公开(公告)号：US4457941A

公开(公告)日：1984-07-03

申请号：US360753

申请日：1982-03-22

Applicant: Howard J. Ringold ,  L. David Waterbury

Inventor： Howard J. Ringold ,  L. David Waterbury

IPC: A61K31/40

CPC classification number: A61K31/40

Abstract: The present invention concerns a new use of certain pyrrolo-pyrrole compounds of chemical formulas (A), (B), (C), and (D): ##STR1## for the treatment of microvascular complications associated with diabetes such as, for example, diabetic retinopathy, diabetic nephropathy and diabetic neuropathy. Pyrrolo-pyrrole compounds prevent development, restrain further progress and relieve symptoms of already developed microvascular complications of diabetes.

Abstract translation: 本发明涉及化学式（A），（B），（C）和（D）的某些吡咯并吡咯化合物的新用途：（A） ）（D）用于治疗与糖尿病有关的微血管并发症，例如糖尿病性视网膜病变，糖尿病肾病和糖尿病性神经病变。 吡咯并吡咯化合物预防发展，抑制进一步的进展，缓解已发展的糖尿病微血管并发症的症状。

公开(公告)号：US06197826B1

公开(公告)日：2001-03-06

申请号：US09354577

申请日：1999-07-16

Applicant: L. David Waterbury ,  John M. Carney ,  Allan L. Wilcox

Inventor： L. David Waterbury ,  John M. Carney ,  Allan L. Wilcox

IPC: A01N3324

CPC classification number: C07C291/02

Abstract: Disclosed are novel &agr;-(2-hydroxyphenyl) nitrone compounds and pharmaceutical compositions containing such compounds. The disclosed compositions are useful as therapeutics for inflammation-related conditions in mammals, such as arthritis, and as analytical reagents for detecting free radicals.

Abstract translation: 公开了新的α-（2-羟基苯基）硝酮化合物和含有这些化合物的药物组合物。 所公开的组合物可用作哺乳动物例如关节炎中的炎症相关病症的治疗剂，以及用作检测自由基的分析试剂。

公开(公告)号：US5057621A

公开(公告)日：1991-10-15

申请号：US39560

申请日：1987-04-16

Applicant: Gary F. Cooper ,  John H. Fried ,  L. David Waterbury

Inventor： Gary F. Cooper ,  John H. Fried ,  L. David Waterbury

IPC: C07C405/00 ,  C07C177/00

CPC classification number: C07C405/00

Abstract: This invention covers a compound of the formula ##STR1## wherein R is hydrogen, lower alkyl or a pharmaceutically acceptable, non-toxic salt of a compound wherein R is hydrogen; X is hydrogen, halo, trifluoromethyl, lower alkyl or lower alkoxy, Y is lower alkyl or ##STR2## wherein Z is hydrogen, halo, methyl, methoxy or trifluoromethyl; and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta..

Abstract translation: 本发明涵盖下式的化合物，其中R是氢，其中R是氢的化合物的低级烷基或药学上可接受的无毒盐; X是氢，卤素，三氟甲基，低级烷基或低级烷氧基，Y是低级烷基或者其中Z是氢，卤素，甲基，甲氧基或三氟甲基; 波浪线表示α或β配置，条件是当一条波浪线为α时，另一条波长为β。

公开(公告)号：US4847269A

公开(公告)日：1989-07-11

申请号：US899449

申请日：1986-08-22

Applicant: Robin D. Clark ,  L. David Waterbury

Inventor： Robin D. Clark ,  L. David Waterbury

IPC: A61K31/16 ,  A61K31/17 ,  A61K31/445 ,  C07C275/40 ,  C07D295/135

CPC classification number: C07D295/135 ,  A61K31/16 ,  A61K31/17 ,  A61K31/445 ,  C07C275/40 ,  Y10S514/913

Abstract: Intraocular hypertensive diseases such as glaucoma are treated with compounds represented by formula I ##STR1## or a pharmaceutically acceptable acid addition salt thereof, whereinR.sub.1 is alkyl of two to four carbon atoms; andR.sub.2 is alkyl of three or four carbon atoms; orR.sub.1 and R.sub.2 taken together with N form ##STR2## wherein n is 0, 1, or 2 and R.sub.5 and R.sub.6 are each independently lower alkyl or hydro;R.sub.3 is hydro or hydroxy;R.sub.4 is hydro, lower alkyl, amino, or lower alkylamino.

Abstract translation: 用式I（I）表示的化合物或其药学上可接受的酸加成盐处理眼内高血压疾病如青光眼，其中R1是2-4个碳原子的烷基; R2为3或4个碳原子的烷基; 或者R 1和R 2与N一起形成，其中n是0,1或2，R 5和R 6各自独立地是低级烷基或氢; R3是氢或羟基; R4是氢，低级烷基，氨基或低级烷基氨基。

公开(公告)号：US4826869A

公开(公告)日：1989-05-02

申请号：US158197

申请日：1988-02-19

Applicant: Joseph M. Muchowski ,  Robin D. Clark ,  L. David Waterbury

Inventor： Joseph M. Muchowski ,  Robin D. Clark ,  L. David Waterbury

IPC: A61K31/40 ,  A61P27/02 ,  A61P27/06 ,  C07D207/09 ,  C07D207/32 ,  C07D207/335

CPC classification number: C07D207/335 ,  C07D207/09

Abstract: N-(lower alkyl)-2-(3'-ureidobenzyl)pyrrolidines and N-(lower alkyl)-2-(3'-ureidobenzyl)-5-(lower alkyl)pyrrolidines are useful for lowering intraocular pressure in mammals, for example, in the treatment of glaucoma.

公开(公告)号：US4642378A

公开(公告)日：1987-02-10

申请号：US722046

申请日：1985-04-11

Applicant: Robin D. Clark ,  L. David Waterbury

Inventor： Robin D. Clark ,  L. David Waterbury

IPC: C07C275/40 ,  C07C127/19

CPC classification number: C07C275/40

Abstract: Intraocular hypertensive diseases such as glaucoma are treated with compounds represented by formula I ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein R.sub.1 is alkyl of two to four carbon atoms;R.sub.2 is --(CH.sub.2).sub.n --C.sub.6 H.sub.4 --R.sub.5 ; wheren is an integer from 1 to 4; andR.sub.5 is --H, --OH, halo, lower alkyl, lower alkoxy, ureido, lower alkyl-ureido, lower alkyl-amido, or formamido;R.sub.3 is hydro or hydroxy; andR.sub.4 is hydro, lower alkyl, amino, or lower alkylamino.

公开(公告)号：US4752621A

公开(公告)日：1988-06-21

申请号：US900199

申请日：1986-08-25

Applicant: Robin D. Clark ,  L. David Waterbury

Inventor： Robin D. Clark ,  L. David Waterbury

IPC: C07C275/40 ,  A61K31/165 ,  A61K31/135 ,  A61K31/17

CPC classification number: C07C275/40 ,  Y10S514/913

Abstract: Intraocular hypertensive diseases such as glaucoma are treated with compounds represented by formula I ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein R.sub.1 is alkyl of two to four carbon atoms;R.sub.2 is --(CH.sub.2).sub.n --C.sub.6 H.sub.4 --R.sub.5 ; wheren is an integer from 1 to 4; andR.sub.5 is --H, --OH, halo, lower alkyl, lower alkoxy, ureido, lower alkyl-ureido, lower alkyl-amido, or formamido;R.sub.3 is hydro or hydroxy; andR.sub.4 is hydro, lower alkyl, amino, or lower alkylamino.

Abstract translation: 用式I（I）表示的化合物或其药学上可接受的酸加成盐处理眼内高血压疾病如青光眼，其中R1是2-4个碳原子的烷基; R2是 - （CH2）n-C6H4-R5; 其中n是1至4的整数; 并且R 5是-H，-OH，卤素，低级烷基，低级烷氧基，脲基，低级烷基 - 脲基，低级烷基 - 酰氨基或甲酰氨基; R3是氢或羟基; 并且R 4是氢，低级烷基，氨基或低级烷基氨基。

公开(公告)号：US4558066A

公开(公告)日：1985-12-10

申请号：US611245

申请日：1984-05-17

Applicant: L. David Waterbury

Inventor： L. David Waterbury

IPC: C07D405/06 ,  A61K31/40

CPC classification number: C07D405/06

Abstract: This invention relates to a method of treatment of ocular hypertension and to a topical ophthalmic pharmaceutical composition useful for management of ocular hypertension.When administered topically to an eye with increased intraocular pressure, .+-.2-[(3,4-methylenedioxy)phenethyl]-5-[(3-carboxamido-4-hydroxy)-.alpha.-hydroxybenzyl]pyrrolidines effectively decrease intraocular pressure, inhibit the deterioration of the eye due to intraocular hypertension or glaucoma and relieve the symptoms of already existing glaucoma or other ophthalmic disease.

Abstract translation: 本发明涉及治疗高眼压症的方法和用于治疗高眼压症的局部眼用药物组合物。 当局部施用眼压增高的眼睛时，+/- 2 - [（3,4-亚甲二氧基）苯乙基] -5 - [（3-甲酰胺基-4-羟基）-α-羟基苄基]吡咯烷有效降低眼内压， 抑制由于眼内高血压或青光眼引起的眼睛的退化，并缓解已经存在的青光眼或其它眼科疾病的症状。