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1. 发明授权

US5618816A Antimigraine 1,2,5-thiadiazole derivatives of indolylalkyl-pyridnyl and pyrimidinylpiperazines 失效
标题翻译：吲哚烷基 - 吡啶基和嘧啶基哌嗪的反映异构体1,2,5-噻二唑衍生物
公开(公告)号：US5618816A
公开(公告)日：1997-04-08
申请号：US396825
申请日：1995-03-02
申请人： Ronnie R. Crenshaw , Edward H. Ruediger , David W. Smith , Carola Solomon , Joseph P. Yevich
发明人： Ronnie R. Crenshaw , Edward H. Ruediger , David W. Smith , Carola Solomon , Joseph P. Yevich
IPC分类号： C07D417/12 , A61K31/41 , A61K31/495 , A61K31/496 , A61K31/505 , A61P25/04 , A61P25/06 , C07D403/14 , C07D417/14
CPC分类号： C07D417/14
摘要： A series of novel 5-(3,4-diamino-1,2,5-thiadiazole and S-oxide) derivatives of indolylalkylpiperazinyl pyridines and pyrimidines of Formula I are intended for use in the alleviation of vascular headaches. ##STR1## In Formula I, X is selected from S, SO and SO.sub.2.
摘要翻译：吲哚基烷基哌嗪基吡啶的新型5-（3,4-二氨基-1,2,5-噻二唑和S-氧化物）衍生物和式I的嘧啶的一系列用于减轻血管性头痛。在式I中，X选自S，SO和SO 2。

2. 发明授权

US4528377A Substituted 3,4-diamino-1,2,5-thiadiazoles having histamine H.sub.2 -receptor antagonist activity 失效
标题翻译：具有组胺H2受体拮抗剂活性的取代的3,4-二氨基-1,2,5-噻二唑
公开(公告)号：US4528377A
公开(公告)日：1985-07-09
申请号：US473791
申请日：1983-03-16
申请人： Ronnie R. Crenshaw , Aldo A. Algieri
发明人： Ronnie R. Crenshaw , Aldo A. Algieri
IPC分类号： C07D285/10 , C07D417/12 , C07D417/10
CPC分类号： C07D285/10 , C07D417/12
摘要： Histamine H.sub.2 -receptor antagonists of the formula ##STR1## wherein A, m, Z, n and R.sup.1 are as defined herein, and their nontoxic pharmaceutically acceptable salts, hydrates and solvates are novel anti-ulcer agents which are prepared by ring closure of a substituted ethanediimidamide of the formula ##STR2## .
摘要翻译：式（I）其中A，m，Z，n和R 1如本文所定义的组胺H2受体拮抗剂及其无毒的药学上可接受的盐，水合物和溶剂合物是新的抗溃疡剂，其通过闭环式II的取代的乙二亚胺酰胺。

3. 发明授权

US4528375A Substituted 3,4-diamino-1,2,5-thiadiazoles having histamine H.sub.2 -receptor antagonist activity 失效
公开(公告)号：US4528375A
公开(公告)日：1985-07-09
申请号：US600880
申请日：1984-04-16
申请人： Ronnie R. Crenshaw , Aldo A. Algieri
发明人： Ronnie R. Crenshaw , Aldo A. Algieri
IPC分类号： C07D285/10 , C07D417/12 , C07D417/14 , C07D419/12 , C07D419/14
CPC分类号： C07D285/10 , C07D417/12
摘要： Histamine H.sub.2 -receptor antagonists of the formula ##STR1## wherein A, m, Z, n and R.sup.1 are as defined herein, and their nontoxic pharmaceutically acceptable salts, hydrates and solvates are novel anti-ulcer agents which are prepared by ring closure of a substituted ethanediimidamide of the formula ##STR2##

4. 发明授权

US4522943A Chemical compounds 失效
标题翻译：化合物
公开(公告)号：US4522943A
公开(公告)日：1985-06-11
申请号：US369971
申请日：1982-04-21
申请人： Aldo A. Algieri , Ronnie R. Crenshaw
发明人： Aldo A. Algieri , Ronnie R. Crenshaw
IPC分类号： C07D209/48 , C07D211/46 , C07D211/70 , C07D213/38 , C07D213/61 , C07D213/64 , C07D295/096 , C07D307/52 , C07D333/20 , C07D211/06 , A61K31/445 , A61K31/55 , C07D295/10
CPC分类号： C07D209/48 , C07D211/46 , C07D211/70 , C07D213/38 , C07D213/61 , C07D213/64 , C07D295/096 , C07D307/52 , C07D333/20
摘要： Compounds of the formula ##STR1## wherein R.sup.12 is a leaving group, Z is S, O or CH.sub.2 and A is a phenyl, furyl, thienyl or pyridyl ring substituted by a ##STR2## moiety, in which R.sup.8 and R.sup.9 are various substituents or, when taken together with the nitrogen, may be a specified heterocyclic ring, are intermediates in the preparation of histamine H.sub.2 -antagonist anti-ulcer agents of the formula ##STR3## in which R.sup.1 and R.sup.2 are any of several specified substituents.
摘要翻译：其中R 12是离去基团的化合物，Z是S，O或CH 2，A是被一个或多个取代基取代的苯基，呋喃基，噻吩基或吡啶基，其中R8和R9是各种取代基或当与氮一起使用时，可以是指定的杂环，是制备式“IMAGE”的组胺H2拮抗剂抗溃疡剂的中间体，其中R1和R2是若干指定取代基中的任何一个。

5. 发明授权

US4289876A Antisecretory agents 失效
标题翻译：防雾剂
公开(公告)号：US4289876A
公开(公告)日：1981-09-15
申请号：US129158
申请日：1980-03-10
申请人： Aldo A. Algieri , Ronnie R. Crenshaw
发明人： Aldo A. Algieri , Ronnie R. Crenshaw
IPC分类号： C07D213/32 , C07D213/28
CPC分类号： C07D213/32
摘要： Compounds of the formula ##STR1## wherein R.sup.1 is a straight or branched chain alkynyl group containing from 3 to 9 carbon atoms, inclusive; R.sup.2 is hydrogen, hydroxy, cyano, (lower)alkyl, (lower)alkoxy, halogen or amino; n is 2 or 3; X is NR.sup.3 or CHR.sup.3 ; R.sup.3 is cyano, nitro, SO.sub.2 Ar; or SO.sub.2 (lower)alkyl; R.sup.12 is hydrogen or (CH.sub.2).sub.p NR.sup.13 R.sup.14 ; p is an integer of from 1 to 4, inclusive; R.sup.13 and R.sup.14 each are independently hydrogen or (lower)alkyl; and Ar is phenyl or phenyl containing 1 or 2 substituents independently selected from halogen and (lower)alkyl; and nontoxic, pharmaceutically acceptable salts thereof, are potent anti-ulcer agents.
摘要翻译：式Ⅰ的化合物，其中R 1是含有3至9个碳原子的直链或支链炔基，包括端值; R2是氢，羟基，氰基，（低级）烷基，（低级）烷氧基，卤素或氨基; n为2或3; X是NR 3或CHR 3; R3是氰基，硝基，SO2Ar; 或SO 2（低级）烷基; R12是氢或（CH2）pNR13R14; p是1至4的整数，包括1和4; R 13和R 14各自独立地为氢或（低级）烷基; 和Ar是苯基或含有1或2个独立地选自卤素和（低级）烷基的取代基的苯基; 和无毒的药学上可接受的盐是有效的抗溃疡剂。

6. 发明授权

US4157347A N-cyano isothioureas 失效
标题翻译： N-氰基异硫脲
公开(公告)号：US4157347A
公开(公告)日：1979-06-05
申请号：US936668
申请日：1978-08-24
申请人： Ronnie R. Crenshaw , George M. Luke
发明人： Ronnie R. Crenshaw , George M. Luke
IPC分类号： C07C335/38 , A61K31/415 , A61P1/00 , A61P1/04 , C07C67/00 , C07C313/00 , C07C323/44 , C07C325/00 , C07D233/54 , C07D233/64 , C07D277/64 , C07C125/08
CPC分类号： C07D233/64 , C07C323/44 , C07D277/64
摘要： Anti-ulcer agents of the formula ##STR1## wherein R.sup.1 is a straight or branched chain alkynyl group containing from 3 to 9 carbon atoms, inclusive, and non-toxic pharmaceutically acceptable acid addition salts thereof, are prepared by reacting a compound of the formula ##STR2## with a compound of the formula ##STR3## wherein R.sup.1 is as defined above and R.sup.5 is (lower)alkyl, phenylalkyl or phenyl containing 1 or 2 substituents independently selected from nitro, chloro and bromo. The intermediates of Formula IV may be prepared by reacting the desired alkynylamine with a compound of the formula(R.sup.5 S).sub.2 C.dbd.NCN Vin which R.sup.5 is as described above.
摘要翻译：其中R 1为含有3至9个碳原子的直链或支链炔基，及其无毒的药学上可接受的酸加成盐的式ⅠA抗溃疡剂通过使式其中R 1如上所定义，R 5是（低级）烷基，苯基烷基或含有1或2个独立地选自硝基，氯和溴的取代基的苯基的式（III）化合物。式IV的中间体可以通过使所需的炔基胺与式（R5S）2C = NCNV的化合物反应来制备，其中R 5如上所述。

7. 发明授权

US4528378A Substituted 3,4-diamino-1,2,5-thiadiazoles having histamine H.sub.2 -receptor antagonist activity 失效
公开(公告)号：US4528378A
公开(公告)日：1985-07-09
申请号：US600744
申请日：1984-04-16
申请人： Ronnie R. Crenshaw , Aldo A. Algieri
发明人： Ronnie R. Crenshaw , Aldo A. Algieri
IPC分类号： C07D285/10 , C07D417/12 , C07D417/14 , C07D419/14 , C07D419/12
CPC分类号： C07D285/10 , C07D417/12
摘要： Histamine H.sub.2 -receptor antagonists of the formula ##STR1## wherein A, m, Z, n and R.sup.1 are as defined herein, and their nontoxic pharmaceutically acceptable salts, hydrates and solvates are novel anti-ulcer agents which are prepared by ring closure of a substituted ethanediimidamide of the formula ##STR2##

8. 发明授权

US4390701A 1-Amino-2-[3-(3-piperidinomethylphenoxy)propylamino]cyclobutene-3,4-dione 失效
标题翻译： 1-氨基-2- [3-（3-哌啶基甲基苯氧基）丙基氨基]环丁烯-3,4-二酮
公开(公告)号：US4390701A
公开(公告)日：1983-06-28
申请号：US264533
申请日：1981-05-18
申请人： Aldo A. Algieri , Ronnie R. Crenshaw
发明人： Aldo A. Algieri , Ronnie R. Crenshaw
IPC分类号： A61K31/135 , A61K31/10 , A61K31/13 , A61K31/132 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/395 , A61K31/40 , A61K31/435 , A61K31/4402 , A61K31/4406 , A61K31/4418 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/5375 , A61K31/54 , A61P1/04 , A61P43/00 , C07C67/00 , C07C213/00 , C07C225/20 , C07C253/00 , C07C255/24 , C07C313/00 , C07C319/20 , C07C323/25 , C07C323/29 , C07C323/32 , C07C323/52 , C07D209/48 , C07D211/46 , C07D211/70 , C07D213/38 , C07D213/61 , C07D213/64 , C07D213/73 , C07D213/74 , C07D233/64 , C07D295/00 , C07D295/08 , C07D295/096 , C07D295/12 , C07D307/52 , C07D333/20 , C07D417/12
CPC分类号： C07D209/48 , C07D211/46 , C07D211/70 , C07D213/38 , C07D213/61 , C07D213/64 , C07D295/096 , C07D307/52 , C07D333/20 , Y10S514/927
摘要： Certain 1-(substituted amino)-2-(amino or substituted amino)cyclobutene-3,4-diones are potent histamine H.sub.2 -antagonists useful in the treatment of peptic ulcers.
摘要翻译：某些1-（取代氨基）-2-（氨基或取代的氨基）环丁烯-3,4-二酮是用于治疗消化性溃疡的有效组胺H2拮抗剂。

9. 发明授权

US4380639A Substituted 1,2,5-thiadiazole derivatives 失效
标题翻译：取代的1,2,5-噻二唑衍生物
公开(公告)号：US4380639A
公开(公告)日：1983-04-19
申请号：US276606
申请日：1981-06-23
申请人： Ronnie R. Crenshaw , Aldo A. Algieri
发明人： Ronnie R. Crenshaw , Aldo A. Algieri
IPC分类号： C07D213/38 , C07D213/81 , C07D271/06 , C07D271/08 , C07D271/10 , C07D277/28 , C07D277/40 , C07D277/42 , C07D277/48 , C07D277/56 , C07D285/10 , C07D307/52
CPC分类号： C07D213/81 , C07D213/38 , C07D271/06 , C07D271/08 , C07D271/10 , C07D277/28 , C07D277/40 , C07D277/42 , C07D277/48 , C07D277/56 , C07D285/10 , C07D307/52 , Y10S514/927
摘要： Histamine H.sub.2 -antagonists of the formula ##STR1## wherein p is 1 or 2; R.sup.1 is hydroxy, amino, substituted amino or a 5- to 9-membered fully saturated nitrogen-containing heterocyclic ring attached via its nitrogen atom; m is an integer of from 0 to 2; n is an integer of from 2 to 4; Z is sulfur, oxygen or methylene; and A is an optionally substituted phenyl, imidazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, triazolyl, thiadiazolyl, oxadiazolyl, furyl, thienyl or pyridyl ring; and nontoxic pharmaceutically acceptable salts, hydrates, solvates or N-oxides thereof are novel anti-ulcer agents. Intermediates and processes for their preparation are disclosed.
摘要翻译：组氨酸H2拮抗剂，其中p为1或2; R1是通过其氮原子连接的羟基，氨基，取代的氨基或5至9元饱和的含氮杂环; m为0〜2的整数; n为2〜4的整数， Z是硫，氧或亚甲基; 并且A是任选取代的苯基，咪唑基，噻唑基，异噻唑基，恶唑基，异恶唑基，三唑基，噻二唑基，恶二唑基，呋喃基，噻吩基或吡啶基环。和无毒的药学上可接受的盐，水合物，溶剂合物或N-氧化物是新的抗溃疡剂。公开了中间体及其制备方法。

10. 发明授权

US4380638A Chemical compounds 失效
公开(公告)号：US4380638A
公开(公告)日：1983-04-19
申请号：US276602
申请日：1981-06-23
申请人： Ronnie R. Crenshaw , Aldo A. Algieri
发明人： Ronnie R. Crenshaw , Aldo A. Algieri
IPC分类号： C07D213/38 , C07D213/81 , C07D271/06 , C07D271/08 , C07D271/10 , C07D277/28 , C07D277/40 , C07D277/42 , C07D277/48 , C07D277/56 , C07D285/10 , C07D307/52
CPC分类号： C07D213/81 , C07D213/38 , C07D271/06 , C07D271/08 , C07D271/10 , C07D277/28 , C07D277/40 , C07D277/42 , C07D277/48 , C07D277/56 , C07D285/10 , C07D307/52 , Y10S514/927
摘要： Histamine H.sub.2 -antagonists of the formula ##STR1## wherein p is 1 or 2; R.sup.1 is hydroxy, amino, substituted amino or a 5- to 9-membered fully saturated nitrogen-containing heterocyclic ring attached via its nitrogen atom; m is an integer of from 0 to 2; n is an integer of from 2 to 4; Z is sulfur, oxygen or methylene; and A is an optionally substituted phenyl, imidazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, triazolyl, thiadiazolyl, oxadiazolyl, furyl, thienyl or pyridyl ring; and nontoxic pharmaceutically acceptable salts, hydrates, solvates or N-oxides thereof are novel anti-ulcer agents. Intermediates and processes for their preparation are disclosed.

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