Isoxazolines as inhibitors of fatty acid amide hydrolase
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A01N-043/00
A61K-031/55
A01N-043/42
A61K-031/44
A01N-043/80
A61K-031/42
C07D-261/02
C07D-401/00
출원번호
US-0782658
(2010-05-18)
등록번호
US-8765735
(2014-07-01)
발명자
/ 주소
Behnke, Mark L.
Castro, Alfredo C.
Chan, Lawrence K.
Evans, Catherine A.
Grenier, Louis
Grogan, Michael J.
Leblanc, Yves
Liu, Tao
Peluso, Stephane
Snyder, Daniel A.
Tibbitts, Thomas T.
출원인 / 주소
Infinity Pharmaceuticals, Inc.
대리인 / 주소
Day, Jones
인용정보
피인용 횟수 :
0인용 특허 :
48
초록▼
The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmac
The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.
대표청구항▼
1. A compound of formula (I): or a pharmaceutically acceptable form thereof, wherein: Rc and Rd are joined to form a C3-10 carbocyclyl spiro-fused ring, and Ra and Rb are independently selected from the group consisting of —H, “C7-10” alkyl and C1-10 perhaloalkyl;G is selected from the group consist
1. A compound of formula (I): or a pharmaceutically acceptable form thereof, wherein: Rc and Rd are joined to form a C3-10 carbocyclyl spiro-fused ring, and Ra and Rb are independently selected from the group consisting of —H, “C7-10” alkyl and C1-10 perhaloalkyl;G is selected from the group consisting of —Br, —I, —F, —Cl, and —ORe; andRe is selected from the group consisting of C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-10 carbocycyl, C6-14 aryl, 3-14 membered heterocyclyl and 5-14 membered heteroaryl. 2. The compound according to claim 1, wherein Ra and Rb are both —H. 3. The compound according to claim 1, wherein the compound is of the formula: or a pharmaceutically acceptable form thereof;wherein W24, W25, W26, W27, W28 and W29 are, independently, CH2, CHR15, or C(R15)2, or optionally wherein W25 and W26 are substituted with a fused C6 aryl ring or fused 6-membered heteroaryl ring; t and v are, independently, 0 or 1; andeach R15 is independently selected from the group consisting of fluoro, bromo, chloro, iodo, —CN, —NO2, —N3, —SO2H, —SO3H, —OH, —OR16, —ON(R18)2, —N(R18)2, —N(R18)3, +X−, —N(OR17) R18, —SH, —SR16, —SSR17, —C(═O)R16, —CO2H, —CHO, —C(OR17)2, —CO2R16, —OC(═O)R16, —OCO2R16, —C(═O)N(R18)2, —OC(═O)N(R18)2, —NR18C(═O)R16, —NR18CO2R16, —NR18C(═O)N(R18)2, —C(R18)R16, —C(═NR18)OR16, —OC(═NR18)R16, OC(═NR18)OR16, —C(═NR18)N(R18)2, —OC(═NR18)N(R18)2, —NR18C(═NR18)N(R18)2, C(═O)NR18SO2R16, —NR18SO2R16, —SO2N(R18)2, —SO2R16, —SO2OR16, —OSO2R16, —S(═O)R16, —OS(═O)R16, —Si(R16)3, —OSi(R16)3—C(═S)N(R18)2, —C(═O)SR16, —C(═S)SR16, —SC(S)SR16, —P(═O)2R16, —OP(═O)2R16, —P(═O)(R16)2, —OP(═O)(R16)2, —OP(═O)(OR17)2, —P(═O)2N(R18)2, —OP(═O)2N(R18)2, —P(═O)(NR18)2, —OP(═O)(NR18)2, —NR18P(═O)(OR17)2, —NR18P(═O)(NR18)2, —P(R17)2, —P(R17)3, —OP(R17)2, —OP(R17)3, —B(OR17)2, —BR16(OR17), C1-10 alkyl, C1-10 perhaloalkyl, C2-10 alkenyl, C2-10 alkynyl, C3-14 carbocyclyl, 3-14 membered heterocyclyl, C6-14 aryl, and 5-14 membered heteroaryl, wherein each alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl is independently substituted with 0, 1, 2, 3, 4, or 5 R19 groups; or two vicinal R15 groups are replaced with the group —O(C(R2)2)1-2O— wherein each R2 is independently —H, C1-6 alkyl or halogen;each instance of R16 is, independently, selected from the group consisting of C1-10 alkyl, C1-10 perhaloalkyl, C2-10 alkenyl, C2-10 alkynyl, C3-10 carbocyclyl, 3-14 membered heterocyclyl, C6-14 aryl, and 5-14 membered heteroaryl, wherein each alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl is independently substituted with 0, 1, 2, 3, 4, or 5 R19 groups;each instance of R18 is, independently, selected from the group consisting of hydrogen, —OH, —OR16, —N(R17)2, —CN, —C(═O)R16, —C(═O)N(R17)2, —CO2R16, —SO2R16, —C(═NR17)OR16, —C(═NR17)N(R17)2, —SO2N(R17)2, —SO2R17, —SO2OR17, —SOR16, —C(═S)N(R17)2, —C(═O)SR17, —C(═S)SR17, —P(═O)2R16, —P(═O)(R16)2, —P(═O)2N(R17)2, —P(═O)(NR17)2, C1-10 alkyl, C1-10 perhaloalkyl, C2-10 alkenyl, C2-10 alkynyl, C3-10 carbocyclyl, 3-14 membered heterocyclyl, C6-14 aryl, and 5-14 membered heteroaryl, or two R18 groups attached to an N atom are joined to form a 3-14 membered heterocyclyl or 5-14 membered heteroaryl ring, wherein each alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl is independently substituted with 0, 1, 2, 3, 4, or 5 R19 groups;each instance of R17 is, independently, selected from the group consisting of hydrogen, C1-10 alkyl, C1-10 perhaloalkyl, C2-10 alkenyl, C2-10 alkynyl, C3-10 carbocyclyl, 3-14 membered heterocyclyl, C6-14 aryl, and 5-14 membered heteroaryl, or two R17 groups attached to an N atom are joined to form a 3-14 membered heterocyclyl or 5-14 membered heteroaryl ring, wherein each alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl is independently substituted with 0, 1, 2, 3, 4, or 5 R19 groups;each instance of R19 is, independently, selected from the group consisting of halogen, —CN, —NO2, —N3, —SO2H, —SO3H, —OH, OR20, —ON(R21)2, —N(R21)2, —N(R21)3+X−, —N(OR20)R21, —SH, —SR20, SSR20, —C(═O)R20, —CO2H, —CO2R20, OC(═O)R20, —OCO2R20, —C(═O)N(R21)2, —OC(═O)N(R21)2, —NR21C(═O)R20, —NR21CO2R20, —R21C(═O)N(R21)2, —C(═NR21)2, —OC(═NR21)R20, —OC(═NR21)OR20, C(═NR21)N(R21)2, —OC(═NR21)N(R21)2, —NR21C(═NR21)N(R21)2, —NR21SO2R20, —SO2N(R21)2, SO2R20, —SO2OR20, —OSO2R20, —S(═O)R20, —Si(R20)3, —OSi(R20)3, —C(═S)N(R21)2, —C(═O)SR20, —C(═S)SR20, —SC(═S)SR20, —P(═O)2R20, —P(═O)(R20)2, —OP(═O)(R20)2, —OP(═O)(OR20)2, C1-6 alkyl, C1-6 perhaloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 carbocyclyl, 3-10 membered heterocyclyl, C6-10 aryl, and 5-10 membered heteroaryl, wherein each alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl is independently substituted with 0, 1, 2, 3, 4, or 5 R22 groups, or two geminal R19 substituents can be joined to form ═O or ═S;each instance of R20 is, independently, selected from the group consisting of C1-6 alkyl, C1-6 perhaloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 carbocyclyl, C6-10 aryl, 3-10 membered heterocyclyl, and 3-10 membered heteroaryl, wherein each alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl is independently substituted with 0, 1, 2, 3, 4, or 5 R22 groups;each instance of R21 is, independently, selected from the group consisting of hydrogen, C1-6 alkyl, C1-6 perhaloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 carbocyclyl, 3-10 membered heterocyclyl, C6-10 aryl and 5-10 membered heteroaryl, or two R21 groups attached to an N atom are joined to form a 3-14 membered heterocyclyl or 5-14 membered heteroaryl ring, wherein each alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl is independently substituted with 0, 1, 2, 3, 4, or 5 R22 groups; andeach instance of R22 is, independently, selected from the group consisting of halogen, —CN, —NO2, —N3, —SO2H, —SO3H, —OH, —OC1-6 alkyl, —ON(C1-6 alkyl), —N(C1-6 alkyl), —N(C1-6 alkyl)3X, —NH(C1-6 alkyl)2X, —NH2(C1-6 alkyl)X, —NH3X, —N(OC1-6 alkyl)(C1-6 alkyl), —N(OH)(C1-6 alkyl), —NH(OH), —SH, —SC1-6 alkyl, —SS(C1-4 alkyl), —C(═O)(C1-6 alkyl), —CO2H, —CO2(C1-6 alkyl), —OC(═O)(C1-6 alkyl), —OCO2(C1-6 alkyl), —C(═O)NH2, —C(═O)N(C1-6 alkyl)2, —OC(═O)NH(C1-6 alkyl), —NHC(═O)(C1-6 alkyl), —N(C1-6 alkyl)C(═O)(C1-6 alkyl), —NHCO2(C1-6 alkyl), —NHC(═O)N(C1-6 alkyl), —NHC(═O)NH(C1-6 alkyl), —NHC(═O)NH2, —C(═NH)O(C1-6 alkyl), —OC(═NH)(C1-6 alkyl), —OC(═NH)OC1-6 alkyl, —C(═NH)N(C1-6 alkyl), —C(═NH)NH(C1-6 alkyl), —C(═NH)NH2, —OC(═NH)N(C1-6 alkyl), —OC(NH)NH(C1-6 alkyl), —OC(NH)NH2, —NHC(NH)N(C1-6 alkyl), —NHC(═NH)NH2, —NHSO2(C1-6 alkyl), —SO2N(C1-6 alkyl)2, —SO2NH(C1-6 alkyl), —SO2NH2, —SO2C1-4, alkyl, —SO2OC1-6 alkyl, —OSO2C1-6 alkyl, —SOC1-6 alkyl, —Si(C1-6 alkyl)3, —OSi(C1-6 alkyl)3 —C(═S)N(C1-6 alkyl), C(═S)NH(C1-6 alkyl), C(═S)NH2, —C(═O)S(C1-6 alkyl), —C(═S)SC1-6 alkyl, —SC(═S)SC1-6 alkyl, —P(═O)2(C1-6 alkyl), —P(═O)(C1-6 alkyl)2, —OP(═O)(C1-6 alkyl), —OP(═O)(OC1-6 alkyl), C1-6 alkyl, C1-6 perhaloalkyl, C2-4 alkenyl, C2-6 alkynyl, C3-10 carbocyclyl, C6-10 aryl, 3-10 membered heterocyclyl, and 5-10 membered heteroaryl; or two geminal R22 substituents can be joined to form ═O or ═S;wherein X− is a counterion. 4. The compound according to 3, wherein t is 0, v is 0 and W25 and W26 are substituted with a fused C6 aryl ring, and wherein W27 and W28 are, independently, CH2, CHR15, or C(R15)2. 5. The compound according to claim 4, wherein the compound is of the formula: or a pharmaceutically acceptable form thereof; wherein z is 0, 1, 2, 3 or 4. 6. The compound according to claim 5, wherein W27 and W28 are both CH2 groups. 7. The compound according to claim 6, wherein the compound is of the formula: or a pharmaceutically acceptable form thereof. 8. The compound according to claim 1, wherein G is —ORe. 9. The compound according to claim 8, wherein Re is 5-14 membered heteroaryl. 10. The compound according to claim 9, wherein Re is a 6-membered heteroaryl. 11. The compound according to claim 10, wherein Re is a pyridinyl group. 12. The compound according to claim 11, wherein Re is a monosubstituted pyridinyl group. 13. The compound according to claim 11, wherein Re is a 3-pyridinyl group. 14. The compound according to claim 11, wherein Re is a pyridinyl group of the formula: wherein x is 0, 1, 2, 3 or 4, andeach Rh is, independently, selected from the group consisting of fluoro, bromo, chloro, iodo, —CN, —NO2, —N3, —SO2H, —SO3H, —OH, —ORi, —ON(Rk)2, —N(Rk)2, —N(Rk)3+X−, —N(ORj)Rk, —SH, —SRi, —SSRj, —C(═O)Ri, —CO2H, —CHO, —CO2Ri, —OC(═O)Ri, —OCO2Ri, —C(═O)N(Rk)2, —OC(═O)N(Rk)2, —NRkC(═O)Ri, —NRkCO2Ri, —NRkC(═O)N(Rk)2, —C(═NRk) Ri, —C(═NRk)ORi, —OC(═NRk)Ri, —OC(═NRk)ORi, —C(═NRk)N(Rk)2, —OC(═NRk)N(Rk)2, —NRkC(═NRk)N(Rk)2, —C(═O)NRkSO2Ri, —NRkSO2Ri, —SO2N(Rk)2, —SO2Ri, —SO2ORi, —OSO2Ri, —S(═O)Ri, —OS(═O)Ri, —Si(Ri)3, —OSi(Ri)3—C(═S)N(Rk)2, —C(═O)SRi, —C(═S)SRi, —SC(S)SRi, —P(═O)2Ri, —OP(═O)2Ri, —P(═O)(Ri)2, —OP(═O)(Ri)2, —OP(═O)(ORj)2, —P(═O)2N(Rk)2, —OP(═O)2N(Rk)2, —P(═O)(NRk)2, —OP(═O)(NRk)2, —NRkP(═O)(ORj)2, —NRkP(═O)(NRk)2, —P(Rj)2, —P(Rj)3, —OP(Rj)2, —OP(Rj)3, —B(ORj)2, —BRi(ORj), C1-10 alkyl, C1-10 perhaloalkyl, C2-10 alkenyl, C2-10 alkynyl, C3-14 carbocyclyl, 3-14 membered heterocyclyl, C6-14 aryl, and 5-14 membered heteroaryl, wherein each alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl is independently substituted with 0, 1, 2, 3, 4, or 5 Rm groups;each instance of Ri is, independently, selected from the group consisting of C1-10 alkyl, C1-10 perhaloalkyl, C2-10 alkenyl, C2-10 alkynyl, C3-10 carbocyclyl, 3-14 membered heterocyclyl, C6-14 aryl, and 5-14 membered heteroaryl, wherein each alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl is independently substituted with 0, 1, 2, 3, 4, or 5 Rm groups;each instance of Rk is, independently, selected from the group consisting of hydrogen, —OH, —ORi, —N(Rj)2, —CN, —C(═O)Ri, —C(═O)N(Rj)2, —CO2Ri, —SO2Ri, —C(═NRj)ORi, —C(═NRj)N(Rj)2, —SO2N(Rj)2, —SO2Rj, —SO2ORj, —C(═S)N(Rj)2, —C(═O)SRj, —C(═S)SRj, —P(═O)2Ri, —P(═O)(Ri)2, —P(═O)2N(Rj)2, —P(═O)(NRj)2, C1-10 alkyl, C1-10 perhaloalkyl, C2-10 alkenyl, C2-10 alkynyl, C3-10 carbocyclyl, 3-14 membered heterocyclyl, C6-14 aryl, and 5-14 membered heteroaryl, or two Rk groups attached to an N atom are joined to form a 3-14 membered heterocyclyl or 5-14 membered heteroaryl ring, wherein each alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl is independently substituted with 0, 1, 2, 3, 4, or 5 Rm groups;each instance of Rj is, independently, selected from the group consisting of hydrogen, C1-10 alkyl, C1-10 perhaloalkyl, C2-10 alkenyl, C2-10 alkynyl, C3-10 carbocyclyl, 3-14 membered heterocyclyl, C6-14 aryl, and 5-14 membered heteroaryl, or two Rj groups attached to an N atom are joined to form a 3-14 membered heterocyclyl or 5-14 membered heteroaryl ring, wherein each alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl is independently substituted with 0, 1, 2, 3, 4, or 5 Rm groups;each instance of Rm is, independently, selected from the group consisting of fluoro, bromo, chloro, iodo, —CN, —NO2, —N3, —SO2H, —SO3H, —OH, —ORo, —ON(Rn)2, —N(Rn)2, —N(Rn)3+X−, —N(ORo)Rn, —SH, —SRo, —SSRo, —C(═O)Ro, —CO2H, —CO2Ro, —OC(═O)Ro, —OCO2Ro, —C(═O)N(Rn)2, —OC(═O)N(Rn)2, —NRnC(═O)Ro, —NRnCO2Rn, —NRnC(═O)N(Rn)2, —C(═NRn)ORo, —OC(═NRn)Ro, —OC(═NRn)ORo, —C(═NRn)N(Rn)2, —OC(═NRn)N(Rn)2, —NRnC(═NRn)N(Rn)2, —NRnSO2Ro, —SO2N(Rn)2, —SO2Ro, —SO2ORo, —OSO2Ro, —S(═O)Ro, —Si(Ro)3, —OSi(Ro)3, —C(═S)N(Rn)2, —C(═O)SRo, —C(═S)SRo, —SC(═S)SRo, —P(═O)2Ro, —P(═O)(Ro)2, —OP(═O)(Ro)2, —OP(═O)(ORo)2, C1-6 alkyl, C1-6 perhaloalkyl, C2-6 alkenyl, C2—6 alkynyl, C3-10 carbocyclyl, 3-14 membered heterocyclyl, C6-14 aryl, and 5-14 membered heteroaryl, wherein each alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl is independently substituted with 0, 1, 2, 3, 4, or 5 RP groups, or two geminal Rm substituents can be joined to form ═O or ═S;each instance of Ro is, independently, selected from the group consisting of C1-6 alkyl, C1-6 perhaloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 carbocyclyl, C6-10 aryl, 3-10 membered heterocyclyl, and 3-10 membered heteroaryl, wherein each alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl is independently substituted with 0, 1, 2, 3, 4, or 5 Rp groups;each instance of Rn is, independently, selected from the group consisting of hydrogen, C1-6 alkyl, C1-6 perhaloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 carbocyclyl, 3-10 membered heterocyclyl, C6-10 aryl, and 5-10 membered heteroaryl, or two Rn groups attached to an N atom are joined to form a 3-14 membered heterocyclyl or 5-14 membered heteroaryl ring, wherein each alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl is independently substituted with 0, 1, 2, 3,4, or 5 RP groups; andeach instance of Rp is, independently, selected from the group consisting of fluoro, bromo, chloro, iodo, —CN, —NO2, —N3, —SO2H, —SO3H, —OH, —OC1-6 alkyl, —ON(C1-6 alkyl)2, —N(C1-6 alkyl)2, —N(C1-6 alkyl)3X, —NH(C1-6 alkyl)2X, —NH2(C1-6 alkyl)X, —NH3X, —N(OC1-6 alkyl)(C1-6 alkyl), —N(OH)(C1-6 alkyl), —NH(OH), —SH, —SC1-6 alkyl, —SS(C1-6 alkyl), —C(═O)(Ci-k, alkyl), —CO2H, —CO2(C1-6 alkyl), —OC(═O)(C1-6 alkyl), —OCO2(C1-6 alkyl), —C(═O)NH2, —C(═O)N(C1-6 alkyl)2, —OC(═O)NH(C1-6 alkyl), —NHC(═O)(C1-6 alkyl), —N(C1-6 alkyl)C(═O)(C1-6 alkyl), —NHCO2(C1-6 alkyl), —NHC(═O)N(C1-6 alkyl)2, —NHC(═O)NH(C1-6 alkyl), —NHC(═O)NH2, —C(═NH)O(C1-6 alkyl), —OC(═NH)(C1-6 alkyl), —OC(═NH)OC1-6 alkyl, —C(═NH)N(C1-6 alkyl)2, —C(═NH)NH(C1-6 alkyl), —C(═NH)NH2, —OC(═NH)N(C1-6 alkyl)2, —OC(NH)NH(C1-6 alkyl), —OC(NH)NH2, —NHC(NH)N(C1-6 alkyl)2, —NHC(═NH)NH2, —NHSO2(C1-6 alkyl), —SO2N(C1-6 alkyl)2, —SO2NH(C1-6 alkyl), —SO2NH2, —SO2C1-6 alkyl, —SO2OC1-6 alkyl, —OSO2C1-6 alkyl, —SOC1-6 alkyl, —Si(C1-6 alkyl)3, alkyl)3—C(═S)N(C1-6 alkyl)2, C(═S)NH(C1-6 alkyl), C(═S)NH2, —C(═O)S(C1-6 alkyl), —C(═S)SC1-6 alkyl, —SC(═S)SC1-6 alkyl, —P(═O)2(C1-6 alkyl), —P(═O)(C1-6 alkyl)2, —OP(═O)(C1-6 alkyl)2, —OP(═O)(OC1-6 alkyl)2, C1-6 alkyl, C1-6 perhaloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 carbocyclyl, C6-14 aryl, 3-14 membered heterocyclyl, and 5-14 membered heteroaryl; or two geminal Rp substituents can be joined to form ═O or ═S;wherein X− is a counterion. 15. The compound according to claim 14, wherein Rh is selected from the group consisting of fluoro, bromo, chloro, iodo, —CN, —NO2, —OH, —ORi, —SRi, N(Rk)2, —N(Rk)3+X−, —C(═O)Ri, —CO2Ri, —CO2H, —OC(═O)Ri, —OCO2Ri, —C(═O)N(Rk)2, —OC(═O)N(Rk)2, —NRkC(═O)Ri, —NRkCO2Ri, —NRkC(═O)N(Rk)2, —C(═O)NRkSO2Ri, —NRkSO2Ri, —SO2N(Rk)2, —SO2Ri, C1-10 alkyl, C6 aryl, and 5-6 membered heteroaryl, wherein each alkyl, aryl, and heteroaryl is independently substituted with 0, 1, 2, 3 or 4 Rm groups; and wherein is a counterion. 16. The compound according to claim 15, wherein Rh is selected from the group consisting of —C(═O)Ri, —CO2H, —SO2Ri, and 5-membered heteroaryl independently substituted with 0 or 1 Rm groups. 17. The compound according to claim 16, wherein the 5-membered heteroaryl is selected from the group consisting of pyrrolyl, furanyl, thiophenyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, triazolyl, oxadiazolyl, thiadiazolyl, and tetrazolyl. 18. The compound according to claim 14, wherein the pyridinyl group is a 3-pyridinyl group of the formulae: 19. The compound according to claim 8, wherein G is —ORe selected from the group consisting of: 20. The compound according to claim 1, wherein the compound is substantially enantiomerically pure. 21. A pharmaceutical composition comprising a compound of claim 1, or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. 22. The compound according to claim 19, wherein G is —ORe selected from the group consisting of: 23. The compound according to claim 1, wherein the compound is: Com-poundGR15III-63—BrIII-64III-66—Br—OCF3III-67—OCF3III-68—OCF3III-70—OCF3III-71—OCF3III-73—OCF3III-74—OCF3III-1III-2III-3III-4III-8III-62or a pharmaceutically acceptable form thereof. 24. The compound according to claim 1, wherein the compound is: or a pharmaceutically acceptable form thereof. 25. The compound according to claim 1, wherein the compound is: or a pharmaceutically acceptable form thereof. 26. The compound according to claim 1, wherein the compound is: or a pharmaceutically acceptable form thereof. 27. The compound according to claim 1, wherein the compound is: or a pharmaceutically acceptable form thereof. 28. The pharmaceutical composition according to claim 21, wherein the compound is: or a pharmaceutically acceptable form thereof. 29. The pharmaceutical composition according to claim 21, wherein the compound is: or a pharmaceutically acceptable form thereof. 30. The pharmaceutical composition according to claim 21, wherein the compound is: or a pharmaceutically acceptable form thereof.
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Schwab Wilfried (Wiesbaden DEX) Anagnostopulos Hiristo (Wiesbaden DEX) Porsche-Wiebking Elena (Wiesbaden DEX) Grome John (Wiesbaden DEX), 3,5-disubstituted 2-isoxazolines and isoxazoles, agents containing them and their use.
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Wityak John ; Xue Chu-Biao ; Sielecki-Dzurdz Thais Motria ; Olson Richard Eric ; Degrado William Frank ; Cain Gary Avonn ; Batt Douglas Guy ; Pinto Donald ; Hussain Munir Alwan ; Mousa Shaker Ahmed, Isoxazoline and isoxazole fibrinogen receptor antagonists.
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Lilley Stephen J. (Sawston GBX) Taylor Hugh F. (Sawston GBX) Theobald David R. (Huntingdon GBX) Carlson Craig J. (Andover MA) Rosen David I. (Arlington MA) Johnson Thomas R. (Milford NH), Medical injection system and method, gas spring thereof and launching device using gas spring.
Limburg William W. (Penfield NY) Mammino Joseph (Penfield NY) Liebermann George (Mississauga NY CAX) Griffiths Clifford H. (Pittsford NY) Shahin Michael M. (Pittsford NY) Malhotra Shadi L. (Mississau, Method for obtaining improved image contrast in migration imaging members.
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Hudson Derek (San Anselmo CA) Johnson Charles R. (Berkeley CA) Ross Michael J. (Hillsborough CA) Shoemaker Kevin R. (San Francisco CA) Cass Robert T. (San Mateo CA) Giebel Lutz B. (Burlingame CA), Thin film HPMP matrix systems and methods for constructing and displaying ligands.
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