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1. 发明申请

WO2007100990A3 OCTAHYDRO-PYRROLO[3,4-B] PYRROLE DERIVATIVES AND THEIR USE AS HISTAMINE-3 RECEPTOR LIGANDS 审中-公开
公开(公告)号：WO2007100990A3
公开(公告)日：2007-09-07
申请号：PCT/US2007/062329
申请日：2007-02-16
申请人： ABBOTT LABORATORIES , COWART, Marlon, D. , ZHAO, Chen , SUN, Minghua , BLACK, Lawrence, A. , ZHENG, Guo Zhu , GREGG, Robert, J. , ZHANG, Geoff, G.Z. , SHEIKH, Ahmad, Y. , LOU, Xiaochun , HENRY, Rodger, F. , BARNES, David, M. , KOLACZKOWSKI, Lawrence , HAIGHT, Anthony, R. , CHANG, Sou-Jen , WITTENBERGER, Steven, J. , FICKES, Michael, G.
发明人： COWART, Marlon, D. , ZHAO, Chen , SUN, Minghua , BLACK, Lawrence, A. , ZHENG, Guo Zhu , GREGG, Robert, J. , ZHANG, Geoff, G.Z. , SHEIKH, Ahmad, Y. , LOU, Xiaochun , HENRY, Rodger, F. , BARNES, David, M. , KOLACZKOWSKI, Lawrence , HAIGHT, Anthony, R. , CHANG, Sou-Jen , WITTENBERGER, Steven, J. , FICKES, Michael, G.
IPC分类号： C07D487/04 , A61K31/407
摘要： Octahydro-pyrrolo[3,4-b]pyrrole derivatives or a pharmaceutically acceptable salt, ester, amide, prodrug, or radiolabeled form thereof, wherein R 1 is alkyl, C 3 -C 5 cycloalkyl. or (C 3 -C 5 cycloalkyl)methyl; R 2a , R 2b , R 2c , R 2d , R 2e , and R 2f each are independently hydrogen, methyl, or fluoromethyl; R 3a , R 3b , R 3c , and R 3d each are independently hydrogen, alkyl, fluoroalkyl, fluoroalkoxy, alkoxy, thioalkoxy, halogen, or nitrile, with the proviso that when one or more of R 3a , R 3b , R 3c , and R 3d are alkyl, then at least one of R 3a , R 3b , R 3c , and R 3d is fluoroalkyl, fluoroalkoxy, alkoxy, thioalkoxy, halogen, or nitrile; L 1 is a bond, oxygen, sulfur, carbonyl, alkylene,. alkylcarbonyl, alkylamino, -C(=N-Oalkyl)-, NR 4 , -C(=O) NR 4 -, or -NR4C(=O)-; R 4 is hydrogen or alkyl; Cy 1 is aryl, cycloalkyl, cycloalkenyl, heteroaryl, or heterocycle; Z is a substituent R 6 or a group represented by -L 3 -Cy 3 ; R 6 is hydrogen, acyl, acyloxy, alkenyl, alkoxy, alkoxyalkoxy, alkoxyalkyl, alkoxycarbonyl, alkoxyimino, alkoxysulfonyl, alkyl, alkylcarbonyl, alkylsulfonyl, alkynyl, amido, carboxy, cyano, cycloalkyl, fiuoroalkoxy, haloalkoxy, haloalkyl, halogen, hydroxy, hydroxyalkyl, mercapto, nitro, alkylthio, amino, NHR 7 , NR 7 R 8 , -N(R 7 )C(=O)R 9 , -C(=O)NR 7 R 8 , or N(R 7 )SO 2 (R 10 ); L 3 is a bond, oxygen, sulfur, carbonyl, alkylene, alkylcarbonyl, alkylamino, -C(=N-Oalkyl)-, NR 11 , -C(=O) NR 11 -, or -NR 11 C(=O)-;Cy 3 is aryl, cycloalkyl, cycloalkenyl, heteroaryl, or heterocycle; R 7 , R 8 , R 9 , R 10 , and R 11 at each occurrence are independently hydrogen,C 1-4 alkyl, C 3 -C 4 cycloalkyl, or a (C 3 -C 4 cycloalkyl)amine; are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.

2. 发明申请

WO2009114575A1 TRICYCLIC SPIRO PYRIMIDINE DERIVATIVES AS HISTAMINE H4 LIGAND 审中-公开
标题翻译：作为HISTAMINE H4 LIGAND的三螺旋螺吡啶衍生物
公开(公告)号：WO2009114575A1
公开(公告)日：2009-09-17
申请号：PCT/US2009/036728
申请日：2009-03-11
申请人： ABBOTT LABORATORIES , LIU, Huaqing , KOENIG, John, R. , COWART, Marlon, D. , BLACK, Lawrence, A.
发明人： LIU, Huaqing , KOENIG, John, R. , COWART, Marlon, D. , BLACK, Lawrence, A.
IPC分类号： C07D239/95 , C07D471/10 , C07D487/10 , A61K31/517 , A61P25/00
CPC分类号： C07D239/95 , C07D471/10 , C07D487/10
摘要： Macrocyclic spiro pyrimidine compounds, of formula (I) compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions, and disorders using such compounds and compositions are described herein. (I)
摘要翻译：本文描述了包含这种化合物的式（I）组合物的大环螺嘧啶化合物，制备该化合物的方法，以及使用这些化合物和组合物治疗和预防疾病进展，病症和病症的方法。（一世）

3. 发明申请

WO2005113536A2 TRI- AND BI-CYCLIC HETEROARYL HISTAMINE-3 RECEPTOR LIGANDS 审中-公开
标题翻译： TRI-和BI-CYCLIC HETEROARYL组胺3受体配体
公开(公告)号：WO2005113536A2
公开(公告)日：2005-12-01
申请号：PCT/US2005/014866
申请日：2005-04-29
申请人： ABBOTT LABORATORIES , ALTENBACH, Robert, J. , BLACK, Lawrence, A. , CHANG, Sou-jen , COWART, Marlon, D. , FAGHIH, Ramin , GFESSER, Gregory, A. , KU, Yi-yin , LIU, Huaqing , LUKIN, Kirill, A. , NERSESIAN, Diana, L. , PU, Yu-ming , CURTIS, Michael, P.
发明人： ALTENBACH, Robert, J. , BLACK, Lawrence, A. , CHANG, Sou-jen , COWART, Marlon, D. , FAGHIH, Ramin , GFESSER, Gregory, A. , KU, Yi-yin , LIU, Huaqing , LUKIN, Kirill, A. , NERSESIAN, Diana, L. , PU, Yu-ming , CURTIS, Michael, P.
IPC分类号： C07D401/00
CPC分类号： C07D401/14 , C07D405/14 , C07D409/14 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , C07D513/04
摘要： Compounds of formula (I) wherein R 1 or R 2 is a tricyclic or bicyclic ring, each of which contains at least two heteroatoms, and R 1 , R 2 , R 3 , R 3a , R 3b , R 4 , R 5 , L, X, X', Y, Y', Z, and Z' are as defined herein, are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
摘要翻译：式（I）化合物其中R 1或R 2是三环或双环，其各自含有至少两个杂原子，R 1，R 2，R 3，R 3a，R 3b，R 4，R 5，L，X，X'，Y， Y'，Z和Z'如本文所定义，可用于治疗由组胺-3受体配体预防或改善的病症或病症。还公开了包含组胺-3受体配体的药物组合物，使用这些化合物和组合物的方法，以及制备式（I）范围内的化合物的方法。

4. 发明申请

WO2009123967A1 5,6,7,8-TETRAHYDROQUINAZOLIN-2-AMINE DERIVATIVES AND RELATED COMPOUNDS AS HISTAMINE H4 RECEPTOR MODULATORS FOR THE TREATMENT OF ASTHMA 审中-公开
标题翻译： 5,6,7,8-四氢喹唑啉-2-胺衍生物及相关化合物作为治疗ASTHMA的HISTAMINE H4受体调节剂
公开(公告)号：WO2009123967A1
公开(公告)日：2009-10-08
申请号：PCT/US2009/038775
申请日：2009-03-30
申请人： ABBOTT LABORATORIES , LIU, Huaqing , DRIZIN, Irene , KOENIG, John, R. , COWART, Marlon, D. , ZHAO, Chen , WAKEFIELD, Brian, D. , BLACK, Lawrence, A. , ALTENBACH, Robert, J.
发明人： LIU, Huaqing , DRIZIN, Irene , KOENIG, John, R. , COWART, Marlon, D. , ZHAO, Chen , WAKEFIELD, Brian, D. , BLACK, Lawrence, A. , ALTENBACH, Robert, J.
IPC分类号： C07D239/84 , C07D403/04 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10 , A61K31/517 , A61P11/06
CPC分类号： C07D401/04 , C07D239/70 , C07D239/84 , C07D239/88 , C07D401/12 , C07D403/04 , C07D403/12 , C07D453/02 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10
摘要： Macrocyclic pyrimidine compounds, compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions, and disorders using such compounds and compositions are described herein.
摘要翻译：本文描述了大环嘧啶化合物，包含这些化合物的组合物，制备化合物的方法，以及使用这些化合物和组合物治疗和预防疾病，病症和病症进展的方法。

5. 发明申请

WO1994026264A1 (4-ALKOXYPYRAN-4-YL) SUBSTITUTED ARYLALKYLARYL-, ARYLALKENYLARYL-, AND ARYLALKYNYLARYLUREA INHIBITORS OF 5-LIPOXYGENASE 审中-公开
标题翻译：（4-ALKOXYPYRAN-4-YL）取代的芳基乙烯基-L-亚苄基胆碱酯酶和5-氯吡咯烷酮的芳基烯丙基胺抑制剂
公开(公告)号：WO1994026264A1
公开(公告)日：1994-11-24
申请号：PCT/US1994005341
申请日：1994-05-12
申请人： ABBOTT LABORATORIES
发明人： ABBOTT LABORATORIES , DELLARIA, Joseph, F. , BASHA, Anwer , BLACK, Lawrence, A. , CHERNESKY, Linda, J. , LEE, Wendy
IPC分类号： A61K31/335
CPC分类号： C07D405/12 , C07D309/12
摘要： Compounds of structure (I), wherein W is selected from (a), and (b), where Q is oxygen or sulfur, R and R are hydrogen or alkyl, or R and R , together with the nitrogen atoms to which they are attached, define a radical of formula (II) or (III), R is selected from hydrogen, alkyl, haloalkyl, optionally substituted phenyl, hydroxyalkyl, aminoalkyl, carboxyalkyl, (alkoxycarbonyl)alkyl, and (alkylaminocarbonyl)alkyl; Z is -CH2-, oxygen, sulfur, or -NR where R is hydrogen or alkyl, L and L are selected from a valence bond, alkylene, propenylene, and propynylene, R , R , R , and R are independently selected from alkyl, haloalkyl, halogen, cyano, amino, alkoxycarbonyl, and dialkylaminocarbonyl, Y is selected from oxygen, -NR , where R is hydrogen or alkyl, and (c), where n = 0, 1, or 2, and R is alkyl, inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.
摘要翻译：其中W选自（a）和（b）中的结构（I）的化合物，其中Q是氧或硫，R 6和R 7是氢或烷基，或R 6和R 6，（II）或（III）的基团，其中R 8与它们所连接的氮原子一起定义为式（II）或（III）的基团，R 8选自氢，烷基，卤代烷基，任选取代的苯基，羟基烷基，氨基烷基，羧基烷基，（烷氧基羰基）烷基和（烷基氨基羰基）烷基; Z是-CH 2 - ，氧，硫或-NR 9，其中R 9是氢或烷基，L 1和L 2选自价键，亚烷基，亚丙烯基和亚丙炔基，R R 1，R 2，R 3和R 4独立地选自烷基，卤代烷基，卤素，氰基，氨基，烷氧基羰基和二烷基氨基羰基，Y选自氧，-NR 10，其中R 10是氢或烷基，和（c）其中n = 0,1或2，R 5是烷基，抑制白细胞三烯的生物合成。这些化合物可用于治疗或改善过敏性和炎性疾病状态。

6. 发明申请

WO2005113551A1 BICYCLIC-SUBSTITUTED AMINES HAVING CYCLIC-SUBSTITUTED MONOCYCLIC SUBSTITUENTS 审中-公开
标题翻译：具有循环取代的单环取代基的双环取代的氨基
公开(公告)号：WO2005113551A1
公开(公告)日：2005-12-01
申请号：PCT/US2005/014863
申请日：2005-04-29
申请人： ABBOTT LABORATORIES , ALTENBACH, Robert, J. , BLACK, Lawrence, A. , CHANG, Sou-jen , COWART, Marlon, D. , FAGHIH, Ramin , GFESSER, Gregory, A. , KU, Yi-yin , LIU, Huaqing , LUKIN, Kirill, A. , NERSESIAN, Diana, L. , PU, Yu-ming , CURTIS, Michael, P.
发明人： ALTENBACH, Robert, J. , BLACK, Lawrence, A. , CHANG, Sou-jen , COWART, Marlon, D. , FAGHIH, Ramin , GFESSER, Gregory, A. , KU, Yi-yin , LIU, Huaqing , LUKIN, Kirill, A. , NERSESIAN, Diana, L. , PU, Yu-ming , CURTIS, Michael, P.
IPC分类号： C07D417/14
CPC分类号： C07D215/12 , C07D401/04 , C07D401/08 , C07D401/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14
摘要： Compounds of formula (I) wherein R 1 or R 2 is an aromatic or non-aromatic ring directly joined or joined by a linker, as represented by L 2 and L 3 , to a heteroaromatic core, and X, X', Y, Y', Z, Z', R 1 , R 2 , R 3 , R 3a , R 3b , R 4 , R 5 , L, L 2 , and L 3 are as defined herein, are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
摘要翻译：式（I）的化合物，其中R 1或R 2是通过由L 2和L 3表示的连接基直接连接或连接到杂芳族核心上的芳族或非芳族环，X，X'，Y，Y'，Z ，Z'，R1，R2，R3，R3a，R3b，R4，R5，L，L2和L3如本文所定义，可用于治疗组胺3受体配体预防或改善的病症或病症。还公开了包含组胺-3受体配体的药物组合物，使用这些化合物和组合物的方法，以及制备式（I）范围内的化合物的方法。

7. 发明申请

WO2004043458A1 BICYCLIC-SUBSTITUTED AMINES AS HISTAMINE-3 RECEPTOR LIGANDS 审中-公开
标题翻译：作为组胺-3受体配体的双相取代的氨基酸
公开(公告)号：WO2004043458A1
公开(公告)日：2004-05-27
申请号：PCT/US2003/035365
申请日：2003-11-05
申请人： ABBOTT LABORATORIES
发明人： ALTENBACH, Robert, J. , BLACK, Lawrence, A. , CHANG, Sou-Jen , COWART, Marlon, D. , FAGHIH, Ramin , GFESSER, Gregory, A. , KU, Yi-Yin , LIU, Huaqing , LUKIN, Kirill, A. , NERSESIAN, Diana, L. , PU, Yu-ming , SHARMA, Padam, N. , BENNANI, Youssef, L. , CURTIS, Michael, P.
IPC分类号： A61K31/40
CPC分类号： C07C255/58 , C07D207/08 , C07D207/12 , C07D207/14 , C07D207/20 , C07D213/30 , C07D213/38 , C07D213/61 , C07D213/64 , C07D213/85 , C07D215/12 , C07D215/14 , C07D215/20 , C07D217/14 , C07D237/12 , C07D237/14 , C07D237/28 , C07D239/26 , C07D239/28 , C07D239/42 , C07D239/52 , C07D241/12 , C07D241/42 , C07D263/32 , C07D277/28 , C07D295/073 , C07D295/088 , C07D295/096 , C07D295/112 , C07D295/135 , C07D295/155 , C07D401/04 , C07D401/10 , C07D403/04 , C07D403/10 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D471/04
摘要： Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
摘要翻译：式（I）化合物可用于治疗由组胺-3受体配体预防或改善的病症或病症。还公开了包含组胺-3受体配体的药物组合物，使用这些化合物和组合物的方法，以及制备式（I）范围内的化合物的方法。

8. 发明申请

WO2002074758A2 NOVEL AMINES AS HISTAMINE-3 RECEPTOR LIGANDS AND THEIR THERAPEUTIC APPLICATIONS 审中-公开
标题翻译：作为组胺-3受体配体的新型氨基酸及其治疗应用
公开(公告)号：WO2002074758A2
公开(公告)日：2002-09-26
申请号：PCT/US2002/007107
申请日：2002-03-11
申请人： ABBOTT LABORATORIES
发明人： COWART, Marlon, D. , BENNANI, Youssef, L. , FAGHIH, Ramin , GFESSER, Gregory, A. , BLACK, Lawrence, A.
IPC分类号： C07D307/79
CPC分类号： C07D307/79 , C07D231/12 , C07D233/56 , C07D249/08 , C07D307/81 , C07D333/54 , C07D405/04 , C07D405/06 , C07D407/04 , C07D409/04 , C07D409/10 , C07D413/04 , C07D417/04 , C07D491/08 , C07D491/10
摘要： Compounds of formula (I), or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof, which are useful for the modulation of the histamine-3 receptors in mammals and which are useful for the treatment of disorders ameliorated by histamine-3 receptor ligands.
摘要翻译：式（I）化合物或其药学上可接受的盐，酯，酰胺或前药，其可用于调节哺乳动物中组胺3受体，并且其可用于治疗组胺3受体改善的疾病配体。

9. 发明申请

WO1994005638A1 TRANS 1,4-DIETHER CYCLOHEXANE INHIBITORS OF 5-LIPOXYGENASE 审中-公开
标题翻译： 5-LIPOXYGENASE的转化1,4-二环胞嘧啶抑制剂
公开(公告)号：WO1994005638A1
公开(公告)日：1994-03-17
申请号：PCT/US1993008036
申请日：1993-08-25
申请人： ABBOTT LABORATORIES
发明人： ABBOTT LABORATORIES , DELLARIA, Joseph, F. , BLACK, Lawrence, A. , BROOKS, Dee, W.
IPC分类号： C07D215/22
CPC分类号： C07D213/30 , C07C43/21 , C07C43/225 , C07C43/23 , C07C43/315 , C07C45/511 , C07C45/59 , C07C49/753 , C07C2601/14 , C07D215/14 , C07D215/227 , C07D233/64 , C07D235/26 , C07D239/26 , C07D265/36 , C07D277/24 , C07D307/42 , C07D307/80 , C07D333/16 , C07D333/56
摘要： Compounds having structure (I) where Ar is carbocyclic or heterocyclic aryl; A is propynyl or methylene; X is oxygen, sulfur, sulfonyl, or NH; Y is hydrogen, alkyl of from one to six carbon atoms, haloalkyl of from one to six carbon atoms, alkoxy of from one to six carbon atoms, or halogen; R1 is alkyl of from one to four carbon atoms; R2 and R3 are hydrogen or alkyl of from one to four carbon atom; R4 is hydroxyl or -OR1 where R1 is as defined above; and R5 is hydrogen or alkyl of from one to four carbon atoms; are inhibitors of leukotriene biosynthesis and are useful in the treatment of inflammatory and allergic disease states.
摘要翻译：具有结构（I）的化合物，其中Ar是碳环或杂环芳基; A是丙炔基或亚甲基; X是氧，硫，磺酰基或NH; Y是氢，1至6个碳原子的烷基，1至6个碳原子的卤代烷基，1至6个碳原子的烷氧基或卤素; R1是1-4个碳原子的烷基; R2和R3是氢或1-4个碳原子的烷基; R4是羟基或-OR1，其中R1如上定义; 和R5是氢或1-4个碳原子的烷基; 是白三烯生物合成的抑制剂，可用于治疗炎症和过敏性疾病状态。

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