[미국특허]
Thyronamine derivatives and analogs and methods of use thereof
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
C07C-211/27
C07C-211/00
A61K-031/135
출원번호
US-0099959
(2005-04-05)
등록번호
US-7355079
(2008-04-08)
발명자
/ 주소
Scanlan,Thomas S.
Hart,Matthew E.
Grandy,David K.
Bunzow,James R.
Miyakawa,Motonori
Tan,Edwin Saavedra
Suchland,Katherine L.
출원인 / 주소
The Regents of the University of California
Oregon Health & Science University
대리인 / 주소
Woodcock Washburn LLP
인용정보
피인용 횟수 :
1인용 특허 :
30
초록
Thyronamine derivatives and analogs, methods of using such compounds, and pharmaceutical compositions containing them are disclosed. Methods of preparing such compounds are also disclosed.
대표청구항▼
What is claimed is: 1. A compound of formula IV: or a stereoisomer, prodrug, pharmaceutically acceptable salt, hydrate, solvate, acid salt hydrate, N-oxide or isomorphic crystalline form therof; wherein independently, R1 and R2 are H, lower alkyl, cyclic alkyl, or benzyl; Y is--[C(R'R")]n--, whe
What is claimed is: 1. A compound of formula IV: or a stereoisomer, prodrug, pharmaceutically acceptable salt, hydrate, solvate, acid salt hydrate, N-oxide or isomorphic crystalline form therof; wherein independently, R1 and R2 are H, lower alkyl, cyclic alkyl, or benzyl; Y is--[C(R'R")]n--, where R' is H, and R" is aryl optionally substituted with 1-3 substituents selected from the group consisting of lower alkyl, halo, hydroxyl, and alkoxy; or benzyl wherein the phenyl portion thereof is optionally substituted with 1-3 substituents selected from the group consisting of lower alkyl, halo, hydroxyl, and alkoxy; Z is--[C(R)2]n--, CHOR, O, S, NR, CONH, or NHCO; R3, R4, R5, and R7 I, Br, Cl, F, H, CH3, CF3, CN, SR, OCH3, CH2CH3, or CH(CH3)2; R6 is OH, H, SH, F, CF3, lower alkyl, or N(R)2; R8 is OR, R, CH2OR, CH2NR2, CH2N+R3, SR, or CH2SR; X is O, S, SO, SO2, NR, C(R)2,-lower alkyl-O--,--O-lower alkyl-, COCH2O, or OCH2CO; R is H, lower alkyl, aryl optionally substituted with 1-3 substituents selected from the group consisting of lower alkyl, halo, hydroxy, and alkoxy; or benzyl wherein the phenyl portion thereof is optionally substituted with 1-3 substituents selected from the group consisting of lower alkyl, halo, hydroxy, and alkoxy; and n is 1 to 6. 2. The compound of claim 1, wherein R1 and R2 are H or lower alkyl, R6 is H, X is O, Y is O, and Z is alkyl. 3. The compound of claim 1, wherein R" is phenyl optionally substituted with 1-3 substituents selected from the group consisting of lower alkyl, halo, hydroxyl, and alkoxy. 4. A pharmaceutical composition, comprising at least one compound of claim 1 in combination with at least one pharmaceutically acceptable carrier or excipient. 5. A method for alleviating a disease state in a mammal believed to be responsive to treatment with a thyronamine antagonist comprising the step of administering to the mammal a therapeutic amount of a compound of claim 1, or a stereoisomer, prodrug, pharmaceutically acceptable salt, hydrate, solvate, acid salt hydrate, N-oxide or isomorphic crystalline form thereof. 6. The method of claim 5, wherein the disease state is depression, bipolar disorder, schizophrenia, eating disorders, anxiety, seizure, epilepsy, insomnia and sleeping disorders, gastro esophageal reflux disease, diseases involving gastrointestinal motility or asthma. 7. The method of claim 5, wherein the disease state is diabetes, hyperglycemia, hypoglycemia, cardiac arrhythmia, stroke, osteoporosis, obesity, atherosclerosis, hypertension, hyperthyroidism or hypothyroidism. 8. The method of claim 5, wherein the disease state is congestive heart failure. 9. The method of claim 5, wherein the disease state is fever or heatstroke. 10. A method of treating depression in a mammalian subject believed to be responsive to treatment with a thyronamine antagonist comprising administering a therapeutically effective amount of a compound of claim 1, or a stereoisomer, prodrug, pharmaceutically acceptable salt, hydrate, solvate, acid salt hydrate, N-oxide or isomorphic crystalline form thereof, to the subject. 11. The compound of claim 1, wherein R1 through R8 are H. 12. The compound of claim 1, wherein X is O. 13. The compound of claim 3, wherein R" is phenyl. 14. The compound of claim 1, wherein Z is--CH2--. 15. The compound of claim 11, wherein X is O. 16. The compound of claim 15, wherein Y is--CH(phenyl)--. 17. The compound of claim 16, wherein Z is--CH2--.
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