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1. 发明授权

US06639074B2 Process for preparing azacycloalkanoylaminothiazoles 有权
标题翻译：制备氮杂环烷酰氨基噻唑的方法
公开(公告)号：US06639074B2
公开(公告)日：2003-10-28
申请号：US10100129
申请日：2002-03-18
申请人： Bang-Chi Chen , Kyoung S. Kim , S. David Kimball , Raj N. Misra , Mark E. Salvati , Joseph E. Sundeen , Hai-Yun Xiao , Rulin Zhao
发明人： Bang-Chi Chen , Kyoung S. Kim , S. David Kimball , Raj N. Misra , Mark E. Salvati , Joseph E. Sundeen , Hai-Yun Xiao , Rulin Zhao
IPC分类号： C07D47100
CPC分类号： C07D417/12 , A61K31/427 , A61K31/454 , C07D231/12 , C07D233/56 , C07D249/08 , C07D417/14
摘要： The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I or a pharmaceutically acceptable salt thereof, wherein: R is alkyl, aryl or heteroaryl; R1, R2, R3, R4 and R5 are each independently hydrogen, alkyl, aryl or heteroaryl; R6 and R7 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; R8 is hydrogen, alkyl, aryl, heteroaryl, CONR9R10, COR11 or COOR12; R9, R10, R11 and R12 are each independently hydrogen, alkyl or aryl; m equals 0 to 5; and n equals 0 to 5, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention further concerns new key intermediate compounds, a quaternary ammonium salt of formula III′ and a 2-oxazolylalkyl derivative of formula IX.
摘要翻译：本发明涉及制备式I的5-（2-恶唑基烷硫基）-2-氮杂环烷酰氨基噻唑化合物或其药学上可接受的盐的新的，有效的方法，其中：R是烷基，芳基或杂芳基; R 1，R 2 R 3，R 4和R 5各自独立地为氢，烷基，芳基或杂芳基; R 6和R 7各自独立地为氢，烷基，芳基，杂芳基，卤素，羟基或烷氧基; R 8是氢，烷基，芳基，杂芳基，CONR 9 R 10，COR 11或COOR 12; R 9，R 10，R 11 且R 12各自独立地为氢，烷基或芳基; m等于0至5; 和等于0至5，这是细胞周期蛋白依赖性激酶（cdks）的新型有效抑制剂。本发明还涉及新的关键中间体化合物，式III'的季铵盐和式IX的2-恶唑基烷基衍生物。

2. 发明授权

US06562994B2 Process for the preparation of N-(substituted phenyl)-3-alkyl-,aryl- and heteroarylsulfonyl-2-hydroxy-2-alkyl- and haloalkylpropanamide compounds 失效
标题翻译：制备N-（取代的苯基）-3-烷基 - ，芳基 - 和杂芳基磺酰基-2-羟基-2-烷基 - 和卤代烷基丙酰胺化合物的方法
公开(公告)号：US06562994B2
公开(公告)日：2003-05-13
申请号：US09953759
申请日：2001-09-17
申请人： Bang-Chi Chen , Joseph E. Sundeen , Rulin Zhao
发明人： Bang-Chi Chen , Joseph E. Sundeen , Rulin Zhao
IPC分类号： C07C25500
CPC分类号： C07D303/48 , C07C253/30 , C07C315/02 , C07C319/14 , C07C317/46 , C07C323/60 , C07C255/60
摘要： The present invention provides an improved process for the preparation of N-(substituted phenyl)-3-alkyl-, aryl- and heteroarylsulfonyl-2-hydroxy-2-alkyl- and haloalkylpropanamide compounds of formula I that exhibit antiandrogenic activity and are useful in the treatment of malignant or benign prostatic disease or of androgen dependent disease conditions such as acne, hirsutism or seborrhea.
摘要翻译：本发明提供了制备具有抗雄激素活性的式I的N-（取代的苯基）-3-烷基 - ，芳基 - 和杂芳基磺酰基-2-羟基-2-烷基 - 和卤代烷基丙酰胺化合物的改进方法，治疗恶性或良性前列腺疾病或雄激素依赖性疾病状况，如痤疮，多毛症或皮脂溢。

3. 发明授权

US06392053B2 Process for preparing arylacetylaminothiazoles 有权
标题翻译：制备芳基乙酰氨基噻唑的方法
公开(公告)号：US06392053B2
公开(公告)日：2002-05-21
申请号：US09746059
申请日：2000-12-22
申请人： Bang-Chi Chen , Kyoung S. Kim , S. David Kimball , Raj N. Misra , Joseph E. Sundeen , Rulin Zhao
发明人： Bang-Chi Chen , Kyoung S. Kim , S. David Kimball , Raj N. Misra , Joseph E. Sundeen , Rulin Zhao
IPC分类号： C07D41712
CPC分类号： C07D417/12 , A61K31/427 , A61K31/454 , C07D231/12 , C07D233/56 , C07D249/08 , C07D417/14
摘要： The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-arylacetylaminothiazole compounds of formula I or a pharmaceutically acceptable salt thereof, wherein: R1, R2, R4, R5, R6, R8, R9, R12 and R13 are each independently hydrogen, alkyl, aryl or heteroaryl; R3, R7, R10 and R11 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; and X is CH or N, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention also concerns a new process for the preparation of formylarylacetates and formylarylacetic acids.
摘要翻译：本发明涉及制备式I的5-（2-恶唑基烷硫基）-2-芳基乙酰氨基噻唑化合物或其药学上可接受的盐的新的，有效的方法，其中：R1，R2，R4，R5，R6，R8，R9， R 12和R 13各自独立地为氢，烷基，芳基或杂芳基; R 3，R 7，R 10和R 11各自独立地为氢，烷基，芳基，杂芳基，卤素，羟基或烷氧基; 而X是CH或N，它们是细胞周期蛋白依赖性激酶（cdks）的新型有效抑制剂。本发明还涉及制备甲酰芳基乙酸酯和甲酰芳基乙酸的新方法。

4. 发明授权

US6160134A Process for preparing chiral cyclopropane carboxylic acids and acyl guanidines 失效
标题翻译：制备手性环丙烷羧酸和酰基胍的方法
公开(公告)号：US6160134A
公开(公告)日：2000-12-12
申请号：US329472
申请日：1999-06-10
申请人： Bang-Chi Chen , Joseph E. Sundeen , Jeffrey T. North , Annie J. Pullockaran , Saleem Ahmad , Shung C. Wu , Karnail S. Atwal , Sundeep Dugar
发明人： Bang-Chi Chen , Joseph E. Sundeen , Jeffrey T. North , Annie J. Pullockaran , Saleem Ahmad , Shung C. Wu , Karnail S. Atwal , Sundeep Dugar
IPC分类号： C07D307/78 , C07B57/00 , C07C51/295 , C07C61/35 , C07C279/22 , C07D207/16 , C07D207/32 , C07D207/327 , C07D213/56 , C07D213/61 , C07D213/64 , C07D233/54 , C07D233/62 , C07D271/12 , C07D307/79 , C07D307/81 , C07D311/58 , C07D317/60 , C07D317/62 , C07D409/10 , C07D413/04 , C07D521/00 , C07D307/87 , C07C49/293 , C07C61/04 , C07D307/80
CPC分类号： C07D307/79 , C07C279/22 , C07C2601/02 , C07C2602/42 , C07D207/16 , C07D207/327 , C07D213/56 , C07D213/61 , C07D213/64 , C07D231/12 , C07D233/56 , C07D233/64 , C07D249/08 , C07D271/12 , C07D307/81 , C07D311/58 , C07D317/60 , C07D317/62 , C07D409/10 , C07D413/04
摘要： A process is provided for preparing chiral cyclopropane carboxylic acids, preferably of the structure ##STR1## which are intermediates used in preparing acyl guanidine sodium/proton exchange (NHE) inhibitors.
摘要翻译：提供了一种制备手性环丙烷羧酸的方法，优选具有用于制备酰基胍/质子交换（NHE）抑制剂的中间体的结构。

5. 发明授权

US6100395A Reductive alkylation of secondary amines with hydrosilane 有权
标题翻译：用氢硅烷还原烷基化仲胺
公开(公告)号：US6100395A
公开(公告)日：2000-08-08
申请号：US480202
申请日：2000-01-10
申请人： Bang-Chi Chen , Joseph E. Sundeen , Peng Guo
发明人： Bang-Chi Chen , Joseph E. Sundeen , Peng Guo
IPC分类号： C07C209/28 , C07D233/64 , C07D243/14 , C07D333/64
CPC分类号： C07D243/14 , C07C209/28
摘要： A novel process for the production of tertiary amines by reductive alkylation of second amine using hydrosilane and a Lewis acid is disclosed. The novel process has applications in the preparation of imidazole-containing benzodiazepines, inhibitors of farnesyl protein transferase.
摘要翻译：公开了通过使用氢硅烷和路易斯酸的第二胺的还原烷基化生产叔胺的新方法。该新方法可用于制备含咪唑的苯并二氮杂，法呢基蛋白转移酶的抑制剂。

6. 发明授权

US5077432A Monobactam hydrazides containing catechol sulfonic acid groups 失效
标题翻译：含有邻苯二酚磺酸基团的单链酰肼
公开(公告)号：US5077432A
公开(公告)日：1991-12-31
申请号：US651871
申请日：1991-02-07
申请人： Joseph E. Sundeen , Robert Zahler , Stefan Jendrzejewski
发明人： Joseph E. Sundeen , Robert Zahler , Stefan Jendrzejewski
IPC分类号： C07C309/51 , C07D417/12
CPC分类号： C07D417/12 , C07C309/51
摘要： Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.3 and R.sub.4 are the same or different and each is hydrogen or alkyl or R.sub.3 and R.sub.4 taken together with the nitrogen atoms to which they are attached form a 1,2-diazacyclobutane, 1,2-diazacyclopentane, 1,2-diazacyclohexane, or 1,2-diazacycloheptane ring and Y, and Y.sub.2 are either hydrogen or hydroxy but are not the same; are useful chemical intermediates for the preparation of .beta.-lactam antibiotics.
摘要翻译：具有式“IMAGE”的化合物及其药学上可接受的盐，其中R 3和R 4相同或不同，并且各自为氢或烷基或R 3和R 4与它们所连接的氮原子一起形成1,2-二氮环丁烷，1,2-二氮杂环戊烷，1,2-二氮杂环己烷或1,2-二氮杂环庚烷环，Y和Y2分别是氢或羟基，但不相同; 是制备β-内酰胺抗生素的有用化学中间体。

7. 发明授权

US4382081A Inhibitors of mammalian collagenase 失效
标题翻译：哺乳动物胶原酶抑制剂
公开(公告)号：US4382081A
公开(公告)日：1983-05-03
申请号：US273142
申请日：1981-06-12
申请人： Joseph E. Sundeen , Tamara Dejneka
发明人： Joseph E. Sundeen , Tamara Dejneka
IPC分类号： C12N9/99 , A61K31/195 , A61K38/00 , A61K38/55 , C07C55/02 , C07C67/00 , C07C313/00 , C07C323/52 , C07C323/56 , C07C323/60 , C07C327/20 , C07C327/32 , C07K5/02 , C07K5/04 , C07K5/06 , C07K5/08 , C07K5/083 , C07K5/10 , C07K5/103 , C07K14/81 , A61K37/00 , C07C103/52
CPC分类号： C07K5/1008 , C07C323/52 , C07C323/56 , C07C327/00 , C07C55/02 , C07K5/06026 , C07K5/0806
摘要： Mammalian collagenase is inhibited by compounds of the formula ##STR1## or salts thereof, wherein R is hydrogen, alkanoyl of 2 to 10 carbon atoms or arylcarbonyl;R.sub.1 is of 3 to 8 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, aryl or arylalkyl; ##STR2## R.sub.4 is hydrogen, methyl, ethyl, or ##STR3## R.sub.5 and R.sub.6 are each independently selected as --OCH.sub.3 or --OCH.sub.2 CH.sub.3 or are combined as --OCH.sub.2 CH.sub.2 O-- or --O--(CH.sub.2)--O--;R.sub.7 and R.sub.8 are each independently selected as hydrogen, methyl or ethyl or are combined as --(CH.sub.2).sub.4 --, --(CH.sub.2).sub.5 -- or --CH.sub.2 CH.sub.2 --O--CH.sub.2 CH.sub.2 --;R.sub.9 is hydrogen, methyl, ethyl ##STR4## m is an integer from 0 to 7; p is an integer from 1 to 3; AA.sub.n is an amino acid chain of from one to three amino acids; n is 1 or 1, 2 or 1, 2, 3;when p is 1, AA.sub.n is AA.sub.1 ;when p is 2, AA.sub.n is AA.sub.1 --AA.sub.2 ;when p is 3, AA.sub.n is AA.sub.1 --AA.sub.2 --AA.sub.3 ;AA.sub.1 is glycine or alanine;AA.sub.2 is glycine or alanine;AA.sub.3 is leucine, glutamine or isoleucine.A method of reducing the adverse effects of mammalian collagenase in a mammalian host in need thereof, which comprises administering to the mammal an effective amount of a compound having the above formula is within the scope of the invention.
摘要翻译：哺乳动物胶原酶被下式化合物或其盐抑制，其中R是氢，2-10个碳原子的烷酰基或芳基羰基; R1为3〜8个碳原子的烷基，3〜7个碳原子的环烷基，芳基或芳基烷基; R 4是氢，甲基，乙基或者R 5，R 6和R 6各自独立地选自-OCH 3或-OCH 2 CH 3，或者作为-OCH 2 CH 2 O-或-O - （CH 2）-O-; R 7和R 8各自独立地选自氢，甲基或乙基，或者作为 - （CH 2）4 - ， - （CH 2）5 - 或-CH 2 CH 2 -O-CH 2 CH 2 - R9是氢，甲基，乙基，是0至7的整数; p是1至3的整数; AAn是一至三个氨基酸的氨基酸链; n为1或1,2或1，2，3; 当p为1时，AAn为AA1; 当p为2时，AAn为AA1-AA2; 当p为3时，AAn为AA1-AA2-AA3; AA1是甘氨酸或丙氨酸; AA2是甘氨酸或丙氨酸; AA3是亮氨酸，谷氨酰胺或异亮氨酸。减少有需要的哺乳动物宿主中哺乳动物胶原酶的不利影响的方法，其包括向哺乳动物施用有效量的具有上式的化合物在本发明的范围内。

8. 发明授权

US4208415A 4-[2-(2-Substituted phenyl)ethenyl]-N-alkenyl or alkinyl substituted 1,2,3,6-tetrahydropyridines 失效
标题翻译： 4- [2-（2-取代的苯基）乙烯基] -N-烯基或炔基取代的1,2,3,6-四氢吡啶
公开(公告)号：US4208415A
公开(公告)日：1980-06-17
申请号：US875276
申请日：1978-02-06
申请人： Joseph E. Sundeen , Frederick P. Hauck
发明人： Joseph E. Sundeen , Frederick P. Hauck
IPC分类号： A61K31/445 , A61K31/451 , A61P1/04 , A61P43/00 , C07D211/70 , A61K31/44
CPC分类号： C07D211/70
摘要： Compounds of the formula and their pharmaceutically acceptable acid addition salts ##STR1## wherein X is lower alkoxy, Cl, Br, or F; R is ##STR2## or --C.tbd.C--R.sub.4 ; R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are independently selected from hydrogen and methyl; n is an integer from 1 to 3 provided that when n is 3 at least two of R.sub.1, R.sub.2 and R.sub.3 are hydrogen and R.sub.4 is hydrogen, and further provided that when n is 2 at least one of R.sub.1, R.sub.2 and R.sub.3 is hydrogen; are disclosed. These compounds possess useful pharmaceutical activities due to their ability to inhibit the prostaglandin-inactivating enzyme 15-.alpha.-hydroxyprostaglandin dehydrogenase.
摘要翻译：式的化合物及其药学上可接受的酸加成盐，其中X是低级烷氧基，Cl，Br或F; R为或-C 3BOND C-R4; R 1，R 2，R 3和R 4独立地选自氢和甲基; n为1至3的整数，条件是当n为3时，R 1，R 2和R 3中的至少两个为氢，R 4为氢，并且进一步规定，当n为2时，R 1，R 2和R 3中的至少一个为氢; 被披露。这些化合物由于其抑制前列腺素失活酶15-α-羟基前列腺素脱氢酶的能力而具有有用的药物活性。

9. 发明授权

US4138497A Indanpentol derivatives for treating hypertension 失效
标题翻译：茚满醇衍生物用于治疗高血压
公开(公告)号：US4138497A
公开(公告)日：1979-02-06
申请号：US820290
申请日：1977-07-29
申请人： Frederic P. Hauck , Joseph E. Sundeen , Joyce Reid
发明人： Frederic P. Hauck , Joseph E. Sundeen , Joyce Reid
IPC分类号： C07D295/08 , A61K31/13 , A61K31/215 , A61K31/27 , A61K31/395 , A61K31/40 , A61K31/435 , A61K31/495 , A61K31/535 , A61K31/5375 , A61K31/54 , A61K31/55 , A61P9/12 , C07C17/32 , C07C31/137 , C07C67/00 , C07C213/00 , C07C215/42 , C07C217/52 , C07C219/24 , C07C239/00 , C07C269/00 , C07D211/14 , C07D211/32 , C07D211/42 , C07D211/46 , C07D211/54 , C07D211/70 , C07D213/20 , C07D223/04 , C07D295/02 , C07D295/03 , C07D295/04 , C07D295/096 , C07C103/00
CPC分类号： C07D295/03 , C07C17/32 , C07C309/00 , C07C31/137 , C07D211/42 , C07D211/70 , C07D213/20 , C07D295/096 , C07C2102/08
摘要： Compounds are provided having the structure ##STR1## wherein n is 1, 2 or 3, m is 0, 1 or 2, R.sub.1 R.sub.2, R.sub.3, R.sub.4 and R.sub.5 may be the same or different and can be hydrogen, lower alkyl, halo-lower alkyl, acyl, lower alkoxy-carbonyl ##STR2## amido ##STR3## or lower alkoxylakylene, X is a straight or branched bivalent aliphatic radical and Y is ##STR4## These compounds are useful in the treatment of hypertension.

10. 发明授权

US3936465A Cyclohexane tetrols and derivatives thereof 失效
标题翻译：环己烷四环及其衍生物
公开(公告)号：US3936465A
公开(公告)日：1976-02-03
申请号：US383642
申请日：1973-07-30
申请人： Frederic Peter Hauck , Joseph E. Sundeen
发明人： Frederic Peter Hauck , Joseph E. Sundeen
IPC分类号： C07D207/08 , C07C33/34 , C07C67/00 , C07C213/00 , C07C219/24 , C07C227/00 , C07C227/18 , C07C229/06 , C07D207/06 , C07D211/14 , C07D211/22 , C07D213/80 , C07D295/096 , C07D211/32
CPC分类号： C07D213/80 , C07C33/34 , C07D207/06 , C07D211/14 , C07D211/22 , C07D295/096 , Y10S514/96 , Y10S514/962
摘要： The compounds of the invention have the formula ##SPC1##Wherein Y is a radical of the formula ##SPC2##Wherein n is 1, 2, 3, 4, 5, or 6, m is 0 or 1, and R.sup.5 is hydrogen or alkyl of 1 to 3 carbons;R.sup.1, r.sup.2, r.sup.3 and R.sup.4 are the same or different and are alkanoyl of 1 to 4 carbons; haloalkanoyl of 1 to 4 carbons; or alkoxycarbonyl of the formula ##EQU1## wherein R is an alkyl radical of 1 to 4 carbons; R.sup.7 and R.sup.8 are the same or different and are hydrogen or alkyl having 1 to 4 carbon atoms; andR.sup.9 is hydrogen or a straight or branched chain alkyl radical having 1 to 6 carbon atoms.These compounds have been found useful in the treatment of hypertension in mammalian species, as surface active agents, as in vivo antibacterial compounds and as water softeners.
摘要翻译：本发明的化合物具有式WHEREIN Y是下式的基团：其中N为1,2,3,4,5或6，M为0或1，R5为氢或1至3个碳的烷基; R1，R2，R3和R4相同或不同，为1至4个碳原子的烷酰基; 1至4个碳的卤代烷酰基; 或式O-PARALLEL -COR的烷氧基羰基，其中R是1至4个碳的烷基; R 7和R 8相同或不同，为氢或具有1至4个碳原子的烷基; 并且R 9为氢或具有1至6个碳原子的直链或支链烷基。

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