Fused heterocyclic compounds and analogs thereof, modulators of nuclear hormone receptor function
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-031/425
C07D-498/02
C07D-498/00
출원번호
US-0111606
(2005-04-21)
등록번호
US-7291637
(2007-11-06)
발명자
/ 주소
Salvati,Mark E.
Balog,James Aaron
Pickering,Dacia A.
Zhu,Hong
출원인 / 주소
Bristol Myers Squibb Company
인용정보
피인용 횟수 :
0인용 특허 :
110
초록
Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.
대표청구항▼
We claim: 1. A compound of the following formula or a salt thereof: wherein the symbols have the following meanings and are, for each occurrence, independently selected: G is an aryl or heterocyclo group, where said group is mono-or polycyclic, and which is optionally substituted at one or more p
We claim: 1. A compound of the following formula or a salt thereof: wherein the symbols have the following meanings and are, for each occurrence, independently selected: G is an aryl or heterocyclo group, where said group is mono-or polycyclic, and which is optionally substituted at one or more positions; E is SO, SO2, or NR7; Y is O, S or (CR7R7')n wherein n=1 or 2; W is CR7R7'--CR7R7', CR8═CR8', or CR7R7'--C═O; Q1 is H, alkyl, or substituted alkyl; Q2 is H, alkyl, or substituted alkyl; R1 and R1' are each independently H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkyalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl; R2 is alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkylalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl; R4 is H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkylalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl, R1C═O, R1NHC═O, R1OC═O; SO2OR1, or SO2NR1R1'; R5 is alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkylalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl, R1C═O, R1NHC═O, SO2R1, SO2OR1, or SO2NR1R1'; R7 and R7' are each independently H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkylalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl, halo, N3, CN, OR1, O(C═O)R1, O(C═O)NHR1, O(C═O)OR1, nitro, hydroxylamine, hydroxylamide, amino, SR1, SeR1, NHR4, NR2R5, NOR1, thiol, alkylthio or substituted alkylthio, R1C═O, R1OC═O, R1NHC═O, SO2R1, SOR1, PO3R1R1', R1R1'NC═O, C═OSR1, SO2R1, SO2OR1, SO2NR1R1', OSO2-aryl, OSO2-(substituted aryl), OSO2-heterocyclo, OSO2-(substituted heterocyclo), or COCl; and R8 and R8' are each independently H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkyalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl, nitro, halo, CN, OR1, amino, NHR4, NR2R5, NOR1, alkylthio or substituted alkylthio, C═OSR1, R1OC═O, R1C═O, R1NHC═O, R1R1'NC═O, SO2OR1, S═OR1, SO2R1, PO3R1R1', or SO2NR1R1'. 2. The compound of claim 1 or a salt thereof, wherein W is CR7R7'--CR7R7' or CR8═CR8'. 3. The compound of claim 1 or a salt thereof, wherein E is SO or SO2. 4. The compound of claim 3 wherein said compound is: (3aα,4α,7α,7aα)-2-(3-Chloro-4-fluorophenyl)-3a,4,7,7a-tetrahydro-4,7-methano-1, 2-benzisothiazol-3(2H)-one-1,1-dioxide; (3aα,4α,7α,7aα)-4-(2,3,3a,4,7, 7a-Hexahydro-1,1-dioxido-3-oxo-4,7-methano-1,2-benzisothiazol-2-yl)benzoic acid, ethyl ester; (3aα,4α,7α,7aα)-2-(3-Chloro-2-fluorophenyl)-3a,4,7,7a-tetrahydro-4,7-methano-1, 2-benzisothiazol-3(2H)-one, 1,1-dioxide; or (3aα,4α,7α,7aα)-3a,4,7, 7a-Tetrahydro-2-(2,3,4-trifluorophenyl)-4,7-methano-1,2-benzisothiazol-3 (2H)-one, 1,1-dioxide. 5. The compound of claim 1 or a salt thereof, wherein E is NR7. 6. The compound of claim 3 wherein said compound is: (3aα,4α,7α,7aα)-Octahydro-3a-hydroxy-2-[4-nitro-3-(trifluoromethyl)phenyl]-4, 7-ethano-3H-indazol-3-one; or (3aα,4α,7α,7aα)-Octahydro-3a-hydroxy-2-[3-(trifluoromethyl)phenyl]-4,7-ethano-3H-indazol-3-one.
연구과제 타임라인
LOADING...
LOADING...
LOADING...
LOADING...
LOADING...
이 특허에 인용된 특허 (110)
Pinto, Donald Joseph Philip; Galemmo, Jr., Robert Anthony; Orwat, Michael James; Quan, Mimi Lifen, 1,4,5,6-tetrahydropyrazolo-[3,4,-c]-pyridin-7-ones useful as factor Xa inhibitors.
Poss Michael A. (Lawrenceville NJ) Pansegrau Paul D. (E. Windsor NJ) Wang Shaopeng (E. Windsor NJ) Thottathil John K. (Robbinsville NJ) Singh Janak (Lawrenceville NJ) Mueller Richard H. (Ringoes NJ), 7-oxabicycloheptane carboxylic acid prostaglandin analog intermediates useful in the preparation of anti-thrombotic and.
Moguilewsky Martine (Paris FRX) Bouton Marie M. (Paris FRX), Application of 1-(3′-trifluoromethyl-4′-nitrophenyl)-4,4′-dimethylimidazoline 2,5-dione in the treatment of hormone-d.
Vincent Michel (Bagneux FRX) Remond Georges (Versailles FRX) Laubie Michel (Vaucresson FRX), Azabicyclooctane-carboxylic acids and pharmaceutical compositions containing them and antihypertensive use thereof.
Schweikert Hans-Udo (Bonn-Roettgen DEX) Tunn Ulf (Castrup-Rauxel DEX) Senge Theodor (Castrup-Rauxel DEX) Nmann Friedmund (Berlin DEX), Combinations of an aromatase-inhibitor and an antiandrogen for prophylaxis and/or treatment of benign prostatic hyperpla.
Lubowitz Hyman R. (Rolling Hills Estates CA) Sheppard Clyde H. (Bellevue WA) Stephenson Ronald R. (Kirkland WA), Crosslinkable polyamideimide oligomers and a method of preparation.
Lubowtiz Hyman R. (Rolling Hills Estates CA) Sheppard Clyde H. (Post Falls ID), Heterocycle or heterocycle sulfone oligomers with multiple chemically functional end caps.
Wilde, Richard Gerald; Bakthavatchalam, Rajagopal; Beck, James Peter; Arvanitis, Argyrios Georgious, Imidazopyrimidines and imidazopyridines for the treatment of neurological disorders.
Bentley, Jonathan Mark; Roffey, Jonathan Richard Anthony; Davidson, James Edward Paul; Mansell, Howard Langham; Hamlyn, Richard John; Cliffe, Ian Anthony; Adams, David Reginald; Monck, Nathaniel Juli, Indole derivatives process for their preparation, pharmaceutical compositions containing them and their medicinal application.
Duane D. Miller ; Leonid I. Kirkovsky ; James T. Dalton ; Arnab Mukherjee, Irreversible non-steroidal antagonist compound and its use in the treatment of prostate cancer.
Miller Duane D. ; Kirkovsky Leonid I. ; Dalton James T. ; Mukherjee Arnab, Irreversible non-steroidal antagonist compound and its use in the treatment of prostate cancer.
Abou-Gharbia Magid A. (Wilmington DE) Schiehser Guy A. (Malvern PA) Patel Usha R. (Audubon PA), Isothiazolone 1,1-dioxide derivatives with psychotropic activity.
Salvati, Mark E.; Mitt, Toomas; Patel, Ramesh N.; Hanson, Ronald L.; Brzozowski, David; Goswami, Animesh; Chu, Linda Nga Hoong; Li, Wen-sen; Simpson, James H.; Totleben, Michael J.; He, Weixuan, Method for the preparation of fused heterocyclic succinimide compounds and analogs thereof.
Salvati, Mark E.; Gottardis, Marco M.; Attar, Ricardo M.; Krystek, Jr., Stanley R.; Sack, John S., Method for the treatment of a condition remediable by administration of a selective androgen receptor modulator.
Sekut Les ; Carter Adam ; Ghayur Tariq ; Banerjee Subhashis ; Tracey Daniel E., Methods and compositions for modulating responsiveness to corticosteroids.
Sheppard Clyde H. (Boeing Aerospace Company ; P.O. Box 399 ; M/S 73-09 Seattle WA 98124-2499) Lubowitz Hyman R. (26 Coral Tree Ln. Rolling Hills Estates CA 90274), Methods for making liquid molding compounds using diamines and dicyanates.
Vincent Michel (Bagneux FRX) Remond Georges (Versailles FRX) Portevin Bernard (Elancourt FRX) Herve Yolande (Puteaux FRX) Lepagnol Jean (Chatou FRX) Biton Catherine (Nanterre FRX), New heterocyclic tripeptide compounds.
Claussner Andre,FRX ; Goubet Francois,FRX ; Teutsch Jean,FRX, Optionally substituted phenylimidazolidines, their preparation process and intermediates, their use as medicaments and.
Tesoro Giuliana C. (Dobbs Ferry NY) Sastri Vinod R. (Brooklyn NY) Narang Subash C. (Menlo Park CA), Siloxane-containing polyimide coatings for electronic devices.
※ AI-Helper는 부적절한 답변을 할 수 있습니다.