 1-azabicyclo[2.2.1]heptan-4-ylmethyl 6-(difluoromethoxy)-1h-indole-3-carboxylate Chemical compound FC(F)OC1=CC=C2C(C(=O)OCC34CCN(CC3)C4)=CNC2=C1 OUCGTTDCRABIMA-UHFFFAOYSA-N 0.000 claims 5
- KHNZERYFIOUCKX-UHFFFAOYSA-N 1-azabicyclo[2.2.1]heptan-4-ylmethyl 6-methoxy-1h-indole-3-carboxylate Chemical compound COC1=CC=C2C(C(=O)OCC34CCN(CC3)C4)=CNC2=C1 KHNZERYFIOUCKX-UHFFFAOYSA-N 0.000 claims 5
- GFXKYBZVBAFFEB-UHFFFAOYSA-N 1-azabicyclo[2.2.2]octan-4-ylmethyl 1h-indazole-3-carboxylate Chemical compound C1=CC=C2C(C(OCC34CCN(CC3)CC4)=O)=NNC2=C1 GFXKYBZVBAFFEB-UHFFFAOYSA-N 0.000 claims 5
- WCVKQCWPYGAONY-UHFFFAOYSA-N 1-azabicyclo[2.2.2]octan-4-ylmethyl 2-methyl-1h-indole-3-carboxylate Chemical compound C1CN(CC2)CCC12COC(=O)C1=C(C)NC2=CC=CC=C21 WCVKQCWPYGAONY-UHFFFAOYSA-N 0.000 claims 5
- VIMBZXPMHGSCMR-UHFFFAOYSA-N 1-azabicyclo[2.2.2]octan-4-ylmethyl 5-(cyclopropylmethoxy)-1h-indole-3-carboxylate Chemical compound C1CN(CC2)CCC12COC(=O)C(C1=C2)=CNC1=CC=C2OCC1CC1 VIMBZXPMHGSCMR-UHFFFAOYSA-N 0.000 claims 5
- PAUBQJDZIFBTBK-UHFFFAOYSA-N 1-azabicyclo[2.2.2]octan-4-ylmethyl 5-(difluoromethoxy)-1h-indole-3-carboxylate Chemical compound C1CN(CC2)CCC12COC(=O)C1=CNC2=CC=C(OC(F)F)C=C21 PAUBQJDZIFBTBK-UHFFFAOYSA-N 0.000 claims 5
- TUCUBBVRRKXMII-UHFFFAOYSA-N 1-azabicyclo[2.2.2]octan-4-ylmethyl 5-(trifluoromethoxymethyl)-1h-indole-3-carboxylate Chemical compound C1CN(CC2)CCC12COC(=O)C1=CNC2=CC=C(COC(F)(F)F)C=C21 TUCUBBVRRKXMII-UHFFFAOYSA-N 0.000 claims 5
- CQPWZYTUOGSVFZ-UHFFFAOYSA-N 1-azabicyclo[2.2.2]octan-4-ylmethyl 5-carbamoyl-1h-indole-3-carboxylate Chemical compound C1CN(CC2)CCC12COC(=O)C1=CNC2=CC=C(C(=O)N)C=C21 CQPWZYTUOGSVFZ-UHFFFAOYSA-N 0.000 claims 5
- MDDRPRHJXXDKKV-UHFFFAOYSA-N 1-azabicyclo[2.2.2]octan-4-ylmethyl 5-chloro-1h-indole-3-carboxylate Chemical compound C1CN(CC2)CCC12COC(=O)C1=CNC2=CC=C(Cl)C=C21 MDDRPRHJXXDKKV-UHFFFAOYSA-N 0.000 claims 5
- GCEPLXYEEIJUJZ-UHFFFAOYSA-N 1-azabicyclo[2.2.2]octan-4-ylmethyl 5-cyano-1h-indole-3-carboxylate Chemical compound C1=C(C#N)C=C2C(C(OCC34CCN(CC3)CC4)=O)=CNC2=C1 GCEPLXYEEIJUJZ-UHFFFAOYSA-N 0.000 claims 5
- TVBLCSQOLNHLAF-UHFFFAOYSA-N 1-azabicyclo[2.2.2]octan-4-ylmethyl 5-methoxy-1h-indole-3-carboxylate Chemical compound C1CN(CC2)CCC12COC(=O)C1=CNC2=CC=C(OC)C=C21 TVBLCSQOLNHLAF-UHFFFAOYSA-N 0.000 claims 5
- OHANUTMZXQOBOM-UHFFFAOYSA-N 1-azabicyclo[2.2.2]octan-4-ylmethyl 5-methoxy-2-methyl-1h-indole-3-carboxylate Chemical compound C1CN(CC2)CCC12COC(=O)C1=C(C)NC2=CC=C(OC)C=C21 OHANUTMZXQOBOM-UHFFFAOYSA-N 0.000 claims 5
- OEIJNTVNSOQULQ-UHFFFAOYSA-N 1-azabicyclo[2.2.2]octan-4-ylmethyl 5-propan-2-yloxy-1h-indole-3-carboxylate Chemical compound C1CN(CC2)CCC12COC(=O)C1=CNC2=CC=C(OC(C)C)C=C21 OEIJNTVNSOQULQ-UHFFFAOYSA-N 0.000 claims 5
- GUKIAYZQCGKGEC-UHFFFAOYSA-N 1-azabicyclo[2.2.2]octan-4-ylmethyl 6-(difluoromethoxy)-1h-indole-3-carboxylate Chemical compound C1CN(CC2)CCC12COC(=O)C1=CNC2=CC(OC(F)F)=CC=C21 GUKIAYZQCGKGEC-UHFFFAOYSA-N 0.000 claims 5
- XIQPDIUHKIOZOL-UHFFFAOYSA-N 1-azabicyclo[2.2.2]octan-4-ylmethyl 6-methoxy-1h-indole-3-carboxylate Chemical compound C1CN(CC2)CCC12COC(=O)C1=CNC2=CC(OC)=CC=C21 XIQPDIUHKIOZOL-UHFFFAOYSA-N 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 5
- PKBVKBLTOFEJGO-UHFFFAOYSA-N n-(1-azabicyclo[2.2.2]octan-4-ylmethyl)-1,2-benzothiazole-3-carboxamide Chemical compound C1=CC=C2C(C(NCC34CCN(CC3)CC4)=O)=NSC2=C1 PKBVKBLTOFEJGO-UHFFFAOYSA-N 0.000 claims 5
- IMRMDIBVFXYZFZ-UHFFFAOYSA-N n-(1-azabicyclo[2.2.2]octan-4-ylmethyl)-1h-indazole-3-carboxamide Chemical compound C1=CC=C2C(C(NCC34CCN(CC3)CC4)=O)=NNC2=C1 IMRMDIBVFXYZFZ-UHFFFAOYSA-N 0.000 claims 5
- CWKWTCNBOIXQKP-UHFFFAOYSA-N n-(1-azabicyclo[2.2.2]octan-4-ylmethyl)-1h-indole-3-carboxamide Chemical compound C1=CC=C2C(C(NCC34CCN(CC3)CC4)=O)=CNC2=C1 CWKWTCNBOIXQKP-UHFFFAOYSA-N 0.000 claims 5
- QAYPIHUQZWFFNR-UHFFFAOYSA-N n-(1-azabicyclo[2.2.2]octan-4-ylmethyl)-5-fluoro-1h-indazole-3-carboxamide Chemical compound C1CN(CC2)CCC12CNC(=O)C1=NNC2=CC=C(F)C=C21 QAYPIHUQZWFFNR-UHFFFAOYSA-N 0.000 claims 5
- 230000002265 prevention Effects 0.000 claims 5
- 208000030507 AIDS Diseases 0.000 claims 4
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 4
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 4
- 208000003174 Brain Neoplasms Diseases 0.000 claims 4
- 208000032841 Bulimia Diseases 0.000 claims 4
- 206010006550 Bulimia nervosa Diseases 0.000 claims 4
- 201000010374 Down Syndrome Diseases 0.000 claims 4
- 208000012661 Dyskinesia Diseases 0.000 claims 4
- 208000027534 Emotional disease Diseases 0.000 claims 4
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 4
- 208000011688 Generalised anxiety disease Diseases 0.000 claims 4
- 201000004311 Gilles de la Tourette syndrome Diseases 0.000 claims 4
- 208000010412 Glaucoma Diseases 0.000 claims 4
- 208000023105 Huntington disease Diseases 0.000 claims 4
- 208000019022 Mood disease Diseases 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 208000018737 Parkinson disease Diseases 0.000 claims 4
- 208000000609 Pick Disease of the Brain Diseases 0.000 claims 4
- 206010036631 Presenile dementia Diseases 0.000 claims 4
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 4
- 206010039966 Senile dementia Diseases 0.000 claims 4
- 206010040070 Septic Shock Diseases 0.000 claims 4
- 208000000323 Tourette Syndrome Diseases 0.000 claims 4
- 208000016620 Tourette disease Diseases 0.000 claims 4
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 4
- 230000002159 abnormal effect Effects 0.000 claims 4
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 claims 4
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 4
- 206010064930 age-related macular degeneration Diseases 0.000 claims 4
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 4
- 208000022531 anorexia Diseases 0.000 claims 4
- 231100000871 behavioral problem Toxicity 0.000 claims 4
- 230000003542 behavioural effect Effects 0.000 claims 4
- 208000030963 borderline personality disease Diseases 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 230000001149 cognitive effect Effects 0.000 claims 4
- 231100000870 cognitive problem Toxicity 0.000 claims 4
- 206010061428 decreased appetite Diseases 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 230000037406 food intake Effects 0.000 claims 4
- 235000012631 food intake Nutrition 0.000 claims 4
- 208000029364 generalized anxiety disease Diseases 0.000 claims 4
- 208000035231 inattentive type attention deficit hyperactivity disease Diseases 0.000 claims 4
- 210000004558 lewy body Anatomy 0.000 claims 4
- 208000002780 macular degeneration Diseases 0.000 claims 4
- 208000027061 mild cognitive impairment Diseases 0.000 claims 4
- 230000036651 mood Effects 0.000 claims 4
- 208000028173 post-traumatic stress disease Diseases 0.000 claims 4
- 230000005586 smoking cessation Effects 0.000 claims 4
- 208000011580 syndromic disease Diseases 0.000 claims 4
- 230000009529 traumatic brain injury Effects 0.000 claims 4
- 230000029663 wound healing Effects 0.000 claims 4
- 238000009472 formulation Methods 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- MZOFCQQQCNRIBI-VMXHOPILSA-N (3s)-4-[[(2s)-1-[[(2s)-1-[[(1s)-1-carboxy-2-hydroxyethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-[[2-[[(2s)-2,6-diaminohexanoyl]amino]acetyl]amino]-4-oxobutanoic acid Chemical compound OC[C@@H](C(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(O)=O)NC(=O)CNC(=O)[C@@H](N)CCCCN MZOFCQQQCNRIBI-VMXHOPILSA-N 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 206010002198 Anaphylactic reaction Diseases 0.000 claims 2
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 2
- 210000002237 B-cell of pancreatic islet Anatomy 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 208000010392 Bone Fractures Diseases 0.000 claims 2
- 206010006895 Cachexia Diseases 0.000 claims 2
- 206010063094 Cerebral malaria Diseases 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims 2
- 208000011231 Crohn disease Diseases 0.000 claims 2
- 241000701022 Cytomegalovirus Species 0.000 claims 2
- 206010012442 Dermatitis contact Diseases 0.000 claims 2
- 206010013754 Drug withdrawal syndrome Diseases 0.000 claims 2
- 206010017076 Fracture Diseases 0.000 claims 2
- 201000005569 Gout Diseases 0.000 claims 2
- 206010018634 Gouty Arthritis Diseases 0.000 claims 2
- 208000031886 HIV Infections Diseases 0.000 claims 2
- 206010020164 HIV infection CDC Group III Diseases 0.000 claims 2
- 208000007514 Herpes zoster Diseases 0.000 claims 2
- 241000700588 Human alphaherpesvirus 1 Species 0.000 claims 2
- 241000701074 Human alphaherpesvirus 2 Species 0.000 claims 2
- 241000713772 Human immunodeficiency virus 1 Species 0.000 claims 2
- 241000713340 Human immunodeficiency virus 2 Species 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 2
- 208000034578 Multiple myelomas Diseases 0.000 claims 2
- 206010028289 Muscle atrophy Diseases 0.000 claims 2
- 208000000112 Myalgia Diseases 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 2
- 208000010191 Osteitis Deformans Diseases 0.000 claims 2
- 208000001132 Osteoporosis Diseases 0.000 claims 2
- 208000027868 Paget disease Diseases 0.000 claims 2
- 208000002193 Pain Diseases 0.000 claims 2
- 208000024571 Pick disease Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 206010037660 Pyrexia Diseases 0.000 claims 2
- 208000033464 Reiter syndrome Diseases 0.000 claims 2
- 206010063837 Reperfusion injury Diseases 0.000 claims 2
- 208000034189 Sclerosis Diseases 0.000 claims 2
- 206010040047 Sepsis Diseases 0.000 claims 2
- 208000006011 Stroke Diseases 0.000 claims 2
- 208000009205 Tinnitus Diseases 0.000 claims 2
- 206010044248 Toxic shock syndrome Diseases 0.000 claims 2
- 231100000650 Toxic shock syndrome Toxicity 0.000 claims 2
- 206010052779 Transplant rejections Diseases 0.000 claims 2
- 108060008682 Tumor Necrosis Factor Proteins 0.000 claims 2
- 102000000852 Tumor Necrosis Factor-alpha Human genes 0.000 claims 2
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 2
- 206010046851 Uveitis Diseases 0.000 claims 2
- 230000001154 acute effect Effects 0.000 claims 2
- 102000047725 alpha7 Nicotinic Acetylcholine Receptor Human genes 0.000 claims 2
- 108700006085 alpha7 Nicotinic Acetylcholine Receptor Proteins 0.000 claims 2
- 230000036783 anaphylactic response Effects 0.000 claims 2
- 208000003455 anaphylaxis Diseases 0.000 claims 2
- 210000001367 artery Anatomy 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 230000003143 atherosclerotic effect Effects 0.000 claims 2
- 208000019664 bone resorption disease Diseases 0.000 claims 2
- 208000010247 contact dermatitis Diseases 0.000 claims 2
- 230000006378 damage Effects 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 230000035876 healing Effects 0.000 claims 2
- 208000019622 heart disease Diseases 0.000 claims 2
- 208000015181 infectious disease Diseases 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 206010022000 influenza Diseases 0.000 claims 2
- 208000012947 ischemia reperfusion injury Diseases 0.000 claims 2
- 208000027202 mammary Paget disease Diseases 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 208000031225 myocardial ischemia Diseases 0.000 claims 2
- 201000008482 osteoarthritis Diseases 0.000 claims 2
- 208000002574 reactive arthritis Diseases 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 206010039083 rhinitis Diseases 0.000 claims 2
- 230000036303 septic shock Effects 0.000 claims 2
- 238000001356 surgical procedure Methods 0.000 claims 2
- 231100000886 tinnitus Toxicity 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- 241000701161 unidentified adenovirus Species 0.000 claims 2
- 241001529453 unidentified herpesvirus Species 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US97672407P | 2007-10-01 | 2007-10-01 | |
| US60/976,724 | 2007-10-01 | ||
| PCT/US2008/078320 WO2009046025A1 (en) | 2007-10-01 | 2008-09-30 | Quinuclidin-4-ylmethyl 1h-indole-3-carboxylate derivatives as alpha 7 nicotinic acetylcholine receptor ligands for the treatment of alzheimer's disease |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010540562A JP2010540562A (ja) | 2010-12-24 |
| JP2010540562A5 true JP2010540562A5 (enExample) | 2011-11-17 |
| JP5022494B2 JP5022494B2 (ja) | 2012-09-12 |
Family
ID=40344599
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010527249A Expired - Fee Related JP5022494B2 (ja) | 2007-10-01 | 2008-09-30 | アルツハイマー病治療用のα７ニコチン性アセチルコリン受容体リガンドとしてのキヌクリジン−４−イルメチル１Ｈ−インドール−３−カルボキシレート誘導体 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US8114891B2 (enExample) |
| EP (1) | EP2217597B1 (enExample) |
| JP (1) | JP5022494B2 (enExample) |
| KR (1) | KR101565469B1 (enExample) |
| CN (2) | CN104193741B (enExample) |
| AT (1) | ATE503754T1 (enExample) |
| CA (1) | CA2701126A1 (enExample) |
| DE (1) | DE602008005928D1 (enExample) |
| DK (1) | DK2217597T3 (enExample) |
| ES (1) | ES2362326T3 (enExample) |
| MX (1) | MX2010003375A (enExample) |
| WO (1) | WO2009046025A1 (enExample) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10164139A1 (de) | 2001-12-27 | 2003-07-10 | Bayer Ag | 2-Heteroarylcarbonsäureamide |
| KR20140146216A (ko) | 2008-11-19 | 2014-12-24 | 포럼 파마슈티칼즈 인크. | (ｒ)-７-클로로-ｎ-(퀴누클리딘-３-일)벤조［ｂ］티오펜-２-카르복사미드 및 그 약학적으로 허용가능한 염을 이용한 인지 장애의 치료 |
| PE20120324A1 (es) * | 2009-05-11 | 2012-04-17 | Envivo Pharmaceuticals Inc | Combinacion que comprende (r)-7-cloro-n-(quinuclidin-3-il)benzo[b]tiofeno-2-carboxamida y donezepilo como moduladora de trastornos cognitivos |
| TWI558398B (zh) | 2009-09-22 | 2016-11-21 | 諾華公司 | 菸鹼乙醯膽鹼受體α７活化劑之用途 |
| MY165234A (en) | 2010-05-17 | 2018-03-14 | Forum Pharmaceuticals Inc | A crystalline form of (r)-7-chloro-n-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate |
| WO2011163539A2 (en) * | 2010-06-25 | 2011-12-29 | The Johns Hopkins University | nAChRα7 AGONISTS AND nAChRα7 ANTAGONISTS FOR TREATING ULCERATIVE COLITIS (UC) AND CROHN'S DISEASE (CD) |
| RU2014103474A (ru) * | 2011-07-01 | 2015-08-10 | Энвиво Фармасьютикалз, Инк. | Способы лечения умеренных когнитивных нарушений |
| JP6088491B2 (ja) * | 2012-04-10 | 2017-03-01 | 大日本住友製薬株式会社 | 新規１位置換インダゾール誘導体 |
| US9585877B2 (en) | 2012-05-08 | 2017-03-07 | Forum Pharmaceuticals, Inc. | Methods of maintaining, treating or improving cognitive function |
| JP6261048B2 (ja) * | 2012-12-05 | 2018-01-17 | 国立大学法人 新潟大学 | 破骨細胞が関与する疾患の予防又は治療剤 |
| CA2903431C (en) | 2013-03-14 | 2022-12-06 | Kalyra Pharmaceuticals, Inc. | Bicyclopentane analgesic compounds |
| EA032196B1 (ru) | 2013-10-03 | 2019-04-30 | Кура Онколоджи, Инк. | Ингибиторы erk и способы применения |
| US10189780B2 (en) | 2013-12-12 | 2019-01-29 | Zeno Royalties & Milestones, LLC | Bicyclic alkyl compounds and synthesis |
| WO2015134710A1 (en) | 2014-03-07 | 2015-09-11 | Kalyra Pharmaceuticals, Inc. | Propellane derivates and synthesis |
| EP3166940A4 (en) * | 2014-07-11 | 2018-04-25 | Alpharmagen, LLC | Quinuclidine compounds for modulating alpha7 -nicotinic acetylcholine receptor activity |
| EP3193855B1 (en) | 2014-09-17 | 2021-05-19 | Recurium IP Holdings, LLC | Bicyclic compounds |
| WO2017120532A1 (en) * | 2016-01-08 | 2017-07-13 | Alpharmagen, Llc | Polymorphs of a phosphate salt of quinuclidin-4-ylmethyl 4-methyl-1h-indole-3-carboxylate and uses thereof |
| US20190083460A1 (en) * | 2016-03-16 | 2019-03-21 | Zeno Royalties & Milestones, LLC | Analgesic compounds |
| MX389668B (es) | 2017-05-15 | 2025-03-20 | Recurium Ip Holdings Llc | Compuestos biciclo[1.1.1]pentilo sustituidos y uso de los mismos para el tratamiento del dolor y fiebre. |
| EP3520803A1 (en) * | 2018-01-31 | 2019-08-07 | Zarodex Therapeutics Limited | Novel uses |
Family Cites Families (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ203861A (en) | 1982-04-14 | 1986-07-11 | Beecham Group Plc | Bicyclic heterocyclic compounds and pharmaceutical compositions containing such |
| WO1985001048A1 (en) | 1983-08-26 | 1985-03-14 | Sandoz Ag | Aromatic esters or amides of carboxylic acid and sulfonic acid |
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| BRPI0517494A (pt) | 2004-12-22 | 2008-10-14 | Memory Pharm Corp | composto, composição farmacêutica, método de ativação/estimulação seletiva de receptores nicotìnicos de a-7 em um paciente em que tal ativação/estimulação tem um efeito terapêutico, método de tratamento de um paciente que sofre de uma doença psicótica, uma doença neurodegenerativa que envolve uma disfunção do sistema colinérgico, e/ou uma condição de debilitação da memória e/ou da cognição, método de tratamento de um paciente que sofre de demência e/ou uma outra condição com perda da memória, método de tratamento de um paciente que sofre de debilitação da memória devido à debilitação cognitiva suave devido ao envelhecimento, mal de alzheimer, esquizofrenia, mal de parkinson, mal de huntington, mal de pick, mal de creutzfeldt-jakob, depressão, envelhecimento, trauma na cabeça, acidente vascular cerebral, hipoxia do snc, senilidade cerebral, demência de multiinfarto, hiv e/ou doença cardiovascular, método de tratamento e/ou prevenção da demência em um paciente com o mal de alzheimer, método de tratamento de um paciente para cortar o vìcio do álcool ou o tratamento de um paciente com a terapia anti-intoxicação, método de tratamento de um paciente para propiciar neuroproteção contra os danos associados com acidentes vasculares cerebrais e isquemia e excitotoxicidade induzida por glutamatos, método de tratamento de um paciente que sofre do vìcio da nicotina, dor, tontura do fuso horário, obesidade e/ou diabetes, método de indução do ato de parar fumar em um paciente, método de tratamento de um paciente que sofre de debilitação cognitiva suave (mci), demência vascular (vad), declìnio cognitivo associado com a idade (aacd), amnésia associada com a cirurgia com o coração aberto, parada cardìaca, anestesia geral, deficiências da memória devido à exposição a agentes anestésicos, debilitação cognitiva induzida pela privação do sono, sìndrome de fadiga crÈnica, narcolepsia, demência relacionada com a aids, debilitação cognitiva relacionada com a epilepsia, sìndrome de down, demência relacionada ao alcoolismo, debilitações da memória induzidas por drogas/substáncias, demência pugilìstica (sìndrome do boxeador), ou demência animal, método para o tratamento da perda da memória, método para o tratamento de um paciente que sofre de debilitação da memória, método para o tratamento ou a profilaxia de uma doença ou de uma condição resultante da disfunção da transmissão do receptor nicotìnico de acetilcolina em um paciente, método para o tratamento ou a profilaxia de uma doença ou de uma condição resultante de receptores nicotìnicos de acetilcolina defeituosos ou funcionando mal em um paciente, método para o tratamento ou a profilaxia de uma doença ou de uma condição resultante da transmissão suprimida do receptor nicotìnico de acetilcolina em um paciente, método para o tratamento ou a profilaxia de uma doença ou de uma condição resultante da perda de sinapses colinérgicas em um paciente, método para a proteção dos neurÈnios em um paciente com neurotoxicidade induzi |
-
2008
- 2008-09-30 EP EP08835512A patent/EP2217597B1/en not_active Not-in-force
- 2008-09-30 KR KR1020107008479A patent/KR101565469B1/ko not_active Expired - Fee Related
- 2008-09-30 JP JP2010527249A patent/JP5022494B2/ja not_active Expired - Fee Related
- 2008-09-30 DK DK08835512.8T patent/DK2217597T3/da active
- 2008-09-30 CN CN201410331886.8A patent/CN104193741B/zh not_active Expired - Fee Related
- 2008-09-30 AT AT08835512T patent/ATE503754T1/de active
- 2008-09-30 MX MX2010003375A patent/MX2010003375A/es active IP Right Grant
- 2008-09-30 DE DE602008005928T patent/DE602008005928D1/de active Active
- 2008-09-30 CN CN2008801186316A patent/CN101883771A/zh active Pending
- 2008-09-30 US US12/242,389 patent/US8114891B2/en not_active Expired - Fee Related
- 2008-09-30 ES ES08835512T patent/ES2362326T3/es active Active
- 2008-09-30 CA CA2701126A patent/CA2701126A1/en not_active Abandoned
- 2008-09-30 WO PCT/US2008/078320 patent/WO2009046025A1/en not_active Ceased
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