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1. 发明授权

US5405851A Pharmaceutical compounds 失效
标题翻译：药物化合物
公开(公告)号：US5405851A
公开(公告)日：1995-04-11
申请号：US869989
申请日：1992-04-16
申请人： William Pendergast , Scott H. Dickerson , Julius V. Johnson , Robert Ferone
发明人： William Pendergast , Scott H. Dickerson , Julius V. Johnson , Robert Ferone
IPC分类号： C07D239/70 , C07D403/12 , A61K31/505
CPC分类号： C07D403/12 , C07D239/70
摘要： The present invention relates to novel benzoquinazoline thymidylate synthase inhibitors, to pharmaceutical formulations containing them and to their use in medicine.
摘要翻译：本发明涉及新颖的苯并喹唑啉胸苷酸合酶抑制剂，含有它们的药物制剂及其在药物中的应用。

2. 发明授权

US06306865B1 Pharmaceutically active benzoquinazoline compounds 失效
标题翻译：药用活性苯并喹唑啉化合物
公开(公告)号：US06306865B1
公开(公告)日：2001-10-23
申请号：US09588790
申请日：2000-06-06
申请人： William Pendergast , Scott Howard Dickerson , Julius Vass Johnson , Robert Ferone
发明人： William Pendergast , Scott Howard Dickerson , Julius Vass Johnson , Robert Ferone
IPC分类号： C07D23970
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, R1 is alkyl or amino optionally substituted by alkyl, alkanoyl or benzyl group; R2, R3, R4 and R5 are the same or different and each is selected from hydrogen, phenyl, halo, nitro, a group S(O)nR8 wherein n is the integer 0, 1 or 2 and R8 is halo or alkyl or a group NR9R10 wherein R9 and R10 are both hydrogen, a group NR11R12 wherein R11 and R12 are the same or different and each is hydrogen or alkyl, a group OR13 wherein R13 is hydrogen or C1-4 of alkyl optionally substituted by halo; a C1-4 aliphatic group optionally substituted by a group OR14 or NR14R15 wherein R14 and R15 are the same or different and each is hydrogen or alkyl; or two of R2 to R5 are linked together to form a benzo group, or one of R2 to R5 is a group X—Y—R16 wherein X is CH2, NR17, CO or S(O)m and Y is CH2, NR17, O or S(O)m, or X—Y is O, NR17, —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，R1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，且R 8为卤素或烷基或 NR 9 R 10基团，其中R 9和R 10均为氢，NR 11 R 12基团，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，或者R 2至R 5中的一个为XY-R 16基团，其中X为CH 2，NR 17，CO或S（O）m，Y为CH 2，NR 17，O或公开了S（O）m或XY为O，NR 17，-CH = CH-或N = N-作为可用于治疗肿瘤的药理学试剂。还描述了制备式（I）化合物的药物组合物和方法。

3. 发明授权

US6090941A Pharmaceutically active benzoquinazoline compounds 失效
标题翻译：药用活性苯并喹唑啉化合物
公开(公告)号：US6090941A
公开(公告)日：2000-07-18
申请号：US956018
申请日：1993-01-13
申请人： William Pendergast , Scott Howard Dickerson , Julius Vass Johnson , Robert Ferone
发明人： William Pendergast , Scott Howard Dickerson , Julius Vass Johnson , Robert Ferone
IPC分类号： A61K31/505 , A61K31/00 , A61K31/50 , A61K31/501 , A61K31/517 , A61P31/00 , A61P31/04 , A61P35/00 , A61P35/02 , C07D20060101 , C07D239/70 , C07D239/88 , C07D239/90 , C07D239/95 , C07D403/12 , C07D417/12
CPC分类号： C07D403/12 , C07D239/70 , C07D239/88 , C07D417/12
摘要： Compounds of the formula (I) or salts thereof, ##STR1## wherein the dotted line represents a single or double bond, R.sup.1 is alkyl or amino optionally substituted by alkyl, alkanoyl or benzyl group: R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and each is selected from hydrogen, phenyl, halo, nitro, a group S(O).sub.n R.sup.8 wherein n is the integer 0, 1 or 2 and R.sup.8 is halo or alkyl or a group NR.sup.9 R.sup.10 are both hydrogen, a group NR.sup.11 R.sup.12 wherein R.sup.11 and R.sup.12 are the same or different and each is hydrogen or alkyl, a group OR.sup.13 wherein R.sup.13 is hydrogen or C.sub.1-4 alkyl substituted by halo; a C.sub.1-4 aliphatic group optionally substituted by a group OR.sup.14 or NR.sup.14 R.sup.15 wherein R.sup.14 and R.sup.15 are the same or different and each is hydrogen or alkyl; ot two of R.sup.2 to R.sup.5 are linked together to form a benzp group, one of R.sup.2 to R.sup.3 is a group X--Y--R.sup.16 wherein X is CH.sub.2, NR.sup.17, CO, or S(O).sub.m and Y is CH.sub.2, NR.sup.17, O or S(O).sub.m, or X--Y is CH.sub.2,NR.sup.17, --CH.dbd.CH-- or --N.dbd.N--, are disclosed as pharmacological agents useful in the treatment of tumors. Pharmaceutical compositions and methods for the preparation of compounds of formula (I) are also disclosed.
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是整数0,1或2，且R 8是卤素或烷基或基团NR 9 R 10都是氢，NR 11 R 12基团，其中R 11和R 12 相同或不同，各自为氢或烷基，OR 13基团，其中R 13为氢或被卤素取代的C 1-4烷基; 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; R2至R5中的两个连接在一起形成苯并基团，R2至R3中的一个为XY-R16基团，其中X为CH 2，NR 17，CO或S（O）m，Y为CH 2，NR 17，O或公开了S（O）m或XY为CH 2，NR 17，-CH = CH-或-N = N-作为可用于治疗肿瘤的药理学试剂。还公开了制备式（I）化合物的药物组合物和方法。

4. 发明授权

US06762188B1 Pharmaceutically active benzoquinazoline compounds 失效
标题翻译：药用活性苯并喹唑啉化合物
公开(公告)号：US06762188B1
公开(公告)日：2004-07-13
申请号：US09952394
申请日：2001-09-12
申请人： William Pendergast , Scott Howard Dickerson , Julius Vass Johnson , Robert Ferone
发明人： William Pendergast , Scott Howard Dickerson , Julius Vass Johnson , Robert Ferone
IPC分类号： A61K31502
CPC分类号： C07D403/12 , C07D239/70
摘要： Compounds of formula (I) or salts thereof, wherein the dotted Line represents a single or double bond, R1 is alkyl or amino optionally substituted by alkyl, alkanoyl or benzyl group; R2, R3, R4 and R5 are the same or different and each is selected from hydrogen, phenyl, halo, nitro, a group S(O)nR8 wherein n is the integer 0, 1 or 2 and R8 is halo or alkyl or a group NR9R10 wherein R9 and R10 are both hydrogen, a group NR11R12 wherein R11 and R12 are the same or different and each is hydrogen or alkyl, a group OR13 wherein R13 is hydrogen or C1-4 of alkyl optionally substituted by halo; a C1-4 aliphatic group optionally substituted by a group OR14 or NR14R15 wherein R14 and R15 are the same or different and each is hydrogen or alkyl; or two of R2 to R5 are linked together to form a benzo group, or one of R2 to R5 is a group X—Y—R16 wherein X is CH2, NR17, CO or S(O)m and Y is CH2, NR17, O or S(O)m, or X—Y is O, NR17, —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物。还描述了制备式（I）化合物的药物组合物和方法。

5. 发明申请

US20080214490A1 METHOD OF PROMOTING CERVICAL AND VAGINAL SECRETIONS 审中-公开
标题翻译：促进宫颈和阴道分泌的方法
公开(公告)号：US20080214490A1
公开(公告)日：2008-09-04
申请号：US12043845
申请日：2008-03-06
申请人： William Pendergast , Sammy Ray Shaver , David J. Drutz , Janet L. Rideout , Benjamin R. Yerxa
发明人： William Pendergast , Sammy Ray Shaver , David J. Drutz , Janet L. Rideout , Benjamin R. Yerxa
IPC分类号： A61K31/7076 , A61P15/02
CPC分类号： C07H21/00 , A61K31/00
摘要： The present invention provides a method of stimulating cervical and vaginal secretions in a mammal by treatment with P2Y2 and/or P2Y4 purinergic receptor agonists. Treatment of vaginal dryness associated with menopause, chemotherapy, and various disease states as well as the treatment of vulvar pain is discussed. Suitable agonists such as UTP, CTP, ATP, dinucleotides and analogs thereof are disclosed.
摘要翻译：本发明提供了通过用P2Y2和/或P2Y4N4嘌呤能受体激动剂治疗来刺激哺乳动物的宫颈和阴道分泌物的方法。讨论了与绝经，化疗和各种疾病状态相关的阴道干燥的治疗以及外阴疼痛的治疗。公开了合适的激动剂，例如UTP，CTP，ATP，二核苷酸及其类似物。

6. 发明申请

US20080009463A1 Method of treating dry eye disease with purinergic receptor agonists 有权
标题翻译：用嘌呤能受体激动剂治疗干眼病的方法
公开(公告)号：US20080009463A1
公开(公告)日：2008-01-10
申请号：US11821091
申请日：2007-06-20
申请人： Benjamin Yerxa , Karla Jacobus , William Pendergast , Janet Rideout
发明人： Benjamin Yerxa , Karla Jacobus , William Pendergast , Janet Rideout
IPC分类号： A61K31/7084 , A61P27/02
CPC分类号： C07H19/10 , A61K9/0048 , A61K31/7084 , A61K45/06 , C07H19/20 , C07H21/00 , Y10S514/912 , Y10S514/915
摘要： A method and preparation for the stimulation of tear secretion in a subject in need of such treatment is disclosed. The method comprises administering to the ocular surfaces of the subject a purinergic receptor agonist such as uridine 5′-triphosphate (UTP), dinucleotides, cytidine 5′-triphosphate (CTP), adenosine 5′-triphosphate (ATP), or their therapeutically useful analogs and derivatives, in an amount effective to stimulate tear fluid secretion and enhance drainage of the lacrimal system. 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.
摘要翻译：公开了用于刺激需要这种治疗的受试者的泪液分泌的方法和制剂。该方法包括向受试者的眼表面施用嘌呤能受体激动剂如尿苷5'-三磷酸（UTP），二核苷酸，胞苷5'-三磷酸（CTP），腺苷5'-三磷酸（ATP）或其治疗上有用的类似物和衍生物，其量有效地刺激泪液分泌并增强泪液系统的引流。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。

7. 发明申请

US20070066625A1 METHOD OF TREATING PARKINSON'S DISEASE WITH DIARYLMETHYLPIPERAZINE COMPOUNDS EXHIBITING DELTA RECEPTOR AGONIST ACTIVITY 有权
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：US20070066625A1
公开(公告)日：2007-03-22
申请号：US11470012
申请日：2006-09-05
申请人： Kwen-Jen Chang , William Pendergast , Jonathon Holt
发明人： Kwen-Jen Chang , William Pendergast , Jonathon Holt
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。

8. 发明授权

US06921755B2 Method of treating dry eye disease with purinergic receptor agonists 有权
标题翻译：用嘌呤能受体激动剂治疗干眼病的方法
公开(公告)号：US06921755B2
公开(公告)日：2005-07-26
申请号：US10010055
申请日：2001-11-09
申请人： Benjamin R. Yerxa , Karla M. Jacobus , William Pendergast , Janet L. Rideout
发明人： Benjamin R. Yerxa , Karla M. Jacobus , William Pendergast , Janet L. Rideout
IPC分类号： A61K45/06 , A61K31/70
CPC分类号： A61K45/06 , Y10S514/912
摘要： A method and preparation for the stimulation of tear secretion in a subject in need of such treatment is disclosed. The method comprises administering to the ocular surfaces of the subject a purinergic receptor agonist such as uridine 5′-triphosphate (UTP), dinucleotides, cytidine 5′-triphosphate (CTP), adenosine 5′-triphosphate (ATP), or their therapeutically useful analogs and derivatives, in an amount effective to stimulate tear fluid secretion and enhance drainage of the lacrimal system. 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.
摘要翻译：公开了用于刺激需要这种治疗的受试者的泪液分泌的方法和制剂。该方法包括向受试者的眼表面施用嘌呤能受体激动剂如尿苷5'-三磷酸（UTP），二核苷酸，胞苷5'-三磷酸（CTP），腺苷5'-三磷酸（ATP）或其治疗上有用的类似物和衍生物，其量有效地刺激泪液分泌并增强泪液系统的引流。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。

9. 发明授权

US06420347B1 Method of treating ciliary dyskinesia with uridine triphosphates and related compounds 失效
标题翻译：用尿苷三磷酸和相关化合物治疗睫状肌运动障碍的方法
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。

10. 发明授权

US5972904A Method of treating sinusitis with uridine triphosphates and related compounds 失效
公开(公告)号：US5972904A
公开(公告)日：1999-10-26
申请号：US4786
申请日：1998-01-09
申请人： Karla Jacobus , Janet Rideout , Ben Yerxa , William Pendergast , Suhaib Siddiqi , David Drutz
发明人： Karla Jacobus , Janet Rideout , Ben Yerxa , William Pendergast , Suhaib Siddiqi , David Drutz
IPC分类号： C07H19/067 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61P11/02 , A61P43/00 , C07H19/10 , C07H19/167 , C07H19/20 , A61K31/70
CPC分类号： A61K31/7048 , A61K31/7068 , A61K31/7072 , A61K31/7076 , C07H19/10 , C07H19/20
摘要： A method of promoting drainage of congested mucous secretions in the sinuses of a subject in need of such treatment is disclosed. The method comprises administering to the sinuses of the subject a uridine phosphate such as uridine 5'-triphosphate (UTP) or P.sup.1,P.sup.4 -di(uridine-5') tetraphosphate (U.sub.2 P.sub.4), an analog of UTP, or any other analog, in an amount effective to promote drainage of congested fluid in the sinuses by hydrating mucous secretions or by stimulating ciliary beat frequency in the sinuses. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include any liquid suspension (including nasal drops or spray), oral form (liquid or pill), aerosol inhalation, powder form, topical, injected, intra-operative instillation or suppository form.

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