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1. 发明申请

WO1997003072A1 NEW OXAZOLIDINONE DERIVATIVES, PROCESS FOR PREPARING THE SAME AND MEDICAMENTS THAT CONTAIN THESE COMPOUNDS 审中-公开
标题翻译：新的恶唑烷酮衍生物，方法为生产和药物含有它们的
公开(公告)号：WO1997003072A1
公开(公告)日：1997-01-30
申请号：PCT/EP1996002939
申请日：1996-07-04
申请人： BOEHRINGER MANNHEIM GMBH , TSAKLAKIDIS, Christos , SCHÄFER, Wolfgang , DÖRGE, Liesel , FRIEBE, Walter-Gunar , ESSWEIN, Angelika
发明人： BOEHRINGER MANNHEIM GMBH
IPC分类号： C07D413/14
CPC分类号： C07D413/14
摘要： New oxazolidinone derivatives are disclosed, as well as a process for preparing the same and medicaments that contain these substances. The disclosed compounds have general formula (I), in which X, Y and Q independently represent nitrogen or CH; W stands for hydrogen or NR R ; Z stands for nitrogen, CH or C-OH; A, E and G independently represent the valence dash or an alkylene chain -(CH2)n-; B stands for a valence dash and, when Z equals N, it may also stand for a carbonyl group; D stands for a side chain having the form -(CHR )m-COO- or =CR -COO-; n equals 1 to 5; m equals 0.1; R , R independently represent hydrogen, lower alkyl or aryl, or form together a carbocyclic five- or six-membered ring; R stands for hydrogen or a group -OR or -NR R ; R stands for hydrogen or a group -OR ; R stands for hydrogen, lower alkyl, aryl or arylalkyl; R stands for hydrogen, lower alkyl or arylalkyl; R stands for hydrogen, lower alkyl, arylalkyl, acyl, alkylsulphonyl or arylsulphonyl.
摘要翻译：本发明涉及新的恶唑烷酮衍生物，其制备方法和含有这些物质的药物组合物。本发明涉及通式（I）中的X，Y和Q彼此独立地表示氮或CH的化合物; W是氢或NR <0> - [R <00>基; Z是氮，CH或C-OH; A，E和G彼此独立地化合价破折号或亚烷基链的 - 平均（CH 2）N-; 乙价破折号和用于Z为等于N的情况下，也意味着羰基; D是形式的侧链 - （CHR <3>）M-COO-或= CR <3>为-COO-; N = 1-5烷基; m为= 0.1; [R <1>，R <2>独立地是氢，低级烷基或芳基，或一起形成碳环五元或六元环; [R <3>是氢或基团-OR <5>或-NR <6> - [R <7>基; [R <4>是氢或基团-OR <5>基; [R <5>是氢，低级烷基，芳基或芳基烷基; [R <6>是氢，低级烷基或芳基烷基; ，R <7>是氢，低级烷基，芳烷基，酰基，烷基磺酰基或芳基磺酰。

3. 发明申请

WO1996024586A1 NEW DERIVATIVES OF PYRIDINE OR PYRIDAZINE, PROCESS FOR PRODUCTION THEREOF AND MEDICAMENTS CONTAINING THESE COMPOUNDS 审中-公开
标题翻译：新的吡啶或哒嗪衍生物，其制造方法相同，含药物
公开(公告)号：WO1996024586A1
公开(公告)日：1996-08-15
申请号：PCT/EP1996000523
申请日：1996-02-08
申请人： BOEHRINGER MANNHEIM GMBH , TSAKLAKIDIS, Christos , MERTENS, Alfred , ZIMMERMANN, Gerd , SCHÄFER, Wolfgang , DÖRGE, Liesel
发明人： BOEHRINGER MANNHEIM GMBH
IPC分类号： C07D213/74
CPC分类号： C07D213/74 , C07D237/20 , C07D401/12 , Y02P20/55
摘要： Compounds of formula (I), in which R stands for hydrogen, lower alkyl, lower alkenyl, cycloalkyl, cycloalkenyl, a possibly substituted mono- or bi-cyclic aryl, a possibly substituted hetaryl, a possibly substituted arylalkyl or one of the groups -OR , -NR R , W stands for nitrogen or CR , X, Y, Z independently of each other stand for nitrogen or the group CH, and where W stands for the group CR and X stands for the group CH, Y cannot be the group CH, A stands for oxygen, =NR or =N-P, n represents 0-5, P stands for a protective group for amines such as acetyl, tert.-butyloxycarbonyl or benzyloxycarbonyl, R stands for hydrogen, lower alkyl or aryl alkyl, R , R independently of each other stand for hydrogen or lower alkyl, or form a five- or six-membered heterocyclic ring together with the nitrogen atom to which they are linked, R stands for hydrogen or a group OR . The invention also relates to a process for the production of these compounds, and medicaments containing them for the treatment of diseases which are attributable to thromboembolic conditions.
摘要翻译：式（I），其中R <1>是氢，低级烷基，低级烯基，环烷基，环烯基的化合物，任选取代的单环或双环芳基，任选取代的杂芳基，任选取代的芳基烷基或以下基团之一-OR < 2>，-NR <3> [R <4>中，W为氮或CR <5>表示，X，Y，Z独立地为氮或CH的基团，并且在W是基团CR的情况下<5> 且X是CH，Y不是CH基团可以是，一个是氧，= <2>或= NP表示NR，n为0-5，P为胺，例如乙酰基，叔丁氧羰基或苄保护基，R <2>是氢，低级烷基或芳烷基，R <3>，R <4>独立地是氢，或低级烷基，或一起与氮原子到它们所连接形成5-至6元杂环环形式中，R <5>是氢或基团或<2>，美去它们的制备方法和含有这些化合物为那些由于血栓栓塞事件的疾病的治疗药物组合物。

4. 发明申请

WO1997019909A1 AMINO ALCOHOL DERIVATIVES, METHODS OF PRODUCING SAID DERIVATIVES AND MEDICAMENTS CONTAINING THEM 审中-公开
标题翻译： AMINOALKOHOLDERIVATIVE，其制造方法相同，含药物
公开(公告)号：WO1997019909A1
公开(公告)日：1997-06-05
申请号：PCT/EP1996005212
申请日：1996-11-26
申请人： BOEHRINGER MANNHEIM GMBH , ESSWEIN, Angelika , KLING, Lothar , LESER, Ulrike , FRIEBE, Walter-Gunar
发明人： BOEHRINGER MANNHEIM GMBH
IPC分类号： C07C233/18
CPC分类号： C07C233/18 , C07C233/20
摘要： The disclosure relates to compounds of formula (I), in which R stands for hydrogen or methyl, R stands for lower straight-chain or branched alkyl with 1-10 carbon atoms, R stands for hydrogen or lower alkyl, n is 0-12, and R stands for alkyl, alkenyl or alkinyl with 6-24 carbon atoms; and to methods of producing said compounds and medicaments containing said compounds and intended for use in the treatment of osteoporosis.
摘要翻译：式（I）的化合物，其中R <1> =氢或甲基，R <2> =低级的直链或碳原子数为1〜10，R支链烷基<3> =氢或低级烷基，n = 0-12，从6到24个碳原子具有R- <4> =烷基，烯基或炔基，它们的制备方法和含有这些化合物的，用于治疗骨质疏松症的药物组合物。

5. 发明申请

WO1995000522A1 PHOSPHOSUCCINIC ACID DERIVATIVES AND THEIR USE AS MEDICAMENTS 审中-公开
标题翻译： PHOSPHONOBERNSTEINSÄUREDERIVATE及其作为药物
公开(公告)号：WO1995000522A1
公开(公告)日：1995-01-05
申请号：PCT/EP1994001980
申请日：1994-06-17
申请人： BOEHRINGER MANNHEIM GMBH , TSAKLAKIDIS, Christos , ESSWEIN, Angelika , ZIMMERMANN, Gerd , BAUSS, Frieder
发明人： BOEHRINGER MANNHEIM GMBH
IPC分类号： C07F09/38
CPC分类号： C07F9/655345 , C07F9/3808 , C07F9/3826 , C07F9/383 , C07F9/3882 , C07F9/572 , C07F9/59 , C07F9/6533 , C07F9/65515 , C07F9/6552
摘要： Compounds have formula (I), in which R , R may represent independently from each other hydrogen, lower alkyl, cycloalkyl or arylmethyl; R , R may represent independently from each other hydrogen, lower alkyl, or one of the groups -OR or -NR R , or they may form together with the atoms to which they are bound a five- to seven-membered carbocyclic ring or an heterocyclic ring containing one or two heteroatoms; R stands for lower alkenyl, cycloalkyl, cycloalkenyl, monocyclic arylalkyl, bicyclic aryl, biaryl or a group having formulae (a): R -X-alk- or (b), or forms together with R and the carbon atom to which it is bound a possibly substituted five- to seven-membered carbocyclic or heterocyclic ring; R stands for hydrogen, lower alkyl or arylmethyl; R , R represent independently from each other hydrogen or lower alkyl or form together with the nitrogen atom to which they are bound a five- or six-membered heterocyclic ring; R stands for hydrogen, lower alkyl, lower alkenyl, cycloalkyl, cycloalkenyl, mono- or bicyclic aryl, biaryl; R stands for a group having formula (a); X stands for a valence dash, oxygen or sulphur; Q stands for oxygen, sulphur or nitrogen; alk stands for a valence dash, a methylene chain, a saturated or unsaturated alkylene chain with 2-6 carbon atoms; n equals 0-3, m equals 0-2 and p equals 0-5. Also disclosed is a process for preparing said compounds and medicaments containing the same used for treating calcium metabolism disturbances.
摘要翻译：式（I）的化合物，其中R <1>，R <2>可以是氢，低级烷基，环烷基或彼此独立地芳甲基; [R <3>，R <4>各自独立地是氢，低级烷基，或以下基团之一-OR <6>，或-NR可以是<7> - [R <8>，或连同原子它们所连接可形成五至七元碳环或含有一到两个杂原子的杂环; [R <5>低级链烯基，环烷基，环烯基，单环芳基烷基，二环芳基，联芳基或式的基团（一）：R <9> -X-烷 - 或（b）指，或者与R一起<4> 和的碳原子其所连接形成任选经取代的五到形成七元碳环或杂环; [R <6>是氢，低级烷基或芳基甲基; [R <7> - [R <8>各自独立地表示氢或低级烷基，或一起与氮原子到它们所连接，形成五至六元杂环; [R <9>是氢，低级烷基，低级烯基，环烷基，环烯基，单环或双环芳基，联芳基，R <10>为式（a）的装置; X的化合价键，代表氧或硫; Q是氧，硫或氮; alk是价键，亚甲基，一个饱和或不饱和的亚烷基链与2 - 6个碳原子的装置; N = 0-3; M = 0-2且p = 0-5的装置，其制备方法和含有这些化合物，钙代谢紊乱的治疗的药物组合物的方法。

6. 发明申请

WO1995026358A1 2,4-DIPHOSPHONOGLUTARIC ACID DERIVATIVES, METHODS OF PREPARING SUCH COMPOUNDS AND DRUGS CONTAINING THEM 审中-公开
标题翻译：新的2.4DIPHOSPHONOGLUTARSÄUREDERIVATE，方法为生产和药物含有它们的
公开(公告)号：WO1995026358A1
公开(公告)日：1995-10-05
申请号：PCT/EP1995001062
申请日：1995-03-22
申请人： BOEHRINGER MANNHEIM GMBH , ZIMMERMANN, Gerd , ESSWEIN, Angelika , TSAKLAKIDIS, Christos , BAUSS, Frieder
发明人： BOEHRINGER MANNHEIM GMBH
IPC分类号： C07F09/38
CPC分类号： C07F9/3869 , C07F9/3873 , C07F9/572
摘要： The invention concerns compounds of the formula (I) in which R is lower alkyl (which may optionally be substituted by hydroxy, alkoxy, amino, dialkylamino, alkylmercapto, alkylsulphinyl, alkansulphonyl, cycloalkyl, aryl or a heterocyclic ring), lower alkenyl, cycloalkyl, cycloalkenyl, aryl or a heterocyclic ring and R1 and R2, independently of each other, may be hydrogen, lower alkyl, cycloalkyl, aryl or arylmethyl, as well as their optically active compounds and their pharmacologically acceptable salts. The invention also concerns methods of preparing such compounds and drugs containing them for the treatment of metabolic calcium disorders. The invention further concerns compounds of the formula (II) for use as intermediates in the preparation of compounds of the formula (I).
摘要翻译：式（I）的化合物，其可任选地被羟基，烷氧基，氨基，二烷基氨基，烷基巯基，烷基亚磺酰基，烷磺酰基，环烷基，芳基或杂环，低级烯基，环烷基，环烯基，芳基或取代将R烷基低级杂环和R1和R2各自为氢，低级Aklyl，环烷基，芳基或芳甲基可以是彼此独立，它们的光学活性化合物及其药理学上可接受的盐，它们的制备方法和含有这些化合物的药物组合物，钙代谢障碍的治疗，此外，式（II）的本发明的化合物作为中间体用于制备式（I）的化合物。

7. 发明申请

WO1995011249A1 2,4-DIPHOSPHONOGLUTARIC ACID DERIVATIVES, METHODS OF PREPARING THEM AND DRUGS CONTAINING THEM 审中-公开
标题翻译：新的2.4DIPHOSPHONOGLUTARSÄUREDERIVATE，方法为生产和药物含有它们的
公开(公告)号：WO1995011249A1
公开(公告)日：1995-04-27
申请号：PCT/EP1994003434
申请日：1994-10-19
申请人： BOEHRINGER MANNHEIM GMBH , ESSWEIN, Angelika , TSAKLAKIDIS, Christos , ZIMMERMANN, Gerd , BAUSS, Frieder
发明人： BOEHRINGER MANNHEIM GMBH
IPC分类号： C07F09/38
CPC分类号： C07F9/3873 , C07F9/386 , C07F9/3869 , C07F9/572 , C07F9/58 , C07F9/59 , C07F9/6506 , C07F9/6533 , C07F9/65515 , C07F9/655345
摘要： The invention concerns compounds of formula (I) in which R is hydrogen, lower alkyl (which may be substituted by hydroxy, alkoxy, amino, dialkylamino, alkylmercapto, alkylsulphinyl, alkansulphonyl, cycloalkyl, aryl or a heterocyclic ring), lower alkenyl, cycloalkyl, cycloalkenyl, aryl or a heterocyclic ring and R1 and R2, independently of each other, may be hydrogen, lower alkyl, cycloalkyl or arylmethyl, plus pharmacologically acceptable salts of these compounds. The invention also concerns methods of preparing such compounds and drugs containing them for the treatment of metabolic disorders relating to calcium.
摘要翻译：式（I）的化合物，其中其可任选地被羟基，烷氧基，氨基，二烷基氨基，烷基巯基，烷基亚磺酰基，烷磺酰基，环烷基，芳基或杂环，低级烯基，环烷基，环烯基被取代R =氢，低级烷基基，芳基或杂环，R1和R2unhabhängig可以是氢，低级烷基，环烷基或芳甲基另一在每种情况下，以及它们的药理学上可接受的盐，它们的制备方法和含有这些化合物，钙代谢紊乱的治疗药物组合物。

8. 发明申请

WO1993001195A1 DIBENZ[b,e]AZEPINE DERIVATIVES AND DRUGS CONTAINING THEM 审中-公开
标题翻译： DIBENZ（B，E）AZEPINE衍生物和含有他们的药物
公开(公告)号：WO1993001195A1
公开(公告)日：1993-01-21
申请号：PCT/EP1992001465
申请日：1992-06-30
申请人： BOEHRINGER MANNHEIM GMBH , FRIEBE, Walter-Gunar , LEINERT, Herbert , MERTENS, Alfred , SCHÄFER, Wolfgang , ZILCH, Harald
发明人： BOEHRINGER MANNHEIM GMBH
IPC分类号： C07D513/08
CPC分类号： C07D513/08
摘要： The invention relates to dibenz[b,e]azepine derivatives of formula (I), in which A is a methylene, carbonyl, thiocarbonyl, carbimino, N-hydroxycarbimino or sulphonyl group; X is a valency bond or an oxygen or sulphur atom, a sulphinyl or sulphonyl group, a CH2S group or an NH group; n is a whole number from 1 to 3; and R1 to R4, which can be the same or different, are, independently of each other, a hydrogen atom or an aliphatic group with 1-6 C-atoms, as well as their tautomers, enantiomers, diastereomers and their physiologically tolerated salts. In addition, the invention concerns drugs containing compounds of formula (I), in particular drugs for use in treating viral infections.

9. 发明申请

WO1993012122A1 NOVEL PHOSPHONO-SUCCINIC ACID DERIVATIVES, PROCESS FOR PRODUCING THEM AND MEDICAMENTS CONTAINING THESE COMPOUNDS 审中-公开
标题翻译：新型磷酸化合物衍生物，其制备方法和含有这些化合物的药物
公开(公告)号：WO1993012122A1
公开(公告)日：1993-06-24
申请号：PCT/EP1992002890
申请日：1992-12-14
申请人： BOEHRINGER MANNHEIM GMBH , TSAKLAKIDIS, Christos , BOSIES, Elmar , ESSWEIN, Angelika , BAUSS, Frieder
发明人： BOEHRINGER MANNHEIM GMBH
IPC分类号： C07F09/38
CPC分类号： C07F9/4006 , C07F9/3808 , C07F9/5532 , C07F9/572 , C07F9/58 , C07F9/6506
摘要： PCT No. PCT/EP92/02890 Sec. 371 Date Jun. 3, 1994 Sec. 102(e) Date Jun. 3, 1994 PCT Filed Dec. 14, 1992 PCT Pub. No. WO93/12122 PCT Pub. Date Jun. 24, 1993 (I) Compounds of the formula (I) in which: R is a possibly substituted amino group of the general form -NR1R2, in which R1 and R2 are independently hydrogen, lower alkyl, lower alkenyl or lower alkinyl, or R is a saturated, unsaturated or aromatic heterocyclic ring which may be mono or bi-substituted by lower alkyl or halogen; alk is a valency bond, a methylene, a saturated or unsaturated, straight or branched-chain alkylene chain with 2-6 carbon atoms; and R3, R4, R5 are independently hydrogen, lower alkyl or benzyl; and their pharmacologically acceptable salts and enantiomers where, if R3=R4=R5=CH3 and alk is a valency bond, R may not be the dimethyl amino group. Process for their production and medicaments containing these compounds, for the treatment of calcium metabolic complaints.

10. 发明申请

WO1994014781A1 USE OF BENZOTRIAZINES AS PLA2 INHIBITORS, AND NEW BENZOTRIAZINES 审中-公开
标题翻译：使用苯并三嗪类AS PLA2抑制剂和新型苯并三嗪类的
公开(公告)号：WO1994014781A1
公开(公告)日：1994-07-07
申请号：PCT/EP1993003542
申请日：1993-12-15
申请人： BOEHRINGER MANNHEIM GMBH , FRIEBE, Walter-Gunar , SCHEUER, Werner , TIBES, Ulrich
发明人： BOEHRINGER MANNHEIM GMBH
IPC分类号： C07D251/08
CPC分类号： C07D253/10 , A61K31/53 , Y02A50/395
摘要： Described is the use, in the preparation of drugs with a PLA2-inhibiting action, of compounds of the formula (I) in which R1 is an amino, a C1-C6 alkylamino, a di(C1-C6 alkyl)amino or a hydroxy group; R2 and R3, which may be the same or different, are hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, cyano, carboxy, halo(C1-C6 alkyl), cyano(C1-C6 alkyl), carboxy(C1-C6 alkyl), hydroxy, carboxy(C1-C6 alkoxy), (C1-C6 alkoxy)carbonyl(C1-C6 alkoxy), aminocarbonyl(C1-C6 alkoxy), (C1-C6 alkyl)aminocarbonyl(C1-C6 alkoxy) or di(C1-C6 alkyl)aminocarbonyl(C1-C6 alkoxy) and n is 0 or 1, plus their tautomers and salts with non-toxic acids or bases. Also described are new compounds of formula I and methods or preparing them.

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