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1. 发明授权

US07138524B2 Processes for preparing anhydrous and hydrate forms of antihistaminic piperidine derivatives, polymorphs and pseudomorphs thereof 失效
公开(公告)号：US07138524B2
公开(公告)日：2006-11-21
申请号：US10162011
申请日：2002-06-03
申请人： Frederick J. McCarty , Albert A. Carr
发明人： Frederick J. McCarty , Albert A. Carr
IPC分类号： C07D211/22
CPC分类号： A61K31/445 , C07D211/22
摘要： The present invention is related to novel processes for preparing anhydrous and hydrated forms of piperidine derivatives, polymorphs and pseudomorphs thereof of the formulas which are useful as antihistamines, antiallergic agents and bronchodilators.

2. 发明授权

US07662835B2 Methods of treating allergic reactions using an anhydrous form of antihistaminic piperidine derivatives 失效
标题翻译：使用无水形式的抗组胺型哌啶衍生物治疗过敏反应的方法
公开(公告)号：US07662835B2
公开(公告)日：2010-02-16
申请号：US11534839
申请日：2006-09-25
申请人： Frederick J. McCarty , Albert A. Carr
发明人： Frederick J. McCarty , Albert A. Carr
IPC分类号： A61K31/445
CPC分类号： A61K31/445 , C07D211/22
摘要： The present invention is related to novel processes for preparing anhydrous and hydrated forms of piperidine derivatives, polymorphs and pseudomorphs thereof of the formulas which are useful as antihistamines, antiallergic agents and bronchodilators.
摘要翻译：本发明涉及用于制备可用作抗组胺剂，抗过敏剂和支气管扩张剂的式的哌啶衍生物，多晶型物和假晶体的无水和水合形式的新方法。

3. 发明授权

US06777555B2 Intermediates useful for the preparation of antihistaminic piperidine derivatives 失效
标题翻译：用于制备抗组胺型哌啶衍生物的中间体
公开(公告)号：US06777555B2
公开(公告)日：2004-08-17
申请号：US10364641
申请日：2003-02-12
申请人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
发明人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
IPC分类号： C07D21114
CPC分类号： C07D295/185 , C07C33/46 , C07C45/46 , C07C45/63 , C07C45/65 , C07C45/673 , C07C49/792 , C07C49/798 , C07C49/80 , C07C49/813 , C07C49/82 , C07C49/825 , C07C49/83 , C07C49/835 , C07C49/86 , C07C59/86 , C07C59/88 , C07C69/007 , C07C69/738 , C07C235/78 , C07C255/16 , C07C259/06 , C07C2601/02 , C07D211/22 , C07D401/06 , C07D401/10
摘要： The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, n is an integer 0.
摘要翻译：本发明涉及一种新的中间体和方法，其可用于制备W代表-C（= O） - 或-CH（OH） - 的某些抗组胺型哌啶衍生物; R 1表示氢或羟基; R 2表示氢 R 1和R 2一起形成在具有R 1和R 2的碳原子之间的第二个键; n是1至5的整数; m是整数0或1; R 3是-COOH或-COO烷基，其中烷基部分具有 1至6个碳原子，并且是直链或支链的，每个A是氢或羟基; 其药学上可接受的盐和单独的光学异构体，条件是其中R 1和R 2一起形成在具有R 1和R 2的碳原子之间或其中R 1表示羟基的第二个键，n是整数0。

4. 发明授权

US6147216A Intermediates useful for the preparation of antihistaminic piperidine derivatives 失效
标题翻译：用于制备抗组胺型哌啶衍生物的中间体
公开(公告)号：US6147216A
公开(公告)日：2000-11-14
申请号：US458747
申请日：1995-06-02
申请人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
发明人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
IPC分类号： C07C45/46 , C07C45/63 , C07C45/65 , C07C45/67 , C07C49/792 , C07C49/798 , C07C49/80 , C07C49/813 , C07C49/82 , C07C49/825 , C07C49/83 , C07C49/835 , C07C49/86 , C07C59/86 , C07C59/88 , C07C69/007 , C07C69/738 , C07C235/78 , C07C255/16 , C07C259/06 , C07D211/22 , C07D295/185 , C07D401/06 , C07D401/10 , C07D211/14
CPC分类号： C07D295/185 , C07C235/78 , C07C255/16 , C07C259/06 , C07C45/46 , C07C45/63 , C07C45/65 , C07C45/673 , C07C49/792 , C07C49/798 , C07C49/80 , C07C49/813 , C07C49/82 , C07C49/825 , C07C49/83 , C07C49/835 , C07C49/86 , C07C59/86 , C07C59/88 , C07C69/007 , C07C69/738 , C07D211/22 , C07D401/06 , C07D401/10 , C07C2101/02
摘要： The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula ##STR1## wherein W represents --C(.dbd.O)-- or --CH(OH)--;R.sub.1 represents hydrogen or hydroxy;R.sub.2 represents hydrogen;R.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ;n is an integer of from 1 to 5;m is an integer 0 or 1;R.sub.3 is --COOH or --COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; andpharmaceutically acceptable salts and individual optical isomers thereof,with the proviso that where R.sub.1 and R.sub.2 are ta to form a second bond between the carbon R.sub.1 and R.sub.2 or where R.sub.1 represented hydroxy integer 0.
摘要翻译：本发明涉及可用于制备下式其中W代表-C（= O） - 或-CH（OH） - 的某些抗组氨酸哌啶衍生物的新中间体和方法; R1代表氢或羟基; R2表示氢; R1和R2一起形成带有R1和R2的碳原子之间的第二个键; n为1〜5的整数， m为整数0或1; R3是-COOH或-COO烷基，其中烷基部分具有1至6个碳原子，并且是直链或支链的，每个A是氢或羟基; 以及其药学上可接受的盐和单独的光学异构体，条件是其中R 1和R 2为ta以在碳R 1和R 2之间形成第二个键，或其中R 1表示羟基整数0。

5. 发明授权

US5650416A Piperidinyl thiacyclic derivatives 失效
公开(公告)号：US5650416A
公开(公告)日：1997-07-22
申请号：US449615
申请日：1995-05-24
申请人： Albert A. Carr , John M. Kane , George D. Maynard , Hsien C. Cheng , Mark W. Dudley
发明人： Albert A. Carr , John M. Kane , George D. Maynard , Hsien C. Cheng , Mark W. Dudley
IPC分类号： A61K31/4433 , A61K31/445 , A61K31/454 , A61P37/08 , C07D409/06 , C07D409/14 , C07D417/06 , C07D417/14 , C07D417/02
CPC分类号： C07D409/06 , C07D409/14 , C07D417/06 , C07D417/14
摘要： Piperidinyl thiacyclic derivatives of the formula ##STR1## wherein X, Y, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are defined in the specification, are useful in the treatment of allergic diseases and diseases responding to antagonism of 5HT.sub.2 receptors. Pharmaceutical compositions and methods of treatment using these compounds are also disclosed.

6. 发明授权

US5631268A Piperidinyl thiacyclic derivatives 失效
标题翻译：哌啶基硫辛酸衍生物
公开(公告)号：US5631268A
公开(公告)日：1997-05-20
申请号：US449034
申请日：1995-05-24
申请人： Albert A. Carr , John M. Kane , George D. Maynard , Hsien C. Cheng , Mark W. Dudley
发明人： Albert A. Carr , John M. Kane , George D. Maynard , Hsien C. Cheng , Mark W. Dudley
IPC分类号： A61K31/4433 , A61K31/445 , A61K31/454 , A61P37/08 , C07D409/06 , C07D409/14 , C07D417/06 , C07D417/14 , C07D417/02
CPC分类号： C07D409/06 , C07D409/14 , C07D417/06 , C07D417/14
摘要： Piperidinyl thiacyclic derivatives of the formula ##STR1## wherein X, Y, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are defined in the specification, are useful in the treatment of allergic diseases and diseases responding to antagonism of 5HT.sub.2 receptors. Pharmaceutical compositions and methods of treatment using these compounds are also disclosed.
摘要翻译：其中X，Y，R 1，R 2，R 3和R 4在本说明书中定义的式IMA图形的哌啶基thiacyclic衍生物可用于治疗对5HT2受体拮抗作用的过敏性疾病和疾病。还公开了使用这些化合物的药物组合物和治疗方法。

7. 发明授权

US5397789A Cyclic nitrones 失效
标题翻译：环状硝酮
公开(公告)号：US5397789A
公开(公告)日：1995-03-14
申请号：US170543
申请日：1993-12-20
申请人： Albert A. Carr , Craig E. Thomas , Ronald C. Bernotas , George Ku
发明人： Albert A. Carr , Craig E. Thomas , Ronald C. Bernotas , George Ku
IPC分类号： C07D209/44 , C07D209/96 , C07D217/08 , C07D217/24 , C07D221/20 , C07D223/16 , A61K31/47
CPC分类号： C07D221/20 , C07D209/44 , C07D209/96 , C07D217/08 , C07D217/24 , C07D223/16
摘要： The present invention is directed to a new class of cyclic nitrones and their use as spin trapping agents.
摘要翻译：本发明涉及一类新的环状硝酸盐及其作为自旋捕获剂的用途。

8. 发明授权

US5292752A Antithrombotic compounds 失效
标题翻译：抗血栓化合物
公开(公告)号：US5292752A
公开(公告)日：1994-03-08
申请号：US847971
申请日：1992-03-05
申请人： Albert A. Carr , Richard C. Dage , John E. Koerner , Tung Li , Francis P. Miller , Thaddeus R. Nieduzak
发明人： Albert A. Carr , Richard C. Dage , John E. Koerner , Tung Li , Francis P. Miller , Thaddeus R. Nieduzak
IPC分类号： C07D211/32 , A61K31/445
CPC分类号： C07D211/32 , Y10S514/81 , Y10S514/811 , Y10S514/812 , Y10S514/813 , Y10S514/821 , Y10S514/822
摘要： The present invention is directed to a new class of piperidinyl medicinal agents which are useful as antithrombotic agents and as serotonin 5HT.sub.2 antagonists.
摘要翻译：本发明涉及可用作抗血栓形成剂和5-羟色胺5HT 2拮抗剂的新一类哌啶基药物。

9. 发明授权

US4341698A Enkaphalin derivatives 失效
标题翻译：恩考芬素衍生物
公开(公告)号：US4341698A
公开(公告)日：1982-07-27
申请号：US130431
申请日：1980-03-14
申请人： Albert A. Carr , Robert A. Farr , John M. Kane
发明人： Albert A. Carr , Robert A. Farr , John M. Kane
IPC分类号： A61K38/00 , C07D241/08 , C07K5/078 , C07K5/117 , C07C103/52
CPC分类号： C07K5/06139 , C07D241/08 , C07K5/1024 , A61K38/00
摘要： Novel analgesic and antipsychotic agents having the formula ##STR1## wherein Q is ##STR2## in which R.sub.1 is hydrogen, hydroxy or halogen and R.sub.4 is hydrogen or, R.sub.1 and R.sub.4 are both hydroxy; Z is hydrogen or straight chain lower alkyl having from 1 to 4 carbon atoms and X is methylene, carbonyl, hydroxymethylene, thio, sulfinyl or sulfonyl, or Z and X, taken together, are methylidenyl, with the proviso that when X is sulfonyl or sulfinyl, Z is other than hydrogen; R.sub.5 is hydrogen or halogen, and R.sub.2 is H, a straight or branched lower alkyl group having from 1 to 4 carbon atoms, the group ##STR3## or the group ##STR4## wherein R.sub.3 is hydroxy, amino, alkylamino or dialkylamino wherein the alkyl moiety is straight or branched and has from 1 to 4 carbon atoms, diastereomers, enantiomers and pharmaceutically acceptable salts thereof.
摘要翻译：其中Q为的新型止痛剂和抗精神病药，其中R1为氢，羟基或卤素，R4为氢或R1和R4均为羟基; Z是氢或具有1至4个碳原子的直链低级烷基，X是亚甲基，羰基，羟基亚甲基，硫代，亚磺酰基或磺酰基，或Z和X一起是亚甲基，条件是当X是磺酰基或亚磺酰基，Z不是氢; R 5是氢或卤素，R 2是H，具有1至4个碳原子的直链或支链低级烷基，基团“IMAGE”或基团“IMAGE”，其中R 3是羟基，氨基，烷基氨基或二烷基氨基，其中烷基部分是直链或支链的并且具有1至4个碳原子，非对映异构体，对映异构体和药学上可接受的盐。

10. 发明授权

US3957986A Antiviral compositions containing bis-basic esters and amides of xanthene and xanthone 失效
标题翻译：含有呫吨和呫吨酮的双碱性酯和酰胺的抗病毒组合物
公开(公告)号：US3957986A
公开(公告)日：1976-05-18
申请号：US375754
申请日：1973-07-02
申请人： Albert A. Carr , Robert W. Fleming , Arthur D. Sill
发明人： Albert A. Carr , Robert W. Fleming , Arthur D. Sill
IPC分类号： A01N9/00
CPC分类号： Y10S514/889
摘要： Novel bis-basic esters and amides of xanthene and xanthone of the formula ##SPC1##Wherein:Z is oxygen or H.sub.2 ; each of R.sup.1 and R.sup.2 is hydrogen, (lower)-alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 ring carbon atoms, alkenyl of 3 to 6 carbon atoms having the vinyl unsaturation in other than the 1-position of the alkenyl group, or each set of R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached is pyrrolidino, piperidino, N-(lower)alkylpiperazino, or morpholino;Each A is alkylene of 2 to about 8 carbon atoms and separates its adjacent Y and amino nitrogen by an alkylene chain of at least 2 carbon atoms; and each Y is oxygen, or >N--R wherein R is hydrogen or (lower)-alkyl of 1 to 4 carbon atoms;Or a pharmaceutically acceptable acid addition salt thereof. These compounds can be used as pharmaceuticals for preventing or inhibiting a viral infection.
摘要翻译：呫吨和呫吨酮的新型双碱性酯和酰胺，式为：

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