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1. 发明专利

CA1302263C THERAPEUTIC NUCLEOSIDES 未知
公开(公告)号：CA1302263C
公开(公告)日：1992-06-02
申请号：CA518308
申请日：1986-09-16
申请人： RIDEOUT JANET L
发明人： RIDEOUT JANET L , BARRY DAVID W , LEHRMAN SANDRA N , ST CLAIR MARTHA H , FURMAN PHILLIP A , FREEMAN GEORGE A , ZIMMERMAN THOMAS P , WOLBERG GERALD , DE MIRANDA PAULO M , SHAVER SAMMY R , WHITE GEOFFREY , KIRK LEONE E III , KING DANNIE H , CLEMONS RICHARD H
IPC分类号： C07H19/06 , C07H19/10 , C07H19/16 , A61K31/505 , A61K31/70 , C07H19/073
摘要： B461 The present invention relates to certain novel 3'-azidonucleosides and pharmaceutically acceptable derivatives thereof; the use of certain 3'azidonucleosides, their pharmaceutically acceptable derivatives and therapeutic combinations containing them, in therapy, particularly in the treatment and prophylaxis of gram negative bacterial infections and retroviral infections, especially AIDS; to processes for the preparation of 3'-azidonucleosides; and toformulations containing them.

2. 发明专利

CA1321387C THERAPEUTIC NUCLEOSIDES 未知
公开(公告)号：CA1321387C
公开(公告)日：1993-08-17
申请号：CA561458
申请日：1988-03-15
申请人： RIDEOUT JANET L
发明人： RIDEOUT JANET L , FREEMAN GEORGE A , SHAVER SAMMY R
IPC分类号： C07H19/067 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61P31/12 , A61P31/18 , C07H19/06 , C07H19/073
摘要： B507 1-(3-Azido-2,3-dideoxy-.beta.-D-erythro-pentofuranosyl)-5-methyl-2(1H)-pyrimidinone is capable of conversion in vivo to 3'-azido-3'-deoxythymidine (zidovudine) and is therefore useful in human medical therapy, e.g. in the treatment or prophylaxis of Human Immunodeficiency Virus (HIV) infections such as Acquired Immune Deficiency Syndrome (AIDS). MG/AC/B507ABST/24.02.88

3. 发明专利

CA1285935C THERAPEUTIC NUCLEOSIDES 未知
公开(公告)号：CA1285935C
公开(公告)日：1991-07-09
申请号：CA504095
申请日：1986-03-14
申请人： RIDEOUT JANET L
发明人： RIDEOUT JANET L , BARRY DAVID W , LEHRMAN SANDRA N , ST CLAIR MARTHA H , FURMAN PHILLIP A , BEACHAM LOWRIE M III , LEBLANC HARRY S , FREEMAN GEORGE A
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7072 , A61K38/21 , A61P31/04 , A61P31/12 , A61P35/02 , C07H19/06 , C07H19/10 , C07H19/067
摘要： 3'-Azido-3'-deoxythymidine and its threo-3'-azido isomer and their pharmaceutically acceptable derivatives have been found to possess potent therapeutic activity, particularly against human and animal retroviral infections such as HTLV-I, HTLV-III and feline leukaemia virus, as well as against human and animal gram-negative bacterial infections.

4. 发明专利

CA2027052A1 THERAPEUTIC NUCLEOSIDES 未知
公开(公告)号：CA2027052A1
公开(公告)日：1991-04-07
申请号：CA2027052
申请日：1990-10-05
申请人： KOSZALKA GEORGE W , BURNS CHARLENE L , KRENITSKY THOMAS A , RIDEOUT JANET L
发明人： KOSZALKA GEORGE W , BURNS CHARLENE L , KRENITSKY THOMAS A , RIDEOUT JANET L
IPC分类号： C07D473/16 , A61K31/52 , A61K31/522 , A61P43/00 , C07D473/00 , C07D473/18 , C07D473/24 , C07D473/30 , C07D473/38 , C07D473/40 , C07H19/16 , C07H19/073 , A61K31/70
摘要： PB1170A 6- Substituted 2',3'-dideoxynucleosides for use in the treatment or prophylaxis of hepatitis B virus (HBV) infections and a specific novel compound, 6-(cyclopropylmethylamino)purine-9-.beta.-D-2',3'-dideoxyribo furanoside for use in the treatment of prophylaxis of HBV and human retrovirus such as Human Immunodeficiency Virus (HIV) infections and pharmaceutical formulations containing the latter compound. MG.MF.PB1170A.14th September 1990

5. 发明专利

CA2026730A1 THERAPEUTIC NUCLEOSIDES 未知
公开(公告)号：CA2026730A1
公开(公告)日：1991-04-04
申请号：CA2026730
申请日：1990-10-02
申请人： RIDEOUT JANET L , FREEMAN GEORGE A , SHORT STEVEN A , ALMOND MERRICK R , COLLINS JON L
发明人： RIDEOUT JANET L , FREEMAN GEORGE A , SHORT STEVEN A , ALMOND MERRICK R , COLLINS JON L
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61K31/708 , A61P31/12 , C07H19/16 , C12P19/40 , C07H19/173
摘要： PB1102AB The present invention relates to 3'-azido purine nucleosides and their use in medical therapy, particularly for the treatment or prophylaxis of human immunodeficiency virus and hepatitis B virus infections, to methods for their preparation and to compositions containing them. LL/AC/7th September 1990

6. 发明申请

WO9735591B1 METHOD OF TREATING CILIARY DYSKINESIA WITH URIDINE TRIPHOSPHATES AND RELATED COMPOUNDS 审中-公开
标题翻译：用尿苷磷酸酯及相关化合物处理胆固醇的方法
公开(公告)号：WO9735591B1
公开(公告)日：2001-04-26
申请号：PCT/US9705101
申请日：1997-03-27
申请人： INSPIRE PHARMACEUTICALS INC , JACOBUS KARLA M , YERXA BENJAMIN R , PENDERGAST WILLIAM , BOUCHER RICHARD C JR , RIDEOUT JANET L , DRUTZ DAVID J , JAMES MICHAEL K , STUTTS MONROE JACKSON , GEARY CARY , LAZAROWSKI EDWARDO R
发明人： JACOBUS KARLA M , YERXA BENJAMIN R , PENDERGAST WILLIAM , BOUCHER RICHARD C JR , RIDEOUT JANET L , DRUTZ DAVID J , JAMES MICHAEL K , STUTTS MONROE JACKSON , GEARY CARY , LAZAROWSKI EDWARDO R
IPC分类号： C07H19/10 , A61K9/06 , A61K9/08 , A61K9/10 , A61K9/12 , A61K9/70 , A61K31/00 , A61K31/505 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/706 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/7084 , A61P11/00 , A61P13/00 , A61P15/00 , A61P27/00 , A61P27/02 , A61P27/16 , A61P37/00 , A61P37/04 , C07H19/20 , C07H21/02
CPC分类号： A61K31/7076 , A61K31/7072
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。

7. 发明申请

WO9961012A3 THERAPEUTIC DINUCLEOTIDE AND DERIVATIVES 审中-公开
标题翻译：治疗性胆汁和衍生物
公开(公告)号：WO9961012A3
公开(公告)日：2000-02-10
申请号：PCT/US9910948
申请日：1999-05-19
申请人： INSPIRE PHARMACEUTICALS INC , UNIV NORTH CAROLINA , YERXA BENJAMIN R , PENDERGAST WILLIAM , RIDEOUT JANET L , PICHER MARYSE , BOUCHER RICHARD C , STUTTS MONROE JACKSON
发明人： YERXA BENJAMIN R , PENDERGAST WILLIAM , RIDEOUT JANET L , PICHER MARYSE , BOUCHER RICHARD C , STUTTS MONROE JACKSON
IPC分类号： C07H19/10 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7072 , A61K31/7084 , A61P11/00 , A61P11/10 , A61P11/12 , A61P27/04 , A61P27/16 , C07H19/207 , C07H21/00
CPC分类号： A61K31/7048 , A61K31/70 , C07H19/207 , C07H21/00
摘要： The present invention relates to P -(cytidine 5'-)-P -(uridine 5'-)tetraphosphates and its salts, esters and amides, and formulations thereof which are highly stable and selective agonists of the P2Y2 and/or P2Y4 purinergic receptor. The compounds of the invention are useful in the treatment of chronic obstructive pulmonary diseases such as chronic bronchitis, primary ciliary dyskinesia, cystic fibrosis, as well as prevention of pneumonia due to immobility, and the induction of sputum and its expectoration. Furthermore, because of their general ability to clear retained mucus secretions and stimulate ciliary beat frequency, the compounds of the present invention are also useful in the treatment of sinusitis and otitis media. They are also useful in the treatment of dry eye disease and retinal detachment.
摘要翻译：本发明涉及P2Y2的高稳定性和选择性激动剂的P 1 - （胞苷5' - ） - P 4 - （尿苷5'-）四磷酸及其盐，酯和酰胺及其制剂和/或P2Y4嘌呤能受体。本发明的化合物可用于治疗慢性阻塞性肺疾病如慢性支气管炎，原发性纤毛运动障碍，囊性纤维化，以及预防由于不动的肺炎，以及诱导痰及其咳痰。此外，由于它们具有清除保留的粘液分泌物和刺激睫状肌搏动频率的一般能力，本发明的化合物也可用于治疗鼻窦炎和中耳炎。它们也可用于治疗干眼症和视网膜脱离。

8. 发明申请

WO9932085A2 NOVEL PHARMACEUTICAL COMPOSITIONS OF URIDINE TRIPHOSPHATE 审中-公开
标题翻译：尿苷三磷酸的新型药物组合物
公开(公告)号：WO9932085A2
公开(公告)日：1999-07-01
申请号：PCT/US9827409
申请日：1998-12-23
申请人： INSPIRE PHARMACEUTICALS INC , LACROIX KAROL K , SHAFFER CHRISTY L , JACOBUS KARLA M , RIDEOUT JANET L , DRUTZ DAVID J , EVANS RICHARD M , PENDERGAST WILLIAM
发明人： LACROIX KAROL K , SHAFFER CHRISTY L , JACOBUS KARLA M , RIDEOUT JANET L , DRUTZ DAVID J , EVANS RICHARD M , PENDERGAST WILLIAM
IPC分类号： A61K9/00 , A61K9/08 , A61K9/72 , A61K31/70 , A61K31/7072 , A61K47/02 , A61P43/00
CPC分类号： A61K9/0078 , A61K9/08 , A61K31/7072 , A61K47/02
摘要： Novel pharmaceutical compositions of uridine 5'-triphosphate (UTP) for use in promoting increased mucociliary clearance of retained mucous secretions of the human airways, middle/inner ears or sinuses are disclosed. Novel Formulation (I) comprises UTP and aqueous solution having a therapeutic concentration between 5 and 45 mg/mL, a controlled tonicity within the range of 250 to 100 mOsM, a pH between 7.0 and 7.5, and is sterile. The pH-adjusted composition is capable of long-term storage in the refrigerated state with a shelf life of up to 30 months. Formulation (I) may be delivered therapeutically either in a nebulized form or in a liquid form. Novel Formulation (II) comprises UTP in an aqueous solution having a therapeutic concentration approaching the limit of UTP's solubility at ambient temperature or in a suspension which exceeds drug solubility. This high concentration allows delivery of a therapeutic amount of UTP in very small volumes (50 to 100 mu L) suitable for administration via portable hand-held devices such as metered dose inhalers. Formulation (II) has extended shelf life without the need for refrigeration after being dispensed to the patient.
摘要翻译：公开了用于促进对人气道，中耳/内耳或窦的保留的粘液分泌物的增加的粘膜纤毛清除的尿苷5'-三磷酸（UTP）的新型药物组合物。新配方（I）包括UTP和治疗浓度为5至45mg / mL的水溶液，控制张力在250至100mOsM范围内，pH在7.0至7.5之间，并且是无菌的。经pH调节的组合物能够在冷藏状态下长期储存，保质期长达30个月。制剂（I）可以以雾化形式或液体形式递送。新型制剂（II）在具有接近UTP在环境温度下的溶解度或超过药物溶解度的悬浮液中的治疗浓度的水溶液中包含UTP。这种高浓度允许以非常小的体积（50至100μL）递送治疗量的UTP，其适用于经由便携式手持式装置例如计量吸入器的给药。制剂（II）延长了保质期，而不需要在分配给患者后进行制冷。

9. 发明申请

WO0050024A2 METHOD OF PROMOTING MUCOSAL HYDRATION WITH CERTAIN URIDINE, ADENINE AND CYTIDINE DIPHOSPHATES AND ANALOGS THEREOF 审中-公开
标题翻译：使用某些酸，腺嘌呤和硫酸二氢钾促进粘膜水化的方法及其类似物
公开(公告)号：WO0050024A2
公开(公告)日：2000-08-31
申请号：PCT/US0005282
申请日：2000-02-25
申请人： INSPIRE PHARMACEUTICALS INC , YERXA BENJAMIN R , RIDEOUT JANET L , JONES ARTHUR C
发明人： YERXA BENJAMIN R , RIDEOUT JANET L , JONES ARTHUR C
IPC分类号： A61K31/7068 , A61K31/7072 , A61K31/00
CPC分类号： A61K31/7064 , A61K31/7048 , A61K31/7068 , A61K31/7072 , A61K31/7076 , Y10S514/912
摘要： A method and preparation for the stimulation of mucosal hydration in a subject in need of such treatment is disclosed. The method comprises administering to the mucosal surfaces of the subject a purinergic receptor agonist such as uridine 5'-diphosphate (UDP), dinucleotides, cytidine 5'-diphosphate (CDP), adenosine 5'-diphosphate (ADP), or their therapeutically useful analogs and derivatives, in an amount effective to stimulate mucin secretion. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include: topical administration via a liquid, gel, cream, or as part of a contact lens or selective release membrane; or systemic administration via nasal drops or spray, inhalation by nebulizer or other device, oral form (liquid or pill), injectable, intra-operative instillation or suppository form. A method for facilitating the expectoration of sputum for the purpose of detecting cellular abnormalities indicative of lung disease is also disclosed.
摘要翻译：公开了在需要这种治疗的受试者中刺激粘膜水合的方法和制剂。该方法包括向受试者的粘膜表面施用嘌呤能受体激动剂如尿苷5'-二磷酸（UDP），二核苷酸，胞苷5'-二磷酸（CDP），腺苷5'-二磷酸（ADP）或其治疗上有用的类似物和衍生物，有效刺激粘蛋白分泌的量。还公开了药物制剂及其制备方法。施用该方法的方法将包括：通过液体，凝胶，霜剂或作为隐形眼镜或选择性释放膜的一部分局部给药; 或通过鼻滴或喷雾进行全身给药，通过喷雾器或其它装置吸入，口服形式（液体或丸剂），可注射的，术中滴注或栓剂形式。还公开了为了检测指示肺部疾病的细胞异常的目的而促进痰吐出的方法。

10. 发明申请

WO1998015835A1 METHOD OF EARLY LUNG CANCER DETECTION VIA SPUTUM INDUCTION AND ANALYSIS OF SPUTUM TO DETECT CANCER ASSOCIATED SUBSTANCES 审中-公开
标题翻译：早期肺癌检测方法通过SPUTUM诱导和SPUTUM分析检测癌症相关物质
公开(公告)号：WO1998015835A1
公开(公告)日：1998-04-16
申请号：PCT/US1997018137
申请日：1997-10-08
申请人： INSPIRE PHARMACEUTICALS, INC. , LACROIX, Karol, K. , SHAFFER, Christy, L. , JACOBUS, Karla, M. , RIDEOUT, Janet, L. , DRUTZ, David, J. , PENDERGAST, William , YERXA, Benjamin, R.
发明人： INSPIRE PHARMACEUTICALS, INC.
IPC分类号： G01N33/574
CPC分类号： G01N33/57423
摘要： A method of early detection of lung cancer is disclosed. The method comprises using uridine 5'-triphosphate (UTP) or related compounds to induce a sputum sample from the lungs of a subject, then using labeled reagents to detect substances in the sputum whose presence is associated with the development of lung cancer. Methods to detect cancer-associated substances in the sputum include monoclonal antibody immunostaining to detect cancer associated cellular antigens, or PCR analysis to amplify and detect cancer associated gene mutations. The UTP sputum induction agent is administered to subject by means of a liquid solution, a liquid suspension in nebulized form or by means of a dry power inhalant.
摘要翻译：公开了早期检测肺癌的方法。该方法包括使用尿苷5'-三磷酸（UTP）或相关化合物从受试者的肺中诱导痰样品，然后使用标记的试剂检测痰中与肺癌发展相关的物质。检测痰中癌症相关物质的方法包括单克隆抗体免疫染色以检测癌症相关细胞抗原，或PCR分析来扩增和检测癌症相关基因突变。通过液体溶液，雾化形式的液体悬浮液或通过干力吸入剂将UTP痰诱导剂施用于受试者。

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