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1. 发明授权

US4383993A Nasal dosage forms containing natural female sex hormones 失效
标题翻译：含有天然雌性性激素的鼻剂
公开(公告)号：US4383993A
公开(公告)日：1983-05-17
申请号：US277000
申请日：1981-06-24
申请人： Anwar A. Hussain , Shinichiro Hirai , Rima Bawarshi
发明人： Anwar A. Hussain , Shinichiro Hirai , Rima Bawarshi
IPC分类号： A61K9/00 , A61K31/57 , A01N45/00
CPC分类号： A61K9/0043 , A61K31/57 , Y10S514/843
摘要： The invention relates to a novel method of administering the natural female sex hormones, 17 .beta.-estradiol and progesterone, to achieve enhanced bioavailability thereof. The invention further relates to novel dosage forms of 17 .beta.-estradiol and/or progesterone which are adapted for nasal administration, such as solutions, suspensions, gels and ointments. The dosage forms containing a combination of 17 .beta.-estradiol and progesterone are particularly useful as contraceptives, while the dosage forms containing only one of the hormonal components find utility in the treatment of conditions such as menopause, menstrual disorders, etc., which are known to respond to administration of a natural or synthetic female hormone.
摘要翻译：本发明涉及一种施用天然雌性激素17β-雌二醇和孕酮的新方法，以实现其增强的生物利用度。本发明还涉及适于鼻内给药的17β-雌二醇和/或孕酮的新型剂型，例如溶液，悬浮液，凝胶和软膏。含有17β-雌二醇和孕酮组合的剂型特别适用于避孕药，而含有仅一种激素成分的剂型可用于治疗已知的诸如更年期，月经紊乱等病症对天然或合成雌激素的施用作出反应。

2. 发明授权

US4284648A Nasal administration of propranolol 失效
标题翻译：普萘洛尔的鼻内给药
公开(公告)号：US4284648A
公开(公告)日：1981-08-18
申请号：US63176
申请日：1979-08-03
申请人： Anwar A. Hussain , Shinichiro Hirai , Rima Bawarshi
发明人： Anwar A. Hussain , Shinichiro Hirai , Rima Bawarshi
IPC分类号： A61K31/13 , A61K9/00 , A61K9/08 , A61K9/107 , A61K9/12 , A61K31/135 , A61K31/138 , A61P25/02
CPC分类号： A61K9/0043 , A61K31/135 , Y10S514/821
摘要： The invention relates to a novel method of administering propranolol, a known .beta.-andrenergic blocking agent widely used in the treatment of angina pectoris, arrhythmias, hypertension and other cardiac conditions, and migraine. The invention further relates to novel dosage forms of propranolol which are adapted for nasal administration and which include solutions, suspensions, gels and ointments.
摘要翻译：本发明涉及一种广泛用于治疗心绞痛，心律失常，高血压和其他心脏病以及偏头痛的已知β-肾上腺素能阻断剂的普萘洛尔的新方法。本发明还涉及适于鼻内给药的普萘洛尔的新型剂型，其包括溶液，悬浮液，凝胶和软膏。

3. 发明授权

US4394390A Nasal dosage forms of propranol 失效
标题翻译：萘酚的鼻剂
公开(公告)号：US4394390A
公开(公告)日：1983-07-19
申请号：US194786
申请日：1980-10-07
申请人： Anwar A. Hussain , Shinichiro Hirai , Rima Bawarshi
发明人： Anwar A. Hussain , Shinichiro Hirai , Rima Bawarshi
IPC分类号： A61K9/00 , A61K31/13 , A61K31/135 , A61K9/06 , C07C93/00
CPC分类号： A61K31/135 , A61K31/13 , A61K9/0043 , Y10S514/821
摘要： The invention relates to a novel method of administering propranolol, a known .beta.-adrenergic blocking agent widely used in the treatment of angina pectoris, arrhythmias, hypertension and other cardiac conditions, and migraine. The invention further relates to novel dosage forms of propranolol which are adapted for nasal administration and which include solutions, suspensions, gels and ointments.
摘要翻译：本发明涉及一种施用普萘洛尔，广泛用于治疗心绞痛，心律失常，高血压和其他心脏病以及偏头痛的已知β-肾上腺素能阻断剂的新方法。本发明还涉及适于鼻内给药的普萘洛尔的新型剂型，其包括溶液，悬浮液，凝胶和软膏。

4. 发明授权

US4315925A Method of administering natural female sex hormones 失效
标题翻译：施用天然雌性激素的方法
公开(公告)号：US4315925A
公开(公告)日：1982-02-16
申请号：US154995
申请日：1980-05-30
申请人： Anwar A. Hussain , Shinichiro Hirai , Rima Bawarshi
发明人： Anwar A. Hussain , Shinichiro Hirai , Rima Bawarshi
IPC分类号： A61K9/00 , A61K31/57 , A01N45/00
CPC分类号： A61K9/0043 , A61K31/57 , Y10S514/843
摘要： The invention relates to a novel method of administering the natural female sex hormones, 17 .beta.- estradiol and progesterone, to achieve enhanced bioavailability thereof. The invention further relates to novel dosage forms of 17 .beta.- estradiol and/or progesterone which are adapted for nasal administration, such as solutions, suspensions, gels and ointments. The dosage forms containing a combination of 17 .beta.-estradiol and progesterone are particularly useful as contraceptives, while the dosage forms containing only one of the hormonal components find utility in the treatment of conditions such as menopause, menstrual disorders, etc., which are known to respond to administration of a natural or synthetic female hormone.
摘要翻译：本发明涉及一种施用天然雌性激素17β-雌二醇和孕酮的新方法，以实现其增强的生物利用度。本发明还涉及适于鼻腔给药的17β-雌二醇和/或孕酮的新型剂型，例如溶液，悬浮液，凝胶和软膏。含有17β-雌二醇和孕酮组合的剂型特别适用于避孕药，而含有仅一种激素成分的剂型可用于治疗已知的诸如更年期，月经紊乱等病症对天然或合成雌激素的施用作出反应。

5. 发明授权

US06200591B1 Method of administration of sildenafil to produce instantaneous response for the treatment of erectile dysfunction 失效
标题翻译：施用西地那非以治疗勃起功能障碍的瞬间反应的方法
公开(公告)号：US06200591B1
公开(公告)日：2001-03-13
申请号：US09208439
申请日：1998-12-10
申请人： Anwar A. Hussain , Lewis W. Dittert
发明人： Anwar A. Hussain , Lewis W. Dittert
IPC分类号： A61F1302
CPC分类号： A61K9/0043
摘要： This invention provides a method of rapidly and reliably delivering sildenafil, or derivatives thereof, alone or in combination with other compounds, to the systemic circulation by administration via the nasal route so as to produce virtually instantaneous onset of beneficial effects in the treatment of erectile dysfunction. The present invention further provides pharmaceutical compositions comprising sildenafil, or derivatives thereof, and/or pharmaceutically acceptable salts thereof in a variety of unique pharmaceutical dosage forms, with and without apomorphine.
摘要翻译：本发明提供了一种通过经鼻途径给药而将西地那非或其衍生物单独或与其它化合物组合快速可靠地递送至全身循环的方法，从而在勃起功能障碍的治疗中产生几乎瞬间的有益效果。本发明进一步提供药物组合物，其包含西地那非或其衍生物，和/或其药学上可接受的盐，其具有和不含阿扑吗啡的各种独特的药物剂型。

6. 发明授权

US6150420A Method for enhanced brain delivery of bupropion 失效
标题翻译：增强安非他酮大脑输送的方法
公开(公告)号：US6150420A
公开(公告)日：2000-11-21
申请号：US235833
申请日：1999-01-22
申请人： Abdulghani A. Houdi , Anwar A. Hussain
发明人： Abdulghani A. Houdi , Anwar A. Hussain
IPC分类号： A61K9/00 , A61K31/135
CPC分类号： A61K9/0043 , A61K31/135
摘要： This invention provides to a method for enhancement of delivery of bupropion by administration via the nasal route, and methods of treatment comprising intranasal administration of bupropion. The present invention further provides pharmaceutical compositions comprising bupropion and/or pharmaceutically acceptable salts thereof.
摘要翻译：本发明提供一种通过经鼻途径给药来增强安非他酮递送的方法，以及包括鼻内施用安非他酮的治疗方法。本发明还提供包含安非他酮和/或其药学上可接受的盐的药物组合物。

7. 发明授权

US5753701A N-chloro-N-methyl glucamine and N-chloro-N-methyl glucamine esters as novel safe agents for water disinfection 失效
标题翻译： N-氯-N-甲基葡糖胺和N-氯-N-甲基葡糖胺酯作为水消毒的新型安全剂
公开(公告)号：US5753701A
公开(公告)日：1998-05-19
申请号：US736913
申请日：1996-10-25
申请人： Anwar A. Hussain , Bassam Tashtoush , Lewis W. Dittert
发明人： Anwar A. Hussain , Bassam Tashtoush , Lewis W. Dittert
IPC分类号： A01N37/12 , C07C239/04 , G01N33/534 , C07C219/06 , A01N37/04
CPC分类号： A01N37/12 , C07C239/04 , G01N33/534
摘要： The present invention relates to N-chloro-N-methyl glucamine and N-chloro-N-methyl glucamine esters, and their use as agents for water disinfection and as mild oxidizing agents for the radiolabeling of oxidation-sensitive biomolecules.
摘要翻译：本发明涉及N-氯-N-甲基葡糖胺和N-氯-N-甲基葡糖胺酯，以及它们作为水消毒剂和用作放射性标记氧化敏感生物分子的温和氧化剂的用途。

8. 发明授权

US4241055A Derivatives of aspirin 失效
标题翻译：阿司匹林衍生物
公开(公告)号：US4241055A
公开(公告)日：1980-12-23
申请号：US43815
申请日：1979-05-30
申请人： Anwar A. Hussain , James E. Truelove , Harry B. Kostenbauder
发明人： Anwar A. Hussain , James E. Truelove , Harry B. Kostenbauder
IPC分类号： C07H13/08 , C07H15/04 , C07H15/12 , A61K31/70 , C07H13/02
CPC分类号： C07H13/08 , C07H15/04 , C07H15/12
摘要： There are provided novel derivatives of 2-acetoxybenzoic acid, which are substituted 1-0-(2'acetoxy)benzoyl-.alpha.-D-2-deoxyglucopyranose derivatives and are suitable for the attainment of high 2-acetoxybenzoic acid blood levels without irritation of the gastrointestinal lining.
摘要翻译：提供2-乙酰氧基苯甲酸的新衍生物，它们是取代的1-0-（2'-乙酰氧基）苯甲酰-α-D-2-脱氧葡萄糖吡喃糖衍生物，适合于获得高的2-乙酰氧基苯甲酸血液水平而不刺激胃肠内衬。

9. 发明授权

US4065566A N-Nicotinoyl-3,4-dinicotinoyloxy-L-phenylalanine and derivatives pharmaceutical compositions and methods containing same 失效
标题翻译： N-烟酰基-3,4-二烟酰氧基-L-苯丙氨酸及其衍生物药物组合物和含有其的方法
公开(公告)号：US4065566A
公开(公告)日：1977-12-27
申请号：US720781
申请日：1976-09-07
申请人： Nicolae S. Bodor , Kenneth B. Sloan , Anwar A. Hussain
发明人： Nicolae S. Bodor , Kenneth B. Sloan , Anwar A. Hussain
IPC分类号： A61K31/195 , C07D213/55 , C07D213/56 , C07K5/06 , A61K31/44
CPC分类号： C07D213/56 , A61K31/195 , C07D213/55 , C07K5/06 , Y10S930/29
摘要： There is provided, novel, transient pro-drug forms of L-DOPA (3,4-dihydroxy-L-phenylalanine), having the formula: ##STR1## wherein R represents a hydrogen atom, an acyl group, a ##STR2## group, a --CO-pyridyl group, and a --CO--R.sub.3 group, wherein R.sub.3 represents the residue of any N,N-C.sub.1 -C.sub.2 dialkylamino acid or a C.sub.4 -C.sub.6 cycloalkylamino acid ##STR3## wherein R.sub.1 represents a member selected from the group consisting of a hydroxyl group and a --OM group, wherein M is an alkali metal (Na, K, etc.) or an ammonium ion; and wherein R.sub.2 represents a member selected from the group consisting of a ##STR4## group, a --CO-pyridyl group, and a --CO--R.sub.3 group, wherein R.sub.3 represents the residue of any N,N-(C.sub.1 -C.sub.2)-dialkylamino acid or a C.sub.4 -C.sub.6 -cycloalkylamino acid ##STR5## wherein R represents an acyl group; wherein R.sub.2 represents a hydrogen atom; and wherein R.sub.1 represents a --NHCH(R.sub.4)COOR.sub.5 group, wherein R.sub.4 represents the residue of any naturally occurring amino acid, and wherein R.sub.5 represents a member selected from the group consisting of a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group (e.g., methyl, ethyl, propyl, butyl, pentyl), and a C.sub.1 -C.sub.5 alkylaryl group (e.g., --CH.sub.2 --C.sub.6 H.sub.5, --CH.sub.2 --CH.sub.2 --C.sub.6 H.sub.5, etc.), and the HX salts thereof, wherein X is a conventional pharmaceutically acceptable acid addition salt anion (e.g. chloride, bromide, perchlorate, methanesulfonate, succinate, etc.).These compounds are all useful in the treatment of Parkinson's Disease.
摘要翻译：提供了具有下式的新型瞬时前药L-DOPA（3,4-二羟基-L-苯丙氨酸），其具有下式：（I）其中R表示氢原子，酰基， IMAGE>基团，-CO-吡啶基和-CO-R3基团，其中R3表示任何N，N-C 1 -C 2二烷基氨基酸或C 4 -C 6环烷基氨基酸的残基，其中R 1表示成员选自羟基和-OM基团，其中M为碱金属（Na，K等）或铵离子; 并且其中R 2表示选自由以下组成的组的成员：其中R 3表示任何N，N-（C 1 -C 2） - 二烷基氨基酸或C 4 -C 6环烷基氨基酸（II）其中R表示酰基; 其中R2表示氢原子; 并且其中R 1表示-NHCH（R 4）COOR 5基团，其中R 4表示任何天然存在的氨基酸的残基，并且其中R 5表示选自氢原子，C 1 -C 5烷基（例如，甲基，乙基，丙基，丁基，戊基）和C1-C5烷基芳基（例如-CH2-C6H5，-CH2-CH2-C6H5等）及其HX盐，其中X是常规药学上可接受的酸加成盐阴离子（如氯化物，溴化物，高氯酸盐，甲磺酸盐，琥珀酸盐等）。

10. 发明授权

US4242330A Derivative of aspirin 失效
标题翻译：阿司匹林衍生物
公开(公告)号：US4242330A
公开(公告)日：1980-12-30
申请号：US43814
申请日：1979-05-30
申请人： Anwar A. Hussain , James E. Truelove , Harry B. Kostenbauder
发明人： Anwar A. Hussain , James E. Truelove , Harry B. Kostenbauder
IPC分类号： C07H13/08 , C07H15/04 , C07H15/18 , A61K31/70 , C07H13/02
CPC分类号： C07H13/08 , C07H15/04 , C07H15/18 , Y10S514/825
摘要： There is provided a novel derivative of 2-acetoxybenzoic acid, i.e., 1-O-(2'-acetoxy)benzoyl-.alpha.-D-2-deoxyglucopyranose, which is suitable for the attainment of high 2-acetoxybenzoic acid blood levels without irritation of the gastrointestinal lining.
摘要翻译：提供了2-乙酰氧基苯甲酸的新型衍生物，即1-O-（2'-乙酰氧基）苯甲酰-α-D-2-脱氧吡喃葡萄糖，其适用于无刺激性地获得高的2-乙酰氧基苯甲酸血液水平的胃肠内衬。

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