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23 条记录 (耗时 0.027 秒)

    Preparation of dialkyl- and diarylphosphonoalkanoic acids and substituted acrylic acids
    11.
    发明授权
    Preparation of dialkyl- and diarylphosphonoalkanoic acids and substituted acrylic acids 失效

    公开(公告)号：US4307232A

    公开(公告)日：1981-12-22

    申请号：US132502

    申请日：1980-03-21

    申请人： David R. Brittelli

    发明人： David R. Brittelli

    IPC分类号： C07C51/353 ,  C07D317/60 ,  C07F9/40 ,  C07C51/00

    CPC分类号： C07D317/60 ,  C07C51/353 ,  C07F9/4006

    摘要： Process for preparing the substituted phosphonoalkanoic acid of the formula ##STR1## wherein: R.sup.1 is alkyl of 1-8 carbon atoms, aralkyl of 7-10 carbon atoms, phenyl, or substituted phenyl of 6-10 carbon atoms;R.sup.2 is H, hydrocarbyl of 1-18 carbon atoms, or substituted hydrocarbyl of 1-18 carbon atoms, wherein in said hydrocarbyl groups the carbon atom attached to the ##STR2## moiety is substituted with two or three hydrogen atoms or is a carbon atom of an aromatic ring; andY is oxygen or sulfur,which process comprises contacting and reacting, at a temperature of about -70.degree. C. to about 125.degree. C., a pressure of about 1-100 atmospheres (0.1-10 MPa), and for a time sufficient to effect reaction, the phosphite ester of the formula ##STR3## wherein R.sup.1 and Y are as defined above, with the .alpha.-halocarboxylic acid of the formula R.sup.2 CHXCO.sub.2 H, wherein X is Cl, Br, or I and R.sup.2 is as defined above, in the presence of at least two moles of base per mole of limiting reagent, said base having a pKa greater than about 15, to produce the substituted phosphonoalkanoic acid, and process for preparing the substituted acrylic acid of the formula R.sup.3 R.sup.4 C.dbd.CR.sup.2 COOH wherein:R.sup.2 is as defined above; andR.sup.3 and R.sup.4 are the same or different and are selected from H, hydrocarbyl of 1-18 carbon atoms, and substituted hydrocarbyl of 1-18 carbon atoms or R.sup.3 and R.sup.4 taken together are cycloalkylene or substituted cycloalkylene of 4-18 carbon atoms,which process comprises:(a) carrying out the aforesaid reaction to produce the substituted phosphonoalkanoic acid except that at least three moles of base are present; and(b) contacting and reacting, at a temperature of about -70.degree. to about 125.degree. C., a pressure of about 1-100 atmospheres (0.1-10 MPa), and for a time sufficient to effect reaction, the substituted phosphonoalkanoic acid produced in step (a) with the carbonyl compound of the formula R.sup.3 R.sup.4 C.dbd.O, wherein R.sup.3 and R.sup.4 are as defined above, to produce the substituted acrylic acid.

    Tetraphosphinylquinodimethanes
    14.
    发明授权
    Tetraphosphinylquinodimethanes 失效
    四膦氧基喹诺酮类

    公开(公告)号：US4650609A

    公开(公告)日：1987-03-17

    申请号：US748661

    申请日：1985-06-25

    申请人： David R. Brittelli

    发明人： David R. Brittelli

    IPC分类号： C07F9/38 ,  C07F9/40 ,  C07F9/42

    CPC分类号： C07F9/409 ,  C07F9/3843 ,  C07F9/4025 ,  C07F9/4056 ,  C07F9/42

    摘要： Compounds having a quinodimethane or a 7,8-dihydroquinodimethane nucleus and four substituted phosphinyl groups at the 7- and 8-positions are disclosed. A process for preparing the specified compounds is also disclosed.

    摘要翻译： 公开了具有醌二甲烷或7,8-二氢醌二甲烷核的化合物和7位和8位的4个取代的氧膦基。 还公开了制备指定化合物的方法。

    CERTAIN SUBSTITUTED UREAS, AS MODULATORS OF KINASE ACTIVITY
    17.
    发明申请
    CERTAIN SUBSTITUTED UREAS, AS MODULATORS OF KINASE ACTIVITY 有权
    某些替代的UREAS，作为激酶的调节剂

    公开(公告)号：US20100286190A1

    公开(公告)日：2010-11-11

    申请号：US12840246

    申请日：2010-07-20

    申请人： Scott A. Mitchell ,  Mihaela Diana Danca ,  Peter A. Blomgren ,  David R. Brittelli ,  Pavel Zhichkin ,  Matthew E. Voss

    发明人： Scott A. Mitchell ,  Mihaela Diana Danca ,  Peter A. Blomgren ,  David R. Brittelli ,  Pavel Zhichkin ,  Matthew E. Voss

    IPC分类号： A61K31/444 ,  C07D471/04 ,  A61K31/4439 ,  C07D401/06 ,  A61K31/4709 ,  A61P35/00 ,  A61P29/00 ,  A61P19/02 ,  A61P17/06 ,  A61P27/02

    CPC分类号： C07D471/04 ,  C07D401/06

    摘要： Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, and prodrugs thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicles chosen from carriers, adjuvants, and excipients, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to angiogenic kinase modulation, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Methods of treatment include administering at least one chemical entity as a single active agent or administering such at least one chemical entity in combination with one or more other therapeutic agents. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with at least one chemical entity under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom determining the presence or absence of the angiogenic kinase in the sample.

    摘要翻译： 本文提供了选自式1化合物的某些化学实体及其药学上可接受的盐，溶剂合物，螯合物，非共价复合物及其前体药物。 还提供了包含至少一种化学实体和一种或多种选自载体，佐剂和赋形剂的药学上可接受的载体的药物组合物。 公开了治疗患有对血管生成激酶调节反应的某些疾病和病症的患者的方法，其包括向这些患者施用一定量的至少一种有效减少疾病或病症体征或症状的化学实​​体。 这些疾病包括癌症，包括乳腺肿瘤，子宫内膜癌，结肠癌和颈部鳞状细胞癌。 治疗方法包括给予至少一种化学实体作为单一活性剂或者与一种或多种其它治疗剂组合施用这样的至少一种化学实体。 一种用于确定样品中存在或不存在血管生成激酶的方法，包括在允许检测血管生成激酶活性，检测血管生成激酶活性水平的条件下将样品与至少一种化学实体接触 确定样品中存在或不存在血管生成激酶。

    Certain substituted ureas, as modulators of kinase activity
    18.
    发明授权
    Certain substituted ureas, as modulators of kinase activity 有权
    某些取代的脲，作为激酶活性的调节剂

    公开(公告)号：US07777040B2

    公开(公告)日：2010-08-17

    申请号：US11415419

    申请日：2006-05-02

    申请人： Scott A. Mitchell ,  Mihaela Diana Danca ,  Peter A. Blomgren ,  David R. Brittelli ,  Pavel Zhichkin ,  Matthew E. Voss

    发明人： Scott A. Mitchell ,  Mihaela Diana Danca ,  Peter A. Blomgren ,  David R. Brittelli ,  Pavel Zhichkin ,  Matthew E. Voss

    IPC分类号： C07D215/38

    CPC分类号： C07D471/04 ,  C07D401/06

    摘要： Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, and prodrugs thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicles chosen from carriers, adjuvants, and excipients, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to angiogenic kinase modulation, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Methods of treatment include administering at least one chemical entity as a single active agent or administering such at least one chemical entity in combination with one or more other therapeutic agents. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with at least one chemical entity under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom determining the presence or absence of the angiogenic kinase in the sample.

    摘要翻译： 本文提供了选自式1化合物的某些化学实体及其药学上可接受的盐，溶剂合物，螯合物，非共价复合物及其前体药物。 还提供了包含至少一种化学实体和一种或多种选自载体，佐剂和赋形剂的药学上可接受的载体的药物组合物。 公开了治疗患有对血管生成激酶调节反应的某些疾病和病症的患者的方法，其包括向这些患者施用一定量的至少一种有效减少疾病或病症体征或症状的化学实​​体。 这些疾病包括癌症，包括乳腺肿瘤，子宫内膜癌，结肠癌和颈部鳞状细胞癌。 治疗方法包括给予至少一种化学实体作为单一活性剂或者与一种或多种其它治疗剂组合施用这样的至少一种化学实体。 一种用于确定样品中存在或不存在血管生成激酶的方法，包括在允许检测血管生成激酶活性，检测血管生成激酶活性水平的条件下将样品与至少一种化学实体接触 确定样品中存在或不存在血管生成激酶。

    Inhibition of matrix metalloproteases by substituted biaryl oxobutyric acids
    20.
    发明授权
    Inhibition of matrix metalloproteases by substituted biaryl oxobutyric acids 失效
    通过取代的联芳基氧代丁酸抑制基质金属蛋白酶

    公开(公告)号：US06911449B2

    公开(公告)日：2005-06-28

    申请号：US10735040

    申请日：2003-12-12

    申请人： Michael C. VanZandt ,  David R. Brittelli ,  Brian R. Dixon

    发明人： Michael C. VanZandt ,  David R. Brittelli ,  Brian R. Dixon

    IPC分类号： A61K31/425 ,  A61K31/426 ,  A61K31/4706 ,  A61K31/502 ,  A61K31/513 ,  A61K31/517 ,  A61K31/53 ,  A61K31/5513 ,  C07C62/38 ,  C07D237/32 ,  C07D253/08 ,  A61K31/519 ,  C07D239/72

    CPC分类号： C07D253/08 ,  A61K31/425 ,  A61K31/426 ,  A61K31/4706 ,  A61K31/502 ,  A61K31/513 ,  A61K31/517 ,  A61K31/53 ,  A61K31/5513 ,  C07C62/38 ,  C07D237/32

    摘要： Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formulas: wherein r is 0-2, T is selected from and R40 is a mono- or bi-heterocyclic structure. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, corneal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempero mandibular joint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from athrosclerotic plaque rupture. The present invention also provides pharmaceutical compositions and methods for treating such conditions.

    摘要翻译： 提出了基质金属蛋白酶抑制化合物，其药物组合物和使用这些化合物的疾病治疗方法。 本发明的化合物具有以下通式：其中r为0-2，T选自并且R 40是单或双杂环结构。 这些化合物可用于抑制基质金属蛋白酶，因此可用于抗MMP的作用，例如骨关节炎，类风湿性关节炎，脓毒性关节炎，牙周病，角膜溃疡，蛋白尿，动脉瘤性主动脉疾病，疏水性表皮松解症，大疱疹，导致炎症的病症 反应，MMP活性介导的骨质减少，颞下颌关节疾病，神经系统脱髓鞘疾病，创伤性关节损伤后的肿瘤转移或退行性软骨损失，以及来自动脉粥样硬化斑块破裂的冠状动脉血栓形成。 本发明还提供了用于治疗这些病症的药物组合物和方法。