Imidazolidine carboxamide derivatives as lipase and phospholipase inhibitorsThe invention relates to imidazolidine carboxamide derivatives of general formula (I) having the meanings indicated in the description, the pharmaceutically usable salts thereof, and the use thereof as medicaments.The salt that can tolerate on the tautomeric form of formula i compound, described compound and the physiology thereofimplication wherein is:x, y be in the same manner or differently-c (r3) (r4)-,-(c=o)-,-(c=s), wherein at least-individual x or y be-(c=o)-or-(c=s)-; but can not all be simultaneously-(c=o)-or-(c=s)-; or x and y are c (r3)=c (r3) together;r is hydrogen, (c 1-c 8)-alkyl, (c 1-c 5)-haloalkyl, (cr5r6) m-o (r7), (c 1-c 3)-alkoxyl group-(c 1-c 3)-alkylidene group, aryl, heterocycle, (c 1-c 4)-alkylidene group-aryl, (c 1-c 4)-alkylidene group-heteroaryl, (c 1-c 4)-alkylidene group-(c 5-c 12)-cycloalkyl, wherein cycloalkyl, aryl, heterocycle or heteroaryl can be by f, cl, br, i, oh, cf 3, no 2, cn, ocf 3, o-(c 1-c 6)-alkyl, o-(c 1-c 4)-alkoxyl group-(c 1-c 4)-alkyl, s-(c 1-c 6)-alkyl, (c 1-c 6)-alkyl, (c 2-c 4)-haloalkyl, o-(c 2-c 4)-haloalkyl, (c 2-c 6)-alkenyl, (c 3-c 8)-cycloalkyl, o-(c 3-c 8)-cycloalkyl, (c 2-c 6)-alkynyl, (c 0-c 8)-alkylidene group-aryl, o-(c 0-c 8)-alkylidene group-aryl, s-aryl, (c 0-c 8)-alkylidene group-heteroaryl, n (r5) (r6), so 2-ch 3, so 2-nh 2, sf 5, cooh, coo-(c 1-c 6)-alkyl, con (r5) (r6), n (r5) co (r6), n (r5) so 2(r6), co (r5), (cr5r6) m '-o (r7), o-co-n (r5) (r6), o-co-(c 1-c 6)-alkylidene group-co-o-(c 1-c 6)-alkyl, o-co-(c 1-c 6)-alkylidene group-co-oh, o-co-(c 1-c 6)-alkylidene group-co-n (r5) (r6) replaces one or many, wherein aryl or heteroaryl can be successively by f, cl, br, i, oh, cf 3, no 2, cn, ocf 3, o-(c 1-c 6)-alkyl, o-(c 1-c 4)-alkoxyl group-(c 1-c 4)-alkyl, s-(c 1-c 6)-alkyl, (c 1-c 6)-alkyl, (c 2-c 6)-alkenyl, (c 3-c 8)-cycloalkyl, o-(c 3-c 8)-cycloalkyl, (c 2-c 6)-alkynyl, n (r8) (r9), so 2-ch 3, sf 5, cooh, coo-(c 1-c 6)-alkyl, con (r8) (r9), n (r8) co (r9), n (r8) so 2(r9), co (r8), (cr8r9) m '-o (r10), o-co-n (r8) (r9), o-co-(c 1-c 6)-alkylidene group-co-o-(c 1-c 6)-alkyl, o-co-(c 1-c 6)-alkylidene group-co-oh, o-co-(c 1-c 6)-alkylidene group-co-n (r8) (r9) replaces one or many; m, m ', m ' are 0,1,2,3,4,5,6;r5、r6、r7、r8、r9、r10be hydrogen, (c in the same manner or differently 1-c 8)-alkyl; or-(c=o)-nr1ar2a;or-(c=o)-o-r1b;orr and x for x=-c (r3) (r4)-form monocycle, saturated or undersaturated 4 to 7 yuan of ring systems of part or dicyclo saturated or undersaturated 8 to the 14 yuan of ring systems of part, each member of ring system can be replaced by one to three atom or the atomic group from following series: a chr11-,-cr11r12-,-(c=r11)-,=c (r11)-,-nr11-,-c (=o)-,-o-,-s-,-so-,-so 2-, condition be from series-o-,-s-,-so-,-so 2-two unit cannot be adjacent; r11, r12 are hydrogen, (c in the same manner or differently 1-c 6)-alkyl, aryl, (c 3-c 12)-cycloalkyl, (c 1-c 4)-alkylidene group-aryl, (c 1-c 3)-alkylidene group-(c 3-c 12)-cycloalkyl; wherein aryl or cycloalkyl can be by f, cl, br, i, oh, cf 3, no 2, cn, ocf 3, o-(c 1-c 6)-alkyl, o-(c 1-c 4)-alkoxyl group-(c 1-c 4)-alkyl, s-(c 1-c 6)-alkyl, (c 1-c 6)-alkyl, (c 2-c 4)-haloalkyl, o-(c 2-c 4)-haloalkyl, (c 2-c 6)-alkenyl, (c 2-c 6)-alkynyl, n (r13) (r14), so 2-ch 3, so 2-nh 2, sf 5, cooh, coo-(c 1-c 6)-alkyl, con (r13) (r14), n (r13) co (r14), n (r13) so 2(r14), co (r13), (cr13r14) n-o (r15), o-co-n (r13) (r14), o-co-(c 1-c 6)-alkylidene group-co-o-(c 1-c 6)-alkyl, o-co-(c 1-c 6)-alkylidene group-co-oh, o-co-(c 1-c 6)-alkylidene group-co-n (r13) (r14) replaces; n is 0,1,2,3,4,5,6;r13, r14, r15 are hydrogen, (c in the same manner or differently 1-c 8)-alkyl; r1, r1a, r1b are (c in the same manner or differently 5-c 16)-alkyl, ch 2-aryl, (c 1-c 2)-alkylidene group-heteroaryl, ch 2-(c 5-c 12)-cycloalkyl, wherein aryl, heteroaryl or cycloalkyl can be by f, cl, br, i, oh, cf 3, no 2, cn, ocf 3, o-(c 1-c 6)-alkyl, o-(c 1-c 4)-alkoxyl group-(c 1-c 4)-alkyl, s-(c 1-c 6)-alkyl, (c 1-c 6)-alkyl, (c 2-c 4)-haloalkyl, o-(c 2-c 4)-haloalkyl, (c 2-c 6)-alkenyl, (c 3-c 8)-cycloalkyl, o-(c 3-c 8)-cycloalkyl, (c 2-c 6)-alkynyl, (c 0-c 8)-alkylidene group-aryl, o-(c 0-c 8)-alkylidene group-aryl, s-aryl, (c 0-c 8)-alkylidene group-heteroaryl, n (r16) (r17), so 2-ch 3, so 2-nh 2, sf 5, cooh, coo-(c 1-c 6)-alkyl, con (r16) (r17), n (r16) co (r17), n (r16) so 2(r17), co (r16), (cr16r17) o-o (r18), o-co-n (r16) (r17), o-co-(c 1-c 6)-alkylidene group-co-o-(c 1-c 6)-alkyl, o-co-(c 1-c 6)-alkylidene group-co-oh, o-co-(c 1-c 6)-alkylidene group-co-n (r16) (r17) replaces one or many, and wherein aryl or heteroaryl successively can be by f, cl, br, i, oh, cf 3, no 2, cn, ocf 3, o-(c 1-c 6)-alkyl, o-(c 1-c 4)-alkoxyl group-(c 1-c 4)-alkyl, s-(c 1-c 6)-alkyl, (c 1-c 6)-alkyl, (c 2-c 6)-alkenyl, (c 3-c 8)-cycloalkyl, o-(c 3-c 8)-cycloalkyl, (c 2-c 6)-alkynyl, n (r19) (r20), so 2-ch 3, sf 5, cooh, coo-(c 1-c 6)-alkyl, con (r19) (r20), n (r19) co (r20), n (r19) so 2(r20), co (r19), (cr19r20) o '-o (r21), o-co-n (r19) (r20), o-co-(c 1-c 6)-alkylidene group-co-o-(c 1-c 6)-alkyl, o-co-(c 1-c 6)-alkylidene group-co-oh, o-co-(c 1-c 6)-alkylidene group-co-n (r19) (r20) replaces one or many; o, o ' are 0,1,2,3,4,5,6;r16、r17、r18、r...
리파제 및 포스포리파제 억제제로서의 이미다졸리딘 카복사미드 유도체본 발명은 본 명세서에 지시된 의미를 갖는 화학식 I의 이미다졸린 카복사미드 유도체, 이의 약제학적으로 사용가능한 염 및 약제로서의 이의 용도에 관한 것이다. 화학식 I 화학식 I의 화합물, 이의 토오토머 형태 및 이의 생리학적으로 허용되는 염. 화학식 I [이미지] 위의 화학식 I에서, X 및 Y는 동일하거나 상이하게 -C(R3)(R4)-, -(C=O)-, -(C=S)이고, 여기서 하나 이상의 X 또는 Y는 -(C=O)- 또는 -(C=S)-이지만, 둘 다 동시에 -(C=O)- 또는 -(C=S)-일 수는 없거나; X 및 Y는 함께 C(R3)=C(R3)이고; R은 수소, (C1-C8)-알킬, (C1-C5)-할로알킬, (CR5R6)m-O(R7), (C1-C3)-알킬옥시-(C1-C3)-알킬렌, 아릴, 헤테로사이클, (C1-C4)-알킬렌-아릴, (C1-C4)-알킬렌-헤테로아릴, (C1-C4)-알킬렌-(C5-C12)-사이클로알킬이고; 여기서 사이클로알킬, 아릴, 헤테로사이클 또는 헤테로아릴은 F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O-(C1-C6)-알킬, O-(C1-C4)-알콕시-(C1-C4)-알킬, S-(C1-C6)-알킬, (C1-C6)-알킬, (C2-C4)-할로알킬, O-(C2-C4)-할로알킬, (C2-C6)-알케닐, (C3-C8)-사이클로알킬, O-(C3-C8)-사이클로알킬, (C2-C6)-알키닐, (C0-C8)-알킬렌-아릴, O-(C0-C8)-알킬렌-아릴, S-아릴, (C0-C8)-알킬렌-헤테로아릴, N(R5)(R6), SO2-CH3, SO2-NH2, SF5, COOH, COO-(C1-C6)-알킬, CON(R5)(R6), N(R5)CO(R6), N(R5)SO2(R6), CO(R5), (CR5R6)m'-O(R7), O-CO-N(R5)(R6), O-CO-(C1-C6)-알킬렌-CO-O-(C1-C6)-알킬, O-CO-(C1-C6)-알킬렌-CO-OH, O-CO-(C1-C6)-알킬렌-CO-N(R5)(R6)에 의해 1회 이상 치환될 수 있고, 여기서 아릴 또는 헤테로아릴은 다시 F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O-(C1-C6)-알킬, O-(C1-C4)-알콕시-(C1-C4)-알킬, S-(C1-C6)-알킬, (C1-C6)-알킬, (C2-C6)-알케닐, (C3-C8)-사이클로알킬, O-(C3-C8)-사이클로알킬, (C2-C6)-알키닐, N(R8)(R9), SO2-CH3, SF5, COOH, COO-(C1-C6)-알킬, CON(R8)(R9), N(R8)CO(R9), N(R8)SO2(R9), CO(R8), (CR8R9)m"-O(R10), O-CO-N(R8)(R9), O-CO-(C1-C6)-알킬렌-CO-O-(C1-C6)-알킬, O-CO-(C1-C6)-알킬렌-CO-OH, O-CO-(C1-C6)-알킬렌-CO-N(R8)(R9)에 의해 1회 이상 치환될 수 있고; m, m' 및 m"은 0, 1, 2, 3, 4, 5 또는 6이고; R5, R6, R7, R8, R9 및 R10은 동일하거나 상이하게 수소, (C1-C8)-알킬, -(C=O)-NR1aR2a, -(C=O)-O-R1b이거나; X가 -C(R3)(R4)-인 경우, R 및 X는 4 내지 7원의 모노사이클릭 포화 또는 부분 불포화 환 시스템 또는 8 내지 14원의 바이사이클릭 포화 또는 부분 불포화 환 시스템을 형성할 수 있고, 상기 환 시스템의 개별적인 구성원은 일련의 -CHR11-, -CR11R12-, -(C=R11)-, =C(R11)-, -NR11-, -C(=O)-, -O-, -S-, -SO-, -SO2-로부터의 1 내지 3개의 원자 또는 원자 그룹에 의해 교체될 수 있고, 단 일련의 -O-, -S-, -SO-, -SO2- 중의 2개의 단위는 인접할 수 없으며; R11 및 R12는 동일하거나 상이하게 수소, (C1-C6)-알킬, 아릴, (C3-C12)-사이클로알킬, (C1-C4)-알킬렌-아릴, (C1-C3)-알킬렌-(C3-C12)-사이클로알킬이고; 여기서, 아릴 또는 사이클로알킬은 F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O-(C1-C6)-알킬, O-(C1-C4)-알콕시-(C1-C4)-알킬, S-(C1-C6)-알킬, (C1-C6)-알킬, (C2-C4)-할로알킬, O-(C2-C4)-할로알킬, (C2-C6)-알케닐, (C2-C6)-알키닐, N(R13)(R14), SO2-CH3, SO2-NH2, SF5, COOH, COO-(C1-C6)-알킬, CON(R13)(R14), N(R13)CO(R14), N(R13)SO2(R14), CO(R13), (CR13R14)n-O(R15), O-CO-N(R13)(R14), O-CO-(C1-C6)-알킬렌-CO-O-(C1-C6)-알킬, O-CO-(C1-C6)-알킬렌-CO-OH, O-CO-(C1-C6)-알킬렌-CO-N(R13)(R14)에 의해 치환될 수 있고; n은 0, 1, 2, 3, 4, 5 또는 6이고; R13, R14 및 R15는 동일하거나 상이하게 수소, (C1-C8)-알킬이고; R1, R1a 및 R1b는 동일하거나 상이하게 (C5-C16)-알킬, CH2-아릴, (C1-C2)-알킬렌-헤테로아릴, CH2-(C5-C12)-사이클로알킬이고; 여기서 아릴, 헤테로아릴 또는 사이클로알킬은 F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O-(C1-C6)-알킬, O-(C1-C4)-알콕시-(C1-C4)-알킬, S-(C1-C6)-알킬, (C1-C6)-알킬, (C2-C4)-할로알킬, O-(C2-C4)-할로알킬, (C2-C6)-알케닐, (C3-C8)-사이클로알킬, O-(C3-C8)-사이클로알킬, (C2-C6)-알키닐, (C0-C8)-알킬렌-아릴, O-(C0-C8)-알킬렌-아릴, S-아릴, (C0-C8)-알킬렌-헤테로아릴, N(R16)(R17), SO2-CH3, SO2-NH2, SF5, COOH, COO-(C1-C6)-알킬, CON(R16)(R17), N(R16)CO(R17), N(R16)SO2(R17), CO(R16), (CR16R17)o-O(R18), O-CO-N(R16)(R17), O-CO-(C1-C6)-알킬렌-CO-O-(C1-C6)-알킬, O-CO-(C1-C6)-알킬렌-CO-OH, O-CO-(C1-C6)-알킬렌-CO-N(R16)(R17)에 의해 1회 이상 치환될 수 있고, 여기서 아릴 또는 헤테로아릴은 다시 F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O-(C1-C6)-알킬, O-(C1-C4)-알콕시-(C1-C4)-알킬, S-(C1-C6)-알킬, (C1-C6)-알킬, (C2-C6)-알케닐, (C3-C8)-사이클로알킬, O-(C3-C8)-사이클로알킬, (C2-C6)-알키닐, N(R19)(R20), SO2-CH3, SF5, COOH, COO-(C1-C6)-알킬, CON(R19)(R20), N(R19)CO(R20), N(R19)SO2(R20), CO(R19), (CR19R20)o'-O(R21), O-CO-N(R19)(R20), O-CO-(C1-C6)-알킬렌-CO-O-(C1-C6)-알킬, O-CO-(C1-C6)-알킬렌-CO-OH, O-CO-(C1-C6)-알킬렌-CO-N(R19)(R20)에 의해 1회 이상 치환될 수 있고; o 및 o'는 0, 1, 2, 3, 4, 5 또는 6이고; R16, R17, R18, R19, R20 및 R21는 동일하거나 상이하게 수소, (C1-C8)-알킬이고; 또는 R1, R1a 및 R1b는 동일하거나 상이하게 화학식 Ia [이미지]의 라디칼이고; W는 -C(R28)(R29)-, -C(R28)(R29)-C(R28a)(R29a)- 또는 -C(R28)(R29)-O-이고; R22, R23, R24, R25, R26, R27, R28, R29, R28a 및 R29a는 동일하거나 상이하게 수소, F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, SF5, O-(C1-C6)-알킬, O-(C1-C4)-알콕시-(C1-C4)-알킬, S-(C1-C6)-알킬, (C1-C6)-알킬, (C2-C4)-할로알킬, O-(C2-C4)-할로알킬, (C2-C6)-알케닐, (C3-C8)-사이클로알킬, O-(C3-C8)-사이클로알킬, (C3-C8)-사이클로알케닐, (C2-C6)-알키닐, N(R30)(R31), SO2-CH3, COOH, COO-(C1-C6)-알킬, CON(R30)(R31), N(R30)CO(R31), N(R30)SO2(R31), CO(R30), (CR30R31)p-O(R32), O-CO-N(R30)(R31), O-CO-(C1-C6)-알킬렌-CO-O-(C1-C6)-알킬, O-CO-(C1-C6)-알킬렌-CO-OH, O-CO-(C1-C6)-알킬렌-CO-N(R30)(R31)이고; p는 0, 1, 2, 3, 4, 5 또는 6이고; R30, R31 및 R32는 동일하거나 상이하게 수소, (C1-C6)-알킬이거나; R22와 R28 또는 R23과 R29는, 이들을 함유하는 탄소 원자와 함께, 5 또는 6원의 모노사이클릭 포화, 부분 불포화 또는 방향족 환 시스템을 형성하고, 상기 환 시스템의 개별적인 구성원은 -CHR33-, -CR33R34-, =(C-R33)-에 의해 교체될 수 있거나; R24와 R26 또는 R25와 R27은, 이들을 함유하는 탄소 원자와 함께, 5 또는 6원의 모노사이클릭 포화, 부분 불포화 또는 방향족 환 시스템을 형성하고, 상기 환 시스템의 개별적인 구성원은 -CHR33-, -CR33R34-, =(C-R33)-에 의해 교체될 수 있고; R33 및 R34는 동일하거나 상이하게 F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, SF5, O-(C1-C6)-알킬, O-(C1-C4)-알콕시-(C1-C4)-알킬, S-(C1-C6)-알킬, (C1-C6)-알킬, (C2-C4)-할로알킬, O-(C2-C4)-할로알킬, (C2-C6)-알케닐, (C3-C8)-사이클로알킬, O-(C3-C8)-사이클로알킬, (C2-C6)-알키닐, N(R35)(R36), SO2-CH3, COOH, COO-(C1-C6)-알킬, CON(R35)(R36), N(R35)CO(R36), N(R35)SO2(R36), CO(R35), (CR35R36)q-O(R37), O-CO-N(R35)(R36), O-CO-(C1-C6)-알킬렌-CO-O-(C1-C6)-알킬, O-CO-(C1-C6)-알킬렌-CO-OH, O-CO-(C1-C6)-알킬렌-CO-N(R35)(R36)이고; q는 0, 1, 2, 3, ...