JP2007519646A - 体重の持続的低減のための化合物 - Google Patents
体重の持続的低減のための化合物 Download PDFInfo
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- JP2007519646A JP2007519646A JP2006549961A JP2006549961A JP2007519646A JP 2007519646 A JP2007519646 A JP 2007519646A JP 2006549961 A JP2006549961 A JP 2006549961A JP 2006549961 A JP2006549961 A JP 2006549961A JP 2007519646 A JP2007519646 A JP 2007519646A
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- JP
- Japan
- Prior art keywords
- alkyl
- group
- alkynyl
- alkenyl
- heteroaryl
- 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
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- 230000002459 sustained effect Effects 0.000 title claims abstract description 7
- 150000001875 compounds Chemical class 0.000 title claims description 22
- 230000004580 weight loss Effects 0.000 title claims description 11
- XLRPYZSEQKXZAA-OCAPTIKFSA-N tropane Chemical group C1CC[C@H]2CC[C@@H]1N2C XLRPYZSEQKXZAA-OCAPTIKFSA-N 0.000 claims abstract description 25
- 150000003839 salts Chemical class 0.000 claims abstract description 24
- 239000003112 inhibitor Substances 0.000 claims abstract description 17
- 230000001561 neurotransmitter reuptake Effects 0.000 claims abstract description 17
- 239000012453 solvate Substances 0.000 claims abstract description 12
- 230000037396 body weight Effects 0.000 claims abstract description 9
- 239000003814 drug Substances 0.000 claims abstract description 7
- 238000004519 manufacturing process Methods 0.000 claims abstract description 5
- 230000009467 reduction Effects 0.000 claims abstract description 4
- 125000000217 alkyl group Chemical group 0.000 claims description 49
- 125000003342 alkenyl group Chemical group 0.000 claims description 38
- 125000000304 alkynyl group Chemical group 0.000 claims description 38
- 125000001072 heteroaryl group Chemical group 0.000 claims description 33
- 229910052736 halogen Inorganic materials 0.000 claims description 31
- 125000001424 substituent group Chemical group 0.000 claims description 31
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 30
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 30
- 125000003545 alkoxy group Chemical group 0.000 claims description 29
- 150000002367 halogens Chemical class 0.000 claims description 23
- -1 3,4-methylenedioxyphenyl Chemical group 0.000 claims description 21
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 20
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 20
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 14
- 239000003901 neurotransmitter uptake inhibitor Substances 0.000 claims description 13
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 11
- 125000005843 halogen group Chemical group 0.000 claims description 10
- 229910052739 hydrogen Inorganic materials 0.000 claims description 10
- 239000001257 hydrogen Substances 0.000 claims description 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 7
- 125000000000 cycloalkoxy group Chemical group 0.000 claims description 6
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 claims description 6
- 125000001544 thienyl group Chemical group 0.000 claims description 6
- 125000000319 biphenyl-4-yl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims description 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 4
- 239000013543 active substance Substances 0.000 claims description 4
- XBBDACCLCFWBSI-ZETCQYMHSA-N melevodopa Chemical compound COC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 XBBDACCLCFWBSI-ZETCQYMHSA-N 0.000 claims description 4
- 238000000034 method Methods 0.000 claims description 4
- 229910052760 oxygen Inorganic materials 0.000 claims description 4
- 125000004076 pyridyl group Chemical group 0.000 claims description 4
- 229910052717 sulfur Inorganic materials 0.000 claims description 4
- 229940086609 Lipase inhibitor Drugs 0.000 claims description 3
- 150000001204 N-oxides Chemical class 0.000 claims description 3
- 239000000556 agonist Substances 0.000 claims description 3
- 239000002830 appetite depressant Substances 0.000 claims description 3
- 125000003118 aryl group Chemical group 0.000 claims description 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 3
- 229960003638 dopamine Drugs 0.000 claims description 3
- 150000002431 hydrogen Chemical group 0.000 claims description 3
- GELJVTSEGKGLDF-QDSMGTAFSA-N (2s)-2-[(benzylamino)methyl]-2,3,7,9-tetrahydro-[1,4]dioxino[2,3-e]indol-8-one;(e)-but-2-enedioic acid Chemical compound OC(=O)\C=C\C(O)=O.C([C@H]1COC=2C=CC3=C(C=2O1)CC(N3)=O)NCC1=CC=CC=C1 GELJVTSEGKGLDF-QDSMGTAFSA-N 0.000 claims description 2
- IVTMXOXVAHXCHI-YXLMWLKOSA-N (2s)-2-amino-3-(3,4-dihydroxyphenyl)propanoic acid;(2s)-3-(3,4-dihydroxyphenyl)-2-hydrazinyl-2-methylpropanoic acid Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1.NN[C@@](C(O)=O)(C)CC1=CC=C(O)C(O)=C1 IVTMXOXVAHXCHI-YXLMWLKOSA-N 0.000 claims description 2
- DVLKVIJLALMCBQ-VENMBWNLSA-N (3R,4aR,10aS)-3-(diethylsulfamoylamino)-6-hydroxy-1-propyl-3,4,4a,5,10,10a-hexahydro-2H-benzo[g]quinoline hydrochloride Chemical compound Cl.C1=CC=C2C[C@@H]3N(CCC)C[C@H](NS(=O)(=O)N(CC)CC)C[C@H]3CC2=C1O DVLKVIJLALMCBQ-VENMBWNLSA-N 0.000 claims description 2
- NHCWZEQEFHNLBQ-PPHPATTJSA-N (4s)-4-(3,4-dihydroxyphenyl)-1,2,3,4-tetrahydroisoquinoline-7,8-diol;hydrochloride Chemical compound Cl.C1=C(O)C(O)=CC=C1[C@H]1C2=CC=C(O)C(O)=C2CNC1 NHCWZEQEFHNLBQ-PPHPATTJSA-N 0.000 claims description 2
- MNIXOHSBCFNRSH-UQGUCNKVSA-N (6ar,9r,10ar)-7-methyl-9-(1,2,4-triazol-1-ylmethyl)-6,6a,8,9,10,10a-hexahydro-4h-indolo[4,3-fg]quinoline;(z)-but-2-enedioic acid Chemical compound OC(=O)\C=C/C(O)=O.C([C@H]1CN([C@H]2[C@@H](C=3C=CC=C4NC=C(C=34)C2)C1)C)N1C=NC=N1 MNIXOHSBCFNRSH-UQGUCNKVSA-N 0.000 claims description 2
- BGOQGUHWXBGXJW-YOEHRIQHSA-N (6as,12br)-5,6,6a,7,8,12b-hexahydrobenzo[a]phenanthridine-10,11-diol Chemical compound N1CC2=CC=CC=C2[C@@H]2[C@@H]1CCC1=C2C=C(O)C(O)=C1 BGOQGUHWXBGXJW-YOEHRIQHSA-N 0.000 claims description 2
- SNPPWIUOZRMYNY-SECBINFHSA-N (R)-bupropion Chemical compound CC(C)(C)N[C@H](C)C(=O)C1=CC=CC(Cl)=C1 SNPPWIUOZRMYNY-SECBINFHSA-N 0.000 claims description 2
- JUDKOGFHZYMDMF-UHFFFAOYSA-N 1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol Chemical compound C1=2C=C(O)C(O)=CC=2CCNCC1C1=CC=CC=C1 JUDKOGFHZYMDMF-UHFFFAOYSA-N 0.000 claims description 2
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims description 2
- JTYVLKBMXTUORS-UHFFFAOYSA-N 6-(dipropylamino)-3,4,5,6,7,8-hexahydro-2h-naphthalen-1-one Chemical compound C1C(N(CCC)CCC)CCC2=C1CCCC2=O JTYVLKBMXTUORS-UHFFFAOYSA-N 0.000 claims description 2
- DHSSDEDRBUKTQY-UHFFFAOYSA-N 6-prop-2-enyl-4,5,7,8-tetrahydrothiazolo[4,5-d]azepin-2-amine Chemical compound C1CN(CC=C)CCC2=C1N=C(N)S2 DHSSDEDRBUKTQY-UHFFFAOYSA-N 0.000 claims description 2
- NQRIKTDKFHAOKC-UHFFFAOYSA-N 7-(4-methylpiperazin-1-yl)-3h-1,3-benzoxazol-2-one;hydrochloride Chemical compound Cl.C1CN(C)CCN1C1=CC=CC2=C1OC(=O)N2 NQRIKTDKFHAOKC-UHFFFAOYSA-N 0.000 claims description 2
- RRLWEQBPSAFVAS-UHFFFAOYSA-N 7-[3-[4-(2,3-dimethylphenyl)piperazin-1-yl]propoxy]-1h-quinolin-2-one Chemical compound CC1=CC=CC(N2CCN(CCCOC=3C=C4NC(=O)C=CC4=CC=3)CC2)=C1C RRLWEQBPSAFVAS-UHFFFAOYSA-N 0.000 claims description 2
- XKTGLDSNABUNGD-UHFFFAOYSA-N 9-bromo-5-phenyl-2,3,4,5-tetrahydro-1h-3-benzazepine-7,8-diol Chemical compound C1NCCC=2C(Br)=C(O)C(O)=CC=2C1C1=CC=CC=C1 XKTGLDSNABUNGD-UHFFFAOYSA-N 0.000 claims description 2
- GHWJEDJMOVUXEC-UHFFFAOYSA-N 9-chloro-5-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol Chemical compound C1NCCC=2C(Cl)=C(O)C(O)=CC=2C1C1=CC=CC=C1 GHWJEDJMOVUXEC-UHFFFAOYSA-N 0.000 claims description 2
- HJWHHQIVUHOBQN-UHFFFAOYSA-N 9-chloro-5-phenyl-3-prop-2-enyl-1,2,4,5-tetrahydro-3-benzazepine-7,8-diol Chemical compound C1N(CC=C)CCC=2C(Cl)=C(O)C(O)=CC=2C1C1=CC=CC=C1 HJWHHQIVUHOBQN-UHFFFAOYSA-N 0.000 claims description 2
- CEUORZQYGODEFX-UHFFFAOYSA-N Aripirazole Chemical compound ClC1=CC=CC(N2CCN(CCCCOC=3C=C4NC(=O)CCC4=CC=3)CC2)=C1Cl CEUORZQYGODEFX-UHFFFAOYSA-N 0.000 claims description 2
- CYGODHVAJQTCBG-UHFFFAOYSA-N Bifeprunox Chemical compound C=12OC(=O)NC2=CC=CC=1N(CC1)CCN1CC(C=1)=CC=CC=1C1=CC=CC=C1 CYGODHVAJQTCBG-UHFFFAOYSA-N 0.000 claims description 2
- KORNTPPJEAJQIU-KJXAQDMKSA-N Cabaser Chemical compound C1=CC([C@H]2C[C@H](CN(CC=C)[C@@H]2C2)C(=O)N(CCCN(C)C)C(=O)NCC)=C3C2=CNC3=C1 KORNTPPJEAJQIU-KJXAQDMKSA-N 0.000 claims description 2
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 claims description 2
- 201000007114 MHC class I deficiency Diseases 0.000 claims description 2
- MNHDKMDLOJSCGN-UHFFFAOYSA-N N-[4-[4-(2-methoxyphenyl)-1-piperazinyl]butyl]-2-naphthalenecarboxamide Chemical compound COC1=CC=CC=C1N1CCN(CCCCNC(=O)C=2C=C3C=CC=CC3=CC=2)CC1 MNHDKMDLOJSCGN-UHFFFAOYSA-N 0.000 claims description 2
- QBUVZVXIRYFENV-UHFFFAOYSA-N N-allyl-1-phenyl-2,3,4,5-tetrahydro-3-benzazepine-7,8-diol Chemical compound C1=2C=C(O)C(O)=CC=2CCN(CC=C)CC1C1=CC=CC=C1 QBUVZVXIRYFENV-UHFFFAOYSA-N 0.000 claims description 2
- FHYWNBUFNGHNCP-UHFFFAOYSA-N N-methyl-6-chloro-1-(3-methylphenyl)-2,3,4,5-tetrahydro-3-benzazepine-7,8-diol hydrobromide Chemical compound Br.C1N(C)CCC(C(=C(O)C(O)=C2)Cl)=C2C1C1=CC=CC(C)=C1 FHYWNBUFNGHNCP-UHFFFAOYSA-N 0.000 claims description 2
- JOAHPSVPXZTVEP-YXJHDRRASA-N Terguride Chemical compound C1=CC([C@H]2C[C@@H](CN(C)[C@@H]2C2)NC(=O)N(CC)CC)=C3C2=CNC3=C1 JOAHPSVPXZTVEP-YXJHDRRASA-N 0.000 claims description 2
- HGMLOQOHAYKVJN-UHFFFAOYSA-N [4-[4-(1h-benzimidazol-2-ylmethyl)piperazin-1-yl]-2-chlorophenyl]methanol Chemical compound C1=C(Cl)C(CO)=CC=C1N1CCN(CC=2NC3=CC=CC=C3N=2)CC1 HGMLOQOHAYKVJN-UHFFFAOYSA-N 0.000 claims description 2
- KTEBZVJGMARTOQ-GCJKJVERSA-N adrogolide Chemical compound CC(=O)OC1=C(OC(C)=O)C=C2[C@H]3C(C=C(S4)CCC)=C4CN[C@@H]3CCC2=C1 KTEBZVJGMARTOQ-GCJKJVERSA-N 0.000 claims description 2
- 229950007871 adrogolide Drugs 0.000 claims description 2
- 229960004046 apomorphine Drugs 0.000 claims description 2
- CXWQXGNFZLHLHQ-DPFCLETOSA-N apomorphine hydrochloride Chemical compound [H+].[H+].O.[Cl-].[Cl-].C([C@H]1N(C)CC2)C3=CC=C(O)C(O)=C3C3=C1C2=CC=C3.C([C@H]1N(C)CC2)C3=CC=C(O)C(O)=C3C3=C1C2=CC=C3 CXWQXGNFZLHLHQ-DPFCLETOSA-N 0.000 claims description 2
- 229960004372 aripiprazole Drugs 0.000 claims description 2
- 229960002802 bromocriptine Drugs 0.000 claims description 2
- OZVBMTJYIDMWIL-AYFBDAFISA-N bromocriptine Chemical compound C1=CC(C=2[C@H](N(C)C[C@@H](C=2)C(=O)N[C@]2(C(=O)N3[C@H](C(N4CCC[C@H]4[C@]3(O)O2)=O)CC(C)C)C(C)C)C2)=C3C2=C(Br)NC3=C1 OZVBMTJYIDMWIL-AYFBDAFISA-N 0.000 claims description 2
- 229960001058 bupropion Drugs 0.000 claims description 2
- SNPPWIUOZRMYNY-UHFFFAOYSA-N bupropion Chemical compound CC(C)(C)NC(C)C(=O)C1=CC=CC(Cl)=C1 SNPPWIUOZRMYNY-UHFFFAOYSA-N 0.000 claims description 2
- 229960004596 cabergoline Drugs 0.000 claims description 2
- REHAKLRYABHSQJ-KDOFPFPSSA-N chembl28338 Chemical compound OC1=C(O)C=C2[C@H]3C(C=C(S4)CCC)=C4CN[C@@H]3CCC2=C1 REHAKLRYABHSQJ-KDOFPFPSSA-N 0.000 claims description 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 2
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- XFBDGHFDKJITGC-JLHYYAGUSA-N gbr-12783 Chemical compound C=1C=CC=CC=1C(C=1C=CC=CC=1)OCCN(CC1)CCN1C\C=C\C1=CC=CC=C1 XFBDGHFDKJITGC-JLHYYAGUSA-N 0.000 claims description 2
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- WFGNJLMSYIJWII-FJXQXJEOSA-N methyl (2s)-2-amino-3-(3,4-dihydroxyphenyl)propanoate;hydrochloride Chemical compound Cl.COC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WFGNJLMSYIJWII-FJXQXJEOSA-N 0.000 claims description 2
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- YYMXEVCLZQHDGV-UHFFFAOYSA-N n-[2-(3,4-dihydroxyphenyl)ethyl]-3-(6-oxo-3h-purin-9-yl)propanamide Chemical compound C1=C(O)C(O)=CC=C1CCNC(=O)CCN1C(NC=NC2=O)=C2N=C1 YYMXEVCLZQHDGV-UHFFFAOYSA-N 0.000 claims description 2
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- LCHVZQDOKNCPDQ-BSDSXHPESA-N methyl (1s,3s,4r,5r)-3-(4-tert-butylphenyl)-8-methyl-8-azabicyclo[3.2.1]octane-4-carboxylate Chemical compound C1([C@@H]2[C@H]([C@]3(CC[C@@](C2)(N3C)[H])[H])C(=O)OC)=CC=C(C(C)(C)C)C=C1 LCHVZQDOKNCPDQ-BSDSXHPESA-N 0.000 description 1
- YHWZJYKIOUHJGH-CAOSSQGBSA-N methyl (1s,3s,4r,5r)-3-benzyl-8-methyl-8-azabicyclo[3.2.1]octane-4-carboxylate Chemical compound C([C@@H]1[C@H]([C@]2(CC[C@@](C1)(N2C)[H])[H])C(=O)OC)C1=CC=CC=C1 YHWZJYKIOUHJGH-CAOSSQGBSA-N 0.000 description 1
- MMKZDDDDODERSJ-ZJIFWQFVSA-N methyl (1s,3s,4r,5r)-8-methyl-3-(4-methylphenyl)-8-azabicyclo[3.2.1]octane-4-carboxylate Chemical compound C1([C@@H]2[C@H]([C@]3(CC[C@@](C2)(N3C)[H])[H])C(=O)OC)=CC=C(C)C=C1 MMKZDDDDODERSJ-ZJIFWQFVSA-N 0.000 description 1
- HGNMYGRBKGXPFK-DOIPELPJSA-N methyl (1s,3s,4r,5r)-8-methyl-3-(4-phenylphenyl)-8-azabicyclo[3.2.1]octane-4-carboxylate Chemical compound C1=CC([C@@H]2[C@H]([C@]3(CC[C@@](C2)(N3C)[H])[H])C(=O)OC)=CC=C1C1=CC=CC=C1 HGNMYGRBKGXPFK-DOIPELPJSA-N 0.000 description 1
- RVCJYYIKKXDKHI-JEDBISTDSA-N methyl (1s,3s,4r,5r)-8-methyl-3-naphthalen-1-yl-8-azabicyclo[3.2.1]octane-4-carboxylate Chemical compound C1=CC=C2C([C@@H]3[C@H]([C@]4(CC[C@@](C3)(N4C)[H])[H])C(=O)OC)=CC=CC2=C1 RVCJYYIKKXDKHI-JEDBISTDSA-N 0.000 description 1
- ITFWLAOOLMWNLG-WJFTUGDTSA-N methyl (1s,3s,4r,5r)-8-methyl-3-naphthalen-2-yl-8-azabicyclo[3.2.1]octane-4-carboxylate Chemical compound C1=CC=CC2=CC([C@@H]3[C@H]([C@]4(CC[C@@](C3)(N4C)[H])[H])C(=O)OC)=CC=C21 ITFWLAOOLMWNLG-WJFTUGDTSA-N 0.000 description 1
- 238000012544 monitoring process Methods 0.000 description 1
- PQGYICACOSZSFB-FUTJPDQTSA-N n-[[(1s,3s,4r,5r)-3-(3,4-dichlorophenyl)-8-methyl-8-azabicyclo[3.2.1]octan-4-yl]methylidene]hydroxylamine Chemical compound C1([C@@H]2[C@@H](C=NO)[C@]3(CC[C@@](C2)(N3C)[H])[H])=CC=C(Cl)C(Cl)=C1 PQGYICACOSZSFB-FUTJPDQTSA-N 0.000 description 1
- 235000020824 obesity Nutrition 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 201000008482 osteoarthritis Diseases 0.000 description 1
- 230000001590 oxidative effect Effects 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 230000004962 physiological condition Effects 0.000 description 1
- 230000036470 plasma concentration Effects 0.000 description 1
- 239000011505 plaster Substances 0.000 description 1
- 229920002689 polyvinyl acetate Polymers 0.000 description 1
- 239000011118 polyvinyl acetate Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 229950001815 preclamol Drugs 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000007939 sustained release tablet Substances 0.000 description 1
- 230000002195 synergetic effect Effects 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- VCVWXKKWDOJNIT-ZOMKSWQUSA-N tesofensine Chemical compound C1([C@H]2C[C@@H]3CC[C@@H](N3C)[C@@H]2COCC)=CC=C(Cl)C(Cl)=C1 VCVWXKKWDOJNIT-ZOMKSWQUSA-N 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 238000004448 titration Methods 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 1
- 208000019553 vascular disease Diseases 0.000 description 1
- 238000009423 ventilation Methods 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 239000008215 water for injection Substances 0.000 description 1
- 230000003442 weekly effect Effects 0.000 description 1
Images
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
- C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
- C07H17/08—Hetero rings containing eight or more ring members, e.g. erythromycins
-
- 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
- A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/08—Bridged systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Genetics & Genomics (AREA)
- Emergency Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Molecular Biology (AREA)
- Child & Adolescent Psychology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04001282 | 2004-01-22 | ||
| EP04005816 | 2004-03-11 | ||
| PCT/EP2005/000165 WO2005070427A1 (en) | 2004-01-22 | 2005-01-11 | Compounds for the sustained reduction of body weight |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2007519646A true JP2007519646A (ja) | 2007-07-19 |
| JP2007519646A5 JP2007519646A5 (enExample) | 2008-02-14 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
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| JP2006549961A Pending JP2007519646A (ja) | 2004-01-22 | 2005-01-11 | 体重の持続的低減のための化合物 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20050203124A1 (enExample) |
| EP (1) | EP1727547A1 (enExample) |
| JP (1) | JP2007519646A (enExample) |
| AU (1) | AU2005205880B2 (enExample) |
| CA (1) | CA2553649A1 (enExample) |
| NZ (1) | NZ547919A (enExample) |
| WO (1) | WO2005070427A1 (enExample) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA06003762A (es) * | 2003-10-16 | 2006-06-14 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende un inhibidor de recaptacion de neurotransmisor monoamina y un inhibidor de acetilcolinesterasa. |
| AU2005205882A1 (en) * | 2004-01-22 | 2005-08-04 | Neurosearch A/S | Pharmaceutical composition comprising a monoamine neurotransmitter re-uptake inhibitor and an N-methyl-D-aspartate (NMDA) receptors antagonist |
| EP1779851A1 (en) * | 2005-10-31 | 2007-05-02 | Boehringer Ingelheim Pharma GmbH & Co.KG | Treatment of diabetes |
| EP2222303A1 (en) * | 2007-11-20 | 2010-09-01 | NeuroSearch A/S | A method for treating addiction |
| WO2009065845A1 (en) * | 2007-11-20 | 2009-05-28 | Neurosearch A/S | A method for treating over-eating disorders |
| WO2009080693A2 (en) * | 2007-12-20 | 2009-07-02 | Neurosearch A/S | Pharmaceutical composition comprising tesofensine or its analogue and a beta blocker |
| EP2237781A2 (en) * | 2007-12-20 | 2010-10-13 | NeuroSearch A/S | Pharmaceutical composition comprising tesofensine or its analogue and an anti-obesity |
| JP6203760B2 (ja) | 2012-02-16 | 2017-09-27 | サニオナ・エー／エス | 併用療法のための医薬組成物 |
| LT3265126T (lt) | 2015-03-03 | 2021-09-10 | Saniona A/S | Tesofensino ir metoprololio derinio kompozicija |
| WO2020084065A1 (en) * | 2018-10-24 | 2020-04-30 | Saniona A/S | Transdermal tropane compositions and methods for using the same |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH07501074A (ja) * | 1991-11-15 | 1995-02-02 | リサーチ・トライアングル・インスティテュート | コカイン受容体結合性リガント |
| JP2000504739A (ja) * | 1996-02-22 | 2000-04-18 | ニューロサーチ・アクティーゼルスカブ | トロパン―誘導体、その製造方法及びその使用方法 |
| WO2003028710A2 (de) * | 2001-09-28 | 2003-04-10 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verbindungen zur reduzierung übermässiger nahrungsaufnahme |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK154192D0 (da) * | 1992-12-23 | 1992-12-23 | Neurosearch As | Heterocycliske forbindelser |
| US5554626A (en) * | 1992-12-23 | 1996-09-10 | Neurosearch A/S | Substituted heterocyclic compounds as dopamine-reuptake inhibitors |
| ATE222587T1 (de) * | 1994-04-19 | 2002-09-15 | Neurosearch As | TROPAN-2-ALDOXIMDERIVATE ALS NEUROTRANSMITTER ßREUPTAKEß INHIBITOREN |
| US6262081B1 (en) * | 1998-07-10 | 2001-07-17 | Dupont Pharmaceuticals Company | Composition for and method of treating neurological disorders |
| WO2002102801A1 (en) * | 2001-05-23 | 2002-12-27 | Neurosearch A/S | Tropane derivatives and their use as monoamine neurotransmitter re-uptake inhibitors |
| EP1594874A1 (en) * | 2003-02-12 | 2005-11-16 | Neurosearch A/S | Novel 8-aza-bicyclo[3.2.1]octane derivatives and their use as monoamine neurotransmitter re-uptake inhibitors |
| MXPA06003762A (es) * | 2003-10-16 | 2006-06-14 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende un inhibidor de recaptacion de neurotransmisor monoamina y un inhibidor de acetilcolinesterasa. |
| AU2005205882A1 (en) * | 2004-01-22 | 2005-08-04 | Neurosearch A/S | Pharmaceutical composition comprising a monoamine neurotransmitter re-uptake inhibitor and an N-methyl-D-aspartate (NMDA) receptors antagonist |
| WO2005117874A1 (en) * | 2004-06-04 | 2005-12-15 | Neurosearch A/S | MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITOR FOR THE INHIBITION OF BETA-AMYLOID (Aß40 AND Aß42) -GENERATION |
-
2005
- 2005-01-11 EP EP05700803A patent/EP1727547A1/en not_active Withdrawn
- 2005-01-11 CA CA002553649A patent/CA2553649A1/en not_active Abandoned
- 2005-01-11 JP JP2006549961A patent/JP2007519646A/ja active Pending
- 2005-01-11 NZ NZ547919A patent/NZ547919A/en not_active IP Right Cessation
- 2005-01-11 AU AU2005205880A patent/AU2005205880B2/en not_active Ceased
- 2005-01-11 WO PCT/EP2005/000165 patent/WO2005070427A1/en not_active Ceased
- 2005-01-21 US US11/039,991 patent/US20050203124A1/en not_active Abandoned
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH07501074A (ja) * | 1991-11-15 | 1995-02-02 | リサーチ・トライアングル・インスティテュート | コカイン受容体結合性リガント |
| JP2000504739A (ja) * | 1996-02-22 | 2000-04-18 | ニューロサーチ・アクティーゼルスカブ | トロパン―誘導体、その製造方法及びその使用方法 |
| WO2003028710A2 (de) * | 2001-09-28 | 2003-04-10 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verbindungen zur reduzierung übermässiger nahrungsaufnahme |
Also Published As
| Publication number | Publication date |
|---|---|
| NZ547919A (en) | 2009-12-24 |
| EP1727547A1 (en) | 2006-12-06 |
| WO2005070427A8 (en) | 2005-11-17 |
| CA2553649A1 (en) | 2005-08-04 |
| US20050203124A1 (en) | 2005-09-15 |
| WO2005070427A1 (en) | 2005-08-04 |
| AU2005205880A1 (en) | 2005-08-04 |
| AU2005205880B2 (en) | 2010-06-10 |
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