JP2016537431A5 - - Google Patents

Info

Publication number

JP2016537431A5

JP2016537431A5 JP2016554826A JP2016554826A JP2016537431A5 JP 2016537431 A5 JP2016537431 A5 JP 2016537431A5 JP 2016554826 A JP2016554826 A JP 2016554826A JP 2016554826 A JP2016554826 A JP 2016554826A JP 2016537431 A5 JP2016537431 A5 JP 2016537431A5

Authority

JP

Japan

Prior art keywords

obese

pharmaceutical formulation

pharmaceutical

formulation according

obesity

Prior art date

2014-11-25

Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)

Granted

Links

• Espacenet
• Global Dossier
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• 239000008194 pharmaceutical composition Substances 0.000 claims description 30
• 238000000034 method Methods 0.000 claims description 22
• 238000009472 formulation Methods 0.000 claims description 15
• 239000000203 mixture Substances 0.000 claims description 15
• RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 12
• 239000000825 pharmaceutical preparation Substances 0.000 claims description 12
• 150000001875 compounds Chemical class 0.000 claims description 9
• KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical group NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims description 8
• 125000000217 alkyl group Chemical group 0.000 claims description 8
• 125000003118 aryl group Chemical group 0.000 claims description 8
• 230000014101 glucose homeostasis Effects 0.000 claims description 8
• NRYBAZVQPHGZNS-ZSOCWYAHSA-N leptin Chemical compound O=C([C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CC(C)C)CCSC)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CS)C(O)=O NRYBAZVQPHGZNS-ZSOCWYAHSA-N 0.000 claims description 8
• 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 claims description 7
• 239000008103 glucose Substances 0.000 claims description 7
• -1 -COOR 8) Chemical class 0.000 claims description 6
• 238000006845 Michael addition reaction Methods 0.000 claims description 6
• 210000000577 adipose tissue Anatomy 0.000 claims description 6
• 150000001408 amides Chemical class 0.000 claims description 6
• 235000013877 carbamide Nutrition 0.000 claims description 6
• 150000001732 carboxylic acid derivatives Chemical class 0.000 claims description 6
• 150000002148 esters Chemical class 0.000 claims description 6
• 229910052736 halogen Inorganic materials 0.000 claims description 6
• 150000002367 halogens Chemical class 0.000 claims description 6
• 150000002825 nitriles Chemical class 0.000 claims description 6
• 150000003568 thioethers Chemical class 0.000 claims description 6
• 102000016267 Leptin Human genes 0.000 claims description 4
• 108010092277 Leptin Proteins 0.000 claims description 4
• OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 4
• XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims description 4
• 125000003342 alkenyl group Chemical group 0.000 claims description 4
• 125000002877 alkyl aryl group Chemical group 0.000 claims description 4
• 125000000304 alkynyl group Chemical group 0.000 claims description 4
• 150000001412 amines Chemical class 0.000 claims description 4
• 239000008280 blood Substances 0.000 claims description 4
• 210000004369 blood Anatomy 0.000 claims description 4
• 239000004202 carbamide Substances 0.000 claims description 4
• 125000000753 cycloalkyl group Chemical group 0.000 claims description 4
• BYUYRWRYAISPPF-UHFFFAOYSA-N cyclobutyloxycyclobutane Chemical compound C1CCC1OC1CCC1 BYUYRWRYAISPPF-UHFFFAOYSA-N 0.000 claims description 4
• 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 4
• 235000012631 food intake Nutrition 0.000 claims description 4
• 230000037406 food intake Effects 0.000 claims description 4
• 238000007306 functionalization reaction Methods 0.000 claims description 4
• 125000001072 heteroaryl group Chemical group 0.000 claims description 4
• 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 4
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 4
• 229940039781 leptin Drugs 0.000 claims description 4
• 125000001424 substituent group Chemical group 0.000 claims description 4
• 208000016261 weight loss Diseases 0.000 claims description 4
• 230000004580 weight loss Effects 0.000 claims description 4
• 239000003472 antidiabetic agent Substances 0.000 claims description 3
• 206010007134 Candida infections Diseases 0.000 claims description 2
• LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 2
• 125000002252 acyl group Chemical group 0.000 claims description 2
• 229940125708 antidiabetic agent Drugs 0.000 claims description 2
• 230000037396 body weight Effects 0.000 claims description 2
• 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 2
• 235000021316 daily nutritional intake Nutrition 0.000 claims description 2
• 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims description 2
• 229910052739 hydrogen Inorganic materials 0.000 claims description 2
• 239000001257 hydrogen Substances 0.000 claims description 2
• 125000004435 hydrogen atom Chemical class [H]* 0.000 claims description 2
• 230000001939 inductive effect Effects 0.000 claims description 2
• 150000003140 primary amides Chemical class 0.000 claims description 2
• 150000003141 primary amines Chemical class 0.000 claims description 2
• 239000000651 prodrug Substances 0.000 claims description 2
• 229940002612 prodrug Drugs 0.000 claims description 2
• 150000003839 salts Chemical class 0.000 claims description 2
• 150000003334 secondary amides Chemical class 0.000 claims description 2
• 150000003335 secondary amines Chemical class 0.000 claims description 2
• 125000000213 sulfino group Chemical group [H]OS(*)=O 0.000 claims description 2
• 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims description 2
• 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 2
• 150000003512 tertiary amines Chemical class 0.000 claims description 2
• 150000003573 thiols Chemical class 0.000 claims description 2
• 150000003672 ureas Chemical class 0.000 claims description 2
• 208000008589 Obesity Diseases 0.000 claims 9
• 235000020824 obesity Nutrition 0.000 claims 6
• 208000012696 congenital leptin deficiency Diseases 0.000 claims 3
• 208000001022 morbid obesity Diseases 0.000 claims 3
• 239000003814 drug Substances 0.000 claims 1
• 230000003178 anti-diabetic effect Effects 0.000 description 1
• 239000000883 anti-obesity agent Substances 0.000 description 1
• 238000002560 therapeutic procedure Methods 0.000 description 1