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1. 发明申请

US20150252069A1 Anthracycline Derivatives For Treating Tumor Diseases 审中-公开
标题翻译：蒽环类衍生物治疗肿瘤疾病
公开(公告)号：US20150252069A1
公开(公告)日：2015-09-10
申请号：US14435907
申请日：2013-10-15
申请人： Produkem Molekulares Design GmbH
发明人： Christian R. Noe , Michael Sonntagbauer , Sébastien Queva , Ernst Urban
IPC分类号： C07H15/244 , C07D317/34 , C07C45/59 , C07D317/26 , C07D307/20 , C07D317/32 , C07F7/18
CPC分类号： C07H15/244 , C07C15/28 , C07C45/59 , C07C2603/24 , C07C2603/44 , C07D307/20 , C07D317/26 , C07D317/32 , C07D317/34 , C07F7/1804 , C07H15/08 , C07H15/252
摘要： The invention relates to compounds of the general formula (I) in which R1 is a hydrogen atom, a hydroxy or methoxy group, a halogen atom, or an NO2 group; R2 is a hydrogen atom, a hydroxy or methoxy group, or an acyl or aroyl group; R3 is hydrogen, trifluoroacetyl (C(═O)CF3), or p-nitrobenzoyl (C(═O)PhNO2), and in each case the wavy line represents both possible configurations of —OR3 relative to the skeleton; Y is [C(═O)], [C(═N)—OH], [CH—OH], or [CH—NR5R6] in the two possible stereoisomer arrangements, wherein R5 and R6 either each represent a hydrogen atom or a hydrogen atom and a trifluoroacetyl group (TFA); X=O, S, or NR, in which R=hydrogen or a C1 to C4 alkyl group; and R4 is an unbranched or branched alkyl or heteroalkyl chain with a chain length of 1 to 19 elements, maximally 6 heteroatoms (O, N, S) being separated from one another in any combination by at least two carbon atoms. The invention further relates to, among others, methods for producing the compounds according to formula (I), to pharmaceutical compositions, to a pharmaceutical kit, and to the use thereof as a medicament for treating proliferative diseases or conditions, preferably cancer.
摘要翻译：本发明涉及其中R 1为氢原子，羟基或甲氧基，卤素原子或NO 2基团的通式（I）的化合物; R2是氢原子，羟基或甲氧基，或酰基或芳酰基; R3是氢，三氟乙酰基（C（= O）CF 3）或对硝基苯甲酰基（C（= O）PhNO 2），并且在每种情况下，波浪线表示-OR3相对于骨架的可能构型; 两种可能的立体异构体排列中Y是[C（= O）]，[C（= N）-OH]，[CH-OH]或[CH-NR5R6]，其中R5和R6各自表示氢原子或氢原子和三氟乙酰基（TFA）; X = O，S或NR，其中R =氢或C1至C4烷基; 并且R4是链长为1至19个元素的非支链或支链烷基或杂烷基链，最多6个杂原子（O，N，S）以任何组合彼此分开至少两个碳原子。本发明还涉及用于制备式（I）化合物，药物组合物，药物试剂盒及其用作治疗增殖性疾病或病症（优选癌症）的药物的用途的方法。

2. 发明申请

US20150119573A1 METHOD FOR SYNTHESIZING SAPROPTERIN DIHYDROCHLORIDE 有权
标题翻译：合成SAPROPTERIN二氢氯化物的方法
公开(公告)号：US20150119573A1
公开(公告)日：2015-04-30
申请号：US14394079
申请日：2012-12-27
申请人： ASYMCHEM LABORATORIES (TIANJIN)CO., LTD. , ASYMCHEM LIFE SCIENCE (TIANJIN) CO., LTD , TIANJIN ASYMCHEM PHARMACEUTICAL CO., LTD. , ASYMCHEM LABORATORIES (FUXIN) CO., LTD. , JILIN ASYMCHEM LABORATORIES CO. LTD.
发明人： Hao Hong , James Gage , Chaoyong Chen , Jiangping Lu , Yan Zhou , Shuangyong Liu
IPC分类号： C07D475/04 , C07D317/32 , C07D317/26 , C07C221/00 , C07D239/50 , C07C209/62 , C07D317/28 , C07D303/48 , C07C225/06
CPC分类号： C07D475/04 , C07C209/62 , C07C221/00 , C07C225/06 , C07D239/50 , C07D303/48 , C07D317/26 , C07D317/28 , C07D317/32
摘要： Disclosed is a method for synthesizing sapropterin dihydrochloride. The present disclosure reduces a synthesis route of the sapropterin dihydrochloride, and resolves a racemate intermediate or an intermediate having a low antimer isomerism value by using a chiral resolving reagent, thereby obtaining an intermediate having a high antimer isomerism value. Raw materials are cheap and readily available, and the cost is significantly reduced, hence providing an effective scheme for mass industrial production of the sapropterin dihydrochloride.
摘要翻译：披露了一种合成沙rop in二盐酸盐的方法。本公开内容减少了沙棘蛋白二盐酸盐的合成途径，并且通过使用手性拆分试剂拆分外消旋体中间体或具有低antimer异构值的中间体，从而获得具有高antimer异构值的中间体。原材料便宜，易于获得，成本显着降低，为大规模工业生产四氢叶酸二盐酸盐提供了有效的方案。

3. 发明授权

US06977292B2 Nucleophile-stable thioester generating compounds, methods of production and use 失效
标题翻译：亲核稳定硫酯生成化合物，生产和使用方法
公开(公告)号：US06977292B2
公开(公告)日：2005-12-20
申请号：US10332454
申请日：2001-08-30
申请人： Paolo Botti , James A. Bradburne , Stephen B. H. Kent
发明人： Paolo Botti , James A. Bradburne , Stephen B. H. Kent
IPC分类号： C07D317/32 , C07C323/52 , C07C323/59 , C07D317/34 , C07D319/06 , C07K1/00 , C07K1/02 , C07K1/04 , C07K7/00
CPC分类号： C07K1/023 , C07C323/52 , C07K1/006 , C07K1/026 , C07K1/04
摘要： The invention is directed to nucleophile-stable thioester generating compounds comprising a carboxyester thiol. The compounds have wide applicability in organic synthesis, including the generation of peptide-, polypeptide- and other polymer-thioesters. The invention is particularly useful for generating activated-thioesters from precursors that are made under conditions in which strong nucleophiles are employed, such as peptides or polypeptides made using Fmoc SPPS, as well as multi-step ligation or conjugation schemes that require (or benefit from the use of) compatible selective approaches for directing a specific ligation or conjugation reaction of interest.
摘要翻译：本发明涉及包含羧基酯硫醇的产生亲核试剂的硫代酯化合物。这些化合物在有机合成中具有广泛的应用，包括产生肽，多肽和其他聚合物 - 硫酯。本发明特别可用于从在其中使用强亲核试剂的条件下制备的前体产生活化硫酯，例如使用Fmoc SPPS制备的肽或多肽，以及需要（或从中获益）的多步连接或缀合方案用于引导感兴趣的特异性连接或缀合反应的相容性选择性方法。

4. 发明授权

US06905739B2 Optically active materials 失效
标题翻译：光学活性材料
公开(公告)号：US06905739B2
公开(公告)日：2005-06-14
申请号：US10168137
申请日：2000-12-20
申请人： Zoubair Mohammed Cherkaoui , Klaus Schmitt
发明人： Zoubair Mohammed Cherkaoui , Klaus Schmitt
IPC分类号： G02F1/13 , C07C69/92 , C07C69/94 , C07D207/12 , C07D317/24 , C07D317/32 , C08F20/20 , C09K19/20 , C09K19/38 , C09K19/54 , C09K19/58 , C09K19/52 , C09K19/30 , C09K19/32 , C09K19/34
CPC分类号： C09K19/586 , C09K19/2014 , C09K19/2028 , C09K2019/0448 , Y10T428/10
摘要： A compound is of formula (I), in which: A1 to A4, E1 and E2 each independently represent hydrogen or an optionally-substituted hydrocarbon group; B1 and B2 each independently represent a single bond, an oxygen atom or an optionally-substituted hydrocarbon group; MG1 and MG2 each independently represent an optionally-substituted ring system; CG is a divalent or polyvalent chiral group. The optically active compound may be used as a doping agent for liquid crystals for a wide range of applications including solid state cholesteric filters for projection displays, circular polarisers, optical filters, etc.
摘要翻译：化合物为式（I）化合物，其中：A 1至A 4，E 1和E 2 >各自独立地表示氢或任选取代的烃基; B 1和B 2各自独立地表示单键，氧原子或任选取代的烃基; MG 1和MG 2各自独立地表示任选取代的环系; CG是二价或多价手性基团。光学活性化合物可以用作液晶的掺杂剂，用于广泛的应用，包括用于投影显示器的固态胆甾醇型滤光器，圆形偏振器，滤光器等。

5. 发明申请

US20050014833A1 Cyclic compound and ppar agonist 失效
标题翻译：循环化合物和ppar激动剂
公开(公告)号：US20050014833A1
公开(公告)日：2005-01-20
申请号：US10486396
申请日：2002-08-16
申请人： Richard Clark , Fumiyoshi Matsuura , Eita Emori , Masanobu Shinoda , Shunji Kasai , Hideki Yoshitomi , Kazuto Yamazaki , Takashi Inoue , Sadakazu Miyashita , Taro Hihara
发明人： Richard Clark , Fumiyoshi Matsuura , Eita Emori , Masanobu Shinoda , Shunji Kasai , Hideki Yoshitomi , Kazuto Yamazaki , Takashi Inoue , Sadakazu Miyashita , Taro Hihara
IPC分类号： A61P1/00 , A61P1/04 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P19/10 , A61P29/00 , A61P35/00 , A61P37/02 , C07C233/87 , C07C251/60 , C07D213/53 , C07D263/32 , C07D277/56 , C07D307/24 , C07D307/30 , C07D317/32 , C07D339/08 , C07D405/06 , C07D405/12 , C07D407/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07C229/02 , A61K31/195
CPC分类号： C07D213/53 , C07C233/87 , C07C251/60 , C07C2601/02 , C07C2601/14 , C07D263/32 , C07D277/56 , C07D307/24 , C07D307/30 , C07D317/32 , C07D339/08 , C07D405/06 , C07D405/12 , C07D407/12 , C07D413/12 , C07D417/12 , C07D417/14
摘要： The present invention provides a novel compound having an excellent PPAR agonist action. More specifically, it provides a compound represented by the following formula, a salt thereof, an ester thereof or a hydrate of them. Wherein a, b and c are the same as or different from one another and each represents 0 to 4; R1 to R6 are the same as or different from one another and each represents a hydrogen atom, a hydroxyl group, a cyano group, a halogen atom, etc.; A1 and A2 are the same as or different from each other and each represents a single bond, an oxygen atom, etc.; L, M and T each represent a single bond, an alkylene group having one to six carbon atoms, etc.; W represents a carboxyl group; the partial structure represented by the formula: represents a single bond or a double bond; X represents a single bond, an oxygen atom, —NRX1CQ1O—, etc.; Y represents Y1—Y2— (wherein Y1 represents a 5 to 14-membered aromatic ring having one to four substituents, etc.; and Y2 represents a single bond or a 5 to 14-membered aromatic ring); and the ring Z represents a 5 to 14-membered aromatic ring which have one to four substituents selected form the above-mentioned Group A, may have one or more hetero atoms and may be partially saturated.
摘要翻译：本发明提供具有优异的PPAR激动剂作用的新化合物。更具体地，它提供由下式表示的化合物，其盐，其酯或它们的水合物。其中a，b和c彼此相同或不同，各自表示0〜4; R 1〜R 6彼此相同或不同，表示氢原子，羟基，氰基，卤素原子等; A 1和A 2彼此相同或不同，各自表示单键，氧原子等; L，M和T各自表示单键，具有1〜6个碳原子的亚烷基等; W表示羧基; 由式表示的部分结构表示单键或双键; X表示单键，氧原子，-NR X 1 C 10 O等; Y表示Y 1 -Y 2 - （其中Y 1表示具有1〜4个取代基的5〜14元芳环等，Y 2表示单键或5〜14个芳环）; 并且环Z表示具有一至四个选自上述A组的取代基的5至14元芳环，可具有一个或多个杂原子并且可部分饱和。

6. 发明授权

US5962699A Process for decolorizing organic carbonates 失效
标题翻译：脱色有机碳酸酯的方法
公开(公告)号：US5962699A
公开(公告)日：1999-10-05
申请号：US121773
申请日：1998-07-23
申请人： Edward T. Marquis , Robert E. Baldwin
发明人： Edward T. Marquis , Robert E. Baldwin
IPC分类号： C07D317/38 , C07C68/08 , C07C69/96 , C07D317/36 , C07D319/06 , C07D321/06 , C07D317/32
CPC分类号： C07D317/36 , C07C68/08
摘要： A process for decolorizing organic carbonates, for example, cyclic alkylene carbonates, which involves contacting a discolored organic carbonate with hydrogen peroxide, is disclosed.
摘要翻译：公开了一种使有机碳酸酯脱色的方法，例如环状亚烷基碳酸酯，其涉及将变色的有机碳酸酯与过氧化氢接触。

7. 发明授权

US5889037A Pharmacologically active catechol derivatives 失效
标题翻译：药理活性儿茶酚衍生物
公开(公告)号：US5889037A
公开(公告)日：1999-03-30
申请号：US472658
申请日：1995-06-07
申请人： Reijo Backstrom , Erkki Honkanen , Inge-Britt Linden , Erkki Nissinen , Aino Pippuri , Pentti Pohto , Tapio Korkolainen
发明人： Reijo Backstrom , Erkki Honkanen , Inge-Britt Linden , Erkki Nissinen , Aino Pippuri , Pentti Pohto , Tapio Korkolainen
IPC分类号： C07D233/72 , A61K31/00 , A61K31/05 , A61K31/335 , A61K31/357 , A61K31/385 , A61K31/39 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4166 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/426 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/513 , A61K31/535 , A61K31/5377 , A61K31/54 , A61P3/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P29/00 , A61P35/00 , A61P37/06 , A61P39/00 , A61P39/06 , A61P43/00 , C07C20060101 , C07D20060101 , C07D233/78 , C07D233/86 , C07D233/88 , C07D233/96 , C07D239/40 , C07D239/52 , C07D239/54 , C07D239/60 , C07D239/62 , C07D263/38 , C07D263/44 , C07D263/46 , C07D263/48 , C07D265/06 , C07D277/20 , C07D277/32 , C07D277/34 , C07D277/36 , C07D277/40 , C07D277/42 , C07D279/06 , C07D317/32 , C07D317/34 , C07D327/04 , C07D339/06
CPC分类号： C07D239/54 , C07D233/96 , C07D239/40 , C07D239/60 , C07D239/62 , C07D263/46 , C07D277/20
摘要： ##STR1## Compounds of formula (I), wherein R
1 is an electronegative substituent such as nitro, halogeno or cyano group and R
2 is a group selected from (Ia) and (Ib), wherein R is hydrogen, or an alkyl, cycloalkyl, aralkyl or aryl group, wherein X
1 , X
2 , Y and Z are independently oxygen, sulfur of NR, wherein R may be as defined above and pharmaceutically acceptable esters and salts thereof are useful in the prevention or treatment of tissue damage induced by lipid peroxidation.
摘要翻译：（Ⅰ）式（Ⅰ）化合物其中R 1为硝基，卤代或氰基等电负性取代基，R 2为选自（Ia）和（Ib），其中R是氢或烷基，环烷基，芳烷基或芳基，其中X 1，X 2，Y和Z独立地是氧，NR的硫，其中R可以如上所定义，及其药学上可接受的酯和盐可用于预防或治疗由脂质过氧化引起的组织损伤。

8. 发明授权

US5371069A Organoleptic compositions 失效
标题翻译：感官组合物
公开(公告)号：US5371069A
公开(公告)日：1994-12-06
申请号：US870104
申请日：1992-04-17
申请人： Philip A. Christenson , Paul J. Riker , Denise A. Anderson , John M. Yurecko, Jr.
发明人： Philip A. Christenson , Paul J. Riker , Denise A. Anderson , John M. Yurecko, Jr.
IPC分类号： A23G3/34 , A24B15/40 , C07D317/32 , C07D317/54 , C11B9/00 , A51K7/46 , C07D317/26
CPC分类号： C11B9/0076 , A23G3/346 , A24B15/406 , C07D317/32 , C07D317/54 , A23G2220/00
摘要： The present invention provides organoleptic compositions which upon thermolyis, hydrolysis or both, release an odorant molecule. They find utility, for example, in tobacco, in tobacco paper, and as additives to food, beverages or gum. The compositions contain one or more dicarboalkoxy dioxolane derivatives having the following formula: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, --CO.sub.2 R.sup.3 wherein R.sup.3 is --H.sub.3 or lower alkyl, provided that in at least one of R.sup.1 and R.sup.2, R.sup.3 is lower alkyl; wherein Z is a direct bond, or --CH.dbd.C(R.sup.4)--; where R.sup.4 is --H or alkyl group; and Y is ##STR2## where R.sup.5 and R.sup.6 are independently --H, lower alkyl or --OR.sup.7 where R.sup.7 is --H or lower alkyl.
摘要翻译：本发明提供了在热解，水解或两者时释放气味分子的感官组合物。它们可以用于例如烟草，烟草纸以及作为食品，饮料或口香糖的添加剂。所述组合物含有一种或多种具有下式的二烷氧基二氧戊环衍生物：其中R 1和R 2独立地为-CO 2 R 3，其中R 3为-H 3或低级烷基，条件是在R 1和R 2中的至少一个中，R 3较低烷基; 其中Z是直接键，或-CH = C（R4） - ; 其中R4是-H或烷基; 且Y为，其中R 5和R 6独立地为-H，低级烷基或-OR 7，其中R 7为-H或低级烷基。

9. 发明授权

US5164519A Process for the separation of R and S-2,2-R.sub.1,R.sub.2 -1,3-dioxolane-4-carboxylic acid 失效
标题翻译：分离R和S-2,2-R 1，R 2，1,3-二氧戊环-4-羧酸的方法
公开(公告)号：US5164519A
公开(公告)日：1992-11-17
申请号：US801437
申请日：1991-12-02
申请人： Hubertus G. M. Walraven , Paulus B. M. Groen , Everardus J. A. M. Leenderts
发明人： Hubertus G. M. Walraven , Paulus B. M. Groen , Everardus J. A. M. Leenderts
IPC分类号： C07B57/00 , C07D317/32 , C07D317/72
CPC分类号： C07D317/32
摘要： A process is disclosed for preparing a 2,2-R.sub.1, R.sub.2 -1,3-dioxolane-4-carboxylic acid or salt thereof rich in either the R or S enantiomer which process comprisesa) preparing a solution which contains a non-racemic mixture of R and S enantiomer of a carboxylate of the formula ##STR1## and M.sup.n+ ions, wherein R.sub.1 and R.sub.2 are each, independently, H or an unsubstituted or substituted alkyl group, or R.sub.1 and R.sub.2, together with the carbon atom to which they are attached, form an unsubstituted or substituted carbocyclic ring, and M is an alkali metal, an alkaline earth metal, a group IIb metal, boron, or an ammonium, di- or tri-alkanolammonium ion having 2 or 3 carbon atoms or a tetra C.sub.1 -C.sub.16 alkyl ammonium ion, and n is the valency of M;b) reducing the solubility of the M.sup.n+ salt of compound (I); andc) separating the resulting crystals from the mother liquor.

10. 发明授权

US4937379A Carboxylic acid synthesis process 失效
标题翻译：羧酸合成工艺
公开(公告)号：US4937379A
公开(公告)日：1990-06-26
申请号：US79426
申请日：1987-07-30
申请人： Claudio Giordano , Marco Villa
发明人： Claudio Giordano , Marco Villa
IPC分类号： C07B53/00 , B01J31/00 , B01J31/02 , C07B31/00 , C07B61/00 , C07C51/00 , C07C51/09 , C07C57/30 , C07C57/32 , C07C59/64 , C07C67/00 , C07C67/475 , C07C69/612 , C07C69/65 , C07C69/734 , C07D317/32
CPC分类号： C07D317/32 , C07C51/00
摘要： A process is described for preparing alpha-arylalkanoic acids, which comprises preparing and subsequently rearranging ketals of formula ##STR1## (in which Ar, R, R.sub.1, R.sub.2 and R.sub.4 have the meanings given in the description).The ketals of formula II are prepared from the corresponding alpha-hydroxyketals.The rearrangement reaction is conducted under mild conditions.

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