公开(公告)号：WO2009066152A3

公开(公告)日：2009-12-30

申请号：PCT/IB2008003124

申请日：2008-11-19

Applicant: PHARMAXIS LTD ,  MCDONALD IAN ALEXANDER ,  TURNER CRAIG IVAN ,  DEODHAR MANDAR ,  FOOT JONATHAN STUART

Inventor： MCDONALD IAN ALEXANDER ,  TURNER CRAIG IVAN ,  DEODHAR MANDAR ,  FOOT JONATHAN STUART

IPC: A01N33/02

CPC classification number: C07C217/46 ,  C07C235/46 ,  C07C235/54 ,  C07C235/56 ,  C07C255/54 ,  C07C311/29 ,  C07C317/22 ,  C07C323/27 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2603/74 ,  C07D209/88 ,  C07D231/12 ,  C07D277/24 ,  C07D277/64 ,  C07D277/66 ,  C07D295/26

Abstract: The present invention is related to the preparation and pharmaceutical use of novel haloallylamine derivatives as SSAO/VAP-1 inhibitors having the structure of Formula I, as defined in the specification:(I). The invention also relates to methods of using invention compounds, or pharmaceutically acceptable salt or derivatives thereof, for the treatment of a variety of indications, e.g., inflammatory diseases.

Abstract translation: 本发明涉及如说明书：（I）中所定义的具有式I结构的新型卤代烯丙胺衍生物作为SSAO / VAP-1抑制剂的制备和药物用途。 本发明还涉及使用本发明化合物或其药学上可接受的盐或衍生物治疗多种适应症例如炎性疾病的方法。

公开(公告)号：WO2010125445A1

公开(公告)日：2010-11-04

申请号：PCT/IB2010/000960

申请日：2010-04-28

Applicant: PHARMAXIS PTY LTD. ,  ROBERTSON, Alan, D. ,  SILVA, Diego ,  MCDONALD, Ian, Alexander

Inventor： ROBERTSON, Alan, D. ,  SILVA, Diego ,  MCDONALD, Ian, Alexander

IPC: A61K31/665 ,  A61P17/02 ,  A61P11/00 ,  A61P27/02 ,  A61P29/00

CPC classification number: A61K31/665

Abstract: Methods of using phosphotetrahydropyran compounds for treatment of fibrotic and scarring disorders, e.g. pulmonary fibrosis, fibrosis associated with surgical procedures, wound healing disorders, scar formation, sclerotic disorders, ocular fibrotic disorders, ocular healing disorders, ocular fibrosis after surgery, glaucoma, tendon scarring disorders, joint scarring disorders, kidney interstitial fibrosis and glomerular fibrosis and tubular fibrosis of the kidney.

Abstract translation: 使用磷酸四氢吡喃化合物治疗纤维化和瘢痕障碍的方法，例如 肺纤维化，与外科手术相关的纤维化，伤口愈合障碍，瘢痕形成，硬化性疾病，眼部纤维化病症，眼部愈合障碍，手术后眼部纤维化，青光眼，腱瘢痕障碍，关节瘢痕形成障碍，肾间质性纤维化和肾小球纤维化和肾小管 肾纤维化。

公开(公告)号：WO9620725A3

公开(公告)日：1996-10-17

申请号：PCT/US9600360

申请日：1996-01-05

Applicant: SALK INST BIOTECH IND ,  MUNOZ BENITO ,  MCDONALD IAN ALEXANDER ,  ALBRECHT ELISABETH

Inventor： MUNOZ BENITO ,  MCDONALD IAN ALEXANDER ,  ALBRECHT ELISABETH

IPC: A61K38/00 ,  C07C237/22 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/078 ,  C07K5/083 ,  A61K38/55

CPC classification number: C07K5/0808 ,  A61K38/00 ,  C07C237/22 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/06043 ,  C07K5/06078 ,  C07K5/06165 ,  C07K5/06191

Abstract: Methods of use of compounds and compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided. Among the compounds are those of formulae (I), (II) and (III), in which R1 is preferably 2-methyl propene, 2-butene, norleucine; R2, R4, and R8 are each independently methyl or ethyl; R3 is preferably iso-butyl or phenyl; R5 is preferably iso-butyl; R6 is H or methyl; R7 - (Q)n is preferably benzyloxycarbonyl or acetyl; Q is preferably -C(O)-; RB is preferably iso-butyl; RA = -(T)m-(D)m-R1, in which T is preferably oxygen or carbon, and D is preferably a mono-unsaturated C3-4 alkenyl; and X is an alcohol, particularly a secondary alcohol.

公开(公告)号：WO1996020949A1

公开(公告)日：1996-07-11

申请号：PCT/US1996000359

申请日：1996-01-05

Applicant: THE SALK INSTITUTE BIOTECHNOLOGY/INDUSTRIAL ASSOCIATES, INC. ,  MCDONALD, Ian, Alexander ,  ALBRECHT, Elisabeth ,  MUNOZ, Benito ,  ROWE, Blake, Alan ,  SIEGEL, Robert, Steven ,  WAGNER, Steven, Lee

Inventor： THE SALK INSTITUTE BIOTECHNOLOGY/INDUSTRIAL ASSOCIATES, INC.

IPC: C07K05/06

CPC classification number: C07K5/0808 ,  A61K38/00 ,  C07C237/22 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/06043 ,  C07K5/06078 ,  C07K5/06139 ,  C07K5/06165 ,  C07K5/06191

Abstract: Methods of use of compounds and compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided. Among the compounds are those of formulae (I) and (II), in which R1 is preferably 2-methyl propene, 2-butene, cyclohexyl or cyclohexylmethyl; R2, R4, and R8 are each independently methyl or ethyl; R3 is preferably iso-butyl or phenyl; R5 is preferably iso-butyl; R6 is H or methyl; R7 - (Q)n is preferably benzyloxycarbonyl or acetyl; Q is preferably -C(O)-; RB is preferably iso-butyl; RA = -(T)m-(D)m-R1, in which T is preferably oxygen or carbon, and D is preferably a mono-unsaturated C3-4 alkenyl; and X is preferably a alpha -ketoester or alpha -ketoamide or aldehyde.

Abstract translation: 提供了化合物和化合物用于治疗以沉淀淀粉样蛋白为特征的疾病的方法。 其中R 1优选为2-甲基丙烯，2-丁烯，环己基或环己基甲基;式（I）和（II） R2，R4和R8各自独立地是甲基或乙基; R3优选为异丁基或苯基; R5优选为异丁基; R6是H或甲基; R 7 - （Q）n优选为苄氧基羰基或乙酰基; Q优选为-C（O） - ; RB优选为异丁基; RA = - （T）m-（D）m -R 1，其中T优选为氧或碳，D优选为单不饱和C 3-4烯基; X优选为α-酮酯或α-酮酰胺或醛。

公开(公告)号：WO1996020725A2

公开(公告)日：1996-07-11

申请号：PCT/US1996000360

申请日：1996-01-05

Applicant: THE SALK INSTITUTE BIOTECHNOLOGY/INDUSTRIAL ASSOCIATES, INC. ,  MUNOZ, Benito ,  MCDONALD, Ian, Alexander ,  ALBRECHT, Elisabeth

Inventor： THE SALK INSTITUTE BIOTECHNOLOGY/INDUSTRIAL ASSOCIATES, INC.

IPC: A61K38/55

CPC classification number: C07K5/0808 ,  A61K38/00 ,  C07C237/22 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/06043 ,  C07K5/06078 ,  C07K5/06165 ,  C07K5/06191

Abstract: Methods of use of compounds and compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided. Among the compounds are those of formulae (I), (II) and (III), in which R1 is preferably 2-methyl propene, 2-butene, norleucine; R2, R4, and R8 are each independently methyl or ethyl; R3 is preferably iso-butyl or phenyl; R5 is preferably iso-butyl; R6 is H or methyl; R7 - (Q)n is preferably benzyloxycarbonyl or acetyl; Q is preferably -C(O)-; RB is preferably iso-butyl; RA = -(T)m-(D)m-R1, in which T is preferably oxygen or carbon, and D is preferably a mono-unsaturated C3-4 alkenyl; and X is an alcohol, particularly a secondary alcohol.

Abstract translation: 提供了化合物和化合物用于治疗以淀粉样蛋白沉积为特征的疾病的方法。 其中R 1优选为2-甲基丙烯，2-丁烯，正亮氨酸;式（I），（II）和（III） R2，R4和R8各自独立地为甲基或乙基; R3优选为异丁基或苯基; R5优选为异丁基; R6是H或甲基; R 7 - （Q）n优选为苄氧基羰基或乙酰基; Q优选为-C（O） - ; RB优选为异丁基; RA = - （T）m-（D）m -R1，其中T优选为氧或碳，D优选为单不饱和C 3-4烯基; X是醇，特别是仲醇。

公开(公告)号：WO2009066152A2

公开(公告)日：2009-05-28

申请号：PCT/IB2008/003124

申请日：2008-11-19

Applicant: PHARMAXIS LTD. ,  MCDONALD, Ian, Alexander ,  TURNER, Craig, Ivan ,  DEODHAR, Mandar ,  FOOT, Jonathan, Stuart

Inventor： MCDONALD, Ian, Alexander ,  TURNER, Craig, Ivan ,  DEODHAR, Mandar ,  FOOT, Jonathan, Stuart

IPC: A61K31/55

CPC classification number: C07C217/46 ,  C07C235/46 ,  C07C235/54 ,  C07C235/56 ,  C07C255/54 ,  C07C311/29 ,  C07C317/22 ,  C07C323/27 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2603/74 ,  C07D209/88 ,  C07D231/12 ,  C07D277/24 ,  C07D277/64 ,  C07D277/66 ,  C07D295/26

Abstract: The present invention is related to the preparation and pharmaceutical use of novel haloallylamine derivatives as SSAO/VAP-1 inhibitors having the structure of Formula I, as defined in the specification:(I). The invention also relates to methods of using invention compounds, or pharmaceutically acceptable salt or derivatives thereof, for the treatment of a variety of indications, e.g., inflammatory diseases.

Abstract translation: 本发明涉及新型卤代烯丙胺衍生物作为具有式I结构的SSAO / VAP-1抑制剂的制备和药物用途，如说明书（I）中所定义。 本发明还涉及使用本发明化合物或其药学上可接受的盐或衍生物用于治疗各种适应症例如炎性疾病的方法。