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1. 发明授权

US5731289A Double-chain hemoregulatory peptides 失效
标题翻译：双链调节肽
公开(公告)号：US5731289A
公开(公告)日：1998-03-24
申请号：US648016
申请日：1996-08-08
申请人： Kjell Undheim , Meinolf Lange , Jessie Sandosham
发明人： Kjell Undheim , Meinolf Lange , Jessie Sandosham
IPC分类号： C07D241/18 , A61K38/00 , A61P7/06 , A61P31/12 , A61P35/00 , A61P43/00 , C07K7/02 , C07K7/06 , A61K38/04 , A61K38/08 , C07K7/00
CPC分类号： C07K7/06 , C07K7/067 , A61K38/00
摘要： The present invention relates to peptide compounds comprising two single-chain hemoregulatory, for example haemopoiesis-inhibiting, peptides linked by a bridging group terminally attached to the C.alpha. atoms of non-terminal amino acids wherein at least one of the C.alpha. atoms is independently substituted by an alkyl group. The bridged dipeptide compounds have a stimulating activity on cell division, especially in myelopoietic and bone marrow cells.
摘要翻译： PCT No.PCT / GB94 / 02621 Sec。 371日期：1996年8月8日 102（e）日期1996年8月8日PCT 1994年11月30日PCT PCT。公开号WO95 / 15336 日期：1995年6月8日本发明涉及包含两个单链调控性的肽化合物，例如由造血作用抑制的肽，其通过末端连接至非末端氨基酸的Cα原子的桥连基团连接，其中至少一个 Cα原子独立地被烷基取代。桥联二肽化合物对细胞分裂具有刺激活性，特别是在骨髓细胞和骨髓细胞中。

2. 发明授权

US5610141A Double chain peptide compounds having hemoregulatory activity 失效
标题翻译：具有调节活性的双链肽化合物
公开(公告)号：US5610141A
公开(公告)日：1997-03-11
申请号：US362411
申请日：1994-11-30
申请人： Kjell Undheim , Magne Solbakken , Erik Agner , Peter Kremminger , Meinolf Lange
发明人： Kjell Undheim , Magne Solbakken , Erik Agner , Peter Kremminger , Meinolf Lange
IPC分类号： C07D241/18 , A61K38/00 , A61P7/00 , A61P43/00 , C07D241/08 , C07D317/30 , C07K7/06 , C07K14/47
CPC分类号： C07D241/08 , C07D317/30 , C07K14/4722 , C07K7/067 , A61K38/00
摘要： Dipeptide compounds are disclosed, the two peptide chains being joined together at a C.alpha.-atom of a non-terminal amino acid by a divalent bridging group --A--. The C.alpha.-atoms joined to group --A-- are located in equivalent positions in each peptide and each lack their native .alpha.-side chain. The bridged dipeptide compounds disclosed have a stimulating activity on cell division, especially for myelopoietic and bone marrow cells.
摘要翻译： PCT No.PCT / GB93 / 01171 Sec。 371日期1994年11月30日 102（e）1994年11月30日日期PCT提交1993年6月2日PCT公布。出版物WO93 / 24523 日期1993年12月9日公开了二肽化合物，两条肽链通过二价桥连基团-A在非末端氨基酸的Cα原子原子连接在一起。连接到组-A的Cα-原子在每个肽中位于相同的位置，并且各自缺乏其天然的α侧链。所公开的桥连二肽化合物对细胞分裂具有刺激活性，特别是对于骨髓细胞和骨髓细胞。

3. 发明授权

US5629293A Single chain peptide compounds having hemoregulatory activity 失效
标题翻译：单链肽化合物具有调节活性
公开(公告)号：US5629293A
公开(公告)日：1997-05-13
申请号：US343602
申请日：1994-11-30
申请人： Kjell Undheim , Peter Kremminger , Michael Hartmann
发明人： Kjell Undheim , Peter Kremminger , Michael Hartmann
IPC分类号： C07D241/18 , A61K38/00 , A61P7/00 , A61P43/00 , C07C271/22 , C07D241/08 , C07D261/08 , C07D307/54 , C07D317/28 , C07K7/06 , A61K38/08 , C07K1/02
CPC分类号： C07C271/22 , C07D241/08 , C07D261/08 , C07D307/54 , C07D317/28 , C07K7/067 , A61K38/00 , C07C2103/18
摘要： There is disclosed single chain peptide compounds, substituted at a C.alpha.-atom of a non-terminal amino acid by a group--A which is defined in claim 1. The native .alpha.-side chain of the C.alpha. atom bonded group to group --A absent. The peptide derivatives according to the invention are useful for inhibiting cell proliferation, especially myelopoietic and bone marrow cells.
摘要翻译： PCT No.PCT / GB93 / 01172 Sec。 371日期1994年11月30日 102（e）1994年11月30日日期PCT提交1993年6月2日PCT公布。第WO93 / 24524B PCT公开日期1993年12月9日公开了通过权利要求1所定义的基团A在非α-氨基酸的Cα原子取代的单链肽化合物.Cα原子的天然α侧链绑定组到组-A缺席。根据本发明的肽衍生物可用于抑制细胞增殖，特别是骨髓细胞和骨髓细胞。

4. 发明授权

US4423047A Pyrimidine-2-sulphides and their S-oxides for use in medicine and methods of use therefor, pharmaceutical compositions containing them, processes for their preparation and per se novel sulphides and S-oxides 失效
标题翻译：嘧啶-2-硫化物及其用于医药及其使用方法的S-氧化物，含有它们的药物组合物，其制备方法和本身的新型硫化物和S-氧化物
公开(公告)号：US4423047A
公开(公告)日：1983-12-27
申请号：US223760
申请日：1981-01-09
申请人： Tore Benneche , Mikkel J. Gacek , Kjell Undheim
发明人： Tore Benneche , Mikkel J. Gacek , Kjell Undheim
IPC分类号： A61K31/505 , A61K31/675 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61P17/00 , A61P35/00 , A61P43/00 , C07C233/07 , C07D239/38 , C07D239/40 , C07D403/12 , C07D405/12 , C07D409/12 , C07F9/6512 , C07H17/02
CPC分类号： C07D239/40 , C07C233/07 , C07D239/38 , C07F9/65122 , C07H17/02 , Y10S514/863 , Y10S514/885 , Y10S514/908
摘要： Compounds of the formula ##STR1## (wherein X represents a halogen atom; n is 0, 1 or 2; R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen atom or a carboxyl, esterified carboxyl, amido or mono- or di-C.sub.1-4 alkylamido group or a C.sub.1-4 alkyl group which may if desired carry a carboxyl or esterified carboxyl group; and R.sup.3 represents a C.sub.1-32 saturated or unsaturated, straight or branched, cyclic or acyclic aliphatic group or an araliphatic or heterocyclic substituted aliphatic group, a heterocyclic group or an aryl group which groups may if desired carry one or more substituents selected from halogen atoms and oxo, nitro, hydroxy, etherified hydroxy, esterified hydroxy, primary, secondary or tertiary amino, acylamino etherified mercapto or S.dbd.O or --SO.sub.2 derivatives thereof and esterified phosphonic acid groups) and, where an acidic or basic group is present, physiologically compatible salts thereof have been found to be of use in combating abnormal cell proliferation. The compounds are prepared inter alia by oxidation of the corresponding sulfide, displacement of a leaving atom or group from the 2-position of the pyrimidine by reaction with a sulfinic acid or by ring closure of the pyrimidine ring.
摘要翻译：式（I）的化合物（其中X表示卤素原子; n为0,1或2; R 1和R 2可相同或不同，表示氢原子或羧基，酯化的羧基，酰氨基或单或二-C 1-4烷基酰氨基或C 1-4烷基，如果需要，可带有羧基或酯化羧基; R3表示C1-32饱和或不饱和的直链或支链，环状或无环脂族基团或硝基，羟基，醚化的羟基，酯化的羟基，伯，仲或叔氨基，酰基氨基，芳基，芳基，芳基或杂环取代的脂族基，杂环基或芳基，醚化巯基或S = O或-SO 2衍生物和酯化膦酸基团），并且其中存在酸性或碱性基团时，已发现其生理上相容的盐可用于对抗异常细胞增殖。化合物特别是通过氧化相应的硫化物，通过与亚磺酸反应或通过环嘧啶环的闭合将离去的原子或基团从嘧啶的2-位置换出来。

5. 发明申请

US20100035832A1 Macrolides 审中-公开
标题翻译：大环内酯类
公开(公告)号：US20100035832A1
公开(公告)日：2010-02-11
申请号：US11813682
申请日：2006-01-12
申请人： Audun Heggelund , Kjell Undheim
发明人： Audun Heggelund , Kjell Undheim
IPC分类号： A61K31/7048 , C07H17/08 , A61P31/00
CPC分类号： C07H17/08
摘要： This invention relates to a novel class of antibiotic agents, more specifically to macrolides comprising an oxazolidinone structure, their preparation, pharmaceutical compositions containing them, their use and methods of treatment using them.
摘要翻译：本发明涉及一类新型抗生素，更具体地涉及包含恶唑烷酮结构的大环内酯类，其制备方法，含有它们的药物组合物，它们的用途和使用它们的治疗方法。

6. 发明授权

US07608596B2 10-substituted macrolide antibiotics 失效
标题翻译： 10-取代的大环内酯类抗生素
公开(公告)号：US07608596B2
公开(公告)日：2009-10-27
申请号：US10539759
申请日：2003-12-22
申请人： Kjell Undheim , Solvi Gunnes
发明人： Kjell Undheim , Solvi Gunnes
IPC分类号： A61K31/70 , C07H17/08
CPC分类号： C07H17/08
摘要： Disclosed herein are 10-desmethyl, 10 substituted-macrolides, their preparation, pharmaceutical compositions containing them, their use and methods of treatment using them. The 10-desmethyl macrolides are particularly useful as antibiotics.
摘要翻译：本文公开了10-去甲基，10个取代大环内酯类，其制备方法，含有它们的药物组合物，它们的用途和使用它们的治疗方法。 10-脱甲基大环内酯类作为抗生素特别有用。

7. 发明授权

US5589595A Process for tetraazacycloalkane preparation 失效
标题翻译：四氮杂环烷烃制备方法
公开(公告)号：US5589595A
公开(公告)日：1996-12-31
申请号：US483189
申请日：1995-06-07
申请人： Rolf W. Sandnes , Kjell Undheim , Michel Gacek , Janis Vasilevskis
发明人： Rolf W. Sandnes , Kjell Undheim , Michel Gacek , Janis Vasilevskis
IPC分类号： C07D487/14 , C07D257/02 , A61K49/00
CPC分类号： C07D257/02
摘要： The present invention provides a synthetic route for tetraazacycloalkane preparation which facilitates heteropoly-N-alkylation of the macrocyclic product, and is thereby beneficial for the production of chelating agents and chelates useful in diagnostic imaging. The process involves (i) reacting a tetraazaalkane with a bridging agent to couple four amine nitrogens of said tetraazaalkane to a bridging moiety to yield a fused tricyclic intermediate, (ii) reacting said intermediate to introduce an alkylene bridge between the secondary amine nitrogens in the outer rings of the fused tricyclic intermediate, optionally by decoupling an alkanediylidene bridging moiety from the tertiary amine nitrogens at the ring fusion sites of the fused tricyclic intermediate, and (iii) where necessary, decoupling said bridging moiety to yield a macrocyclic tetraazacycloalkane.
摘要翻译：本发明提供了促进大环杂多杂-N-烷基化的四氮杂环烷烃制备的合成路线，从而有利于生产可用于诊断成像的螯合剂和螯合物。该方法包括（i）使四氮杂链烷烃与桥连剂反应以将四氮杂烷烃的四个胺氮偶联到桥连部分以产生稠合的三环中间体，（ii）使所述中间体在所述仲胺氮中引入亚烷基桥，稠合三环中间体的外环，任选地通过在稠合三环中间体的环融合位点处将烷二亚烷基桥连部分与叔胺氮脱去，和（iii）必要时将所述桥连部分解偶联以产生大环四氮杂环烷烃。

8. 发明授权

US08304531B2 Process for the preparation of an (RP)-8-substituted cAMPS 失效
标题翻译：制备（RP）-8取代的cAMPS的方法
公开(公告)号：US08304531B2
公开(公告)日：2012-11-06
申请号：US12441317
申请日：2007-09-17
申请人： Kjell Undheim , Mioara Andrei
发明人： Kjell Undheim , Mioara Andrei
IPC分类号： C07H21/00
CPC分类号： C07H19/20
摘要： This invention relates to a process for the preparation of an (Rp)-8-substituted adenosine-3′,5′-cyclic phosphorothioic acid, or a salt or ester thereof, which comprises P-amidating 8-bromoadenosine-3′,5′-cyclic phosphoric acid, and reacting the P-amidate with a base and with carbon disulphide to yield (Rp)-8-bromoadenosine-3′,5′-cyclic phosphorothioic acid or a salt or ester thereof.
摘要翻译：本发明涉及制备（Rp）-8-取代腺苷-3'，5'-环硫代磷酸或其盐或酯的方法，其包括将8-溴腺苷-3'，5 并且使β-氨基甲酸酯与碱和二硫化碳反应，得到（Rp）-8-溴腺苷-3'，5'-环硫代磷酸或其盐或酯。

9. 发明授权

US4399140A 5-Halo-pyrimidin-2-ones, the salts thereof 失效
标题翻译： 5-卤代 - 嘧啶-2-酮，其盐
公开(公告)号：US4399140A
公开(公告)日：1983-08-16
申请号：US222959
申请日：1981-01-06
申请人： Mikkel Gacek , Kjell Undheim
发明人： Mikkel Gacek , Kjell Undheim
IPC分类号： C07D409/06 , A61K31/505 , A61K31/55 , A61P17/00 , A61P35/00 , A61P43/00 , C07D239/30 , C07D243/08 , C07D277/42 , C07D277/56 , C07D333/16 , C07D333/28 , C07D401/06 , C07D403/06 , C07D405/06 , C07D413/06 , C07D417/06
CPC分类号： C07D239/30 , C07D243/08 , C07D277/42 , C07D277/56 , C07D333/16 , C07D333/28
摘要： Compounds of the formula: ##STR1## wherein X represents a halogen atom;R.sup.1 and R.sup.2, which may be same or different, each represents a hydrogen atom, or a C.sub.1-4 alkyl group;Het represents a C-attached 3-9 membered, saturated, unsaturated or aromatic heterocyclic ring containing one or more hetero atoms selected from O, N and S and optionally carrying a fused ring and/or optionally substituted by one or more substituents selected from halogen atoms and hydroxy, C.sub.1-4 alkoxy, amino, acylamino, nitro, oxo, C.sub.1-4 alkyl groups and monocyclic carbocyclic and heterocyclic aryl groups having 5 to 8 ring members; such a heterocyclic ring being saturated and having only a single heteroatom when there are 3 or 4 ring members; andalk represents a C.sub.1-4 saturated or unsaturated, straight or branched chain, divalent aliphatic hydrocarbyl group optionally substituted by one or more groups selected from carbocyclic aryl groups and heterocyclic groups as defined for Het above, and the salts thereof have been found to possess metaphase arresting ability which by virtue of its reversibility is of use in combating abnormal cell proliferation. Thus a knowledge of the cell division cycles of the normal and abnormal cells enables a cytotoxic drug to be administered while the abnormal cells are in a phase susceptible to attack and while the normal cells are in a non-susceptible phase.The compounds of the invention are prepared by alkylation, ring closure of the pyrimidine ring, halogenation or ring closure of the heterocyclic ring Het.
摘要翻译：下式的化合物：其中X表示卤素原子; R 1和R 2可以相同或不同，各自表示氢原子或C 1-4烷基; Het表示含有一个或多个选自O，N和S的杂原子的C连接的3-9元饱和，不饱和或芳族杂环，并且任选地带有稠环和/或任选被一个或多个选自以下的取代基取代：羟基，C 1-4烷氧基，氨基，酰氨基，硝基，氧代，C 1-4烷基和具有5-8个环成员的单环碳环和杂环芳基; 当存在3或4个环成员时，这样的杂环是饱和的并且仅具有单个杂原子; 并且alk表示任选被一个或多个选自上述Het定义的碳环芳基和杂环基团的基团取代的C 1-4饱和或不饱和的直链或支链二价脂族烃基，并且其盐被发现具有由于其可逆性，中期阻滞能力可用于对抗异常细胞增殖。因此，正常和异常细胞的细胞分裂周期的知识使得能够施用细胞毒性药物，同时异常细胞处于易受攻击的阶段，而正常细胞处于非易感相。本发明的化合物通过烷基化，嘧啶环的闭环，杂环Het的卤化或闭环来制备。

10. 发明授权

US4395406A 5-Halopyrimid-2-ones 失效
标题翻译： 5-卤代嘧啶-2-酮
公开(公告)号：US4395406A
公开(公告)日：1983-07-26
申请号：US166600
申请日：1980-07-07
申请人： Mikkel J. Gacek , Reidar Oftebro , Soren Laland , Kjell Undheim
发明人： Mikkel J. Gacek , Reidar Oftebro , Soren Laland , Kjell Undheim
IPC分类号： C07D215/08 , A61K31/505 , A61K31/70 , A61P35/00 , A61P35/02 , C07D239/36 , C07D239/56 , C07H19/06
CPC分类号： C07D239/36 , C07D239/56 , C07H19/06 , Y10S514/908
摘要： Novel derivatives of pyrimid-2-one having interesting pharmacological properties are described. The compounds of the invention have been found to be of use in the control of, and in particular in the inhibition of the metaphase of malignant tumours and leukaemias. Processes for the preparation of the novel compounds and pharmaceutical compositions containing them are also described.
摘要翻译：描述了具有有趣的药理学性质的嘧啶-2-酮的新型衍生物。已经发现本发明的化合物可用于控制，特别是抑制恶性肿瘤和白血病的中期。还描述了制备新化合物和含有它们的药物组合物的方法。

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