公开(公告)号：US08481782B2

公开(公告)日：2013-07-09

申请号：US13151465

申请日：2011-06-02

Applicant: Hitesh Batra ,  Raju Penmasta ,  Vijay Sharma ,  Sudersan M. Tuladhar ,  David A. Walsh

Inventor： Hitesh Batra ,  Raju Penmasta ,  Vijay Sharma ,  Sudersan M. Tuladhar ,  David A. Walsh

IPC: C07C51/36

CPC classification number: C07C51/00 ,  C07B2200/07 ,  C07C29/143 ,  C07C29/42 ,  C07C45/00 ,  C07C45/29 ,  C07C45/61 ,  C07C45/64 ,  C07C51/09 ,  C07C51/367 ,  C07C59/72 ,  C07C67/343 ,  C07C253/30 ,  C07F7/1892 ,  Y02P20/55 ,  C07C69/736 ,  C07C255/13

Abstract: The present invention is directed to a novel method for preparing a synthetic intermediate for treprostinil via a stereoselective alkyne addition reaction. Also described are methods of preparing treprostinil comprising the alkyne addition reaction described herein as well as novel intermediates useful for synthesis prostacyclin derivatives, such as treprostinil.

Abstract translation: 本发明涉及通过立体选择性炔炔加成反应制备曲前列素的合成中间体的新方法。 还描述了制备包含本文所述的炔炔加成反应的曲前列素的方法以及可用于合成前列环素衍生物例如曲前列素的新型中间体。

公开(公告)号：US20120283470A1

公开(公告)日：2012-11-08

申请号：US13548446

申请日：2012-07-13

Applicant: Hitesh Batra ,  Sudersan M. Tuladhar ,  Raju Penmasta ,  David A. Walsh

Inventor： Hitesh Batra ,  Sudersan M. Tuladhar ,  Raju Penmasta ,  David A. Walsh

IPC: C07C51/08 ,  C07C59/72

CPC classification number: A61K31/192 ,  A01N37/10 ,  C07C39/12 ,  C07C39/17 ,  C07C51/08 ,  C07C51/41 ,  C07C51/412 ,  C07C59/60 ,  C07C59/72 ,  C07C213/08 ,  C07C253/00 ,  C07C405/0075 ,  C07C2103/12

Abstract: This present invention relates to an improved process to prepare prostacyclin derivatives. One embodiment provides for an improved process to convert benzindene triol to treprostinil via salts of treprostinil and to purify treprostinil.

Abstract translation: 本发明涉及制备前列环素衍生物的改进方法。 一个实施方案提供了通过曲前列腺素盐将苯三烯三醇转化成曲前列腺素并净化曲前列素的改进方法。

公开(公告)号：US08242305B2

公开(公告)日：2012-08-14

申请号：US12334731

申请日：2008-12-15

Applicant: Hitesh Batra ,  Sudersan M. Tuladhar ,  Raju Penmasta ,  David A. Walsh

Inventor： Hitesh Batra ,  Sudersan M. Tuladhar ,  Raju Penmasta ,  David A. Walsh

IPC: C07C62/00 ,  C07C65/00

CPC classification number: A61K31/192 ,  A01N37/10 ,  C07C39/12 ,  C07C39/17 ,  C07C51/08 ,  C07C51/41 ,  C07C51/412 ,  C07C59/60 ,  C07C59/72 ,  C07C213/08 ,  C07C253/00 ,  C07C405/0075 ,  C07C2103/12

Abstract: This present invention relates to an improved process to prepare prostacyclin derivatives. One embodiment provides for an improved process to convert benzindene triol to treprostinil via salts of treprostinil and to purify treprostinil.

Abstract translation: 本发明涉及制备前列环素衍生物的改进方法。 一个实施方案提供了通过曲前列腺素盐将苯三烯三醇转化成曲前列腺素并净化曲前列素的改进方法。

公开(公告)号：US20100023061A1

公开(公告)日：2010-01-28

申请号：US12179136

申请日：2008-07-24

Applicant: David S. Randol ,  David A. Walsh

Inventor： David S. Randol ,  David A. Walsh

IPC: A61B17/70 ,  A61B17/04

CPC classification number: A61B17/7037 ,  A61B17/7032 ,  A61B2090/037

Abstract: Locking mechanisms and methods of fixation, such as the fixation of a fixation device like a bone screw and of a rod to the spine. The locking mechanism includes a body, a rod seat and a set screw. The rod seat is configured to separate into two pieces when the rod exerts force on the top portion of the washer and the set screw limits movement of the washer toward the bottom of the locking mechanism.

Abstract translation: 锁定机构和固定方法，例如将固定装置如骨螺钉和杆固定到脊柱上。 锁定机构包括主体，杆座和固定螺钉。 当杆在垫圈的顶部施加力时，杆座构造成分成两部分，并且固定螺钉限制垫圈朝向锁定机构的底部的运动。

公开(公告)号：US20090281189A1

公开(公告)日：2009-11-12

申请号：US12437054

申请日：2009-05-07

Applicant: David A. Walsh

Inventor： David A. Walsh

IPC: A61K31/192 ,  C07C59/72 ,  A61P35/00

CPC classification number: C07C59/72 ,  C07B2200/07 ,  C07B2200/13 ,  C07C51/487 ,  C07C2603/14

Abstract: There is provided a stable monohydrate form of treprostinil and pharmaceutical formulation comprising the same, method of making and using the same.

Abstract translation: 提供了一种稳定的一水合物形式的曲前列素和药物制剂，其包含其制备和使用它们的方法。

公开(公告)号：US20090240284A1

公开(公告)日：2009-09-24

申请号：US12053924

申请日：2008-03-24

Applicant: David Scott Randol ,  David A. Walsh ,  Carl Arthur Knobloch

Inventor： David Scott Randol ,  David A. Walsh ,  Carl Arthur Knobloch

IPC: A61B17/58

CPC classification number: A61B17/7004 ,  A61B17/701 ,  A61B17/7011 ,  A61B17/7029 ,  A61B17/7031 ,  A61B17/7032 ,  A61B2017/00526

Abstract: A rod, such as that used for spinal stabilization, made of both metal material and elastomeric material. The rod may have a metal infrastructure, which may be non-cylindrical, to provide a desired stiffness for bending in at least one direction and may also have metal exterior surfaces for engaging metal components of spinal fixation locking mechanisms. In addition, the elastomeric material may only partially circumferentially encapsulate the metal material so that the metal material forms part of the surface of the rod.

Abstract translation: 杆，例如用于脊柱稳定的杆，由金属材料和弹性体材料制成。 杆可以具有可以是非圆柱形的金属基础结构，以提供用于在至少一个方向上弯曲的期望的刚度，并且还可以具有用于接合脊柱固定锁定机构的金属部件的金属外表面。 此外，弹性体材料可以仅部分地周向地包封金属材料，使得金属材料形成杆的表面的一部分。

公开(公告)号：US5273993A

公开(公告)日：1993-12-28

申请号：US965140

申请日：1992-11-19

Applicant: Young S. Lo ,  Joseph C. Nolan ,  William J. Welstead, Jr. ,  David A. Walsh ,  Dwight A. Shamblee ,  Ibrahim M. Uwaydah

Inventor： Young S. Lo ,  Joseph C. Nolan ,  William J. Welstead, Jr. ,  David A. Walsh ,  Dwight A. Shamblee ,  Ibrahim M. Uwaydah

IPC: A61K31/255 ,  A61K31/33 ,  C07C307/02 ,  C07D207/26 ,  C07D207/27 ,  C07D209/08 ,  C07D211/22 ,  C07D213/65 ,  C07D215/26 ,  C07D233/54 ,  C07D277/24 ,  C07D277/28 ,  C07D285/10 ,  C07D311/16 ,  C07D319/20 ,  C07D521/00 ,  C07H11/00 ,  A61K31/415

CPC classification number: C07D207/27 ,  A61K31/255 ,  A61K31/33 ,  C07C307/02 ,  C07D209/08 ,  C07D211/22 ,  C07D213/65 ,  C07D215/26 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D249/08 ,  C07D277/24 ,  C07D277/28 ,  C07D285/10 ,  C07D311/16 ,  C07D319/20 ,  C07H11/00

Abstract: Methods of treating chronic arthritis and osteoporosis which utilize both known and novel compounds which would fall under the general formula:(HO)p--A--[--OS(O).sub.2 NR.sup.1 R.sup.2 ].sub.zwherein A encompasses a wide range of values including but not limited to aryl, loweralkyl, cycloalkyl, and carbohydrates including sucrose and fructose; p is equal to the number of unreacted hydroxy groups contained on the molecule and may be zero; z is the number of --OS(O).sub.2 NR.sup.1 R.sup.2 groups and is always at least one; R.sup.1 and R.sup.2 are selected from hydrogen, loweralkyl, carboxy and the like; a novel process for preparing the compounds is provided wherein an appropriate sulfamic acid aryl ester is reacted with a hydroxy substituted A radical which may or may not contain thereon protected carboxyl, amino or hydroxy substituents, in an aprotic solvent containing a tertiary amine base. Pharmaceutical compositions for the treatment of chronic arthritis and osteoporosis are also provided.

Abstract translation: 治疗慢性关节炎和骨质疏松症的方法，其利用了下列通式所示的已知和新型化合物：（HO）pA - [ - OS（O）2NR1R2] z其中A包括宽范围的值，包括但不限于芳基 ，低级烷基，环烷基和碳水化合物，包括蔗糖和果糖; p等于分子上包含的未反应羟基的数目，可以为零; z是-OS（O）2NR1R2基团的数目，并且总是至少一个; R1和R2选自氢，低级烷基，羧基等; 提供了一种制备该化合物的新方法，其中将适当的氨基磺酸芳基酯与羟基取代的A基团反应，羟基取代的A基团可含有或不含有保护的羧基，氨基或羟基取代基，在含有叔胺碱的非质子溶剂中。 还提供了用于治疗慢性关节炎和骨质疏松症的药物组合物。

公开(公告)号：US5063235A

公开(公告)日：1991-11-05

申请号：US516570

申请日：1990-04-30

Applicant: David A. Walsh

Inventor： David A. Walsh

IPC: C07D211/22 ,  C07D401/06 ,  C07D401/14

CPC classification number: C07D401/06 ,  C07D211/22 ,  C07D401/14

Abstract: Novel compounds of the formula: ##STR1## are disclosed wherein Ar and Ar.sup.1 are phenyl, sustituted phenyl or pyridinyl, "alk" is a C.sub.1 -C.sub.12 straight or branched hydrocarbon chain, and R is H, loweralkylcarbonyl, arylcarbonyl, or aminocarbonyl where the amino is unsubstituted or substituted by one or two groups selected from loweralkyl or aryl. The compounds of this invention are useful in the treatment of allergic disorders.

Abstract translation: 公开了新的下式化合物：其中Ar和Ar 1是苯基，维持苯基或吡啶基，“alk”是C1-C12直链或支链烃链，R是H，低级烷基羰基，芳基羰基或氨基羰基，其中 氨基未被取代或被一个或两个选自低级烷基或芳基的基团取代。 本发明的化合物可用于治疗过敏性疾病。

公开(公告)号：US5025031A

公开(公告)日：1991-06-18

申请号：US443146

申请日：1989-11-30

Applicant: Young S. Lo ,  David A. Walsh ,  Ibrahim M. Uwaydah

Inventor： Young S. Lo ,  David A. Walsh ,  Ibrahim M. Uwaydah

IPC: A61K31/255 ,  A61K31/415 ,  C07C307/02 ,  C07D215/26 ,  C07D233/22 ,  C07D233/54 ,  C07D285/10 ,  C07D311/18 ,  C07D521/00

CPC classification number: C07D233/64 ,  A61K31/255 ,  A61K31/415 ,  C07C307/02 ,  C07D215/26 ,  C07D231/12 ,  C07D233/22 ,  C07D233/56 ,  C07D249/08 ,  C07D285/10 ,  C07D311/18

Abstract: Herein disclosed is a method of treating convulsions with a pharmaceutical composition containing a compound of the formula:(HO).sub.p --A--[OSO.sub.2 NR.sup.1 R.sup.2 ].sub.zwhere A is an aryl, arylalkyl, or aryloxyalkyl group and is substituted on 1 or more carbon atoms with a sulfamate group (--OSO.sub.2 NR.sup.1 R.sup.2) wherein R.sup.1 and R.sup.2, same or different, are hydrogen or loweralkyl wherein p is 0 or 1 and is the number of untreated hydroxyl groups and z is 1 or 2 and is the number of --OS(O.sub.2)NR.sup.1 R.sup.2 groups. Aryl is selected from phenyl, substituted phenyl, pyridinyl, naphthyl, quinolinyl, and the like. Phenyl substituents are selected from hydrogen, halo, hydroxy, phenyl, phenoxy, benzoyl, loweralkyl, loweralkoxy, carboxy, amino, loweralkylamino, diloweralkylamino, acetamido, cyano, nitro, loweralkoxycarboyl, aminosulfonyl, imidazolyl, triazolyl, and the like. Novel compounds not previously disclosed are also described.

Abstract translation: 本文公开了一种用药物组合物治疗惊厥的方法，所述药物组合物含有下式化合物：（HO）pA- [OSO 2 NR 1 R 2] z，其中A是芳基，芳基烷基或芳氧基烷基，并被一个或多个碳原子取代， 氨基磺酸酯基（-OSO2NR1R2）其中R1和R2相同或不同，为氢或低级烷基，其中p为0或1，为未经处理的羟基数，z为1或2，为-OS（O 2）NR 1 R 2的数目 团体 芳基选自苯基，取代的苯基，吡啶基，萘基，喹啉基等。 苯基取代基选自氢，卤素，羟基，苯基，苯氧基，苯甲酰基，低级烷基，低级烷氧基，羧基，氨基，低级烷基氨基，二低级烷基氨基，乙酰氨基，氰基，硝基，低级烷氧基羰基，氨基磺酰基，咪唑基，三唑基等。 还描述了以前未公开的新型化合物。

公开(公告)号：US20130090690A1

公开(公告)日：2013-04-11

申请号：US13611700

申请日：2012-09-12

Applicant: David A. Walsh

Inventor： David A. Walsh

IPC: A61B17/70

CPC classification number: A61B17/7023

Abstract: A dynamic rod assembly, such as that used for spinal stabilization, made of a number of interlocking segments whereby a limited amount of relative motion is permitted between each pair of adjacent segments. The dynamic rod assembly may also incorporate a separate central element that extends at least partially through a central channel within the interlocking segments to prevent the interlocking segments from disengaging while adding to the desired bending properties of the dynamic rod assembly.

Abstract translation: 诸如用于脊柱稳定的动态杆组件由多个互锁段制成，由此在每对相邻节段之间允许有限量的相对运动。 动态杆组件还可以包括分离的中心元件，该中心元件至少部分地延伸穿过互锁段内的中心通道，以防止互锁段脱离，同时增加动态杆组件的期望的弯曲特性。