CN103347523A - 向具有肾损伤的个体给药氯卡色林 - Google Patents
向具有肾损伤的个体给药氯卡色林 Download PDFInfo
- Publication number
- CN103347523A CN103347523A CN2011800528271A CN201180052827A CN103347523A CN 103347523 A CN103347523 A CN 103347523A CN 2011800528271 A CN2011800528271 A CN 2011800528271A CN 201180052827 A CN201180052827 A CN 201180052827A CN 103347523 A CN103347523 A CN 103347523A
- Authority
- CN
- China
- Prior art keywords
- individuality
- less
- chloro
- aza
- benzo
- 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
- 206010062237 Renal impairment Diseases 0.000 title claims abstract description 280
- XTTZERNUQAFMOF-QMMMGPOBSA-N lorcaserin Chemical compound C[C@H]1CNCCC2=CC=C(Cl)C=C12 XTTZERNUQAFMOF-QMMMGPOBSA-N 0.000 title abstract description 5
- 229960005060 lorcaserin Drugs 0.000 title description 2
- 238000000034 method Methods 0.000 claims abstract description 723
- 150000003839 salts Chemical class 0.000 claims abstract description 425
- 239000012453 solvate Substances 0.000 claims abstract description 425
- 238000011282 treatment Methods 0.000 claims abstract description 346
- DDRJAANPRJIHGJ-UHFFFAOYSA-N creatinine Chemical compound CN1CC(=O)NC1=N DDRJAANPRJIHGJ-UHFFFAOYSA-N 0.000 claims description 446
- 150000001875 compounds Chemical class 0.000 claims description 425
- 230000003907 kidney function Effects 0.000 claims description 357
- 210000003734 kidney Anatomy 0.000 claims description 314
- 230000037396 body weight Effects 0.000 claims description 249
- 229940109239 creatinine Drugs 0.000 claims description 216
- 208000027418 Wounds and injury Diseases 0.000 claims description 214
- 230000006378 damage Effects 0.000 claims description 214
- 208000014674 injury Diseases 0.000 claims description 214
- 239000003814 drug Substances 0.000 claims description 149
- 229940079593 drug Drugs 0.000 claims description 133
- 230000036186 satiety Effects 0.000 claims description 130
- 235000019627 satiety Nutrition 0.000 claims description 130
- 210000002966 serum Anatomy 0.000 claims description 122
- 230000037406 food intake Effects 0.000 claims description 120
- 235000012631 food intake Nutrition 0.000 claims description 120
- 238000004260 weight control Methods 0.000 claims description 102
- 208000037974 severe injury Diseases 0.000 claims description 96
- 230000009528 severe injury Effects 0.000 claims description 96
- 230000002411 adverse Effects 0.000 claims description 91
- 239000000203 mixture Substances 0.000 claims description 91
- 208000020832 chronic kidney disease Diseases 0.000 claims description 88
- 201000000523 end stage renal failure Diseases 0.000 claims description 88
- 238000009472 formulation Methods 0.000 claims description 68
- 208000008589 Obesity Diseases 0.000 claims description 60
- 235000020824 obesity Nutrition 0.000 claims description 60
- 235000005911 diet Nutrition 0.000 claims description 34
- 230000037213 diet Effects 0.000 claims description 34
- DHHVAGZRUROJKS-UHFFFAOYSA-N phentermine Chemical compound CC(C)(N)CC1=CC=CC=C1 DHHVAGZRUROJKS-UHFFFAOYSA-N 0.000 claims description 24
- 231100000419 toxicity Toxicity 0.000 claims description 23
- 230000001988 toxicity Effects 0.000 claims description 23
- 206010020772 Hypertension Diseases 0.000 claims description 21
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 17
- 201000002859 sleep apnea Diseases 0.000 claims description 17
- 208000032928 Dyslipidaemia Diseases 0.000 claims description 15
- 208000002705 Glucose Intolerance Diseases 0.000 claims description 15
- 206010018429 Glucose tolerance impaired Diseases 0.000 claims description 15
- 208000017170 Lipid metabolism disease Diseases 0.000 claims description 15
- 239000002904 solvent Substances 0.000 claims description 15
- 229960003562 phentermine Drugs 0.000 claims description 12
- 230000037221 weight management Effects 0.000 abstract 2
- 201000010099 disease Diseases 0.000 description 82
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 82
- 208000017169 kidney disease Diseases 0.000 description 82
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 66
- 208000028208 end stage renal disease Diseases 0.000 description 66
- 230000036541 health Effects 0.000 description 59
- 239000000243 solution Substances 0.000 description 59
- 230000009467 reduction Effects 0.000 description 49
- 229940125904 compound 1 Drugs 0.000 description 48
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 45
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical group C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 description 44
- 239000000460 chlorine Substances 0.000 description 42
- 230000002265 prevention Effects 0.000 description 42
- 239000007787 solid Substances 0.000 description 42
- 238000003756 stirring Methods 0.000 description 42
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 description 40
- 229910052801 chlorine Inorganic materials 0.000 description 40
- 238000013213 extrapolation Methods 0.000 description 40
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 39
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 33
- 238000001914 filtration Methods 0.000 description 27
- JMMWKPVZQRWMSS-UHFFFAOYSA-N isopropanol acetate Natural products CC(C)OC(C)=O JMMWKPVZQRWMSS-UHFFFAOYSA-N 0.000 description 26
- 229940011051 isopropyl acetate Drugs 0.000 description 26
- GWYFCOCPABKNJV-UHFFFAOYSA-N isovaleric acid Chemical compound CC(C)CC(O)=O GWYFCOCPABKNJV-UHFFFAOYSA-N 0.000 description 26
- 208000024891 symptom Diseases 0.000 description 26
- 210000000577 adipose tissue Anatomy 0.000 description 21
- 206010033307 Overweight Diseases 0.000 description 20
- 239000000725 suspension Substances 0.000 description 18
- 238000001816 cooling Methods 0.000 description 17
- 230000003203 everyday effect Effects 0.000 description 17
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 15
- 239000002775 capsule Substances 0.000 description 15
- 210000002700 urine Anatomy 0.000 description 15
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 14
- PXQPEWDEAKTCGB-UHFFFAOYSA-N orotic acid Chemical compound OC(=O)C1=CC(=O)NC(=O)N1 PXQPEWDEAKTCGB-UHFFFAOYSA-N 0.000 description 13
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 13
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 12
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 11
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 11
- 238000011160 research Methods 0.000 description 11
- ZWEHNKRNPOVVGH-UHFFFAOYSA-N 2-Butanone Chemical compound CCC(C)=O ZWEHNKRNPOVVGH-UHFFFAOYSA-N 0.000 description 10
- 238000010521 absorption reaction Methods 0.000 description 10
- 206010012601 diabetes mellitus Diseases 0.000 description 10
- 239000003517 fume Substances 0.000 description 10
- 229950005216 napadisilate Drugs 0.000 description 10
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 description 9
- 239000003513 alkali Substances 0.000 description 9
- 210000004369 blood Anatomy 0.000 description 9
- 239000008280 blood Substances 0.000 description 9
- 239000002552 dosage form Substances 0.000 description 9
- 230000024924 glomerular filtration Effects 0.000 description 9
- 238000012423 maintenance Methods 0.000 description 9
- 239000002207 metabolite Substances 0.000 description 9
- 239000008194 pharmaceutical composition Substances 0.000 description 9
- 230000036470 plasma concentration Effects 0.000 description 9
- 238000002360 preparation method Methods 0.000 description 9
- 238000012360 testing method Methods 0.000 description 9
- 238000002560 therapeutic procedure Methods 0.000 description 9
- OFOBLEOULBTSOW-UHFFFAOYSA-L Malonate Chemical compound [O-]C(=O)CC([O-])=O OFOBLEOULBTSOW-UHFFFAOYSA-L 0.000 description 8
- 238000002288 cocrystallisation Methods 0.000 description 8
- 230000000875 corresponding effect Effects 0.000 description 8
- 230000018109 developmental process Effects 0.000 description 8
- NTHXOOBQLCIOLC-UHFFFAOYSA-N iohexol Chemical compound OCC(O)CN(C(=O)C)C1=C(I)C(C(=O)NCC(O)CO)=C(I)C(C(=O)NCC(O)CO)=C1I NTHXOOBQLCIOLC-UHFFFAOYSA-N 0.000 description 8
- 150000003891 oxalate salts Chemical class 0.000 description 8
- 230000035807 sensation Effects 0.000 description 8
- 235000019615 sensations Nutrition 0.000 description 8
- KPGXRSRHYNQIFN-UHFFFAOYSA-L 2-oxoglutarate(2-) Chemical compound [O-]C(=O)CCC(=O)C([O-])=O KPGXRSRHYNQIFN-UHFFFAOYSA-L 0.000 description 7
- 229920001202 Inulin Polymers 0.000 description 7
- 239000013078 crystal Substances 0.000 description 7
- 238000009826 distribution Methods 0.000 description 7
- 238000005516 engineering process Methods 0.000 description 7
- 229940029339 inulin Drugs 0.000 description 7
- JYJIGFIDKWBXDU-MNNPPOADSA-N inulin Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)OC[C@]1(OC[C@]2(OC[C@]3(OC[C@]4(OC[C@]5(OC[C@]6(OC[C@]7(OC[C@]8(OC[C@]9(OC[C@]%10(OC[C@]%11(OC[C@]%12(OC[C@]%13(OC[C@]%14(OC[C@]%15(OC[C@]%16(OC[C@]%17(OC[C@]%18(OC[C@]%19(OC[C@]%20(OC[C@]%21(OC[C@]%22(OC[C@]%23(OC[C@]%24(OC[C@]%25(OC[C@]%26(OC[C@]%27(OC[C@]%28(OC[C@]%29(OC[C@]%30(OC[C@]%31(OC[C@]%32(OC[C@]%33(OC[C@]%34(OC[C@]%35(OC[C@]%36(O[C@@H]%37[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O%37)O)[C@H]([C@H](O)[C@@H](CO)O%36)O)[C@H]([C@H](O)[C@@H](CO)O%35)O)[C@H]([C@H](O)[C@@H](CO)O%34)O)[C@H]([C@H](O)[C@@H](CO)O%33)O)[C@H]([C@H](O)[C@@H](CO)O%32)O)[C@H]([C@H](O)[C@@H](CO)O%31)O)[C@H]([C@H](O)[C@@H](CO)O%30)O)[C@H]([C@H](O)[C@@H](CO)O%29)O)[C@H]([C@H](O)[C@@H](CO)O%28)O)[C@H]([C@H](O)[C@@H](CO)O%27)O)[C@H]([C@H](O)[C@@H](CO)O%26)O)[C@H]([C@H](O)[C@@H](CO)O%25)O)[C@H]([C@H](O)[C@@H](CO)O%24)O)[C@H]([C@H](O)[C@@H](CO)O%23)O)[C@H]([C@H](O)[C@@H](CO)O%22)O)[C@H]([C@H](O)[C@@H](CO)O%21)O)[C@H]([C@H](O)[C@@H](CO)O%20)O)[C@H]([C@H](O)[C@@H](CO)O%19)O)[C@H]([C@H](O)[C@@H](CO)O%18)O)[C@H]([C@H](O)[C@@H](CO)O%17)O)[C@H]([C@H](O)[C@@H](CO)O%16)O)[C@H]([C@H](O)[C@@H](CO)O%15)O)[C@H]([C@H](O)[C@@H](CO)O%14)O)[C@H]([C@H](O)[C@@H](CO)O%13)O)[C@H]([C@H](O)[C@@H](CO)O%12)O)[C@H]([C@H](O)[C@@H](CO)O%11)O)[C@H]([C@H](O)[C@@H](CO)O%10)O)[C@H]([C@H](O)[C@@H](CO)O9)O)[C@H]([C@H](O)[C@@H](CO)O8)O)[C@H]([C@H](O)[C@@H](CO)O7)O)[C@H]([C@H](O)[C@@H](CO)O6)O)[C@H]([C@H](O)[C@@H](CO)O5)O)[C@H]([C@H](O)[C@@H](CO)O4)O)[C@H]([C@H](O)[C@@H](CO)O3)O)[C@H]([C@H](O)[C@@H](CO)O2)O)[C@@H](O)[C@H](O)[C@@H](CO)O1 JYJIGFIDKWBXDU-MNNPPOADSA-N 0.000 description 7
- 239000000463 material Substances 0.000 description 7
- 239000000047 product Substances 0.000 description 7
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 6
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 6
- 210000001015 abdomen Anatomy 0.000 description 6
- 239000002253 acid Substances 0.000 description 6
- 238000010171 animal model Methods 0.000 description 6
- 238000011156 evaluation Methods 0.000 description 6
- 235000013305 food Nutrition 0.000 description 6
- 229960001025 iohexol Drugs 0.000 description 6
- 229940116298 l- malic acid Drugs 0.000 description 6
- 239000007788 liquid Substances 0.000 description 6
- XTEGVFVZDVNBPF-UHFFFAOYSA-N naphthalene-1,5-disulfonic acid Chemical compound C1=CC=C2C(S(=O)(=O)O)=CC=CC2=C1S(O)(=O)=O XTEGVFVZDVNBPF-UHFFFAOYSA-N 0.000 description 6
- 210000002381 plasma Anatomy 0.000 description 6
- 210000002784 stomach Anatomy 0.000 description 6
- YXUZGLGRBBHYFZ-UHFFFAOYSA-N 2,4-dioxo-1h-pyrimidine-6-carboxylic acid;hydrate Chemical compound O.OC(=O)C1=CC(=O)NC(=O)N1 YXUZGLGRBBHYFZ-UHFFFAOYSA-N 0.000 description 5
- QCXJEYYXVJIFCE-UHFFFAOYSA-N 4-acetamidobenzoic acid Chemical class CC(=O)NC1=CC=C(C(O)=O)C=C1 QCXJEYYXVJIFCE-UHFFFAOYSA-N 0.000 description 5
- ODHCTXKNWHHXJC-VKHMYHEASA-N 5-oxo-L-proline Chemical compound OC(=O)[C@@H]1CCC(=O)N1 ODHCTXKNWHHXJC-VKHMYHEASA-N 0.000 description 5
- 241000282693 Cercopithecidae Species 0.000 description 5
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 description 5
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 description 5
- 229930195714 L-glutamate Natural products 0.000 description 5
- 239000002269 analeptic agent Substances 0.000 description 5
- 239000007864 aqueous solution Substances 0.000 description 5
- 230000008859 change Effects 0.000 description 5
- 238000004807 desolvation Methods 0.000 description 5
- 239000003937 drug carrier Substances 0.000 description 5
- 230000000694 effects Effects 0.000 description 5
- 238000002347 injection Methods 0.000 description 5
- 239000007924 injection Substances 0.000 description 5
- 238000005259 measurement Methods 0.000 description 5
- 230000007170 pathology Effects 0.000 description 5
- 230000001225 therapeutic effect Effects 0.000 description 5
- 238000002411 thermogravimetry Methods 0.000 description 5
- WBYWAXJHAXSJNI-VOTSOKGWSA-N trans-cinnamic acid Chemical class OC(=O)\C=C\C1=CC=CC=C1 WBYWAXJHAXSJNI-VOTSOKGWSA-N 0.000 description 5
- LSPHULWDVZXLIL-UHFFFAOYSA-N (+/-)-Camphoric acid Chemical class CC1(C)C(C(O)=O)CCC1(C)C(O)=O LSPHULWDVZXLIL-UHFFFAOYSA-N 0.000 description 4
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical class OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 description 4
- KPGXRSRHYNQIFN-UHFFFAOYSA-N 2-oxoglutaric acid Chemical compound OC(=O)CCC(=O)C(O)=O KPGXRSRHYNQIFN-UHFFFAOYSA-N 0.000 description 4
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 4
- 102100028007 Cystatin-SA Human genes 0.000 description 4
- 101710144510 Cysteine proteinase inhibitor Proteins 0.000 description 4
- AEMOLEFTQBMNLQ-AQKNRBDQSA-N D-glucopyranuronic acid Chemical class OC1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O AEMOLEFTQBMNLQ-AQKNRBDQSA-N 0.000 description 4
- 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 4
- 206010019233 Headaches Diseases 0.000 description 4
- OFOBLEOULBTSOW-UHFFFAOYSA-N Malonic acid Chemical compound OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 4
- 229910002651 NO3 Inorganic materials 0.000 description 4
- NHNBFGGVMKEFGY-UHFFFAOYSA-N Nitrate Chemical compound [O-][N+]([O-])=O NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 description 4
- 229910019142 PO4 Inorganic materials 0.000 description 4
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 4
- WNLRTRBMVRJNCN-UHFFFAOYSA-L adipate(2-) Chemical compound [O-]C(=O)CCCCC([O-])=O WNLRTRBMVRJNCN-UHFFFAOYSA-L 0.000 description 4
- 238000013019 agitation Methods 0.000 description 4
- 229950005953 camsilate Drugs 0.000 description 4
- 239000003795 chemical substances by application Substances 0.000 description 4
- 230000001276 controlling effect Effects 0.000 description 4
- 208000029078 coronary artery disease Diseases 0.000 description 4
- 238000002425 crystallisation Methods 0.000 description 4
- 230000008025 crystallization Effects 0.000 description 4
- 239000002852 cysteine proteinase inhibitor Substances 0.000 description 4
- 238000011161 development Methods 0.000 description 4
- VFNGKCDDZUSWLR-UHFFFAOYSA-L disulfate(2-) Chemical compound [O-]S(=O)(=O)OS([O-])(=O)=O VFNGKCDDZUSWLR-UHFFFAOYSA-L 0.000 description 4
- AFAXGSQYZLGZPG-UHFFFAOYSA-N ethanedisulfonic acid Chemical compound OS(=O)(=O)CCS(O)(=O)=O AFAXGSQYZLGZPG-UHFFFAOYSA-N 0.000 description 4
- 238000001704 evaporation Methods 0.000 description 4
- 230000002496 gastric effect Effects 0.000 description 4
- 231100000869 headache Toxicity 0.000 description 4
- 235000003642 hunger Nutrition 0.000 description 4
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 4
- 239000003550 marker Substances 0.000 description 4
- 230000004060 metabolic process Effects 0.000 description 4
- 210000003205 muscle Anatomy 0.000 description 4
- 231100000062 no-observed-adverse-effect level Toxicity 0.000 description 4
- AHLBNYSZXLDEJQ-FWEHEUNISA-N orlistat Chemical compound CCCCCCCCCCC[C@H](OC(=O)[C@H](CC(C)C)NC=O)C[C@@H]1OC(=O)[C@H]1CCCCCC AHLBNYSZXLDEJQ-FWEHEUNISA-N 0.000 description 4
- 229960005010 orotic acid Drugs 0.000 description 4
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 4
- 239000010452 phosphate Substances 0.000 description 4
- 239000000902 placebo Substances 0.000 description 4
- 229940068196 placebo Drugs 0.000 description 4
- 239000000843 powder Substances 0.000 description 4
- 235000018102 proteins Nutrition 0.000 description 4
- 102000004169 proteins and genes Human genes 0.000 description 4
- 108090000623 proteins and genes Proteins 0.000 description 4
- 229940043131 pyroglutamate Drugs 0.000 description 4
- 230000002285 radioactive effect Effects 0.000 description 4
- 102000005962 receptors Human genes 0.000 description 4
- 108020003175 receptors Proteins 0.000 description 4
- UNAANXDKBXWMLN-UHFFFAOYSA-N sibutramine Chemical compound C=1C=C(Cl)C=CC=1C1(C(N(C)C)CC(C)C)CCC1 UNAANXDKBXWMLN-UHFFFAOYSA-N 0.000 description 4
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 4
- 239000003826 tablet Substances 0.000 description 4
- 230000000007 visual effect Effects 0.000 description 4
- -1 β2Wei Qiudanbai Proteins 0.000 description 4
- DBGIVFWFUFKIQN-VIFPVBQESA-N (+)-Fenfluramine Chemical compound CCN[C@@H](C)CC1=CC=CC(C(F)(F)F)=C1 DBGIVFWFUFKIQN-VIFPVBQESA-N 0.000 description 3
- FRASJONUBLZVQX-UHFFFAOYSA-N 1,4-naphthoquinone Chemical compound C1=CC=C2C(=O)C=CC(=O)C2=C1 FRASJONUBLZVQX-UHFFFAOYSA-N 0.000 description 3
- YJZDPFHZDKVOTR-UHFFFAOYSA-N 2-[2-[bis(carboxymethyl)amino]ethyl-(carboxymethyl)amino]acetic acid;chromium Chemical compound [Cr].OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O YJZDPFHZDKVOTR-UHFFFAOYSA-N 0.000 description 3
- UVKNREAAHQRBKA-IEOVAKBOSA-I 2-[bis[2-[bis(carboxylatomethyl)amino]ethyl]amino]acetate;technetium-99(4+) Chemical compound [99Tc+4].[O-]C(=O)CN(CC([O-])=O)CCN(CC(=O)[O-])CCN(CC([O-])=O)CC([O-])=O UVKNREAAHQRBKA-IEOVAKBOSA-I 0.000 description 3
- CNDXWMWBOHJYJJ-UHFFFAOYSA-N 2-hydroxy-2-phenylacetic acid;hydrate Chemical compound O.OC(=O)C(O)C1=CC=CC=C1 CNDXWMWBOHJYJJ-UHFFFAOYSA-N 0.000 description 3
- 229920002261 Corn starch Polymers 0.000 description 3
- 206010019280 Heart failures Diseases 0.000 description 3
- 241001465754 Metazoa Species 0.000 description 3
- QPCDCPDFJACHGM-UHFFFAOYSA-N N,N-bis{2-[bis(carboxymethyl)amino]ethyl}glycine Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(=O)O)CCN(CC(O)=O)CC(O)=O QPCDCPDFJACHGM-UHFFFAOYSA-N 0.000 description 3
- 208000028389 Nerve injury Diseases 0.000 description 3
- 208000006011 Stroke Diseases 0.000 description 3
- 206010000059 abdominal discomfort Diseases 0.000 description 3
- 239000000556 agonist Substances 0.000 description 3
- 238000004458 analytical method Methods 0.000 description 3
- 230000015572 biosynthetic process Effects 0.000 description 3
- 239000004202 carbamide Substances 0.000 description 3
- 235000013877 carbamide Nutrition 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
- 239000002872 contrast media Substances 0.000 description 3
- 239000008120 corn starch Substances 0.000 description 3
- 229960004597 dexfenfluramine Drugs 0.000 description 3
- 238000001035 drying Methods 0.000 description 3
- 230000002526 effect on cardiovascular system Effects 0.000 description 3
- 239000000839 emulsion Substances 0.000 description 3
- 206010015037 epilepsy Diseases 0.000 description 3
- 239000001530 fumaric acid Substances 0.000 description 3
- 230000006870 function Effects 0.000 description 3
- 239000008103 glucose Substances 0.000 description 3
- 230000003993 interaction Effects 0.000 description 3
- 238000009588 inulin clearance Methods 0.000 description 3
- 229940029378 iothalamate Drugs 0.000 description 3
- IWYDHOAUDWTVEP-UHFFFAOYSA-N mandelic acid Chemical compound OC(=O)C(O)C1=CC=CC=C1 IWYDHOAUDWTVEP-UHFFFAOYSA-N 0.000 description 3
- 230000004048 modification Effects 0.000 description 3
- 238000012986 modification Methods 0.000 description 3
- 230000008764 nerve damage Effects 0.000 description 3
- 230000000474 nursing effect Effects 0.000 description 3
- 235000006408 oxalic acid Nutrition 0.000 description 3
- 229960003330 pentetic acid Drugs 0.000 description 3
- 239000000825 pharmaceutical preparation Substances 0.000 description 3
- 238000000634 powder X-ray diffraction Methods 0.000 description 3
- 239000002244 precipitate Substances 0.000 description 3
- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 description 3
- 239000000376 reactant Substances 0.000 description 3
- 230000002829 reductive effect Effects 0.000 description 3
- 229960004425 sibutramine Drugs 0.000 description 3
- 230000002269 spontaneous effect Effects 0.000 description 3
- 210000001519 tissue Anatomy 0.000 description 3
- 206010000087 Abdominal pain upper Diseases 0.000 description 2
- 208000030090 Acute Disease Diseases 0.000 description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- 206010008190 Cerebrovascular accident Diseases 0.000 description 2
- 208000017667 Chronic Disease Diseases 0.000 description 2
- 206010010144 Completed suicide Diseases 0.000 description 2
- 206010052895 Coronary artery insufficiency Diseases 0.000 description 2
- 206010012735 Diarrhoea Diseases 0.000 description 2
- IAJILQKETJEXLJ-UHFFFAOYSA-N Galacturonsaeure Natural products O=CC(O)C(O)C(O)C(O)C(O)=O IAJILQKETJEXLJ-UHFFFAOYSA-N 0.000 description 2
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 description 2
- 206010028980 Neoplasm Diseases 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- LCHYVQSEPWUPAD-UHFFFAOYSA-N S(N)(O)(=O)=O.[Cl] Chemical compound S(N)(O)(=O)=O.[Cl] LCHYVQSEPWUPAD-UHFFFAOYSA-N 0.000 description 2
- 102000007562 Serum Albumin Human genes 0.000 description 2
- 108010071390 Serum Albumin Proteins 0.000 description 2
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 2
- 208000037063 Thinness Diseases 0.000 description 2
- 206010044565 Tremor Diseases 0.000 description 2
- 206010047513 Vision blurred Diseases 0.000 description 2
- 206010047700 Vomiting Diseases 0.000 description 2
- 208000005946 Xerostomia Diseases 0.000 description 2
- CBWUNQZJGJFJLZ-UHFFFAOYSA-N [Cl].Cl Chemical compound [Cl].Cl CBWUNQZJGJFJLZ-UHFFFAOYSA-N 0.000 description 2
- 239000000654 additive Substances 0.000 description 2
- WNLRTRBMVRJNCN-UHFFFAOYSA-N adipic acid Chemical compound OC(=O)CCCCC(O)=O WNLRTRBMVRJNCN-UHFFFAOYSA-N 0.000 description 2
- AEMOLEFTQBMNLQ-WAXACMCWSA-N alpha-D-glucuronic acid Chemical compound O[C@H]1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O AEMOLEFTQBMNLQ-WAXACMCWSA-N 0.000 description 2
- 206010003549 asthenia Diseases 0.000 description 2
- 125000004429 atom Chemical group 0.000 description 2
- 230000006399 behavior Effects 0.000 description 2
- 239000011230 binding agent Substances 0.000 description 2
- 230000036772 blood pressure Effects 0.000 description 2
- 238000004364 calculation method Methods 0.000 description 2
- 201000011510 cancer Diseases 0.000 description 2
- 230000015556 catabolic process Effects 0.000 description 2
- 239000001913 cellulose Substances 0.000 description 2
- 229920002678 cellulose Polymers 0.000 description 2
- 238000011284 combination treatment Methods 0.000 description 2
- 238000012937 correction Methods 0.000 description 2
- CVSVTCORWBXHQV-UHFFFAOYSA-N creatine Chemical compound NC(=[NH2+])N(C)CC([O-])=O CVSVTCORWBXHQV-UHFFFAOYSA-N 0.000 description 2
- 230000034994 death Effects 0.000 description 2
- 230000018044 dehydration Effects 0.000 description 2
- 238000006297 dehydration reaction Methods 0.000 description 2
- 230000008034 disappearance Effects 0.000 description 2
- 208000002173 dizziness Diseases 0.000 description 2
- 238000002651 drug therapy Methods 0.000 description 2
- 206010013781 dry mouth Diseases 0.000 description 2
- 201000006549 dyspepsia Diseases 0.000 description 2
- 230000008020 evaporation Effects 0.000 description 2
- 210000002468 fat body Anatomy 0.000 description 2
- 206010016256 fatigue Diseases 0.000 description 2
- 239000012065 filter cake Substances 0.000 description 2
- 208000020694 gallbladder disease Diseases 0.000 description 2
- 239000000499 gel Substances 0.000 description 2
- 229930182480 glucuronide Natural products 0.000 description 2
- 229960002989 glutamic acid Drugs 0.000 description 2
- 239000004519 grease Substances 0.000 description 2
- 238000000227 grinding Methods 0.000 description 2
- 150000004677 hydrates Chemical class 0.000 description 2
- 230000006872 improvement Effects 0.000 description 2
- 238000001990 intravenous administration Methods 0.000 description 2
- 239000010410 layer Substances 0.000 description 2
- 150000002632 lipids Chemical class 0.000 description 2
- 239000000314 lubricant Substances 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- 239000002547 new drug Substances 0.000 description 2
- 239000003921 oil Substances 0.000 description 2
- 230000008520 organization Effects 0.000 description 2
- 229960001243 orlistat Drugs 0.000 description 2
- 239000006201 parenteral dosage form Substances 0.000 description 2
- 208000035824 paresthesia Diseases 0.000 description 2
- 230000002093 peripheral effect Effects 0.000 description 2
- RLLPVAHGXHCWKJ-UHFFFAOYSA-N permethrin Chemical compound CC1(C)C(C=C(Cl)Cl)C1C(=O)OCC1=CC=CC(OC=2C=CC=CC=2)=C1 RLLPVAHGXHCWKJ-UHFFFAOYSA-N 0.000 description 2
- 229920001592 potato starch Polymers 0.000 description 2
- 208000020016 psychiatric disease Diseases 0.000 description 2
- 238000007789 sealing Methods 0.000 description 2
- 238000004088 simulation Methods 0.000 description 2
- 230000003238 somatosensory effect Effects 0.000 description 2
- 238000007920 subcutaneous administration Methods 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- KDYFGRWQOYBRFD-UHFFFAOYSA-N succinic acid Chemical compound OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 description 2
- 239000001117 sulphuric acid Substances 0.000 description 2
- 235000011149 sulphuric acid Nutrition 0.000 description 2
- 238000003786 synthesis reaction Methods 0.000 description 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 2
- 206010048828 underweight Diseases 0.000 description 2
- 238000002562 urinalysis Methods 0.000 description 2
- 239000003981 vehicle Substances 0.000 description 2
- 230000008673 vomiting Effects 0.000 description 2
- 229940002552 xenical Drugs 0.000 description 2
- DBGIVFWFUFKIQN-UHFFFAOYSA-N (+-)-Fenfluramine Chemical compound CCNC(C)CC1=CC=CC(C(F)(F)F)=C1 DBGIVFWFUFKIQN-UHFFFAOYSA-N 0.000 description 1
- MIOPJNTWMNEORI-GMSGAONNSA-N (S)-camphorsulfonic acid Chemical compound C1C[C@@]2(CS(O)(=O)=O)C(=O)C[C@@H]1C2(C)C MIOPJNTWMNEORI-GMSGAONNSA-N 0.000 description 1
- WBYWAXJHAXSJNI-VOTSOKGWSA-M .beta-Phenylacrylic acid Natural products [O-]C(=O)\C=C\C1=CC=CC=C1 WBYWAXJHAXSJNI-VOTSOKGWSA-M 0.000 description 1
- 102000003966 Alpha-1-microglobulin Human genes 0.000 description 1
- 101800001761 Alpha-1-microglobulin Proteins 0.000 description 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
- 206010003210 Arteriosclerosis Diseases 0.000 description 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
- 206010007559 Cardiac failure congestive Diseases 0.000 description 1
- 208000002177 Cataract Diseases 0.000 description 1
- 102100032559 Clathrin light chain B Human genes 0.000 description 1
- 208000028698 Cognitive impairment Diseases 0.000 description 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 1
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 description 1
- 208000002249 Diabetes Complications Diseases 0.000 description 1
- 206010012655 Diabetic complications Diseases 0.000 description 1
- 206010016803 Fluid overload Diseases 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- 208000010412 Glaucoma Diseases 0.000 description 1
- 201000005569 Gout Diseases 0.000 description 1
- 208000031886 HIV Infections Diseases 0.000 description 1
- 208000037357 HIV infectious disease Diseases 0.000 description 1
- 101000942271 Homo sapiens Clathrin light chain B Proteins 0.000 description 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 1
- 238000003109 Karl Fischer titration Methods 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
- 235000000391 Lepidium draba Nutrition 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- 206010027336 Menstruation delayed Diseases 0.000 description 1
- 206010029155 Nephropathy toxic Diseases 0.000 description 1
- 241001597008 Nomeidae Species 0.000 description 1
- 206010029897 Obsessive thoughts Diseases 0.000 description 1
- 208000002193 Pain Diseases 0.000 description 1
- 102000019280 Pancreatic lipases Human genes 0.000 description 1
- 108050006759 Pancreatic lipases Proteins 0.000 description 1
- 239000004820 Pressure-sensitive adhesive Substances 0.000 description 1
- ODHCTXKNWHHXJC-GSVOUGTGSA-N Pyroglutamic acid Natural products OC(=O)[C@H]1CCC(=O)N1 ODHCTXKNWHHXJC-GSVOUGTGSA-N 0.000 description 1
- 208000001647 Renal Insufficiency Diseases 0.000 description 1
- 206010063530 Single functional kidney Diseases 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 208000000223 Solitary Kidney Diseases 0.000 description 1
- YZCKVEUIGOORGS-NJFSPNSNSA-N Tritium Chemical compound [3H] YZCKVEUIGOORGS-NJFSPNSNSA-N 0.000 description 1
- LEHOTFFKMJEONL-UHFFFAOYSA-N Uric Acid Chemical compound N1C(=O)NC(=O)C2=C1NC(=O)N2 LEHOTFFKMJEONL-UHFFFAOYSA-N 0.000 description 1
- PNNCWTXUWKENPE-UHFFFAOYSA-N [N].NC(N)=O Chemical compound [N].NC(N)=O PNNCWTXUWKENPE-UHFFFAOYSA-N 0.000 description 1
- 235000010489 acacia gum Nutrition 0.000 description 1
- 239000001785 acacia senegal l. willd gum Substances 0.000 description 1
- 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 1
- ODHCTXKNWHHXJC-UHFFFAOYSA-N acide pyroglutamique Natural products OC(=O)C1CCC(=O)N1 ODHCTXKNWHHXJC-UHFFFAOYSA-N 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 230000000996 additive effect Effects 0.000 description 1
- 239000001361 adipic acid Substances 0.000 description 1
- 235000011037 adipic acid Nutrition 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 239000003708 ampul Substances 0.000 description 1
- 239000000883 anti-obesity agent Substances 0.000 description 1
- 230000002421 anti-septic effect Effects 0.000 description 1
- 229940125710 antiobesity agent Drugs 0.000 description 1
- 238000013459 approach Methods 0.000 description 1
- 235000003704 aspartic acid Nutrition 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 1
- 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 1
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 description 1
- 210000001124 body fluid Anatomy 0.000 description 1
- 239000010839 body fluid Substances 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 229910052799 carbon Inorganic materials 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 230000003130 cardiopathic effect Effects 0.000 description 1
- 208000026106 cerebrovascular disease Diseases 0.000 description 1
- 238000002512 chemotherapy Methods 0.000 description 1
- 210000002987 choroid plexus Anatomy 0.000 description 1
- 238000005352 clarification Methods 0.000 description 1
- 208000010877 cognitive disease Diseases 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 238000002591 computed tomography Methods 0.000 description 1
- 229960003624 creatine Drugs 0.000 description 1
- 239000006046 creatine Substances 0.000 description 1
- 239000002178 crystalline material Substances 0.000 description 1
- 125000004122 cyclic group Chemical group 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 238000006731 degradation reaction Methods 0.000 description 1
- 230000001934 delay Effects 0.000 description 1
- 229910052805 deuterium Inorganic materials 0.000 description 1
- 239000008121 dextrose Substances 0.000 description 1
- 238000000502 dialysis Methods 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- VCSZKSHWUBFOOE-UHFFFAOYSA-N dioxidanium;sulfate Chemical compound O.O.OS(O)(=O)=O VCSZKSHWUBFOOE-UHFFFAOYSA-N 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 239000000890 drug combination Substances 0.000 description 1
- 238000012377 drug delivery Methods 0.000 description 1
- 230000004064 dysfunction Effects 0.000 description 1
- 239000008157 edible vegetable oil Substances 0.000 description 1
- 239000003792 electrolyte Substances 0.000 description 1
- 239000003995 emulsifying agent Substances 0.000 description 1
- 230000007515 enzymatic degradation Effects 0.000 description 1
- 230000029142 excretion Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 208000030533 eye disease Diseases 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 238000011049 filling Methods 0.000 description 1
- 239000000706 filtrate Substances 0.000 description 1
- 239000012634 fragment Substances 0.000 description 1
- ZZUFCTLCJUWOSV-UHFFFAOYSA-N furosemide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC(C(O)=O)=C1NCC1=CC=CO1 ZZUFCTLCJUWOSV-UHFFFAOYSA-N 0.000 description 1
- 229960003883 furosemide Drugs 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 238000001631 haemodialysis Methods 0.000 description 1
- 210000003709 heart valve Anatomy 0.000 description 1
- 230000000322 hemodialysis Effects 0.000 description 1
- 230000010224 hepatic metabolism Effects 0.000 description 1
- 238000002017 high-resolution X-ray diffraction Methods 0.000 description 1
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 description 1
- 229910052739 hydrogen Inorganic materials 0.000 description 1
- 239000001257 hydrogen Substances 0.000 description 1
- 210000003016 hypothalamus Anatomy 0.000 description 1
- 230000001771 impaired effect Effects 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 238000002329 infrared spectrum Methods 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 229940102223 injectable solution Drugs 0.000 description 1
- 239000008353 injections by composition Substances 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 238000010253 intravenous injection Methods 0.000 description 1
- 238000004750 isotope dilution mass spectroscopy Methods 0.000 description 1
- 150000002576 ketones Chemical class 0.000 description 1
- 201000006370 kidney failure Diseases 0.000 description 1
- 238000011813 knockout mouse model Methods 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 208000019423 liver disease Diseases 0.000 description 1
- 230000033001 locomotion Effects 0.000 description 1
- 210000003141 lower extremity Anatomy 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 238000002595 magnetic resonance imaging Methods 0.000 description 1
- 150000002689 maleic acids Chemical class 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 238000001819 mass spectrum Methods 0.000 description 1
- 230000002503 metabolic effect Effects 0.000 description 1
- 229940098779 methanesulfonic acid Drugs 0.000 description 1
- 238000012544 monitoring process Methods 0.000 description 1
- 230000007694 nephrotoxicity Effects 0.000 description 1
- 231100000417 nephrotoxicity Toxicity 0.000 description 1
- 210000000653 nervous system Anatomy 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 239000002687 nonaqueous vehicle Substances 0.000 description 1
- 239000002767 noradrenalin uptake inhibitor Substances 0.000 description 1
- 229940126569 noradrenaline reuptake inhibitor Drugs 0.000 description 1
- 239000006186 oral dosage form Substances 0.000 description 1
- 229940116369 pancreatic lipase Drugs 0.000 description 1
- 230000037361 pathway Effects 0.000 description 1
- 230000008447 perception Effects 0.000 description 1
- 235000020030 perry Nutrition 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 238000001050 pharmacotherapy Methods 0.000 description 1
- 235000011007 phosphoric acid Nutrition 0.000 description 1
- 230000035790 physiological processes and functions Effects 0.000 description 1
- 230000003449 preventive effect Effects 0.000 description 1
- 238000009117 preventive therapy Methods 0.000 description 1
- 230000037452 priming Effects 0.000 description 1
- 239000011241 protective layer Substances 0.000 description 1
- 230000005180 public health Effects 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 238000001953 recrystallisation Methods 0.000 description 1
- 235000018770 reduced food intake Nutrition 0.000 description 1
- 230000008521 reorganization Effects 0.000 description 1
- 208000017443 reproductive system disease Diseases 0.000 description 1
- 210000001525 retina Anatomy 0.000 description 1
- 102000029752 retinol binding Human genes 0.000 description 1
- 108091000053 retinol binding Proteins 0.000 description 1
- 210000002027 skeletal muscle Anatomy 0.000 description 1
- 238000010583 slow cooling Methods 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000012265 solid product Substances 0.000 description 1
- 239000006104 solid solution Substances 0.000 description 1
- 238000000935 solvent evaporation Methods 0.000 description 1
- GOLXNESZZPUPJE-UHFFFAOYSA-N spiromesifen Chemical compound CC1=CC(C)=CC(C)=C1C(C(O1)=O)=C(OC(=O)CC(C)(C)C)C11CCCC1 GOLXNESZZPUPJE-UHFFFAOYSA-N 0.000 description 1
- 230000001954 sterilising effect Effects 0.000 description 1
- 238000004659 sterilization and disinfection Methods 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 239000001384 succinic acid Substances 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 230000005062 synaptic transmission 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
- 235000012222 talc Nutrition 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 210000001103 thalamus Anatomy 0.000 description 1
- 238000004448 titration Methods 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 231100000027 toxicology Toxicity 0.000 description 1
- 229910052722 tritium Inorganic materials 0.000 description 1
- 230000001228 trophic effect Effects 0.000 description 1
- 230000010248 tubular secretion Effects 0.000 description 1
- 210000005239 tubule Anatomy 0.000 description 1
- 238000002604 ultrasonography Methods 0.000 description 1
- 238000000870 ultraviolet spectroscopy Methods 0.000 description 1
- 230000002485 urinary effect Effects 0.000 description 1
- 238000003828 vacuum filtration Methods 0.000 description 1
- 210000001215 vagina Anatomy 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
Images
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
- A61K31/55—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
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
-
- 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
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/70—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving creatine or creatinine
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10T—TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION
- Y10T436/00—Chemistry: analytical and immunological testing
- Y10T436/14—Heterocyclic carbon compound [i.e., O, S, N, Se, Te, as only ring hetero atom]
- Y10T436/145555—Hetero-N
- Y10T436/147777—Plural nitrogen in the same ring [e.g., barbituates, creatinine, etc.]
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Immunology (AREA)
- Biomedical Technology (AREA)
- Molecular Biology (AREA)
- Physiology (AREA)
- Nutrition Science (AREA)
- Microbiology (AREA)
- General Physics & Mathematics (AREA)
- Biotechnology (AREA)
- Food Science & Technology (AREA)
- Physics & Mathematics (AREA)
- Analytical Chemistry (AREA)
- Biochemistry (AREA)
- Cell Biology (AREA)
- Pathology (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US40262810P | 2010-09-01 | 2010-09-01 | |
| US61/402,628 | 2010-09-01 | ||
| US40314910P | 2010-09-10 | 2010-09-10 | |
| US61/403,149 | 2010-09-10 | ||
| PCT/US2011/049936 WO2012030939A1 (en) | 2010-09-01 | 2011-08-31 | Administration of lorcaserin to individuals with renal impairment |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103347523A true CN103347523A (zh) | 2013-10-09 |
Family
ID=44653552
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2011800528271A Pending CN103347523A (zh) | 2010-09-01 | 2011-08-31 | 向具有肾损伤的个体给药氯卡色林 |
Country Status (14)
| Country | Link |
|---|---|
| US (3) | US8999970B2 (enExample) |
| EP (2) | EP2611449A1 (enExample) |
| JP (4) | JP2013540719A (enExample) |
| KR (2) | KR20180094131A (enExample) |
| CN (1) | CN103347523A (enExample) |
| AU (3) | AU2011296015B2 (enExample) |
| BR (1) | BR112013004707A2 (enExample) |
| CA (1) | CA2808890A1 (enExample) |
| EA (1) | EA201390335A1 (enExample) |
| HK (1) | HK1210419A1 (enExample) |
| MX (1) | MX2013002418A (enExample) |
| NZ (2) | NZ630494A (enExample) |
| SG (2) | SG188365A1 (enExample) |
| WO (1) | WO2012030939A1 (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8822727B2 (en) * | 2008-03-04 | 2014-09-02 | Arena Pharmaceuticals, Inc. | Processes for the preparation of intermediates related to the 5-HT2C agonist (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine |
| KR20130112848A (ko) | 2010-06-02 | 2013-10-14 | 아레나 파마슈티칼스, 인크. | 5-ｈｔ2ｃ 수용체 아고니스트의 제조 방법 |
| US8999970B2 (en) * | 2010-09-01 | 2015-04-07 | Arena Pharmaceuticals, Inc. | Administration of an anti-obesity compound to individuals with renal impairment |
| KR20130138770A (ko) | 2010-09-01 | 2013-12-19 | 아레나 파마슈티칼스, 인크. | 광학적으로 활성 산을 갖는 로르카세린의 염 |
| SG188361A1 (en) * | 2010-09-01 | 2013-04-30 | Arena Pharm Inc | Non-hygroscopic salts of 5-ht2c agonists |
| US20130267500A1 (en) * | 2010-09-01 | 2013-10-10 | Arena Pharmaceuticals, Inc. | 5-ht2c receptor agonists in the treatment of disorders ameliorated by reduction of norepinephrine level |
| EP3485878A1 (en) * | 2010-09-01 | 2019-05-22 | Arena Pharmaceuticals, Inc. | Modified-release dosage forms of 5-ht2c agonists useful for weight management |
| CA2886875A1 (en) | 2012-10-09 | 2014-04-17 | Arena Pharmaceuticals, Inc. | Method of weight management |
| WO2016069875A1 (en) | 2014-10-30 | 2016-05-06 | Arena Pharmaceuticals, Inc. | Compositions and methods for ceasing tobacco smoking |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101123955A (zh) * | 2004-12-23 | 2008-02-13 | 艾尼纳制药公司 | 5HT2c受体调节剂组合物和使用方法 |
| CN101547892A (zh) * | 2006-12-05 | 2009-09-30 | 艾尼纳制药公司 | 制备(r)-8-氯-1-甲基-2，3，4，5-四氢-1h-3-苯并氮杂卓的方法和其中间体 |
Family Cites Families (131)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2900415A (en) | 1954-12-14 | 1959-08-18 | Lakeside Lab Inc | Synthesized antispasmodic compounds |
| CH481110A (de) | 1967-02-17 | 1969-11-15 | Geigy Ag J R | Verfahren zur Herstellung von 1,2,4,5-Tetrahydro-3-azepinen |
| CH498122A (de) | 1968-02-09 | 1970-10-31 | Geigy Ag J R | Verfahren zur Herstellung eines neuen Tetrahydroazepinderivates |
| CH500194A (de) | 1968-02-15 | 1970-12-15 | Ciba Geigy Ag | Verfahren zur Herstellung von Tetrahydroazepinderivaten |
| US4233217A (en) | 1968-03-11 | 1980-11-11 | Pennwalt Corporation | Substituted 1,2,4,5-tetrahydro-3H, 3 benzazepines |
| GB1268243A (en) | 1968-03-11 | 1972-03-22 | Wallace & Tiernan Inc | 0,2,4,5,-tetrahydro-3h,3-benzazepines |
| FR314F (enExample) | 1968-03-22 | 1970-05-25 | ||
| FR7736M (enExample) | 1968-09-02 | 1970-03-09 | ||
| US3716639A (en) | 1970-03-11 | 1973-02-13 | Ciba Geigy Corp | Anorexigenic tetrahydrobenzazepines |
| US3795683A (en) | 1970-08-19 | 1974-03-05 | Hoffmann La Roche | 2,3,4,5-tetrahydro-1h-3-benzazepines |
| LU65954A1 (enExample) | 1972-08-25 | 1974-03-07 | ||
| US4210749A (en) | 1974-11-12 | 1980-07-01 | Pennwalt Corporation | Substituted 1,2,4,5-tetrahydro-3H,3 benzazepines |
| SE7510988L (sv) | 1975-10-01 | 1977-04-02 | Draco Ab | Nya farmaceutiskt aktiva foreningar |
| DE2627479C2 (de) | 1976-06-18 | 1983-09-22 | Bergwerksverband Gmbh, 4300 Essen | Verwendung eines Formkokses als Adsorptionsmittel für Schwefeloxide aus Abgasen |
| US4111957A (en) | 1977-02-02 | 1978-09-05 | Smithkline Corporation | Substituted 1-thienyl and furyl-2,3,4,5-tetrahydro-1H-3-benzazepine compounds |
| US4108989A (en) | 1977-04-01 | 1978-08-22 | Smithkline Corporation | 2,3,4,5-tetrahydro-1h-3-benzazepine-7,8-diones |
| DE2758001A1 (de) | 1977-12-24 | 1979-07-12 | Hoechst Ag | Cephalosporinderivate und verfahren zu ihrer herstellung |
| CA1090797A (en) | 1978-06-20 | 1980-12-02 | Kenneth G. Holden | Substituted 1-thienyl and furyl-2,3,4,5-tetrahydro-1h- 3-benzazepine compounds |
| AU515236B2 (en) | 1978-06-26 | 1981-03-26 | Smithkline Corporation | Substituted-1-thienyl and furyl-2,3,4,5-tetrahydro-14-3 benzazepine derivatives |
| ZA792785B (en) | 1978-07-07 | 1980-08-27 | Smithkline Corp | Mercapto substituted-2,3,4,5-tetrahydro-1h-3-benzazepines |
| IE50355B1 (en) | 1979-10-20 | 1986-04-02 | Wyeth John & Brother Ltd | Morpholine derivatives |
| US4477378A (en) | 1980-02-05 | 1984-10-16 | Schering Corp. | Esters of substituted 8-hydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines |
| ZA827887B (en) | 1981-11-27 | 1983-11-30 | Smithkline Beckman Corp | Pharmaceutical compositions and method of producing alpha2 antagonism |
| EP0080779B1 (en) | 1981-11-27 | 1986-07-16 | Smithkline Beckman Corporation | 3-benzazepines as alpha-2 antagonists |
| FR2518544A1 (fr) | 1981-12-22 | 1983-06-24 | Lipha | Benzodiazepines-1,3 thione-2, procede de preparation et medicament les contenant |
| FR2525603A1 (fr) | 1982-04-27 | 1983-10-28 | Adir | Benzoazacycloalkyl-spiro-imidazolinines, leur preparation et leur application en therapeutique |
| US4988690A (en) | 1982-06-14 | 1991-01-29 | Hoechst-Roussel Pharmaceuticals Inc. | 1-aryloxy-2,3,4,5-tetrahydro-3-benzazepines and anti-depressant use thereof |
| DE3418270A1 (de) | 1984-05-17 | 1985-11-21 | Dr. Karl Thomae Gmbh, 7950 Biberach | Neue aminotetralinderivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung |
| US4541954A (en) | 1984-09-05 | 1985-09-17 | Smithkline Beckman Corporation | Method for preparing 6-chloro-N-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine |
| EP0204349A3 (de) | 1985-06-01 | 1990-01-03 | Dr. Karl Thomae GmbH | Neue heteroaromatische Aminderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung |
| GB8610668D0 (en) | 1986-05-01 | 1986-06-04 | Pfizer Ltd | Anti-arrhythmia agents |
| EG18188A (en) | 1986-05-01 | 1992-09-30 | Pfizer Ltd | Process for preparation anti-arhythmia agents |
| US4762845A (en) | 1986-05-21 | 1988-08-09 | Abbott Laboratories | 7-(3-Substituted imino-1-pyrrolidinyl)-quinolone-3-carboxylic acids |
| EP0285287A3 (en) | 1987-03-23 | 1990-08-16 | Smithkline Beecham Corporation | 3-benzazepine compounds for use in treating gastrointestinal motility disorders |
| US5015639A (en) | 1987-03-27 | 1991-05-14 | Schering Corporation | Substituted benzazepines, their preparation and pharmaceutical compositions containing them |
| US5247080A (en) | 1987-03-27 | 1993-09-21 | Schering Corporation | Substituted benzazepines useful as intermediates for producing pharmaceutically active compounds |
| ZA882080B (en) | 1987-03-27 | 1989-04-26 | Schering Corp | Substituted benzazepines,their preparation and pharmaceutical compositions containing them |
| AU1700688A (en) | 1987-04-09 | 1988-11-04 | Smithkline Beckman Corporation | Sulfinyl and sulfonyl substituted 3-benzazepines |
| US4957914A (en) | 1987-05-15 | 1990-09-18 | Syntex (U.S.A.) Inc. | 1,9-alkano-bridged-2,3,4,5-tetrahydro-1H-3-benzazepines |
| DK107688D0 (da) | 1988-03-01 | 1988-03-01 | Novo Industri As | Carbaminsyreestere af substituerede 7-hydroxy-2,3,4,5-tetrahydro-1h-3-benzazepiner |
| US5422355A (en) | 1989-06-02 | 1995-06-06 | John Wyeth & Brother, Limited | Composition for treating depression with (N-heteroaryl)alkylamines |
| US5178786A (en) | 1989-08-04 | 1993-01-12 | The Lubrizol Corporation | Corrosion-inhibiting compositions and functional fluids containing same |
| MTP1076B (en) | 1990-01-12 | 1991-09-30 | Ciba Geigy Ag | Hemihydrate |
| EP0513174B1 (en) | 1990-02-02 | 1995-08-16 | Schering Corporation | 4,5-cycloalkano-3-benzazepin-7-ol-derivatives and their use |
| CA2037162A1 (en) | 1990-03-12 | 1991-09-13 | Steven Howard Shaber | Heterocyclicacetonitriles and fungicidal use |
| ZA914536B (en) | 1990-06-15 | 1992-03-25 | Schering Corp | 8-lower alkyl-5-cycloalkyl or 5-cycloakenyl substituted benzazepines and pharmaceutical compositions containing them |
| US5275915A (en) | 1991-06-05 | 1994-01-04 | Dainippon Ink And Chemicals, Inc. | Developer for light-sensitive material |
| CA2110575A1 (en) | 1991-06-21 | 1993-01-07 | John Gerard Ward | Use of tetrahydrobenzazepine derivatives for the treatment of portal hypertension and migraine |
| GB9116824D0 (en) | 1991-08-05 | 1991-09-18 | Smithkline Beecham Corp | Chemical compounds |
| EP0558824A1 (en) | 1992-02-04 | 1993-09-08 | Duphar International Research B.V | Method for the preparation of vicinal aminoalcohols and optically active O-protected derivatives thereof |
| US5241065A (en) | 1992-02-25 | 1993-08-31 | Schering Corporation | 2,3,4,5-tetrahydro-1h-3-benzazepines having anti-psychotic activity |
| JPH05339263A (ja) | 1992-06-08 | 1993-12-21 | Wakunaga Pharmaceut Co Ltd | ジヒドロピリジン誘導体 |
| JP2987258B2 (ja) | 1992-07-13 | 1999-12-06 | 沖電気工業株式会社 | 非同期転送モード通信網におけるトラヒック監視方式 |
| JPH06298746A (ja) | 1993-04-19 | 1994-10-25 | Showa Denko Kk | 環状イミド酸エステルの製造法 |
| US6087346A (en) | 1993-06-23 | 2000-07-11 | Cambridge Neuroscience, Inc. | Sigma receptor ligands and the use thereof |
| US5387685A (en) | 1993-07-16 | 1995-02-07 | American Cyanamid Co | MDR reversal agents |
| GB9322976D0 (en) | 1993-11-08 | 1994-01-05 | Pfizer Ltd | Therapeutic agents |
| DE4419247A1 (de) | 1994-06-01 | 1995-12-07 | Merckle Gmbh | Sulfonylierte Pyrrolizincarbonsäureamide und deren Anwendung in der Pharmazie |
| DE4419246A1 (de) | 1994-06-01 | 1995-12-07 | Merckle Gmbh | Heteroarylsubstituierte Pyrrolizinverbindungen und deren Anwendung in der Pharmazie |
| DE4419315A1 (de) | 1994-06-01 | 1995-12-07 | Merckle Gmbh | Heteropyrrolizinverbindungen und deren Anwendung in der Pharmazie |
| DE4427838A1 (de) | 1994-08-05 | 1996-02-08 | Thomae Gmbh Dr K | Kondensierte Azepinderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung |
| DE4429079A1 (de) | 1994-08-17 | 1996-02-22 | Thomae Gmbh Dr K | Cyclische Harnstoffderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung |
| JPH08134048A (ja) | 1994-11-08 | 1996-05-28 | Sumitomo Chem Co Ltd | オキサゾリン類の製造法 |
| DE19510566A1 (de) | 1995-03-23 | 1996-09-26 | Kali Chemie Pharma Gmbh | Benzazepin-, Benzoxazepin- und Benzothiazepin-N-essigsäurederivate sowie Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel |
| GB9508622D0 (en) | 1995-04-28 | 1995-06-14 | Pfizer Ltd | Therapeutic agants |
| US5958543A (en) | 1995-07-07 | 1999-09-28 | Stor Media,Inc. | Micro-texturing for sputtered, thin film magnetic media disks utilizing titanium sputtered in the presence of hydrogen to form micro-texturing |
| JPH0930960A (ja) | 1995-07-18 | 1997-02-04 | Takasago Internatl Corp | 真菌感染症治療剤 |
| CA2190708A1 (en) | 1995-12-08 | 1997-06-09 | Johannes Aebi | Aminoalkyl substituted benzo-heterocyclic compounds |
| US5892116A (en) | 1996-01-03 | 1999-04-06 | Georgetown University | Gelators |
| US5925651A (en) | 1996-04-03 | 1999-07-20 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| US5691362A (en) | 1996-06-05 | 1997-11-25 | Schering-Plough Corporation | Substituted benzene-fused hetero- and carbocyclics as nuerokinin antagonists |
| EP0920417A4 (en) | 1996-08-15 | 1999-12-29 | Smithkline Beecham Corp | IL-8 RECEPTOR ANTAGONISTS |
| US5908830A (en) | 1996-10-31 | 1999-06-01 | Merck & Co., Inc. | Combination therapy for the treatment of diabetes and obesity |
| EP0973778A1 (en) | 1997-03-07 | 2000-01-26 | Novo Nordisk A/S | 4,5,6,7-TETRAHYDRO-THIENO 3,2-c]PYRIDINE DERIVATIVES, THEIR PREPARATION AND USE |
| AUPP020297A0 (en) | 1997-11-05 | 1997-11-27 | University Of Melbourne, The | A novel receptor, and compounds which bind thereto |
| JP4345230B2 (ja) | 1998-03-10 | 2009-10-14 | 小野薬品工業株式会社 | カルボン酸誘導体およびその誘導体を有効成分として含有する薬剤 |
| JP3603177B2 (ja) | 1998-03-26 | 2004-12-22 | 参天製薬株式会社 | 新規ウレア誘導体 |
| EP1072591A4 (en) | 1998-03-26 | 2005-01-05 | Santen Pharmaceutical Co Ltd | NEW UREA CONNECTIONS |
| EP0987235B1 (en) | 1998-08-25 | 2003-03-12 | MERCK PATENT GmbH | Method for the conversion of arenes or alkenes with iodoalkenes, aryl iodides or arenediazonium salts |
| US20080103179A1 (en) | 2006-10-27 | 2008-05-01 | Tam Peter Y | Combination Therapy |
| US20080255093A1 (en) | 1999-06-14 | 2008-10-16 | Tam Peter Y | Compositions and methods for treating obesity and related disorders |
| DE60006618T2 (de) | 1999-08-06 | 2004-09-23 | F. Hoffmann-La Roche Ag | Tetrahydro-benzo(d)azepine und deren Verwendung als metabotrope Glutamatrezeptor-Antagonisten |
| EP1074549B1 (en) | 1999-08-06 | 2003-11-19 | F. Hoffmann-La Roche Ag | Tetrahydro-benzo(d)azepines and their use as antagonists at metabotropic glutamate receptors |
| JP2001076413A (ja) | 1999-09-06 | 2001-03-23 | Sony Corp | フレキシブル磁気ディスク用ヘッドスライダー |
| US6403657B1 (en) | 1999-10-04 | 2002-06-11 | Martin C. Hinz | Comprehensive pharmacologic therapy for treatment of obesity |
| DE10003708A1 (de) | 2000-01-28 | 2001-08-02 | Solvent Innovation Gmbh | Neuartige chirale ionische Flüssigkeiten und Verfahren zu ihrer Darstellung in enantiomerenreiner oder enantiomerenangereicherter Form |
| BR0111947A (pt) | 2000-06-30 | 2003-05-06 | Glaxo Group Ltd | Composto, composição farmacêutica, método para o tratamento de um distúrbio em um mamìfero, uso de um composto e processo para preparar, um composto |
| CN1254474C (zh) | 2000-11-14 | 2006-05-03 | 史密斯克莱·比奇曼公司 | 作为多巴胺D<sub>3</sub>受体调节剂(精神抑制药)的四氢苯并氮杂䓬衍生物 |
| DE10057751A1 (de) | 2000-11-22 | 2002-05-23 | Bayer Ag | Neue Carbamat-substituierte Pyrazolopyridinderivate |
| GB0030710D0 (en) | 2000-12-15 | 2001-01-31 | Hoffmann La Roche | Piperazine derivatives |
| WO2002074746A1 (en) | 2001-03-16 | 2002-09-26 | Yamanouchi Pharmaceutical Co., Ltd. | Benzazepine derivatives |
| US6825198B2 (en) | 2001-06-21 | 2004-11-30 | Pfizer Inc | 5-HT receptor ligands and uses thereof |
| US7550261B2 (en) | 2001-08-21 | 2009-06-23 | Smithkline Beecham Corporation | Method of screening for drug hypersensitivity reaction |
| BR0212787A (pt) | 2001-09-24 | 2005-01-25 | Elan Pharm Inc | Composto ou sal farmaceuticamente aceitável do mesmo, métodos de tratamento ou prevenção de doenças e de preparação de um composto, uso de um composto ou sal, e, composição farmacêutica |
| JP2005518414A (ja) | 2001-12-21 | 2005-06-23 | スミスクライン ビーチャム パブリック リミテッド カンパニー | ドーパミン受容体のモジュレーターとしての７−スルホニル−３−ベンゾアゼピン誘導体およびｃｎｓ障害の治療のためのその使用 |
| WO2003057161A2 (en) | 2001-12-28 | 2003-07-17 | Bayer Pharmaceuticals Corporation | BENZOTHIENO [3,2-c]PYRAZOLYL AND BENZOFURANO [3,2-c] PYRAZOLYL COMPOUNDS, THEIR USE IN DISEASES ASSOCIATED WITH THE 5-HT2C RECEPTOR AND INTERMEDIATE COMPOUNDS THEREOF |
| JP2005519915A (ja) | 2002-01-18 | 2005-07-07 | セレテック・リミテッド・ライアビリティ・カンパニー | Ｅｄｇ受容体に関連する症状の処置方法 |
| ATE486842T1 (de) | 2002-03-12 | 2010-11-15 | Merck Sharp & Dohme | Substituierte amide |
| US6953787B2 (en) | 2002-04-12 | 2005-10-11 | Arena Pharmaceuticals, Inc. | 5HT2C receptor modulators |
| CA2482195A1 (en) | 2002-04-12 | 2003-10-23 | The University Of Chicago | Farnesoid x-activated receptor agonists |
| US7105505B2 (en) | 2002-04-18 | 2006-09-12 | Schering Corporation | Benzimidazole derivatives useful as histamine H3 antagonists |
| DE10220570A1 (de) | 2002-05-08 | 2003-11-20 | Bayer Ag | Carbamat-substituierte Pyrazolopyridine |
| GB0224557D0 (en) | 2002-10-22 | 2002-11-27 | Glaxo Group Ltd | Novel compounds |
| DE10261131A1 (de) | 2002-12-20 | 2004-07-01 | Grünenthal GmbH | Substituierte 5-Aminomethyl-1H-pyrrol-2-carbonsäureamide |
| US7145012B2 (en) | 2003-04-23 | 2006-12-05 | Pfizer Inc. | Cannabinoid receptor ligands and uses thereof |
| US7232823B2 (en) | 2003-06-09 | 2007-06-19 | Pfizer, Inc. | Cannabinoid receptor ligands and uses thereof |
| US7704993B2 (en) | 2003-06-17 | 2010-04-27 | Arena Pharmaceuticals, Inc. | Benzazepine derivatives and methods of prophylaxis or treatment of 5ht2c receptor associated diseases |
| MXPA05013364A (es) | 2003-06-17 | 2006-03-17 | Arena Pharm Inc | Procedimiento para preparar 3-benzazepinas. |
| AU2004265243A1 (en) | 2003-06-20 | 2005-02-24 | Arena Pharmaceuticals, Inc. | N-phenyl-piperazine derivatives and methods of prophylaxis or treatment of 5HT2c receptor associated diseases |
| TW200510324A (en) | 2003-08-11 | 2005-03-16 | Lilly Co Eli | 6-(2,2,2-trifluoroethylamino)-7-chiloro-2, 3, 4, 5-tetrahydro-1h-benzo[d]azepine as a 5-ht2c receptor agonist |
| US20080009478A1 (en) | 2003-10-22 | 2008-01-10 | Arena Pharmaceuticals, Inc. | Benzazepine Derivatives and Methods of Prophylaxis or Treatment of 5Ht2c Receptor Associated Diseases |
| US20070275949A1 (en) | 2003-10-22 | 2007-11-29 | Arena Pharmaceuticals, Inc. | Benzazepine Derivatives and Methods of Prophylaxis or Treatment of 5Ht2C Receptor Associated Diseases |
| EA011011B1 (ru) | 2004-02-25 | 2008-12-30 | Эли Лилли Энд Компани | 6-ЗАМЕЩЁННЫЕ 2,3,4,5-ТЕТРАГИДРО-1H-БЕНЗО[d]АЗЕПИНЫ В КАЧЕСТВЕ АГОНИСТОВ РЕЦЕПТОРОВ 5-HT |
| US7157445B2 (en) | 2004-02-26 | 2007-01-02 | Aventis Pharma S.A. | Administration of enoxaparin sodium to patients with severe renal impairment |
| SE0401871D0 (sv) | 2004-07-15 | 2004-07-15 | Glucogene Medical Hfm Ab | New compositions |
| MX2007001337A (es) | 2004-08-02 | 2008-03-13 | Genmedica Therapeutics Sl | Compuestos para inhibir amina-oxidasas que contienen cobre y usos de los mismos. |
| US8178077B2 (en) | 2004-10-19 | 2012-05-15 | Reverse Proteomics Research Institute Co., Ltd. | Drug development target protein and target gene, and method of screening |
| BRPI0519726B8 (pt) | 2004-12-21 | 2021-05-25 | Arena Pharm Inc | composto de hemidrato de (r)-8-cloro-1-metil-2,3,4,5-tetraidro-1h-3-benzazepina, composição compreendendo o referido composto e seus usos |
| JP5199997B2 (ja) | 2006-04-03 | 2013-05-15 | アリーナ ファーマシューティカルズ， インコーポレイテッド | ８−クロロ−１−メチル−２，３，４，５−テトラヒドロ−１ｈ−３−ベンズアゼピンおよびこれに関連する中間体を調製するためのプロセス |
| JP5513378B2 (ja) | 2007-06-15 | 2014-06-04 | ユニバーシティ オブ フロリダ リサーチ ファウンデーション，インコーポレイテッド | 治療化合物 |
| EP2237781A2 (en) | 2007-12-20 | 2010-10-13 | NeuroSearch A/S | Pharmaceutical composition comprising tesofensine or its analogue and an anti-obesity |
| WO2009097416A1 (en) | 2008-01-29 | 2009-08-06 | Vanda Pharmaceuticals, Inc. | Imidazolylalkyl- pyridines as dbh inhibitors |
| US8822727B2 (en) | 2008-03-04 | 2014-09-02 | Arena Pharmaceuticals, Inc. | Processes for the preparation of intermediates related to the 5-HT2C agonist (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine |
| US7608616B1 (en) | 2008-06-03 | 2009-10-27 | Questcor Pharmaceuticals, Inc. | Methods for reducing the risk of an adverse drug interaction in a patient suffering from insomnia |
| WO2010148207A2 (en) | 2009-06-18 | 2010-12-23 | Arena Pharmaceuticals, Inc. | Processes for the preparation of 5-ht2c receptor agonists |
| EP2611781A1 (en) | 2010-09-01 | 2013-07-10 | Arena Pharmaceuticals, Inc. | Fast-dissolve dosage forms of 5-ht2c agonists |
| US20130267500A1 (en) | 2010-09-01 | 2013-10-10 | Arena Pharmaceuticals, Inc. | 5-ht2c receptor agonists in the treatment of disorders ameliorated by reduction of norepinephrine level |
| EP3485878A1 (en) | 2010-09-01 | 2019-05-22 | Arena Pharmaceuticals, Inc. | Modified-release dosage forms of 5-ht2c agonists useful for weight management |
| KR20130138770A (ko) | 2010-09-01 | 2013-12-19 | 아레나 파마슈티칼스, 인크. | 광학적으로 활성 산을 갖는 로르카세린의 염 |
| US8999970B2 (en) | 2010-09-01 | 2015-04-07 | Arena Pharmaceuticals, Inc. | Administration of an anti-obesity compound to individuals with renal impairment |
| CN102126988A (zh) | 2010-12-17 | 2011-07-20 | 张家港瀚康化工有限公司 | 4-(4-氯苯基)-2-溴甲基-2-苯基丁腈的制备方法 |
-
2011
- 2011-08-31 US US13/511,639 patent/US8999970B2/en active Active
- 2011-08-31 NZ NZ630494A patent/NZ630494A/en not_active IP Right Cessation
- 2011-08-31 SG SG2013015631A patent/SG188365A1/en unknown
- 2011-08-31 AU AU2011296015A patent/AU2011296015B2/en not_active Ceased
- 2011-08-31 CA CA2808890A patent/CA2808890A1/en not_active Abandoned
- 2011-08-31 KR KR1020187023062A patent/KR20180094131A/ko not_active Ceased
- 2011-08-31 WO PCT/US2011/049936 patent/WO2012030939A1/en not_active Ceased
- 2011-08-31 KR KR1020137008393A patent/KR20140091458A/ko not_active Ceased
- 2011-08-31 MX MX2013002418A patent/MX2013002418A/es unknown
- 2011-08-31 NZ NZ608266A patent/NZ608266A/en not_active IP Right Cessation
- 2011-08-31 EP EP11758012.6A patent/EP2611449A1/en not_active Ceased
- 2011-08-31 EP EP15169002.1A patent/EP2939677A1/en not_active Withdrawn
- 2011-08-31 BR BR112013004707A patent/BR112013004707A2/pt not_active Application Discontinuation
- 2011-08-31 JP JP2013527258A patent/JP2013540719A/ja active Pending
- 2011-08-31 CN CN2011800528271A patent/CN103347523A/zh active Pending
- 2011-08-31 EA EA201390335A patent/EA201390335A1/ru unknown
- 2011-08-31 SG SG10201506896RA patent/SG10201506896RA/en unknown
-
2015
- 2015-03-27 US US14/671,151 patent/US20150196567A1/en not_active Abandoned
- 2015-11-12 HK HK15111171.1A patent/HK1210419A1/en unknown
-
2016
- 2016-02-10 AU AU2016200860A patent/AU2016200860B2/en not_active Ceased
- 2016-03-15 JP JP2016050724A patent/JP2016106148A/ja active Pending
-
2017
- 2017-01-05 US US15/398,997 patent/US9770455B2/en not_active Expired - Fee Related
- 2017-05-10 JP JP2017093900A patent/JP2017132811A/ja not_active Withdrawn
-
2018
- 2018-01-05 AU AU2018200108A patent/AU2018200108A1/en not_active Abandoned
- 2018-12-03 JP JP2018226624A patent/JP2019031577A/ja active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101123955A (zh) * | 2004-12-23 | 2008-02-13 | 艾尼纳制药公司 | 5HT2c受体调节剂组合物和使用方法 |
| CN101547892A (zh) * | 2006-12-05 | 2009-09-30 | 艾尼纳制药公司 | 制备(r)-8-氯-1-甲基-2，3，4，5-四氢-1h-3-苯并氮杂卓的方法和其中间体 |
Non-Patent Citations (4)
| Title |
|---|
| ARENA PHARMACEUTICALS: "Pharmacokinetic Properties of Lorcaserin in Subjects With Renal Impairment", 《CLINICALTRIALS.GOV》, 22 July 2009 (2009-07-22) * |
| BO BAI ET AL.: "The use of lorcaserin in the management of obesity:a critical appraisal", 《DRUG DESIGN,DEVELOPMENT AND THERAPY》, 20 December 2010 (2010-12-20), pages 1 - 7 * |
| Y.WANG ET.AL: "Lorcaserin Hydrochloride", 《DRUGS OF THE FUTURE》, vol. 32, no. 9, 31 December 2007 (2007-12-31), pages 766 - 770, XP 055010380, DOI: doi:10.1358/dof.2007.032.09.1135518 * |
| Y.WANG ET.AL: "Lorcaserin Hydrochloride", 《DRUGS OF THE FUTURE》, vol. 32, no. 9, 31 December 2007 (2007-12-31), pages 766 - 770, XP055010380, DOI: doi:10.1358/dof.2007.032.09.1135518 * |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2018200108A1 (en) | 2018-01-25 |
| JP2013540719A (ja) | 2013-11-07 |
| NZ630494A (en) | 2016-05-27 |
| WO2012030939A1 (en) | 2012-03-08 |
| AU2011296015B2 (en) | 2015-11-12 |
| CA2808890A1 (en) | 2012-03-08 |
| EA201390335A1 (ru) | 2013-09-30 |
| SG10201506896RA (en) | 2015-10-29 |
| US9770455B2 (en) | 2017-09-26 |
| AU2011296015A1 (en) | 2013-04-04 |
| EP2611449A1 (en) | 2013-07-10 |
| AU2016200860A1 (en) | 2016-02-25 |
| NZ608266A (en) | 2015-09-25 |
| US20120252787A1 (en) | 2012-10-04 |
| MX2013002418A (es) | 2013-08-01 |
| JP2019031577A (ja) | 2019-02-28 |
| AU2016200860B2 (en) | 2017-10-12 |
| HK1210419A1 (en) | 2016-04-22 |
| EP2939677A1 (en) | 2015-11-04 |
| US20150196567A1 (en) | 2015-07-16 |
| US8999970B2 (en) | 2015-04-07 |
| KR20140091458A (ko) | 2014-07-21 |
| JP2016106148A (ja) | 2016-06-16 |
| SG188365A1 (en) | 2013-04-30 |
| BR112013004707A2 (pt) | 2016-05-10 |
| JP2017132811A (ja) | 2017-08-03 |
| US20170216307A1 (en) | 2017-08-03 |
| KR20180094131A (ko) | 2018-08-22 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US9770455B2 (en) | Administration of an anti-obesity compound to individuals with renal impairment | |
| JP4782003B2 (ja) | ５ｈｔ２ｃレセプター関連疾患の処置に有用なベンズアゼピン誘導体 | |
| EP2416795B1 (en) | Inhibitors of cognitive decline | |
| WO2021084495A1 (en) | The use of a splicing modulator for a treatment slowing progression of huntington's disease | |
| NO332764B1 (no) | Preparat omfattende karbostyril-derivat og stemningsleie-stabilisator, samt anvendelse derav | |
| JP2022516662A (ja) | Ｓ１ｐ１受容体に関連する状態を治療する方法 | |
| US12486287B2 (en) | Solid forms of a promoter of spinogenesis | |
| KR20210098487A (ko) | S1p1 수용체와 관련된 병태의 치료 방법 | |
| DE60317098T2 (de) | Carbostyril-derivate mit selektiven serotonin-aufnahmeinhibitoren zur behandlung von gemütskrankheiten | |
| KR20150070249A (ko) | 체중 관리 방법 | |
| CN119730849A (zh) | 用于在表现出正常认知表现的受试者中预防或减缓认知减退或损害的进展的方法 | |
| US20170348323A1 (en) | Methods and medical uses | |
| WO2021229519A1 (en) | Sterols in the treatment and/or prevention of sars-cov-2 infection | |
| US20260048069A1 (en) | Methods of treatment | |
| US6469008B2 (en) | (R)-hydroxynefazodone antipsychotic therapy | |
| WO2025226591A1 (en) | Methods of administering 9-[4-(cyclohexyloxy)phenyl]-7-methyl-3,4-dihydropyrazino[2,1-c][1,2,4]thiadiazine 2,2-dioxide without side effects | |
| US6586437B2 (en) | (S)-hydroxynefazodone antipsychotic therapy | |
| TW202521119A (zh) | 用於投與特定vmat2抑制劑之方法 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| WD01 | Invention patent application deemed withdrawn after publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20131009 |