| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 21 | Immunoproteasome inhibitor analogs | US16078348 | 2017-03-10 | US10584105B2 | 2020-03-10 | Michael C. Pirrung; Nicole A. Bakas; Andre Bachmann |
| The disclosure provides for compounds having immunoproteasome inhibitory activity, and pharmaceutical compositions made thereof. The disclosure further provides for the use of the compounds and compositions in treating various diseases and disorders in a subject that are associated with immunoproteasome activity, including inflammatory disorders, autoimmune disorders, hematological disorders, and neurodegenerative disorders. | ||||||
| 22 | SYNTHESIS OF SYRBACTIN PROTEASOME INHIBITORS | US13513855 | 2010-12-03 | US20130065872A1 | 2013-03-14 | Michael C. Pirrung |
| The disclosure relates generally to methods for the preparation of a family of natural compounds, the syrbactins and their analogs. | ||||||
| 23 | Rapamycin 29-Enols | US10224971 | 2002-08-22 | US20030114477A1 | 2003-06-19 | Tianmin Zhu; Mahdi B. Fawzi |
| This invention provides non-immunosuppressive rapamycin 29-enols, which are useful as neurotrophic agents, in the treatment of solid tumors, and vascular disease. | ||||||
| 24 | Hypolipidemic 1,4-benzothiazepine-1,1-dioxides | US361530 | 1999-07-27 | US6114322A | 2000-09-05 | Alfons Enhsen; Eugen Falk; Heiner Glombik; Siegfried Stengelin |
| The present invention is concerned with new hypolipidemic compounds, with processes and novel intermediates for their preparation, with pharmaceutical compositions containing them and with their use in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions, such as atherosclerosis.Compounds of the formula (I): ##STR1## wherein R.sup.1 to R.sup.10 and X are as defined in the Specification and useful as hypolipidemic compounds. | ||||||
| 25 | Process for preparing diltiazem | US601182 | 1996-02-14 | US5644054A | 1997-07-01 | Martti Hytonen |
| A process is provided for preparing cis-(+)-hydroxy-5-[2-(dimethylamine)ethyl]-2,3-dihydro-2-(4-methoxyphenyl)-benzothiazepin-4(5H)-one that is a useful intermediate in the preparation of diltiazem. It has been found that the requisite N-alkylation reaction proceeds rapidly and with an excellent yield when the solvent is a mixture of toluene and N-methylpyrrolidin-2-one and the base is finely-divided sodium carbonate under anhydrous conditions. Such diltiazem commonly is used in the treatment of angina pectoris. | ||||||
| 26 | 8-substituted-2-aminotetralins | US33013 | 1993-03-18 | US5635537A | 1997-06-03 | Nils-Erik Anden; Berit C. E. Backlund Hook; Anna L. Bjork; Uli A. Hacksell; Sven-Erik Hillver; Ye Liu; Eva C. Mellin; Eva M. Persson; Karl J. Vallg.ang.rda; Hong Yu |
| A compound of the formula ##STR1## Z is hydrogen or halogen, Q is COR.sup.1 or 5-or 6-membered aryl which may contain 1 or 2 heteroatoms selected from N, 0 or S and may be substituted or fused wherein R is hydrogen or C.sub.1 -methyl (cis-configuration), R.sup.1 is C.sub.1 -C.sub.6 alkyl or an aromatic ring which may contain heteroatoms selected from O and S and may be substituted or fused to an optionally substituted benzene ring, R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sup.3 may be different groups defined in claim 1, and enantiomers/salts thereof, processes for preparation of said compounds, pharmaceutical preparations containing said compounds, use of and method of treatment of disorders in CNS by using said compounds. | ||||||
| 27 | Cyclic renin inhibitors containing 2-substituted (3S,4S)-4-amino-5-cyclohexyl-3-hydroxy pentanoic acid, 2-substituted (3S,4S)-5-cyclohexyl-3,4-di-hydroxy pentanoic acid or 2-substituted (4S,5S)-5-amino-6-cyclohexyl-4-hydroxyhexanoic acid or its analogs | US714115 | 1991-06-11 | US5194605A | 1993-03-16 | William J. Greenlee; Ralph A. Rivero; Ann E. Weber; Lihu Yang |
| Compounds of the formula ##STR1## are disclosed. These compounds inhibit the angiotensinogen-cleaving action of the natural proteolytic enzyme, renin, are useful in treating, preventing or managing renin-associated hypertension, hyperaldosteronism, congestive heart failure, and glaucoma. | ||||||
| 28 | Condensed, seven-membered ring compounds and their use | US599187 | 1984-04-11 | US4564612A | 1986-01-14 | Hirosada Sugihara; Kohei Nishikawa; Katsumi Ito |
| Novel condensed, seven-membered ring compounds of the formula: ##STR1## [wherein R.sup.1 and R.sup.2 each represent hydrogen, halogen, trifluoromethyl, lower alkyl or alkoxy, or both jointly form tri- or tetramethylene; R.sup.3 is hydrogen, lower alkyl or aralkyl; R.sup.4 is hydrogen or alkyl, aralkyl or cycloalkylalkyl which may be substituted; X is a group represented by the formula S(O).sub.n (where n is an integer of 0 to 2); Y is a carboxyl group which may be esterified or amidated; m is 1 or 2] and salts thereof.These compounds exhibit inhibitory activity on angiotensin converting enzyme and so forth, and are of value as an agent for diagnosis, prevention and treatment of hypertension. | ||||||
| 29 | Tricyclic compounds | US331303 | 1981-12-16 | US4374133A | 1983-02-15 | Johannes H. Wieringa |
| The present invention relates to new dibenzoxazonine, dibenz-oxazecine or dibenzo-oxaazacycloundecane derivatives and corresponding thia- and aza derivatives thereof, of the general formula I: ##STR1## or a pharmaceutically acceptable acid addition salt or nitrogen oxide thereof, in whichX represents oxygen, sulphur or the group NR.sub.5,R.sub.5 is hydrogen or alkyl (1-4 C),R.sub.1, R.sub.2, R.sub.3, R.sub.4 each represent hydrogen, hydroxy, halogen, cyano, alkyl, alkoxy, aralkoxy, alkylthio, methylenedioxy, CF.sub.3, NO.sub.2, NH.sub.2, hydroxyalkyl or an acyloxy group,R represents hydrogen, alkyl, alkenyl or aralkyl, hydroxyalkyl or acyloxyalkyl andn represents the number 0, 1 or 2, having valuable C.N.S. properties. | ||||||
| 30 | Pharmaceutical group of compounds | JP51195998 | 1997-08-29 | JP4364944B2 | 2009-11-18 | アル―アウォー，リマ・エス; エールハート，ウィリアム・ジェイ; ゴットゥムッカラ，サバラジュ・ブイ; シー，チュアン; トス，ジョン・イー; ノーマン，ブライアン・エイチ; バスデバン，ベンカトラガバン; ペイテル，ビノッド・エフ; マルティネリ，マイケル・ジェイ; マンロー，ジョン・イー; ムーア，リチャード・イー; モーアー，エリック・ディ; レイ，ジェイムズ・イー |
| 31 | 9-amino-substituted 9,10-dihydro-pyrrolo [2,1-b] [1,3] a process for the preparation of benzothiazepine | JP2002515903 | 2001-07-20 | JP2004505089A | 2004-02-19 | ドメニコ・マストロヤンニ; パトリツィア・ミネッティ |
| 下記式の化合物の調製方法を記載する。 ここで、各基は明細書中に定義するとおりであり、特に、Ｒ
１は置換アミンである；前記方法は本質的にピロロベンゾチアゼピン−９−オンとアミンＲ
１ Ｈとの反応を含み、これによって対応するエナミンが生じ、これがその後続いて最終化合物へと変換される。
【化１】 |
||||||
| 32 | Dual action inhibitor | JP11587493 | 1993-05-18 | JP3487611B2 | 2004-01-19 | エドワード・ダブリュー・ペトリロ・ジュニア; ジェフリー・エイ・ロブル; ジョエル・シー・バリッシュ; デニス・イー・リオノ; ドナルド・エス・カラネウスキ |
| 33 | Teiaburachisei 1,4-benzothiazepine 1,1-dioxide | JP6266598 | 1998-03-13 | JP3282998B2 | 2002-05-20 | アルフオンス・エンゼン; オイゲン・フアルク; ジークフリート・シユテンゲリン; ハイナー・グロムビク |
| 34 | Tricyclic benzazepine vasopressin antagonist | JP19588694 | 1994-07-28 | JPH07179430A | 1995-07-18 | JIEI DEI ARUBURAITO; MAABIN EFU REIKU; FUKUUWA SAMU; SHIYUEMEI DOU |
| PURPOSE: To obtain a novel tricyclic compound which has antagonist activity at V 1 and/or V 2 receptors and exhibits in vivo vasopressin antagonist activity and is useful for treatment of diseases characterized by excess renal reabsorption of water. CONSTITUTION: A compound of formula I {wherein Y is (CH 2) n ((n) is 0-2), O, S, NH, NCOCH 3, an N-alkyl, a CH-alkyl, CO or the like; A-B is formula II, formula III {(m) is 1 or 2; R 3 is a CO-Ar [Ar is formula IV-formula VI (X is O, S, NCH 3 or the like; R 4 is H, an alkyl or the like; R 5 is H, CH, Cl, Br or the like; R 6 is formula VII or he like; R 7 is R 5 or CF 3)]}; R 1 is H, a halogen, OH, an S-alkyl, an alkyl or the like; R 2 is H, a halogen, an alkyl or the like; formula VIII is a substitutable united phenyl, a 5-membered aromatic (unsaturated) heterocycle having one htereroatome, a 6-membered aromatic (unsaturated) heterocycle having one N}, for example, N-[(10,11-dihydro-5- dibenz[b,f]azepin-5-yl)carbonyl]phenyl-2-methylbenzamide. COPYRIGHT: (C)1995,JPO | ||||||
| 35 | Cyclic renin inhibitor containing 3(s)-amino-4-cyclohexyl-2(r)-hydroxybutanoic acid, 4-cyclohexyl-(2r,3s)-dihydroxybutanoic acid, or related analogue | JP41928990 | 1990-12-10 | JPH07173142A | 1995-07-11 | DARUJITSUTO ESU DANOA; AASAA EE PACHIETSUTO; UIRIAMU JIEE GURIINRII; UIRIAMU ETSUCHI PAASONZU; TOOMASU EE HARUGUREN; AN II UEBAA |
| PURPOSE: To obtain the subject novel inhibitor which inhibits the angiotensinogen-cleaving action of a natural proteolytic enzyme, renin, and is useful in treating or preventing renin-associated hypertension, hyperaldosteronism, glaucoma, or the like. CONSTITUTION: There is provided an inhibitor of formula I {wherein A is H, or a heterocyclic group such as quinuclidinyl, piperidinyl or oxazolyl; B is O-CH[(CH 2) rR 3]CO-O, N(A 1)CH{(CH 2) rR 3} CH(OH)CH 2 (wherein (r) is 0-2; A 1 is H or a 1-4C alkyl; R 3 is H, a 1-4C alkyl, or the like), or the like; W is O, N(R 23) (wherein R 23 is H or a 1-4C alkyl); Y is O-CO, CH 2-CO, or the like; D is N(R 25)CO (wherein R 25 is H or a 1-4C alkyl), or the like; R 1 and R 16 are each H, a 1-4C alkyl, or the like; R 15 is a 1-4C alkyl, phenyl, or the like; R 24 is H or a 1-4C alkyl; (s) is 0-1; (r) is 0-2; (t) is 1-4; and Z is NH-OH or the like}, for example, a compound of formula II. COPYRIGHT: (C)1995,JPO | ||||||
| 36 | JPH0374660B2 - | JP7335785 | 1985-04-05 | JPH0374660B2 | 1991-11-27 | |
| 37 | JPH0374222B2 - | JP15413083 | 1983-08-25 | JPH0374222B2 | 1991-11-26 | |
| 38 | JPS6156236B2 - | JP18444585 | 1985-08-21 | JPS6156236B2 | 1986-12-01 | MURAI HIROSHI; MATSUMURA SHINGO; MORITA IWAO; SUNO KENJI; ENOMOTO HIROSHI; KIMURA KYOSHI; KIMURA YUTAKA |
| 39 | 1,5-benzothiazepine derivative and its preparation | JP7335785 | 1985-04-05 | JPS60226867A | 1985-11-12 | TAKEDA MIKIO; OOISHI ATSUO; NAKAJIMA HIROMICHI; NAGAO HIROSHI |
| NEW MATERIAL:The 1,5-benzothiazepine derivative of formula I (R 1 is lower alkyl; R 2 is H or lower alkanoyl; R 3 is lower alkyl) or its salt. EXAMPLE: (±)-cis-2-(4-methylphenyl)-3-hydroxy-5-[ 2-( N-methylamino )-ethyl ]-2,3- dihydro-1,5-benzothiazepin-4(5H)-one. USE: A drug having thrombocyte coagulation inhibiting action and useful for the remedy, remission and prevention of diseases such as cerabral infarction, cerebral thrombosis, transient ischemic attack, myocardial infarction, coronary thrombosis, pulmonary thrombosis, thrombotic vasculitis, etc. PREPARATION: The compound of formula I can be prepared by reacting the compound of formula II or its salt with the compound of formula III (Q is H or protecting group; X is halogen) or its sale, and when the substituent group Q is protecting group, removing the protecting group from the compound of formula IV. COPYRIGHT: (C)1985,JPO&Japio | ||||||
| 40 | Benzothiazepine derivative | JP24467583 | 1983-12-27 | JPS60139682A | 1985-07-24 | KATAUE ISAO; FUKAZAWA NOBUYUKI; IIZUKA HAJIME; NISHINA TAKASHI; SHIRAKAWA ISAO |
| NEW MATERIAL:A compound expressed by formula I (R 1 is H, 1W15C straight chain, branched or cyclic alkyl or phenyl substituted lower alkyl; either one or both of R 2 and R 3 are hydroxyl group, lower alkoxyl, amino-substituted lower alkoxyl, etc.; R 4 is H, lower alkyl or phenyl), stereoisomers, various salts and complexes thereof. EXAMPLE: 3-( 1-Ethoxycarbonyl-3-phenylpropylamino )-5-ethoxycarbonylmethyl-2,3- dihydro-1,5-benzothiazepin-4(5H)-one. USE: Useful as a remedy for cardiovascular systems, e.g. an antihypertensive agent and antiangina pectoris agent, etc., and capable of very powerfully inhibiting angiotensin converting enzymes. PREPARATION: An amine compound expressed by formula (A) and an α-detocarboxylic acid derivative expressed by formula (B) are mixed and dissolved in a solvent, e.g. dimethylformamide (DMF), and the reductive reaction is carried out using a suitable reducing agent to afford the aimed compound expressed by formula I . COPYRIGHT: (C)1985,JPO&Japio | ||||||
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