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公开(公告)号：US4241055A
公开(公告)日：1980-12-23
申请号：US43815
申请日：1979-05-30
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。
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12.发明授权N-Nicotinoyl-3,4-dinicotinoyloxy-L-phenylalanine and derivatives pharmaceutical compositions and methods containing same 失效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
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）。
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公开(公告)号：US4242330A
公开(公告)日：1980-12-30
申请号：US43814
申请日：1979-05-30
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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公开(公告)号：US3998799A
公开(公告)日：1976-12-21
申请号：US569009
申请日：1975-04-17
IPC分类号： A61K31/195 , A61K38/00 , C07D213/55 , C07D213/56 , C07K5/06 , C07C103/52 , A61K37/00
CPC分类号： C07D213/56 , A61K31/195 , C07D213/55 , C07K5/06 , A61K38/00 , 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 n represents an integer of from 2 to 50 with respect to formula (V-A), and wherein n represents an integer of from 1 to 50 with respect to formula (V-B);R represents a hydrogen atom, an acyl group, ##STR2## --CO-pyridyl, or --CO--R.sub.3, wherein R.sub.3 is the residue of any N,N-C.sub.1 -C.sub.2 dialkylamino acid or a C.sub.4 -C.sub.6 cycloalkylamino acid; R.sub.1 represents --OH, --O-lower alkyl, --O-benzyl, or a naturally occurring protein amino acid; and R.sub.2 represents ##STR3## --CO-pyridyl, a naturally occurring protein amino acid, 3',4'-L-diacyloxy phenylalanine, or --CO-R.sub.3.These compounds are all useful in the treatment of Parkinson's Disease.
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15.发明授权Intranasal codeine for the rapid suppression of cough and rapid relief of pain 失效鼻内可待因可快速抑制咳嗽和快速缓解疼痛公开(公告)号：US06608073B1
公开(公告)日：2003-08-19
申请号：US09410033
申请日：1999-10-01
IPC分类号： A61K31435
CPC分类号： A61K31/60 , A61K31/435 , A61K31/485 , A61K45/06 , A61K2300/00
摘要： This invention provides a method of rapidly and reliably delivering codeine, alone or in combination with other compounds, to the systemic circulation by administration via the nasal route to produce rapid onset of beneficial effects in the treatment of pain or cough. The present invention further provides pharmaceutical compositions comprising codeine, and/or pharmaceutically acceptable salts thereof in a variety of unique pharmaceutical dosage forms, with and without other analgesic and/or antitussive compounds.
摘要翻译： 本发明提供了一种通过经鼻途径给药可快速可靠地将可待因单独或与其它化合物组合输送至全身循环的方法，从而在治疗疼痛或咳嗽方面产生快速的有益效果。 本发明进一步提供包含可待因和/或其药学上可接受的盐的药物组合物，其具有多种独特的药物剂型，具有和不具有其它镇痛药和/或镇咳药物。
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公开(公告)号：US06423701B1
公开(公告)日：2002-07-23
申请号：US08591767
申请日：1996-01-25
申请人： Anwar A. Hussain
发明人： Anwar A. Hussain
IPC分类号： A61K3156
CPC分类号： A61K31/5685 , C07J1/00
摘要： The present invention provides novel water soluble testosterone analogs. These testosterone analogs are suitable for intranasal administration to patients requiring increased plasma testosterone levels. The present invention also provides pharmaceutical compositions containing the testosterone analogs of the present invention. The present invention further provides a method of increasing plasma testosterone levels in patients in need of such treatment comprising the intranasal administration of the water-soluble testosterone analogs and pharmaceutical compositions of the present invention.
摘要翻译： 本发明提供了新的水溶性睾酮类似物。 这些睾酮类似物适用于需要增加血浆睾酮水平的患者的鼻内给药。 本发明还提供含有本发明的睾酮类似物的药物组合物。 本发明还提供了在需要这种治疗的患者中增加血浆睾酮水平的方法，包括鼻内施用本发明的水溶性睾酮类似物和药物组合物。
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公开(公告)号：US4394390A
公开(公告)日：1983-07-19
申请号：US194786
申请日：1980-10-07
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。
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公开(公告)号：US4315925A
公开(公告)日：1982-02-16
申请号：US154995
申请日：1980-05-30
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。
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19.发明授权
公开(公告)号：US4885287A
公开(公告)日：1989-12-05
申请号：US229963
申请日：1988-08-09
CPC分类号： A61K9/0043 , A61K31/60
摘要： The invention relates to a novel method of administering aspirin to achieve improved delivery thereof. The invention further relates to novel dosage forms of neutralized aspirin adapted for nasal administration, such as solutions, suspensions, gels and ointments. These dosage forms find utility in the treatment of conditions known to respond to the administration of aspirin, particularly in the treatment of migraine and in the mitigation of cardiovascular damage resulting from heart attack.
摘要翻译： 本发明涉及一种给予阿斯匹林以改善其递送的新方法。 本发明还涉及适于鼻腔给药的中和阿司匹林的新型剂型，例如溶液，悬浮液，凝胶和软膏。 这些剂型可用于治疗已知对阿司匹林施用有反应的病症，特别是在治疗偏头痛和缓解由心脏病发作引起的心血管损伤中。
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20.发明授权Method of administering narcotic antagonists and analgesics and novel dosage forms containing same 失效管理麻醉拮抗剂和止痛剂的方法和含有其的新型剂型
公开(公告)号：US4464378A
公开(公告)日：1984-08-07
申请号：US258308
申请日：1981-04-28
申请人： Anwar A. Hussain
发明人： Anwar A. Hussain
IPC分类号： A61K9/00 , A61K31/35 , A61K31/485
CPC分类号： A61K31/35 , A61K31/485 , A61K9/0043
摘要： The invention provides a novel method of administering narcotic antagonists, narcotic analgesics and related compounds, and novel dosage forms containing those compounds which are adapted for nasal administration. The nasal dosage forms disclosed include solutions, suspensions, gels and ointments. Especially preferred compounds which can be advantageously administered in accordance with the invention include naloxone, naltrexone, nalbuphine, levorphanol, buprenorphine, butorphanol, .DELTA..sup.9 -tetrahydrocannabinol (THC), cannabidiol (CBD) and levonantradol.
摘要翻译： 本发明提供了一种管理麻醉拮抗剂，麻醉止痛剂和相关化合物的新方法，以及含有适于鼻内给药的那些化合物的新型剂型。 所公开的鼻用剂型包括溶液，悬浮液，凝胶和软膏。 根据本发明可以有利地施用的特别优选的化合物包括纳洛酮，纳曲酮，纳布啡，左啡诺，丁丙诺啡，丁诺啡，DELTA 9-四氢大麻酚（THC），大麻二醇（CBD）和左旋他兰。
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