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1. 发明授权

US5635509A Piperidine derivatives useful as neurokinin antagonists 失效
标题翻译：哌啶衍生物可用作神经激肽拮抗剂
公开(公告)号：US5635509A
公开(公告)日：1997-06-03
申请号：US432309
申请日：1995-05-01
申请人： Robert T. Jacobs , Scott C. Miller , Ashokkumar B. Shenvi , Cyrus J. Ohnmacht, Jr. , Chris A. Veale
发明人： Robert T. Jacobs , Scott C. Miller , Ashokkumar B. Shenvi , Cyrus J. Ohnmacht, Jr. , Chris A. Veale
IPC分类号： A61K31/4427 , A61K31/445 , A61K31/505 , A61P11/00 , A61P11/06 , A61P43/00 , C07D401/06 , C07D401/14 , C07D239/10
CPC分类号： C07D401/06 , C07D401/14
摘要： Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
摘要翻译：式I的化合物其中Q1，Q2，Q3和Q4具有本说明书中给出的任何含义，其N-氧化物及其药学上可接受的盐是神经激肽A的非肽拮抗剂，可用于治疗哮喘等。还公开了药物组合物，制备式I化合物的方法和中间体。

2. 发明授权

US5521199A Piperidinyl compounds as neurokinin receptor antagonists 失效
标题翻译：哌啶基化合物作为神经激肽受体拮抗剂
公开(公告)号：US5521199A
公开(公告)日：1996-05-28
申请号：US242949
申请日：1994-05-16
申请人： Robert T. Jacobs , Ashokkumar B. Shenvi
发明人： Robert T. Jacobs , Ashokkumar B. Shenvi
IPC分类号： A61K31/445 , A61K31/4427 , A61K31/451 , A61P11/00 , A61P11/06 , A61P43/00 , C07D211/14 , C07D211/22 , C07D211/26 , C07D211/28 , C07D211/32 , C07D211/62 , C07D295/13 , C07D401/12
CPC分类号： C07D295/13 , C07D211/22 , C07D211/26 , C07D211/28 , C07D211/32 , C07D211/62
摘要： The present invention concerns the novel alkyl substituted heterocycles of formula I, set out below, wherein Q, Q.sup.1, Q.sup.2 and R have the values defined herein, which antagonize the pharmacological actions of one of the endogenous neuropeptide tachykinins at the neurokinin 2 (NK.sup.2) receptor making them useful whenever such antagonism is desired, such as in the treatment of asthma and related conditions. The invention also provides pharmaceutical compositions containing the alkyl substituted heterocycles for use in such treatment, methods for their use, and processes and novel intermediates for their manufacture. ##STR1##
摘要翻译：本发明涉及式I的新的烷基取代的杂环，如下所述，其中Q，Q1，Q2和R具有本文定义的值，其拮抗神经激肽2（NK2）内的内源性神经肽速激肽之一的药理作用，受体使其在需要这种拮抗作用时有用，例如在治疗哮喘和相关病症中。本发明还提供含有用于这种治疗的烷基取代的杂环的药物组合物，其用途及其制备方法和新型中间体。我

3. 发明授权

US4415736A Certain tetrahydropyridine intermediates 失效
标题翻译：某些四氢吡啶中间体
公开(公告)号：US4415736A
公开(公告)日：1983-11-15
申请号：US334838
申请日：1981-12-28
申请人： Engelbert Ciganek , Ashokkumar B. Shenvi
发明人： Engelbert Ciganek , Ashokkumar B. Shenvi
IPC分类号： C07D211/52 , C07D211/70 , C07D211/74 , C07D217/16 , C07D491/08 , C07D491/10 , C07D491/107 , C07D405/04 , C07D213/50
CPC分类号： C07D491/08 , C07D211/52 , C07D211/70 , C07D217/16 , C07D491/10
摘要： Process for preparing analgesic and narcotic antagonistic isoquinolines comprising:(a) contacting and reacting a lithiated anisole or alkyl phenyl ether, optionally substituted at the 3-position to the lithium atom, with a 4-piperidone to yield a 4-aryl-4-piperidinol;(b) dehydrating the piperidinol to a 4-aryl-1,2,3,6-tetrahydropyridine;(c) metalating and acylating the 1,2,3,6-tetrahydropyridine to yield a 1-(4-aryl-1,2,3,4-tetrahydropyrid-4-yl)-4-hydroxy-1-butanone;(d) reducing the ketone moiety of the butanone to yield a 5-aryl-7-oxa-2-azabicyclo[3.2.1]-octane-6-propanol;(e) converting the alcohol moiety of the propanol to L to yield a 5-aryl-6-[3-(L)propyl]-7-oxa-2-azabicyclo[3.2.1]octane in which L is a leaving group selected from the group consisting of -Cl, -Br, -I, p-MeC.sub.6 H.sub.4 SO.sub.3 - and MeSO.sub.3 -.(f) opening the amino furan ring of the bicyclooctane to yield a 4-(L)-1-(4-aryl-1,2,3,4-tetrahydropyrid-4-yl)-1-butanol derivative;(g) closing the 6-carbon ring of the butanol derivative by intramolecular reaction of the enamine and leaving group to yield a 4a-aryl-2,3,4,4a,5,6,7,8-octahydro-5-isoquinolinol or derivative thereof; and(h) reducing the enamine double bond of the octahydro-5-isoquinolinol or derivative thereof to yield a 4a-aryldecahydro-5-isoquinolinol or derivative thereof and (i) cyclizing the decahydro-5-isoquinolinol or derivative to yield a 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro-[3,2-e]isoquinoline, or,(h) cyclizing the octahydro-5-isoquinolinol or derivative thereof to yield a 2,3,5,6,7,7a-hexahydro-1H-benzofuro-[3,2-e]isoquinoline and (i) reducing the enamine double bond of the isoquinoline.
摘要翻译：制备镇痛和麻醉拮抗性异喹啉的方法，包括：（a）使任选在3-位上被锂取代的锂化苯甲醚或烷基苯基醚与4-哌啶酮接触并使其反应，得到4-芳基-4- 哌啶醇（b）将哌啶醇脱水为4-芳基-1,2,3,6-四氢吡啶; （c）金属化和酰化1,2,3,6-四氢吡啶，得到1-（4-芳基-1,2,3,4-四氢吡啶-4-基）-4-羟基-1-丁酮; （d）还原丁酮的酮部分，得到5-芳基-7-氧杂-2-氮杂双环[3.2.1] - 辛烷-6-丙醇; （e）将丙醇的醇部分转化为L，得到其中L为离去基团的5-芳基-6- [3-（L）丙基] -7-氧杂-2-氮杂双环[3.2.1]辛烷选自-Cl，-Br，-I，对-MeC 6 H 4 SO 3 - 和MeSO 3 - 。（f）打开双环辛烷的氨基呋喃环，得到4-（L）-1-（4-芳基-1,2,3,4-四氢吡啶-4-基）-1-丁醇衍生物; （g）通过烯胺和离去基团的分子内反应封闭丁醇衍生物的6-碳环，得到4a-芳基-2,3,4,4a，5,6,7,8-八氢-5-异喹啉醇或其衍生物; 和（h）还原八氢-5-异喹啉醇或其衍生物的烯胺双键，得到4a-芳基十氢-5-异喹啉醇或其衍生物，和（i）使十氢-5-异喹啉醇或衍生物环化，得到2， 3,4,4a，5,6,7,7a-八氢-1H-苯并呋喃并[3,2-e]异喹啉，或（h）使八氢-5-异喹啉醇或其衍生物环化，得到2,3 ，5,6,7,7a-六氢-1H-苯并呋喃并[3,2-e]异喹啉和（i）还原异喹啉的烯胺双键。

4. 发明授权

US06235757B1 Substituted heterocycles 失效
标题翻译：取代的杂环
公开(公告)号：US06235757B1
公开(公告)日：2001-05-22
申请号：US09519307
申请日：2000-03-06
申请人： Scott C. Miller , Robert T. Jacobs , Ashokkumar B. Shenvi
发明人： Scott C. Miller , Robert T. Jacobs , Ashokkumar B. Shenvi
IPC分类号： A61K31445
CPC分类号： C07D401/06 , C07D401/14
摘要： Compounds of formula I wherein Q1, Q2, Q3, Q4 and Q5 have any of the meanings given in the specification, their N-oxides, and their pharmacuetically acceptable salts are nonpeptide antagonists NKA, useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
摘要翻译：在Q1，Q2，Q3，Q4和Q5中的式I化合物具有说明书中给出的任何含义，它们的N-氧化物及其药理学上可接受的盐是可用于治疗哮喘的非肽拮抗剂NKA等。还公开了药物组合物，制备式I化合物的方法和中间体。

5. 发明授权

US4537963A Intermediates for octahydrobenzofuro[3,2-E]isoquinolines 失效
标题翻译：八氢苯并呋喃并[3,2-E]异喹啉的中间体
公开(公告)号：US4537963A
公开(公告)日：1985-08-27
申请号：US522094
申请日：1983-08-11
申请人： Ashokkumar B. Shenvi
发明人： Ashokkumar B. Shenvi
IPC分类号： C07D211/52 , C07D211/70 , C07D217/16 , C07D491/08 , C07D491/10 , C07D491/107 , C07D491/048
CPC分类号： C07D491/08 , C07D211/52 , C07D211/70 , C07D217/16 , C07D491/10
摘要： Process for preparing analgesic and narcotic antagonistic isoquinolines comprising:(a) contacting and reacting a lithiated anisole or alkyl phenyl ether, optionally substituted at the 3-position to the lithium atom, with a 4-piperidone to yield a 4-aryl-4-piperidinol;(b) dehydrating the piperidinol to a 4-aryl-1,2,3,6-tetrahydropyridine;(c) metalating and acylating the 1,2,3,6-tetrahydropyridine to yield a 1-(4-aryl-1,2,3,4-tetrahydropyrid-4-yl)-4-hydroxy-1-butanone;(d) reducing the ketone moiety of the butanone to yield a 5-aryl-7-oxa-2-azabicyclo[3,2.1]-octane-6-propanol;(e) converting the alcohol moiety of the propanol to L to yield a 5-aryl-6-[3-(L)propyl]-7-oxa-2-azabicyclo[3.3.1]octane in which L is a leaving group selected from the group consisting of --Cl, --Br, --I, p--MeC.sub.6 H.sub.4 SO.sub.3 -- and MeSO.sub.3 --.(f) opening the amino furan ring of the bicyclooctane to yield a 4-(L)-1-(4-aryl-1,2,3,4-tetrahydropyrid-4-yl)-1-butanol derivative;(g) closing the 6-carbon ring of the butanol derivative by intramolecular reaction of the enamine and leaving group to yield a 4a-aryl-2,3,4,4a,5,6,7,8-octahydro-5-isoquinolinol or derivative thereof; and(h) reducing the enamine double bond of the octahydro-5-isoquinolinol or derivative thereof to yield a 4a-aryldecahydro-5-isoquinolinol or derivative thereof and (i) cyclizing the decahydro-5-isoquinolinol or derivative to yield a 2,3,4,4a,5,6,7,7A-octahydro-1H-benzofuro[3,2-e]isoquinoline, or,(h') cyclizing the octahydro-5-isoquinolinol or derivative thereof to yield a 2,3,5,6,7,7a-hexahydro-1H-benzofuro-[3,2-e]isoquinoline and (i') reducing the enamine double bond of the isoquinoline.
摘要翻译：制备镇痛和麻醉拮抗性异喹啉的方法，包括：（a）使任选在3-位上被锂取代的锂化苯甲醚或烷基苯基醚与4-哌啶酮接触并使其反应，得到4-芳基-4- 哌啶醇（b）将哌啶醇脱水为4-芳基-1,2,3,6-四氢吡啶; （c）金属化和酰化1,2,3,6-四氢吡啶，得到1-（4-芳基-1,2,3,4-四氢吡啶-4-基）-4-羟基-1-丁酮; （d）还原丁酮的酮部分，得到5-芳基-7-氧杂-2-氮杂双环[3,2,1] - 辛烷-6-丙醇; （e）将丙醇的醇部分转化为L，得到其中L为离去基团的5-芳基-6- [3-（L）丙基] -7-氧杂-2-氮杂双环[3.3.1]辛烷选自-Cl，-Br，-I，对-MeC 6 H 4 SO 3 - 和MeSO 3 - 。（f）打开双环辛烷的氨基呋喃环，得到4-（L）-1-（4-芳基-1,2,3,4-四氢吡啶-4-基）-1-丁醇衍生物; （g）通过烯胺和离去基团的分子内反应封闭丁醇衍生物的6-碳环，得到4a-芳基-2,3,4,4a，5,6,7,8-八氢-5-异喹啉醇或其衍生物; 和（h）还原八氢-5-异喹啉醇或其衍生物的烯胺双键，得到4a-芳基十氢-5-异喹啉醇或其衍生物，和（i）使十氢-5-异喹啉醇或衍生物环化，得到2， 3,4,4a，5,6,7,7a-八氢-1H-苯并呋喃并[3,2-e]异喹啉，或（h'）使八氢-5-异喹啉醇或其衍生物环化，得到2,3 ，5,6,7,7a-六氢-1H-苯并呋喃并[3,2-e]异喹啉和（i'）还原异喹啉的烯胺双键。

6. 发明授权

US4537773A .alpha.-Aminoboronic acid derivatives 失效
标题翻译： α-氨基硼酸衍生物
公开(公告)号：US4537773A
公开(公告)日：1985-08-27
申请号：US558361
申请日：1983-12-05
申请人： Ashokkumar B. Shenvi
发明人： Ashokkumar B. Shenvi
IPC分类号： A01N55/08 , C07F5/02 , C07F5/04 , C07F7/02 , C07F7/08
CPC分类号： A01N55/08 , C07F5/025
摘要： .alpha.-Aminoboronic acids and derivatives of formula ##STR1## are potent, reversible inhibitors of aminopeptidases.
摘要翻译： α-氨基宝酸和式的衍生物是氨基肽酶的有效的可逆抑制剂。

7. 发明授权

US5187157A Peptide boronic acid inhibitors of trypsin-like proteases 失效
标题翻译：肽类抗坏血酸蛋白酶抑制剂
公开(公告)号：US5187157A
公开(公告)日：1993-02-16
申请号：US178368
申请日：1988-04-06
申请人： Charles A. Kettner , Ashokkumar B. Shenvi
发明人： Charles A. Kettner , Ashokkumar B. Shenvi
IPC分类号： C07K5/06 , A61K20060101 , A61K38/00 , A61K38/06 , A61K38/55 , A61P7/02 , A61P29/00 , C07F20060101 , C07F5/00 , C07F5/02 , C07K20060101 , C07K5/00 , C07K5/04 , C07K5/065 , C07K5/08 , C07K5/097 , C07K5/10 , C07K5/103 , C07K14/81 , C12N9/99
CPC分类号： C07K5/00 , C07F5/025
摘要： Peptides comprising C-terminal boronic acid derivatives of lysine, ornithine, and arginine, homoarginine and corresponding isothiouronium analogs thereof, are reversible inhibitors of trypsin-like serine proteases such as thrombin, plasma kallikrein and plasmin.

8. 发明授权

US4692528A Intermediates for octahydrobenzofuro[3,2-e]isoquinolines 失效
标题翻译：八氢苯并呋喃并[3,2-e]异喹啉的中间体
公开(公告)号：US4692528A
公开(公告)日：1987-09-08
申请号：US743415
申请日：1985-06-11
申请人： Ashokkumar B. Shenvi
发明人： Ashokkumar B. Shenvi
IPC分类号： C07D211/52 , C07D211/70 , C07D217/16 , C07D491/08 , C07D491/10
CPC分类号： C07D491/08 , C07D211/52 , C07D211/70 , C07D217/16 , C07D491/10
摘要： Process for preparing analgesic and narcotic antagonistic isoquinolines comprising:(a) contacting and reacting a lithiated anisole or alkyl phenyl ether, optionally substituted at the 3-position to the lithium atom, with a 4-piperidone to yield a 4-aryl-4-piperidinol;(b) dehydrating the piperidinol to a 4-aryl-1,2,3,6-tetrahydropyridine;(c) metalating and acylating the 1,2,3,6-tetrahydropyridine to yield a 1-(4-aryl-1,2,3,4-tetrahydropyrid-4-yl)-4-hydroxy-1-butanone;(d) reducing the ketone moiety of the butanone to yield a 5-aryl-7-oxa-2-azabicyclo[3.2.1]-octane-6-propanol;(e) converting the alcohol moiety of the propanol to L to yield a 5-aryl-6-[3-(L)propyl]-7-oxa-2-azabicyclo[3.2.1]octane in which L is a leaving group selected from the group consisting of --Cl, --Br, --I, p-MeC.sub.6 H.sub.4 SO.sub.3 and MeSO.sub.3 --.(f) opening the amino furan ring of the bicyclooctane to yield a 4-(L)-1-(4-aryl-1,2,3,4-tetrahydropyrid-4-yl)-1-butanol derivative;(g) closing the 6-carbon ring of the butanol derivative by intramolecular reaction of the enamine and leaving group to yield a 4a-aryl-2,3,4,4a,5,6,7,8-octahydro-5-isoquinolinol or derivative thereof; and(h) reducing the enamine double bond of the octahydro-5-isoquinolinol or derivative thereof to yield a 4a-aryldecahydro-5-isoquinolinol or derivative thereof and (i) cyclizing the decahydro-5-isoquinolinol or derivative to yield a 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinoline, or,(h') cyclizing the octahydro-5-isoquinolinol or derivative thereof to yield a 2,3,5,6,7,7a-hexahydro-1H-benzofuro-[3,2-e]isoquinoline and(i') reducing the enamine double bond of the isoquinoline.
摘要翻译：制备镇痛和麻醉拮抗性异喹啉的方法，包括：（a）使任选在3-位上被锂取代的锂化苯甲醚或烷基苯基醚与4-哌啶酮接触并使其反应，得到4-芳基-4- 哌啶醇（b）将哌啶醇脱水为4-芳基-1,2,3,6-四氢吡啶; （c）金属化和酰化1,2,3,6-四氢吡啶，得到1-（4-芳基-1,2,3,4-四氢吡啶-4-基）-4-羟基-1-丁酮; （d）还原丁酮的酮部分，得到5-芳基-7-氧杂-2-氮杂双环[3.2.1] - 辛烷-6-丙醇; （e）将丙醇的醇部分转化为L，得到其中L为离去基团的5-芳基-6- [3-（L）丙基] -7-氧杂-2-氮杂双环[3.2.1]辛烷选自-Cl，-Br，-I，对-MeC 6 H 4 SO 3和MeSO 3 - 。（f）打开双环辛烷的氨基呋喃环，得到4-（L）-1-（4-芳基-1,2,3,4-四氢吡啶-4-基）-1-丁醇衍生物; （g）通过烯胺和离去基团的分子内反应封闭丁醇衍生物的6-碳环，得到4a-芳基-2,3,4,4a，5,6,7,8-八氢-5-异喹啉醇或其衍生物; 和（h）还原八氢-5-异喹啉醇或其衍生物的烯胺双键，得到4a-芳基十氢-5-异喹啉醇或其衍生物，和（i）使十氢-5-异喹啉醇或衍生物环化，得到2， 3,4,4a，5,6,7,7a-八氢-1H-苯并呋喃并[3,2-e]异喹啉，或（h'）使八氢-5-异喹啉醇或其衍生物环化，得到2,3 ，5,6,7,7a-六氢-1H-苯并呋喃并[3,2-e]异喹啉和（i'）还原异喹啉的烯胺双键。

9. 发明授权

US09463450B1 Polymeric acid catalysis 有权
标题翻译：聚合酸催化
公开(公告)号：US09463450B1
公开(公告)日：2016-10-11
申请号：US15078065
申请日：2016-03-23
申请人： Ning Shangguan , Andrew Feiring , Ashokkumar B. Shenvi
发明人： Ning Shangguan , Andrew Feiring , Ashokkumar B. Shenvi
IPC分类号： C07D493/00 , B01J31/06 , C07D493/04 , C07C213/00
CPC分类号： C07D493/04 , B01J31/10 , B01J2231/40 , C07C231/12 , C07C233/25
摘要： A highly fluorinated polymer is very useful as an acid catalyst. The highly fluorinated polymer has at least two repeating unit types that are the polymerized derivatives of a perfluorinated cyclic or cyclizable compound and a highly fluorinated vinyl ether compound having a sulfur containing functional group. The polymer can be formed by radical copolymerization of the fluorinated monomers with the sulfur-containing functional group in sulfonyl fluoride form (—SO2F) that is subsequently converted to sulfonic acid form (—SO3H). The highly fluorinated polymer can be used to advantage in a solution comprising an aprotic, polar organic solvent that has a dielectric constant of at least 15 and preferably is free of hydroxyl functional groups. Suitable solvents are those in which the polymer is soluble to at least 1 wt %. Hydroxyl group-containing protic, polar organic solvents are less preferred. The highly fluorinated polymer can be an effective heterogeneous catalysts when used in form of solid, fine particles insolubly suspended in or in contact with a fluid reaction mass.
摘要翻译：高度氟化的聚合物作为酸催化剂是非常有用的。高氟化聚合物具有至少两种重复单元类型，它们是全氟化环状化合物和可环化化合物的聚合衍生物和具有含硫官能团的高氟化乙烯基醚化合物。聚合物可以通过氟化单体与磺酰氟形式（-SO 2 F）的含硫官能团自由基共聚形成，随后转化为磺酸形式（-SO 3 H）。高度氟化的聚合物可以在包含非质子极性有机溶剂的溶液中有利地使用，所述非质子极性有机溶剂的介电常数至少为15，优选不含羟基官能团。合适的溶剂是聚合物可溶于至少1重量％的溶剂。含羟基的质子，极性有机溶剂不太优选。当以固体悬浮在液体反应物质中或与流体反应物质接触的固体细颗粒的形式使用时，高度氟化的聚合物可以是有效的非均相催化剂。

10. 发明授权

US6051580A Substituted heterocycles 失效
标题翻译：取代的杂环
公开(公告)号：US6051580A
公开(公告)日：2000-04-18
申请号：US262509
申请日：1999-03-02
申请人： Scott C. Miller , Robert T. Jacobs , Ashokkumar B. Shenvi
发明人： Scott C. Miller , Robert T. Jacobs , Ashokkumar B. Shenvi
IPC分类号： A61K31/4427 , A61K31/445 , A61P11/00 , A61P43/00 , C07D401/06 , C07D401/14 , C07D403/06 , C07D239/00 , A61K31/505
CPC分类号： C07D401/06 , C07D401/14
摘要： Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, Q.sup.4 and Q.sup.5 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists NKA, useful for the treatment of asthma etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
摘要翻译：其中Q1，Q2，Q3，Q4和Q5具有本说明书中给出的任何含义，其N-氧化物及其药学上可接受的盐的式I化合物是可用于治疗哮喘等的非肽拮抗剂NKA。还公开了药物组合物，制备式I化合物的方法和中间体。

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