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1. 发明申请

US20080318997A1 NOVEL 4-PHENYL SUBSTITUTED TETRAHYDROISOQUINOLINES AND THERAPEUTIC USE THEREOF 审中-公开
标题翻译：新型4-苯基取代的四氢喹啉和其治疗用途
公开(公告)号：US20080318997A1
公开(公告)日：2008-12-25
申请号：US12193509
申请日：2008-08-18
申请人： James P. Beck , Anthony D. Pechulis , Arthur E. Harms
发明人： James P. Beck , Anthony D. Pechulis , Arthur E. Harms
IPC分类号： A61K31/437 , A61K31/4355 , A61K31/4365
CPC分类号： C07D491/04 , C07D493/04 , C07D495/04
摘要： Compounds are provided that, by way of their selective neurotransmitter binding useful for the treatment of various neurological and psychological disorders, e.g., ADHD. Such compounds are 4-phenyl substituted tetrahydroisoquinolines having the Formula IA, IB, IIA, IIB, IIIA or IIIC as set forth herein.
摘要翻译：提供化合物，其通过其可用于治疗各种神经和心理障碍（例如ADHD）的选择性神经递质结合。这样的化合物是如本文所述的具有式IA，IB，IIA，IIB，IIIA或IIIC的4-苯基取代的四氢异喹啉。

2. 发明申请

US20080293728A1 Complexes Comprising alpha2-Adrenergic Receptor Agonists and Compositions 审中-公开
标题翻译：包含α2-肾上腺素能受体激动剂和组合物的复合物
公开(公告)号：US20080293728A1
公开(公告)日：2008-11-27
申请号：US12121083
申请日：2008-05-15
申请人： Gregory L. McIntire , Stephen R. Davio , Arthur E. Harms , Hongna Wang
发明人： Gregory L. McIntire , Stephen R. Davio , Arthur E. Harms , Hongna Wang
IPC分类号： A61K31/498 , C07D403/12 , C07C55/20 , C07C57/03 , C07C65/10 , A61P25/00 , C07C65/05 , C07C229/36 , C07C61/29
CPC分类号： C07D403/12 , C07D498/04
摘要： A complex comprises at least an α2-adrenergic receptor agonist and a compound that provides an opposite charge to a charge on the α2-adrenergic receptor agonist, wherein the complex is charge neutral as a whole and has a solubility in a range from about 0.3 μg/ml to about 2.5 mg/ml in water at pH of about 7 and temperature of about 25° C. The complex is included in a composition, device, or implant for use in the neuroprotection of components of a neurological tissue to prevent progressive degeneration of such components. In particular, such a composition, device, or implant can be used to provide neuroprotection to cells and components of the optic nerve system.
摘要翻译：复合物包含至少一种α2-肾上腺素能受体激动剂和向α2-肾上腺素能受体激动剂上的电荷提供相反电荷的化合物，其中该络合物作为整体为电荷中性，并且在约0.3μm的范围内具有溶解度 / ml至约2.5mg / ml，pH约7，温度约25℃。该复合物包含在组合物，装置或植入物中，用于神经保护神经组织的组分以防止进行性退化的这些组件。特别地，这样的组合物，装置或植入物可用于向视神经系统的细胞和组分提供神经保护。

3. 发明申请

US20080171873A1 Synthesis of selected stereoisomers of certain substituted alcohols 审中-公开
标题翻译：某些取代的醇的选择性立体异构体的合成
公开(公告)号：US20080171873A1
公开(公告)日：2008-07-17
申请号：US11652767
申请日：2007-01-12
申请人： Arthur E. Harms
发明人： Arthur E. Harms
IPC分类号： C07D209/04 , C07D215/00 , C07D237/00 , C07D307/00 , C07D401/00
CPC分类号： C07D405/12
摘要： A process for producing one selected stereoisomer of a substituted alcohol comprises reacting a stereoisomeric amine with a halogen-substituted heterocyclic compound, or a stereoisomeric ketone or aldehyde with an amino-substituted heterocyclic compound. The process avoids the production of a racemic mixture of stereoisomers of the prior art. Such a stereoisomeric substituted alcohol can be used for anti-inflammatory therapy.
摘要翻译：制备取代醇的一种选择的立体异构体的方法包括使立体异构胺与卤素取代的杂环化合物或立体异构酮或醛与氨基取代的杂环化合物反应。该方法避免生产现有技术的立体异构体的外消旋混合物。这种立体异构取代的醇可用于抗炎治疗。

4. 发明申请

US20080114172A1 Synthesis of Selected Stereoisomers of Certain Substituted Alcohols 审中-公开
标题翻译：某些取代醇选择的立体异构体的合成
公开(公告)号：US20080114172A1
公开(公告)日：2008-05-15
申请号：US11874995
申请日：2007-10-19
申请人： Arthur E. Harms
发明人： Arthur E. Harms
IPC分类号： C07D405/12
CPC分类号： C07D405/12
摘要： A process for producing one selected stereoisomer of a substituted alcohol comprises reacting a stereoisomeric epoxide with an amine, a carboxylic acid, an amide, a sulfonyl, or a cyanide. The process avoids the production of a racemic mixture of stereoisomers of the prior art. Such a stereoisomeric substituted alcohol can be used for anti-inflammatory therapy.
摘要翻译：制备取代醇的一种所选立体异构体的方法包括使立体异构环氧化物与胺，羧酸，酰胺，磺酰基或氰化物反应。该方法避免生产现有技术的立体异构体的外消旋混合物。这种立体异构取代的醇可用于抗炎治疗。

5. 发明申请

US20120157447A1 Quinolone Carboxylic Acids, Derivatives Thereof, and Methods of Making and Using Same 失效
标题翻译：喹诺酮羧酸，其衍生物及其制备和使用方法
公开(公告)号：US20120157447A1
公开(公告)日：2012-06-21
申请号：US11864016
申请日：2007-09-28
申请人： Arthur E. Harms
发明人： Arthur E. Harms
IPC分类号： A61K31/55 , A61P31/00 , C07D223/12 , C07D215/58 , A61K31/47 , C07D401/10
CPC分类号： C07D215/233 , C07D401/04 , C07D413/04 , C07D417/04
摘要： A process of preparing a quinolone carboxylic acid or its derivatives having Formula I, Ia, or IV, as shown herein, comprises using a starting quinolone that already has one or more desired substituents at one or more particular positions on the quinolone ring and preserving the orientation of such substituents throughout the synthesis. The present process comprises fewer steps than prior-art processes. The present process also can include a simple separation of a desired enantiomer of the quinolone carboxylic acid or its derivatives from the enantiomeric mixture. Pharmaceutical compositions comprising fluoroquinolones prepared by the present process can be used effectively against a variety of microbial pathogens.
摘要翻译：如本文所示，制备具有式I，Ia或IV的喹诺酮羧酸或其衍生物的方法包括使用在喹诺酮环上的一个或多个特定位置已经具有一个或多个所需取代基的起始喹诺酮，并保留这些取代基在整个合成过程中的取向。本方法包括比现有技术方法更少的步骤。本方法还可以包括从对映异构体混合物中简单分离喹诺酮羧酸或其衍生物的所需对映异构体。包含通过本方法制备的氟喹诺酮类的药物组合物可以有效地用于各种微生物病原体。

6. 发明授权

US07632944B2 Quinolone carboxylic acids, derivatives thereof, and methods of making and using same 失效
标题翻译：喹诺酮羧酸，其衍生物及其制备和使用方法
公开(公告)号：US07632944B2
公开(公告)日：2009-12-15
申请号：US11626397
申请日：2007-01-24
申请人： Arthur E. Harms
发明人： Arthur E. Harms
IPC分类号： C07D223/00
CPC分类号： C07D401/04 , C07D215/233 , C07D413/04 , C07D417/04
摘要： A process of preparing a quinolone carboxylic acid or its derivatives having Formula I, Ia, or IV, as shown herein, comprises using a starting quinolone that already has one or more desired substituents at one or more particular positions on the quinolone ring and preserving the orientation of such substituents throughout the synthesis. The present process comprises fewer steps than prior-art processes. The present process also can include a simple separation of a desired enantiomer of the quinolone carboxylic acid or its derivatives from the enantiomeric mixture. Pharmaceutical compositions comprising fluoroquinolones prepared by the present process can be used effectively against a variety of microbial pathogens.
摘要翻译：如本文所示，制备具有式I，Ia或IV的喹诺酮羧酸或其衍生物的方法包括使用在喹诺酮环上的一个或多个特定位置已经具有一个或多个所需取代基的起始喹诺酮，并保留这些取代基在整个合成过程中的取向。本方法包括比现有技术方法更少的步骤。本方法还可以包括从对映异构体混合物中简单分离喹诺酮羧酸或其衍生物的所需对映异构体。包含通过本方法制备的氟喹诺酮类的药物组合物可以有效地用于各种微生物病原体。

7. 发明授权

US07309789B2 4-phenyl substituted tetrahydroisoquinolines and therapeutic use thereof 失效
标题翻译： 4-苯基取代的四氢异喹啉及其治疗用途
公开(公告)号：US07309789B2
公开(公告)日：2007-12-18
申请号：US11438725
申请日：2006-05-22
申请人： James P. Beck , Anthony D. Pechulis , Arthur E. Harms
发明人： James P. Beck , Anthony D. Pechulis , Arthur E. Harms
IPC分类号： C07D471/02 , C07D495/02
CPC分类号： C07D491/04 , C07D493/04 , C07D495/04
摘要： Compounds are provided that, by way of their selective neurotransmitter binding useful for the treatment of various neurological and psychological disorders, e.g., ADHD. Such compounds are 4-phenyl substituted tetrahydroisoquinolines having the Formula IA, IB, IIA, IIB, IIIA or IIIC as set forth herein.
摘要翻译：提供化合物，其通过其可用于治疗各种神经和心理障碍（例如ADHD）的选择性神经递质结合。这样的化合物是如本文所述的具有式IA，IB，IIA，IIB，IIIA或IIIC的4-苯基取代的四氢异喹啉。

8. 发明授权

US08252783B2 Quinolone carboxylic acids, derivatives thereof, and methods of making and using same 失效
标题翻译：喹诺酮羧酸，其衍生物及其制备和使用方法
公开(公告)号：US08252783B2
公开(公告)日：2012-08-28
申请号：US12561283
申请日：2009-09-17
申请人： Arthur E. Harms , Ramakrishnan Arul , Anil K. Soni
发明人： Arthur E. Harms , Ramakrishnan Arul , Anil K. Soni
IPC分类号： A61K31/553 , C07D401/04
CPC分类号： C07D401/04 , C07D215/233 , C07D403/04 , C07D413/04 , C07D417/04
摘要： A process of preparing a quinolone carboxylic acid or its derivatives having Formula I, Ia, Ib, or IV, as shown herein, comprises using a starting quinolone that already has one or more desired substituents at one or more particular positions on the quinolone ring and preserving the orientation of such substituents throughout the synthesis. The present process comprises fewer steps than prior-art processes. The present process also can include a simple separation of a desired enantiomer of the quinolone carboxylic acid or its derivatives from the enantiomeric mixture. Pharmaceutical compositions comprising fluoroquinolones prepared by the present process can be used effectively against a variety of microbial pathogens.
摘要翻译：如本文所示，制备具有式I，Ia，Ib或IV的喹诺酮羧酸或其衍生物的方法包括使用在喹诺酮环上的一个或多个特定位置已经具有一个或多个所需取代基的起始喹诺酮和在整个合成过程中保留这些取代基的取向。本方法包括比现有技术方法更少的步骤。本方法还可以包括从对映异构体混合物中简单分离喹诺酮羧酸或其衍生物的所需对映异构体。包含通过本方法制备的氟喹诺酮类的药物组合物可以有效地用于各种微生物病原体。

9. 发明申请

US20110183946A1 Complexes Comprising alpha2-Adrenergic Receptor Agonists and Methods of Providing Neuroprotection or Treating or Inhibiting Progression of Glaucoma 审中-公开
标题翻译：包含α2-肾上腺素能受体激动剂的复合物和提供神经保护作用或治疗或抑制青光眼进展的方法
公开(公告)号：US20110183946A1
公开(公告)日：2011-07-28
申请号：US13078024
申请日：2011-04-01
申请人： Gregory L. McIntire , Stephen R. Davio , Arthur E. Harms , Hongna Wang
发明人： Gregory L. McIntire , Stephen R. Davio , Arthur E. Harms , Hongna Wang
IPC分类号： A61K31/498 , A61K31/60 , A61P25/00 , A61P27/06
CPC分类号： C07D403/12 , C07D498/04
摘要： A complex comprises at least an α2-adrenergic receptor agonist and a compound that provides an opposite charge to a charge on the α2-adrenergic receptor agonist, wherein the complex is charge neutral as a whole and has a solubility in a range from about 0.3 μg/ml to about 2.5 mg/ml in water at pH of about 7 and temperature of about 25° C. The complex is included in a composition, device, or implant for use in the neuroprotection of components of a neurological tissue to prevent progressive degeneration of such components. In particular, such a composition, device, or implant can be used to provide neuroprotection to cells and components of the optic nerve system or to inhibit progression of damage to the optic nerve system resulting from glaucoma.
摘要翻译：复合物包含至少一种α2-肾上腺素能受体激动剂和向α2-肾上腺素能受体激动剂上的电荷提供相反电荷的化合物，其中该络合物作为整体为电荷中性，并且具有在约0.3μg / ml至约2.5mg / ml，pH约7，温度约25℃。该复合物包含在组合物，装置或植入物中，用于神经保护神经组织的组分以防止进行性退化的这些组件。特别地，这种组合物，装置或植入物可用于向视神经系统的细胞和组分提供神经保护，或抑制由青光眼引起的视神经系统损伤的进展。

10. 发明申请

US20100029936A1 Quinolone Carboxylic Acids, Derivatives Thereof, and Methods of Making and Using Same 失效
标题翻译：喹诺酮羧酸，其衍生物及其制备和使用方法
公开(公告)号：US20100029936A1
公开(公告)日：2010-02-04
申请号：US12561283
申请日：2009-09-17
申请人： Arthur E. Harms , Ramakrishnan Arul , Anil K. Soni
发明人： Arthur E. Harms , Ramakrishnan Arul , Anil K. Soni
IPC分类号： C07D401/10
CPC分类号： C07D401/04 , C07D215/233 , C07D403/04 , C07D413/04 , C07D417/04
摘要： A process of preparing a quinolone carboxylic acid or its derivatives having Formula I, Ia, Ib, or IV, as shown herein, comprises using a starting quinolone that already has one or more desired substituents at one or more particular positions on the quinolone ring and preserving the orientation of such substituents throughout the synthesis. The present process comprises fewer steps than prior-art processes. The present process also can include a simple separation of a desired enantiomer of the quinolone carboxylic acid or its derivatives from the enantiomeric mixture. Pharmaceutical compositions comprising fluoroquinolones prepared by the present process can be used effectively against a variety of microbial pathogens.
摘要翻译：如本文所示，制备具有式I，Ia，Ib或IV的喹诺酮羧酸或其衍生物的方法包括使用在喹诺酮环上的一个或多个特定位置已经具有一个或多个所需取代基的起始喹诺酮和在整个合成过程中保留这些取代基的取向。本方法包括比现有技术方法更少的步骤。本方法还可以包括从对映异构体混合物中简单分离喹诺酮羧酸或其衍生物的所需对映异构体。包含通过本方法制备的氟喹诺酮类的药物组合物可以有效地用于各种微生物病原体。

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