公开(公告)号：US5508279A

公开(公告)日：1996-04-16

申请号：US206764

申请日：1994-03-07

Applicant: Nancy M. Gray

Inventor： Nancy M. Gray

IPC: C07D405/12 ,  A61K9/20 ,  A61K9/48 ,  A61K31/496 ,  A61K31/505 ,  A61K31/517 ,  A61P9/10 ,  A61P13/08 ,  A61P35/00 ,  C07D237/10 ,  A61K31/495

CPC classification number: A61K31/505

Abstract: Methods are disclosed utilizing the optically pure (+) isomer of doxazosin. This compound is a potent drug for the treatment of benign prostatic hyperplasia while avoiding the concomitant liability of hypotensive effects associated with the racemic mixture of doxazosin.

Abstract translation: 利用多沙唑嗪的光学纯（+）异构体公开了方法。 该化合物是治疗良性前列腺增生的有效药物，同时避免与多沙唑嗪的外消旋混合物相关的降压作用的伴随责任。

公开(公告)号：US5470463A

公开(公告)日：1995-11-28

申请号：US90968

申请日：1993-07-13

Applicant: Pierre Girot ,  Egisto Boschetti

Inventor： Pierre Girot ,  Egisto Boschetti

IPC: B01D15/08 ,  B01J20/32 ,  B01J39/16

CPC classification number: B01D15/20 ,  B01J20/08 ,  B01J20/28004 ,  B01J20/28057 ,  B01J20/28069 ,  B01J20/28078 ,  B01J20/288 ,  B01J20/3204 ,  B01J20/321 ,  B01J20/327 ,  B01J20/3282 ,  B01J20/3289 ,  B01J39/165 ,  B01D15/363 ,  B01D15/3804 ,  B01J2220/54 ,  B01J2220/58

Abstract: This invention relates generally to modified porous solid supports and processes for the preparation and use of same. In particular, passivated porous mineral oxide supports are disclosed which are characterized by a reversible high sorptive capacity substantially unaccompanied by non-specific adsorption of or interaction with biomolecules. Passivation is achieved by use of a passivation mixture comprising a main monomer, a passivating monomer and a crosslinking agent, which mixture upon polymerization results in the substantial elimination of the undesirable non-specific interaction with biomolecules.

Abstract translation: 本发明一般涉及改性多孔固体载体及其制备和使用方法。 特别地，公开了钝化的多孔矿物氧化物载体，其特征在于具有可逆的高吸附能力，其基本上不伴随生物分子的非特异性吸附或相互作用。 通过使用包含主单体，钝化单体和交联剂的钝化混合物实现钝化，该聚合物上的该混合物导致基本上消除了与生物分子的不期望的非特异性相互作用。

公开(公告)号：US5375693A

公开(公告)日：1994-12-27

申请号：US191061

申请日：1994-02-02

Applicant: Raymond L. Woosley ,  James W. Young ,  Yiwang Chen

Inventor： Raymond L. Woosley ,  James W. Young ,  Yiwang Chen

IPC: C07D211/22 ,  A61K9/48 ,  A61K31/137 ,  A61K31/165 ,  A61K31/192 ,  A61K31/445 ,  A61K31/451 ,  A61K31/60 ,  A61K45/00 ,  A61K45/06 ,  A61P17/00 ,  A61P27/16 ,  A61P37/08 ,  A61P43/00

CPC classification number: A61K45/06 ,  A61K31/445

Abstract: Methods and compositions are disclosed utilizing metabolic derivatives of terfenadine for the treatment of allergic disorders while avoiding the concomitant liability of adverse effects associated with the terfenadine. The metabolic derivatives of terfenadine are also useful for the treatment of retinopathy and other small vessel disorders associated with diabetes mellitus and such other conditions as may be related to the antihistamine activity of terfenadine. For example, the metabolic derivatives of terfenadine are useful for the treatment of asthma, motion sickness, and vertigo, without the concomitant liability of adverse effects associated with terfenadine. Furthermore, the metabolic derivatives of terfenadine, in combination with non-steroidal anti-inflammatory agents or other nonnarcotic analgesics, or in combination with a decongestant, cough suppressant/antitussive or expectorant, are useful for the treatment of cough, cold, cold-like, and/or flu symptoms and the discomfort, headache, pain, fever, and general malaise associated therewith, without the concomitant liability of adverse effects associated with terfenadine.

Abstract translation: 公开了使用特非那定的代谢衍生物用于治疗过敏性疾病的方法和组合物，同时避免与特非那定相关的副作用的伴随的责任。 特非那定的代谢衍生物也可用于治疗与糖尿病相关的视网膜病变和其它小血管障碍以及可能与特非那定的抗组胺药活性相关的其它病症。 例如，特非那定的代谢衍生物可用于治疗哮喘，晕车和眩晕，而不伴随与特非那定相关的副作用的责任。 此外，特非那定的代谢衍生物与非甾体抗炎药或其他非麻醉性止痛药组合，或与减充血剂，止咳剂/镇咳药或祛痰剂组合可用于治疗咳嗽，感冒，感冒 ，和/或流感症状以及与之相关的不适，头痛，疼痛，发烧和全身不适，而不伴随与特非那定相关的副作用的责任。

公开(公告)号：US5362859A

公开(公告)日：1994-11-08

申请号：US920240

申请日：1992-07-27

Applicant: Stephen E. Zale

Inventor： Stephen E. Zale

IPC: B01J20/32 ,  C07K1/22 ,  C07K16/06 ,  C07K3/20 ,  C07K17/08 ,  C07K17/12 ,  C08G63/91

CPC classification number: C07K1/22 ,  B01J20/28004 ,  B01J20/28016 ,  B01J20/28033 ,  B01J20/28057 ,  B01J20/28069 ,  B01J20/28078 ,  B01J20/3204 ,  B01J20/321 ,  B01J20/3212 ,  B01J20/3219 ,  B01J20/3227 ,  B01J20/3246 ,  B01J20/3255 ,  B01J20/3274 ,  C07K16/065 ,  B01J2220/46 ,  Y10S530/81 ,  Y10S530/811 ,  Y10S530/812 ,  Y10S530/813 ,  Y10S530/814 ,  Y10S530/815 ,  Y10S530/816

Abstract: An affinity support having an improved capacity for binding target compounds. The support includes an immobilized modified ligand of increased molecular weight. The molecular weight of the ligand is increased via the action of condensation reagents or crosslinkers prior to immobilization. The affinity support is useful in affinity separations of proteins and other biomolecules from complex, biologically-derived fluids.

Abstract translation: 具有改善的靶化合物结合能力的亲和载体。 载体包括分子量增加的固定化的修饰配体。 在固定之前，配体的分子量通过缩合试剂或交联剂的作用而增加。 亲和支持物可用于蛋白质和其他生物分子与复杂的生物衍生液体的亲和​​分离。

公开(公告)号：US5274300A

公开(公告)日：1993-12-28

申请号：US309769

申请日：1989-02-10

Applicant: David R. Dodds ,  Jorge L. Lopez

Inventor： David R. Dodds ,  Jorge L. Lopez

IPC: C07D281/10 ,  C07D303/48 ,  C12P17/02 ,  C12P41/00 ,  C12P7/62 ,  C12P7/40

CPC classification number: C12P17/02 ,  C07D281/10 ,  C07D303/48 ,  C12P41/005

Abstract: This invention relates to a method for the production of (2R,3S)-3-(4-methoxyphenyl)glycidic acids and esters thereof, which are synthetic intermediates for the production of the calcium antagonist diltiazem. The method involves the stereoselective enzymatic ester hydrolysis of racemic trans-3-(4-methoxyphenyl)glycidic acid ester to yield the resolved 2R,3S compound as the ester. Membrane reactor methods and apparatus for the conduct of this enzymatic resolution process are also disclosed herein, as is the use of bisulfite anion in the aqueous reaction phase as a means of minimizing the inhibitory effect of an aldehyde reaction by-product on the reaction's progress.

公开(公告)号：US5258517A

公开(公告)日：1993-11-02

申请号：US926254

申请日：1992-08-06

Applicant: Charles M. Zepp ,  Yun Gao ,  Donald L. Heefner

Inventor： Charles M. Zepp ,  Yun Gao ,  Donald L. Heefner

IPC: C07D211/22 ,  C07D211/88 ,  C12P41/00

CPC classification number: C07D211/88 ,  C07D211/22 ,  C12P41/005

Abstract: A biocatalytic method of preparing optically pure precursors of paroxetine and a method of preparing paroxetine therefrom are disclosed. A racemic trans ester precursor compound of paroxetine is first prepared. The racemic trans ester precursor compound comprises a mixture of (3S,4R) and (3R,4S) enantiomers. The (3R,4S) enantiomer is hydrolyzed biocatalytically to the corresponding (3R,4S)-trans carboxylic acid or alternatively, the (3S,4R) enantiomer is biocatalytically hydrolyzed the to (3S,4R)-trans carboxylic acid in a reaction catalyzed by a isolated enzyme or a microorganism. In the first instance, the unhydrolyzed (3S,4R) enantiomer is separated from the (3R,4S)-trans carboxylic acid, whereas in the second instance the (3S,4R)-trans carboxylic acid is separated from the unhydrolyzed (3R,4S) enantiomer. The (3S,4R) enantiomer obtained following the selective hydrolysis is reduced to form a (-)-trans-(3S,4R) primary alcohol precursor of paroxetine. Paroxetine is then formed from the (-)-trans-(3S,4R) primary alcohol precursor.

Abstract translation: 公开了制备帕罗西汀光学纯的前体的生物催化方法及其制备帕罗西汀的方法。 首先制备帕罗西汀的外消旋转酯前体化合物。 外消旋反式酯前体化合物包含（3S，4R）和（3R，4S）对映异构体的混合物。 将（3R，4S）对映异构体生物催化水解生成至相应的（3R，4S） - 羧酸，或者（3S，4R）对映异构体在反应催化下生物催化水解成（3S，4R） - 反式羧酸 通过分离的酶或微生物。 在第一种情况下，从（3R，4R） - 反式羧酸分离出未水解的（3S，4R）对映异构体，而在第二种情况下，将（3S，4R） - 反式羧酸与未水解的（3R， 4S）对映异构体。 在选择性水解后获得的（3S，4R）对映异构体被还原形成帕罗西汀的（ - ） - 反 - （3S，4R）伯醇前体。 然后由（ - ） - 反 - （3S，4R）伯醇前体形成帕罗西汀。

公开(公告)号：US5237073A

公开(公告)日：1993-08-17

申请号：US664515

申请日：1991-03-05

Applicant: Charles M. Zepp

Inventor： Charles M. Zepp

IPC: C07D205/04 ,  C07D207/16 ,  C07D211/60

CPC classification number: C07D211/60 ,  C07D205/04 ,  C07D207/16

Abstract: This invention relates to novel S-protected derivatives of an orally active inhibitor of an angiotensin-converting enzyme (ACE) and its analogues, which derivatives are useful for the reasons that they are (1) easily prepared from novel precursors, (2) resolvable to their optically purified stereoisomeric species and (3) convertible to non-derivatized stereoisomeric species which correspond to the pharmacologically active inhibitor and its analogues. Consequently, this invention also relates to the novel precursors. Novel methods for preparing the derivatives and their precursors are also noted herein. In addition, methods for converting the derivatives to the resolved de-derivatized stereoisomeric species of the ACE inhibitor and its analogues are described.

Abstract translation: 本发明涉及血管紧张素转换酶（ACE）及其类似物的口服活性抑制剂的新型S-保护衍生物，其衍生物是有用的，原因是它们（1）容易由新型前体制备，（2）可分解 （3）转化成对应于药理学活性抑制剂及其类似物的非衍生的立体异构物质。 因此，本发明还涉及新颖的前体。 本文还注意到制备衍生物及其前体的新方法。 此外，描述了将衍生物转化成ACE抑制剂及其类似物的分解的去衍生的立体异构体物种的方法。

公开(公告)号：US5198568A

公开(公告)日：1993-03-30

申请号：US756950

申请日：1991-09-09

Applicant: Charles M. Zepp ,  Stephen A. Wald ,  David R. Dodds

Inventor： Charles M. Zepp ,  Stephen A. Wald ,  David R. Dodds

IPC: B01J19/24 ,  C07C219/10 ,  C07C305/04 ,  C07C305/10 ,  C07C309/65 ,  C07C309/66 ,  C07C327/32 ,  C07F9/09 ,  C12N11/02 ,  C12P1/00 ,  C12P7/40 ,  C12P41/00

CPC classification number: C12P41/005 ,  B01J19/2475 ,  C07C219/10 ,  C07C305/04 ,  C07C305/10 ,  C07C309/65 ,  C07C309/66 ,  C07C327/32 ,  C07F9/091 ,  C12N11/02 ,  C12P1/00 ,  C12P41/00 ,  C12P7/40 ,  B01J2219/00159 ,  B01J2219/00162 ,  B01J2219/00177

Abstract: This invention relates to novel compositions of matter which are esters with enhanced water solubility, for use in aqueous enzymatic resolution reactions of racemic mixtures of these esters for producing the separate chiral isomers of the racemic mixture. The invention also relates to novel methods for preparing these esters. The importance of the production of the separate chiral isomers of the racemic mixtures resides in the isolation of the isomers which frequently have different biological activities. Of particular significance regarding the water soluble esters of this invention is that they are derivatized with groups which enhance their aqueous solubility and their reactivity with enzymatic resolving methods which are mediated in an aqueous environment.

Abstract translation: 本发明涉及物质的新型组合物，其是具有增强的水溶性的酯，用于这些酯的外消旋混合物的水性酶拆分反应中用于产生外消旋混合物的分离的手性异构体。 本发明还涉及制备这些酯的新方法。 外消旋混合物的分离手性异构体的生产的重要性在于分离经常具有不同生物活性的异构体。 对于本发明的水溶性酯具有特别意义的是它们用增强其水溶性的基团和它们与在水性环境中介导的酶拆分方法的反应性的基团衍生化。

公开(公告)号：US20110009416A1

公开(公告)日：2011-01-13

申请号：US12498751

申请日：2009-07-07

Applicant: Richard HSIA ,  Tushar MISRA ,  Priya CAPILA ,  Ge BAI

Inventor： Richard HSIA ,  Tushar MISRA ,  Priya CAPILA ,  Ge BAI

IPC: A61K31/4985 ,  A61P1/00

CPC classification number: A61K31/4985 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2054 ,  A61K9/2095 ,  A61K47/12

Abstract: Pharmaceutical compositions of zopiclone [(6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine)] that render the aqueous solubility/dissolution of the free base independent of the pH of the gastrointestinal tract are disclosed. The compositions are useful for oral administration.

Abstract translation: 佐匹克隆[（6-（5-氯-2-吡啶基）-5 - [（4-甲基-1-哌嗪基）羰氧基] -7-氧代-6,7-二氢-5H-吡咯并[3,4 -b]吡嗪）]，其使得游离碱的水溶性/溶解与胃肠道的pH无关。 组合物可用于口服给药。

公开(公告)号：US20100280038A1

公开(公告)日：2010-11-04

申请号：US12838554

申请日：2010-07-19

Applicant: Thomas Wessel ,  Judy Caron

Inventor： Thomas Wessel ,  Judy Caron

IPC: A61K31/4985 ,  A61P29/00

CPC classification number: A61K31/4985 ,  Y02A50/401

Abstract: The invention relates to the use of eszopiclone for the treatment of low-level, chronic pain and fatigue associated with pain.

Abstract translation: 本发明涉及使用依佐唑隆治疗与疼痛相关的低水平，慢性疼痛和疲劳。