公开(公告)号：US4652556A

公开(公告)日：1987-03-24

申请号：US767009

申请日：1985-08-19

申请人： Joseph E. Moore ,  Yuh-Lin Yang ,  Robert K. Griffith ,  David C. K. Chan

发明人： Joseph E. Moore ,  Yuh-Lin Yang ,  Robert K. Griffith ,  David C. K. Chan

IPC分类号： A01N41/06 ,  A01N43/10 ,  A01N47/04 ,  C07C313/18 ,  C07D333/24 ,  C07C143/72

CPC分类号： C07C255/00 ,  A01N41/06 ,  A01N43/10 ,  A01N47/04 ,  C07D333/24

摘要： Compounds of the formula: ##STR1## wherein R is aryl of 6 to 12 carbon atoms or aralkyl of 7 to 14 carbon atoms either optionally substituted with 1 to 3 substituents independently selected from lower alkyl of 1 to 6 carbon atoms, lower alkoxy of 1 to 6 carbon atoms, lower alkylthio of 1 to 6 carbon atoms, lower alkylsulfinyl of 1 to 6 carbon atoms, lower alkylsulfonyl of 1 to 6 carbon atoms, halogen, trihalomethyl, nitro, cyano or carboxyl; alkyl of 1 to 10 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, lower alkenyl of 2 to 6 carbon atoms, or lower alkynyl of 2 to 6 carbon atoms, all optionally substituted with 1 to 3 halogen atoms; lower alkoxyalkylene; lower alkylene carbalkoxy; lower alkylthioalkylene; lower alkylsulfinylalkylene; or lower alkylsulfonylalkylene; R.sup.1 and R.sup.2 are independently hydrogen, lower alkyl of 1 to 6 carbon atoms, aryl of 6 to 12 carbon atoms, or thienyl, or taken together form an alkylene bridge to give a cycloalkyl group of 3 to 10 carbon atoms; and R.sup.3 is alkyl of 1 to 3 carbon atoms substituted with 3 to 6 halogen atoms or trihalovinyl are fungicidal.

摘要翻译： 下式的化合物：其中R为6至12个碳原子的芳基或7至14个碳原子的芳烷基，任选被1至3个独立地选自1至6个碳原子的低级烷基的取代基取代，1个低级烷氧基 1-6个碳原子的低级烷硫基，1至6个碳原子的低级烷基亚磺酰基，1至6个碳原子的低级烷基磺酰基，卤素，三卤甲基，硝基，氰基或羧基; 具有1至10个碳原子的烷基，3至10个碳原子的环烷基，2至6个碳原子的低级烯基或2至6个碳原子的低级炔基，全部可被1至3个卤素原子取代; 低级烷氧基亚烷基; 低级亚烷基烷氧基; 低级烷硫基亚烷基; 低级烷基亚磺酰基亚烷基; 或低级烷基磺酰基亚烷基; R 1和R 2独立地为氢，1至6个碳原子的低级烷基，6至12个碳原子的芳基或噻吩基，或一起形成亚烷基桥，得到3至10个碳原子的环烷基; R3为被3〜6个卤素原子取代的1〜3个碳原子的烷基或三卤乙烯基是杀真菌剂。

公开(公告)号：US6046229A

公开(公告)日：2000-04-04

申请号：US3317

申请日：1998-01-06

申请人： Ching Te Chang ,  Yuh-Lin Yang

发明人： Ching Te Chang ,  Yuh-Lin Yang

IPC分类号： C07D333/16 ,  C07D333/20 ,  C07D333/22 ,  A01N43/10 ,  C07D333/32 ,  C07D333/36 ,  C07D49/10

CPC分类号： C07D333/20 ,  C07D333/16 ,  C07D333/22

摘要： A compound of the formula:Ar.sub.1 --B--Ar.sub.2wherein Ar.sub.1 is unsubstituted or substituted phenyl, thienyl, furanyl, or pyrrolyl, in which each substituent of the substituted phenyl, substituted thienyl, substituted furanyl, and substituted pyrrolyl, independently, is aldehyde, acyl, ester, carboxyl, amido, nitrile, nitro, cyano, acetal, ketal, oxoalkyl, aminoalkyl, hydroxyalkyl, haloalkyl, iminoalkyl, acid halide, aminoalkylaminoalkyl, aminoalkylaminoalkylamino, hydroxyalkylaminoalkyl, or hydroxyalkylaminoalkylaminoalkyl; B is, --CH.dbd.CH--, or --C C--, in which R is H, alkyl, hydroxyl, alkoxy, ester, aldehyde, hydroxyalkyl, aminoalkyl, carboxyl, --CH(OR.sub.1).sub.2, or NR.sub.2 R.sub.3, where each R.sub.1, independently, is H, alkyl, or acyl; and each of R.sub.2 and R.sub.3, independently, is H, alkyl, hydroxyalkyl, or aminoalkyl; and Ar.sub.2 is substituted phenyl, substituted thienyl, substituted furanyl, or substituted pyrrolyl, in which each substituent of the substituted phenyl, substituted thienyl, substituted furanyl, and substituted pyrrolyl, independently, is amido, nitrile, nitro, cyano, acetal, ketal, oxoalkyl, aminoalkyl, haloalkyl, iminoalkyl, acid halide, aminoalkylaminoalkyl, aminoalkylaminoalkylamino, hydroxyalkylaminoalkyl, or hydroxyalkylaminoalkylaminoalkyl; or a salt thereof. Also disclosed is a composition which contains a pharmaceutical acceptable carrier and an effective amount of a compound of the above formula.

摘要翻译： 式中Ar1-B-Ar2的化合物是未取代或取代的苯基，噻吩基，呋喃基或吡咯基，其中取代的苯基，取代的噻吩基，取代的呋喃基和取代的吡咯基的各取代基独立地为醛，酰基 ，酯，羧基，酰氨基，腈，硝基，氰基，缩醛，缩酮，氧代烷基，氨基烷基，羟基烷基，卤代烷基，亚氨基烷基，酰卤，氨基烷基氨基烷基，氨基烷基氨基烷基氨基，羟基烷基氨基烷基或羟烷基氨基烷基氨基烷基。 B是-CH = CH-或-C≡C，其中R是H，烷基，羟基，烷氧基，酯，醛，羟基烷基，氨基烷基，羧基，-CH（OR 1）2或NR 2 R 3， 独立地是H，烷基或酰基; R 2和R 3各自独立地为H，烷基，羟基烷基或氨基烷基; 并且Ar 2是取代的苯基，取代的噻吩基，取代的呋喃基或取代的吡咯基，其中取代的苯基，取代的噻吩基，取代的呋喃基和取代的吡咯基的各取代基独立地是酰氨基，腈，硝基，氰基，缩醛，缩酮， 氧代烷基，氨基烷基，卤代烷基，亚氨基烷基，酰卤，氨基烷基氨基烷基，氨基烷基氨基烷基氨基，羟基烷基氨基烷基或羟烷基氨基烷基氨基烷基; 或其盐。 还公开了含有药学上可接受的载体和有效量的上式化合物的组合物。

公开(公告)号：US6002021A

公开(公告)日：1999-12-14

申请号：US106278

申请日：1998-06-29

申请人： Yuh-Lin Yang ,  Yeuk-Chuen Liu

发明人： Yuh-Lin Yang ,  Yeuk-Chuen Liu

IPC分类号： C07D309/30 ,  C07F7/18

CPC分类号： C07F7/1892 ,  C07D309/30 ,  Y02P20/55

摘要： An acylation process using a sulfonic acid, a salt of the sulfonic acid, or a mixture thereof, as a catalyst. Compound 6 is prepared by protecting the 4-hydroxyl group on the pyranone ring of the 8'-hydroxy compound 2 to form a .beta.-protected compound 3, acylating the 8-hydroxy group on the polyhydronaphthyl ring of compound 3 to give protected ester, compound 4, then removing the protecting group, where the compounds 6, 2, 3 and 4 are as described in the specification.

摘要翻译： 使用磺酸，磺酸的盐或其混合物作为催化剂的酰化方法。 通过保护8'-羟基化合物2的吡喃酮环上的4-羟基以形成β-保护的化合物3，酰化化合物3的多羟基萘基上的8-羟基，得到保护的酯，制备化合物6， 化合物4，然后除去保护基，其中化合物6,2,3和4如说明书中所述。

公开(公告)号：US5994566A

公开(公告)日：1999-11-30

申请号：US106277

申请日：1998-06-29

申请人： Yuh-Lin Yang ,  Yeuk-Chuen Liu

发明人： Yuh-Lin Yang ,  Yeuk-Chuen Liu

IPC分类号： C07D309/30

CPC分类号： C07D309/30

摘要： The process for preparing compound 2 by reacting the compound 1, each as described in the specification hereof, with a tetraalkyl ammonium hydroxide having the formula R.sub.1 R.sub.2 R.sub.3 R.sub.4 N.sup.+ OH.sup.-, wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently a C.sub.1 -C.sub.10 alkyl group or a (C.sub.6 -C.sub.10) aryl (C.sub.1 -C.sub.10) alkyl group, to obtain an triol carboxylate thereof, acidifying the triol carboxylate, then lactonizing the product to obtain diol lactone, a key intermediate for production of antihypercholesterolemia agents.

摘要翻译： 通过使本说明书中所述化合物1与式R1R2R3R4N + OH-的四烷基氢氧化铵反应来制备化合物2的方法，其中R 1，R 2，R 3和R 4各自独立地为C 1 -C 10烷基 或（C 6 -C 10）芳基（C 1 -C 10）烷基，得到其三羧酸羧酸酯，酸化三醇羧酸酯，然后将产物内酯化，得到二醇内酯，其是生产抗高胆固醇血症药物的关键中间体。

公开(公告)号：US5994394A

公开(公告)日：1999-11-30

申请号：US821472

申请日：1997-03-21

申请人： Ching Te Chang ,  Yuh-Lin Yang

发明人： Ching Te Chang ,  Yuh-Lin Yang

IPC分类号： C07D307/46 ,  C07D409/14 ,  A61K31/34 ,  A61K31/38 ,  C07D307/36 ,  C07D307/40

CPC分类号： C07D409/14 ,  C07D307/46

摘要： The present invention relates to a group of polyheterocyclic compounds covered by the following formula: ##STR1## wherein each of X.sub.1, X.sub.2, X.sub.3, and X.sub.4, independently, is O, S, NH, or N(C.sub.1-6 alkyl), but one of them must be O, NH, or N(C.sub.1-6 alkyl); each of R.sub.1, R.sub.2, R.sub.5, and R.sub.6, independently, is H or a substituent (e.g., halogen, CN, NO.sub.2, or C.sub.1-4 haloalkyl), but at least one of them must be a substituent; each of R.sub.3 and R.sub.4, independently, is H, C.sub.1-6 alkyl, CHO, CH.sub.2 OH, or CH.sub.2 NH.sub.2 ; and each of m and n, independently, is 0 or 1.

摘要翻译： 本发明涉及由下式涵盖的一组多杂环化合物：其中X1，X2，X3和X4各自独立地为O，S，NH或N（C1-6烷基），但其中之一必须 是O，NH或N（C 1-6烷基）; R 1，R 2，R 5和R 6各自独立地是H或取代基（例如卤素，CN，NO 2或C 1-4卤代烷基），但它们中的至少一个必须是取代基; R 3和R 4各自独立地为H，C 1-6烷基，CHO，CH 2 OH或CH 2 NH 2; m和n各自独立地为0或1。