JP2019526639A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2019526639A5 JP2019526639A5 JP2019533307A JP2019533307A JP2019526639A5 JP 2019526639 A5 JP2019526639 A5 JP 2019526639A5 JP 2019533307 A JP2019533307 A JP 2019533307A JP 2019533307 A JP2019533307 A JP 2019533307A JP 2019526639 A5 JP2019526639 A5 JP 2019526639A5
- Authority
- JP
- Japan
- Prior art keywords
- disease
- pharmaceutical composition
- group
- mammal
- 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.)
- Granted
Links
- 239000008194 pharmaceutical composition Substances 0.000 claims 29
- 150000001875 compounds Chemical class 0.000 claims 27
- 241000124008 Mammalia Species 0.000 claims 21
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 11
- 208000024827 Alzheimer disease Diseases 0.000 claims 10
- -1 CH 3 Inorganic materials 0.000 claims 10
- 201000010099 disease Diseases 0.000 claims 9
- 208000010877 cognitive disease Diseases 0.000 claims 7
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- 208000037259 Amyloid Plaque Diseases 0.000 claims 5
- 210000004556 brain Anatomy 0.000 claims 5
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 4
- 208000027061 mild cognitive impairment Diseases 0.000 claims 4
- 208000024891 symptom Diseases 0.000 claims 4
- 230000009529 traumatic brain injury Effects 0.000 claims 4
- 108010090849 Amyloid beta-Peptides Proteins 0.000 claims 3
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims 3
- 208000028698 Cognitive impairment Diseases 0.000 claims 3
- 208000023105 Huntington disease Diseases 0.000 claims 3
- 208000018737 Parkinson disease Diseases 0.000 claims 3
- 206010064930 age-related macular degeneration Diseases 0.000 claims 3
- 150000004703 alkoxides Chemical class 0.000 claims 3
- 150000001408 amides Chemical class 0.000 claims 3
- 125000004103 aminoalkyl group Chemical group 0.000 claims 3
- AUZONCFQVSMFAP-UHFFFAOYSA-N disulfiram Chemical compound CCN(CC)C(=S)SSC(=S)N(CC)CC AUZONCFQVSMFAP-UHFFFAOYSA-N 0.000 claims 3
- 150000002148 esters Chemical class 0.000 claims 3
- 201000010901 lateral sclerosis Diseases 0.000 claims 3
- 208000002780 macular degeneration Diseases 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 208000005264 motor neuron disease Diseases 0.000 claims 3
- ISWSIDIOOBJBQZ-UHFFFAOYSA-M phenolate Chemical class [O-]C1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-M 0.000 claims 3
- 239000000651 prodrug Substances 0.000 claims 3
- 229940002612 prodrug Drugs 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- KJNNWYBAOPXVJY-UHFFFAOYSA-N 3-[4-[2-butyl-1-[4-(4-chlorophenoxy)phenyl]imidazol-4-yl]phenoxy]-n,n-diethylpropan-1-amine Chemical compound CCCCC1=NC(C=2C=CC(OCCCN(CC)CC)=CC=2)=CN1C(C=C1)=CC=C1OC1=CC=C(Cl)C=C1 KJNNWYBAOPXVJY-UHFFFAOYSA-N 0.000 claims 2
- 101710137189 Amyloid-beta A4 protein Proteins 0.000 claims 2
- 101710151993 Amyloid-beta precursor protein Proteins 0.000 claims 2
- 102100022704 Amyloid-beta precursor protein Human genes 0.000 claims 2
- 208000005145 Cerebral amyloid angiopathy Diseases 0.000 claims 2
- 102100038018 Corticotropin-releasing factor receptor 1 Human genes 0.000 claims 2
- 101100061417 Homo sapiens CRHR1 gene Proteins 0.000 claims 2
- 208000012902 Nervous system disease Diseases 0.000 claims 2
- 208000025966 Neurological disease Diseases 0.000 claims 2
- YASAKCUCGLMORW-UHFFFAOYSA-N Rosiglitazone Chemical compound C=1C=CC=NC=1N(C)CCOC(C=C1)=CC=C1CC1SC(=O)NC1=O YASAKCUCGLMORW-UHFFFAOYSA-N 0.000 claims 2
- 125000005001 aminoaryl group Chemical group 0.000 claims 2
- 125000005214 aminoheteroaryl group Chemical group 0.000 claims 2
- 108010064539 amyloid beta-protein (1-42) Proteins 0.000 claims 2
- DZHSAHHDTRWUTF-SIQRNXPUSA-N amyloid-beta polypeptide 42 Chemical compound C([C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)NCC(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(O)=O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC(O)=O)C(C)C)C(C)C)C1=CC=CC=C1 DZHSAHHDTRWUTF-SIQRNXPUSA-N 0.000 claims 2
- 229950001863 bapineuzumab Drugs 0.000 claims 2
- 230000015572 biosynthetic process Effects 0.000 claims 2
- 208000013677 cerebrovascular dementia Diseases 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- ADEBPBSSDYVVLD-UHFFFAOYSA-N donepezil Chemical compound O=C1C=2C=C(OC)C(OC)=CC=2CC1CC(CC1)CCN1CC1=CC=CC=C1 ADEBPBSSDYVVLD-UHFFFAOYSA-N 0.000 claims 2
- 208000025688 early-onset autosomal dominant Alzheimer disease Diseases 0.000 claims 2
- 208000015756 familial Alzheimer disease Diseases 0.000 claims 2
- ASUTZQLVASHGKV-JDFRZJQESA-N galanthamine Chemical compound O1C(=C23)C(OC)=CC=C2CN(C)CC[C@]23[C@@H]1C[C@@H](O)C=C2 ASUTZQLVASHGKV-JDFRZJQESA-N 0.000 claims 2
- FVYXIJYOAGAUQK-UHFFFAOYSA-N honokiol Chemical compound C1=C(CC=C)C(O)=CC=C1C1=CC(CC=C)=CC=C1O FVYXIJYOAGAUQK-UHFFFAOYSA-N 0.000 claims 2
- 230000003902 lesion Effects 0.000 claims 2
- 230000003387 muscular Effects 0.000 claims 2
- GWUSZQUVEVMBPI-UHFFFAOYSA-N nimetazepam Chemical compound N=1CC(=O)N(C)C2=CC=C([N+]([O-])=O)C=C2C=1C1=CC=CC=C1 GWUSZQUVEVMBPI-UHFFFAOYSA-N 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- 239000002464 receptor antagonist Substances 0.000 claims 2
- 229940044551 receptor antagonist Drugs 0.000 claims 2
- PKXWXXPNHIWQHW-RCBQFDQVSA-N (2S)-2-hydroxy-3-methyl-N-[(2S)-1-[[(5S)-3-methyl-4-oxo-2,5-dihydro-1H-3-benzazepin-5-yl]amino]-1-oxopropan-2-yl]butanamide Chemical compound C1CN(C)C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](O)C(C)C)C2=CC=CC=C21 PKXWXXPNHIWQHW-RCBQFDQVSA-N 0.000 claims 1
- LIYLTQQDABRNRX-UHFFFAOYSA-N 1-[4-(3,4-dichlorophenyl)-3-fluorophenyl]cyclopropane-1-carboxylic acid Chemical compound C=1C=C(C=2C=C(Cl)C(Cl)=CC=2)C(F)=CC=1C1(C(=O)O)CC1 LIYLTQQDABRNRX-UHFFFAOYSA-N 0.000 claims 1
- 108010067409 AN-1792 Proteins 0.000 claims 1
- 108700028369 Alleles Proteins 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- XEAOPVUAMONVLA-QGZVFWFLSA-N Avagacestat Chemical compound C=1C=C(Cl)C=CC=1S(=O)(=O)N([C@H](CCC(F)(F)F)C(=O)N)CC(C(=C1)F)=CC=C1C=1N=CON=1 XEAOPVUAMONVLA-QGZVFWFLSA-N 0.000 claims 1
- 229940126077 BACE inhibitor Drugs 0.000 claims 1
- 206010008874 Chronic Fatigue Syndrome Diseases 0.000 claims 1
- DSCFFEYYQKSRSV-KLJZZCKASA-N D-pinitol Chemical compound CO[C@@H]1[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)[C@H]1O DSCFFEYYQKSRSV-KLJZZCKASA-N 0.000 claims 1
- MQJKPEGWNLWLTK-UHFFFAOYSA-N Dapsone Chemical compound C1=CC(N)=CC=C1S(=O)(=O)C1=CC=C(N)C=C1 MQJKPEGWNLWLTK-UHFFFAOYSA-N 0.000 claims 1
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 1
- 208000001640 Fibromyalgia Diseases 0.000 claims 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 1
- BYTORXDZJWWIKR-UHFFFAOYSA-N Hinokiol Natural products CC(C)c1cc2CCC3C(C)(CO)C(O)CCC3(C)c2cc1O BYTORXDZJWWIKR-UHFFFAOYSA-N 0.000 claims 1
- ZRJBHWIHUMBLCN-SEQYCRGISA-N Huperzine A Natural products N1C(=O)C=CC2=C1C[C@H]1/C(=C/C)[C@]2(N)CC(C)=C1 ZRJBHWIHUMBLCN-SEQYCRGISA-N 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- WHXSMMKQMYFTQS-UHFFFAOYSA-N Lithium Chemical compound [Li] WHXSMMKQMYFTQS-UHFFFAOYSA-N 0.000 claims 1
- PFELQGNXJDRKDW-DSSYAJFBSA-N NC1=N[C@@](c2cccc(c2)c3cncnc3)(c4ccnc(c4)C(F)F)c5cccc(F)c15.OC(=O)\C=C\C(=O)O Chemical compound NC1=N[C@@](c2cccc(c2)c3cncnc3)(c4ccnc(c4)C(F)F)c5cccc(F)c15.OC(=O)\C=C\C(=O)O PFELQGNXJDRKDW-DSSYAJFBSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- DFPAKSUCGFBDDF-UHFFFAOYSA-N Nicotinamide Chemical compound NC(=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-UHFFFAOYSA-N 0.000 claims 1
- 208000010067 Pituitary ACTH Hypersecretion Diseases 0.000 claims 1
- 208000007913 Pituitary Neoplasms Diseases 0.000 claims 1
- 208000020627 Pituitary-dependent Cushing syndrome Diseases 0.000 claims 1
- 208000005107 Premature Birth Diseases 0.000 claims 1
- 206010036590 Premature baby Diseases 0.000 claims 1
- 206010036618 Premenstrual syndrome Diseases 0.000 claims 1
- XSVMFMHYUFZWBK-NSHDSACASA-N Rivastigmine Chemical compound CCN(C)C(=O)OC1=CC=CC([C@H](C)N(C)C)=C1 XSVMFMHYUFZWBK-NSHDSACASA-N 0.000 claims 1
- 201000001880 Sexual dysfunction Diseases 0.000 claims 1
- ZRJBHWIHUMBLCN-UHFFFAOYSA-N Shuangyiping Natural products N1C(=O)C=CC2=C1CC1C(=CC)C2(N)CC(C)=C1 ZRJBHWIHUMBLCN-UHFFFAOYSA-N 0.000 claims 1
- 208000007107 Stomach Ulcer Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 239000000443 aerosol Substances 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 230000007815 allergy Effects 0.000 claims 1
- 230000003281 allosteric effect Effects 0.000 claims 1
- 108010064397 amyloid beta-protein (1-40) Proteins 0.000 claims 1
- 230000003941 amyloidogenesis Effects 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 230000002490 cerebral effect Effects 0.000 claims 1
- 230000003930 cognitive ability Effects 0.000 claims 1
- 229960000860 dapsone Drugs 0.000 claims 1
- DWLTUUXCVGVRAV-XWRHUKJGSA-N davunetide Chemical compound N([C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCC(N)=O)C(O)=O)C(C)C)C(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@@H](N)CC(N)=O DWLTUUXCVGVRAV-XWRHUKJGSA-N 0.000 claims 1
- 230000001934 delay Effects 0.000 claims 1
- 229960002563 disulfiram Drugs 0.000 claims 1
- 229960003530 donepezil Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- OPQRBXUBWHDHPQ-UHFFFAOYSA-N etazolate Chemical compound CCOC(=O)C1=CN=C2N(CC)N=CC2=C1NN=C(C)C OPQRBXUBWHDHPQ-UHFFFAOYSA-N 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 229960003980 galantamine Drugs 0.000 claims 1
- ASUTZQLVASHGKV-UHFFFAOYSA-N galanthamine hydrochloride Natural products O1C(=C23)C(OC)=CC=C2CN(C)CCC23C1CC(O)C=C2 ASUTZQLVASHGKV-UHFFFAOYSA-N 0.000 claims 1
- 201000005917 gastric ulcer Diseases 0.000 claims 1
- 230000002068 genetic effect Effects 0.000 claims 1
- VVOAZFWZEDHOOU-UHFFFAOYSA-N honokiol Natural products OC1=CC=C(CC=C)C=C1C1=CC(CC=C)=CC=C1O VVOAZFWZEDHOOU-UHFFFAOYSA-N 0.000 claims 1
- ZRJBHWIHUMBLCN-YQEJDHNASA-N huperzine A Chemical compound N1C(=O)C=CC2=C1C[C@H]1\C(=C/C)[C@]2(N)CC(C)=C1 ZRJBHWIHUMBLCN-YQEJDHNASA-N 0.000 claims 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 238000010255 intramuscular injection Methods 0.000 claims 1
- 239000007927 intramuscular injection Substances 0.000 claims 1
- 239000007928 intraperitoneal injection Substances 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 238000010253 intravenous injection Methods 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- RPCVIAXDAUMJJP-PZBABLGHSA-N ispronicline Chemical compound CN[C@@H](C)C\C=C\C1=CN=CC(OC(C)C)=C1 RPCVIAXDAUMJJP-PZBABLGHSA-N 0.000 claims 1
- JNODQFNWMXFMEV-UHFFFAOYSA-N latrepirdine Chemical compound C1N(C)CCC2=C1C1=CC(C)=CC=C1N2CCC1=CC=C(C)N=C1 JNODQFNWMXFMEV-UHFFFAOYSA-N 0.000 claims 1
- 229910052744 lithium Inorganic materials 0.000 claims 1
- BUGYDGFZZOZRHP-UHFFFAOYSA-N memantine Chemical compound C1C(C2)CC3(C)CC1(C)CC2(N)C3 BUGYDGFZZOZRHP-UHFFFAOYSA-N 0.000 claims 1
- 229960004640 memantine Drugs 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000000116 mitigating effect Effects 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 210000003205 muscle Anatomy 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 208000029766 myalgic encephalomeyelitis/chronic fatigue syndrome Diseases 0.000 claims 1
- SSRDSYXGYPJKRR-ZDUSSCGKSA-N n-[(3r)-1-azabicyclo[2.2.2]octan-3-yl]-7-chloro-1-benzothiophene-2-carboxamide Chemical compound C1N(CC2)CCC2[C@H]1NC(=O)C1=CC(C=CC=C2Cl)=C2S1 SSRDSYXGYPJKRR-ZDUSSCGKSA-N 0.000 claims 1
- CMRLNEYJEPELSM-BTQNPOSSSA-N n-[(3s)-1-azabicyclo[2.2.2]octan-3-yl]-1h-indazole-3-carboxamide;hydrochloride Chemical compound Cl.C1=CC=C2C(C(N[C@H]3C4CCN(CC4)C3)=O)=NNC2=C1 CMRLNEYJEPELSM-BTQNPOSSSA-N 0.000 claims 1
- NIDRNVHMMDAAIK-YPMLDQLKSA-N n-[3-[(4as,7as)-2-amino-4,4a,5,7-tetrahydrofuro[3,4-d][1,3]thiazin-7a-yl]-4-fluorophenyl]-5-fluoropyridine-2-carboxamide Chemical compound C=1C=C(F)C([C@@]23N=C(SC[C@@H]2COC3)N)=CC=1NC(=O)C1=CC=C(F)C=N1 NIDRNVHMMDAAIK-YPMLDQLKSA-N 0.000 claims 1
- 230000000926 neurological effect Effects 0.000 claims 1
- 229950001981 nimetazepam Drugs 0.000 claims 1
- 230000037361 pathway Effects 0.000 claims 1
- YZPOQCQXOSEMAZ-UHFFFAOYSA-N pbt2 Chemical compound ClC1=CC(Cl)=C(O)C2=NC(CN(C)C)=CC=C21 YZPOQCQXOSEMAZ-UHFFFAOYSA-N 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 230000001817 pituitary effect Effects 0.000 claims 1
- 230000007505 plaque formation Effects 0.000 claims 1
- 235000020777 polyunsaturated fatty acids Nutrition 0.000 claims 1
- YRVIKLBSVVNSHF-JTQLQIEISA-N pozanicline Chemical compound CC1=NC=CC=C1OC[C@H]1NCCC1 YRVIKLBSVVNSHF-JTQLQIEISA-N 0.000 claims 1
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 1
- 230000001737 promoting effect Effects 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- SCHKZZSVELPJKU-UHFFFAOYSA-N prx-03140 Chemical compound O=C1N(C(C)C)C=2SC=CC=2C(O)=C1C(=O)NCCCN1CCCCC1 SCHKZZSVELPJKU-UHFFFAOYSA-N 0.000 claims 1
- 208000020016 psychiatric disease Diseases 0.000 claims 1
- 125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 claims 1
- ZRJBHWIHUMBLCN-BMIGLBTASA-N rac-huperzine A Natural products N1C(=O)C=CC2=C1C[C@@H]1C(=CC)[C@@]2(N)CC(C)=C1 ZRJBHWIHUMBLCN-BMIGLBTASA-N 0.000 claims 1
- 229960004136 rivastigmine Drugs 0.000 claims 1
- 229960004586 rosiglitazone Drugs 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 229950001900 semagacestat Drugs 0.000 claims 1
- 231100000872 sexual dysfunction Toxicity 0.000 claims 1
- 208000019116 sleep disease Diseases 0.000 claims 1
- AEQFSUDEHCCHBT-UHFFFAOYSA-M sodium valproate Chemical compound [Na+].CCCC(C([O-])=O)CCC AEQFSUDEHCCHBT-UHFFFAOYSA-M 0.000 claims 1
- 229950007874 solanezumab Drugs 0.000 claims 1
- 238000010254 subcutaneous injection Methods 0.000 claims 1
- 239000007929 subcutaneous injection Substances 0.000 claims 1
- 229960001685 tacrine Drugs 0.000 claims 1
- YLJREFDVOIBQDA-UHFFFAOYSA-N tacrine Chemical compound C1=CC=C2C(N)=C(CCCC3)C3=NC2=C1 YLJREFDVOIBQDA-UHFFFAOYSA-N 0.000 claims 1
- 230000037317 transdermal delivery Effects 0.000 claims 1
- UIVFDCIXTSJXBB-ITGUQSILSA-N tropisetron Chemical compound C1=CC=C[C]2C(C(=O)O[C@H]3C[C@H]4CC[C@@H](C3)N4C)=CN=C21 UIVFDCIXTSJXBB-ITGUQSILSA-N 0.000 claims 1
- 229960003688 tropisetron Drugs 0.000 claims 1
- 229940102566 valproate Drugs 0.000 claims 1
- 108010084171 vanutide cridificar Proteins 0.000 claims 1
- 208000009935 visceral pain Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662384656P | 2016-09-07 | 2016-09-07 | |
| US62/384,656 | 2016-09-07 | ||
| PCT/US2017/050347 WO2018048953A1 (en) | 2016-09-07 | 2017-09-06 | Allosteric corticotropin-releasing factor receptor 1 (crfr1) antagonists that decrease p-tau and improve cognition |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019526639A JP2019526639A (ja) | 2019-09-19 |
| JP2019526639A5 true JP2019526639A5 (enExample) | 2020-10-22 |
| JP7187037B2 JP7187037B2 (ja) | 2022-12-12 |
Family
ID=61562356
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019533307A Active JP7187037B2 (ja) | 2016-09-07 | 2017-09-06 | ｐ－タウを減少させ、認知機能を改善させるアロステリック副腎皮質刺激ホルモン放出因子受容体１（ＣＲＦＲ１）アンタゴニスト |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US11077108B2 (enExample) |
| EP (1) | EP3510029B1 (enExample) |
| JP (1) | JP7187037B2 (enExample) |
| KR (1) | KR102571296B1 (enExample) |
| CN (1) | CN109906222B (enExample) |
| AU (1) | AU2017324942B2 (enExample) |
| CA (1) | CA3039026A1 (enExample) |
| WO (1) | WO2018048953A1 (enExample) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113710147B (zh) | 2019-04-15 | 2025-01-28 | 詹森药业有限公司 | 使用语音分析检测认知衰退的系统和方法 |
| CN116832160A (zh) * | 2023-03-15 | 2023-10-03 | 上海市宝山区吴淞中心医院 | Aβ1-42在制备子痫前期治疗药物或诊断试剂盒中的用途 |
| CN118121593B (zh) * | 2024-02-26 | 2025-02-14 | 首都医科大学宣武医院 | 一种用于预防和/或治疗阿尔茨海默病的药物组合物及其用途 |
Family Cites Families (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB590706A (en) * | 1945-02-27 | 1947-07-25 | Frederick Robert Basford | New pyrimidine compounds |
| TW574214B (en) * | 1994-06-08 | 2004-02-01 | Pfizer | Corticotropin releasing factor antagonists |
| US6020492A (en) | 1995-05-12 | 2000-02-01 | Neurogen Corporation | Deazapurine derivatives; a new class of CRF1 specific ligands |
| US6956047B1 (en) * | 1995-06-06 | 2005-10-18 | Pfizer Inc. | Corticotropin releasing factor antagonists |
| US6403599B1 (en) * | 1995-11-08 | 2002-06-11 | Pfizer Inc | Corticotropin releasing factor antagonists |
| AU738304B2 (en) | 1995-10-13 | 2001-09-13 | Neurogen Corporation | Certain pyrrolopyridine derivatives; novel CRF 1 specific ligands |
| US5760225A (en) | 1996-11-15 | 1998-06-02 | Neurogen Corporation | Certain pyrazole derivatives as corticotropin-releasing factor receptor CRF1 specific ligands |
| CA2275686C (en) | 1996-12-18 | 2006-10-17 | Neurogen Corporation | Isoquinolinamine and phthalazinamine derivatives which interact with crf receptors |
| US6756367B2 (en) | 1998-02-03 | 2004-06-29 | Novartis Ag | Benzo-oxadiazoles, -thiadiazoles and -1,4-diazines, pharmaceutical compositions containing them and a process for preparing them |
| GB9802251D0 (en) | 1998-02-03 | 1998-04-01 | Ciba Geigy Ag | Organic compounds |
| US6472402B1 (en) | 1998-04-02 | 2002-10-29 | Neurogen Corporation | Aminoalkyl substituted 5,6,7,8-Tetrahydro-9H-Pyridino [2,3-B]indole derivatives |
| AU4556999A (en) | 1998-06-09 | 1999-12-30 | Neurogen Corporation | Pyrido[2,3-b]indolizine derivatives and aza analogues thereof; crf1 specific ligands |
| EP1175421A1 (en) | 1999-04-30 | 2002-01-30 | Neurogen Corporation | 9H-PYRIMIDO[4,5-b]INDOLE DERIVATIVES: CRF1 SPECIFIC LIGANDS |
| US6387894B1 (en) * | 1999-06-11 | 2002-05-14 | Pfizer Inc. | Use of CRF antagonists and renin-angiotensin system inhibitors |
| US6548509B2 (en) | 1999-10-22 | 2003-04-15 | Neurogen Corporation | 3-aryl substituted pyrazolo[4,3-D]pyrimidine derivatives; corticotropin-releasing factor receptor (CRF1) specific ligands |
| HRP20020599A2 (en) * | 2000-01-18 | 2004-08-31 | Pfizer Prod Inc | Corticotropin releasing factor antagonists |
| BRPI0409505A (pt) | 2003-05-09 | 2006-04-18 | Pharmacia & Upjohn Co Llc | compostos como antagonistas do receptor crf1 |
| EP1626965A1 (en) | 2003-05-09 | 2006-02-22 | Pharmacia & Upjohn Company LLC | Pyrazinones as crf1 receptor antagonists for the treatment of cns disorders |
| CN1878773A (zh) | 2003-09-05 | 2006-12-13 | 神经能质公司 | 作为crf1受体配位体的杂芳基稠合的吡啶,吡嗪及嘧啶 |
| EP1718311A1 (en) * | 2004-02-13 | 2006-11-08 | Pfizer Products Incorporated | Therapeutic combinations of atypical antipsychotics with corticotropin releasing factor antagonists |
| US20080015196A1 (en) | 2004-04-16 | 2008-01-17 | Neurogen Corporation | Imidazopyrazines, Imidazopyridines, and Imidazopyrimidines as Crf1 Receptor Ligands |
| MY148521A (en) * | 2005-01-10 | 2013-04-30 | Arena Pharm Inc | Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto |
| NL2000323C2 (nl) | 2005-12-20 | 2007-11-20 | Pfizer Ltd | Pyrimidine-derivaten. |
| EP1834641A1 (en) | 2006-03-16 | 2007-09-19 | Sanofi-Aventis | Use of CRF1 receptor antagonists for preparing a drug for treating metabolic syndrome and/or obesity and/or dyslipoproteinemia |
| JP5161226B2 (ja) | 2006-09-20 | 2013-03-13 | イーライ リリー アンド カンパニー | Ｃｒｆ１受容体アンタゴニストとしてのチアゾールピラゾロピリミジン |
| TW200906825A (en) * | 2007-05-30 | 2009-02-16 | Scripps Research Inst | Inhibitors of protein kinases |
| CA2683152A1 (en) | 2007-06-11 | 2008-12-18 | Miikana Therapeutics, Inc. | Substituted pyrazole compounds |
| US20100249138A1 (en) | 2007-09-14 | 2010-09-30 | Koob George F | Mpzp: a small molecule corticotropin-releasing factor type 1 receptor (crf1) antogonist |
| US20110301087A1 (en) | 2008-11-04 | 2011-12-08 | Mcbride Edward | Crf1 receptor compounds |
| WO2013123426A1 (en) * | 2012-02-18 | 2013-08-22 | Buck Institute For Research On Aging | Formulations and methods for the treatment or prophylaxis of pre-mci and/or pre-alzheimer's conditions |
| TWI557112B (zh) * | 2012-03-05 | 2016-11-11 | 百靈佳殷格翰國際股份有限公司 | β－分泌酶抑制劑 |
| EP2970219B1 (en) * | 2013-03-15 | 2019-02-27 | Epizyme, Inc. | Carm1 inhibitors and uses thereof |
| CA3155599A1 (en) | 2014-01-21 | 2015-07-30 | Neurocrine Biosciences, Inc. | Crf1 receptor antagonists for the treatment of congenital adrenal hyperplasia |
-
2017
- 2017-09-06 CN CN201780067124.3A patent/CN109906222B/zh active Active
- 2017-09-06 WO PCT/US2017/050347 patent/WO2018048953A1/en not_active Ceased
- 2017-09-06 CA CA3039026A patent/CA3039026A1/en active Pending
- 2017-09-06 KR KR1020197009639A patent/KR102571296B1/ko active Active
- 2017-09-06 JP JP2019533307A patent/JP7187037B2/ja active Active
- 2017-09-06 EP EP17849486.0A patent/EP3510029B1/en active Active
- 2017-09-06 US US16/330,754 patent/US11077108B2/en active Active
- 2017-09-06 AU AU2017324942A patent/AU2017324942B2/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP7607732B2 (ja) | 置換ピロロピリミジンｊａｋ阻害剤ならびにこれを作製および使用する方法 | |
| RU2404189C9 (ru) | Новые пептиды как ингибиторы ns3-серинпротеазы вируса гепатита c | |
| JP2013531040A5 (enExample) | ||
| JP2019526639A5 (enExample) | ||
| JP2019031560A5 (enExample) | ||
| JP7051853B2 (ja) | ヘテロアリールフェノキシベンズアミドカッパオピオイドリガンド | |
| JP2008526888A5 (enExample) | ||
| JP2022542595A (ja) | ガンを処置するためのｂｃｌ－ｘｌタンパク質阻害剤及びアポトーシス促進剤としての、６，７－ジヒドロ－５ｈ－ピリド［２，３－ｃ］ピリダジン誘導体及び関連化合物。 | |
| JP2020517667A (ja) | 抗ウイルス剤としての融合インダゾールピリドン化合物 | |
| JP2018524333A5 (enExample) | ||
| TWI568733B (zh) | 新穎的唏及１，１ａ，２，７ｂ－四氫環丙烷［ｃ］唏吡啶并吡化合物 | |
| RU2007128062A (ru) | Лиганды никотинового рецептора а-7, их получение и применение | |
| RU2013150349A (ru) | 5-замещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов васе, содержащие их композиции и их применение | |
| TW201427959A (zh) | 新穎化合物 | |
| JP2009521483A5 (enExample) | ||
| JP2014528433A5 (enExample) | ||
| JP2014524472A5 (enExample) | ||
| JP2008525464A5 (enExample) | ||
| JP2015531764A5 (enExample) | ||
| JP4490482B2 (ja) | アミノ−プロパノール誘導体 | |
| WO2019177937A1 (en) | Substituted 2-pyridone tricyclic compounds, analogues thereof, and methods using same | |
| JP2021508318A5 (enExample) | ||
| JP2014532730A5 (ja) | オピオイド受容体の調節物質およびそれを含む薬学的組成物 | |
| JP2019529460A5 (enExample) | ||
| TWI616445B (zh) | 新穎環丙苯并呋喃基吡啶并吡二酮類 |