公开(公告)号：US06420347B1

公开(公告)日：2002-07-16

申请号：US09101840

申请日：1998-07-17

申请人： Karla M. Jacobus ,  Benjamin R. Yerxa ,  William Pendergast ,  Richard C. Boucher, Jr. ,  Janet L. Rideout ,  David J. Drutz ,  Michael K. James ,  Monroe Jackson Stutts ,  Cary Geary ,  Edwardo R. Lazarowski

发明人： Karla M. Jacobus ,  Benjamin R. Yerxa ,  William Pendergast ,  Richard C. Boucher, Jr. ,  Janet L. Rideout ,  David J. Drutz ,  Michael K. James ,  Monroe Jackson Stutts ,  Cary Geary ,  Edwardo R. Lazarowski

IPC分类号： A61K3170

CPC分类号： A61K31/70

摘要： A method of stimulating ciliary beat frequency in a subject in need of such treatment is disclosed. The method comprises administering to the airways, ears, eyes, or genito-urinary tract of the subject a triphosphate nucleotide such as uridine 5′-triphosphate (UTP), an analog of UTP, or any other analog, in an amount effective to stimulate ciliary beat frequency. This method is useful for treating patients afflicted with ciliary dyskinesia, Kartagener's syndrome, or any other disease involving dysfunction of ciliary movement, such as male infertility caused by impairment of propulsion of the spermatozoa or immune deficiency caused by impairment of ciliary movement in neutrophils or macrophages. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include any liquid suspension (including nasal spray or nasal or eye drops), oral, inhaled by nebulization, topical, injected, suppository, intra-operative by instillation or application, or ex vivo direct application to spermatozoa.

摘要翻译： 公开了一种在需要这种治疗的受试者中刺激睫状肌搏动频率的方法。 该方法包括向受试者的气道，耳朵，眼睛或生殖泌尿道施用有效刺激的量的三磷酸核苷酸，例如尿苷5'-三磷酸（UTP），UTP类似物或任何其它类似物 睫毛拍频。 该方法可用于治疗患有睫状肌运动障碍，Kartagener综合征或涉及睫状肌运动功能障碍的任何其他疾病，例如由嗜中性粒细胞或巨噬细胞的睫状肌运动损伤引起的精子推进或免疫缺陷引起的男性不育症 。 还公开了药物制剂及其制备方法。 给药方法包括任何液体悬浮液（包括鼻喷雾或鼻腔或滴眼液），口服，通过雾化吸入，局部注射，注射，栓剂，通过滴注或施用手术，或离体直接施用于精子。

公开(公告)号：US5725842A

公开(公告)日：1998-03-10

申请号：US583671

申请日：1996-01-05

申请人： Richard C. Boucher, Jr. ,  Michael R. Knowles

发明人： Richard C. Boucher, Jr. ,  Michael R. Knowles

IPC分类号： A61K9/12 ,  A61K9/00 ,  A61K9/72 ,  A61K31/495 ,  A61K31/4965 ,  A61M11/02

CPC分类号： A61K9/0075 ,  A61K31/495 ,  A61K31/4965 ,  A61K9/008 ,  Y10S514/851

摘要： Methods are disclosed for removing retained mucus secretions from the lungs of a human subject. The method includes (1) generating an aerosol suspension of respirable solid, dry particulate amiloride, and (2) delivering by inhalation the aerosol suspension to the respiratory system of the subject. The solid particulate amiloride is comprised of particles of about 1 to 5 microns and is free of liquid amiloride particles. The aerosol suspension of respirable solid particulate amiloride is administered in an amount sufficient to achieve concentrations of amiloride on the airway surfaces of from about 10.sup.-7 to 10.sup.-3 Moles/liter. As a result of the treatment, the secretions are hydrated and more easily transported from the lung via mucociliary action. Methods are also disclosed for the treatment of cystic fibrosis in humans.

摘要翻译： 公开了用于从人受试者的肺中除去保留的粘液分泌物的方法。 该方法包括（1）产生可吸入固体，干燥颗粒状阿米洛利的气溶胶悬浮液，和（2）通过吸入将气溶胶悬浮液输送到受试者的呼吸系统。 固体微粒阿米洛利由约1至5微米的颗粒组成，并且不含液体阿米洛利颗粒。 可呼吸性固体颗粒状阿米洛利的气溶胶悬浮液以足以达到气道表面上的阿米洛利浓度为约10-7至10-3摩尔/升的量施用。 作为治疗的结果，分泌物水合并且更容易地通过粘膜纤毛作用从肺转运。 还公开了用于治疗人类囊性纤维化的方法。

公开(公告)号：US5651957A

公开(公告)日：1997-07-29

申请号：US432984

申请日：1995-05-02

申请人： Luis Miguel Molina y Vedia ,  Monroe Jackson Stutts ,  Richard C. Boucher, Jr. ,  David C. Henke

发明人： Luis Miguel Molina y Vedia ,  Monroe Jackson Stutts ,  Richard C. Boucher, Jr. ,  David C. Henke

IPC分类号： A61K9/12 ,  A61K31/4409 ,  A61K31/496 ,  A61K31/7036 ,  A61K38/00 ,  A61K38/04 ,  A61K38/12 ,  A61K38/16 ,  A61K45/00 ,  A61P11/00 ,  A61P11/08 ,  A61P11/12 ,  A61P31/04 ,  A61P31/06

CPC分类号： A61K38/164 ,  A61K38/04 ,  A61K38/12 ,  Y10S514/826 ,  Y10S514/851 ,  Y10S514/924

摘要： A method of facilitating the clearance of retained pulmonary secretions in a subject using lantibiotics is disclosed. The method comprises administering to the lungs of the subject an effective amount of a lantibiotic. The lantibiotic is preferably administered by topically applying it to the respiratory epithelia, such as by generating an aerosol thereof which is then inhaled by the subject. A preferred lantibiotic for carrying out the present invention is duramycin. The method may be used in treating disorders such as cystic fibrosis, chronic bronchitis, and asthma. Also disclosed is a method of combatting tuberculosis comprising administering a lantibiotic to a subject in need of such treatment.

公开(公告)号：US5635160A

公开(公告)日：1997-06-03

申请号：US486988

申请日：1995-06-07

申请人： Monroe J. Stutts, III ,  Richard C. Boucher, Jr. ,  Eduardo R. Lazarowski ,  Cara A. Geary

发明人： Monroe J. Stutts, III ,  Richard C. Boucher, Jr. ,  Eduardo R. Lazarowski ,  Cara A. Geary

IPC分类号： C07H19/10 ,  A61K9/00 ,  A61K9/12 ,  A61K9/72 ,  A61K31/445 ,  A61K31/495 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/7084 ,  A61P11/10 ,  C07H19/20 ,  C07H21/00

CPC分类号： C07H21/00 ,  A61K31/70 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/7084 ,  A61K9/0073 ,  Y10S514/851

摘要： A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is disclosed: ##STR1## wherein: n is from 1 to 6;X is --OH or --SH;A and B are each independently selected from the group consisting of: ##STR2## wherein R is H or Br. The compounds are useful in the treatment of airway diseases such as cystic fibrosis. Pharmaceutical formulations comprising a compound of Formula (I), and methods of hydrating mucous secretions in the lungs of a subject in need of such treatment, comprising administering to the lungs of the subject a compound of Formula I as given above, are also disclosed.

摘要翻译： 公开了式（I）化合物或其药学上可接受的盐：其中：n为1至6; X是-OH或-SH; A和B各自独立地选自：其中R是H或Br。 该化合物可用于治疗气道疾病如囊性纤维化。 包含式（I）化合物的药物制剂以及对需要这种治疗的受试者的肺中的粘液分泌物进行水合的方法，包括向受试者的肺部施用如上所述的式I化合物。