知搜-全球专利检索

  1. Login
  2. Sign Up

Search Results

24 records (took 0.027 seconds)

    (dl)-16-Phenoxy- and 16-substituted phenoxy-9-keto prostatrienoic acid derivatives and processes for the production thereof
    2.
    发明授权
    (dl)-16-Phenoxy- and 16-substituted phenoxy-9-keto prostatrienoic acid derivatives and processes for the production thereof 失效
    （dl）-16-苯氧基 - 和16-取代的苯氧基-9-酮前列腺烯酸衍生物及其制备方法

    公开(公告)号：US4178457A

    公开(公告)日：1979-12-11

    申请号：US922957

    申请日：1978-07-10

    Applicant: Albert R. Van Horn ,  Gabriel Garay ,  John A. Edwards

    Inventor： Albert R. Van Horn ,  Gabriel Garay ,  John A. Edwards

    IPC: A61K31/23 ,  A61K31/557 ,  A61K31/5575 ,  A61P1/04 ,  A61P43/00 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07C177/00

    CPC classification number: C07C405/00 ,  Y02P20/582

    Abstract: Novel 16-phenoxy and 16-(o, m or p)-substituted phenoxy derivatives of (dl)-9-keto-11.alpha.,15.alpha.-dihydroxy-17,18,19,20-tetranorprosta-4,5,13-trans-trienoic acid, the pharmaceutically acceptable, non-toxic lower alkyl esters and salts thereof and processes for the production of such compounds. These compounds possess prostaglandin-like activities and thus are useful in the treatment of mammals where prostaglandins are indicated. They are particularly useful as inhibitors of gastric acid secretion; and as agents for the control of asthmatic attack, because of their bronchodilating activity.

    Abstract translation: （dl）-9-酮-11α，15α-二羟基-17,18,19,20-四前列腺素-4,5,13的新的16-苯氧基和16-（o，m或p） - 取代的苯氧基衍生物 - 反式三烯酸，其药学上可接受的，无毒的低级烷基酯及其盐及其制备方法。 这些化合物具有前列腺素样活性，因此可用于治疗表达前列腺素的哺乳动物。 它们特别可用作胃酸分泌抑制剂; 并且作为控制哮喘发作的药剂，因为它们的支气管扩张活性。

    1,5(6)-Disubstituted benzimidazole-2-carbamate derivatives having anthelmintic activity
    3.
    发明授权
    1,5(6)-Disubstituted benzimidazole-2-carbamate derivatives having anthelmintic activity 失效
    1,5（6）具有驱虫活性的二取代苯并咪唑-2-氨基甲酸酯衍生物

    公开(公告)号：US4031234A

    公开(公告)日：1977-06-21

    申请号：US697499

    申请日：1976-06-18

    Applicant: Colin C. Beard ,  John A. Edwards ,  John H. Fried

    Inventor： Colin C. Beard ,  John A. Edwards ,  John H. Fried

    IPC: A61K31/415

    Abstract: This application relates to 1,5(6)-disubstituted benzimidazole-2-carbamate derivatives represented by the following formula: ##STR1## where R is lower alkyl having 1 to 4 carbon atoms; R.sup.1 is --SOR.sup.2, --SR.sup.5, --OR.sup.5 or M'(CH.sub.2).sub.n MR.sup.7 ; R.sup.2 is lower alkyl having from 1 to 6 carbon atoms, cycloalkyl having 3 to 7 carbon atoms, lower alkenyl or lower alkynyl having 3 to 6 carbon atoms, or aralkyl or aryl; R.sup.5 is lower alkenyl, lower alkynyl or aralkyl; R.sup.7 is lower alkyl having 1 to 4 carbon atom, or aryl; M and M' are independently O, S, ##STR2## n is 1-4; and R.sup.8 is lower alkyl having 1 to 12 carbon atoms optionally substituted with a --COOR group where R is lower alkyl having 1 to 4 carbon atoms, aryl or aralkyl. The R.sup.1 substitution is at the 5(6)-position.The compounds are useful as pesticides, particularly as anthelmintic and antifungal agents.

    Abstract translation: 本申请涉及由下式表示的1,5（6） - 二取代的苯并咪唑-2-氨基甲酸酯衍生物：其中R是具有1至4个碳原子的低级烷基; R 1是-SOR 2，-SR 5，-OR 5或M'（CH 2）nMR 7; R2是具有1至6个碳原子的低级烷基，具有3至7个碳原子的环烷基，具有3至6个碳原子的低级链烯基或低级炔基，或芳烷基或芳基; R5是低级烯基，低级炔基或芳烷基; R7是具有1至4个碳原子的低级烷基，或芳基; M和M'独立地为O，S，n为1-4; R8是具有1〜12个碳原子的低级烷基，任选被-COOR基团取代，其中R是具有1-4个碳原子的低级烷基，芳基或芳烷基。 R1取代为5（6）位。

    Clinical Applications of Tetrahydrobiopterin, Lipoic Acid and Their Salts and Methods of Preparing Tetrahydrobiopterin Bis-Lipoate
    5.
    发明申请
    Clinical Applications of Tetrahydrobiopterin, Lipoic Acid and Their Salts and Methods of Preparing Tetrahydrobiopterin Bis-Lipoate 审中-公开
    四氢生物喋呤，硫辛酸及其盐的临床应用及制备四氢生物蝶呤双脂肪酸酯的方法

    公开(公告)号：US20090068264A1

    公开(公告)日：2009-03-12

    申请号：US12268244

    申请日：2008-11-10

    Applicant: Kenneth T. Richardson ,  Don C. Pearson ,  John A. Edwards

    Inventor： Kenneth T. Richardson ,  Don C. Pearson ,  John A. Edwards

    IPC: A61K9/24 ,  A61K31/4985 ,  A61P3/10 ,  A61P3/00 ,  A61P3/06

    CPC classification number: A61K31/385 ,  A61K31/519 ,  A61K2300/00

    Abstract: Dosage forms and methods of use are disclosed for: a) the simultaneous administration of tetrahydrobiopterin (BH4) or a derivative, homolog or precursor thereof and lipoic acid (LA), or dihydrolipoic acid (DHLA), or a derivative, homolog or salt thereof or, b) the administration of a conjugate consisting of tetrahydrobiopterin bis-lipoate (TBL). The invention is useful for the amelioration of diabetes mellitus types 1 and 2 (including impaired glucose tolerance, pre-diabetes, insulin resistance, metabolic syndrome X and as an adjunct to oral antidiabetic agents and/or insulin), diabetic and non-diabetic microvascular diseases (including nephropathy, neuropathy and retinopathy), diabetic and non-diabetic macrovascular diseases (including heart attack, stroke, peripheral vascular disease and ischemia-reperfusion injury), hypertension, vasoconstriction, obesity, dyslipedemia, and neurodegenerative disorders (including Parkinson's disease, mild cognitive impairment, senile dementia, Alzheimer's disease, hearing loss and chronic glaucomas). A novel method for the preparation of TBL is also disclosed.

    Abstract translation: 公开了剂量形式和使用方法：a）同时施用四氢生物喋呤（BH4）或其衍生物，同系物或其前体和硫辛酸（LA）或二氢硫辛酸（DHLA）或其衍生物，同系物或其盐 或b）施用由四氢生物蝶呤双油酸酯（TBL）组成的缀合物。 本发明可用于改善1型和2型糖尿病（包括葡萄糖耐量降低，前期糖尿病，胰岛素抵抗，代谢综合征X和作为口服抗糖尿病剂和/或胰岛素的辅助剂），糖尿病和非糖尿病微血管 糖尿病和非糖尿病大血管病（包括心脏病发作，中风，外周血管疾病和缺血再灌注损伤），高血压，血管收缩， 轻度认知障碍，老年痴呆，阿尔茨海默病，听力损失和慢性青光眼）。 还公开了一种制备TBL的新方法。

    Certain thiazole compounds
    6.
    发明授权
    Certain thiazole compounds 失效
    某些噻唑化合物

    公开(公告)号：US4089865A

    公开(公告)日：1978-05-16

    申请号：US718441

    申请日：1976-08-27

    Applicant: John A. Edwards

    Inventor： John A. Edwards

    IPC: A61K31/425 ,  C07D417/12

    CPC classification number: C07D417/12 ,  A61K31/425

    Abstract: 1-Amino-3-(4- or 5-substituted thiazol-2-oxy)-2-propanol and/or substituted amino derivatives thereof; 3-(4- or 5-substituted thiazol-2-oxy)-1,2-epoxypropane and 5-(4- or 5-substituted thiazol-2-oxymethylene)-oxazolidine and/or N- and/or 2-substituted oxazolidine derivatives thereof, and methods of making such compounds. The compounds are characterized by an aminocarbonyl or carbonylamino type substituent at the 5- or 4-position on the thiazole ring. The above 1-amino-3-(4- or 5-substituted thiazol-2-oxy)-2-propanol and derivatives exhibit cardiovascular activity and are useful in the treatment of abnormal heart conditions in mammals. The 3-(4- or 5-substituted thiazol-2-oxy)-1,2-epoxypropanes are useful as intermediates for the aforementioned cardiovascular agents. The 5-(4- or 5-substituted thiazol-2-oxymethylene)-oxazolidine and derivatives are intermediates for the aforementioned cardiovascular agents and further exhibit cardiovascular activity and thus are useful in the treatment of abnormal heart conditions in mammals. The 1-amino-3-(4- or 5-substituted thiazol-2-oxy)-2-propanol and derivatives can be prepared by base or acid hydrolysis of the corresponding 5-(4- or 5-aminocarbonylthiazol-2-oxymethylene)-oxazolidine or derivative; or by treatment of the corresponding 3-(4- or 5-substituted thiazol-2-oxy)-2,3-epoxypropane or derivative with the desired amine or amine derivative.

    Abstract translation: 1-氨基-3-（4-或5-取代的噻唑-2-氧）-2-丙醇和/或其取代的氨基衍生物; 3-（4-或5-取代的噻唑-2-氧基）-1,2-环氧丙烷和5-（4-或5-取代的噻唑-2-甲醛） - 恶唑烷和/或N-和/或2-取代 恶唑烷衍生物及其制备方法。 该化合物的特征在于噻唑环上5-或4-位上的氨基羰基或羰基氨基取代基。 上述1-氨基-3-（4-或5-取代的噻唑-2-氧基）-2-丙醇及其衍生物具有心血管活性，可用于治疗哺乳动物异常心脏病。 3-（4-或5-取代的噻唑-2-氧）-1,2-环氧丙烷可用作上述心血管药物的中间体。 5-（4-或5-取代的噻唑-2-甲醛）恶唑烷及其衍生物是上述心血管药物的中间体，并且进一步显示心血管活性，因此可用于治疗哺乳动物的异常心脏病。 1-氨基-3-（4-或5-取代的噻唑-2-氧基）-2-丙醇及其衍生物可以通过相应的5-（4-或5-氨基羰基噻唑-2-甲醛 ） - 恶唑烷或其衍生物; 或通过用所需的胺或胺衍生物处理相应的3-（4-或5-取代的噻唑-2-氧）-2,3-环氧丙烷或衍生物。

    Thio etianic acid derivatives
    9.
    发明授权
    Thio etianic acid derivatives 失效
    硫代乙酸衍生物

    公开(公告)号：US4310466A

    公开(公告)日：1982-01-12

    申请号：US206494

    申请日：1980-11-07

    Applicant: John A. Edwards

    Inventor： John A. Edwards

    IPC: C07J3/00 ,  C07J31/00 ,  C07J71/00 ,  A61K31/56 ,  C07J9/00

    CPC classification number: C07J3/005 ,  C07J31/006 ,  C07J71/0031

    Abstract: Certain 16.beta.-methyl-3-oxoandrost-4-ene and 16.beta.-methyl-3-oxoandrosta-1,4-diene 17.beta.-thiocarboxylic acid esters are useful as anti-inflammatory steroids. These compounds are optionally substituted at the 6.alpha.-position with fluoro or chloro; optionally substituted at the 9.alpha. position with fluoro, chloro or bromo; substituted at the 11 position with a keto, a .beta.-hydroxy or a .beta.-chloro (the latter only when there is a 9.alpha.-chloro); and substituted with 17.alpha.-hydroxy (or an ester thereof).

    Abstract translation: 某些16个β-甲基-3-氧代雄甾-4-烯和16个β-甲基-3-氧代雄甾-1,4-二烯17β-硫代羧酸酯可用作抗炎类固醇。 这些化合物任选在6位上被氟或氯取代; 任选在9α位被氟，氯或溴取代; 在11位置用酮，β-羟基或β-氯代替（后者仅在存在9α-氯的情况下）; 并用17α-羟基（或其酯）取代。

    5(6)-Benzene ring substituted benzimidazole-2-carbamate derivatives having anthelmintic activity
    10.
    发明授权
    5(6)-Benzene ring substituted benzimidazole-2-carbamate derivatives having anthelmintic activity 失效
    5（6）具有驱虫活性的苯并环取代的苯并咪唑-2-氨基甲酸酯衍生物

    公开(公告)号：US4080461A

    公开(公告)日：1978-03-21

    申请号：US729229

    申请日：1976-10-04

    Applicant: Colin C. Beard ,  John A. Edwards ,  John H. Fried

    Inventor： Colin C. Beard ,  John A. Edwards ,  John H. Fried

    IPC: C07D235/32 ,  A61K31/415

    CPC classification number: C07D235/32

    Abstract: Benzene ring substituted benzimidazole-2-carbamate derivatives represented by the formula: ##STR1## where R is a lower alkyl group having 1 to 4 carbon atoms; R.sup.1 is --SOR.sup.2, --SO.sub.2 R.sup.2, --SCN, --SR.sup.5, --OR.sup.5 or M'(CH.sub.2).sub.n MR.sup.7 where M and M' are independently O, S, ##STR2## R.sup.7 is lower alkyl having 1 to 4 carbon atoms or aryl, and n is 1-4; R.sup.2 is lower alkyl having from 1 to 6 carbon atoms, cycloalkyl having 3 to 7 carbon atoms, lower alkenyl or lower alkynyl having 3 to 6 carbon atoms, or aralkyl or aryl; andR.sup.5 is lower alkenyl, lower alkynyl, or aralkyl. The R.sup.1 substitution is at the 5(6)-position.The compounds are useful as pesticides, particularly as anthelmintic and antifungal agents.

    Abstract translation: 由下式表示的苯环取代的苯并咪唑-2-氨基甲酸酯衍生物：其中R是具有1至4个碳原子的低级烷基; R1是-SOR2，-SO2R2，-SCN，-SR5，-OR5或M'（CH2）nMR7，其中M和M'独立地是O，S，R7是具有1-4个碳原子的低级烷基或芳基， n为1-4; R2是具有1至6个碳原子的低级烷基，具有3至7个碳原子的环烷基，具有3至6个碳原子的低级链烯基或低级炔基，或芳烷基或芳基; 并且R 5为低级链烯基，低级炔基或芳烷基。 R1取代为5（6）位。

Patent Agency Ranking