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203 results about "Basal bolus" patented technology

A large amount of glucose absorbed into the body quickly is a called a “bolus,” and the rise and fall of insulin that accompanies our meals is called “bolus” insulin. When the body is not capable of making that insulin, we inject short-acting or “bolus” insulin to do the job.

Pyrrolobenzodiazepines and conjugates thereof

Conjugate compounds of formula (A):wherein:R2 iswhere R36a and R36b are independently selected from H, F, C1-4 saturated alkyl, C2-3 alkenyl, which alkyl and alkenyl groups are optionally substituted by a group selected from C1-4 alkyl amido and C1-4 alkyl ester or, when one of R36a and R36b is H, the other is selected from nitrile and a C1-4 alkyl ester;R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR′, NO2, Me3Sn and halo;R7 is independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR′, NO2, Me3Sn and halo;Y is selected from formulae A1, A2, A3, A4, A5 and A6:L is a linker connected to a cell binding agent;CBA is the cell binding agent;n is an integer selected in the range of 0 to 48;RA4 is a C1-6 alkylene group;either(a) R10 is H, and R11 is OH, ORA, where RA is C1-4 alkyl; or(b) R10 and R11 form a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are bound; or(c) R10 is H and R11 is OSOzM, where z is 2 or 3 and M is a monovalent pharmaceutically acceptable cation;R and R′ are each independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups, and optionally in relation to the group NRR′, R and R′ together with the nitrogen atom to which they are attached form an optionally substituted 4-, 5-, 6- or 7-membered heterocyclic ring;wherein R16, R17, R19, R20, R21 and R22 are as defined for R6, R7, R9, R10, R11 and R2 respectively;wherein Z is CH or N;wherein T and T′ are independently selected from a single bond or a C1-9 alkylene, which chain may be interrupted by one or more heteroatoms e.g. O, S, N(H), NMe, provided that the number of atoms in the shortest chain of atoms between X and X′ is 3 to 12 atoms; andX and X′ are independently selected from O, S and N(H).
Owner:GENENTECH INC +1

Novel antidiabetic agents

Compounds which are 1-(2'-aminoacyl)-2-cyanopyrrolidine derivatives according to general formula (1) are DP-IV inhibitors for treatment of impaired glucose tolerance or type 2 diabetes; wherein A is selected from groups (2,3 and 4); X is selected from aminoacyl groups corresponding to the natural amino acids, acyl groups R3CO, groups R4COOC(R5)(R6)OCO, methoxycarbonyl, ethoxycarbonyl and benzyloxycarbonyl; R1 is selected from H, C1-C6 alkyl residues, (CH2)aNHW1, (CH2)bCOW2, (CH2)cOW3, CH(Me)OW4, (CH2)d-C6H4-W5 and (CH2)eSW6, where a is 2-5, b is 1-4, c is 1-2, d is 1-2, e is 1-3, W1 is COW6, CO2W6 or SO2W6, W2 is OH, NH2, OW6 or NHW6, W3 is H or W6, W4 is H or W6, W5 is H, OH or OMe, and W6 is C1-C6 alkyl, optionally substituted phenyl, optionally substituted heteroaryl or benzyl and R2 is selected from H and (CH2)n-C5H3N-Y, where n is 2-4 and Y is H, F, Cl, NO2 or CN, or R1 and R2 together are -(CH2)p-where p is 3 or 4; R3 is selected from H, C1-C6 alkyl and phenyl; R4 is selected from H, C1-C6 alkyl, benzyl and optionally substitued phenyl; R5 and R6 are each independently selected from H and C<highlight>
Owner:FERRING BV

Carboxylic acid derivative and medicine comprising salt or ester of the same

The present invention provides novel carboxylic acid derivatives useful as an insulin sensitizer, a salt thereof or a hydrate of them, and a medicament comprising the derivative as the active ingredient. Specifically, it provides a carboxylic acid derivative represented by the following formula: (wherein L represents a single bond, or a C1 to C6 alkylene group, a C2 to C6 alkenylene group or a C2 to C6 alkynylene group, each of which may have one or more substituent groups; M represents a single bond, or a C1 to C6 alkylene group, a C2 to C6 alkenylene group or a C2 to C6 alkynylene group, each of which may have one or more substituent groups; T represents a single bond, or a C1 to C3 alkylene group, a C2 to C3 alkenylene group or a C2 to C3 alkynylene group, each of which may have one or more substituent groups; W represents a carboxyl group; X represents a single bond, an oxygen atom, or a group represented by the various substituent groups including -NR<X1>CQ<1>O- (wherein Q<1 >represents an oxygen atom or a sulfur atom; R<X1 >represents a hydrogen atom, a cyano group, a formyl group, or various groups including a C1 to C6 alkyl group and a C1 to C6 hydroxyalkyl group, each of which may have one or more substituent groups), ONR<X1>CQ<1>-, -NR<X1>CQ<1>-, -CQ<1>NR<X1>-, -NR<X1a>CQ<1>NR<X1b>-, -Q<2>SO2- and -SO2Q<2>-; Y represents a 5 to 14-membered aromatic group which may have one or more substituent groups and one or more hetero atoms, or a C3 to C7 alicyclic hydrocarbon group; and the rings Z and U may be the same as or different from each other and each represents a 5 to 14-membered aromatic group which may have 1 to 4 substituent groups and one or more hetero atoms, and the ring may be partially saturated.), a salt thereof, an ester thereof or a hydrate of them.
Owner:EISIA R&D MANAGEMENT CO LTD

Imidazo[4, 5-b]pyridin-2-one and oxazolo[4, 5-b]pyridin-2-one compounds and analogs thereof as cancer therapeutic compounds

InactiveUS20090325945A1Promote apoptosisInhibiting cell cycle progressionBiocideOrganic chemistryDiseaseMelanoma
The present invention pertains to certain imidazo[4,5-b]pyridin-2-one and oxazolo[4,5 b]pyridin-2-one compounds and analogs thereof, which, inter alia, inhibit RAF (e.g., B RAF) activity, inhibit cell proliferation, treat cancer, etc., and more particularly to compounds of the formulae: wherein: J is independently —O— or —NRN1−; RN1, if present, is independently —H or a substituent; RN2 is independently —H or a substituent; Y is independently —CH═ or —N═; Q is independently —(CH2)j-M-(CH2)k— wherein: j is independently 0, 1 or 2; k is independently 0, 1, or 2; j+k is 0, 1, or 2; M is independently O—, —S—, —NH—, —NMe-, or —CH2—; each of RP1, RP2, RP5, and RP4 is independently —H or a substituent; and additionally RP1 and RP2 taken together may be CH═CH—CH═CH—; and additionally RP1 and RP5 taken together may be CH═CH—CH═CH—; L is independently: a linker group formed by a chain of 2, 3, or 4 linker moieties; each linker moiety is independently CH2—, —NRN—, —C(═X)—, or —S(═O)2—; either: exactly one linker moiety is —NRN—, or: exactly two linker moieties are —NRN—; either: exactly one linker moiety is —C(═X)—, and no linker moiety is —S(═O)2—, or: exactly one linker moiety is —S(═O)2—, and no linker moiety is —C(═X)—; no two adjacent linker moieties are —NRN—; X is independently ═O or ═S; each RN is independently —H or a substituent; A is independently: C6-14carboaryl, C5-14heteroaryl, C3-12carbocyclic, C3-12heterocyclic; and is independently unsubstituted or substituted; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, N-oxides, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., B-RAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and conditions that are ameliorated by the inhibition of RAF, RTK, etc., proliferative conditions such as cancer (e.g., colorectal cancer, melanoma), etc.
Owner:CANCER RES TECH LTD +1

Thyroid receptor ligands and method II

New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen; R4 is a carboxylic acid amide (CONR′R″) or an acylsulphonamide (CONHSO2R′) derivative, or a pharmaceutically acceptable salt thereof, and all stereoisomers thereof; or when n is equal to or greater than one, R4 may be a heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR′R″). R5 is hydrogen or an acyl (such as acetyl or benzoyl) or other group capable of bioconversion to generate the free phenol structure (wherein R5=H). In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount. Examples of such diseases associated with metabolism dysfunction or are dependent upon the expression of a T3 regulated gene include obesity, hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression, osteoporosis, hypothyroidism, goiter, thyroid cancer as well as glaucoma, congestive heart failure and skin disorders.
Owner:KARO BIO AB

Carboxylic acid derivative and salt thereof

The present invention provides a novel carboxylic acid compound, a salt thereof or a hydrate of them useful as an insulin sensitizer, and a medicament comprising the compound as an active ingredient. That is, the present invention provides a carboxylic acid compound represented by the following formula, a salt thereof, an ester thereof or a hydrate of them. Wherein R<1 >represents a hydrogen atom, hydroxyl group, halogen, carboxyl group, or a C1-6 alkyl group etc., each of which may have one or more substituents; L represents a single bond, or a C1-6 alkylene group, a C2-6 alkenylene group or a C2-6 alkynylene group, each of which may have one or more substituents; M represents a single bond, or a C1-6 alkylene group, a C2-6 alkenylene group or a C2-6 alkynylene group, each of which may have one or more substituents; T represents a single bond, or a C1-3 alkylene group, a C2-3 alkenylene group or a C2-3 alkynylene group, each of which may have one or more substituents; W represents a carboxyl group; represents a single bond etc.; X represents a single bond, oxygen atom, a group represented by -NR<X1>CQ<1>O- (wherein Q<1 >represents an oxygen atom or sulfur atom; and R<X1 >represents a hydrogen atom, formyl group, or a C1-6 alkyl group etc., each of which may have one or more substituents), -OCQ<1>NR<X1>- (wherein Q<1 >and R<X1 >are as defined above), -CQ<1>NR<X1>O- (wherein Q<1 >and R<X1 >are as defined above), ONR<X1>CQ<1>- (wherein Q<1 >and R<X1 >are as defined above), -Q<2>SO2- (wherein Q<2 >is an oxygen atom or -NR<X10>- (wherein R<X10 >represents a hydrogen atom, formyl group, or a C1-6 alkyl group etc., each of which may have one or more substituents)) or -SO2Q<2>- (wherein Q<2 >is as defined above), (wherein, provided that R<X2 >and R<X3>, and / or R<X4 >and R<X5 >may together form a ring, Q<3 >and Q<4 >are the same as or different from each other and each represents an oxygen atom, (O)S(O) or NR<X10 >< /
Owner:EISIA R&D MANAGEMENT CO LTD

Prostaglandin E1 lipid microsphere injection with charge effect and preparation method thereof

The invention relates to a method for preparing a prostaglandin E1 lipid microsphere injection of a charging non-homogeneous phase (comprising a water phase, an oil / water interfacial film phase and an oil phase) dispersion system, of which the surface of the lipid microsphere can be charged with positive electricity or negative electricity. The prostaglandin E1 is alprostadil, of which the chemical structure comprises a basic skeleton of 20-carbon fatty acid with a 5-carbon ring and two side chains, wherein one side chain is provided with a hydrophilic carboxylic acid group, so that the prostaglandin E1 has the characteristic of light surface activity action. By utilizing the characteristic, and according to the formula and the preparation process provided in the invention, the prostaglandin E1 has an unique drug-carrying mode in a solution of lipid microsphere with the non-homogeneous phase dispersion system, and the prepared lipid microsphere injection is fundamentally different from an alprostadil injection(Kaishi, and is prepared by adopting the technology of the Japanese business corporation LTT Bio-Pharma Co., Ltd. already sold in markets, and the difference lies in that the drug-carrying mode is completely different, the content of degradation products in the preparation such as impurities is more than 50 percent lower than that of in the Kaishi, so that the prostaglandin E1 lipid microsphere injection and the alprostadil injection are fundamentally different. The invention relates to a method for preparing the prostaglandin E1 lipid microsphere injection and the drug-carrying characteristics thereof in a three-phase system; in the formula, 0.0001 to 0.1 weight portion of prostaglandin E1 is used as a drug, the prostaglandin E1 is added with auxiliary materials for medical purpose to prepare the prostaglandin E1 lipid microsphere injection, and the auxiliary materials for medical purpose comprises the following materials in portion by weight: 5 to 20.
Owner:李淑斌

Conjugates of insulin-like growth factor binding protein-4 and poly (ethylene glycol)

A conjugate consisting of insulin-like growth factor binding protein 4 (IGFBP-4) and one or two polyethylene glycol) group(s), said polyethylene glycol) group(s) having an overall molecular weight of from about 30 to about 40 kDa is disclosed. This conjugate is useful for the treatment of cancer.
Owner:F HOFFMANN LA ROCHE INC

Composition crosslinkable by real michael addition (RMA) reaction

The present invention relates to a crosslinkable composition crosslinkable by Real Michael Addition (RMA) reaction comprising a component with at least 2 activated unsaturated groups (hereafter referred to as the RMA acceptor groups) and a component with at least 2 acidic protons C-H in activated methylene or methine groups (hereafter referred to as the RMA donor groups) which components can react to form a crosslinked network. The composition comprises: f. Component(s) A having at least 2 acidic C-H donor groups in activated methylene or methine and having a pKa(A) between 10.5 and 14; g. Component(s) B having at least 2 activated unsaturated acceptor groups, wherein a molar ratio R of acceptor groups to donor groups is between 3:1 to 1:6 and which component(s) B react with component(s) A by Real Michael Addition (RMA) to form a crosslinked network; h. basic component(s) C being a salt of a basic anion X- from an acidic X-H group containing compound wherein X is N, P, O, S or C: iv. in an amount xc between 0.001 and 1 meq/(gr of components A, B, C, D), v. anion X- being a Michael Addition donor reactable with component B and vi. anion X- is characterized by a pKa(C) of the corresponding acid X-H of more than two units lower than the pKa(A) of the majority component A and being lower than 10.5; i. optional component(s) D comprising one or more acidic X'-H groups wherein X' is N, P, O, S or C: v. X' being a same or different group as group X in component C, vi. the X'- anion being a Michael Addition donor reactable with component B, vii. the pKa(D) of the X'-H group in component D being more than two units lower than pKa(A) of the majority component A and being lower than 10.5, viii. the equivalent ratio Rd/c of acidic X'-H groups in component D over basic anion X- in component C is between 1% and 5000%.
Owner:欧尼克斯荷兰有限公司

Kaurene diterpene derivative, medicinal composition thereof and application of kaurene diterpene derivative to medicament

The invention provides a kaurene diterpene derivative shown as a general formula (I) and replaced by different groups at loci C-11, C-15, C-16 and C-19, a medicinal composition taking the kaurene diterpene derivative as an active ingredient, preparation methods thereof, and an application of the kaurene diterpene derivative to preparation of a type 1 11beta-hydroxysteroid dehydrogenase (11beta-HSD1) inhibitor. The invention further provides an application of a compound shown as a general formula (I) to preparation of a medicament for treating diabetes and relevant metabolic diseases (hypertension, obesity, senile dementia and the like).
Owner:KUNMING INST OF BOTANY - CHINESE ACAD OF SCI

Quinoline compound

InactiveUS20050209213A1Prevent obesitySuperior receptor antagonistic actionBiocideNervous disorderQuinolinium CompoundsBasal bolus
A compound, which has a melanin-concentrating hormone antagonistic action and useful as an agent for preventing or treating obesity, and which is represented by the formula: wherein Ar is a cyclic group optionally having substituent(s); X is a bond or a spacer having a main chain of 1 to 6 atoms; R1 and R2 are the same or different and each is a hydrogen atom or a hydrocarbon group optionally having substituent(s), or R1 and R2 may form, together with the adjacent nitrogen atom, a nitrogen-containing heterocycle optionally having substituent(s); Y is a divalent hydrocarbon group optionally having substituent(s) (except CO); R3 is a hydrogen atom or a hydrocarbon group optionally having substituent(s); and ring A and ring B may further have substituents, and when ring B further has a substituent, the substituent may be linked to R1 to form a ring, or a salt thereof, or a prodrug thereof, is provided.
Owner:TAKEDA PHARMACEUTICALS CO LTD
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