SA516371298B1 - مشتق الكرومون كمضاد لمستقبل الدوبامين د3 واستخدامه في علاج اضطراب طيف التوحد - Google Patents
مشتق الكرومون كمضاد لمستقبل الدوبامين د3 واستخدامه في علاج اضطراب طيف التوحد Download PDFInfo
- Publication number
- SA516371298B1 SA516371298B1 SA516371298A SA516371298A SA516371298B1 SA 516371298 B1 SA516371298 B1 SA 516371298B1 SA 516371298 A SA516371298 A SA 516371298A SA 516371298 A SA516371298 A SA 516371298A SA 516371298 B1 SA516371298 B1 SA 516371298B1
- Authority
- SA
- Saudi Arabia
- Prior art keywords
- phenyl
- butyl
- dioxolo
- methanesulfonamide
- dopamine
- Prior art date
Links
- 208000029560 autism spectrum disease Diseases 0.000 title claims abstract description 22
- 150000004777 chromones Chemical class 0.000 title abstract description 7
- 229940088353 Dopamine D3 receptor antagonist Drugs 0.000 title abstract 2
- 239000002300 dopamine 3 receptor blocking agent Substances 0.000 title abstract 2
- 230000006735 deficit Effects 0.000 claims abstract description 19
- 230000003997 social interaction Effects 0.000 claims abstract description 14
- 150000003839 salts Chemical class 0.000 claims abstract description 11
- 239000003814 drug Substances 0.000 claims abstract description 10
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 3
- 238000004519 manufacturing process Methods 0.000 claims abstract 3
- 150000001875 compounds Chemical class 0.000 claims description 21
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 12
- 229940079593 drug Drugs 0.000 claims description 7
- 239000000203 mixture Substances 0.000 claims description 7
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 6
- QZHPTGXQGDFGEN-UHFFFAOYSA-N chromene Chemical compound C1=CC=C2C=C[CH]OC2=C1 QZHPTGXQGDFGEN-UHFFFAOYSA-N 0.000 claims description 6
- 239000011780 sodium chloride Substances 0.000 claims description 5
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical group Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 3
- 229960000794 baclofen Drugs 0.000 claims description 3
- KPYSYYIEGFHWSV-UHFFFAOYSA-N Baclofen Chemical compound OC(=O)CC(CN)C1=CC=C(Cl)C=C1 KPYSYYIEGFHWSV-UHFFFAOYSA-N 0.000 claims description 2
- GXBMIBRIOWHPDT-UHFFFAOYSA-N Vasopressin Natural products N1C(=O)C(CC=2C=C(O)C=CC=2)NC(=O)C(N)CSSCC(C(=O)N2C(CCC2)C(=O)NC(CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(CCC(N)=O)NC(=O)C1CC1=CC=CC=C1 GXBMIBRIOWHPDT-UHFFFAOYSA-N 0.000 claims description 2
- 108010004977 Vasopressins Proteins 0.000 claims description 2
- 102000002852 Vasopressins Human genes 0.000 claims description 2
- AFCGFAGUEYAMAO-UHFFFAOYSA-N acamprosate Chemical compound CC(=O)NCCCS(O)(=O)=O AFCGFAGUEYAMAO-UHFFFAOYSA-N 0.000 claims description 2
- 229960004047 acamprosate Drugs 0.000 claims description 2
- DKNWSYNQZKUICI-UHFFFAOYSA-N amantadine Chemical compound C1C(C2)CC3CC2CC1(N)C3 DKNWSYNQZKUICI-UHFFFAOYSA-N 0.000 claims description 2
- 229960003805 amantadine Drugs 0.000 claims description 2
- KBZOIRJILGZLEJ-LGYYRGKSSA-N argipressin Chemical compound C([C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CSSC[C@@H](C(N[C@@H](CC=2C=CC(O)=CC=2)C(=O)N1)=O)N)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)C1=CC=CC=C1 KBZOIRJILGZLEJ-LGYYRGKSSA-N 0.000 claims description 2
- BUGYDGFZZOZRHP-UHFFFAOYSA-N memantine Chemical compound C1C(C2)CC3(C)CC1(C)CC2(N)C3 BUGYDGFZZOZRHP-UHFFFAOYSA-N 0.000 claims description 2
- 229960004640 memantine Drugs 0.000 claims description 2
- 238000001228 spectrum Methods 0.000 claims description 2
- 229960003726 vasopressin Drugs 0.000 claims description 2
- 241000196324 Embryophyta Species 0.000 claims 1
- NWPJLRSCSQHPJV-UHFFFAOYSA-N carpipramine Chemical compound C1CN(CCCN2C3=CC=CC=C3CCC3=CC=CC=C32)CCC1(C(=O)N)N1CCCCC1 NWPJLRSCSQHPJV-UHFFFAOYSA-N 0.000 claims 1
- 229960000700 carpipramine Drugs 0.000 claims 1
- KLOYLPZTHLSRRB-UHFFFAOYSA-N n-[3-[4-[4-(8-oxo-[1,3]dioxolo[4,5-g]chromen-7-yl)butyl]piperazin-1-yl]phenyl]methanesulfonamide Chemical compound CS(=O)(=O)NC1=CC=CC(N2CCN(CCCCC=3C(C4=CC=5OCOC=5C=C4OC=3)=O)CC2)=C1 KLOYLPZTHLSRRB-UHFFFAOYSA-N 0.000 abstract 1
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 description 32
- 208000020706 Autistic disease Diseases 0.000 description 22
- 206010003805 Autism Diseases 0.000 description 21
- AEQFSUDEHCCHBT-UHFFFAOYSA-M sodium valproate Chemical compound [Na+].CCCC(C([O-])=O)CCC AEQFSUDEHCCHBT-UHFFFAOYSA-M 0.000 description 17
- 229960003638 dopamine Drugs 0.000 description 16
- 102000005962 receptors Human genes 0.000 description 14
- 108020003175 receptors Proteins 0.000 description 14
- 208000024891 symptom Diseases 0.000 description 13
- 229940102566 valproate Drugs 0.000 description 12
- 108050004812 Dopamine receptor Proteins 0.000 description 11
- NIJJYAXOARWZEE-UHFFFAOYSA-N Valproic acid Chemical compound CCCC(C(O)=O)CCC NIJJYAXOARWZEE-UHFFFAOYSA-N 0.000 description 11
- 230000006399 behavior Effects 0.000 description 11
- 102000015554 Dopamine receptor Human genes 0.000 description 10
- 241000700159 Rattus Species 0.000 description 9
- 208000035475 disorder Diseases 0.000 description 9
- 230000000694 effects Effects 0.000 description 6
- 239000002773 nucleotide Substances 0.000 description 6
- 108700028369 Alleles Proteins 0.000 description 5
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 5
- 238000004891 communication Methods 0.000 description 5
- 238000003745 diagnosis Methods 0.000 description 5
- 125000003729 nucleotide group Chemical group 0.000 description 5
- 230000036961 partial effect Effects 0.000 description 5
- 208000029726 Neurodevelopmental disease Diseases 0.000 description 4
- 102000054765 polymorphisms of proteins Human genes 0.000 description 4
- 108090000623 proteins and genes Proteins 0.000 description 4
- 229940084026 sodium valproate Drugs 0.000 description 4
- 230000001225 therapeutic effect Effects 0.000 description 4
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 description 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- 229940121891 Dopamine receptor antagonist Drugs 0.000 description 3
- 239000000556 agonist Substances 0.000 description 3
- VREFGVBLTWBCJP-UHFFFAOYSA-N alprazolam Chemical compound C12=CC(Cl)=CC=C2N2C(C)=NN=C2CN=C1C1=CC=CC=C1 VREFGVBLTWBCJP-UHFFFAOYSA-N 0.000 description 3
- 230000037396 body weight Effects 0.000 description 3
- 210000004027 cell Anatomy 0.000 description 3
- -1 chromene-7-yl Chemical group 0.000 description 3
- 239000003210 dopamine receptor blocking agent Substances 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 230000002068 genetic effect Effects 0.000 description 3
- 238000000034 method Methods 0.000 description 3
- 210000000276 neural tube Anatomy 0.000 description 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 3
- 230000004044 response Effects 0.000 description 3
- 230000001953 sensory effect Effects 0.000 description 3
- 229960000604 valproic acid Drugs 0.000 description 3
- 208000020925 Bipolar disease Diseases 0.000 description 2
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 2
- 125000002842 L-seryl group Chemical group O=C([*])[C@](N([H])[H])([H])C([H])([H])O[H] 0.000 description 2
- 206010026749 Mania Diseases 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 208000012902 Nervous system disease Diseases 0.000 description 2
- 208000025966 Neurological disease Diseases 0.000 description 2
- 208000002192 Parkinson disease 3 Diseases 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- 208000028017 Psychotic disease Diseases 0.000 description 2
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 2
- 238000010171 animal model Methods 0.000 description 2
- 239000005557 antagonist Substances 0.000 description 2
- 239000000729 antidote Substances 0.000 description 2
- 230000003542 behavioural effect Effects 0.000 description 2
- 210000004556 brain Anatomy 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 230000007812 deficiency Effects 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 125000003630 glycyl group Chemical group [H]N([H])C([H])([H])C(*)=O 0.000 description 2
- 201000001881 impotence Diseases 0.000 description 2
- 239000007928 intraperitoneal injection Substances 0.000 description 2
- 150000007522 mineralic acids Chemical class 0.000 description 2
- 230000036651 mood Effects 0.000 description 2
- 230000035772 mutation Effects 0.000 description 2
- 150000007524 organic acids Chemical class 0.000 description 2
- 208000020016 psychiatric disease Diseases 0.000 description 2
- 238000011552 rat model Methods 0.000 description 2
- 230000003252 repetitive effect Effects 0.000 description 2
- 102220300572 rs167771 Human genes 0.000 description 2
- 229910052708 sodium Inorganic materials 0.000 description 2
- 239000011734 sodium Substances 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- 238000002560 therapeutic procedure Methods 0.000 description 2
- 230000001755 vocal effect Effects 0.000 description 2
- BMYNFMYTOJXKLE-UHFFFAOYSA-N 3-azaniumyl-2-hydroxypropanoate Chemical compound NCC(O)C(O)=O BMYNFMYTOJXKLE-UHFFFAOYSA-N 0.000 description 1
- 208000007848 Alcoholism Diseases 0.000 description 1
- 208000019901 Anxiety disease Diseases 0.000 description 1
- CEUORZQYGODEFX-UHFFFAOYSA-N Aripirazole Chemical compound ClC1=CC=CC(N2CCN(CCCCOC=3C=C4NC(=O)CCC4=CC=3)CC2)=C1Cl CEUORZQYGODEFX-UHFFFAOYSA-N 0.000 description 1
- 208000036640 Asperger disease Diseases 0.000 description 1
- 201000006062 Asperger syndrome Diseases 0.000 description 1
- COVZYZSDYWQREU-UHFFFAOYSA-N Busulfan Chemical compound CS(=O)(=O)OCCCCOS(C)(=O)=O COVZYZSDYWQREU-UHFFFAOYSA-N 0.000 description 1
- 108091026890 Coding region Proteins 0.000 description 1
- 206010010904 Convulsion Diseases 0.000 description 1
- 206010012559 Developmental delay Diseases 0.000 description 1
- 101150097070 Drd3 gene Proteins 0.000 description 1
- 208000012661 Dyskinesia Diseases 0.000 description 1
- 241001504264 Enteromius jae Species 0.000 description 1
- 239000004471 Glycine Substances 0.000 description 1
- 206010021030 Hypomania Diseases 0.000 description 1
- 201000006347 Intellectual Disability Diseases 0.000 description 1
- 206010022998 Irritability Diseases 0.000 description 1
- 102000043136 MAP kinase family Human genes 0.000 description 1
- 108091054455 MAP kinase family Proteins 0.000 description 1
- 208000019022 Mood disease Diseases 0.000 description 1
- 101100442582 Neurospora crassa (strain ATCC 24698 / 74-OR23-1A / CBS 708.71 / DSM 1257 / FGSC 987) spe-1 gene Proteins 0.000 description 1
- 206010057852 Nicotine dependence Diseases 0.000 description 1
- 101800000989 Oxytocin Proteins 0.000 description 1
- XNOPRXBHLZRZKH-UHFFFAOYSA-N Oxytocin Natural products N1C(=O)C(N)CSSCC(C(=O)N2C(CCC2)C(=O)NC(CC(C)C)C(=O)NCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(CCC(N)=O)NC(=O)C(C(C)CC)NC(=O)C1CC1=CC=C(O)C=C1 XNOPRXBHLZRZKH-UHFFFAOYSA-N 0.000 description 1
- 102100031951 Oxytocin-neurophysin 1 Human genes 0.000 description 1
- 208000001431 Psychomotor Agitation Diseases 0.000 description 1
- 208000027465 Psychotic Affective disease Diseases 0.000 description 1
- 206010038583 Repetitive speech Diseases 0.000 description 1
- 206010038743 Restlessness Diseases 0.000 description 1
- 206010039424 Salivary hypersecretion Diseases 0.000 description 1
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 description 1
- 208000025569 Tobacco Use disease Diseases 0.000 description 1
- 206010044565 Tremor Diseases 0.000 description 1
- 230000001594 aberrant effect Effects 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 230000005856 abnormality Effects 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 230000016571 aggressive behavior Effects 0.000 description 1
- 201000007930 alcohol dependence Diseases 0.000 description 1
- 230000004075 alteration Effects 0.000 description 1
- 150000001413 amino acids Chemical group 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 210000003484 anatomy Anatomy 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 230000000844 anti-bacterial effect Effects 0.000 description 1
- 239000001961 anticonvulsive agent Substances 0.000 description 1
- 239000000935 antidepressant agent Substances 0.000 description 1
- 229940005513 antidepressants Drugs 0.000 description 1
- 229940121375 antifungal agent Drugs 0.000 description 1
- 239000003429 antifungal agent Substances 0.000 description 1
- 230000036506 anxiety Effects 0.000 description 1
- 229960004372 aripiprazole Drugs 0.000 description 1
- 239000003693 atypical antipsychotic agent Substances 0.000 description 1
- 229940127236 atypical antipsychotics Drugs 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid group Chemical group C(C1=CC=CC=C1)(=O)O WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 230000001364 causal effect Effects 0.000 description 1
- 210000003169 central nervous system Anatomy 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 230000002759 chromosomal effect Effects 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 230000009194 climbing Effects 0.000 description 1
- 230000019771 cognition Effects 0.000 description 1
- 230000001149 cognitive effect Effects 0.000 description 1
- 238000012937 correction Methods 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 230000003111 delayed effect Effects 0.000 description 1
- 229940075925 depakote Drugs 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- GLUUGHFHXGJENI-UHFFFAOYSA-N diethylenediamine Natural products C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 description 1
- 239000013583 drug formulation Substances 0.000 description 1
- 230000008451 emotion Effects 0.000 description 1
- 230000002996 emotional effect Effects 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 230000007608 epigenetic mechanism Effects 0.000 description 1
- 206010015037 epilepsy Diseases 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 230000001815 facial effect Effects 0.000 description 1
- 230000004720 fertilization Effects 0.000 description 1
- 230000001605 fetal effect Effects 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 230000003370 grooming effect Effects 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 230000005802 health problem Effects 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 150000007529 inorganic bases Chemical class 0.000 description 1
- 230000003993 interaction Effects 0.000 description 1
- 230000002452 interceptive effect Effects 0.000 description 1
- 210000000936 intestine Anatomy 0.000 description 1
- 238000003674 kinase activity assay Methods 0.000 description 1
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical class CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- 239000003446 ligand Substances 0.000 description 1
- 230000000670 limiting effect Effects 0.000 description 1
- 230000036244 malformation Effects 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 230000003340 mental effect Effects 0.000 description 1
- HNQIVZYLYMDVSB-UHFFFAOYSA-N methanesulfonimidic acid Chemical compound CS(N)(=O)=O HNQIVZYLYMDVSB-UHFFFAOYSA-N 0.000 description 1
- BABMCXWQNSQAOC-UHFFFAOYSA-M methylmercury chloride Chemical compound C[Hg]Cl BABMCXWQNSQAOC-UHFFFAOYSA-M 0.000 description 1
- 230000000877 morphologic effect Effects 0.000 description 1
- 238000010172 mouse model Methods 0.000 description 1
- 230000000926 neurological effect Effects 0.000 description 1
- 210000002569 neuron Anatomy 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 150000007530 organic bases Chemical class 0.000 description 1
- 230000008520 organization Effects 0.000 description 1
- XNOPRXBHLZRZKH-DSZYJQQASA-N oxytocin Chemical compound C([C@H]1C(=O)N[C@H](C(N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CSSC[C@H](N)C(=O)N1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)=O)[C@@H](C)CC)C1=CC=C(O)C=C1 XNOPRXBHLZRZKH-DSZYJQQASA-N 0.000 description 1
- 229960001723 oxytocin Drugs 0.000 description 1
- 239000004031 partial agonist Substances 0.000 description 1
- 230000002093 peripheral effect Effects 0.000 description 1
- 230000002085 persistent effect Effects 0.000 description 1
- 230000006461 physiological response Effects 0.000 description 1
- 239000011148 porous material Substances 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 210000002442 prefrontal cortex Anatomy 0.000 description 1
- 230000035935 pregnancy Effects 0.000 description 1
- 206010036596 premature ejaculation Diseases 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 230000008707 rearrangement Effects 0.000 description 1
- 229940044551 receptor antagonist Drugs 0.000 description 1
- 239000002464 receptor antagonist Substances 0.000 description 1
- 230000002829 reductive effect Effects 0.000 description 1
- 230000003989 repetitive behavior Effects 0.000 description 1
- 208000013406 repetitive behavior Diseases 0.000 description 1
- 230000002441 reversible effect Effects 0.000 description 1
- 229960001534 risperidone Drugs 0.000 description 1
- RAPZEAPATHNIPO-UHFFFAOYSA-N risperidone Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCCC4=NC=3C)=NOC2=C1 RAPZEAPATHNIPO-UHFFFAOYSA-N 0.000 description 1
- 102220005833 rs6280 Human genes 0.000 description 1
- 208000026451 salivation Diseases 0.000 description 1
- 239000012266 salt solution Substances 0.000 description 1
- 201000000377 schizophrenia 3 Diseases 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 239000012896 selective serotonin reuptake inhibitor Substances 0.000 description 1
- 229940124834 selective serotonin reuptake inhibitor Drugs 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 230000011273 social behavior Effects 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 238000007619 statistical method Methods 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 229940124530 sulfonamide Drugs 0.000 description 1
- 150000003456 sulfonamides Chemical class 0.000 description 1
- 230000003390 teratogenic effect Effects 0.000 description 1
- 230000004797 therapeutic response Effects 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 239000013598 vector Substances 0.000 description 1
- 210000001030 ventral striatum Anatomy 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4168—1,3-Diazoles having a nitrogen attached in position 2, e.g. clonidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/08—Peptides having 5 to 11 amino acids
- A61K38/095—Oxytocins; Vasopressins; Related peptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13306726 | 2013-12-13 | ||
| PCT/EP2014/077635 WO2015086836A1 (en) | 2013-12-13 | 2014-12-12 | A chromone derivative as a dopamine d3 receptor antagonist for its use for the treatment of autism spectrum disorder |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SA516371298B1 true SA516371298B1 (ar) | 2018-06-07 |
Family
ID=49883003
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SA516371298A SA516371298B1 (ar) | 2013-12-13 | 2016-06-12 | مشتق الكرومون كمضاد لمستقبل الدوبامين د3 واستخدامه في علاج اضطراب طيف التوحد |
Country Status (29)
| Country | Link |
|---|---|
| US (1) | US10028948B2 (enExample) |
| EP (1) | EP3079688B1 (enExample) |
| JP (1) | JP6419826B2 (enExample) |
| KR (1) | KR102280530B1 (enExample) |
| CN (1) | CN105792824B (enExample) |
| AU (1) | AU2014363428B2 (enExample) |
| BR (1) | BR112016012552A8 (enExample) |
| CA (1) | CA2932791C (enExample) |
| CY (1) | CY1119907T1 (enExample) |
| DK (1) | DK3079688T3 (enExample) |
| ES (1) | ES2657706T3 (enExample) |
| HR (1) | HRP20180323T8 (enExample) |
| HU (1) | HUE036035T2 (enExample) |
| IL (1) | IL245996B (enExample) |
| LT (1) | LT3079688T (enExample) |
| MA (1) | MA39076A1 (enExample) |
| MX (1) | MX372922B (enExample) |
| MY (1) | MY172937A (enExample) |
| NO (1) | NO3079688T3 (enExample) |
| NZ (1) | NZ720868A (enExample) |
| PL (1) | PL3079688T3 (enExample) |
| PT (1) | PT3079688T (enExample) |
| RS (1) | RS56931B1 (enExample) |
| RU (2) | RU2019104946A (enExample) |
| SA (1) | SA516371298B1 (enExample) |
| SI (1) | SI3079688T1 (enExample) |
| TN (1) | TN2016000213A1 (enExample) |
| UA (1) | UA117271C2 (enExample) |
| WO (1) | WO2015086836A1 (enExample) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI2317852T1 (sl) | 2008-07-16 | 2015-04-30 | Richter Gedeon Nyrt. | Farmacevtske formulacije, ki vsebujejo ligande dopaminskega receptorja |
| US11274087B2 (en) | 2016-07-08 | 2022-03-15 | Richter Gedeon Nyrt. | Industrial process for the preparation of cariprazine |
| HU231500B1 (hu) | 2019-04-10 | 2024-04-28 | Richter Gedeon Nyrt | Karbamoil-ciklohexán származékok autizmus spektrum betegség kezelésére |
| US11547707B2 (en) | 2019-04-10 | 2023-01-10 | Richter Gedeon Nyrt. | Carbamoyl cyclohexane derivatives for treating autism spectrum disorder |
| WO2021048544A1 (en) * | 2019-09-11 | 2021-03-18 | Oxford Biodynamics Limited | Diagnostic chromosome marker |
| KR20220021157A (ko) | 2020-08-13 | 2022-02-22 | 원광대학교산학협력단 | 옥시토신 호르몬 증가효과를 갖는 자폐스펙트럼장애 아동 개선용 교육시스템 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2682953B1 (fr) | 1991-10-23 | 1995-04-21 | Inst Nat Sante Rech Med | Nouveaux derives de naphtamides, leur procede de preparation et leur application dans le domaine therapeutique. |
| DE4229880A1 (de) | 1992-09-04 | 1994-03-31 | Knauf Siegfried | Medikament bzw. Medikamentenzusammensetzung |
| PE20001088A1 (es) * | 1998-10-08 | 2000-12-02 | Smithkline Beecham Plc | Compuestos derivados de tetrahidrobenzazepina |
| ES2367868T3 (es) * | 2004-09-20 | 2011-11-10 | Mount Sinai School Of Medicine | Uso de memantina (namenda) para tratar el autismo, la compulsividad y la impulsividad. |
| EP2263665A1 (en) | 2009-06-02 | 2010-12-22 | Pharnext | New compositions for treating CMT and related disorders |
| FR2949465B1 (fr) * | 2009-09-01 | 2011-08-12 | Pf Medicament | Derives chromones, leur procede de preparation et leurs applications therapeutiques |
| WO2011150380A1 (en) | 2010-05-28 | 2011-12-01 | Xenoport, Inc. | Methods of treatment of fragile x syndrome, down's syndrome, autism and related disorders |
| KR101921772B1 (ko) * | 2011-05-13 | 2018-11-23 | 가부시키가이샤 한도오따이 에네루기 켄큐쇼 | 반도체 장치 |
| FR2976179A1 (fr) | 2011-06-09 | 2012-12-14 | Pf Medicament | Utilisation de la carpipramine dans le traitement de troubles psychiatriques et du developpement chez l'enfant et l'adolescent |
-
2014
- 2014-12-12 CA CA2932791A patent/CA2932791C/en active Active
- 2014-12-12 EP EP14812465.4A patent/EP3079688B1/en not_active Not-in-force
- 2014-12-12 AU AU2014363428A patent/AU2014363428B2/en not_active Ceased
- 2014-12-12 JP JP2016538587A patent/JP6419826B2/ja not_active Expired - Fee Related
- 2014-12-12 PT PT148124654T patent/PT3079688T/pt unknown
- 2014-12-12 PL PL14812465T patent/PL3079688T3/pl unknown
- 2014-12-12 RS RS20180196A patent/RS56931B1/sr unknown
- 2014-12-12 HU HUE14812465A patent/HUE036035T2/hu unknown
- 2014-12-12 UA UAA201607311A patent/UA117271C2/uk unknown
- 2014-12-12 DK DK14812465.4T patent/DK3079688T3/da active
- 2014-12-12 MX MX2016007612A patent/MX372922B/es active IP Right Grant
- 2014-12-12 MA MA39076A patent/MA39076A1/fr unknown
- 2014-12-12 MY MYPI2016702136A patent/MY172937A/en unknown
- 2014-12-12 ES ES14812465.4T patent/ES2657706T3/es active Active
- 2014-12-12 WO PCT/EP2014/077635 patent/WO2015086836A1/en not_active Ceased
- 2014-12-12 US US15/103,470 patent/US10028948B2/en active Active
- 2014-12-12 CN CN201480066587.4A patent/CN105792824B/zh not_active Expired - Fee Related
- 2014-12-12 TN TN2016000213A patent/TN2016000213A1/en unknown
- 2014-12-12 RU RU2019104946A patent/RU2019104946A/ru unknown
- 2014-12-12 KR KR1020167015313A patent/KR102280530B1/ko not_active Expired - Fee Related
- 2014-12-12 LT LTEP14812465.4T patent/LT3079688T/lt unknown
- 2014-12-12 BR BR112016012552A patent/BR112016012552A8/pt not_active Application Discontinuation
- 2014-12-12 NZ NZ720868A patent/NZ720868A/en not_active IP Right Cessation
- 2014-12-12 NO NO14812465A patent/NO3079688T3/no unknown
- 2014-12-12 HR HRP20180323TT patent/HRP20180323T8/hr unknown
- 2014-12-12 RU RU2016125829A patent/RU2686110C1/ru active
- 2014-12-12 SI SI201430603T patent/SI3079688T1/en unknown
-
2016
- 2016-06-02 IL IL245996A patent/IL245996B/en active IP Right Grant
- 2016-06-12 SA SA516371298A patent/SA516371298B1/ar unknown
-
2018
- 2018-02-09 CY CY20181100159T patent/CY1119907T1/el unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| SA516371298B1 (ar) | مشتق الكرومون كمضاد لمستقبل الدوبامين د3 واستخدامه في علاج اضطراب طيف التوحد | |
| Haure-Mirande et al. | Deficiency of TYROBP, an adapter protein for TREM2 and CR3 receptors, is neuroprotective in a mouse model of early Alzheimer’s pathology | |
| Costa et al. | Prospects for improving brain function in individuals with Down syndrome | |
| Saldarriaga et al. | Phenobarbital use and neurological problems in FMR1 premutation carriers | |
| US20220096455A1 (en) | Use of roluperidone to treat negative symptoms and disorders, increase neuroplasticity, and promote neuroprotection | |
| Cao et al. | ErbB4 deletion in noradrenergic neurons in the locus coeruleus induces mania-like behavior via elevated catecholamines | |
| IL319305A (en) | Pridopidine and analogues for the treatment of mitochondrial diseases and disorders and symptoms associated with these diseases | |
| Streata et al. | Phenotype heterogeneity in 3q29 microduplication syndrome | |
| Miziak et al. | Approaches for the discovery of drugs that target K Na 1.1 channels in KCNT1-associated epilepsy | |
| WO2022047212A1 (en) | Compositions and methods for treating neurodegenerative disorders | |
| US20240068035A1 (en) | Method for diagnosing and treating subjects having single nucleotide polymorphisms in chromosome 2, 2:107,510,000-107,540,000 locus | |
| US20220364172A1 (en) | Method for diagnosing and treating subjects having single nucleotide polymorphisms in chromosome 2, 2:107,510,000-107,540,000 locus | |
| OA17906A (en) | A chromone derivative as a dopamine D3 receptor antagonist for its use for the treatment of autism spectrum disorder. | |
| HK1223563B (zh) | 色酮衍生物作为多巴胺d3受体拮抗剂用於治疗自闭症谱系障碍的用途 | |
| Prananjaya et al. | DRD2 Gene Polymorphisms in Schizophrenia Patients | |
| RU2812786C2 (ru) | Применение ролуперидона для лечения негативных симптомов и заболеваний, повышения нейропластичности и содействия нейрозащите | |
| Acevedo-Triana | Social Dominance and Cortical Neuronal Synchrony in Male Mecp2 Knockout Mice | |
| Kaur | Rare autosomal dominant mutations in GNAL are associated with primary torsion dystonia. | |
| EP4322946A1 (en) | Treatment of prodromal huntington disease | |
| Li | Autosomal Recessive Spastic Ataxia of Charlevoix-Saguenay (ARSACS): a once obscure neurodegenerative disease with increasing significance for neurological research. | |
| Caron | Using Förster Resonance Energy Transfer (FRET) To Define the Conformational Changes of Huntingtin at the Clinical Threshold for Huntington’s Disease | |
| Gambina et al. | Energy expenditure and Alzheimer disease | |
| Langen et al. | P. 7. a. 001 Changes in the developmental trajectories of striatum in autism | |
| Juhász et al. | P. 2.019 Serotonin 2A receptor gene T102C polymorphismand the response to treatment with second-generation antipsychotics in schizophrenia | |
| Tsuboi et al. | Clinical Diagnosis of Familial Atypical Parkinsonian Disorders |