公开(公告)号：WO2012037258A1

公开(公告)日：2012-03-22

申请号：PCT/US2011/051603

申请日：2011-09-14

Applicant: ABBOTT LABORATORIES ,  KU, Yi-Yin ,  GRIEME, Timothy A. ,  KALLEMEYN, Jeffrey M. ,  MULHERN, Matthew M.

Inventor： KU, Yi-Yin ,  GRIEME, Timothy A. ,  KALLEMEYN, Jeffrey M. ,  MULHERN, Matthew M.

IPC: C07D237/14 ,  C07C51/00

CPC classification number: C07D237/14 ,  C07B2200/07 ,  C07C51/09 ,  C07C51/412 ,  C07C51/43 ,  C07C61/40 ,  C07C67/347 ,  C07C211/17 ,  C07C233/58 ,  C07C2601/02 ,  C07C2601/14 ,  C07D207/06 ,  C07D295/073 ,  C07D295/104 ,  C07D403/10 ,  C07C69/753

Abstract: The present invention relates to processes for preparing enantiomerically pure cyclopropyl amine derivatives and salts thereof; the chiral intermediates such as the chiral salts are useful for the preparation of such chiral compounds and salts; pharmaceutical compositions comprising the compounds and salts; and method of using such compositions. The chiral cyclopropyl amine derivatives are useful for binding to histamine H3 receptor sites and for providing therapeutic agents for histamine H3 mediated disease.

Abstract translation: 本发明涉及制备对映体纯的环丙基胺衍生物及其盐的方法; 手性中间体如手性盐可用于制备这种手性化合物和盐; 包含该化合物和盐的药物组合物; 以及使用这些组合物的方法。 手性环丙基胺衍生物可用于结合组胺H3受体位点并用于提供组胺H3介导的疾病的治疗剂。

公开(公告)号：WO2004024707A2

公开(公告)日：2004-03-25

申请号：PCT/US2003/028396

申请日：2003-09-10

Applicant: ABBOTT LABORATORIES

Inventor： KU, Yi-Yin ,  PU, Yu-Ming ,  COWART, Marlon, D. ,  GRIEME, Timothy, A. ,  GUPTA, Ashok, K. ,  PLATA, Daniel, J.

IPC: C07D307/81

CPC classification number: C07D405/04 ,  C07C253/30 ,  C07C255/53 ,  C07D307/81

Abstract: The present invention relates to processes for preparing amine substituted benzofurans, and more particularly 4-(2-{2-[(2R)-2-methyl-1-pyrrolidinyl]ethyl}-1-benzofuran-5-yl)benzonitrile, and salts thereof. Compounds prepared by the processes of the invention have demonstrated activity as histamine-3 receptor ligands.

Abstract translation: 本发明涉及制备胺取代的苯并呋喃的方法，特别是4-（2- {2 - [（2R）-2-甲基-1-吡咯烷基]乙基} -1-苯并呋喃-5-基）苄腈，和 的盐。 通过本发明方法制备的化合物已经证明作为组胺-3受体配体的活性。

公开(公告)号：WO2004037240A1

公开(公告)日：2004-05-06

申请号：PCT/US2003/033688

申请日：2003-10-22

Applicant: ABBOTT LABORATORIES

Inventor： BENNANI, Youssef, L. ,  BUNNELLE, William, H. ,  CHANG, Sou-Jen ,  CHEMBURKAR, Sanjay, R. ,  CHEN, Jinhua ,  DART, Michael, J. ,  FERNANADO, Dilinie, P. ,  KU, Yi-Yin ,  LOCKWOOD, Mark ,  WANG, Lei

IPC: A61K31/16

CPC classification number: C07C69/753 ,  C07C61/13 ,  C07C61/135 ,  C07C233/58 ,  C07C233/60 ,  C07C233/63 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/10 ,  C07C2602/20 ,  C07C2602/42 ,  C07C2603/95

Abstract: The present invention relates to the use of compounds of Formula (I) for the treatment of epilepsy, bipolar disorder, psychiatric disorders, migraine, pain, or movement disorders, and to provide neuroprotection.

Abstract translation: 本发明涉及式（I）化合物用于治疗癫痫，双相情感障碍，精神障碍，偏头痛，疼痛或运动障碍的用途，并提供神经保护作用。

公开(公告)号：WO1997036913A1

公开(公告)日：1997-10-09

申请号：PCT/US1997001955

申请日：1997-02-06

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  KU, Yi-Yin

IPC: C07H17/08

CPC classification number: C07H17/08

Abstract: A process of preparing 6-O-alkylerythromycin A using 9-oximesilyl erythromycin A derivatives is provided. 9-Oximesilyl- and 6-O-alkylerythromycin A derivatives used in the preparation of 6-O-alkylerythromycin A are also provided.

Abstract translation: 提供了使用9-肟基红霉素A衍生物制备6-O-烷基红霉素A的方法。 还提供了用于制备6-O-烷基红霉素A的9-氧化肟基和6-O-烷基红霉素A衍生物。

公开(公告)号：WO2011075525A1

公开(公告)日：2011-06-23

申请号：PCT/US2010/060499

申请日：2010-12-15

Applicant: ABBOTT LABORATORIES ,  PU, Yu-Ming ,  CHRISTESEN, Alan ,  CULLEN, Steven ,  KU, Yi-Yin

Inventor： PU, Yu-Ming ,  CHRISTESEN, Alan ,  CULLEN, Steven ,  KU, Yi-Yin

IPC: C07D513/04 ,  A61K31/429 ,  A61P25/04

CPC classification number: C07D513/04

Abstract: A process for the preparation of compounds of formula (I) or a salt thereof wherein X 1 , X 2 , X 3 , X 4 , R x , u, R 2, R 1g , z, and A 1 are as defined in the specification is disclosed.

Abstract translation: 公开了制备式（I）化合物或其盐的方法，其中X1，X2，X3，X4，Rx，u，R2，R1g，z和A1如说明书中所定义。

公开(公告)号：WO2004076388A3

公开(公告)日：2004-09-10

申请号：PCT/US2004/005573

申请日：2004-02-25

Applicant: ABBOTT LABORATORIES

Inventor： KU, Yi-Yin ,  COWART, Marlon, D. ,  SHARMA, Padam, N.

IPC: C07D207/08

Abstract: The invention relates to a process according to scheme for preparing 2-methylpyrrolidine and, more particularly, specific enantiomers of 2-methylpyrrolidine. The corresponding 2-Iodomethylderivatives intermediates also are described. Scheme 1 (I)

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

Applicant: ABBOTT LABORATORIES

Inventor： 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: A61K31/40

CPC classification number: 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

Abstract: 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).

Abstract translation: 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。

公开(公告)号：WO2003027117A1

公开(公告)日：2003-04-03

申请号：PCT/US2002/028864

申请日：2002-09-11

Applicant: ABBOTT LABORATORIES

Inventor： KU, Yi-Yin ,  GRIEME, Timothy, A. ,  SHARMA, Padam, N. ,  RAJE, Prasad, S. ,  FITZGERALD, Mike, A. ,  MORTON, Howard, E.

IPC: C07D491/04

CPC classification number: C07D491/04

Abstract: The present invention relates to an efficient process for the preparation of 5-(substituted)-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-chromeno[3,4-f]quinolines.

Abstract translation: 本发明涉及制备5-（取代的）-10-甲氧基-2,2,4-三甲基-2,5-二氢-1H-色烯并[3,4-f]喹啉的有效方法。

公开(公告)号：WO2003002548A1

公开(公告)日：2003-01-09

申请号：PCT/US2002/019115

申请日：2002-06-11

Applicant: ABBOTT LABORATORIES

Inventor： KU, Yi-Yin ,  GRIEME, Tim ,  MORTON, Howard, E. ,  KING, Steven, A.

IPC: C07D311/80

CPC classification number: C07D491/04 ,  C07D215/14

Abstract: The present invention relates to the preparation of chiral glucocorticoid receptor agents via biaryl atropisomers.

Abstract translation: 本发明涉及通过联芳基阻转异构体制备手性糖皮质激素受体剂。

公开(公告)号：WO1995012589A1

公开(公告)日：1995-05-11

申请号：PCT/US1994012062

申请日：1994-10-21

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  RATAJCZYK, James, D. ,  CHEMBURKAR, San jay, R. ,  KU, Yi-Yin ,  PATEL, Ramesh, R. ,  BUSSE, Juliette, K. ,  DICKMAN, Daniel, A. ,  PATEL, Hemantkumar, H. ,  SAWICK, David, P.

IPC: C07D333/20

CPC classification number: C07D333/20 ,  C07D307/52

Abstract: A process for preparing a compound of structure (I), where A is oxygen and sulfur and R is selected from the group consisting of hydrogen, halogen, alkyl of one to six carbon atoms, alkoxy of one to six carbon atoms, and trifluoromethyl, and R is alkyl of one to four carbon atoms, comprising coupling a compound of formula (II), where X is bromine or iodine, with an N-hydroxyurea compound of formula (III), in the presence of a palladium catalyst. The compounds of formula (I) are inhibitors of the enzyme 5-lipoxygenase and are thus useful as therapeutic agents for the treatment of allergic and inflammatory disease conditions.

Abstract translation: 制备式（I）化合物的方法，其中A是氧和硫，R 1选自氢，卤素，1至6个碳原子的烷基，1至6个碳原子的烷氧基， 和三氟甲基，R 2是1-4个碳原子的烷基，包括式（II）化合物（其中X是溴或碘）与式（III）的N-羟基脲化合物在式 钯催化剂。 式（I）化合物是5-脂氧合酶的抑制剂，因此可用作治疗过敏性和炎性疾病病症的治疗剂。