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1. CN1474810 - Substituted urea neuropeptide YY5 antagonists

Office
China
Application Number 01818782.X
Application Date 12.09.2001
Publication Number 1474810
Publication Date 11.02.2004
Publication Kind A
IPC
A61K 31/4465
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
445Non-condensed piperidines, e.g. piperocaine
4465only substituted in position 4
C07D 211/58
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06having no double bonds between ring members or between ring members and non-ring members
36with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
56Nitrogen atoms
58attached in position 4
CPC
A61P 1/14
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
A61P 1/16
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
16for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 3/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
A61P 3/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
04Anorexiants; Antiobesity agents
A61P 3/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
06Antihyperlipidemics
A61P 3/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
08for glucose homeostasis
10for hyperglycaemia, e.g. antidiabetics
Applicants Schering Corp.
先灵公司
Inventors W.J. Greenlee
W·J·格林李
Huang Ying
黄颖
J.M. Kelly
J·M·凯利
S·W·麦克坎比
A·W·斯塔姆福德
吴豫生
Agents zhang yuanzhong xu yanyi
中国专利代理(香港)有限公司
中国专利代理(香港)有限公司
Priority Data 60/232,255 14.09.2000 US
Title
(EN) Substituted urea neuropeptide YY5 antagonists
(ZH) 取代脲,神经肽YY5受体拮抗剂
Abstract
(EN)
A novel class of compounds such as antagonists of the neuropeptide Y Y5 receptor, methods of making such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention or amelioration of one or more diseases associated with the neuropeptide Y Y5 receptor are disclosed.Compounds represented by structural formula (I) including its N-oxides wherein Y is (I') R1 is H or (C1-C6)alkyl; R2 is H, (C1-C6)alkyl, (C3-C9)cycloalkyl or (C3-C7)cycloalkyl(C1-C6)alkyl; R3 is (II'); Z is OR10, -N(R9)(R10) or - NH2; j is 0, 1 or 2; k is 1 or 2; l is 0, 1 or 2; m is 0, 1 or 2; R4 is 1- 3 substituents independently selected from the group consisting of H, -OH, halogen, haloalkyl, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl(C1-C6)alkyl, -CN, -O(C1-C6)alkyl, -O(C3-C7)cycloalkyl, -O(C1-C6)alkyl(C3-C7)cycloalkyl, -S(C1-C6)alkyl, -S(C3-C7)cycloalkyl, -S(C1-C6)alkyl(C3-C7)cycloalkyl, -NH2, -NR9R10, -NO2, -CONH2, -CONR9R10 and NR2COR10.

(ZH)

要求保护结构式(I)表示的化合物,包括其N-氧化物,其中Y为(I’);R1为H或(C1-C6)烷基;R2为H,(C1-C6)烷基,(C3-C9)环烷基或(C3-C7)环烷基(C1-C6)烷基;R3为(II’);Z为OR10,-N(R9)(R10)或-NH2;j为0,1或2;k为1或2;l为0,1或2;m为0,1或2;R4为1-3个取代基,其独立地选自H,-OH,卤素,卤代烷基,(C1-C6)烷基,(C3-C7)环烷基,(C3-C7)环烷基(C1-C6)烷基,-CN,-O(C1-C6)烷基,-O(C3-C7)环烷基,-O(C1-C6)烷基(C3-C7)环烷基,-S(C1-C6)烷基,-S(C3-C7)环烷基,-S(C1-C6)烷基(C3-C7)环烷基,-NH2,-N(R9)(R10),-NO2,-CONH2,-CONR9R10和NR2COR10;R5为1-3个取代基,其独立地选自H,卤素,-OH,卤代烷基,卤代烷氧基,-CN,-NO2,(C1-C6)烷基,(C3-C7)环烷基,(C3-C7)环烷基(C1-C6)烷基,-O(C1-C6)烷基,-O(C3-C7)环烷基,-O(C1-C6)烷基(C3-C7)环烷基,-CONH2和-CONR9R10;R6为-SO2(C1-C6)烷基,-SO2(C3-C7)环烷基,-SO2(C1-C6)烷基(C3-C7)环烷基,-SO2(C1-C6)卤代烷基,-SO2(羟基(C2-C6)烷基),-SO2(氨基(C2-C6)烷基),-SO2(烷氧基(C2-C6)烷基),-SO2(烷基氨基(C2-C6)烷基),-SO2(二烷基氨基(C2-C6)烷基),-SO2(芳基),-SO2(杂芳基),-SO2(芳基(C2-C6)烷基),-SO2NH2,-SO2NR9R10,-C(O)(C1-C6)烷基,-C(O)(C3-C7)环烷基,-C(O)芳基,-C(O)杂芳基,-C(O)NR9R10,-C(O)NH2,-C(S)NR9R10,C(S)NH2,芳基,杂芳基,-(CH2)nC(O)NH2,-(CH2)nC(O)NR9R10,-C(=NCN)烷硫基,-C(=NCN)NR9R10,(C1-C6)烷基,(C3-C7)环烷基,(C3-C7)环烷基(C1-C6)烷基,芳基(C1-C6)烷基,杂芳基(C1-C6)烷基或-C(O)OR9,n=1-6;R7=H或烷基;R8为H,(C1-C6)烷基,(C3-C7)环烷基,(C3-C7)环烷基(C1-C6)烷基,芳基,杂芳基,-SO2(C1-C6)烷基,-SO2(C3-C7)环烷基,-SO2(C3-C7)环烷基(C1-C6)烷基,-SO2(C1-C6)卤代烷基或-SO2(芳基);R9为(C1-C6)烷基,(C3-C7)环烷基,(C3-C7)环烷基(C1-C6)烷基,芳基(C1-C6)烷基,芳基或杂芳基;及,R10为氢,(C1-C6)烷基,(C3-C7)环烷基,(C3-C7)环烷基(C1-C6)烷基,芳基(C1-C6)烷基,芳基或杂芳基;或其药学可接受的加合盐和/或水合物,或其前体药物,或R9和R10相联形成含有1-2个杂原子的4-7元环;或其可使用的几何或光学异构体或其外消旋混合物,以及另外的新型化合物;同时也要求保护使用前述化合物的药物组合物和其在治疗肥胖、进食障碍疾患,如食欲过盛和糖尿病中的方法。