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1. 发明申请

WO2007027987A2 METHOD OF TREATING PARKINSON'S DISEASE WITH DIARYLMETHYLPIPERAZINE COMPOUNDS EXHIBITING DELTA RECEPTOR AGONIST ACTIVITY 审中-公开
标题翻译：二胺嘧啶化合物治疗帕金森病的方法展示DELTA受体激动剂活性
公开(公告)号：WO2007027987A2
公开(公告)日：2007-03-08
申请号：PCT/US2006034181
申请日：2006-09-01
申请人： MOUNT COOK BIOSCIENCES INC , CHANG KWEN-JEN , PENDERGAST WILLIAM , HOLT JONATHAN D S
发明人： CHANG KWEN-JEN , PENDERGAST WILLIAM , HOLT JONATHAN D S
IPC分类号： A61K31/495
CPC分类号： A61K31/495 , A61K9/7023 , A61K31/496 , A61K45/06 , C07D241/04 , A61K2300/00
摘要： Compositions and methods for treatment of Parkinson's disease to reduce the negative side effects of the disease by administering a therapeutically effective diarylmethylpiperazine compound which exhibits delta opioid receptor agonist activity, and optionally, mu receptor antagonist activity.
摘要翻译：用于治疗帕金森病的组合物和方法，通过施用具有δ阿片受体激动剂活性的治疗有效的二芳基甲基哌嗪化合物和任选的mu受体拮抗剂活性来减少疾病的负面副作用。

2. 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。

3. 发明申请

WO1998003177A1 METHOD OF TREATING SINUSITIS WITH URIDINE TRIPHOSPHATES AND RELATED COMPOUNDS 审中-公开
标题翻译：用尿苷磷酸酯和相关化合物处理辛烷肟的方法
公开(公告)号：WO1998003177A1
公开(公告)日：1998-01-29
申请号：PCT/US1997011795
申请日：1997-07-03
申请人： INSPIRE PHARMACEUTICALS, INC. , JABOBUS, Karla , RIDEOUT, Janet , YERXA, Ben , PENDERGAST, William , SIDDIQI, Suhaib , DRUTZ, David, J.
发明人： INSPIRE PHARMACEUTICALS, INC.
IPC分类号： A61K31/52
CPC分类号： A61K31/7048 , A61K31/7068 , A61K31/7072 , A61K31/7076 , C07H19/10 , C07H19/20
摘要： The invention is the method of treating sinusitis using nucleoside phosphates selected from UTP, ATP, CTP or derivative thereof, or using dinucleoside tetraphosphates of adenosine or uridine.
摘要翻译：本发明是使用选自UTP，ATP，CTP或其衍生物的核苷磷酸盐或使用腺苷或尿苷的二核苷四磷酸治疗鼻窦炎的方法。

4. 发明申请

WO0145691A3 METHOD OF TREATING GASTROINTESTINAL TRACT DISEASE WITH PURINERGIC RECEPTOR AGONISTS 审中-公开
标题翻译：用纯化受体激动剂治疗胃肠疾病的方法
公开(公告)号：WO0145691A3
公开(公告)日：2002-04-18
申请号：PCT/US0035439
申请日：2000-12-22
申请人： INSPIRE PHARMACEUTICALS INC , YERXA BENJAMIN R , RIDEOUT JANET L , PENDERGAST WILLIAM , SHAVER SAMMY R , ZHANG ZHEN , PETERSON WARD M , COWLEN MATHEW
发明人： YERXA BENJAMIN R , RIDEOUT JANET L , PENDERGAST WILLIAM , SHAVER SAMMY R , ZHANG ZHEN , PETERSON WARD M , COWLEN MATHEW
IPC分类号： C07H19/048 , A61K9/02 , A61K31/00 , A61K31/706 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61K31/7084 , A61K45/00 , A61P1/00 , A61P1/02 , A61P1/04 , A61P1/10 , A61P1/12 , A61P31/10 , A61P43/00 , C07H19/10 , C07H19/20 , C07H19/207 , A61K31/70
CPC分类号： A61K31/7072 , A61K31/00 , A61K31/7068 , A61K31/7084
摘要： The invention provides a method of regulating water and mucin secretions and fluid transport in the gastrointestinal tract. The invention also provides a method for treating a gastrointestinal disease in which the mucosal barrier of the gastrointestinal system is impaired. The invention additionally provides a method for correcting disorders of fluid secretion or absorption in the gastrointestinal system. The method comprises administering to a patient a pharmaceutical composition comprising a purinergic P2Y receptor agonist, in an amount effective to regulate water and mucin secretions or to correct abnormal fluid transport in the gastrointestinal tract. The pharmaceutical composition used in this invention comprises a P2Y purinergic receptor agonist such as uridine 5'-diphosphate (UDP), uridine 5'-triphosphate (UTP), cytidine 5'-diphosphate (CDP), cytidine 5'-triphosphate (CTP), adenosine 5'-diphosphate (ADP), adenosine 5'-triphosphate (ATP), and their analogs; and dinucleotide polyphosphate compounds of general Formula (IV). Said compound is prepared in an oral form, an injectable form, or a suppository form, and administered to a patient.
摘要翻译：本发明提供调节胃肠道中水分和粘蛋白分泌物和液体输送的方法。本发明还提供了一种治疗消化道疾病的方法，其中胃肠系统的粘膜屏障受损。本发明另外提供了一种校正胃肠系统中的流体分泌或吸收紊乱的方法。该方法包括向患者施用含有嘌呤能P2Y受体激动剂的药物组合物，其量可有效调节水和粘蛋白分泌物或纠正在胃肠道中的异常流体转运。用于本发明的药物组合物包含P2Y嘌呤能受体激动剂如尿苷5'-二磷酸（UDP），尿苷5'-三磷酸（UTP），胞苷5'-二磷酸（CDP），胞苷5'-三磷酸（CTP），腺苷5'-二磷酸（ADP），腺苷5'-三磷酸（ATP）及其类似物; 和通式（IV）的二核苷酸多磷酸酯化合物。所述化合物以口服形式，可注射形式或栓剂形式制备，并施用于患者。

5. 发明申请

WO9834942A2 CERTAIN DINUCLEOTIDES AND THEIR USE AS MODULATORS OF MUCOCILIARY CLEARANCE AND CILIARY BEAT FREQUENCY 审中-公开
标题翻译：某些蛋白质及其作为微粒间隔和半球形频率的调制器使用
公开(公告)号：WO9834942A2
公开(公告)日：1998-08-13
申请号：PCT/US9802702
申请日：1998-02-06
申请人： INSPIRE PHARMACEUTICALS INC , PENDERGAST WILLIAM , YERXA BENJAMIN R , RIDEOUT JANET L , SIDDIQI SUHAIB M
发明人： PENDERGAST WILLIAM , YERXA BENJAMIN R , RIDEOUT JANET L , SIDDIQI SUHAIB M
IPC分类号： C07H19/207 , A61K9/00 , A61K31/7084 , A61P11/00 , A61P27/02 , A61P27/16 , A61P43/00 , C07H19/10 , C07H19/20 , C07H21/00 , C07H
CPC分类号： C07H19/10 , A61K9/0048 , C07H19/20 , C07H21/00
摘要： The present invention relates to certain novel dinucleotides and formulations thereof which are highly selective agonists of the P2Y2 and/or P2Y4 purinergic receptor. They are useful in the treatment of chronic obstructive pulmonary diseases such as chronic bronchitis, PCD, cystic fibrosis, as well as prevention of pneumonia due to immobility. 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, otitis media and nasolacrimal duct obstruction. They are also useful for treatment of dry eye disease and retinal detachment.
摘要翻译：本发明涉及作为P2Y2和/或P2Y4嘌呤能受体的高选择性激动剂的某些新型二核苷酸及其制剂。它们可用于治疗慢性阻塞性肺疾病如慢性支气管炎，PCD，囊性纤维化，以及由于不动而预防肺炎。此外，由于其清除保留的粘液分泌物和刺激睫状肌痉挛频率的一般能力，本发明的化合物也可用于治疗鼻窦炎，中耳炎和鼻泪管阻塞。它们也可用于治疗干眼症和视网膜脱离。

6. 发明申请

WO2007027987A3 METHOD OF TREATING PARKINSON'S DISEASE WITH DIARYLMETHYLPIPERAZINE COMPOUNDS EXHIBITING DELTA RECEPTOR AGONIST ACTIVITY 审中-公开
公开(公告)号：WO2007027987A3
公开(公告)日：2007-03-08
申请号：PCT/US2006/034181
申请日：2006-09-01
申请人： MOUNT COOK BIOSCIENCES, INC. , CHANG, Kwen-Jen , PENDERGAST, William , HOLT, Jonathan, D.S.
发明人： CHANG, Kwen-Jen , PENDERGAST, William , HOLT, Jonathan, D.S.
IPC分类号： A61K31/50
摘要： Compositions and methods for treatment of Parkinson's disease to reduce the negative side effects of the disease by administering a therapeutically effective diarylmethylpiperazine compound which exhibits delta opioid receptor agonist activity, and optionally, mu receptor antagonist activity.

7. 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。

8. 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。

9. 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。

10. 发明申请

WO1991019700A1 PHARMACEUTICALLY ACTIVE BENZOQUINAZOLINE COMPOUNDS 审中-公开
标题翻译：药用活性苯并噻唑化合物
公开(公告)号：WO1991019700A1
公开(公告)日：1991-12-26
申请号：PCT/GB1991000977
申请日：1991-06-18
申请人： THE WELLCOME FOUNDATION LIMITED , PENDERGAST, William , DICKERSON, Scott, Howard , JOHNSON, Julius, Vass , FERONE, Robert
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： C07D239/70
CPC分类号： C07D403/12 , C07D239/70 , C07D239/88 , C07D417/12
摘要： Compounds of formula (I) or salts thereof, wherein the dotted line represents a single or double bond, R is alkyl or amino optionally substituted by alkyl, alkanoyl or benzyl group; R , R , R and R are the same or different and each is selected from hydrogen, phenyl, halo, nitro, a group S(O)nR wherein n is the integer 0, 1 or 2 and R is halo or alkyl or a group NR R wherein R and R are both hydrogen, a group NR R wherein R and R are the same or different and each is hydrogen or alkyl, a group OR wherein R is hydrogen or C1-4 of alkyl optionally substituted by halo; a C1-4 aliphatic group optionally substituted by a group OR or NR R wherein R and R are the same or different and each is hydrogen or alkyl; or two of R to R are linked together to form a benzo group, or one of R to R is a group X-Y-R wherein X is CH2, NR , CO or S(O)m and Y is CH2, NR , O or S(O)m, or X-Y is O, NR , -CH=CH- or N=N-, are disclosed as pharmacological agents useful in the treatment of tumours. Pharmaceutical compositions and methods for the preparation of compounds of formula (I) are also described.
摘要翻译：式（I）化合物或其盐，其中虚线表示单键或双键，R 1是任选被烷基，烷酰基或苄基取代的烷基或氨基; R 2，R 3，R 4和R 5相同或不同，各自选自氢，苯基，卤素，硝基，基团S（O）n R 8，其中n为整数0,1或2和R 8是卤素或烷基或基团NR 9 R 10，其中R 9和R 10均为氢，NR 11 R 12 其中R 11和R 12相同或不同，各自为氢或烷基，OR 13，其中R 13为氢或任选被卤素取代的烷基的C 1-4; 任选被OR 14或NR 14 R 15基团取代的C 1-4脂族基团，其中R 14和R 15相同或不同，各自为氢或烷基; 或R 2至R 5中的两个连接在一起形成苯并基团，或R 2至R 5之一为XYR 16基团，其中X为CH 2，NR 17， CO或S（O）m，Y是CH 2，NR 17，O或S（O）m，或XY是O，NR 17，-CH = CH-或N = N- 可用于治疗肿瘤的药剂。还描述了制备式（I）化合物的药物组合物和方法。

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