公开(公告)号：US08350079B2

公开(公告)日：2013-01-08

申请号：US12437054

申请日：2009-05-07

Applicant: David A. Walsh

Inventor： David A. Walsh

IPC: A61K31/19

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：US20110319641A1

公开(公告)日：2011-12-29

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: C07D309/12 ,  C07C51/08 ,  C07C41/08 ,  C07C67/347 ,  C07C253/30 ,  C07F7/18 ,  C07C51/09

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：USD562728S1

公开(公告)日：2008-02-26

申请号：US29270435

申请日：2006-12-22

Applicant: Mark Downing ,  David A. Walsh ,  Dana Wright Gleason, Jr.

Designer： Mark Downing ,  David A. Walsh ,  Dana Wright Gleason, Jr.

公开(公告)号：US06196969B1

公开(公告)日：2001-03-06

申请号：US09316231

申请日：1999-05-21

Applicant: Leon W. Bester ,  David A. Walsh

Inventor： Leon W. Bester ,  David A. Walsh

IPC: A61B132

CPC classification number: A61B17/0206

Abstract: A tissue retractor with an adjustable center claw. The retractor includes two pivoted retractor arms. An axially and angularly displaceable, spring biased clamping mechanism is positioned on the pivot axis. In a mounting position, a elongated clamping element aligns with a slot in the center claw. When the center claw is positioned and the clamp moves to its clamping position, the elongated clamping member clamps the center claw in position. The counterfacing surfaces of the center claw and the clamping member are toothed to provide a positive one-way ratchet clamp.

Abstract translation: 具有可调中心爪的组织牵开器。 牵开器包括两个枢转牵开臂。 轴向和角度可移位的弹簧偏压夹紧机构位于枢轴上。 在安装位置，细长夹紧元件与中心爪中的狭槽对准。 当中心爪定位并且夹具移动到其夹紧位置时，细长夹紧构件将中心爪夹紧就位。 中心爪和夹紧构件的相对表面是齿形的，以提供正单向棘轮夹。

公开(公告)号：US5057524A

公开(公告)日：1991-10-15

申请号：US476803

申请日：1990-02-08

Applicant: David A. Walsh

Inventor： David A. Walsh

IPC: C07D211/22 ,  C07D401/06

CPC classification number: C07D401/06 ,  C07D211/22

Abstract: Novel compounds useful in the treatment of allergic disorders and having the formula: ##STR1## where Ar and Ar.sup.1 are pyridinyl, phenyl, or substituted phenyl and where Y is --OH,--O.sup..crclbar. M.sup..sym. m,--O--loweralkyl, --O--Aryl, or NR.sup.1 R.sup.2 (R.sup.1, R.sup.2 .dbd.H, loweralkyl, aryl) are herein disclosed.

Abstract translation: 可用于治疗过敏性疾病并具有下式的新型化合物：其中Ar和Ar 1是吡啶基，苯基或取代的苯基，其中Y是-OH，-O（ - ）M（+）m，-O- 低级烷基，-O-芳基或NR 1 R 2（R 1，R 2 = H，低级烷基，芳基）。

公开(公告)号：US4960776A

公开(公告)日：1990-10-02

申请号：US7592

申请日：1987-01-28

Applicant: David A. Walsh ,  Albert D. Cale, Jr.

Inventor： David A. Walsh ,  Albert D. Cale, Jr.

IPC: C07D213/84 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/495 ,  A61K31/55 ,  A61P37/08 ,  C07D205/04 ,  C07D207/09 ,  C07D211/26 ,  C07D211/70 ,  C07D213/74 ,  C07D213/75 ,  C07D213/79 ,  C07D213/81 ,  C07D223/04 ,  C07D223/12 ,  C07D295/20 ,  C07D295/215

CPC classification number: C07D213/74 ,  C07D205/04 ,  C07D207/09 ,  C07D211/26 ,  C07D211/70 ,  C07D295/215

Abstract: Novel 4-aryl-N-[2-(dialkylamino and heterocyclicamino)alkyl]-1-piperazinecarboxamides of the formula: ##STR1## wherein B is oxygen or sulfur; Ar is selected from ##STR2## or 2, 3 or 4-pyridyl; X is selected from hydrogen, halogen, loweralkyl, loweralkoxy, amino, dimethylamino, nitro, trifluoromethyl, cyano, acetyl, acetylamino, aminocarbonyl, carboxy or loweralkylcarboxylic acid ester; Y is selected from hydrogen, halogen, loweralkyl, loweralkoxy, nitro, trifluoromethyl, cyano, acetylamino, aminocarbonyl, carboxy or loweralkyl carboxylic acid ester; Z is selected from hydrogen, loweralkyl or loweralkoxy; Q is selected from ##STR3## m is 1 to 3 inclusive; n is zero or 1; p is zero to 3 inclusive; R.sup.1, R.sup.2 and R.sup.3 are loweralkyl and may be the same or different, or R.sup.1 and R.sup.2 taken together with the adjacent nitrogen atom may be form a heterocyclic residue; and the pharmaceutically acceptable salts thereof are disclosed. The compounds are useful in a method of combating allergic response associated with anaphylactic sensitivity in animals and humans.

公开(公告)号：US4950674A

公开(公告)日：1990-08-21

申请号：US159940

申请日：1988-02-24

Applicant: John M. Yanni ,  David A. Walsh

Inventor： John M. Yanni ,  David A. Walsh

IPC: C07C43/225 ,  A61K31/4402 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/445 ,  A61K31/451 ,  A61K31/47 ,  A61P37/08 ,  C07C41/00 ,  C07C67/00 ,  C07D207/08 ,  C07D211/12 ,  C07D211/14 ,  C07D211/18 ,  C07D211/22 ,  C07D211/34 ,  C07D211/46 ,  C07D211/62 ,  C07D211/70 ,  C07D211/96 ,  C07D213/127 ,  C07D213/16 ,  C07D213/30 ,  C07D215/26 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07F9/6558

CPC classification number: C07D207/08 ,  C07D211/14 ,  C07D211/18 ,  C07D211/22 ,  C07D211/70 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  Y10S514/826

Abstract: A method of inhibiting Type 1 allergic responses in a living animal body with substituted heterocyclic amines is disclosed wherein the active agents are expressed generally by the formula which includes certain known and certain known compounds: ##STR1## wherein P is zero, one or two; m is one to six inclusive; A is selected from hydrogen, hydroxy or cyano; d is zero or one; Q is --CH--, CH.sub.2 -- or ##STR2## n is zero or one and when Q is --CH-- and n is one, a double bond is formed with one of the adjacent carbons but not both at the same time, and when n and d are zero at the same time, a double bond is formed between the .alpha. carbon and a carbon of the central heterocyclic amine ring; Ar, D and R are selected from phenyl, substituted phenyl, pyridinyl, thienyl, furanyl or naphthyl and in addition, R may have the values benzyl, substituted benzyl, cycloalkyl or loweralkyl and D may additionally have the values: 2H-1-benzopyran-2-one,4-oxo-4H-1-benzopyran-2-carboxylic acid loweralkyl ester, 2,3-dihydro-4H-1-benzopyran-4-one, 1,4-benzodioxanloweralkyl-2-yl or 1,1'-biphenyl-4-yl and the pharmaceutically acceptable salts thereof.

Abstract translation: 公开了一种在具有取代的杂环胺的活体动物体中抑制1型过敏反应的方法，其中活性剂通常由包括某些已知和某些已知化合物的式表示：其中P为0，1或2; m是一到六个包含; A选自氢，羟基或氰基; d为零或一; Q是-CH-，CH 2 - 或者n是0或1，当Q是-CH-并且n是1时，与相邻的碳之一形成双键，而不是同时形成双键，而当 n和d同时为零，在α碳和中心杂环胺环的碳之间形成双键; Ar，D和R选自苯基，取代的苯基，吡啶基，噻吩基，呋喃基或萘基，此外，R可以具有苄基，取代的苄基，环烷基或低级烷基，D可另外具有以下值：2H-1-苯并吡喃 -2-酮，4-氧代-4H-1-苯并吡喃-2-羧酸低级烷基酯，2,3-二氢-4H-1-苯并吡喃-4-酮，1,4-苯并二恶烷烷基-2-基或1， 1'-联苯-4-基及其药学上可接受的盐。

公开(公告)号：US4898874A

公开(公告)日：1990-02-06

申请号：US906965

申请日：1986-09-15

Applicant: David A. Walsh ,  Ibrahim M. Uwaydah

Inventor： David A. Walsh ,  Ibrahim M. Uwaydah

IPC: A61K31/42 ,  A61K31/423 ,  A61P29/00 ,  C07D261/20

CPC classification number: C07D261/20

Abstract: 3-Aryl-2,1-benzisoxazole compounds having the formula: ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or methyl;R.sup.3 and R.sup.4 are hydroxyl, loweralkoxy, amino or --OM wherein M is a pharmaceutically acceptable cation;X is hydrogen, halogen, loweralkyl or nitro;Y is selected from hydrogen, halogen, loweralkyl, loweralkoxy, nitro or trifluoromethyl;n and p are zero or one with the proviso that either n or p must be oneare disclosed, having anti-inflammatory activity and novel intermediates in the preparation thereof.

公开(公告)号：US4782089A

公开(公告)日：1988-11-01

申请号：US900599

申请日：1986-08-26

Applicant: David A. Walsh

Inventor： David A. Walsh

IPC: A61K31/195 ,  A61K31/215 ,  A61P7/02 ,  A61P25/04 ,  A61P29/00 ,  C07C67/00 ,  C07C227/00 ,  C07C227/18 ,  C07C229/42 ,  C07C229/66 ,  C07D209/14 ,  C07D209/18 ,  C07C101/447 ,  A61K31/24

CPC classification number: C07D209/18 ,  C07D209/14

Abstract: 2-Amino-3-aroyl-.gamma.-oxobenzenebutanoic acids and derivatives having the formula: ##STR1## wherein X is hydrogen, halogen, or loweralkyl; Y is hydrogen, halogen, loweralkyl, loweralkoxy, nitro, or trifluoromethyl; n is 1 or 2; and R is hydrogen, loweralkyl, or a pharmaceutically acceptable cation, are disclosed having anti-inflammatory activity.

Abstract translation: 2-氨基-3-芳酰基-γ-氧苯丁酸及其衍生物，其具有下式：其中X是氢，卤素或低级烷基; Y是氢，卤素，低级烷基，低级烷氧基，硝基或三氟甲基; n为1或2; 和R是氢，低级烷基或药学上可接受的阳离子，其具有抗炎活性。

公开(公告)号：US08940930B2

公开(公告)日：2015-01-27

申请号：US13435708

申请日：2012-03-30

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: C07C51/353 ,  C07C59/72 ,  C07C51/09 ,  C07C51/367 ,  C07C67/343 ,  C07C253/30 ,  C07F7/18

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 intermediates for treprostinil. Also described are methods of preparing treprostinil comprising utilizing novel intermediates described herein as well as novel intermediates useful for synthesis prostacyclin derivatives, such as treprostinil.

Abstract translation: 本发明涉及一种制备曲前列素合成中间体的新方法。 还描述了制备曲前列环素的方法，其包括利用本文所述的新型中间体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。