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    Phthalazine derivatives for treating inflammatory diseases
    1.
    发明申请
    Phthalazine derivatives for treating inflammatory diseases 审中-公开

    公开(公告)号：US20050176711A1

    公开(公告)日：2005-08-11

    申请号：US11099292

    申请日：2005-04-05

    申请人： Guido Bold ,  Janet King ,  Joerg Frei ,  Richard Heng ,  Paul Manley ,  Bernhard Wietfeld ,  Jeanette Wood

    发明人： Guido Bold ,  Janet King ,  Joerg Frei ,  Richard Heng ,  Paul Manley ,  Bernhard Wietfeld ,  Jeanette Wood

    IPC分类号： A61K31/502 ,  A61K31/506 ,  A61P1/16 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P9/14 ,  A61P13/12 ,  A61P17/06 ,  A61P19/02 ,  A61P25/04 ,  A61P25/28 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P43/00 ,  C07D401/06 ,  C07D401/14 ,  A61K31/53 ,  A61K31/501 ,  C07D43/02

    CPC分类号： C07D401/06 ,  A61K31/501 ,  A61K31/502 ,  C07D401/14

    摘要： The invention relates to the treatment of an inflammatory disease, especially an inflammatory rheumatoid or rheumatic disease, and/or pain with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I, wherein r is 0 to 2, n is 0 to 3 R1 and R2 a) are independently in each case a lower alkyl; b) together form a bridge of subformula I*, wherein the bond is achieved via the two terminal C atoms and m is 0 to 4, or c) together form a bridge of subformula I**, wherein one or two of the ring members T1, T2, T3 and T4 are nitrogen, and the others are in each case CH, and the bond is achieved via atoms T1 and T4; G is —C(═O)—, —CHF—, —CF2—, lower alkylene, C2-C6alkenylene, lower alkylene or C3-C6alkenylene substituted by acyloxy or hydroxy, —CH2—O—, —CH2S—, —CH2—NH—, —CH2—O—CH2—, —CH2—S—CH2—, —CH2—NH—CH2—, oxa (—O—), thia (—S—), imino (—NH—), —CH2—O—CH2—, —CH2S—CH2— or —CH2—NH—CH2—; A, B, D, E and T are independently N or CH subject to the proviso that at least one and not more than three of these radicals are N; Q is lower alkyl, lower alkoxy or halogen; Ra and Ra′ are each independently H or lower alkyl; X is imino, oxa, or thia; Y is hydrogen, aryl, heteroaryl, or unsubstituted or substituted cycloalkyl; and Z is mono- or disubstituted amino, halogen, alkyl, substituted alkyl, hydroxy, etherified or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono- or N,N-disubstituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, phenyl lower alkylthio, alkylphenylthio, phenylsulfinyl, phenyl-lower alkylsulfinyl, alkylphenylsulfinyl phenylsulfonyl, phenyl-lower alkylsulfonyl, alkylphenylsulfonyl, or (alternatively or, in a broader aspect of the invention, in addition) selected from the group consisting of ureido, halo-lower alkylthio, halo-lower alkansulfonyl, pyrazolyl, lower-alkyl pyrazolyl and C2-C7alkenyl; wherein—if more than 1 radical Z (m≧2) is present—the substituents Z are selected independently from each other; and wherein the bonds characterized in subformula I* by a wavy line are either single or double bonds; or an N-oxide of said compound, wherein 1 or more N atoms carry an oxygen atom; or a pharmaceutically acceptable salt thereof; as well as to new phthalazine derivatives; processes for the preparation thereof; the application thereof in a process for the treatment of the human or animal body; the use thereof for the treatment of a disease, especially a disease caused by ocular neovascularisation, such as age-related macula degeneration or diabetic retinopathy, or other diseases that respond to the inhibition of tyrosine kinases, such as a proliferative disease; a method for the treatment of such disease in mammals; and the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment especially of a disease as mentioned above.

    COMBINATIONS COMPRISING EPOTHILONES AND PHARMACEUTICAL USES THEREOF
    2.
    发明申请
    COMBINATIONS COMPRISING EPOTHILONES AND PHARMACEUTICAL USES THEREOF 失效
    包含EPOTHILONES及其药物用途的组合

    公开(公告)号：US20080119529A1

    公开(公告)日：2008-05-22

    申请号：US12019294

    申请日：2008-01-24

    申请人： TianLing Chen ,  Diane Greeley ,  John Rothermel ,  Markus Wartmann ,  Jeanette Wood

    发明人： TianLing Chen ,  Diane Greeley ,  John Rothermel ,  Markus Wartmann ,  Jeanette Wood

    IPC分类号： A61K31/426 ,  A61P43/00 ,  C07D417/06

    CPC分类号： A61K31/663 ,  A61K31/427 ,  A61K31/502 ,  A61K31/555 ,  A61K33/24 ,  A61K45/06 ,  A61K2300/00

    摘要： The invention relates to a combination which comprises (a) a bisphosphonate, a platinum compound or a vasculostatic compound and (b) an epothilone derivative of formula I wherein A represents O or NRN, wherein RN is hydrogen or lower alkyl, R is hydrogen or lower alkyl, and Z is O or a bond, in which the active ingredients (a) and (b) are present in each case in free form or in the form of a pharmaceutically acceptable salt and optionally at least one pharmaceutically acceptable carrier for simultaneous, separate or sequential use, in particular for the delay of progression or treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition, a commercial package or product comprising such a combination; the use of such a combination for the preparation of a medicament for the delay of progression or treatment of a proliferative disease and to a method of treatment of a warm-blooded animal.

    摘要翻译： 本发明涉及一种组合，其包含（a）二膦酸盐，铂化合物或血管平滑化合物和（b）式I的埃坡霉素衍生物，其中A表示O或NR N，其中R

    Phthalazine derivatives for treating inflammatory diseases
    3.
    发明申请
    Phthalazine derivatives for treating inflammatory diseases 失效
    用于治疗炎性疾病的酞嗪衍生物

    公开(公告)号：US20060217388A1

    公开(公告)日：2006-09-28

    申请号：US11441961

    申请日：2006-05-26

    申请人： Guido Bold ,  Janet King ,  Jorg Frei ,  Richard Heng ,  Paul Manley ,  Bernhard Wietfeld ,  Jeanette Wood

    发明人： Guido Bold ,  Janet King ,  Jorg Frei ,  Richard Heng ,  Paul Manley ,  Bernhard Wietfeld ,  Jeanette Wood

    IPC分类号： A61K31/501 ,  C07D403/02

    CPC分类号： C07D401/06 ,  A61K31/501 ,  A61K31/502 ,  C07D401/14

    摘要： The invention relates to the treatment of leukemias with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I, the substituents being defined in the specification; as well as to new phthalazine derivatives; processes for the preparation thereof; the application thereof in a process for the treatment of the human or animal body; the use thereof for the treatment of a disease, especially a disease caused by ocular neovascularization, such as age-related macula degeneration or diabetic retinopathy, or other diseases that respond to the inhibition of tyrosine kinases, such as a proliferative disease; a method for the treatment of such disease in mammals; and the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment especially of a disease as mentioned above.

    摘要翻译： 本发明涉及用式I的VEGF受体酪氨酸激酶的活性抑制剂治疗白血病，所述取代基在说明书中定义; 以及新的酞嗪衍生物; 制备方法; 其用于治疗人或动物体的方法中的应用; 其用于治疗疾病，特别是由眼睛新生血管形成引起的疾病，例如年龄相关性黄斑变性或糖尿病性视网膜病，或其它对酪氨酸激酶（例如增殖性疾病）的抑制作用的疾病; 哺乳动物治疗这种疾病的方法; 以及这种化合物用于制造特别是上述疾病的药物制剂的用途。

    Pharmaceutical use of cox-2-inhibitors in angiogenesis-mediated ocular disorders
    6.
    发明申请
    Pharmaceutical use of cox-2-inhibitors in angiogenesis-mediated ocular disorders 审中-公开
    cox-2抑制剂在血管生成介导的眼部疾病中的药物用途

    公开(公告)号：US20050043410A1

    公开(公告)日：2005-02-24

    申请号：US10502180

    申请日：2003-01-22

    申请人： Romulus Brazzell ,  George Lambrou ,  Elisabeth Latour ,  Anna Ottlecz ,  Jeanette Wood

    发明人： Romulus Brazzell ,  George Lambrou ,  Elisabeth Latour ,  Anna Ottlecz ,  Jeanette Wood

    IPC分类号： A61P27/02 ,  A61K31/196 ,  A61P27/06 ,  A61P29/00 ,  A61P43/00 ,  A61K31/195

    CPC分类号： A61K31/196

    摘要： The invention provides a method of treating an angiogenesis-mediated ocular disorder, e.g. ocular neovascularisation, retinal neovascularisation, including neovascularisation following injury or infection, retrolental fibroplasias, and neovascular glaucoma, age-related macular degeneration, diabetic retinopathy, pathologic myopia, ocular histoplasmosis, neovascular glaucoma, retinopathy of prematurity, the after effects of corneal transplantation, control of postsurgical ocular inflammation (e.g. after cataract surgery), cystoid macular edema (CME), herpes keratitis, in a subject in need of such treatment which comprises administering to the subject an effective amount of a COX-2 inhibitor of formula I wherein R, R1, R2, R3, R4, and R5 are as defined; a pharmaceutically acceptable salts thereof; or a pharmaceutically acceptable prodrug esters thereof.

    摘要翻译： 本发明提供了治疗血管生成介导的眼部疾病的方法，例如， 眼新生血管形成，视网膜新生血管形成，包括损伤或感染后新生血管形成，复发性纤维增生和新生血管性青光眼，年龄相关性黄斑变性，糖尿病性视网膜病变，病理性近视，眼组织胞浆菌病，新生血管性青光眼，早产儿视网膜病变，角膜移植后期作用 的术后眼部炎症（例如白内障手术后），囊性黄斑水肿（CME），疱疹角膜炎，需要治疗的受试者，其包括向受试者施用有效量的式I的COX-2抑制剂，其中R， R1，R2，R3，R4和R5如上所定义; 其药学上可接受的盐; 或其药学上可接受的前药酯。