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1. 发明申请

US20030144256A1 Male anti-fertility agents 审中-公开
公开(公告)号：US20030144256A1
公开(公告)日：2003-07-31
申请号：US10304665
申请日：2002-11-25
申请人： Allergan Sales, Inc.
发明人： Elliott S. Klein , Yang-Dar Yuan , Roshantha A. Chandraratna
IPC分类号： A61K031/695 , A61K031/655 , A61K031/506 , A61K031/501 , A61K031/497 , A61K031/4709 , A61K031/47 , A61K031/4436 , A61K031/427 , A61K031/422 , A61K031/4178 , A61K031/416 , A61K031/382 , A61K031/353
CPC分类号： A61K31/382 , A61K31/00 , A61K31/192 , A61K31/195 , A61K31/196 , A61K31/203 , A61K31/353 , A61K31/47 , A61K31/695 , Y10S514/841
摘要： Methods and compositions for inhibiting or preventing spermatogenesis in a male mammal. Also disclosed are compounds and formulations for use in such methods.

2. 发明申请

US20020077360A1 Methods of treatment with compounds having RAR alpha receptor specific or selective activity 失效
标题翻译：用具有RARα受体特异性或选择性活性的化合物治疗的方法
公开(公告)号：US20020077360A1
公开(公告)日：2002-06-20
申请号：US09998358
申请日：2001-11-29
申请人： Allergan Sales, Inc.
发明人： Min Teng , Tien T. Duong , Roshantha A. Chandraratna
IPC分类号： A61K031/203 , A01N037/12 , A61K031/11 , A61K031/07
CPC分类号： A61K31/353 , A61K31/203 , A61K31/44 , G01N25/4866
摘要： Retinoid compounds which act specifically or selectively on RARnull receptor subtypes in preference over RARnull and RARnull receptor subtypes, posses desirable pharmaceutical properties associated with retinoids, and are particularly suitable for treatment of tumors, such as acute monocytic leukemia, cervical carcinoma, myeloma, ovarian carcinomas and head and neck carcinomas, without having one or more undesirable side effects of retinoids, such as inducement of weight loss, mucocutaneous toxicity, skin irritation and teratogenecity.
摘要翻译：在RARbeta和RAR＆Ggr上优先选择性地对RARα受体亚型起作用的类视色素化合物; 受体亚型，具有与类视黄醇相关的期望的药物性质，并且特别适用于治疗肿瘤，例如急性单核细胞白血病，宫颈癌，骨髓瘤，卵巢癌和头颈部癌，而不具有类维生素A的一种或多种不期望的副作用，如诱导体重减轻，皮肤粘膜毒性，皮肤刺激和致畸性。

3. 发明申请

US20030144360A1 Composition and method for modulating BAR/FXR receptor activity 审中-公开
标题翻译：用于调节BAR / FXR受体活性的组合物和方法
公开(公告)号：US20030144360A1
公开(公告)日：2003-07-31
申请号：US10104385
申请日：2002-03-22
申请人： Allergan Sales, Inc.
发明人： Barry M. Forman , Richard L. Beard , Isabelle Dussault , Roshantha A. Chandraratna
IPC分类号： A61K031/192
CPC分类号： A61K31/192 , A61K31/202 , A61K31/203 , A61K31/695
摘要： Methods for modulating the activity of the mammalian BAR/FXR receptor. The methods include methods of treating a hypocholesterolemic mammal comprising contacting the mammal with synthetic compounds able to modulate an activity characteristic of the BAR/FXR receptor. Other methods include a method of treating colon cancer in a mammal comprising administering a compound having a BAR/FXR antagonistic activity.
摘要翻译：调节哺乳动物BAR / FXR受体活性的方法。所述方法包括治疗低胆固醇血症哺乳动物的方法，包括使哺乳动物与能够调节BAR / FXR受体活性特征的合成化合物接触。其他方法包括在哺乳动物中治疗结肠癌的方法，包括给予具有BAR / FXR拮抗活性的化合物。

4. 发明申请

US20020193403A1 Methods of treating hyperlipidemia 审中-公开
标题翻译：治疗高脂血症的方法
公开(公告)号：US20020193403A1
公开(公告)日：2002-12-19
申请号：US09848159
申请日：2001-05-03
申请人： Allergan Sales, Inc.
发明人： Yang-Dar Yuan , Scott M. Thacher , Elliott S. Klein , Roshantha A. Chandraratna
IPC分类号： A61K031/47 , A61K031/353 , A61K031/38
CPC分类号： A61K31/382 , A61K31/00 , A61K31/196 , A61K31/202 , A61K31/352
摘要： The current invention relates to methods for treating hyperlipidemia in mammals, including humans. More specifically, the current invention relates to the use of retinoid or retinoid derivative that is able to act as an antagonist or inverse agonist of a retinoid receptor to treat hyperlipidemia.
摘要翻译：本发明涉及用于治疗哺乳动物包括人类的高脂血症的方法。更具体地，本发明涉及能够作为类视黄醇受体的拮抗剂或反向激动剂作用以治疗高脂血症的类视色素或类视色素衍生物的用途。

5. 发明申请

US20030228632A1 Stable RXR expressing cell line 审中-公开
标题翻译：稳定的RXR表达细胞系
公开(公告)号：US20030228632A1
公开(公告)日：2003-12-11
申请号：US09850835
申请日：2001-05-08
申请人： Allergan Sales, Inc.
发明人： Jyotirmoy Kusari , Sheila X. Zhou , Hongzhi Liu , Ramilla O. Lewis , Roshantha A. Chandraratna
IPC分类号： G01N033/53 , G01N033/567 , C07K014/705
CPC分类号： G01N33/5005 , C12N5/0656 , C12N2503/02 , G01N2333/70567 , G01N2500/10
摘要： Stable cell lines which express retinoid receptors and the insulin receptor are prepared and are useful in identifying agonists and antagonists of retinoid receptors. Agonists and antagonists of the RXR receptor can be determined using the cell lines of the invention which are producers of RXR alone; agonists and antagonists of other retinoid receptors can be determined using cell lines transfected with RXR and the desired retinoid receptor.
摘要翻译：制备表达类视黄醇受体和胰岛素受体的稳定细胞系，可用于鉴定类视黄醇受体的激动剂和拮抗剂。 RXR受体的激动剂和拮抗剂可以使用本发明的单独的RXR的生产者来确定; 可以使用用RXR转染的细胞系和所需的类视黄醇受体来测定其它类视黄醇受体的激动剂和拮抗剂。

6. 发明申请

US20030078294A1 Methods and compositions for the treatment and prevention of lung disease 审中-公开
公开(公告)号：US20030078294A1
公开(公告)日：2003-04-24
申请号：US10305049
申请日：2002-11-25
申请人： Allergan Sales, Inc
发明人： Roshantha A. Chandraratna , Donald Massaro , Gloria DeCarlo Massaro
IPC分类号： A61K031/353 , A61L009/04
CPC分类号： A61K31/381 , A61K31/00 , A61K31/07 , A61K31/203
摘要： Methods and compositions for the treatment of lung disease such as emphysema and/or bronchopulmonary dysplasia in a mammal. Also disclosed are methods and compositions promoting the formation of alveolar septa and increasing the gas-exchange surface area of a mammalian lung, and for the prevention and/or treatment of alveolar destruction.

7. 发明申请

US20020082419A1 2,4-pentadienoic acid derivatives having retinoid-like biological activity 审中-公开
标题翻译：具有类视黄醇样生物活性的2,4-戊二烯酸衍生物
公开(公告)号：US20020082419A1
公开(公告)日：2002-06-27
申请号：US10012735
申请日：2001-11-05
申请人： Allergan Sales, Inc.
发明人： Vidyasagar Vuligonda , Roshantha A. Chandraratna
IPC分类号： C07D49/02 , C07D47/02 , C07D417/02 , C07D413/02 , C07D43/02
CPC分类号： C07D333/54 , A61K31/20 , A61K31/23 , C07C57/50 , C07C69/618 , C07D311/58 , C07D335/06
摘要： Compounds of Formula 1 1 wherein Z is selected from the group consisting of the radicals shown in Formula 2 and in Formula 3, 2 Y is cycloalkyl or cycloalkenyl of 3 to 8 carbons optionally substituted with one or two R4 groups, or Y is selected from phenyl, pyridyl, thienyl, furyl, pyrrolyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, and imidazolyl, said groups being optionally substituted with one or two R4 groups, the divalent Y radical being substituted by the Z and nullCR1nullCR1nullCR1nullCR1 groups on adjacent carbons; X is S, O, or NR5; n is 1 or 2; R1 and R2 independently are H, lower alkyl or fluoroalkyl; R3 is hydrogen, lower alkyl, Cl or Br; R4 is lower alkyl, fluoroalkyl or halogen; R5 is H or lower alkyl, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR8, CONR9R10, nullCH2OH, CH2OR11, CH2OCOR11, CHO, CH(OR12)2, CHOR13O, nullCOR7, CR7(OR12)2, CR7OR13O, or tri-lower alkylsilyl, where R7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R8 is an alkyl group of 1 to 10 carbons, a cycloalkyl group of 5 to 10 carbons or trimethylsilylalkyl where the alkyl group has 1 to 10 carbons, or R8 is phenyl or lower alkylphenyl, R9 and R10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R11 is lower alkyl, phenyl or lower alkylphenyl, R12 is lower alkyl, and R13 is divalent alkyl radical of 2-5 carbons, have retinoid like biological activity.
摘要翻译：式1的化合物，其中Z选自式2和式3中所示的基团，Y是任选被一个或两个R 4基团取代的3-8个碳原子的环烷基或环烯基，或Y选自苯基，吡啶基，噻吩基，呋喃基，吡咯基，哒嗪基，嘧啶基，吡嗪基，噻唑基，恶唑基和咪唑基，所述基团任选被一个或两个R 4基团取代，二价Y基团被Z代替，-CR1 = CR1-CR1 = 相邻碳上的CR1基团; X是S，O或NR5; n为1或2; R1和R2独立地为H，低级烷基或氟代烷基; R3是氢，低级烷基，Cl或Br; R4是低级烷基，氟烷基或卤素; R 5是H或低级烷基，B是氢，COOH或其药学上可接受的盐，COOR8，CONR9R10，-CH2OH，CH2OR11，CH2OCOR11，CHO，CH（OR12）2，CHOR13O，-COR7，CR7（OR12） CR 7OR 13 O或三低级烷基甲硅烷基，其中R 7为含有1至5个碳的烷基，环烷基或烯基，R 8为碳原子数1至10的烷基，碳原子数为5至10的环烷基或烷基具有的三甲基甲硅烷基烷基 1至10个碳，或R8为苯基或低级烷基苯基，R9和R10独立地为氢，1-10个碳原子的烷基或5-10个碳原子的环烷基，或苯基或低级烷基苯基，R11为低级烷基，苯基或低级烷基苯基，R12为低级烷基，R13为2-5个碳原子的二价烷基，具有类视黄醇类生物活性。

8. 发明申请

US20010039293A1 Treatment of tumors with RARalpha selective retinoid compounds in combination with other anti-tumor agents 失效
标题翻译：用RARalpha选择性类视黄醇化合物与其他抗肿瘤剂联合治疗肿瘤
公开(公告)号：US20010039293A1
公开(公告)日：2001-11-08
申请号：US09824111
申请日：2001-04-02
申请人： Allergan Sales, Inc.
发明人： Alissar Nehme , Richard L. Beard , Roshantha A. Chandraratna
IPC分类号： C07C233/45 , A61K031/216 , A61K031/195
CPC分类号： A61K31/165 , A61K31/167 , C07C235/66 , C07C2602/10
摘要： Compounds which are specific or selective agonists of RARnull receptors in preference over RARnull and RARnull receptors, and particularly compounds of the formula 1 where R is a H, lower alkyl of 1 to 6 carbons, or a pharmaceutically acceptable salt, are useful for treating a malignant disease or condition in a mammal. In treatment of solid tumors the compound exhibit synergistic anti-proliferative effect with human recombinant interferon.
摘要翻译：作为优选RARα和RARγ受体的RARα受体的特异性或选择性激动剂的化合物，特别是下式的化合物，其中R是1至6个碳的H，低级烷基或其药学上可接受的盐，可用于治疗恶性疾病或状况。在实体瘤治疗中，该化合物与人重组干扰素具有协同的抗增殖作用。

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