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1. 发明公开

EP3239143A2 BIARYL DERIVATIVE AS GPR120 AGONIST 有权
标题翻译： BIARYL衍生物作为GPR120激动剂
公开(公告)号：EP3239143A2
公开(公告)日：2017-11-01
申请号：EP15873645.4
申请日：2015-12-23
申请人： LG Chem, Ltd.
发明人： KIM, Young Kwan , PARK, Sang Yun , JOO, Hyun Woo , CHOI, Eun Sil , PAEK, Seung Yup , KANG, Seung Wan , KIM, Byung Gyu , LEE, Chang Seok , KIM, Sung Wook , LEE, Sang Dae
IPC分类号： C07D401/04 , A61K31/4725 , A61P3/10 , A61P3/04
CPC分类号： C07D487/04 , A61K31/4725 , C07C59/31 , C07C229/42 , C07C229/44 , C07C317/22 , C07C2601/04 , C07C2601/08 , C07D207/06 , C07D209/08 , C07D211/34 , C07D213/30 , C07D213/64 , C07D213/70 , C07D231/56 , C07D235/16 , C07D239/34 , C07D241/18 , C07D261/08 , C07D277/34 , C07D307/42 , C07D307/80 , C07D311/58 , C07D317/46 , C07D317/72 , C07D333/16 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/04 , C07D409/04 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/12 , C07D417/10
摘要： The present invention relates to a biaryl derivative expressed by the chemical formula 1, a method for producing the biaryl derivative, a pharmaceutical composition comprising same, and use of same, the biaryl derivative expressed by the chemical formula 1, as a GPR120 agonist, promoting GLP-1 generation in the gastro-intestinal tract, reducing insulin resistance in the liver, muscles and the like from anti-inflammatory activity in the macrophage, pancreatic cells and the like, and allowing effective use in prevention or treatment of inflammation or metabolic diseases such as diabetes, complications from diabetes, obesity, non-alcoholic fatty liver disease, fatty liver disease, and osteoporosis.
摘要翻译：本发明涉及化学式1表示的联芳衍生物，联芳衍生物的制备方法，包含它的药物组合物及其用途，由化学式1表示的联芳衍生物作为GPR120激动剂，促进 GLP-1在胃肠道中的产生，降低肝脏，肌肉等中的巨噬细胞，胰腺细胞等中的抗炎活性的胰岛素抵抗性，并且允许有效用于预防或治疗炎症或代谢疾病如糖尿病，糖尿病并发症，肥胖症，非酒精性脂肪肝疾病，脂肪肝疾病和骨质疏松症。

2. 发明公开

EP2643286A1 TERPENETHER 审中-公开
公开(公告)号：EP2643286A1
公开(公告)日：2013-10-02
申请号：EP11802628.5
申请日：2011-11-22
申请人： CABB GmbH
发明人： WAGNER, Adalbert , GICK, Robert
IPC分类号： C07C59/31 , C07C43/196 , C07C69/734 , C07C235/06 , C11D3/00
CPC分类号： C07C59/31 , C07C43/196 , C07C69/734 , C07C235/06 , C07C2602/42
摘要： The invention relates to a terpene ether of the general formula (I) Z-O-R, in which Z denotes a bicyclo[a, b, c]heptenyl group or bicyclo[a, b, c]heptyl group, wherein: a + b + c = 5, a = 2, 3 or 4, b = 2 or 1, and c = 0, 1, said group being optionally substituted with at least one C
1-6 alkyl group, preferably a methyl group, and having a skeleton selected from the skeletons (Z
1 to Z
7 ) specified below and from the corresponding heptyl skeletons without a double bond: (Z
1 ) [3.2.0], (Z
2 ) [3.2.0], (Z
3 ) [2.2.1], (Z
4 ) [3.1.1], (Z
5 ) [3.1.1], (Z
6 ) [4.1.0], (Z
7 ) [4.1.0]; and R is a substituted aliphatic or cycloaliphatic group that comprises at least two oxygen atoms, each of which is connected to only one carbon atom, at least one of said oxygen atoms being bonded to the second carbon atom of the group R.
摘要翻译：萜烯醚化合物（Q）是新的。式（Z-O-R）（I），（Z-O-R19）（II）或（Z-O-R21）（III）的萜醚化合物（Q）是新的。 Z：双环[a，b，c]庚烯基或双环[a，b，c]庚基，其中a + b + c为5，a为2-4，b为2或1，c为0或 1，Z任选被至少一个1-6C-烷基，优选CH 3取代，并且具有双环[3.2.0]庚-2-烯，双环[3.2.0]庚-1-烯，双环[2.2.1]庚-2-烯，双环[3.1.1]庚-2-烯，双环[3.1.1]庚-3-烯，双环[4.1.0]庚-2-烯或双环[ 4.1.0]庚-3-烯或上述不具有双键的骨架，优选为1,7,7-三甲基降冰片烷-2-基; R：包含至少两个氧原子的取代（环）脂族基团，每个氧原子仅与一个碳原子连接，其中至少一个氧原子与基团R的第二个碳原子键合，优选为乳酸酸残; R19：任选取代的（环）脂族残基，其含有至少一个-O-CO-R20残基或至少一个1,3-二氧戊环-2-酮结构单元; R20，R22：任选取代的1-40C-（环）脂族残基; R21：-CR10R11-R12-COX; R10，R11，R23，R24：H或任选取代的1-40C-（环）脂族残基; R12：键或任选取代的1-40C-（环）脂族残基; 和X：-O-R 22或-NR 23 R 24。包括（Q）的水性组合物的独立权利要求。

3. 发明公开

EP0045118A2 Intermediates for the synthesis of bicyclo (2,2,1) heptanes and bicyclo (2,2,1) hept-2Z-enes 有权转让
标题翻译：（2,2,1）庚烷和比齐克洛（2,2,1）庚-2Z-烯的Zwischenproduktefürdie Synthese von Bizyklo。
公开(公告)号：EP0045118A2
公开(公告)日：1982-02-03
申请号：EP81201031.2
申请日：1980-01-04
申请人： NATIONAL RESEARCH DEVELOPMENT CORPORATION
发明人： Jones, Robert Leslie , Wilson, Norman Happer
IPC分类号： C07C59/11 , C07C59/205 , C07C59/46 , C07C59/80
CPC分类号： C07C255/00 , C07B2200/07 , C07C41/48 , C07C43/315 , C07C45/44 , C07C59/13 , C07C59/147 , C07C59/31 , C07C59/325 , C07C59/46 , C07C59/54 , C07C59/62 , C07C59/74 , C07C59/80 , C07C59/86 , C07C405/0091 , C07C2602/42 , C07D307/60 , C07D307/93 , Y10S514/826
摘要： Novel bicyclo[2,2,1]heptanes and hept-2Z-enes are substituted at the 5-position by a 6-carboxyhex-2-enyl group or a modification thereof as defined herein, and at the 6-position by a group
in which R 1 represents an aliphatic hydrocarbon residue or an aliphatic hydrocarbon residue substituted directly or through an oxygen or sulphur atom by an aromatic residue, R2 represents hydrogen and R 3 represents a hydroxy group, or R 2 and R 3 together represent the oxygen atom of a carboxyl group. These compounds are of value for use in the synthesis of certain biologically active 5,6-disubstituted bicyclo[2,2,1]heptanes and hept-2Z-enes.
摘要翻译：新的双环[2,2,1]庚烷和庚-2Z-烯通过如本文所定义的6-羧基己-2-烯基或其修饰在5位上被取代，并且在6-位上被一个基团其中R1表示脂肪族烃残基或由芳香族残基直接或通过氧或硫原子取代的脂族烃残基，R2表示氢，R3表示羟基，或R2和R3一起代表羧基。这些化合物对于合成某些生物活性的5,6-二取代的双环[2,2,1]庚烷和庚-2Z-烯有价值。

4. 发明公开

EP3390346A1 COMPOSITIONS AND METHODS RELATED TO HALF SALTS OF HERBICIDAL CARBOXYLIC ACIDS 有权转让
公开(公告)号：EP3390346A1
公开(公告)日：2018-10-24
申请号：EP16876546.9
申请日：2016-12-14
申请人： Dow Agrosciences LLC
发明人： LIU, Lei , TANK, Holger , OLDS, Melissa Gail , WILSON, Stephen L.
IPC分类号： C07C211/14 , A01N43/40
CPC分类号： C07C59/31 , A01N37/10 , A01N39/02 , A01N39/04 , A01N43/40 , A01N57/20 , C07D213/64
摘要： Half salts of certain synthetic auxin herbicides are provided. These half salts are useful for controlling unwanted plant growth. The half salts have low solubility in water, low volatility relative to commercial compositions of the corresponding synthetic auxin herbicides, and offer comparable herbicidal performance when compared to existing salts of the synthetic auxin herbicides.

5. 发明公开

EP0045118A3 Intermediates for the synthesis of bicyclo (2,2,1) heptanes and bicyclo (2,2,1) hept-2Z-enes 有权转让
标题翻译：二氨基（2,2,1）庚二酸和二巯基（2,2,1）HEPT-2Z-烯的合成中间体
公开(公告)号：EP0045118A3
公开(公告)日：1982-03-24
申请号：EP81201031
申请日：1980-01-04
申请人： Jones, Robert Leslie , Wilson, Norman Happer
发明人： Jones, Robert Leslie
IPC分类号： C07C59/11 , C07C59/205 , C07C59/46 , C07C59/80 , C07C177/00
CPC分类号： C07C255/00 , C07B2200/07 , C07C41/48 , C07C43/315 , C07C45/44 , C07C59/13 , C07C59/147 , C07C59/31 , C07C59/325 , C07C59/46 , C07C59/54 , C07C59/62 , C07C59/74 , C07C59/80 , C07C59/86 , C07C405/0091 , C07C2602/42 , C07D307/60 , C07D307/93 , Y10S514/826
摘要： Novel bicyclo[2,2,1]heptanes and hept-2Z-enes are substituted at the 5-position by a 6-carboxyhex-2-enyl group or a modification thereof as defined herein, and at the 6-position by a group
in which R 1 represents an aliphatic hydrocarbon residue or an aliphatic hydrocarbon residue substituted directly or through an oxygen or sulphur atom by an aromatic residue, R2 represents hydrogen and R 3 represents a hydroxy group, or R 2 and R 3 together represent the oxygen atom of a carboxyl group. These compounds are of value for use in the synthesis of certain biologically active 5,6-disubstituted bicyclo[2,2,1]heptanes and hept-2Z-enes.
摘要翻译：新的双环[2,2,1]庚烷和庚-2Z-烯通过如本文所定义的6-羧基己-2-烯基或其修饰在5位上被取代，并且在6-位上被一个基团其中R1表示脂肪族烃残基或由芳香族残基直接或通过氧或硫原子取代的脂族烃残基，R2表示氢，R3表示羟基，或R2和R3一起代表羧基。这些化合物对于合成某些生物活性的5,6-二取代的双环[2,2,1]庚烷和庚-2Z-烯有价值。

6. 发明公开

EP2066667A1 PROCESS FOR THE PREPARATION OF PYRIDO[2,1-A]ISOQUINOLINE DERIVATIVES COMPRISING OPTICAL RESOLUTION OF AN ENAMINE 有权
标题翻译：用于生产吡啶并[2,1-A]异喹啉，一个烯胺的分辨率INCLUDES
公开(公告)号：EP2066667A1
公开(公告)日：2009-06-10
申请号：EP07803228.1
申请日：2007-09-05
申请人： F. Hoffmann-La Roche AG
发明人： ABRECHT, Stefan , ADAM, Jean-Michel , FETTES, Alec , HILDBRAND, Stefan
IPC分类号： C07D471/04
CPC分类号： C07D455/06 , C07C59/31 , C07D471/04
摘要： This invention relates to a process for the preparation of pyrido[2,1-a] isoquinoline derivatives of the formula wherein R1, R2, R3 and R4 are defined in the specification, comprising the optical resolution of an enamine of the formula wherein R1 is lower alkyl, in the presence of an optical active resolving agent to form an (S)-enamine salt of the formula wherein RCO2− is the conjugate base of the resolving agent.

7. 发明公开

EP0089674A1 Pentanedioic acid derivatives 有权
标题翻译： Derivate derGlutarsäure。
公开(公告)号：EP0089674A1
公开(公告)日：1983-09-28
申请号：EP83102809.7
申请日：1983-03-22
申请人： G.D. Searle & Co.
发明人： Lowrie, Harman Smith , Baran, John Stanislaus
IPC分类号： C07C59/29 , C07C59/245 , C07C59/31 , C07C57/26 , C07F9/54 , C07C69/608 , C07C33/20 , C07C69/675 , A61K31/19
CPC分类号： C07C59/31 , C07C33/20 , C07C57/26 , C07C59/245 , C07C59/29 , C07F9/5407
摘要： Derivates of β-hydroxy-β-alkylglutaric acid are described which are useful to inhibit the formation of serum cholesterol by virtue of their ability to inhibit β-hydroxy-β-methylglutaryl-CoA(HMG CoA), the rate-controlling substance in the synthesis of serum cholesterol.
摘要翻译：描述了β-羟基-β-烷基戊二酸的衍生物，其可用于通过抑制β-羟基-β-甲基戊二酰辅酶A（HMG CoA）的抑制能力来抑制血清胆固醇的形成，合成血清胆固醇。

8. 发明授权

EP0013607B1 Substituted bicyclo (2,2,1)heptanes and bicyclo (2,2,1) hept-2-enes and their pharmaceutical compositions 有权转让
标题翻译：替代双酚A（2,2,1）HEPTANES和BICYCLO（2,2,1）HEPT-2-ENES及其药物组合物
公开(公告)号：EP0013607B1
公开(公告)日：1983-03-23
申请号：EP80300039.7
申请日：1980-01-04
申请人： NATIONAL RESEARCH DEVELOPMENT CORPORATION
发明人： Jones, Robert Leslie , Wilson, Norman Happer
IPC分类号： C07C131/00 , A61K31/15
CPC分类号： C07C255/00 , C07B2200/07 , C07C41/48 , C07C43/315 , C07C45/44 , C07C59/13 , C07C59/147 , C07C59/31 , C07C59/325 , C07C59/46 , C07C59/54 , C07C59/62 , C07C59/74 , C07C59/80 , C07C59/86 , C07C405/0091 , C07C2602/42 , C07D307/60 , C07D307/93 , Y10S514/826

9. 发明公开

EP3239143A4 BIARYL DERIVATIVE AS GPR120 AGONIST 有权
公开(公告)号：EP3239143A4
公开(公告)日：2018-05-30
申请号：EP15873645
申请日：2015-12-23
申请人： LG CHEMICAL LTD
发明人： KIM YOUNG KWAN , PARK SANG YUN , JOO HYUN WOO , CHOI EUN SIL , PAEK SEUNG YUP , KANG SEUNG WAN , KIM BYUNG GYU , LEE CHANG SEOK , KIM SUNG WOOK , LEE SANG DAE
IPC分类号： C07D401/04 , A61K31/4725 , A61P3/04 , A61P3/10
CPC分类号： C07D487/04 , A61K31/4725 , C07C59/31 , C07C229/42 , C07C229/44 , C07C317/22 , C07C2601/04 , C07C2601/08 , C07D207/06 , C07D209/08 , C07D211/34 , C07D213/30 , C07D213/64 , C07D213/70 , C07D231/56 , C07D235/16 , C07D239/34 , C07D241/18 , C07D261/08 , C07D277/34 , C07D307/42 , C07D307/80 , C07D311/58 , C07D317/46 , C07D317/72 , C07D333/16 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/04 , C07D409/04 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/12 , C07D417/10
摘要： The present invention relates to a biaryl derivative expressed by the chemical formula 1, a method for producing the biaryl derivative, a pharmaceutical composition comprising same, and use of same, the biaryl derivative expressed by the chemical formula 1, as a GPR120 agonist, promoting GLP-1 generation in the gastro-intestinal tract, reducing insulin resistance in the liver, muscles and the like from anti-inflammatory activity in the macrophage, pancreatic cells and the like, and allowing effective use in prevention or treatment of inflammation or metabolic diseases such as diabetes, complications from diabetes, obesity, non-alcoholic fatty liver disease, fatty liver disease, and osteoporosis.

10. 发明公开

EP2465840A1 Terpenether 审中-公开
公开(公告)号：EP2465840A1
公开(公告)日：2012-06-20
申请号：EP10014859.2
申请日：2010-11-23
申请人： CABB GmbH
发明人： Wagner, Adalbert, Dr. , Gick, Robert
IPC分类号： C07C59/31 , C07C43/196 , C07C69/734 , C07C235/06 , C11D3/00
CPC分类号： C07C59/31 , C07C43/196 , C07C69/734 , C07C235/06 , C07C2602/42
摘要： Terpenether der allgemeinen Formel (I)

Z-O-R (I)

worin
■ Z eine Bicyclo[a, b, c]heptenylgruppe oder Bicyclo[a, b, c]heptylgruppe bedeutet, mit:
• a+b+c=5,
• a = 2,3 oder 4,
• b = 2 oder 1,
• c = 0,1,

wobei diese Gruppe gegebenenfalls mit mindestens einer C 1-6 -Alkylgruppe, vorzugsweise einer Methylgruppe, substituiert ist und ein Gerüst aufweist, das ausgewählt ist unter den im folgenden angegebenen Gerüsten (Z 1 bis Z 7 ) sowie unter den entsprechenden Heptylgerüsten ohne Doppelbindung:

■
R für einen substituierten, aliphatischen oder cycloaliphatischen Rest steht, der mindestens zwei Sauerstoffatome umfasst, die jeweils nur mit einem Kohlenstoffatom verbunden sind, wobei mindestens eins dieser Sauerstoffatome an das zweite Kohlenstoffatom des Rests R gebunden ist.
摘要翻译：萜烯醚化合物（Q）是新的。式（Z-O-R）（I），（Z-O-R19）（II）或（Z-O-R21）（III）的萜醚化合物（Q）是新的。 Z：双环[a，b，c]庚烯基或双环[a，b，c]庚基，其中a + b + c为5，a为2-4，b为2或1，c为0或 1，Z任选被至少一个1-6C-烷基，优选CH 3取代，并且具有双环[3.2.0]庚-2-烯，双环[3.2.0]庚-1-烯，双环[2.2.1]庚-2-烯，双环[3.1.1]庚-2-烯，双环[3.1.1]庚-3-烯，双环[4.1.0]庚-2-烯或双环[ 4.1.0]庚-3-烯或上述不具有双键的骨架，优选为1,7,7-三甲基降冰片烷-2-基; R：包含至少两个氧原子的取代（环）脂族基团，每个氧原子仅与一个碳原子连接，其中至少一个氧原子与基团R的第二个碳原子键合，优选为乳酸酸残; R19：任选取代的（环）脂族残基，其含有至少一个-O-CO-R20残基或至少一个1,3-二氧戊环-2-酮结构单元; R20，R22：任选取代的1-40C-（环）脂族残基; R21：-CR10R11-R12-COX; R10，R11，R23，R24：H或任选取代的1-40C-（环）脂族残基; R12：键或任选取代的1-40C-（环）脂族残基; 和X：-O-R 22或-NR 23 R 24。包含（Q）的水性组合物的独立权利要求。

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