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1. 发明申请

WO2007022947A3 5-RING HETEROAROMATIC COMPOUNDS AND THEIR USE AS BINDING PARTNERS FOR 5-HT5 RECEPTORS 审中-公开
标题翻译： 5环杂芳化合物及其作为约束性合作伙伴5-HT5受体
公开(公告)号：WO2007022947A3
公开(公告)日：2007-05-03
申请号：PCT/EP2006008223
申请日：2006-08-21
申请人： ABBOTT GMBH & CO KG , AMBERG WILHELM , NETZ ASTRID , KLING ANDREAS , OCHSE MICHAEL , LANGE UDO , HAUPT ANDREAS , GARCIA-LADONA FRANCISCO JAVIER , WERNET WOLFGANG
发明人： AMBERG WILHELM , NETZ ASTRID , KLING ANDREAS , OCHSE MICHAEL , LANGE UDO , HAUPT ANDREAS , GARCIA-LADONA FRANCISCO JAVIER , WERNET WOLFGANG
IPC分类号： C07D233/88 , A61K31/13 , A61P25/00 , C07D233/70 , C07D405/04 , C07D409/04
CPC分类号： C07D417/04 , C07D231/38 , C07D233/70 , C07D233/88 , C07D249/14 , C07D405/04 , C07D409/04 , C07D413/04
摘要： The invention relates to 5-ring heteroaromatic compounds of general formula (I), their use for treating and/or preventing diseases, and to medicaments containing them.
摘要翻译：本发明涉及通式（I）中的用途，用于治疗和/或预防疾病，以及含有它们的药物组合物的5-环杂芳族化合物。

2. 发明申请

WO9722621A3 ANTINEOPLASTIC PEPTIDES 审中-公开
标题翻译：抗生素PEPTIDES
公开(公告)号：WO9722621A3
公开(公告)日：1998-02-26
申请号：PCT/EP9605518
申请日：1996-12-11
申请人： BASF AG , AMBERG WILHELM , BARLOZZARI TERESA , BERNARD HARALD , BUSCHMANN ERNST , HAUPT ANDREAS , HEGE HANS GUENTHER , JANSSEN BERND , KLING ANDREAS , LIETZ HELMUT , RITTER KURT , ULLRICH MARTINA , WEYMANN JUERGEN , ZIERKE THOMAS
发明人： AMBERG WILHELM , BARLOZZARI TERESA , BERNARD HARALD , BUSCHMANN ERNST , HAUPT ANDREAS , HEGE HANS-GUENTHER , JANSSEN BERND , KLING ANDREAS , LIETZ HELMUT , RITTER KURT , ULLRICH MARTINA , WEYMANN JUERGEN , ZIERKE THOMAS
IPC分类号： A61K38/00 , A61K31/00 , A61K38/08 , A61P35/00 , A61P35/02 , C07K1/00 , C07K7/06
CPC分类号： A61K38/08
摘要： Novel peptides of the following formula (I): R1R2N-CHX-CO-A-B-D-E-(G)¿s?-K in which R?1, R2¿, A, B, D, E, G, K, X, and s have the meanings stated in the description, and the preparation thereof are described. The novel peptides have an antineoplastic effect.

3. 发明申请

WO2006040178A9 ARYLSULFONYLMETHYL OR ARYLSULFONAMIDE SUBSTITUTED AROMATIC COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MADULATION OF THE DOPAMINE D3 RECEPTOR 审中-公开
标题翻译： ARYLSULFONYLMETHYL或ARYLSULFANAMID替代芳香化合物适用于治疗多巴胺D3受体制剂的病症
公开(公告)号：WO2006040178A9
公开(公告)日：2007-04-19
申请号：PCT/EP2005011091
申请日：2005-10-14
申请人： ABBOTT GMBH & CO KG , DRESCHER KARLA , HAUPT ANDREAS , UNGER LILIANE , TURNER SEAN C , BRAJE WILFRIED , GRANDEL ROLAND , HENRY CHRISTOPHE
发明人： DRESCHER KARLA , HAUPT ANDREAS , UNGER LILIANE , TURNER SEAN C , BRAJE WILFRIED , GRANDEL ROLAND , HENRY CHRISTOPHE
IPC分类号： C07D311/04 , A61K31/13 , A61K31/35 , A61K31/47 , A61P25/16 , C07C211/19 , C07D215/38
CPC分类号： C07C311/21 , C07C311/29 , C07C311/44 , C07C2601/02 , C07C2602/10 , C07D207/10 , C07D211/10 , C07D215/38 , C07D239/84 , C07D263/32 , C07D277/82 , C07D311/04 , C07D413/04 , C07D491/04
摘要： The present invention relates to aromatic compounds of the formula (I), wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical R a and wherein Ar may also carry 1 or 2 radicals R b ; X is N or CH; Y is O, S, -CH=N-, -CH=CH- or -N=CH-; A is CH 2i O or S; E is CR 6 R 7 or NR 3 ; R 1 is C 1 -C 4 -alkyl, C 3 -C 4 -cycloalkyl, C 3 -C4-cycloalkylmethyl, C 3 -C 4 -alkenyl, fluorinated C 1 -C 4 -alkyl, fluorinated C 3 -C 4 -cycloalkyl, fluorinated C 3 -C 4 -cycloalkylmethyl, fluorinated C 3 -C 4 -alkenyl, formyl or C,-C 3 -alkylcarbonyl; R 1a is H, C 2 -C 4 -alkyl, C 3 -C 4 -cycloalkyl, C 3 -C 4 -alkenyl, fluorinated C 1 -C 4 -alkyl, fluorinated C 3 -C 4 -cycloalkyl, or R 1a and R 2 together are (CH 2 ) n with n being 2 or 3, or R 1
摘要翻译：本发明涉及式（I）的芳族化合物，其中Ar是苯基或芳族5-或6-元C-结合杂芳族基团，其中Ar可以带有1个基团R a，并且其中 Ar也可以携带1或2个基团R bb; X为N或CH; Y是O，S，-CH = N-，-CH = CH-或-N = CH-; A为CH 2或O; E是CR 6，R 7或NR 3; R 1是C 1 -C 4 - 烷基，C 3 -C 4亚烷基，C 3 -C 4 - 烷基，C 3 -C 4 - C 3 -C 4环烷基甲基，C 3 -C 4 - 烯基，氟化C 1 -C 4 - 环烷基，C 3 -C 4环烷基甲基，C 3 -C 4 - 氟化C 3 -C 4 - 环烷基，氟化C 3 -C 3 - 亚烷基，C 3 - 氟化C 3 -C 4 - 亚烷基，甲酰基或C 1 -C 3 - 烷基羰基; R 1是H，C 2 -C 4 - 烷基，C 3 -C 4烷基， C 3 -C 4 - 亚烷基，氟化C 1 -C 4 - 亚烷基，C 3 -C 4 - 氟化C 3 -C 4 - 环烷基或R 1a和R 2一起是（CH

4. 发明申请

WO2005118558A3 PYRIMIDINE COMPOUNDS AND USE THEREOF 审中-公开
标题翻译：嘧啶及其用途
公开(公告)号：WO2005118558A3
公开(公告)日：2006-02-09
申请号：PCT/EP2005006000
申请日：2005-06-03
申请人： ABBOTT GMBH & CO KG , GENESTE HERVE , HAUPT ANDREAS , BRAJE WILFRIED , LUBISCH WILFRIED , STEINER GERD , UNGER LILIANE
发明人： GENESTE HERVE , HAUPT ANDREAS , BRAJE WILFRIED , LUBISCH WILFRIED , STEINER GERD , UNGER LILIANE
IPC分类号： C07D401/12 , A61K31/506 , A61P25/00 , A61P25/36 , C07D239/00 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
CPC分类号： C07D417/12 , C07D401/12 , C07D413/12
摘要： The invention relates to pyrimidine compounds of general formula (I), and to the use of these compounds of general formula (I) and of the physiologically compatible acid addition salts of compounds (I) for producing a pharmaceutical agent for treating diseases, which respond to the influence of dopamine D
摘要翻译：本发明涉及通式（I），以及使用通式（I）的这些化合物的嘧啶化合物和所述化合物的生理学可接受的酸加成盐用于制备药物的用于治疗疾病的对多巴胺的影响响应 ð<子

5. 发明申请

WO0118032A2 DOLASTATIN PEPTIDES 审中-公开
公开(公告)号：WO0118032A2
公开(公告)日：2001-03-15
申请号：PCT/US0024658
申请日：2000-09-08
申请人： BASF AG , UNIV ARIZONA , PETIT GEORGE R , SRIRANGAM JAYARAM K , WILLIAMS MICHAEL D , DURKIN KIERAN P M , BARLOZZARI TERESA , KLING ANDREAS , JANSSEN BERND , HAUPT ANDREAS
发明人： PETIT GEORGE R , SRIRANGAM JAYARAM K , WILLIAMS MICHAEL D , DURKIN KIERAN P M , BARLOZZARI TERESA , KLING ANDREAS , JANSSEN BERND , HAUPT ANDREAS
IPC分类号： C07K5/02 , C07K7/02 , C07K5/00
CPC分类号： C07K5/0202 , C07K5/0205 , C07K7/02
摘要： The present invention provides compounds of formula (I) where R1-R5 are each, independently, a hydrogen atom or a normal or branched C1-C6-alkyl group; A is a methionyl, phenylalanyl or phenylglycyl residue; n is 0 or 1; R6 is a hydrogen atom; and R7 is a carbocyclic group, an aromatic group, a C1-C4-alkyl group, a pyridylalkyl group or a heterocyclic group. In another embodiment, R6 is benzyl or -C(O)OR8, where R8 is a C1-C6-alkyl group, and R7 is a heteroaromatic group, such as a 2-thiazolyl group.
摘要翻译：本发明提供式（I）化合物，其中R 1 -R 5各自独立地为氢原子或正
或支链C 1 -C 6烷基; A是甲硫氨酰基，苯丙氨酰或苯基甘氨酰残基; n为0或1; R6是氢原子; 并且R 7是碳环基，芳基，C 1 -C 4 - 烷基，吡啶基烷基或杂环基。在另一个实施方案中，R 6为苄基或-C（O）OR 8，其中R 8为C 1 -C 6烷基，R 7为杂芳族基团，例如2-噻唑基。

6. 发明专利

JP2012211164A Dolastatin 15 derivative 审中-公开
标题翻译： DOLASTATIN 15 DERIVATIVE
公开(公告)号：JP2012211164A
公开(公告)日：2012-11-01
申请号：JP2012138485
申请日：2012-06-20
申请人： Abbott Gmbh & Co Kg , アボットゲーエムベーハーウントカンパニーカーゲー
发明人： JANSSEN BERND , BARLOZZARI TERESA , HAUPT ANDREAS , ZIERKE THOMAS , KLING ANDREAS
IPC分类号： A61K38/00 , C07K7/06 , A61K38/08 , A61P35/00 , C12P19/34
CPC分类号： C07K7/06 , A61K38/00 , C12P19/34
摘要： PROBLEM TO BE SOLVED: To provide synthetic compounds with the biological activity of Dolastatin 15.SOLUTION: The compounds include cell growth inhibitors which are peptides of formula (I), A-B-D-E-F-(G)-(K)-L, and salts thereof, wherein A, B, D, E, F, G and K are α-amino acid residues, and s and r are each, independently, 0 or 1, L is a monovalent radical, such as, for example, an amino group, an N-substituted amino group, a β-hydroxylamino group, a hydrazido group, an alkoxy group, a thioalkoxy group, an aminoxy group, or an oximato group. A method for treating cancer in a mammal, such as a human, includes administering to the mammal an effective amount of the compound of the formula (I) in a pharmaceutically acceptable composition.
摘要翻译：要解决的问题：提供具有Dolastatin 15生物活性的合成化合物。解决方案：该化合物包括作为式（I）的肽的细胞生长抑制剂，ABDEF-（G）

7. 发明专利

JP2004149538A Dolastatin derivative 审中-公开
标题翻译： DOLASTATIN衍生物
公开(公告)号：JP2004149538A
公开(公告)日：2004-05-27
申请号：JP2003384393
申请日：2003-11-13
申请人： Abbott Gmbh & Co Kg , アボットゲーエムベーハーウントカンパニーカーゲー
发明人： HAUPT ANDREAS , EMLING FRANZ , ROMERDAHL CYNTHIA
IPC分类号： A61K38/00 , A61K38/08 , A61P35/00 , A61P35/02 , C07K5/062 , C07K5/08 , C07K5/083 , C07K5/087 , C07K5/10 , C07K5/103 , C07K5/107 , C07K7/06
CPC分类号： C07K7/06 , A61K38/00 , C07K5/101
摘要： PROBLEM TO BE SOLVED: To provide derivatives of dolastatin useful for inhibition of solid tumor or hematological malignant tumor, or other treatments.
SOLUTION: Novel peptide is expressed by formula 1 in which R
1 is a 1-4C alkoxy group, etc., R
2 is H, a 1-4C alkyl group, etc., combined R
1 -N-R
2 expresses a phthalimide group, etc., A is a valyl residue, a isoleucyl residues, etc., B is a N-alkyl residue, etc., D, E, F or G are each a prolyl residue, homoprolyl residue, etc. X is H, an alkyl residue, etc., t, u, v or w are each independently 0 or 1, K expresses a hydroxyl part, an alkoxy part, etc.
COPYRIGHT: (C)2004,JPO
摘要翻译：待解决的问题：提供可用于抑制实体瘤或血液恶性肿瘤或其他治疗的多拉司他汀衍生物。解决方案：新型肽由式1表示，其中R 1 SP 1是1-4C烷氧基等，R 2是H，1-4C 烷基等，组合的R“SP”表示邻苯二甲酰亚胺基等，A是缬氨酰残基，异亮氨酰残基等，B是 N-烷基残基等，D，E，F或G各自为脯氨酰残基，同质残基等。X为H，烷基残基等，t，u，v或w各自独立地为0或1 ，K表示羟基部分，烷氧基部分等。版权所有（C）2004，JPO

8. 发明专利

JP2009137967A Dolastatine 15 derivative 有权
标题翻译： DOLASTATINE 15衍生物
公开(公告)号：JP2009137967A
公开(公告)日：2009-06-25
申请号：JP2008315263
申请日：2008-12-11
申请人： Abbott Gmbh & Co Kg , アボットゲーエムベーハーウントカンパニーカーゲー
发明人： JANSSEN BERND , BARLOZZARI TERESA , HAUPT ANDREAS , ZIERKE THOMAS , KLING ANDREAS
IPC分类号： A61K38/00 , C07K7/06 , A61K38/08 , A61P35/00 , A61P35/02 , C12P19/34
CPC分类号： C07K7/06 , A61K38/00 , C12P19/34
摘要： PROBLEM TO BE SOLVED: To provide a dolastatine 15 derivative that has sufficient water solubility and can economically be produced. SOLUTION: A cell growth inhibitor that is a peptide represented by formula (I): A-B-D-E-F-(G) r -(K) s -L, and its salt are provided. Therein, A, B, D, E, F, G and K are each an α-amino acid residue; (s) and (r) are each independently 0 or 1; L is a monovalent radical such as an amino group, an N-substituted amino group, a β-hydroxylamino group, a hydrazide group, an alkoxy group, a thioalkoxy group, an aminoxy group or an oximato group. In addition, provided is a method for treating the cancer of a mammal such as human characterized by administering an active amount of the compound of formula (I) as a medically acceptable composition into the mammal. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：待解决的问题：提供具有足够的水溶性并且可以经济地生产的多拉曲坦15衍生物。解决方案：作为由式（I）表示的肽的细胞生长抑制剂：ABDEF-（G） - （K） -L，及其提供盐。其中，A，B，D，E，F，G和K各自为α-氨基酸残基; （s）和（r）各自独立地为0或1; L是一价基团，例如氨基，N-取代氨基，β-羟基氨基，酰肼基，烷氧基，硫代烷氧基，氨氧基或肟基。此外，提供了治疗哺乳动物（例如人）癌症的方法，其特征在于向哺乳动物施用活性量的式（I）化合物作为医学上可接受的组合物。版权所有（C）2009，JPO＆INPIT

9. 发明专利

JP2012006946A Aminoethylaromatic compounds suitable for treating disorders that respond to modulation of the dopamine d3 receptor 审中-公开
标题翻译：适用于治疗多巴胺D3受体调节障碍的氨基甲醛化合物
公开(公告)号：JP2012006946A
公开(公告)日：2012-01-12
申请号：JP2011168735
申请日：2011-08-01
申请人： Abbott Gmbh & Co Kg , アボットゲーエムベーハーウントカンパニーカーゲー
发明人： DRESCHER KARLA , HAUPT ANDREAS , UNGER LILIANE , TURNER SEAN C , BRAJE WILFRIED , GRANDEL ROLAND
IPC分类号： C07C311/21 , A61K31/18 , A61K31/40 , A61K31/44 , A61P13/12 , A61P25/00 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/30 , A61P25/36 , A61P43/00 , C07C311/29 , C07C317/14 , C07C317/22 , C07D207/09 , C07D213/76
CPC分类号： C07D213/76 , C07C311/21 , C07C311/29 , C07C2601/02 , C07D207/09
摘要： PROBLEM TO BE SOLVED: To provide compounds which act as a dopamine D3 receptor ligand with more high selectivity.SOLUTION: The compounds are aromatic compounds of formula (I) and physiologically acceptable acid addition salts thereof. In the formula, Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical; X is N or CH; E is CRRor NR; Ris C-C-alkyl, C-C-cycloalkyl or the like; Ris H, C-C-alkyl or the like, or Rand Rtogether are (CH)or Rand Rtogether are (CH)wherein n is 2-4; Rand Reach independently are H, C-C-alkyl or fluorinated C-C-alkyl, or Rand Rtogether are (CH)wherein m is 1-5; and Rand Reach independently H, fluorine, C-C-alkyl or the like.
摘要翻译：待解决的问题：提供具有更高选择性的充当多巴胺D3受体配体的化合物。化合物是式（I）的芳族化合物及其生理上可接受的酸加成盐。在该式中，Ar是苯基或芳族5-或6-元C-结合的杂芳族基; X为N或CH; E是CR 6 R 7 或NR 3 ; R 1 是C 1 -C 4 - 烷基，C 3 -C 4 - 环烷基等; R 1a 是H，C 1 -C 4 或者R 1a 和R 2 一起是（CH 2 ）或者 1a 和R 2a 一起是（CH 2 ） n 其中n为2-4; R 2 和R 2a 各自独立地为H，C 1 -C 或者，或者是（C 1 -C 4）烷基或氟化的C 1 -C 6 POS =“POST”> 4 R 2a 和R 2 一起是（CH 2 ） m 其中m为1-5; 和R 6 和R 7 各自独立为H，氟，C 1 -C 4 - 烷基等。版权所有（C）2012，JPO＆INPIT

10. 发明专利

JP2009137968A Dolastatine 15 derivative 有权
标题翻译： DOLASTATINE 15衍生物
公开(公告)号：JP2009137968A
公开(公告)日：2009-06-25
申请号：JP2008315269
申请日：2008-12-11
申请人： Abbott Gmbh & Co Kg , アボットゲーエムベーハーウントカンパニーカーゲー
发明人： JANSSEN BERND , BARLOZZARI TERESA , HAUPT ANDREAS , ZIERKE THOMAS , KLING ANDREAS
IPC分类号： A61K38/00 , C07K14/435 , A61K38/08 , A61P35/00 , C07K7/06 , C12P19/34
CPC分类号： C07K7/06 , A61K38/00 , C12P19/34
摘要： PROBLEM TO BE SOLVED: To provide a synthetic compound that has sufficient water solubility, can efficiently and economically be produced, and has the same biological activity as those of dolastatine 15. SOLUTION: A cell growth inhibitor that is a peptide represented by formula (I): A-B-D-E-F-(G) r -(K) s -L, and its salt are provided. Therein, A, B, D, E, F, G and K are each an α-amino acid residue; (s) and (r) are each independently 0 or 1; L is a monovalent radical such as an amino group, an N-substituted amino group, a β-hydroxylamino group, a hydrazide group, an alkoxy group, a thioalkoxy group, an aminoxy group or an oximato group. An active amount of the compound of formula (I), the inhibitor, is administered into mammals as a pharmaceutically acceptable composition. The inhibitor is effective for a method for treating, for example, human cancers. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：要解决的问题：提供具有足够的水溶性，可以有效和经济地生产并具有与多拉斯他汀15相同的生物活性的合成化合物。解决方案：一种细胞生长抑制剂，其为由式（I）表示的肽：ABDEF-（G） - （K） -L及其盐。其中A，B，D，E，F，G和K各自为α-氨基酸残基; （s）和（r）各自独立地为0或1; L是一价基团，例如氨基，N-取代氨基，β-羟基氨基，酰肼基，烷氧基，硫代烷氧基，氨氧基或肟基。将活性量的式（I）化合物，抑制剂，作为药学上可接受的组合物施用于哺乳动物。抑制剂对于治疗例如人类癌症的方法是有效的。版权所有（C）2009，JPO＆INPIT

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