专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US4208428A Prostaglandin analogues 失效
标题翻译：前列腺素类似物
公开(公告)号：US4208428A
公开(公告)日：1980-06-17
申请号：US924343
申请日：1978-07-13
申请人： Masayasu Kurono , Nobuyuki Hamanaka , Shigeru Sakuyama , Takeshi Chiba , Hisao Nakai
发明人： Masayasu Kurono , Nobuyuki Hamanaka , Shigeru Sakuyama , Takeshi Chiba , Hisao Nakai
IPC分类号： A61K31/557 , A61K31/19 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07D309/12 , C07F9/40 , C07C177/00 , A61K31/215
CPC分类号： C07D307/935 , C07C405/00 , C07D309/12 , C07F9/4018
摘要： The invention relates to prostaglandin analogues of the general formula: ##STR1## (wherein A represents a grouping of the formula: ##STR2## B represents an alkylene group containing from 1 to 7 carbon atoms or a group ##STR3## (wherein the group --(CH.sub.2).sub.n --may be attached to the ortho, meta or para position of the phenyl ring and m and n, which may be the same or different, each represent an integer from 1 to 5 inclusive, the sum of the integers represented by m and n being from 2 to 6 inclusive), X represents ethylene or cis-vinylene, Y represents ethylene or trans-vinylene, W represents ethylene or trans-vinylene, Z represents a halogen atom, and R.sup.1 represents a hydrogen atom or an alkyl group containing from 1 to 12 carbon atoms) and cyclodextrin clathrates of such acids and esters and, when R.sup.1 represents a hydrogen atom, non-toxic salts thereof, which possess characteristic prostaglandin-like properties.
摘要翻译：本发明涉及以下通式的前列腺素类似物：其中A代表下式的基团：B代表含有1至7个碳原子的亚烷基或基团（IMAGE）（其中基团 - （CH 2）n - 可以连接到苯环的邻位，间位或对位，m和n可以相同或不同，各自表示1至5的整数，包括端值的整数，由 m和n为2至6的整数），X表示亚乙基或顺式亚乙烯基，Y表示亚乙基或反式亚乙烯基，W表示亚乙基或反式亚乙烯基，Z表示卤素原子，R1表示氢原子或烷基含有1至12个碳原子的基团）和这些酸和酯的环糊精包合物，并且当R 1表示氢原子时，其无毒盐具有特征性前列腺素样特性。

2. 发明授权

US4275075A 15-cylobutyl-trans-.DELTA..sup.2 -prostaglandin analogues 失效
标题翻译： 15-cylobutyl-trans-DELTA 2-prostaglandin类似物
公开(公告)号：US4275075A
公开(公告)日：1981-06-23
申请号：US915493
申请日：1978-06-14
申请人： Masayasu Kurono , Hisao Nakai , Shigeru Sakuyama
发明人： Masayasu Kurono , Hisao Nakai , Shigeru Sakuyama
IPC分类号： A61K31/557 , A61K31/19 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07F9/40 , C07C177/00
CPC分类号： C07D307/935 , C07C405/00 , C07F9/4018
摘要： The present invention relates to prostaglandin analogues of the general formula: ##STR1## [wherein A represents a grouping of the formula: ##STR2## X represents trans-vinylene or ethylene and Y represents cis-vinylene or ethylene, R represents a group of the formula --COOR.sup.4, in which R.sup.4 represents hydrogen or straight- or branched-chain alkyl of 1 to 12 carbon atoms, or a group of the formula --CH.sub.2 OR.sup.5, in which R.sup.5 represents hydrogen or alkylcarbonyl of 2 to 5 carbon atoms and R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, each represent hydrogen, straight- or branched-chain alkyl of 1 to 12 carbon atoms, or an aryl group unsubstituted or substituted by one, two or three substituents selected from alkyl, alkoxy, alkylthio, monoalkylamino and dialkylamino groups and halogen atoms, the alkyl groups or moieties of the said groups containing from 1 to 5 carbon atoms in a straight- or branched-chain, with the proviso that at least one of the symbols R.sup.1, R.sup.2 and R.sup.3 is other than hydrogen and the double bond between C.sub.2 -C.sub.3 is trans] and cyclodextrin clathrates of such prostaglandin analogues and, when R.sup.4 in the group - COOR.sup.4 represents hydrogen, non-toxic salts thereof, which exhibit characteristic prostaglandin-like activities.
摘要翻译：本发明涉及以下通式的前列腺素类似物：其中A表示下式的基团：X表示反式亚乙烯基或亚乙基，Y表示顺式亚乙烯基或亚乙基，R表示式-COOR4，其中R 4表示氢或1至12个碳原子的直链或支链烷基，或式-CH 2 OR 5的基团，其中R 5表示氢或2至5个碳原子的烷基羰基，R 1，R 2 和可以相同或不同的R 3各自表示氢，1至12个碳原子的直链或支链烷基，或未取代或被1,2或3个选自烷基，烷氧基，烷硫基的取代基取代的芳基，单烷基氨基和二烷基氨基和卤素原子，所述基团的直链或支链含有1至5个碳原子的烷基或部分，条件是R1，R2和R3中的至少一个符号是除了氢和 C2-C3之间的双键是反式]和这种前列腺素类似物的环糊精包合物，当组COOR4中的R4表示氢时，其无毒性盐显示出特征性的前列腺素样活性。

3. 发明授权

US4045468A 16-Cyclobutyl-prostaglandins 失效
标题翻译： 16-环丁基 - 前列腺素
公开(公告)号：US4045468A
公开(公告)日：1977-08-30
申请号：US557437
申请日：1975-03-11
申请人： Masayasu Kurono , Hisao Nakai , Takashi Muryobayashi
发明人： Masayasu Kurono , Hisao Nakai , Takashi Muryobayashi
IPC分类号： A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07D309/12 , C07F9/40 , C07C177/00
CPC分类号： C07D307/935 , C07C405/00 , C07C405/0016 , C07C405/0025 , C07D309/12 , C07F9/4018 , Y10S514/927
摘要： Prostaglandin analogues of the formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## X represents trans-vinylene or ethylene and Y represents cis-vinylene or ethylene, R represents hydrogen or alkyl of 1 through 12 carbon atoms, R.sup.1, R.sup.2 and R.sup.3 represent hydrogen, or alkyl of 1 through 12 carbon atoms or an aryl group, with the proviso that at least one of the symbols R.sup.1, R.sup.2 and R.sup.3 represents an alkyl or aryl group, are new compounds possessing useful pharmacological properties; they are especially useful for the treatment of gastric ulceration.
摘要翻译：其中A表示下式的组：X表示反式亚乙烯基或亚乙基，Y表示顺式亚乙烯基或亚乙基，R表示氢或1至12个碳原子的烷基，R 1 R 2和R 3表示氢或1〜12个碳原子的烷基或芳基，条件是R1，R2和R3中的至少一个表示烷基或芳基，是具有有用药理特性的新化合物; 它们特别适用于治疗胃溃疡。

4. 发明授权

US4117119A 15-Cyclobutyl-prostaglandins 失效
标题翻译： 15-CYCLOBUTYL-PROSTAGLANDINS
公开(公告)号：US4117119A
公开(公告)日：1978-09-26
申请号：US794580
申请日：1977-05-06
申请人： Masayasu Kurono , Hisao Nakai , Takashi Muryobayashi
发明人： Masayasu Kurono , Hisao Nakai , Takashi Muryobayashi
IPC分类号： C07C51/353 , C07C51/60 , C07C61/04 , C07C405/00 , C07D307/935 , C07D309/12 , C07F9/40 , C07C177/00 , A61K31/19 , A61K31/215
CPC分类号： C07D307/935 , C07C405/00 , C07C51/353 , C07C51/60 , C07C61/04 , C07D309/12 , C07F9/4018 , Y10S514/899 , Y10S514/925
摘要： Prostaglandin analogues of the formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## X represents trans-vinylene or ethylene and Y represents cis-vinylene or ethylene, R represents hydrogen or alkyl of 1 through 12 carbon atoms, R.sup.1, R.sup.2 and R.sup.3 represent hydrogen, or alkyl of 1 through 12 carbon atoms or an aryl group, with the proviso that at least one of the symbols R.sup.1, R.sup.2 and R.sup.3 represents an alkyl or aryl group, are new compounds possessing useful pharmacological properties; they are especially useful for the treatment of gastric ulceration.

5. 发明授权

US07649095B2 Piperidine derivatives and agent comprising the derivative as active ingredient 失效
标题翻译：哌啶衍生物和包含该衍生物作为活性成分的试剂
公开(公告)号：US07649095B2
公开(公告)日：2010-01-19
申请号：US11401846
申请日：2006-04-12
申请人： Hisao Nakai , Katsuya Kishikawa
发明人： Hisao Nakai , Katsuya Kishikawa
IPC分类号： C07D211/08 , C07D211/26 , C07D211/20
CPC分类号： C07D211/22 , C07D211/64
摘要： Piperidine derivatives represented by formula (I) or nontoxic salts thereof (wherein symbols are defined in the description): Since the compound represented by formula (I) has a PDE4 inhibitory activity, it is useful for preventing and/or treating inflammatory diseases, diabetic diseases, allergic diseases, autoimmune diseases, osteoporosis, bone fracture, obesity, depression, Parkinson's disease, dementia, ischemia-reperfusion injury, leukemia and the like.
摘要翻译：由式（I）表示的哌啶衍生物或其无毒盐（其中符号在说明书中定义）：由于式（I）表示的化合物具有PDE4抑制活性，因此可用于预防和/或治疗炎性疾病，糖尿病疾病，过敏性疾病，自身免疫性疾病，骨质疏松症，骨折，肥胖症，抑郁症，帕金森病，痴呆，缺血再灌注损伤，白血病等。

6. 发明申请

US20080027094A1 Tropane Compounds and Pharmaceutical Compositions Comprising the Same as an Active Ingredient 审中-公开
标题翻译：包含与活性成分相同的托烷化合物和药物组合物
公开(公告)号：US20080027094A1
公开(公告)日：2008-01-31
申请号：US11661310
申请日：2005-08-29
申请人： Hisao Nakai , Toshihiko Nishiyama , Nobuyuki Nakamura , Manabu Fujita
发明人： Hisao Nakai , Toshihiko Nishiyama , Nobuyuki Nakamura , Manabu Fujita
IPC分类号： A61K31/46 , A61P11/06 , C07D451/02
CPC分类号： C07D451/06 , A61K31/00
摘要： The conventional anticholinergic drugs for administration through inhalation have been considered to have the possibility of aggravating dysuria associated with prostatic hyperplasia mediated by blood, and it has been demanded that the conventional anticholinergic drugs for administration through inhalation will have to show reduced side effects or adverse reactions. The present invention relates to a compound represented by the general formula (I): (wherein A represents; and R1, R2, R3 and R1 each a hydrogen atom or a substituent; R5 is a substituent; X− is an anion; the symbol: denotes an exo-form or endo-form, or their mixture), its salt or solvation product thereof. They are useful as a prophylactic and/or therapeutic agent with reduced side effects or adverse reactions for the diseases mediated by the muscarinic receptor.
摘要翻译：通过吸入给药的常规抗胆碱能药物被认为具有加重与血液介导的前列腺增生相关的排尿困难的可能性，并且已经要求用于通过吸入给药的常规抗胆碱能药物必须显示减少的副作用或不良反应。本发明涉及由通式（I）表示的化合物：（其中A表示; R 1，R 2，R 3，和R 1各自为氢原子或取代基; R 5为取代基; X为 - 阴离子;符号为：img id =“custom-character-00001”he =“2.46mm”wi =“3.89mm”file =“US20080027094A1-20080131-P00001.TIF”img-content =“character”img-format =“tif”/> 外部形式或内在形式，或其混合物），其盐或溶剂化产物。它们可用作对由毒蕈碱受体介导的疾病的副作用或不良反应降低的预防和/或治疗剂。

7. 发明申请

US20050222138A1 Nitrogen-containing bicyclic compounds and drugs containing the same as the active ingredient 失效
标题翻译：含氮双环化合物和含有与活性成分相同的药物
公开(公告)号：US20050222138A1
公开(公告)日：2005-10-06
申请号：US10502884
申请日：2003-01-30
申请人： Akira Ohhata , Yoshikazu Takaoka , Mikio Ogawa , Hisao Nakai , Susumu Yamamoto , Hiroshi Ochiai
发明人： Akira Ohhata , Yoshikazu Takaoka , Mikio Ogawa , Hisao Nakai , Susumu Yamamoto , Hiroshi Ochiai
IPC分类号： A61K31/4035 , A61K31/472 , A61K31/4725 , A61K31/4738 , A61K31/496 , A61K31/497 , A61K31/536 , A61K31/5377 , A61K31/541 , A61K31/5415 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/04 , A61P3/10 , A61P9/00 , A61P9/10 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , C07D217/04 , C07D491/107 , C07D279/16
CPC分类号： C07D217/04 , A61K31/4035 , A61K31/472 , A61K31/4725 , A61K31/4738 , A61K31/496 , A61K31/497 , A61K31/536 , A61K31/5377 , A61K31/541 , A61K31/5415
摘要： A nitrogen-containing bicyclic compound of formula (I) or a pharmaceutically acceptable salt thereof (wherein the symbols have the same meanings as described in the specification). The compound of formula (I) has an inhibitory activity against PDE7 and it is useful for the prevention and/or treatment of various diseases, i.e. autoimmune diseases (ulcerative colitis, Crohn's disease, rheumatism, psoriasis, multiple sclerosis, collagenosis, etc.), inflammatory diseases (obstructive pulmonary disease, sepsis, pancreatitis, sarcoidosis, nephritis, hepatitis, enteritis, etc.), allergic diseases (asthma, allergic rhinitis, allergic conjunctivitis, seasonal conjunctivitis, atopic dermatitis, etc.), rejection of organ transplants, serious graft versus host disease (GVHD), diabetic disease, osteoporosis, bone fracture, restenosis, atherosclerosis, obesity, ischemic reperfusion injury, depression, Parkinson's disease, dementia, leukemia, etc.
摘要翻译：式（I）的含氮双环化合物或其药学上可接受的盐（其中符号具有与说明书中所述相同的含义）。式（I）化合物对PDE7具有抑制活性，可用于预防和/或治疗各种疾病，即自身免疫性疾病（溃疡性结肠炎，克罗恩病，风湿病，牛皮癣，多发性硬化症，胶原病等），炎性疾病（阻塞性肺病，败血症，胰腺炎，结节病，肾炎，肝炎，肠炎等），过敏性疾病（哮喘，过敏性鼻炎，过敏性结膜炎，季节性结膜炎，特应性皮炎等），器官移植排斥，严重的移植物抗宿主病（GVHD），糖尿病，骨质疏松症，骨折，再狭窄，动脉粥样硬化，肥胖，缺血再灌注损伤，抑郁症，帕金森病，痴呆，白血病等。

8. 发明授权

US06583177B2 Leukotriene B4 antagonist compounds and method for treatment 失效
标题翻译：白三烯B4拮抗剂化合物及其治疗方法
公开(公告)号：US06583177B2
公开(公告)日：2003-06-24
申请号：US09897451
申请日：2001-07-03
申请人： Hisao Nakai , Koumei Kamiyasu
发明人： Hisao Nakai , Koumei Kamiyasu
IPC分类号： A61K31216
CPC分类号： C07D233/64 , C07C257/14 , C07C257/16 , C07C257/18 , C07C2602/10 , C07D209/42 , C07D211/14 , C07D211/26 , C07D307/14 , C07F9/3241 , C07F9/4015
摘要： Novel amidinophenol derivatives of formula (IB) and processes for the preparation thereof; compositions containing a compound of formula (IB) as active ingredient useful as antagonists of leukotine B4 and inhibitors of phospholipase A2 and/or trypsin; methods for preventing or treating diseases induced by phospholipase A2 and/or trypsin comprising administering to a patient a compound of formula (IB); and methods for treating diseases induced by leukotine B4 comprising administering to a patient a compound of formula (IB) or a known amidinophenol derivative of formula (IA)
摘要翻译：式（IB）的新型脒基苯酚衍生物及其制备方法; 含有式（IB）化合物作为白细胞素B4拮抗剂和磷脂酶A2和/或胰蛋白酶抑制剂的活性成分的组合物; 用于预防或治疗由磷脂酶A2和/或胰蛋白酶诱导的疾病的方法，包括向患者施用式（IB）化合物; 以及用于治疗由白细胞素B4诱导的疾病的方法，包括向患者施用式（IB）化合物或已知的式（IA）的脒基苯酚衍生物，

9. 发明申请

US20080081825A1 Nitrogen-Containing Heterocyclic Compounds and Medicinal Use Thereof 审中-公开
标题翻译：含氮杂环化合物及其药物用途
公开(公告)号：US20080081825A1
公开(公告)日：2008-04-03
申请号：US11587825
申请日：2005-04-27
申请人： Hisao Nakai , Shingo Yamamoto , Masafumi Sugitani
发明人： Hisao Nakai , Shingo Yamamoto , Masafumi Sugitani
IPC分类号： A61K31/4412 , A61K31/4545 , A61P11/00 , A61P19/02 , A61P19/08 , A61P29/00 , A61P43/00 , A61P9/00 , C07D211/86 , C07D401/02
CPC分类号： C07D211/76 , A61K31/438 , A61K31/4418 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D211/86 , C07D213/64 , C07D213/89 , C07D401/12 , C07D401/14 , C07D413/12 , C07D417/12
摘要： The present invention provides a compound having p38 MAP kinase inhibitory activity. Because of having p38 MAP kinase inhibitory activity, the compounds represented by the formula (I): wherein each symbol is as defined in the description, salts thereof, N-oxides thereof, solvates thereof, or prodrugs thereof are useful in preventing and/or treating diseases that are supposedly caused or deteriorated by abnormal production of cytokines including inflammatory cytokines or chemokines, or by overresponse thereto, namely cytokine-mediated diseases such as inflammatory diseases, respiratory diseases, cardiovascular diseases and bone diseases.
摘要翻译：本发明提供具有p38 MAP激酶抑制活性的化合物。由于具有p38 MAP激酶抑制活性，式（I）表示的化合物：其中每个符号如说明书中所定义，其盐，其N-氧化物，其溶剂化物或其前药可用于预防和/或治疗由于异常产生包括炎性细胞因子或趋化因子的细胞因子或其过度反应，即细胞因子介导的疾病如炎性疾病，呼吸系统疾病，心血管疾病和骨骼疾病引起或恶化的疾病。

10. 发明申请

US20070027156A1 Crf antagonists and heterobicyclic compounds 审中-公开
标题翻译： Crf拮抗剂和杂双环化合物
公开(公告)号：US20070027156A1
公开(公告)日：2007-02-01
申请号：US10571271
申请日：2004-09-08
申请人： Hisao Nakai , Tetsuji Saito , Tetsuo Obitsu , Chiaki Minamoto , Mayuki Yoshida , Akihiro Kishi , Seishi Katsumata , Hideo Katayama
发明人： Hisao Nakai , Tetsuji Saito , Tetsuo Obitsu , Chiaki Minamoto , Mayuki Yoshida , Akihiro Kishi , Seishi Katsumata , Hideo Katayama
IPC分类号： A61K31/53 , A61K31/519 , C07D487/02
CPC分类号： C07D239/70 , C07D221/04 , C07D487/04 , C07D491/04
摘要： CRF antagonists comprising as an active ingredient, the compound of formula (I) wherein A ring is 5-6 membered mono-cyclic ring which may be substituted; B ring is 5-7 membered unsaturated mono-heterocyclic ring which may be contained another 1-2 of hetero atom(s) and substituted by another substituents; W1 and W2 is carbon atom or nitrogen atom; Z is NR3, oxygen atom, sulfur which may be oxidized or CR4R5; R1 is alkyl, alkenyl or alkynyl that may be substituted, amino which may be protected, hydroxyl which may be protected, S(O)nR6, COR7, or cyclic group which may be substituted; R2 is unsaturated cyclic group which may be substituted.
摘要翻译： CRF拮抗剂，其包含作为活性成分的式（I）化合物，其中A环是可被取代的5-6元单环; B环是5-7元不饱和单杂环，其可以含有另外1-2个杂原子并被另一个取代基取代; W 1和W 2是碳原子或氮原子; Z是NR 3，氧原子，可被氧化的硫或CR 4 R 5; R 1是可被取代的烷基，烯基或炔基，可被保护的氨基，可被保护的羟基，S（O）n R 6， COR 7或可以被取代的环状基团; R 2是可以被取代的不饱和环状基团。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式