公开(公告)号：WO2002102250A1

公开(公告)日：2002-12-27

申请号：PCT/US2000/029181

申请日：2000-10-20

申请人： GLAXO GROUP LIMITED ,  MACLEAN, Derek ,  STAR-LACK, Joshua, M.

发明人： MACLEAN, Derek ,  STAR-LACK, Joshua, M.

IPC分类号： A61B6/00

CPC分类号： A61K51/04 ,  A61B6/508 ,  C07B2200/11 ,  C07C237/22 ,  C07C303/40 ,  C07C311/51 ,  C07C2601/14 ,  C40B30/04 ,  G01N33/5005 ,  G01N33/532 ,  G01N33/54353 ,  G01N33/54373 ,  G01N33/58 ,  G01N33/6842 ,  G01N33/6845 ,  Y02P20/582 ,  C07C311/16 ,  C07C311/29

摘要： A positron emission tomography (PET)-ready library of candidate pharmaceutical agents is provided which can be prepared by a multistep process wherein the final or penultimate step is a reaction using a PET-ready reagent or a plurality of PET-ready reagents. Methods of preparing and using the libraries are also provided.

摘要翻译： 提供了一种候选药剂的正电子发射断层摄影（PET）已经存在的文库，其可以通过多步法制备，其中最终或倒数第二步是使用PET就绪试剂或多种PET待测试剂的反应。 还提供了制备和使用文库的方法。

公开(公告)号：WO2008089491A3

公开(公告)日：2008-07-24

申请号：PCT/US2008/051706

申请日：2008-01-22

申请人： KAI PHARMACEUTICALS, INC. ,  MACLEAN, Derek

发明人： MACLEAN, Derek

IPC分类号： C07K14/00

摘要： The disclosed invention relates to methods of modifying peptide compositions to increase stability and delivery efficiency. Specifically, the disclosed invention relates to methods to increase the stability and delivery efficiency of protein kinase C (PKC) modulatory peptide compositions. A "therapeutic peptide composition" comprises a "carrier peptide" and a "cargo peptide." A "carrier peptide" is a peptide or amino acid sequence within a peptide that facilitates the cellular uptake of the therapeutic peptide composition. The "cargo peptide" is a PKC modulatory peptide. Peptide modifications to either the carrier peptide, the cargo peptide, or both, which are described herein increase the stability and delivery efficiency of therapeutic peptide compositions by reducing disulfide bond exchange, physical stability, reducing proteolytic degradation, and increasing efficiency of cellular uptake.

公开(公告)号：WO2011014707A2

公开(公告)日：2011-02-03

申请号：PCT/US2010/043792

申请日：2010-07-29

申请人： KAI PHARMACEUTICALS, INC. ,  KARIM, Felix ,  BARUCH, Amos ,  MACLEAN, Derek

发明人： KARIM, Felix ,  BARUCH, Amos ,  MACLEAN, Derek

IPC分类号： A61K38/08 ,  C07K7/06 ,  A61P3/14 ,  A61P5/20 ,  A61P5/00

CPC分类号： C07K7/06 ,  A61K9/0019 ,  A61K9/08 ,  A61K38/00 ,  A61K47/60 ,  C07K5/1013 ,  C07K7/08

摘要： Compounds having activity for lowering parathyroid hormone levels are described. In one embodiment, the compounds are comprised of a contiguous sequence of subunits, X 1 - X 2 - X 3 - X 4 - X 5 - X 6 - X 7 , wherein the X 1 subunit comprises a thiol-containing moiety and the distribution of charge on the X 2 -X 7 subunits provides the desired activity. Methods of using the compounds for treating hyperparathyroidism, bone disease and/or hypercalcemic disorders are also described, and in particular, methods for lowering plasma PTH and serum calcium are provided. The compounds can be used to treat subjects having, for example: primary, secondary or tertiary hyperparathyroidism; hypercalcemia of malignancy; metastatic bone disease; or osteoporosis.

摘要翻译： 描述了具有降低甲状旁腺激素水平的活性的化合物。 在一个实施方案中，化合物由亚单位X1-X2-X3-X4-X5-X6-X7的连续序列组成，其中X1亚基包含含巯基的部分以及X2-X7亚基上的电荷分布 提供所需的活动。 还描述了使用该化合物治疗甲状旁腺功能亢进，骨疾病和/或高钙血症的方法，特别是提供降低血浆PTH和血清钙的方法。 这些化合物可用于治疗患有例如：原发性，继发性或甲状腺功能亢进的受试者; 恶性高钙血症; 转移性骨病; 或骨质疏松。

公开(公告)号：WO2007035782A2

公开(公告)日：2007-03-29

申请号：PCT/US2006/036568

申请日：2006-09-19

申请人： KAI PHARMACEUTICALS, INC. ,  CHEN, Leon, E. ,  WALTER, Sarah ,  MACLEAN, Derek

发明人： CHEN, Leon, E. ,  WALTER, Sarah ,  MACLEAN, Derek

IPC分类号： C07K14/82 ,  C12N9/12 ,  A61K38/14

CPC分类号： C12Y207/11013 ,  A61K9/0048 ,  A61K9/08 ,  A61K38/00 ,  A61K47/645 ,  C12N9/1205

摘要： The present invention provides peptides for inhibiting various protein kinase isozymes. The peptide can be directed to any region of the protein kinase C isozyme, and in one embodiment, is directed to the V5 domain. The peptide can be conjugated to a carrier, in a releasable or non-releasable manner. The peptides can be used to inhibit angiogenesis and/or vascular permeability. The peptides can be used to treat subjects having, for example, cancer, diabetic blindness, macular degeneration, rheumatoid arthritis, or psoriasis.

摘要翻译： 本发明提供用于抑制各种蛋白激酶同功酶的肽。 肽可以被引导到蛋白激酶C同功酶的任何区域，并且在一个实施方案中，涉及V5结构域。 肽可以以可释放或不可释放的方式与载体缀合。 肽可以用于抑制血管发生和/或血管通透性。 肽可用于治疗患有例如癌症，糖尿病性失明，黄斑变性，类风湿性关节炎或牛皮癣的受试者。

公开(公告)号：WO2020096695A1

公开(公告)日：2020-05-14

申请号：PCT/US2019/050708

申请日：2019-09-11

申请人： APPLIED MOLECULAR TRANSPORT INC. ,  MRSNY, Randall J. ,  OLSON, Charles ,  MACLEAN, Derek ,  POSTLETHWAITE, Sally

发明人： MRSNY, Randall J. ,  OLSON, Charles ,  MACLEAN, Derek ,  POSTLETHWAITE, Sally ,  PORAT, Amir

IPC分类号： A61K47/64

摘要： The present disclosure provides delivery constructs comprising a carrier coupled to a heterologous payload, wherein coupling of the carrier to the payload can result in transportation of the payload (e.g., a therapeutic payload) into and/or across intact polarized epithelial cells (e.g., epithelial cells of the gut of a mammal). The delivery construct can be part of a pharmaceutical composition that can be orally administered to a subject to provide for improved, effective therapies for treatment of, e.g., inflammatory diseases or autoimmune diseases.

公开(公告)号：WO2008089494A3

公开(公告)日：2008-07-24

申请号：PCT/US2008/051736

申请日：2008-01-22

申请人： KAI PHARMACEUTICALS, INC. ,  MACLEAN, Derek ,  YIN, Kevin

发明人： MACLEAN, Derek ,  YIN, Kevin

IPC分类号： A61K38/00 ,  A61K38/03 ,  A61K38/04 ,  A61K38/08 ,  A61K38/10 ,  A61K38/16

摘要： The disclosure herein relates to modified εPKC inhibitory peptides, methods of generating such peptides, and method for using εPKC inhibitory peptides for the treatment of pain.