公开(公告)号：WO2011003418A1

公开(公告)日：2011-01-13

申请号：PCT/DK2010/000105

申请日：2010-07-08

Applicant: LEO PHARMA A/S ,  NIELSEN, Simon Feldbæk ,  GREVE, Daniel, Rodriguez ,  RYTTERSGAARD, Carsten ,  GRUE-SØRENSEN, Gunnar ,  OTTOSEN, Erik, Rytter ,  POULSEN, Tina, Dahlerup ,  SCHOU, Søren, Christian ,  MURRAY, Anthony

Inventor： NIELSEN, Simon Feldbæk ,  GREVE, Daniel, Rodriguez ,  RYTTERSGAARD, Carsten ,  GRUE-SØRENSEN, Gunnar ,  OTTOSEN, Erik, Rytter ,  POULSEN, Tina, Dahlerup ,  SCHOU, Søren, Christian ,  MURRAY, Anthony

IPC: C07D487/04 ,  C07D487/08 ,  C07D471/04 ,  A61K31/437 ,  A61K31/499 ,  A61K31/519 ,  A61P3/00 ,  A61P17/00 ,  A61P27/00 ,  A61P25/00 ,  A61P35/00 ,  A61P37/00

CPC classification number: C07D487/04 ,  C07D471/04 ,  C07D519/00

Abstract: The invention relates to compounds of general formula (I) wherein A, R 1 , R 2 , R 3 , R 4 , R 5 , R 9 , m and n are defined as defined herein, and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use -alone or in combination with one or more other pharmaceutically active compounds- in therapy, as JAK kinase and protein tyrosine kinase inhibitors for preventing, treating or ameliorating diseases and complications thereof, including, for example, psoriasis, atopic dermatitis, rosacea, lupus, multiple sclerosis, rheumatoid arthritis, Type I diabetes, asthma, cancer, autoimmune thyroid disorders, ulcerative colitis, Crohn's disesase, Alzheimer's disease, leukaemia, eye diseases such as diabetic retinopathy and macular degeneration as well as other autoimmune diseases and indications where immunosuppression would be desirable for example in organ transplantation.

Abstract translation: 本发明涉及通式（I）的化合物，其中A，R 1，R 2，R 3，R 4，R 5，R 9，m和n如本文所定义，及其药学上可接受的盐，水合物或溶剂化物， 或与治疗中的一种或多种其它药学活性化合物组合用作用于预防，治疗或改善疾病及其并发症的JAK激酶和蛋白酪氨酸激酶抑制剂，包括例如牛皮癣，特应性皮炎，红斑痤疮，狼疮，多发性硬化 ，类风湿性关节炎，I型糖尿病，哮喘，癌症，自身免疫性甲状腺疾病，溃疡性结肠炎，克罗恩病，阿尔茨海默氏病，白血病，眼睛疾病如糖尿病性视网膜病变和黄斑变性以及其他自身免疫疾病和适应症，其中需要免疫抑制 器官移植的例子。

公开(公告)号：WO2012003829A1

公开(公告)日：2012-01-12

申请号：PCT/DK2011/000080

申请日：2011-07-08

Applicant: LEO PHARMA A/S ,  NIELSEN, Simon, Feldbæk ,  GREVE, Daniel, Rodriguez ,  GRUE-SØRENSEN, Gunnar ,  RYTTERSGAARD, Carsten ,  SCHOU, Søren, Christian ,  SAMS, Anette, Graven

Inventor： NIELSEN, Simon, Feldbæk ,  GREVE, Daniel, Rodriguez ,  GRUE-SØRENSEN, Gunnar ,  RYTTERSGAARD, Carsten ,  SCHOU, Søren, Christian ,  SAMS, Anette, Graven

IPC: C07D487/04 ,  A61K31/519 ,  A61P29/00 ,  A61P37/02

CPC classification number: C07D487/04 ,  A61K31/5513 ,  A61K45/00

Abstract: The invention relates to compounds of general formula (I) wherein R 1 ,R 2 , R 3 , R 4 , m and n are defined as defined herein, and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use -alone or in combination with one or more other pharmaceutically active compounds- in therapy, as JAK kinase and protein tyrosine kinase inhibitors for preventing, treating or ameliorating diseases and complications thereof, including, for example, psoriasis, atopic dermatitis, rosacea, lupus, multiple sclerosis, rheumatoid arthritis, Type I diabetes, asthma, cancer, autoimmune thyroid disorders, ulcerative colitis, Crohn's disesase, Alzheimer's disease, leukaemia, eye diseases such as diabetic retinopathy and macular degeneration as well as other autoimmune diseases and indications where immunosuppression would be desirable for example in organ transplantation.

Abstract translation: 本发明涉及通式（I）的化合物，其中R 1，R 2，R 3，R 4，m和n如本文所定义，以及其药学上可接受的盐，水合物或溶剂合物，可单独使用或与一种或多种 更多其他药物活性化合物 - 在治疗中，作为用于预防，治疗或改善疾病及其并发症的JAK激酶和蛋白酪氨酸激酶抑制剂，包括例如牛皮癣，特应性皮炎，酒渣鼻，狼疮，多发性硬化，类风湿性关节炎，I型 糖尿病，哮喘，癌症，自身免疫性甲状腺疾病，溃疡性结肠炎，克罗恩病，阿尔茨海默病，白血病，眼睛疾病如糖尿病性视网膜病变和黄斑变性以及其他自身免疫性疾病以及例如在器官移植中需要免疫抑制的适应症。

公开(公告)号：WO2004056988A2

公开(公告)日：2004-07-08

申请号：PCT/DK2003/000851

申请日：2003-12-11

Applicant: NOVOZYMES A/S ,  DE MARIA, Leonardo ,  SVENDSEN, Allan ,  BORCHERT, Torben, Vedel ,  CHRISTENSEN, Lars, Lehmann, Hylling ,  LARSEN, Sine ,  RYTTERSGAARD, Carsten

Inventor： DE MARIA, Leonardo ,  SVENDSEN, Allan ,  BORCHERT, Torben, Vedel ,  CHRISTENSEN, Lars, Lehmann, Hylling ,  LARSEN, Sine ,  RYTTERSGAARD, Carsten

IPC: C12N9/38

CPC classification number: C12N9/2468 ,  C12Y302/01089

Abstract: Variants of Glycoside Hydrolase family 53 galactanases, e.g. variants of the galactanasesfrom strains of Yersinia, Aspergillus, Humicola, Meripilus, Myceliophthora, Thermomyces, Bacillus, Bifidobacterium, Cellvibrio, Clostridium, Pseudomonas, Thermotoga, or Xanthomonas.

Abstract translation: 糖苷水解酶家族53半乳聚糖酶的变体，例如， 来自耶尔森氏菌，曲霉菌，腐质霉属，麦角菌属，Myceliophthora，Thermomyces，芽孢杆菌属，双歧杆菌属，纤维弧菌属，梭菌属，假单胞菌属，Thermotoga或黄单胞菌属的菌株的半乳聚糖酶变体。

公开(公告)号：WO2004056988A3

公开(公告)日：2004-08-12

申请号：PCT/DK0300851

申请日：2003-12-11

Applicant: NOVOZYMES AS ,  MARIA LEONARDO DE ,  SVENDSEN ALLAN ,  BORCHERT TORBEN VEDEL ,  CHRISTENSEN LARS LEHMANN HYLLI ,  LARSEN SINE ,  RYTTERSGAARD CARSTEN

Inventor： DE MARIA LEONARDO ,  SVENDSEN ALLAN ,  BORCHERT TORBEN VEDEL ,  CHRISTENSEN LARS LEHMANN HYLLI ,  LARSEN SINE ,  RYTTERSGAARD CARSTEN

IPC: C12N9/38

CPC classification number: C12N9/2468 ,  C12Y302/01089

Abstract: Variants of Glycoside hydrolase family 53 galactanases having an ateration in at least one position out of a large number of positions. The variants may be used in the dairy industry, for preparation of galacto-oligo-saccharides or for hydrolysis of lactose, and may be derived from strains of Yersinia, Aspergillus, Humicola, Meripilus, Myceliophthora, Thermomyces, Bacillus, Bifidobacterium, Cellvibrio, Clostridium, Pseudomonas, Thermotoga, or Xanthomonas.

Abstract translation: 糖苷水解酶家族的53个半乳聚糖酶在大量位置上具有至少一个位置的位置。 这些变体可以用于乳制品工业，用于制备低聚半乳糖或用于水解乳糖，并且可以衍生自耶尔森氏菌，曲霉属，腐质霉属，Meripilus，Myceliophthora，Thermomyces，Bacillus，Bifidobacterium，Cellvibrio，Clostridium ，假单胞菌属，热氧化酵母或黄单胞菌属。