- 2-(1H-INDOLE-3-CARBONYL)-THIAZOLE-4-CARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS AS ARYL HYDROCARBON RECEPTOR (AHR) AGONISTS FOR THE TREATMENT OF E.G. ANGIOGENESIS IMPLICATED OR INFLAMMATORY DISORDERS
-
2-(1H-lndole-3-carbonyl)-thiazole-4-carboxamide derivatives and the corresponding imidazole, oxazole and thiophene derivatives and related compounds as aryl hydrocarbon receptor (AHR) agonists for the treatment of angiogenesis implicated disorders, such as e.g. retinopathy, psoriasis, rheumatoid arthritis, obesity and cancer, or inflammatory disorders. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 27 to 32 and 59 to 219; examples 1 to 8; compounds 1-1 to 1-97; tables 1-a, 2 and 3).
- -
-
Paragraph 00162; 00257
(2021/06/26)
-
- Electrochemical Deoxygenative Thiolation of Preactivated Alcohols and Ketones
-
This work describes an electrochemically promoted nickel-catalyzed deoxygenative thiolation of alcohols and ketones under mild conditions. Excellent substrate tolerance and good chemical yields can be achieved by graphene/nickel foam electrodes in an undivided cell. Further study to gain mechanistic insight into this electrochemical cross-coupling has been carried out.
- Zhang, Feng,Wang, Yang,Wang, Yi,Pan, Yi
-
supporting information
p. 7524 - 7528
(2021/10/02)
-
- ASK1 ISOINDOLIN-1-ONE INHIBITORS AND METHODS OF USE THEREOF
-
Isoindolin-1-one compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an isoindolin-1-one compound or analogs thereof, in the treatment of disorders characterized by the activ
- -
-
Paragraph 0339-0340
(2020/01/22)
-
- GLYCOLATE OXIDASE INHIBITORS FOR THE TREATMENT OF DISEASE
-
Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with a defect in glyoxylate metabolism, for example a disease or disorder associated with the enzyme glycolate oxidase (GO) or alterations in oxalate metabolism. Such diseases or disorders include, for example, disorders of glyoxylate metabolism, including primary hyperoxaluria, that are associated with production of excessive amounts of oxalate.
- -
-
Paragraph 001555; 001556
(2021/01/22)
-
- Cyclic Alkenylsulfonyl Fluorides: Palladium-Catalyzed Synthesis and Functionalization of Compact Multifunctional Reagents
-
A series of low-molecular-weight, compact, and multifunctional cyclic alkenylsulfonyl fluorides were efficiently prepared from the corresponding alkenyl triflates. Palladium-catalyzed sulfur dioxide insertion using the surrogate reagent DABSO effects sulfinate formation, before trapping with an F electrophile delivers the sulfonyl fluorides. A broad range of functional groups are tolerated, and a correspondingly large collection of derivatization reactions are possible on the products, including substitution at sulfur, conjugate addition, and N-functionalization. Together, these attributes suggest that this method could find new applications in chemical biology.
- Lou, Terry Shing-Bong,Bagley, Scott W.,Willis, Michael C.
-
supporting information
p. 18859 - 18863
(2019/11/19)
-
- MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE
-
Provided are IDO1 inhibitor compounds of Formula (I) and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of diseases.
- -
-
Page/Page column 38
(2019/06/23)
-
- PYRIMIDINE CYCLOHEXENYL GLUCOCORTICOID RECEPTOR MODULATORS
-
The present invention provides a class of pyrimidinedione cyclohekenyl compounds and methods of using these compounds as glucocorticoid receptor modulators.
- -
-
Paragraph 0247-0248
(2019/12/28)
-
- NOVEL BENZOIMIDAZOLES AS SELECTIVE INHIBITORS OF INDOLEAMINE 2, 3-DIOXYGENASES
-
Disclosed herein are novel benzoimidazoles and pharmaceutical compositions comprising at least one such novel benzoimidazoles, processes for the preparation thereof, and the method for using the same in therapy. In particular, disclosed herein are certain novel benzoimidazoles that are useful for inhibiting indoleamine 2, 3-dioxygenase and for treating diseases or disorders mediated thereby.
- -
-
Paragraph 0510; 0511
(2019/06/11)
-
- Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease
-
We have identified chemical probes that act as dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors (>1 log unit difference versus class I HDACs) to decipher the contribution of HDAC isoforms to the positive impact of dua
- Rabal, Obdulia,Sánchez-Arias, Juan A.,Cuadrado-Tejedor, Mar,de Miguel, Irene,Pérez-González, Marta,García-Barroso, Carolina,Ugarte, Ana,Estella-Hermoso de Mendoza, Ander,Sáez, Elena,Espelosin, Maria,Ursua, Susana,Haizhong, Tan,Wei, Wu,Musheng, Xu,Garcia-Osta, Ana,Oyarzabal, Julen
-
supporting information
p. 506 - 524
(2018/03/21)
-
- TRICYCLIC COMPOUND SERVING AS IMMUNOMODULATOR
-
Provided are compounds of formula I and formula II or pharmaceutically acceptable salts of the compounds and pharmaceutical compositions thereof. The compounds of formula I and formula II or the pharmaceutically acceptable salts of the compounds provide indole 2,3-dioxygenase (IDO) inhibitory activity and are capable of treating IDO-mediated immunosuppressive diseases, such as infectious diseases or cancer.
- -
-
Paragraph 0710-0711
(2019/01/04)
-
- Multimetallic Ni- and Pd-Catalyzed Cross-Electrophile Coupling to Form Highly Substituted 1,3-Dienes
-
The synthesis of highly substituted 1,3-dienes from the coupling of vinyl bromides with vinyl triflates is reported for the first time. The coupling is catalyzed by a combination of (5,5′-bis(trifluoromethyl)-2,2′-bipyridine)NiBr2 and (1,3-bis(diphenylphosphino)propane)PdCl2 in the presence of a zinc reductant. This method affords tetra- and penta-substituted 1,3-dienes that would otherwise be difficult to access and tolerates electron-rich and -poor substituents, heterocycles, an aryl bromide, and a pinacol boronate ester. Mechanistically, the reaction appears to proceed by an unusual zinc-mediated transfer of a vinyl group between the nickel and palladium centers.
- Olivares, Astrid M.,Weix, Daniel J.
-
supporting information
p. 2446 - 2449
(2018/02/28)
-
- CYCLOHEXYL GPR40 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES
-
Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (I) as follows: (Formula (I)) wherein R1, R2, R3, A, W, L, Ra, and G are defined herein: and by Formula (II) as follows: (Formula (II)) wherein R1B, WB, LB, and GB are defined herein.
- -
-
Page/Page column 136
(2018/05/24)
-
- Heterocyclic compound used as MNK inhibitor
-
The invention relates to a heterocyclic compound, a pharmaceutical composition containing the heterocyclic compound, a preparation method thereof, and application thereof used as a mitogen activated protein kinase interacting kinase 1 and 2-MNK1/MNK2 inhibitor. The inhibitor is the heterocyclic compound as shown in the formula (I), or its pharmaceutically acceptable salt, prodrug, solvent compound, polycrystal, isomer, stable isotope derivative or a pharmaceutical composition containing the heterocyclic compound. The compound of the invention can be used for treating or preventing MNK-mediatedrelated diseases, such as cancers.
- -
-
Paragraph 0156
(2019/01/08)
-
- NOVEL COMPOUNDS FOR USE IN CANCER
-
It relates to the compounds of formula (I), or their pharmaceutically or veterinary acceptable salts, or their stereoisomers or mixtures of stereoisomers, wherein X, L,R1, R 2, and R 3 are as defined herein, which are cancer cell differentiation inducing agents. It also relates to pharmaceutical or veterinary compositions containing them, and to their use in medicine, in particular in the treatment and/or prevention of cancer, in particular by cell differentiation therapy.
- -
-
Page/Page column 43
(2019/01/07)
-
- NOVEL IMIDAZOLE COMPOUND AND USE THEREOF AS MELANOCORTIN RECEPTOR AGONIST
-
The present invention relates to a novel imidazole compound or a pharmaceutically acceptable salt thereof having a melanocortin receptor agonistic activity, and medical use thereof. The present invention relates to an imidazole compound represented by general formula [I] [wherein: Ring A represents an optionally substituted aryl group or the like; R1 represents a hydrogen atom, an optionally substituted alkyl group, or the like; R2 represents a hydrogen atom, a halogen atom, or the like; and R3 represents an optionally substituted alkyl group] or a pharmaceutically acceptable salt thereof.
- -
-
Paragraph 0514
(2018/10/04)
-
- Pharmaceutical compositions (by machine translation)
-
[Problem] imidazole compound or its pharmacologically acceptable salt in the melanocortin receptor activity that operates as an active ingredient of a pharmaceutical composition comprising. "I" general formula [a]" Formula, the aryl group may be substituted A ring represents a; R1 Represents a hydrogen atom, or an alkyl group which may be substituted represented; R2 Represents a hydrogen atom, a halogen atom or represents a; R3 The alkyl group may be substituted " represented by the imidazole compound, its pharmacologically acceptable salt as an active ingredient in a pharmaceutical composition. [Drawing] no (by machine translation)
- -
-
Paragraph 0186
(2019/01/31)
-
- CYCLOHEXENE DERIVATIVE, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING METABOLIC DISEASES, CONTAINING SAME AS ACTIVE INGREDIENT
-
The present invention relates to: a cyclohexene derivative; a preparation method therefor; and a pharmaceutical composition for preventing or treating metabolic diseases, containing the same as an active ingredient. The cyclohexene derivative according to the present invention increases the intracellular activity of cyclic adenosine monophosphate (cAMP) by activating G protein-coupled receptor 119 (GPR-119) and simultaneously exhibits weight loss and hypoglycemic effects by inducing the release of glucagon-like peptide-1 (GLP-1), which is a neuroendocrine protein, and thus can be useful as a pharmaceutical composition for preventing or treating metabolic diseases such as obesity, type 1 diabetes, type 2 diabetes, inadequate glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia and syndrome X.
- -
-
Paragraph 0077; 0078; 0079
(2017/03/21)
-
- CYCLOHEXENE DERIVATIVE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING METABOLIC DISEASE COMPRISING THE SAME AS ACTIVE INGREDIENT
-
The present invention relates to: a cyclohexene derivative; a preparation method thereof; and a pharmaceutical composition for preventing or treating metabolic disease comprising the same as an active ingredient. The cyclohexene derivative according to the present invention increases the intracellular activity of cyclic adenosine monophosphate (cAMP) by activating G protein-coupled receptor 119 (GPR-119) and simultaneously exhibits weight loss and hypoglycemic effects by inducing the release of glucagon-like peptide-1 (GLP-1), which is a neuroendocrine protein, and thus can be useful as a pharmaceutical composition for preventing or treating metabolic diseases such as obesity, type 1 diabetes, type 2 diabetes, inadequate glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia and syndrome X.
- -
-
Paragraph 639; 640; 641; 642
(2017/05/19)
-
- COMPOUNDS THAT INHIBIT MCL-1 PROTEIN
-
Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
- -
-
Page/Page column 185; 186
(2017/09/15)
-
- NOVEL COMPOUNDS FOR USE IN COGNITION IMPROVEMENT
-
Novel compounds for use in cognition improvement It relates to certain compounds having a polycyclic structure and a -(C=O)NRaRb moiety, wherein the polycyclic structure comprises at least three ring systems, wherein one ring system is a polycyclic ring system comprising from 2 to 4 rings; at least one ring is an aromatic ring; and wherein the structure comprises at least 3 nitrogen atoms and 1 oxygen atom. It also relates to pharmaceutical compositions containing them, and to their use in medicine, in particular in the treatment and/or prevention of neurological disorders coursing with a cognition deficit or impairment, or neurodegenerative diseases.
- -
-
Page/Page column 47
(2016/04/19)
-
- Cyclohexylpropionic polypyridine deriv.
-
A problem of the present invention is to provide a new compound which has NK 1 receptor antagonist activity ,whose CYP3A4 inhibitory activity is reduced compared to aprepitant, and which are useful for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting. That is, the present invention relates to cyclohexyl pyridine derivatives represented by the following formula (I) or a pharmaceutically acceptable salt thereof. wherein, ring A is 4-fluoro-2-methylphenyl or the like; X is a hydrogen atom or the like; R 1 is carboxymethyl or the like; R 2 is alkyl or the like; Y is 0-2 or the like; U is-N(CH 3 )COC(CH 3 ) 2 -3,5-bistrifluoromethylphenyl or the like.
- -
-
Paragraph 0053
(2016/10/27)
-
- 3-CYCLOHEXENYL AND CYCLOHEXYL SUBSTITUTED INDOLE AND INDAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
-
The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts or solvates thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.
- -
-
Paragraph 0290
(2015/07/15)
-
- Cobalt- and Nickel-Catalyzed Carboxylation of Alkenyl and Sterically Hindered Aryl Triflates Utilizing CO2
-
A highly efficient cobalt-catalyzed reductive carboxylation reaction of alkenyl trifluoromethanesulfonates (triflates) has been developed. By employing Mn powder as a reducing reagent under 1 atm pressure of CO2 at room temperature, diverse alkenyl triflates can be converted to the corresponding α,β-unsaturated carboxylic acids. Moreover, the carboxylation of sterically hindered aryl triflates proceeds smoothly in the presence of a nickel or cobalt catalyst.
- Nogi, Keisuke,Fujihara, Tetsuaki,Terao, Jun,Tsuji, Yasushi
-
p. 11618 - 11623
(2015/12/01)
-
- AROMATIC HETEROCYCLIC COMPOUND
-
The compound represented by the general formula: wherein ring A is benzene which may be substituted and the like; ring B is benzene which may be substituted and the like; X is a single bond and the like; Y is alkyl which may be substituted and the like; Z is CR1 or nitrogen atom; R1 is hydrogen and the like; R2 is alkyl which may be substituted and the like or a pharmaceutically acceptable salt thereof is useful as a prevention/treatment agent of obesity, diabetes, and the like.
- -
-
Paragraph 0617; 0618
(2015/05/05)
-
- Cyclohexyl-4H,6H-5-oxa-2,3,10b-triaza-benzo[e]azulenes as V1a antagonists
-
The present invention provides 4H,6H-5-oxa-2,3,10b-triaza-benzo[e]azulenes, which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
- -
-
Paragraph 0146
(2014/08/19)
-
- PYRIMIDINE PDE10 INHIBITORS
-
The present invention is directed to pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
- -
-
Page/Page column 127; 128
(2014/06/11)
-
- LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS
-
Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.
- -
-
Paragraph 0971; 0972
(2014/07/23)
-
- NOVEL COMPOUNDS AS DUAL INHIBITORS OF PHOSPHODIESTERASES AND HISTONE DEACETYLASES
-
It relates to certain compounds having a polycyclic structure and a hydroxamic acid moiety, wherein the polycyclic structure comprises at least three ring systems, wherein one ring system is a polycyclic ring system comprising from 2 to 4 rings; at least one ring is an aromatic ring; and wherein the structure comprises at least 3 nitrogen atoms and 1 oxygen atom. It also relates to a process for their preparation, as well as to pharmaceutical compositions containing them, and to their use in medicine, in particular in the treatment and/or prevention of neurological disorders coursing with a cognition deficit or impairment, or neurodegenerative diseases. wherein B1 is a radical selected from the group consisting of formula (A"), formula (B"), formula (C"), and formula (D"):
- -
-
Page/Page column 76; 77
(2014/09/16)
-
- 3-CYCLOHEXENYL AND CYCLOHEXYL SUBSTITUTED INDOLE AND INDAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
-
The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts or solvates thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.
- -
-
Page/Page column 52
(2014/03/22)
-
- CYCLOHEXYL-4H,6H-5-OXA-2,3,10B-TRIAZA-BENZO[E]AZULENES AS V1A ANTAGONISTS
-
The present invention provides 4H,6H-5-oxa-2,3,10b-triaza-benzo[e]azulenes, which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
- -
-
Page/Page column 33; 34
(2013/04/24)
-
- ARYL-CYCLOHEXYL-TETRAAZABENZO[E]AZULENES
-
The present invention is concerned with aryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I wherein R1, R2 and R3 are as described herein. The invention further provides methods for the manufacture of such compounds and
- -
-
Page/Page column 19
(2011/10/13)
-
- ARYL-CYCLOHEXYL-TETRAAZABENZO[E]AZULENES
-
The present invention is concerned with aryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I, wherein R1, R2 and R3 are as described herein. The compounds according to the invention act as Via receptor modulators, and in
- -
-
Page/Page column 34-35
(2011/10/13)
-
- ARYL-/HETEROARYL-CYCLOHEXENYL-TETRAAZABENZO[E]AZULENES
-
The present invention is concerned with aryl-/heteroaryl-cyclohexenyl-tetraazabenzo[e]azulenes of formula I wherein R1, R2 and R3 are as described herein. The invention further provides methods for the manufacture of such compounds and pharmaceutical compositions containing them. The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, in appropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
- -
-
Page/Page column 18
(2011/10/19)
-
- HETEROARYL-CYCLOHEXYL-TETRAAZABENZO[E]AZULENES
-
The present invention is concerned with heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I wherein R1, R2 and R3 are as described herein. The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
- -
-
Page/Page column 33-34
(2011/11/06)
-
- ARYL - /HETEROARYL - CYCLOHEXENYL - TETRAAZABENZO [E] AZULENES AS VASOPRESSIN ANTAGONISTS
-
The present invention is concerned with aryl-/heteroaryl-cyclohexenyl-tetraazabenzo[e]azulenes of formula I wherein R1, R2 and R3 are as described herein. The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
- -
-
Page/Page column 33; 34
(2011/11/01)
-
- HETEROARYL-CYCLOHEXYL-TETRAAZABENZO[E]AZULENES
-
The present invention provides heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I wherein R1, R2 and R3 are as described herein. The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
- -
-
Page/Page column 48
(2011/11/13)
-
- HETEROARYL-CYCLOHEXYL-TETRAAZABENZO[E]AZULENES AS VASOPRESSIN V1A RECEPTOR ANTAGONISTS
-
The present invention is concerned with heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes of formula (I) wherein R1, R2 and R 3 are as described herein. The compounds according to the invention act as Via receptor modulators, and in particular as Via receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
- -
-
Page/Page column 55
(2011/11/06)
-
- HETEROARYL-CYCLOHEXYL-TETRAAZABENZO[E]AZULENES
-
The present invention is concerned with heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes of formula (I) wherein R1, R2 and R3 are as described herein. The compounds according to the invention act as Via receptor modulators, and in particular as Via receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
- -
-
Page/Page column 93; 94
(2011/12/02)
-
- A practical synthesis of the PDE4 inhibitor, KW-4490
-
A practical and scalable synthesis of a PDE4 inhibitor KW-4490 (1) was developed. This improved synthesis features the construction of the 1-arylcyclohexene (9) by the Diels-Alder reaction followed by a newly established Brnsted acid-promoted hydrocyanation. Subsequent crystallization-induced dynamic resolution enabled the high-yield production of the desired cis-isomer (cis-8). The synthesis was achieved in seven steps in 37% overall yield.
- Yanagisawa, Arata,Nishimura, Koichiro,Ando, Kyoji,Nezu, Tetsuya,Maki, Ayako,Kato, Sachiko,Tamaki, Wakako,Imai, Eiichiro,Mohri, Shin-Ichiro
-
experimental part
p. 1182 - 1187
(2011/04/17)
-
- 1,3,4-OXADIAZOLE DERIVATIVES AND THEIR USES TO TREAT DIABETES
-
DGAT-1 inhibitor compounds of formula (I) and pharmaceutically-acceptable salts thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity (I) wherein n is 0, 1, 2 or 3, R is independently selected from fluoro, chloro, bromo, trifluoromethyl, methoxy, difluoromethoxy and trifluoromethoxy and Z is carboxy or a mimic or bioisostere thereof, hydroxyl, hydroxymethyl, or ?CONRbRc wherein Rb and Rc are independently selected from hydrogen and (1-4C)alkyl, which (1-4C)alkyl group may be optionally substituted by carboxy or a mimic or bioisostere thereof.
- -
-
Page/Page column 44
(2010/08/05)
-
- CETP INHIBITORS
-
Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), B is a cyclic group other than phenyl, and B has a cyclic substituent at a position that is ortho to the position at which B is connected to the remainder of the structure of Formula (I). The 5-membered ring of Formula (I) has a second cyclic substituent in addition to B.
- -
-
Page/Page column 95
(2008/06/13)
-
- 2-AMINOQUINAZOLINE DERIVATIVE
-
The present invention provides a compound represented by Formula (I) (wherein R 1 and R 2 are the same or different, and each represents a hydrogen atom, substituted or unsubstituted lower alkyl and the like, R 3 represents substituted or unsubstituted aryl, a substituted or unsubstituted aromatic heterocyclic group and the like, R 4 and R 5 are the same or different, and each represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl and the like, proviso that they are not simultaneously hydrogen atoms, and R 6 represents hydroxy or substituted or unsubstituted lower alkoxy), or a pharmaceutically acceptable salt thereof and the like.
- -
-
Page/Page column 57
(2010/11/24)
-
- NOVEL ETHYLENEDIAMINE DERIVATIVES
-
A compound represented by the following formula (1):Q-Q-T-N(R)-Q-N(R)-T-Q [wherein, R1 and R2 are hydrogen atoms or the like; Q1 is a saturated or unsaturated, 5- or 6- membered cyclic hydrocarbon group which may have a substituent, or the like; Q2 is a single bond or the like; Q3 represents the following group: -C(R3a)(R4a)-{C(R3b)(R4b)}m1-{C(R3c)(R4c)}m2-{C(R3d)(R4d)}m3-{C(R3e)(R4e)}m4-C(R3f)(R4f)- (in which, R3a to R4e represent hydrogen or the like); T0 represents a carbonyl group or the like; and T1 represents -COCONR- or the like]; or salt thereof, solvate thereof, or N-oxide thereof. The compound is useful as a preventive and/or therapeutic agent for cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.
- -
-
Page/Page column 125
(2010/02/14)
-
- PROCESS FOR PRODUCTION OF VINYL PERFLUOROALKANESULFONATE DERIVATIVES
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(wherein R1, R2, R3, R4 and R5 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, or the like; R17 represents trifluoromethyl or the like; R18, R19, R20, R21 and R22 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like). An easy and simple process for producing a vinyl perfluoroalkanesulfonate derivative represented by general formula (IV) which is a useful intermediate in synthesis of medicines, natural products, or the like, at a low cost, is provided. The process is characterized by, for example, reacting a carbonyl compound represented by general formula (I) described above with a perfluoroalkanesulfonic anhydride represented by general formula (II) described above in the presence of a pyridine derivative represented by general formula (III) described above in an amount of 0.1 to 1.0 equivalent to the perfluoroalkanesulfonic anhydride.
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Page/Page column 16-18
(2010/02/12)
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- Sulfonyl derivatives
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Sulfonyl derivatives represented by general formula (I), salts of the same, and solvates of both: and application of them as drugs: [wherein R1is hydrogen, hydroxyl, nitro or the like; R2and R3are each independently hydrogen, halogeno or the like; R4and R5are each dependently hydrogen, halogeno or the like; Q1is an optionally substituted saturated or unsaturated 5- or 6-membered cyclic hydrocarbon group or the like; Q2is a single bond, oxygen or the like; Q3is, e.g., a group represented by formula (a): T1is carbonyl or the like; and X1and X2are each independently methylidyne or nitrogen]. These compounds exhibit potent Fxa inhibiting activities and serve as excellent anticoagulants which speedily exert satisfactory and persistent anti-thrombotic effects through oral administration and little cause adverse effects.
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- ARYL-SUBSTITUTED ALICYCLIC COMPOUND AND MEDICAL COMPOSITION COMPRISING THE SAME
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An aryl-substituted alicyclic compound of the formula (I): wherein U is 1,4,5,6-tetrahydropyrimidin-2-yl, etc., A is phenylene, etc., B is piperidine-1,4-diyl, etc., Z is -CONH-, etc., R3 is hydrogen, etc., R5 is hydrogen, aryl, etc.
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- NOVEL SULFONYL DERIVATIVES
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Sulfonyl derivatives represented by the following general formula (I): Q1-Q2-T1-Q3-SO2-QA and drugs containing the same (wherein Q1 is an optionally substituted, saturated or unsaturated, five- or six-membered cyclic hydrocarbon group, a five- or six-membered heterocyclic group, or the like; Q2 is a single band, oxygen, sulfur, C1-C6 alkylene or the like; QA is optionally substituted arylalkenyl, heteroarylalkenyl or the like; and T1 is carbonyl or the like). These compounds have potent FXa-inhibitory effects and promptly exert satisfactory and persistent antithrombotic effects through oral administration, thus being useful as anticoagulant agents little accompanied with side effects.
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