JP2008517977A - 小児用nk2アンタゴニストに基づく製剤処方 - Google Patents
小児用nk2アンタゴニストに基づく製剤処方 Download PDFInfo
- Publication number
- JP2008517977A JP2008517977A JP2007538414A JP2007538414A JP2008517977A JP 2008517977 A JP2008517977 A JP 2008517977A JP 2007538414 A JP2007538414 A JP 2007538414A JP 2007538414 A JP2007538414 A JP 2007538414A JP 2008517977 A JP2008517977 A JP 2008517977A
- Authority
- JP
- Japan
- Prior art keywords
- piperidin
- dichlorophenyl
- cyclo
- ylmethyl
- phenyl
- 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.)
- Pending
Links
- 239000005557 antagonist Substances 0.000 title claims description 36
- 238000009472 formulation Methods 0.000 title description 6
- 239000000203 mixture Substances 0.000 title description 6
- 206010021746 Infantile colic Diseases 0.000 claims abstract description 18
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 12
- 239000002746 neurokinin 2 receptor antagonist Substances 0.000 claims abstract description 4
- -1 benzo [b] thiophenyl-2-ylcarbonyl Chemical group 0.000 claims description 20
- 108010092101 MEN 11420 Proteins 0.000 claims description 14
- NGCNKEZHGRXHNL-WVWQGFTISA-N n-[(2r,3r,4r,5s,6r)-3-acetamido-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]-2-[(1s,4s,7s,10s,13s,16s)-13-benzyl-16-(1h-indol-3-ylmethyl)-7-(2-methylpropyl)-3,6,9,12,15,18,20-heptaoxo-2,5,8,11,14,17,21-heptazabicyclo[8.8.4]docosan-4-yl]acetamide Chemical compound C([C@H]1C(=O)N[C@H]2CC(=O)NC[C@H](NC(=O)[C@H](CC=3C=CC=CC=3)NC(=O)[C@H](CC=3C4=CC=CC=C4NC=3)NC2=O)C(=O)N[C@H](C(N1)=O)CC(C)C)C(=O)N[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1NC(C)=O NGCNKEZHGRXHNL-WVWQGFTISA-N 0.000 claims description 14
- 229950000640 nepadutant Drugs 0.000 claims description 14
- 102000003141 Tachykinin Human genes 0.000 claims description 12
- 108060008037 tachykinin Proteins 0.000 claims description 12
- 239000000556 agonist Substances 0.000 claims description 7
- PGKXDIMONUAMFR-AREMUKBSSA-N saredutant Chemical compound C([C@H](CN(C)C(=O)C=1C=CC=CC=1)C=1C=C(Cl)C(Cl)=CC=1)CN(CC1)CCC1(NC(C)=O)C1=CC=CC=C1 PGKXDIMONUAMFR-AREMUKBSSA-N 0.000 claims description 7
- 125000004189 3,4-dichlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(Cl)C([H])=C1* 0.000 claims description 6
- 125000005605 benzo group Chemical group 0.000 claims description 6
- 125000003003 spiro group Chemical group 0.000 claims description 6
- RMRHFQVHSFCBEO-UHFFFAOYSA-N n-[2-(3,4-dichlorophenyl)-4-(3-oxospiro[2,4-dihydroisoquinoline-1,4'-piperidine]-1'-yl)butyl]-3,4,5-trimethoxy-n-methylbenzamide Chemical compound COC1=C(OC)C(OC)=CC(C(=O)N(C)CC(CCN2CCC3(CC2)C2=CC=CC=C2CC(=O)N3)C=2C=C(Cl)C(Cl)=CC=2)=C1 RMRHFQVHSFCBEO-UHFFFAOYSA-N 0.000 claims description 4
- 239000006188 syrup Substances 0.000 claims description 4
- 235000020357 syrup Nutrition 0.000 claims description 4
- YZOZCHDVAUTVSW-BPBFJQSFSA-N (e)-but-2-enedioic acid;3-cyano-n-[(2s)-2-(3,4-dichlorophenyl)-4-[4-[2-[(s)-methylsulfinyl]phenyl]piperidin-1-yl]butyl]-n-methylnaphthalene-1-carboxamide Chemical compound OC(=O)\C=C\C(O)=O.C([C@H](CN(C)C(=O)C=1C2=CC=CC=C2C=C(C=1)C#N)C=1C=C(Cl)C(Cl)=CC=1)CN(CC1)CCC1C1=CC=CC=C1[S@](C)=O YZOZCHDVAUTVSW-BPBFJQSFSA-N 0.000 claims description 3
- KCUILQGDURJIIL-WLHGVMLRSA-N (e)-but-2-enedioic acid;n-[2-(3,4-dichlorophenyl)-4-(3-oxospiro[2,4-dihydroisoquinoline-1,4'-piperidine]-1'-yl)butyl]-4-fluoro-n-methylbenzamide Chemical compound OC(=O)\C=C\C(O)=O.C=1C=C(F)C=CC=1C(=O)N(C)CC(CCN1CCC2(CC1)C1=CC=CC=C1CC(=O)N2)C1=CC=C(Cl)C(Cl)=C1 KCUILQGDURJIIL-WLHGVMLRSA-N 0.000 claims description 3
- MZDYAVCNKNXCIS-ONEGZZNKSA-N (e)-pent-2-enamide Chemical compound CC\C=C\C(N)=O MZDYAVCNKNXCIS-ONEGZZNKSA-N 0.000 claims description 3
- QNLIUVLFRVYNCV-XIFFEERXSA-N 3-[1-[2-[(2r)-4-benzoyl-2-(3,4-difluorophenyl)morpholin-2-yl]ethyl]-4-phenylpiperidin-4-yl]-1,1-dimethylurea Chemical compound C([C@@](OCC1)(CCN2CCC(CC2)(NC(=O)N(C)C)C=2C=CC=CC=2)C=2C=C(F)C(F)=CC=2)N1C(=O)C1=CC=CC=C1 QNLIUVLFRVYNCV-XIFFEERXSA-N 0.000 claims description 3
- YQYSVMKCMIUCHY-WJOKGBTCSA-N 6-methyl-n-[1-[[(2r)-1-[[1-(oxan-4-ylmethyl)piperidin-4-yl]methylamino]-1-oxo-3-phenylpropan-2-yl]carbamoyl]cyclopentyl]-1-benzothiophene-2-carboxamide Chemical compound S1C2=CC(C)=CC=C2C=C1C(=O)NC1(C(=O)N[C@H](CC=2C=CC=CC=2)C(=O)NCC2CCN(CC3CCOCC3)CC2)CCCC1 YQYSVMKCMIUCHY-WJOKGBTCSA-N 0.000 claims description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims description 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 3
- WQZGKKKJIJFFOK-DVKNGEFBSA-N alpha-D-glucose Chemical compound OC[C@H]1O[C@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-DVKNGEFBSA-N 0.000 claims description 3
- 125000001488 beta-D-galactosyl group Chemical group C1([C@H](O)[C@@H](O)[C@@H](O)[C@H](O1)CO)* 0.000 claims description 3
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 3
- RWTNPBWLLIMQHL-UHFFFAOYSA-N fexofenadine Chemical compound C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RWTNPBWLLIMQHL-UHFFFAOYSA-N 0.000 claims description 3
- RCCPEORTSYDPMB-UHFFFAOYSA-N hydroxy benzenecarboximidothioate Chemical compound OSC(=N)C1=CC=CC=C1 RCCPEORTSYDPMB-UHFFFAOYSA-N 0.000 claims description 3
- 235000013336 milk Nutrition 0.000 claims description 3
- 239000008267 milk Substances 0.000 claims description 3
- 210000004080 milk Anatomy 0.000 claims description 3
- 125000004312 morpholin-2-yl group Chemical group [H]N1C([H])([H])C([H])([H])OC([H])(*)C1([H])[H] 0.000 claims description 3
- WKNPCENNHUVUFW-UHFFFAOYSA-N n-methyl-3,5-bis(trifluoromethyl)benzamide Chemical compound CNC(=O)C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1 WKNPCENNHUVUFW-UHFFFAOYSA-N 0.000 claims description 3
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 claims description 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 3
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 3
- LEWDKQKVAFOMPI-UHFFFAOYSA-N quinoline-4-carboxamide Chemical compound C1=CC=C2C(C(=O)N)=CC=NC2=C1 LEWDKQKVAFOMPI-UHFFFAOYSA-N 0.000 claims description 3
- 229950004387 saredutant Drugs 0.000 claims description 3
- DUIOPKIIICUYRZ-UHFFFAOYSA-N semicarbazide Chemical compound NNC(N)=O DUIOPKIIICUYRZ-UHFFFAOYSA-N 0.000 claims description 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 2
- 239000002462 tachykinin receptor antagonist Substances 0.000 claims 4
- 235000013305 food Nutrition 0.000 claims 3
- CVZIVLWQSXJHER-UUWRZZSWSA-N 6-bromo-n-[1-[[(2r)-1-[[1-(oxan-4-ylmethyl)piperidin-4-yl]methylamino]-1-oxo-3-phenylpropan-2-yl]carbamoyl]cyclopentyl]naphthalene-2-carboxamide Chemical compound C1=CC2=CC(Br)=CC=C2C=C1C(=O)NC1(C(=O)N[C@H](CC=2C=CC=CC=2)C(=O)NCC2CCN(CC3CCOCC3)CC2)CCCC1 CVZIVLWQSXJHER-UUWRZZSWSA-N 0.000 claims 2
- KQOZGMVAKCVJHO-UHFFFAOYSA-N 5-iodo-1-benzofuran-2-carboxylic acid Chemical compound IC1=CC=C2OC(C(=O)O)=CC2=C1 KQOZGMVAKCVJHO-UHFFFAOYSA-N 0.000 claims 1
- NWPCYSBUHRRUPL-SSEXGKCCSA-N 5-iodo-n-[1-[[(2r)-1-[[1-(oxan-4-ylmethyl)piperidin-4-yl]methylamino]-1-oxo-3-phenylpropan-2-yl]carbamoyl]cyclopentyl]-1-benzofuran-2-carboxamide Chemical compound C=1C2=CC(I)=CC=C2OC=1C(=O)NC1(C(=O)N[C@H](CC=2C=CC=CC=2)C(=O)NCC2CCN(CC3CCOCC3)CC2)CCCC1 NWPCYSBUHRRUPL-SSEXGKCCSA-N 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 239000008203 oral pharmaceutical composition Substances 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 description 11
- 230000000694 effects Effects 0.000 description 9
- 208000002551 irritable bowel syndrome Diseases 0.000 description 9
- 241000700159 Rattus Species 0.000 description 8
- 230000000968 intestinal effect Effects 0.000 description 8
- 239000003814 drug Substances 0.000 description 7
- 229940079593 drug Drugs 0.000 description 7
- 239000002253 acid Substances 0.000 description 6
- QNAYBMKLOCPYGJ-UHFFFAOYSA-N D-alpha-Ala Natural products CC([NH3+])C([O-])=O QNAYBMKLOCPYGJ-UHFFFAOYSA-N 0.000 description 5
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 5
- 101800000399 Neurokinin A Proteins 0.000 description 5
- 102400000097 Neurokinin A Human genes 0.000 description 5
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 5
- UCMIRNVEIXFBKS-UHFFFAOYSA-N beta-alanine Chemical compound NCCC(O)=O UCMIRNVEIXFBKS-UHFFFAOYSA-N 0.000 description 5
- BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 description 5
- 239000000796 flavoring agent Substances 0.000 description 5
- 235000019634 flavors Nutrition 0.000 description 5
- 239000008103 glucose Substances 0.000 description 5
- 235000010199 sorbic acid Nutrition 0.000 description 5
- 229940075582 sorbic acid Drugs 0.000 description 5
- 239000004334 sorbic acid Substances 0.000 description 5
- ZBUZIBZYOBBFML-XMMPIXPASA-N 1-amino-n-[(2r)-1-[[1-(oxan-4-ylmethyl)piperidin-4-yl]methylamino]-1-oxo-3-phenylpropan-2-yl]cyclopentane-1-carboxamide Chemical compound N([C@H](CC=1C=CC=CC=1)C(=O)NCC1CCN(CC2CCOCC2)CC1)C(=O)C1(N)CCCC1 ZBUZIBZYOBBFML-XMMPIXPASA-N 0.000 description 4
- 208000004454 Hyperalgesia Diseases 0.000 description 4
- 208000035154 Hyperesthesia Diseases 0.000 description 4
- HEAUFJZALFKPBA-YRVBCFNBSA-N Neurokinin A Chemical compound C([C@@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(N)=O)C(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CC=1NC=NC=1)C(C)O)C1=CC=CC=C1 HEAUFJZALFKPBA-YRVBCFNBSA-N 0.000 description 4
- 208000002193 Pain Diseases 0.000 description 4
- 239000007864 aqueous solution Substances 0.000 description 4
- 239000001768 carboxy methyl cellulose Substances 0.000 description 4
- 230000009278 visceral effect Effects 0.000 description 4
- 208000004998 Abdominal Pain Diseases 0.000 description 3
- 208000002881 Colic Diseases 0.000 description 3
- 235000011034 Rubus glaucus Nutrition 0.000 description 3
- 244000235659 Rubus idaeus Species 0.000 description 3
- 235000009122 Rubus idaeus Nutrition 0.000 description 3
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 239000006071 cream Substances 0.000 description 3
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 3
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 3
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 3
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 3
- 230000000638 stimulation Effects 0.000 description 3
- QDZOEBFLNHCSSF-PFFBOGFISA-N (2S)-2-[[(2R)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-1-[(2R)-2-amino-5-carbamimidamidopentanoyl]pyrrolidine-2-carbonyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-N-[(2R)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]pentanediamide Chemical compound C([C@@H](C(=O)N[C@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)NC(=O)[C@@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCCCN)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](N)CCCNC(N)=N)C1=CC=CC=C1 QDZOEBFLNHCSSF-PFFBOGFISA-N 0.000 description 2
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 2
- 206010010904 Convulsion Diseases 0.000 description 2
- 208000018522 Gastrointestinal disease Diseases 0.000 description 2
- 206010020751 Hypersensitivity Diseases 0.000 description 2
- 206010061218 Inflammation Diseases 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 102000046798 Neurokinin B Human genes 0.000 description 2
- NHXYSAFTNPANFK-HDMCBQFHSA-N Neurokinin B Chemical compound C([C@@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(N)=O)C(C)C)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CCSC)NC(=O)[C@@H](N)CC(O)=O)C1=CC=CC=C1 NHXYSAFTNPANFK-HDMCBQFHSA-N 0.000 description 2
- 108010040722 Neurokinin-2 Receptors Proteins 0.000 description 2
- 101800002813 Neurokinin-B Proteins 0.000 description 2
- 108090000189 Neuropeptides Proteins 0.000 description 2
- 102100024304 Protachykinin-1 Human genes 0.000 description 2
- 101800003906 Substance P Proteins 0.000 description 2
- 102100037342 Substance-K receptor Human genes 0.000 description 2
- 208000026935 allergic disease Diseases 0.000 description 2
- 238000010171 animal model Methods 0.000 description 2
- 125000002619 bicyclic group Chemical group 0.000 description 2
- 230000004071 biological effect Effects 0.000 description 2
- 229910052799 carbon Inorganic materials 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 230000008602 contraction Effects 0.000 description 2
- 230000036461 convulsion Effects 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 239000003205 fragrance Substances 0.000 description 2
- 230000005176 gastrointestinal motility Effects 0.000 description 2
- 210000001035 gastrointestinal tract Anatomy 0.000 description 2
- 230000009610 hypersensitivity Effects 0.000 description 2
- 235000021129 infant diet Nutrition 0.000 description 2
- 230000004054 inflammatory process Effects 0.000 description 2
- 230000001575 pathological effect Effects 0.000 description 2
- 210000001428 peripheral nervous system Anatomy 0.000 description 2
- 239000000546 pharmaceutical excipient Substances 0.000 description 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 2
- 102000005962 receptors Human genes 0.000 description 2
- 108020003175 receptors Proteins 0.000 description 2
- 239000000725 suspension Substances 0.000 description 2
- 230000008961 swelling Effects 0.000 description 2
- 208000009935 visceral pain Diseases 0.000 description 2
- 208000009079 Bronchial Spasm Diseases 0.000 description 1
- 208000014181 Bronchial disease Diseases 0.000 description 1
- 206010006482 Bronchospasm Diseases 0.000 description 1
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 1
- 206010010774 Constipation Diseases 0.000 description 1
- 206010011224 Cough Diseases 0.000 description 1
- 206010011469 Crying Diseases 0.000 description 1
- 206010012735 Diarrhoea Diseases 0.000 description 1
- 239000004278 EU approved seasoning Substances 0.000 description 1
- 235000016623 Fragaria vesca Nutrition 0.000 description 1
- 240000009088 Fragaria x ananassa Species 0.000 description 1
- 235000011363 Fragaria x ananassa Nutrition 0.000 description 1
- 206010017999 Gastrointestinal pain Diseases 0.000 description 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- 208000009793 Milk Hypersensitivity Diseases 0.000 description 1
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 1
- 206010035664 Pneumonia Diseases 0.000 description 1
- 108010083785 TAC 363 Proteins 0.000 description 1
- 230000003042 antagnostic effect Effects 0.000 description 1
- 230000001078 anti-cholinergic effect Effects 0.000 description 1
- 229940125681 anticonvulsant agent Drugs 0.000 description 1
- 239000001961 anticonvulsive agent Substances 0.000 description 1
- 229940125714 antidiarrheal agent Drugs 0.000 description 1
- 239000003793 antidiarrheal agent Substances 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 235000006708 antioxidants Nutrition 0.000 description 1
- 235000010323 ascorbic acid Nutrition 0.000 description 1
- 229960005070 ascorbic acid Drugs 0.000 description 1
- 239000011668 ascorbic acid Substances 0.000 description 1
- 208000006673 asthma Diseases 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 235000019658 bitter taste Nutrition 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 1
- 230000001364 causal effect Effects 0.000 description 1
- 210000003169 central nervous system Anatomy 0.000 description 1
- 201000003146 cystitis Diseases 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- XXJWXESWEXIICW-UHFFFAOYSA-N diethylene glycol monoethyl ether Chemical compound CCOCCOCCO XXJWXESWEXIICW-UHFFFAOYSA-N 0.000 description 1
- 229940075557 diethylene glycol monoethyl ether Drugs 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 235000011194 food seasoning agent Nutrition 0.000 description 1
- 235000003599 food sweetener Nutrition 0.000 description 1
- 239000008369 fruit flavor Substances 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 235000020256 human milk Nutrition 0.000 description 1
- 210000004251 human milk Anatomy 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 230000008991 intestinal motility Effects 0.000 description 1
- 238000007912 intraperitoneal administration Methods 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000008141 laxative Substances 0.000 description 1
- 229940125722 laxative agent Drugs 0.000 description 1
- 230000000873 masking effect Effects 0.000 description 1
- 230000035800 maturation Effects 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 125000002950 monocyclic group Chemical group 0.000 description 1
- BHCJHYIMNHXLOM-WVDRJWPYSA-N n-[(e,2r)-1-(3,4-dichlorophenyl)-5-oxo-5-[[(3r)-2-oxoazepan-3-yl]amino]pent-3-en-2-yl]-n-methyl-3,5-bis(trifluoromethyl)benzamide Chemical compound C([C@@H](N(C)C(=O)C=1C=C(C=C(C=1)C(F)(F)F)C(F)(F)F)\C=C\C(=O)N[C@H]1C(NCCCC1)=O)C1=CC=C(Cl)C(Cl)=C1 BHCJHYIMNHXLOM-WVDRJWPYSA-N 0.000 description 1
- 239000002744 neurokinin 2 receptor agonist Substances 0.000 description 1
- 230000001991 pathophysiological effect Effects 0.000 description 1
- 238000011170 pharmaceutical development Methods 0.000 description 1
- 229940068196 placebo Drugs 0.000 description 1
- 239000000902 placebo Substances 0.000 description 1
- 229940069328 povidone Drugs 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 210000002460 smooth muscle Anatomy 0.000 description 1
- 230000016160 smooth muscle contraction Effects 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 230000001052 transient effect Effects 0.000 description 1
- ODLHGICHYURWBS-LKONHMLTSA-N trappsol cyclo Chemical compound CC(O)COC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)COCC(O)C)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1COCC(C)O ODLHGICHYURWBS-LKONHMLTSA-N 0.000 description 1
- 210000000626 ureter Anatomy 0.000 description 1
- 210000001835 viscera 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
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
-
- 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
- A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Plural Heterocyclic Compounds (AREA)
- Coloring Foods And Improving Nutritive Qualities (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IT000221A ITFI20040221A1 (it) | 2004-10-27 | 2004-10-27 | Composizioni farmaceutiche a base di nk2 antagonisti per uso pediatrico |
| ITFI2004A000221 | 2004-10-27 | ||
| PCT/EP2005/055575 WO2006045820A1 (en) | 2004-10-27 | 2005-10-26 | Pharmaceutical compositions based on nk2 antagonists for pediatric use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008517977A true JP2008517977A (ja) | 2008-05-29 |
| JP2008517977A5 JP2008517977A5 (enExample) | 2011-10-06 |
Family
ID=35613882
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007538414A Pending JP2008517977A (ja) | 2004-10-27 | 2005-10-26 | 小児用nk2アンタゴニストに基づく製剤処方 |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US7727955B2 (enExample) |
| EP (1) | EP1809267B1 (enExample) |
| JP (1) | JP2008517977A (enExample) |
| CN (1) | CN101052386A (enExample) |
| AR (1) | AR051595A1 (enExample) |
| AT (1) | ATE422881T1 (enExample) |
| AU (1) | AU2005298629B2 (enExample) |
| CA (1) | CA2584481C (enExample) |
| CY (1) | CY1109803T1 (enExample) |
| DE (1) | DE602005012857D1 (enExample) |
| DK (1) | DK1809267T3 (enExample) |
| EA (1) | EA012264B1 (enExample) |
| ES (1) | ES2325413T3 (enExample) |
| HR (1) | HRP20090225T1 (enExample) |
| IT (1) | ITFI20040221A1 (enExample) |
| MX (1) | MX2007004461A (enExample) |
| NO (1) | NO338586B1 (enExample) |
| NZ (1) | NZ555380A (enExample) |
| PL (1) | PL1809267T3 (enExample) |
| PT (1) | PT1809267E (enExample) |
| RS (1) | RS50780B (enExample) |
| SI (1) | SI1809267T1 (enExample) |
| UA (1) | UA91988C2 (enExample) |
| WO (1) | WO2006045820A1 (enExample) |
| ZA (1) | ZA200703909B (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2015522063A (ja) * | 2012-07-12 | 2015-08-03 | ラボラトリ ギドッティ ソシエタ ペル アチオニ | ネパデュタントを含有する小児用経口液体組成物 |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0614970D0 (en) * | 2006-07-27 | 2006-09-06 | R & D Sosei Ltd | Compounds For Use In Therapy |
| IT1394304B1 (it) * | 2009-05-21 | 2012-06-06 | Malesci Sas | Processo per la preparazione di ibodutant (men15596) e relativi intermedi |
| US9867857B2 (en) | 2014-08-21 | 2018-01-16 | Food Industry Research And Development Institute | Acetobacter and gluconacetobacter strains and their metabolites for use in inhibiting xanthine oxidase |
| US20160051596A1 (en) * | 2014-08-21 | 2016-02-25 | Food Industry Research And Development Institute | Novel acetobacter and gluconacetobacter strains and their metabolites for use in inhibiting xanthine oxidase |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH0219318A (ja) * | 1988-06-30 | 1990-01-23 | Carl R Thornfeldt | 疝痛及び生歯に対する治療 |
| WO2003037916A2 (en) * | 2001-10-29 | 2003-05-08 | Malesci Istituto Farmacobiologico S.P.A. | Linear basic compounds having nk-2 antagonist activity and formulations thereof |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1277835B1 (it) * | 1995-03-13 | 1997-11-12 | Menarini Farma Ind | Composti biciclici, loro preparazione ed uso in composizioni farmaceutiche |
| IT1307809B1 (it) * | 1999-10-21 | 2001-11-19 | Menarini Ricerche Spa | Composti monociclici basici ad azione nk-2 antagonista, processi difabbricazione e formulazioni che li contengono. |
| GB0224788D0 (en) * | 2002-10-24 | 2002-12-04 | Novartis Ag | Organic compounds |
-
2004
- 2004-10-27 IT IT000221A patent/ITFI20040221A1/it unknown
-
2005
- 2005-10-24 AR ARP050104429A patent/AR051595A1/es unknown
- 2005-10-26 PL PL05810894T patent/PL1809267T3/pl unknown
- 2005-10-26 MX MX2007004461A patent/MX2007004461A/es active IP Right Grant
- 2005-10-26 CN CNA2005800370703A patent/CN101052386A/zh active Pending
- 2005-10-26 AU AU2005298629A patent/AU2005298629B2/en not_active Ceased
- 2005-10-26 EA EA200700949A patent/EA012264B1/ru not_active IP Right Cessation
- 2005-10-26 HR HR20090225T patent/HRP20090225T1/xx unknown
- 2005-10-26 WO PCT/EP2005/055575 patent/WO2006045820A1/en not_active Ceased
- 2005-10-26 SI SI200530661T patent/SI1809267T1/sl unknown
- 2005-10-26 PT PT05810894T patent/PT1809267E/pt unknown
- 2005-10-26 UA UAA200705837A patent/UA91988C2/ru unknown
- 2005-10-26 JP JP2007538414A patent/JP2008517977A/ja active Pending
- 2005-10-26 NZ NZ555380A patent/NZ555380A/en not_active IP Right Cessation
- 2005-10-26 AT AT05810894T patent/ATE422881T1/de active
- 2005-10-26 DK DK05810894T patent/DK1809267T3/da active
- 2005-10-26 DE DE602005012857T patent/DE602005012857D1/de not_active Expired - Lifetime
- 2005-10-26 ES ES05810894T patent/ES2325413T3/es not_active Expired - Lifetime
- 2005-10-26 US US11/666,204 patent/US7727955B2/en not_active Expired - Fee Related
- 2005-10-26 CA CA2584481A patent/CA2584481C/en not_active Expired - Fee Related
- 2005-10-26 RS RSP-2009/0169A patent/RS50780B/sr unknown
- 2005-10-26 EP EP05810894A patent/EP1809267B1/en not_active Expired - Lifetime
-
2007
- 2007-05-15 ZA ZA200703909A patent/ZA200703909B/xx unknown
- 2007-05-29 NO NO20072720A patent/NO338586B1/no not_active IP Right Cessation
-
2009
- 2009-05-07 CY CY20091100493T patent/CY1109803T1/el unknown
-
2010
- 2010-04-19 US US12/799,176 patent/US20100234284A1/en not_active Abandoned
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH0219318A (ja) * | 1988-06-30 | 1990-01-23 | Carl R Thornfeldt | 疝痛及び生歯に対する治療 |
| WO2003037916A2 (en) * | 2001-10-29 | 2003-05-08 | Malesci Istituto Farmacobiologico S.P.A. | Linear basic compounds having nk-2 antagonist activity and formulations thereof |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2015522063A (ja) * | 2012-07-12 | 2015-08-03 | ラボラトリ ギドッティ ソシエタ ペル アチオニ | ネパデュタントを含有する小児用経口液体組成物 |
Also Published As
| Publication number | Publication date |
|---|---|
| US20080090795A1 (en) | 2008-04-17 |
| ZA200703909B (en) | 2008-09-25 |
| CA2584481A1 (en) | 2006-05-04 |
| ITFI20040221A1 (it) | 2005-01-27 |
| AU2005298629A1 (en) | 2006-05-04 |
| AR051595A1 (es) | 2007-01-24 |
| RS50780B (sr) | 2010-08-31 |
| SI1809267T1 (sl) | 2009-06-30 |
| WO2006045820A1 (en) | 2006-05-04 |
| US20100234284A1 (en) | 2010-09-16 |
| UA91988C2 (ru) | 2010-09-27 |
| NZ555380A (en) | 2008-12-24 |
| PL1809267T3 (pl) | 2009-07-31 |
| NO20072720L (no) | 2007-07-09 |
| EA200700949A1 (ru) | 2007-10-26 |
| DE602005012857D1 (de) | 2009-04-02 |
| EA012264B1 (ru) | 2009-08-28 |
| CN101052386A (zh) | 2007-10-10 |
| MX2007004461A (es) | 2007-07-11 |
| PT1809267E (pt) | 2009-05-28 |
| EP1809267B1 (en) | 2009-02-18 |
| CY1109803T1 (el) | 2014-09-10 |
| AU2005298629B2 (en) | 2011-02-17 |
| US7727955B2 (en) | 2010-06-01 |
| CA2584481C (en) | 2014-07-15 |
| ATE422881T1 (de) | 2009-03-15 |
| DK1809267T3 (da) | 2009-05-18 |
| HK1109335A1 (en) | 2008-06-06 |
| EP1809267A1 (en) | 2007-07-25 |
| ES2325413T3 (es) | 2009-09-03 |
| NO338586B1 (no) | 2016-09-12 |
| HRP20090225T1 (hr) | 2009-05-31 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2021181465A (ja) | レム睡眠行動障害の予防および処置のために有用なジアリールおよびアリールヘテロアリール尿素誘導体 | |
| JP2008531714A (ja) | 不安障害の治療用及び/又は予防用の医薬組成物 | |
| RU2324484C2 (ru) | Антагонисты метаботропного глутаматного рецептора 5 (mglur5) и способ для профилактики и лечения гастроэзофагеальной рефлюксной болезни (варианты) | |
| HUT76852A (en) | Use of benzotiophene derivatives for production of pharmaceutical compositions useful for inhibiting conditions associated with neuro-peptide y | |
| JP2011513196A (ja) | ドーパミン作動系が破壊された障害もしくは状態の症状を軽減するためまたはその障害もしくは状態を処置するためのkcnqカリウムチャネル開口薬の使用 | |
| TWI428130B (zh) | 治療急性躁狂症之藥學組成物及方法 | |
| EA014189B1 (ru) | Применение флибансерина для лечения расстройств полового влечения в предклимактерический период | |
| CA2641564C (en) | Use of kcnq-openers for treating or reducing the symptoms of schizophrenia | |
| WO1997029739A2 (en) | Use of 5ht4 receptor antagonists for overcoming gastrointestinal effects of serotonin reuptake inhibitors | |
| JP2017119702A (ja) | ギラン・バレー症候群に伴う神経因性疼痛の予防又は治療剤 | |
| US20100234284A1 (en) | Pharmaceutical compositions based on NK2 antagonists for pediatric use | |
| US20220008414A1 (en) | Pharmaceutical composition comprising histone deacetylase 6 inhibitors | |
| JP2002500651A (ja) | 精神分裂病及び精神病の治療方法 | |
| CN116075302A (zh) | GABAAα5激动剂和SV2A抑制剂的组合以及在认知损害的治疗中的使用方法 | |
| US20200129528A1 (en) | Methods for treating blood pressure conditions using aminosterol compositions | |
| KR20060123183A (ko) | 탈리도미드를 포함하는 섬유근육통 치료용 조성물 및 그방법 | |
| CN1216598C (zh) | 药物用途 | |
| JP2008525413A (ja) | 双極性障害を治療するための単剤としてのサブコメリン、または、気分安定剤または抗躁病薬と併用されるサブコメリン | |
| KR20190013847A (ko) | 불안 장애를 치료하기 위한 (2S)-1-[4-(3,4-디클로로페닐)피페리딘-1-일]-3-[2-(5-메틸-1,3,4-옥사디아졸-2-일)벤조[b]푸란-4-일옥시]프로판-2-올 또는 그의 대사산물 | |
| JP2008189616A (ja) | 注意欠陥多動性障害の治療薬 | |
| US20200155495A1 (en) | Pharmaceutical compositions and methods utilizing neostigmine and a nk-1 antagonist for treating myasthenia gravis | |
| JP2002524509A (ja) | 新規組成物 | |
| JP2025502526A (ja) | てんかんにおける突然の予期せぬ死に関連する疾患を治療するためのセロトニン5-ht1a受容体アゴニストの使用 | |
| WO2024102802A1 (en) | Zelatriazin for the treatment of depression | |
| HK1109335B (en) | Pharmaceutical compositions based on nk2 antagonists for pediatric use |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20081007 |
|
| RD01 | Notification of change of attorney |
Free format text: JAPANESE INTERMEDIATE CODE: A7421 Effective date: 20110303 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A821 Effective date: 20110303 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20110531 |
|
| A524 | Written submission of copy of amendment under article 19 pct |
Free format text: JAPANESE INTERMEDIATE CODE: A524 Effective date: 20110819 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20120213 |
|
| A02 | Decision of refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A02 Effective date: 20120723 |