公开(公告)号：US4457942A

公开(公告)日：1984-07-03

申请号：US410018

申请日：1982-08-20

申请人： Saul W. Brusilow

发明人： Saul W. Brusilow

IPC分类号： A61K31/19

CPC分类号： A61K31/19

摘要： A method of alleviating the accumulation of waste nitrogen in human beings is disclosed, wherein phenylbutyrate, or even numbered conger thereof, is administered to a patient having such waste nitrogen accumulation. The phenylbutyrate or other compound is broken down by beta-oxidation to eventually yield phenylacetate, which is known to be useful for removing waste nitrogen from the blood stream.The present invention provides a solution to the offensive odor of phenylacetate, which is unpalatable to patients, and also can eliminate peaks and valleys of drug levels in the patient, due to the gradual formation of the desired compound phenylacetate in the patient's body.

摘要翻译： 公开了一种减轻人体中废氮积累的方法，其中向具有这种废氮积累的患者施用苯丁酸酯或甚至编号的它们。 苯基丁酸酯或其他化合物通过β-氧化分解，最终产生苯乙酸酯，这已知可用于从血液中除去废氮。 本发明提供了一种对于乙酸苯乙酯的令人反感的气味的解决方案，其对于患者来说是不可口的，并且由于在患者体内逐渐形成所需化合物苯乙酸乙酯，可以消除患者中药物水平的峰值和谷值。

公开(公告)号：US6130035A

公开(公告)日：2000-10-10

申请号：US240866

申请日：1999-02-01

申请人： Saul W. Brusilow

发明人： Saul W. Brusilow

IPC分类号： C12Q1/527 ,  G01N33/94 ,  C12Q1/00 ,  G01N33/48

CPC分类号： C12Q1/527 ,  G01N33/94 ,  G01N2800/52

摘要： The present invention provides a method of screening for the presence or absence of cancer characterized by increased DNA synthesis. The present invention also provides a method of monitoring the effectiveness of treatment of cancer characterized by increased DNA synthesis. The methods are based on the observation that increased de novo pyrimidine biosynthesis is characteristic of malignant solid tumors. An initial step of pyrimidine biosynthesis is the conversion of orotidine monophosphate (OMP) to uridine monophosphate by OMP decarboxylase which is inhibited by mononucleotide precursors such as 6-hydroxyuridine, 6-azauridine, uridine, allopurinol and oxipurinol. Inhibition of OMP decarboxylase results in accumulation of orotidine and orotate which can be measured in a urine sample. The accumulation of oritidine and orotate, in amounts above that of a control, provides an indicator that the subject has a cancer characterized by having increased DNA synthesis.

摘要翻译： 本发明提供一种筛选以DNA合成增加为特征的癌症的存在或不存在的方法。 本发明还提供了监测以DNA合成增加为特征的癌症治疗有效性的方法。 这些方法基于观察到增加的从头嘧啶生物合成是恶性实体瘤的特征。 嘧啶生物合成的初始步骤是通过被单核苷酸前体如6-羟基尿苷，6-氮尿苷，尿苷，别嘌呤醇和肟基尿素抑制的OMP脱羧酶将单磷酸的乳清苷酸（OMP）转化为尿苷单磷酸。 OMP脱羧酶的抑制导致可以在尿样中测量的乳清酸和乳清酸的积聚。 以高于对照的量的量的奥立替丁和乳清酸的积累提供了指标，该受试者具有以增加的DNA合成为特征的癌症。

公开(公告)号：US6083984A

公开(公告)日：2000-07-04

申请号：US317900

申请日：1999-05-25

申请人： Saul W. Brusilow

发明人： Saul W. Brusilow

IPC分类号： A01N37/10 ,  A61K31/235 ,  C07C57/30 ,  C07C69/612 ,  C07C69/618

CPC分类号： C07C57/30 ,  C07C69/612 ,  C07C69/618 ,  Y10S514/814 ,  Y10S514/815 ,  Y10S514/885

摘要： Two new forms of prodrug for phenylacetate, of even congeners of phenylalkanoic acid and phenylalkenoic acids, which are the phenylalkanoic or phenylalkenoic esters of glycerol, or the ethyl esters of phenylalkanoic acid or phenylalkenoic acids. These forms of the drugs provide a convenient dosage form of the drugs. The prodrugs of the invention are useful to treat patients with diseases of nitrogen accumulation, patients with certain .beta.-hemoglobinopathies, anemia, and cancer.

公开(公告)号：US6060510A

公开(公告)日：2000-05-09

申请号：US317901

申请日：1999-05-25

申请人： Saul W. Brusilow

发明人： Saul W. Brusilow

IPC分类号： A01N37/10 ,  A61K31/235 ,  C07C57/30 ,  C07C69/612 ,  C07C69/618

CPC分类号： C07C57/30 ,  C07C69/612 ,  C07C69/618 ,  Y10S514/814 ,  Y10S514/815 ,  Y10S514/885

摘要： Two new forms of prodrug for phenylacetate, of even congeners of phenylalkanoic acid and phenylalkenoic acids, which are the phenylalkanoic or phenylalkenoic esters of glycerol, or the ethyl esters of phenylalkanoic acid or phenylalkenoic acids. These forms of the drugs provide a convenient dosage form of the drugs. The prodrugs of the invention are useful to treat patients with diseases of nitrogen accumulation, patients with certain .beta.-hemoglobinopathies, anemia, and cancer.

摘要翻译： 苯乙酸酯的两种新形式的前药，甚至是苯基链烷酸和苯基链烯酸的同系物，它们是甘油的苯基链烷酸或苯基链烯酸酯，或苯基链烷酸或苯基链烯酸的乙基酯。 这些形式的药物提供了方便的药物剂型。 本发明的前药可用于治疗患有氮积聚疾病，具有某些β-血红蛋白病，贫血和癌症的患者。

公开(公告)号：US5968979A

公开(公告)日：1999-10-19

申请号：US6432

申请日：1998-01-13

申请人： Saul W. Brusilow

发明人： Saul W. Brusilow

IPC分类号： A01N37/10 ,  A61K31/235 ,  C07C57/30 ,  C07C69/612 ,  C07C69/618

CPC分类号： C07C57/30 ,  C07C69/612 ,  C07C69/618 ,  Y10S514/814 ,  Y10S514/815 ,  Y10S514/885

摘要： Two new forms of prodrug for phenylacetate, of even congeners of phenylalkanoic acid and phenylalkenoic acids, which are the phenylalkanoic or phenylalkenoic esters of glycerol, or the ethyl esters of phenylalkanoic acid or phenylalkenoic acids. These forms of the drugs provide a convenient dosage form of the drugs. The prodrugs of the invention are useful to treat patients with diseases of nitrogen accumulation, patients with certain .beta.-hemoglobinopathies, anemia, and cancer.

摘要翻译： 苯乙酸酯的两种新形式的前药，甚至是苯基链烷酸和苯基链烯酸的同系物，它们是甘油的苯基链烷酸或苯基链烯酸酯，或苯基链烷酸或苯基链烯酸的乙基酯。 这些形式的药物提供了方便的药物剂型。 本发明的前药可用于治疗患有氮积聚疾病，具有某些β-血红蛋白病，贫血和癌症的患者。

公开(公告)号：US4284647A

公开(公告)日：1981-08-18

申请号：US135685

申请日：1980-03-31

申请人： Saul W. Brusilow ,  Mark L. Batshaw ,  Norman S. Radin

发明人： Saul W. Brusilow ,  Mark L. Batshaw ,  Norman S. Radin

IPC分类号： A61K31/19

CPC分类号： A61K31/19 ,  Y10S514/893

摘要： A process for controlling waste nitrogen accumulation diseases in humans which comprises administering an effective amount of at least one compound selected from the group consisting of benzoic acid, phenylacetic acid and the non-toxic, pharmaceutically-acceptable salts of the acids to a human suffering from waste nitrogen accumulation.

摘要翻译： 一种用于控制人类中的氮积存疾病的方法，其包括将有效量的至少一种选自苯甲酸，苯乙酸和无毒的药学上可接受的酸的化合物给予患有 废氮积累。