公开(公告)号：US20080261939A1

公开(公告)日：2008-10-23

申请号：US12107658

申请日：2008-04-22

Applicant: George S. Drummond ,  Philip C. Lang

Inventor： George S. Drummond ,  Philip C. Lang

IPC: A61K31/555

CPC classification number: A61K9/0019 ,  A61K31/555

Abstract: Pharmaceutical compositions including stannsoporfin, drug products incorporating pharmaceutical compositions, methods of making pharmaceutical compositions, and methods of treating hyperbilirubinemia with drug products and compositions are disclosed.

Abstract translation: 本发明公开了包含不溶性苯乙烯的药物组合物，掺入药物组合物的药物产品，制备药物组合物的方法以及用药物产品和组合物治疗高胆红素血症的方法。

公开(公告)号：US06479529B1

公开(公告)日：2002-11-12

申请号：US09290904

申请日：1999-04-12

Applicant: Philip C. Lang

Inventor： Philip C. Lang

IPC: A61K3142

CPC classification number: A61K31/42

Abstract: Chemically stable pharmaceutical formulations comprising a therapeutically effective amount of a material of formula I are provided which formulations contain a stabilizer system comprising an organic carboxylic acid containing more than 1 carboxylic acid group and an antioxidant. The preferred organic carboxylic acid is citric acid and the preferred antioxidants are ascorbic acid and butylated hydroxytoluene, which antioxidants are preferred to be used in admixture. The chemically stable pharmaceutical formulations are particularly useful for treating Irritable Bowel Syndrome (IBS) in mammals and comprises administering to the mammal needing treatment an effective dose of the above chemically stable pharmaceutical formulation. The stabilizer system is also effective for use in other pharmaceutical formulations containing active ingredients having oxidizable groups such as amino, phenolic, hydryoxyl amino, aldehyde, unsaturated compounds, sulfoxide, sulfone and mercapto. The preferred Formula I compound is as follows: wherein R and R1 are propyl; R2 and R3 are hydrogen; Y is CH2 and the compound is an HCl salt.

Abstract translation: 提供包含治疗有效量的式I的物质的化学稳定的药物制剂，其中哪些制剂含有包含含有多于1个羧酸基团的有机羧酸和抗氧化剂的稳定剂体系。 优选的有机羧酸是柠檬酸，优选的抗氧化剂是抗坏血酸和丁基化羟基甲苯，该抗氧化剂优选用于混合物。 化学稳定的药物制剂特别可用于治疗哺乳动物中的肠易激综合征（IBS），并且包括向需要治疗的哺乳动物施用有效剂量的上述化学稳定的药物制剂。 稳定剂系统也可用于含有具有可氧化基团的活性成分的其它药物制剂，例如氨基，酚，羟基氧基氨基，醛，不饱和化合物，亚砜，砜和巯基。 优选的式I化合物如下：其中R和R 1是丙基; R2和R3是氢; Y是CH 2，该化合物是HCl盐。

公开(公告)号：US06194420B1

公开(公告)日：2001-02-27

申请号：US09452008

申请日：1999-11-30

Applicant: Philip C. Lang

Inventor： Philip C. Lang

IPC: C07D48704

CPC classification number: C07D239/84 ,  A61K31/517

Abstract: The compound 2-amino-5,6-dichloro-3,4-dihydroquinazoline has been found to have enhanced platelet count reducing properties. Also provided are methods for synthetically making the compound and a method of reducing the platelet count in a patient by administering to the patient a platelet reducing effective amount of the compound preferably together with a pharmaceutically acceptable carrier. A pharmaceutical composition is also provided which contains the above compound as the active ingredient together with pharmaceutically acceptable excipients.

Abstract translation: 化合物2-氨基-5,6-二氯-3,4-二氢喹唑啉已被发现具有增强的血小板计数降低性质。 还提供了合成制备化合物的方法和通过向患者施用血小板减少有效量的化合物，优选与药学上可接受的载体一起降低患者血小板计数的方法。 还提供了含有上述化合物作为活性成分以及药学上可接受的赋形剂的药物组合物。

公开(公告)号：US5801245A

公开(公告)日：1998-09-01

申请号：US919964

申请日：1997-08-28

Applicant: Philip C. Lang

Inventor： Philip C. Lang

IPC: C07C201/08 ,  C07C205/12 ,  C07C227/14 ,  C07C227/18 ,  C07C229/36 ,  C07D235/00 ,  C07D339/00 ,  C07D487/04 ,  C07D239/00

CPC classification number: C07D487/04 ,  C07C201/08 ,  C07C201/12 ,  C07C227/16 ,  C07C227/18

Abstract: The known blood platelet reducing agent Anagrelide is prepared via an improved process starting with commercially available 2,3-dichlorotoluene and involving novel intermediates represented by the formulas: ##STR1## wherein Y is Br, Cl or I. Compound (G) is reacted with ethyl glycine to form the well-known intermediate ethyl-N-(2,3-dichloro-6-nitro benzyl) glycine which is then used following conventional process steps to form Anagrelide.

Abstract translation: 已知的血小板减少剂阿那格雷通过改进的方法从市售的2,3-二氯甲苯开始制备，并涉及由下式表示的新型中间体：其中Y是Br，Cl 或I.化合物（G）与乙基甘氨酸反应以形成公知的中间体N-（2,3-二氯-6-硝基苄基）甘氨酸，然后按照常规方法步骤使用甘氨酸形成阿那格雷。

公开(公告)号：US4283556A

公开(公告)日：1981-08-11

申请号：US119245

申请日：1980-02-07

Applicant: Philip C. Lang

Inventor： Philip C. Lang

IPC: C07C233/12 ,  C07C102/00

CPC classification number: C07C233/12

Abstract: A process for the manufacture of a substantially isomerically pure acylanilide of the structure ##STR1## where R is hydrogen, lower alkyl, hydroxy-lower alkyl or lower alkoxy-lower alkyl;R.sub.1 is lower alkyl, phenyl, lower alkylphenyl, lower alkoxy, lower alkoxyphenyl, chlorophenyl, nitrophenyl, dichlorophenyl, chloro-lower alkyl, cyano-lower alkyl, lower alkyl amino, sulfamoylphenyl, carbamoylphenyl or lower alkoxy-lower alkyl; andX is --CO-- or --SO.sub.2 --;comprising the step of treating an alcohol solution of a diamino compound of the structure ##STR2## with an acylating agent, to give an alcohol solution of the acylanilide, wherein substantially equivalent amounts of the acylating agent and the diamino compound are used and wherein the treatment is carried out by the slow, drop-wise addition of the acylating agent at a temperature in the range of about 0.degree. to 5.degree. C. The process is particularly advantageous when the alcohol solution of the diamino compound is produced by reduction of a suspension of the corresponding dinitro compound in the alcohol.

Abstract translation: 制备基本上异构体纯的酰基苯胺的方法，其结构为：其中R是氢，低级烷基，羟基 - 低级烷基或低级烷氧基 - 低级烷基; R 1是低级烷基，苯基，低级烷基苯基，低级烷氧基，低级烷氧基苯基，氯苯基，硝基苯基，二氯苯基，氯代低级烷基，氰基 - 低级烷基，低级烷基氨基，氨磺酰基苯基，氨基甲酰基苯基或低级烷氧基 - 低级烷基。 并且X是-CO-或-SO 2 - ; 包括用酰化剂处理结构为“IMAGE”的二氨基化合物的醇溶液的步骤，得到酰基酰苯胺的醇溶液，其中使用基本上相当量的酰化剂和二氨基化合物，其中处理 通过在约0℃至5℃的温度下缓慢逐滴加入酰化剂进行。当二氨基化合物的醇溶液通过还原悬浮液产生时，该方法是特别有利的 的相应的二硝基化合物在酒精中。

公开(公告)号：US06653500B2

公开(公告)日：2003-11-25

申请号：US10134088

申请日：2002-04-25

Applicant: Philip C. Lang ,  Roxanne P. Spencer ,  Wen-Lung Yeh ,  Michael Joseph Roth

Inventor： Philip C. Lang ,  Roxanne P. Spencer ,  Wen-Lung Yeh ,  Michael Joseph Roth

IPC: C07C20500

CPC classification number: C07D487/04 ,  C07C201/08 ,  C07C201/12 ,  C07C227/04 ,  C07C227/16 ,  C07C229/16 ,  C07C205/12 ,  C07C205/26 ,  C07C205/44

Abstract: Methods are provided for making Anagrelide base from 2,3-dichlorobenzaldehyde. A method is also provided for making an intermediate compound ethyl N-(2,3-dichloro-6-nitrobenzyl)glycine from 2,3-dichlorobenzaldehyde and for reducing the glycine compound using either SnCl2 or a specially defined catalyst. A cyclization method to form Anagrelide base from the corresponding iminoquinazoline compound is further provided.

公开(公告)号：US06583152B2

公开(公告)日：2003-06-24

申请号：US09845141

申请日：2001-04-30

Applicant: Robert E. Sosnowski ,  Philip C. Lang

Inventor： Robert E. Sosnowski ,  Philip C. Lang

IPC: A61K3144

CPC classification number: A61K31/015 ,  A61K31/525 ,  A61K31/7048 ,  A61K36/16 ,  A61K36/45 ,  A61K36/67 ,  A61K36/8962 ,  A61K2300/00

Abstract: Elevated levels of homocysteine have been implicated as an important risk factor for cardiovascular and other diseases. A composition for decreasing levels of plasma homocysteine and a method for administering the composition are provided the composition containing dextromethorphan (DM), folic acid and vitamins B6 and B12. The composition provides a synergistic therapeutic effect so that lower amounts of the above ingredients may be employed to minimize any undesirable side effects caused by the use of high levels of a component such as DM. Preferred compositions for cardiovascular diseases further include lecithin, vitamin E, beta-carotene, procyanidins/flavonoids, trimethylglycine, garlic oil and minerals. Other compositions for treating glaucoma include bilberry, bioflavonoids and beta-carotene and for treating tardive dyskinesia include an antioxidant such as grape seed extract and pine bark extract, lecithin and oligomeric proanthocyanidins. The compositions may be administered using any suitable means such as orally or intravenous.

Abstract translation: 升高的同型半胱氨酸水平被认为是心血管和其他疾病的重要危险因素。 提供了降低血浆高半胱氨酸水平的组合物和给予组合物的方法，所述组合物含有右美沙芬（DM），叶酸和维生素B6和B12。 该组合物提供协同的治疗效果，使得可以使用较低量的上述成分以使由使用高含量的组分如DM引起的任何不期望的副作用最小化。 心血管疾病的优选组合物还包括卵磷脂，维生素E，β-胡萝卜素，原花青素/类黄酮，三甲基甘氨酸，大蒜油和矿物质。 用于治疗青光眼的其它组合物包括越桔，生物类黄酮和β-胡萝卜素，并用于治疗迟发性运动障碍，包括抗氧化剂如葡萄籽提取物和松树皮提取物，卵磷脂和低聚原花青素。 组合物可以使用任何合适的方法如口服或静脉内施用。

公开(公告)号：US06541043B2

公开(公告)日：2003-04-01

申请号：US09941422

申请日：2001-08-28

Applicant: Philip C. Lang

Inventor： Philip C. Lang

IPC: A61K3300

CPC classification number: A61K33/02 ,  A61K31/07 ,  A61K31/133 ,  A61K31/20 ,  A61K31/205 ,  A61K31/355 ,  A61K31/375 ,  A61K31/525 ,  A61K31/714 ,  A61K33/06 ,  A61K33/30 ,  A61K36/074 ,  A61K36/16 ,  A61K36/258 ,  A61K36/38 ,  A61K36/67 ,  A61K2300/00

Abstract: A composition and method for treating Attention Deficit/Hyperactivity Disorder (ADHD) is provided which can be used both with and without ethical drugs now used to treat ADHD. The composition contains dimethylaminoethanol (DMAE), omega 3-fatty acids, betaine, oligomeric proanthocyanidins (OPC), folic acid, vitamins C, E, B12, B6, B5 and beta-carotene and minerals (calcium, magnesium, zinc and selenium). Ethical drugs such as amphetamines, methylphenidate HCl and pemoline are known to control ADHD, but each has significant side effects when used in their therapeutic dose. When combining the composition with such ethical drugs, the amount of the ethical drug can be lowered below a level which causes undesirable side effects which is an important feature. Preferred compositions contain one or more of lecithin, choline, 5-hydroxytryptophan, tyrosine, Reishi Extract, Kava Extract, Gingko, Ginseng and St. John's Wort.

Abstract translation: 提供了一种用于治疗注意力缺陷/多动障碍（ADHD）的组合物和方法，其可以与现在用于治疗ADHD的道德药物一起使用。 组合物含有二甲基氨基乙醇（DMAE），ω-3-脂肪酸，甜菜碱，低聚原花色素（OPC），叶酸，维生素C，E，B12，B6，B5和β-胡萝卜素和矿物质（钙，镁，锌和硒） 。 众所周知，安非他明，哌甲酯盐酸盐和哌莫林等伦理药物可以控制ADHD，但是当其治疗剂量使用时，各种药物都具有显着的副作用。 当将组合物与这种伦理药物组合时，可以将伦理药物的量降低到导致不期望的副作用的水平，这是重要的特征。 优选的组合物含有一种或多种卵磷脂，胆碱，5-羟色氨酸，酪氨酸，Reishi Extract，Kava Extract，Gingko，人参和St. John's Wort。

公开(公告)号：US06388073B1

公开(公告)日：2002-05-14

申请号：US09625962

申请日：2000-07-26

Applicant: Philip C. Lang ,  Roxanne P. Spencer ,  Wen-Lung Yeh ,  Michael Joseph Roth

Inventor： Philip C. Lang ,  Roxanne P. Spencer ,  Wen-Lung Yeh ,  Michael Joseph Roth

IPC: C07D48704

CPC classification number: C07D487/04 ,  C07C201/08 ,  C07C201/12 ,  C07C227/04 ,  C07C227/16 ,  C07C229/16 ,  C07C205/12 ,  C07C205/26 ,  C07C205/44

Abstract: Methods are provided for making Anagrelide base from 2,3-dichlorobenzaldehyde. A method is also provided for making an intermediate compound ethyl N-(2,3-dichloro-6-nitrobenzyl)glycine from 2,3-dichlorobenzaldehyde and for reducing the glycine compound using either SnCl2 or a specially defined catalyst. A cyclization method to form Anagrelide base from the corresponding iminoquinazoline compound is further provided.

Abstract translation: 提供了从2,3-二氯苯甲醛制备阿那格雷碱的方法。 还提供了一种制备中间体化合物N-（2,3-二氯-6-硝基苄基）甘氨酸由2,3-二氯苯甲醛制备的乙腈和用于使用SnCl 2或特别定义的催化剂还原甘氨酸化合物的方法。 进一步提供了从相应的亚氨基喹唑啉化合物形成阿那格雷碱的环化方法。

公开(公告)号：US5962488A

公开(公告)日：1999-10-05

申请号：US57260

申请日：1998-04-08

Applicant: Philip C. Lang

Inventor： Philip C. Lang

IPC: C07D261/06 ,  A61K31/42 ,  A61K47/12 ,  A61P1/00 ,  C07D413/04

CPC classification number: A61K31/42

Abstract: Chemically stable pharmaceutical formulations comprising a therapeutically effective amount of a material of formula I are provided which formulations contain a stabilizer system comprising an organic carboxylic acid containing more than 1 carboxylic acid group and an antioxidant. The preferred organic carboxylic acid is citric acid and the preferred antioxidants are ascorbic acid and butylated hydroxytoluene, which antioxidants are preferred to be used in admixture. The chemically stable pharmaceutical formulations are particularly useful for treating Irritable Bowel Syndrome (IBS) in mammals and comprises administering to the mammal needing treatment an effective dose of the above chemically stable pharmaceutical formulation. The stabilizer system is also effective for use in other pharmaceutical formulations containing active ingredients having oxidizable groups such as amino, phenolic, hydryoxyl amino, aldehyde, unsaturated compounds, sulfoxide, sulfone and mercapto. The preferred Formula I compound is as follows: ##STR1## wherein R and R.sup.1 are propyl; R.sub.2 and R.sub.3 are hydrogen; Y is CH.sub.2 and the compound is an HCl salt.

Abstract translation: 提供包含治疗有效量的式I的物质的化学稳定的药物制剂，其中哪些制剂含有包含含有多于1个羧酸基团的有机羧酸和抗氧化剂的稳定剂体系。 优选的有机羧酸是柠檬酸，优选的抗氧化剂是抗坏血酸和丁基化羟基甲苯，该抗氧化剂优选用于混合物。 化学稳定的药物制剂特别可用于治疗哺乳动物中的肠易激综合征（IBS），并且包括向需要治疗的哺乳动物施用有效剂量的上述化学稳定的药物制剂。 稳定剂体系也可用于含有具有可氧化基团的活性成分的其他药物制剂，例如氨基，酚，羟基氧基氨基，醛，不饱和化合物，亚砜，砜和巯基。 优选的式I化合物如下：其中R和R 1是丙基; R2和R3是氢; Y是CH 2，该化合物是HCl盐。